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Trazodone 100 mg side effects: Trazodone Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

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Trazodone Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

See also the Warning section.

Nausea, vomiting, diarrhea, drowsiness, dizziness, tiredness, blurred vision, changes in weight, headache, muscle ache/pain, dry mouth, bad taste in the mouth, stuffy nose, constipation, or change in sexual interest/ability may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

To relieve dry mouth, suck on (sugarless) hard candy or ice chips, chew (sugarless) gum, drink water, or use a saliva substitute.

To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: shaking (tremors), nightmares, ringing in the ears, problems urinating, blood in urine, signs of infection (e.g., fever, persistent sore throat), shortness of breath, stomach/abdominal pain.

Get medical help right away if you have any very serious side effects, including: chest/jaw/left arm pain, fainting, fast/irregular heartbeat, seizures, eye pain/swelling/redness, widened pupils, vision changes (such as seeing rainbows around lights at night).

This medication may increase serotonin and rarely cause a very serious condition called serotonin syndrome/toxicity. The risk increases if you are also taking other drugs that increase serotonin, so tell your doctor or pharmacist of all the drugs you take (see Drug Interactions section). Get medical help right away if you develop some of the following symptoms: fast heartbeat, hallucinations, loss of coordination, severe dizziness, severe nausea/vomiting/diarrhea, twitching muscles, unexplained fever, unusual agitation/restlessness.

For males, in the very unlikely event you have a painful or prolonged erection (priapism) lasting 4 or more hours, stop using this drug and seek immediate medical attention, or permanent problems could occur.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US –

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Trazodone (Desyrel) – Side Effects, Interactions, Uses, Dosage, Warnings

You should not use trazodone if you are allergic to it.

Do not use trazodone if you have used an MAO inhibitor in the past 14 days. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, tranylcypromine, and others.

After you stop taking trazodone, you must wait at least 14 days before you start taking an MAOI.

Tell your doctor if you have ever had:

  • liver or kidney disease;
  • heart disease, or a recent heart attack;
  • a bleeding or blood clotting disorder;
  • seizures or epilepsy;
  • narrow-angle glaucoma;
  • long QT syndrome;
  • drug addiction or suicidal thoughts; or
  • bipolar disorder (manic depression).

Be sure your doctor knows if you also take stimulant medicine, opioid medicine, herbal products, or medicine for depression, mental illness, Parkinson’s disease, migraine headaches, serious infections, or prevention of nausea and vomiting. These medicines may interact with trazodone and cause a serious condition called serotonin syndrome.

Some young people have thoughts about suicide when first taking an antidepressant. Your doctor should check your progress at regular visits. Your family or other caregivers should also be alert to changes in your mood or symptoms.

Ask your doctor about taking this medicine if you are pregnant. It is not known whether trazodone will harm an unborn baby. However, you may have a relapse of depression if you stop taking your antidepressant. Tell your doctor right away if you become pregnant. Do not start or stop taking this medicine without your doctor’s advice.

If you are pregnant, your name may be listed on a pregnancy registry to track the effects of trazodone on the baby.

It may not be safe to breastfeed while using this medicine. Ask your doctor about any risk.

Trazodone is not approved for use by anyone younger than 18 years old.

Trazodone: MedlinePlus Drug Information

A small number of children, teenagers, and young adults (up to 24 years of age) who took antidepressants (‘mood elevators’) such as trazodone during clinical studies became suicidal (thinking about harming or killing oneself or planning or trying to do so). Children, teenagers, and young adults who take antidepressants to treat depression or other mental illnesses may be more likely to become suicidal than children, teenagers, and young adults who do not take antidepressants to treat these conditions. However, experts are not sure about how great this risk is and how much it should be considered in deciding whether a child or teenager should take an antidepressant. Children younger than 18 years of age should not normally take trazodone, but in some cases, a doctor may decide that trazodone is the best medication to treat a child’s condition.

You should know that your mental health may change in unexpected ways when you take trazodone or other antidepressants even if you are an adult over age 24. You may become suicidal, especially at the beginning of your treatment and any time that your dose is increased or decreased. You, your family, or your caregiver should call your doctor right away if you experience any of the following symptoms: new or worsening depression; thinking about harming or killing yourself, or planning or trying to do so; extreme worry; agitation; panic attacks; difficulty falling asleep or staying asleep; aggressive behavior; irritability; acting without thinking; severe restlessness; and frenzied abnormal excitement. Be sure that your family or caregiver knows which symptoms may be serious so they can call the doctor when you are unable to seek treatment on your own.

Your healthcare provider will want to see you often while you are taking trazodone, especially at the beginning of your treatment. Be sure to keep all appointments for office visits with your doctor.

The doctor or pharmacist will give you the manufacturer’s patient information sheet (Medication Guide) when you begin treatment with trazodone. Read the information carefully and ask your doctor or pharmacist if you have any questions. You also can obtain the Medication Guide from the FDA website: http://www.fda.gov/Drugs/DrugSafety/ucm085729.htm.

No matter your age, before you take an antidepressant, you, your parent, or your caregiver should talk to your doctor about the risks and benefits of treating your condition with an antidepressant or with other treatments. You should also talk about the risks and benefits of not treating your condition. You should know that having depression or another mental illness greatly increases the risk that you will become suicidal. This risk is higher if you or anyone in your family has or has ever had bipolar disorder (mood that changes from depressed to abnormally excited) or mania (frenzied, abnormally excited mood) or has thought about or attempted suicide. Talk to your doctor about your condition, symptoms, and personal and family medical history. You and your doctor will decide what type of treatment is right for you.

Side Effects Of Taking Trazodone For Sleep

While primarily an antidepressant, more doctors are now prescribing trazodone for sleep issues.

We’ll look today at whether or not trazodone is an effective agent for insomnia and other sleep disorders and, more importantly, whether it’s safe to use in this capacity.

Before anything else, though, what is trazodone?

 

What Is Trazodone

Trazodone is an antidepressant drug mainly prescribed to treat the symptoms of depression. Doctors also commonly prescribe trazodone for the treatment of anxiety, schizophrenia, and uncontrollable movements that crop up as a side effect of other meds.

First approved by the FDA in 1981 (under the brand name Desyrel), trazodone is now available as a generic medication produced by several leading drug companies. Oleptro is the only remaining brand name for trazodone.

Trazodone belongs to a class of medications called serotonin modulators. These drugs work by moderating levels of serotonin – a neurotransmitter – in the brain and increasing its availability in the CNS (central nervous system).

Categorized as a SARI (serotonin antagonist reuptake inhibitor), trazodone stops neurons from reabsorbing serotonin once the neurotransmitter has been released into the CNS. It’s through this mechanism that trazodone can help with some cases of depression.

Unfortunately, many other antidepressants are much more effective for treating depression while the chemical composition of trazodone gives it mild sedating properties, often unwanted if being used to treat depression.

So, although not designed as a sedative or hypnotic to address sleep disorders, doctors are now prescribing trazodone off-label to mitigate insomnia.

Before we move on to examine the side effects of using trazodone for sleep, what is insomnia? We’ll briefly highlight that right now.

 

What Is Insomnia?

There are many different types of insomnia, and the word is used to describe a range of sleep problems from difficulty falling asleep to waking up in the night and being unable to sleep again.

 

There are 2 broad categories of insomnia, primary and secondary:

  • Primary insomnia: With primary insomnia, you have standalone problems with sleep not brought about by other physical or psychological disorders.
  • Secondary insomnia: Difficulties sleeping caused by either a medical condition or a mental health disorder is known as secondary insomnia.

 

Treatment of primary insomnia involves addressing and attacking the sleep problem itself.

With secondary insomnia, the condition causing the insomnia needs to be dealt with alongside medical or behavioral treatment of the insomnia itself.

 

There are multiple sub-types of insomnia.

  • Acute insomnia: Typically triggered by a stressful life event, acute insomnia is a brief, fleeting episode of sleep disturbance that often resolves with no need for treatment.
  • Chronic insomnia: Insomnia is normally labelled chronic if you have problems falling asleep or staying asleep for at least 3 nights weekly over 3 months or more. There are many causes and treatment varies accordingly.
  • Comorbid insomnia: If insomnia occurs alongside another condition, it’s termed comorbid insomnia. Conditions like anxiety and depression often precipitate sleeping problems. Debilitating back pain or conditions like arthritis can also make it hard to sleep.
  • Late insomnia: Waking extremely early in the morning and being unable to sleep again.
  • Maintenance insomnia: An inability to stay asleep is known as maintenance insomnia and it’s characterized by waking during the night then finding it tough to get back to sleep.
  • Sleep onset insomnia: You’re suffering from onset insomnia if you find it tough to fall asleep when you climb into bed.

 

Many medications are used to address the issues that come with insomnia including Ambien and trazodone.

So, does taking an antidepressant really work if you’ve got insomnia?

Does This Help You Sleep

In 2017, a systematic review of trazodone for insomnia yielded 45 studies into the safety and efficacy of off-label use of this medication. The study concluded that trazodone is useful for treating both primary and secondary insomnia. Trazodone was also shown to be effective for treating symptoms caused by depression and dementia.

That said, physicians and sleep scientists often baulk at the idea of using antidepressants like trazodone for the treatment of insomnia. Popular alternatives like Lunesta and Ambien better deal with the neurological upset often associated with insomnia. CBT (cognitive behavioral therapy) is also promoted as an effective non-pharmacologic solution.

A key advantage of using trazodone to counter sleep issues is that it can be safely used for much longer than most common sleep aids. Normally, prescription sleeping pills are used for no more than 2 weeks. Trazodone can be safely used for longer than this.

The 3 to 6 hour half-life of trazodone makes it most suitable for treating sleep onset insomnia or maintenance insomnia.

 

Trazodone as a sleep aid has several core benefits:

  • Scientifically proven to effectively treat both primary insomnia and secondary insomnia
  • Trazodone can be used to treat sleep issues at low doses
  • This medication is safely than the alternative medications for elderly patients
  • You can find generic trazodone much more cheaply than Ambien
  • Trazodone has fewer side effects than most common sleep aids
  • Unlike benzodiazepines, trazodone is not addictive
  • Trazodone can be used to treat sleep apnea

 

Sleep scientists recommend CBT along with other appropriate behavioral modifications as a first line of attack against insomnia. If these modalities are not suitable for you or don’t work, the sedative effects of trazodone can be beneficial.

So, how much do you need?

 

Dosage for Sleep

Trazodone tablets come in multiple doses:

When used as a sleep aid, start off with 25 to 50mg and increase the dose if necessary up to 100mg. Studies have also shown that trazodone has utility even in lower doses.

So, you can see that trazodone works well for combatting insomnia and that you don’t need to take this non-addictive medication in high doses either.

What about the downside of trazodone for sleep, though?

We’ll look now at what side effects you can expect if trazodone is prescribed for insomnia.

 

Side Effects of Trazodone

If you use trazodone to alleviate insomnia and suddenly discontinue use, you might experience symptoms like anxiety, irritability, depression and mild flu-like symptoms. These side effects can be largely eliminated by slowly tapering off and using less trazodone over time.

When compared to Ambien, withdrawal symptoms are pretty mild.

How about more general side effects, then?

 

Experiencing any of the following is commonplace:

  • Blurred vision
  • Confusion
  • Constipation
  • Diarrhea
  • Difficulties with walking or coordination
  • Dizziness
  • Dry mouth
  • Fatigue
  • Headache
  • Lightheadedness
  • Low blood pressure
  • Muscle pain
  • Nausea or vomiting
  • Nervousness
  • Palpitations
  • Rapid heart rate
  • Sleepiness
  • Skin reactions, such as a rash
  • Tremors
  • Weight changes

 

While much less common, you might also experience the following serious side effects:

  • Abnormal heart rhythms
  • Anemia
  • Extrapyramidal symptoms
  • Fainting
  • Hallucinations
  • Heart attack
  • Hepatitis (liver inflammation)
  • Hypertension (high blood pressure)
  • Hypomania
  • Mania
  • Neutropenia (low white blood cell count)
  • Orthostatic hypotension (low blood pressure when standing)
  • Priapism (persistent painful erection)
  • Psychosis exacerbation
  • Seizures
  • SIADH (Syndrome of Inappropriate Anti-Diuretic Hormone secretion)
  • Stroke
  • Suicidal thoughts
  • Tardive dyskinesia
  • Worsening depression

 

In rare instances, trazodone can provoke serious reactions. If you find difficulty breathing or experience any other severe reaction, call 911 immediately.

 

According to the Food and Drug Administration, trazodone poses the following serious risks:

  • Cardiac arrhythmias: Changed in heart rhythm can occur. The risk is heightened if you have existing heart problems.
  • Serotonin syndrome: Too much serotonin accumulating in the body can trigger negative reactions. If you’re taking migraine medication or other supplements, the risk of this is magnified. Symptoms include dizziness, seizures, agitation, and hallucinations.
  • Suicidal thoughts: There’s a risk of suicidal thoughts when using trazodone. This is most prevalent in young adults.
  • Hypotension: When you stand up, hypotension is an abrupt drop in blood pressure. This happens more frequently when some people use trazodone.
  • Heightened danger of bleeding: If you’re taking blood-thinning drugs like Warfarin or Heparin along with trazodone, you should be aware that your risk of bleeding increases.
  • Mania: Trazodone can induce feelings of hyperactivity, euphoria, and excessive excitement.
  • Priapism: In very rare cases, trazodone can cause priapism, an erection that lasts a long time and causes pain.

 

We reiterate, you are highly unlikely to experience most of the above side effects if you use trazodone for insomnia. You should nevertheless be aware of everything that could happen.

How about overdose, then? Is this a danger with trazodone?

 

Trazodone Overdose

Although uncommon, there have been a handful of reports of trazodone overdose.

The risk of overdose is heightened if you’re drinking alcohol. You should also avoid taking benzodiazepines or any other CNS depressant drugs. All of these can arrest your breathing and slow your reactions.

 

Symptoms of a trazodone overdose include:

  • Drowsiness
  • Heart rhythm changes
  • Respiratory arrest (breathing stops)
  • Seizures
  • Vomiting

 

Any drug overdose can be fatal so call 911 immediately if you think you might have taken too many trazodone tablets.

If you or someone you know is struggling with an addiction to Trazodone or other antidepressants and is searching for an inpatient rehab facility, call us at 888-448-0302 to chat with a recovery specialist. We are available 24/7 to answer your questions and get you the information you need to make the best recovery decision for you. Your call is 100% confidential, and we are ready to help you get started whenever you decide that it’s the right time

Trazodone: FDA Warning

Just like a number of antidepressants, this medication has been issued with an FDA Black Box Warning.

This concerns the increased risk of suicidal thoughts or behaviors in children and young adults. The FDA states that anyone taking trazodone should be “closely monitored” and add that this medication “is not approved for use in pediatric patients”.

 

The Bottom Line

Despite generally positive results with trazodone for both primary insomnia and secondary insomnia, the American Academy of Sleep Medicine suggests that the potential damage and risk of using trazodone for insomnia outweigh the advantages.

Studies have shown that you might only shave off 10 minutes from the time it takes you to fall asleep, and you only reduce the amount of time you’re awake by 8 minutes. Admittedly, these are not impressive stats.

While not recommended the first line of treatment against insomnia, trazodone can be a highly effective sleep aid. If you haven’t had much luck with behavioral therapy or other types of medication from Ambien to Valium, you could find some benefit from trying trazodone.

 

Final Word

If you’d like advice about any aspect of medication, don’t hesitate to get in touch. Since trazodone is non-addictive and you won’t experience severe withdrawal symptoms, you won’t need residential rehab to stop taking it.

You may, however, like the idea of exploring cognitive behavioral therapy as an alternative to medication for sleep. If so, call us on 888-448-0302 and we can help you out.

 

Your Path to Recovery Starts Here

Recovery starts here. Talk to a Recovery Specialist now.

888-448-0302

Your Path to Recovery Starts Here

Recovery starts here. Talk to a Recovery Specialist now.

888-448-0302

About the Author

Landmark Recovery Staff

This post was written by a Landmark Recovery staff member. If you have any questions, please contact us at 888-448-0302.

Nov 26, 2019

Posted in: Drug

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Trazodone (Oral Route) Side Effects

Side Effects

Drug information provided by: IBM Micromedex

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

  1. Blurred vision

  2. confusion

  3. dizziness

  4. dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position

  5. lightheadedness

  6. sweating

  7. unusual tiredness or weakness
Less common

  1. Burning, crawling, itching, numbness, prickling, “pins and needles”, or tingling feelings

  2. confusion about identity, place, and time

  3. decreased concentration

  4. fainting

  5. general feeling of discomfort or illness

  6. headache

  7. lack of coordination

  8. muscle tremors

  9. nervousness

  10. pounding in the ears

  11. shortness of breath

  12. slow or fast heartbeat

  13. swelling
Rare

  1. Skin rash

  2. unusual excitement

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  1. Dry mouth (usually mild)

  2. muscle or bone pain

  3. trouble sleeping

  4. trouble with remembering

  5. unpleasant taste
Less common

  1. Constipation

  2. continuing ringing or buzzing or other unexplained noise in the ears

  3. diarrhea

  4. hearing loss

  5. muscle aches or pains

  6. weight loss

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Portions of this document last updated: May 01, 2021

Copyright © 2021 IBM Watson Health. All rights reserved. Information is for End User’s use only and may not be sold, redistributed or otherwise used for commercial purposes.


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Trazodone Hydrochloride 50mg and 100mg Capsules – Patient Information Leaflet (PIL)

What is a Patient Information Leaflet and why is it useful?

The Patient Information Leaflet (PIL) is the leaflet included in the pack with a medicine. It is written for patients and gives information about taking or using a medicine. It is possible that the leaflet in your medicine pack may differ from this version because it may have been updated since your medicine was packaged.


Below is a text only representation of the Patient Information Leaflet.
The original leaflet can be viewed using the link above.


The text only version may be available in large print, Braille or audio CD.
For further information call emc accessibility on 0800 198 5000.
The product code(s) for this leaflet are: PL04425/0609, PL17780/0617, PL17780/0618, PL04425/0180.

TRAZODONE HYDROCHLORIDE 50MG AND 100MG CAPSULES

  • Keep this leaflet. You may need to read it again.
  • If you have any further questions, ask your doctor or pharmacist.
  • This medicine has been prescribed for you. Do not pass it on to others. It may harm them, even if their symptoms are the same as yours.
  • If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.

1. What trazodone is and what it is used for

2. Before you take trazodone

3. How to take trazodone

4. Possible side effects

5. How to store trazodone

6. Further information

The name of your medicine is Trazodone Hydrochloride 50mg or 100mg Capsules (called trazodone in this leaflet). This belongs to a group of medicines called antidepressants.

Trazodone can be used to treat anxiety and depression.

Do not take this medicine and tell your doctor if you:

  • are allergic to trazodone or any of the other ingredients of these capsules (listed in section 6).

    Signs of an allergic reaction can include: a rash, swallowing or breathing problems, swelling of your lips, face, throat or tongue.
  • have recently had a heart attack.
  • are a heavy drinker or are taking sleeping tablets.
  • are under 18 years of age.

Do not take this medicine if any of the above applies to you. If you are not sure, talk to your doctor or pharmacist before taking trazodone.

Thoughts of suicide and worsening of your depression or anxiety disorder

If you are depressed and/or have anxiety disorders you can sometimes have thoughts of harming or killing yourself. These may be increased when first starting antidepressants, since these medicines all take time to work, usually about two weeks but sometimes longer.

You may be more likely to think like this if you:

  • have previously had thoughts about killing or harming yourself.
  • are a young adult. Information from clinical trials has shown an increased risk of suicidal behaviour in adults aged less than 25 years with psychiatric conditions who were treated with an antidepressant.

If you have thoughts of harming or killing yourself at any time, contact your doctor or go to a hospital straight away.

You may find it helpful to tell a relative or close friend that you are depressed or have an anxiety disorder, and ask them to read this leaflet. You might ask them to tell you if they think your depression or anxiety is getting worse, or if they are worried about changes in your behaviour.

Trazodone should not be used in children and adolescents under 18 years of age.

If you are elderly, you may be more prone to side effects, increased caution is necessary especially when taking other medicines at the same time as trazodone or if you have some other diseases.

  • have or have ever had fits or seizures (epilepsy)
  • have severe liver, kidney or heart problems
  • are pregnant, trying to become pregnant or are breast-feeding
  • have an overactive thyroid gland (hyperthyroidism)
  • have problems passing water or need to pass water (urine) frequently
  • have narrow angle glaucoma (an eye disorder)
  • have schizophrenia or other type of mental disorder
  • are elderly, as you may be more prone to side effects
  • are taking buprenorphine (a strong pain killer). The use of buprenorphine with trazodone can lead to serotonin syndrome, a potentially life-threatening condition (see “Other medicines and trazodone”).

If you are not sure if any of the above applies to you, talk to your doctor or pharmacist before taking trazodone.

Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines.

This includes medicines you buy without a prescription, including herbal medicines.

This is because trazodone can affect the way some other medicines work. Also some medicines can affect the way trazodone work.

  • MAOI (MonoAmine Oxidase Inhibitors) medicines such as tranylcypromine, phenelzine and isocarboxazid (for depression) or selegiline (for Parkinson’s disease), or have taken them in the last 2 weeks
  • Other antidepressants (such as amitriptyline or fluoxetine)
  • Buprenorphine/opioids. These medicines may interact with trazodone and you may experience symptoms such as involuntary, rhythmic contractions of muscles, including the muscles that control movement of the eye, agitation, hallucinations, coma, excessive sweating, tremor, exaggeration of reflexes, increased muscle tension, body temperature above 38°C. Contact your doctor when experiencing such symptoms.
  • Sedatives (such as tranquilizers or sleeping pills)
  • Medicines used to treat epilepsy such as carbamazepine and phenytoin
  • Medicines used to treat high blood pressure, for example, clonidine
  • Digoxin (used to treat heart problems)
  • Medicines used to treat fungal infections such as ketoconozole and itraconazole
  • Some medicines used to treat HIV such as ritonavir and indinavir
  • Erythromycin, an antibiotic used to treat infections
  • Levodopa (used to treat Parkinson’s disease)
  • St. John’s Wort (a herbal remedy)
  • Warfarin (used to stop your blood from clotting)

If you are going to have an anaesthetic (for an operation), tell your doctor or dentist that you are taking trazodone.

You should avoid drinking alcohol while taking trazodone.

Talk to your doctor before taking this medicine if you are pregnant, might become pregnant, or think you may be pregnant.

Trazodone should only be taken during pregnancy if your doctor tells you that treatment with trazodone is essential for you and tells you to take this medicine.

Taking trazodone in the late stages of pregnancy may lead to your baby experiencing withdrawal symptoms when they are born.

If you are breast-feeding or planning to breast-feed, talk to your doctor or pharmacist before taking any medicine.

Trazodone may make you feel sleepy or dizzy. If this happens do not drive or use any tools or machines.

Trazodone Capsules contain lactose. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this this medicine.

Always take trazodone exactly as your doctor has told you. You should check with your doctor or pharmacist if you are not sure.

  • Take this medicine by mouth
  • Swallow the capsules whole with a drink of water
  • Take with or after food. This can help lower the chances of side effects
  • If you have been told to take trazodone only once each day then you should take it before going to bed
  • If you feel the effect of your medicine is too weak or strong, do not change the dose yourself, but ask your doctor

Adults:

Depression

  • Adults usually start by taking 150mg each day
  • Your doctor may increase the dose to 300mg each day depending on your condition
  • For adults in hospital the dose may be as high as 600mg each day

Anxiety

  • Adults usually start by taking 75mg each day
  • Your doctor may increase the dose to 300mg each day

Elderly

  • Older people or those who are frail will usually be given a starting dose of 100mg each day

Children

Children and adolescents under 18 years should not take trazodone.

If you take more trazodone than you should, tell a doctor or go to a hospital casualty department straight away. Take the medicine pack with you. This is so the doctor knows what you have taken.

The following effects may happen: feeling sick or being sick, feeling sleepy, dizzy or faint, fits (seizures), confusion, breathing or heart problems.

If you forget to take a dose, take it as soon as you remember it. However, if it is nearly time for the next dose, skip the missed dose.

Do not take a double dose to make up for a forgotten dose.

Keep taking trazodone until your doctor tells you to stop. Do not stop taking trazodone just because you feel better. When your doctor tells you to stop taking these capsules he/she will help you to stop taking them gradually.

Like all medicines, trazodone can cause side effects, although not everybody gets them.

  • You get swelling of the hands, feet, ankles, face, lips or throat which may cause difficulty swallowing or breathing, itching of the skin and nettle rash. This may mean you are having an allergic reaction to trazodone.
  • Painful erection of the penis, unrelated to sexual activity, that will not go away (priapism)
  • Yellowing of the eyes or skin. This could be a liver problem (such as jaundice)
  • Getting infections more easily than usual. This could be because of a blood disorder (agranulocytosis)
  • Bruising more easily than usual. This could be because of a blood disorder (thrombocytopenia)
  • You have severe abdominal pain and bloating, are being sick (vomiting) and have constipation.

    These may be signs that your intestine is not working properly (paralytic ilius)
  • You have thoughts of harming or killing yourself
  • Feeling tired, faint, dizzy, having pale skin. These could be signs of anaemia
  • Convulsions/fits
  • Unusual skin sensations such as numbness, tingling, pricking, burning or creeping on the skin (parasthesia)
  • Feeling confused, restless, sweating, shaking, shivering, hallucinations (strange visions or sounds), sudden jerks of the muscles or a fast heartbeat, you may have something called Serotonin syndrome.
  • Feeling very unwell, possibly with shortness of breath (dyspnoea), difficulty in walking or walking with a shuffling gait, shaking, uncontrolled muscle twitching and a high temperature (above 38°C).

    This could be a rare condition known as Neuroleptic Malignant Syndrome.
  • Rapid, slow or irregular heartbeat.
  • Feeling drowsy or sleepy, tiredness
  • Feeling less alert than usual
  • Feeling sick (nausea) or being sick (vomiting), indigestion
  • Constipation, diarrhoea
  • Dry mouth, altered taste, increased amounts of saliva, blocked nose
  • Sweating more than usual
  • Dizziness, headache, confusion, weakness, tremor (shaking)
  • Blurred vision
  • Loss of appetite and weight loss
  • Feeling dizzy or light-headed on standing or sitting up quickly (postural hypotension), fainting (syncope)
  • Feeling restless and having difficulty sleeping
  • Water retention which may cause swollen arms or legs
  • Skin rash, itching
  • Chest pain
  • Pain in limbs, back pain, pain in your muscles, pain in your joints
  • Jerking movements that you can not control, mainly in the arms and legs, uncontrolled muscle movements or twitches
  • Frequent infections with high temperature, severe chills, sore throat or mouth ulcers. These could be signs of a blood problem called leucopenia.
  • Feeling anxious or more nervous than usual, feeling agitated
  • Overactive behaviour or thoughts (mania), believing things that are not true (delusions), memory disturbance
  • Nightmares
  • Decreased sex drive
  • Feeling dizzy, possibly with a “spinning” feeling (vertigo)
  • High blood pressure
  • High temperature
  • Flu type symptoms
  • Difficulty with speaking
  • Higher than normal number of white blood cells (seen by a blood test)
  • High levels of liver enzymes in your blood (shown by a blood test)
  • Severe liver disorders such as hepatitis
  • Liver failure with potentially fatal outcome
  • Feeling tired, weak and confused, having muscles that ache, are stiff or do not work well. There may also be headache, loss of appetite, nausea or vomiting, convulsion. This may be due to low sodium levels in your blood.

If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet. You can also report side effects directly via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.

By reporting side effects you can help provide more information on the safety of this medicine.

Keep this medicine in a safe place where children cannot see or reach it.

Do not use trazodone after the expiry date which is stated on the blister and carton after EXP. The expiry date refers to the last day of that month.

Store below 30°C in a dry place.

Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment.

  • Each trazodone hydrochloride 50mg capsule contains 50mg of the active substance, trazodone hydrochloride.
  • Each trazodone hydrochloride 100mg capsule contains 100mg of the active substance, trazodone hydrochloride.
  • Other ingredients include lactose, magnesium stearate, gelatin, titanium dioxide (E171), erythrosine (E127), indigo carmine (E132), yellow iron oxide (E172) and ink (black iron oxide E172, shellac, propylene glycol and ammonium hydroxide (pH adjustment) or black iron oxide E172, shellac, propylene glycol, strong ammonia solution (pH adjustment) and potassium hydroxide (pH adjustment). The 100mg capsules also contain red iron oxide (E172).

Trazodone hydrochloride 50mg capsules are violet and green, printed with the Roussel logo on one half and R365B on the other.

Trazodone hydrochloride 100mg capsules are violet and fawn coloured, printed with the Roussel logo on one half and R365C on the other.

Trazodone 50mg Capsules are supplied in blister packs of 84 and 100 capsules.

Trazodone 100mg Capsules are supplied in blister packs of 56 and 100 capsules.

Not all pack sizes may be marketed.

Marketing Authorisation Holder

Zentiva Pharma UK Limited
12 New Fetter Lane
London
EC4A 1JP
United Kingdom

Manufacturer

Sanofi-Aventis Sp.z.0.0
Drug Production and Distribution Plant
Ul. Lubelska 52 35-233
Rzeszow
Poland

or

Zentiva, k. s.
U Kabelovny 130
102 37 Prague 10
Dolni Mecholupy
Czech Republic

This leaflet does not contain all the information about your medicine. If you have any questions or are not sure about anything, ask your doctor or pharmacist.

This leaflet was last revised in February 2021

© Zentiva, 2021

ZV/650 76

Trazodone: Antidepressant, Sleeping Pill or Both?

What is trazodone?

Trazodone was developed in Italy in the 1960s as an antidepressant medication. Due to negative side effects associated with the drug early on—including dizziness, fainting, irregular heartbeat (and in rare cases, priapism in men)—the antidepressant wasn’t widely favored in the medical community. Eventually, however, internists and clinicians recognized potential benefits of the drug, particularly when administered at low doses. In 1981, trazodone (the generic name of the pharmaceutical) was approved by the U.S. Food and Drug Administration (FDA) under the brand name Desyrel for use in treating major depressive disorder. Today, the medication is prescribed under the brand name Oleptro to treat sleep disorders such as insomnia as well as anxiety disorder and unipolar depression.

Does trazodone cause sleepiness?

For many patients, the drug has a sedative effect, inducing a relaxed, sleepy feeling. In prescribing the drug for sleep disorders, physicians typically recommend taking a low dose at bedtime in order to limit the effects of drowsiness. Still, some people report lingering effects, including sluggishness and feeling zapped of energy, particularly upon waking.

How does trazodone help to alleviate depression?

Trazodone increases natural neurotransmitters in the central nervous system, essentially restoring depleted chemicals in the brain. One of these important neurotransmitters—serotonin—regulates our internal clock for resting and being awake, as well as mood, appetite, digestion, memory, sexual function and desire. Many experts believe depression involves an imbalance among the brain’s neurotransmitters (acetylcholine, norepinephrine, dopamine and serotonin.) While the cause of depression is not fully understood, trazodone affects the brain’s neurotransmitters by inhibiting the uptake of serotonin by nerves and stimulating other nerves.

How quickly does the drug take effect?

Patients who take the drug for a sleep disorder can experience the sedative effects within 30 minutes, depending on the type used. Patients who take the drug as an antidepressant may not notice symptom relief for one to two weeks, and it may take up to four weeks to experience the full benefits.

Is it safe to take trazodone to treat depression?

Like all medications, trazodone can cause side effects in some people. Ask your physician to discuss all potential side effects as well as drug interactions and potential withdrawal symptoms associated with the medication.

Do all antidepressant drugs work the same way?

While all antidepressant medications are designed to affect brain chemistry, various pharmaceutical formulations of the drugs have different targets and paths. The most commonly prescribed antidepressants are reuptake inhibitors. Reuptake, as described by WebMD, is “the process in which neurotransmitters are naturally reabsorbed back into nerve cells in the brain after they are released to send messages between nerve cells.” A reuptake inhibitor, then, keeps levels of neurotransmitters in the gap between nerves, potentially strengthening circuits in the brain that regulate mood. There are three different types: selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), and norepinephrine and dopamine reuptake inhibitors (NDRIs). Common SSRIs are Prozac, Zoloft, Paxil, Lexapro, Celexa and Luvox; common SNRIs include Cymbalta and Effexor; and NDRIs are found in only one drug: Wellbutrin.

Because trazodone doesn’t fall under any of these categories, it’s often referred to as an “atypical antidepressant.”

Is it safe to take trazodone for insomnia?

Although trazodone was designed to treat depression and anxiety disorders, the medication is now widely prescribed as a nighttime sleep aid for patients who suffer from acute insomnia.

How is trazodone different from other “sleeping pill” drugs?

Trazodone differs from Ambien, Sonata, Lunesta and other “sleeping pill” medications in a few ways:

  • Both Ambien and Lunesta are classified by the FDA as controlled substances because they have the potential for misuse and abuse, including dependence or addiction
  • Because trazodone is not a controlled substance, physicians aren’t limited in how many pills they can prescribe
  • It’s an inexpensive generic drug covered by most insurance companies
  • It’s not considered to be an addictive substance when used as prescribed

Trazodone should not be taken by pregnant women or women who are breastfeeding. 

What risks are associated with taking trazodone to treat depression?

There are heightened risks for patients under age 24, particularly with regard to mental health. According to Medline Plus, the following side effects and symptoms can occur among patients under age 24: “new or worsening depression; thinking about harming or killing yourself, or planning or trying to do so; extreme worry; agitation; panic attacks; difficulty falling asleep or staying asleep; aggressive behavior; irritability; acting without thinking; severe restlessness; and frenzied abnormal excitement.” If any of these symptoms or side effects are experienced, it’s crucial to consult a physician or medical professional immediately.

It’s also imperative that patients know what to avoid while taking SSRIs, SNRIs or other antidepressants. Whether a person has a cold, is having trouble sleeping or is searching for allergy relief, they should talk to their doctor before self-treating with an over-the-counter medication. According to Psychiatry Advisor, one patient who was taking melatonin for insomnia while also prescribed an SSRI woke up with a “headache, dizziness and feeling like his face was on fire”—signs of elevated blood pressure that could have been severe had he taken higher doses. Taking an antidepressant medication in combination with supplements, such as St. John’s wort or aspirin, can increase the likelihood of upper gastrointestinal bleeding. To avoid adverse drug reactions, experts advise making a list of all medications, supplements and other OTC drugs, and sharing it with your physician prior to taking trazodone.

Is it safe to use trazodone with alcohol or other drugs?

Absolutely not. Since both alcohol and trazodone affect the central nervous system, the consequences of mixing the two can be deadly. And mixing the medication with drugs of abuse can result in the onset of serotonin syndrome, a potentially lethal adverse drug reaction. While the potential for trazodone abuse is fairly low, any amount over 600 mg. in 24 hours is an overdose.

What happens if you take too much trazodone? Can it cause serotonin syndrome?

Serotonin syndrome occurs when, according to Mayo Clinic, “high levels of serotonin accumulate in the body.” This is a drug-to-drug interaction involving the over-stimulation of central and peripheral receptors. According to the journal U.S. Pharmacist, “Serotonin syndrome (SS) is caused most often when certain antidepressant agents are taken concurrently with other drugs that modulate synaptic serotonin levels. When patients take two or more antidepressants from different pharmacologic classes, drug-drug interactions may occur; these interactions may lead to potentially severe serotonin toxicity, or serotonin syndrome.” Clinical symptoms of serotonin syndrome can develop within two hours—or up to 24 hours—after taking an increased dose or adding another serotonergic drug.

Signs and symptoms of serotonin syndrome:

  • Tremors
  • Muscle aches
  • Sweating
  • Anxiety
  • Confusion
  • Tachycardia
  • Delirium
  • Hallucinations
  • Seizures
  • Renal failure
  • Death
What are the side effects of trazodone?

Trazodone usage can cause a decrease in sodium levels in the body, a disruption of the nervous system or serotonin syndrome. The most common side effects include:

  • Drowsiness (including feeling groggy the next day)
  • Dizziness (including an increased risk of fainting/falling)
  • Dry mouth
  • Constipation
  • Headache
  • Fatigue
  • Tingling or numbness in hands, arms or legs
  • Blurred vision
  • Disorientation
  • Vertigo
  • Nasal congestion
  • Shaking
  • Anxiety
  • Muscle aches
  • Prolonged and painful erections lasting longer than six hours (priapism) 
  • Abnormally low blood pressure
  • Heart rhythm disorders 
  • Increased risk of suicidal thoughts and behavior in children and adolescents (even when taken at approved doses for depression)
  • Acting on dangerous impulses
  • Insomnia (at high doses)
  • Weight gain or loss

The drug can stay in a person’s system for 42 hours after the final dose. Higher doses can produce more severe side effects.

Can you become addicted to trazodone?

While the drug is considered non-addictive and non-habit-forming, it should only be taken as prescribed and under a physician’s care in order to avoid misuse. This is especially important for individuals who have a history of substance abuse or other drug addiction. Warning signs of drug misuse include using the sleep aid/antidepressant without a prescription, using the medication at higher doses than prescribed, or snorting or crushing the tablets to speed up the intended effects.

Can you fail a drug test while taking trazodone?

Even though the antidepressant/sleep aid is not classified as a narcotic, it can cause false positives on drug tests. According to the National Center for Biotechnology Information, “The trazodone metabolite meta-Chlorophenylpiperazine [m-CPP] can cause false-positive urine amphetamine immunoassay results.…Further, we found that patients taking trazodone can produce urine with sufficient m-CPP to result in false-positive Amphetamines II results.”

What are trazodone’s withdrawal symptoms?

Although technically a non-addictive substance, regular use of the medication can result in mild physical dependence. For this reason, trazodone withdrawal is a concern. Rather than discontinuing use “cold-turkey,” physicians typically recommend a gradual tapering. This approach is considered a better protocol to avoid potential discomfort associated with trazadone withdrawal syndrome, also known as discontinuation syndrome.

Symptoms of trazodone withdrawal include:

  • Agitation
  • Confusion
  • Rapid mood swings
  • Muscle pain
  • Weakness
  • Dizziness
  • Stomach pain
  • Sweating
  • Insomnia
  • Fatigue

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Description TRAZODONE indications, dosages, contraindications of the active substance TRAZODONE

Rec.INN
registered by WHO

Part of the preparations:
list

Pharmacological action

Antidepressant, thiazolopyridine derivative.It also has thymoleptic, anxiolytic, sedative and muscle relaxant effects. Has a high affinity for some subtypes of serotonin receptors, inhibits the reuptake of serotonin; the neuronal seizure of norepinephrine and dopamine has little effect.

Has no anticholinergic effect, does not inhibit MAO, does not change body weight. Eliminates both mental (affective tension, irritability, fear, insomnia) and somatic manifestations of anxiety (palpitations, headache, myalgia, frequent urination, increased sweating).Increases the depth and duration of sleep in depressed patients, restores its physiological structure.

Reduces the pathological craving for ethanol. It is effective for withdrawal symptoms in patients with drug dependence on benzodiazepine derivatives anxiolytic drugs, eliminates anxiety-depressive state and sleep disorders (during remission, benzodiazepines can be completely replaced with trazodone). Not addictive. Promotes the restoration of libido and potency.

The therapeutic effect in 50% of patients is observed after 3-7 days, in 25% – after 2-4 weeks.

Pharmacokinetics

After oral administration, absorption from the gastrointestinal tract is high. The time to reach C max in blood plasma is 1-2 hours. Taking trazodone during or immediately after a meal increases absorption, reduces C max and increases the time to reach it.

Penetrates through histohematological barriers, including the BBB.Penetrates into tissues and fluids (bile, saliva, breast milk). Plasma protein binding – 89-95%.

Metabolized in the liver by hydroxylation. The isoenzymes CYP3A4, CYP3A5 and CYP3A7 are involved in the metabolism of the drug.

T 1/2 in the α-phase 3-6 hours, in the β-phase – 5-9 hours. Excreted by the kidneys – 75% in the form of inactive metabolites within 98 hours after administration; 20% – with bile.

Indication of the active substance
TRAZODON

Various forms of depression (endogenous, psychotic, neurotic, somatogenic), incl.h / thoughts; bulimia, kleptomania, anxiety, phobias. Benzodiazepine drug dependence; acute alcohol withdrawal syndrome. Decreased libido, impotence.Prevention of migraine attacks.

Dosing regimen

The initial daily dose is 150-200 mg (in 3 divided doses). In mild forms of depression, the average maintenance dose is 150 mg / day; with moderate and severe forms – 300 mg / day. If necessary, the dose can be increased to 600 mg / day. The main part of the daily dose is recommended to be taken at bedtime.

Side effects

From the side of the central nervous system and peripheral nervous system: drowsiness, fatigue, dizziness, insomnia, headache, agitation, myalgia, impaired coordination of movements, paresthesia, disorientation, darkening of consciousness, tremor.

From the cardiovascular system: arrhythmia, conduction disturbance, bradycardia, ventricular fibrillation, decreased blood pressure, orthostatic hypotension, fainting.

From the digestive system: nausea, vomiting, diarrhea, dryness and bitterness in the mouth.

From the side of the organ of vision: visual impairment, eye irritation.

From the hematopoietic system: leukopenia, neutropenia (usually insignificant).

Other: nasal congestion, priapism followed by impotence, allergic reactions.

Contraindications to use

Ventricular arrhythmia, tachycardia, myocardial infarction (early recovery period), history of priapism, pregnancy, lactation, hypersensitivity to trazodone.

Application during pregnancy and lactation

Use during pregnancy and lactation is contraindicated.

Application for violations of liver function

Use with caution in liver failure.

Application for impaired renal function

Use with caution in renal impairment.

Use in children

Use with caution in children and adolescents under the age of 18 years.

Special instructions

Use with caution in heart disease, arterial hypotension, arterial hypertension, renal and / or hepatic failure, in children and adolescents under the age of 18 years.

Should not be used concomitantly with MAO inhibitors.

Drug interactions

A case of “pirouette” -type arrhythmia with the simultaneous use of trazodone with amiodarone is described.

A case of a moderately pronounced decrease in the anticoagulant effect of warfarin while being used with trazodone is described.

With simultaneous use, it is possible to increase the concentration of digoxin in the blood plasma and develop symptoms of intoxication.

With simultaneous use with carbamazepine, a case of an increase in the concentration of carbamazepine in the blood plasma has been described.

With simultaneous use with lithium salts, tremors are possible, reversible symptoms of neurotoxic action.

When taking pseudoephedrine against the background of trazodone therapy, a case of the development of anxiety, panic, darkening of consciousness, depersonalization was described.

With simultaneous use with thioridazine, an increase in the concentration of trazodone in the blood plasma is possible; with tryptophan – a case of the development of anorexia, psychosis, hypomania is described; with phenytoin – a case of increased side effects of phenytoin has been described; with fluoxetine – side effects may increase; with chlorpromazine, trifluoperazine – the development of arterial hypotension is possible.

With simultaneous use with ethanol, the inhibitory effect on the central nervous system is enhanced.

Trazodonum – PsyAndNeuro.ru

Trade names in Russia

Trittico, Azona

Form of issue

Tablets: 150 mg

Pharmacological group

Antidepressant

Nomenclature NbN

Serotonin receptor antagonist [2]

Readings

◊ Recommendations of the Ministry of Health of Russia

F32 Depressive episode

F52 Sexual dysfunction not due to organic disorders or diseases

R52.2 Other persistent pain

Y47.1 Adverse reactions in the therapeutic use of benzodiazepines

Z50.2 Rehabilitation for alcoholism

Z50.3 Drug addiction rehabilitation

◊ FDA Recommendations

Depression

◊ UK Medicines and Healthcare Products Regulatory Agency recommendations

  • Anxiety
  • Depression

Target symptoms

  • Depression
  • Anxiety
  • Insomnia

Mechanism of action and pharmacokinetics

Trazodone, being a triazolopyridine derivative, has the ability to selectively inhibit the reuptake of serotonin in the brain, the drug acts as an antagonist of 5-HT2A / 2C receptors.Has no anticholinergic effect, does not inhibit MAO.

  • After oral administration, absorption from the gastrointestinal tract is high.
  • Time to reach C max in blood plasma – 1-2 h
  • Half-life: 1st phase 3-6 hours, 2nd phase 5-9 hours
  • The isoenzymes CYP3A4, CYP3A5 and CYP3A7 are involved in metabolism.

Treatment regimen

◊ Dosage and dose selection

  • 150-600 mg / day
  • Depression (as monotherapy): start with 150 mg in two divided doses, if necessary increase every 3-4 days by 50 mg, maximum 400 mg (outpatient), 600 mg (inpatient).
  • Insomnia: start with 25-50 mg at bedtime, then, if well tolerated, increase to 50-100 mg
  • There is no need to rush to increase doses [1]
  • At the beginning of treatment, sedation may be very noticeable
  • If a dose of less than 50 mg does not work, it is not necessary to quit treatment, it is better to increase it to 150-300 mg
  • Due to the short half-life, take the daily dose in two divided doses

◊ How quickly does it work

  • In some patients with insomnia, when the dosage is correct, begins to act immediately.
  • Begins to act after 2-4 weeks for depression.
  • If there is no effect after 6-8 weeks, increase the dose or switch to another drug.
  • May be used for many years to prevent relapse.

◊ Expected Result

  • In the treatment of depression: complete remission.
  • After the disappearance of symptoms of depression, you should continue taking it for 1 year if it was the treatment of the first episode.If this treatment is a recurrent episode, the treatment can be extended indefinitely.
  • Use in the treatment of anxiety may be indefinite.
  • For insomnia, use may be indefinite, since there is no data on the formation of tolerance, dependence or withdrawal syndrome [1].

◊ If not working

  • Change dose, change medication, or add ancillary medication;
  • Connect psychotherapy;
  • Reconsider the diagnosis to clarify comorbid conditions;
  • Patients with undiagnosed bipolar disorder may have poor treatment success, in which case a Mood Stabilizer should be considered [1].

◊ How to stop taking

The dose can be gradually reduced, although there is no evidence of a withdrawal syndrome [1].

◊ Treatment Combinations

  • Trazodone is rarely used as monotherapy for insomnia, in severe cases it can be combined with benzodiazepines
  • Trazodone is the most common drug in combination with antidepressants, it not only treats insomnia, but also enhances the antidepressant effect

Warnings and contraindications

  • Stop taking if the erection becomes unusually long – there is a risk of erectile dysfunction;
  • If an erection lasts more than 1 hour, see a doctor immediately;
  • Use caution if patient has convulsions;
  • Use caution if patient has bipolar disorder;
  • Do not use if allergic to trazodone [1].

Special patient groups

◊ Patients with kidney problems

No special selection of doses is required [1].

◊ Patients with liver disease

With care [1].

◊ Patients with heart disease

  • May cause arrhythmias.
  • Closely observe the patient.
  • Not recommended after a heart attack.

◊ Elderly patients

In the elderly, side effects are more common.

◊ Children and adolescents

  • The patient should be checked regularly and personally, especially during the first weeks of treatment.
  • Inform adults about risks.
  • Start with low doses.
  • Boys have a higher risk of priapism than adult men

◊ Pregnant

  • Not recommended for pregnant women, especially in the first trimester
  • All risks should be weighed and compared
  • Bleeding may be expected during childbirth

◊ Breastfeeding

  • The drug passes into breast milk.
  • If infant shows signs of irritation or sedation, stop feeding or taking sertraline
  • However, postpartum treatment may be necessary, so risks should be weighed.

Interaction with other substances

  • Tramadol increases the risk of seizures when taken with antidepressants
  • Cannot be used with MAO inhibitors. After you stop taking MAO inhibitors, 14 days should pass.Start treatment with MAO inhibitors 7 days after you stop taking vortioxetine.
  • Trazodone may reduce the effect of antihypertensive drugs [1].

Analyzes during treatment

Not required.

Side effects and other risks

◊ Mechanism of side effects

  • Sedation likely due to antihistamines
  • Most side effects occur immediately after treatment is started and resolve over time.

◊ Side effects

  • Nausea, vomiting, constipation, dry mouth
  • Sedation, fatigue, headache
  • Reduced pressure
  • Dangerous side effects : rarely priapism, rarely seizures, rarely mania, rarely suicidal ideation
  • Weight gain : rare
  • Sedation : often
  • Sexual dysfunction: no

◊ Dealing with side effects

  1. Wait
  2. If heavily sedated, take at night
  3. Change drug [1]

◊ Long-term use

Safe

◊ Addictive

No.

◊ Overdose

  • Rare cases of fatal overdose.
  • Priapism.

Benefits

  • Good for the treatment of insomnia when you do not want to use drugs with a dependent potential;
  • Good as an adjunct to anti-depressants to relieve anxiety and insomnia;
  • Good in cases where the absence of side effects in the sexual sphere and the absence of the risk of weight gain are essential [1].

Weakness

  • Not suitable for tiredness and sleepiness.
  • Not suitable if patient does not tolerate sedation.

Expert Advice

Less likely to cause mania than other antidepressants [1]

Footnotes

1. Stephen Stahl “Prescriber’s Guide”, 6th edition, 2017

2. Neuroscience-Based Nomenclature (https: //www.nbn2.com / taskforce)

instructions for use, classification, articles »Drug Handbook

Application for children and adolescents

Trazodone should not be used in children and adolescents. In a clinical study in children and adolescents, suicidal behavior (attempted suicide and planning suicide) and hostility (mainly aggressiveness, protest behavior, and anger) were more common in the antidepressant group than in the placebo group. In addition, there are currently no data on the long-term safety of the drug in children and adolescents, given its effects on growth, puberty, and cognitive and behavioral development.

Suicide / suicidal ideation or clinical deterioration

Depression is associated with an increased risk of suicidal thoughts, self-harm and suicide (manifestations of suicidal behavior) by the patient. This risk persists until significant remission occurs. There may be no improvement in the condition during the first few weeks of therapy or longer. Patients should be carefully monitored until such improvement occurs. General clinical experience indicates a possible increased risk of suicide in the early stages of recovery.

It is known that patients with a history of suicidal behavior or patients who had a significant degree of suicidal ideation before starting therapy have a higher risk of developing suicidal thoughts or suicidal attempts, therefore, during treatment, they need careful supervision. In a meta-analysis of placebo-controlled clinical trials of antidepressants for mental disorders, it was shown that among patients under 25 years of age, individuals in the antidepressant group had a higher risk of suicidal behavior than in the placebo group.

Drug therapy should be accompanied by careful monitoring of patients, including those from a high-risk group, especially at the beginning of treatment and after changing the dose of the drug. Patients (and their caregivers) should be warned to watch for any clinical signs of deterioration, suicidal behavior or thoughts, and unusual changes in behavior, and if they are found, seek medical advice immediately.

To minimize the potential risk of suicidal attempts, especially at the beginning of therapy, the physician should only prescribe a limited amount of trazodone to the patient at each visit.

It is recommended to carefully select the dosing regimen and carry out regular monitoring of patients with the following conditions:

  • epilepsy, particularly in such patients, do not sharply increase or decrease the dose;
  • impaired liver or kidney function, especially severe;
  • heart diseases such as angina pectoris, cardiac conduction disorders, or various degrees of blockade; recent myocardial infarction
  • hyperthyroidism
  • Violation of urination, for example, with hypertrophy of the prostate gland, although such problems are not expected, since the anticholinergic effect of trazodone is negligible;
  • Acute glaucoma, increased intraocular pressure, although significant changes in position are not expected because the anticholinergic effect of trazodone is negligible.

If the patient develops jaundice, trazodone therapy should be discontinued.

With the use of antidepressants in patients with schizophrenia or other psychotic disorders, psychotic symptoms may increase. Paranoid thoughts may become more pronounced. Against the background of trazodone therapy, the depressive phase in manic-depressive psychosis can change into the manic phase. In this case, the use of trazodone should be discontinued.

Against the background of simultaneous use with other serotonergic drugs, such as other antidepressants (for example, tricyclic antidepressants, selective serotonin reuptake inhibitors, serotonin and norepinephrine reuptake inhibitors and MAO inhibitors) and antipsychotics, drug interactions with the development of serotonin / malignant neuroleptics have been reported syndrome.Cases of fatal neuroleptic malignant syndrome have been reported with simultaneous use with antipsychotics, for which this syndrome is a known possible adverse reaction. For more information, see sections Interaction with other medicinal products and other forms of interaction and Adverse reactions.

Since agranulocytosis can clinically present as a flu-like condition, sore throat and fever, laboratory blood counts should be checked if these symptoms appear.

The occurrence of arterial hypotension, including orthostatic hypotension and syncope, has been reported in patients treated with trazodone. With the simultaneous use of antihypertensive drugs and trazodone, it may be necessary to reduce the dose of the antihypertensive drug. Elderly patients are often more susceptible to the unwanted effects of antidepressants, especially orthostatic hypotension and other anticholinergic effects.

At the end of the course of trazodone therapy, especially if this course was long, it is recommended to gradually reduce the dose until the drug is completely discontinued in order to minimize the likelihood of withdrawal symptoms, which include nausea, headache and general malaise.

There is currently no indication that trazodone hydrochloride is addictive.

During the use of trazodone, very rare cases of prolongation of the QT interval have been reported – an effect characteristic of other antidepressants. It is necessary to use trazodone with caution simultaneously with drugs with a known ability to prolong the QT interval. Trazodone should be used with caution in patients with diagnosed cardiovascular diseases, including those accompanied by prolongation of the QT interval.

Against the background of the use of powerful inhibitors of cytochrome CYP3A4, the level of trazodone in the serum may increase. For more information, see section Interaction with other medicinal products and other forms of interaction.

Like other drugs with alpha-adrenergic blocking activity, trazodone in very rare cases causes priapism. If it occurs, an intracavernous injection of an alpha-adrenergic agent such as epinephrine or metaraminol should be administered.However, cases of trazodone-induced priapism have been reported when surgery was necessary or when permanent sexual dysfunction resulted. In patients with suspicion of this adverse reaction, trazodone should be discontinued immediately.

Sustained-release tablets Trittico contains sucrose. This drug should not be used in patients with rare hereditary diseases such as fructose intolerance, glucose-galactose malabsorption syndrome or sucrase-isomaltose deficiency.

pregnancy

Data from a limited number (<200) of pregnant women exposed to trazodone indicate no adverse effects on pregnancy or fetal / newborn health. There is currently no other adequate epidemiological data. Data from animal studies does not indicate the presence of any direct or indirect harmful effects of this substance, used in therapeutic doses, on the course of pregnancy, embryo / fetal development, childbirth or postnatal development of offspring.

Pregnant women should use this drug with caution. If trazodone is administered to the mother before delivery, the infant should be monitored after birth to identify possible withdrawal symptoms based on the maternal benefit / fetal risk ratio.

breastfeeding

Limited data indicate that trazodone passes into breast milk in small quantities. Due to insufficient data, the decision to prolong / discontinue breastfeeding or continue / discontinue trazodone therapy should be made in view of the benefits of breastfeeding for the baby and the benefits of trazodone therapy for the mother.

Trazodone insignificantly or moderately affects the ability to drive vehicles and mechanisms. Patients should be warned that before driving and operating machinery, it is necessary to make sure that there is no drowsiness, sedation, dizziness, states of confusion or blurred vision while taking trazodone.

Trittico (trazodone) – an unique serotonergic antidepressant with some interesting properties

PSYCHIATRY AND PSYCHOPHARMACOTHERAPY Vol. 20, №3–CH4, 2018 / PS20, No. 3-4, 2018

IN OUR FRIENDS / FROM OUR FRIENDS

52

transmission, while the impairment of noradrenergic neurotransmission

plays a lesser role, pharmaceutical chemists

were synthesized by kologami in the 1960s and 70s the first

selective serotonin reuptake inhibitors

(SSRIs) – zimelidine, brompheniramine, etc. These drugs

were practically devoid of interactions with M-cho-

linergic, h2-histamine and a1-adrenergic

-adrenergic receptors and therefore had a low level of the corresponding PE (S.Stahl, 2013).

Already at the beginning of the clinical use of these first

SSRIs, it was revealed that SSRIs, as a class of blood pressure, are not devoid of

of their specific PE. So, in particular, it turned out that

SSRIs, being, in contrast to TCAs, are practically devoid of the dative effect, often cause insomnia, nightmares,

dreams, psychomotor agitation or exacerbation of anxiety and anxiety. , especially at the beginning of te-

rapia.Other common problems associated with

with the use of SSRIs were sexual dysfunctions

(decreased libido and orgasm brightness up to complete

anorgasmia in both sexes, erectile dysfunction or ejaculation

in men), as well as gastrointestinal disturbances. –

intestinal tract (GIT): decreased appetite, nausea, vomiting;

that, diarrhea. Common to all SSRIs PE (sexual, dissom-

nicheskie, anxious and from the gastrointestinal tract) to varying degrees

are characteristic of all modern, clinically used –

m to this day, SSRIs – from the historically first fluoxe –

tin and fluvoxamine until the most recent

in the SSRI group escitalopram (S.Stahl, 2013).

Studies have shown that the reason for the development of the indicated

PE when using SSRIs is the non-selective

stimulation of various subtypes of serotonin re-

receptors, primarily 5-HT2A, 5-HT2C, 5-HT3, to a lesser extent

least – 5-HT6 and 5-HT7 with an increase under the influence of

SSRIs in the serotonin content in synapses. At the same time,

but it turned out that for the implementation of the antidepressant effect

of the most different classes of blood pressure (not only TCAs, but

and MAOIs, and SSRIs) is the most important and, in general,

stimulation of only 5-HT1A subtype of serotonin recipes –

tori.At the same time, studies have shown that

the mentioned “undesirable” subtypes of serotonin

receptors (5-HT2A / C, 5-HT3, 5-HT6, 5-HT7) are more expedient than

not to stimulate, but, on the contrary, to block … Moreover,

has shown that the blockade of, for example, 5-HT2A / C or

5-HT3-serotonin receptors is associated not only with

kb with a decrease in sexual PE, nausea, anorexia,

anxiety and dyssomnic disorders, but also with an independent

antidepressant effect or with an increase in the

antidepressant effect from the reuptake of mono

amines (S.Stahl, 2013).

From the second generation of antidepressants (selective

monoamine reuptake inhibitors)

to the third generation (drugs of receptor action,

and in particular Trittico)

All this together led to the birth of the idea back in

1960s to synthesize a blood pressure that would

at the same time and inhibit the reuptake of serotonium-

on, like TCAs or the first SSRIs (zimelidine, bromo-

feniramine), and had the properties of a strong blocker

5-HT2A / C and a number of other undesirable subtypes of serotonin –

new receptors, similar to some TCAs, but

did not have unwanted M-anticholinergic blocking PE.

Scientists who put forward such an idea believed that the drug

with such receptor properties would not only be better tolerated and give on average less PE compared to

nii with the then available SSRIs (zimelidine, bromphe-

niramine) and even more so compared to TCAs, but

will also be more effective than SSRIs. As time has shown, these

a priori expectations have largely come true during the subsequent

clinical study and comparison with other AD

of the drug Trittico (trazodone), synthesized by specialists of the research laboratory

“Angelini Research Laboratory” in Italy at the end of the 1960s

precisely within the framework of the implementation of the mentioned idea

(S.Stahl, 2013).

In the English-language classifications of types of blood pressure Trittico

(trazodone) is called an antagonist of serotonin re-

type 2 receptors and at the same time an inhibitor of serotonin reuptake

(Serotonin-2 receptor Anta-

Initor ) [I.V. Zabozlaeva, E.V. Mali –

nina, 2011; S. Stahl, 2013]. In the Russian-language classifications of

types of blood pressure, trazodone is usually called “specific

serotonergic blood pressure” or “atypical blood pressure”

(I.V. Zabozlaeva, E. V. Malinina, 2011; Yu.V. Bykov et al,

2013). The complex complex and atypical mechanism

of Trittico action determines both its uniqueness

among all other blood pressure, and the frequent effectiveness of

Trittico in cases resistant to various other

HELL (E. Freshska, 2013).

Trazodone under the trade names Trittico and Trittico

was used and is used in Europe and the USSR (and now in

post-Soviet countries) for the treatment of depressive, tre-

anxiety and dyssomnic disorders since the early 1970s

(J.Feighner, W. Boyer, 1988). In the United States, however, the Food and Drug Administration

(Food and Drug Administration, FDA) issued trazodone a solution for use under the trade name Desyrel®

only in 1981, despite the late entry to American market, already in the early 1980s, trazodone in the USA

became the most sold and most frequently prescribed of

all clinically used at that time blood pressure,

even ahead of the newly appeared at that time, very

popular and widely advertised “1st modern-

mens SSRI” – fluoxetine.The reason for such a wide

popularity and commercial success of trazodone in the USA

was its good tolerance, a small amount of PE,

in particular, the absence of M-anticholinergic action,

pronounced hypnotic and anti-anxiety effects,

its absence, in contrast fluoxetine and

other SSRIs, a tendency to give sexual AE (by

against, trazodone often improves sexual function

, impaired with depression or due to the use of other blood pressure), his lack of tendency to cause

or aggravate insomnia, anorexia, anxiety at the end of treatment

(E.Freshska, 2013).

It is interesting to note that the idea of ​​combining in one preparation the ability to inhibit the reuptake of mono-

amines (primarily serotonin) and selectively stimulate the “desired” subtype of serotonin receptors

(5-HT1A) and / or block “unnecessary” subtypes (before

only 5-HT2A / C, 5-HT3, but also 5-HT6, 5-HT7), first realized in the synthesis of trazodone, turned out to be very fruitful

creative and currently implemented in such co-

temporary multimodal blood pressure (blood pressure IV generation), as

vilazodone (Viibryd), vortioxetine (Brintellix).Thus,

, trazodone can be considered a drug, in many ways

ahead of its time. Despite the fact that trazodone

appeared on the market earlier than modern SSRIs (but later

of the short-term appearance on the market of zimelidine and

brompheniramine), it is legitimate to consider it AD III, and not

II generation, devoid of a number of PEs inherent in all

SSRIs as a class, while SSRIs can be considered as

HELL II generation (S.Stahl, 2013).

Trazodone is currently available in many

countries around the world in various forms. In the USA and non-

of which other countries it is known under the trade name

as Desyrel®, in Europe – Trittico, in Canada – Trazorel®,

in Great Britain and Ireland – Molipaxin®. In the world it is

indications and contraindications, composition and dosage – Pharmacy Mos

Dosage forms

tablets 75mg
tablets 150mg

International Non-Proprietary Name

?

Trazodone

Composition of Trittico tablets 150mg

One extended-release tablet contains: Active ingredient: trazodone hydrochloride 150.0 mg.Excipients: sucrose 84.0 mg; carnauba wax 24.0 mg; povidone 24.0 mg; magnesium stearate 6.0 mg.

Group

?

Antidepressants – Selective Neuronal Uptake Inhibitors

Manufacturers

Aziende Chimike (Italy), Andelini (Italy)

Indications for use Trittico tablets 150mg

Depression with or without anxiety.

Dosage and administration of Trittico tablets 150mg

The tablets should be taken orally 30 minutes before meals or 2 to 4 hours after meals.The tablets should be taken whole without chewing and drinking plenty of water.
Initial dose of the drug: 100 mg, taken once before bedtime after meals. On the 4th day, you can increase the dose to 150 mg. Further dose increases in order to achieve an optimal therapeutic effect should be carried out at 50 mg / day every 3 to 4 days until the optimal dose is reached.
A daily dose of more than 150 mg should be divided into 2 doses, with a smaller dose taken in the afternoon, and the main dose at bedtime.The maximum daily dose for outpatients is 450 mg. The maximum daily dose for inpatients is 600 mg.
For elderly and debilitated patients, the initial dose is up to 100 mg / day in divided doses or once at bedtime. It can be increased under the supervision of a physician, depending on the effectiveness and tolerability of the drug. A dose exceeding 300 mg / day is usually not required.

Contraindications Trittico tablets 150mg

Hypersensitivity to the active substance or any excipient; period of pregnancy; lactation period; alcohol intoxication and intoxication with sleeping pills; the safety of trazodone for children under the age of 18 has not been established, therefore, the use of the drug by children and adolescents is not recommended; deficiency of sucrase / isomaltase, fructose intolerance, glucose-galactose malabsorption, since the drug contains sucrose.With caution: the drug should be prescribed with caution to patients with AV block, myocardial infarction (early recovery period), with arterial hypertension (dose adjustment of antihypertensive drugs may be required), ventricular arrhythmia, a history of priapism, with renal and / or hepatic insufficiency.
The drug is not recommended for pregnant women.
The drug is not recommended for use during breastfeeding.

Pharmacological action

Pharmacodynamics: trazodone inhibits the neuronal reuptake of serotonin, is an antagonist of 5-HT2A / 2C-serotonin receptors and blocker of alpha1-adrenergic receptors and has an antidepressant effect.Pharmacokinetics: Absorption of trazodone from the gastrointestinal tract after oral administration is high. Taking trazodone during or immediately after a meal slows down the rate of absorption, reduces the maximum concentration of trazodone in the blood plasma, and increases the time to reach the maximum concentration (TCmax). TCmax is reached within 1/2 – 2 hours after ingestion.
Trazodone crosses the histohematogenous barriers into tissues and fluids (bile, saliva, breast milk).
Communication with plasma proteins 89 – 95%.Trazodone is metabolized in the liver, the active metabolite is 1-m-chlorophenylpiperazine. The half-life is 3-6 hours, in the second phase 5-9 hours. Excretion of most of the metabolized trazodone is carried out by the kidneys in the urine – about 75%, and is completely completed 98 hours after ingestion; with bile, about 20% is introduced. In vitro studies on human microsomes have shown that trazodone is mainly metabolized by the cytochrome P450 isoenzyme (CYP3A4 isoenzyme).

Side effects of Trittico tablets 150mg

May cause side effects, although not everybody gets them.On the part of the blood and lymphatic system: agranulocytosis, thrombocytopenia, eosinophilia, leukopenia and anemia.
From the immune system: allergic reactions.
From the endocrine system: syndrome of inappropriate secretion of antidiuretic hormone (SNS ADH).
Mental disorders: suicidal thoughts or suicidal behavior, confusion, mania, phobias, emotional instability, delirium, hallucinations.
From the nervous system: epileptic seizures, dizziness, headache, insomnia or drowsiness, amnesia, tremors, convulsions, paresthesia, impaired taste.From the side of the cardiovascular system: palpitations, tachycardia, bradycardia, ventricular extrasystoles, ventricular paroxysmal tachycardia, prolongation of the QT interval, increased blood pressure (BP), lowering blood pressure, fainting.
From the gastrointestinal tract: nausea, vomiting, dry mouth, dyspepsia; abdominal pain, diarrhea, increased salivation, paralytic intestinal obstruction.
Skin and subcutaneous tissue disorders: itching, erythematous rash, sweating.
Musculoskeletal and connective tissue disorders: myalgia, arthralgia.On the part of the kidneys and urinary tract: urinary disorders.
On the part of the genitals and mammary gland: priapism (patients who experience this side effect should immediately stop taking the drug and consult a doctor).
Others: increased fatigue, weakness, fever, flu-like syndrome.

Overdose

Symptoms: drowsiness, dizziness, nausea, vomiting.In more severe cases, coma, tachycardia, hypotension, hyponatremia, convulsions, and respiratory failure. Dysfunction of the cardiovascular system (prolongation of the QT interval, bradycardia).
After an overdose, symptoms may last for 24 hours or more.
Treatment: There is no specific antidote to trazodone. In cases of overdose, gastric lavage and the appointment of activated charcoal are necessary within 1 hour after taking the overdose. Symptomatic and supportive treatment is performed….

Interaction Trittico tablets 150mg

Trazodone can increase the effect of some antihypertensive drugs and usually requires a reduction in their doses.Simultaneous use with drugs that depress the central nervous system (including clonidine, methyldopa), enhances the effect of the latter. Blockers of h2-histamine receptors and drugs with m-anticholinergic activity enhance the m-anticholinergic effect of trazodone. Trazodone enhances and lengthens the sedative and m-anticholinergic effects of tricyclic antidepressants, haloperidol, loxaline, maprotiline, phenothiazine, pimozidan and thioxanthine. With the simultaneous use of tricyclic antidepressants and, trazodone, cardiovascular side effects may occur.MAO inhibitors increase the risk of side effects. When used together, it increases the concentration of digoxin and phenytoin in blood plasma. In vitro studies of drug metabolism indicate. on the possibility of pharmacological interaction of trazodone with inhibitors of the cytochrome P450 isoenzyme (CYP3A4 isoenzyme), such as ketoconazole, ritonavir, indinavir and fluoxetine. Inhibitors of the isoenzyme CYP3A4 can lead to a significant increase in plasma concentrations of trazodone, thereby increasing the likelihood of adverse events.Therefore, if taken in combination with potent inhibitors of the isoenzyme CYP3A4, the dose of trazodone should be reduced. When trazodone is taken in combination with carbamazepine, the plasma concentration of trazodone decreases. Therefore, patients concomitantly taking trazodone and carbamazepine should be closely monitored.

Special instructions

Suicide / suicidal ideation or worsening clinical symptoms: People with depression are at increased risk of suicidal thoughts, self-harm or suicide.The risk may last until significant remission occurs. Since improvement may not occur within the first few weeks of treatment or more, patients should be closely monitored until such improvement occurs. According to general clinical experience, the risk of suicide may increase in the early stages of recovery. It is known that patients with a history of suicidal events, or patients who exhibit a significant degree of suicidal ideation even before starting treatment, have a higher risk of suicidal ideation or attempted suicide and should be closely monitored during treatment.A meta-analysis of placebo-controlled clinical trials of antidepressants used in adults with mental disorders showed an increased risk of suicidal behavior in patients younger than 24 years of age with antidepressants compared with placebo. Close monitoring of patients, especially those at high risk, should accompany drug therapy, especially in the early stages and after dose changes. Patients (and their carers) should be warned to monitor for any clinical deterioration, suicidal behavior or suicidal thoughts, unusual changes in behavior, and immediately seek professional advice if such symptoms appear.Since the drug has some adrenergic blocking activity, the development of bradycardia and a decrease in blood pressure is possible.
Therefore, caution should be exercised when prescribing the drug to patients with a tendency to lengthen the QT interval, atrioventricular block of varying severity, patients with recent myocardial infarction. With trazodone therapy in patients with bipolar disorder, depressive attacks can range from manic-depressive to manic psychosis.In these cases, it is necessary to interrupt the treatment.
For epilepsy, trazodone should be taken with caution, in particular avoiding sudden increases or decreases in dose.
With the simultaneous use of trazodone with drugs with serotonergic activity (tricyclic antrideprinting agents, selective serotonin reuptake inhibitors, norepinephrine and serotonin reuptake inhibitors and monoamine oxidase inhibitors) and antipsychotics, serotonin syndrome may occur.With the simultaneous use of trazodone with drugs containing St. John’s wort, side effects may be more frequent.
With the use of trazodone, agranulocytosis may develop, therefore, it is recommended to carry out studies of peripheral blood, especially in the presence of sore throat when swallowing and the appearance of fever.
Trazodone is effective for sleep disorders in patients with depression, increases the depth and duration of sleep, restores its physiological structure and quality.The use of the drug does not affect body weight.
The drug is not addictive.

Storage conditions

Store out of the reach of children at a temperature not exceeding 25 ° C.

instructions for use, analogs, composition, indications

Skin rash

It has been reported about the development of skin adverse reactions, which usually appear within the first 8 weeks from the start of therapy with lamotrigine.Most rash cases were mild and self-limited, and rash cases have been reported leading to hospitalization and discontinuation of lamotrigine.

These include potentially life-threatening skin rashes such as Stevens-Johnson syndrome, toxic epidermal necrolysis, and drug reactions with eosinophilia and drug-induced systemic symptoms (DRESS), also known as hypersensitivity syndrome (HSS) (see …section “Side effects”).

In adult patients enrolled in clinical trials that were conducted using current dosing recommendations, the incidence of severe cases of skin rash was approximately 1 in 500 patients with epilepsy. Approximately half of the reported cases were Stevens-Johnson syndrome (1 in 1000). In clinical studies in patients with bipolar disorder, the incidence of severe cases of skin rash was approximately 1 in 1000.

The risk of developing severe cases of skin rash in children is higher than in adults. The available results from a large number of studies indicate that the incidence of hospitalization-related rash in children with epilepsy ranges from 1 in 300 to 1 in 100.

In children, the initial manifestation of the rash can be mistaken for an infection, doctors should be aware of the likelihood of a reaction to lamotrigine therapy in children with symptoms of rash and fever within the first eight weeks of starting the drug.

In addition, the overall risk of developing skin rash is believed to be significantly related to:

– high initial dose of lamotrigine and exceeding the recommended rate of increasing doses of lamotrigine (see section “Dosage and Administration”) – concomitant use of valproate (see section “Method of administration and doses”).

In addition, caution should be exercised when using the drug in patients with a history of allergic or skin reactions to other AEDs, since the incidence of non-serious rashes after lamotrigine in this group of patients was approximately three times higher compared with this parameter in patients without a history of allergic or skin reactions to other AEDs.

All patients (adults and children) with the development of similar symptoms should be immediately examined by a doctor and, unless another cause of the onset of symptoms is established, Lamolep should be canceled. It is not recommended to restart lamotrigine in patients who have stopped taking the drug due to the development of a rash, unless the potential benefit of prescribing the drug significantly outweighs the risk. If the patient develops Stevens-Johnson syndrome, toxic epidermal necrolysis or a drug reaction with eosinophilia and systemic symptoms caused by taking lamotrigine, do not resume taking lamotrigine.

The rash is also considered part of a hypersensitivity syndrome associated with various systemic manifestations, including fever, lymphadenopathy, facial swelling, blood and liver disorders, and aseptic meningitis (see Side Effects). This syndrome can be of any severity and, in rare cases, can lead to disseminated intravascular coagulation and multiple organ failure. It should be noted that early manifestations of hypersensitivity (eg, fever, lymphadenopathy) may occur even in the absence of overt signs of rash.With the development of such symptoms, the patient should be immediately examined by a doctor and, unless another cause of the symptoms is established, Lamolep should be canceled.

Aseptic meningitis in most cases was reversible when the drug was discontinued, however, when lamotrigine was resumed at , lamotrigine was resumed appeared again. Resuming the drug led to a rapid return of symptoms, which were often more severe. Lamotrigine should not be resumed in patients discontinued due to the development of aseptic meningitis associated with prior lamotrigine treatment.

Clinical deterioration and risk of suicide

Suicidal thoughts and behaviors have been reported in patients taking AED for some indications. A meta-analysis of randomized, placebo-controlled trials of PEP also showed a modest increase in the risk of suicidal ideation and behavior. The mechanism of this risk is unknown, the available data do not exclude the possibility of an increase in this risk when taking lamotrigine.

Thus, when taking the drug Lamolep, patients should be monitored for signs of suicidal thoughts and behavior, if necessary, appropriate therapy should be prescribed. Patients (and patient caregivers) should be advised to seek medical attention in the event of suicidal thoughts or suicidal behavior.

Patients with bipolar disorder, depending on whether they are taking medications for the treatment of bipolar disorder (including lamolep), may experience worsening depressive symptoms and / or the occurrence of suicidal thoughts or suicidal behavior.Thus, patients receiving Lamolep in connection with bipolar disorder should be carefully monitored for clinical deterioration (including the appearance of new symptoms) and suicidality, especially at the beginning of the course of the drug or when the dosage is changed. Some patients, such as those with a history of suicidal behavior or thoughts, adolescents, and those who exhibit significant suicidal behavior prior to starting treatment, have a higher risk of developing suicidal thoughts and should therefore be closely monitored during treatment. …

In patients who show worsening symptoms (including the appearance of new symptoms) and / or show suicidal thoughts or behavior, especially if these symptoms are severe, sudden and not symptoms of the patient’s illness, the possibility of changing the dosage regimen of the drug should be considered. including the possibility of interrupting the drug intake.

Hormonal contraceptives

Effect of hormonal contraceptives on the effectiveness of lamotrigine

The use of a combination of ethinylestradiol / levonorgestrel (30 μg / 150 μg) approximately doubles the clearance of lamotrigine, which leads to a decrease in the concentration of lamotrigine in the blood plasma (see.section “Interaction with other medicinal products”). A decrease in lamotrigine concentration resulted in a loss of seizure control. After dose selection, to achieve maximum therapeutic effect, in most cases, higher doses of lamotrigine will be required (no more than doubled). When you stop taking hormonal contraceptives, the clearance of lamotrigine can be halved. An increase in lamotrigine concentrations may be associated with the appearance of dose-dependent adverse events.Patient NTs should be monitored at the subject is indicated x events .

In women who do not take lamotrigine glucuronidation inducers, but take hormonal contraceptives with a 7-day break in active pill intake, a gradual transient increase in blood lamotrigine concentration will be observed during the week of taking inactive pills (see.(see section “Method of administration and dosage”). Changes in the concentration of lamotrigine in this case can b yt b are associated with with undesirable phenomena.

Therefore, continuous contraception should be considered as a first-line treatment (eg, non-interrupted hormonal contraception or non-hormonal methods of contraception).

The interaction of lamotrigine with other oral contraceptives or hormone replacement therapy has not been studied, although they may similarly affect the pharmacokinetic parameters of lamotrigine.

Effect of lamotrigine on the effectiveness of hormonal contraceptives

Interaction studies conducted in 16 healthy volunteers have shown that when lamotrigine is co-administered with hormonal contraceptives (ethinyl estradiol / levonorgestrel combination), there is a moderate increase in levonorgestrel clearance and a change in serum FSH and LH activity (see.section “Interaction with other medicinal products”). The effect of these changes on ovulatory function of the ovaries is unknown. However, the likelihood of the influence of these changes on the decrease in the effectiveness of contraception in some patients taking hormonal drugs in conjunction with lamotrigine is not excluded. For this reason, patients should be instructed to promptly report changes in their menstrual cycle, i.e. intermenstrual bleeding.

Dihydrofolate reductase

Lamotrigine has a slight inhibitory effect on dihydrofolic acid reductase, therefore, with prolonged use of the drug, an effect on folate metabolism is possible (see.(See section “Use during pregnancy and breastfeeding”). However, it was shown that lamotrigine did not cause significant changes in the concentration of hemoglobin, the average volume of red blood cells, as well as the concentration of folate in erythrocytes or serum when taking the drug for up to 1 year or the concentration of folate in red blood cells when taking the drug for up to 5 years.

Renal failure

In a study in patients with end-stage renal failure, the concentration of lamotrigine in the blood plasma did not change significantly after a single dose of the drug.However, accumulation of the glucuronide (metabolite) lamotrigine is expected to occur; therefore, caution should be exercised when taking lamotrigine in patients with renal impairment.

Patients taking other drugs containing lamotrigine

Do not use Lamolep without consulting a doctor in patients who are already taking any other drugs containing lamotrigine.

Excipients of the drug Lamolep, tablets

Lamolep tablets contain lactose monohydrate.Patients with rare hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not use this drug.

Use in children

There is a lack of information on the effects of lamotrigine on growth, puberty, and cognitive, emotional and behavioral development in children.

Precautions related to epilepsy

As with the cancellation of other AEDs, abrupt withdrawal of the drug Lamolep can provoke a relapse of seizures.With the exception of cases (for example, the appearance of a skin rash) related to the safety of the patient, requiring an abrupt discontinuation of the drug, discontinuation of the drug Lamolep should take place gradually over two weeks.

There have been several reports in the literature that severe seizures, including status epilepticus, can lead to rhabdomyolysis, multiple organ failure and disseminated intravascular coagulation, sometimes fatal. Similar cases have also been observed with lamotrigine.

Instead of improvement, there may be a clinically significant increase in seizure frequency. In patients with more than one seizure type, the observed benefit for one seizure type must be weighed against any other observed worsening of other seizure types.

Myoclonic seizures may be more severe with lamotrigine.

There is an assumption that the effectiveness of the combination of lamotrigine with drugs-inducers of enzymes is lower in comparison with the effectiveness of the combination of lamotrigine and PEP, which do not have an inducing effect on enzymes.The reason for this phenomenon is unknown.

In children taking lamotrigine for the treatment of simple minor epileptic seizures, the effectiveness of the drug is not the same in all patients.

Precautions for bipolar disorder

Children and adolescents under the age of 18

Taking antidepressants is associated with an increased risk of suicidal thoughts and suicidal behavior in children and adolescents with major depressive disorder and other mental illnesses.

Influence on the ability to drive vehicles and work with mechanisms:

Due to the differences in clinical response to all AEDs among different patients, regarding specific issues related to driving and epilepsy, patients taking Lamolep for the treatment of epilepsy should consult a doctor.

Studies of the effect of the drug on the ability to drive vehicles and mechanisms have not been conducted. Results from two studies in healthy volunteers showed that the effect of lamotrigine on fine hand-eye coordination, eye movement, body balance, and subjective sedation did not differ from placebo.In clinical trials with lamotrigine, cases of neurological adverse reactions, such as dizziness and diplopia, have been reported. Thus, before driving a vehicle or working with mechanisms, patients should observe how Lamolep affects them.

Trazodone: description, recipe, instruction

Trazodone

Analogues (generics, synonyms)

Trittico, Azona, Beneficat, Bimaran, Desirel, Menegan, Pragmarel, Sideril, Tombran, Trazolan, Geripax, Molypaxin, Pragmazin, Tramensan, Trazon Trezin

Active ingredient

Trazodonum

Pharmacological group

Antidepressants

Recipe

International:

Rp.: Sol. Trazodoni 1% – 5.0
D.t.d. No. 10 in amp.
S. According to the scheme.

Rr .: Caps. “Trazodon” 0.1 No. 25
D.S. once before bedtime 50 – 100 mg per day.

Russia:

Prescription form 107-1 / y

Pharmacological action

Antidepressant.
The mechanism of action is not fully understood. Preclinical studies have shown that trazodone selectively inhibits the reuptake of serotonin by synaptosomes in the brain and acts as a 5-HT2A / 2C serotonin receptor antagonist.Does not inhibit MAO, does not stimulate the central nervous system. It is an antagonist of alpha1-adrenergic receptors.

Relieves mental (affective tension, fear, insomnia) and somatic (palpitations, headache, myalgia, frequent urination, increased sweating) manifestations of anxiety. Increases the depth and duration of sleep in depressed patients, restores the physiological structure of sleep.

Well absorbed from the gastrointestinal tract. Taking trazodone during or immediately after a meal slows down the rate of absorption, reduces the Cmax of trazodone in the blood and increases the Tmax (Tmax is 0.5–2 hours).Plasma protein binding 89–95%. Passes through histohematogenous barriers, including the BBB. It is metabolized in the liver, mainly with the participation of the isoenzyme CYP3A4 of cytochrome P450, the active metabolite is m-chlorophenylpiperazine. T1 / 2 biphasic: the duration of the early phase is 3–6 hours, the late 5–9 hours; in some patients, cumulation is possible. It is excreted in the bile (20%) and in the urine (75%, including 70% in the form of inactive metabolites) within 98 hours after administration.

There is evidence of the effectiveness of trazodone in bulimia, kleptomania, pain syndrome in diabetic neuropathy and other types of chronic pain, phobias, incl.including agoraphobia, panic attacks, acute withdrawal symptoms in alcoholism and for the prevention of migraine.

Method of application

For adults:

Adults: the initial dose is 50-100 mg once before bedtime, the dose is increased, if necessary, by 50 mg every 3-4 days until a therapeutic effect is achieved. The maximum daily dose on an outpatient basis is 450 mg, in an inpatient setting it is 600 mg.
For debilitated and elderly patients, the initial dose is equal to 100 mg per day, can be increased, if necessary, up to 300 mg per day.
Children 6 – 18 years old: 1.5 – 2 mg / kg per day, the dose is increased, if necessary, up to 6 mg / kg per day.

Libido disorders: 50 mg per day. Impotence: 200 mg per day with monotherapy, 50 mg per day as part of complex treatment. Benzodiazepine dependence: gradually reducing the dose of benzodiazepines by 0.25 or 0.5 tablets, add 50 mg of trazodone together for 3 weeks, then continue to reduce the dose of benzodiazepines until complete cancellation, then reduce the dose of trazodone by 50 mg per day every 3 weeks.
During trazodone therapy, it is necessary to regularly conduct a general blood test (for the timely detection of blood changes), ECG monitoring in patients with diseases of the circulatory system is desirable.
Careful monitoring of patients with suicidal tendencies is necessary, especially in the first weeks of therapy. With the development of severe neutro – and leukopenia, priapism, treatment is immediately canceled; in other cases, trazodone should be withdrawn gradually. Alcohol should be avoided during trazodone therapy.Use trazodone with caution for vehicle drivers during work and for people whose activities are associated with increased concentration.

Readings

– various forms of depression (endogenous, psychotic, neurotic, somatogenic), incl. with severe anxiety, including at least 4 of the following: disturbances in sleep, appetite, psychomotor agitation or lethargy, decreased interest in the environment, decreased sexual activity, guilt, increased fatigue, slow thinking, decreased ability to concentrate, suicidal attempts / thoughts ; bulimia, kleptomania, anxiety, phobias.
– benzodiazepine drug dependence;
– acute alcohol withdrawal syndrome.
– decreased libido, impotence. Prevention of migraine attacks.

Contraindications

– ventricular arrhythmia, tachycardia, myocardial infarction (early recovery period)
– history of priapism
– pregnancy, lactation period
– hypersensitivity to trazodone.

Side effects

– From the side of the central nervous system and peripheral nervous system: drowsiness, increased fatigue, dizziness, insomnia, headache, agitation, myalgia, impaired coordination of movements, paresthesia, disorientation, darkening of consciousness, tremor.
– From the side of the cardiovascular system: arrhythmia, conduction disturbance, bradycardia, ventricular fibrillation, decreased blood pressure, orthostatic hypotension, fainting.
– From the digestive system: nausea, vomiting, diarrhea, dryness and bitterness in the mouth.
– From the side of the organ of vision: visual impairment, eye irritation.