What are the common and rare side effects of nefazodone oral? Find out the facts about this antidepressant’s side effects, uses, and warnings.

Nefazodone: Overview and Uses

Nefazodone is an antidepressant medication used to treat depression, including major depressive disorder. Unlike other antidepressants like selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants, or monoamine oxidase inhibitors (MAOIs), nefazodone is not chemically similar to these groups. Nefazodone may also be used for other purposes not listed in its medication guide.

Warnings and Precautions

Some young people have experienced thoughts about suicide when first taking an antidepressant like nefazodone. It’s important to stay alert to changes in mood or symptoms and report any new or worsening symptoms to your doctor.

You should not take nefazodone if you are allergic to it or trazodone, or if you have ever had liver problems caused by taking nefazodone. Certain other medications should not be used with nefazodone, so be sure to tell your doctor about all the medicines you use.

Nefazodone is not approved for use by anyone younger than 18 years old. Pregnant or breastfeeding women should also discuss the risks and benefits with their doctor before taking nefazodone.

How to Take Nefazodone

Follow all directions on your prescription label and take nefazodone exactly as directed. You may need to take it at the same time each day, with or without food. Your doctor may occasionally change your dose.

Be sure to tell your doctor if you have a planned surgery, as you may need to stop taking nefazodone temporarily. Store nefazodone at room temperature away from moisture and heat.

If you miss a dose, skip it and take your next dose at the regular time. Do not use two doses at once.

Common Side Effects of Nefazodone

Some of the more common side effects associated with nefazodone include:

• Drowsiness
• Dizziness
• Dry mouth
• Constipation
• Nausea
• Lightheadedness

These side effects are generally mild and tend to improve over time as your body adjusts to the medication.

Serious Side Effects and Reactions

Seek emergency medical attention if you experience signs of an allergic reaction, such as hives, difficulty breathing, or swelling of the face, lips, tongue, or throat.

Call your doctor right away if you have any new or worsening symptoms, such as:

• Changes in mood or behavior
• Anxiety, panic attacks, or trouble sleeping
• Feelings of impulsiveness, irritability, or aggression
• Thoughts about suicide or self-harm

You should also contact your doctor if you experience any of the following:

• Vision problems
• Seizures
• Lightheadedness or feeling like you might pass out
• Symptoms of mania, such as racing thoughts, increased energy, or risk-taking behavior
• Signs of liver problems, such as loss of appetite, stomach pain, tiredness, itching, dark urine, clay-colored stools, or jaundice

Dosage and Administration

The typical adult dosage for nefazodone is:

• Initial dose: 200 mg per day in two divided doses
• Maintenance dose: 300 to 600 mg per day

Dose increases should be made in increments of 100 to 200 mg per day, with at least 1 week between increases. It may take several weeks for the full effect of nefazodone to be seen.

Elderly or debilitated patients may start at a lower initial dose of 100 mg per day and have a maintenance dose up to 300 to 600 mg per day, as they may have reduced drug clearance and increased sensitivity to side effects.

Interactions and Contraindications

You must wait at least 14 days after stopping an MAOI before you can take nefazodone. You must also wait 7 days after stopping nefazodone before you can take an MAOI.

Certain other medications should not be used with nefazodone, as they can interact and cause serious side effects. Be sure to inform your doctor about all the medicines you are taking.

Avoid drinking alcohol while taking nefazodone, as it can increase the risk of side effects. You should also avoid driving or engaging in other hazardous activities until you know how nefazodone affects you, as it may impair your reactions.

Nefazodone Uses, Side Effects & Warnings

Generic name: nefazodone (ne FAZ oh done)
Brand name: Serzone
Dosage forms: oral tablet (100 mg; 150 mg; 200 mg; 250 mg; 50 mg)
Drug class: Phenylpiperazine antidepressants

Medically reviewed by Drugs.com on June 14, 2021. Written by Cerner Multum.

What is nefazodone?

Nefazodone is an antidepressant that is used to treat depression, including major depressive disorder.

Nefazodone is not chemically similar to other groups of antidepressants, such as selective serotonin reuptake inhibitors or “SSRIs”, tricyclic antidepressants, or monoamine oxidase inhibitors or “MAOIs.”

Nefazodone may also be used for other purposes not listed in this medication guide.

Warnings

Some young people have thoughts about suicide when first taking an antidepressant. Stay alert to changes in your mood or symptoms. Report any new or worsening symptoms to your doctor.

Tell your doctor about all your other medicines. Some drugs should not be used with nefazodone.

Before taking this medicine

You should not take nefazodone if you are allergic to nefazodone or trazodone, or if you have ever had liver problems caused by taking nefazodone.

Some drugs should not be used with nefazodone. Your treatment plan may change if you also use:

You must wait at least 14 days after stopping an MAO inhibitor before you can take nefazodone. You must wait 7 days after stopping nefazodone before you can take an MAOI.

Tell your doctor if you have ever had:

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.

Tell your doctor if you are pregnant or breastfeeding.

Not approved for use by anyone younger than 18 years old.

How should I take nefazodone?

Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose. Use the medicine exactly as directed.

Take the medicine at the same time each day, with or without food.

You may need frequent blood tests to check your liver function.

Your symptoms may not improve for up to several weeks.

Tell your doctor if you have a planned surgery.

Store at room temperature away from moisture and heat.

What happens if I miss a dose?

Skip the missed dose and use your next dose at the regular time. Do not use two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking nefazodone?

Avoid drinking alcohol.

Avoid driving or hazardous activity until you know how nefazodone will affect you. Your reactions could be impaired.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.

Nefazodone side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Report any new or worsening symptoms to your doctor, such as: mood or behavior changes, anxiety, panic attacks, trouble sleeping, or if you feel impulsive, irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), more depressed, or have thoughts about suicide or hurting yourself.

Call your doctor at once if you have:

• problems with vision;

• a seizure;

• a light-headed feeling, like you might pass out;

• manic episodes–racing thoughts, increased energy, decreased need for sleep, risk-taking behavior, being agitated or talkative; or

• liver problems–loss of appetite, stomach pain (upper right side), tiredness, itching, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Common side effects may include:

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Nefazodone dosing information

Usual Adult Dose for Depression:

Initial dose: 200 mg orally per day in two divided doses
Maintenance dose: 300 to 600 mg orally per day

Comments:
-Dose increases should occur in increments of 100 mg per day to 200 mg per day, on a 2 times a day schedule, and at intervals of no less than 1 week.
-Several weeks may be required for full effect.
-Patients in long-term studies were followed for up to 52 weeks; patients receiving prolonged treatment should be periodically assessed for usefulness.

Use: Treatment of depression, including major depressive disorder

Usual Geriatric Dose for Depression:

Elderly or debilitated patients:
-Initial dose: 100 mg orally per day administered in two divided doses
-Maintenance dose: Up to 300 to 600 mg orally per day

Comments:
-Since these patients often have reduced drug clearance and/or increased sensitivity to the side effects, it may be appropriate to modify the rate of subsequent dose titration.
-Several weeks may be required for full effect.
-Patients in long-term studies were followed for up to 52 weeks; patients receiving prolonged treatment should be periodically assessed for usefulness.

Use: Treatment of depression, including major depressive disorder

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What other drugs will affect nefazodone?

Using nefazodone with other drugs that make you drowsy can worsen this effect. Ask your doctor before using opioid medication, a sleeping pill, a muscle relaxer, or medicine for anxiety or seizures.

Tell your doctor about all your other medicines, especially:

• buspirone;

• digoxin;

• fluoxetine, Prozac, Symbyax;

• propranolol;

• cholesterol medication–atorvastatin, lovastatin, simvastatin;

• immunosuppressive medicine–cyclosporine, tacrolimus; or

• a sedative like Valium–alprazolam, estazolam, midazolam, triazolam, Xanax, Versed, Halcion.

This list is not complete and many other drugs may affect nefazodone. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

More about nefazodone

Consumer resources

Other brands

Serzone

Professional resources

Related treatment guides

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer

Copyright 1996-2021 Cerner Multum, Inc. Version: 8.02.

Taking Nefazodone as an Antidepressant

Nefazodone is an antidepressant that may help those who have not responded well to other antidepressants. It does carry a rare, but serious, risk of liver damage so it must be used carefully. 

Overview

Let’s learn more about nefazodone, including its black box warnings, side effects, and dosages based on information from the U.S. Food and Drug Administration (FDA). 

It’s important to note that the sale of Serzone, the brand medication of Nefazodone, was discontinued in 2003 in the United States due to the rare occurrence of severe liver damage. But generic formulations of nefazodone are still available.

Liver Failure Warning

In rare cases, people taking nefazodone have developed liver failure. If you notice any of the following symptoms, call your doctor immediately:

• Yellowing of the skin or whites of eyes (jaundice)
• Unusually dark urine
• Loss of appetite that lasts several days or longer
• Nausea
• Abdominal (lower stomach) pain
• Feeling unwell

People who already have any liver problems should not take this medication.

Doctors will regularly check your liver blood tests while taking nefazodone. 

Suicide Black Box Warning

As with all antidepressants, in the United States, nefazodone carries the black box warning regarding suicidality. Doctors prescribing this medication are advised to closely watch their patients for worsening of their depression or suicidal thoughts, especially at the start of the medication, or whenever there is a change in the dose. 

Dosage

According to the FDA, the manufacturer’s recommended starting dose is 200 mg/day in two doses, morning and evening. Dosage may be gradually increased, waiting for side effects to subside before going up to a new level. In clinical trials, the effective dose range was generally 300 to 600 mg/day. 

Some improvement, especially in anxiety and sleeplessness (if present), should be felt by the patient within the first week or two. But it can several weeks to a few months for the full benefits of nefazodone to be experienced.

Drug Interactions

Consult your doctor before taking nefazodone if you are also taking any of the following medications, because serious interactions may occur:

• Tegretol (carbamazepine) – Often prescribed as a mood stabilizer for bipolar disorder
• Any MAOI antidepressant
• Xanax (alprazolam) – An anti-anxiety medication
• Orap (pimozide) – A rarely prescribed antipsychotic medication
• Halcion (triazolam) – A rarely prescribed anti-anxiety medication

Allow two weeks between stopping any MAOI and starting nefazodone, and one week between discontinuing nefazodone and starting treatment with any MAOI.

There are many other drug interactions with nefazodone, so read the patient information accompanying your prescription completely. Notify your doctor if you discover any potential problems.

Also, the manufacturer recommends that patients notify their doctor if they become pregnant or are planning a pregnancy while on the medication.

Patients should also contact their doctor if they are breastfeeding. 

Side Effects

Nefazodone is a serotonin antagonist and reuptake inhibitor (SARI) that potently and selectively blocks postsynaptic serotonin (5-hydroxytryptamine; 5-HT) 5-HT2A receptors and moderately inhibits serotonin and noradrenaline (norepinephrine) reuptake. Unlike the SSRI antidepressants, nefazodone associated with minimal weight gain and minimal sexual side effects.

In addition, the reported activation of mania/hypomania may be lower with nefazodone than with some other antidepressants in bipolar patients. That being said, some risk remains, so patients should be monitored by their doctor for the onset of mania or hypomania when taking this or any antidepressant.

Most common side effects include:

• Sleepiness
• Dry mouth
• Nausea
• Constipation
• Weakness
• Dizziness
• Problems with vision
• Lightheadedness
• Confusion

What Should I Do?

If your doctor is considering nefazodone for your depression, be sure you follow up with him closely.  

Nefazodone tablets

What is this medicine?

NEFAZODONE (nef AY zoe done) is used to treat depression.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

COMMON BRAND NAME(S): Serzone

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:

• bipolar disorder or mania
• glaucoma
• heart disease
• liver disease
• seizures
• suicidal thoughts, plans, or attempt; a previous suicide attempt by you or a family member
• an unusual or allergic reaction to nefazodone, other medicines, food, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. You may take this medicine with or without food. Take your medicine at regular intervals. Do not take your medicine more often than directed. Do not stop taking this medicine suddenly except upon the advice of your doctor. Stopping this medicine too quickly may cause serious side effects or your condition may worsen.

A special MedGuide will be given to you by the pharmacist with each prescription and refill. Be sure to read this information carefully each time.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.

NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

What may interact with this medicine?

Do not take this medicine with any of the following medications:

• carbamazepine
• cisapride
• duloxetine
• eplerenone
• ergot alkaloids like dihydroergotamine, ergotamine, methysergide
• linezolid
• lovastatin
• medicines called MAO Inhibitors like Nardil, Parnate, Marplan, Eldepryl
• methylene blue
• naloxegol
• pimozide
• ranolazine
• simvastatin
• SSRIs like citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline
• trazodone
• triazolam
• venlafaxine
• red yeast rice

This medicine may also interact with the following medications:

• atorvastatin
• buspirone
• cyclosporine
• desipramine
• digoxin
• erythromycin
• general anesthetics
• haloperidol
• ketoconazole
• lithium
• medicines for anxiety or sleeping problems, such as alprazolam, diazepam, or clonazepam
• phenytoin
• tacrolimus
• warfarin

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Tell your doctor if your symptoms do not get better or if they get worse. Visit your doctor or health care professional for regular checks on your progress. Because it may take several weeks to see the full effects of this medicine, it is important to continue your treatment as prescribed by your doctor.

Patients and their families should watch out for new or worsening thoughts of suicide or depression. Also watch out for sudden changes in feelings such as feeling anxious, agitated, panicky, irritable, hostile, aggressive, impulsive, severely restless, overly excited and hyperactive, or not being able to sleep. If this happens, especially at the beginning of treatment or after a change in dose, call your health care professional.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water will help. Contact your doctor if the problem does not go away or is severe.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:

• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• changes in vision
• confusion
• elevated mood, decreased need for sleep, racing thoughts, impulsive behavior
• eye pain
• feeling faint or lightheaded, falls
• feeling agitated, angry, or irritable
• fever or chills, sore throat
• hallucination, loss of contact with reality
• irregular heartbeat
• loss of balance or coordination
• painful or prolonged erections
• redness, blistering, peeling or loosening of the skin, including inside the mouth
• restlessness, pacing, inability to keep still
• seizures
• signs and symptoms of liver injury like dark yellow or brown urine; general ill feeling or flu-like symptoms; light-colored stools; loss of appetite; nausea; right upper belly pain; unusually weak or tired; yellowing of the eyes or skin
• stiff muscles
• suicidal thoughts or other mood changes
• trouble passing urine or change in the amount of urine
• trouble sleeping
• vomiting

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):

• change in sex drive or performance
• constipation
• dizziness
• dry mouth
• indigestion, stomach upset
• nausea

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature below 40 degrees C (104 degrees F). Keep container tightly closed. Throw away any unused medicine after the expiration date.

NOTE: This sheet is a summary. It may not cover all possible information. If you have questions about this medicine, talk to your doctor, pharmacist, or health care provider.

Memorial Sloan Kettering Cancer Center

This information from Lexicomp^® explains what you need to know about this medication, including what it’s used for, how to take it, its side effects, and when to call your healthcare provider.

Warning

• Drugs like this one have raised the chance of suicidal thoughts or actions in children and young adults. The risk may be greater in people who have had these thoughts or actions in the past. All people who take this drug need to be watched closely. Call the doctor right away if signs like low mood (depression), nervousness, restlessness, grouchiness, panic attacks, or changes in mood or actions are new or worse. Call the doctor right away if any thoughts or actions of suicide occur.
• This drug is not approved for use in children. Talk with the doctor.
• Liver problems have happened with this drug. Sometimes, this has been severe and has led to a liver transplant or death. If you have questions, talk with the doctor.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• If you have liver disease, talk with your doctor.
• Call your doctor right away if you have signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.

What is this drug used for?

• It is used to treat low mood (depression).

What do I need to tell my doctor BEFORE I take this drug?

• If you are allergic to this drug; any part of this drug; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
• If you have had liver problems in the past while taking this drug.
• If you are taking any of these drugs: Astemizole, carbamazepine, cisapride, pimozide, terfenadine, or triazolam.
• If you have taken certain drugs for depression or Parkinson’s disease in the last 14 days. This includes isocarboxazid, phenelzine, tranylcypromine, selegiline, or rasagiline. Very high blood pressure may happen.
• If you are taking any of these drugs: Linezolid or methylene blue.

This is not a list of all drugs or health problems that interact with this drug.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this drug with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take this drug?

• Tell all of your health care providers that you take this drug. This includes your doctors, nurses, pharmacists, and dentists.
• Avoid driving and doing other tasks or actions that call for you to be alert until you see how this drug affects you.
• To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
• It may take several weeks to see the full effects.
• Avoid drinking alcohol while taking this drug.
• Talk with your doctor before you use marijuana, other forms of cannabis, or prescription or OTC drugs that may slow your actions.
• If you are 65 or older, use this drug with care. You could have more side effects.
• Tell your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

What are some side effects that I need to call my doctor about right away?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Very bad dizziness or passing out.
• Seizures.
• Feeling confused.
• Fever, chills, or sore throat.
• Some people may have a higher chance of eye problems with this drug. Your doctor may want you to have an eye exam to see if you have a higher chance of these eye problems. Call your doctor right away if you have eye pain, change in eyesight, or swelling or redness in or around the eye.
• Call your doctor right away if you have a painful erection (hard penis) or an erection that lasts for longer than 4 hours. This may happen even when you are not having sex. If this is not treated right away, it may lead to lasting sex problems and you may not be able to have sex.

What are some other side effects of this drug?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Feeling dizzy, sleepy, tired, or weak.
• Headache.
• Upset stomach.
• Diarrhea or constipation.
• More hungry.
• Dry mouth.
• Trouble sleeping.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to your national health agency.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

How is this drug best taken?

Use this drug as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take with or without food.
• Keep taking this drug as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

• Skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

How do I store and/or throw out this drug?

• Store at room temperature.
• Store in a dry place. Do not store in a bathroom.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.

General drug facts

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else’s drugs.
• Some drugs may have another patient information leaflet. If you have any questions about this drug, please talk with your doctor, nurse, pharmacist, or other health care provider.
• This drug comes with an extra patient fact sheet called a Medication Guide. Read it with care. Read it again each time this drug is refilled. If you have any questions about this drug, please talk with the doctor, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Consumer Information Use and Disclaimer

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine. The use of this information is governed by the Lexicomp End User License Agreement, available at https://www. wolterskluwer.com/en/solutions/lexicomp/about/eula.

Last Reviewed Date

2019-11-08

Copyright

© 2021 UpToDate, Inc. and its affiliates and/or licensors. All rights reserved.

Nefazodone Drug Information – Indications, Dosage, Side Effects and Precautions

Generic Name : Nefazodone

Pronunciation : neff-AZ-oh-done

Latest prescription information about Nefazodone. Learn how to pronounce the drug’s name, its indications, dosage, how to take, when to take, when not to take, side effects, special precautions, warnings and its storage instructions . Also listed are the International and Indian trade name(s) of the drug and its price list.

ICD Code : Y49.2 |

Therapeutic Classification : Psychotherapeutics

Note: The brand is not available in US market.

This medication is a phenylpiperazine antidepressant, prescribed for depression.  It increases the amount of certain natural substances in the brain that are needed to maintain mental balance.

Contraindicated in patients who experienced liver injury due to previous administration of this drug; co-administration with terfenadine, astemizole, cisapride, pimozide, or carbamazepine is contraindicated.

Adult- PO- The recommended starting dose is 200 mg, 2 times per day.

It comes as a tablet to take by mouth, with or without food.

Caution should be exercised in patients with seizures, heart attack, chest pain, stroke, or other heart disease, liver disease, stomach bleeding, suicidal tendencies, who are taking other medications, any allergy, during pregnancy and breastfeeding.

It may cause drowsiness, dizziness, blurred vision, or lightheadedness, do not drive a car or operate machinery while taking this medication.

Avoid alcohol consumption.

Monitor liver function, kidney function, and complete blood cell counts regularly while taking this medication.

Patient may develop with increased risk of suicidal thoughts; watch them carefully.

   Most Common :


Drowsiness, dry mouth, dizziness, constipation, weakness, lightheadedness, blurred vision, confusion and abnormal vision.



   Body as a Whole :

Headache, infection, flu syndrome, chills, fever, neck rigidity.


   Heart :

Low blood pressure, dilatation of blood vessels.


   Skin :

Itching, rash.


   Gastrointestinal :

Indigestion, diarrhea, increased appetite, nausea, vomiting.


   Metabolic :

Swelling in the extremities, increased thirst.


   Musculoskeletal :

Joint pain.


   Central Nervous system :

Sleeplessness, confusion, memory impairment, tingling, abnormal dreams, concentration decreased, incoordination, tremor, increased muscle tone, decreased libido.


   Respiratory :

Inflammation of pharynx, increased cough.


   Eye and ENT :

Blurred vision, abnormal vision, ringing in the ear, taste perversion.



   Genitourinary :
Urinary frequency, urinary tract infection, urinary retention, vaginal inflammation, breast pain.

COGNITIVE AND DRIVING PERFORMANCE EFFECTS OF NEFAZODONE AND IMIPRAMINE IN HEALTHY VOLUNTEERS

Nefazodone is a new serotonergic antidepressant that produces fewer side effects than tricyclic antidepressants. The present study compared the acute and subchronic effects of nefazodone and the tricyclic antidepressant imipramine on driving performance, cognitive functions and daytime sleepiness. Twenty-four healthy subjects received the treatments for seven days with a seven days washout period. Measurements included a standard over-the road driving test, a psychomotor test battery and sleep latency tests, using objective EEG recordings. The results showed that imipramine had a detrimental effect after a single dose on driving performance that diminished after repeated dosing. Minor impairment of psychomotor test performance was found on both days. A single administration of both doses of nefazodone did not impair driving performance, and had also no or only minor effects on psychomotor performance. Repeated doses of nefazodone produced slight driving performance impairment. Cognitive and memory functions as measured in the psychomotor tests were modestly impaired by nefazodone. Alerting effects of single doses of nefazodone were found in the sleep latency tests. Neither drug induced daytime sleepiness. Effects on memory were significantly related to steady state plasma concentrations of both nefazodone and imipramine. (a) For the record of the covering entry of this conference, please see IRRD abstract no 868581.

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  NH&MRC ROAD ACCIDENT RESEARCH UNIT

  UNIVERSITY OF ADELAIDE
  ADELAIDE, SOUTH AUSTRALIA 
  Australia 
  5005

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  Authors:
  • VAN LAAR, M W
  • VOLKERTS, E R

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  Publication Date: 1995

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  Accession Number: 00731317
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  Source Agency: ARRB
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  ISBN: 0-908204-21-3
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  Created Date:
  Feb 27 1997 12:00AM

Focus on Nefazodone

by Dr Ivan Goldberg, MD

Nefazodone is a relatively new antidepressant with a chemical
structure that is somewhat similar to that of the phenylpiperazine antidepressant,
trazodone.

The antidepressant action of nefazodone is thought to be dependent
on its ability to block postsynaptic serotonin type-2 receptors and inhibit presynaptic
serotonin reuptake. Nefazodone also blocks norepinephrine reuptake. Nefazodone does not
have a chemical structure similar to the SSRIs, tricyclic anti- depressants, monoamine
oxidase inhibitors, bupropion, or venlafaxine.

2. How does nefazodone differ from other
antidepressants?

One possibly important way in which nefazodone differs from other
SSRIs is that while use of SSRIs is often associated with sexual dysfunction, and sleep
disturbances, these side effects have been reported infrequently in people taking
nefazodone.

3. What kinds of depression can be treated with
nefazodone?

While the pre-marketing studies were restricted to patients with a
DSM-III-R diagnosis of non-melancholic Major Depressive Disorder, it is expected that
nefazodone will be prescribed for patients with Dysthymia, Major Depression, and Bipolar
Disorder.

Although nefazodone has mostly been studied for periods of admin-
istration of up to 8-weeks, it is expected that patients with long-standing depressions
will take the drug for longer periods of time. Data on about 250 patients who took
nefazodone for 12 or more months, did not reveal any problems with administration for that
length of time.

As yet, there is no data on the effectiveness of nefazodone when
used to treat patients whose depressions were so severe as to make hospitalization
necessary

4. What are the side-effects of nefazodone?

The side-effects that occurred significantly more commonly in people
taking nefazodone as compared to placebo are:

Side effect % of nefazodone treated patients Dry mouth 25%
Sleepiness/sedation 25% Nausea 22% Dizziness 17% Visual problems 16% Weakness 11%
Lightheadedness 10% Confusion 7%: Orthostatic hypotension 5% Note: The Psychopharmacology
Forum of InterPsych has received one report of inappropriate erections in a patient taking
nefazodone. It is expected that priapism will be reported shortly as inappropriate
erections and priapism are often associated.

5. Which side effects force people to stop taking
nefazodone?

In the premarketing studies 16% of the 3496 depressed patients
taking nefazodone discontinued the medication because of side- effects. The side effects,
that the patients cited as the reason they dropped out that were mentioned at least twice
as often for nefazodone as compared to placebo are:

6.

Are there any special hazards for people with
bipolar disorder?

As with other antidepressants, people with bipolar disorder who are
not being treated with a mood regulator such as lithium, valproate, or carbamazepine, may
be pushed into a manic episode when treated with nefazodone. In the pre- marketing
studies, the rate of manic episodes in patients with bipolar disorder was 1.6%

7. Does nefazodone interact with other
medications?

Nefazodone increases the blood level of Seldane and Hismanal to
possibly life-threatening levels. These antihistamines should never be taken while taking
nefazodone.

The blood levels of Halcion and Xanax are also increased by
nefazodone. If Halcion is taken with nefazodone, its dose should be reduced by 75%. A
reduction of 50% in the dose of Xanax is suggested if it is taken with nefazodone.

8.

Does nefazodone interact with alcohol?

Although nefazodone has not been found to increase the impairment of
cognitive or motor skills caused by alcohol, the manufacturer warns against drinking while
taking nefazodone.

9. Is nefazodone safe for a woman who is
pregnant, about to become pregnant, or nursing an infant?

There is no data to establish the safety of nefazodone for the fetus
or nursing infant.

10. Is nefazodone a satisfactory antidepressant for
children and adolescents?

Although here have been no published studies on the use of
nefazodone for the treatment of children and adolescents with depression, it is expected
that the drug will be prescribed for depressed children and adolescents.

11. Is nefazodone a satisfactory antidepressant
for the elderly?

No special problems were encountered when nefazodone was studied in
a group of 500 people over the age of 65 with depression. As with most drugs, when
administered to the elderly, it is useful to start low and go slow.

12. How is treatment with nefazodone initiated?

Most psychiatrists start people with depression on 50 mg or 100 mg
of nefazodone twice a day. At intervals of about one-week, the dose can be increased by
100 mg per day.

When nefazodone was first was released in the US the usual starting
dose for adults was 100 mg twice a day. As many people found this dose to be too high, it
has been replaced by a lower initial dose

When nefazodone is given to elderly patients the starting dose is
usually 50 mg twice a day.

13. What is the usual final dose of nefazodone?

While doses up to 600 mg per day are approved by the FDA, some
severely depressed patients have been treated with higher doses. Most depressed people
respond to doses under 600 mg per day.

14. How rapidly may a person with depression feel
some relief from taking nefazodone?

While most people taking nefazodone become aware of some lessening
of depression within two to four weeks, there are some who experience relief within the
first week and others who only experience relief after a many weeks of therapy.

15. Are there withdrawal effects if nefazodone
is suddenly discontinued?

A withdrawal syndrome following the abrupt discontinuation of
nefazodone has not been described. Because the half-life of nefazodone and its active
metabolites are 18-hours or less, it is prudent to taper nefazodone than abruptly
discontinue it.

16. Is nefazodone toxic if an overdose is taken?

Seven overdoses of nefazodone have been reported. The highest
reported overdose was 11,200 mg. In some cases nefazodone was taken along with alcohol
and/or other medications. All seven people who took an overdose recovered.

17. What precautions are necessary when switching
between nefazodone and a MAO inhibitor?

When switching from an MAO inhibitor to nefazodone, there should be
a 14-day interval between the discontinuation of the MAOI and the initiation of nefazodone
therapy. When switching from nefazodone to an MAOI a 7-day interval is adequate, because
of nefazodone’s short half-life.

18. Might nefazodone be effective when a person
has not responded to other antidepressants?

Although there is no data on this, it is expected that some
individuals who have failed to be helped by other antidepressants will be helped by
nefazodone.

19. What are the advantages of nefazodone?

The low incidence of sexual side effects and disturbed sleep are
possible advantages of nefazodone.

20. Has nefazodone been available in other
countries? What do psycho- pharmacologists from those countries think of the drug?

Nefazodone has been available in Canada for over six months. Most of
the psychopharmacologists to whom I have spoken think that it is less effective than the
SSRIs, and some have stopped writing prescriptions for it. Most of the nefazodone being
prescribed in Canada is prescribed by nonpsychiatric physicians, not by psychiatrists.

21. What did the Medical letter conclude about
nefazodone?

The Medical Letter [1995, 37 (946), 33-35] concluded its review of
nefazodone with the words: “Available data are inadequate to determine how nefazodone
compares with other antidepressants. Better established drugs are preferred.”

22. Additions and corrections to:Dr Ivan Goldberg, MD

Psychiatry On-Line, 1995-9

Serotonin neurotransmission and treatment options for depression

The neurobiological basis of depression is not fully understood. At the same time, the monoamine hypothesis, which appeared in the 70s of the last century, remains relevant and very convincing, according to which mood disorders are associated with impaired synaptic transport of serotonin, norepinephrine and dopamine. The validity of this hypothesis is proved not only by modern research, but also by the clinical effects of antidepressants ^{1 ᠎} .

Antidepressants used in modern psychiatric practice can be systematized (taking into account different classifications) approximately as follows ^{2 ᠎} .

– tricyclic antidepressants (TCAs): imipramine, clomipramine, amitriptyline;

– tetracyclic antidepressants: maprotiline;

– monoamine oxidase inhibitors (IMAO ^{3 ᠎} ): pirlindol, moclobemide;

– serotonin antagonists and inhibitors of its reuptake ( serotonin antagonists and reuptake inhibitors , SARI ): trazodone, nefazodone;

– selective serotonin reuptake inhibitors (SSRIs): fluoxetine, fluvoxamine, paroxetine, sertraline, citalopram, escitalopram;

– selective serotonin and norepinephrine reuptake inhibitors (SNRIs): venlafaxine, duloxetine, milnacipran;

– norepinephrine reuptake inhibitors: atomoxetine ^{4 ᠎} , reboxetine, viloxazine;

– norepinephrine and dopamine reuptake inhibitors: bupropion;

– noradrenergic and specific serotonin antidepressants , NaSSA ): mirtazapine, mianserin;

– serotonin modulators and stimulants: vilazodone, vortioxetine;

– melatonergic antidepressants: agomelatine.

The disadvantage of the modern classification of antidepressants is its eclecticity: some groups of drugs are distinguished on the basis of the predominant type of pharmacological action (for example, suppression of presynaptic serotonin uptake), others on the basis of structural features. The TCA group is heterogeneous in terms of pharmacological properties of drugs: for example, clomipramine and imipramine predominantly inhibit serotonin reuptake and to a much lesser extent prevent presynaptic uptake of norepinephrine, while amitriptyline has a balanced effect on both of these neurotransmitters.The imperfect and, to some extent, conditional nature of the given taxonomy is also manifested in the fact that, for example, mirtazapine in different classifications is referred to both TCA (in terms of chemical structure) and NaSSA (based on the characteristics of pharmacological mechanisms). Although SSRIs are considered selective serotonergic antidepressants, all six drugs in this group also (to varying degrees) affect the synaptic transport of norepinephrine and dopamine.

The list presented begins with TCAs and MAOIs as first-generation antidepressants, although, in accordance with current international and many national clinical guidelines, the first choice drugs in the treatment of depression and anxiety disorders are SSRIs, which is determined by the optimal balance of their effectiveness and tolerance. …

Of course, for the successful treatment of depression, it is important to improve the interneuronal transmission of three key monoamines – serotonin, norepinephrine and dopamine, but it is believed that an increase in the neurotransmission of serotonin plays a special role in the clinical efficacy of modern antidepressants [1].

The following groups of drugs have serotonergic properties: TCAs, tetracyclic antidepressants, MAOIs, SARI, SSRIs, SNRIs, NaSSA, as well as serotonin modulators and stimulants.

TCAs – especially clomipramine – show a significant ability to facilitate the synaptic transport of serotonin and demonstrate high efficacy in the treatment of depression, including its most severe, including psychotic, forms. Significant disadvantages of TCAs include frequent side effects (including cardiotoxicity and the ability to provoke the development of type 2 diabetes mellitus) and poor overall tolerance.

SSRIs, as first-line drugs in the treatment of depression and anxiety disorders, are much better tolerated by patients with TCAs and other first-generation antidepressants, but they are also not completely free of adverse events; Sexual dysfunction – most often decreased libido and decreased erection (in men) – is a typical cause of premature withdrawal of SSRIs.

An intermediate position between TCAs and SSRIs is occupied by SARI, and primarily trazodone ^{5 ᠎} .

Trazodone is the first serotonergic antidepressant ^{6 ᠎} , proposed for clinical use in the treatment of depression in 1981 and preceded by the appearance of fluoxetine seven years later, followed by other SSRIs. Trazodone is marketed on the Russian pharmaceutical market under the name Trittico.

Trazodone affects various types of serotonin receptors. The predominant pharmacological effect of trazodone is considered to be the antagonistic effect on serotonin 5-HT _2A – and 5-HT _2C – receptors ^{7 ᠎} ; a certain value in the antidepressant effect of the drug is also attached to the suppression of the reuptake of serotonin, which brings trazodone closer to SSRIs and SNRIs.The complex effect of trazodone on the neurotransmission of serotonin makes it possible to consider it as a multifunctional serotonergic antidepressant [2].

Trazodone is used in many countries as a treatment for major depressive disorder in adults. Clinical studies indicate a significant efficacy of trazodone in the treatment of depression, comparable to that of TCAs, SSRIs and SNRIs [3]. Pronounced thymoanaleptic properties and proven clinical efficacy make it possible to prescribe trazodone for depression of varying severity; in addition, the drug is used to augment (enhance) the action of other antidepressants, including SSRIs such as fluoxetine [4].

If the combination of two antidepressants is customary in clinical practice, then the advisability of the simultaneous prescription of three antidepressants is controversial to many specialists and causes debate, mainly due to the increase in the overall risk of side effects of therapy. Emphasizing the controversial nature of the simultaneous use of three antidepressants, R. Lopes et al. [15] described a case of successful treatment of therapeutically resistant depression by adding trazodone to an insufficiently effective combination of paroxetine and mirtazapine.

Due to its multifunctional effect on serotonin receptors, trazodone is especially effective in the treatment of depression accompanied by insomnia and anxiety [6]. According to E. Frecska [7], the introduction of trazodone, which has hypnotic and anxiolytic (anti-anxiety) effects, into the widespread practice of treating depression, makes it possible to reduce the need for benzodiazepines as an additional component of antidepressant therapy.

A wide range of pharmacological effects of trazodone served as the basis for its use in clinical practice in a number of countries, along with the treatment of depression for additional indications, and primarily for the treatment of insomnia.The drug is most commonly used in the treatment of sleep disorders in the USA ^{8 ᠎} ; trazodone is invariably included in the list of antidepressants with hypnotic effects, and often leads this list [8, 9].

In addition to the treatment of depression and insomnia, trazodone is used in the treatment of generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, bulimia nervosa, alcohol dependence and dependence on benzodiazepines ^{9 ᠎} , as well as neuropathic pain and other chronic pain syndromes [7 , 10].

According to some reports, trazodone has a moderate beneficial effect on the negative symptoms of schizophrenia, and also in some cases contributes to the reduction of delusional disorders resistant to antipsychotics [7, 11]. In the practice of treating elderly patients, the ability of trazodone has been noted not only to alleviate the negative symptoms of schizophrenia, but also to reduce the manifestations of tardive dyskinesia [12].

Improving sleep under the influence of trazodone expands the indications for its use in combination therapy for depression: on the one hand, the drug is prescribed in addition to other antidepressants in order to augment their thymoanaleptic effect, and on the other hand, it is used as a corrector to eliminate anxiety and insomnia caused by others. antidepressants, including fluoxetine, bupropion, and monoamine oxidase inhibitors [7].

It should be noted that the obvious hypnotic effect of trazodone entailed certain undesirable consequences: many doctors stopped perceiving the drug as a significant treatment for major depressive disorder and prescribe it mainly for the treatment of insomnia, which does not allow full use of the therapeutic potential of trazodone and significantly narrows the range patients who can benefit from this antidepressant; in other words, trazodone can and should be prescribed in the treatment of depression, whether it is accompanied by sleep disorders or not.

Showing efficacy in the treatment of depression comparable to that of other antidepressants, trazodone is better tolerated not only by TCAs, but also by newer generation drugs; its appointment as an alternative to SSRIs avoids such undesirable effects associated with taking the latter, such as anxiety, insomnia and sexual dysfunction [3].

The high adherence of patients to trazodone therapy is largely due to the lack of the ability to impair sexual function.On the contrary, trazodone is able to enhance libido (in both men and women) and even, in some cases, cause priapism; however, the incidence of this side effect does not exceed 0.01% [13-17]. Unlike a number of antidepressants, trazodone does not cause or increase movement disorders, in particular, restless legs syndrome and periodic limb movements [18]. A significant advantage of trazodone in comparison with some new generation antidepressants that promote adherence to therapy (especially in women) is the lack of its effect on body weight [7].

Unlike TCAs, which can increase insulin resistance and provoke the development of type 2 diabetes mellitus and aggravate its course, trazodone does not adversely affect carbohydrate metabolism [16].

Effects on anxiety and sleep disorders, combined with good tolerance, including in elderly patients, make trazodone one of the drugs of choice for the treatment of depression in later life; in addition, the indication for the appointment of trazodone is depression, comorbid with dementia or psychomotor agitation; there was also an increase in the quality of life of patients with cerebral atrophy under the influence of trazodone [6].

Proven clinical efficacy, comparable to the efficacy of TCAs, SSRIs and SNRIs, combined with good tolerance, warrants the question of re-discovery ( English: rediscovering) trazodone for the practice of treating depression [3].

Summarizing the data from various studies, A. Fagiolini et al. [3] concluded that trazodone is an effective and well-tolerated antidepressant that plays an important role in the modern treatment of major depressive disorder, both as a monotherapy and as a component of combination therapy. They emphasize that trazodone can control a wide range of symptoms of depression and does not negatively affect sleep, but rather has the ability to significantly improve sleep function.

In conclusion, it can be added that trazodone, the high clinical efficacy of which was actively discussed in scientific publications of the 80s and 90s of the previous century, is currently undeservedly forgotten for a number of reasons, although the pharmacological spectrum of this drug provides every reason for its successful use in the treatment of depression (as well as a number of other mental disorders) as an alternative to both TCAs and newer antidepressants.

Conflict of interest: This article was prepared with the support of the pharmaceutical company CSC.

90,000 uses and side effects of this antidepressant

Throughout history, several psychopharmaceuticals have been developed to treat various disorders and diseases, both physical and mental. Among the various mental disorders, depression is one of the most common, resulting in the synthesis of various types of substances to combat their symptoms.

One of them is nefazodone, a little-known antidepressant that we will talk about in this article.

• You may be interested: “Psychotropic drugs: drugs that act on the brain”

Nefazodone: the main characteristics of the drug

Nefazodone is a psychotropic antidepressant drug derived from phenylpiperazines and is synthesized to relieve and treat the symptoms of depression : Low mood, lack of motivation, anhedonia, passivity, and trouble sleeping, among others.

It is part of the so-called atypical antidepressants, since its mechanism of action does not coincide with the mechanism of action of other antidepressants. In particular, it will be part of a group of drugs known as mild serotonin, norepinephrine and dopamine reuptake inhibitors or SDRI like mazindol. Other substances function similarly, although they work through different mechanisms of action, such as ketamine, cocaine, and ecstasy.

As with most antidepressants, it takes time to make the necessary changes in the brain to visualize the real effect, this time about four weeks.This drug is an effective antidepressant that also has with the advantage of not causing much sexual changes, weight gain or appetite changes.

However, despite the fact that it is an effective antidepressant, its prescription is not routine, and in fact, between 2003 and 2004, its marketing was suspended in various countries (including Spain and the United States), as it was shown that it can pose a high health risk.While highly toxic at the liver level, it can even lead to death.

• Related article: “Types of antidepressants: characteristics and effects”

Mechanism of action

The main mechanism of action of nefazodone is its action on the receptors of various monoamines: serotonin, dopamine and norepinephrine. Similar to non-selective MAOIs, the effects of the three main monoamines are increased, but at a weaker and more controlled level.

It mainly acts as a 5-HT2 serotonin receptor antagonist at the postsynaptic level, while at the same time inhibiting its reuptake.This leads to an increase in the level of serotonin in the brain. It also helps to inhibit the reuptake of norepinephrine and dopamine, albeit at much lower levels. Finally, also has a minor effect on the level of histamine and acetylcholine , but these latter are practically not noticeable.

Uses and Applications of this Medication

Nefazodone is mainly known as an antidepressant, the main indication of which is severe depression. It is also used for premenstrual syndrome or other types of depression, such as those associated with suffering from various pathologies.However, in addition to activities for depressive disorders This drug may be useful in the treatment of other psychopathologies and problems.

Among them, we see that nefazodone is useful in treating various anxiety problems and PTSD and insomnia problems, although it increases REM sleep latency.

Side effects of this antidepressant

Despite the great benefits, the consumption of nefazodone can cause various side effects, and in some cases may have its own risks, there are various contraindications.

The most common side effects of nefazodone are dry mouth and drowsiness, as well as nausea and dizziness. Confusion, vision problems, and asthenia are also relatively common. Hypotension and bradycardia are rarely observed, which is dangerous, especially for those patients who already suffer from cardiac pathology.

However, the most serious problem associated with this drug (and which actually led to the termination of its commercialization) is its high hepatotoxicity.In some cases, liver failure is observed, which can even lead to death or jaundice. That is why, if prescribed (something not very common), it is necessary to constantly monitor the health of the patient’s liver , periodically conducting tests. It can also have renal effects, eliminating the drug mainly this way.

Another aspect to consider is the risk of developing serotonin syndrome, a problem caused by excess serotonin (often caused by overdose or drug interactions). may cause anxiety, impaired consciousness, hyperactivity, tremors, vomiting , tachycardia, impaired motor coordination, mydriasis, seizures, breathing problems, or even death.

Contraindications

With regard to contraindications, one of the main ones occurs in those people who already suffer from liver problems, as well as from coronary disorders. also is contraindicated in people who use certain drugs and especially MAOIs, as it can cause serotonin syndrome and even cause death.

Its administration with SSRI is not recommended as they interact. Likewise, some retroviral drugs, such as those used with HIV, interact with this substance, because it is necessary that when using nefazodone (for the treatment of depression associated with the condition of this disease), the doses and possible interactions are largely regulated.

Children and pregnant women should not take this medicine. In addition, people with epilepsy or a history of suicide attempts should not use this medication or do so with extreme caution.This is generally not recommended for bipolar disorder.

Bibliographic references:

• Jufe G. (2001). Practical psychopharmacology. Buenos Aires, Edited by Polemos.
• McConville, B.J .; Cheney, R.O .; Brown, K.L. et al. (1998). Newer antidepressants – outside of SSRI. Ped Clin North Am. 45: 1157-71.
• Tatsumi, M .; Groshan, K .; Blakely, R.D. & Richelson E. (1997). “Pharmacological profile of antidepressants and related compounds in human monoamine transporters.”Eur J Pharmacol. 340 (2-3): 249-258.

Latuda – indications for use (July 2021).

Nefazodone: Uses and side effects of this antidepressant – Psychology

2021

This medicine is especially used for depressive disorders. Throughout history, many psychotropic drugs have been developed to treat various disorders and diseases, such as

Contents

This medicine is especially used in depressive disorders.

Throughout history, many psychotropic drugs have been developed to treat various disorders and diseases, both physical and mental. Among the various mental disorders, depression is one of the most common, resulting in the synthesis of several types of substances to combat its symptoms.

One of them is nefazodone, a little-known antidepressant. and used, which we will talk about in this article.

• You may be interested in: “Psychopharmaceuticals: drugs acting on the brain”

Nefazodone: main characteristics of the drug

Nefazodone is a psychotropic antidepressant drug derived from phenylpiperazines and synthesized for the relief and treatment of symptoms of depression: bad mood, lack of motivation, anhedonia, passivity and sleep problems, among others.

It is a part of the so-called atypical antidepressants, since its mechanism of action does not coincide with the mechanism of action of other antidepressants. In particular, it will be part of a group of drugs known as mild serotonin, norepinephrine and dopamine reuptake inhibitors or SDRI, such as mazindol. Other substances act in a similar way, although they work through other mechanisms of action, such as ketamine, cocaine, and ecstasy.

As with most antidepressants, it takes about four weeks for the brain to undergo the necessary changes to see the real effect.This drug is an effective antidepressant that also has with the advantage of causing almost no changes at the sexual level, weight gain or appetite disturbances.

However, although it is an effective antidepressant, its prescriptions are not common and in fact, its marketing was suspended in various countries (including Spain and the United States) between 2003 and 2004 because it has been shown to pose a high risk for health. very toxic at the liver level and can even be fatal.

• Related article: “Types of antidepressants: characteristics and action”

Mechanism of action

The main mechanism of action of nefazodone is its action on the receptors of various monoamines: serotonin, dopamine and norepinephrine. Like non-selective MAOS, it potentiates the action of the three main monoamines, but at a weaker and more controlled level.

It mainly acts as an antagonist of serotonin 5-HT2 receptors at the postsynaptic level, inhibiting its reuptake.This causes an increase in the level of serotonin in the brain. Likewise, it also helps to inhibit the reuptake of norepinephrine and dopamine, albeit at much lower levels. Finally, also slightly affects histamine and acetylcholine , but the latter are practically priceless.

Uses and Applications of this Medication

Nefazodone is mainly known as an antidepressant, the main indication of which is major depression. It is also used for premenstrual syndrome or other types of depression, such as those associated with various pathologies.However, in addition to the activities of depressive disorders , this drug may be useful in the treatment of other psychopathologies and problems.

Among them, we can observe that nefazodone is useful in the treatment of various anxiety problems and in PTSD, as well as in problems with insomnia, although it increases the latency of REM sleep.

Side effects of this antidepressant

Despite its great utility, the consumption of nefazodone can cause various side effects, and in some cases it can have risks with different contraindications.

The most common side effects of nefazodone are dry mouth and drowsiness, as well as nausea and dizziness. Confusion, vision problems, and asthenia are also relatively common. Less often, hypotension and bradycardia are observed, which is dangerous, especially for those who already suffer from cardiac pathologies.

However, the most serious problem associated with this drug (and which actually led to its withdrawal) is its high hepatotoxicity. In some cases, liver failure is observed, which can even lead to death or jaundice.Therefore, to prescribe (something not very common), should constantly monitor the health of the patient’s liver , periodically performing tests. It can also have an effect on the kidneys, as the drug is eliminated primarily by this route.

Another aspect to consider is the risk of developing serotonin syndrome, a problem arising from excess serotonin (often caused by overdose or interactions with other medications and medications), which can cause anxiety, altered consciousness, hyperactivity, tremors , vomiting , tachycardia, impaired motor coordination, mydriasis, seizures, trouble breathing, or even death.

Contraindications.

As for contraindications, one of the main ones occurs in those people who already suffer from liver problems, as well as coronary diseases. Also, is contraindicated in people using certain drugs and especially MAOIs, as they can cause serotonin syndrome and even lead to death.

Taking it with SSRIs is not recommended. how they interact. Likewise, some retroviral drugs, such as those used to treat HIV, interact with this substance, making it imperative that when nefazodone is used (for treating depression associated with this disease), doses and potential interactions are largely regulated.

Minors and pregnant women should not use this medicine. In addition, people with a history of epilepsy or a history of suicide attempts should not take this drug or use it with extreme caution. Not generally recommended for bipolar disorder.

Bibliographic references:

• Jufe, G. (2001). Practical psychopharmacology. Buenos Aires, edited by Polemos.
• McConville, B.J .; Cheney, R.O .; Brown, K. and others. (1998). Newer antidepressants – in addition to selective antidepressants that inhibit serotonin reuptake.Ped Wedge North Am. 45: 1157-71.
• Tatsumi, M .; Groshan, K .; Blakely, R. & Richelson, E. (1997). “Pharmacological profile of antidepressants and related compounds on human monoamine transporters.” Eur J Pharmacol. 340 (2-3): 249-258.

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Quetiapine (Ketilept, Quentiax, Quetiapel, Ketiap) – Empathy

Pharmacological action

Quetiapine is an atypical antipsychotic drug that exhibits a higher affinity for serotonin (hydroxytryptamine) receptors (5HT2) than for dopamine D1 and D2 receptors in the brain.Quetiapine also has a more pronounced affinity for histamine and alpha1-adrenergic receptors and less in relation to alpha2-adrenergic receptors. No noticeable affinity of quetiapine for muscarinic and benzodiazepine receptors was found. In standard tests, quetiapine exhibits antipsychotic activity.

Pharmacokinetics

When administered orally, quetiapine is well absorbed from the gastrointestinal tract and is actively metabolized in the liver.The main metabolites in plasma do not have pronounced pharmacological activity.

Food intake does not significantly affect the bioavailability of quetiapine. T1 / 2 is about 7 hours. Approximately 83% of quetiapine binds to plasma proteins.

The pharmacokinetics of quetiapine is linear, there are no differences in pharmacokinetic parameters in men and women.

The average clearance of quetiapine in elderly patients is 30-50% less than in patients aged 18 to 65 years.

The mean plasma clearance of quetiapine is approximately 25% less in patients with severe renal impairment (creatinine clearance less than 30 ml / min / 1.73 m2) and in patients with liver damage, but the interindividual clearance values ​​are within the range corresponding to healthy volunteers. Approximately 73% of quetiapine is excreted in the urine and 21% in the faeces. Less than 5% of quetiapine is not metabolized and is excreted unchanged by the kidneys or faeces.It has been established that CYP3A4 is a key isoenzyme of quetiapine metabolism mediated by cytochrome P450.

In a study of the pharmacokinetics of quetiapine at different doses, the use of quetiapine before taking ketoconazole or simultaneously with ketoconazole led to an increase, on average, Cmax and the area under the concentration-time curve (AUC) of quetiapine by 235% and 522%, respectively, as well as a decrease the clearance of quetiapine, on average, by 84%. T1 / 2 of quetiapine increased, but Tmax did not change.

Quetiapine and some of its metabolites have a weak inhibitory activity against cytochrome P450 isoenzymes 1A2, 2C9, 2C19, 2D6 and 3A4, but only at a concentration 10-50 times higher than the concentration observed at a commonly used effective dose of 300-450 mg / day.

Based on in vitro results, one should not expect that the simultaneous use of quetiapine with other drugs will lead to a clinically pronounced inhibition of cytochrome P450-mediated metabolism of other drugs.

Readings

– acute and chronic psychoses, including schizophrenia;

– manic episodes in the structure of bipolar disorder.

Contraindications

– hypersensitivity to any component of the drug;

– concomitant use with CYP3A4 inhibitors, such as HIV protease inhibitors, azole antifungal drugs, erythromycin, clarithromycin, nefazodone;

– children up to age 18;

– lactation period.

Use with caution in patients with cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension; in old age; with liver failure; history of seizures; pregnancy.

Dosage

Adults:

Acute and chronic psychoses, including schizophrenia

The daily dose for the first 4 days of therapy is: 1st day – 50 mg, 2nd day – 100 mg, 3rd day – 200 mg, 4th day – 300 mg.Starting from the 4th day, the dose should be adjusted to the clinically effective dose, which usually ranges from 300 to 450 mg / day. Depending on the clinical effect and individual tolerance, the dose can vary from 150 to 750 mg / day.

Treatment of manic episodes in the structure of bipolar disorder

Quetiapine is used as monotherapy or as adjuvant therapy to stabilize mood.

The daily dose for the first 4 days of therapy is: 1st day – 100 mg, 2nd day – 200 mg, 3rd day – 300 mg, 4th day – 400 mg. In the future, by the 6th day of therapy, the daily dose of the drug can be increased to 800 mg. The increase in the daily dose should not exceed 200 mg per day.

Depending on the clinical effect and individual tolerance, the dose can vary from 200 to 800 mg / day. The usual effective dose is 400 to 800 mg / day.

For the treatment of schizophrenia , the maximum recommended daily dose of quetiapine is 750 mg; for the treatment of manic episodes in the structure of bipolar disorder, the maximum recommended daily dose of quetiapine is 800 mg / day.

In elderly patients , the initial dose of quetiapine is 25 mg / day. The dose should be increased daily by 25-50 mg until an effective dose is reached, which is likely to be less than in younger patients.

In patients with renal or hepatic impairment , it is recommended to start quetiapine therapy at 25 mg / day. It is recommended to increase the dose daily by 25-50 mg until the effective dose is reached.

Side effects

The most common adverse reactions associated with taking the drug: drowsiness (17.5%), dizziness (10%), constipation (9%), dyspepsia (6%), orthostatic hypotension and tachycardia (7%), dry mouth (7%) ), an increase in the activity of “liver” enzymes in the blood serum (6%), an increase in the concentration of cholesterol and triglycerides in the blood plasma.

Reception of quetiapine may be accompanied by the development of moderate asthenia, rhinitis and dyspepsia, an increase in body weight (mainly in the first weeks of treatment). Quetiapine can cause orthostatic hypotension (accompanied by dizziness), tachycardia and, in some patients, fainting; these adverse reactions mainly occur in the initial period of dose selection (see section “Special instructions”). Quetiapine therapy is associated with a small dose-dependent decrease in the concentration of thyroid hormones, in particular, total T4 and free T4.The maximum decrease in total and free T4 was recorded at the 2nd and 4th week of quetiapine therapy, without further decrease in the concentration of hormones during long-term treatment. Subsequently, there were no signs of clinically significant changes in the concentration of thyroid-stimulating hormone.

With long-term use of quetiapine, there is a potential for the development of tardive dyskinesia. If symptoms of tardive dyskinesia occur, it is necessary to reduce the dose or stop further treatment with quetiapine.With the abrupt withdrawal of high doses of antipsychotic drugs, the following acute reactions (“withdrawal” syndrome) may occur: nausea, vomiting, rarely insomnia.

Cases of exacerbation of psychotic symptoms and the appearance of involuntary movement disorders (akathisia, dystonia, dyskinesia) are possible. In this connection, the withdrawal of the drug is recommended to be carried out gradually.

The following are the side reactions observed with the use of quetiapine and distributed over organs and systems:

From the nervous system : drowsiness, dizziness, headache, anxiety, asthenia, hostility, agitation, insomnia, akathisia, tremor, convulsions, depression, paresthesia, neuroleptic malignant syndrome (hyperthermia, muscle rigidity, changes in mental autonomic status, lability system, increased activity of creatine phosphokinase), “restless legs” syndrome.

From the cardiovascular system: orthostatic hypotension, tachycardia, prolongation of the Q-T interval.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, diarrhea or constipation, increased activity of “liver” transaminases, jaundice, hepatitis.

Respiratory system: pharyngitis, rhinitis.

Allergic reactions: to the skin rash, eosinophilia, angioedema, Stevens-Johnson syndrome, anaphylactic reactions.

Laboratory indicators: leukopenia, neutropenia, hypercholesterolemia, hypertriglyceridemia, decreased T4 concentration (first 4 weeks), hyperglycemia.

Other: back pain, chest pain, subfebrile condition, weight gain (mainly in the first weeks of treatment), myalgia, dry skin, visual impairment, incl. blurred vision, decompensation of existing diabetes mellitus, priapism, galactorrhea.

Overdose

Data on overdose of quetiapine are limited. Cases of taking quetiapine in a dose exceeding 20 g without fatal consequences and with full recovery have been described, however, there are reports of extremely rare cases of overdose of quetiapine, leading to death or coma.

Symptoms may be due to an increase in the known pharmacological effects of the drug, such as drowsiness and excessive sedation, tachycardia and a decrease in blood pressure.

Treatment: no specific antidotes for quetiapine. In cases of overdose, gastric lavage is possible (after intubation, if the patient is unconscious), intake of activated charcoal and laxatives to remove unabsorbed quetiapine, however, the effectiveness of these measures has not been studied. Symptomatic therapy and measures aimed at maintaining respiratory function, cardiovascular system, ensuring adequate oxygenation and ventilation are shown.Medical control and observation should be continued until the patient is fully recovered.

Drug interactions

With the simultaneous use of drugs that have a powerful inhibitory effect on the CYP3A4 isoenzyme (such as antifungal agents of the azole group and erythromycin, clarithromycin, nefazodone), the plasma concentration of quetiapine increases, therefore, their simultaneous administration with quetiapine is contraindicated.With the simultaneous use of quetiapine with drugs that induce the liver enzyme system, such as carbamazepine, it is possible to reduce the concentration of the drug in the plasma, which may require an increase in the dose of quetiapine, depending on the clinical effect. In a study of the pharmacokinetics of quetiapine in various doses, when used before or simultaneously with carbamazepine (an inducer of hepatic enzymes), it led to a significant increase in the clearance of quetiapine. This increase in the clearance of quetiapine reduced the AUC by an average of 13% compared with the use of quetiapine without carbamazepine.The simultaneous use of quetiapine with another inducer of liver microsomal enzymes – phenytoin, also led to an increase in the clearance of quetiapine. With the simultaneous use of quetiapine and phenytoin (or other inducers of liver enzymes, such as barbiturates, rifampicin), an increase in the dose of quetiapine may be required. It may also be necessary to reduce the dose of quetiapine if phenytoin or carbamazepine or another inducer of the liver enzyme system is discontinued or if a drug does not induce liver microsomal enzymes (for example, valproic acid).

The pharmacokinetics of lithium preparations does not change with the simultaneous use of quetiapine.

Quetiapine did not induce the hepatic enzyme systems involved in the metabolism of antipyrine. Pharmacokinetics of quetiapine does not change significantly when used simultaneously with antipsychotic drugs – risperidone or haloperidol. However, the simultaneous administration of quetiapine and thioridazine led to an increase in the clearance of quetiapine. CYP3A4 is a key enzyme involved in the cytochrome P450-mediated metabolism of quetiapine.The pharmacokinetics of quetiapine does not significantly change with the simultaneous use of cimetidine, which is a P450 inhibitor.

The pharmacokinetics of quetiapine did not significantly change with the simultaneous use of imipramine (CYP2D6 inhibitor) or fluoxetine (CYP3A4 and CYP2D6 inhibitor). CNS depressants and ethanol increase the risk of side effects from quetiapine.

Special instructions

Quetiapine can cause orthostatic hypotension, especially during the initial period of dose selection (in older patients it is observed more often than in young people).There was no relationship between the intake of quetiapine and an increase in the QTc interval. However, when using quetiapine simultaneously with drugs that prolong the QTc interval, care must be taken, especially in the elderly. During the period of treatment, with a decrease in the number of neutrophils less than 1000 / μl, quetiapine should be discontinued.

With the development of orthostatic hypotension during treatment with the drug, it is necessary to reduce the dose or more slowly titrate the doses.The drug is not indicated for the treatment of psychosis associated with dementia. In case of development of symptoms of tardive dyskinesia, the dose of the drug should be reduced or the drug should be gradually withdrawn. The symptoms of tardive dyskinesia may worsen or even appear after the drug is discontinued.

In the event of the development of neuroleptic malignant syndrome, the drug must be canceled.

Considering that quetiapine mainly affects the central nervous system, the drug should be used with caution in combination with other drugs that depress the central nervous system, or alcohol.In children, adolescents and young people (under 24 years of age) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing Quetiapine or any other antidepressants in children, adolescents and young people (under 24 years of age), the risk of suicide and the benefits of their use should be correlated. In short-term studies, the risk of suicide did not increase in people over 24 years old, and in people over 65 years old it was slightly reduced.Any depressive disorder in itself increases the risk of suicide. Therefore, during treatment with antidepressants, all patients should be monitored for early detection of behavioral disturbances or changes, as well as suicidal tendencies.

Influence on the ability to drive vehicles and use mechanisms

Quetiapine can cause drowsiness, therefore, during the period of treatment, patients are advised to refrain from driving vehicles and engaging in activities that require increased concentration of attention and speed of psychomotor reactions.

Pregnancy and lactation

Use with caution during pregnancy. Contraindicated during lactation.

Pediatric use

Contraindicated in children and adolescents under 18 years of age.

For impaired renal function

In patients with renal impairment , it is recommended to start quetiapine therapy at 25 mg / day.It is recommended to increase the dose daily by 25-50 mg until the effective dose is reached.

For impaired liver function

In patients with hepatic impairment , it is recommended to start quetiapine therapy at 25 mg / day. It is recommended to increase the dose daily by 25-50 mg until the effective dose is reached.

Elderly use

In elderly patients , the initial dose of quetiapine is 25 mg / day.The dose should be increased daily by 25-50 mg until an effective dose is reached, which is likely to be less than in younger patients.

Terms and conditions of storage

Keep out of the reach of children, dry, protected from light at a temperature not exceeding 25 ° C.

Shelf life is 2 years.

Form of issue, composition and packaging

10 pieces. – contour cell packaging (3) – cardboard packs.

10 pieces.- contour cell packaging (3) – cardboard packs.

10 pieces. – contour cell packaging (3) – cardboard packs.

10 pieces. – contour cell packaging (3) – cardboard packs.
10 pieces. – contour cell packaging (6) – cardboard packs.

Antidepressant “Serzon” (Nefazodone) – Trazodone

Antidepressant: Serzone
Active ingredient: Nefazodone

Pharmacological action of antidepressant

Nefazodone is an antidepressant, chemically similar to trazodone.It affects the reuptake of norepinephrine and serotonin, increasing their free concentration in the brain.
The drug is well suited for depression accompanied by increased anxiety, as well as sleep disturbances. A noticeable improvement in patients with these symptoms usually occurs within the first week of nefazodone administration.
The drug has a high degree of safety, usually does not affect weight changes and does not provoke sexual dysfunction. Thus, it is perfectly suited for long-term therapy.

Indications for use

Treatment of depression of varying severity, also complicated by sleep disorders and increased anxiety.

Contraindications

Should not be used concomitantly with MAO inhibitors until two weeks have passed. Also, the manufacturer of the antidepressant is advised not to take the drug during pregnancy and lactation.

Method of application and dosage

Nefazodone should be taken orally, preferably twice a day, both with food and separately.Typically, treatment is started with a minimum dose of 50 mg / day. Take at night. Further, in the absence of daytime sleepiness and positive tolerance, the dose should be gradually increased to the recommended dose.
The recommended dose ranges from 150 to 300 mg twice daily. The maximum dosage is therefore 600 mg / day. Very often, the dosage is slowly adjusted upward in order to find the optimal amount of the drug. Moreover, if side effects appear, you should wait for them to end before moving to a new dosage level.For elderly and debilitated patients, a reduction in the initial dose and a slower dose change may be required, but the therapeutic dosage range is well within the range for younger patients.

Side effects

Nefazodone may cause the following side effects: nausea, dry mouth, weakness, drowsiness or insomnia, constipation, excessive sweating. Moreover, most of these effects are observed at a dosage exceeding 300 mg / day.

Storage conditions

Store away from excessive heat and moisture, out of the reach of children and pets at room temperature (below 40 ° C).
Nefazodone is also available under the brand names (generics) :

Serzon price: function temporarily inactive
Serzon buy: function temporarily inactive

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