Antidepressants can cause excess sweating and overheating – how to cope

Feeling the heat? Your medication might be to blame (Picture: Getty/Metro.co.uk)

Yes, it is extremely hot right now.

But if you’ve noticed that you’re sweating more than you ever have before, there might be another reason: your antidepressants.

Many antidepressants increase your likelihood of excessive sweating, known as hyperhidrosis.

It’s not clear why mental health medication can trigger a major case of sweaty upper lip syndrome, but the good news is that if you are experiencing this, you’re certainly not alone – and there are ways to reduce the struggles.

Let’s get into it.

Why do antidepressants make you sweat more?

‘The majority of antidepressants increase the risk of hyperhidrosis,’ explains Dr Kandi Ejiofor. ‘Some American studies cite that excess sweating can affect up to 15% of people take antidepressants.

‘Specifically, Tricyclic Acid and SSRI (selective serotonin reuptake inhibitors) antidepressants are responsible for this.

‘The way in which antidepressants cause excessive sweating is still relatively unknown – it is thought to be linked to the effects of serotonin, the happy hormone, in trying to maintain the internal core temperature of the body.

‘Your body sweats to try and cool down the body but overstimulation of this process can lead to overheating and excess sweating.’

What risks do antidepressants pose in hot weather?

In the current heatwave, some people who are taking antidepressants will notice not only more sweating than usual, but also simply feeling the heat more.

This can then lead to dehydration, heat stroke, heat rash, and other heat related issues, so it’s essential that you’re really on top of all the regular hot-weather-related care, such as drinking plenty of water, taking time out of the sun, and avoiding overexertion.

Dr Stephanie Ooi, GP at MyHealthcare Clinic, notes that the hot weather could also disguise the symptoms of serotonin syndrome, a rare, but potentially serious set of side effects that are linked to SSRIs

‘Serotonin syndrome occurs when the levels of serotonin in your brain are too high,’ says Dr Stephanie. ‘This can occur if you take an SSRI in combination with something else that also raises serotonin levels, such as another antidepressant or St John’s Wort.’

Symptoms of serotonin syndrome can include:

• confusion
• agitation
• muscle twitching
• sweating
• shivering
• diarrhoea

That is unlikely, by the way. The main risks you’ll face in the UK heatwave when taking antidepressants are the minor, but annoying ones: feeling super sweaty, hot, and uncomfortable.

This poses a greater risk though: that you might get so fed up of being covered in sweat that you stop taking your medication in an attempt to lower your temperature.

This is not a good idea.

‘Sweating secondary to antidepressant medication is usually not a cause for concern on its own but the symptoms can be so bothersome that it causes people to stop taking their medication, which of course could be problematic,’ says Dr Kandi.

Your GP might be able to help tackle the sweaty effects of your meds (Picture: Getty Images/iStockphoto)

What should you do if your antidepressants are causing excess sweating?

First things first: keep taking your meds. Don’t do a sudden stop out of desperation to cool down.

Instead, it’s worth talking to your GP if hyperhidrosis is negatively affecting your life.

‘They may consider prescribing you another medication to counteract the effects of the medication you are on,’ suggests Dr Kandi.

Along with this, there are many things you can do on your own to reduce any hot weather induced discomfort.

Measure your temperature

Dr Kandi recommends investing in a thermometer, so you can regularly measure your temperature and thus know when there’s a problem.

‘If your core temperature is consistently raised above the baseline, it is worthwhile discussing with your doctor to review you and manage your symptoms appropriately,’ she notes.

Drink plenty of fluids

Make sure you’re sipping water throughout the day, carrying a bottle with you wherever you go.

This is key to avoid dehydration, especially if you’re losing a lot of fluid from excess sweating.

Take it easy

Now might not be a great time to rush around doing loads of things at once, or to do super intense workouts. Give yourself plenty of rest and prioritise keeping cool.

Wear the right clothes

‘Wear loose clothing in breathable materials such as cotton or linen,’ Dr Stephanie suggests. ‘Avoid tight clothing or synthetic materials.’

More: Health

Avoid other triggers for increased sweating

Drinking alcohol and eating spicy food can make your sweating worse.

Get a good antiperspirant

Speak to your pharmacist about one that will work best for excess sweating.

You can also buy armpit or sweat shields if you’re worried about protecting your clothing.

Prioritise lowering stress and anxiety

You know the drill: you sweat, then you get self-conscious and panic about sweating, then you sweat more, and so the awful cycle continues.

Remind yourself that sweating is perfectly natural, and people will understand – it’s boiling right now, so we doubt anyone is judging you for perspiring.

In moments when your excess stress is bothering you, try to ground yourself and do breathing exercises to slow your heartrate and bring you back to a place of calm.

Do you have a story to share?

Get in touch by emailing [email protected].

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Does Zoloft Cause Night Sweats? (5 Things You Need To Know)

In this blog, we will learn about zoloft induced night sweats. We will also discuss the reason behind it and how to overcome this condition. If you’ve noticed you are sweating more than usual, you need to take a look at your medication list.

Does zoloft cause night sweats?

Yes, zoloft is associated with many side effects, one of which is excessive sweating at night, called ‘night sweats’. In fact, zoloft induced night sweats are one of the most disturbing side effects. 

The thought of sweating profusely, in the might of the night, even during winters, is quite disturbing. Zoloft not only causes excessive sweating at night, but at any part of the day. 

Not only zoloft, a lot of other antidepressants do the same. Zoloft belongs to the class of SSRIs. SSRIs increase serotonin levels in the brain. Serotonin can affect hypothalamus, which is responsible for regulating your homeostasis. 

It can have an impact on your body temperature and your ability to sweat. Abnormal sweating, is in fact, a very common side effect of SSRI antidepressants, occurring in around 10–20% of patients. It usually sticks around, or even worsens. 

Antidepressant-induced sweating is different for everyone. For some people, it is so severe that they need to find a different drug, or quit antidepressants altogether.  

Is zoloft induced excessive sweating that bad?

Excessive sweating is quite problematic. In short, it is disabling. It affects the quality of life as it ends up disturbing people more than they could imagine. It becomes socially embarrassing for them, and in some cases, they are embarrassed in front of their spouses as well. 

Imagine snowing outside, literally it’s that cold. You wake up in the middle of the night just to find out that you’re sweating profusely. It not only ruins your sleep quality, but also your hygiene as well.

Zoloft induced sweating is more prominent in the upper body, face, scalp, neck and chest. Do not wait for it to subside on its own. This does not go away that easy. 

What could be done? 

If the night sweats are disrupting your life that terribly, one of the few things might help:

Dose reduction

Dose reduction can be considered, if possible. If there’s a chance of your condition worsening with a lower dose, then this option is not so helpful. But if there is a chance to minimise side effects by reducing the dose, without affecting the therapeutic response, this might help. 

Consider changing antidepressant

If feasible, you can switch to a different SSRI or any other class of antidepressant (except bupropion, which has a higher rate of night sweats as compared to any other antidepressant). 

For example, if zoloft (Sertraline) is inducing night sweats in you, ask your healthcare provider to prescribe another antidepressant of the same family (SSRIs), which might help you with depression without inducing excessive sweating. 

Give your body time

Your body might need some time to adapt to the presence of zoloft. These meds affect your brain and alter the amounts of excitatory neurotransmitters, to get rid of your anxiety and depression. It can not happen overnight. 

Side effects associated with zoloft start to fade away within a few weeks. Make sure you give your body enough time to adjust. Do not stop your med abruptly.

What if it gets worse?

If your night sweats get worse and even after weeks of treatment, this side effect persists, your healthcare provider may prescribe some medical treatment to overcome your night sweats. Medications used to reduce excessive sweating include:

TERAZOSIN 

Terazosin is an alpha-1 adrenergic antagonist, generally used in the treatment of symptomatic benign prostatic hyperplasia and management of hypertension. 

In a study conducted in 2013, it was observed that in the beginning of the study, 48.5% patients suffered from high grade sweating. After 14 days of treatment with terazosin, the percentage reduced down by half.

This concludes that terazosin is effective in decreasing sweating severity in patients using zoloft (Sertraline).

Side effects of terazosin 

As it’s nothing new to know that every medicine has its own side effects. Let’s take a look at side effects associated with the use of terazosin.  

• Chest tightness and pain
• Dizziness/lightheadedness/vertigo
• Shortness of breath.
• Unconsciousness 
• Arrhythmia or irregular heartbeat.
• Swelling of lower extremities
• Impotence (inability to have an erection)
• Blurred vision
• Nausea
• Stuffy or runny nose

One thing that I always try to tell my readers is, every human body is different, and no I don’t mean physically or the way we look, I mean internally! Just like every human being reacts differently to different situations.

Similarly every human body reacts differently when they are exposed to medications. Every single individual out there has a different physiological composition. A certain medicine might be beneficial for one but ends up producing serious side effects in another. 

GLYCOPYRROLATE AND OXYBUTYNIN

Glycopyrrolate and Oxybutynin are also known as ‘The sweat pills’. Glycopyrrolate (sold under the brand name Robinul) is one of the anticholinergics used most often in the treatment of excessive sweating.  

The effectiveness of glycopyrrolate is often related to the dose a patient is able to handle, and obviously how the patient responds to the drug. Studies suggest that glycopyrrolate reduces sweating efficiently but it is not tolerated by some people because of its side effects.

Side effects of Glycopyrrolate 

Side effects include:

• Dry mouth (the most common side effect) 
• Dry eyes or decreased lacrimation
• Constipation
• Nausea 

Drinking more water, mints, eye-drops and increased fibre consumption might help fight these side effects.

Fear of serotonin syndrome 

Yes, it is very important to rule out serotonin syndrome as sometimes, you think that excessive sweating is a side effect you’re getting from the use of zoloft, but what if it’s something else? 

Serotonin syndrome (SD), also known as serotonin toxicity, is a potentially life threatening condition involving excessive serotonergic activation. It has many symptoms to talk about.  

The basic cause of this condition is the serotonin overload and the antidepressants are considered the main culprit for this condition. The syndrome is pretty rare, so it is unlikely to occur when a patient is sticking to the dose recommended by the healthcare provider.

Sometimes, they combine the use of these types of medications, for the sake of achieving better results, so if you are already on a stable dose but you combine zoloft with other medications. 

Other non psychological medications, which somehow increase the amount of serotonin in the body, it also results in serotonin syndrome. 

For example, if selene, which is a Parkinson’s disease medication, is also added on a patient when a patient is already on zoloft, it increases the risk for serotonin syndrome. 

Now, let’s briefly talk about the path of physiology behind this condition. It all begins with the amino acid tryptophan, which is used to produce serotonin. 

It actually undergoes a couple of enzymatic reactions and ends up producing serotonin, which can act on a variety of different receptors in the brain to modulate mood, appetite, sleep and attention but it also has other regulatory functions in the body.  

One of the main symptoms of serotonin syndrome is profuse sweating, which is why I had to mention this condition, as oftentimes it is not even a side effect of zoloft but an actual syndrome, and the patient has no clue of it. 

Signs and symptoms of serotonin syndrome 

• Excessive sweating 
• Restlessness and fatigue
• Headache, which often feels like your head is pounding
• Changes in blood pressure and/or temperature
• Nausea
• Vomiting
• Diarrhoea
• Bradycardia
• Tremors
• Muscle twitching and muscle pain
• Shivering and goosebumps

Conclusion

Zoloft, an antidepressant, is often seen to be associated with profuse sweating, especially at night. This is indeed a pretty depressing condition, as it decreases the quality of life. 

In this blog, we discussed the options you have if you’re going through this problem. You can either reduce the dose or change the kind of antidepressant you’re on right now. If that doesn’t solve your problem, then terazosin and glycopyrrolate are prescribed to take your excessive sweating down a notch. 

In the end, always look out for serotonin syndrome. Immediately notify your healthcare provider, if you feel excessively increased heartbeat, chills and fever along with sweating. 

FAQs : Zoloft night sweats 

How long do night sweats last with Zoloft?

It depends on the dose you’re prescribed. Antidepressants usually take 4 to 6 weeks to produce their effects, as well as side effects. Most probably, these side effects subside when your body adapts to the presence of the med. 

Some side effects don’t. Make sure you discuss the do’s and don’ts with your healthcare provider. 

Why do antidepressants cause night sweats?

SSRIs induce sweating by blocking muscarinic receptors. Abnormal sweating, is in fact, a very common side effect of SSRI antidepressants, occurring in around 10–20% of patients. 

It usually sticks around, or even worsens. Antidepressant-induced sweating can take various forms, one of which is night sweats.

For some patients, the antidepressant-induced sweating is so severe that they need to find a different drug, or quit antidepressants altogether.

How do I stop night sweats from antidepressants?

As we have discussed in this blog, dose reduction can be considered, if possible. If there’s a chance of your condition worsening with a lower dose, then this option is not so helpful. But if there is a chance of doing so, this might help. 

Consider changing your antidepressant, if feasible. You can switch to a different SSRI or any other class of antidepressant (except bupropion, which has a higher rate of night sweats as compared to any other antidepressant).

In severe cases, terazosin or glycopyrrolate are recommended. 

Can paroxetine cause night sweats?

Yes, it can. Paroxetine is a member of SSRIs family. Its side effect profile is somewhat similar to other members of this class of antidepressants. Make sure you don’t exceed the recommended dose. 

What are the most common side effects of Zoloft?

Most common side effects include nausea, dizziness, drowsiness, dry mouth, loss of appetite, increased sweating, diarrhoea, upset stomach, trouble sleeping, weight gain and decreased libido. 

Nausea and vomiting may be more likely to occur with initial use of zoloft. It improves over time when the body starts to accept it. Within a few weeks, gastrointestinal side effects subside. 

Always remember, the proper use of medicines is the key to their maximum beneficial effect. Avoid deviating from the dose suggested by your healthcare provider, and never stop it abruptly.

References 

• James W. Mold and Barbara J. Holtzclaw – Selective Serotonin Reuptake Inhibitors and Night Sweats in a Primary Care Population https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4883206/
• Pilot Study of Terazosin in Treatment of Antidepressant Induced Excessive Sweating https://clinicaltrials. gov/ct2/show/NCT00237510
• Ali Ghaleiha et al. Int J Psychiatry Clin Pract. 2013 – Effect of terazosin on sweating in patients with major depressive disorder receiving sertraline: a randomized controlled trial https://pubmed.ncbi.nlm.nih.gov/22731399/
• Rajnish Mago et al. Ann Clin Psychiatry. 2013 – Antidepressant-induced excessive sweating: clinical features and treatment with terazosin https://pubmed.ncbi.nlm.nih.gov/23638448/
• Hyun Ho Lee, MD, Do Won Kim, MD. Efficacy of Glycopyrrolate in Primary Hyperhidrosis Patients https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3259134/

Zoloft tab. 100mg №28 – PHARMACY Folk

The appearance of the product may differ from that shown in the photo

International (non-proprietary) name (INN): Sertraline / Sertraline

Chemical name – cis-4 -(3,4-dichlorophenyl )-1,2,3,4-tetrahydro-N-methyl-1-naphthaleneamine

Dosage form : coated tablets.

Composition. Active ingredient: sertraline hydrochloride at a dose corresponding to 50 mg or 100 mg sertraline. Excipients: calcium phosphate, microcrystalline cellulose, hydroxypropyl cellulose, sodium starch glycolate, magnesium stearate, hydroxypropyl methylcellulose, polyethylene glycol, polysorbates, titanium dioxide (E171).

Description : white oblong tablets. On the surface of the tablet, “Pfizer” is squeezed out on one side, on the other side for a dosage of 50 mg “ZLT-50” (with a risk), for a dosage of 100 mg – “ZLT-100”.

Pharmacotherapeutic group: antidepressant; ATX code N06AB06

Pharmacodynamic properties. Sertraline is an antidepressant, a powerful specific inhibitor of serotonin (5-HT) reuptake in neurons. It has very little effect on the reuptake of norepinephrine and dopamine. At therapeutic doses, sertraline blocks the uptake of serotonin in human platelets. It has no stimulant, sedative or anticholinergic effect. Due to selective inhibition of 5-HT uptake, sertraline does not enhance adrenergic activity. Sertraline has no affinity for muscarinic (cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA or benzodiazepine receptors. Sertraline does not cause drug dependence, does not cause an increase in body weight with long-term use.

Pharmacokinetic properties. Absorption – high (but at a slow rate). Bioavailability is increased by 25% during meals. Food increases the maximum concentration (Cmax) by 25% and shortens the time to reach the maximum concentration (Tcmax). In humans, when treated with sertraline at a dose of 50 to 200 mg once a day for 14 days, the plasma concentration of the drug reached a peak (Cmax) 4.5-8.4 hours after administration. Cmax and the area under the concentration-time curve (AUC) are proportional to the dose in the range of 50-200 mg of sertraline 1 time per day for 14 days, while a linear pharmacokinetic dependence is revealed. The pharmacokinetic profile in adolescents and the elderly does not differ significantly from that in patients aged 18 to 65 years. The mean half-life (T1 / 2) of sertraline in young and elderly men and women is 22-36 hours. According to the final T1 / 2, approximately two-fold accumulation of the drug is observed before equilibrium concentrations are reached after 1 week of treatment (dose once a day). Plasma protein binding is approximately 98%. The pharmacokinetics of sertraline in children with OCD (see below) has been shown to be similar to that in adults (although sertraline metabolism is somewhat more active in children). However, given the lower body weight in children (especially those aged 6-12 years), the drug is recommended to be used at a lower dose in order to avoid excessive plasma levels.
Sertraline undergoes active biotransformation during the first passage through the liver. The main metabolite found in plasma, N-desmethylsertraline, is significantly inferior (about 20 times) to sertraline in activity in vitro and is actually not active in models of depression in vivo. T1 / 2 N-desmethylsertraline varies within 62-104 hours. Sertraline and N-desmethylsertraline are actively biotransformed; the resulting metabolites are excreted in equal amounts with feces and urine. Unchanged sertraline is excreted in the urine in small amounts (<0.2%). In patients with cirrhosis of the liver, T1 / 2 of the drug and AUC increase compared to those in healthy people.

Indications for use. Depression of various etiologies (treatment and prevention), Obsessive-compulsive disorders (OCD) Panic disorders.
Post-traumatic stress disorder (PTSD). social phobia.

Contraindications
Known hypersensitivity to sertraline, children under 6 years of age, pregnancy and breastfeeding (see section Pregnancy and breastfeeding). The drug should not be administered to patients simultaneously receiving monoamine oxidase inhibitors (MAOIs) and pimozide. With caution: organic diseases of the brain (including mental retardation), epilepsy, liver and / or kidney failure, marked weight loss.
Pregnancy and breastfeeding: There are no controlled results of the use of sertraline in pregnant women, so it is worth prescribing the drug to them only if the expected benefit to the mother outweighs the potential risk to the fetus. Women of reproductive age who are to be prescribed sertraline should be advised to use effective contraception.
Sertraline is found in breast milk, and therefore, treatment with this drug during breastfeeding is not recommended. There is no reliable data on the safety of its use in this case. If treatment is still necessary, then it is better to stop breastfeeding. In the case of the use of sertraline during pregnancy and lactation, some newborns whose mothers took antidepressants from the group of selective serotonin reuptake inhibitors (SSRIs), including serotonin, may experience symptoms similar to the reaction to drug withdrawal.

Side effects
Digestive system: dyspeptic disorders (flatulence, nausea, vomiting, diarrhea, constipation), abdominal pain, pancreatitis, dry mouth.
Cardiovascular system: palpitations, tachycardia, arterial hypertension.
Musculoskeletal system: arthralgia, muscle cramps.
Central and peripheral nervous system: Extrapyramidal disorders (dyskinesias, akathisias, teeth grinding, gait disturbance), involuntary muscle contractions, paresthesias, syncope, drowsiness, headache, migraine, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, hallucinations, euphoria, nightmares, psychosis, decreased libido, suicide, coma.
Respiratory system: Bronchospasm, yawning.
Urinary system: Enuresis, incontinence or urinary retention.
Reproductive system and mammary gland: sexual dysfunction (delayed ejaculation, reduced potency), galactorrhea, gynecomastia, menstrual disorders, priapism.
Organs of vision : blurred vision, mydriasis.
Endocrine system: hyperprolactinemia, hypothyroidism, syndrome of inappropriate ADH secretion.
Hepatobiliary system: hepatitis, jaundice, liver failure.
Allergic reactions: urticaria, pruritus, anaphylactoid reaction.
Other: Weakness, flushing or flushing of the face, ringing in the ears, alopecia, angioedema, swelling of the face, periorbital edema, photosensitivity reaction, purpura, increased sweating, decreased appetite (rarely increased), up to anorexia, decrease or increase in body weight, bleeding (including nasal, gastrointestinal or hematuria), peripheral edema, occasionally Steven-Johnson syndrome and epidermal necrolysis.
Laboratory data: Rare, with prolonged use, an asymptomatic increase in serum transaminase activity occurs. Cancellation of the drug in this case leads to the normalization of enzyme activity. Perhaps the development of leukopenia and thrombocytopenia, as well as an increase in the level of cholesterol in the blood serum. With the termination of treatment with sertraline, rare cases of withdrawal syndrome have been described. Paresthesias, hypesthesias, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety, or symptoms of psychosis that cannot be distinguished from the symptoms of the underlying disease may appear.

Overdose
Sertraline overdose did not cause severe symptoms even when the drug was administered in high doses. However, with simultaneous administration with other drugs or alcohol, severe poisoning can occur, up to coma and death. Overdose can cause serotonin syndrome with nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia. Treatment: There are no specific antidotes. Intensive maintenance therapy and constant monitoring of vital body functions are required. Inducing vomiting is not recommended. The introduction of activated charcoal may be more effective than gastric lavage. The airway must be maintained. Sertraline has a large volume of distribution, and therefore increased diuresis, dialysis, hemoperfusion, or blood transfusion may be ineffective.

Interactions with other medicinal products
Pimozide – When sertraline and pimozide were co-administered, an increase in pimozide levels was noted when it was given once at a low dose (2 mg). The increase in pimozide levels was not associated with any ECG changes. Since the mechanism of this interaction is not known, and pimozide has a narrow therapeutic index, the simultaneous use of pimozide and sertraline is contraindicated.
Monoamine oxidase inhibitors (MAOIs). Severe complications have been noted with the simultaneous use of sertraline and MAOIs (including selectively acting (selegiline) MAOIs and with a reversible type of action (moclobemide, as well as linezolid). Serotonin syndrome may develop (hyperthermia, rigidity, myoclonus, autonomic nervous system lability (rapid fluctuations in parameters respiratory and cardiovascular system), changes in mental status, including increased irritability, marked agitation, confusion, which in some cases can turn into a delirious state or coma). Similar complications, sometimes fatal, occur when MAOIs are prescribed during treatment with antidepressants, inhibiting neuronal uptake of monoamines or immediately after their withdrawal.0039 Central nervous system depressants and ethanol.
The combined use of sertraline and substances that depress the central nervous system requires close attention, and the use of alcoholic beverages and drugs containing alcohol during treatment with sertraline is prohibited. There was no potentiation of the effect of ethanol, carbamazepine, haloperidol or phenytoin on cognitive and psychomotor function in healthy people; however, co-administration of sertraline and alcohol is not recommended.
Indirect anticoagulants (earfarin) – when co-administered with sertraline, there is a slight but statistically significant increase in prothrombin time – in these cases, it is recommended to control prothrombin time at the beginning of treatment with sertraline and after its withdrawal.

Precautions
Sertraline should not be co-administered with an MAOI or for 14 days after stopping MAOI treatment. Similarly, after the abolition of sertraline, MAOIs are not prescribed for 14 days.
Serotonin syndrome and neuroleptic malignant syndrome. When using selective serotonin reuptake inhibitors (SSRIs), cases of serotonin syndrome (SS) and neuroleptic malignant syndrome (NMS) have been described, the risk of which increases when SSRIs are combined with other serotonergic drugs (including triptans), as well as drugs that affect serotonin metabolism (including monoamine oxidase inhibitors), antipsychotics and other dopamine receptor antagonists. Manifestations of SS may include changes in mental status (in particular, agitation, hallucinations, coma), autonomic lability (tachycardia, fluctuations in blood pressure, hyperthermia), changes in neuromuscular transmission (hyperreflexia, impaired coordination of movements) and / or disorders of the gastrointestinal tract. intestinal tract (nausea, vomiting and diarrhea). Some manifestations of SS, including hyperthermia, muscle rigidity, autonomic lability with the possibility of rapid fluctuations in vital signs, and changes in mental status, may resemble the symptoms that develop in NMS. It is necessary to monitor patients for the development of clinical manifestations of SS and NMS.
Other serotonergic agents – Caution should be exercised when sertraline is co-administered with other drugs that enhance serotonergic neurotransmission, such as tryptophan, fenfluramine, or 5-HT agonists. Such co-administration, if possible, should be excluded, given the likelihood of pharmacodynamic interaction.
Switching from other selective serotonin reuptake inhibitors (SSRIs), antidepressants or anti-obsessional drugs. The experience of clinical studies, the purpose of which was to determine the optimal time required for the transfer of patients from other antidepressant and anti-obsessional drugs to sertraline, is limited. Care must be taken when switching, especially from long-acting drugs such as fluoxetine. The necessary interval between the abolition of one selective serotonin reuptake inhibitor and the start of another similar drug has not been established. It should be noted that there is no sufficient experience with sertraline in patients undergoing electroconvulsive therapy.
The possible success or risk of such combined treatment has not been studied. There is no experience with the use of sertraline in patients with convulsive syndrome, so its use in patients with unstable epilepsy should be avoided, and patients with controlled epilepsy should be carefully monitored during treatment. If convulsions occur, the drug should be discontinued. Patients suffering from depression are at risk for suicidal attempts. This danger persists until remission develops. Therefore, from the beginning of treatment until the achievement of the optimal clinical effect, patients should be under constant medical supervision.
Mania/hypomania activation. During clinical trials prior to the introduction of sertraline to the market, hypomania and mania were observed in approximately 0.4% of patients receiving sertraline. Cases of activation of mania/hypomania are also described in a small proportion of patients with manic-depressive psychosis treated with other antidepressant or anti-obsessional drugs.
Use in liver failure. Sertraline is actively biotransformed in the liver. According to a pharmacokinetic study, with repeated administration of sertraline in patients with stable cirrhosis of the lung, an increase in the half-life of the drug and an almost threefold increase in AUC (area under the concentration/time curve) and maximum concentration of the drug were observed compared with those in healthy people. There were no significant differences in plasma protein binding between the two groups. Sertraline should be used with caution in patients with liver disease. When prescribing the drug to a patient with impaired liver function, it is necessary to discuss the advisability of reducing the dose or increasing the interval between taking the drug.
Use in renal failure. Sertraline undergoes active biotransformation, therefore, unchanged in the urine, it is excreted in small quantities. In patients with mild to moderate renal insufficiency (creatinine clearance 30-60 ml / min) and patients with moderate or severe renal insufficiency (creatinine clearance 10-29 ml / min), pharmacokinetic parameters (AUC0-24 and Cmax) of sertraline with repeated its intake did not differ significantly from the control group. In all groups, the half-life of the drug was the same, as well as there were no differences in plasma protein binding. The results of this study suggest that, as expected given the negligible renal excretion of sertraline, no dosage adjustment is required based on the severity of renal impairment.
Abnormal bleeding/hemorrhage. Caution is advised when prescribing selective serotonin reuptake inhibitors in combination with drugs that have an established ability to alter platelet function, as well as in patients with a history of hemorrhagic diseases.
Hyponatremia. Transient hyponatremia may occur during treatment with sertraline. This often develops in elderly patients, as well as when taking diuretics or a number of other drugs. A similar side effect is associated with the syndrome of inappropriate secretion of antidiuretic hormone. With the development of symptomatic hyponatremia, sertraline should be discontinued and adequate therapy aimed at correcting the level of sodium in the blood should be prescribed. Signs and symptoms of hyponatremia include headache, difficulty concentrating, memory impairment, weakness, and unsteadiness, which can lead to falls. In more severe cases, hallucinations, fainting, convulsions, coma, respiratory arrest, and death may occur.
Influence on the ability to drive vehicles and control mechanisms. Appointment, sertraline, as a rule, is not accompanied by a violation of psychomotor functions. However, its use simultaneously with other drugs can lead to impaired attention and coordination of movements. Therefore, during treatment with sertraline, it is not recommended to drive vehicles, special equipment or engage in activities associated with an increased risk.

Shelf life :
5 years old. Do not use after the expiry date stated on the package.

Storage conditions
List B.
At a temperature not exceeding 30°C, out of the reach of children.

official instructions for use, analogues, price, availability in pharmacies 174

International (nonproprietary) name (INN) : Sertraline/Sertraline

Chemical name – cis-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthaleneamine

Dosage form : tablets, coated.

Composition

Active ingredient: sertraline hydrochloride at a dose corresponding to 50 mg or 100 mg sertraline.
Excipients: calcium phosphate, microcrystalline cellulose, hydroxypropyl cellulose, sodium starch glycolate, magnesium stearate, hydroxypropyl methylcellulose, polyethylene glycol, polysorbates, titanium dioxide (E171).

Description : white oblong tablets. On the surface of the tablet, “Pfizer” is squeezed out on one side, on the other side for a dosage of 50 mg “ZLT-50” (with a risk), for a dosage of 100 mg – “ZLT-100”.

Pharmacotherapeutic group:

antidepressant; ATX code N06AB06

Pharmacodynamic properties

Sertraline is an antidepressant, a powerful specific inhibitor of serotonin (5-HT) reuptake in neurons. It has very little effect on the reuptake of norepinephrine and dopamine. At therapeutic doses, sertraline blocks the uptake of serotonin in human platelets. It has no stimulant, sedative or anticholinergic effect. Due to selective inhibition of 5-HT uptake, sertraline does not enhance adrenergic activity. Sertraline has no affinity for muscarinic (cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA or benzodiazepine receptors. Sertraline does not cause drug dependence, does not cause an increase in body weight with long-term use.

Pharmacokinetic properties

Absorption – high (but at a slow rate). Bioavailability is increased by 25% during meals. Food increases the maximum concentration (Cmax) by 25% and shortens the time to reach the maximum concentration (Tcmax). In humans, when treated with sertraline at a dose of 50 to 200 mg once a day for 14 days, the plasma concentration of the drug reached a peak (Cmax) 4.5-8.4 hours after administration. Cmax and the area under the concentration-time curve (AUC) are proportional to the dose in the range of 50-200 mg of sertraline 1 time per day for 14 days, while a linear pharmacokinetic dependence is revealed. The pharmacokinetic profile in adolescents and the elderly does not differ significantly from that in patients aged 18 to 65 years. The mean half-life (T1 / 2) of sertraline in young and elderly men and women is 22-36 hours. According to the final T1 / 2, approximately two-fold accumulation of the drug is observed before equilibrium concentrations are reached after 1 week of treatment (dose once a day). Plasma protein binding is approximately 98%. The pharmacokinetics of sertraline in children with OCD (see below) has been shown to be similar to that in adults (although sertraline metabolism is somewhat more active in children). However, given the lower body weight in children (especially those aged 6-12 years), the drug is recommended to be used at a lower dose in order to avoid excessive plasma levels.
Sertraline undergoes active biotransformation during the first passage through the liver. The main metabolite found in plasma, N-desmethylsertraline, is significantly inferior (about 20 times) to sertraline in activity in vitro and is actually not active in models of depression in vivo. T1 / 2 N-desmethylsertraline varies within 62-104 hours. Sertraline and N-desmethylsertraline are actively biotransformed; the resulting metabolites are excreted in equal amounts with feces and urine. Unchanged sertraline is excreted in the urine in small amounts (<0.2%). In patients with cirrhosis of the liver, T1 / 2 of the drug and AUC increase compared to those in healthy people.

Indications for use

Depression of various etiologies (treatment and prevention), Obsessive-compulsive disorders (OCD) Panic disorders.
Post-traumatic stress disorder (PTSD). social phobia.

Contraindications

Known hypersensitivity to sertraline, children under 6 years of age, pregnancy and breastfeeding (see section Pregnancy and breastfeeding). The drug should not be administered to patients simultaneously receiving monoamine oxidase inhibitors (MAOIs) and pimozide. With caution: organic diseases of the brain (including mental retardation), epilepsy, liver and / or kidney failure, marked weight loss.
Pregnancy and breastfeeding: There are no controlled results of the use of sertraline in pregnant women, therefore, it is worth prescribing the drug to them only if the expected benefit to the mother outweighs the potential risk to the fetus. Women of reproductive age who are to be prescribed sertraline should be advised to use effective contraception.
Sertraline is found in breast milk, and therefore, treatment with this drug during breastfeeding is not recommended. There is no reliable data on the safety of its use in this case. If treatment is still necessary, then it is better to stop breastfeeding. In the case of the use of sertraline during pregnancy and lactation, some newborns whose mothers took antidepressants from the group of selective serotonin reuptake inhibitors (SSRIs), including serotonin, may experience symptoms similar to the reaction to drug withdrawal.

Side effect

Digestive system: dyspeptic disorders (flatulence, nausea, vomiting, diarrhea, constipation), abdominal pain, pancreatitis, dry mouth.
Cardiovascular system: palpitations, tachycardia, arterial hypertension.
Musculoskeletal system: arthralgia, muscle cramps.
Central and peripheral nervous system: extrapyramidal disorders (dyskinesias, akathisias, teeth grinding, gait disturbance), involuntary muscle contractions, paresthesias, syncope, drowsiness, headache, migraine, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, hallucinations, euphoria, nightmares, psychosis, decreased libido, suicide, coma.
Respiratory system: bronchospasm, yawning.
Urinary system: enuresis, incontinence or urinary retention.
Reproductive system and mammary gland: sexual dysfunction (delayed ejaculation, reduced potency), galactorrhea, gynecomastia, menstrual disorders, priapism.
Organs of vision : blurred vision, mydriasis.
Endocrine system: hyperprolactinemia, hypothyroidism, syndrome of inappropriate ADH secretion.
Hepatobiliary system: hepatitis, jaundice, liver failure.
Allergic reactions: urticaria, pruritus, anaphylactoid reaction.
Other: weakness, reddening of the skin or flushing of the face, ringing in the ears, alopecia, angioedema, swelling of the face, periorbital edema, photosensitivity reaction, purpura, increased sweating, decreased appetite (rarely increased), up to anorexia, decrease or increase in body weight, bleeding (including nasal, gastrointestinal or hematuria), peripheral edema, occasionally Steven-Johnson syndrome and epidermal necrolysis.
Laboratory data: rarely, with prolonged use, an asymptomatic increase in serum transaminase activity occurs. Cancellation of the drug in this case leads to the normalization of enzyme activity. Perhaps the development of leukopenia and thrombocytopenia, as well as an increase in the level of cholesterol in the blood serum. With the termination of treatment with sertraline, rare cases of withdrawal syndrome have been described. Paresthesias, hypesthesias, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety, or symptoms of psychosis that cannot be distinguished from the symptoms of the underlying disease may appear.

Overdose

Sertraline overdose did not cause severe symptoms even when the drug was administered in high doses. However, with simultaneous administration with other drugs or alcohol, severe poisoning can occur, up to coma and death. Overdose can cause serotonin syndrome with nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia. Treatment: There are no specific antidotes. Intensive maintenance therapy and constant monitoring of vital body functions are required. Inducing vomiting is not recommended. The introduction of activated charcoal may be more effective than gastric lavage. The airway must be maintained. Sertraline has a large volume of distribution, and therefore increased diuresis, dialysis, hemoperfusion, or blood transfusion may be ineffective.

Interaction with other drugs

Pimozide – Co-administration of sertraline and pimozide has been associated with increased levels of pimozide at a single low dose (2 mg). The increase in pimozide levels was not associated with any ECG changes. Since the mechanism of this interaction is not known, and pimozide has a narrow therapeutic index, the simultaneous use of pimozide and sertraline is contraindicated.
Monoamine oxidase inhibitors (MAOIs). There have been severe complications with the simultaneous use of sertraline and MAOIs (including selectively acting (selegiline) MAOIs and with a reversible type of action (moclobemide, as well as linezolid). Serotonin syndrome may develop (hyperthermia, rigidity, myoclonus, autonomic nervous system lability (rapid fluctuations in parameters respiratory and cardiovascular system), changes in mental status, including increased irritability, marked agitation, confusion, which in some cases can turn into a delirious state or coma). Similar complications, sometimes fatal, occur when MAOIs are prescribed during treatment with antidepressants, inhibiting neuronal uptake of monoamines or immediately after their withdrawal.0039 Central nervous system depressants and ethanol.

The combined use of sertraline and substances that depress the central nervous system requires close attention, and the use of alcoholic beverages and preparations containing alcohol during treatment with sertraline is also prohibited. There was no potentiation of the effect of ethanol, carbamazepine, haloperidol or phenytoin on cognitive and psychomotor function in healthy people; however, co-administration of sertraline and alcohol is not recommended.
Indirect anticoagulants (earfarin) – when co-administered with sertraline, there is a slight but statistically significant increase in prothrombin time – in these cases, it is recommended to control prothrombin time at the beginning of treatment with sertraline and after its withdrawal.

Special instructions

Sertraline should not be co-administered with an MAOI or for 14 days after stopping MAOI treatment. Similarly, after the abolition of sertraline, MAOIs are not prescribed for 14 days.
Serotonin syndrome and neuroleptic malignant syndrome

When using selective serotonin reuptake inhibitors (SSRIs), cases of serotonin syndrome (SS) and neuroleptic malignant syndrome (NMS) have been described, the risk of which increases when SSRIs are combined with other serotonergic drugs (including triptans), as well as drugs that affect serotonin metabolism (including monoamine oxidase inhibitors), antipsychotics and other dopamine receptor antagonists. Manifestations of SS may include changes in mental status (in particular, agitation, hallucinations, coma), autonomic lability (tachycardia, fluctuations in blood pressure, hyperthermia), changes in neuromuscular transmission (hyperreflexia, impaired coordination of movements) and / or disorders of the gastrointestinal tract. intestinal tract (nausea, vomiting and diarrhea). Some manifestations of SS, including hyperthermia, muscle rigidity, autonomic lability with the possibility of rapid fluctuations in vital signs, and changes in mental status, may resemble the symptoms that develop in NMS. It is necessary to monitor patients for the development of clinical manifestations of SS and NMS.
Other serotonergic agents – Caution should be exercised when sertraline is co-administered with other drugs that enhance serotonergic neurotransmission, such as tryptophan, fenfluramine, or 5-HT agonists. Such co-administration, if possible, should be excluded, given the likelihood of pharmacodynamic interaction.
Switching from other selective serotonin reuptake inhibitors (SSRIs), antidepressants or anti-obsessional drugs. The experience of clinical studies, the purpose of which was to determine the optimal time required for the transfer of patients from taking other antidepressant and anti-obsessional drugs to sertraline, is limited. Care must be taken when switching, especially from long-acting drugs such as fluoxetine. The necessary interval between the abolition of one selective serotonin reuptake inhibitor and the start of another similar drug has not been established. It should be noted that there is no sufficient experience with sertraline in patients undergoing electroconvulsive therapy.
The possible success or risk of such combined treatment has not been studied. There is no experience with the use of sertraline in patients with convulsive syndrome, so its use in patients with unstable epilepsy should be avoided, and patients with controlled epilepsy should be carefully monitored during treatment. If convulsions occur, the drug should be discontinued. Patients suffering from depression are at risk for suicidal attempts. This danger persists until remission develops. Therefore, from the beginning of treatment until the achievement of the optimal clinical effect, patients should be under constant medical supervision.
Mania/hypomania activation. During clinical trials prior to the introduction of sertraline to the market, hypomania and mania were observed in approximately 0.4% of patients receiving sertraline. Cases of activation of mania/hypomania are also described in a small proportion of patients with manic-depressive psychosis treated with other antidepressant or anti-obsessional drugs.
Use in liver failure. Sertraline is actively biotransformed in the liver. According to a pharmacokinetic study, with repeated administration of sertraline in patients with stable cirrhosis of the lung, an increase in the half-life of the drug and an almost threefold increase in AUC (area under the concentration/time curve) and maximum concentration of the drug were observed compared with those in healthy people. There were no significant differences in plasma protein binding between the two groups. Sertraline should be used with caution in patients with liver disease. When prescribing the drug to a patient with impaired liver function, it is necessary to discuss the advisability of reducing the dose or increasing the interval between taking the drug.
Use in renal failure

Sertraline undergoes active biotransformation, therefore, unchanged in the urine, it is excreted in small quantities. In patients with mild to moderate renal insufficiency (creatinine clearance 30-60 ml / min) and patients with moderate or severe renal insufficiency (creatinine clearance 10-29 ml / min), pharmacokinetic parameters (AUC0-24 and Cmax) of sertraline with repeated its intake did not differ significantly from the control group. In all groups, the half-life of the drug was the same, as well as there were no differences in plasma protein binding. The results of this study suggest that, as expected given the negligible renal excretion of sertraline, no dosage adjustment is required based on the severity of renal impairment.
Pathological bleeding/hemorrhage

Caution is advised when prescribing selective serotonin reuptake inhibitors in combination with drugs that have an established ability to alter platelet function, as well as in patients with a history of hemorrhagic diseases.
Hyponatremia

Transient hyponatremia may occur during treatment with sertraline. This often develops in elderly patients, as well as when taking diuretics or a number of other drugs. A similar side effect is associated with the syndrome of inappropriate secretion of antidiuretic hormone. With the development of symptomatic hyponatremia, sertraline should be discontinued and adequate therapy aimed at correcting the level of sodium in the blood should be prescribed. Signs and symptoms of hyponatremia include headache, difficulty concentrating, memory impairment, weakness, and unsteadiness, which can lead to falls. In more severe cases, hallucinations, fainting, convulsions, coma, respiratory arrest, and death may occur.