Paroxetine, pills 20mg, 30pcs

Composition

Active ingredient:

paroxetine hydrochloride hemihydrate;

Auxiliary substances:

calcium hydrophosphate,

microcrystalline cellulose,

crospovidone,

copovidone,

colloidal silicon dioxide,

magnesium stearate,

talc;

Shell:

hypromellose, macrogol 6000, talc, titanium dioxide

Pharmacological action

Paroxetine is an antidepressant. It is a selective inhibitor of serotonin (5-hydroxytryptamine,5-HT) reuptake by brain neurons, which determines its antidepressant effect and effectiveness in the treatment of obsessive-compulsive (OCD) and panic disorder.

Paroxetine has a low affinity for m-cholinergic receptors (it has a weak anticholinergic effect), α1 -, α2-and β-adrenergic receptors, as well as for dopamine (D2),5HT1-like,5HT2-like and histamine H1-receptors. Paroxetine does not interfere with psychomotor functions and does not potentiate the depressing effect of ethanol on them.

According to a behavioral and EEG study, paroxetine has weak activating properties when given at doses higher than those required to inhibit serotonin uptake. It does not cause significant changes in blood pressure, heart rate and EEG.

Pharmacokinetics

Suction

After oral use, paroxetine is well absorbed from the gastrointestinal tract and undergoes first-pass metabolism through the liver.

Css distribution is achieved 7-14 days after the start of therapy. When increasing the dose and/or duration of treatment, a non-linear dependence of pharmacokinetic parameters on the dose is observed.

Paroxetine is extensively distributed in tissues, only 1% of it is present in plasma.

Binds to proteins by 95%.

Metabolism

It is metabolized in the liver to form inactive metabolites. It is an inhibitor of the CYP2D6 isoenzyme.

The main metabolites of paroxetine are polar and conjugated products of oxidation and methylation, which are rapidly eliminated from the body, have weak pharmacological activity and do not affect its therapeutic effect. During the metabolism of paroxetine, the selective uptake of serotonin by neurons due to its action is not disturbed.

Deduction

About 64% of paroxetine is excreted in the urine (2% – unchanged,64% – in the form of metabolites); approximately 36% is excreted in the bile through the intestine, mainly in the form of metabolites, less than 1% – unchanged.

The elimination of paroxetine metabolites is biphasic, first as a result of first-pass metabolism through the liver, and then it is controlled by systemic elimination. T1 / 2 of paroxetine varies, but on average is 24 hours

. Pharmacokinetics in special clinical cases

The concentration of paroxetine in the blood plasma increases with impaired liver and kidney function, as well as in the elderly.

Indications

Depression of various etiologies, obsessive-compulsive disorder, panic disorder, social phobias, generalized anxiety disorder, post-traumatic stress disorder.

Use during pregnancy and lactation

During pregnancy, the appointment is allowed only if absolutely necessary.

Category of action on the fetus according to the FDA-C.

Breast-feeding should be discontinued for the duration of treatment (paroxetine passes into breast milk at concentrations close to those in the blood serum).

Contraindications

Hypersensitivity, concomitant use of MAO inhibitors (and 2 weeks after their withdrawal), age up to 18 years (efficacy and safety have not been established).

Side effects

Nervous system and sensory disorders:  dizziness, headache, migraine, drowsiness, insomnia, increased excitability, nervousness, anxiety, irritability, emotional lability, asthenia, neurosis, impaired concentration, impaired thinking, aggressiveness, hostility, tremor, convulsions, extrapyramidal disorders, hallucinations, euphoria, mania or hypomania, confusion, agitation, depersonalization, amnesia, panic attacks, paresthesia, serotonin syndrome, visual impairment, taste changes.

From the musculoskeletal system:  arthralgia, myalgia, myopathy, myasthenia gravis.

From the genitourinary system:  sexual dysfunction, including ejaculation disorders, decreased libido, anorgasmia, urinary retention, or increased urination.

From the digestive tract:  decreased / increased appetite, nausea, vomiting, dry mouth, constipation/diarrhea; in very rare cases — hepatitis.

From the cardiovascular system:  promotion or demotion Blood pressure, orthostatic hypotension, palpitation.

Allergic reactions:  rash, urticaria, ecchymosis, pruritus, angioedema.

Other services:  myalgia, rhinorrhea, increased sweating, hyponatremia, impaired AH secretion, hyperprolactinemia/galactorrhea, weight loss/increase, withdrawal syndrome (with abrupt withdrawal of paroxetine).

Interaction

Concomitant use of antacids does not affect the absorption and pharmacokinetic parameters of Paroxetine.

Concomitant use of Paroxetine with MAO inhibitors is contraindicated.

Concomitant use with Paroxetine increases the concentration of procyclidine.

Due to the inhibition of cytochrome P 450 by paroxetine, it is possible to increase the effect of barbiturates, phenytoin, indirect anticoagulants, tricyclic antidepressants, phenothiazine neuroleptics and class 1 C antiarrhythmics, metoprolol and increase the risk of side effects with simultaneous use of these drugs.

When administered concomitantly with drugs that inhibit liver enzymes, it may be necessary to reduce the dose of Paroxetine.

Paroxetine increases the bleeding time with simultaneous use of warfarin (with unchanged prothrombin time).

When Paroxetine is co-administered with atypical antipsychotics, tricyclic antidepressants, phenothiazine-type drugs, NSAIDs (including acetylsalicylic acid), blood clotting may be disrupted.

Concomitant use of Paroxetine with serotonergic drugs (tramadol, sumatriptan) may increase the serotonergic effect.

The mutual strengthening of the action of tryptophan, lithium preparations and paroxetine was noted.

When Paroxetine is co-administered with phenytoin and other anticonvulsants, the frequency of side effects may increase.

Paroxetine has a much weaker inhibition of the antihypertensive effects of guanethidine compared to antidepressants that inhibit norepinephrine uptake.

How to take, course of use and dosage

Tablets should be taken orally,1 time a day, in the morning, with meals, swallowed whole, washed down with water.

The dose is selected individually during the first 2-3 weeks after the start of therapy and subsequently adjusted if necessary.

For depression, the recommended dose is 20 mg once a day. If necessary, the dose is gradually increased by 10 mg / day, the maximum daily dose should not exceed 50 mg.

For obsessive-compulsive disorders, the initial therapeutic dose is 20 mg / day, followed by a weekly increase of 10 mg. The recommended average therapeutic dose is 40 mg / day, if necessary, the dose can be increased to 60 mg / day.

For panic disorders, the initial dose is 10 mg / day (to reduce the possible risk of developing an exacerbation of panic symptoms), followed by a weekly increase of 10 mg. The average therapeutic dose is 40 mg / day. The maximum dose is 50 mg / day.

For social anxiety disorders / social phobias, the initial dose is 20 mg / day, if there is no effect for at least 2 weeks, it is possible to increase the dose to a maximum of 50 mg/day. The dose should be increased by 10 mg at intervals of at least a week in accordance with the clinical effect.

In generalized anxiety disorders, the initial and therapeutic doses are 20 mg / day.

In patients with renal and/or hepatic insufficiency, the recommended dose is 20 mg/day.

For elderly patients, the daily dose should not exceed 40 mg.

In order to prevent the development of withdrawal syndrome, discontinuation of the drug should be carried out gradually.

Overdose

Symptoms:  nausea, vomiting, tremor, mydriasis, dry mouth, irritability, nystagmus, restlessness, sweating, drowsiness, sinus tachycardia, convulsions, bradycardia, increased blood pressure, nodular rhythm. In very rare cases, when taken simultaneously with other psychotropic drugs and/or alcohol, ECG changes and coma may occur. With severe overdose – serotonin syndrome, rarely-rhabdomyolysis.

Treatment:  gastric lavage, taking activated charcoal. If necessary, conduct symptomatic therapy. There is no specific antidote.

Special instructions

In order to avoid the development of neuroleptic malignant syndrome, Paroxetine should be prescribed with caution to patients taking neuroleptics.

Treatment with Paroxetine is prescribed 2 weeks after the withdrawal of MAO inhibitors.

In elderly patients, hyponatremia is possible while taking Paroxetine.

In some cases, it is necessary to adjust the dose of concomitantly administered insulin and / or oral hypoglycemic drugs.

If seizures develop, treatment with Paroxetine is discontinued.

At the first sign of mania, Paroxetine therapy should be discontinued.

During the first few weeks of Paroxetine therapy, the patient’s condition should be carefully monitored for possible suicide attempts.

During therapy with Paroxetine, you should refrain from taking alcohol due to its increased toxic effect.

Use in pediatrics

The use of Paroxetine in children is not recommended, since its safety and efficacy in this group of patients have not been established.

Influence on the ability to drive motor vehicles and manage mechanisms

Despite the fact that paroxetine does not impair cognitive and psychomotor functions, patients should refrain or exercise extreme caution when driving a car and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Tablet Form of production

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Paroxetine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Depression, Mental disorders, Obsessive-Compulsive Disorder, Phobias and Panic attacks