Adepress - instructions for use, doses, side effects, contraindications

Excipients: calcium hydrophosphate (calcium phosphate disubstituted) - 207.8 mg, corn starch - 134.8 mg, primogel (sodium carboxymethyl starch) - 11.4 mg, magnesium stearate - 3.8 mg;

Shell composition: Opadrai II [hypromellose (hydroxypropylmethylcellulose), lactose monohydrate, macrogol (polyethylene glycol 3350, polyethylene glycol 4000), titanium dioxide] - 10.0 mg.

Description:The tablets covered with a film membrane of white or almost white color, round, biconcave.

Pharmacotherapeutic group:Antidepressant

ATX: & nbsp

N.06.A.B Selective serotonin reuptake inhibitors

N.06.A.B.05 Paroxetine

Pharmacodynamics:

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

The main metabolites of paroxetine are polar and conjugated products of oxidation and methylation, which are rapidly excreted from the body, have weak pharmacological activity and do not affect its therapeutic effect.

In the metabolism of paroxetine, the selective uptake of 5-HT neurons due to its action is not impaired.

Paroxetine has low affinity for muscarinic cholinergic receptors.

Having selective action, in contrast to tricyclic antidepressants, paroxetine showed a low affinity for α-1, α-2, β-adrenoceptors, as well as to dopaminovym, 5-HT1 similar, 5-HT₂ similar and histamine (H1) receptors. Paroxetine does not violate psychomotor functions and does not potentiate the inhibitory effect of ethanol on them.

According to the behavioral and EEG studies, paroxetine reveals weak activating properties when it is administered at doses higher than those required to inhibit 5-HT capture. In healthy volunteers, it does not cause a significant change in blood pressure, heart rate and EEG.

In contrast to antidepressants, which inhibit the seizure of norepinephrine, paroxetine much weaker suppresses the antihypertensive effects of guanethidine.

Pharmacokinetics:

Paroxetine is well absorbed after ingestion and is metabolized first pass through the liver. The excretion of unchanged paroxetine in the urine is usually less than 2% of the dose, with metabolites accounting for about 64% of the dose. The intestine excretes about 36% of the dose, probably through bile, in which the unchanged paroxetine is less than 1% of the dose. In this way, paroxetine is excreted mainly as a result of metabolism.

Excretion of metabolites of paroxetine from the body is biphasic, first as a result of the metabolism of the first passage through the liver, and then it is controlled by systemic elimination. The half-life period varies, but usually is about one day. Stable systemic levels are reached by 7-14 days after the start of treatment, and pharmacokinetics during prolonged treatment does not change. The clinical effects of paroxetine (side effect and efficacy) do not correlate with its concentration in the plasma.

Since the metabolism of paroxetine involves the stage of the first passage through the liver, its quantity, determined in the systemic circulation, is less than that which is absorbed from the gastrointestinal tract. With an increase in the dose of paroxetine or with multiple dosing, when the load on the body increases, a partial absorption of the effect of the first passage through the liver and a decrease in the plasma clearance of paroxetine occur. As a result, an increase in the plasma paroxetine concentration and fluctuations in the pharmacokinetic parameters is possible, which can be observed only in those patients who, when taking low doses, reach low plasma levels of the drug.

Paroxetine is extensively distributed in tissues, and pharmacokinetic calculations show that only 1% of it is present in the plasma, and at therapeutic concentrations 95% is associated with plasma proteins.

In elderly patients, as well as those who suffer from severe renal and hepatic insufficiency, the concentration of paroxetine in plasma is increased, and the range of plasma concentrations in them almost coincides with the range of healthy adult volunteers.

Indications:

- depression of all types, including reactive, severe endogenous depression and depression, accompanied by anxiety;

- obsessive-compulsive disorder (OCD);

- panic disorder, including agoraphobia;

- social anxiety disorder / social phobia;

- generalized anxiety disorder;

- post-traumatic stress disorder.

Contraindications:

- hypersensitivity to the components of the drug;

- simultaneous administration with MAO inhibitors and within 14 days after their cancellation;

- unstable epilepsy

- pregnancy and lactation;

Carefully:

liver failure; kidney failure; angle-closure glaucoma; hyperplasia of the prostate; mania; pathology of the heart; epilepsy; convulsive conditions; the appointment of electropulse therapy; taking drugs that increase the risk of bleeding; presence of risk factors for increased bleeding and diseases that increase the risk of bleeding, elderly age.

Pregnancy and lactation:

The use of paroxetine during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

Adepress is taken orally, once a day, in the morning, while eating. The tablet is swallowed whole, washed down with water. The dose is selected individually during the first two to three weeks after the start of therapy and is subsequently adjusted if necessary. The effect in most cases develops gradually.

With depression - The recommended dose of 20 mg once a day. If necessary, the dose is gradually increased by 10 mg with an interval of 1 week before the therapeutic effect is achieved, the maximum daily dose should not exceed 50 mg / day. In obsessive-compulsive disorders the initial therapeutic dose is 20 mg / day followed by a weekly increase of 10 mg until a therapeutic response is achieved.The recommended average therapeutic dose is 40 mg / day, if necessary, the dose may be increased to 60 mg / day.

In panic disorders The initial dose is 10 mg / day (to reduce the possible risk of developing panic symptoms), followed by a weekly increase of 10 mg. The average therapeutic dose is 40 mg / day. The maximum daily dose should not exceed - 60 mg / day.

Socially-disturbing disorders / social phobia: the initial dose is 20 mg per day, in the absence of effect for at least two weeks, an increase in the dose to a maximum of 50 mg per day is possible. The dose should be increased by 10 mg at intervals of at least a week in accordance with the clinical effect.

Post-Traumatic Stress Disorder: for the majority of patients, the initial and therapeutic doses are 20 mg per day. In some cases, a dose increase of up to 50 mg per day is recommended. The dose should be increased by 10 mg every week in accordance with the clinical effect.

Generalized anxiety disorders: the initial and recommended dose is 20 mg per day.

With renal and / or liver failure the recommended dose is 20 mg per day.

For elderly patients daily dose should not exceed 40 mg.

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

Paroxetine application in children is not recommended, since its safety and effectiveness in this population are not established.

To prevent relapses it is necessary to carry out maintenance therapy. After the disappearance of the symptoms of depression, this course can be 4-6 months, and with obsessive and panic disorders - more than 4-6 months. Avoid abrupt discontinuation of the drug.

Precautions for use

To avoid the development of malignant neuroleptic syndrome with caution appoint patients receiving neuroleptics.

Paroxetine does not impair cognitive and psychomotor functions, however, as with other psychotropic medications, patients should be careful when driving and moving machinery.

During the treatment period, one should refrain from using ethanol and from practicing potentially dangerous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Treatment with paroxetine is prescribed 2 weeks after the abolition of MAO inhibitors.

In elderly patients, hyponatremia is possible.

In some cases, correction of the dose of insulin and / or oral hypoglycemic drugs is required.

With the development of seizures, paroxetine treatment is discontinued.

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

During the first few weeks, the patient's condition should be carefully monitored in connection with possible suicidal attempts.

Side effects:

From the nervous system: Drowsiness or insomnia, tremors, asthenia, dizziness, anxiety; Cases of confusion of consciousness, hallucinations, extrapyramidal disorders, paresthesias, and decreased ability to concentrate attention are described. There are isolated reports of convulsions, mania, serotonin syndrome (agitation, hyperreflexia, diarrhea), panic disorders.

From the side of the musculoskeletal system: there were cases of myasthenia gravis, myoclonia, arthralgia, myalgia.

From the sense organs: in some cases - visual impairment, mydriasis.

From the genitourinary system: frequent urination, ejaculatory disorders, libido disorders, single reports - urinary retention, hyperprolactinaemia / galactorrhea, anorgasmia.

From the digestive system: decreased appetite, nausea, vomiting, dry mouth. Cases are described - constipation or diarrhea, in single reports - hepatitis.

From the cardiovascular system: orthostatic hypotension.

Other: increased sweating. In some cases - allergic reactions (rash, urticaria, ecchymatosis, itching, angioedema), in a few cases - hyponatremia, a violation of the secretion of antidiuretic hormone.

Overdose:

Symptoms: nausea, dilated pupils, fever, changes in the arterial pressure, headache, involuntary muscle contractions, agitation, anxiety, tachycardia. In very rare cases, while taking with other psychotropic drugs and / or alcohol, changes in the electrocardiogram, coma are possible.

Treatment: gastric lavage, Activated carbon. If necessary, symptomatic therapy. There is no specific antidote.

Interaction:

The intake of food and anhacids does not affect the absorption and pharmacokinetic parameters of Adepress.

Adepress should not be taken concomitantly with MAO inhibitors and within 14 days after their cancellation.

During therapy, Adeptress should refrain from drinking alcohol because of the increased toxic effect of alcohol.

In connection with paroxetine inhibition of cytochrome P450, the effect of barbiturates, phenytoin, indirect anticoagulants, tricyclic antidepressants, phenothiazine antipsychotics and antiarrhythmics of the class 1C, metoprolol and an increased risk of side effects with the simultaneous administration of these drugs.

At simultaneous appointment with the preparations, inhibiting enzymes of a liver, the dose of paroxetine can be required.

Paroxetine increases bleeding time against the background of taking warfarin, with the same prothrombin time.

With the simultaneous administration of paroxetine with atypical antipsychotic agents, phenothiazines, tricyclic antidepressants, aspirin, nonsteroidal anti-inflammatory drugs, caution should be exercised in connection with possible coagulation disordersblood.

Simultaneous appointment with serotonergic drugs (tramadol, sumatriptan) can lead to an increase in the serotonergic effect.

Mutual enhancement of the action of tryptophan, lithium and paroxetine preparations was noted.

With the simultaneous administration of paroxetine with phenytoin and other anticonvulsants may reduce the concentration of paroxetine in the plasma and increase the incidence of side effects.

Special instructions:

Effect on the ability to drive transp. cf. and fur:

The experience with paroxetine indicates that it does not impair cognitive and psychomotor functions. However, as with any other psychotropic medications, patients should be especially cautious when driving a car and working with mechanisms.

Form release / dosage:

The tablets covered with a cover, 20 mg.

Packaging:For 7, 10 or 14 tablets in a contour mesh package. 2 contour packs of 14 tablets or 3 contour packs of 10 tablets or 4 contour packs of 7 tablets together with instructions for use in a cardboard box. For 30 tablets in a jar of lightproof glass.Each jar along with instructions for use in a cardboard box.

Storage conditions:

At a temperature of no higher than 30 ° C. Store in inaccessible to children.

Shelf life:

3 years.

Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002455

Date of registration:21.03.2012/17.09.2015

Expiration Date:Unlimited

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp04.02.2017

Illustrated instructions

Instructions

Adress (Adepress)