Producer: JSC VEROPHARM Russia
Code of automatic telephone exchange: N06AB05
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active agent: a paroksetina of a hydrochloride гемигидрат ( in terms of пароксетин) — 20 mg;
excipients: calcium hydrophosphate (calcium phosphate disubstituted), starch corn, примогель (sodium carboxymethylstarch), magnesium stearate;
structure of a cover: Опадрай II [gipromelloz (gidroksipropilmetiltsellyuloz), lactose monohydrate, macrogoal (polyethyleneglycol 3350, polyethyleneglycol 4000), titanium dioxide].
Description: tablets, film coated white or almost white color, round, biconvex.
Paroksetin is powerful and selection inhibitor of capture of a 5-gidroksitriptamin (5-HT, serotonin) brain neurons that defines its antidepressive action and efficiency at treatment of obsessivno-compulsive ROC) and panic frustration.
The main metabolites of a paroksetin represent the polar and conjugated products of oxidation and methylation which are quickly brought out of an organism, have weak pharmacological activity and do not influence its therapeutic action. At metabolism of a paroksetin the selection capture caused by its action is not broken by 5-HT neurons.
Paroksetin has low affinity to muskarinovy cholinergic receptors.
Possessing the selection action, in difference from tricyclic antidepressants, пароксетин showed low affinity to α-1, α-2, to β-adrenoceptors, and also to opaminovy, 5-HT1 similar, 5-HT2 similar and histamine (H1) receptors.
Paroksetin does not break psychomotor functions and does not potentiate oppressing effect of ethanol on them.
According to a research of behavior and EEG, at a paroksetin the weak activating properties when it is appointed in doses come to light is higher than those which are necessary for inhibition of capture 5-HT. It does not cause considerable change of level of arterial pressure, heart rate and EEG in healthy volunteers.
Unlike antidepressants which inhibit capture of noradrenaline пароксетин suppresses anti-hypertensive effects of a guanetidin much more weakly.
Pharmacokinetics. Paroksetin is well soaked up after intake and is exposed to metabolism of the first passing through a liver. Allocation of not changed paroksetin with urine usually makes less than 2% of a dose, and metabolites make about 64% of a dose. Intestines excrete about 36% of a dose probably through bile in which not changed пароксетин makes less than 1% of a dose. Thus, пароксетин it is removed preferential as a result of metabolism.
Removal from an organism of metabolites of a paroksetin bi-phase, at first as a result of metabolism of the first passing through a liver, and then it is controlled by system elimination. The elimination half-life varies, but usually makes about one day. Steady system levels are reached by 7–14 day after an initiation of treatment, and the pharmacokinetics during prolonged treatment does not change. Clinical effects of a paroksetin (side effect and efficiency) do not correlate with its concentration in plasma.
As metabolism of a paroksetin includes a stage of the first passing through a liver, its quantity defined in system circulation is less than that which is absorbed from a zhedudochno-intestinal path. At increase in a dose of a paroksetin or at repeated dosing when load of an organism increases, there is a partial absorption of effect of the first passing through a liver and decrease in plasma clearance of a paroksetin. As a result of it increase in concentration of a paroksetin in plasma and fluctuations of pharmacokinetic parameters is possible that can be observed only at those patients who at reception of low doses reach low levels of drug in plasma.
Paroksetin is extensively distributed in fabrics, and pharmacokinetic calculations show that only 1 his % is present at plasma, and in therapeutic concentration of 95% is connected with proteins of plasma.
At elderly patients, and also at those who have a heavy renal and liver failure concentration of a paroksetin in plasma is increased, and the range of plasma concentration at them almost matches the range of healthy adult volunteers.
Indications to use:
- depression of all types, including the situational, heavy endogenous depression and a depression which is followed by alarm;
- panic frustration, including with an agoraphobia;
- social alarming frustration / social phobia;
- generalized alarming frustration;
- posttraumatic stressful frustration.
Route of administration and doses:
Адепресс accept inside, 1 time a day, in the morning, during food. The tablet is swallowed entirely, washing down with water. The dose is selected individually within the first two-three weeks after the beginning of therapy and afterwards if necessary is adjusted. The effect in most cases develops gradually.
At depressions — the recommended dose of 20 mg of 1 times a day. In case of need the dose is gradually increased by 10 mg at an interval of 1 week before achievement of therapeutic effect, the maximum daily dose should not exceed 50 mg/days.
At obsessivno-compulsive frustration an initial therapeutic dose — 20 mg/days with the subsequent weekly increase by 10 mg before achievement of the therapeutic answer. The recommended average therapeutic dose — 40 mg/days, if necessary a dose can be increased to 60 mg/days.
At panic frustration an initial dose — 10 mg/days (for decrease in possible risk of development of an aggravation of panic symptomatology), with the subsequent weekly increase by 10 mg. An average therapeutic dose — 40 mg/days. The maximum daily dose should not exceed — 60 mg/days.
Social and alarming frustration / sociophobia: the initial dose makes 20 mg a day, in the absence of effect within at least two weeks increase in a dose as much as possible to 50 mg a day is possible. It is necessary to increase a dose by 10 bucketed mg not less than a week according to clinical effect.
Posttraumatic stressful frustration: for most of patients initial and therapeutic doses make 20 mg a day. Increase in a dose as much as possible to 50 mg a day is in certain cases recommended. The dose should be increased by 10 mg every week according to clinical effect.
Generalized alarming frustration: the initial and recommended doses — 20 mg a day.
At a renal and/or liver failure the recommended dose makes 20 mg a day.
For elderly patients the daily dose should not exceed 40 mg.
For the prevention of development of a withdrawal the termination of administration of drug is carried out gradually.
Use of a paroksetin for children is not recommended as its safety and efficiency in this population are not established.
For prevention of a recurrence it is necessary to carry out a maintenance therapy. After disappearance of symptoms of a depression this course can make 4–6 months, and at obsessivny and panic frustration — more than 4-6 months. It is necessary to avoid sharp drug withdrawal.
Features of use:
In order to avoid development of a malignant antipsychotic syndrome with care appoint to the patients accepting neuroleptics.
Paroksetin does not worsen cognitive and psychomotor functions , nevertheless, as well as at treatment by other psychotropic drugs, patients have to be careful when driving and moving mechanisms.
During treatment it is necessary to abstain from the use of ethanol and from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.
Treatment paroksetiny is appointed 2 weeks later after cancellation of MAO inhibitors.
At patients of advanced age the hyponatremia is possible.
In certain cases it is required to dose adjustment of insulin and/or oral hypoglycemic drugs.
At development of spasms treatment paroksetiny is stopped.
At the first symptoms of a mania it is necessary to cancel therapy paroksetiny.
Within the first several weeks it is necessary to watch carefully a condition of the patient in connection with possible suicide attempts.
From a nervous system: often — drowsiness or sleeplessness, a tremor, an adynamy, dizziness, alarm; infrequently — confusion of consciousness, a hallucination, extrapyramidal frustration, paresthesias, decline in the ability to concentration of attention; seldom — spasms, manias; very seldom — a serotoninovy syndrome (agitation, a hyperreflexia, diarrhea), panic frustration.
From sense bodys: in some cases — a vision disorder, a mydriasis.
From urinogenital system: the speeded-up urination, frustration of an ejaculation, frustration of a libido, is rare — an ischuria, is rare гиперпролактинемия / a galactorrhoea, an anorgazmiya.
From cardiovascular system: orthostatic hypotension.
Others: the increased sweating, is rare: allergic reactions (rash, urticaria, ekhimatoza, an itch, a Quincke's disease), in isolated cases a hyponatremia, disturbance of secretion of antidiuretic hormone.
Interaction with other medicines:
Meal and antiacid means does not influence absorption and pharmacokinetic parameters of Adepress.
It is not necessary to accept Adepress along with MAO inhibitors and within 14 days after their cancellation.
During therapy by Adepress it is necessary to abstain from alcohol intake in connection with strengthening of toxic effect of alcohol.
In communication by inhibition paroksetiny P450 cytochrome strengthening of effect of barbiturates, Phenytoinum, indirect anticoagulants, tricyclic antidepressants, fenotiazinovy neuroleptics and antiaritmik of a class 1C, metoprolol and increase in risk of development of side effects at co-administration of these medicines is possible.
At co-administration with the drugs inhibiting liver enzymes the dose decline of a paroksetin can be required.
Paroksetin increases a bleeding time against the background of warfarin reception, at an invariable prothrombin time.
At co-administration of a paroksetin it is recommended to be careful with atypical antipsychotic means, fenotiazina, tricyclic antidepressants, aspirin, non-steroidal anti-inflammatory drugs in connection with possible disturbances of coagulability of blood.
Co-administration with serotonergic drugs (трамадол, суматриптан) can lead to strengthening of serotonergic effect.
Mutual strengthening of effect of tryptophane, drugs of lithium and paroksetin is noted.
At co-administration of a paroksetin with Phenytoinum and other antikonvulsant decrease in concentration of a paroksetin in plasma and increase in frequency of side effects is possible.
Concomitant use with MAO inhibitors and within 14 days after their cancellation;
pregnancy and period of a lactation;
With care: liver failure; renal failure; closed-angle glaucoma; prostate hyperplasia; mania; heart pathology; epilepsy; convulsive states; purpose of a countershock; administration of drugs, increasing risk of bleeding; existence of risk factors of the raised bleeding and the diseases increasing risk of bleeding, advanced age.
Seldom or never, at a concomitant use with other psychotropic drugs and/or alcohol changes on the electrocardiogram, a coma are possible.
Treatment: gastric lavage, absorbent carbon. If necessary symptomatic therapy. There is no specific antidote.
List B. In the dry place at a temperature not above 25 °C. To store in the place, unavailable to children.
Period of validity - 2 years. Not to apply after the expiry date specified on packaging.
According to the recipe
Tablets, coated, 20 mg. On 7, 10 or 14 tablets in a blister strip packaging. 2 blister strip packagings on 14 tablets or 3 blister strip packagings on 10 tablets or 4 blister strip packagings on 7 tablets together with the application instruction in a pack. On 30 tablets in bank of orange glass. Each can together with the application instruction in a pack.