Paksil

Паксил Drug photo

The description is actual on 09.12.2014

  • Latin name: Paxil
  • ATH code: N06AB05
  • Active ingredient: Paroksetin (Paroxetine)
  • Producer: GLAXO WELLCOME PRODUCTION (France)

Structure

Paroksetina a hydrochloride gemigidrat 22,8 milligrams (it is equivalent to 20,0 milligrams of a paroksetin), as excipients: calcium dihydrophosphate a dihydrate, carboxymethylstarch of sodium of type A, magnesium a stearin cover of a tablet — Opadry of white YS color — 1R — 7003 (a macrogoal 400, titanium dioxide, a gipromelloz, polysorbate 80).

Release form

Drug is issued in the tablets of a biconvex form packed in blisters on 10 pieces, in one packaging there can be one, three or ten blisters.

Pharmacological action

Has antidepressive effect on the mechanism of specific oppression by the return serotonin reuptake in functional cells of a brain — neurons.

Pharmacodynamics and pharmacokinetics

Has low affinity with muskarinovy cholinergic receptors. As a result of researches obtained data that:

  • On animals anticholinergic properties are shown poorly.
  • Researches of a paroksetin in vitro — weak affinity to α1-, α2-and to β-adrenoceptors, including to dopamine (D2), serotoninovy a subtype 5-HT1-and 5-HT2-, including to histamine receptors (H1).
  • The researches in vivo confirmed results of in vitro — does not interact with postsynaptic receptors and TsNS does not oppress and does not cause arterial hypotension.
  • Without breaking psychomotor functions, paroksetin does not increase the oppressing effect of ethanol on the central nervous system.
  • Studying of behavioural changes and EEG showed that paroksetin the weak activating effect in the dose exceeding delay of the return serotonin reuptake is capable to cause, at the same time the mechanism is not amfetaminopodobny.
  • AP (arterial pressure), ChSS and ECG does not render significant changes on a healthy organism paroksetin.

As for pharmacokinetics, after intake drug is absorbed and metabolized at "the first passing" of a liver therefore less paroksetin comes to blood, than absorbed from a gastrointestinal tract. Increasing quantity of a paroksetin in an organism (a single dose of high doses or a multiple dose of usual doses) try to obtain partial saturation of a metabolic way and decrease in clearance of a paroksetin of plasma, leading to disproportionate increase in concentration of a paroksetin in plasma. It means that pharmacokinetic parameters are unstable and the kinetics is nonlinear. However, nonlinearity is usually expressed poorly and observed at the patients accepting low doses of drug which cause the low level of a paroksetin in plasma. It is possible to achieve equilibrium concentration in plasma in 1-2 weeks.

Paroksetin is distributed in fabrics, and by pharmacokinetic calculations in plasma there is 1% of all quantity of a paroksetin which is present at an organism. In plasma is in therapeutic concentration about 95% of a paroksetin connected with proteins. Dependence between concentration of a paroksetin in plasma and clinical effects, side reactions is not revealed. It is capable to get into breast milk and into embryos.

Biotransformation occurs in 2 phases: including primary metabolism and system elimination to the inactive polar and conjugated products as a result of process of oxidation and methylation. Time of half-decay varies within 16–24 h. About 64% are brought with urine as metabolites, 2% — in not changed look; the rest — with a stake as metabolites and 1% — in not changed look.

Indications to use

Drug is used at all types of a depression at adults, including reactive and heavy, accompanied with alarm, obsessivno-compulsive frustration for the supporting and preventive therapy. Children and teenagers are 7–17 years old at panic frustration with an agoraphobia and without, social phobias, generalized alarming frustration, posttraumatic stressful frustration.

Contraindications

Hypersensitivity to a paroksetin or other making components.

Side effects

Decrease in frequency and intensity of separate side effects of a paroksetin happens in process of the course of treatment therefore do not demand appointment cancellation. Gradation of frequency is as follows:

  • very often (≥1/10);
  • often (≥1/100, <1/10);
  • sometimes it happens (≥1/1000, <1/100);
  • seldom (≥1/10 000, <1/1000);
  • very seldom (<1/10 000), considering separate cases.

Frequent and very frequent occurrence is defined on the basis of the generalized data about safety of drug at more than 8 thousand patients. Clinical tests were carried out for calculation of distinction of frequency of side effects in group with Paksil and the second group of placebo. Occurrence of side effects of Paksil of rare or very rare is defined on the basis of post-marketing information on the frequency of messages, but not true frequency of these effects.

Indicators of side effects are stratified on bodies and frequency:

  • Blood and lymphatic system: seldom there are abnormal bleedings (hemorrhage in skin and mucous). Thrombocytopenia is very seldom possible.
  • Endocrine system: very seldom — disturbance of secretion of ADG.
  • Immune system: very seldom there are allergic reactions like small tortoiseshell and a Quincke's disease.
  • Metabolism: "often" cases of loss of appetite, sometimes at elderly patients at disturbance are secretions of ADG — a hyponatremia.
  • TsNS: often there is a drowsiness or sleeplessness, convulsive attacks; seldom — opacification of consciousness, a hallucination, maniacal reactions as possible symptoms actually diseases.
  • Sight: very seldom there is an exacerbation of glaucoma, however is "frequent" — a sight illegibility.
  • Cardiovascular system: sinus tachycardia, and also tranzitorny decrease or increase of the ABP was "seldom" noted.
  • Respiratory organs, thorax and mediastinum: yawning was "often" noted.
  • Gastrointestinal tract: "it is very frequent" nausea is fixed; often — a lock or diarrhea at dryness in a mouth; very seldom register gastrointestinal bleedings.
  • Gepatobiliarny system: increase of level of a producing liver enzymes was rather "seldom" noted; cases of the hepatitis which is followed by jaundice and/or a liver failure are very rare.
  • Epidermis: often registered perspiration; are rare a case of skin rashes and are very rare — photosensitivity reactions.
  • Urinary system: seldom registered an ischuria.
  • Reproductive system: very often — cases of sexual dysfunction; seldom — a giperprolaktinemiya and a galactorrhoea.
  • Among the general disturbances: the adynamy is often fixed, and it is very rare — peripheral hypostases.

The approximate list of symptoms which can arise after end of a course paroksetiny is established: "often" noted dizziness and other touch disturbances, disturbances of a sleep pattern, presence of feeling of alarm, headaches; sometimes — strong contagious excitation, nausea, a tremor, perspiration, and also diarrhea. Most often these symptoms at patients are easy and poorly expressed, pass without intervention. The groups of patients put the increased risk of side effects are not registered, but if there is no bigger need for treatment paroksetiny, reduce a dose smoothly to full cancellation.

Tablets Paksil, application instruction (Way and dosage)

Pill is taken orally, swallowing entirely and not chewing. Accept one time a day since morning during food.

At a depression for adults the dose of 20 mg a day is recommended, if necessary the dose can be increased every week by 10 mg a day to the maximum daily concentration — 50 mg. Adjust a dose of a paroksetin after 2–3 weeks of a course of treatment and further — everything depends on clinical indications.

Dose at obsessivno-compulsive frustration for adults — 40 mg a day, since a dose in 20 mg a day and each 7 days increasing on 10 mg a day. The maximum dose in days — 60. For age from 7 to 17 years it is necessary to begin with a dose in 10 mg a day, weekly raising to 10 mg a day, as much as possible — 50 mg a day.

At panic frustration usually appoint for adult 40 mg a day, since 10 mg a day and each 7 days raising on 10 mg a day depending on clinical effects, as much as possible — 60 mg a day. Minimize an initial dose not to aggravate the symptomatology of panic frustration arising in an initiation of treatment of any sort antidepressants.

Social phobias: for adult 20 mg a day, in case of need a dose increase every week by 10 mg a day up to 50 mg a day. Treatment of children age from 7 to 17 years is appointed from a dose of 10 mg a day and the subsequent weekly increase to 10 mg a day, the most admissible daily dose of 50 mg a day.

Generalized alarming frustration: the dose for adult 20 mg a day increased every week by 10 mg a day, extreme value – 50 mg a day.

The application instruction of Paksil for posttraumatic stressful frustration assumes a dosage for adults: 20 mg a day, in case of need increased by 10 mg a day every week to 50 mg a day.

Overdose

There are following symptoms of overdose:

  • vomiting;
  • mydriatic pupils;
  • fever;
  • alarm;
  • in any of the parties of change of the ABP;
  • involuntary reductions of muscular tissue;
  • agitation;
  • tachycardia.

Patients settled into shape without serious damage to health even after one-time reception of a dose within 2000 mg. Messages with the description of such symptoms as a coma, changes of an ECG are registered. At the patients accepting paroksetin with various psychotropic drugs or with alcohol death cases were very seldom noted.

The following general measures are shown: a gastric lavage, absorbent carbon of 20-30 mg each 4–6 h in the first days, the maintenance therapy and regular research of the main physiological indicators is also necessary.

Paroksetin has no specific antidote.

Interaction

Paroksetin is not recommended to apply with MAO inhibitors, and also within 2 weeks after end of a course; in a combination with thioridazine because, as well as other drugs which oppress activity of CYP2 D6 enzyme of P450 cytochrome increases concentration of thioridazine in plasma. Paksil is capable to strengthen action of alkogolsoderzhashchy means and to reduce efficiency of Digoxin and Tamoxifenum. Inhibitors of a microsomal oxidation and Cimetidinum increase activity of a paroksetin. Applying with indirect coagulants or antitrombichesky means increase of bleeding is observed.

Terms of sale

According to the recipe.

Storage conditions

In the dry place, unavailable to children, protected from light. Admissible temperature of no more than 30 ° Celsius.

Period of validity

To be stored till three years.

Paksil and alcohol

As a result of clinical trials data were obtained that absorption and pharmacokinetics of active ingredient — a paroksetin does not depend or almost does not depend (that is dependence does not demand change of doses) on a diet and alcohol. It is not established that paroksetin strengthened a negative impact of ethanol on a psychomotor system, however, it is not recommended to accept it together with alcohol as generally alcohol suppresses effect of drug — reducing efficiency of treatment.

Concerning alcohol intake at treatment by Paksil show that if to drink once, then a medicine metabolism sharply to decrease – without causing negative effects, however if to drink regularly — it on the contrary — will accelerate. The patients suffering from hard drinkings at overdose by Paksil usually or are hospitalized in a serious condition, or there can be a lethal outcome.

Paksil's analogs

The listed below drugs are analogs of drug, that is they have the international unlicensed name or available other ingredients in addition to active ingredient too — a paroksetina:

For drug replacement Paksil on any analog, it is necessary to consult with the doctor!

Zdravzona

  • Paksil of 20 mg No. 30 of a tablet
  • Paksil of 20 mg No. 100 of a tablet

Drugstore of IFC

  • Paksil tbl p / about 20 mg No. 30 *, Es. SI. Evrofarm of Es. A.Rumyniya
  • Paksil tbl p / about 20 mg No. 100 *, Es. SI. Evrofarm of Es. A.Rumyniya
to show still
Section: For a nervous system
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Education: Graduated from the Nikolaev national university of V. A. Sukhomlinsky, gained the diploma of the specialist with honors as "An embryologist, a cytologist, a histologist". Also, the human physiology and animals, the teacher of biology" graduated from a magistracy majoring in ". The course on discipline "Pharmacology" is with honors passable.

Experience: Worked as the senior laboratory assistant of department of Physiology and biochemistry of the Nikolaev national university of V. A. Sukhomlinsky in 2010 - 2011.

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