Paksil

Paksil – drug with antidepressive action.

Form of release and structure

Dosage form of release of Paksil – a tablet, film coated: white, biconvex, oval; on one party – risk, on another – an engraving "20" (on 10 pieces in blisters, on 1, 3 or 10 blisters in a cardboard pack).

Structure of 1 tablet:

• Active ingredient: пароксетин – 20 mg (a paroksetina of a hydrochloride гемигидрат – 22,8 mg);
• Additional components and cover: Opadry white – 7 mg (a macrogoal of 400 - 0,6 mg, a gipromelloza – 4,2 mg, titanium dioxide – 2,2 mg, polysorbate of 80 - 0,1 mg), magnesium stearate – 3,5 mg, a calcium hydrophosphate dihydrate – 317,75 mg, sodium carboxymethylstarch (type A) – 5,95 mg.

Indications to use

• Depression of all types, including heavy and situational depression, and also the depression proceeding with alarm. By efficiency effect of drug has similarity to tricyclic antidepressants. There are data that it yields good results at patients at inefficiency of standard treatment with antidepressants. At long therapy Paksil is effective for prevention of a recurrence of a depression;
• Panic frustration with an agoraphobia and without it – as means of the supporting and preventive therapy; drug is most effective at use in a combination with cognitive and behavioural treatment;
• The Obsessivno-kompulsivnye Frustration (OKF) – as the supporting and preventive therapy; drug is effective at use with the preventive purpose for prevention of a recurrence;
• Social phobia – as the supporting and preventive therapy;
• Generalized alarming frustration – as the long supporting and preventive therapy; drug is effective for prevention of a recurrence;
• Posttraumatic stressful frustration – treatment.

Contraindications

• The combined use with methylene blue, Pimozidum, thioridazine and monoamine oxidase inhibitors (with the last it is necessary to observe an interval not less than 14 days);
• Age up to 18 years;
• Hypersensitivity to drug components.

In case of need Paksil's uses by pregnant women to women, and also when planning pregnancy it is recommended to consider the possibility of purpose of alternative treatment.

Route of administration and dosage

Pill Paksil should be taken inside, without chewing, entirely, it is desirable – in the morning along with meal.

It is recommended to observe the following mode of dosing (a daily dose with frequency rate of reception once a day):

• Depression: 20 mg (initial dose). In case of need perhaps step-by-step increase in a dose (on 10 mg of 1 times in 7 days) before achievement of maximum – 50 mg. It is necessary to estimate Paksil's efficiency for the purpose of dose adjustment in 2-3 weeks of therapy. Duration of a course is defined by indications (up to several months);
• Panic frustration: 10 mg (initial dose). In case of need perhaps step-by-step increase in a dose (on 10 mg of 1 times in 7 days) to recommended or maximum (40/60 mg). Course duration – several months and longer;
• ROC: 20 mg (initial dose). In case of need perhaps step-by-step increase in a dose (on 10 mg of 1 times in 7 days) to recommended or maximum (40/60 mg). Course duration – several months and longer;
• Social phobia, generalized alarming and posttraumatic stressful frustration: 20 mg (initial dose). In case of need perhaps step-by-step increase in a dose (on 10 mg of 1 times in 7 days) to 50 mg.

After the end of therapy to reduce probability of emergence of a withdrawal, it is necessary to reduce a drug dose before achievement of 20 mg step by step – on 10 mg a week. In 7 days Paksil it is possible to cancel completely. If symptoms of cancellation are observed at decrease in a dose or after drug withdrawal, it is reasonable to resume therapy in the dose appointed earlier, and then to reduce a dose more slowly.

Patients at advanced age need to begin therapy with the recommended initial dose which it is possible to increase gradually to 40 mg a day. Patients with heavy functional disturbances of kidneys (the clearance of creatinine – is less than 30 ml in a minute) should appoint reduced doses (in the lower part of therapeutic range).

Side effects

Frequency and intensity of some listed below disturbances connected with Paksil's reception in process of continuation of therapy can decrease. In this case usually drug withdrawal is not required.

During treatment there can be following side effects (> 1/10 – very often;> 1/100, <1/10 – it is frequent;> 1/1000, <1/100 – infrequently;> 1/10 000, <1/1000 – it is rare; <1/10 000, taking into account separate cases – it is very rare):

• Respiratory system: often – yawning;
• Nervous system: often – dizziness, a tremor, a headache; infrequently – extrapyramidal frustration; seldom – an akathisia, spasms, a syndrome of uneasy legs; very seldom – a serotoninovy syndrome (in the form of hallucinations, agitation, confusion of consciousness, the strengthened sweating, a hyperreflexia, a myoclonus, tachycardia with a shiver and a tremor); in rare instances at simultaneous use with neuroleptics or disturbance of motive functions – extrapyramidal symptomatology, including orofatsialny dystonia;
• Cardiovascular system: infrequently – postural hypotonia, sinus tachycardia;
• Gepatobiliarny system: seldom – increase in level of liver enzymes; very seldom – a liver failure and/or the hepatitis which is followed in certain cases by jaundice; sometimes – increase in levels of liver enzymes; seldom or never (on the basis of results of post-marketing observations) – damages of a liver (in the form of a liver failure and/or hepatitis, sometimes with jaundice);
• Hemopoietic system: infrequently – abnormal bleedings, mainly, in mucous membranes and skin (in most cases – bruises); very seldom – thrombocytopenia;
• Digestive tract: very often – nausea; often – dryness in a mouth, vomiting, diarrhea, a lock; very seldom – gastrointestinal bleedings;
• Immune system: very seldom – allergic reactions (including a Quincke's disease, a small tortoiseshell);
• Mentality: often – agitation, sleeplessness, drowsiness, unusual dreams (including dreadful dreams); infrequently – hallucinations, confusion of consciousness; seldom – maniacal reactions (also these disturbances can be connected with a disease);
• Urinary system: seldom – an urination delay, an urine incontience;
• Endocrine system: very seldom – a syndrome of disturbance of secretion of antidiuretic hormone;
• Food and metabolism: often – appetite reduction, increase in level of cholesterol; seldom – a hyponatremia (in most cases – at elderly patients);
• Sight: often – a sight illegibility; infrequently – a mydriasis; very seldom – acute glaucoma;
• Reproductive system and mammary glands: very often – sexual dysfunction; seldom – гиперпролактинемия / a galactorrhoea;
• Hypodermic fabrics and skin: often – perspiration; infrequently – skin rashes; very seldom – heavy skin reactions, photosensitivity reactions;
• Others: often – increase in weight, an adynamy; very seldom – peripheral hypostases.

At cancellation of reception of Paksil such disturbances can develop:

• Often: sleep disorders, alarm, touch disturbances, headache, dizziness;
• Infrequently: confusion of consciousness, diarrhea, nausea, perspiration, agitation, tremor.

Paksil's reception at children can lead to emergence of the following side effects: emotional lability (including suicide attempts and thoughts, mood swings, infliction of harm to, tearfulness), perspiration, hyperkinesia, appetite reduction, hostility, agitation, tremor.

Special instructions

At patients at young age, especially during treatment of big depressive frustration, Paksil's reception can increase risk of development of suicide behavior.

The aggravation of symptoms at a depression and/or emergence of suicide thoughts and suicide behavior can occur irrespective of whether the patient receives antidepressants. The probability of their development remains until approach of the expressed remission. Because improvement of a condition of patients, as a rule, occurs in several weeks of reception of Paksil, during this period they need to provide careful control of a state, especially at the beginning of a medical course.

It is necessary to consider that at other mental disorders at which Paksil is shown there is a high risk of suicide behavior too.

In some cases, most often in the first several weeks of therapy, use of drug can lead to developing of an akathisia (it is shown in the form of internal concern and psychomotor excitement when the patient cannot be in a quiet state – to sit or stand).

Such disturbances as agitation, akathisia or mania, can be displays of the main disease or develop as side effect of reception of Paksil. Therefore in cases when the available symptoms worsen, or at development of new, it is necessary to address the specialist for consultation.

Sometimes, most often during the combined use with other serotonergic drugs and/or neuroleptics, development of a serotoninovy syndrome or symptoms which are similar to a malignant antipsychotic syndrome is possible. If there are such symptoms as the vegetative frustration, a myoclonus, a hyperthermia, muscular rigidities which are followed at the same time by fast changings of indicators of functions, important for life, and also the changes of the mental status including confusion of consciousness and irritability cancel treatment.

Big depressive episodes in certain cases are initial display of bipolar disorders. It is considered that monotherapy by Paksil can increase probability of the accelerated development of the maniacal / mixed episode in the patients subject to risk of emergence of this state. Before purpose of drug for assessment of risk of development of bipolar disorder it is necessary to carry out the careful screening including the detailed psychiatric family anamnesis with data on cases of a depression, a suicide and bipolar disorder. Within bipolar disorder Paksil is not intended for therapy of a depressive episode. With care patients should appoint it with the anamnestic data indicating existence of a mania. Also purpose of drug demands care against the background of epilepsy, the closed-angle glaucoma contributing to bleedings of diseases including use of the substances/medicines increasing probability of development of bleedings.

Development of symptoms of cancellation (in the form of suicide thoughts and attempts, changeability of mood, nausea, tearfulness, nervousness, dizziness, pains in a stomach) does not mean that Paksil causes dependence or the fact that abuse it.

If during treatment convulsive attacks develop, Paksil cancel.

Because of the existing risk of development of side effects from mentality and a nervous system, in operating time with mechanisms and at control of motor transport it is necessary to be sick especially careful.

Medicinal interaction

Absorption (absorption) and Paksil's pharmacokinetics at alcohol intake, food, digoxin, antacids, propranolol does not change, however it is not recommended to take the drinks containing alcohol during therapy.

At the combined use of Paksil with some substances / medicines development of the following effects is possible:

• Pimozidum: its level in blood increases, QT interval is extended (such combination of drugs is contraindicated; in need of the combined use it is necessary to be careful and carry out careful monitoring of a state);
• Serotonergic medicines (including lithium, triptanes, fentanyl, L-tryptophane, SIOZS group drugs, трамадол and vegetable means with the maintenance of the made a hole St. John's Wort): the probability of development of a serotoninovy syndrome increases (the combined use of Paksil with monoamine oxidase inhibitors and linezolidy is contraindicated);
• Ritonavir and/or фосампренавир: considerably Paksil's concentration in a blood plasma decreases;
• Inhibitors and enzymes which take part in metabolism of medicines: the pharmacokinetics and metabolism of a paroksetin changes;
• Drugs which are metabolized by CYP2D6 liver enzyme (tricyclic antidepressants, thioridazine, Perfenazinum and other antipsychotic drugs of a fenotiazinovy row, атомоксетин, рисперидон, флекаинид, пропафенон and some other antiarrhytmic means of a class 1 C): their concentration in plasma increases;
• Protsiklidin: its concentration in a blood plasma (at development of anticholinergic effects its dose needs to be reduced) increases.

Terms and storage conditions

To store in the place, unavailable to children, at a temperature up to 30 °C.

Period of validity – 3 years.