Paxil

Description overdue on 09/12/2014

• Latin name: Paxil
• ATC code: N06AB05
• Active substance: Paroxetine (Paroxetine)
• Manufacturer: GLAXO WELLCOME PRODUCTION (France)

Photos of the drug

Tweet

• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Paxil tablets, instructions for use (method and dosage)
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• With alcohol
• Analogs
• Reviews
• Price, where to buy

Composition

Paroxetine hydrochloride hemihydrate   22, 8 milligrams (equivalent to 20 milligrams 0 paroxetine ), As auxiliary substances: calcium dihydrogen phosphate dihydrate . sodium carboxymethyl starch   Type A   stearic magnesium shell   Tablets - Opadry white YS - 1R - 7003 (macrogol 400, titanium dioxide, hypromellose, polysorbate 80).

Product form

The drug is available in tablets lenticular shape, packaged in blister packs of 10 pcs., In the same package can be one, three or ten blisters.

Pharmacological action

Renders antidepressant action   the mechanism of inhibition by specific reuptake Serotonin   in functional brain cells - neurons .

Pharmacodynamics and pharmacokinetics

It has a low affinity muscarinic cholinergic receptors . As a result of research data received that:

• Animal anticholinergic properties   are weak.
• Studies in vitro paroxetine - weak affinity for α1-, α2- and β-adrenoceptor , Including the dopamine (D2) . subtype of serotonin 5-NT1- and   5 NT2- , including histamine receptors (H1) .
• The in vivo studies confirmed the results of in vitro - does not interact with postsynaptic   and depresses the central nervous system and causes hypotension .
• Without prejudice psychomotor functions , Paroxetine does not increase the inhibitory effect ethanol on central nervous system .
• The study of behavioral changes and EEG   It showed that paroxetine is able to induce weak activating effect in the dose exceeding the deceleration of serotonin reuptake, wherein the mechanism is not amphetamine .
• In a healthy body paroxetine does not have any significant changes in blood pressure ( Blood Pressure ) Heart Rate and ECG.

With regard to pharmacokinetics after oral drug absorbed and metabolized when "first pass" of the liver, resulting in blood paroxetine receives less than absorbed from the gastrointestinal tract. By increasing the amount of paroxetine in the body (a single intake of large doses or multiple receiving conventional doses) achieve partial saturation pathway   and reducing the clearance of paroxetine plasma , Resulting in a disproportionate increase in the plasma concentration of paroxetine. This means that the pharmacokinetic parameters are unstable and the kinetics are nonlinear. However, the non-linearity is usually expressed weakly observed in patients taking low doses of the drug, which causes a low level of paroxetine plasma. To achieve equilibrium concentration in the plasma can be 1-2 weeks.

Paroxetine tissue distribution and pharmacokinetic calculations plasma is 1% of the total amount of paroxetine present in the body. At therapeutic concentrations of about 95% of paroxetine in plasma is associated with proteins . There was no relationship between the plasma concentration of paroxetine and clinical effects, adverse reactions. It is able to penetrate into the breast milk   and in Embryos .

Biotransformation It takes place in 2 phases, including primary metabolism and a system elimination before inactive polar and conjugated products   resulting from the process oxidation and methylation . The half-life   It varies within 16-24 hours. Approximately 64% excreted in urine as metabolites, 2% - not in a modified form; the rest - in the faeces as the metabolites and 1% - in the non-modified form.

Indications

The drug is used in all types of depression   in adults, including reactive and severe, accompanied by anxiety, obsessive compulsive disorder   for maintenance and preventive care. Children and adolescents 7-17 years with panic disorder with agoraphobia and without social phobia, generalized anxiety disorder, posttraumatic stress disorder.

Contraindications

Hypersensitivity to paroxetine   or other ingredients.

Side effects

Reducing the frequency and severity of certain side effects of paroxetine as occurs during treatment, therefore did not require discontinuation of use. Graduation rate is as follows:

• very common (≥1 / 10);
• often (≥1 / 100, & lt; 1/10);
• sometimes happens (≥1 / 1000, & lt; 1/100);
• rarely (≥1 / 10 000, & lt; 1/1000);
• very rare (& lt; 1/10 000), taking into account individual cases.

Frequent and very frequent occurrence is determined on the basis of aggregated data about the safety of the drug in more than 8000 patients. Clinical Trials   performed to calculate the differences in the frequency of side effects in the group with Paxil and second placebo. The incidence of side effects of Paxil rare or very rare defined on the basis of post-marketing data on the frequency of messages, rather than the true frequency of these effects.

Indicators stratified side effects to organs and frequency:

• Blood and lymphatic system : Rarely happen abnormal bleeding (bleeding into the skin and mucous membranes). Very rare opportunity thrombocytopenia .
• Endocrine system : Very rarely - a violation of secretion ADH .
• The immune system : Very rare cases allergic reactions   type hives   and angioedema .
• Metabolism "Often" cases decrease Appetite Sometimes in elderly patients in violation of secretion of ADH - hyponatremia .
• CNS : Often drowsiness or insomnia . seizures ; rarely - dizziness . hallucinations . manic reactions   as the possible symptoms of the disease itself.
• Sight Very rarely aggravation of glaucoma But "often" - blurred vision.
• Cardiovascular system "Seldom" marked sinus tachycardia , And transitory reduction or increased blood pressure.
• Respiratory . thoracic and mediastinal disorders "Often" marked yawn .
• GI : "Very often" fixed nausea ; often - constipation or diarrhea   at dry mouth ; very rarely recorded gastrointestinal bleeding.
• Hepatobiliary System : Sufficient "rarely" marked increase in production liver enzymes ; very rare cases hepatitis Accompanied by jaundice and / or hepatic insufficiency .
• The epidermis Frequently recorded Sweating ; rare cases skin rash and very rare - reaction photosensitivity .
• The urinary system : Seldom recorded delay Urine .
• Reproductive system : Very often - Cases sexual dysfunction ; rarely - hyperprolactinemia   and galaktorei .
• Among the general disorders: often fixed asthenia And very rarely - peripheral edema.

Installed a rough list of symptoms that may occur after completion of the course paroxetine "Often" marked dizziness   and others sensory impairment , Sleep disorders, there is a feeling of anxiety, headache ; sometimes - strong emotional excitement . nausea . tremor . Sweating , and diarrhea . In most patients, these symptoms are mild and easy pass without interference. Not yet registered group of patients subjected to an increased risk of side effects, but if there is no greater need in the treatment of paroxetine, reduce the dose gradually to a complete cancellation.

Paxil tablets, instructions for use (method and dosage)

Tablets are taken orally by swallowing whole and without chewing. Take one every day in the morning during meals.

At depression Adult recommended dose of 20 mg per day, if necessary dose can be increased every week by 10 mg per day to a maximum daily concentration - 50 mg. Correct dosage of paroxetine after 2-3 weeks of treatment and then - it all depends on clinical indications.

Dose obsessive compulsive disorder   Adult - 40 mg per day starting from the dose of 20 mg per day, and every 7 days increasing by 10 mg per day. The maximum dose per day - 60. For ages 7 to 17 years should start with a dose of 10 mg daily, weekly, increasing to 10 mg per day, maximum - 50 mg per day.

At panic disorders   usually prescribed for adults in the 40 mg per day, from 10 mg per day, and every 7 days increasing by 10 mg per day, depending on the clinical effect, the maximum - 60 mg per day. Minimize initial dose, so as not to aggravate the symptoms of panic disorder, occurring in the early treatment of any kind antidepressants .

Social phobia : 20 mg for adult per day, if necessary, increase the dose every week at 10 mg per day to about 50 mg per day. Treatment of children age 7 to 17 years with the assigned dose of 10 mg per day and then weekly increase of 10 mg per day, the maximum daily dose of 50 mg per day.

Generalized anxiety disorder : Adult dose of 20 mg per day, increased every week by 10 mg per day, the limit value - 50 mg per day.

Instructions for use of Paxil for post-traumatic stress disorder   It assumes the dosage for adults: 20 mg a day, if necessary increased by 10 mg per day, every week to 50 mg per day.

Overdose

There are the following symptoms of overdose:

• vomiting ;
• dilated pupils ;
• fever ;
• alarm ;
• any of the parties changes in blood pressure;
• involuntary contraction of muscle tissue ;
• agitation ;
• tachycardia .

Patients returned to normal without serious damage to health even after a single dose receiving within 2,000 mg. Joined Posts description of symptoms such as coma Changes ECG . Patients taking paroxetine with various psychotropic drugs   or alcohol rarely were cases death .

Showing the following general steps: gastric lavage . Activated carbon   20-30 mg every 4-6 hours during the first day, as needed maintenance therapy   and regular study vital signs .

Paroxetine has no specific antidote .

Cooperation

Paroxetine is not recommended for use with MAO inhibitors As well as for 2 weeks following completion of the course; in combination with thioridazine Because, as well as other drugs that inhibit the activity of enzyme CYP2 D6 Cytochrome P450 Increases in the plasma concentration of thioridazine. Paxil is able to increase the effects of alcohol-drugs and reduce the effectiveness of Digoxin   and T amoksifena . Inhibitors of microsomal oxidation   and Cimetidine increase the activity of paroxetine. Applying with indirect coagulants and antithrombotic agents there is an increase of bleeding.

Terms of sale

Prescription.

Storage conditions

In a dry place inaccessible to children, protected from light. Permissible temperature not exceeding 30 ° C.

Shelf life

Store up to three years.

Paxil and alcohol

As a result, clinical studies have provided evidence that the pharmacokinetics and absorption of the active substance - paroxetine independent or nearly independent of (i.e., does not require changing the dependence of dose) of diet   and alcohol. Not applicable to paroxetine increased the negative effect of ethanol on psychomotor However, it is not recommended to take it with alcohol, since alcohol mainly inhibits the action of the drug - reducing the effectiveness of treatment.

Comments regarding the use of alcohol in the treatment of Paxil show that if you drink once, metabolism drug dramatically reduced - without causing negative effects, but if you drink regularly - it is the opposite - accelerated. Patients suffering heavily, with an overdose of Paxil usually either get to the hospital in serious condition, or it may be death .

Analogs of Paxil

Match code ATC 4th level:

• Reksetin
• Luvox
• Tsipraleks
• Fluoxetine

The following drugs - is an analogue of the drug, that is, they have the same International Non-proprietary name or in the presence of other ingredients in addition to the active ingredient - paroxetine:

• Paroxetine
• Paroksin
• Reksetin

To replace the drug Paxil for any analog should definitely consult a doctor!

Reviews of Paxil

Most often, a patient testimonials about Paxil positive: the effect occurs after the first week of admission. The forums have noted that in the majority, side effects and other undesirable symptoms are weak and eventually eliminated spontaneously.

At the same time reviews of the doctors described the danger of Paxil drug withdrawal Because it can take severe and require the use of tranquilizers . sleeping pills .

After reviewing the various reviews and opinions, it can be argued that Paxil should not be used independently without the appointment and control of the dosage the doctor. It is important to remember not to change the dosage, forget about the interaction with other drugs and alcohol.

The price of Paxil where to buy

Buy Paxil prescription drug in the Russian Federation can be priced at about 700 rubles, in Ukraine the price of 300 USD.

Get the best price and buy