Sertraline

Chemical name

(1S,4S)-4-(3,4-Дихлорфенил)-1 ,2,3,4-тетрагидро-N-метил -1-нафтиламина (as hydrochloride)

Gross

C17-H17-Cl2-N

Characteristics

The white crystalline powder. Poor soluble in water and alcohol izopropilovom, soluble in ethanol.

Of drugs

Drugs, the antidepressant. Yes blocking reverse takeover presinapticescoy serotonin neuronal membrane brain and trombozitami; Had little impact on the others. Neiromediatorov (norarenalina and dopamine) in the synaptic junctions. With long-term use reduces adrenoretseptorov in Zns.posle intake of fully absorbed. The food in their stomachs Boosts C_max (25%), and shortens the time to achieve it. C_max determined through 4,5-8,4 h (depending on dose). Linking plasma protein is 98%. The "first pass" through the liver is the active metabolite - N-desmetilsertralin, which (as sertralin) has been intense biotransformation with izofermenta 3A4 zitohroma P450 (dezaminiruetsa, gidrauxiliruetsa) and kongugiruet glukuronova with acid. T_1/2-26 hour methylated gomologa - 62-104 hours Excreted in the same degree (45%) with urine and faeces, and from 12 to 14% in an unmodified form.

Indications

Depression, обсессивно-компульси��ные disorder.

Contraindications

Hypersensitivity, the children's ages, breast-feeding (at the end of treatment).

Side-Effects

Violation of consciousness ataxy, discoordination hyper and parestesia, giperkineza, hypothesis and diskinesia, Generalized convulsions, migraine, midriaz, movement, dizziness, ptos, giporeflexia, insomnia, aggressiveness, amnesia, apathy, depersonalization, emotional lability, euphoria, hallucinations, paranoid reactions somnambulism, the syndrome of "lifting", headache, arterial hypertension or hypotension, tachycardia, the kollaptoidnye, oedema (including periorbitale) bronhospazm, cough, despnoe, disfagia, irritation of mucous membrane digestion, gipersalivacia, glossit, Denmark gums, Ulcerative disease, arthralgia, dismenorea increasing pain and thoracic glands, anaemia, limfoadenopatia, dizuria, allergic reactions.

Patient interaction

The joint appointment with MAO inhibitors is gipertermiu, mioclonus, irritability, ajitatia violation consciousness deliri, rolling into a coma. Is cumulation (blocking biotransformatia) H_1-blokatorov (astemizol, terfenadin, cizaprid) with elongation QT interval and the eventual fatal arrhythmias jeludockovh type pirouette. " Increases the level of plasma free fraction (excluding from the protein) H_2-blokatorov, tricyclic antidepressants, derivatives sulfanilmocevina, anxiety, racumin, digoxin.

Overdosing

Symptoms : mood, anxiety, nausea, vomiting, tachycardia, changes Ekg.lechenie : activated carbon washed stomach, big diurez, maintaining vital functions.

Precautions

If the patient takes drugs other groups (MAO inhibitors, imipramine), the sertralin may be nominated only two weeks after the sanctions have been lifted.

Dosing and Administration

Inside, in the 50 mg once a day, morning or evening; In the absence of effective dose gradually (within 8 weeks) increased to a daily maximum of 200 mg per reception.

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