Carbamazepine

Chemical name

5H-Дибенз[b,f]азепин-5-ка��боксамид

Gross

C15-H12-N2-O

Characteristics

The white crystalline powder, insoluble in water.

Of drugs

The drugs-protivosudorozhnoe, protevoepilepticescoe, antipsihoticescoe, antidepressant, normotimicescoe, analgezirutee. Does sodium channels giperaktiveh membranes of nerve cells blunts the impact of hate neiromediatornah amino acids (glutamate, aspartata) increases brake (Gamkergicakie) processes, and interaction with the central adenozinovmi receptor. Antimaniakale properties from oppression metabolism and start norarenalina. Protivosudorozhnoe effect is the partial and Generalized pripadkah (grand mal). Effective (especially among children and adolescents) for short symptoms of anxiety and depression, as well as reducing irritability, and aggression (epilepsy). Prevents disease attacks nerve troinicnogo, reduces the severity of clinical manifestations of alcohol abstinence (including initiation, tremor, gait violations), and reduces sudorojnuu activity. In nesharnom diabetes affects diurez and sense Jajda.v blood drawn, albeit slowly, but almost completely; Food is not affected by the speed and extent of absorption. C_max by a single admission standard pill is 12 hours When one or reappointment retard tablets C_max (25% less than the normal tablets) in 24 hours Retardnaya form reduces the daily fluctuations in plasma levels (determined in 1-2 weeks), without changing the minimum value of the equilibrium concentration. Bioavailability to the reception retard tablets at 15% lower than after other dosage forms. Linking blood supply is 70-80%. The spinal fluid and saliva concentrations are directly proportional to neswaznogo protein active substance (20-30%). Penetrates into breast milk (25-60% of the level of plasma), and the placental barrier. Apparent volume of distribution 0,8-1,9 l / kg Biotransformiroetsa in the liver (mainly epoksidnomu ways) with the formation of several metabolites - 10,11-trans-diolovoe derivative and compared with glukuronova acid моногидроксилированн ые derivatives, as well as N-glukuronida. T_1/2-p 25-65, with a long reception, 8-29 hrs (induction as a result of metabolic enzymes); In patients receiving induktora monoxigenazna system (phenytoin, phenobarbital), T_1/2 is 8-10 hours After a single intake of 400 mg 72% of the dose appears kidneys and 28% through the intestine. Urine is 2% unchanged carbamazepina, 1% of the active (10,11-epoksidnyi derivative), and about 30% of other metabolites. Children accelerated excretion (may be required in terms of the weight higher doses). Home protivosudorozhnogo actions ranging from several hours to several days (sometimes up to 1 month). Antinevralgiceski effect is a 72 hour-antimaniakalny after 7-10 days.

Indications

Epilepsy (excluding petit mal), maniakale state prevention маниакально-депресси��ных disorders, alcohol cravings, nevralgia troinicnogo and yazyko-glotocnogo nerves, neiropatia diabetic.

Contraindications

Гиперчувствительност ь (including the tricyclic antidepressants), AV blockade mielosuprescia or acute porphyria in history, pregnancy (I term).

Side-Effects

Vertigo, causing hallucinations, depression, aggressive behaviour, enabling psychosis, headache, diplopia, violations ccomodation, clouded aphykia, eye, conjunctivitis, noise in the ears, change the taste sensations, speech disorders (dizartria, it baffling), abnormal inadvertent movement, peripheral neuritis, parestesia, muscle weakness and symptoms pareza, AV blockade long cardiac insufficiency, or hypermarkets gipotenzia, embolism, kidney dysfunction, intersticialny jade, nausea, vomiting, increased liver enzymes, jaundice, hepatitis, osteomalacia, the violation of sexual moderate lakopenia, B19, human blood, giponatriemia, multiorganne reaction �иперчувствительност�� slow type exfoliativei dermatitis, volchanochnopodobnyy syndrome (skin rash, urticaria, hyperthermia, pain, sore throat, joint pain, weakness), the syndrome of Stevens-Johnson, Laiella, anaphylacticskie reaction.

Patient interaction

Incompatible with MAO inhibitors. Increases gepatotoksicnosti tests. Reduces effects of anticoagulants, protivosudorozhnykh funds (derivatives gidantoina or suktinimida), barbiturates, klonazepama, primidona, valproeva acid. Fenotiazina, pimozid, tioksantena reinforce oppression CNS (reduced sudorozhny threshold), zimetidin, klaritromicin, diltiazem, verapamil, erythromycin, propoksifen lower metabolism (increased risk of toxicity). Reduced activity Corticosteroids, estrogen and estrogensoderjath oral contraceptives, hinidina, cardiac glycosides (induction metabolism). While carboangidraza inhibitors, the risk of surgery.

Overdosing

Symptoms : disorientation, drowsiness, and the initiation, hallucinations and coma, the fog, dizartria, movement, ataxy, diskinesia, giper-/giporeflexia, convulsions, mioclonus, hypothermia; Respiratory depression, swelling light; Tachycardia, gipo-/gipertenzia, cardiac arrest, with the loss of consciousness; Vomiting, eye drop large bowel; Delay fluid oligouria or anuria, changing laboratory indicators : giponatriemia possible metabolic acidosis, giperglikemia, increasing muscle factions Kreatininfosfokinaza.lechenie : induction vomiting or stomach wash, the appointment of activated carbon and salt slabitelnogo, diurez bang. To maintain the road respiratory tract-tracheal intubation, and artificial respiration and (or) use of oxygen. Hypotension or shock-plazmozameniteli, dofamin or dobutamin, with the emergence of convulsing-introduction of benzodiazepines (diazepam), or other means protivosudorozhnykh (children may increase respiratory depression in the giponatriemii to restrict fluid prudent in / in cefuroxim izotoniceski solution of sodium chloride. The combination of heavy poisoning with renal insufficiency shows kidney dialysis. The specific antidote is not available. It is anticipated re increase exposure overdose on the second and third day after its inception, because of the slow state of preparation.

Precautions

Before and during the therapy recommended regular blood tests (cell elements), and urine, control functions of the liver. Be wary designate when a history of heart disease, liver and kidney, and blood violations vnutriglaznom increased pressure psihozah delayed, inadequate response to external stimuli, anxiety, diseases characterized by convulsions, mixed in old age, drivers of vehicles and persons operating mechanisms. Do not suddenly stop treatment. Women are encouraged to receive additional folic acid (prior to the onset of pregnancy or during her); With the aim of preventing bleeding increased in the last week of pregnancy and in newborns may use vitamin K.

Dosing and Administration

Inside, adults, 100-1600 mg / day (depending on the evidence and extent illness), children between 10 and 20 mg / kg / day in a few receptions.

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