Thiethylperazine (Thiaethylperazinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Antiemetic drugs

Included in the formulation
  • Torekan
    pills inwards 
    KRKA, dd, Novo mesto, AO    
  • Torekan
    suppositories rect. 
    KRKA, dd, Novo mesto, AO    
  • Torekan
    solution w / m in / in 
    KRKA, dd, Novo mesto, AO    
    • АТХ:

    R.06.A.D.   Phenothiazine derivatives

    R.06.A.D.03   Thiethylperazine

    Pharmacodynamics:

    Effects on the chemoreceptor trigger zone and the emetic center of the medulla oblongata; competitive blockade of H1-receptors of effector cells, prevention (but not elimination) of effects mediated by histamine. Blockade of m-cholinergic receptors, α-adrenergic receptors.

    Pharmacokinetics:

    Absorption is good. VD - 2,7 l / kg. Biotransformation of the liver. The elimination half-life is 12 hours. Elimination by the kidneys, unchanged - 3%.

    Indications:

    Nausea and vomiting of various etiologies (including surgical procedures and antitumor therapy), dizziness of central and vestibular origin.

    ICD-10

    VIII.H80-H83.H81   Violations of the vestibular function

    XVIII.R10-R19.R11   Nausea and vomiting

    XVIII.R40-R46.R42   Dizziness and dizziness

    Contraindications:

    Hypersensitivity, depression, coma, closed-angle glaucoma (acute attack), hepatic and / or renal failure, arterial hypotension, CNS depression, diseases of the blood and cardiovascular system,A bronchial asthma, a hypertrophy of a prostate, Parkinson's disease and a parkinsonism; pregnancy, breast-feeding, children's age (up to 15 years).

    Carefully:

    Apply with severe liver failure, kidney failure.

    Pregnancy and lactation:

    Adequate and well-controlled studies in humans have not been carried out, but neonates whose mothers took phenothiazines have experienced extrapyramidal disorders and jaundice. Do not apply!

    Category of recommendations FDA is not defined.

    Dosing and Administration:

    Inside or rectally adults and children over 15 years - 6.5 mg 1-3 times / day, in more severe cases, injected w / k, / m or IV in 6.5 mg.

    For the prevention of postoperative vomiting - in / m 6.5 mg for 30 minutes before the end of the operation.

    Side effects:

    From the side digestive system: dry mouth; with prolonged use and hypersensitivity to thiethylperazine - a violation of liver function.

    From the side CNS: dizziness, drowsiness; with prolonged use and hypersensitivity to thiethylperazine - extrapyramidal disorders.

    From the side of cardio-vascular system: arterial hypotension, tachycardia.

    Overdose:

    Children: excitement, anxiety, hallucinations, ataxia, athetosis, convulsions, mydriasis and pupil immobility, hyperemia of the facial skin, hyperthermia, vascular collapse, coma.

    In adults - retardation, depression, coma; then psychomotor agitation, convulsions; rarely - hyperthermia, hyperemia of the skin.

    Treatment is symptomatic. Do not use respiratory analeptics due to the threat of seizures!

    Interaction:

    β-Adrenoblockers - increase (mutually) in plasma concentrations, severe arterial hypotension, arrhythmias, irreversible retinopathy, tardive dyskinesia.

    Analgesics, hypnotics, tranquilizers, antipsychotics, anesthetics, local anesthetics, m-holinoblokatory, hypotensive drugs, other means, depressing breathing - enhancing effects, correction of doses is required.

    Barbiturates - acceleration of elimination and reduction of thiethylperazine activity.

    Bromocriptine - weakening of its action, increasing serum prolactin concentration.

    Hepatotoxic agents - increased hepatotoxicity.

    MAO inhibitors (simultaneous use is not recommended),derivatives of phenothiazine - increased risk of developing arterial hypotension and extrapyramidal disorders.

    Nalbuphine is a pharmaceutical incompatibility.

    Ototoxic agents - enhancement of ototoxicity.

    Derivatives of amphetamine, m-cholinomimetics, anticholinesterase drugs, ephedrine, guanethidine, levodopa, dopamine - weakening of their action.

    Riboflavin - an increase in the dose of riboflavin is necessary.

    Means that suppress appetite - decrease anoreksigennogo effect.

    Tricyclic antidepressants, anticholinergics - enhance m-cholinoblocking activity.

    Quinidine - increased likelihood of cardiodepressive action.

    Epinephrine - blockade of α-adrenergic effect, risk of serious hypotension.

    Ethanol, clonidine, anticonvulsants - increased oppression of the central nervous system.

    Special instructions:

    H1-blocker of the first generation, a representative of the phenothiazines group, has a pronounced m-cholinoblocking effect.

    Instructions
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