Trifluoperazine
When ATH:
N05AB06
Characteristic.
Piperazine phenothiazine. Трифлуоперазина гидрохлорид — белый или слегка зеленовато-желтый кристаллический порошок. Hygroscopic. Easily soluble in water, soluble in alcohol, soluble in dilute base, ether, benzene. pK1 3,9; pK2 8,1. pH 5% aqueous 2,2. In the light darkens. Molecular weight 480,43.
Pharmacological action.
Antipsychotic, neuroleptic, antiemetic.
Application.
Psychosis, schizophrenia, hallucinatory and delusional affective state, psychomotor agitation, nausea and vomiting of central origin.
Contraindications.
Hypersensitivity, coma or heavily marked CNS depression (incl. caused deprimiruyuschie PM), heart disease in violation of conductivity and being decompensation, acute blood disease, acute inflammatory liver disease, severe kidney disease, pregnancy, lactation.
Restrictions apply.
CHD, angina, glaucoma, prostatic hyperplasia, epilepsy, Parkinson's disease.
Side effects.
From the nervous system and sensory organs: extrapyramidal disorder, incl. dystonic (including spasms of the neck muscles, floor of the mouth, language, oculogyric crises), pozdnyaya dyskinesia, akinetorigidnye phenomenon, akathisia, tremor, autonomic disorders, drowsiness (in the first days of treatment), insomnia, dizziness, fatigue, muscular weakness, blurred vision.
From the digestive tract: abnormal liver function, dry mouth, anorexia.
Other: agranulocytosis, amenorrhea, unusual secretion of breast milk, allergic skin reactions, neuroleptic malignant syndrome (development is possible on the background of any classical neuroleptics).
Cooperation.
Dampening effect on the central nervous system of alcohol, hypnotics, tranquilizers, and narcotic analgesics.
Dosing and Administration.
/ M, inside. / M (deep), начальная доза — по 1–2 мг каждые 4–6 ч, суточная доза обычно до 6 mg, в редких случаях — до 10 mg. After reliever move on ingestion. Inside (after meal), обычно начальная разовая доза — 1–5 мг, затем ее постепенно увеличивают на 5 mg per day, средняя суточная доза — 15–80 мг (the daily dose is divided into 2-4 reception), максимальная суточная доза — 100–120 мг. When the desired effect optimal dose is maintained for 1-3 months, then reduce them to support (usually 5-20 mg).
Babies 6 and older - for 1 mg 1-2 times a day. In the elderly increase of the dose should be carried out more slowly, starting dose is 50% or less of the recommended.
As an antiemetic: по 1–4 мг в сутки.
Precautions.
Neuromuscular (extrapyramidal) reaction there are a significant number of hospitalized mental patients. They are characterized by restlessness, can be dystonic type, or are similar to Parkinson's.
Depending on the severity of symptoms of extrapyramidal disorders should reduce the dose or cancel the therapy trifluoperazina, and then consider resuming treatment, perhaps, at lower doses. In more severe cases, correction of extrapyramidal symptoms appoint holinoliticheskie antiparkinsonian agents, barbiturates, when dyskinesia can be effective in / with the introduction of caffeine (Caffeine-sodium benzoate). If necessary, carry out appropriate supportive measures, incl. airway, adequate hydration.
Symptoms motor restlessness may include agitation or jitters, insomnia (sometimes) and often disappear spontaneously. Sometimes these symptoms may be similar to the original neurotic or psychotic symptoms. To reduce the severity of symptoms is usually reduce the dose or replace neuroleptic. Do not increase the dose, while the severity of these side effects is reduced. Possibly application holinolitičeskih protivoparkinsoničeskih sredstv, benzodiazepines, propranolol.
Dystonia. Symptoms may include muscle spasms of the neck, sometimes progressing, stiff back muscles, until opisthotonos, spazmofilii, difficulties glotanii, oculogyric crises, tongue protrusion. These symptoms usually decrease within a few days (almost always within 24-48 hours) after stopping the drug. To reduce the symptoms of mild to moderate severity may barbiturates, In more severe cases in adults effectively appointment of anti-PM (excluding levodopa).
Psevdoparkinsonizm. Symptoms may include a mask-like face, tremor, rigidity, shuffling gait, etc..
Pozdnyaya dyskinesia can develop during long-term therapy or after the cancellation trifluoperazina. This syndrome may also develop, although less frequently, after a relatively short period of treatment at low doses. The syndrome may occur in patients of all age groups, but more common in elderly patients, especially in women. The symptoms are stable, а у некоторых больных — необратимыми. The syndrome is characterized by rhythmical involuntary movements of the tongue, bombast etc. Sometimes the symptoms may be accompanied by involuntary movements of extremities, which in rare cases are the only manifestations of tardive dyskinesia. A variant of tardive dyskinesia may be tardive dystonia.
When, If the patient has a hypersensitivity reaction during previous treatment phenothiazines (such as blood dyscrasia, jaundice) can not be administered to a patient phenothiazines, incl. trifluoperazine, except, when the doctor says, that the potential benefit of treatment exceeds potential risk.
In the period of treatment should refrain from activities potentially hazardous activities, using machinery, driving car, tk. trifluoperazine may impair mental and / or physical performance, as well as causing drowsiness (especially in the first few days of treatment).
Trifluoperazina antiemetic effect may mask the signs and symptoms of toxicity, caused by an overdose of other drugs, and also complicate diagnosis of diseases, as an intestinal obstruction, brain tumor, Reye's syndrome.
When prolonged administration of high doses should consider the possibility of cumulative effects with the sudden appearance of severe symptoms from the CNS or vasomotor disturbances.
Like other phenothiazine derivatives, trifluoperazine should be abolished, at least 48 no, before the myelography (not recommended to resume treatment, at least 24 no, after treatment), and should not be used to prevent emesis before this procedure.