Dilantin
Dilantin (Phenytoin)The characteristic
The White crystalline powder. It is practically insoluble in water, we will dissolve in 1 % solutions of caustic alkalis.
Pharmacology
Pharmacological action - antiepileptic, anticonvulsant, antiarrhytmic.
Possesses anticonvulsant activity (without the expressed sedative and somnolent effect), shown at generalised and partial attacks. In high doses breaks coordination of movements. On Central nurvice system (shortens the immovability period in the test of "despair" and reduces a ptosis caused by Reserpinum), antiarrhytmic - activating impact makes on heart (reduces the maximum rate, raises an excitation threshold, slows down conductivity on a ventriculonector). Suppresses vestibular reflexes, reduces implications of some forms of syndrome Minier. Influences active and passive transport of ions of sodium and calcium through cellular and subcellular membranes of nervous cells. Significantly reduces sodium level in a neurone as reduces its entering, blocking facilitates active transport from a cell. Changes calcium-fosfolipidnoe interaction in a cellular membrane and reduces active transport of a potassium and calcium, emission of neuromediator amino acids (a glutamate, aspartate) from the nervous terminations brakes, than provides anticonvulsant effect. Antiarrhythmic activity is realised through depression of the central adrenergic influences on heart, stabilisation of membranes of cardiomyocytes at incrise their permeability for potassium ions.
At intake it is easily soaked up. Rate of absorption is various at different patients. It is bound on 70-90 % to fibers of plasma (at renal insufficiency - 43 %). Freely passes barriers and it is quickly distributed on organs and tissues (including cerebral). Less than 5 % are allocated with urine in not changed kind, other quantity is transformed by enzymes of a liver to inactive metabolites - mainly, glucuronides (are excreted by kidneys); the last are partially allocated with bile. T1/2 in plasma at i.v. introduction - 9-14 h, after peroral reception - 22-28 h. Children (especially in growth) are recommended to prescribe Phenytoinum in a combination to vitamins D and To since development of osteopathies of type of a rachitis is possible, hypocalcemias, disturbances of coagulation of blood. At insufficient effect it is necessary to apply in addition phenobarbital or other antiepileptic preparation. It is used, besides, in resistance cases to carbamazepine at epileptiform neuralgia treatment. Eliminates (50 - 90 %) the supraventricular and ventricular arrhythmias caused by an overdosage of warm glycosides, but it is ineffective at supraventricular arrhythmias of other genesis. The distinct effect becomes perceptible at disturbances of a rhythm during a narcosis, a heart catheterization, after operations on heart i.e. when function of the central structures regulating activity of sympathetic nervous system is broken.
Application: the Epilepsy (the big convulsive attacks), preventive maintenance of a posttraumatic and postneurosurgical epilepsy, ventricular arrhythmias, including at an intoxication the warm glycosides, an epileptiform neuralgia.
Contraindications
Hypersensitivity, disturbance of function of a liver and kidneys, a heart failure, a cachexia, a porphyria.
Restrictions to application: In pregnancy it is prescribed only under vital indications.
Side effects
Giddiness, excitation, a tremor, a nystagmus, a fever, a nausea, vomiting, change of a connecting tissue ( a palmar fibromatosis), dermal allergic reactions (an eruption, an itch); at long application (especially at children) - a dyspepsia, a hyperplasia of gums, osteopathies, a hypocalcemia, a hirsutism.
Interaction: Accelerate a biotransformation phenobarbital and carbamazepine, slow down (can strengthen by-effects) - Isoniazidum and its derivatives, Levomycetinum, Acidum acetylsalicylicum, Teturamum.
Overdosage
At concentration in blood at children more than 20 mg/l probably development of an acute intoxication - a nystagmus, disturbances of mentality, a joint pain; in more serious cases - a bradycardia, a ventricular fibrillation, an atrial flutter, an asystolia and a coma. Treatment symptomatic (the specific antidote is not present).
Way of application and dose
Inside, during time or after meal (in order to avoid a boring of a mucosa of a stomach). The adult - on 1/2-1 tab. 2-3 of time a day, if necessary a daily dose enlarge to 3-4 tab., the maximum daily dose - 8 tab. to Children till 5 years - on 1/4 tab. 2 of time a day, 5-8 years - on 1/4 tab. 3-4 of time a day, is more senior 8 years - on 1/2-1 tab. 2 of time a day.
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