DR. DOPING

Instructions

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Instructions / Instruction for use: Naratriptan

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The Latin name of the substance Naratriptan

Naratriptanum (genus. Naratriptani)

Chemical name

N-Methyl-3- (1-methyl-4-piperidinyl) -1H-indole-5-ethanesulfonamide (as monohydrochloride)

Gross formula

C17H25N3O2S

Pharmacological group

Serotonergic agents

The nosological classification (ICD-10)

G43 Migraine: The pain of migraine; Migraine; hemiplegic migraine; Migraine headache; A migraine attack; Continuous headache; hemicranias

G43.0 Migraine without aura [simple migraine]: Migraine without aura

G43.1 Migraine with aura [classic migraine]: Basilar migraine; Migraine with aura

CAS Code

121679-13-8

Characteristics of substance Naratriptan

Naratriptan hydrochloride is a powder from white to pale yellow, easily soluble in water. Molecular weight 371.93.

Pharmacology

Pharmacological action - antimigraine.

Highly selective stimulates 5-HT1B / 1D serotonin receptors. Narrows extended during a migraine attack intracranial vessels, inhibits output of neurotransmitters and vasoactive neuropeptides from trigeminal endings (blockade of 5-HT1D-receptor).

Quickly absorbed from the digestive tract. Bioavailability is 63% in men and 74% in women. Time to Cmax (5,4 ng / ml in males and 8.3 ng / ml in females after receiving 2.5 mg) 2-3 hours Volume of Distribution -. 170 l. Binding to plasma proteins does not exceed 30%. Penetrates through GEB. In the liver with the participation of cytochrome P450 forms inactive metabolites. T1 / 2 averages 6 hours. The clearance after IV administration is 470 ml / min in men and 380 ml / min in women. It is excreted mostly with urine in unchanged form (about 50%) and in the form of metabolites. The clearance is reduced by 50% with moderate renal failure and by 30% when the liver function is impaired. Kidney Cl - 220 ml / min.

Quickly (within an hour) and effectively stops migraine attacks. Complete disappearance of pain in the first 4 hours is noted in 60-65% of patients. Effective in menstrual migraines. The effect is dose-dependent, incl. For accompanying migraine nausea, phonopathy and photophobia, optimal results are observed with the intake of 2.5 mg.

Application of substance Naratriptan

Migraine with aura and without aura (relief of seizures), migraine status (as part of complex therapy)

Contraindications

Hypersensitivity, incl. sulfonamide, hemiplegic basilar or oftalmoplegicheskaya form of migraine, ischemic heart disease, myocardial infarction, stroke, peripheral vascular disease syndrome (intermittent claudication), uncontrolled hypertension, renal failure, severe (Cl creatinine less than 15 ml / min), pregnancy, juvenile ( Up to 18 years) and old age.

Application in pregnancy and lactation

The action category for fetus by FDA is C.

Side effects of substance Naratriptan

Paraesthesia, dizziness, drowsiness, weakness, feeling pain, or compression of the compression in the throat and neck, coronary vasospasm, peripheral circulatory disorders, nausea, vomiting.

Interaction

Strengthens the effect of sedatives. Ergotamine and other anti-migraine drugs increase the likelihood of adverse events.

Routes of administration

Inside.

Precautions for substance Naratriptan

In patients with renal and hepatic insufficiency, the daily dose should not exceed 2.5 mg. It is not recommended to use for migraine prevention (except menstrual). Do not use within 24 hours after using other tryptanes or ergotamine and similar preparations. During the treatment period, it is necessary to refrain from managing motor vehicles and working with potentially dangerous mechanisms requiring increased attention and speed of response.