Rizatripan  (Tablets)

COMPOSITION:
Each tablet contains 7.265 or 14.530mg Rizatriptan Benzoate, equivalent to 5 or 10mg Rizatriptan.

MECHANISM OF ACTION:
Rizatripan binds selectively with high affinity to human 5-HT (1B) and 5-HT (1D) receptors, and has little or no effect at 5-HT2 or 5-HT3, adrenergic a1, a2 or b1, b2, dopaminergic D1, D2, histaminic H1, muscarinic, or benzodiazepine receptors.
The therapeutic activity of Rizatripan in treating migraine headache may be attributed to its agonist effects at 5-HT (1B) and 5-HT (1D) receptors on the extra cerebral intracranial blood vessels that become dilated during an attack and on the trigeminal sensory nerves that innervate them. Activation of these 5-HT (1B) and 5-HT (1D) receptors may result in constriction of pain-producing intracranial blood vessels and inhibition of neuropeptide release that leads to decreased inflammation in sensitive tissues and reduced central trigeminal pain signal transmission.

INDICATIONS:
Rizatripan is efficient in the acute treatment of migraine attacks with or without aura, reduction of moderate to severe headache pain to no or mild pain.

DOSAGE:
Generally the drug should not be used prophylactically, and the tablets should be swallowed whole with liquid. The absorption of Rizatripan is delayed by approximately one hour when administered together with food.
Children or pediatric under 18 years of age:
Not recommended.
Adults: 10mg, doses should be separated by at least two hours, no more than 30mg should be taken in any 24-hour period. The safety for treating, on average, more than 40mg in a 30 days period has not been established. After non-response, it’s not effective to use a second dose for treatment of the same attack, if a patient does not respond to the first dose. Clinical studies have shown that patients who do not respond to treatment of an attack are still likely to respond to treatment for subsequent attacks. Some patients should receive the lower dose of Rizatripan 5mg, in particular patients on propranolol, they should be separated by at least two hours between the two drugs, also Patients with mild to moderate renal or hepatic insufficiency.

SIDE EFFECTS:
It may cause dizziness, sleepiness, tiredness, fatigue, pain or pressure sensation (e.g. in the chest or throat), increased blood pressure, cold extremities, muscles weakness, nervousness, tremor, sleep disturbance, dry mouth, thirst, diarrhea or constipation, dyspepsia, sweating, rash, difficult or rapid breathing, swelling of the throat. It may in rare cases cause coronary vasospasm, transit myocardial ischemia, ventricular tachycardia.

CONTRAINDICATIONS:
Hypersensitivity to the drug, prophylaxis treatment, ischemic heart disease, previous myocardial infection, coronary vasospasm including Prinzmetal’s angina, uncontrolled hypertension, peripheral vascular disease.

DRUG INTERACTIONS:
Risk of CNS toxicity with MAOI including moclobemide, avoid the drug for 2 weeks after MAOI. No interactions were observed when the drug was administered with SSRI, however the theoretical possibility in case of concomitant treatment with SSRI cannot be ruled out. Propranolol may increase plasma concentration of the drug, reduce Rizatripan dose. Ergotamine type derivatives increase the risk of vasospasm, avoid ergotamine for 6 hours after RIZATRIPAN.

PRECAUTIONS:

  • The drug should not be used in conditions with predispose to coronary artery disease, hepatic impairment, or renal impairment.
  • The drug should not be taken until 24 hours after stopping an ergotamine type preparation, and it should not to be taken until 6 hours after Rizatriptan.
  • Drowsiness may affect performance of skilled tasks especially driving and use machines.

USE IN PREGNANCY OR LACTATION:
It’s not recommended to use during pregnancy or lactation (category C).

PRESENTATION:
Carton pack contains glass bottle of 6 tablets of 5 or 10mg, with leaflet.

 

 
 
 

© 2010 Domina Pharmaceuticals