| Composition |
GRANDAPEN F.C Tablets contain naratriptan as the hydrochloride, which is a selective 5-hydroxytryptamine 1 receptor subtype agonist.
Each GRANDAPEN 1 F.C Tablet for oral administration contains 1 mg of naratriptan.
Each GRANDAPEN 2.5 F.C Tablet for oral administration contains 2.5 mg of naratriptan |
| Pharmacodynamics properties |
| Naratriptan binds with high affinity to 5-HT 1D and 5-HT 1B receptors and has no significant affinity or pharmacological activity at 5-HT 2-4 receptor subtypes or at adrenergic (alpha) 1, (alpha) 2, or (beta); dopaminergic D1 or D2; muscarinic; or benzodiazepine receptors. |
| Therapeutic indications |
GRANDAPEN Tablets are indicated for the acute treatment of migraine attacks with or without aura in adults. |
| Side effect |
Frequent warm/cold temperature sensations. Infrequent feeling strange and burning/stinging sensation. Infrequent palpitations, increased blood pressure, tachyarrhythmias, and abnormal ECG and syncope. Frequent ear, nose, and throat infections. Infrequent thirst and polydipsia, dehydration, and fluid retention. Frequent photophobia. Infrequent blurred vision.
Frequent hyposalivation and vomiting. Infrequent increased white cells. Rare thrombocytopenia, quantitative red cell or hemoglobin defects, anemia, and purpura. Frequent vertigo. Frequent pressure/heaviness sensations.
Observed During Clinical Practice: These events do not include those already listed in the side effects section above.
Because the reports cite events reported spontaneously from worldwide postmarketing experience, frequency of events and the role of GRANDAPEN in their causation cannot be reliably determined. |
| Warnings and precautions |
WARNINGS:
GRANDAPEN F.C Tablets should only be used where a clear diagnosis of migraine has been established.
It is strongly recommended that 5-HT 1 agonists (including naratriptan) not be given to patients in whom unrecognized CAD is predicted by the presence of risk factors (e.g., hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, or male over 40 years of age) unless a cardiovascular evaluation provides satisfactory clinical evidence that the patient is reasonably free of coronary artery and ischemic myocardial disease or other significant underlying cardiovascular disease.
PRECAUTIONS:
General: Chest discomfort has been reported after administration of 5-HT 1 agonists, including GRANDAPEN F.C Tablets. Because naratriptan may cause coronary artery vasospasm, patients who experience signs or symptoms suggestive of angina following naratriptan should be evaluated for the presence of CAD
Laboratory Tests: No specific laboratory tests are recommended for monitoring patients prior to and/or after treatment with GRANDAPEN F.C Tablets. |
| Contraindication |
GRANDAPEN F.C Tablets should not be given to patients with: history, symptoms, or signs of ischemic cardiac, cerebrovascular, or peripheral vascular syndromes.
In addition, patients with other significant underlying cardiovascular diseases should not receive GRANDAPEN Tablets.
Uncontrolled hypertension. Severe renal impairment (creatinine clearance: <15 mL/min). Severe hepatic impairment. Hemiplegic or basilar migraine.
GRANDAPEN F.C Tablets should not be used within 24 hours of treatment with another 5-HT 1 agonist, an ergotamine-containing or ergot-type medication like dihydroergotamine or methysergide.
GRANDAPEN F.C Tablets are contraindicated in patients with hypersensitivity to naratriptan or any of the components. |
| Pregnancy and lactation |
Pregnancy: Pregnancy Category C.
There are no adequate and well-controlled studies in pregnant women; therefore, naratriptan should be used during pregnancy only if the potential benefit justifies the potential risk to the
fetus.
Caution should be exercised when considering the administration of GRANDAPEN F.C.Tablets to a nursing woman.
Pediatric Use: Safety and effectiveness of GRANDAPEN Tablets in pediatric patients (less than 18 years of age) have not been established.
Geriatric Use: The use of naratriptan in elderly patients is not recommended. |
| Drug interactions |
From population pharmacokinetic analyses, coadministration of naratriptan and fluoxetine, beta-blockers, or tricyclic antidepressants did not affect the clearance of naratriptan.
Naratriptan does not inhibit monoamineoxidase (MAO) enzymes and is a poor inhibitor of P450; metabolic interactions between naratriptan and drugs metabolized by P450 or MAO are therefore unlikely.
Oral contraceptives reduced clearance by 32% and volume of distribution by 22%, resulting in slightly higher concentrations of naratriptan.
Hormone replacement therapy had no effect on pharmacokinetics in older female patients.
Smoking increased the clearance of naratriptan by 30%. |
| DOSAGE & ADMINISTRATION |
In controlled clinical trials, single doses of 1 and 2.5 mg of GRANDAPEN F.C Tablets taken with fluid were effective for the acute treatment of migraines in adults.
A greater proportion of patients had headache response following a 2.5-mg dose than following a 1-mg dose.
If the headache returns or if the patient has only partial response, the dose may be repeated once after 4 hours, for a maximum dose of 5 mg in a 24-hour period.
Renal Impairment: In patients with mild to moderate renal impairment, the maximum daily dose should not exceed 2.5 mg over a 24-hour period and a lower starting dose should be
considered.
Hepatic Impairment: In patients with mild or moderate hepatic impairment, the maximum daily dose should not exceed 2.5 mg over a 24-hour period and a lower starting dose should be considered. |
| Overdose |
A patient who was mildly hypertensive experienced a significant increase in blood pressure after administration of a 10-mg dose starting at 30 minutes.
Blood pressure returned to near baseline by 8 hours after dosing without any pharmacological intervention.
Another subject experienced asymptomatic ischemic ECG changes likely due to coronary artery vasospasm approximately 2 hours following a 7.5-mg oraldose.
The elimination half-life of naratriptan is about 6 hours, and therefore monitoring of patients after overdose with GRANDAPEN Tablets should continue for at least 24 hours or while symptoms or signs persist. There is no specific antidote to naratriptan. Standard supportive treatment should be
applied as required. |
| Package |
| Carton box contains 10 F.C Tablets in blister with insert. |
| Storage |
| Store in cool dry temperature. Keep away from children. |
