ACT-Sumatriptan

Uses

ACT-Sumatriptan Succinate is used for adults for the acute treatment of migraine (with or without aura), and the acute treatment of cluster headache.

ACT-Sumatriptan is also used to associated treatment for these conditions: Acute Migraine, Acute Cluster headaches

How ACT-Sumatriptan works

ACT-Sumatriptan is an agonist of 5-HT_1B and 5-HT_1D. This agonism leads to constriction of cranial blood vessels and inhibits the release of pro-inflammatory neuropeptides. ACT-Sumatriptan decreases carotid arterial blood flow, but increases blood flow velocity in the internal carotid artery and middle cerebral artery.

Dosage

ACT-Sumatriptan dosage

Migraine: 50-100 mg repeated at 2-hr intervals if migraine recurs. Max: 300 mg/24 hr.

Take thismedicationbymouthwith or without food as directed by your doctor, at the first sign of amigraine. The dosage is based on your medical condition and response to treatment. If there is no improvement in your symptoms, do not take more doses of this medication before talking to your doctor. If your symptoms are only partly relieved, or if yourheadachecomes back, you may take another dose at least two hours after the first dose. Do not take more than 200 milligrams in a 24-hour period.

If you are using drugs formigraineattacks on 10 or more days each month, the drugs may actually make yourheadachesworse (medication overuseheadache). Do not usemedicationsmore often or for longer than directed. Tell your doctor if you need to use this medication more often, or if the medication is not working as well, or if yourheadachesget worse.

Side Effects

Transient hypertension, hypotension, dizziness, flushing, fatigue, drowsiness, weakness, seizures, nausea and vomiting, heat, tightness in any part of body, paraesthesia, seizures, inj site reactions, irritation of nasal mucosa and epistaxis. Rebound headache with frequent use.

Toxicity

Symptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation. Overdoses may be fatal and patients should be monitored for 3-5 half lives or while symptoms persist.

Precaution

Conditions predisposing to seizures, presence of coronary risk factors, cardiac arrhythmias, renal or hepatic impairment, elderly, pregnancy, lactation.

Interaction

Concurrent use increased risk of vasospastic reaction with ergotamine and related compounds.

Food Interaction

• Avoid excessive or chronic alcohol consumption. Alcohol increased the risk of GI bleeding, ulcer, and perforation when taken with sumatriptan.
• Take with or without food.

ACT-Sumatriptan Cholesterol interaction

[Major] The group of drugs known as 5-hydroxytryptamine1 receptor (5-HT1) agonists can cause vasospastic reactions, including coronary vasospasm, peripheral vascular ischemia, and colonic ischemia.

Rarely, serious adverse cardiac events including acute myocardial infarction, arrhythmia, cardiac arrest, and death have been reported within a few hours following the administration of 5-HT1 agonists, in some cases even in patients with no prior history or findings of coronary artery disease (CAD).

Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension, as have transient increases in blood pressure and peripheral vascular resistance.

In general, patients with potentially unrecognized CAD as predicted by the presence of risk factors (e.g., hypertension, hypercholesterolemia, tobacco use, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, or male over 40 years of age) should not be administered 5-HT1 agonists unless a cardiovascular evaluation provides satisfactory clinical evidence indicating the lack of CAD, ischemic heart disease, or other significant underlying cardiovascular disease.

As a precaution, the manufacturers recommend that the first dose be administered under medical surveillance in such patients, and that electrocardiographic monitoring be considered during the interval immediately following administration to help detect any asymptomatic cardiac ischemia that may occur.

Periodic cardiovascular evaluations should be performed during intermittent, long-term use.

ACT-Sumatriptan Drug Interaction

Major: duloxetine, cyclobenzaprine, ondansetron, sertralineModerate: acetaminophen / hydrocodoneUnknown: amphetamine / dextroamphetamine, diphenhydramine, omega-3 polyunsaturated fatty acids, fluticasone nasal, pregabalin, albuterol, montelukast, levothyroxine, topiramate, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, alprazolam, cetirizine

ACT-Sumatriptan Disease Interaction

Major: CAD risk factors, cardiovascular disease, liver diseaseModerate: seizure disorders

Volume of Distribution

ACT-Sumatriptan has a volume of distribution of 50±8L for a 6mg subcutaneous dose, or 2.7L/kg.

Elimination Route

A 6mg subcutaneous injection of sumatriptan reaches a C_max of 69.5ng/mL (95% CI of 62.8-76.9ng/mL) with a T_max of 0.17h (95% CI of 0.08-0.33h), an AUC of 9.0h*ng/mL (95% CI of 7.5-10.9h*ng/mL), and a bioavailability of 100%.

A 25mg oral dose of sumatriptan reaches a C_max of 16.5ng/mL (95% CI of 13.5-20.1ng/mL) with a T_max of 1.50h (95% CI of 0.50-2.00h), an AUC of 8.7h*ng/mL (95% CI of 6.1-12.5h*ng/mL), and a bioavailability of 14.3% (95% CI of 11.4-17.9%).

A 20mg intranasal dose of sumatriptan reaches a C_max of 12.9ng/mL (95% CI of 10.5-15.9ng/mL) with a T_max of 1.50h (95% CI of 0.25-3.00h), an AUC of 7.4h*ng/mL (95% CI of 5.0-10.8h*ng/mL), and a bioavailability of 15.8% (95% CI of 12.6-19.8%).

A 25mg rectal dose of sumatriptan reaches a C_max of 22.9ng/mL (95% CI of 18.4-28.6ng/mL) with a T_max of 1.00h (95% CI of 0.75-3.00h), an AUC of 14.6h*ng/mL (95% CI of 11.3-18.8h*ng/mL), and a bioavailability of 19.2% (95% CI of 15.3-24.1%).

Half Life

Subcutaneous sumatriptan has a half life of 1.9h (95% CI of 1.7-2.0h). Oral sumatriptan has a half life of 1.7h (95% CI of 1.4-1.9h). Rectal sumatriptan has a half life of 1.8h (95% CI of 1.6-2.2h). Intrsnasal sumatriptan has a half life of 1.8h (95% CI of 1.7-2.0h).

Clearance

Subcutaneous sumatriptan has a clearance of 0.22L/min (95% CI of 0.19-0.25L/min). Oral sumatriptan has a clearance of 0.17L/min (95% CI of 0.14-0.21L/min). Rectal sumatriptan has a clearance of 0.17L/min (95% CI of 0.14-0.21L/min). Intrsnasal sumatriptan has a clearance of 0.21L/min (95% CI of 0.18-0.25L/min). Total plasma clearance of sumatriptan is approximately 1200mL/min.

Elimination Route

22±4% is excreted in the urine as unchanged sumatriptan and 38±7% in urine as indole acetic acid approximately 40% is excreted in the feces.

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

Not to be used prophylactically and in patients with basilar or hemiplegic or ophthalmoplegic migraine. History of MI or stroke, severe hepatic impairment, ischaemic heart disease, uncontrolled hypertension, peripheral vascular disease, hypersensitivity to sulfonamides.

Innovators Monograph

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