Onzetra Xsail (sumatriptan succinate)

Dosage of sumatriptan succinate is expressed in terms of sumatriptan.

Although the effect of renal impairment on the pharmacokinetics of sumatriptan has not been evaluated, little clinical effect would be expected since the drug is largely inactivated metabolically.

The liver plays an important role in the presystemic clearance of orally administered sumatriptan. Accordingly, the bioavailability of sumatriptan following oral administration may be increased markedly in patients with liver disease. (See Pharmacokinetics: Elimination.) If oral sumatriptan therapy is considered in patients with hepatic impairment, the manufacturers state that the maximum single dose generally should not exceed 50 mg. Fixed-combination tablets containing sumatriptan 85 mg and naproxen sodium 500 mg should not be used in patients with hepatic impairment since sumatriptan dosage cannot be appropriately adjusted. Sumatriptan is contraindicated in patients with severe hepatic impairment.

Sumatriptan succinate is administered orally. The drug also can be administered parenterally but only by subcutaneous injection. Sumatriptan also can be administered intranasally. Sumatriptan should not be given IV because of the potential risk of inducing coronary vasospasm. (See Cautions: Precautions and Contraindications.) Sumatriptan has been administered as an iontophoretic transdermal system; however, the manufacturer voluntarily suspended marketing of the formulation because of reports of serious application site reactions. (See Cautions: Local Effects.)

The manufacturer states that tablets containing sumatriptan succinate in fixed combination with naproxen sodium may be administered without regard to meals. The fixed-combination tablets should not be split, crushed, or chewed.

Autoinjection devices are available for subcutaneous administration of sumatriptan to facilitate self-administration of the drug by patients for whom the commercially available doses of 4 or 6 mg are deemed appropriate. An injection pen is available for use with prefilled cartridges labeled as containing 4 or 6 mg of sumatriptan; the needles that accompany this device penetrate approximately 5-6 mm (1/4 inch). In addition, a prefilled, single-use injection pen labeled as containing 6 mg of sumatriptan (also with 1/4-inch projection of the needle following activation of the device) is available. Patients using these devices should be instructed to use injection sites with adequate skin and subcutaneous thickness to accommodate the length of the needle (e.g., lateral thigh, upper arm); care should be taken to avoid IM or IV administration. A prefilled needleless device for subcutaneous administration that is labeled as containing 6 mg of sumatriptan also is available; patients using this device should be instructed to use sites on the abdomen (avoiding the 2-inch area around the umbilicus) or thigh with adequate subcutaneous thickness to accommodate penetration of the injection solution into the subcutaneous space; use of administration sites on the upper arm should be avoided since the delivered dose may be suboptimal. Patients should be given adequate instructions by their clinician, as well as the written instructions supplied with the autoinjection device, before they self-administer sumatriptan injection for the first time.

The patient information provided by the manufacturer should be consulted for directions on intranasal administration of sumatriptan.

Consideration should be given to administering the initial dose of sumatriptan under medical supervision in patients with multiple risk factors for cardiovascular disease (e.g., postmenopausal women, men older than 40 years of age, smokers, patients with hypertension, hypercholesterolemia, obesity, diabetes mellitus, or a family history of coronary artery disease) but who have had a satisfactory cardiovascular evaluation. Electrocardiographic evaluation during the interval immediately after administration of sumatriptan should be considered in these patients since cardiac ischemia can occur in the absence of symptoms.

If a patient does not respond to the first dose of sumatriptan for a given attack, the diagnosis of migraine or cluster headache should be reconfirmed before administration of subsequent doses.

Although sumatriptan generally is effective at whatever stage of a migraine attack it is administered, it is advisable to initiate therapy with the drug as soon as possible after the onset of an attack so that the patient may experience maximum relief.

No dosing information is available for this tab.

No dosing information is available for this tab.

There is no enhanced messaging for this drug.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

There is no enhanced messaging for this drug.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

There are no moderate contraindications for this drug.

There is no enhanced messaging for this drug.

There are no severe adverse reactions for this drug.

There are no less severe adverse reactions for this drug.

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No enhanced messaging available.

There are no adequate and well-controlled studies evaluating the use of sumatriptan in pregnant women. Although a causal relationship to the drug has not been definitely established, agenesis of the corpus callosum has been reported in an infant whose mother received oral sumatriptan at week 4 and 6 of pregnancy. Sumatriptan should be used during pregnancy only if the potential benefit justifies the risk to the fetus.

Sumatriptan has been associated with fetal abnormalities and embryo and fetal mortality in animals. Embryolethality was noted in pregnant rabbits given IV sumatriptan throughout the period of organogenesis in daily doses at or close to those producing maternal toxicity, representing systemic exposures less than the maximum recommended daily subcutaneous dosage in humans of 12 mg (on a mg/m2 basis). The mechanism of the embryolethality is not known. This effect was not seen in pregnant rats given IV sumatriptan throughout organogenesis at dosages representing approximately 10 times the maximum recommended daily subcutaneous human dosage of 12 mg (on a mg/m2 basis) or in pregnant rats given subcutaneous sumatriptan prior to and throughout pregnancy. In pregnant rabbits, oral sumatriptan dosages of 100 mg/kg daily (representing 18 times the maximum single human oral dose of 100 mg on a mg/m2 basis) throughout the period of organogenesis produced embryolethality and maternotoxicity; these effects were not observed at oral sumatriptan dosages of 50 mg/kg daily. No fetal effects were observed in rats receiving 50 mg/kg daily (representing 5 times the maximum single oral human dose of 100 mg on a mg/m2 basis).

Sumatriptan has been shown to be teratogenic in pregnant rats given long-term oral sumatriptan dosages of 500 mg/kg daily (representing 50 times the maximum single human oral dose of 100 mg on a mg/m2 basis); an increased incidence of a syndrome of malformations (short tail/short body and vertebral disorganization) was observed in these animals. Sumatriptan was associated with an increased incidence of cervicothoracic vascular defects and skeletal abnormalities in fetuses of rabbits receiving oral dosages greater than 15 mg/kg daily (representing 3 times the maximum single human oral dose of 100 mg on a mg/m2 basis); these effects were not observed at lower dosages. Blood vessel abnormalities (cervicothoracic and umbilical) occurred in offspring of pregnant rats given oral dosages of 250 mg/kg daily or greater (representing 25 times the maximum single human oral dose of 100 mg on a mg/m2 basis); these effects were not observed at oral dosages of approximately 60 mg/kg daily or less (representing 6 times the maximum single human oral dose of 100 mg on a mg/m2 basis). In a study in rats dosed daily with subcutaneous sumatriptan prior to and throughout pregnancy, there was no evidence of teratogenicity.

Oral sumatriptan produced a decrease in pup survival between birth and postnatal day 4 when administered to pregnant rats at dosages of 250 mg/kg daily or higher (representing 25 times the maximum single human oral dose of 100 mg on a mg/m2 basis) during the period of organogenesis; pups were not affected when dams were given 60 mg/kg daily (representing 6 times the maximum single human dose of 100 mg on a mg/m2 basis). In rats given oral dosages of 1000 mg/kg daily (representing 100 times the maximum single human oral dose of 100 mg on a mg/m2 basis) from gestational day 17 through postnatal day 21, decreased pup survival was found at postnatal days 2, 4, and 20; pups were not affected when dams were given 100 mg/kg of sumatriptan daily.

Sumatriptan is distributed into breast milk following administration of the drug to lactating animals or nursing women. (See Pharmacokinetics: Distribution.) Some manufacturers state that caution is advised when sumatriptan is administered to nursing women. It has been suggested that exposure of the infant to the limited amount of drug distributed into milk following a single 6-mg subcutaneous dose could be minimized by expressing and discarding all milk for 8 hours after the dose. The manufacturers recommend minimizing infant exposure to sumatriptan by avoiding breast-feeding for 12 hours after receiving the drug as oral tablets or nasal spray.

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