VA Class:CV900
Isoxsuprine is a vasodilating agent.
Isoxsuprine is used as adjunctive therapy in the treatment of peripheral vascular diseases such as arteriosclerosis obliterans, thromboangiitis obliterans (Buerger's disease), and Raynaud's disease, and for the relief of symptoms associated with cerebrovascular insufficiency. The drug is not a substitute for appropriate medical or surgical programs for the treatment of peripheral or cerebral vascular disease. The efficacy of isoxsuprine in the treatment of peripheral or cerebral vascular disease has not been established, and well-controlled clinical studies demonstrating the usefulness of vasodilators, such as isoxsuprine, in the treatment of these disorders are not available.
Isoxsuprine has also been used in the treatment of dysmenorrhea†, threatened abortion†, and premature labor†, but the efficacy of the drug in the treatment of these disorders has not been established.
Isoxsuprine hydrochloride is administered orally.
In the treatment of peripheral vascular and cerebrovascular disorders, the usual adult oral dosage of isoxsuprine hydrochoride is 10-20 mg administered 3 or 4 times daily.
Adverse effects of isoxsuprine include trembling, nervousness, weakness, dizziness, flushing, transient palpitation, tachycardia, chest pain, hypotension, abdominal distress, nausea, vomiting, intestinal distention, and severe rash.
Precautions and Contraindications
If rash occurs in patients receiving isoxsuprine, the drug should be discontinued. Isoxsuprine should not be administered immediately postpartum or in the presence of arterial bleeding.
Isoxsuprine causes vasodilation by direct relaxation of vascular smooth muscle. Although the drug stimulates β-adrenergic receptors, this action is not essential to its vasodilating effect. Isoxsuprine decreases peripheral resistance, and parenteral administration or large oral doses may decrease blood pressure. In healthy individuals, skeletal muscle blood flow is increased. Cerebral blood flow may increase slightly; cutaneous blood flow is generally unchanged. Isoxsuprine also relaxes uterine smooth muscle. The drug may have positive inotropic and chronotropic effects on the heart and may increase cardiac output. Fetal heart rate increases following IV administration of isoxsuprine hydrochloride to the mother late in pregnancy.
Isoxsuprine hydrochloride is almost completely absorbed from the GI tract. After oral administration of the drug, peak plasma concentrations occur within 1 hour and persist for about 3 hours. Mean plasma half-life of the drug is 1.25 hours. Isoxsuprine crosses the placenta. The drug is partially conjugated in the body and is excreted in urine. Fecal excretion of the drug is negligible.
Isoxsuprine is a vasodilating agent that is structurally related to nylidrin. Isoxsuprine hydrochloride occurs as a white, crystalline powder with a bitter taste and is slightly soluble in water and sparingly soluble in alcohol.
Isoxsuprine hydrochloride tablets should be stored in tight containers at a temperature less than 40°C, preferably between 15-30°C.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Oral | Tablets | 10 mg* | Isoxsuprine Hydrochloride Tablets | |
20 mg* | Isoxsuprine Hydrochloride Tablets |
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name