ISOXSUPRINE HCl

ISOXSUPRINE HCl

10 mg Tablet

5mg/ml (10mg/2ml) Solution for Injection (IM or IV)

DRUG CATERCORY: Tocolytic

BRAND NAME: Duvadilan®

DESCRIPTION

Isoxsuprine is a beta adrenoceptor agonist with selectivity of action for the smooth muscles of the blood vessels, particularly the cerebral vessels and the deeper vessels of the limbs. In higher doses, isoxsuprine has a relaxant action on the smooth muscles of the uterus. Isoxsuprine also has a beneficial effect on blood viscosity.

FORMULATION

Each tablet contains isoxsuprine hydrochloride 10 mg; each solution for injection (IM or IV) contains isoxsuprine hydrochloride 10mg/2ml.

INDICATIONS

1. Circulatory disturbances
   Cerebral vascular insufficiency with a spastic component showing symptoms such as: dizziness, forgetfulness, disorientation, confusion, visual, auditory and speech abnormalities and transient ischemic attacks.
   Peripheral vascular insufficiency with a spastic component showing symptoms such as: coldness and numbness of the limbs, intermittent claudication, color changes, and ischemic ulcers.
2. Uterine hypermotility
   Uncomplicated premature labor.

DOSAGE AND ADMINISTRATION

1. Circulatory disturbance
   Adult Oral Dose: Two tablets (20mg) 3-4 times daily after meals.
   Adult Parenteral Dose: 5-10 mg (1-2 ml) intramuscularly up to three times daily. Intramuscular administration may be used for the initial control of acute or severe symptoms after which treatment should be maintained on oral therapy.
2. Uterine hypemotility
   Suppression of uterine hypermotility can be achieved by intravenous infusion of isoxsuprine (in glucose or saline solution) within a dosage range of between 0.2-0.5 mg per minute.

• Intravenous Infusion: Add the contents of 10 ampules isoxsuprine (equivalent to 100mg) to 500ml of normal saline or dextrose solution. Each ml (20 drops) of this solution will contain approximately 0.2mg of isoxsuprine.
  Recommended infusione Rate: Start with 10 drops/minute (0.5 ml/min) for the first 10 minutes. Gradually increase the rate of infusion by increments of 10 drops/ minute at 10 minute intervals. Dosage adjustment is dependent on response and/or the side effects. Regular monitoring of blood pressure and maternal and fetal heart rates are essential during intravenous infusion therapy. The patient should be maintained in the lateral position during infusion.
  When uterine motility has been controlled during a period of at least 12 hours, the infusion may be stopped and treatment can be maintained on oral therapy of 20mg 3-4 times daily.
• Intramuscular Injection: If intravenous infusion is not feasible, treatment may be started with intramuscular injections of 10mg to be repeated every 3 hours.

ADVERSE EFFECTS

Occasional transient palpitations, fall in blood pressure or dizziness have been noted, particularly with parenteral use. These can be controlled by dosage reduction. A slight increase in the rate of the fetal heart-beat has been noted when isoxsuprine has been given by intravenous infusion in premature labor. Rarely, skin rashes have been associated with its use.

CONTRAINDICATIONS

Isoxsuprine is contraindicated following recent arterial hemorrhage, in patients with known heart disease, or in severe anemia. It should not be administered parenterally to patients with hypotension, tachycardia, premature detachment of the placenta or immediately postpartum.

USE IN PREGNANCY

Animal studies and large-scale clinical applications confirm the absence of any teratogenic effect of isoxsuprine.

OVERDOSAGE

Gross overdosage has not been reported. Should it occur, it is expected that the symptoms would be cardiovascular in nature. Treatment would be gastric lavage, and if necessary, a nonselective beta-blocker may be administered intramuscularly.

STORAGE CONDITION

Isoxsuprine tablets and Isoxsuprine Solution for Injection (IM or IV) should be stored at temperatures not exceeding 25^oC and protected from light.