ISOXSUPRINE HCL TABLET

NAME OF THE MEDICINAL PRODUCT

Isoxsuprine HCl Tablet IP 10 mg,

Isoxsuprine HCl  Tablet USP 10 mg,

Isoxsuprine HCl  Tablet USP 20 mg

QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet taken orally contains 10mg Isoxsuprine HCl

PHARMACEUTICAL FORM
White, round Tablet

CLINICAL PARTICULARS

Therapeutic indications
Isoxsuprine belongs to the group of medicines called vasodilators. Vasodilators increase the size of blood vessels. Isoxsuprine is used to treat problems resulting from poor blood circulation.
It may also be used for other conditions as determined by your doctor.
Isoxsuprine is available only with your doctor’s prescription.

Posology and method of administration

Posology

Oral
Peripheral vascular disease
Adult: 10-20 mg 3 or 4 times daily.
Elderly: Initiate with lower doses.
Parenteral
To arrest premature labour
Adult: 200-500 mcg/minute as IV infusion; adjust according to response until control is achieved. Monitor maternal BP and hydration, maternal and foetal heart rates during the infusion. Once labour has been arrested, administer 10 mg every 3-8 hr for several days via IM injections. May continue prophylaxis orally by giving 30-90 mg daily in divided doses.

Food(before/after)
May be taken with or without food. (May be taken w/ meals, milk or antacids to minimise GI discomfort.)

CONTRAINDICATION
The medicalconsiderations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significanc
For use in management of premature labor only:
» Cardiac disorders, especially those associated with arrhythmias, or
» Hyperthyroidism, maternal(isoxsuprine may precipitate arrhythmias or heart failure; occult cardiac disease may be unmasked)e).
» Chorioamnionitis (intrauterine infection) or
» Hemorrhage or
» Intrauterine fetal death or known abnormality(immediate delivery required)
» Eclampsia (toxemia) and severe pre-eclampsia
» Pulmonary hypertension

Risk-benefit should be considered when the following medical problems exist
For all indications:

Bleeding disorders
» Cerebrovascular disease, severe, or
Myocardial infarction, recent, or
» Obliterative coronary artery disease, severe    (a “steal effect” may occur, since isoxsuprine has a greater effect on peripheral than on cerebral and coronary vessels, leading to a further decrease in flow to ischemic areas)

Glaucoma
» Hypotension—for parenteral administration only; intravenous administration not recommended

Sensitivity to isoxsuprine
» Tachycardia—for parenteral administration only; intravenous administration not recommended

For use in management of premature labor only (in addition to the above):

Asthma being treated with beta-adrenergic stimulants and/or steroids
» Diabetes mellitu (may be aggravated)

Hypertension
» Pre-eclampsia, mild to moderate

Patient monitoring
The following may be especially important in patient monitoring (other tests may be warranted in some patients, depending on condition; » = major clinical significance):

For all indications
Blood pressure measurement in lying, sitting, and standing positions (recommended at periodic intervals to detect hypotension in patients receiving isoxsuprine)

For use in premature labor only
» Blood glucose concentrations and
» Fluid and electrolyte status (should be monitored carefully during prolonged intravenous administration, especially in diabetic patients or those receiving adrenocorticoids, potassium-depleting diuretics, or digitalis glycosides)
Fetal heart rate and
Maternal heart rate and blood pressure and
Uterine activity    (should be monitored frequently during intravenous administration)

SPECIAL PRECAUTIONS & WARNINGS

Isoxsuprine may increase the animal’s heart rate, cause changes in blood pressure, and irritate the GI tract. It should therefore be used with caution if conbined with other drugs that affect blood pressure, such as sedatives and anesthetic drugs Because it is a vasodilator, it should not be used in horses that are bleeding, or in mares following foaling.
Isoxsuprine is a prohibited class B drug in FEI-regulated competition, and is often prohibited by other equine associations. It may be detected in the urine for several weeks or months following administration. It is therefore important to check the drug-rules within an animal’s given competitive organization, before administering the drug.
Caution should be exercised in patients with history of bleeding problems, who are taking other medications, any allergy, during pregnancy and breastfeeding.
It may cause dizziness, do not drive a car or operate machinery while taking isoxsuprine HCl 10 MG Oral Tablet.
WARNING:
Avoid excess dosage.

Interaction with other medicinal products and other forms of interaction

The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):
Smoking, tobacco    (concurrent heavy use may interfere with the therapeutic effects of isoxsuprine because nicotine constricts blood vessels)
Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):
With physiology/laboratory test values
Free fatty acids, serum and
Glucose, blood and Insulin,
serum    (concentrations may be transiently increased during intravenous infusion but usually return to pretreatment values within 24 to 72 hours, even with continued infusion)
Potassium, serum    (concentrations may be decreased during intravenous infusion; related to changes in glucose and insulin)

Fertility, pregnancy and lactation

Pregnancy
Isoxsuprine crosses the placenta. Maternal isoxsuprine administration for prevention of premature labor has been associated with tachycardia, hypoglycemia, hypocalcemia, ileus, and hypotension in the neonate. Incidence of toxicity is related directly to neonatal blood concentrations of isoxsuprine, which are affected by both gestational age and the interval between administration of isoxsuprine and delivery (with regard to rate of elimination of the drug).
Breast-feeding
Problems in humans have not been documented..

UNDESIRABLE EFFECTS
On rare occasion oral administration of the drug has been associated in time with the occurrence of hypotension, tachycardia, chest pain, nausea, vomiting, dizziness, abdominal distress, and severe rash. If rash appears, the drug should be discontinued.
Although available evidence suggests a temporal association of these reactions with Isoxsuprine Hydrochloride, a causal relationship can be neither confirmed nor refuted.
Beta Adrenergic receptor stimulants such as Isoxsuprine Hydrocholoride have been used to inhibit preterm labor.
Maternal and fetal tachycardia may occur under such use. Hypocalcemia, hypoglycemia, hypotension and ileus have been reported to occur in infants whose mothers received Isoxsuprine Hydrochloride. Pulmonary edema has been reported in mothers treated with beta stimulants. Isoxsuprine Hydrochloride is neither approved nor recommended for use in the treatment of premature labor
Along with its needed effects, isoxsuprine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor as soon as possible if any of the following side effects occur while taking isoxsuprine:
Rare

  • Chest pain
  • dizziness or faintness (more common for injection)
  • fast heartbeat (more common for injection)
  • shortness of breath
  • skin rash

Some side effects of isoxsuprine may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Less Common

  • Nausea or vomiting (more common for injection)

Pharmacological properties

Pharmacodynamic properties

Molecular weight—
337.85
Mechanism of action/Effect:
Vasospastic therapy adjunct and senility symptoms treatment adjunct—Isoxsuprine produces peripheral vasodilation by a direct effect on vascular smooth muscle, primarily within skeletal muscle with little effect on cutaneous blood flow. Its effects were once thought to be due to beta-adrenergic receptor stimulation but are not reversed by beta-adrenergic blocking agents.
Labor (premature) inhibitor and antidysmenorrheal—Isoxsuprine produces uterine relaxation through a direct effect on smooth muscles

Other actions/effects:
Isoxsuprine-induced cardiac stimulation leads to increases in heart rate and cardiac output.
Isoxsuprine-induced peripheral vasodilation leads to decreased peripheral vascular resistance.

 Pharmacokinetic properties

Absorption:
Isoxsuprine is well absorbed from the gastrointestinal tract.

Biotransformation:
Partially conjugated in the blood.

Half-life:
Adults:
Approximately 1.25 hours.

Neonates (following maternal administration [to inhibit premature labor]):
Near term: 1.5 to 3 hours.
Less mature: 6 to 8 hours.

Onset of action:
Oral—1 hour.
Intravenous— 10 minutes.

Elimination:
Primarily in the urine; fecal excretion insignificant.

Preclinical safety data
No data available

Pharmaceutical particulars

List of excipients
Corn starch
Lactose monohydrate
Magnesium stearate (vegetable) Microcrystalline cellulose

 Incompatibilities
Not applicable.

.Special precautions for storage
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Nature and contents of container

Isoxsuprine HCl tablets, USP 10 mg Bottles of 100 NDC 42582-100-10 Isoxsuprine HCl tablets, USP 20 mg Bottles of 1000 NDC 42582-200-20 Isoxsuprine HCl tablets, USP 20 mg Bottles of 100 NDC 42582-200-10

 Special precautions for disposal and other handling

No special requirements.

MARKETING AUTHORISATION HOLDER

TAJ PHARMA CIS LTD.
Marksistsky lane 6, office 221, Moscow, 109147, Russia

MANUFACTURER:

Manufactured in India by:
TAJ PHARMACEUTICALS LTD,
220, Mahagujarat Ind. Estate,  Moraiya,

Tal. Sanand , Dist. Ahmedabad,

Gujarat, INDIA.

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