Flexital CR

Oxpentifylline.

Each controlled release tablet of Flexital contains Oxpentifylline BP 400 mg.

Pharmacology: Oxpentifylline and its metabolites improve the flow properties of blood. In patients with occlusive arterial disease, oxpentifylline increases blood flow to the affected microcirculation and enhances tissue oxygenation. Oxpentifylline administration has been shown to produce dose-related hemorheologic effects, lowering blood viscosity, and improving erythrocyte flexibility. It also reduces plasma fibrinogen levels and inhibits platelet aggregation. Tissue oxygen levels have been shown to be significantly increased by therapeutic doses of oxpentifylline in patients with peripheral arterial disease.
Pharmacokinetics: On oral administration, oxpentifylline is almost completely absorbed and undergoes first-pass metabolism producing various metabolites which appear in plasma very soon after dosing. Peak plasma levels of the parent compound and its metabolites are reached within 1 hour. The major metabolites are Metabolite 1 (1-[5-hydroxyhexyl]-3,7-dimethylxanthine) and Metabolite V (1-[3-carboxypropyl]-3,-7-dimethylxanthine), and plasma levels of these metabolites are 5 and 8 times greater, respectively, than oxpentifylline.
The apparent plasma half-life of oxpentifylline varies from 0.4 to 0.8 hours and the apparent plasma half-life of its metabolites vary from 1 to 1.6 hours. Excretion is almost totally urinary; essentially no parent drug is found in the urine. Less than 4% of the administered dose is recovered in faeces.
Administration of the 400 mg controlled release Flexital tablet produces plasma levels of the parent compound and its metabolites within 2 to 4 hours which remain constant over an extended period of time. The controlled release of oxpentifylline from the tablet eliminates peaks and troughs in plasma levels and improves gastrointestinal tolerance.

Flexital is indicated for the treatment of chronic occlusive vascular disorders.

The usual dosage of Flexital is one tablet (400 mg) three times a day with meal. The effect of Flexital may be seen within 2 to 4 weeks, to be used only if the expected therapeutic benefit in thought for outweigh very possible risk.
Dosage may be kept at one tablet 2-3 times daily depending on digestive and central nervous system side effects.
Administration of Flexital may be discontinued if side effects persist.

History of previous intolerance to the drug or methylxanthines, such as caffeine, theophylline and theobromine.

General: Oxpentifylline has been used safely for treatment of peripheral arterial disease in patients with concurrent coronary artery and cerebrovascular diseases, but there have been occasional reports of angina, hypotension and arrhythmia. As it is a methylxanthine derivative, it is possible some individuals will experience such responses.
Drug Interactions: There have been reports of bleeding and/or prolonged prothrombin time in patients treated with oxpentifylline with and without anticoagulants or platelet aggregation inhibitors. Patients on anticoagulants should have more frequent monitoring of prothrombin time, while patients with other risk factors complicated by hemorrhage (e.g. recent surgery, peptic ulceration) should have periodic examinations for bleeding including hematocrit and/or hemoglobin.
Periodic systemic blood pressure monitoring is recommended for patients receiving concomitant antihypertensive therapy. If indicated, dosage of the antihypertensive agents should be reduced.
Use in Pregnancy: There are no adequate and well-controlled studies in pregnant women, therefore, Flexital should be used during pregnancy only if benefit outweigh the risk.

Pregnancy: There are no adequate and well-controlled studies in pregnant women, therefore, Flexital should be used during pregnancy only if benefit outweigh the risk.

The adverse effects of Flexital are dose-related and usually involve the gastrointestinal tract. The incidence of nausea and vomiting, the more common side effects, can be reduced by giving Flexital with food.
Adverse effects with Flexital involving the central nervous and cardiovascular systems have been less frequently observed. Dizziness, headache and flushing are more commonly noted. Nervousness, insomnia, drowsiness, anxiety and confusion occur occasionally with Flexital; and palpitations, angina, arrhythmias, hypotension, dyspnea, edema and epistaxis, flu-like syndrome and sore throat, rarely occur.
Malaise, bad taste, excessive salivation, blurred vision, conjunctivitis, scotoma, earache, rash, pruritus, urticaria, brittle finger nails, weight change, swollen glands and nasal congestion can occasionally occur with Flexital; rarely, cholecystitis, hepatitis, jaundice and blood dyscrasias have been reported with oxpentifylline.

Store in a cool dry place, protected from light (preferably between 15°C - 30°C).

Haemorrheologicals

C04AD03 - pentoxifylline ; Belongs to the class of purine derivative agents. Used as peripheral vasodilators.

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