Orphegesic Forte

White coloured, elongated, biconvex film-coated tablets, scored on one side and plain on the other side.
Each film-coated tablet contains: Paracetamol BP 650 mg, Orphenadrine Citrate BP 35 mg.

Pharmacology: Paracetamol, a para-aminophenol derivative, is a peripherally acting analgesic with antipyretic and weak anti-inflammatory activity. Orphenadrine is a skeletal muscle relaxant and is postulated to act on cerebral motor center or on the medulla through an atropine-like central action. It has anticholinergic, local anaesthetic effects and some antihistaminic effects.
Pharmacodynamics: Mechanism of Action: Orphenadrine is a skeletal muscle relaxant. Paracetamol is an analgesic and antipyretic.
Pharmacokinetics: Paracetamol is readily absorbed from the gastrointestinal tract with peak plasma concentrations occurring about 10 to 60 minutes after oral doses. Paracetamol is distributed into most body tissues. It crosses the placenta and is present in breast milk. Plasma-protein binding is negligible at usual therapeutic concentrations but increases with increasing concentrations. The elimination half-life of Paracetamol varies from about 1 to 3 hours.
Paracetamol is metabolised mainly in the liver and excreted in the urine mainly as the glucuronide and sulfate conjugates. Less than 5% is excreted as unchanged Paracetamol. A minor hydroxylated metabolite (N-acetyl-p-benzoquinoneimine), is usually produced in very small amounts by cytochrome P450 isoenzymes (mainly CYP2E1 and CYP3A4) in the liver and kidney. It is usually detoxified by conjugation with glutathione but may accumulate after Paracetamol overdosage and cause tissue damage.
Orphenadrine is readily absorbed from the gastrointestinal tract. It is almost completely metabolised to at least 8 metabolites. It is mainly excreted in the urine as metabolites and small amount of unchanged drug. The half-life of Orphenadrine has been reported to 14 hours.

Paracetamol has analgesic and antipyretic properties and used for the short-term treatment of moderate pain, particularly after surgery, and for fever.
Orphenadrine is also used as to relieve pain due to skeletal muscle spasm and with the Paracetamol used in the treatment of musculoskeletal and joint disorders.

Usual Oral Dose: Two tablets, three or four times daily.
Or a prescribed by the physician.

Signs and Symptoms: Orphenadrine Overdosage: Known symptoms of overdose with Orphenadrine include tachycardia, excitement, confusion and delirium leading to coma. Convulsions, dilated pupils and urinary retention may occur.
Paracetamol Overdosage: Toxic symptoms following an overdose with paracetamol include vomiting, abdominal pain, hypotension, sweating, central stimulation with exhilaration and convulsions in children, drowsiness, respiratory depression, cyanosis and coma.
In adults, hepatotoxicity may occur after ingestion of a single dose of Paracetamol 10 to 15 g; a dose of 25 g or more is potentially fatal.

Hypersensitivity to the active substance or to any of the excipients.

Paracetamol should be given with care to patients with impaired kidney or liver function. It should also be given with care to patients with alcohol dependence. Caution is advised for patients with impaired kidney or liver function, or in patients with cardiac failure, coronary insufficiency, cardiac arrhythmias and tachycardia.

Pregnancy: Paracetamol + Orphenadrine Citrate is not recommended for use during pregnancy.
Lactation: It is unknown whether Orphenadrine is excreted during lactation. However, it is established that Paracetamol is excreted into the breast milk, one to two hours after oral administration.

Adverse effects of Paracetamol are rare and usually mild, although haematological reactions including thrombocytopenia, leucopenia, pancytopenia, neutropenia, and agranulocytosis have been reported. Skin rashes and other hypersensitivity reactions occur occasionally.
Orphenadrine adverse effects include dryness of mouth with difficulty in swallowing and talking, thirst, reduced bronchial secretions, dilation of the pupils with loss of accommodation and photophobia, flushing and dryness of skin, transient bradycardia followed by tachycardia with palpitation and arrhythmias and difficulty in micturition as well as reduction in the tone and motility of the gastrointestinal tract leading to constipation.

The risk of Paracetamol toxicity may be increased in patients receiving other potentially hepatotoxic drugs or drugs that induce liver microsomal enzymes. The absorption of Paracetamol may be accelerated by drugs such as metoclopramide. Excretion may be affected and plasma concentrations altered when given with probenecid.
Colestyramine reduces the absorption of Paracetamol if given within 1 hour of Paracetamol.
Orphenadrine is an inhibitor of the cytochrome P450 isoenzymes CYP2B6 which is involved in the metabolism of buproprion to its major metabolites, should be used with caution in patients also receiving buproprion.

Store at temperatures not exceeding 30°C.

Analgesics (Non-Opioid) & Antipyretics / Muscle Relaxants

M03BC51 - orphenadrine, combinations ; Belongs to the class of ethers. Used as centrally-acting muscle relaxants.

Rx