COMPOSITION

Fap-Plus TM : Each tablet contains Paracetamol BP 500 mg & caffeine BP 65 mg.

PHARMACOLOGICAL INFORMATION

Pharmacological action

Paracetamol is a peripherally acting analgesic and is well absorbed orally. Paracetamol also have antipyretic activity.

Mechanism of action

Paracetamol is a peripherally acting analgesic. Paracetamol produces analgesia by elevation of the pain threshold and antipyresis through action on the hypothalamic heat-regulating center. New cyclooxygenase enzyme COX -3, found in the brain and spinal cord, is selectively inhibited by Paracetamol, and is distinct from the two already known cyclooxygenase enzymes COX -1 and COX -2. This selective inhibition of the enzyme COX -3 in the brain and spinal cord explains the effectiveness of Paracetamol in relieving pain and reducing fever. Caffeine has significant pharmacological action on Paracetamol. It increases the solubility and transmembrane permeation of Paracetamol. It gives stimulant action on the central nervous system with psychotropic effects and stimulant action on respiration, heart rate, and has a mild diuretic effect.

Pharmacokinetic properties

Absorption:

Paracetamol is absorbed readily and completely from the small intestine after oral administration. Peak plasma Paracetamol concentration occurs within 30 to 120 minutes after oral administration.

Distribution:

It is uniformly distributed throughout most body fluids with an apparent volume of distribution of 1 to 1.2 L/kg. Plasma protein binding is negligible at the usual therapeutic concentrations but increases with increasing concentrations.

Metabolism:

Approximately 90 to 95% of a dose of Paracetamol is metabolized by the hepatic microsomal system. In adults at therapeutic doses, Paracetamol is mainly conjugated with glucuronide (45-55%) or sulphate (20-30%). A minor proportion (less than 20%) is metabolized to catechol derivatives. Paracetamol is metabolized differently by infants and children compared with adults, the sulphate conjugate being predominant.

Elimination:

Paracetamol is excreted in the urine mainly as the glucuronide and sulphate conjugates. Less than 5% is excreted as unchanged paracetamol with 85-90% of the dose being eliminated in the urine within 24 hours of ingestion. The elimination half-life of paracetamol varies from about 1 to 4 hours.

CLINICAL INFORMATION

Indication and uses

It is indicated for the relief of pain and fever such as headache, migraine, neuritis, common colds and flu, sore throat, earache, toothache, backache, rheumatic and muscular pain and neuralgia.

Dosage and Administration

1-2 tablets 4-6 times daily, up to a maximum of 4 gm in 24 hours.

Use in Pregnancy and lactation

Pregnant Woman: Paracetamol crosses the placenta but the drug has been used widely as an analgesic in pregnancy and no adverse fetal effects have been recorded.

Lactating Mother: Paracetamol does appear in breast milk but has not been detected in the urine of breast-fed infant. Breast-feeding is not a contra-indication to paracetamol use.

Side effects

In recommended doses, it is usually free from side effects. However-

This medicine commonly causes drowsiness and dizziness and should not be taken with alcohol.

Other side effects may include:

Nausea

Vomiting

Diarrhea

Drug interaction

Possible drug interactions may occur with:

Other sedating medications

Phenothiazines

Some antidepressant medications.

Anticoagulant agents.

Caution

Avoid alcohol while taking this medicine. Alcohol can increase side effects such as dizziness or drowsiness.

Be cautious when driving or performing other hazardous activities. This medicine can impair judgment.

This medicine may be habit-forming.

Over dose and treatment

In massive over dosage exceeding 10 gm may cause liver damage. Early symptoms may cause pallor, nausea, vomiting and malaise. Overdose should be promptly treated by gastric lavage followed by intravenous N-acetylcysteine or methionine.

Contraindication

Paracetamol is contraindicated in patients with severe renal function impairment and hepatic disease (Viral Hepatitis).Known hypersensitivity to Paracetamol.

PHARMACEUTICAL INFORMATION

Storage conditions

Store in a cool and dry place. Keep away from light and out of children's reach.

Presentation & Packaging

Fap-PlusTM: Each commercial box contains 200 tablets in Alu-PVC blister pack.