Paracetamol

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Paracetamol

Introduction: Paracetamol is a widely used over-the-counter analgesic (pain


reliever) and antipyretic (fever reducer).
Mechanism of action: The mechanism by which paracetamol reduces fever and
pain is debated largely because paracetamol reduces the production of
prostaglandins (pro-inflammatory chemicals). Aspirin also inhibits the production
of prostaglandins, but, unlike aspirin, paracetamol has little anti-inflammatory
action. Likewise, whereas aspirin inhibits the production of the pro-clotting
chemicals thromboxanes, paracetamol does not. Aspirin is known to inhibit the
cyclooxygenase (COX) family of enzymes, and, because of paracetamol's partial
similarity of aspirin's action, much research has focused on whether paracetamol
also inhibits COX. It is now clear that paracetamol acts via at least two
pathways.The COX family of enzymes are responsible for the metabolism of
arachidonic acid to prostaglandin H2, an unstable molecule, which is, in turn,
converted to numerous other pro-inflammatory compounds. Classical antinflammatories, such as the NSAIDs, block this step. Only when appropriately
oxidized is the COX enzyme highly active. Paracetamol reduces the oxidized
form of the COX enzyme, preventing it from forming pro-inflammatory chemicals.

Pharmacology:
Bioavailability Peak
Plasma
plasma level half-life
constant 80% 40 to
minutes

Active
metabolites

60 2 to 3 hours none

Elimination
predominantly
extrarenal

Indications: Paracetamol has good analgesic and antipyretic properties. It is


suitable for the treatment of pains of all kinds (headaches, dental pain,
postoperative pain, pain in connection with colds, post-traumatic muscle pain).
Migraine headaches, dysmenorrhea and joint pain can also be influenced
advantageously. In cancer patients, paracetamol is used for mild pain or it can be
administered in combination with opioids (e.g. codeine).
Dosage:
Usual adult and adolescent dose
Analgesic and Antipyretic: Oral, 325 to 500 mg every three hours, 325 to 650 mg
every four hours, 650 mg to 1 gram every six hours as needed, or 1300 mg every
8 hours, while symptoms persist
Usual pediatric dose
Analgesic and Antipyretic: Oral, 1.5 grams per square meter of body surface a
day in divided doses; or for

Infants up to 3 months of ageOral, 40 mg every four hours as needed.


Infants 4 to 12 months of ageOral, 80 mg every four hours as needed.
Children 1 to 2 years of ageOral, 120 mg every four hours as needed.
Children 2 to 4 years of ageOral, 160 mg every four hours as needed, while
symptoms persist.
Children 4 to 6 years of ageOral, 240 mg every four hours as needed, while
symptoms persist.
Children 6 to 9 years of ageOral, 320 mg every four hours as needed, while
symptoms persist.
Children 9 to 11 years of ageOral, 320 to 400 mg every four hours as needed,
while symptoms persist.
Children 11 to 12 years of ageOral, 320 to 480 mg every four hours as needed,
while symptoms persist.
Side effects: Medicines and their possible side effects can affect individual
people in different ways. The following are some of the side effects that are
known to be associated with this medicine. Because a side effect is stated here,
it does not mean that all people using this medicine will experience that or any
side effect.
Blood disorders
Skin rashes
The side effects listed above may not include all of the side effects reported by
the drug's manufacturer.
Precautions:
Paracetamol should be used with caution in patients with:
impaired hepatic function
impaired renal function
Use in pregnancy: Category A: Paracetamol has been taken by a large number
of pregnant women and women of childbearing age without any proven increase
in the frequency of malformations or other direct or indirect harmful effects on the
foetus having been observed.
Lactation: Paracetamol is excreted in small amounts (< 0.2%) in breast milk.
Maternal ingestion of paracetamol in usual analgesic doses does not appear to
present a risk to the breastfed infants.

Contraindications: Paracetamol should not be used in hypersensitivity to the


preparation and in severe liver diseases.
How supplied: Customized as per request.

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