Paracetamol

Paracetamol

Paracetamol (Tylenol, Panadol)

Mechanism of action

Analgesic-antipyretic drug.

Mechanism of action is still not fully understood. 

Like NSAIDs, paracetamol inhibits cyclooxygenase 1 and 2 which results in block of production of prostaglandins, normally involved in the mechanism of pain signalling. Paracetamol does not affect these enzymes in peripheral tissues, which is a reason for its lack of anti-inflammatory effect. 

Antipyretic action is caused by direct effect on heat-regulating center in the brain. 

Indications and dose

Pharmacokinetics

Onset of action

  • Peroral: 37 minutes
  • Intravenous: 8 minutes

Duration of action: 4–6 hours

Half-life of elimination: 1–4 hours

Metabolism: Hepatic 

Elimination: Kidneys (95 % metabolites, 5 % free drug)

Directions for administration

In a case of low reserves of hepatic glutathione (hepatic insufficiency, chronic alcoholism, malnutrition) the maximum daily dose should be reduced to 3000 mg.

Medicinal forms

Pills – 500 mg

Solution for injection/infusion (10 mg/ml)

  • 1 vial = 100 ml (1000 mg)

Many forms and combinations with other analgesics.

Side-effects

Malaise

Hypotension

Nausea, vomiting

Increased levels of hepatic transaminases, hepatic failure

Renal failure (tubular necrosis)

Thrombocytopenia, Leukopenia, Neutropenia

HAGMA

Reversal

N-acetylcysteine (NAC) is an effective antidote. 

See more in N-acetylcystein page. 

References

  1. Acetaminophen: Uses, Interactions, Mechanism of Action | DrugBank Online
  2. Paracetamol Uses, Dosage, Side Effects, Warnings - Drugs.com
  3. Buccal acetaminophen provides fast analgesia: two randomized clinical trials in healthy volunteers - PMC (nih.gov)
  4. https://www.medicines.org.uk/emc/search?q=paracetamol