DRUG STUDY

NAME OF DRUG: Paracetamol (Biogesic)

DOSAGE: Adult : PO 0.5-1 g 4-6 hourly. IV 33-50 kg: 15 mg/kg 4-6 hourly if needed. Max: 3 g/day: >50 kg: 1 g 4-6 hourly if needed. Rectal As supp:
0.5-1 g 4-6 hourly. Max: 4 g daily. Intravenous

Fever, Mild to moderate pain

Adult: 33-50 kg: 15 mg/kg 4-6 hourly if needed. Max: 3 g daily. >50 kg: 1 g 4-6 hourly if needed. Max: 4 g daily. Administer by infusion over 15
minutes.

Child: Full-term neonates and children <10 kg: 7.5 mg/kg as a single dose, at least 4 hourly. Max: 30 mg/kg/day; 10-33 kg: 15 mg/kg as a single
dose, at least 4 hourly. Max: 2 g daily; 33-50 kg: 15 mg/kg as a single dose, at least 4 hourly. Max: 3 g daily; >50 kg: Same as adult dose.

Oral

Post-immunisation pyrexia

Child: 2-3 months 60 mg as a single dose. May give 2nd dose after 4-6 hours if needed. Max: 4 doses daily.

Oral

Fever, Mild to moderate pain

Adult: 0.5-1 g 4-6 hourly. Max: 4 g daily.

Child: 1-2 months 30-60 mg 8 hourly. Max: 60 mg/kg/day; 3-<6 months 60 mg. 6 months to <2 years 120 mg; 2-<4 years 180 mg; 4-<6 years 240
mg; 6-<8 years 240 or 250 mg; 8-<10 years 360 or 375 mg; 10-<12 years 480 or 500 mg; 12-16 years 480 or 750mg. Administer 4-6 hourly if
necessary. Max: 4 doses in 24 hours.

Rectal

Fever, Mild to moderate pain

Adult: As supp: 0.5-1 g 4-6 hourly. Max: 4 g daily.

Child: 3 months to <1 year 60-125 mg; 1-<5 years 125-250 mg: 5-<12 years 250-500 mg; 12-17 years 500 mg. Given 4-6 hourly if needed. Max: 4
doses/day.
Rectal
Post-immunisation pyrexia
Child: 2-3 months 60 mg as a single dose. May give 2nd dose after 4-6 hours if needed.
ROUTE: Rectal or Orally administered
PREGNANCY CATEGORY: PO/Rectal: B; IV/Parenteral: C
INDICATION
Mild to moderate pain and fever.
MECHANISM OF ACTION
Description: Paracetamol exhibits
analgesic action by peripheral
blockage of pain impulse
generation. It produces
antipyresis by inhibiting the
hypothalamic heat-regulating
centre. Its weak anti-
inflammatory activity is related
to inhibition of prostaglandin
synthesis in the CNS.
Synonym: acetaminophen.
Onset: Oral: <1 hour. IV: 5-10
minutes (analgesia); within 30
minutes (antipyretic).
Duration: Oral, IV: 4-6 hours
(analgesia). IV: ≥6 hours
(antipyretic).
Pharmacokinetics:
Absorption: Well absorbed after
oral and rectal administration.
Time to peak plasma
concentration: Approx 10-60
minutes (oral); 15 minutes (IV);
approx 2-3 hours (rectal).
ADVERSE REACTION
Significant: Thrombocytopenia,
leucopenia, neutropenia,
pancytopenia,
methaemoglobinaemia,
agranulocytosis, angioedema,
pain and burning sensation at inj
site. Rarely, hypotension and
tachycardia.
Gastrointestinal disorders:
Nausea, vomiting, constipation.
Nervous system disorders:
Headache.
Psychiatric disorders: Insomnia.
Skin and subcutaneous tissue
disorders: Erythema, flushing,
pruritus.
Potentially Fatal: Hepatotoxicity,
acute renal tubular necrosis.
Rarely, hypersensitivity reactions
such as acute generalised
exanthematous pustulosis
(AGEP), Stevens-Johnson
syndrome (SJS), toxic epidermal
necrolysis (TEN).
DRUG TO DRUG INTERACTION
Decreased absorption with
colestyramine. Decreased serum
concentrations with rifampicin
and some anticonvulsants (e.g.
phenytoin, phenobarbital,
carbamazepine, primidone).
Enhances the anticoagulant
effect of warfarin and other
coumarins with prolonged use.
Increased absorption with
metoclopramide and
domperidone. Increased serum
concentration with probenecid.
May increase serum
concentration of
chloramphenicol.
Distribution: Distributed into
most body tissues. Crosses
placenta and enters breast milk.
Plasma protein binding: Approx
10-25%.
Metabolism: Mainly metabolised
in the liver via glucuronic and
sulfuric acid conjugation. N-
acetyl-p-benzoquinone imine
(NAPQI), a minor metabolite
produced by CYP2E1 and CYP3A4,
is further metabolised via
conjugation with glutathione in
the liver and kidneys.
Excretion: Mainly via urine (<5%
as unchanged drug; 60-80% as
glucuronide metabolites and 20-
30% as sulphate metabolites).
Elimination half-life: Approx 1-3
hours.