Paracetamol

Registered South African indications:

• Relief of pain and fever - mild to moderate
  - When oral therapy is not feasible

Contraindications

South African recommendations & Recommendations in other jurisdictions

• Hypersensitivity to paracetamol or to any of the excipients

Cautions

• Renal impairment
• Hepatic impairment
• Elderly

No specific recommendations have been provided for use in adults

Paed. forms avail. in SA and covered in this monograph: sup

Paed. dosages below include:

• South African Standard Treatment Guidelines indications and dosages
• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

South African Standard Treatment Guidelines indications and dosages

• Click here for the Pain Control (Standard Treatment Guidelines And Essential Medicines List For South Africa, Hospital Level, Paediatrics, 2023 Edition)
• Click here for the Anaesthetics (Standard Treatment Guidelines And Essential Medicines List For South Africa, Hospital Level, Paediatrics, 2023 Edition)
• Click here for the Palliative Care (Standard Treatment Guidelines And Essential Medicines List For South Africa, Hospital Level, Paediatrics, 2023 Edition)

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South African registered indications and dosages

Relief of pain and fever - mild to moderate
- When oral therapy is not feasible

Younger than 6 months and/or <7kg

• Not recommended for use

Between 6 months and ≤2 years, and ≥7kg

125mg

• Rectal (sup): 125mg, up to 6hrly (up to 4 times, dly); Max: 60mg/kg body weight/24hrs

Between 2-8 years

125mg
250mg (if ≥13kg)

• Rectal (sup): 250mg, up to 6hrly (up to 4 times, dly); Max: 60mg/kg body weight/24hrs

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Single dose range: 10-15mg/kg body weight/dose

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The recommended dose should not be exceeded. Dosage should be based on age and weight

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The dosage interval depends on the symptoms and the maximum daily dose, and should be at least 6 hours

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A medical practitioner should be consulted if symptoms persist for more than 3 days

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Paracetamol suppositories should be inserted deeply into the rectum after a bowel movement. They may be warmed up in the hands or dipped for a short time into warm water to improve their sliding properties

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Children and adolescents with low body weight:
The use of paracetamol 125mg suppositories in children under 6 months or weighing less than 7kg
OR
Paracetamol 250mg suppositories in children under 2 years or weighing less than 13kg, is not recommended

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Indications and dosages registered in other jurisdictions

Pain and pyrexia - mild to moderate
- Especially useful in patients unable to take oral forms of paracetamol, e.g. post-operatively or with nausea and vomiting

Younger than 1 year

• Use appropriate strength as available in jurisdiction

Between 1-12 years

• 1 year (10kg): Rectal (sup): 125mg, not to be repeated more frequently than 4hrly (up to max. 4 times dly)
• 5-6 years (20kg): Rectal (sup): 250mg, not to be repeated more frequently than 4hrly (up to max. 4 times dly)
• 12 years (40kg): Rectal (sup): 500mg, not to be repeated more frequently than 4hrly (up to max. 4 times dly)

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The recommended dose should not be exceeded. Higher doses do not produce any increase in analgesic effect. Only whole suppositories should be administered, do not break suppository before administration

Pregnancy

South African recommendations

• Safe; no evidence of risk in studies
• A large amount of data on pregnant women indicate neither malformative, nor foeto/neonatal toxicity
• Epidemiological studies on neurodevelopment in children exposed to paracetamol in utero show inconclusive results
• If clinically needed, paracetamol can be used during pregnancy however it should be used at the lowest effective dose for the shortest possible time, at the lowest possible frequency and not in combination with other medicines

Recommendations in other jurisdictions

• Safe; no evidence of risk in studies
• A large amount of data on pregnant women indicate neither malformative, nor feto/neonatal toxicity
• Epidemiological studies on neurodevelopment in children exposed to paracetamol in utero show inconclusive results
• If clinically needed, paracetamol can be used during pregnancy, however, it should be used at the lowest effective dose for the shortest possible time and at the lowest possible frequency

Breastfeeding

South African recommendations

• Safe; no evidence of risk in studies
• Small amounts of paracetamol are excreted in human milk
• No deleterious effects or adverse reactions during lactation have been observed
• Thus, paracetamol may be given to nursing women in therapeutic doses

Recommendations in other jurisdictions

• Safe; no evidence of risk in studies
• Paracetamol is excreted in breast milk but not in clinically significant amounts
• Available published data do not contraindicate breastfeeding

Renal Impairment

South African recommendations

• Caution; dose adjustment recommended
  Mild: The dose should be reduced and the dosage interval should be increased. Without medical advice, a daily dose of 2g should not be exceeded
  Severe: In the presence of severe kidney failure (GFR≤30ml/min) the dosage interval should be ≥8 hours

Recommendations in other jurisdictions

• Caution; no dose adjustment recommended

Hepatic Impairment

South African recommendations

• Caution; dose adjustment recommended
  The dose should be reduced and the dosage interval should be increased. Without medical advice, a daily dose of 2g should not be exceeded

Recommendations in other jurisdictions

• Caution; dose adjustment recommended
  Lower doses are recommended, avoid prolonged use

Elderly

South African recommendations

• Caution; no dose adjustment recommended

In debilitated, immobilized elderly patients with impaired liver/kidney function

• Caution; dose adjustment recommended
  A dose reduction or prolongation of the dosing interval may be required
  Without medical advice, the maximum daily dose of 60mg/kg body weight (up to a maximum of 2g/day) should not be exceeded in the following cases: body weight <50kg, chronic alcoholism, dehydration and chronic malnutrition

Recommendations in other jurisdictions

• Caution; no information available

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Gastrointestinal Disorders

• Redness of the rectal mucous membranes

Hepatobiliary Disorders

• Hepatic damage
• Hepatic necrosis

Genitourinary Disorders

• Increased creatinine

Skin and Subcutaneous Tissue Disorders

• Exanthema
• Urticaria
• Angioedema

Immune, Blood and Lymphatic System Disorders

• Allergic reaction
• Blood dyscrasias
• Thrombocytopenia 
• Agranulocytosis 

• Agents which induce hepatic microsomal enzymes
• Barbiturates
• Phenobarbital
• Anticonvulsants
• Phenytoin
• Carbamazepine
• Primidone
• Rifampicin
• Oral anticoagulants
• Warfarin
• Coumarins
• Probenecid
• Chloramphenicol

Other interactions

• Alcohol
• St John's Wort

None routine. Specific cases may require

• Renal function
• Hepatic function

The mechanism of analgesic action has not been fully determined. Paracetamol may act predominantly by inhibiting prostaglandin synthesis in the central nervous system (CNS) and, to a lesser extent, through a peripheral action by blocking pain impulse generation. The peripheral action may also be due to inhibition of prostaglandin synthesis or to inhibition of the synthesis or actions of other substances that sensitise pain receptors to mechanical or chemical stimulation. Paracetamol probably produces antipyresis by acting centrally on the hypothalamic heat regulating centre to produce peripheral vaso-dilation resulting in increased blood flow through the skin, sweating and heat loss. The central action probably involves inhibition of prostaglandin synthesis in the hypothalamus.

Suppository 125mg

• Empaped (Litha Pharma) originator

Suppository 250mg

• Empaped (Litha Pharma) originator

Also available in the following forms: Syrup, tablet, capsule, injection and drop.