Promethazine

Indications
 Oral
Allergic conditions
Adult: As hydrochloride: 25 mg at night inreased to 25 mg bid, if needed; alternatively, 10-20 mg bid or tid.
Child: As hydrochloride: 5-10 yr: 10-25 mg daily; 2-5 yr: 5-15 mg daily. Doses are given in 1 or 2 divided doses.
Renal impairment: Dose reduction may be required.
Oral
Nausea and vomiting
Adult: As teoclate: 25 mg at night, may be increased to 50 or 75 mg at night or to 25 mg bid/tid, if needed. Max: 100 mg daily.
Child: As teoclate: 5-10 yr: 12.5-37.5 mg daily.
Renal impairment: Dose reduction may be required.
Oral
Prophylaxis of motion sickness
Adult: As hydrochloride: 20 or 25 mg the night before travelling followed by a similar dose in the morning if needed. As teoclate: 25 mg at night or 25 mg 1-2 hr before travelling. Same doses (for HCI) may also be given via rectal route as suppositories.
Child: As hydrochoride: 5-10 yr: 10 mg; 2-5 yr: 5 mg; doses are given at night before travelling, repeated the following morning if needed. As teoclate: 5-10 yr: 12.5 mg daily starting either on the night before long journeys or 1-2 hr before short journeys. Same doses (for HCI) may also be given via rectal route as suppositories.
Renal impairment: Dose reduction may be required.
Oral
Short-term management of insomnia
Adult: As hydrochloride: 20-50 mg at night.
Child: As hydrochloride: 5-10 yr: 20-25 mg; 2-5 yr; 15-20 mg. Doses are taken at night. May also be given as suppository.
Renal impairment: Dose reduction may be required.
Parenteral
Allergic conditions
Adult: As hydrochloride: 25-50 mg, given via IM or slow IV inj or injected into the tubing of a freely running infusion at a concentration of not >25 mg/ml and infused at a rate of not >25 mg/min. Max dose: 100 mg.
Child: As hydrochloride: 5-10 yr: 6.25-12.5 mg by deep IM inj.
Renal impairment: Dose reduction may be required.
Parenteral
Nausea and vomiting
Adult: As hydrochloride: 12.5-25 mg repeated at intervals of not <4 hr. May be given via deep IM or slow IV inj. Max: 100 mg/24 hr.
Child: As hydrochloride: 5-10 yr: 6.25-12.5 mg by deep IM inj.
Renal impairment: Dose reduction may be required.
Contraindications
 Hypersensitivity, coma, porphyria, cardiac disease, hypokalaemia, intra-arterial or SC inj, neonates and young children, pregnancy, lactation.
Warnings / Precautions
 Elderly, glaucoma, epilepsy, CVS disease, impaired liver function, asthma, urinary retention, prostatic hyperplasia, pyloroduodenal obstruction. May cause drowsiness. For parenteral admin: Drug must be administered carefully and slowly; incorrect admin can lead to severe tissue injury.
Adverse Reactions
 CNS depression, paradoxical excitation in childn, dryness of mouth, blurring of vision, retention of urine, constipation, glaucoma, tachycardia, headache, hypotension, tinnitus.
Overdose Reactions
 May lead to antimuscarinic, extrapyramidal and CNS effects.
Drug Interactions
 Masks ototoxicity of aminoglycoside antibiotics. May enhance the sedative effects of CNS depressants like alcohol, hypnotics, barbiturates and opioids.
Potentially Fatal: Ventricular arrhythmias when used with drugs that prolong QT interval.
See Below for More promethazine Drug Interactions
Lab Interactions
 May interfere with immunological urinary pregnancy tests giving false positive results. Alters intradermal allergen tests flare reponse. Increases serum glucose in glucose tolerance tests.
Mechanism of Actions
 Promethazine, a phenothiazine derivative, blocks postsynaptic dopaminergic receptors in the brain and has a strong α-adrenergic blocking effect. It competitively binds to H1-receptors.
Absorption: Well absorbed (Oral, IM); peak plasma concentrations after 2-3 hr.
Distribution: Widely distributed: Brain, crosses the placenta, enters breast milk. Protein-binding: 76-93%.
Metabolism: Extensive hepatic 1st-pass metabolism; converted to promethazine sulfoxide, N-desmethylpromethazine.
Excretion: Via urine and bile (as metabolites); 5-14 hr (elimination half-life).
Administration
 May be taken with or without food.
ATC Classification
 D04AA10 - promethazine ; Belongs to the class of topical antihistamines used in the treatment of pruritus.
R06AD02 - promethazine ; Belongs to the class of phenothiazine derivatives used as systemic antihistamines.
Available As
  • Promethazine 1.5 mg
  • Promethazine 10 mg
  • Promethazine 2.5 mg
  • Promethazine 25 mg
  • Promethazine 3.6 mg
  • Promethazine 5 mg
  • Promethazine 5.65 mg
  • Promethazine 6.25 mg

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