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NERVOUS SYSTEM › ANALGESICS › OTHER ANALGESICS AND ANTIPYRETICS › Anilides
phenacetin, combinations with psycholeptics
N02BE73
Forms & Strengths
- Fixed-dose combinations containing phenacetin and psycholeptic agents (e.g., barbiturates, tranquilizers)
- Oral tablets or capsules (historical formulations)
Adult Dosing
- Withdrawn from global markets due to severe toxicity
- Historically utilized for analgesic and sedative combination therapy, dosing varied by regional pharmacopoeia
Pediatric Dosing
- Contraindicated and not recommended in pediatric populations
Indications
- Historically used for the relief of tension headaches and mild to moderate pain accompanied by anxiety or insomnia
- Currently obsolete and withdrawn due to severe nephrotoxicity and carcinogenicity
Mechanism of Action
- Phenacetin acts centrally as an analgesic and antipyretic (via active metabolite paracetamol/acetaminophen)
- Psycholeptic component acts on the central nervous system to provide sedative, hypnotic, or anxiolytic effects
Contraindications
- Known hypersensitivity to phenacetin, paracetamol, or psycholeptics
- Severe hepatic impairment
- Severe renal impairment or nephropathy
- Glucose-6-phosphate dehydrogenase (G6PD) deficiency
- History of analgesic abuse
Adverse Reactions
- Analgesic nephropathy (papillary necrosis, interstitial nephritis)
- Urothelial and renal cell carcinoma
- Methemoglobinemia and hemolytic anemia
- CNS depression, sedation, and dependence (due to psycholeptic component)
- Severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis)
Drug Interactions
- CYP1A2 inducers (e.g., smoking, rifampin) increase the formation of toxic phenacetin metabolites
- Alcohol and other CNS depressants produce additive sedation and respiratory depression
- Hepatotoxic drugs increase the risk of liver damage
Curated Content: Needs Vetting Before Put to Clinical Use