Phenobarbitone
Class: anticonvulsant – barbiturate
Indications (NB some may be unlicensed): seizure control, status epilepticus, pre-op anxiety, terminal restlessness
Contraindications/cautions: acute intermittent porphyria, severe respiratory depression or pulmonary insufficiency, elderly, renal/hepatic failure
Adverse reactions: common: drowsiness, headache, hypotension, respiratory depression; less common: GI upset, paradoxical excitement, pain, hypocalcaemia,hallucinations
Metabolism/clearance: may be metabolised by metabolising enzyme CYP2C19 mainly in the liver
Interactions:
- increased clinical effect/toxicity of phenobarbitone (due to increased blood concentrations) may occur with some CYP metabolising enzyme inhibitors (see above) e.g. fluconazole, fluoxetine, ketoconazole
- decreased clinical effect/toxicity of phenobarbitone (due to decreased blood concentrations) may occur with some CYP metabolism enzyme inducers (see above) e.g. phenytoin, rifampicin
- decreased clinical effect/toxicity of some drugs (due to decreased blood concentrations of them) may occur with phenobarbitone due to metabolising enzyme induction by phenobarbitone e.g. aprepitant, buspirone, carbamazepine, clonazepam, dexamethasone, diazepam, domperidone, fentanyl, itraconazole, ketoconazole, methadone, midazolam, NSAIDs (e.g. diclofenac), phenytoin, prednisone, quetiapine, triazolam, warfarin
- additive CNS effects with other CNS depressants e.g. benzodiazepines (e.g. lorazepam), phenothiazines (e.g. chlorpromazine), opioids, alcohol
- Refer to PCF8 or NZF for full interactions
| Dosing: | |
|---|---|
| terminal agitation | |
| oral: | 60 to 180 mg per day (not often given orally) |
| subcut: | 600 to 1,200 mg/24 hours – loading dose 200 mg can be given; increase dose in syringe driver progressively over 24 hours if required. Can be given IV or IM |
| rectal: | not available |
Syringe driver: give alone and watch for irritation at injection site
Mechanism of action: depresses activity of all excitable tissue perhaps via GABA
Notes:
- risk of respiratory depression in overdose