Bambuterol
Bambuterol is an oral prodrug of terbutaline, designed for once-daily dosing in asthma. It is slowly hydrolysed to active terbutaline, giving prolonged bronchodilation from a single tablet. It also inhibits plasma cholinesterase, which is a clinically relevant interaction. It has no established physique or fat-loss use.
01 Overview
Bambuterol is a bis-dimethylcarbamate prodrug of terbutaline. After oral dosing it is slowly and partly enzymatically hydrolysed to terbutaline, producing sustained beta-2 agonist activity that allows convenient once-daily bedtime dosing, particularly useful for nocturnal asthma symptoms.
A distinctive feature is that bambuterol inhibits plasma (butyrylcholinesterase) activity, which prolongs the action of drugs metabolised by that enzyme, notably the muscle relaxant suxamethonium (succinylcholine) used in anaesthesia. Its side-effect profile is that of terbutaline: tremor, palpitations and the usual beta-2 effects. It is not used as a cutting agent; its slow-release pharmacology and cardiovascular effects offer no physique advantage.
02 Mechanism
Oral prodrug slowly hydrolysed to the selective beta-2 agonist terbutaline, giving prolonged bronchodilation. Also inhibits plasma butyrylcholinesterase, prolonging the effect of substrates such as suxamethonium.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Maintenance | 10–20 mg/day | Oral | 10 mg once daily at night, increased to 20 mg if needed; single daily dose. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Prolonged bronchodilationSustained relief from a single daily oral dose, useful for nocturnal symptoms. | once-daily | Clinical | |
| Reduced nocturnal symptomsBedtime dosing provides overnight bronchodilator cover. | overnight cover | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Tremor and palpitationsFine tremor, palpitations and headache from the released terbutaline. | Mild | Common | Clinical | |
| Prolonged suxamethonium effectCholinesterase inhibition prolongs the action of suxamethonium, risking extended neuromuscular blockade during anaesthesia. | Moderate | Perioperative | Clinical | |
| TachycardiaRaised heart rate at higher doses. | Moderate | With high doses | Clinical |