Bambuterol

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Bambuterol
Bambuterol-2D-skeletal.png
Systematic (IUPAC) name
(RS)-5-[2-(tert-butylamino)-1-hydroxyethyl]benzene-1,3-diyl bis(dimethylcarbamate)
Clinical data
AHFS/Drugs.com International Drug Names
Pregnancy cat.
  • Unknown
Legal status
  • Prescription only
Routes Oral
Pharmacokinetic data
Bioavailability 20%
Metabolism Hepatic, extensive
Further metabolized to terbutaline by plasma cholinesterase
Half-life 13 hours (bambuterol)
21 hours (terbutaline)
Excretion Renal
Identifiers
CAS number 81732-46-9 YesY
ATC code R03CC12
PubChem CID 54766
DrugBank DB01408
ChemSpider 49466 YesY
UNII Y1850G1OVC N
KEGG D07377 YesY
ChEBI CHEBI:553827 N
ChEMBL CHEMBL521589 YesY
Chemical data
Formula C18H29N3O5 
Mol. mass 367.44 g/mol
 N (what is this?)  (verify)

Bambuterol is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline. Commercially, the AstraZeneca pharmaceutical company produces and markets bambuterol as Bambec and Oxeol (INN).[1]

Indications[edit]

As other LABAs, bambuterol is used in the long-term management of persistent asthma.[1] It should not be used as a rescue medication for short-term relief of asthma symptoms.

Contraindications[edit]

Bambuterol is contraindicated in pregnancy and in people with seriously impaired liver function. It can be used by people with renal impairment, but dose adjustments are necessary.[1]

Adverse effects[edit]

The adverse effect profile of bambuterol is similar to that of salbutamol, and may include fatigue, nausea, palpitations, headache, dizziness and tremor.[1]

Interactions[edit]

Concomitant administration of bambuterol with corticosteroids, diuretics, and xanthine derivatives (such as theophylline) increases the risk of hypokalemia (decreased levels of potassium in the blood).[2]

Bambuterol acts as a cholinesterase inhibitor, and can prolong the duration of action of suxamethonium (succinylcholine) and other drugs whose breakdown in the body depends on cholinesterase function.[1] Butyrylcholinesterase activity returns to normal approximately two weeks after bambuterol is stopped.[3] It can also enhance the effects of non-depolarizing neuromuscular blockers, such as vecuronium bromide.[2]

References[edit]

  1. ^ a b c d e Sweetman, Sean C., ed. (2009). "Bronchodilators and Anti-asthma Drugs". Martindale: The complete drug reference (36th ed.). London: Pharmaceutical Press. pp. 1115–16. ISBN 978-0-85369-840-1. 
  2. ^ a b Sweetman (2009), pp. 1132–33.
  3. ^ Sitar DS (October 1996). "Clinical pharmacokinetics of bambuterol". Clin Pharmacokinet 31 (4): 246–56. doi:10.2165/00003088-199631040-00002. PMID 8896942.