Jump to content

Salbutamol: Difference between revisions

From Wikipedia, the free encyclopedia
Browse history interactively
← Previous editNext edit →
Content deleted Content added
VisualWikitext
Whosasking (talk | contribs)
2,243 edits
removed essentially unsourced "additional drawbacks of HFA" paragraph. 3rd party sources and it stays.
No edit summary
Line 34: Line 34:
[[Image:Ventolin CFC.JPG|thumb|Ventolin HFA inhaler made by GSK]]
[[Image:Ventolin CFC.JPG|thumb|Ventolin HFA inhaler made by GSK]]
[[Image:Cipla inhaler.jpg|thumb|Asthalin HFA inhaler made by Cipla (India)]]
[[Image:Cipla inhaler.jpg|thumb|Asthalin HFA inhaler made by Cipla (India)]]
'''Salbutamol''' ([[International Nonproprietary Name|INN]]) or '''albuterol''' ([[United States Adopted Name|USAN]]) is a short-acting [[beta2-adrenergic receptor agonist|β<sub>2</sub>-adrenergic receptor agonist]] used for the relief of [[bronchospasm]] in conditions such as [[asthma]] and [[chronic obstructive pulmonary disease]]. It is marketed by [[GlaxoSmithKline]] as '''Ventolin''', '''Aerolin''' or '''Ventorlin''' depending on the market; by [[Cipla]] as '''Asthalin'''; by [[Schering-Plough]] as '''Proventil''' and by [[Teva Pharmaceutical Industries|Teva]] as '''ProAir'''. [[generic drug|Generic]] names are currently not available in the U.S. because of a federal ban on the use of [[CFCs]].<ref>{{cite web| url=http://www.sciam.com/article.cfm?id=unlikely-victims-of-banning-cfcs | title=Unlikely Victims of Banning CFCs--Asthma Sufferers | publisher=Scientific American | date = August 2008 | author=Emily Harrison}}</ref>
'''Salbutamol''' ([[International Nonproprietary Name|INN]]) or '''albuterol''' ([[United States Adopted Name|USAN]]) is a short-acting [[beta2-adrenergic receptor agonist|β<sub>2</sub>-adrenergic receptor agonist]] used for the relief of [[bronchospasm]] in conditions such as [[asthma]] and [[chronic obstructive pulmonary disease]]. Allen & Hanburys launched the first selective Β2-receptor agonist, Ventolin (ie [[salbutamol]]), in 1968. The drug was an instant success, and has been used for the treatment of asthma ever since. <ref>The Pharmaceutical Journal Vol 279 No 7473 p404-405. http://www.pharmj.com/Editorial/20071013/articles/p404ventolin.html</ref> It is now marketed by [[GlaxoSmithKline]] as '''Ventolin''', '''Aerolin''' or '''Ventorlin''' depending on the market; by [[Cipla]] as '''Asthalin'''; by [[Schering-Plough]] as '''Proventil''' and by [[Teva Pharmaceutical Industries|Teva]] as '''ProAir'''. [[generic drug|Generic]] names are currently not available in the U.S. because of a federal ban on the use of [[CFCs]].<ref>{{cite web| url=http://www.sciam.com/article.cfm?id=unlikely-victims-of-banning-cfcs | title=Unlikely Victims of Banning CFCs--Asthma Sufferers | publisher=Scientific American | date = August 2008 | author=Emily Harrison}}</ref>


'''Salbutamol sulfate''' is usually given by the inhaled route for direct effect on bronchial smooth muscle. This is usually achieved through a [[metered dose inhaler]] (MDI), [[nebuliser]] or other proprietary delivery devices (e.g. [[Rotahaler]] or [[Autohaler]]). In these forms of delivery, the maximal effect of Salbutamol can take place within five to twenty minutes of dosing, though some relief is immediately seen. Salbutamol can also be given orally as an [[inhalant]] or [[intravenous]]ly.
'''Salbutamol sulfate''' is usually given by the inhaled route for direct effect on bronchial smooth muscle. This is usually achieved through a [[metered dose inhaler]] (MDI), [[nebuliser]] or other proprietary delivery devices (e.g. [[Rotahaler]] or [[Autohaler]]). In these forms of delivery, the maximal effect of Salbutamol can take place within five to twenty minutes of dosing, though some relief is immediately seen. Salbutamol can also be given orally as an [[inhalant]] or [[intravenous]]ly.

Revision as of 22:12, 5 November 2009

Salbutamol
Clinical data
Pregnancy
category
  • AU: A
Routes of
administration		Oral, inhalational, IV
ATC code
Legal status
Legal status
Pharmacokinetic data
MetabolismHepatic
Elimination half-life1.6 hours
ExcretionRenal
Identifiers
  • (RS)-4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
CAS Number
PubChem CID
DrugBank
ChemSpider
ECHA InfoCard100.038.552 Edit this at Wikidata
Chemical and physical data
FormulaC13H21NO3
Molar mass239.311 g·mol−1
3D model (JSmol)
  • C1=C(C(=CC=C1C(CNC(C)(C)C)O)O)CO
  (verify)
Ventolin HFA inhaler made by GSK
Asthalin HFA inhaler made by Cipla (India)

Salbutamol (INN) or albuterol (USAN) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. Allen & Hanburys launched the first selective Β2-receptor agonist, Ventolin (ie salbutamol), in 1968. The drug was an instant success, and has been used for the treatment of asthma ever since. [2] It is now marketed by GlaxoSmithKline as Ventolin, Aerolin or Ventorlin depending on the market; by Cipla as Asthalin; by Schering-Plough as Proventil and by Teva as ProAir. Generic names are currently not available in the U.S. because of a federal ban on the use of CFCs.[3]

Salbutamol sulfate is usually given by the inhaled route for direct effect on bronchial smooth muscle. This is usually achieved through a metered dose inhaler (MDI), nebuliser or other proprietary delivery devices (e.g. Rotahaler or Autohaler). In these forms of delivery, the maximal effect of Salbutamol can take place within five to twenty minutes of dosing, though some relief is immediately seen. Salbutamol can also be given orally as an inhalant or intravenously.

Salbutamol became available in the United Kingdom in 1969 and in the United States in 1980 under the trade name Ventolin.

Clinical use

Salbutamol is specifically indicated in the following conditions:

As a β2-agonist, salbutamol also finds use in obstetrics. Intravenous salbutamol can be used as a tocolytic to relax the uterine smooth muscle to delay premature labour. While preferred over agents such as atosiban and ritodrine, its role has largely been replaced by the calcium-channel blocker nifedipine which is more effective, better tolerated and orally administered.[4]

In an emergency, EMS providers consider the administration of salbutamol when they see active wheezing, bronchospasm and a past diagnosis of asthma. The drug is most often administered through a nebulizer with 6 liters per minute of oxygen. A normal dose is about 1.25 mg in 3 mL of respiratory saline.

Side effects / health consequences

The most common side effects are of fine tremor, nervousness, headache, muscle cramps, dry mouth, and palpitation.[5] Other symptoms may be tachycardia (rapid heart rate), arrhythmias, flushing, myocardial ischaemia, and disturbances of sleep and behaviour.[5] Rarely occurring, but of importance, are allergic reactions of paradoxical bronchospasm, urticaria, angioedema, hypotension, and collapse, whilst high doses may cause hypokalaemia (low potassium levels), especially in patients with renal failure and those on certain diuretics and xanthine derivaties.[5]


Ban of CFC-containing salbutamol inhalers

The U.S. Food & Drug Administration in April 2005 mandated that all (including salbutamol) inhalers containing chlorofluorocarbons (CFCs) will be prohibited in the United States as of 2008-12-31. CFC inhalers had previously been given "essential use" status, exempting it from a CFC-production ban, however in accordance with the Montreal Protocol they will be phased out; in many other countries patients have been transitioned to non-CFC based inhalers using hydrofluoroalkane (HFA) propellant. Pharmaceutical manufacturers are expected to produce adequate supplies of alternative (HFA) inhalers by 2009.[citation needed]

One drawback of this transition to HFA inhalers is that, due to patent restrictions, all HFA salbutamol inhalers are "brand-name" (ProAir, Proventil, and Ventolin). They cost approximately $20 more per inhaler than existing generic CFC salbutamol inhalers. These new formulations are patented. An industry consortium was formed to spread the costs of the FDA safety studies to get propellants such as 134a and 227 approved.[6]

Generic HFA salbutamol inhalers are not expected on the United States market until 2012 due to existing patents.[7]

Salbutamol is widely used, and accounts for anywhere from 78% of all bronchodilator prescriptions in 2005 to 85% in 2008.[8] However, patients in the United States who cannot tolerate the HFA salbutamol inhalers will not have a single salbutamol alternative available to them domestically after December 31, 2008.[9] The FDA did not approve any alternatives to HFA and there are few standard inhaled lung medications in the United States that come in Dry Powder Inhaler (DPI) versions. Noticeably missing is salbutamol in DPI form in the United States, although it is available in most of the rest of the world in salbutamol DPIs.

Diet and bodybuilding use

Salbutamol is taken by some as an alternative to Clenbuterol for purposes of fat burning.[10]

References

  1. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
  2. ^ The Pharmaceutical Journal Vol 279 No 7473 p404-405. http://www.pharmj.com/Editorial/20071013/articles/p404ventolin.html
  3. ^ Emily Harrison (August 2008). "Unlikely Victims of Banning CFCs--Asthma Sufferers". Scientific American.
  4. ^ Rossi S (Ed.) (2004). Australian Medicines Handbook 2004 (AMH). Adelaide: Australian Medicines Handbook. ISBN 0-9578521-4-2.
  5. ^ a b c "3.1.1.1 Selective beta2 agonists -- side effects". British National Formulary (57 ed.). London: BMJ Publishing Group Ltd and Royal Pharmaceutical Society Publishing. 2008. ISBN 0-85369-778-7. {{cite book}}: |access-date= requires |url= (help); Unknown parameter |month= ignored (help)
  6. ^ IPAC - International Pharmaceutical Aerosol Consortium
  7. ^ HFA inhalers replacing generic albuterol inhalers, driving up costs (pharmacist.com)
  8. ^ IMS Health Sales & Prescription data for all inhalers sales and prescriptions (July 2008)
  9. ^ FDA Advises Patients to Switch to HFA-Propelled Albuterol Inhalers Now
  10. ^ Carter WJ, Lynch ME (1994). "Comparison of the effects of salbutamol and clenbuterol on skeletal muscle mass and carcass composition in senescent rats". Metab. Clin. Exp. 43 (9): 1119–25. PMID 7916118. {{cite journal}}: Unknown parameter |month= ignored (help)

Additional notes

  1. Moore NG, Pegg GG, Sillence MN (1994). "Anabolic effects of the beta 2-adrenoceptor agonist salmeterol are dependent on route of administration". Am. J. Physiol. 267 (3 Pt 1): E475–84. PMID 7943228. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  2. Schiffelers SL, Saris WH, Boomsma F, van Baak MA (2001). "beta(1)- and beta(2)-Adrenoceptor-mediated thermogenesis and lipid utilization in obese and lean men". J. Clin. Endocrinol. Metab. 86 (5): 2191–9. doi:10.1210/jc.86.5.2191. PMID 11344226. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  3. van Baak MA, Mayer LH, Kempinski RE, Hartgens F (2000). "Effect of salbutamol on muscle strength and endurance performance in nonasthmatic men". Med Sci Sports Exerc. 32 (7): 1300–6. doi:10.1097/00005768-200007000-00018. PMID 10912897. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  4. Caruso JF, Hamill JL, De Garmo N (2005). "Oral albuterol dosing during the latter stages of a resistance exercise program". J Strength Cond Res. 19 (1): 102–7. doi:10.1519/R-14793.1. PMID 15705021. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  5. Caruso JF, Signorile JF, Perry AC; et al. (1995). "The effects of albuterol and isokinetic exercise on the quadriceps muscle group". Med Sci Sports Exerc. 27 (11): 1471–6. PMID 8587482. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  6. Martineau L, Horan MA, Rothwell NJ, Little RA (1992). "Salbutamol, a beta 2-adrenoceptor agonist, increases skeletal muscle strength in young men". Clin. Sci. 83 (5): 615–21. PMID 1335400. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)S
  7. Desaphy JF, Pierno S, De Luca A, Didonna P, Camerino DC (2003). "Different ability of clenbuterol and salbutamol to block sodium channels predicts their therapeutic use in muscle excitability disorders". Mol. Pharmacol. 63 (3): 659–70. doi:10.1124/mol.63.3.659. PMID 12606775. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  8. Maki KC, Skorodin MS, Jessen JH, Laghi F (1996). "Effects of oral albuterol on serum lipids and carbohydrate metabolism in healthy men". Metab. Clin. Exp. 45 (6): 712–7. PMID 8637445. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
Retrieved from "https://en.wikipedia.org/w/index.php?title=Salbutamol&oldid=324162710"