Astemizole

Revision as of 14:39, 8 April 2015 by Kiran Singh (talk | contribs)
(diff) ← Older revision | Latest revision (diff) | Newer revision → (diff)
Jump to navigation Jump to search
Astemizole
Clinical data
Pregnancy
category
  • C (USA)
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • In general: unscheduled
Pharmacokinetic data
Bioavailability?
MetabolismHepatic
Elimination half-life24 hours
ExcretionFecal
Identifiers
CAS Number
PubChem CID
DrugBank
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC28H31FN4O
Molar mass458.571

WikiDoc Resources for Astemizole

Articles

Most recent articles on Astemizole

Most cited articles on Astemizole

Review articles on Astemizole

Articles on Astemizole in N Eng J Med, Lancet, BMJ

Media

Powerpoint slides on Astemizole

Images of Astemizole

Photos of Astemizole

Podcasts & MP3s on Astemizole

Videos on Astemizole

Evidence Based Medicine

Cochrane Collaboration on Astemizole

Bandolier on Astemizole

TRIP on Astemizole

Clinical Trials

Ongoing Trials on Astemizole at Clinical Trials.gov

Trial results on Astemizole

Clinical Trials on Astemizole at Google

Guidelines / Policies / Govt

US National Guidelines Clearinghouse on Astemizole

NICE Guidance on Astemizole

NHS PRODIGY Guidance

FDA on Astemizole

CDC on Astemizole

Books

Books on Astemizole

News

Astemizole in the news

Be alerted to news on Astemizole

News trends on Astemizole

Commentary

Blogs on Astemizole

Definitions

Definitions of Astemizole

Patient Resources / Community

Patient resources on Astemizole

Discussion groups on Astemizole

Patient Handouts on Astemizole

Directions to Hospitals Treating Astemizole

Risk calculators and risk factors for Astemizole

Healthcare Provider Resources

Symptoms of Astemizole

Causes & Risk Factors for Astemizole

Diagnostic studies for Astemizole

Treatment of Astemizole

Continuing Medical Education (CME)

CME Programs on Astemizole

International

Astemizole en Espanol

Astemizole en Francais

Business

Astemizole in the Marketplace

Patents on Astemizole

Experimental / Informatics

List of terms related to Astemizole

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Astemizole (marketed under the brand name Hismanal) is a second generation antihistamine drug which has a long duration of action. Astemizole was discovered by Janssen Pharmaceutica in 1977. It has been withdrawn from the market in most countries because of rare but potentially fatal interactions with CYP3A4 enzyme inhibitors (e.g. erythromycin, grapefruit juice).

Pharmacology

Astemizole is an histamine H1-receptor antagonist. It is structurally similar to terfenadine and haloperidol (a butyrophenone antipsychotic). It has anticholinergic and antipruritic effects.

Astemizole competitively binds to histamine H1-receptor sites in the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. This suppresses the formation of edema and pruritus (caused by histamine).

Astemizole does not cross the blood-brain barrier, and H1 receptor binding is mostly in the peripheral rather than central nervous system (CNS depression is thus minimal). Astemizole may also act on histamine H3 receptors, thereby producing adverse effects.

Astemizole is rapidly absorbed from the gastrointestinal tract; protein binding is around 96%.

Toxicity

Astemizole has an oral LD50 of approximately 2052mg/kg (in mice).

Research

It has been reported that this drug might prevent 97% of the muscle wasting (atrophy) that occurs in immobile, bedridden patients.[1] Testing upon mice showed that it blocked the activity of a protein present in the muscle that is involved in muscle atrophy.[2] Recent studies have also suggested anti-malarial properties of astemizole. However the concerns for the drug's longterm effects on the heart preclude its routine use in humans for this indication.

Astemizole has recently been found to be a potent treatment for malaria. It has a mechanism of action similar to chloroquine but has activity even in chloroquine-resistant parasites.[3]

External links

Footnotes

  1. "Drug 'could stop muscle wasting'". NetDoctor.co.uk. 25 May,2006. Retrieved 2006-05-27. Check date values in: |date= (help)
  2. Wang X, Hockerman GH, Green Iii HW, Babbs CF, Mohammad SI, Gerrard D, Latour MA, London B, Hannon KM, Pond AL (2006). "Merg1a K+ channel induces skeletal muscle atrophy by activating the ubiquitin proteasome pathway". FASEB J. PMID 16723379. Unknown parameter |month= ignored (help)
  3. Chong CR, Chen X, Shi L, Liu JO, Sullivan DJ (2006). "A clinical drug library screen identifies astemizole as an antimalarial agent". Nat Chem Biol. 2: 415&ndash, 16. doi:10.1038/nchembio806. PMID 16816845.