Isoxsuprine

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Isoxsuprine.svg
Systematic (IUPAC) name
4-{1-Hydroxy-2-[(1-methyl-2-phenoxyethyl)amino]propyl}phenol
Clinical data
Pronunciation eye-SOCK-syoo-preen
Trade names Duvadilan, Vasodilan
MedlinePlus a682831
Pregnancy
category
  • US: C (Risk not ruled out)
Legal status
  • ℞ (Prescription only)
Routes of
administration
Oral (tablets)
Pharmacokinetic data
Bioavailability ~100% (humans),[1] 2.2% (horses; oral)[2]
Onset of action 1 hour
Biological half-life <3 hours (horses)[3]
Excretion Mainly renal
Identifiers
CAS Number 395-28-8
ATC code C04AA01 (WHO)
PubChem CID: 3783
DrugBank DB08941
ChemSpider 3651 YesY
UNII R15UI3245N YesY
KEGG D08092 YesY
ChEMBL CHEMBL1197051 N
Chemical data
Formula C18H23NO3
Molecular mass 301.39 g·mol−1

Isoxsuprine (used as isoxsuprine hydrochloride) is a drug used as a vasodilator[4] in humans (under the trade name Duvadilan) and equines. Isoxsuprine is a β2 adrenoreceptor agonist that causes direct relaxation of uterine and vascular smooth muscle via β2 receptors.[5]

Use

In humans

Isoxsuprine it is used in humans for treatment of premature labor, i.e. a tocolytic,[6] and as a vasodilator for the treatment of cerebral vascular insufficiency, Raynaud's phenomenon, and other conditions.[7]

Isoxsuprine may increase the heart rate, cause changes in blood pressure, and irritate the GI tract. It should therefore be used with caution if combined with other drugs that affect blood pressure, such as sedatives and anesthetic drugs.

In horses

Isoxsuprine is most commonly used to treat hoof-related problems in the horse, most commonly for laminitis and navicular disease, as its effects as a vasodilator are thought to increase circulation within the hoof to help counteract the problems associated with these conditions. Isoxsuprine is given orally, and many horses find the pills quite palatable.[8] Isoxsuprine is a prohibited class B drug in FEI-regulated competition, and is often prohibited by other equine associations. It may be detected in the urine for several weeks or months following administration. It is therefore important to check the drug-rules within an animal's given competitive organization, before administering the drug.

Because it is a vasodilator, it should not be used in horses that are bleeding, or in mares following foaling.

References

  1. McGuigan, Michael A.; Whyte, Ian MacGregor; Dawson, Andrew H.; Seifert, Steven A.; Schonwald, Seth; Yip, Luke; Keyes, Daniel C.; Hurlbut, Katherine M.; Erdman, Andrew R.; Dart, Richard C. (2004). "125. Vasodilators". In Dart, Richard C. Medical Toxicology (3rd ed.). Philadelphia [u.a.]: Lippincott Williams & Wilkins. p. 718. ISBN 0781728452.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  2. Erkert, RS; Macallister, CG (April 2002). "Isoxsuprine hydrochloride in the horse: a review". Journal of veterinary pharmacology and therapeutics. 25 (2): 81–7. PMID 12000527.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  3. Cole, Cynthia; Bentz, Bradford; Maxwell, Lara, eds. (2014). "13. Clinical pharmacology of the equine musculoskeletal system". Equine pharmacology. Wiley—Blackwell. p. 224. ISBN 978-0-8138-2262-4.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  4. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).
  5. Falkay, G.; Kovács, L. (1986). "Affinity of tocolytic agents on human placental and myometrial beta-adrenergic receptors". Journal of perinatal medicine. 14 (2): 109–113. PMID 2874205.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  6. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).
  7. Drugs.com: Isoxsuprine
  8. Forney, Barbara C (2007). Equine Medications. Lexington, KY: Blood Horse Publications.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>