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Phentolamine



Phentolamine
Systematic (IUPAC) name
3-[4,5-dihydro-1H-imidazol-2-ylmethyl- (4-methylphenyl)-amino]phenol
Identifiers
CAS number 50-60-2
ATC code C04AB01 G04BE05
PubChem 5775
DrugBank APRD00615
Chemical data
Formula C17H19N3O 
Mol. mass 281.352 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life 19 minutes
Excretion  ?
Therapeutic considerations
Pregnancy cat.

C (U.S.)

Legal status
Routes Usually IV or IM

Phentolamine (Regitine) is a reversible nonselective alpha-adrenergic antagonist. Its primary action is vasodilation.[1] The primary application for phentolamine is for the control of hypertensive emergencies, most notably due to phaeochromocytoma (pheochromocytoma).[2] It also has usefulness in the treatment of cocaine induced hypertension, where one would generally avoid beta blockers and where calcium channel blockers are not effective.[3][4] In this context it is probably most safely given by infusion since bolus doses have a propensity towards causing precipitous falls in blood pressure.

Additional recommended knowledge

When given by injection it causes blood vessels to expand, thereby increasing blood flow. When injected into the penis (intracavernosal), it increases blood flow to the penis, which results in an erection.[5]

It may be stored in crash carts to counteract severe peripheral vasoconstriction secondary to extravasation of peripherally placed vasopressor infusions, typically of norepinephrine. Epinephrine infusions are less vasoconstrictive than norepinephrine as they primarily stimulate beta receptor more than alpha receptors, but the effect remains dose dependent.

Phentolamine also has diagnostic and therapeutic roles in complex regional pain syndrome (reflex sympathetic dystrophy).[6]


References

  1. ^ Brock G. Oral phentolamine (Vasomax). Drugs Today (Barcelona). 2000 Feb-Mar;36(2-3):121-4.
  2. ^ Tuncel M, Ram VC. Hypertensive emergencies. Etiology and management. American Journal of Cardiovascular Drugs. 2003;3(1):21-31.
  3. ^ Hollander JE, Henry TD. Evaluation and management of the patient who has cocaine-associated chest pain. Cardiology Clinics. 2006 Feb;24(1):103-14.
  4. ^ Chan GM, Sharma R, Price D, Hoffman RS, Nelson LS. Phentolamine Therapy for Cocaine-Association Acute Coronary Syndrome (CAACS). Journal of Medical Toxicology. 2006 Sep;2(3):108-11.
  5. ^ Bella AJ, Brock GB. Intracavernous pharmacotherapy for erectile dysfunction. Endocrine. 2004 Mar-Apr;23(2-3):149-55.
  6. ^ Rowbotham MC. Pharmacologic management of complex regional pain syndrome. Clinical Journal of Pain. 2006 Jun;22(5):425-9.


 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Phentolamine". A list of authors is available in Wikipedia.
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