Metaradrine
Metaradrine - General Information
An adrenergic agonist that acts predominantly at alpha adrenergic receptors and also stimulates the release of norepinephrine. It has been used primarily as a vasoconstrictor in the treatment of hypotension. [PubChem]
Pharmacology of Metaradrine
Metaradrine is a potent sympathomimetic amine that increases both systolic and diastolic blood pressure. Metaradrine is indicated for prevention and treatment of the acute hypotensive state occurring with spinal anesthesia. It is also indicated as adjunctive treatment of hypotension due to hemorrhage, reactions to medications, surgical complications, and shock associated with brain damage due to trauma or tumor. Metaradrine acts on both α1-adrenergic receptors but appears to have no effect on β-adrenergic receptors. It acts by increasing the force of the heart's pumping action as well as constricting peripheral blood vessels.
Metaradrine for patients
Patient Information:
Metaraminol is for emergency use. A prolonged use may cause perpetuation of the shock state or recurrence of hypotension when the drug is discontinued.
Metaradrine Interactions
ARAMINE should be used with caution in digitalized patients, since the combination of digitalis and sympathomimetic amines may cause ectopic arrhythmias.
Monoamine oxidase inhibitors or tricyclic antidepressants may potentiate the action of sympathomimetic amines. Therefore, when initiating pressor therapy in patients receiving these drugs, the initial dose should be small and given with caution.
Metaradrine Contraindications
Use of ARAMINE with cyclopropane or halothane anesthesia should be avoided, unless clinical circumstances demand such use.
Hypersensitivity to any component of this product, including sulfites.
Additional information about Metaradrine
Metaradrine Indication: For the treatment and prevention of hypotension due to hemorrhage, spinal anesthesia, and shock associated with brain damage
Mechanism Of Action: Metaradrine acts through peripheral vasoconstriction by acting as a pure alpha-1 adrenergic receptor agonist, consequently increasing systemic blood pressure (both systolic & diastolic). Its effect is thought to be associated with the inhibition of adenyl cyclase which leads to an inhibition of the production of cAMP.Another effect of Metaradrine is that it releases norepinephrine from its storage sites indirectly.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Metaraminol
Synonyms: Metaraminolum [Latin]; Metaraminolum [Inn-Latin]; Metaraminol Bitartrate; M-Hydroxypropadrine; M-Hydroxyphenylpropanolamine; M-Hydroxy Norephedrine; L-Metaraminol; Hydroxynorephedrine
Drug Category: Adrenergic Agents; Adrenergic alpha-Agonists; Sympathomimetics; Vasoconstrictor Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Metaraminol: Aramine; Icoral B; Metaradrine; Pressonex; Pressorol;
Absorption: The effect starts 1-2 min after IV injection, 10 min after IM injection, 5-20 min after subcutaneous injection.
Toxicity (Overdose): LD50=240 mg/kg (rat, oral); LD50=99 mg/kg (mouse, oral)
Protein Binding: Approximately 45%
Biotransformation: Hepatic
Half Life: Not Available
Dosage Forms of Metaradrine: Injection, solution Intramuscular
Injection, solution Subcutaneous
Injection, solution Intravenous drip
Chemical IUPAC Name: 3-[(1R,2S)-2-amino-1-hydroxypropyl]phenol
Chemical Formula: C9H13NO2
Metaraminol on Wikipedia: https://en.wikipedia.org/wiki/Metaraminol
Organisms Affected: Humans and other mammals