Metaraminol

Medical uses

Metaraminol is given intravenously as either a bolus (often 0.5–1 mg doses) or as an infusion, usually via peripheral intravenous access. Metaraminol is commonly available as 10 mg in 1 mL, that requires dilution prior to administration (often made up to a 0.5 mg/mL solution), however pre-prepared syringes of metaraminol for bolus use for hypotension are also commonly available.

Metaraminol is also used in the treatment of priapism.

Pharmacology

Pharmacodynamics

The dominant mechanism of action for the vasopressor action of metaraminol is indirect, with metaraminol displacing norepinephrine from neuronal vesicles in order for the noradrenaline to exert these effects. Metaraminol at higher doses may have direct α-adrenergic agonist and β1-adrenergic agonist effects. However at doses common in clinical practice, the indirect α1-adrenergic effects predominate, such that reflex bradycardia is a common side effect.

Chemistry

Metaraminol, also known as (1R,2S)-3,β-dihydroxy-α-methylphenethylamine or as (1R,2S)-3,β-dihydroxyamphetamine, is a substituted phenethylamine and amphetamine derivative. It is the (1R,2S)-enantiomer of meta-hydroxynorephedrine (3,β-dihydroxyamphetamine). The drug is closely related to phenylpropanolamine ((1RS,2SR)-β-hydroxyamphetamine; norephedrine), ephedrine ((1R,2S)-β-hydroxy-N-methylamphetamine), para-hydroxynorephedrine (4,β-dihydroxyamphetamine), and oxilofrine (4,β-dihydroxy-N-methylamphetamine).

The experimental log P of metaraminol is -0.27 and its predicted log P ranges from -0.59 to 0.07.

Metaraminol is used pharmaceutically as the bitartrate salt.

History

Metaraminol was approved for medical use in the United States in September 1954.

Society and culture

Names

Metaraminol is the generic name of the medication and its and , while its is métaraminol and its is metaraminolo. As the bitartrate salt, its generic name is metaraminol bitartrate and this is its and , while metaraminol tartrate is its . A synonym of metaraminol is metaradrine. Brand names of metaraminol include Aramin, Aramine, and Pressonex, among others.

References

References

1. "Injection : Aramine (Metaraminol Bitartrate)".
2. "Metaraminol Bitartrate Injection, USP".
3. (Aug 2003). "Hemodynamic pharmacology of intravenous vasopressors". Crit Care Nurse.
4. "Aaramine: FDA-Approved Drugs".
5. "Metaraminol 0.5 mg/ml, Solution for Injection in pre-filled syringe - Summary of Product Characteristics (SmPC) - (emc)".
6. (21 August 2020). "Pre-filled emergency drugs: The introduction of pre-filled metaraminol and ephedrine syringes into the main operating theatres of a major metropolitan centre". Australasian Anaesthesia.
7. (2004). "Successful management of stuttering priapism using home self-injections of the alpha-agonist metaraminol.". Int Braz J Urol.
8. (1990). "Post-traumatic priapism treated with metaraminol bitartrate: case report.". J Trauma.
9. (1988). "[Metaraminol in therapy of various forms of priapism]". Urologe A.
10. "Metaraminol". Deranged Physiology.
11. (September 1963). "Studies on the Mechanism of Action of Metaraminol (Aramine)". Annals of Internal Medicine.
12. Elks, J.. (2014). "The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies". Springer US.
13. Schweizerischer Apotheker-Verein. (2000). "Index Nominum 2000: International Drug Directory". Medpharm Scientific Publishers.
14. "Metaraminol".
15. (1 September 2024). "Metaraminol".
16. (June 1955). "Clinical studies on a vasopressor agent: metaraminol (aramine). I. Observations in normotensive subjects". Am J Med Sci.
17. (October 1955). "Clinical studies on a vasopressor agent: metaraminol (aramine). II. Observations on its use in the management of shock". The American Journal of the Medical Sciences.
18. "Metaraminol - Drugs.com".