Oxyfedrine
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Oxyfedrine, sold under the brand names Ildamen and Myofedrin among others, is a sympathomimetic agent and coronary vasodilator which is used in the treatment of coronary heart disease, angina pectoris, and acute myocardial infarction.[1][2][3][4][5][6] It is taken by mouth or intravenously.[1]
The drug acts as a β-adrenergic receptor partial agonist.[1][6] It may also act as a norepinephrine releasing agent via its major active metabolite norephedrine.[7] Oxyfedrine is a phenethylamine and amphetamine derivative.[5][6]
Oxyfedrine has been marketed in Europe, Hong Kong, India, Central America, and elsewhere.[3][8][9] It appears to remain marketed only in India.[9]
Pharmacology
Pharmacodynamics
Oxyfedrine is a β-adrenergic receptor partial agonist.[1][6] It appears to be non-selective for the β1- and β2-adrenergic receptors.[6] It is selective for the β-adrenergic receptors over the α-adrenergic receptors.[6] However, it has also been reported to interact with the α-adrenergic receptors at high concentrations, acting as a partial agonist or antagonist of these receptors.[6] Norephedrine, a norepinephrine releasing agent, is a major active metabolite of oxyfedrine, and hence oxyfedrine may additionally act as an indirectly acting sympathomimetic.[7]
It has been found to depress the tonicity of coronary vessels, improve myocardial metabolism (so that heart can sustain hypoxia better) and also exert a positive chronotropic and inotropic effects,[1] thereby not precipitating angina pectoris. The latter property (positive chronotropic and inotropic effects) is particularly important, because other vasodilators used in angina may be counter productive causing coronary steal phenomenon.Template:Additional citation needed
The drug is chemically and pharmacologically unrelated to any other antianginal drugs.[1]
Pharmacokinetics
Oxyfedrine's oral bioavailability is 85%.[1] The plasma protein binding is almost 100%.[1] Its elimination half-life is 4.2Script error: No such module "String".hours.[1] Norephedrine is a major active metabolite of oxyfedrine.[7] The excretion of the active metabolites of oxyfedrine is 90% in urine.[1] About 75 to 100% of oxyfedrine is excreted as norephedrine.[7]
Chemistry
Oxyfedrine is a substituted phenethylamine and amphetamine derivative.[6] It is l-norephedrine with a bulky and lipophilic 3-methoxypropiophenone substituent at the nitrogen atom.[6]
Synthesis
Mannich condensation of phenylpropanolamine (1) with formaldehyde and m-acetanisole (3-acetylanisole) (2) yields oxyfedrine (3).[10]
Research
Synergistic effects of oxyfedrine with antibiotics against bacteria have been suggested.[11]
References
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- ↑ Thiele Kurt, U.S. patent 3225095 (1965 to Degussa)
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