Docarpamine (INNTooltip International Nonproprietary Name, JANTooltip Japanese Accepted Name), sold under the brand name Tanadopa, is an orally active dopamine prodrug which is marketed in Japan for the treatment of acute cardiac insufficiency and/or chronic heart failure.
[1] The N-substitution protects the drug from first-pass metabolism by monoamine oxidase (MAO) until it is cleaved into dopamine and allows it to be orally active.
[6][7] The drug does not cross the blood–brain barrier or affect the central nervous system even at high doses and hence is peripherally selective.
[9] It is thought that the therapeutic effects of docarpamine are mediated by activation of peripheral dopamine D1 receptors.
[3] Although docarpamine is orally active and can achieve therapeutic levels of dopamine in blood,[1] relatively high doses and frequent administration of the drug (e.g., 600–750 mg every 8 hours) are required when it is used by this route.