debrisoquine

Debrisoquine is an adrenergic neuron-blocking antihypertensive drug, structurally related to guanethidine and classified as a peripherally acting antiadrenergic agent. It is primarily used for the treatment of moderate and severe hypertension, including renal hypertension. Debrisoquine acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine from postganglionic adrenergic nerves. It is taken up by norepinephrine transporters into nerve terminals, where it becomes concentrated in neurotransmitter vesicles and gradually replaces norepinephrine (NE), leading to depletion of NE stores in nerve endings. This results in reduced noradrenaline release upon nerve stimulation, lowering blood pressure through decreased peripheral resistance and cardiac output[1][2][5]. Unlike ganglionic blocking agents, it does not produce parasympathetic blockade. Debrisoquine is also notable as a probe drug for phenotyping CYP2D6 enzyme activity due to its metabolism via this polymorphic cytochrome P450 isoenzyme; individuals with certain genetic variants are poor metabolizers[3][6][7]. Additionally, laboratory studies have identified debrisoquine as an inhibitor of TMPRSS2 protease involved in SARS-CoV-2 viral entry[3].

Other names

DebrisoquinDebrisoquine sulfate