A fat-soluble alkaloidal fraction extracted from the root of Rauwolfia serpentina, containing reserpine and other nonadrenolytic amorphous alkaloids; used as a sedative in psychoses, in mild hypertension, and as an adjunct to more potent hypotensive drugs. Alseroxylon has been discontinued in the US market.
For the treatment of hypertension and as an adjunct in the management of angina pectoris.
Alseroxylon is a purified extract of Rauwolfia serpentina, containing reserpine and other amorphous alkaloids. Alseroxylon is an indole alkaloid antipsychotic and antihypertensive drug known to irreversibly bind to storage vesicles of neurotransmitters such as dopamine, norepinephrine, and serotonin. This leads to depletion of the neurotransmitters and subsequent depression in humans.
Mechanism of action
The antihypertensive actions of alseroxylon are a result of its ability to deplete catecholamines from peripheral sympathetic nerve endings. Alseroxylon almost irreversibly blocks the accumulation of noradrenaline and dopamine into synaptic vesicles by inhibiting the Vesicular Monoamine Transporters (VMAT). This depletion ultimately affects the carotid pressoreceptors which leads to a decrease in vascular pressure.
Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles. Requisite for vesicular amine storage prior to secretion via exocytosis.
Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
FORD RV, MOYER JH: Rauwolfia toxicity in the treatment of hypertension; comparative toxicity of reserpine and alseroxylon. Postgrad Med. 1958 Jan;23(1):41-8. [PubMed:13505370 ]
SCHLAGEL CA, NELSON JW: Rauwolfia hypotension. II. Action of the alseroxylon alkaloids and epinephrine on the carotid pressoreceptors. J Am Pharm Assoc Am Pharm Assoc. 1957 Feb;46(2):103-9. [PubMed:13438725 ]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]