Reserpine

Reserpine is an indole alkaloid used in the treatment of hypertension and psychosis. It was originally extracted from the plant Serpentine. Nowadays, due to more side effects and better new drugs on the market, reserpine is no longer the first choice for treatment. Catecholamines (monoamine neurotransmitters) play an important role in the regulation of heart rate, myocardial contractile force and peripheral resistance, and reserpine exerts its antihypertensive effect by consuming catecholamines from peripheral sympathetic nerve endings.

Soluble in chloroform, dichloromethane, glacial acetic acid, can dissolve in benzene, ethyl acetate, slightly soluble in acetone, methanol, ethanol, ether, acetic acid and citric acid solutions. The solution of reserpine turns yellow after a certain period of time, and has significant fluorescence, and the fluorescence is enhanced after acid addition and exposure. Reserpine is a weak base. Reserpine can lower blood pressure and slow heart rate. Its action is slow, mild and long-lasting. It has a long-lasting calming effect on the central nervous system and is a good sedative.

Reserpine primarily affects the uptake of norepinephrine into vesicles in sympathetic nerve endings, causing it to be degraded by monoamine oxidase and depleting the storage of norepinephrine, thus impairing the transmission of sympathetic nerve impulses. This results in vascular dilation, decreased blood pressure, and reduced heart rate. The central nervous system sedation and inhibition may be the result of reserpine entering the brain and depleting the central catecholamine storage. The hypotensive effect appears within 1 hour after intravenous injection. The antihypertensive effect of oral treatment begins approximately 1 week after administration and reaches its peak effect 2-3 weeks later. The effect persists for 3-4 weeks after discontinuation of treatment.

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Drug interaction
General anesthetics can enhance the antihypertensive effect of reserpine. In combination with ethanol or central nervous system inhibitors, the central inhibitory effect can be aggravated.
1. combined with other antihypertensive drugs or diuretics can strengthen the antihypertensive effect, the dose needs to be adjusted; In combination with β-blocker, the latter effect can be enhanced;
2. combined with digitalis or quinidine, large doses can cause arrhythmia;
3. combined with levodopa can cause dopamine depletion, leading to Parkinson's disease;
4. combined with indirect adrenergic drugs such as ephedrine, amphetamine, etc., can make catecholamine storage depletion, inhibit the effect of adrenergic drugs;
5. combined with direct adrenergic drugs such as epinephrine, isoproterenol, norepinephrine, mehydroxyamine, deoxyadrenalin, etc., can prolong its effect;
6. combined with tricyclic antidepressants, the effects of reserpine and antidepressants were weakened;
7. barbiturates can strengthen the central sedative effect of reserpine.

Drug overdose
Reserpine has no specific antidote, can not be eliminated by dialysis, treatment measures are symptomatic and supportive therapy. The overdose causes respiratory depression, coma, low blood pressure, convulsions, and hypothermia. At this point, gastric lavage must be taken to induce vomiting, even after several hours of medication. Patients with severe hypotension were placed in the lying position, their feet were raised, and direct epinephrine drugs were carefully administered to boost blood pressure. Oxygen inhalation and artificial respiration were given to patients with respiratory depression. Anticholinergic drugs treat gastrointestinal symptoms; And correct dehydration, electrolyte imbalance, hepatic coma, and hypotension. Patients should be observed for at least 72 hours because reserpine action lasts for a long time. Blood pressure to satisfactory level.

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