Fullserpine

Fullserpine Uses, Dosage, Side Effects, Food Interaction and all others data.

An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Fullserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.

Fullserpine is an adrenergic blocking agent used to treat mild to moderate hypertension via the disruption of norepinephrine vesicular storage. The antihypertensive actions of Fullserpine are a result of its ability to deplete catecholamines from peripheral sympathetic nerve endings. These substances are normally involved in controlling heart rate, force of cardiac contraction and peripheral resistance.

Fullserpine
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Fullserpine
Availability	Discontinued
Generic	Reserpine
Reserpine Other Names	Reserpin, Reserpine
Related Drugs	amlodipine, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide, quetiapine, Abilify, Seroquel, aripiprazole
Type
Formula	C₃₃H₄₀N₂O₉
Weight	Average: 608.6787 Monoisotopic: 608.273380888
Protein binding	62%
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	Taiwan
Last Updated:	September 19, 2023 at 7:00 am

Uses

For the treatment of hypertension

Fullserpine is also used to associated treatment for these conditions: High Blood Pressure (Hypertension), Agitated psychotic state

How Fullserpine works

Fullserpine's mechanism of action is through inhibition of the ATP/Mg²⁺ pump responsible for the sequestering of neurotransmitters into storage vesicles located in the presynaptic neuron. The neurotransmitters that are not sequestered in the storage vesicle are readily metabolized by monoamine oxidase (MAO) causing a reduction in catecholamines.

Toxicity

Possible human carcinogen. May cause reproductive harm. ORL-RAT LD₅₀ 420 mg/kg; IPR-RAT LD₅₀ 44 mg/kg; IVN-RAT LD₅₀ 15 mg/kg; ORL-MUS LD₅₀ 200 mg/kg; SCU-MUS LD₅₀ 52 mg/kg; IPR-RBT LD₅₀ 7 mg/kg

Food Interaction

Avoid alcohol.
Take with food. Food reduces irritation.

Fullserpine Alcohol interaction

[Moderate]

Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.

Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.

Caution and close monitoring for development of hypotension is advised during coadministration of these agents.

Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.

Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.