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.

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
Fullserpine
Fullserpine

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.

Elimination Route

Fullserpine is extensively metabolized to inactive compounds. It is slowly excreted via the urine and feces.

Innovators Monograph

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*** Taking medicines without doctor's advice can cause long-term problems.
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