Alkaloids
Alkaloids Uses, Dosage, Side Effects, Food Interaction and all others data.
Rauwolfia (Rauwolfia serpentina), also spelled ravolphia, is a medicinal plant in the milkweed family. The root of the plant is ground into a powder or sold in tablets or capsules. It is a compound commonly used in Asian medicine, which includes traditional Ayurvedic medicine native to India. The active ingredients in this drug are alkaloids and about 50 have been identified through various studies, although the primary psychoactive components appear to be reserpine, rescinnamine, and deserpidine .
This product was approved prior to Jan 1, 1982, but since, has been discontinued due to its propensity for leading to depression . Reserpine is derived from Rauwolfia serpentina, and was commonly used as an antihypertensive agent in the 1950s . Rauwolfia serpentina is also commonly referred to as Sarpaghanda . Interestingly, the hairy root component of this plant has shown a remarkable capacity to regenerate into complete Rauwolfia plants and shows survival and unaltered biosynthetic potential during storage at decreased temperatures. For this reason, various studies into biotechnological applications of this plant have been performed. Multiple studies have been done on their biosynthetic potential and numerous biotechnological methods used to study the production of pharmaceutically important alkaloids .
Reserpine is used to treat high blood pressure. It also is used to treat severe agitation in patients with mental disorders. Reserpine is in a class of medications called rauwolfia alkaloids. It works by slowing the activity of the nervous system, causing the heart rate to slow and the blood vessels to dilate .
| Trade Name | Alkaloids |
| Generic | Rauwolfia serpentina root |
| Rauwolfia serpentina root Other Names | Alkaloids, rauwolfia, Alseroxylon, Rauvolfia serpentina root, Rauwolfia, Rauwolfia alkaloids, Rauwolfia root, Rauwolfia serpentina, Rauwolfia serpentina alseroxylon, Snakeroot |
| Type | |
| Protein binding | Reserpine is extensively bound (95%) to plasma proteins . |
| Groups | Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Rauwolfia alkaloids are indicated in the treatment of hypertension . Rauwolfia alkaloids have been used for relief of symptoms in agitated psychotic states such as schizophrenia; however, use as antipsychotics and sedatives have been replaced with the use of more effective, safer agents .
How Alkaloids works
Reserpine is an adrenergic blocking agent used to treat mild to moderate hypertension via the disruption of norepinephrine vesicular storage. The antihypertensive actions of Reserpine are a result of its ability to deplete catecholamines from peripheral sympathetic nerve endings. These substances are normally involved in controlling heart rate, the work of cardiac contraction and peripheral resistance . Reserpine depletes brain (depression) and peripheral (PPH) noradrenaline (NA) storage sites, guanethidine depleted NA storage via blockade of reuptake .
This agent binds and inhibits catecholamine pump on the storage vesicles in central and peripheral adrenergic neurons, thereby inhibiting the uptake of norepinephrine, dopamine serotonin into presynaptic storage vesicles. This results in catecholamines and serotonin lingering in the cytoplasm where they are destroyed by intraneuronal monoamine oxidase, thereby causing the depletion of catecholamine and serotonin stores in central and peripheral nerve terminals. Depletion results in a lack of active transmitter discharge from nerve endings upon nerve depolarization, and consequently leads to a decreased heart rate and decreased arterial blood pressure as well as sedative effects .
Toxicity
Ld50: 390 mg/kg oral mouse .
Reserpine may increase gastric acid secretion and should be used with caution in patients with a history of gastroesophageal reflux disease (GERD) and peptic ulcer. It should also not be administered to patients diagnosed with depression .
Adverse reactions of this drug include: vomiting, diarrhea, arrhythmias , syncope, bradycardia, dyspnea, epistaxis, rare parkinsonian syndrome and other extrapyramidal tract (EPS) symptoms, dizziness, headache, paradoxical anxiety, depression, nervousness, nightmares, dull sensorium, drowsiness, muscular aches, pseudo lactation, weight gain, deafness, optic atrophy, hypersensitive reactions (pruritus) .
The mechanism of reserpine's toxic effects is found to be in parallel with the mechanism of its pharmacologic effects. Reserpine inhibits sympathetic activity in the central nervous system and peripheral nervous system by binding to catecholamine storage vesicles. This prevents the normal storage of catecholamines and serotonin in the nerve, resulting in catecholamine depletion. This drug has also been described as inhibiting catecholamine synthesis by blocking the uptake of dopamine into the storage vesicles .
Elimination Route
Mean maximum plasma levels of plasma concentrations after 0.5 mg of Reserpine, administered as two 0.25 mg tablets or as an aqueous solution, peaked after 2.5 hours. The mean peak level was approximately 1.1 ng/ml. Bioavailability of Reserpine, has been reported to be approximately 50% .
Half Life
After oral ingestion, an initial half-life of approximately 5 hours is followed by a terminal half-life of approximately 200 hours .
Clearance
Hepatically and renally .
Elimination Route
The elimination of reserpine and its metabolites in the feces ranges from 30% after intramuscular administration to about 60% after oral ingestion, primarily as unmetabolized reserpine, over a 4 day period after the ingestionof 0.25 mg to 0.50 mg doses. Over the same time period, about 8% of the ingested dose was recovered in the urine, primarily as the trimethoxybenzoic acid metabolite .
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