Vincamine is a natural indole alkaloid derived from the periwinkle plant, primarily Vinca minor. Recognized as a vasodilator, it is studied for its ability to increase cerebral blood flow and oxygen consumption, which has led to its use in treating certain cerebrovascular and cognitive disorders. In some European countries, vincamine is available only by prescription, whereas in the United States, it is marketed as an over-the-counter dietary supplement. Clinically, it is used to prevent and treat cerebrovascular disorders and circulatory insufficiencies.
BRAND NAMES
Anacervix and Cervitam, Brain Ox, Oxybral, Vincabral, Vincapan, and Vincatreis.
Available in the oral forms.
MECHANISM OF ACTION
Vincamine improves cerebral blood flow and offers neuroprotection through several mechanisms. It promotes vasodilation by inhibiting phosphodiesterase and blocking voltage-gated sodium channels. The compound also enhances brain metabolism by increasing glucose and oxygen utilization. In addition, vincamine exhibits antioxidant, anti-inflammatory, and anti-apoptotic properties, helping to reduce oxidative stress and protect against excitotoxicity. These combined effects support its potential use in treating conditions such as cognitive impairment and stroke.
PHARMACOKINETICS
Absorption
Vincamine is well-absorbed after oral administration, but its bioavailability is limited by poor water solubility and a significant first-pass effect in the liver. The absorption can be improved when vincamine is administered as a standardized whole-leaf extract of Vinca minor rather than as a pure compound.
Distribution
Vincamine is distributed in the body with approximately 64% bound to plasma proteins and around 6% bound to erythrocytes. In gerbils, the apparent volume of distribution for the drug is approximately 2.9 L/kg.
Metabolism
Vincamine is mainly metabolized in the liver, with its metabolites, including hydroxy-vincamines and their conjugates excreted via the kidneys and bile. The main metabolic pathways include hydroxylation and oxidation, leading to the formation of 6α- and 6β-hydroxy-vincamine, which are subsequently oxidized to 6-keto-vincamine. Additional pathways include ester cleavage to form vincaminic acid and possible degradation to eburnamonine.
Excretion
The excretion percentage of unchanged vincamine in urine is around 7%. Most of the drug is initially metabolized in the liver prior to elimination.
PHARMACODYNAMICS
Vincamine's pharmacodynamic actions include vasodilation, especially in the brain, along with antioxidant effects that help protect cells from damage. It functions as an agonist of the G-protein-coupled receptor 40 (GPR40), which plays a key role in its protective effects on tissues such as pancreatic β-cells and nerves. Additionally, vincamine demonstrates anti-inflammatory properties by regulating the NF-κB and Nrf-2 pathways, and may also exhibit mild hypoglycemic and hypolipidemic effects.
ADMINISTRATION
Vincamine administration is available in oral and parenteral (intramuscular or slow intravenous infusion) forms, though it is used differently depending on the country. It functions as a vasodilator by enhancing cerebral blood flow and is used in the treatment of cerebrovascular disorders.
DOSAGE AND STRENGTH
Vincamine is an alkaloid that has been formulated into several dosage forms, including capsules, tablets, and injections. The typical recommended dosage ranges from 10 to 40 milligrams per day.
DRUG INTERACTIONS
Vincamine and its derivative, vinpocetine, may interact with several medications by enhancing their blood-thinning and blood pressure-lowering effects. Using vincamine alongside anticoagulants or antiplatelet medications, such as warfarin or aspirin, may heighten the risk of bleeding. Similarly, its combination with blood pressure medications, including ACE inhibitors and beta-blockers, can cause an unsafe drop in blood pressure. Vincamine may also interact with certain antidepressants, anxiety medications, and other central nervous system drugs.
FOOD INTERACTIONS
For vincamine itself, no clinically significant food interactions have been identified, though taking it with food can help mitigate mild gastrointestinal side effects like nausea. Taking vinpocetine with food can prevent stomach upset, but alcohol should be avoided as it may increase side effects like dizziness. Grapefruit products may also interact with vinpocetine. Given that the FDA has issued warnings regarding vinpocetine and deemed it ineligible as a dietary ingredient, it is always best to consult a healthcare provider for advice before combining any supplements with food or other medications.
CONTRAINDICATIONS
Vincamine is contraindicated in individuals with hypersensitivity to the drug, conditions involving increased intracranial pressure, and a history of certain bleeding or severe cardiovascular disorders. Due to a lack of safety data, it is also contraindicated during pregnancy and breastfeeding.
SIDE EFFECTS
Gastrointestinal discomfort.
Dizziness and lightheadedness.
Headaches.
Sleep disturbances.
Abnormal dreams.
Loss of taste.
Allergic reactions.
Cardiovascular issues.
nausea.
stomach cramps.
diarrhea.
OVER DOSE
Potential overdose symptoms generally reflect an exaggeration of the drug's common side effects and can include:
Gastrointestinal issues.
Nausea and vomiting.
Rapid heartbeat.
Low blood pressure.
Facial flushing and dry mouth.
Dizziness and vertigo.
Anxiety and nervousness.
Insomnia or sleep disturbances.
TOXICITY
Vincamine, an alkaloid from the periwinkle plant (Vinca minor), is considered harmful if swallowed, especially in large doses. While moderate doses are generally well-tolerated, an overdose can lead to severe side effects involving multiple organ systems, with the nervous system being the most commonly affected. Its synthetic derivative, vinpocetine, has been studied more extensively and has similar toxicity concerns.
