vinpocetine

Action and Spectrum

Actions and Spectrum:  

vinpocetine exhibits a multifaceted action, acting on various physiological processes in the body.. vinpocetine has been shown to selectively dilate cerebral blood vessels, increase cerebral blood flow, and improve cerebralmetabolism, leading to improved oxygen and nutrient delivery to the brain tissue. 

vinpocetine has a broad spectrum of activity, with effects on various physiological processes in the body. Its vasodilatory, anti-inflammatory, and antioxidant properties contribute to its potential benefits in cognitive enhancement and neuroprotection

Drug Interaction

Adverse Reaction

Frequency not defined 

Adults 

Transient tachycardia 

Pressure-type headache 

Dizziness 

Insomnia 

Drowsiness 

Nausea 

Facial flushing 

Black Box Warning

Black Box Warning:  

 The Black box warning for vinpocetine should include the following information:  

Cardiovascular Risk: vinpocetine has been reported to have vasodilatory effects, which may lead to a drop in blood pressure. This can pose a significant risk, particularly in individuals with pre-existing cardiovascular conditions, including hypotension, ischemic heart disease, or arrhythmias.   

Bleeding Risk: vinpocetine has been reported to inhibit platelet aggregation and may increase the risk of bleeding.  Avoid in disorders such as hemophilia or thrombocytopenia, and in those taking anticoagulant or antiplatelet medications.  

Neurological Effects: vinpocetine has been reported to have neuroprotective effects, but there have been rare reports of adverse neurological effects, including seizures and worsening of Parkinson’s disease symptoms. 

Contraindication / Caution

Contraindication/Caution:   

Hypersensitivity: vinpocetine is contraindicated in individuals with a known hypersensitivity or allergic reaction to vinpocetine or its ingredients. Hypersensitivity reactions may manifest as rash, itching, swelling, difficulty breathing, or other allergic symptoms. 

Pregnancy and Lactation: Due to limited safety data, vinpocetine is contraindicated during pregnancy and lactation. Animal studies have shown potential reproductive toxicity, including embryotoxicity and teratogenicity, and there is insufficient data on the safety of vinpocetine in human pregnancy or breastfeeding. 

Bleeding Disorders: vinpocetine may have antiplatelet and anticoagulant effects, and, therefore should be used with caution or avoided in individuals with bleeding disorders or a history of bleeding events. vinpocetine may increase the risk of bleeding or interact with other anticoagulant medications, leading to serious bleeding complications.  

Recent Surgery or Trauma: vinpocetine should be avoided in these individuals 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology: 

vinpocetine is a synthetic compound derived from vincamine, Vinpocetine is classified as a selective vasodilator and is commonly used as a nootropic agent due to its cognitive-enhancing properties. The pharmacology of vinpocetine involves its interactions with various receptors and enzymes in the body.  

Pharmacodynamics: The pharmacodynamics mechanism of vinpocetine involves multiple actions on various molecular targets in the CNS. Its vasodilatory, anti-inflammatory, neurotransmitter modulation and antioxidant properties may contribute to its cognitive-enhancing and neuroprotective effects.   

Mechanism of Action: vinpocetine’s primary mechanism of action is its ability to selectively increase blood flow to the brain, which is thought to be mediated through its vasodilatory effects on cerebral blood vessels. vinpocetine has been shown to inhibit the activity of phosphodiesterase type 1 (PDE1), an enzyme that breaks down cyclic guanosine monophosphate (cGMP), resulting in increased levels of cGMP. Elevated cGMP levels lead to vasodilation and increased blood flow in the brain, improving oxygen and nutrient delivery to brain cells. 

Pharmacokinetics: 

Absorption: 

vinpocetine is orally administered and is rapidly absorbed from the gastrointestinal tract. It has a high oral bioavailability, ranging from 60-100%. However, the absolute bioavailability of vinpocetine is still under debate due to its low plasma concentrations and extensive first-pass metabolism. 

Distribution  

vinpocetine is widely distributed throughout the body. It has a relatively low volume of distribution, indicating that it is primarily distributed in the plasma rather than extensively binding to tissues. 

Metabolism 

vinpocetine undergoes extensive metabolism in the liver through various metabolic pathways, including hydrolysis, dehydrogenation, and glucuronidation. 

Elimination and Excretion 

vinpocetine and its metabolites are predominantly excreted via renal elimination. After undergoing metabolism in the liver, the glucuronide conjugates of vinpocetine and its metabolites are eliminated through the kidneys via renal excretion. A small portion of vinpocetine is also excreted unchanged in the urine, accounting for a minor portion of the total excretion. The elimination half-life of vinpocetine is relatively short, ranging from 2 to 4 hours in humans.

Adminstartion

Administration:  

vinpocetine is available in various formulations, including oral tablets and injectable solutions, and its administration should be guided by appropriate dosing and usage guidelines. 

Oral Administration: vinpocetine is commonly administered orally in the form of tablets or capsules. The typical recommended dosage for adults is 5-10 mg, taken 1-3 times per day with meals. It is important to follow the prescribing physician’s instructions and not exceed the recommended dosage. 

Injectable Administration: vinpocetine is also available in injectable formulations, which are typically used in hospital or clinical settings under the supervision of a healthcare professional. The injectable form of vinpocetine is administered intravenously (IV) or intramuscularly (IM). A qualified healthcare provider should determine the dosage and frequency of injections based on the patient’s condition and response to treatment. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: vinpocetine 

Why do we use vinpocetine?  

vinpocetine, a well-known compound, is utilized for various therapeutic purposes due to its neuroprotective and cognitive-enhancing properties. It is a synthetic derivative of the alkaloid vincamine, which is extracted from the periwinkle plant (Vinca minor). vinpocetine has been widely studied for its potential benefits in improving cerebral blood flow, reducing inflammation, and enhancing cognitive function.

It is believed to work through multiple mechanisms of action, including its ability to increase blood flow to the brain, enhance glucose metabolism, scavenge free radicals, and inhibit phosphodiesterase (PDE) enzymes. vinpocetine has been studied for its potential use in treating of various neurological disorders, including dementia, ischemic stroke, and cognitive impairment associated with aging.