Usage
Vinpocetine is primarily prescribed for cognitive impairment related to cerebrovascular diseases, such as stroke, dementia, and memory loss. It is also used as an adjuvant treatment in focal onset epileptic seizures. Other uses include the management of vascular eye and ear diseases, and urge incontinence. Its pharmacological classification is a vasodilator with nootropic (cognitive enhancing) properties. Vinpocetine’s mechanism of action involves improving cerebral blood flow and metabolism, neuroprotection, anticonvulsant effects, and antioxidant activity.
Alternate Names
Vinpocetine is also known as ethyl apovincaminate, Cavinton, and Intelectol.
How It Works
Pharmacodynamics: Vinpocetine improves cerebral blood flow by increasing erythrocyte deformability, inhibiting platelet aggregation, and decreasing blood viscosity. It enhances cerebral metabolism by increasing glucose and oxygen uptake by brain cells and promoting the utilization of these substrates. It acts as an anticonvulsant, although the exact mechanism is not fully elucidated. It also exhibits antioxidant properties, protecting brain cells from free radical damage.
Pharmacokinetics: Vinpocetine is well-absorbed after oral administration, reaching peak plasma concentrations within 1-2 hours. It is extensively metabolized in the liver, primarily to its main active metabolite, cis-apovincaminic acid (cAVA). It is eliminated mainly through renal excretion, with a half-life of approximately 2-4 hours.
Mode of Action: Vinpocetine selectively inhibits phosphodiesterase type 1 (PDE1), leading to increased cyclic guanosine monophosphate (cGMP) levels, which promotes vasodilation. It also modulates voltage-gated sodium channels, potentially contributing to its neuroprotective and anticonvulsant effects. The precise receptor binding and enzyme inhibition profiles of vinpocetine are complex and not fully understood.
Elimination Pathways: Vinpocetine is primarily eliminated via hepatic metabolism, followed by renal excretion of the metabolites. CYP450 enzyme involvement has been reported.
Dosage
Standard Dosage
Adults:
The typical dosage is 5-10 mg orally three times a day, with a maximum daily dose of 30 mg. Some regimes have used up to 60 mg per day.
Children:
Vinpocetine is generally not recommended for use in children and adolescents due to insufficient safety and efficacy data in this age group.
Special Cases:
- Elderly Patients: Dosage adjustment is generally not necessary but should be approached conservatively.
- Patients with Renal Impairment: Dose reduction may be necessary in patients with severe renal failure.
- Patients with Hepatic Dysfunction: Careful monitoring is recommended.
- Patients with Comorbid Conditions: Individualized dosing should be considered for patients with other medical conditions, particularly cardiovascular diseases.
Clinical Use Cases
Vinpocetine has not been indicated for the treatment of acute conditions like intubation, surgical procedures, mechanical ventilation, intensive care unit (ICU) use, or emergency situations such as status epilepticus or cardiac arrest. However, it is sometimes employed as adjunctive therapy in the recovery phase of stroke or for long-term management of cognitive impairment.
Dosage Adjustments
Dosage adjustments should be based on individual patient response and tolerance. Close monitoring of renal and hepatic function is recommended, especially in patients with pre-existing impairment.
Side Effects
Common Side Effects:
Headache, dizziness, nausea, flushing, dry mouth, dyspepsia, and sleep disturbances.
Rare but Serious Side Effects:
Allergic reactions, QT interval prolongation, cardiac arrhythmias, and bleeding.
Long-Term Effects:
Limited data are available on the long-term effects of vinpocetine.
Adverse Drug Reactions (ADR):
Any signs of allergic reactions, severe hypotension, or cardiac abnormalities should be treated immediately.
Contraindications
- Hypersensitivity to vinpocetine.
- Severe ischemic heart disease or cardiac arrhythmia.
- Active bleeding in the central nervous system (CNS).
- Pregnancy and lactation.
Drug Interactions
Vinpocetine may interact with anticoagulants and antiplatelet drugs, increasing the risk of bleeding. It can also interact with certain medications metabolized by CYP450 enzymes. Interactions with common medications, OTC drugs, and supplements should be considered. Alcohol, smoking, and grapefruit juice might influence its effects. Consult a drug interaction database for a detailed list of potential interactions.
Pregnancy and Breastfeeding
Vinpocetine is contraindicated during pregnancy and breastfeeding due to potential fetal risks and insufficient safety data.
Drug Profile Summary
- Mechanism of Action: Enhances cerebral blood flow and metabolism; neuroprotective, anticonvulsant, and antioxidant effects.
- Side Effects: Headache, dizziness, nausea, flushing; rarely, allergic reactions, QT prolongation, bleeding.
- Contraindications: Hypersensitivity, severe heart disease, CNS bleeding, pregnancy, breastfeeding.
- Drug Interactions: Anticoagulants, antiplatelets, CYP450 substrates.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: 5-10 mg TID, up to 30 mg/day.
- Monitoring Parameters: Blood pressure, heart rate, liver and kidney function tests.
Popular Combinations
Vinpocetine is sometimes combined with other nootropics or cognitive enhancers, but the efficacy and safety of these combinations are not well-established.
Precautions
Standard precautions include assessing for allergies, metabolic disorders, and organ dysfunction. Special precautions apply to pregnant/breastfeeding women, children, and the elderly. Driving restrictions might be needed if dizziness occurs.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Vinpocetine?
A: The standard dosage for adults is 5-10 mg three times a day. Dosages up to 60mg per day have been used. Pediatric use is not recommended.
Q2: What are the primary uses of Vinpocetine?
A: Vinpocetine is mainly used to treat cognitive impairment associated with cerebrovascular disease.
Q3: How does Vinpocetine work?
A: Vinpocetine enhances cerebral blood flow and metabolism through various mechanisms, including PDE1 inhibition and modulation of sodium channels.
Q4: What are the common side effects of Vinpocetine?
A: Common side effects include headache, dizziness, nausea, and flushing.
Q5: What are the contraindications for Vinpocetine use?
A: Contraindications include hypersensitivity, severe heart disease, active CNS bleeding, and pregnancy/breastfeeding.
Q6: Does Vinpocetine interact with other medications?
A: Yes, vinpocetine may interact with anticoagulants/antiplatelets and drugs metabolized by CYP450 enzymes.
Q7: Can Vinpocetine be used during pregnancy?
A: No, vinpocetine is contraindicated during pregnancy.
Q8: Is Vinpocetine safe for long-term use?
A: Long-term safety data are limited. Regular monitoring of relevant parameters is advised.
Q9: How should Vinpocetine be administered?
A: Vinpocetine is typically administered orally, ideally with food to enhance absorption.
Q10: Can Vinpocetine be used to treat acute stroke?
A: While some studies have investigated intravenous vinpocetine for acute stroke, its use for this condition is not yet standard practice. There are no studies of the use of oral vinpocetine to treat acute stroke. More research is needed to confirm its role in this context.
