Cerenin

Approved and Common Uses:

• Chronic Cerebral Ischemia: Treatment of symptoms related to poor blood flow in the brain.
• Vascular Dementia: Management of cognitive decline caused by cerebrovascular disease.
• Post-Stroke Recovery: Adjunct therapy to improve cerebral metabolism and blood flow.
• Memory Disorders: Age-related memory impairment and mild cognitive dysfunction of vascular origin.
• Tinnitus and Hearing Disorders: Treatment of tinnitus and sensorineural hearing loss related to vascular insufficiency.
• Meniere’s Disease: Used to relieve vertigo and associated symptoms.
• Retinopathies: Management of vascular-related retinal disorders such as diabetic or hypertensive retinopathy.

Off-label Uses:

• Mild to moderate Alzheimer’s disease (as adjunct therapy).
• Neuroprotective agent in epilepsy.
• Prevention of motion sickness.
• Ischemic optic neuropathy.

• Route: Oral administration.
• Adult Dosage: 5–10 mg, three times daily after meals.
• Maximum Dose: Up to 30 mg daily divided into three doses.
• Duration: Treatment typically lasts for 1 to 2 months; prolonged use only under medical supervision.
• Elderly: Initiate at lower doses with careful monitoring; dose adjustments generally not required.
• Pediatric Use: Not recommended due to insufficient safety data.
• Renal/Hepatic Impairment: Use cautiously; no specific dose adjustment guidelines but monitor patient response.
• Missed Dose: Take as soon as remembered unless it is near the next dose; do not double doses.

Vinpocetine improves cerebral blood flow by selectively inhibiting phosphodiesterase type 1 (PDE1), which increases intracellular cyclic nucleotides (cAMP and cGMP). This results in vasodilation of cerebral arteries, enhancing oxygen and glucose delivery to brain tissues. Additionally, vinpocetine blocks voltage-dependent sodium channels and regulates calcium influx in neurons, providing neuroprotection against ischemic damage. These combined effects enhance cerebral metabolism, support neuronal function, and improve cognitive performance.

• Absorption: Rapidly absorbed orally with peak plasma levels reached within 1 to 2 hours.
• Bioavailability: Low (approximately 6-10%) due to first-pass metabolism.
• Distribution: Widely distributed, including effective penetration across the blood-brain barrier.
• Protein Binding: Approximately 66%.
• Metabolism: Extensively metabolized by the liver, mainly via CYP3A4 to inactive metabolites such as apovincaminic acid.
• Elimination Half-life: 2 to 4 hours for vinpocetine; metabolite half-life approximately 5 hours.
• Excretion: Primarily eliminated through urine as metabolites; minor fecal excretion.

• Pregnancy: No official FDA pregnancy category assigned. Animal studies suggest potential embryotoxicity at high doses; use is contraindicated or should be avoided during pregnancy.
• Lactation: Unknown if excreted in human milk. Due to potential risks to the infant, vinpocetine is not recommended during breastfeeding.
• Recommendation: Use only if clearly needed and when benefits outweigh risks.

• Primary Class: Cerebral vasodilator and neuroprotective agent.
• Subclass: Synthetic alkaloid derivative of vincamine.
• Pharmacologic Category: Phosphodiesterase type 1 (PDE1) inhibitor and nootropic.

• Hypersensitivity to vinpocetine or any formulation components.
• Pregnancy.
• Active hemorrhagic stroke.
• Severe hypotension or unstable cardiovascular conditions.
• Known arrhythmias or prolonged QT interval.

• Pregnancy: Avoid use due to fetal risk.
• Hypotension: Monitor blood pressure closely; vinpocetine may cause hypotension.
• Seizure Disorders: Use cautiously as it may lower seizure threshold.
• Bleeding Risk: May affect platelet aggregation; caution in patients on anticoagulants or with bleeding disorders.
• Cardiac Arrhythmias: Use with caution in patients with heart rhythm abnormalities.
• Monitoring: Regularly monitor neurological status, blood pressure, and cardiovascular function during therapy.

Common:

• Headache.
• Dizziness.
• Gastrointestinal discomfort (nausea, dry mouth).
• Flushing.
• Mild hypotension.

Less Common or Rare:

• Palpitations.
• Allergic skin reactions (rash, pruritus).
• Visual disturbances.
• Aggravation of seizures in predisposed individuals.
• Hepatic enzyme elevations.

• Anticoagulants/Antiplatelets: Potential increased bleeding risk; caution and monitoring required.
• Antihypertensive Agents: Additive blood pressure-lowering effect possible.
• CYP3A4 Modulators: Drugs that inhibit or induce CYP3A4 (e.g., ketoconazole, rifampin) may alter vinpocetine plasma levels.
• Alcohol: May enhance central nervous system effects; consumption should be limited or avoided.

• Regulatory Advisories: FDA issued warnings regarding vinpocetine in dietary supplements due to risks in pregnancy.
• Clinical Use: Not approved as a prescription drug by many regulatory agencies; primarily available as a dietary supplement or investigational agent.
• Safety Considerations: Growing concerns about long-term safety and use during pregnancy, leading to increased regulatory scrutiny.

• Store at room temperature between 20°C and 25°C.
• Protect from moisture, heat, and direct sunlight.
• Keep container tightly closed.
• No refrigeration or special handling required.
• Keep out of reach of children.