tuneTypical Dose
50 mg three times per day
Chemical Compound
Picamilon
Nicotinoyl-GABA
Evidence TierCWADA NOT PROHIBITED
watchEffect Window
4-10 week window for functional signal in available data.
check_circleCompliance
WADA NOT PROHIBITED
Overview
Clinical Summary
Picamilon is a niacin–GABA conjugate developed to combine calming and vasodilatory effects. It is used for anxiety and cerebral circulation claims, but the evidence base is limited and older.
Small studies suggest anxiolytic effects and improvements in certain cerebral blood flow measures, but evidence is limited and not widely replicated. Some users report improved sleep and reduced stress without heavy sedation. Minority research includes headache and cognitive impairment applications, with variable quality. Regulatory status and product quality vary, which can affect both efficacy and safety.
Proposed nicotinoyl-GABA-based activity with limited direct evidence for classic GABA receptor binding in modern target screening.
Outcomes
What This Is Expected To Influence
Primary Outcomes
- MoCA improvement trend in stage I chronic cerebral ischemia
- Autonomic symptom reduction
Secondary Outcomes
- Sleep quality improvement
- Potential endothelial marker shifts
Safety
Contraindications and Interactions
Contraindications
- Pregnancy
- Lactation
- Severe liver disease
- Severe psychiatric instability
Side effects
- Headache
- Nausea
- Lightheadedness
- Skin flushing
Interactions
- Sedatives
- Blood pressure agents
- Other vascular actives
Avoid if
- Uncontrolled hypertension
- Major psychiatric instability
- Unreliable self-monitoring
Evidence
Study-level References
picamilon-SRC-001Open randomized comparative clinical trial
Sourceopen_in_newA B Danilov et al. "Integrative assessment of the effectiveness and safety of outpatient use of Picamilon." Zh Nevrol Psikhiatr Im S S Korsakova. 2024;124(7):119-130. PMID: 39113452, DOI: 10.17116/jnevro2024124071119.
Population: Adults with stage I chronic cerebral ischemia (n=44)
Dose protocol: 50 mg orally three times/day for 60 days. Second arm 100 mg IM x10 days then 50 mg TID x50 days
Key findings: Reported MoCA and autonomic improvements with high response rates by late visits. Tolerability high.
Notes: Open-label and regional context limit strength of inference.
Paper content
Reported MoCA and autonomic improvements with high response rates by late visits; tolerability high.
picamilon-SRC-002Mechanistic safety screen (in silico + in vitro)
Sourceopen_in_newMichael F Santillo, Robert L Sprando. "Picamilon... is inactive against 50 biological targets." Basic Clin Pharmacol Toxicol. 2023;132(4):355-358. PMID: 36668678, DOI: 10.1111/bcpt.13836.
Population: Preclinical models and assay systems
Dose protocol: Screening at 10 µM for target engagement
Key findings: Weak/none binding to tested GABA-related targets. Evidence for direct receptor mechanism is limited.
Notes: Supports cautious interpretation of mechanism, not a safety disproof.
Paper content
Weak/none binding to tested GABA-related targets; evidence for direct receptor mechanism is limited.
picamilon-SRC-003Open multicenter randomized controlled trial.
Sourceopen_in_newZakharov VV, Borodulina IV, Vakhnina NV. Treatment of patients with chronic cerebral ischemia: experience of using the combined neuroprotective drug Picamilon Ginkgo. Zh Nevrol Psikhiatr Im S S Korsakova. 2022;122(9):95-103. doi:10.17116/jnevro202212209195. PMID:36168693.
Population: Adults over 45 years with chronic cerebral ischemia and cognitive impairment.
Dose protocol: Picamilon plus ginkgo biloba combination versus ginkgo monotherapy for 90 days in 278 patients
Key findings: Combination therapy produced significantly greater cognitive improvement than ginkgo alone by day 30.
Notes: Open-label and active comparator design. Largest picamilon sample to date (278 patients). Combination confound limits attribution to picamilon alone.
Paper content
This open-label multicenter RCT compared a combined picamilon-ginkgo formulation to ginkgo biloba monotherapy in 278 patients (over 45 years) with chronic cerebral ischemia and cognitive impairment over 90 days. The combination arm showed significantly greater cognitive improvement by day 30, with benefits persisting through the trial. Both groups tolerated treatment well. The open-label design and active comparator rather than placebo limit confidence, but the larger sample size (compared to earlier picamilon trials) and multicenter setting add some generalizability. The result is consistent with earlier smaller studies suggesting picamilon has modest cerebrovascular and cognitive effects.
picamilon-SRC-004Open cohort clinical study.
Sourceopen_in_newDanilov AB, Shindryaeva NN, Borodulina IV, Lunegov TD, Kristeleva DA. Clinical efficacy and safety of Picamilon in patients with progressive chronic cerebral ischemia. Zh Nevrol Psikhiatr Im S S Korsakova. 2024;124(8):71-80. doi:10.17116/jnevro202412408171. PMID:39269299.
Population: Adults aged 51 to 69 years with stage II chronic cerebral ischemia.
Dose protocol: 200 mg IV x10 days then 50 mg orally TID x60 days in 50 patients with stage II chronic cerebral ischemia
Key findings: MoCA improved from 20.9 to 25.9. Sleep normalized in 81%, neurological improvement in 84%.
Notes: Open-label uncontrolled design. First data on stage II (more advanced) cerebral ischemia specifically.
Paper content
This open-label cohort study evaluated picamilon in 50 patients (mean age 62 years) with stage II chronic cerebral ischemia using a step-therapy protocol (200 mg IV for 10 days followed by 50 mg orally three times daily for 60 days). MoCA scores improved meaningfully from 20.9 to 25.9 across the treatment period. Sleep normalized in 81% and neurological function improved in 84% of patients, with 92% showing a favorable safety profile. The lack of a control group and open-label design are significant limitations, but the study provides the first data specifically on stage II (more advanced) chronic cerebral ischemia and confirms the dosing protocol used in practice.