AICAR

Compound Profile

AICAR is reviewed here for cellular energy, stamina, and recovery.

Research Summary

Evidence Strength Moderate

Primary Evidence

Human studies, published literature, supporting research

Research Focus

Cellular energy, Stamina, Recovery

Mechanism

Target context: AMPK

Long-Term Data

Human data exists, but longer-term context is still developing.

Current Consensus

Human research exists, but confidence depends on product, dose, and population.

Route(s) Subcutaneous

Typical dose 10mg to 25mg

Dosing window Pre-Workout

Receptor / target AMPK

Properties Not listed

Pre-mixed No

Protocols

Protocol logic check

Medical literature and study context

Independent evidence

Regulatory status: no approved label identified

Storage

No approved-label storage guidance was identified for this entry. Use conservative sterile handling and see the general storage guidance in the FAQ.

Contraindications & cautions

Evidence varies by item. Some points come from labels, published literature, or regulatory context; others are mechanism-based cautions that still need confirmation against medical literature. Use the medical sources below to verify details.

• Cardiovascular instability or active cardiac arrhythmia: AICAR affects cardiac adenosine metabolism and can influence heart rate and rhythm; contraindicated in subjects with unstable cardiac conditions.
• Insulin therapy or sulfonylurea use without clinical supervision: AICAR's GLUT4 upregulation and glucose uptake enhancement creates additive hypoglycemia risk with insulin or insulin secretagogues.
• Metformin use: both AICAR and metformin activate AMPK; overlapping activation intensifies the glucose-lowering and metabolic effects; monitor closely.
• Gout or hyperuricemia: AICAR increases uric acid levels through purine catabolism pathway modulation; in subjects with gout, elevated baseline uric acid, or reduced renal uric acid clearance, AICAR may precipitate gout flares.
• Renal impairment: AICAR and its metabolites are renally cleared; impaired elimination may cause accumulation and exaggerated pharmacological effects.
• Active malignancy: AMPK activation has complex effects in cancer metabolism; AICAR's anti-proliferative effects have been noted in some cancer models, but its metabolic support of oxidative phosphorylation in other tumor types is not fully characterized.
• Athletes competing under WADA anti-doping regulations: AICAR is explicitly listed on the WADA Prohibited List as an AMPK activator.
• Known hypersensitivity to AICAR or nucleoside analog compounds.
• Pregnancy: purine metabolism alteration is not established as safe in fetal development.
• Breastfeeding: no safety data.
• Severe hepatic impairment: AICAR metabolism and the downstream purine synthesis pathway changes may be unpredictable with impaired hepatic function.

Possible side effects

Evidence varies by item. Some points come from labels, published literature, or regulatory context; others are mechanism-based cautions that still need confirmation against medical literature. Use the medical sources below to verify details.

• Hypoglycemia: the most significant acute adverse effect; AICAR drives aggressive glucose uptake via GLUT4 in muscle tissue; risk is highest when dosed fasted without planned exercise; always pre-workout, always with subsequent energy expenditure.
• Severe lethargy post-clearance: as AICAR washes out, the metabolic state driven by ZMP-induced AMPK activation resolves; a crash-like fatigue episode is reported by a majority of users after the dose clears, particularly with higher doses; this is a direct pharmacological consequence of the metabolic demand AICAR imposed.
• Elevated uric acid (hyperuricemia): a well-characterized adverse effect from clinical cardiology data; AICAR increases purine catabolism through its adenosine mechanism, elevating urate production; particularly relevant in subjects predisposed to gout.
• Headache: commonly reported; possibly related to adenosine system activity and cerebral vasodilation effects.
• Nausea: reported in clinical trial data at higher doses; dose-related.
• Injection site irritation: redness, swelling, pain at subcutaneous injection site; the large doses required (10-25mg) mean larger injection volumes than most peptides.
• Cardiac rhythm effects: AICAR modulates cardiac adenosine signaling, which has electrophysiological implications; generally mild at research doses but warrants monitoring in subjects with pre-existing arrhythmias.
• Fatigue and muscle soreness: reported during the active dosing window as the metabolic program shifts; paradoxical given the "exercise mimetic" characterization but consistent with the metabolic reorganization.
• Potential AMPK overstimulation impacting muscle protein synthesis: sustained mTOR suppression from prolonged AICAR use may impair muscle hypertrophy signaling; this is the mechanistic basis for the strict 4-week maximum cycle length.
• Lactic acid accumulation at high doses: theoretical; AICAR at very high doses can saturate oxidative phosphorylation pathways and shift toward glycolytic energy production with lactate production.

Compatibility

The relationships below are heuristic compatibility notes and were not independently verified. Treat them as a starting point for a conversation with a clinician. They carry no safety guarantee.

Reported synergistic:

Reported contraindicated combinations:

None listed.

Sources

• FDA drug/regulatory guidance
• PubMed literature search: AICAR
• ClinicalTrials.gov study records: AICAR