AICAR

01 / Dosing schedule

Cited dosing

AICAR is not a peptide and has no approved human product; the human dosing that exists is acute intravenous infusion in small metabolic pharmacology studies, not chronic dosing. Verified figures are 0.75 mg/kg/min IV and, in an earlier cited study, 10 mg/kg/h IV for 3 hours.

AICAR intravenous infusion — human metabolic studies

Phase	Dose & frequency
Infusion rate (Boon et al.)	0.75 mg/kg/min continuous IV, stated in the Discussion as equivalent to 45 mg/kg/h
Control infusion	0.9% NaCl IV
Earlier human study cited (Cuthbertson et al.)	10 mg/kg/h AICAR infusion for 3 h in young healthy males
Design	two experimental tests per volunteer (AICAR vs saline), randomised order, at least 2 weeks apart
Repeat / chronic dosing	n.a. — no chronic human dosing regimen was confirmed from a primary source
Oral or subcutaneous dosing	n.a. — no oral or subQ human dose was confirmed from a primary source

Source · Boon H, Bosselaar M, Praet SFE, et al. Intravenous AICAR administration reduces hepatic glucose output and inhibits whole body lipolysis in type 2 diabetic patients. Diabetologia. 2008;51:1893-1900. ↗

Source indication · Acute metabolic pharmacology — hepatic glucose output and lipolysis during IV AICAR infusion in type 2 diabetes / healthy volunteers

Injection frequency: Acute, single-session infusion in the published human studies. There is no published repeated-dose or multi-week human AICAR schedule.
Injection sites: Not an injection protocol: AICAR was given as a continuous intravenous infusion, with blood sampled by venepuncture from the arm opposite the infusion. No subcutaneous site exists in the human record.

02 / Reconstitution

Reconstitution reference

The human studies infused AICAR intravenously in a clinical research setting alongside 0.9% NaCl; no participant-level reconstitution procedure is published, and no vial strength is given.

Vialn.a. — no vial presentation in the human literature fetched

BAC watern.a.

Concentrationn.a.

Example dose0.75 mg/kg/min IV (45 mg/kg/h)

On a U‑100 syringeweight- and time-based infusion rate, not a bolus dose

Open the reconstitution calculator →

03 / Overview

Protocol overview

AICAR (acadesine) is a nucleoside AMP mimetic that is phosphorylated intracellularly to ZMP and activates AMPK. It is a small molecule, not a peptide, and it has never been approved for a metabolic or performance indication.

The clearest human dosing data comes from a randomised crossover metabolic study in which each volunteer completed one test with continuous IV AICAR at 0.75 mg/kg/min and one with 0.9% NaCl, at least two weeks apart, with stable-isotope glucose and palmitate tracers to quantify hepatic glucose output and lipolysis.

That paper explicitly restates the dose as 45 mg/kg/h and cites an earlier human study by Cuthbertson and colleagues that infused AICAR at 10 mg/kg/h for 3 hours in young healthy males, giving a documented human range of roughly 10-45 mg/kg/h by IV infusion. A pharmacology review of AICAR tabulates the wider human trial record, which is dominated by continuous IV acadesine in cardiac surgery (for example 0.1 mg/kg/min for 7 h) and by oncology dosing (single IV doses of 50-315 mg/kg in relapsed CLL), plus 10, 25, 50 and 100 mg/kg oral and IV doses in 1991 healthy-volunteer work. None of that is a chronic outpatient regimen.

AICAR is also a WADA-prohibited substance. This record is flagged 'limited' because the human evidence is acute infusion pharmacology and surgical/oncology dosing, not therapeutic trials of the use it is marketed for. There is no published chronic subcutaneous or oral regimen and no human half-life in the fetched sources.

04 / References