Ezetimibe
Ezetimibe is a cholesterol-absorption inhibitor that lowers LDL by blocking intestinal uptake of dietary and biliary cholesterol. PED users use it, often alongside or instead of a statin, to counter the LDL rise driven by anabolic steroids, particularly harsh orals. It has solid clinical trial data, including cardiovascular outcome benefit when added to statin therapy.
01 Overview
Ezetimibe acts on the NPC1L1 transporter in the small intestine, reducing cholesterol absorption and prompting the liver to up-regulate LDL receptors and clear more LDL from the blood. As monotherapy it lowers LDL by roughly 15-20%; added to a statin it produces further reductions and, in the IMPROVE-IT trial, modestly improved cardiovascular outcomes.
Because its mechanism is independent of the liver-based HMG-CoA pathway, PED users sometimes prefer it where they wish to avoid or minimise statin dosing, or combine it with a low statin dose to control steroid-driven LDL. It is generally well tolerated, with a low incidence of the myalgia that troubles some statin users.
02 Mechanism
Inhibits the intestinal NPC1L1 sterol transporter, reducing absorption of dietary and biliary cholesterol; the liver responds by up-regulating LDL receptors and clearing more circulating LDL.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| On-cycle LDL control | 10 mg/day | Oral | Used to blunt steroid-driven LDL rise, often with a low statin dose. |
| Hyperlipidaemia (label) | 10 mg/day | Oral | Single fixed 10 mg once-daily dose, alone or with a statin. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Reduced LDL cholesterolLowers LDL by blocking intestinal cholesterol absorption; additive to statins. | -15 to -20% mono; more with statin | Clinical | |
| Cardiovascular outcome benefitAdded to statin therapy it modestly reduced cardiovascular events in high-risk patients. | modest (IMPROVE-IT) | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| MyalgiaMuscle aches, less frequent than with statins. | Mild | Uncommon | Clinical | |
| Transaminase elevationSmall rises in liver enzymes, more likely combined with a statin. | Mild | Uncommon | Clinical |