Key facts about cholesterol medications
- Lipid-lowering therapy reduces cardiovascular events by targeting LDL, triglycerides, and inflammation.
- Statins are first-line for most patients; additional agents are layered on when targets are not met or intolerance occurs.
- Regular lipid monitoring and adherence are crucial because benefits accumulate over years of consistent use.
Medications that modify cholesterol levels range from daily tablets to injectable biologics. Selecting the right combination depends on cardiovascular risk, baseline lipid profile, tolerability, and other health factors. This guide summarises evidence-backed options, dosing considerations, and safety checks to discuss with your care team.
Statins: foundation therapy
| Medicine | Typical daily dose range | LDL reduction (approx.) | Special notes |
|---|---|---|---|
| Rosuvastatin | 5 to 40 mg | 45% to 63% | Potent at lower doses; adjust in renal impairment and Asian populations |
| Atorvastatin | 10 to 80 mg | 38% to 55% | Long half-life allows flexible dosing; monitor for drug interactions |
| Simvastatin | 10 to 40 mg | 27% to 41% | Higher interaction profile; avoid 80 mg dose due to myopathy risk |
| Pravastatin | 10 to 40 mg | 20% to 34% | Hydrophilic; fewer drug interactions, useful for combination therapy |
Add-on oral therapies
| Class | Examples | LDL/TG impact | Ideal candidates | Key cautions |
|---|---|---|---|---|
| Ezetimibe | Ezetimibe 10 mg daily | Additional 18% to 25% LDL reduction | Patients needing further LDL lowering without major side effects | Monitor liver enzymes when combined with statins |
| Bempedoic acid | 180 mg daily | 15% to 20% LDL reduction | Statin-intolerant individuals or those needing extra lowering | Can increase uric acid; watch for tendon pain |
| Fibrates | Fenofibrate, gemfibrozil | 20% to 50% TG reduction, mild HDL increase | Severe hypertriglyceridaemia or persistent high TG with low HDL | Assess renal function; gemfibrozil plus statin raises myopathy risk |
| Niacin | Extended-release niacin | Improves HDL, lowers TG | Limited use today; consider when other options unsuitable | Flushing common; monitor liver enzymes and glucose |
Injectable options
| Therapy | Dosing | Effect | Best suited for | Monitoring |
|---|---|---|---|---|
| PCSK9 inhibitors (evolocumab, alirocumab) | Subcutaneous every 2 to 4 weeks | Up to 60% additional LDL reduction | Familial hypercholesterolaemia, very high-risk ASCVD patients | Lipid panels to confirm response, injection site reactions |
| Inclisiran (siRNA) | Day 0, 3 months, then every 6 months | ~50% LDL reduction | Patients needing infrequent dosing with sustained effect | Lipid panels twice yearly, monitor for injection site reactions |
| Icosapent ethyl | 2 g twice daily with food | Reduces triglycerides and cardiovascular events | Elevated TG (≥ 1.5 mmol/L) despite statins | Monitor TG levels and bleeding risk when on anticoagulants |
Setting LDL targets
- Very high-risk (established ASCVD, familial hypercholesterolaemia): aim for LDL < 1.4 mmol/L and ≥ 50% reduction from baseline.
- High-risk (diabetes with organ damage, severe CKD): aim for LDL < 1.8 mmol/L.
- Moderate-risk: target LDL < 2.6 mmol/L and non-HDL < 3.4 mmol/L.
- Use non-HDL cholesterol or apolipoprotein B as secondary targets when triglycerides are high.
Monitoring plan
| Interval | Key checks | Why it matters |
|---|---|---|
| Baseline | Lipid panel, liver enzymes, creatine kinase (if high myopathy risk) | Establish starting point and safety parameters |
| 6 to 12 weeks after initiation or dose change | Lipid panel, liver enzymes if on statins/ezetimibe | Assess response and tolerance |
| Every 6 to 12 months | Lipid panel, review adherence, assess lifestyle measures | Maintain long-term control and adjust therapy as needed |
Managing side effects
- Muscle symptoms: Verify other causes (exercise, hypothyroidism). Consider lowering statin dose, switching to a hydrophilic statin, or intermittent dosing.
- Liver enzyme elevations: Mild increases are common; discontinue if ALT/AST exceed three times upper limit with symptoms.
- Hyperglycaemia: Statins may slightly raise glucose; monitor HbA1c in diabetes or pre-diabetes.
- Injection site reactions: Rotate sites and allow medication to reach room temperature before administering.
Drug interactions
- CYP3A4 inhibitors (e.g., clarithromycin, certain antifungals) raise levels of simvastatin and atorvastatin; consider dosage adjustment or alternative statin.
- Fibrates, particularly gemfibrozil, increase risk of statin-associated myopathy—prefer fenofibrate when combination therapy is required.
- Grapefruit juice can elevate statin concentrations; limit intake with lovastatin, simvastatin, or atorvastatin.
- Warfarin anticoagulation can be potentiated by statins or fibrates; monitor INR closely after changes.
Frequently asked questions
What if I forget a statin dose?
Take it as soon as remembered on the same day. If the next dose is due, skip the missed tablet and resume the regular schedule.
Can supplements replace statins?
Red yeast rice or omega-3 products may modestly affect lipids but do not replicate the cardiovascular outcome benefits of prescription therapy. Discuss supplement use alongside standard care.
How soon should cholesterol levels improve?
Most statins reach full effect within 4 to 6 weeks. Persistent elevation after adherence confirmation may warrant dose adjustment or add-on therapy.
Are statins safe long term?
Large studies show sustained cardiovascular benefit with acceptable safety profiles over decades. Regular monitoring helps catch rare complications early.
