Atorvastatin
๐ About
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- โฌ๏ธ Reduces LDL & total cholesterol; โฌ๏ธ increases HDL.
- โค๏ธ Proven to reduce MI, stroke, and revascularisation procedures.
- ๐ Taken at night (when cholesterol synthesis is maximal), though atorvastatin has a longer half-life and can be taken any time.
โ๏ธ Action
- ๐ HMG-CoA reductase inhibitor acting on hepatocytes.
- ๐ Blocks the rate-limiting step in cholesterol synthesis.
- โฌ๏ธ Increases hepatic LDL receptor expression โ clears LDL from plasma.
- โฌ๏ธ Lowers LDL, TGs, total cholesterol; modestly โ HDL.
๐ Indications / Dose
- Hypercholesterolaemia, mixed hyperlipidaemia (alongside dietary modification).
- Secondary prevention of CVD (MI, stroke, PAD).
- ๐ Starting dose: 10โ20 mg nocte PO.
- Usual range: 10โ80 mg nocte PO (dose adjusted to cholesterol targets & CVD risk).
- โ ๏ธ Check LFTs before treatment, at 3 months, then annually.
Stop if persistent >3ร ULN.
- ๐ฆต If significant myalgia โ stop drug and check CK.
Discontinue if CK >5ร ULN.
๐ Interactions
- โฌ๏ธ Risk of myopathy with: ciclosporin, erythromycin, clarithromycin, itraconazole, ketoconazole, fibrates.
- โ ๏ธ Myopathy risk โ with macrolides, amiodarone, diltiazem, verapamil.
- ๐ Grapefruit juice (CYP3A4 inhibition) โ โ atorvastatin levels โ avoid.
โ ๏ธ Contraindications
- ๐ซ Active liver disease.
- ๐ซ Pregnancy.
- ๐ซ Breastfeeding.
๐ฅ Side Effects
- ๐ฆต Myalgia, cramps, muscle aches.
- ๐งช Myopathy/rhabdomyolysis (rare, but monitor CK).
- ๐ฝ๏ธ GI upset: diarrhoea, flatulence, abdominal pain.
- ๐ฉบ Elevated LFTs, rare hepatitis or pancreatitis.
- ๐ง Headache, sleep disturbance (less common).
๐ References