Drilldown: Medicines

Cyclosporine (ciclosporin) (1) · Lovastatin (1) · Pravastatin (1) · Simvastatin (1)

Altoprev (ER), Mevacor (discontinued US); mostly generic (1) · Pravachol (1) · Sandimmune, Neoral (modified microemulsion, increased bioavailability), Gengraf, Restasis (ophthalmic) (1) · Zocor (1)

[[:Category:Calcineurin_inhibitors|Calcineurin inhibitor]] (1) · [[:Category:Immunosuppressants|Immunosuppressant]] (1) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (3) · [[:Category:Statins|Statin]] (3)

None (3) · '"`UNIQ--vote-000003D1-QINU`"' SLCO1B1 polymorphism affects exposure but is most clinically actionable for simvastatin'"`UNIQ--ref-000003D2-QINU`"'. (1)

'"`UNIQ--vote-00000178-QINU`"', '"`UNIQ--vote-00000179-QINU`"' (1) · '"`UNIQ--vote-000003D3-QINU`"', '"`UNIQ--vote-000003D4-QINU`"' (1) · '"`UNIQ--vote-00000805-QINU`"', '"`UNIQ--vote-00000806-QINU`"' (1) · '"`UNIQ--vote-00000A8C-QINU`"', '"`UNIQ--vote-00000A8D-QINU`"', '"`UNIQ--vote-00000A8E-QINU`"', '"`UNIQ--vote-00000A8F-QINU`"', '"`UNIQ--vote-00000A90-QINU`"' (1)

10-20 mg PO once daily in the evening (40 mg starting allowed for high CV risk) (1) · 20 mg PO once daily with the evening meal; titrate to 40-80 mg/d (1) · 40 mg PO once daily (10-20 mg in elderly, hepatic impairment, or strong drug interactions) (1) · Transplant: 5-10 mg/kg/d divided BID, titrated to trough levels (typically 100-300 ng/mL depending on regimen and post-transplant interval); ophthalmic Restasis 0.05% one drop BID (1)

10 mg, 20 mg, 40 mg, 80 mg tablets (1) · 10, 20, 40 mg tablets; 20, 40, 60 mg ER tablets (1) · 5, 10, 20, 40, 80 mg tablets; 4 mg/mL oral suspension (1) · Sandimmune 25, 100 mg capsules; Neoral 25, 100 mg modified soft gel; 100 mg/mL oral solution; 50 mg/mL IV; Restasis 0.05% ophthalmic emulsion (1)

40 mg/d standard; 80 mg/d restricted to patients tolerating 80 mg for ≥12 months without myopathy (post-SEARCH 2011 FDA restriction) (1) · 80 mg/d (1) · 80 mg/d (40 mg/d if combined with diltiazem, verapamil, danazol; lower limits with various interactions) (1) · Transplant: regimen-specific (1)

IV (1) · ophthalmic (1) · Oral (4)

None · Hours · 30-60 minutes · 1-2 hours · ~30 min · LDL lowering at 2 weeks, max by 4 weeks · ~1 hour · 15-30 minutes · 15–30 min · 1–2 h · 30–60 min · Antidepressant effect emerges over 1-2 weeks · BP and symptomatic LUTS improvement within 1-2 weeks · BP effect within 1-2 weeks · Clinical improvement within 24-72 hours · Days · Motor improvement over days at therapeutic dose · Over weeks · Postprandial glucose effect within days; HbA1c by 12 weeks · Sleep effect from first dose; antidepressant effect over 1-4 weeks

Other values:

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24 hours (2) · 24 hours (evening dosing aligns with overnight HMG-CoA reductase peak) (1) · Dosing-frequency dependent (1)

~2 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect lasts 24 hours via target turnover'"`UNIQ--ref-0000017A-QINU`"' (1) · ~2-3 hours (parent); pharmacodynamic effect 24 hours via target turnover'"`UNIQ--ref-000003D5-QINU`"' (1) · ~2-4 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect 24 hours via target turnover'"`UNIQ--ref-00000807-QINU`"' (1) · ~8-27 hours (highly variable across the population)'"`UNIQ--ref-00000A91-QINU`"' (1)

<5% (extensive hepatic first-pass; food enhances absorption of IR, hence the evening-meal dosing)'"`UNIQ--ref-00000808-QINU`"' (1) · <5% (extensive hepatic first-pass; statin pharmacology is hepatocellular, not systemic)'"`UNIQ--ref-0000017B-QINU`"' (1) · Sandimmune: highly variable (~30%); Neoral microemulsion: ~50%, less variable; '''Sandimmune and Neoral are NOT bioequivalent and not interchangeable''''"`UNIQ--ref-00000A92-QINU`"' (1) · ~17% (oral; food slightly reduces absorption)'"`UNIQ--ref-000003D6-QINU`"' (1)

Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (3) · Used in transplant pregnancy when continued immunosuppression is required; reassuring data overall but careful monitoring needed.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

[[USLegal:Prescription only|Rx-only]] in US (3) · [[USLegal:Prescription only|Rx-only]] in US. Carries '''Boxed Warning''' for risk of malignancy and serious infection; nephrotoxicity, hypertension, and immunosuppression-associated complications'"`UNIQ--ref-00000A93-QINU`"' (1)