Drilldown: Medicines

Cyclosporine (ciclosporin) (1)

Sandimmune, Neoral (modified microemulsion, increased bioavailability), Gengraf, Restasis (ophthalmic) (1)

[[:Category:Calcineurin_inhibitors|Calcineurin inhibitor]] (1) · [[:Category:Immunosuppressants|Immunosuppressant]] (1)

None (1)

'"`UNIQ--vote-00000A8C-QINU`"', '"`UNIQ--vote-00000A8D-QINU`"', '"`UNIQ--vote-00000A8E-QINU`"', '"`UNIQ--vote-00000A8F-QINU`"', '"`UNIQ--vote-00000A90-QINU`"' (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)

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)

Transplant: regimen-specific (1)

None · Oral · IV · topical · IM · intranasal · rectal · Subcutaneous · Topical ophthalmic · ophthalmic · intramuscular · intravenous · transdermal · vaginal · Subcutaneous (abdomen · sublingual · thigh · inhaled · intra-articular · nebulized

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Days for immunosuppressive effect (1)

Dosing-frequency dependent (1)

None · ~12 hours · ~27 days · ~5 h (caffeine) · '''Autoinduction''': 25-65 hours initially, falling to 12-17 hours after 2-3 weeks of dosing as carbamazepine induces its own CYP3A4 metabolism. Major clinical implication: doses require re-titration after the autoinduction period'"`UNIQ--ref-0000001D-QINU`"' · 0.5-1.5 hours (plasma); pharmacodynamic effect persists 24+ hours'"`UNIQ--ref-000000DE-QINU`"' · 1-1.3 hours'"`UNIQ--ref-000001A1-QINU`"' · 1-1.5 hours'"`UNIQ--ref-00000DE3-QINU`"' · 1-2 hours (parent compound)'"`UNIQ--ref-00000029-QINU`"' · 1-2 hours (parent); 18-30 hours for active metabolite oxypurinol'"`UNIQ--ref-0000030F-QINU`"' · 1-2 hours'"`UNIQ--ref-00000017-QINU`"' · 1-3 hours (normal liver); markedly prolonged in overdose with glutathione depletion'"`UNIQ--ref-000006A5-QINU`"' · 1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' · 1.4 hours (parent); 13-24 hours for active metabolite canrenone'"`UNIQ--ref-00000354-QINU`"' · 1.5-2 hours (longer in renal failure)'"`UNIQ--ref-00000222-QINU`"' · 1.5-2 hours'"`UNIQ--ref-00000020-QINU`"' · 10-11 hours (benazeprilat, the active metabolite)'"`UNIQ--ref-00000A22-QINU`"' · 11-13 h (immediate-release); 11-16 h (extended-release) · 11-15 hours'"`UNIQ--ref-00000842-QINU`"' · 12-15 hours (intermediate); '''no active metabolites''' (key clinical feature)'"`UNIQ--ref-00000023-QINU`"'

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Sandimmune: highly variable (~30%); Neoral microemulsion: ~50%, less variable; '''Sandimmune and Neoral are NOT bioequivalent and not interchangeable''''"`UNIQ--ref-00000A92-QINU`"' (1)

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. Carries '''Boxed Warning''' for risk of malignancy and serious infection; nephrotoxicity, hypertension, and immunosuppression-associated complications'"`UNIQ--ref-00000A93-QINU`"' (1)