Drug reference

Cyclosporine

Immunosuppressant

Also known as Cyclosporin A

Immunosuppressant

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

—

not curated

Top interactionssee all 12 →

RosuvastatinContraindicatedDatabaseKimi deep-research + Cla
SimvastatinContraindicatedDatabaseDDInter
AtazanavirSevereTextbook-citedKDT 7e · p948
ClarithromycinSevereTextbook-citedKDT 7e · p948

Mechanism

Cyclosporine is a substrate for both the CYP3A4 enzyme and the MDR1 (ABCB1) transporter. It inhibits the transport function of BSEP (ABCB11) at clinically relevant concentrations, which can disrupt bile formation.

Indications

Prevention of transplant rejectiontransplant rejection prophylaxistransplant rejection rescue therapyrheumatoid arthritispsoriasis and other skin diseasesxerophthalmiaspecific clinical settings in severe IBDfistulous complications of Crohn’s diseasechronic dry eye associated with inflammationmyasthenia gravis (advanced cases, inhibits NR-antibody synthesis)Interstitial Cystitis/Bladder Pain Syndrome (refractory to standard therapies)IC/BPS with Hunner lesionssevere recalcitrant Atopic Dermatitis (approved in some European countries)severe psoriasis

Dosing

Adult: 4Target area under the concentrationtime curve after a single dose. 5Can be estimated from measured C using CL = V max/(Km + C); Vmax = 415 mg/d, Km = 5 mg/L. See text. 6Varies because of concentrationdependent clearance. 7Bound in whole blood (%). 8Based on whole blood standardized to hematocrit 45%.…

Pharmacokinetics

Onset

Relatively quick (in 1–2 months)

Half-life

Biphasic, with the terminal phase being about 9 to 18 h.

Bioavailability

Intestinal absorption is mainly related to MDR1 levels.

Protein binding

Following absorption, 90% to 98% is bound to serum lipoproteins.

Metabolism

Metabolized via CYP3A4.

Excretion

Not specified directly, but metabolism and protein binding are mentioned.

Side effects

Common

tremordrowsinessnephrotoxicityhypertensionhirsutismhyperlipidemiagum hyperplasia

Serious

Drug-induced cholestasis (disruption of bile formation)
hallucinations
coma
increased susceptibility to infections
renal insufficiency
hypertension
seizures
peripheral neuropathy
nephrotoxicity
renal dysfunction
hyperkalemia
hyperuricemia
hypomagnesemia
hyperlipidemia
increased risk of malignancies
pulmonary toxicity
increased incidence of skin cancer
secondary infections

Drug interactions

Rosuvastatin

Contraindicated

Database

Cyclosporine increases rosuvastatin plasma levels 7-11 fold via OATP1B1 inhibition; high myopathy risk

Contraindicated combination

Source: Kimi deep-research + Cla

Simvastatin

Contraindicated

Database

Increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy. For simvastatin, coadministration is contraindicated.

Source: DDInter

Atazanavir

Severe

Textbook-cited

Nephrotoxicity and immunosuppression toxicity

Monitor cyclosporine levels and reduce dose

Source: KDT 7e · p948

Clarithromycin

Severe

Textbook-cited

Nephrotoxicity and immunosuppression toxicity.

Monitor cyclosporine levels and reduce dose