Cyclosporine

Sandimmune, Neoral, Gengraf, Optimmune, Cequa, Cyclavance, Verkazia, Vevye, Sporimune, Modulis, Restasis, Atopica

Immunosuppressant • Calcineurin inhibitor

Premium

NTIHepatotoxicNephrotoxic

Half-life

8-27 hours

Protein Binding

90%

Metabolized By

CYP3A4

External

Drugs.com

Boxed warning

Increased susceptibility to infection and malignancy
Nephrotoxicity
Hypertension

Clinical alerts

Boxed warning

3 boxed warnings

Narrow therapeutic index

Small dose changes can cause toxicity or loss of effect

Nephrotoxic

Monitor renal function; avoid other nephrotoxins where possible

Hepatotoxic

Monitor liver function

Mechanism of action

Binds to cyclophilin, inhibiting calcineurin and preventing T-cell activation

Recorded indications

From the drug index — may include conditions studied rather than approved indications

·Atopic Dermatitis
·Nephrotic Syndrome
·Proteinuria
·Autoimmune Disease
·Glomerular Disease

Monitoring

Therapeutic range: 100–400 ng/mL; C0 trough; varies by time post-transplant

Interactions

1 curated · 1 major or contraindicated · select a row for management

Interacting drug	Severity	Effect
atorvastatin	major	High risk of myopathy and rhabdomyolysis

Common adverse effects

Nephrotoxicity
Hypertension
Tremor
Hirsutism
Gingival hyperplasia

Food, alcohol & herbal

Food

Grapefruit increases levels — AVOID
Take consistently with meals

Alcohol · moderate

May increase toxicity

Herbal

St. John's Wort (major) — Reduces cyclosporine levels — organ rejection risk

Pharmacokinetics

Published parameters · PMID:12093357

Half-life: 8-27 hours
Protein binding: 90%
Metabolised by: CYP3A4
Inhibits: CYP3A4, P-gp
Clearance: 30 L/h; adult renal transplant recipients
Volume of distribution: 200 L
Bioavailability: 30%
Renally eliminated: 6%
Model: 2-compartment

Pregnancy & lactation

Not recorded for Cyclosporine. Absence here means this database does not hold a category — not that the drug is safe in pregnancy or breastfeeding.

Sources

Assembled from: drug index, curated drug database, curated interaction pairs, published PK literature.

Not a substitute for clinical judgement

Cyclosporine

Sandimmune, Neoral, Gengraf, Optimmune, Cequa, Cyclavance, Verkazia, Vevye, Sporimune, Modulis, Restasis, Atopica

Immunosuppressant • Calcineurin inhibitor

Premium

NTIHepatotoxicNephrotoxic

Half-life

8-27 hours

Protein Binding

90%

Metabolized By

CYP3A4

External

Drugs.com

Boxed warning

Increased susceptibility to infection and malignancy
Nephrotoxicity
Hypertension

Clinical alerts

Boxed warning

3 boxed warnings

Narrow therapeutic index

Small dose changes can cause toxicity or loss of effect

Nephrotoxic

Monitor renal function; avoid other nephrotoxins where possible

Hepatotoxic

Monitor liver function

Mechanism of action

Binds to cyclophilin, inhibiting calcineurin and preventing T-cell activation

Recorded indications

From the drug index — may include conditions studied rather than approved indications

·Atopic Dermatitis
·Nephrotic Syndrome
·Proteinuria
·Autoimmune Disease
·Glomerular Disease

Monitoring

Therapeutic range: 100–400 ng/mL; C0 trough; varies by time post-transplant

Interactions

1 curated · 1 major or contraindicated · select a row for management

Interacting drug	Severity	Effect
atorvastatin	major	High risk of myopathy and rhabdomyolysis

Common adverse effects

Nephrotoxicity
Hypertension
Tremor
Hirsutism
Gingival hyperplasia

Food, alcohol & herbal

Food

Grapefruit increases levels — AVOID
Take consistently with meals

Alcohol · moderate

May increase toxicity

Herbal

St. John's Wort (major) — Reduces cyclosporine levels — organ rejection risk

Pharmacokinetics

Published parameters · PMID:12093357

Half-life: 8-27 hours
Protein binding: 90%
Metabolised by: CYP3A4
Inhibits: CYP3A4, P-gp
Clearance: 30 L/h; adult renal transplant recipients
Volume of distribution: 200 L
Bioavailability: 30%
Renally eliminated: 6%
Model: 2-compartment

Pregnancy & lactation

Not recorded for Cyclosporine. Absence here means this database does not hold a category — not that the drug is safe in pregnancy or breastfeeding.

Sources

Assembled from: drug index, curated drug database, curated interaction pairs, published PK literature.

Not a substitute for clinical judgement

Cyclosporine Drug Profile | PharmaGraphX