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Cyclosporine

Oral
Intravenous
Ophthalmic
Class
Immunophilin ligands
Subclass
Calcineurin inhibitors
Generic name
Cyclosporine, cyclosporin, ciclosporin
Brand names
Neoral®, Sandimmune®, Verkazia®, Vevye®
Common formulations
Capsule, Oral solution
Dosage and administration
Adults patients
Atopic dermatitis • Moderate-to-severe • Off-label
•
3-5 mg/kg PO daily for up to 1 year
Myasthenia gravis • Off-label
•
5 mg/kg PO daily, in 2 divided doses
Plaque psoriasis • Off-label
•
2.5-5 mg/kg PO daily, in 2 divided doses
Other off-label uses
•
Treatment of Behçet's syndrome
•
Treatment of alopecia areata
•
Treatment of aplastic anemia (severe)
•
Treatment of interstitial cystitis
•
Treatment of ulcerative colitis
Indications for use
Labeled indications
Adults
•
Prevention of heart transplant rejection
•
Prevention of kidney transplant rejection
•
Prevention of liver transplant rejection
Off-label indications
Adults
•
Treatment of Behçet's syndrome
•
Treatment of alopecia areata
•
Treatment of aplastic anemia (severe)
•
Treatment of atopic dermatitis (moderate-to-severe)
•
Treatment of interstitial cystitis
•
Treatment of myasthenia gravis
•
Treatment of plaque psoriasis
•
Treatment of ulcerative colitis
Safety risks
Boxed warnings
Malignancy, lymphoma
•
Use extreme caution in patients with high intensity and duration of immunosuppression drugs.
Reactivation of viral infections, polyoma virus infection
•
Use extreme caution in patients with a history of immunosuppressive therapy.
Contraindications
Hypersensitivity to cyclosporine or polyoxyethylated castor oil or any of its components
Warnings and precautions
Cholestasis
•
Use extreme caution in patients with biliary tract disease, jaundice, or have recently received a liver transplant.
Hepatotoxicity, nephrotoxicity
•
Use caution in patients taking high dosage.
Hyperkalemia
•
Use caution in patients using potassium-sparing diuretics.
Neurotoxicity
•
Use caution in adult and pediatric patients receiving cyclosporine, particularly in combination with high-dose methylprednisolone.
Thrombotic microangiopathy
•
Maintain a high level of suspicion as, cyclosporine has been associated with a syndrome of thrombocytopenia and microangiopathic hemolytic anemia which may result in graft failure.
Specific populations
Renal impairment
eGFR 0-90 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required. Monitor complete blood count.
Renal replacement therapy
Continuous renal replacement
•
Use acceptable. No dose adjustment required.
Intermittent hemodialysis
•
Use acceptable. No dose adjustment required.
Peritoneal dialysis
•
Use acceptable. No dose adjustment required.
Hepatic impairment
Child-Pugh A (mild)
•
No guidance available. - For a patient weighing 70 kg, the maximum daily oral dose would deliver about 1 gram of alcohol.
Child-Pugh B (moderate)
•
No guidance available. - For a patient weighing 70 kg, the maximum daily oral dose would deliver about 1 gram of alcohol.
Child-Pugh C (severe)
•
Reduce dose. Monitor serum aminotransferases. Monitor for toxicity. - For a patient weighing 70 kg, the maximum daily oral dose would deliver about 1 gram of alcohol.
Substantial chronic alcohol consumption
•
Reduce dose. - For a patient weighing 70 kg, the maximum daily oral dose would deliver about 1 gram of alcohol.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: C
•
Use only if benefits outweigh potential risks. Evidence of fetal harm in humans. Enroll patients in a dedicated pregnancy outcome monitoring registry. Some formulations of this drug contain ethanol or methanol which should be taken into consideration if it is taken by a pregnant woman.
•
Women of childbearing potential should be appraised of the potential risk to the developing fetus.
•
This drug may cause immunosuppression in the infant.
Breastfeeding
Acceptable for use during breastfeeding.
Low excretion in breastmilk (5-25%).
Very low levels in breastfed infants (< 5%).
Unlikely to cause adverse effects in breastfed infants.
Adverse reactions
Very common > 10%
•
Hirsutism, hypertension, hypertrichosis, ↑ serum triglycerides, abdominal pain, diarrhea, dyspepsia, eye pain, headache, muscle cramps, nausea, paresthesia, skin rash, tremor, rhinitis
Common 1-10%
•
Acne vulgaris, anemia, angioedema, arthropathy, blepharitis, bone fracture, bronchospasm, cataract, conjunctival injection, conjunctivitis, ↓ WBC count, ↓ blood glucose, ↓ serum magnesium, diabetes mellitus, dysgeusia, esophagitis, folliculitis, gastritis, gingivitis, glossitis, goiter, gynecomastia, heart failure, ↑ blood glucose, ↑ liver enzymes, ↑ serum TBIL, ↑ serum cholesterol, ↑ serum potassium, ↑ serum uric acid, influenza virus infection, leukorrhea, lymphadenopathy, lymphoma, migraine, myocardial infarction, peptic ulcer disease, peripheral neuropathy, pharyngitis, psoriasis, purpura, anxiety, arthralgia, asthenia, blurred vision, chest pain, confusion, constipation, cough, ↓ libido, depression, dizziness, dry mouth, dysphagia, dyspnea, dysuria, emotional lability, euphoria, fatigue, fever, flatulence, hair loss, hearing loss, hematuria, hiccups, hot flashes, hypoesthesia, ↑ appetite, ↑ libido, insomnia, itching, itchy eyes, loss of appetite, malaise, menstrual irregularity, musculoskeletal pain, myalgia, nocturia, nosebleed, polyuria, seizure, skin flushing, somnolence, tinnitus, urinary frequency, urinary incontinence, urinary urgency, vertigo, vertigo, vomiting, weight gain, weight loss, sinusitis, skin cancer, skin dryness, skin ulceration, stomatitis, urticaria
Unknown frequency
•
Acute liver failure, acute respiratory distress syndrome, acute pancreatitis, ataxia, cholestasis, ↓ platelet count, encephalopathy, gastrointestinal bleeding, gout, hemolytic uremic syndrome, hemolytic anemia, hyperesthesia, hyperprolactinemia, ↑ BUN, jaundice, lethargy, leukoencephalopathy, metabolic acidosis, papilledema, pulmonary edema, renal tubular necrosis, dysarthria, infertility, night sweats, visual disturbances, weakness, sinus tachycardia, thrombosis, wheezing
Interactions
Drug(s)
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