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Cyclosporine information from DrugsUpdate  

See Available Brands of Cyclosporine in India

Cyclosporine, an immunosuppressant drug is prescribed to prevent graft-rejection reactions (GVHD) following allogenic tissue or organ transplantation. The drug prevents organ rejections after liver, kidney and heart transplantations. Cyclosporine is also prescribed for the treatment of severe form of rheumatoid arthritis and psoriasis.

Pharmacodynamics

Cyclosporine suppresses humoral immunity and also the cell-mediated immune reactions including graft rejection reactions and delayed-type hypersensitivity (dTH). The drug reversibly inhibits formation of immuncompetent lymphocytes (T-lymphocytes and T-suppressor cells) in the G0 or G1 phase of the cell cycle However, the exact pharmacodynamics of cyclosporine is not known. Cyclosporine also inhibits biosynthesis of lymphokines including T-cell growth factor and interleukin-2.

Pharmacokinetics

Cyclosporine absorption via GIT is incomplete and inpredictable. Cmax of cyclosporine is about 3.5 hours. Upon increase in dosage, Cmax and AUC increase in a curvilinear fashion. The distribution of the drug is largely outside the blood. At higher drug concentrations, the leukocytic and erythrocytic uptake is saturated. The drug is mostly bound (90%) to plasma lipoproteins.
The terminal half-life of cyclosporine is 19 hours with biphasic disposition. The drug is eliminated via bile with just 6% excretion via urine. Cyclosporine is metabolized into 15 major metabolites. Only 0.1% of the administered dose is excreted via urine.

Cyclosporine Indications / Cyclosporine Uses

No information available

Cyclosporine Adverse Reactions / Cyclosporine Side Effects

The adverse events of Cyclosporine are jaundice-like reactions, vision changes, retro-orbital pain, polydipsia, anuria, tachypnoea, GI problems, myalgia, fever, chills, convulsion, tremors, constipation, numbness and tingling.

Precautions

Cyclosporine is contraindicated in patients with any malignancies, renal disease and hypertension. The dose of cyclosporine should be adjusted in psoriasis patients who are being treated with coal tar, OUVA, radiation, methotrexate and UVB. Avoid contact with direct sunlight, tanning beds and sunlamps.

Special Precautions

No information available

Other Drug Interactions

Cyclosporine may interact with NSAIDs, lithium, other immunosuppressant drugs, St. John’s wort, ACE inhibitors, etoposide, methotrexate, anti-cancer drugs, anti-fungals, meselamine, beta-blockers, repaglinide and anti-viral drugs. Avoid vaccination (live vaccines) while being treated with cyclosporine.

Other Interactions

Avoid consuming grape wine or grape fruit. It may cause serious adverse events due to impaired cyclosporine metabolism.

Dosage

Start with an initial, single dose of 15 mg/kg, 4-12 hours prior to transplantation procedure. After surgery, the dose should be continued for 1-2 weeks. Then the maintenance dose should be reduced to 5-10 mg/kg/day. In kidney transplanted patients without rejection, the maintenance dose should be 3 mg/kg/day.

Food(before/after)

Cyclosporine can be taken with or without food

List of Contraindications

Cyclosporine and Pregnancy

USFDA pregnancy category C. May be or may not be harmful to an unborn baby. Consult your doctor if you are pregnant or planning to become pregnant during treatment.

Cyclosporine and Lactation

Nursing mothers should consult the healthcare provider before cyclosporine treatment.

Cyclosporine and Children

No information available

Cyclosporine and Geriatic

No information available

Cyclosporine and Other Contraindications

No information available

Storage

No information available

Lab interference

No information available

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