Questions and Answers
What is the therapeutic class of cyclosporine?
What is the pharmacologic class of cyclosporine?
What are the actions of cyclosporine?
Complex chemical obtained from a soil fungus, inhibits helper T cells, less toxic to bone marrow cells, often used with high doses of glucocorticoids for transplant patients.
What is one of the primary uses of cyclosporine?
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Neoral and Sandimmune are bioequivalent and can be used interchangeably.
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What is the onset of cyclosporine?
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What are some common adverse effects of cyclosporine?
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Prior hypersensitivity to cyclosporine can be a contraindication for its use.
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Name one drug that may decrease the levels of cyclosporine.
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Match the following effects of cyclosporine with their descriptions:
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Grapefruit juice can raise the levels of cyclosporine significantly.
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What are the trade names of cyclosporine?
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Study Notes
Cyclosporine Overview
- Cyclosporine is classified as an immunosuppressant used to prevent organ rejection after transplants.
- It acts as a calcineurin inhibitor, interrupting T cell activation.
Mechanism of Action
- Derived from a soil fungus, it specifically inhibits helper T cell activity.
- It is less toxic to bone marrow compared to other immunosuppressants.
- Often administered with high doses of glucocorticoids in transplant patients.
Clinical Uses
- Primarily used for prophylaxis against kidney, heart, and liver transplant rejection.
- Also effective in treating psoriasis and xerophthalmia, an eye condition characterized by reduced tear production.
- IV formulation is available for severe cases of ulcerative colitis and Crohn's disease.
Administration Considerations
- Classified as Pregnancy Category C, indicating potential risks during pregnancy.
- Neoral and Sandimmune formulations are not bioequivalent and require careful monitoring if switched.
Pharmacokinetics
- Onset of action: 7 to 14 days.
- Peak plasma levels occur between 3 to 4 hours after administration.
- Half-life ranges from 16 to 27 hours.
- Duration of action is currently unknown.
Adverse Effects
- Renal issues are common, with approximately 75% of patients experiencing diminished urine output.
- Hypertension and tremors affect over 50% of patients, alongside possible headaches, gingival hyperplasia, and elevated liver enzymes.
- Regular blood monitoring is essential to prevent leukopenia (white blood cells under 4,000) and thrombocytopenia (platelets below 75,000).
- Prolonged use increases the risk of malignancies, notably lymphomas and skin cancers.
Contraindications
- Known hypersensitivity to cyclosporine is a direct contraindication.
Drug Interactions
- Certain drugs such as phenytoin, phenobarbital, carbamazepine, and rifampin can lower cyclosporine levels.
- Azole antifungals, ACE inhibitors, NSAIDs, and macrolide antibiotics may elevate cyclosporine levels.
Laboratory Tests
- Cyclosporine usage can raise serum triglycerides and uric acid levels.
- It may lower hepatic enzyme levels and affect urinary function test results.
Herbal and Food Interactions
- Grapefruit juice significantly increases cyclosporine levels (up to 200%).
- Caution is advised when using immune-stimulating herbal supplements, as they may counteract the effects of immunosuppressants.
Overdose Management
- No specific treatment exists for cyclosporine overdose.
Trade Names
- Commonly marketed under the trade names Neoral and Sandimmune.
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Description
Test your knowledge on cyclosporine with these flashcards. Covering its therapeutic class, pharmacologic class, and mode of action, this quiz is a great resource for medical students and professionals alike. Enhance your understanding of this important immunosuppressant drug.
