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What is the therapeutic class of cyclosporine?
What is the therapeutic class of cyclosporine?
What is the pharmacologic class of cyclosporine?
What is the pharmacologic class of cyclosporine?
What are the actions 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?
What is one of the primary uses of cyclosporine?
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Neoral and Sandimmune are bioequivalent and can be used interchangeably.
Neoral and Sandimmune are bioequivalent and can be used interchangeably.
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What is the onset of cyclosporine?
What is the onset of cyclosporine?
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What are some common adverse effects of cyclosporine?
What are some common adverse effects of cyclosporine?
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Prior hypersensitivity to cyclosporine can be a contraindication for its use.
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.
Name one drug that may decrease the levels of cyclosporine.
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Match the following effects of cyclosporine with their descriptions:
Match the following effects of cyclosporine with their descriptions:
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Grapefruit juice can raise the levels of cyclosporine significantly.
Grapefruit juice can raise the levels of cyclosporine significantly.
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What are the trade names of cyclosporine?
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.
