Cyclosporine

Cyclosporine is a potent immunosuppressant widely used to prevent organ rejection in transplant patients and to manage certain autoimmune diseases.

It belongs to the calcineurin inhibitor class and works by suppressing specific immune cell activity, helping to control unwanted immune responses.

Overview

• Drug Name: Cyclosporine (also spelled Ciclosporin)

• Drug Class: Immunosuppressant (Calcineurin Inhibitor)

• Available Forms: Oral capsules, oral solution, and injection (with major clinical use in capsules)

Description

Cyclosporine is a cyclic undecapeptide derived from the fungus Beauveria nivea.
It acts selectively on T-lymphocytes, which play a critical role in immune response.

• Primary Role: Prevents rejection in organ transplantation and regulates immune-driven inflammatory diseases.

• Enhanced Bioavailability: The microemulsion form of cyclosporine ensures consistent absorption in capsule formulations.

Uses / Indications

• Prevention of rejection in kidney, liver, heart, and lung transplants

• Severe active rheumatoid arthritis (when standard therapy fails)

• Severe plaque psoriasis unresponsive to conventional treatments

Benefits

• Effective in preventing transplant rejection

• Reduces flare-ups in chronic autoimmune diseases

• Faster onset compared to many other immunosuppressants

• May reduce dependency on steroids or additional drugs

• Improves long-term disease control and patient quality of life

Side Effects

Common

• Headache

• Tremors

• Increased hair growth (hirsutism)

• Hypertension (high blood pressure)

• Gingival hyperplasia (gum overgrowth)

• Nausea, abdominal pain

• Fatigue

Serious

• Nephrotoxicity (kidney damage)

• Hepatotoxicity (elevated liver enzymes)

• Serious infections due to immunosuppression

• Increased risk of malignancies (lymphomas, skin cancers)

Mechanism of Action – How It Works

• Cyclosporine binds to cyclophilin, an intracellular protein.

• This complex inhibits calcineurin, an enzyme essential for activating the NFAT pathway in T-cells.

• As a result, production of interleukin-2 (IL-2) and other cytokines is blocked.

• This prevents T-cell activation, reducing immune attacks on transplanted organs or self-tissues.

Dosage Guidelines

Transplant Patients

• Initial dose: 10–15 mg/kg/day (in 2 divided doses), starting 4–12 hours before transplant

• Maintenance dose: 2–6 mg/kg/day, based on blood levels and organ function

Rheumatoid Arthritis

• Start: 2.5 mg/kg/day

• Adjustment: Increase by 0.5–1 mg/kg every 4–8 weeks as tolerated (max 4 mg/kg/day)

Psoriasis / Atopic Dermatitis

• 2.5–5 mg/kg/day, titrated according to patient response

Directions for Use

• Take exactly as prescribed by your doctor

• Maintain consistent timing every day

• Swallow capsules whole with water (do not crush or chew)

• Do not switch between brands or formulations without medical guidance

• Follow food-related instructions given by your doctor

Contraindications – When Not to Use

• Allergy to cyclosporine or formulation components

• Uncontrolled high blood pressure

• History of malignancy

• Concomitant use of other nephrotoxic drugs

• Active serious infections (e.g., hepatitis, tuberculosis)

Drug Interactions

Increases cyclosporine levels:

• Erythromycin, ketoconazole, fluconazole, diltiazem, grapefruit juice

Decreases cyclosporine levels:

• Rifampin, phenytoin, carbamazepine, St. John’s Wort

Increases toxicity risk:

• Aminoglycosides, NSAIDs, amphotericin B

Safety Advice

• Pregnancy: Use only if benefits outweigh risks (may cause fetal harm)

• Breastfeeding: Not recommended (drug passes into breast milk)

• Elderly: Higher risk of kidney damage and hypertension

• Children: Use with caution; individualized dosing required

General Instructions

• Take at the same time daily for steady blood levels

• Monitor blood pressure, kidney function, and drug levels regularly

• Inform your doctor about all medicines, vitamins, or supplements being used

• Do not stop abruptly without medical advice

Lifestyle & Dietary Tips

• Avoid grapefruit or grapefruit juice (raises drug levels)

• Limit potassium-rich foods (bananas, oranges) as kidneys may be affected

• Maintain proper dental hygiene to reduce gum overgrowth

• Avoid alcohol and smoking

• Reduce infection risk by minimizing exposure to sick individuals

• Drink plenty of water and eat a balanced diet

Comparison with Other Immunosuppressants

• Tacrolimus: fewer cosmetic side effects but cyclosporine causes gum overgrowth & hair growth

• Azathioprine: safer for kidneys but slower onset than cyclosporine

• Methotrexate: slower-acting for autoimmune diseases compared to cyclosporine

• Mycophenolate mofetil (MMF): less nephrotoxic but more GI side effects

Warnings & Precautions

• Long-term use increases cancer risk

• Regular monitoring is essential to avoid toxicity

• Caution in patients with kidney, liver, or heart disease

• Avoid live vaccines during treatment

Compatible & Avoid Combinations

Safe with: Paracetamol, proton pump inhibitors, certain antihypertensives
Avoid with: NSAIDs, potassium supplements, potassium-sparing diuretics

Storage

• Store at 20–25°C in a dry, cool place

• Keep away from light and moisture

• Store in original container

• Keep out of reach of children

• Do not refrigerate or freeze

Manufactured & Marketed by

Onco India International
Trusted name in global pharmaceutical solutions, ensuring high-quality immunosuppressants for transplant and autoimmune care.