Generic Cyclosporine (Neoral®/Sandimmune®)
Compared with: Blackmores Conceive Well Gold 28 Tablets + 28 Capsules

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Cyclosporine is a calcineurin inhibitor that suppresses T‑lymphocyte activation by blocking interleukin‑2 transcription. It is used orally (modified‑release or non‑modified‑release) or IV for organ‑transplant rejection prophylaxis, rheumatoid arthritis, psoriasis, and select nephropathies at doses of 2.5–6 mg/kg/day, titrated to therapeutic blood levels to balance efficacy and nephrotoxicity risk
NCBI

Cyclosporine A – available as:

Modified‑release capsules (Neoral®/Gengraf®): 25 mg, 100 mg

Non‑modified‑release capsules (Sandimmune®): 25 mg, 50 mg

Oral solution: 100 mg/mL

Injectable (IV): 5 mg/mL concentrate
Medscape Reference

Other Popular and Common Names
Neoral®, Gengraf® (microemulsion formulations)

Sandimmune® (conventional formulation)

Cyclosporine binds cyclophilin in T‑cells, forming a complex that inhibits calcineurin, a phosphatase required for dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T‑cells). This blocks interleukin‑2 and other cytokine transcription, suppressing T‑cell proliferation and cell‑mediated immunity
NCBI
Organ Transplantation: Prophylaxis of graft rejection (renal, hepatic, cardiac) in combination regimens
NCBI

Rheumatoid Arthritis: In patients unresponsive to methotrexate (off‑label).

Plaque Psoriasis: Severe, recalcitrant disease at 2.5–5 mg/kg/day intermittent courses
PMC
American Academy of Dermatology

Nephrotic Syndrome / Focal Segmental Glomerulosclerosis: Steroid‑resistant cases at 3 mg/kg/day
NCBI

Other Autoimmune Diseases (Off‑Label): Atopic dermatitis, uveitis.

Indication Formulation Initial Dose Maintenance / Titration
Transplant Rejection Prophylaxis Oral (Neoral) 5–6 mg/kg/day in 2 divided doses Adjust to trough levels 100–300 ng/mL
IV (Sandimmune) 1/3 of oral dose as single infusion over 2–6 h Switch to oral when tolerated
Medscape Reference
Rheumatoid Arthritis Oral (Neoral) 2.5 mg/kg/day in 2 divided doses Increase by 0.5–0.75 mg/kg/day every 8 weeks to max 4 mg/kg/day
NCBI
Plaque Psoriasis Oral (Neoral) 2.5 mg/kg/day in 2 divided doses Up to 5 mg/kg/day for ≤12–16 weeks; intermittent courses
PMC
New England Journal of Medicine
Nephrotic Syndrome Oral (Neoral) 3 mg/kg/day in 2 divided doses Continue until remission, then taper

Microemulsion (Neoral®) has improved bioavailability vs Sandimmune®.

Take consistently with or without food—high‑fat meals can reduce absorption.

Measure trough (pre‑dose) blood levels for dose adjustment.

Prescribing Information
Route: Oral or IV

Formulations & Strengths: See Active Ingredient section.

Storage:

Capsules/solution: 2–8 °C or 15–25 °C per label.

IV concentrate: Use immediately or store per manufacturer.

Legal Status: Prescription Only

Pregnancy & Breastfeeding: Category C – Limited human data; use only if benefit justifies risk; excreted in breast milk.

Pediatric: ≥6 months for transplant; dose per body weight; monitor levels.

Renal Impairment: No initial adjustment; nephrotoxicity risk mandates close monitoring.

Hepatic Impairment: Metabolism reduced—consider lower starting dose and monitor levels

Nephrotoxicity (up to 30 %)
NCBI
ASTCT Journal

Hypertension, tremor, hirsutism

Gingival hyperplasia, hyperlipidemia

Serious:

Nephrotoxic acute and chronic injury

Increased risk of infections and malignancies (lymphoma, skin cancer)

Neurotoxicity: seizures, posterior reversible encephalopathy syndrome (PRES)

Nephrotoxicity: Monitor serum creatinine and adjust dose or discontinue.

Hypertension: Monitor BP; treat per guidelines.

Infection/Malignancy: Avoid live vaccines; counsel sun protection.

Drug Monitoring: Trough levels required to optimise therapy and minimise toxicity.

Graft‑Versus‑Host Disease: Use in combination with corticosteroids.

Agent Effect Recommendation
CYP3A4 inhibitors (e.g., ketoconazole) ↑CyA levels → ↑toxicity Reduce cyclosporine dose; monitor levels
CYP3A4 inducers (e.g., rifampin) ↓CyA levels → risk of rejection Increase dose; monitor levels
Nephrotoxins (e.g., aminoglycosides) Additive nephrotoxicity Avoid combination; monitor renal function
Calcium channel blockers (e.g., diltiazem) ↑CyA levels via P‑gp/CYP3A4 inhibition Consider dose reduction; monitor levels
Statins (e.g., simvastatin) ↑Myopathy risk via CYP3A4 inhibition Use lower statin dose; monitor for muscle toxicity
Medscape Reference

FAQs – Cyclosporine
Q1. Why monitor trough levels?
A: To ensure efficacy (prevent rejection) while minimising nephrotoxicity; target 100–300 ng/mL (transplant)
NCBI
Q2. Can I take it with food?
A: For Neoral® take consistently with or without food; avoid high‑fat meals to reduce absorption variability.

Q3. How long until side effects appear?
A: Nephrotoxicity and hypertension can occur within weeks; hirsutism, gingival hyperplasia develop over months.

Q4. Is cyclosporine safe long term?
A: Effective for chronic management but requires lifelong monitoring for renal function, blood pressure, and malignancy risk.

Q5. Can it cause hair growth?
A: Yes. Hirsutism is common—managed by dose reduction or adjunctive therapy.

Q6. What if I miss a dose?
A: Take as soon as remembered; maintain regular dosing interval; do not double doses.

Q7. Can I drink grapefruit juice?
A: No—grapefruit juice inhibits CYP3A4, increasing cyclosporine levels and toxicity risk.

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