Cyclosporine Medications

Cyclosporine is a calcineurin inhibitor that suppresses immune responses. It is used in organ transplantation to prevent graft rejection and in severe autoimmune conditions.

Neoral

Cyclosporine

$4.74 per pill

25 | 100mg

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About Cyclosporine

Cyclosporine is a calcineurin inhibitor that suppresses the immune system by blocking T-cell activation. It is widely used to prevent organ-reject in kidney, liver and heart transplants, and to treat severe psoriasis and dry-eye disease. The drug is available in several branded forms such as Sandimmun, Neoral and Restasis, as well as in lower-cost generic tablets and ophthalmic solutions that can be purchased through our online pharmacy. While the medication offers clear therapeutic benefits, it also carries notable safety considerations that require careful monitoring by a healthcare professional.

What is Cyclosporine?

Cyclosporine belongs to the class of calcineurin inhibitors, a group of immunosuppressants that target intracellular signaling pathways in lymphocytes. The Health Sciences Authority (HSA) of Singapore first approved cyclosporine in the early -s for prophylaxis of organ-reject in renal transplantation, followed by extensions to liver, heart and corneal transplant settings. The drug is also approved for topical ophthalmic use (e.g., Restasis) to increase tear production in chronic dry-eye syndrome, and for systemic treatment of severe, plaque-type psoriasis.

Molecularly, cyclosporine forms a complex with the cytosolic protein cyclophilin. This complex binds to and inhibits calcineurin, a phosphatase required for dephosphorylating nuclear factor of activated T-cells (NF-AT). Inhibition of calcineurin prevents NF-AT from entering the nucleus and thereby blocks transcription of interleukin-2 (IL-2) and other cytokines essential for T-cell proliferation. The result is a dampened immune response, which is why the drug is essential in transplantation medicine and autoimmune dermatology.

Both branded products and generic formulations are stocked by our pharmacy service, offering patients flexible options for obtaining cyclosporine.

How Cyclosporine Works

Mechanism of Action

Cyclosporine-A binds cyclophilin A to create a stable complex that selectively inhibits calcineurin. By blocking calcineurin, the drug stops the dephosphorylation of NF-AT, a transcription factor that drives IL-2 gene expression. With IL-2 production curtailed, clonal expansion of activated T-cells is markedly reduced, leading to suppressed cellular immunity.

Therapeutic Effects

The inhibition of T-cell activation translates directly into clinical outcomes: transplanted organs experience fewer immune-mediated attacks, severe psoriatic plaques diminish as inflammatory signaling wanes, and ocular surface inflammation subsides, allowing the lacrimal glands to restore tear secretion.

Onset and Duration

Oral cyclosporine reaches peak plasma concentrations within 2-4 hours after dosing, and steady-state levels are usually achieved after 5-7 days of consistent use. Therapeutic effects in transplant prophylaxis become evident within the first week, while noticeable improvement in psoriasis may require 8-12 weeks of therapy. The ophthalmic formulation shows measurable tear-production increase as early as 4 weeks, with maximal benefit often observed after 3 months. The drug’s half-life ranges from 6 to 27 hours, depending on individual metabolism and dosing regimen, supporting once- or twice-daily dosing schedules.

Approved Uses and Applications

Approved Indications

Organ transplantation: Prevention of acute rejection in kidney, liver, heart and pancreas transplants (HSA, Singapore).
Severe psoriasis: Systemic treatment of plaque-type psoriasis unresponsive to conventional therapies.
Dry-eye disease: Topical ophthalmic solution to increase tear production in chronic dry-eye syndrome (Restasis, approved by HSA).

Off-Label Uses

Cyclosporine is sometimes employed off-label for conditions such as refractory ulcerative colitis, certain nephrotic syndromes, and severe atopic dermatitis when standard treatments fail. These applications are not officially sanctioned by regulatory agencies, and their use should be guided by specialist expertise.

Clinical Efficacy

A pivotal multicenter trial published in The New England Journal of Medicine demonstrated a 65 % reduction in acute rejection episodes among renal-transplant recipients receiving cyclosporine compared with placebo. In dermatology, a phase-III study in Lancet reported that 72 % of patients with severe psoriasis achieved a ≥75 % improvement in the Psoriasis Area and Severity Index after 12 weeks of cyclosporine therapy. Ocular studies cited in Ophthalmology show a 30 % increase in Schirmer-test scores after 6 weeks of cyclosporine eye drops.

Buying Cyclosporine from Our Online Pharmacy

Why Choose Our Service

Accessing cyclosporine can be challenging due to limited stock in some local pharmacies and the need for discreet handling. Through our online pharmacy, patients across Singapore receive fast, confidential delivery of both branded and generic cyclosporine products, backed by verified sourcing from licensed international partners.

Brand Names and Generic Options

Sandimmun (capsule) - original brand, widely recognized.
Neoral (microemulsion capsule) - enhanced absorption profile.
Gengraf (tablet) - convenient dosing.
Restasis (ophthalmic solution) - approved for dry-eye disease.

Generic cyclosporine tablets are available in 25 mg, 100 mg and 200 mg strengths, typically at 40-60 % lower cost than brand equivalents.

Quality & Safety

We work with suppliers that meet WHO-Good Manufacturing Practice standards and are inspected by the Health Sciences Authority, ensuring that every batch conforms to stringent quality controls.

Pricing & Access

Competitive pricing structures allow patients to save on long-term therapy. A Lifetime 10 % discount applies automatically to all reorders placed via our online service, making chronic treatment more affordable.

Discreet Delivery

Orders ship via express (≈ 7 days) or standard (≈ 3 weeks) options, each packaged in unmarked, tamper-evident containers to protect privacy.

Dosing, Formulations & Administration

Available Formulations

Oral capsules/tablets: 25 mg, 100 mg, 200 mg.
Oral microemulsion capsules (Neoral): 100 mg, 250 mg.
Ophthalmic solution (.05 %): single-dose vial.

Typical Dosing Ranges

For organ-transplant prophylaxis, adults often start at 5 mg/kg/day divided into two doses, with adjustments based on trough blood levels. In severe psoriasis, initial dosing may range from 2.5 mg/kg/day, tapered according to clinical response and toxicity monitoring. Dry-eye treatment usually involves one drop per eye twice daily. These examples reflect common clinical practice; the exact regimen must be individualized by a qualified healthcare provider.

Administration Guidelines

Food: High-fat meals can increase oral absorption, especially for the microemulsion formulation; clinicians may advise dosing on an empty stomach for more predictable levels.
Timing: Consistent dosing times help maintain stable trough concentrations.
Ophthalmic drops: Gently pull the lower eyelid to create a pocket, instill the drop, and close the eye for a few seconds to enhance absorption.

A healthcare professional should determine the precise dose, monitor blood levels, and adjust therapy according to efficacy and safety parameters.

Safety Profile & Considerations

Common Side Effects

Nephrotoxicity: Elevated serum creatinine observed in >10 % of patients in long-term studies.
Hypertension: Occurs in approximately 12 % of transplant recipients.
Gingival hyperplasia: Reported in 5-15 % of chronic users, often reversible upon dose reduction.
Hirsutism: Excess facial or body hair noted in up to 10 % of patients.
Tremor and headache: Frequently mild, affecting 8-12 % of users.

Serious Adverse Events

Severe infections: Immunosuppression predisposes to opportunistic infections; immediate medical evaluation is required if fever or unexplained illness occurs.
Malignancy risk: Long-term use is linked to a modest increase in lymphoma and skin cancer incidence; regular dermatologic screening is advised.
Neurotoxicity: Rare cases of seizures or posterior reversible encephalopathy syndrome have been documented.

Contraindications

Cyclosporine should not be used in patients with uncontrolled hypertension, severe renal impairment (creatinine clearance < 30 mL/min), or known hypersensitivity to the drug or its excipients.

Drug Interactions

CYP3A4 inhibitors: Ketoconazole, erythromycin, and certain antifungals can raise cyclosporine levels, increasing toxicity risk.
CYP3A4 inducers: Rifampin and carbamazepine may lower concentrations, reducing efficacy.
Other immunosuppressants: Concurrent use with sirolimus or tacrolimus can amplify immunosuppressive effects and nephrotoxicity.

Special Populations

Pregnancy & breastfeeding: Classified as Category C; potential teratogenicity has been observed in animal studies. Use only if benefits outweigh risks and under strict medical supervision.
Elderly: Age-related decline in renal function warrants lower starting doses and closer monitoring.
Hepatic or renal impairment: Dose adjustments are essential; therapeutic drug monitoring guides safe titration.

Professional medical guidance is indispensable for safe initiation, dose titration, and ongoing monitoring of cyclosporine therapy.

Frequently Asked Questions

How does cyclosporine differ from tacrolimus? Both are calcineurin inhibitors, but tacrolimus binds FK-binding protein instead of cyclophilin. Tacrolimus generally has a higher potency and a different side-effect profile, with more frequent tremor and hyperglycemia, while cyclosporine is more associated with gingival hyperplasia and hirsutism.
How long before cyclosporine produces noticeable effects for transplant patients? The immunosuppressive effect becomes measurable within 48-72 hours, and most transplant protocols achieve target trough levels by the end of the first week, significantly reducing acute-reject incidence.
What should I do if I experience gum overgrowth while taking cyclosporine? Report the symptom to your clinician promptly. Dose reduction, switching to a different immunosuppressant, or adjunctive dental hygiene measures can mitigate gingival hyperplasia.
Can I take cyclosporine with grapefruit juice? Grapefruit juice inhibits CYP3A4, potentially raising cyclosporine concentrations and increasing toxicity risk. It is advisable to avoid large amounts of grapefruit or its juice during therapy.
Are there specific foods I should avoid while on cyclosporine? High-fat meals can enhance absorption, leading to higher blood levels. Consistency is key: if you start taking the medication with food, maintain the same routine, or discuss an empty-stomach schedule with your provider.
What monitoring is required during cyclosporine treatment? Regular blood tests for trough levels, renal function (creatinine, eGFR), blood pressure, lipids, and liver enzymes are standard. Frequency varies but is typically every 1-2 weeks initially, then monthly once stable.
Is the ophthalmic formulation safe for long-term use? Long-term studies show a favorable safety profile, with transient eye irritation as the most common side effect. Persistent discomfort or visual changes should prompt a review by an eye specialist.
What information should I provide my doctor when discussing cyclosporine?
- Complete medical history, including kidney or liver disease.
- Full list of current medications, over-the-counter drugs, and supplements.
- History of hypertension, infections, or malignancy.
- Specific treatment goals and any concerns about side effects.

Disclaimer

The information provided about cyclosporine is for general knowledge only. It does not replace professional medical consultation or the official prescribing information for medications containing this ingredient. All treatment decisions, including dosing, formulation selection, and monitoring, should be made under the supervision of a qualified healthcare provider who can assess individual medical history, current medications, and specific health needs. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to medications containing cyclosporine for individuals who may have limited availability through traditional pharmacies, prescription-based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication containing cyclosporine.