Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
CEQUA vs AZASAN
Clinician-reviewed, head-to-head comparison of mechanism, dosing, pharmacokinetics, and safety profiles.
Last clinically reviewed: July 2026 · OpiCalc Medical Review Team
Immunosuppressant; binds to cyclophilin D in mitochondria, inhibiting opening of mitochondrial permeability transition pore (m PTP), which reduces T-lymphocyte activation and cytokine release. Also forms complex with cyclophilin A to inhibit calcineurin, suppressing IL-2 production and T-cell proliferation.
Azathioprine is a purine analog that inhibits purine synthesis, thereby interfering with DNA and RNA synthesis. It is metabolized to 6-mercaptopurine, which inhibits T-cell activation and proliferation, leading to immunosuppression.
Dry eye disease due to keratoconjunctivitis sicca (KCS),Post-keratoplasty dry eye,Dry eye in Sjögren's syndrome
Renal transplant rejection prophylaxis,Rheumatoid arthritis,Off-label: inflammatory bowel disease (Crohn's disease, ulcerative colitis), lupus nephritis, autoimmune hepatitis, pemphigus vulgaris, myasthenia gravis, Behçet's disease, dermatomyositis, polymyositis
Instill one drop of 0.09% ophthalmic solution in each eye twice daily, approximately 12 hours apart.
1-3 mg/kg/day orally once daily or divided twice daily; maximum dose 2.5 mg/kg/day for rheumatoid arthritis; usual dose 50-150 mg/day.
Terminal elimination half-life is approximately 8.4 hours (range 6-10 hours) in healthy adults; prolonged in hepatic impairment and pediatric patients.
Terminal elimination half-life of azathioprine is approximately 4.5 hours (range 2–6 h), while its active metabolite 6-mercaptopurine has a half-life of 0.5–2 hours. Clinical context: Renal impairment prolongs half-life.
Hepatic via CYP3A4 and CYP3A5; also undergoes fecal elimination with enterohepatic recirculation.
Metabolized via xanthine oxidase and thiopurine methyltransferase (TPMT) to active and inactive metabolites. Co-administration with allopurinol inhibits xanthine oxidase, requiring dose reduction of azathioprine.
Primarily fecal (90%) with minor renal excretion (<1% unchanged drug). Biliary excretion is the major route for elimination of cyclosporine metabolites.
Renal: 88% as 6-mercaptopurine and metabolites; biliary: <10%
90-98% bound primarily to lipoproteins (HDL, LDL) and to a lesser extent albumin and globulins.
30% bound to plasma proteins, primarily albumin.
4-8 L/kg, indicating extensive distribution into tissues (e.g., fat, liver, kidneys).
0.8–1.0 L/kg, indicating extensive distribution into tissues.
Ophthalmic emulsion: systemic bioavailability is negligible (<0.1%) due to low absorption from the eye.
Oral: 41–47% (azathioprine); 100% for IV administration.
No dosage adjustment required for renal impairment.
GFR >50 m L/min: no adjustment; GFR 10-50 m L/min: 75% of normal dose; GFR <10 m L/min: 50% of normal dose.
No dosage adjustment required for hepatic impairment.
Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: contraindicated.
Safety and efficacy in pediatric patients have not been established.
2-3 mg/kg/day orally once daily; initial dose 1 mg/kg/day in divided doses; not recommended in children <1 year.
No specific dosage adjustment recommended; use with caution due to potential for increased systemic exposure.
Start at low end of dosing range (50 mg once daily); monitor renal function and adjust accordingly.
Increased risk of infection and lymphoproliferative disorders including post-transplant lymphoproliferative disorder (PTLD).
Chronic immunosuppression increases the risk of malignancy, particularly lymphoma and skin cancer. Patients should be monitored for neoplasia. The drug should be used only if potential benefits outweigh risks.
Increased susceptibility to infections,Potential for lymphoproliferative disorders and other malignancies,May cause renal impairment, hypertension, hyperkalemia, and hyperuricemia,Monitor blood cyclosporine levels to avoid toxicity,Avoid concurrent use of live vaccines,Caution with other nephrotoxic drugs
Hematologic toxicity (leukopenia, thrombocytopenia, anemia) - monitor blood counts. Hepatotoxicity. Increased infection risk. Hypersensitivity reactions. TPMT deficiency increases toxicity risk. Monitor for pancreatitis, especially in Crohn's patients. Avoid live vaccines. Photosensitivity and skin cancer risk.
Hypersensitivity to cyclosporine or any component,Uncontrolled hypertension,Severe renal impairment (except in transplant setting),Active infections,Concurrent use with PUVA or UVB therapy
Hypersensitivity to azathioprine or 6-mercaptopurine. Pregnancy (category D) unless potential benefit justifies risk. Lactation. Severe hepatic impairment. Myelosuppression or active infection. Concurrent use with allopurinol without dose adjustment.
No significant food interactions reported for ophthalmic cyclosporine. However, patients should avoid touching the dropper tip to food surfaces. No dietary restrictions are necessary.
No significant food interactions. May be taken with food to reduce gastrointestinal upset. Avoid concurrent use with raw or undercooked meats to reduce risk of infection due to immunosuppression.
CEQUA (cyclosporine ophthalmic solution) is classified as Pregnancy Category C. Animal studies have shown embryotoxic and fetotoxic effects at doses 0.2-0.8 times the human ocular dose. There are no adequate and well-controlled studies in pregnant women. Use only if potential benefit justifies potential risk to the fetus. First trimester: limited data, theoretical risk of immunosuppression. Second and third trimesters: no specific human data, but systemic cyclosporine is associated with increased risk of prematurity and low birth weight.
Azathioprine is FDA Pregnancy Category D. First trimester: Associated with congenital anomalies (e.g., atrial septal defect, limb defects) in case reports, but risk may be lower than with other immunosuppressants. Second and third trimesters: Risk of fetal growth restriction, preterm delivery, and neonatal immunosuppression. Avoid unless benefit outweighs risk.
Systemic cyclosporine is excreted in human milk. The M/P ratio is approximately 0.3-0.6. However, CEQUA is an ophthalmic formulation with minimal systemic absorption. Unknown whether topically applied cyclosporine is excreted in milk. Use caution, considering the importance of the drug to the mother. Breastfeeding infants should be monitored for potential adverse effects such as immune suppression.
Azathioprine is excreted into breast milk in small amounts; milk-to-plasma ratio approximately 0.1. Infant exposure is low, but theoretical risk of immunosuppression. Weigh benefits against risks; consider monitoring infant for leukopenia and infections.
No specific dosing adjustments are recommended for CEQUA in pregnancy due to its local administration and minimal systemic absorption. Pharmacokinetic changes in pregnancy (e.g., increased volume of distribution, altered protein binding) are unlikely to affect ophthalmic drug levels. No dose adjustment required.
Increased clearance and reduced bioavailability during pregnancy may require dose increase to maintain therapeutic levels; monitor thiopurine metabolite levels (6-TGN, 6-MMP) and adjust accordingly. Often no change required if stable disease.
CEQUA (cyclosporine ophthalmic solution 0.09%) is a calcineurin inhibitor immunosuppressant indicated for keratoconjunctivitis sicca (dry eye disease). It increases tear production by inhibiting T-cell activation. Important: CEQUA requires no refrigeration (unlike Restasis), and the vehicle contains no preservatives. Use with caution in patients with active ocular infections; do not administer while wearing contact lenses. Onset of effect may take 2-4 weeks; maximum benefit may require 6 months. Contraindicated in patients with known hypersensitivity to cyclosporine.
Azasan (azathioprine) is a prodrug of 6-mercaptopurine. Screen for TPMT deficiency before initiation to avoid severe myelosuppression. Monitor CBC and liver function weekly for first month, then monthly. Corticosteroid-sparing agent in autoimmune conditions. Avoid live vaccines during therapy.
CEQUA is a prescription eye drop used to increase tear production in dry eye disease.,Instill one drop in each eye twice daily, about 12 hours apart.,Remove contact lenses before use; wait at least 15 minutes before reinserting.,Do not touch the dropper tip to any surface to avoid contamination.,CEQUA comes in a single-use vial; use immediately after opening and discard any remaining solution.,Temporary blurred vision may occur after instillation; wait until vision clears before driving.,Report any eye pain, vision changes, or signs of infection (redness, discharge) to your doctor.,Store CEQUA at room temperature (20-25°C); do not refrigerate or freeze.,It may take several weeks to notice improvement; continue use as prescribed even if you feel no effect initially.
Take exactly as prescribed; do not change dose without consulting your doctor.,Report any signs of infection, unusual bruising/bleeding, or fatigue immediately.,Avoid exposure to individuals with infections; maintain good hand hygiene.,Use effective contraception during treatment and for at least 3 months after stopping.,Do not receive live vaccines (e.g., MMR, varicella) while taking this medication.,Limit sun exposure; use sunscreen and protective clothing due to increased skin cancer risk.
No interactions on record
No interactions on record
Explore head-to-head clinical comparisons of other medications in the same therapeutic classes.
Common clinical questions about CEQUA vs AZASAN, answered by our medical review team.
CEQUA is a Immunosuppressant that works by Immunosuppressant; binds to cyclophilin D in mitochondria, inhibiting opening of mitochondrial permeability transition pore (m PTP), which reduces T-lymphocyte activation and cytokine release. Also forms complex with cyclophilin A to inhibit calcineurin, suppressing IL-2 production and T-cell proliferation.. AZASAN is a Immunosuppressant that works by Azathioprine is a purine analog that inhibits purine synthesis, thereby interfering with DNA and RNA synthesis. It is metabolized to 6-mercaptopurine, which inhibits T-cell activation and proliferation, leading to immunosuppression.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between CEQUA and AZASAN depend on the specific clinical indication. These are both Immunosuppressant agents and are not directly interchangeable by dose. A physician or clinical pharmacist should guide any therapeutic switching decisions.
The standard adult dose of CEQUA is: Instill one drop of 0.09% ophthalmic solution in each eye twice daily, approximately 12 hours apart.. The standard adult dose of AZASAN is: 1-3 mg/kg/day orally once daily or divided twice daily; maximum dose 2.5 mg/kg/day for rheumatoid arthritis; usual dose 50-150 mg/day.. Dosing should always be individualized based on indication, renal and hepatic function, age, and other patient factors.
No direct drug-drug interaction has been formally documented between CEQUA and AZASAN in current clinical databases. However, individual patient risk factors including other medications, organ function, and comorbidities should always be evaluated by a qualified healthcare provider.
The maternal-fetal safety profiles differ. CEQUA is classified as Category C. CEQUA (cyclosporine ophthalmic solution) is classified as Pregnancy Category C. Animal studies have shown embryotoxic and fetotoxic effects at doses 0.2-0.8 times the human ocular . AZASAN is classified as Category C. Azathioprine is FDA Pregnancy Category D. First trimester: Associated with congenital anomalies (e.g., atrial septal defect, limb defects) in case reports, but risk may be lower th. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.