Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
CEQUA vs ASTAGRAF XL
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.
Calcineurin inhibitor that binds to FKBP-12, forming a complex that inhibits calcineurin, thereby preventing dephosphorylation and nuclear translocation of NFAT, which reduces T-cell activation and cytokine production (e.g., IL-2).
Dry eye disease due to keratoconjunctivitis sicca (KCS),Post-keratoplasty dry eye,Dry eye in Sjögren's syndrome
Prophylaxis of organ rejection in kidney transplant recipients,Prophylaxis of organ rejection in liver transplant recipients,Prophylaxis of organ rejection in heart transplant recipients
Instill one drop of 0.09% ophthalmic solution in each eye twice daily, approximately 12 hours apart.
Initial oral dose of 0.1-0.15 mg/kg/day divided every 12 hours, with subsequent adjustments based on trough levels. Typical maintenance dose 0.05-0.15 mg/kg/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 is approximately 43 hours (range 15.8–68.6 hours) in adult kidney transplant recipients. This long half-life supports once-daily dosing. In liver transplant patients, half-life ranges from 12 to 42 hours.
Hepatic via CYP3A4 and CYP3A5; also undergoes fecal elimination with enterohepatic recirculation.
Primarily hepatic via CYP3A4 and CYP3A5; undergoes extensive first-pass metabolism. Substrate of P-glycoprotein.
Primarily fecal (90%) with minor renal excretion (<1% unchanged drug). Biliary excretion is the major route for elimination of cyclosporine metabolites.
Primarily fecal (94.6%) via biliary elimination. Renal excretion accounts for approximately 2.4% of the dose, mainly as metabolites. Less than 1% is excreted unchanged in urine.
90-98% bound primarily to lipoproteins (HDL, LDL) and to a lesser extent albumin and globulins.
Approximately 99% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
4-8 L/kg, indicating extensive distribution into tissues (e.g., fat, liver, kidneys).
Volume of distribution is 3.5–4.5 L/kg (wide distribution, indicating extensive tissue binding). High Vd reflects distribution into erythrocytes, lymphocytes, and tissues.
Ophthalmic emulsion: systemic bioavailability is negligible (<0.1%) due to low absorption from the eye.
Oral bioavailability is highly variable, approximately 20–30% (range 5–89%). Absorption is incomplete and inconsistent; food decreases absorption by up to 33%. The modified-release formulation (Astagraf XL) has a lower peak and more sustained absorption compared to immediate-release.
No dosage adjustment required for renal impairment.
For GFR <30 m L/min: reduce dose by 50% and monitor trough levels closely. No adjustment for GFR >30 m L/min.
No dosage adjustment required for hepatic impairment.
Child-Pugh Class A: no adjustment. Class B: reduce dose by 25%. Class C: reduce dose by 50% and monitor trough levels frequently.
Safety and efficacy in pediatric patients have not been established.
Initial oral dose 0.15-0.2 mg/kg/day divided every 12 hours. Adjust to target trough levels of 5-15 ng/m L. Maximum dose 0.3 mg/kg/day.
No specific dosage adjustment recommended; use with caution due to potential for increased systemic exposure.
Start at lower end of adult dosing range (0.05 mg/kg/day) and titrate slowly due to reduced renal function and increased risk of adverse effects. Monitor trough levels closely.
Increased risk of infection and lymphoproliferative disorders including post-transplant lymphoproliferative disorder (PTLD).
Increased susceptibility to infection and possible development of lymphoma and other malignancies, particularly of the skin, due to immunosuppression. Increased nephrotoxicity, especially when used with other nephrotoxic drugs.
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
Nephrotoxicity, neurotoxicity (tremor, headache, seizures), hypertension, hyperkalemia, hyperglycemia, increased risk of infections and malignancies (especially skin), and lymphoproliferative disorders. Monitor blood pressure, renal function, electrolytes, and drug levels.
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 tacrolimus or any component of the formulation; concurrent use with cyclosporine or other calcineurin inhibitors.
No significant food interactions reported for ophthalmic cyclosporine. However, patients should avoid touching the dropper tip to food surfaces. No dietary restrictions are necessary.
Grapefruit juice significantly increases tacrolimus AUC and Cmax; avoid concurrent use. High-fat meals may decrease absorption; maintain consistent fat intake with each dose to ensure stable levels. Avoid taking with alcohol or herbal supplements like St. John's wort, which may reduce efficacy.
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.
Tacrolimus is classified as FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. In animal studies, tacrolimus caused maternal toxicity and embryotoxicity at doses higher than those used clinically. First trimester exposure is associated with an increased risk of congenital anomalies, including cardiac malformations. Second and third trimester use has been linked with intrauterine growth restriction, preterm delivery, and transient neonatal hyperkalemia and renal dysfunction. Postnatal immunosuppression in the neonate may occur.
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.
Tacrolimus is excreted into human breast milk with a milk-to-plasma (M/P) ratio of approximately 0.3. Limited data suggest low infant exposure (relative infant dose 0.5% of maternal weight-adjusted dose). However, because of potential for infant immunosuppression and growth effects, breastfeeding is generally not recommended unless benefits outweigh risks. Monitor infant for trough levels if breastfeeding.
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.
Pregnancy increases tacrolimus clearance due to expanded plasma volume and altered cytochrome P450 3A4 activity. Dose requirements may increase by 25-50% during the second and third trimesters. Therapeutic drug monitoring is essential, targeting trough levels 5-10 ng/m L. Postpartum, doses should be reduced to prepregnancy levels within 1-2 weeks as clearance normalizes.
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.
Monitor trough levels 5-15 ng/m L; avoid using with sirolimus due to increased risk of thrombotic microangiopathy; conversion from tacrolimus immediate-release is 1:1 (mg:mg) but monitor levels closely for 2 weeks; administer consistently with or without food to avoid fluctuations.
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 at the same time every day, consistently with or without food.,Do not crush, chew, or split the extended-release capsules; swallow whole.,Avoid grapefruit and grapefruit juice as they can increase drug levels and toxicity.,Report signs of infection (fever, sore throat), tremors, or changes in urine output immediately.,Minimize sun exposure and use sunscreen due to increased risk of skin cancer.,Do not change brand or formulation without consulting your transplant team.,Keep all appointments for blood level monitoring.
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 ASTAGRAF XL, 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.. ASTAGRAF XL is a Immunosuppressant, Calcineurin Inhibitor that works by Calcineurin inhibitor that binds to FKBP-12, forming a complex that inhibits calcineurin, thereby preventing dephosphorylation and nuclear translocation of NFAT, which reduces T-cell activation and cytokine production (e.g., IL-2).. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between CEQUA and ASTAGRAF XL depend on the specific clinical indication. These are agents from distinct pharmacological classes 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 ASTAGRAF XL is: Initial oral dose of 0.1-0.15 mg/kg/day divided every 12 hours, with subsequent adjustments based on trough levels. Typical maintenance dose 0.05-0.15 mg/kg/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 ASTAGRAF XL 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 . ASTAGRAF XL is classified as Category C. Tacrolimus is classified as FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. In animal studies, tacrolimus caused maternal toxicity an. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.