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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Cequa
Generic Name
Cyclosporine
Active Ingredient
CyclosporineCategory
Calcineurin Inhibitor Immunosuppressant [EPC]
Variants
2
References used for this content
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Cequa, you must consult a qualified healthcare professional.
Detailed information about Cequa
Cyclosporine is a potent calcineurin inhibitor immunosuppressant used to prevent organ rejection and treat severe autoimmune conditions like rheumatoid arthritis and psoriasis. It works by suppressing the immune system's T-cell response to protect transplanted organs and reduce inflammation.
Dosage of Cyclosporine is highly individualized and depends on the condition being treated, the patient's weight, and their blood concentration levels. According to the FDA-approved labeling, the following are standard starting ranges:
Cyclosporine is used in children for organ transplantation, but dosing can be more challenging. Children often metabolize the drug faster than adults and may require higher doses per kilogram of body weight to achieve therapeutic blood levels. Pediatric dosing must be managed by a specialist in pediatric transplantation or immunology. For RA and psoriasis, the safety and efficacy in children under 18 have not been fully established, and use in these populations is generally considered off-label and requires extreme caution.
Cyclosporine is nephrotoxic (damaging to the kidneys). In patients with pre-existing renal dysfunction, the drug must be used with extreme caution. For RA and psoriasis patients, if serum creatinine levels increase by more than 30% above the patient's baseline, the dose must be reduced by at least 25%. If the levels do not return to baseline, the drug may need to be discontinued.
Since the liver is the primary site of metabolism, patients with liver disease (hepatic impairment) may require significantly lower doses. Close monitoring of Cyclosporine blood levels and liver function tests (LFTs) is essential to prevent toxic accumulation.
Clinical studies have not identified specific differences in response between the elderly and younger patients. However, because older adults are more likely to have decreased renal or hepatic function and take multiple other medications, healthcare providers usually start at the lower end of the dosing range.
Consistency is the most important factor when taking Cyclosporine.
If you miss a dose, take it as soon as you remember. However, if it is almost time for your next dose (within 4 hours), skip the missed dose and return to your regular schedule. Never 'double up' on doses to catch up, as this significantly increases the risk of toxicity.
Signs of a Cyclosporine overdose include severe nausea, vomiting, yellowing of the skin or eyes (jaundice), severe tremors, and decreased urination (indicating kidney failure). If an overdose is suspected, contact emergency services or a poison control center immediately. Treatment usually involves supportive care and monitoring of renal and hepatic function, as Cyclosporine is not easily removed by dialysis.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or switch brands (e.g., from Sandimmune to Neoral) without medical guidance, as they are not interchangeable.
Cyclosporine is a potent medication, and side effects are common, particularly at higher doses used in transplantation.
Cyclosporine is a high-alert medication. This means it requires careful management to avoid serious harm. Patients must be committed to regular blood monitoring and must communicate all other medications and supplements to their healthcare team. You should never start or stop any other medication without first consulting your transplant or rheumatology specialist.
The FDA has issued the following Black Box Warnings for Cyclosporine:
Certain drugs must NEVER be used with Cyclosporine because the risk of severe toxicity or loss of efficacy is too high:
There are several situations where Cyclosporine must NEVER be used because the risks far outweigh any potential benefits:
Cyclosporine is classified as Pregnancy Category C. This means that while there is no evidence of direct 'teratogenicity' (causing birth defects) in humans, the drug does cross the placenta and carries risks. Data from transplant registries suggest an increased risk of premature birth and low birth weight in infants born to mothers taking Cyclosporine. However, for transplant recipients, the risk of organ rejection if the drug is stopped is often considered a greater threat to both mother and fetus than the drug itself. Use in pregnancy must be managed by a high-risk obstetrician and a transplant specialist.
Cyclosporine is excreted into human breast milk. Because of the potential for serious adverse reactions in the nursing infant (including immune suppression and kidney damage), breastfeeding is generally not recommended while taking this medication. Mothers should discuss the risks and benefits of formula feeding versus breastfeeding with their healthcare provider.
In pediatric transplant patients, Cyclosporine is a standard therapy. However, children often require higher doses (on a mg/kg basis) than adults because they clear the drug from their systems more rapidly. Long-term use in children requires careful monitoring of growth, as some studies suggest potential effects on bone metabolism. For RA and psoriasis, Cyclosporine is not FDA-approved for use in patients under 18 years of age.
Cyclosporine is a calcineurin inhibitor. Its molecular target is the intracellular protein cyclophilin. The resulting Cyclosporine-cyclophilin complex binds to calcineurin, preventing it from dephosphorylating the Nuclear Factor of Activated T-cells (NFAT). This prevents NFAT from entering the nucleus and initiating the transcription of Interleukin-2 (IL-2). Without IL-2, T-lymphocytes cannot proliferate or activate, effectively halting the cellular immune response that leads to organ rejection or autoimmune tissue destruction.
The immunosuppressive effect of Cyclosporine is dose-dependent. The onset of action for transplant protection is immediate (within hours of the first dose), but for conditions like psoriasis or RA, it may take 4 to 12 weeks to see the full clinical benefit. There is no evidence of tolerance development (where the drug stops working over time) as long as therapeutic blood levels are maintained. However, the risk of toxicity increases linearly with the concentration of the drug in the blood.
| Parameter | Value |
|---|---|
Common questions about Cequa
Cyclosporine is primarily used to prevent the body from rejecting a transplanted organ, such as a kidney, liver, or heart. It is also FDA-approved to treat severe cases of rheumatoid arthritis and plaque psoriasis that have not responded to other treatments. By suppressing the immune system, it prevents T-cells from attacking foreign tissue or the body's own healthy cells. In some cases, doctors may use it off-label for conditions like ulcerative colitis or certain blood disorders. It is a potent medication that requires a prescription and close medical supervision.
The most frequent side effects include high blood pressure, kidney dysfunction, and tremors (shaking of the hands). Many patients also experience hirsutism, which is an increase in hair growth on the body, and gingival hyperplasia, which is an overgrowth of the gums. Headaches and tingling sensations in the hands and feet are also quite common. Because it suppresses the immune system, patients are at a higher risk for infections. Most of these side effects are dose-related and may improve if your doctor adjusts your dosage.
While there is no direct chemical interaction between alcohol and Cyclosporine, it is generally best to limit or avoid alcohol. Alcohol can dehydrate the body and place additional stress on the liver and kidneys, both of which are already working hard to process Cyclosporine. Additionally, some liquid forms of the medication contain a small amount of ethanol as an inactive ingredient. Drinking alcohol may also make it harder to stick to a strict dosing schedule, which is vital for the drug's success. Always consult your doctor before consuming alcohol while on immunosuppressants.
Cyclosporine is considered a Pregnancy Category C medication, meaning it should only be used if the potential benefits outweigh the risks. It does cross the placenta and has been associated with premature births and lower birth weights in infants. However, for many transplant recipients, the risk of losing the transplanted organ due to stopping the medication is a much greater danger. If you are pregnant or planning to become pregnant, you must have a detailed discussion with your transplant specialist and a high-risk obstetrician. Breastfeeding is generally discouraged while taking Cyclosporine as the drug passes into breast milk.
The time it takes for Cyclosporine to work depends on the condition being treated. For organ transplant patients, the drug begins working within hours of the first dose to prevent rejection. However, for autoimmune conditions like rheumatoid arthritis or psoriasis, it takes much longer to see results. Most patients will begin to see improvement within 4 to 8 weeks, but it can take up to 12 to 16 weeks to reach the full therapeutic effect. Your doctor will monitor your progress and may adjust your dose if you do not see improvement within these timeframes.
No, you should never stop taking Cyclosporine suddenly without your doctor's explicit instructions. For transplant patients, missing even a few doses can trigger an acute rejection episode, which can lead to organ failure and death. For those taking it for RA or psoriasis, stopping the drug abruptly can cause a severe 'rebound' flare-up of symptoms. If the medication needs to be discontinued due to side effects, your doctor will provide a plan to taper the dose slowly. Always ensure you have enough refills so that you never run out of your medication.
If you miss a dose of Cyclosporine, take it as soon as you remember. However, if it is almost time for your next scheduled dose (usually within 4 hours), skip the missed dose and resume your normal schedule. Do not take two doses at once to make up for the one you missed, as this can cause a spike in drug levels and lead to kidney toxicity. To help you remember your doses, it is often helpful to use a pillbox or set an alarm on your phone. Consistency in timing is key to keeping the drug at a steady level in your blood.
Cyclosporine itself is not typically associated with significant weight gain, unlike corticosteroids (like prednisone) which are often taken alongside it. However, some patients may experience fluid retention (edema) due to the drug's effect on the kidneys, which can cause a slight increase in weight. If you notice rapid weight gain, swelling in your ankles, or shortness of breath, you should contact your doctor immediately as this could indicate a problem with your kidney function. Maintaining a healthy diet and monitoring your salt intake can help manage any fluid-related weight changes.
Cyclosporine has a very long list of drug interactions, some of which can be life-threatening. It is metabolized by the liver's CYP3A4 enzyme, so any other drug that affects this enzyme (like certain antibiotics, antifungals, or heart medications) will change your Cyclosporine levels. Common over-the-counter pain relievers like ibuprofen (Advil) and naproxen (Aleve) should be avoided because they can increase the risk of kidney damage. Always provide your healthcare provider with a complete list of all prescriptions, over-the-counter drugs, and herbal supplements you are taking. Never start a new medication without checking for interactions first.
Yes, Cyclosporine is available in generic forms for both the modified (microemulsion) and non-modified versions. However, it is a 'narrow therapeutic index' drug, meaning small changes in blood levels can lead to either toxicity or treatment failure. Because of this, once you start on a specific brand or generic version, you should stay on that same one. If your pharmacy changes your generic manufacturer, you must inform your doctor, as they may need to check your blood levels more frequently to ensure the new version is working the same way for you.
Other drugs with the same active ingredient (Cyclosporine)
> Warning: Stop taking Cyclosporine and call your doctor immediately if you experience any of these serious symptoms:
With prolonged use, Cyclosporine increases the risk of certain chronic conditions:
Cyclosporine carries several FDA Black Box Warnings, the most serious type of warning. These include:
Report any unusual symptoms to your healthcare provider immediately. Regular monitoring is the best way to catch side effects early.
Safe use of Cyclosporine is impossible without rigorous lab testing. This typically includes:
Cyclosporine can cause tremors, headaches, or blurred vision. If you experience these side effects, do not drive or operate heavy machinery until you know how the medication affects you. Always use caution when starting the drug or after a dose increase.
Alcohol does not have a direct chemical interaction with Cyclosporine, but it can contribute to dehydration and liver stress. Furthermore, some liquid formulations of Cyclosporine contain a small amount of ethanol. It is generally advised to limit alcohol consumption while on immunosuppressants to protect your liver and kidney health.
Never stop taking Cyclosporine suddenly. For transplant patients, missing even a few doses can lead to acute organ rejection, which is a medical emergency. For RA or psoriasis patients, stopping the drug can cause a 'rebound' flare-up of symptoms. If the drug must be stopped, it is usually tapered slowly under strict medical supervision.
> Important: Discuss all your medical conditions, especially kidney or liver disease, with your healthcare provider before starting Cyclosporine.
Cyclosporine does not typically interfere with the chemical process of lab tests, but it significantly changes the biological results. It can cause elevations in:
For each major interaction, the mechanism usually involves the CYP3A4 pathway (metabolism) or P-glycoprotein (transport). The clinical consequence is either toxicity (if levels rise) or reduced efficacy/rejection (if levels fall). Management strategies always involve frequent blood level monitoring and dose adjustments.
> Important: Tell your doctor about ALL medications, supplements, vitamins, and herbal products you are taking. Even over-the-counter drugs like Aleve or Advil can be dangerous.
These conditions require a careful 'risk vs. benefit' analysis by a specialist:
There is no known direct cross-sensitivity between Cyclosporine and other classes of immunosuppressants (like Tacrolimus). However, patients who have had severe reactions to other 'calcineurin inhibitors' should be monitored with extreme caution, as the side effect profiles (especially kidney damage) are very similar.
> Important: Your healthcare provider will evaluate your complete medical history, including any history of cancer or kidney disease, before prescribing Cyclosporine.
Patients over 65 may be more sensitive to the effects of Cyclosporine. They are at a higher risk of developing drug-induced hypertension and kidney dysfunction. Furthermore, older adults are often taking multiple medications (polypharmacy), which increases the risk of dangerous drug interactions. Doctors typically start elderly patients at the lower end of the dosing range and monitor renal function very closely.
In patients with pre-existing renal impairment, Cyclosporine is extremely risky. For transplant patients, the drug is used but the dose is titrated based on blood levels and creatinine clearance. For RA and psoriasis patients, a baseline serum creatinine level of >1.5 mg/dL is usually a contraindication to starting therapy. If the GFR is significantly reduced, the drug should be avoided.
Since the liver is responsible for clearing Cyclosporine, patients with liver disease (Child-Pugh Class B or C) will have much higher levels of the drug in their blood. This increases the risk of systemic toxicity. Dose reductions of 50% or more may be necessary, and blood trough levels must be checked more frequently than usual.
> Important: Special populations require individualized medical assessment and more frequent lab monitoring to ensure safety.
| Bioavailability | 10% - 89% (Highly variable) |
| Protein Binding | 90% (Primarily to lipoproteins) |
| Half-life | 8 - 20 hours (Adults) |
| Tmax | 1.5 - 2 hours (Modified/Neoral) |
| Metabolism | Hepatic (CYP3A4 system) |
| Excretion | Fecal (90%), Renal (6%) |
Cyclosporine is the prototypical member of the Calcineurin Inhibitor (CNI) class. Other medications in this class include Tacrolimus (Prograf). While both drugs work by inhibiting calcineurin, they bind to different intracellular proteins (Cyclosporine binds to cyclophilin, while Tacrolimus binds to FKBP-12). These drugs are distinct from other immunosuppressants like corticosteroids, antimetabolites (Mycophenolate), or mTOR inhibitors (Sirolimus).