Cyclosporine (Dosage)
Cyclosporin is an immunosuppressive drug of the calcineurin inhibitor group used in autoimmune diseases and in the prophylaxis of transplant rejection.
It decreases the cellular immune response, inhibiting the production of T-dependent antibodies and inhibiting the production and release of lymphokines, including interleukin 2.
CONTRAINDICATIONS
Hypersensitivity to cyclosporine. Autoimmune diseases with impaired renal function (except proteinuria in patients with nephrotic syndrome), malignant processes or uncontrolled hypertension. Patients with psoriasis who are receiving other immunosuppressants, PUVA, UVD, Coal tar and radiation therapy.
PRECAUTIONS
Due to the active principle. Due to its adverse effects profile, during cyclosporine treatment it is recommended to monitor:
- Renal function. Treatment with cyclosporine may lead to acute dose-dependent nephrotoxicity in the first weeks. Careful monitoring of renal function (in particular serum creatinine) and dose adjustment should be performed by determination of plasma concentrations.
- Hepatic function. It can cause reversible, dose-dependent increases of serum bilirubin and occasionally liver enzymes. Some cases of hepatic impairment have been reported.
- Blood pressure. Monitor the blood pressure regularly. If treatment-related hypertension develops, appropriate antihypertensive treatment may be necessary.
- Lipidic profile. Cyclosporine may produce dyslipidemia. It is recommended to monitor blood lipids periodically.
- Infections / Neoplastic processes. There is an increased risk of lymphomas and skin cancers with prolonged use of cyclosporine. Avoid excessive exposure to ultraviolet light.
Cases of activation of latent polyomavirus infections have been reported in patients treated with cyclosporine, which may lead to nephropathy, especially BK virus nephropathy, or progressive multifocal leukoencephalopathy due to JC virus. In these cases, the possibility of reducing the immunosuppressive burden and using appropriate prophylactic and therapeutic strategies should be considered.
- Vaccines. During treatment with cyclosporine, the effect of vaccination may be reduced; And the use of live attenuated vaccines should be avoided.
Precautions to be taken by the formulation.
The capsules and oral solution contain 11.8% and 12.0%, respectively, of ethanol by volume (alcohol). It should be taken into account in infants and children, especially in high-risk groups, such as patients with liver disease or epilepsy.
Ampoules for intravenous administration contain, in addition to ethanol, polyethoxylated castor oil (Cremophor EL), which may cause anaphylactoid reactions following intravenous administration, therefore close monitoring during infusion is recommended. Prophylactic administration of an antihistamine has also been used successfully to prevent the occurrence of anaphylactoid reactions.
SIDE EFFECTS
Although no well-controlled clinical trials have been conducted in children, no adverse events other than those seen in the adult population have been observed in the administration of cyclosporin in transplant recipients even younger than 1 year of age.
Nephrotoxicity (30%) usually mild, reversible and dose-dependent. It may be accompanied by hypertension, hyperuricemia, hyperkalemia, hypomagnesemia.
Other adverse effects: digestive disorders, hepatotoxicity (transient), hirsutism / hypertrichosis, angioedema, gingival hypertrophy, tremor, headache, paresthesia, myalgia, asthenia and hyperlipidemia.
BRAND NAMES
- Sandimmun ®
- Gengraf ®
- Neoral ®
Genes analyzed