Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Neoral
Active ingredient: Cyclosporine
Available dosage forms: 25, 100 mg
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Cyclosporine general information
Cyclosporine is an alternative drug used when treating eczema that suppresses the immune system. Biological agents are a new category of medications made from synthetic proteins. Studies also report success in certain patients using vitamin D ointments together with phototherapy treatment. Additionally, There are drugs that may be injected. Fourth, you’ve got Cyclosporine An or Neoral. A natural method of treating psoriasis If you would like to try an even more pure approach within the treatment of your own disease, one very excellent fruit that I am able to recommend is acai berry.
Atopic dermatitis has become the most common variety of eczema. These rashes are very itchy. Even if no specific allergy is identified, it’s found that a wholesome diet can continue to keep the entire scalp wholesome and thus decrease the likelihood of dandruff. Nevertheless, frequently the physician can’t account for the reason for the hives. This enables the doctor to detect any eye difficulties early and also to begin appropriate treatment to prevent serious issues. Additionally, There are various supplements of magnesium that can be found in the market in a similarity to tablets.
Treatment is accessible for gout and it needs to be done once a diagnosis is made. These medications might be used to take care of children with arthritis and relevant conditions. Medication doses ought to be adjusted regularly as the kid grows to ensure the appropriate dosages are used. Treatment for RA may also involve occupational as well as physical therapy. Be ready for all of the appointments with your own doctor and receive the required laboratory tests done. The very first ingredient inside this food is brewers rice, which really is a low-quality grain since it is not the entire grain.
Occupational therapy will allow you to maintain your independence. Furthermore, therapy has to be individualized, taking into consideration the severity of symptoms and prognosis. This might also bring about diabetes, hypertension and arthritis. Here are a few indications that can help you identify this disorder.
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So as to prevent gout, you should know what causes this disease and for you to truly be treated, you have to know the various gout symptoms. Even if treatment is accessible for gout, you must always remember that prevention is preferable to cure. Alcohol is only going to make things worse as the liver requires to be detoxified. Cyclosporine can bring about kidney damage and significant blood pressure. This medication can result in serious modifications to your stomach and intestines, which may result in fatal complications with no warnings. Speak to your very own about the protected usage of alcohol whilst taking this drug.
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Cyclosporine (Ciclosporin): instruction, and the use of a formula
The nosological classification (ICD – 10)
Mode of action -. Immunosuppressive
specifically and reversibly inhibits G 0 and G 1 phase of the cell cycle of immunocompetent lymphocytes, particularly T – helper cells, inhibits the formation and yield of IL & minus cell 2 and its binding with specific receptors. Penalized differentiation and proliferation of T – cells involved in graft rejection.
It is enough to quickly and completely absorbed from the gastrointestinal tract. Time to reach C max after oral administration varies from 1 to 6 hours absolute bioavailability .; 20 – 50%. Plasma protein binding (mostly lipoproteins) ; about 90%. It distributed mainly outside the bloodstream, although it is found in red blood cells, granulocytes, lymphocytes. The apparent volume of distribution ; 3.5 l / kg. In the liver, with the participation of cytochrome P450 – dependent monooxygenase system hydroxylated and N – demethylated. All metabolites (up to 15) contain the intact peptide original base conserved some weak immunosuppressive activity. T 1/2 varies ; . 6.3 hours to 20.4 hours is derived mainly from the bile, found in the urine around 6% of the dose, less than 1% ; in unchanged form.
increases (especially in combination with prednisone and azathioprine) survival after transplantation of cadaveric kidneys and reduces the frequency and rejection crises reactions “graft versus host”. Extends safety of allogeneic transplants of skin, heart, lungs and other organs. Effective for bone marrow transplantation, severe exacerbations of Crohn’s disease is not amenable to conventional treatment, rheumatoid arthritis.
Application of the substance Cyclosporine
transplant kidneys, liver, heart, lung, pancreas (prevention of graft rejection, the treatment of rejection reactions), bone marrow (prevention of rejection, prevention and treatment of disease, “graft versus host”); acute non-infectious uveitis, threatening loss of vision, Behçet uveitis with recurrent inflammation and involvement in the process of the retina, chronic glomerulonephritis, accompanied by the development of nephrotic syndrome, rheumatoid arthritis, with a high degree of activity, psoriasis, severe atopic dermatitis.
Hypersensitivity (including to polyoxyethylated castor oil), cancer, severe infectious diseases, renal dysfunction and / or liver, hypertension, hyperuricemia, hyperkalemia, pregnancy, breast-feeding.
Application of pregnancy and breastfeeding
Category effects on the fetus by FDA ; C.
Side effects of substance Cyclosporine
Acute and chronic renal failure, interstitial renal fibrosis, hypertension, tremors, weakness, headache, paresthesia, seizures, myopathy, liver dysfunction, pancreatitis, nausea, vomiting, anorexia, abdominal pain, feeling of heaviness in the epigastric area, diarrhea, gingival hyperplasia, fluid retention in the body, reversible dysmenorrhoea and amenorrhoea, hypertrichosis, thrombocytopenia, anemia, hyperkalemia, hyperuricemia, increased susceptibility to infections.
increases the toxicity of melphalan, diltiazem, nicardipine, verapamil, beta – blockers, fluconazole, imidazole derivatives, glucocorticoids, macrolides ; level in plasma. It increases the risk of myopathy and rhabdomyolysis with the appointment of lipid-lowering drugs (HMG – CoA – reductase), renal dysfunction ; against the backdrop of aminoglycosides, amphotericin B, trimethoprim, co – trimoxazole, ciprofloxacin, some cephalosporins, NSAIDs. propafenone. Phenytoin, carbamazepine, barbiturates, benzodiazepines, aminoglutethimide, estrogen – progestin drugs, progesterone, rifampicin, isoniazid, sodium metamizol weakens the effect of ; accelerate elimination. Enhances the effect of quinidine, theophylline, valproate sodium, potassium drugs and potassium-sparing diuretics (increases the likelihood of hyperkalemia).
Patients treated with amiodarone, an increase in cyclosporine levels were observed in the serum and, as a result, there was nephrotoxicity. On the contrary, in one report described a slight decrease in the level of cyclosporin and increase the level of amiodarone, in another case reported pulmonary toxicity in a patient to stop taking amiodarone and start taking cyclosporine.
Eight patients with cardiac and cardio 3 – lung transplants who received tacrolimus, was also appointed as amiodarone (dose has not been established) for the treatment of fibrillation – atrial flutter. Despite the reduction of cyclosporin dosage is 13 – 14%, the level of the serum increased by 9%, the level of serum creatinine, increased 38% (from 157 to 216 mmol / l) and blood urea nitrogen – 30% 1
in another report, it was noted 50% decrease in clearance of cyclosporine in one patient after administration of amiodarone (1 g, followed by 600 mg daily for 5 days, followed by 400 mg daily) 2.
Eight other patients with cardiac or cardiovascular – lung transplants effectively treated with amiodarone (dose has not been established) in connection with the flicker and / or atrial flutter. They have increased by 31% cyclosporin serum (from 248 to 325 ng / ml), although the dose reduction by 44% (from 6.2 to 3.5 mg / kg / day). Serum creatinine was increased by 39 3%.
In a patient with kidney transplant serum levels of cyclosporine after administration of amiodarone 600 mg twice daily was increased 2-fold 4.
In contrast, 5 patients with heart transplantation amiodarone It was canceled, and cyclosporine was appointed, but the metabolism of cyclosporine period increased by 4 – 5 weeks compared with patients not treated with amiodarone (metabolite plasma levels increased from 720 to 1437 ng / ml). Values of cyclosporine levels were only slightly decreased in patients receiving amiodarov compared to not receiving it (225 ng / ml and 240 ng / ml, respectively) 5. The study was performed in 2 patients amiodarone monitoring level, and it was found that 4 – 5 weeks also increase plasma concentrations of amiodarone and its major metabolite dezetilamiodarona. During this period also witnessed increased adverse effects, including pulmonary toxicity 5.
The mechanism of this interaction is unclear.
The value and a warning
The increase in cyclosporine levels when taking amiodarone – established and clinically important interaction. No need to avoid joint use of cyclosporine and amiodarone, but must be closely monitored and, in order to reduce the risk of nephrotoxicity may need to decrease the dose of cyclosporine.
It is necessary to bear in mind the possibility of adjusting the dose of cyclosporine in connection with the cancellation of amiodarone, since it can take weeks for the complete elimination of amiodarone from the body.
The importance of raising the level of amiodarone, cyclosporine and reducing cases of pulmonary toxicity in patients who stopped taking amiodarone and started taking cyclosporine, incomprehensible.
Stockley’s Drug Interactions / Ed. by Karen Baxter. – 9th ed. – London – Chicago, Pharmaceutical Press, 2010. – P. 1214.
1. Egami J. Mullins P.A. Maprin F. et al. Increase in cyclosporine levels due to amiodarone therapy after heart and heart – lung transplantation // J. Am. Coll. Cardiol. – 1993. – 21. -. P. 141A
2. Nicolau D.P. Uber W.E. Crumbley A.J. et al. Amiodarone – cyclosporine interaction in a heart transplant patient // J.Heart Lung Transplant. – 1992. – 11. – P. 564 – 568.
3. Mamprin F. Mullins P. Graham T. et al. Amiodarone – cyclosporine interaction in a heart transplantation // Am. Heart J. – 1992. – 123. – P. 1725 – 1726.
4. Chitwood K.K. Abdul – Haqq A.J. Heim – Duthoy K.L. Cyclosporine – fmiodarone – interaction // Ann. Pharmacother. – 1993. – 27. – P. 569 – 571.
5. Preuner J.G. Lehle K. Keyser A. et al. Development of severe adverse effects after discontinuing amiodarone therapy in human heart transplant recipients // Transplant. Proc. – 1998. – 30. – P. 3943 -. 3944
Tacrolimus + proton pump inhibitors
Omeprazole usually does not affect the level of serum cyclosporine, but there are isolated reports of 2 – fold increase in the concentration of cyclosporine in one patient, and reduced by more than 2 times – another. Pantoprazole has no effect on cyclosporine serum
In the placebo -. Controlled study in 10 patients with kidney grafts were found significant changes in levels of cyclosporine in the appointment of omeprazole 20 mg / day for 2 weeks 1. in another study, 8 patients with renal transplants, similar results were obtained: after application of 20 mg of omeprazole for 6 days, significant changes were absent levels of cyclosporin compared with the control – patients not taking omeprazole 2. There were no significant changes in cyclosporine levels in the serum and in patients with kidney transplants after administration of 20 mg / day omeprazole for 8 weeks 3
However, in a retrospective analysis of the dose of cyclosporine. necessary to ensure a certain level was 28% lower in patients receiving omeprazole 21 (dose not determined), compared with the 139 patients not taking omeprazole 4. There is also a case where a patient with hepatic graft cyclosporin level increased approximately 2-fold ( from 187 – 261 to 510 ng / ml) for about 2 weeks after initiation of therapy omeprazole (40 mg / day). It was able to restore levels of cyclosporine after reducing the dose of cyclosporin from 130 to 80 mg 2 times a day. Then a stabilization (approximately 171 ng / ml) for the subsequent four months 5. Conversely, in another patient with bone marrow transplantation shown inverse interaction: cyclosporin serum levels during treatment with omeprazole (40 mg / day) reduced her from about 254 up to 100 ng / ml for 14 days and then rose quickly after its cancellation six.
Studies in patients with kidney transplant demonstrated that pantoprazole (40 mg / day every day) has no effect on cyclosporine levels in the serum, if it is taken in the evening of 7 or the combined use of both drugs in the morning 8.
The mechanism of this interaction is not clear.
The value and a warning
There is strong evidence that omeprazole 20 mg daily did not affect the pharmacokinetics of cyclosporine, and it is also obvious that pantoprazole (40 mg daily) did not interact with cyclosporine. No explanation facts increase or decrease the level of cyclosporine in two separate cases, patients receiving omeprazole daily dose of 40 mg. There is no need to avoid the simultaneous application of cyclosporine and proton pump inhibitors, but you must bear in mind the possibility of interaction and exercise caution if the patient receives high-dose omeprazole and cyclosporine level changes in one direction or another.
Stockley’s Drug Interactions / Ed. by Stockley. – 9th ed, 2010. – P. 1250.
1. Blohme I. Idstrom J. – P. Andersson T. A study of the interaction between omeprazole and cyclosporine in renal transplant patients // Br. J. Clin. Pharmacol. – 1993. – 35. – P. 156 – 160.
2. Kahn D. Manas D. Hamilton H. et al. The effect of omeprazole on cyclosporine metabolism in renal transplant recipients // S. Afr. Med. J. – 1993. – 83. – P. 785.
3. Castellote E. Bonet J. Lauzirica R. et al. Does interaction between omeprazole and cyclosporib exist? // Nephron. – 1993. – 65. – 478.
4. Reichenspurner H, Meiser BM, Muschiol F, Nollert G, Uberfuhr P, Markewitz A, Wagner F, Pfeiffer M, Reichart B. The influence of gastrointestinal agents on resorption and metabolism of cyclosporine after heart transplantation: experimental and clinical results. J Heart Lung Transplant (1993) 12, 987 – 92.
5. Schouler L. Dumas F. Couzigou P. et al. Omeprazole – cyclosporin interaction // Am. J. Gastroenterol. – 1991. – 86. – P. 1097.
6. Arranz R. Yanez E. Franceschi J.L. et al. More about omeprazole – cyclosporine interaction // Am. J. Gastroenterol. – 1993. – 88. – P. 154 – 155.
7. Lorf T. Ramadori G. Ringe B. et al. Pantoprazole does not affect cyclosporin A blood concentration in kidney – transplant patients // Eur. J. Clin. Pharmacol. – 2000. – 55. – P. 733 – 735.
8. Lorf T. Ramadori G. Ringe B. et al. The effect of pantiprazole on tacrolimus and cyclosporin A blood concentration in transplant patients // Eur. J. Clin. Pharmacol. – 2000. – 56. – P. 439 – 440.
9. Schwrer H. Lorf T. Ringe B. et al. Pantoprazole and cyclosporine or tacrolimus // Aliment. Pharmacol. Ther. – 2001. – 15. – P. 561 -. 562
There is a separate report on reducing the level of cyclosporine in patients taking griseofulvin, while another report found no interaction
Clinical evidence, mechanism, importance and warning
57. – old man who took almost 1 year cyclosporin, azathioprine and prednisolone after kidney transplantation, due to onychomycosis began to take daily 500 mg of griseofulvin. After 2 weeks, he had decreased levels of cyclosporin with 90 ng / ml to 50 ng / ml, and despite the increase in the dose of cyclosporin from 2.8 to 4.8 mg / kg cyclosporine levels remained low. Later, when canceled griseofulvin, cyclosporin level increased to 200 ng / ml, and the dose of cyclosporine was adjusted 1. On the contrary, the authors of another report notes that have been recorded significant interaction when griseofulvin at a dose of 1 g was applied daily for 8 weeks for the treatment of tinea capitis: a patient with a kidney transplant, receiving cyclosporine, graft function remained stable 2
As for the single message about interacting with griseofulvin – its significance is not clear.
Stockley’s Drug Interactions / Ed. by Stockley. – 9th ed, 2010. – P. 1241.
The original article
1. Abu – Romeh S.H. Rashed A. Cyclosporin A and griseofulvin: another drug interaction // Nephron. – 1991. – 58. – P. 237.
2. Chen CH, Wen MC, Cheng CH, Wu MJ, Yu TM, Chuang YW, Shu KH. Infectious alopecia in a dog breeder after renal transplantation. J Chin Med Assoc (2008) 71, 477 -. 80
Symptoms: vomiting, drowsiness, headache, tachycardia, severe renal failure.
Treatment: stimulation of vomiting and gastric lavage (in the first hours after oral administration), maintaining vital functions; dialysis and hemoperfusion with activated charcoal ineffective.
Dosing and Administration
Inside, intravenously. daily dose divided into 2 doses. The solution for the on / in infusion is prepared ex tempore, by diluting the concentrate of isotonic sodium chloride solution or 5% glucose solution in the ratio 1: 20 – 1: 100; administered for 2 –. 6 hours Starting Dose ; 3 – 5 mg / kg per day. V / applications are considered optimal in the initial phase of treatment of patients with bone marrow transplantation. Oral solution may be diluted in a glass (not plastic) cup of cold chocolate drinks, milk, fruit juice (except grapefruit), Coca – cola, stir well and drink immediately. The capsules should be swallowed whole. When transplanting organs ; oral dose of 10 – 15 mg / kg for 4 – 12 hours before the operation only once, and then in the daily dose for 1 – 2 weeks; further dose was gradually reduced to maintenance (normally 2 – 6 mg / kg). In autoimmune diseases, ; orally at a daily dose of 2,5 – 5 mg / kg (except endogenous uveitis, wherein the short term may increase to a daily dose of 7 mg / kg).
Precautions substance Cyclosporine
The treatment should be carried out in a specialized hospital doctors who have sufficient experience of immunosuppressive therapy. It should be borne in mind that against cyclosporin increased predisposition to lymphoproliferative malignancies, so before assignment to decide whether the expected beneficial effect justifies the risk of adverse effects. Use during pregnancy is allowed only under strict indications. Since there is a possibility of anaphylactoid reactions at / in the introduction, is appropriate prophylactic antihistamines, and as rapidly as possible the patient’s transfer to oral lekform. It is recommended to select a dose depending on the content in the blood. After kidney transplantation, the plasma level is determined during the first 2 – x 2 weeks once a week for 3 – 6 weeks ; 1 time per week, at the outpatient ; 1 every 2 – 3 months. It requires regular monitoring of plasma concentrations of creatinine ; increase may indicate a rejection reaction or on the nephrotoxicity and demand (in the latter case) the reduction of the dose: more than 30% from baseline, and 50% when twice the level rises by 25% when increasing creatinine; when the dose reduction for 4 weeks did not reduce creatinine cyclosporin overturned. It is recommended to monitor blood pressure. potassium content in the blood, uric acid, bilirubin, transaminases, lipid profile, in the period of treatment is contraindicated immunization of live attenuated vaccines. In the treatment of autoimmune diseases lack of adequate positive results after 3 months demonstrates the need for discontinuation of treatment.
To prepare the infusion solution is desirable to use glass containers.
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