Cyclosporine

 
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More about Cyclosporine

What is/are Neoral Capsules?

CYCLOSPORINE is used to decrease the immune system's response to a transplanted organ. The medicine is also used for rheumatoid arthritis and psoriasis. This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care providers before I take this medicine?

They need to know if you have any of these conditions:

  • cancer
  • high blood pressure
  • immune system problems
  • infection
  • kidney disease
  • liver disease
  • previous coal tar, PUVA, ultraviolet, or radiation therapy
  • an unusual or allergic reaction to cyclosporine, alcohol, corn oil (Neoral only), castor oil, other medicines, foods, dyes, or preservatives
  • pregnant or trying to get pregnant
  • breast feeding

How should I use this medicine?

Take this medicine by mouth with a full glass of water. Do not take with grapefruit juice. Swallow the capsules whole. Do not chew or break the capsule. Follow the directions on the prescription label. Take your medicine at regular intervals. Take the capsules at the same time each day and at the same time in relation to meals. Do not take your medicine more often than directed. Do not stop taking except on your doctor's advice.

Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as 1 year for selected conditions, precautions do apply.

Patients over 65 years old may have a stronger reaction and need a smaller dose.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.

Note: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses. Call your doctor or health care professional if you miss more than one dose or if you miss doses on a regular basis.

What may interact with this medicine?

Do not take this medicine with any of the following:

  • bosentan
  • cidofovir
  • cisapride
  • mibefradil
  • ranolazine
  • red yeast rice, monascus purpureus
  • St. John's wort
  • tacrolimus

This medicine may also interact with the following:

  • acyclovir
  • allopurinol
  • amiloride
  • amiodarone
  • bromocriptine
  • carbamazepine
  • certain antibiotics
  • cimetidine
  • colchicine
  • danazol
  • digoxin
  • female hormones, including contraceptive or birth control pills
  • imatinib
  • medicines for fungal infections like amphotericin B, fluconazole, itraconazole, terbinafine, and ketoconazole
  • medicines for blood pressure like diltiazem, nicardipine, verapamil, enalapril, ramipril, and losartan
  • medicines for cholesterol like lovastatin, simvastatin, atorvastatin, and fenofibrate
  • medicines for HIV infection like indinavir, nelfinavir, ritonavir, and saquinavir
  • medicines that suppress the immune system
  • melphalan
  • methotrexate
  • metoclopramide
  • NSAIDs, medicines for pain and inflammation, like ibuprofen or naproxen
  • octreotide
  • orlistat
  • oxcarbazepine
  • phenobarbital
  • phenytoin
  • ranitidine
  • sirolimus
  • spironolactone
  • steroid medicines like prednisone or cortisone
  • sulfinpyrazone
  • ticlopidine
  • triamterene
  • vaccines
  • voriconazole

This list may not describe all possible interactions. Give your health care providers a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What side effects may I notice from this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:

  • allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
  • changes in vision
  • high blood pressure
  • increased urge to urinate or frequent urination
  • numbness or tingling in the hands and feet
  • seizures
  • severe stomach pain
  • vomiting
  • yellowing of the skin or the whites of the eyes

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):

  • bleeding or tender gums, overgrowth of gum tissue
  • diarrhea
  • excessive hair growth on the face or body
  • nausea
  • tremors

This list may not describe all possible side effects.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. You will have regular blood checks. Do not change the brand of medicine unless directed by your doctor or health care professional.

If you get a cold or other infection while receiving this medicine, call your doctor or health care professional. Do not treat yourself. The medicine may decrease your body's ability to fight infections.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

This medicine can make you more sensitive to the sun. Keep out of the sun. If you cannot avoid being in the sun, wear protective clothing and use sunscreen. Do not use sun lamps or tanning beds/booths.

The medicine can cause unusual growth of gum tissue and can make your gums bleed. Practice good oral hygiene, and be careful when brushing and flossing your teeth. See your dentist regularly.

Where should I keep this medicine?

Keep out of the reach of children.

Store Neoral between 20 and 25 degrees C (68 and 77 degrees F).

Store Gengraf between 15 and 30 degrees C (59 and 86 degrees F).

Keep the medicine in the original packaging. Throw away any unused medicine after the expiration date.

Medical uses

The immunosuppressive effect of ciclosporin was discovered on 31 January 1972 by employees of Sandoz (now Novartis) in Basel, Switzerland, in a screening test on immune suppression designed and implemented by Hartmann F. Stähelin, M.D. The success of ciclosporin in preventing organ rejection was shown in kidney transplants by Calne and colleagues at the University of Cambridge, and in liver transplants performed by Dr. Thomas Starzl at the University of Pittsburgh Hospital. The first patient, on 9 March 1980, was a 28-year-old woman. Ciclosporin was subsequently approved for use in 1983. Since then, it has been used to prevent and treat graft-versus-host reactions in bone-marrow transplantation and to prevent rejection of kidney, heart, and liver transplants.

In addition to transplants, ciclosporin is also used in psoriasis, severe atopic dermatitis, pyoderma gangrenosum, chronic autoimmune urticaria, and, infrequently, in rheumatoid arthritis and related diseases, although it is only used in severe cases. It is commonly prescribed in the US as an ophthalmic emulsion for the treatment of dry eyes. It has been investigated for use in many other autoimmune disorders, and is sometimes prescribed in veterinary cases, particularly in extreme cases of immune-mediated hemolytic anemia. Inhaled ciclosporin has been investigated to treat asthma and is being studied as a preventive therapy for chronic rejection of the lungs. Ciclosporin has also been used to help treat patients with acute severe ulcerative colitis that do not respond to treatment with steroids. This drug is also used as a treatment of posterior or intermediate uveitis with noninfective etiology. Ciclosporin is a drug currently used to experimentally treat cardiac hypertrophy (an increase in cell volume).

Ciclosporin has been investigated as a possible neuroprotective agent in conditions such as traumatic brain injury, and has been shown in animal experiments to reduce brain damage associated with injury. Ciclosporin blocks the formation of the mitochondrial permeability transition pore, which has been found to cause much of the damage associated with head injury and neurodegenerative diseases. Ciclosporin's neuroprotective properties were first discovered in the early 1990s when two researchers (Eskil Elmér and Hiroyuki Uchino) were conducting experiments in cell transplantation. An unintended finding was that CsA was strongly neuroprotective when it crossed the blood–brain barrier. This same process of mitochondrial destruction through the opening of the MPT pore is implicated in making traumatic brain injuries much worse. Cyclosporine is currently in a phase II/III (adaptive) clinical study in Europe to determine its ability to ameliorate neuronal cellular damage in traumatic brain injury. This multi-center study is being organized by NeuroVive Pharma and the European Brain Injury Consortium using NeuroVive's formulation of cyclosporine called NeuroSTAT®.

Adverse effects

Treatment may be associated with a number of potentially serious adverse drug reactions (ADRs).

ADRs can include gingival hyperplasia, convulsions, peptic ulcers, pancreatitis, fever, vomiting, diarrhea, confusion, hypercholesterolemia, dyspnea, numbness and tingling particularly of the lips, pruritus, high blood pressure, potassium retention possibly leading to hyperkalemia, kidney and liver dysfunction (nephrotoxicity and hepatotoxicity), burning sensations at finger tips and an increased vulnerability to opportunistic fungal and viral infections.

An alternate form of the drug, cyclosporin G (OG37-324), has been found to be much less nephrotoxic than the standard ciclosporin (cyclosporin A). Cyclosporin G (molecular mass 1217) differs from cyclosporin A in the amino acid 2 position, where an L-norvaline replaces the α-aminobutyric acid.

Ciclosporin is listed as IARC Group 1 carcinogens (sufficient evidence of carcinogenicity in humans).

Mechanism of action

In medicine, the most important effect of cyclosporin is to lower the activity of T cells and their immune response.

Ciclosporin binds to the cytosolic protein cyclophilin (immunophilin) of lymphocytes, especially T cells. This complex of ciclosporin and cyclophilin inhibits calcineurin, which, under normal circumstances, is responsible for activating the transcription of interleukin 2. In T-cells, activation of the T-cell receptor normally increases intracellular calcium, which acts via calmodulin to activate calcineurin. Calcineurin then dephosphorylates the transcription factor nuclear factor of activated T-cells (NFATc), which moves to the nucleus of the T-cell and increases the activity of genes coding for IL-2 and related cytokines. Ciclosporin prevents the dephosphorylation of NF-AT by binding to cyclophilin. It also inhibits lymphokine production and interleukin release and, therefore, leads to a reduced function of effector T-cells. It does not affect cytostatic activity.

Ciclosporin affects mitochondria by preventing the mitochondrial permeability transition pore from opening, thus inhibiting cytochrome c release, a potent apoptotic stimulation factor. This is not the primary mechanism of action for clinical use, but is an important effect for research on apoptosis.

Ciclosporin binds to the cyclophilin D protein (CypD) that constitutes part of the mitochondrial permeability transition pore (MPTP), and by inhibiting the calcineurin phosphatase pathway. The MPTP is found in the mitochondrial membrane of cardiac myocytes (heart muscle cells) and moves calcium ions (Ca2+
) into the mitochondria. When open, Ca2+
enters the mitochondria, disrupting transmembrane potential (the electric charge across a membrane). If unregulated, this can contribute to mitochondrial swelling and dysfunction. To allow for normal contraction, intracellular Ca2+
increases, and the MPTP in turn opens, shuttling Ca2+
into the mitochondria. Calcineurin is a Ca2+
-activated phosphatase (enzyme that removes a phosphate group from substrate) that regulates cardiac hypertrophy. Regulation occurs through NFAT (nuclear factor of activated T-cells) activation, which, when dephosphorylated, binds to GATA and forms a transcription factor (protein that can bind DNA and alter the expression of DNA) with ability to control the hypertrophic gene (2). Activation of calcineurin causes increases in hypertrophy.

This article uses material from the Wikipedia article Cyclosporine, which is released under the Creative Commons Attribution-Share-Alike License 3.0.

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Medicine containing Gengraf

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Medicine containing Cyclosporine

This page uses publicly available data from the U.S. National Library of Medicine (NLM), National Institutes of Health, Department of Health and Human Services; NLM is not responsible for the page and product and does not endorse or recommend this or any other product.

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