Cyclosporine (Oral Route)

When a patient is given an organ transplant they are given Cyclosporine and other medications to help prevent the body from rejecting the new organ.

Overview

Cyclosporine is an immunosuppressive agent. It is given to patients who have received an organ transplant to help prevent their body from rejecting the new organ. Cyclosporine is used alongside other medications in patients receiving organ transplants. These transplants can include kidneys, livers and hearts.

When a transplant is given to a patient the body’s natural response is to try and reject the organ because it is a foreign body. The white blood cells will attack the transplanted organ and in doing so can cause a sometimes fatal rejection of the transplanted organ. Cyclosporine will weaken the immune system and reduce the count of white blood cells so that the body cannot attack the organ.

Cyclosporine can also be used in the treatment of severe rheumatoid arthritis, severe plaque psoriasis and other conditions where treatment with methotrexate has failed previously. This medication is not a first option for the treatment of these conditions.

Cyclosporine is a serious medication that can have severe side effects on the body. It can cause severe kidney problems in patients and will decrease the patient’s ability to fight infections. Before use, you should seriously consider the risks of using this treatment with your doctor.

This medication is available only when prescribed by a doctor and comes in the form of Gengraf, Neoral or SandIMMUNE.

This medication is administered in the following forms:
• Capsule
• Liquid filled capsule
• Solution

Conditions treated

• Organ transplant
• Severe rheumatoid arthritis
• Severe plaque psoriasis

Type of medicine

• Immunosuppressant

Side effects

As an immunosuppressive agent, the use of Cyclosporine will cause unwanted side effects in the body. This treatment works by limiting the natural protection in the patient’s body and as such will cause unwanted side effects as well as increasing the risk of infection. Some of these side effects will require that the patient seeks immediate medical attention, while other side effects will abate over time and do not indicate wide medical problems.

If you experience any of the following side effects then you should inform your doctor immediately:

Occurring more commonly:

• Back pains
• Black stools with a tarry appearance
• Blurring of vision
• Chest pains
• Chills
• Cloudy urine
• Coughing
• Decrease in appetite
• Decrease in volume of urine output
• Decreased ability to concentrate urine
• Dizziness
• Drowsiness
• Feverishness
• Headaches
• Increased or decreased heartbeat
• Itching
• Loss of hunger
• Muscle spasming or twitching
• Nausea
• Nervousness
• Pain or difficulty experienced during urination
• Pain or tenderness in the stomach or abdomen
• Pounding felt in the ears
• Severe throbbing in the head
• Shakiness felt in the legs, arms, hands or feet
• Shortness of breath without exertion
• Skin rash
• Soreness of the throat
• Sores or ulcers on the mouth
• Stools with a clay-like colouration
• Swelling of the glands
• Swollen feet or lower legs
• Trembling or shaking of hands and/or feet
• Unusual bleeding
• Unusual bruising
• Unusual tiredness
• Unusual weakness
• Unusually dark urine
• Vomiting
• White spots appearing on the lips or mouth
• Yellowing of the eyes
• Yellowing of the skin

Occurring less commonly:

• Appearance of hives
• Bleeding from the gums
• Blood in the urine
• Blood in the vomit
• Convulsions or seizures
• Difficulty in swallowing
• Paling of the skin
• Pins and needles feelings or tingling in the skin
• Puffy or swollen around the eyes, face, lips or tongue
• Red spots appearing on the skin
• Severe or ongoing stomach pain
• Tightness in the chest
• Trouble in breathing with exertion

Occurring only rarely:

• Bloating
• Chest discomfort
• Constipation
• Darkening of the urine
• Hoarseness
• Indigestion
• Lower back pain
• Night sweats
• Pain or discomfort experienced in the arms, jaw, back or neck
• Pains experienced in the stomach, side, abdomen and sometimes the back
• Side pain
• Sweating when cool
• Vomiting of a material with the appearance of coffee grounds
• Vomiting of blood

Other side effects can occur that would not normally require the patient to seek medical attention. Some of these side effects will abate over time and some will only be mild. If the side effects do become bothersome or are ongoing, however, then you can always contact your doctor for advice on how best to alleviate these side effects:

Occurring more commonly:

• Abdominal discomfort
• Bleeding, or enlargement of the gums
• Blemishes appearing on the skin
• Blocked nose
• Increased growth of hair, most commonly on the face
• Pimples or spots appearing on face and body
• Runny nose
• Stomach discomfort
• Tender skin around the eyes and cheekbones

Occurring less commonly:

• Brittle fingernails
• Burning feeling in the chest
• Burning feeling in the stomach
• Cramping
• Dry or itchy eyes
• Eye discharge or excessive tearing
• Feeling of warmth when cool
• Hearing changes or loss
• Inflammation or irritation of the eye or eyelid
• Reddening of the face, neck, arms and/or the upper chest
• Ringing or buzzing sounds heard that are not heard by others
• Swollen or tender breasts in both males and females
• Weight loss

Occurring only rarely:

• Blurring of or loss of vision
• Changed colour perception
• Discouragement or loss of confidence
• Double vision
• Experiencing sad or empty feelings
• Fearfulness
• Halos seen around lights
• Irritability or quickness to annoyance and anger
• Joint pains
• Loss of interest
• Loss of pleasure
• Night blindness
• Overbright appearance of lights
• Tiredness
• Trouble in concentrating
• Trouble in sleeping
• Tunnel vision
• Unusual drowsiness
• Unusual dullness
• Unusual feeling of sluggishness
• Unusual tiredness
• Unusual weakness
• Weight loss

Other side effects can occur that have not been listed herein. If you experience any other side effects then you should contact your doctor for advice. If you believe your health is at immediate risk, however, then you should contact the emergency services right away.

Dosage

This medication should only be used as directed by your doctor. Using too much or using it too frequently will put you at risk of developing serious medical conditions. Using too little or missing doses may increase your risk of rejection of the transplanted organ.

This medication will always be given with other medications and you should follow your daily medication plan exactly.

Do not change brands of medications because each brand will work differently. This medication should be taken consistently at the same time every day so that a habit is formed. Missing this medication will have very serious consequences.

The oral liquid should be measured in the provided syringe and should be taken mixed with room temperature liquids in a glass container (not plastic). Stir the medication thoroughly and drink it directly. Do not clean the syringe with either water or cleaning agents.

Do not consume grapefruit or grapefruit juice with this treatment.

Do not stop the use of this treatment or make changes to use without discussing this with your doctor.

The use and dose of this treatment will be determined by your doctor and will differ for the treatment of each condition and for each patient. You should follow the directions given to you by your doctor only.

If you miss a dose of this treatment then you should take it as soon as possible. If you are close to your next dose, however, then you should contact your doctor for advice. Your doctor may tell you to take it or to skip the missed dose, but you should never take a double dose of the treatment as this will expose you to severe risks.

Interactions

Certain medications should never be used together. This is because they can react violently with one another and expose the patient to serious risks. In other cases, medications can stop one another from working or can increase the risk of occurrence of certain side effects. In these cases, your doctor may prescribe both treatments, but they may wish to change the dose or frequency of use of one or more treatment. Before beginning treatment, you should inform your doctor of all medications that you are taking including other prescription treatments, over the counter medications, herbal remedies and vitamin supplements.

The following medications should not be used in conjunction with Cyclosporine. Your doctor may change one medication or may decide not to prescribe Cyclosporine if you are taking any of the following:

• Sitaxsentan
• Simvastatin
• Pitavastatin
• Mifepristone
• Grazoprevir
• Dronedarone
• Colchicine
• Bosentan
• Amifampridine

The use of the following medications would not normally be recommended alongside Cyclosporine. Your doctor may prescribe both in some cases but the doses and frequency of use will need to be managed by your doctor:

• Yellow Fever Vaccine
• Voriconazole
• Vincristine Sulfate Liposome
• Vincristine
• Vilazodone
• Venetoclax
• Varicella Virus Vaccine
• Valdecoxib
• Typhoid Vaccine, Live
• Topotecan
• Tolmetin
• Tolfenamic Acid
• Tiaprofenic Acid
• Tetanus Toxoid
• Tenoxicam
• Telithromycin
• Telaprevir
• Tacrolimus
• Sulindac
• Sulfinpyrazone
• St John's Wort
• Sodium Salicylate
• Smallpox Vaccine
• Simeprevir
• Siltuximab
• Silodosin
• Secukinumab
• Salsalate
• Salicylic Acid
• Rubella Virus Vaccine, Live
• Rotavirus Vaccine, Live
• Rosuvastatin
• Rofecoxib
• Ritonavir
• Rifampin
• Rifabutin
• Red Yeast Rice
• Ranolazine
• Rabies Vaccine
• Pyrazinamide
• Proquazone
• Propyphenazone
• Propionic Acid
• Proglumetacin
• Pravastatin
• Posaconazole
• Poliovirus Vaccine, Live
• Pneumococcal Vaccine, Diphtheria Conjugate
• Pneumococcal Vaccine Polyvalent
• Plague Vaccine
• Pixantrone
• Pitolisant
• Piroxicam
• Piperaquine
• Piketoprofen
• Phenylbutazone
• Pertussis Vaccine
• Perindopril
• Pazopanib
• Paritaprevir
• Parecoxib
• Oxyphenbutazone
• Oxaprozin
• Orlistat
• Ombitasvir
• Octreotide
• Nimesulide Beta Cyclodextrin
• Nimesulide
• Niflumic Acid
• Nicardipine
• Nepafenac
• Naproxen
• Nafcillin
• Nabumetone
• Mycophenolic Acid
• Mumps Virus Vaccine, Live
• Morphine Sulfate Liposome
• Morphine
• Morniflumate
• Meningococcal Vaccine
• Meloxicam
• Mefenamic Acid
• Meclofenamate
• Measles Virus Vaccine, Live
• Lyme Disease Vaccine (Recombinant OspA)
• Lumiracoxib
• Lumacaftor
• Loxoprofen
• Lovastatin
• Lornoxicam
• Lanreotide
• Ketorolac
• Ketoprofen
• Itraconazole
• Isavuconazonium Sulfate
• Influenza Virus Vaccine
• Infliximab
• Indomethacin
• Idelalisib
• Ibuprofen Lysine
• Ibuprofen
• Hepatitis A Vaccine, Inactivated
• Haemophilus B Vaccine
• Golimumab
• Foscarnet
• Flurbiprofen
• Flufenamic Acid
• Fluconazole
• Floctafenine
• Feprazone
• Fepradinol
• Fentanyl
• Fenoprofen
• Felodipine
• Felbinac
• Etravirine
• Etoricoxib
• Etoposide
• Etofenamate
• Etodolac
• Enzalutamide
• Eluxadoline
• Eliglustat
• Efavirenz
• Droxicam
• Doxorubicin Hydrochloride Liposome
• Doxorubicin
• Donepezil
• Domperidone
• Dipyrone
• Diphtheria Toxoid, Adsorbed
• Diltiazem
• Diflunisal
• Diclofenac
• Dexketoprofen
• Dexibuprofen
• Dasabuvir
• Dabigatran Etexilate
• Cyclophosphamide
• Crizotinib
• Conivaptan
• Cobicistat
• Clonixin
• Choline Salicylate
• Cholic Acid
• Cerivastatin
• Ceritinib
• Celecoxib
• Caspofungin
• Carbamazepine
• Bupropion
• Bufexamac
• Bromfenac
• Blinatumomab
• Black Cohosh
• Bacillus of Calmette and Guerin Vaccine, Live
• Atorvastatin
• Aspirin
• Amtolmetin Guacil
• Amlodipine
• Aliskiren
• Alfalfa
• Alefacept
• Afatinib
• Acemetacin
• Aceclofenac

The use of the following medications can increase the risk of certain side effects occurring. They can also increase the risk of experiencing more severe side effects. Your doctor may still prescribe both Cyclosporine and one of the following treatments but they may need to adjust the dose or the frequency of use of one or both treatments:

• Warfarin
• Verapamil
• Troglitazone
• Tolterodine
• Tobramycin
• Terbinafine
• Sulfasalazine
• Sulfadiazine
• Sirolimus
• Saquinavir
• Rifapentine
• Repaglinide
• Quinupristin
• Quinine
• Propafenone
• Probucol
• Phenytoin
• Oxypurinol
• Norgestrel
• Norgestimate
• Norfloxacin
• Norethindrone
• Norelgestromin
• Nevirapine
• Nelfinavir
• Nefazodone
• Mycophenolate Mofetil
• Modafinil
• Miokamycin
• Midazolam
• Mibefradil
• Metronidazole
• Metoclopramide
• Methylprednisolone
• Methotrexate
• Mestranol
• Mercaptopurine
• Melphalan
• Medroxyprogesterone Acetate
• Levonorgestrel
• Ketoconazole
• Josamycin
• Indinavir
• Imipenem
• Glyburide
• Glipizide
• Furosemide
• Fosphenytoin
• Fosamprenavir
• Fluvoxamine
• Fenofibrate
• Famotidine
• Ezetimibe
• Etonogestrel
• Ethynodiol Diacetate
• Ethinyl Estradiol
• Estradiol Valerate
• Estradiol Cypionate
• Erythromycin
• Drospirenone
• Dirithromycin
• Digoxin
• Dienogest
• Desogestrel
• Danazol
• Dalfopristin
• Colesevelam
• Clonidine
• Clindamycin
• Clarithromycin
• Cisapride
• Ciprofloxacin
• Cimetidine
• Chloroquine
• Chloramphenicol
• Bromocriptine
• Boceprevir
• Azathioprine
• Amprenavir
• Amphotericin B Liposome
• Amphotericin B Lipid Complex
• Amphotericin B Cholesteryl Sulfate Complex
• Amphotericin B
• Amiodarone
• Ambrisentan
• Allopurinol
• Acetazolamide

Other interactions with medications that have not been listed herein may also occur. In cases where other side effects occur you should consult your doctor for advice. If you believe your health is at immediate risk, however, then you should contact the emergency services.

The use of Cyclosporine can also be affected by the consumption of certain juices. Patients should avoid consumption of the following during treatment:

• Grapefruit juice
• Pomelo juice

Other medical conditions can also affect the use of this treatment in patients. Certain medical conditions may prohibit the use of certain treatments and some medical conditions can be worsened by the use of Cyclosporine. You should inform your doctor of all medical conditions from which you suffer. This is especially important in the following cases:

Patients being treated for rheumatoid arthritis should not be treated with the Neoral brand of Cyclosporine if they suffer from any of the following conditions:

• Abnormal kidney function
• Cancer
• Hypertension

This medication can worsen the following conditions because it contains alcohol:

• History of alcohol abuse
• Epilepsy
• Liver disease

The following conditions may be worsened by the use of this treatment:

• Anemia
• Bleeding problems
• Brain disease
• Cancer
• Eye problems
• Visual problems
• Hyperkalemia
• Hypertension
• Hyperuricemia
• Kidney disease
• Precancerous skin changes
• History of seizures
• Thrombocytopenia

The patient’s body will have a reduced ability to fight infection during treatment with Cyclosporine. Patients with infections may suffer worse effects when they begin treatment.

Other medical conditions that have not been listed herein may also inhibit the use of this treatment. You should inform your doctor of all medical conditions from which you suffer from or have suffered from in the past before beginning treatment with this medication.

Warnings

Before beginning treatment with the medication, you should very seriously consider the risks of doing so. These should be weighed against the benefits of use to determine whether you should begin treatment. You should make this decision with the help of your doctor, to ensure that all factors have been considered you should ensure that you have discussed the following before use:

Allergies – If you have ever reacted unusually to any medications in the past then it is vital that you inform your doctor of this. Allergies to medications may put you at serious risk once your immune system has been lowered by Cyclosporine. You should inform your doctor of any other allergies from which you suffer before beginning treatment too. These include allergies to dyes, preservatives, foods, animals and other substances.

Pediatric – No appropriate studies have been performed on the use of Cyclosporine in children who are receiving transplants or organs. However, in use, there have been no specific problems reported from the use to date. You should discuss risks with your doctor.
- No appropriate studies have been carried out for use in the treatment of rheumatoid arthritis or psoriasis in children. Neither safety of use nor efficiency of use has been established in children.

Geriatric – No age-specific limitations have been determined for the use of Cyclosporine in the elderly. Elderly patients will, however, have a greater risk of age-related medical conditions. These can include conditions of the kidney, liver, heart and blood that can require adjustments to treatment.

Pregnancy – Serious risks will be posed to the unborn baby with the use of this treatment in a pregnant woman. You should inform your doctor if you are pregnant before use and should follow appropriate contraceptive practices during use to prevent pregnancy. If you believe you may or believe you have become pregnant during use then you should discuss this with your doctor straight away.

Breastfeeding – It is unknown whether a nursing child may be put at risk by the use of this treatment when breastfeeding. Patients should discuss breastfeeding an infant with their doctor and should weight the benefits of doing so against the potential risks before beginning use.

When using this treatment your doctor will need to check on your progress regularly to ensure that the treatment is working effectively and to test for unwanted side effects. Your doctor will need to take blood samples and urine samples in order to ascertain this.

You will need to have your blood pressure recorded before you begin treatment as a benchmark and then again regularly during treatment to look for changes. If you notice any changes in blood pressure or heart behaviour, then it is recommended that you make immediate contact with your doctor.

Serious kidney problems can develop during the use of this treatment. You should be alert to the symptoms of these conditions including the following:

• Changes in urination volume and frequency
• Difficulty in breathing
• Blood in the urine
• Drowsiness
• Increased thirstiness
• Loss of hunger
• Nausea
• Vomiting
• Swelling in the feet
• Swelling in the lower legs

You should not take any supplement that contains salt, salt substitutes or potassium without discussing use with your doctor first. Doing so may put the kidney and liver at risk.

Serious liver problems may occur from the use of this treatment. Symptoms of these problems of the liver can include:

• Tenderness of the upper stomach
• Paling of stools
• Darkening of urine
• Lack of hunger
• Nausea
• Yellowing of the eyes
• Yellowing of the skin
• Vomiting

Patients who use this treatment will be exposed to a greater risk of developing cancer of the skin or cancer of the lymph system. If you have any concerns about these risks then you should inform your doctor.

Patients using this medication will be at greater risk of developing infections. In order to decrease the risk of developing infections patients should follow these simple steps:

• Avoid people who have infections wherever it is possible to do so.
• Avoid prolonged contact with other people and particularly people who have been in public places recently.
• Do not receive vaccinations or immunizations.
• Do not come into contact with people who have received the oral polio vaccination recently.
• Consider wearing face protection when you are outside.
• Use caution when cleaning your mouth and consider using alternative methods of cleaning than toothbrushes and toothpicks.
• Be careful when using sharp implements.
• Wash your hands frequently and carry disinfectant rubs when you are unable to.
• Only touch your eyes or the inside of your nose when you have washed your hands and face immediately beforehand.
• Avoid eating sharp foods like crisps that may cut your mouth or lips.
• Tell your doctor immediately if you think you are developing an infection or a cough or cold.

Patients taking Cyclosporine with be at increased risk of developing rare viral infections. These can include:

• Progressive multifocal leukoencephalopathy (PML)
• Polyoma virus-associated nephropathy (PVAN)

These conditions can affect the effective use of the kidney and could cause a kidney transplant to fail or could cause the development of kidney problems. If you experience any of the following symptoms of these conditions during treatment then you should immediately inform your doctor:

• Bloody urine
• Decreased frequency of urination
• Decreased volume of urination
• Increased thirstiness
• Loss of usual appetite
• Back pain
• Side pain
• Swelling of the hands, finders or feet
• Troubled breathing
• Unusual weakness
• Unusual tiredness
• Vomiting
• Weight gain

During treatment with Cyclosporine, you should not receive any vaccinations or immunizations. As your body’s natural defences will be weakened, there is a high chance that you could actually catch the disease that you are trying to protect against. Members of your household should also avoid the receipt of live vaccines because they could pass these on to you. If you do come into contact with someone who has received a live vaccination then you should keep your distance and consider wearing a protective mask. If you have any questions about this then you should discuss them with your doctor before beginning use.

Some patients and most commonly in younger patients, gum conditions may develop. These conditions can include swelling, bleeding and pain of the gums that will appear shortly after treatment begins. You can help to prevent this by keeping your mouth clean and by massaging your gums. You should seek advice from your dentist about how best you can keep your mouth and gums clean and comfortable during this treatment. Visit a dentist if you start experiencing these side effects and they can help alleviate them. Ensure that you explain that you are taking this treatment when you do visit them.

This medication can make both the skin and eyes more sensitive to light. This will increase your risk of developing skin cancer. You should not use sunbeds or sunlamps during treatment and you should avoid prolonged periods in the sun. Wear suncream at all times when you are in the sun.

This medication may cause serious damage to the nervous system. If you begin to experience the following symptoms then you should contact medical services immediately:

• Confusion or disorientation
• Loss of consciousness
• Mental changes
• Muscle weaknesses
• Seizures or convulsions
• Changes to vision

Do not take any other medications during treatment with this medication. You should consult your doctor before beginning treatment with any other medication and should inform all medical professionals that you are taking this treatment.

Storage

Cyclosporine should be stored in a sealed container at room temperature at all times. It should always be stored out of the reach of children and away from heat, moisture and light. Prevent this medication from freezing.

Unused oral liquid should be disposed of after 60 days of opening. Ask your healthcare professional how to dispose of the unwanted medication. Do not clean the syringe used for application of the liquid treatment with either water or other cleaning products. Simply return it to its original packaging between uses.

Summary

Cyclosporine is an immunosuppressive agent. This means that it suppresses the immune system of the patient and reduces the normal function of the body. Cyclosporine is mainly used in the treatment of patients receiving an organ transplant. By suppressing the immune system the treatment reduces the chance of the patient rejecting the organ that has been transplanted.

Cyclosporine can also be used in the treatment of severe rheumatoid arthritis, severe plaque psoriasis and other conditions where treatment with methotrexate has failed previously. This medication is not a first option for the treatment of these conditions and should only be used when other options have not worked for the patient.

The use of Cyclosporine is a very serious undertaking that can have severe and far-reaching effects. This treatment can put the patient at risk of kidney failure, liver failure and can increase the chances of developing certain forms of cancer including skin cancer and cancer of the lymph system. Patients should not undertake this treatment lightly and should seriously consider the risks in relation to the benefits of use before beginning treatment. If you have any concerns then you should discuss them with your doctor before beginning treatment.