CYCLOSPORINE 100MG SOLUTION

Cyclosporine is a generic form of brand name Iminoral solution and the drug is a potent immunosuppressant drug used in treatment for rheumatoid arthritis, lupus, and other autoimmune diseases. Iminoral solution is studied as disease modifying anti-rheumatic drug (DMARD) because it not only reduces the pain and swelling of arthritis, but it may also prohibit joint damage and decrease the risk of long term disability. Iminoral solution is also admitted to less the progression of arthritis over time. Iminoral is a prescription drug used under the guidance of medical practioners

Cyclosporine

100mg/ml

50 ml in a bottle




Iminoral prescribed for

Iminoral solution is indicated for the prevent rejection of a transplanted organ. Iminoral solution is also indicated to reduce inflammation in active rheumatoid arthritis and severe psoriasis.

Mechanism of action of Iminoral solution

Cyclosporine targets to cyclophilin. The complex then prohibits calcineurin that is commonly responsible for stimulating transcription of interleukin 2. Cyclosporine also prevents lymphokine production and interleukin release. In ophthalmic applications, the actual mechanism of action is not known. Cyclosporine emulsion is thought to work as a partial immunomodulator in patients whose tear results is presumed to be conceal due to ocular inflammation along with keratoconjunctivitis sicca.



ADME properties of Iminoral solution

Incomplete and variable absorption from GI tract and bioavailability is 30% The time to high plasma concentration is 1.5-2.0 hours

Human plasma protein bound is 90%

In liver extensively metabolized by the cytochrome P450 3A enzyme system. To lesser degree is metabolized in gastrointestinal tract and kidney.

Primarily eliminated in biliary and in urine 6% and 0.1% excreted in urine as unchanged drug. Half-life in adults is 19 hours and in children is 7 hours




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cyclosporine-100mg

Ingredients Cyclosporine
Strength 100mg/ml
Pack 50 ml in a bottle
Rating

Solid Organ Transplantation
Precaution of organ rejection in kidney, liver, and heart allogeneic transplants; has been needed in combination with azathioprine and corticosteroids

In Oral route
15 mg/kg orally for 1 dose required for 4-12 hours pre-transplant
15 mg/kg/day orally divided twice daily required for 1-2 weeks post-transplant
5-10 mg/kg/day orally divided twice daily required for reduce 5% per week until

Solid Organ Transplantation, Paediatric (Off-Label)
In 6 months, young children have getting Iminoral toinhibit solid organ transplant rejection Dosage is same as adults, Even if children may necessary higher mg/kg dose than adults

In Oral route
15 mg/kg orally for 1 dose required for 4-12 hours pre-transplant
15 mg/kg/day orally divided twice daily required for 1-2 weeks post-transplant
5-10 mg/kg/day orally divided twice daily required for reduce 5% per week until

Rheumatoid Arthritis
Used for serious active, rheumatoid arthritis where the disease has not sufficient responded to methotrexate; may be needed in combination with methotrexate Iminoral 1.25 mg/kg orally twice daily; may raise by 0.5-0.75 mg/kg/day after 8 weeks and again after 12 weeks if required, not to exceed 4 mg/kg/day Discontinue if no improvement observed by 16 weeks Reduce the dose by 25-50% at any time to regulate adverse effects (e.g., hypertension, elevations in serum creatine greater than 30% pre-treatment level

Psoriasis
Used for treatment of adult, non-immunocompromised patients with serious, recalcitrant, plaque psoriasis who have decline to respond to at least 1 systemic treatment(e.g., PUVA, retinoids, or methotrexate) or in patients for whom other systemic therapies are contraindicated, or may not be tolerated Cyclomune: 1.25 mg/kg orally twice daily; may raise by 0.5 mg/kg/day after 4 weeks and every 2 weeks if required, not to exceed 4 mg/kg/day Interrupt if no improvement seen at 6 weeks on maximum daily dose of 4 mg/kg/day Reduce the dose by 25-50% at any time to regulateside effects (e.g., high blood pressure, elevations in serum creatine greater than 30% pre-treatment level

Side effects caused by Iminoral solution

Iminoral solution will have some common and serious side effects after treatment, some are given below

More common side effects
Hypertension Magnesium level is low in body In kidneys, blood clots occur Stomach pain Hair growth Acne Tremors Headache Gums size increased

Serious side effects
Liver damage - blood in urine; dark urine; pale stools; yellowing of your skin or the whites of your eyes; pain in your upper abdomen Kidney damage. Symptoms may include:blood in urine Heart problems. Symptoms may include:swelling of your feet or lower legs Lung problems. Symptoms may include:trouble breathing

Precautions

  • Iminoral solution may have high risk of serious infections. It may also raise the risk of developing a tumor or skin cancer
  • Iminoral solution weakens the immune system. If you administer this medication, you may be at higher risk for infections from bacteria, fungus, and viruses. These infections may be serious or life-threatening
  • If patient have psoriasis and have been treated with either psoralen plus ultraviolet A therapy, methotrexate, coal tar, radiation therapy, or ultraviolet light therapy, you may have an increased chance of occurring a skin disease while taking Iminoral solution Iminoral solution.
  • Iminoral solution medication may cause hypertension and renal disease.
  • Administrating Iminoral solution may cause liver damage and liver failure, specifically if you take high doses. It may even be fatal.

DRUG – DRUG INTERACTION

  • Adalimumab interaction with Iminoral both increase immunosuppressive effects and cause risk of infection. Avoid the usage of drug
  • Concomitant use with carbamazepine will reduce the level or effect of cyclosporine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid the usage of drug or Use Alternate Drug.
  • Acyclovir combination with Iminoral both increase nephrotoxicity and/or ototoxicity. Modify Therapy/Monitor Closely.
  • Iminoral solution increases levels of digoxin by reducing renal clearance. Avoid the usage of drug or Use Alternate Drug.
  • Azathioprine co administration with Iminoral both increase immunosuppressive effects and cause risk of infection

Contraindications

Iminoral solution is contraindicated to patients having; Hypersensitivity Breastfeeding Uses of Rheumatoid Arthritis (RA)/Psoriasis: Abnormal renal function, uncontrolled hypertension, malignancies Concomitant use of PUVA, UVB radiation, coal tar, methotrexate, other immunosuppressants will cause psoriasis



Iminoral solution Pregnancy category is C
1) studies in animals has revealed adverse effects to the foetus when the mother takes the drug.
2) Have no enough research done in humans to be certain how the drug might affect the foetus.

Iminoral solution passes through breast milk and may cause serious negative effects. Avoid using Iminoral during breastfeeding.

Iminoral solution stored at 20°-25° C Avoid the drug placing in moist or damp areas Protect away from light and high temperature

The patients decline to take a dose then immediately have the missed dose or skip the missed dose and follow regular schedule. Avoid taking extra dose Consult the doctor for more details

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