Ciclosporin


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Immunosuppression in organ transplant Initial: 10-15 mg/kg/day, starting 4-12 hr pre-op and continue for 1-2 wk. Maintenance: 2-6 mg/kg/day. Psoriasis; Severe atopic dermatitis 2.5 mg/kg/day. Max: 5 mg/kg/day. Rheumatoid arthritis 2.5 mg/kg/day for 6-8 wk. Max: 4 mg/kg/day. Nephrotic syndrome 5 mg/kg/day. IV Prevention of graft rejection in bone marrow transplantation Initial: 3-5 mg/kg/day starting on the day before transplant, continue for up to 2 wk until maintenance via oral administration. Organ transplantation Initial: 5-6 mg/kg/day as a single dose infusion. Transfer to oral administration as soon as possible.
Dosage Details
Intravenous
Prophylaxis of graft rejection in bone marrow transplantation
Adult: Intially, 3-5 mg/kg/day starting on the day before transplantation and continue for up to 2 wk or until oral therapy can be initiated at a maintenance of 12.5 mg/kg/day. Continue maintenance dose for at least 3-6 mth.

Intravenous
Immunosuppression in organ transplantation
Adult: Initially: 5-6 mg/kg/day as a single dose, infuse dose over 2-6 hr. Switch to an oral dosage form as soon as possible.

Oral
Nephrotic syndrome
Adult: 5 mg/kg daily, given in 2 divided doses.
Child: 6 mg/kg daily, given in 2 divided doses.

Oral
Psoriasis, Severe atopic dermatitis
Adult: Initially, 2.5 mg/kg/day, in 2 divided doses. Reduce to lowest effective dose once remission is achieved. Stop treatment if there is no sufficient improvement to max dose within 6 wk. Max: 5 mg/kg/day.

Oral
Rheumatoid arthritis
Adult: 2.5 mg/kg/day, in 2 divided doses. Treatment should continue for 6-8 wk. If response is insufficient, may increase dose gradually. Max: 4 mg/kg/day.

Oral
Immunosuppression in organ transplantation
Adult: Initially, 10-15 mg/kg/day, starting 4-12 hr before procedure and continued for 1-2 wk; usual maintenance: 2-6 mg/kg/day. Lower doses may be used when combined with other immunosuppressants.
Administration
May be taken with or without food. Take consistently w/ regard to time of day & relation to meals. Avoid grapefruit juice.
Contraindications
Hypersensitivity; malignant neoplasms; uncontrolled hypertension; psoriasis; lactation.
Special Precautions
Renal and hepatic impairment; hyperuricaemia; anaphylaxis; history of allergic reactions; pregnancy; monitor BP, serum electrolytes, renal and hepatic function.
Adverse Reactions
Hypertension; hepatoxicity; tremor; paraesthesia, hypertrichosis, facial oedema, acne; gingival hypertrophy; hyperkalaemia, fluid retention; increased susceptibility to infections; GI symptoms.
Potentially Fatal: Nephrotoxicity; convulsions.
IV/Parenteral/PO: C
Overdosage
Transient hepatotoxicity and nephrotoxicity may occur. General supportive measures and symptomatic treatment may be used in cases of overdosage.
Drug Interactions
Increased ciclosporin level by diltiazem, doxycycline, erythromycin, ketoconazole, methylprednisolone (high doses), nicardipine, verapamil, oral contraceptives. Drugs which reduce ciclosporin level are carbamazepine, isoniazid, phenobarbitone, phenytoin and rifampicin. Increased risk of convulsion when used concurrently with high-dose methylprednisolone.
Potentially Fatal: Additive nephrotoxicity when used with aminoglycosides, amphotericin B, ciprofloxacin, colchicine, melphalan, co-trimoxazole and NSAIDs.
Action
Description: Ciclosporin is a strong immunosuppressant that acts mainly on the helper T-cells. It inhibits the activation of calcineurin and production of interleukin-2, thus reducing cell-mediated immune response.
Pharmacokinetics:
Absorption: Incompletely and variably absorbed from the GI tract (oral).
Distribution: Widely distributed; crosses the placenta and enters breast milk. Protein-binding: 90%.
Metabolism: Hepatic: Extensive.
Excretion: In faeces via the bile; 5-20 hr (elimination half-life), more rapid in children.
Storage
Store at 25°C.
MIMS Class
ATC Classification
L04AD01 - ciclosporin ; Belongs to the class of calcineurin inhibitors. Used as immunosuppressants.
S01XA18 - ciclosporin ; Belongs to the class of other ophthalmologicals .
Disclaimer: This information is independently developed by MIMS based on Ciclosporin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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