Ciclosporin

Ciclosporin (Cyclosporine): Uses, Dosage and Side Effects

Overview

The action of Ciclosporin is T-lymphocyte inhibition.

Uses of Ciclosporin

• Topical ophthalmic preparation for immune-mediated keratoconjunctivitis sicca in dogs.
• Used as an Immunosuppressant in chronic superficial keratoconjunctivitis (pannus).
• Oral preparation licensed for atopic dermatitis in dogs and cats.
• Used for perianal fistula, sebaceous adenitis, and immune-mediated disease.

Dose of Ciclosporin in Dogs and Cats

Dogs:

• Ocular disease: apply approximately 0.5 cm of ointment to the affected eye q12h. It may take 2–4 weeks for improvement to occur (occasionally up to 12 weeks). Maintenance treatment should be continued with application q12h; in cases of excessive tear production, the application can be reduced to q24h but only with caution and long-term, regular monitoring of tear production.
• Atopic dermatitis: 5 mg/kg p.o. q24h until signs are controlled.
• Perianal fistula, sebaceous adenitis: 5 mg/kg p.o. q24h – may be increased in non-responsive cases to q12h.
• Immune-mediated disease: 5 mg/kg p.o. q12h. A proportion of dogs may require higher doses and pharmacodynamic monitoring is therefore advisable.

Cats:

• Atopic dermatitis: 7 mg/kg p.o. q24h until signs are controlled.
• Immune-mediated disease:  3–5 mg/kg p.o. q12h or 5–7 mg/kg p.o. q24h.

Side Effects of Ciclosporin in Dogs and Cats

• Immediate discomfort on topical application (blepharospasm) has been reported in dogs.
• Transient vomiting and diarrhea may follow systemic administration
• Anorexia; mild to moderate gingival hyperplasia; hypertrichosis; papillomatous lesions of the skin; red and swollen pinnae; muscle weakness; and muscle cramps are infrequently observed signs.
• Systemic and topical treatment may be associated with an increased risk of malignancy.
• Cats that are seronegative for Toxoplasma gondii may be at risk of developing clinical toxoplasmosis if they become infected while undergoing treatment.

Contraindications of Ciclosporin in Dogs and Cats

• Systemic use is not recommended in dogs and cats up to 6 months old or in dogs <2 kg or in cats <2.3 kg.
• Do not use in progressive malignant disorders.
• Do not give live vaccines during treatment or within a 2-week interval before or after
  treatment.
• Ciclosporin may reduce the immune response to vaccines.
• The manufacturer does not recommend use in diabetic dogs or cats infected with FeLV, FIV

Some Notes:

1. It is recommended that bacterial and fungal infections are treated before use. .
2. In dogs with atopic dermatitis, ciclosporin may reduce circulating levels of insulin and cause an increase in blood glucose and fructosamine.
3. In dogs with diabetes mellitus, the effect of treatment on glycemia must be carefully monitored.
4. The metabolism of ciclosporin is reduced, and thus serum levels increased, by various drugs that competitively inhibit or induce enzymes involved in its metabolism, particularly cytochrome P450, including diltiazem, doxycycline and imidazole antifungal drugs.
5. Itraconazole and ketoconazole at 5–10 mg/kg are known to increase the blood concentration of ciclosporin in dogs up to five-fold, which is considered to be clinically relevant.
6. During concomitant use of itraconazole and ciclosporin consider halving the dose or doubling the treatment interval if the dog is on daily treatment.
7. Increased risk of hyperkalemia if used with ACE inhibitors. As a substrate and inhibitor of the MDR 1 P-glycoprotein transporter, co-administration of ciclosporin with P-glycoprotein substrates such as macrocyclic lactones (e.g. ivermectin and milbemycin) could decrease the efflux of such drugs from blood– brain barrier cells, potentially resulting in signs of CNS toxicity.