Apoquel 5.4 mg, 100 tabs

Description

White to off-white, oblong-shaped, film-coated tablets debossed with a score line and the letters “AQ” and “M” on both sides. The letter “M” is indicated on tablets with 5.4 mg of the active substance inside.

Tablets when used can be divided into halves.

Storage

1 tablet in the shell contains the active ingredient:

Oclacitinib (as oclacitinib maleate) – 5.4 mg.

Excipients: microcrystalline cellulose, lactose monohydrate, magnesium stearate, sodium starch glycolate.

The tablet shell contains:

Lactose monohydrate, hydroxypropyl methylcellulose (E464), titanium dioxide (E171), Macrogol 400 (E1521)

Pharmacological properties

Oclacitinib is a Janus kinase inhibitor. It inhibits the function of various cytokines dependent on the activity of Janus kinase enzymes. For oclacitinib, the target cytokines are pro-inflammatory cytokines and those that play a role in allergic reactions or pruritus. However, oclacitinib may also affect other cytokines (for example, those involved in the body’s defense response or hematopoiesis) with the potential for unwanted effects.

After oral administration in dogs, oclacitinib maleate is rapidly and well absorbed and reaches peak plasma concentrations in less than an hour. The absolute bioavailability of oclacitinib maleate reaches 89%. Food intake does not affect the rate and extent of absorption of oclacitinib.

No accumulation of the drug in the body was observed in dogs treated with oclacitinib for 6 months.

Kind of animals

Dogs

Indications for use

Treatment of pruritus associated with allergic dermatitis in dogs.

Treatment of clinical manifestations of atopic dermatitis in dogs.

Method of administration and dosage

For oral use.

The recommended starting dose is 0.4-0.6 mg oclacitinib per 1 kg of body weight, administered orally twice a day for 14 days.

For maintenance therapy, the same dose (0.4 – 0.6 mg oclacitinib per 1 kg of body weight) is given only once a day. The need for long-term maintenance therapy should be based on an individual assessment of benefit and risk.

Apokvel tablets can be given with or without food.

The dosage chart is below. The tablets are fragile along the dividing line in the middle of the tablet.

Use during pregnancy, lactation and influence on fertility

The use of APOKVEL in animals during pregnancy, lactation and in males used for breeding is not recommended due to the lack of such studies.

Overdose

For signs of overdose, oclacitinib was administered to healthy 1-year-old beagle dogs twice daily for 6 weeks at a dose of 0.6 mg per kg body weight, and then once daily for 20 weeks at a dose of 0.3 mg per 1 kg of body weight.

Clinical changes possibly related to oclacitinib included local alopecia, papillomas, dermatitis, erythema, calluses, interdigital cysts, and paw edema.

Dermatitis in most cases was secondary to interdigital furunculosis on one or more paws, and its frequency increased with increasing dose. Enlargement of peripheral lymph nodes was noted in all experimental groups, the number of such phenomena became more frequent with increasing dose, and was often observed together with interdigital furunculosis.

It does not have a specific antidote to the active substance, therefore, in case of an overdose of the drug, the dog should be treated symptomatically.

Contraindication

Do not use with increased sensitivity to the active substance or any filler in the product.

Do not use in dogs under 12 months of age or weighing less than 3 kg.

Do not use in dogs with signs of immunosuppression, such as hyperadrenocorticism, or with signs of progressive malignant neoplasia, because the effect of the active substance has not been studied in such cases.

Side effect

The table shows the side effects that were detected during field studies on the 16th day of using APOQUEL and placebo:

After 16 days, in more than 1% of dogs, such side effects as pyoderma, nonspecific dermal swellings, otitis, histiocytoma, cystitis, candidiasis, pododermatitis, lipomas, enlarged lymph nodes, nausea, increased appetite and aggressiveness were also noted.

During treatment with the drug APOKVEL, changes in such blood parameters as an increase in the average cholesterol in the blood serum and a decrease in the average number of leukocytes were noted, but all other values ​​remained within the normal range. The decrease in the average number of leukocytes was not progressive and affected the number of all white blood cells (neutrophils, eosinophils and monocytes) except for the number of lymphocytes. But all these changes have no significant clinical significance.

During laboratory studies, the development of papillomas was recorded in some dogs.

Special precautions for use

Oclacitinib modulates the immune system and can increase susceptibility to infection and accelerate the development of the tumor process. Therefore, dogs receiving APOKVEL should be monitored for the possibility of developing infections or tumors. Before starting the treatment of allergic dermatitis with APOQUEL, investigate and treat other possible causes of the disease (eg, flea dermatitis, contact dermatitis, or food hypersensitivity, etc.). In addition, in the treatment of allergic dermatitis and atopic dermatitis, it is recommended to investigate and treat complicating factors such as bacterial, fungal or parasitic infections/infestations (eg, fleas or scabies).

When a dog takes APOKVEL for a long time, it is necessary to monitor the body’s condition by controlling the norms of blood parameters (general and biochemical blood analysis).

Special precautions for persons and service personnel

It is necessary to wash hands after administration of the drug.

In case of swallowing an APOKVEL tablet, you should immediately contact a medical doctor and show the leaflet.

Withdrawal period (grace period)

Not relevant.

Release form

Tablets are packed in aluminum/PVC/Aclar blisters of 10 tablets covered with a shell in cardboard boxes of 20, 50 or 100 tablets or in a white plastic bottle with child protection on the lid of 20, 50 or 100 tablets.

Storage

In blisters – 2 years.

In plastic bottles – 18 months.

The unused half of the tablet should be immediately returned to the bottle or blister and used within 3 days.

A dry, dark, inaccessible place for children at temperatures from 15 ^o to 25 ^o C.

For use in veterinary medicine!