Oclacitinib Maleate Tablets
Oclacitinib Maleate
3.6mg/5.4mg/16mg
Tablets, Coated
Immunomodulator,For oral use in dogs only
Description:
Oclacitinib Maleate is a synthetic Janus Kinase (JAK)inhibitor, particularly JAK1 and JAK3. By inhibiting these enzymes, it interferes with the signaling pathway of several cytokines involved in inflammation and pruritus (itching) associated with allergic and atopic dermatitis. The chemical composition of Oclacitinib Maleate is N-methyl[trans-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)cyclohexyl]methanesulfonamide (2Z)-2-butenedioate.
The chemical structure of Oclacitinib Maleate is:
Indications:
Control of pruritus associated with allergic dermatitis and control of atopic dermatitis in dogs at least 12 months of age.
Dosage and Administration:
The dose of Oclacitinib Maleate tablets is 0.18 to 0.27 mg oclacitinib/lb (0.4 to 0.6 mg oclacitinib/kg) body weight, administered orally, twice daily for up to 14 days, and then administered once daily for maintenance therapy. Oclacitinib Maleate may be administered with or without food.
Warnings:
Oclacitinib Maleate is not for use in dogs less than 12 months of age.
Oclacitinib Maleate modulates the immune system.
Oclacitinib Maleate is not for use in dogs with serious infections.
Oclacitinib Maleate may increase susceptibility to infection, including demodicosis, and exacerbation of neoplastic conditions
New neoplastic conditions (benign and malignant) were observed in dogs treated with Oclacitinib Maleate during clinical studies and have been reported in the post-approval period.
Consider the risks and benefits of treatment prior to initiating Oclacitinib Maleate in dogs with a history of recurrent serious infections or recurrent demodicosis or neoplasia.
Keep Oclacitinib Maleate in a secure location out of reach of dogs, cats, and other animals to prevent accidental ingestion or overdose.
Human Warnings:
This product is not for human use. Keep this and all drugs out of reach of children. For use in dogs only. Wash hands immediately after handling the tablets. In case of accidental eye contact, flush immediately with water or saline for at least 15 minutes and then seek medical attention. In case of accidental ingestion, seek medical attention immediately.
Precautions
Dogs receiving Oclacitinib Maleate should be monitored for the development of infections, including demodicosis, and neoplasia.
The use of Oclacitinib Maleate has not been evaluated in combination with glucocorticoids, cyclosporine, or other systemic immunosuppresive agents.
Oclacitinib Maleate is not for use in breeding dogs, or pregnant or lactating bitches.
Adverse Reactions
The following adverse events reported in dogs are listed in decreasing order of reporting frequency.
Vomiting, lethargy, anorexia, diarrhea, elevated liver enzymes, dermatitis (i.e. crusts, pododermatitis, pyoderma), seizures, polydipsia, and demodicosis.
Benign, malignant, and unclassified neoplasms, dermal masses (including papilomas and histiocytomas), lymphoma and other cancers have been reported.
Death (including euthanasia) has been reported.
Clinical Pharmacology
Mechanism of action
Oclacitinib inhibits the function of a variety of pruritogenic cytokines and pro-inflammatory cytokines, as well as cytokines involved in allergy that are dependent on JAK1 or JAK3 enzyme activity. It has little effect on cytokines involved in hematopoiesis that are dependent on JAK2. Oclacitinib is not a corticosteroid or an antihistamine.
Pharmacokinetics
In dogs, oclacitinib maleate is rapidly and well absorbed following oral administration, with mean time to peak plasma concentrations (Tmax) of less than 1 hour. Following oral administration of 0.4-0.6 mg oclacitinib/kg to 24 dogs, the mean (90% confidence limits [CL]) maximum concentration (Cmax) was 324 (281, 372) ng/mL and the mean area under the plasma concentration-time curve from 0 and extrapolated to infinity (AUC0-inf) was 1890 (1690, 2110) ng∙hr/mL. The prandial state of dogs does not significantly affect the rate or extent of absorption. The absolute bioavailability of oclacitinib maleate was 89%.
Oclacitinib has low protein binding with 66.3-69.7% bound in fortified canine plasma at nominal concentrations ranging from 10-1000 ng/mL. The apparent mean (95% CL) volume of distribution at steady-state was 942 (870, 1014) mL/kg body weight.
Oclacitinib is metabolized in the dog to multiple metabolites and one major oxidative metabolite was identified in plasma and urine. Overall the major clearance route is metabolism with minor contributions from renal and biliary elimination. Inhibition of canine cytochrome P450 enzymes by oclacitinib is minimal; the inhibitory concentrations (IC50s) are 50 fold greater than the observed Cmax values at the use dose.
Mean (95% CL) total body oclacitinib clearance from plasma was low – 316 (237, 396) mL/h/kg body weight (5.3 mL/min/kg body weight). Following IV and PO administration, the terminal t1/2 appeared similar with mean values of 3.5 (2.2, 4.7) and 4.1 (3.1, 5.2) hours, respectively.
Storage Conditions
Oclacitinib Maleate should be stored at controlled room temperature between 20° to 25°C (68° to 77°F) with excursions between 15° to 40°C (59° to 104°F).
Generic medication and its counterpart to have the same active ingredients, strength, quality, route of administration, and safety standards.All of our products are produced in GMP factories, Your pet’s health is our top priority.
This summary contains important information about Oclacitinib Maleate. You should read this information before you start giving your dog Oclacitinib Maleate and review it each time the prescription is refilled as there may be new information. This sheet is provided only as a summary and does not take the place of instructions from your veterinarian. Talk with your veterinarian if you do not understand any of this information or if you want to know more about Oclacitinib Maleate.
What is Oclacitinib Maleate?
Oclacitinib Maleate is a selective inhibitor of Janus Kinase enzymes, particularly JAK1 and JAK3. By inhibiting these enzymes, it interferes with the signaling pathway of several cytokines involved in inflammation and pruritus (itching) associated with allergic and atopic dermatitis.
Oclacitinib Maleate is an oral medication primarily used to manage itching associated with allergic dermatitis, including atopy, in dogs that are at least 12 months old. It is also found to be effective in treating other skin conditions in dogs and has been occasionally used for certain skin conditions in cats.
What are the indications for Oclacitinib Maleate?
Oclacitinib Maleate is primarily indicated for the treatment of pruritus (itchiness) associated with allergic dermatitis and the management of atopic dermatitis in dogs. The specific indications are as follows:
Allergic Dermatitis: Oclacitinib Maleate is used to manage itching due to allergic dermatitis in dogs. Allergic dermatitis can be triggered by various allergens, such as fleas, food allergies, or environmental allergens (like pollen or dust mites).
Atopic Dermatitis: It is also indicated for the control of atopic dermatitis, a chronic, inflammatory skin disease associated with allergies to environmental substances.
It's important to note the following usage guidelines and precautions: Oclacitinib Maleate is approved for use in dogs that are at least 12 months old.It should not be used in dogs with serious infections or in dogs that are breeding, pregnant, or lactating.
What are the side effects of Oclacitinib Maleate?
The administration of Oclacitinib Maleate in dogs can lead to various side effects, ranging from mild to more serious. It's important to be aware of these potential side effects and to monitor your pet accordingly. Here are some of the common and serious side effects associated with Oclacitinib Maleate:
Common Side Effects:
Vomiting
Diarrhea
Anorexia (loss of appetite)
Decreased energy (lethargy)
Increased thirst
These side effects are often temporary and may resolve on their own.
Serious Side Effects:
Serious infections (including pneumonia, urinary tract infections, and skin infections)
Demodicosis (a skin disease caused by Demodex mites)
Skin masses, including cysts between the toes and skin cancer
Cancer (new tumors or worsening of existing ones)
Aggression
Low white blood cell count
Monitoring and Management: If any serious side effects are observed, such as trouble breathing, decreased energy, skin or hair coat changes, new masses or changes to existing ones, fever, or changes in urination, it's important to contact a veterinarian immediately.
More severe side effects can occur, although they are less common.
Human Exposure: It's also worth noting that this medication is not intended for human use. In case of accidental ingestion or skin irritation after contact, medical attention should be sought.
Overdose Risks: In cases of overdose, side effects like vomiting, diarrhea, skin inflammation, pneumonia, and others may occur. Immediate veterinary attention is crucial in such scenarios.
Interactions with Other Medications: It is essential to inform the veterinarian about all other medications and supplements your dog is taking, as Oclacitinib Maleate may interact with other drugs.
The information provided here is a guideline and it's always crucial to follow the specific advice and directions given by your veterinarian.
What drug interactions should be noted when using Oclacitinib Maleate?
When using Oclacitinib Maleate in dogs, there are several potential drug interactions to be aware of:
Other Immunosuppressive Drugs: Oclacitinib Maleate may interact with other immunosuppressants, such as corticosteroids (e.g., prednisone) and cyclosporine. The combined effect of these drugs could potentially increase the risk of infections and other immune-related issues.
Vaccinations: There is a potential concern about the interaction of Oclacitinib Maleate with vaccinations. As Oclacitinib Maleate can modulate the immune response, it might interfere with the development of immunity following vaccination. Therefore, it's advisable to discuss vaccination schedules and Oclacitinib Maleate treatment with your veterinarian.
CYP450 Interactions: While Oclacitinib Maleate is primarily metabolized in the liver, it does not appear to have significant interactions with drugs that are metabolized by liver enzymes known as cytochrome P450 (CYP450). However, it's always prudent to inform the veterinarian about all medications and supplements the dog is taking, to assess any potential interactions.
Concurrent Infections: In dogs with concurrent infections, especially if they are on antimicrobial therapy, caution is advised when using Oclacitinib Maleate. The immunomodulatory effects of Oclacitinib Maleate could potentially influence the course of the infection or the effectiveness of the antimicrobial treatment.
Other Allergy Medications: Caution should be taken when using Oclacitinib Maleate with other allergy medications, as there may be overlapping effects or increased risk of side effects.
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): While there is no direct interaction reported, combining Oclacitinib Maleate with NSAIDs should be done cautiously, as both can have effects on the immune system and inflammatory pathways.
It's important to have a thorough discussion with a veterinarian before combining Oclacitinib Maleate with any other medication. Each dog's health situation is unique, and the vet can provide the best guidance based on the individual needs and health status of the pet.
What if I miss giving my pet the medication?
If you miss a dose, give it when you remember, but if it is close to the time for the next dose, skip the dose you missed and give it at the next scheduled time and return to the regular dosing schedule. Never give your pet two doses at once or give extra doses.
Are there any risk factors for this medication?
Oclacitinib Maleate should be avoided in patients with current or recent demodectic mange (Demodex). In clinical trials, a small number of patients developed demodectic mange while on this medication due to changes in the skin’s immune function. Oclacitinib Maleate should also be avoided in patients with serious infections, such as pneumonia.
" Oclacitinib Maleate should be avoided in dogs younger than 12 months old."
Oclacitinib Maleate has not been evaluated for use in pregnant, nursing, or breeding dogs, and therefore should be avoided in these patients. Oclacitinib Maleate should be avoided in dogs younger than 12 months old. There is a small risk that Oclacitinib Maleate may exacerbate some neoplastic (cancerous) conditions. For this reason, Oclacitinib Maleate should be avoided in patients with cancer or with a history of cancer.
Is there any monitoring that needs to be done with this medication?
Periodic bloodwork monitoring is recommended for dogs that will receive Oclacitinib Maleate on a long-term basis. Although uncommon, some patients will develop decreased white blood cell counts on this medication, which may make them more prone to infection. Early detection through routine monitoring bloodwork is important to prevent adverse effects. Talk to your veterinarian to determine the recommended bloodwork monitoring schedule for your pet.
Monitoring for efficacy, for signs of infections, or for masses on/under the skin is also recommended.
What should I do in case of an emergency?
If you suspect an overdose or an adverse reaction to the medication, call your veterinary office immediately. If they are not available, follow their directions in contacting an emergency facility.