1.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.
2.How does Oclacitinib Maleate work?
Oclacitinib works by selectively inhibiting Janus kinase (JAK) enzymes, primarily JAK1 and to a lesser extent JAK3. This inhibition affects the signaling pathway of various cytokines involved in inflammation and itching (pruritus), which are common symptoms of allergic skin conditions in dogs. The cytokines affected by Oclacitinib Maleate 's action include interleukins (IL) such as IL-2, IL-4, IL-6, IL-13, and IL-31. IL-31, in particular, has been identified as playing a significant role in causing itchiness in dogs with allergic skin diseases.
By inhibiting these cytokines, Oclacitinib Maleate effectively reduces both inflammation and the sensation of itching. Oclacitinib Maleate is known for its rapid onset of action. It starts working within 4 hours of administration and significantly reduces itching in dogs within 24 hours.
3.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.
4.What is the dosage and Administration for Oclacitinib Maleate?
The dosage and administration of Oclacitinib Maleate for dogs are as follows:
Initial Dosage: The recommended starting dose is 0.4 to 0.6 mg/kg body weight. This dosage is administered twice daily for up to 14 days.
Maintenance Dosage: After the initial 14-day period, the dosage is typically reduced to once daily for maintenance.
Administration Method: Oclacitinib Maleate tablets are given orally and can be administered with or without food. If a dog vomits after taking the medication, it might be advisable to try giving it with food, but this should be discussed with a veterinarian.
Age and Health Considerations: Oclacitinib Maleate is approved for use in dogs that are 12 months of age and older. It should not be used in dogs with serious infections, nor in breeding, pregnant, or lactating dogs.
Adjustments for Individual Responses: Some dogs may exhibit increased itching when the dosage is reduced to once daily. In such cases, splitting the total daily dose in half and administering it twice daily may be effective, particularly since Oclacitinib Maleate has a short half-life of around 4 hours.
Missed Doses: If a dose is missed, it can be administered as soon as remembered, but a double dose should not be given. If the time for the next dose is near, skip the missed dose and resume the regular dosing schedule.
Remember, this information is a guideline, and the actual dosage and administration should always be determined by a veterinarian based on the individual dog's condition and response to treatment.
5.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.
6.What circumstances should Oclacitinib Maleate not be used?
Oclacitinib Maleate should not be used in certain circumstances due to potential risks or adverse effects. Here are the key situations where its use is contraindicated or advised against:
Age Restrictions: Oclacitinib Maleate is not recommended for use in dogs less than 12 months of age. Younger dogs may have an increased risk of developing severe infections and other complications.
Breeding, Pregnant, or Lactating Dogs: It should not be used in dogs that are breeding, pregnant, or lactating, as the effects on fetal development and nursing puppies have not been thoroughly studied.
Dogs with Serious Infections: Dogs with serious infections, especially those that are systemic or chronic, should not be given Oclacitinib Maleate, as it might exacerbate these conditions.
Dogs with Pre-existing Cancers: Caution is advised in using Oclacitinib Maleate in dogs with a history of cancer. There is a potential risk that it might aggravate the condition due to its immunosuppressive effects.
Concurrent Use with Other Immunosuppressive Drugs: Using Oclacitinib Maleate in combination with other immunosuppressive drugs, such as corticosteroids or cyclosporine, should be done with caution. The combined effects on the immune system could increase the risk of infections and other complications.
Known Hypersensitivity: If a dog has shown a hypersensitivity reaction to Oclacitinib Maleate or any of its components in the past, it should not be used.
It's essential to consult with a veterinarian for a thorough evaluation of the dog's health status and medical history before starting treatment with Oclacitinib Maleate. The veterinarian can provide specific advice and recommendations based on the individual dog's condition.
7.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.
8.Pharmacokinetics of Oclacitinib Maleate.
The pharmacokinetics of Oclacitinib Maleate in dogs involve how the drug is absorbed, distributed, metabolized, and excreted in the body. Here's a summary of its pharmacokinetic properties:
Absorption: Oclacitinib Maleate is rapidly absorbed when taken orally. It reaches peak plasma concentration in less than an hour, indicating quick entry into the bloodstream.
Bioavailability: The drug has a high bioavailability, which means a significant portion of the administered dose is available to exert its therapeutic effect.
Metabolism: Oclacitinib Maleate is primarily metabolized in the liver. This metabolism is an essential aspect of its pharmacokinetic profile as it influences how long the drug stays active in the body.
Half-Life: The drug has a relatively short half-life, around 4 hours. This short half-life contributes to the need for twice-daily dosing during the initial treatment phase.
Elimination: The drug is cleared from the body through both renal (kidneys) and biliary (bile) pathways. The elimination process is crucial for determining the duration of the drug's action and for guiding dosing in dogs with kidney or liver impairment.
Steady State: Steady-state concentrations of Oclacitinib Maleate are typically achieved within a few days of starting the treatment, which is significant for understanding its effectiveness and safety profile over time.
Effectiveness: The rapid absorption and onset of action are key to its effectiveness in quickly reducing itchiness and inflammation associated with allergic dermatitis in dogs.
It's important to note that these pharmacokinetic properties can vary among individual dogs based on factors like age, breed, liver and kidney function, and concurrent medical conditions or medications.