Vetoryl 60 mg (trilostane), 30 tablets

Vetoryl 60 mg (trilostane) Vetoril, 30 tablets

Structure

One capsule contains the active ingredient:

• trilostane 60 mg.

Excipients: titanium dioxide (E171) 1.19 mg, yellow iron oxide (E172) 0.045 mg, black iron oxide (E172) 0.672 mg, corn starch, lactose monohydrate, magnesium stearate, glutin.

Pharmaceutical form

The capsules are hard.

Pharmacological properties

Pharmacotherapeutic group antiadrenal drugs.

АТСvet code: QH02CA01 trilostane.

Pharmacodynamic properties

Trilostane, selectively and reversibly, inhibits the enzyme system 3 beta hydroxysteroid isomerase, thereby blocking the production of cortisol, corticosterone and aldosterone. In the treatment of hyperadrenocorticism, trilostane reduces the production of glucocorticoid and mineralocorticoid steroids in the adrenal cortex. Thus, the circulating concentration of these steroids is reduced. Trilostane also inhibits the action of exogenous ACTH (ACTH) and has no direct effect on either the central nervous system or the cardiovascular system.

Pharmacokinetic properties

Pharmacokinetic studies in dogs have shown high interindividual variability. In a pharmacokinetic study in beagles, the area under the curve ranged from 52 to 281 μg / ml / min in fed dogs and from 16 to 175 μg / ml / min in hungry dogs. Typically, trilostane is rapidly removed from plasma, reaching a maximum concentration of 0.5 to 2.5 hours and returning to nearly baseline levels six to twelve hours after administration. The primary active metabolite of trilostane, ketotrylostane, follows a similar pattern. There is no evidence of accumulation of trilostane or metabolites over time. The study of bioavailability with oral administration of the drug showed that trilostane is absorbed more when taken with food. Studies have shown that trilostane in rats is excreted mainly in excrement, demonstrating the excretion of bile as the main metabolic pathway. In the monkey, trilostane is excreted in equal quantities with excrement and urine. The results showed that trilostane is rapidly and well absorbed from the gastrointestinal tract in both rats and monkeys and accumulates in the rat adrenal glands.

Animal species

Dogs.

Indications for use, target species of animals

For the treatment of pituitary and adrenal hyperadrenocorticism (Cushing’s disease and syndrome) in dogs.

Contraindications

Do not administer to animals suffering from primary liver disease and / or renal failure, as well as hypersensitivity to the active substance or to any of the excipients.

Do not use in dogs weighing less than 3 kg.

Side effect

Corticosteroid withdrawal symptoms or hypocortisolemia should be differentiated from hypoadrenocorticism by measuring serum electrolytes. Signs associated with iatrogenic hypoadrenocorticism may be observed, including weakness, lethargy, anorexia, vomiting, diarrhea, ataxia, increased salivation, bloating, tremors, skin changes, and acute adisonic crisis (collapse). These signs usually disappear after stopping treatment. In the absence of evidence of hypoadrenocortisism, dogs may experience lethargy, vomiting, diarrhea, and anorexia. Exceptionally treated dogs have reported adrenal necrosis, which can lead to hypoadrenocorticism. Subclinical renal dysfunction can be detected during treatment. With treatment, arthritis may also occur due to a decrease in the internal level of corticosteroids.

Special precautions for each type of animal

Unknown.

Precautions for use

Special precautions for use on animals.

Since in most cases, hyperadrenocorticism is diagnosed in dogs between the ages of 10 and 15, other pathological processes are common. It is especially important to control cases of primary liver disease and renal failure, since the drug is contraindicated in these diseases. Diagnostics should be carried out during treatment, monitor liver enzymes, electrolytes, urea and creatinine. The presence of diabetes mellitus and hyperadrenocorticism requires special diagnostics. Adrenal function is reduced if the dog has been previously treated with mitotane. The interval before using trilostane is one month. A thorough diagnosis of adrenal function is recommended as dogs may be more sensitive to the effects of trilostane. The drug should be used with caution in dogs suffering from anemia, as there may be a decrease in the volume of cell mass and hemoglobin. Regular checking is recommended.

Application during pregnancy, lactation and egg production

Do not administer to any pregnant or lactating animal intended for breeding.

Interaction with other means and other forms of interaction

The possibility of interaction with other drugs has not been thoroughly studied. Given that hyperadrenocorticism is commonly seen in older dogs, most will be treated concurrently with therapy. Clinical studies have not shown any interactions with other drugs.

The risk of developing hyperkalemia should be taken into account if trilostane is used together with potassium-sparing diuretics or ACE inhibitors. With concomitant use of drugs, the veterinarian should conduct a risk analysis, since several deaths (including sudden death) have been reported in dogs with concomitant use of trilostane with ACE inhibitors.

Dosage and method of administration

Orally. Once a day with food. The starting dose for treatment is approximately 2 mg / kg body weight, based on the combinations of capsule sizes available. Titrate the dose individually. If dose increases are needed, use combinations of capsule sizes to slowly increase the daily dose. The wide range of capsule sizes allows for optimal dosing for each dog. Use the lowest dose necessary to control clinical signs. Ultimately, if symptoms are not well controlled over the entire 24-hour interval, consideration should be given to increasing the daily dose by 50% and split equally between the morning and evening dose. Do not split or open capsules. A small number of animals may require a dose that is significantly higher than 10 mg per kg of body weight per day.

*Kilograms to a Pounds conversion table

Verification:

It is recommended to take samples for biochemistry (including electrolytes) and a preliminary stimulation test for ACTH before treatment, and then after 10 days, 4 weeks, 12 weeks and every 3 months and after each dose adjustment, monitoring the primary diagnosis. It is recommended that an ACTH test be performed 4-6 hours after dosing to ensure accurate results. The drug should be administered in the morning as this will allow the veterinarian to perform the test 4-6 hours after the dose has been administered. It is recommended that a regular analysis of the clinical progression of the disease be carried out during all of the above time periods. In the absence of stimulation during the stimulating ACTH test, treatment should be discontinued for 7 days and then restarted with a lower dose. Repeat the test after 14 days.

Overdose (symptoms, emergency measures, antidotes)

Overdose can lead to hypoadrenocorticism (lethargy, anorexia, vomiting, diarrhea, cardiovascular signs, collapse). With long-term use of a dose of 36 mg / kg in healthy dogs, not a single death was recorded. However, deaths may occur when the dosage is increased in dogs with hyperadrenocorticism.

There is no specific antidote for trilostane.

Given the clinical signs, it is recommended to cancel the treatment. Instead, supportive care should be given, including corticosteroids, electrolyte imbalance correction, and fluid therapy.

In cases of acute overdose, induction of vomiting followed by the administration of activated charcoal may be helpful. Any iatrogenic adrenocortical insufficiency, as a rule, quickly disappears after discontinuation of treatment. However, a small percentage show a lasting effect.

Treatment with a lower dosage should be reinstated one week after the end of Trilostane.

Withdrawal period (withdrawal)

No data. The drug is used for unproductive animals.

Special precautions for personnel who use a veterinary medicinal product for animals

Trilostane can reduce testosterone synthesis and has anti-progesterone effects.

It is not recommended to take the pills in the hands of pregnant women or women who want to become pregnant.

Wash hands with soap and water after use. The contents of the capsules may irritate the eyes and skin and cause an allergic reaction.

Do not separate or open capsules: in case of accidental breakage of capsules and contact of the granules with eyes or skin, wash immediately with plenty of water. If irritation persists, seek medical attention. People who are hypersensitive to trilostane or any of the excipients should avoid contact with the drug. In case of ingestion of the drug, immediately seek medical attention and show the doctor the leaflet, insert or box of the drug.

The main forms of incompatibility

Unknown.

Shelf life

The shelf life of the veterinary drug is 3 years.

Special precautions for storage

Store at a temperature not exceeding 25 ° C. Keep blister strips in a cardboard box.

The nature and composition of the primary packaging container

Blisters made of polyvinyl chloride – polyvinylidene chloride, coated with aluminum, 10 capsules each. Each box contains 3 blisters.

Special precautions for handling unused product

Dispose of unused product residues and vials in accordance with local regulations.