Vetoryl 30 mg, 30 tablets

Storage

One capsule contains the active substance:

• trilostane 30 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, gluten.

Pharmaceutical form

Hard capsules.

Pharmacological properties

Pharmacotherapeutic group: antiadrenal drugs.

АТСvet code: QH02CA01 trilostan.

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 adrenocorticotropic hormone (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 inter-individual 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 returns almost to baseline six to twelve hours after administration. The primary active metabolite of trilostan, ketotrilostan occurs according to a similar scheme. There is no evidence of accumulation of trilostane or metabolites over time. Oral bioavailability studies have shown that trilostane is more absorbed when administered with food. Studies have shown that trilostane in rats is excreted mainly in the feces, showing bile excretion, as the main metabolic pathway. In monkeys, trilostane is excreted in equal amounts in feces 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

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

Contraindication

Do not use in animals suffering from primary liver disease and / or renal insufficiency, as well as in case of 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 syndrome or hypocortisolemia should be differentiated from hypoadrenocorticism by measuring serum electrolytes. Symptoms associated with iatrogenic hypoadrenocorticism may include weakness, lethargy, anorexia, vomiting, diarrhea, ataxia, increased salivation, bloating, muscle tremor, skin changes, and acute addisonic crisis (collapse). These symptoms usually disappear after stopping treatment. If there is no evidence of hypoadrenocorticism in dogs, lethargy, vomiting, diarrhea, and anorexia may occur. In exceptional cases of treatment of dogs, adrenal necrosis has been reported, which may lead to hypoadrenocorticism. Subclinical renal dysfunction may be detected during treatment with the drug. In the treatment, too,

Features of the warning for each species of animals

Unknown.

Features of the warning when using

Features of caution when used on animals.

Because, in most cases, hyperadrenocorticism is diagnosed in dogs aged 10 to 15 years, other pathological processes are common. It is especially important to control cases of primary liver disease and renal failure, as the drug is contraindicated in these diseases. Diagnosis should be made during treatment, liver enzymes, electrolytes, urea and creatinine should be monitored. The presence of diabetes and hyperadrenocorticism requires special diagnosis. Adrenal function decreases if the dog has previously received mitotane treatment. The interval before the use of trilostan is a month. Careful diagnosis of adrenal function is recommended, as dogs may be more sensitive to trilostan. The drug should be used with extreme caution in dogs suffering from anemia, as there may be a further decrease in cell mass and hemoglobin. Regular inspection is recommended.

Use during pregnancy, lactation and laying

Do not use on any pregnant or lactating animals intended for breeding.

Interaction with other means and other forms of interaction

The possibility of drug interaction with other drugs has not been thoroughly studied. Given the fact that hyperadrenocorticism is usually seen in older dogs, most of them will be treated concomitantly. Clinical studies have not shown any interaction with other drugs.

The risk of developing hyperkalaemia should be considered. if trilostane is used in combination with potassium-sparing diuretics or ACE inhibitors. With concomitant use of such drugs, the veterinarian should perform a risk analysis, as several deaths (including sudden death) have been reported in dogs when trilostan is co-administered with ACE inhibitors.

Dosage and method of application

Orally. Once a day with food. The initial dose for treatment is approximately 2 mg / kg body weight, based on the available combinations of capsule sizes. Titrate the dose individually. If you need to increase the dose, use combinations of capsule sizes to slowly increase the daily dose. A wide range of capsule sizes allows for optimal dosing individually for each dog. Use the lowest dose needed to control clinical signs. Ultimately, if symptoms are insufficiently controlled throughout the 24-hour interval, consideration should be given to increasing the total daily dose by 50% and dividing equally between the morning and evening dose. Do not separate or open the capsules. A small number of animals may require a dose well in excess of 10 mg per 1 kg of body weight per day.

Audit:

It is recommended that biochemical (including electrolyte) samples and a pre-stimulation test for adrenocorticotropic hormone be taken before treatment, followed by 10 days, 4 weeks, 12 weeks, and every 3 months and after each dose adjustment, following the initial diagnosis. It is recommended to test for adrenocorticotropic hormone 4-6 hours after dosing to ensure the accuracy of the results. The drug should be used in the morning, as this will allow the veterinarian to perform the test 4-6 hours after the dose. It is recommended to conduct regular analysis of clinical progression of the disease during all the above time periods. In the absence of stimulation with an adrenocorticotropic hormone test, treatment should be discontinued for 7 days and then restarted at a lower dose.

Overdose (symptoms, emergency procedures, antidotes)

Overdose can lead to hypoadrenocorticism (lethargy, anorexia, vomiting, diarrhea, cardiovascular symptoms, collapse). No long-term deaths have been reported with long-term use of 36 mg / kg in healthy dogs. However, with increasing dosage in dogs with hyperadrenocorticism, deaths may occur.

There is no special antidote for trilostane.

Due to clinical signs, it is recommended to cancel treatment. Instead, maintenance therapy should be prescribed, including corticosteroids, electrolyte imbalance correction, and infusion therapy.

In cases of acute overdose, induction of vomiting with subsequent administration of activated charcoal may be useful. Any iatrogenic adrenocortical insufficiency usually disappears quickly after cessation of treatment. However, a small percentage shows a lasting effect.

Treatment with a lower dose should be resumed one week after the end of trilostan.

Withdrawal period

No data. The drug is used for unproductive animals.

Features of the warning of the personnel applying a veterinary drug to animals

Trilostane can reduce testosterone synthesis and has antiprogesterone action.

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

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

Do not separate or open the capsules: in case of accidental breakage of the capsules and contact of the granules with the eyes or skin, rinse 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. If the drug gets inside, seek medical attention immediately and show the doctor a card-insert or box of the drug.

The main forms of incompatibility

Unknown.

Expiration date

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.

Nature and composition of the primary packaging container

Polyvinyl chloride blisters – aluminum-coated polyvinylidene chloride, 10 capsules. Each box contains 3 blisters.

Special precautions for handling unused product

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