Cardiostimul (pimobendan) 2.5 mg Tablets for Dogs, 50 tab

Storage

1 tablet (0.5 g) contains:

pimobendan — 2.5 mg

Description

Tablets of white or light gray color, biconvex oblong shape with a notch on one side and the manufacturer’s logo on the other.

Pharmacological properties

Pimobendan is a derivative of benzimidazole-pyridazinone, a non-sympathomimetic, non-glycoside inotropic substance with pronounced vasodilator (vasodilator) properties.

In contrast to cardiac glycosides, the positive inotropic effect of pimobendan is due to an increase in the calcium sensitivity of cardiac muscle myofilaments and inhibition of phosphodiesterase III (PDE III) activity. The vasodilator effect is also provided by inhibiting the activity of phosphodiesterase III. Due to its positive inotropic and vasodilatory effects, the drug in heart failure increases the strength of heart contractions and reduces both preload and afterload.

Oral bioavailability is 60-63% and significantly decreases when used with food.

The volume of distribution is 2.6 l/kg. This means that pimobendan is distributed evenly in tissues. Average binding to blood plasma proteins is 93%.

It is demethylated by oxidation to the main active metabolite (UD-CG 212) with subsequent metabolic transformation into phase II conjugates of UD-CG212 (glucuronides and sulfates).

The half-life from the blood plasma is 0.4±0.1 hours, which corresponds to a high clearance of 90±19 ml/min/kg and a short average retention time of 0.5±0.1 hours. The half-life of the most active metabolite is 2.0±0.3 hours. Pimobendan is almost completely excreted from the body with bile.

Indication

Treatment of dogs for diseases:

• heart failure caused by dilated cardiomyopathy or bicuspid or tricuspid valve insufficiency, which is accompanied by characteristic symptoms (cough, shortness of breath, fainting, decreased activity, exercise intolerance, or ascites);
• dilated cardiomyopathy in the preclinical stage (asymptomatic course with an increase in end-systolic and end-diastolic diameter of the left ventricle) in Doberman pinschers after echocardiographic diagnosis of heart disease;
• myxomatous mitral heart failure in the preclinical stage (asymptomatic course with systolic mitral murmur and signs of heart enlargement) in order to postpone the appearance of clinical symptoms of heart failure.

Contraindication

Do not prescribe to animals with increased sensitivity to the active substance of the drug, with hypertrophic cardiomyopathy or clinical conditions when it is not possible to increase cardiac blood output due to functional or anatomical features (for example, stenosis of the aorta), with severe liver function disorders.

Method of application and dosage

The drug is used orally one hour before feeding the animal.

The dose is prescribed by a veterinarian individually, depending on the severity of the disease and the condition of the animal. The daily dose of pimobendan is 0.2-0.6 mg per 1 kg of body weight, divided into two doses and given in the morning and evening. The recommended daily dose is 0.5 mg per 1 kg of body weight.

Dosages of the drug depend on the dog’s body weight and are listed in the table.

For a more accurate dosage, the tablet can be divided into two or four parts.

In case of congestive heart failure, the veterinary medicine doctor selects an individual dose of the drug for use throughout life.

The drug can be used together with diuretics, such as furosemide.

*Kilograms to Pounds conversion table

Reservation

When used in recommended doses, side effects usually do not occur.

Occasionally there is a slight positive chronotropic effect (increased heart rate) and vomiting. However, it can be avoided by reducing the dose of the drug. Sometimes there is transient diarrhea, lack of appetite or lethargy. In some cases, during long-term treatment with pimobendan in dogs with mitral heart disease, an increase in mitral valve regurgitation is found.

Although the connection with the effect of pimobendan has not been clearly established, very rarely during treatment, signs of an effect on primary hemostasis (petechiae on the mucous membranes, subcutaneous bleeding) can be observed. They disappear after stopping treatment.

Blood glucose levels should be checked regularly when treating diabetic dogs.

Cardiac monitoring is recommended for animals receiving pimobendan.

Laboratory studies on rats and rabbits did not reveal teratogenic and fetotoxic effects of pimobendan. However, it is toxic to pregnant females and embryotoxic when used in high doses, and is also excreted in milk. The safety of the drug for pregnant and lactating bitches has not been evaluated. The drug can be used during pregnancy and lactation only after a benefit/risk assessment by a veterinarian.

During pharmacological studies, no interaction was observed between the cardiac glycoside ouabain (strophanthin) and pimobendan. Pimobendan-induced increases in cardiac contractility are attenuated by the calcium antagonists verapamil and diltiazem, as well as by the β-antagonist propranolol.

Overdose may cause a positive chronotropic effect, vomiting, apathy, ataxia, heart murmurs, or hypotension. In this situation, the dose of the drug should be reduced and appropriate symptomatic treatment should be initiated.

With long-term treatment (6 months) of healthy beagle dogs in doses exceeding the recommended 3 and 5 times, thickening of the mitral valve and hypertrophy of the left ventricle were observed in some dogs. These changes have a pharmacodynamic origin.

Personnel who work with the drug must follow the basic rules of hygiene and safety adopted when working with veterinary drugs.

Storage conditions

In a dry, dark place inaccessible to children at temperatures from +4 °C to +25 °C.

Expiration date

2 years.