Pimobendan Chewable Tablet For Veterinary Use Only Ingredients: Animal Extract

COMPOSITION:
SAFEHEART 5
Each chewable tablet contains:
Pimobendan EP: 5 mg
Excipients: q.s.
Colours: Iron Oxide Red NF, Iron Oxide Yellow NF
Approved flavours used.
SAFEHEART 1.25
Each chewable tablet contains:
Pimobendan EP: 1.25 mg
Excipients: q.s.
Colours: Iron Oxide Red NF, Iron Oxide Yellow NF
Approved flavours used.
CHEMISTRY: 4,5-dihydro-6-[2-(4-methoxyphenyl)-1Hbenzimidazole- 5-yl]-5-methyl-3(2H)-pyridazinone.

CATEGORY: Inodilator (calcium sensitizer and phosphodiesterase III inhibitor)

PHARMACOLOGY

PHARMACODYNAMICS:

Pimobendan, a benzimidazole-pyridazinone derivative, is a non-sympathomimetic, non-glycoside inotropic drug with vasodilatative properties. Pimobendan exerts a stimulatory myocardial effect by a dual mechanism of action consisting of an increase in calcium sensitivity of cardiac myofilaments and inhibition of phosphodiesterase (Type III). Pimobendan exhibits vasodilating activity by inhibiting phosphodiesterase III activity.

PHARMACOKINETICS:

Pimobendan is oxidatively demethylated to a pharmacologically active metabolite which is then conjugated with sulfate or glucuronic acid and excreted mainly via feces. The mean extent of protein binding of pimobendan and the active metabolite in dog plasma is >90%.

The total body clearance of pimobendan was approximately 90 mL/min/kg, and the terminal elimination half-life of pimobendan and the active metabolite were approximately 0.5 hours and 2 hours, respectively.

Plasma levels of pimobendan and active metabolite were below quantifiable levels by 4 and 8 hours after oral administration, respectively. The steady-state volume of distribution of pimobendan is 2.6 L/kg indicating that the drug is readily distributed into tissues. Food decreased the bioavailability of an aqueous solution of pimobendan, but the effect of food on the absorption of pimobendan from Safeheart tablet is unknown.

INDICATIONS:

Safeheart (pimobendan) is indicated for the management of the signs of mild, moderate or severe (modified NYHA Class IIa, IIIb or IVc) congestive heart failure in dogs due to atrioventricular valvular insufficiency (AVVI) or dilated cardiomyopathy (DCM).

Safeheart is indicated for use with concurrent therapy for congestive heart failure (e.g., furosemide etc.) as appropriate on a case-by-case basis.

A dog with modified New York Heart Association (NYHA) Class II heart failure has fatigue, shortness of breath, coughing, etc. apparent when ordinary exercise is exceeded.
A dog with modified NYHA Class III heart failure is comfortable at rest, but exercise capacity is minimal.
A dog with modified NYHA Class IV heart failure has no capacity for exercise and disabling clinical signs are present even at rest.
DOSAGE AND ADMINISTRATION:

Safeheart should be administered orally at a total daily dose of 0.23 mg/lb (0.5 mg/kg) body weight, using a suitable combination of whole or half tablet.

The total daily dose should be divided into 2 portions that are not necessarily equal, and the portions should be administered approximately 12 hours apart (i.e., morning and evening).

The tablets are scored and the calculated dosage should be provided to the nearest half-tablet increment.

CONTRAINDICATIONS:

Safeheart should not be given in cases of hypertrophic cardiomyopathy, aortic stenosis, or any other clinical condition where an augmentation of cardiac output is inappropriate for functional or anatomical reasons.