Sava Healthcare Safeheart 1.25 Pimobendan Easy Chews 1.25 mg (30 tabs)

COMPOSITION:

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.

WARNINGS:

Only for use in dogs with clinical evidence of heart failure.

At 3 and 5 times the recommended dosage, administered over a 6-month period of time, pimobendan caused an exaggerated hemodynamic response in the normal dog heart, which was associated with cardiac pathology.

HUMAN WARNINGS:

Not for use in humans. Keep this medication out of reach of children. Consult a physician in case of accidental ingestion by humans.

PRECAUTIONS:

The safety of Safeheart has not been established in dogs with asymptomatic heart disease or in heart failure caused by etiologies other than AVVI or DCM. The safe use of Safeheart has not been evaluated in dogs younger than 6 months of age, dogs with congenital heart defects, dogs with diabetes mellitus or other serious metabolic diseases, dogs used for breeding, or pregnant or lactating bitches.

INTERACTIONS:

Safeheart may be used safely in dogs concurrently receiving furosemide, digoxin, enalapril, atenolol, spironolactone, nitroglycerin, hydralazine, diltiazem, antiparasitic products (including heartworm prevention), antibiotics (metronidazole, cephalexin, amoxicillin-clavulanate, fluoroquinolones), topical ophthalmic and otic products, famotidine, theophylline, levothyroxine sodium, diphenhydramine, hydrocodone, metoclopramide,  butorphanol, and in dogs on sodium-restricted diets.

ADVERSE DRUG REACTIONS:

Common side effects reported are poor appetite, lethargy, diarrhea, dyspnea, azotemia, weakness and ataxia, pleural effusion, syncope, cough, sudden death, ascites, and heart murmur.

PRESENTATION: Bottle of 30 tablets

STORAGE: Store at 20°C to 25°C, excursions permitted between 15°C and 30°C.

CAUTION: Cardiac drug for oral use in dogs only.

Keep out of reach of children.