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Enalapril Maleate 76095-16-4 Treating hypertension
Product Specification
| Description： | Off-white ,crystalline powder |
| Identification： | IR Spectrum accordance with that ofCRS、The retention time of the major peak of theSample solution corresponds to that of theStandard solution, as obtained in the assay |
| Specific rotation： | -41.0°~-43.5° |
| Loss on drying： | Not more than 1.0 % |
| Residue on ignition： | Not more than 0.2% |
| Related substances： | Enalaprilat: not more than 0.3%、Moexipril related compound F:not more than 0.3%、Enalapril cyclohexyl analog: not more than 0.3%、Enalapril related compound D: not more than 0.3%、%Any unspecified impurity: not more than 0.10%、Total impurities: not more than 2.0% |
| Residual solvents： | Ethanol: not more than 5000ppm、Acetone: not more than 5000ppm、Dichloromethane:not more than 600ppm |
| Assay(Calculated on the dried basis): | 98.0%~102.0% |
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PRODUCT DESCRIPTION
Enalapril maleate is the second angiotensin converting enzyme inhibitor to reach the marketplace. Like captopril, the first entry in this area, enalapril is useful in the treatment of hypertension and congestive heart failure. It has a longer effective half-life than captopril, allowing once or twice-daily dosing, and appears to have a somewhat lower incidence of side effects.
Enalapril maleate salt is used as a long-acting ACE inhibitor and antihypertensive, used to study diabetic angiopathy in diabetic rats and inhibition of ACE in hog plasma (I50=1.2nM). ACE inhibitors disturb the enin-angiotensin- aldosterone system. Additional ACE inhibitors include: Enalapril, Enalaprilat dihydrate, Enalaprilat, and Enalapril-d5 Maleate Salt, among others.
Enalapril maleate, 1-[N[(S)-1-carboxy-3-phenylpropyl]-L-alanyl]-L-proline 1 -ethyl estermaleate (Vasotec), is a long-acting ACE inhibitor. It requiresactivation by hydrolysis of its ethyl ester to form thediacid enalaprilat. Enalapril is devoid of the side effects ofrash and loss of taste seen with captopril. These side effectsare similar to those of the mercapto-containing drugpenicillamine. The absence of the thiol group in enalaprilmaleate may free it from these side effects. The half-life is 11 hours.
The principle use of enalapril/enalaprilat in veterinary medicine at present is as a vasodilator in the treatment of heart failure. Recent studies have demonstrated that enalapril, particularly when used in conjunction with furosemide, does improve the quality of life in dogs with heart failure. It is not clear, however, whether it has any significant effect on survival times. It may also be of benefit in treating the effects associated with valvular heart disease (mitral regurgitation) and left to right shunts. It is being explored as adjunctive treatment in chronic renal failure and protein losing nephropathies.
While ACE inhibitors are a mainstay for treating hypertension in humans, they have not been particularly useful in treating hypertension in dogs or cats.