Enalaprilat

Mecanismo de Ação

Enalapril, after hydrolysis to enalaprilat, inhibits angiotensin-converting enzyme (ACE) in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex. The beneficial effects of enalapril in hypertension and heart failure appear to result primarily from suppression of the renin-angiotensin-aldosterone system. Inhibition of ACE results in decreased plasma angiotensin II, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Although the latter decrease is small, it results in small increases of serum potassium. In hypertensive patients treated with VASOTEC alone for up to 48 weeks, mean increases in serum potassium of approximately 0.2 mEq/L were observed. In patients treated with VASOTEC plus a thiazide diuretic, there was essentially no change in serum potassium (see PRECAUTIONS). Removal of angiotensin II negative feedback on renin secretion leads to increased plasma renin activity. ACE is identical to kininase, an enzyme that degrades bradykinin. Whether increased levels of bradykinin, a potent vasodepressor peptide, play a role in the therapeutic effects of VASOTEC remains to be elucidated. While the mechanism through which VASOTEC lowers blood pressure is believed to be primarily suppression of the renin-angiotensin-aldosterone system, VASOTEC is antihypertensive even in patients with low-renin hypertension. Although VASOTEC was antihypertensive in all races studied, black hypertensive patients (usually a low-renin hypertensive population) had a smaller average response to enalapril monotherapy than non-black patients.

Indicação

Hypertension

VASOTEC is indicated for the treatment of hypertension. VASOTEC is effective alone or in combination with other antihypertensive agents, especially thiazidetype diuretics. The blood pressure lowering effects of VASOTEC and thiazides are approximately additive.

Heart Failure

VASOTEC is indicated for the treatment of symptomatic congestive heart failure, usually in combination with diuretics and digitalis. In these patients VASOTEC improves symptoms, increases survival, and decreases the frequency of hospitalization (see CLINICAL PHARMACOLOGY, Heart Failure, Mortality Trials for details and limitations of survival trials).

Asymptomatic Left Ventricular Dysfunction

In clinically stable asymptomatic patients with left ventricular dysfunction (ejection fraction ≤35 percent), VASOTEC decreases the rate of development of overt heart failure and decreases the incidence of hospitalization for heart failure (see CLINICAL PHARMACOLOGY, Heart Failure, Mortality Trials for details and limitations of survival trials).

In using VASOTEC consideration should be given to the fact that another angiotensin-converting enzyme inhibitor, captopril, has caused agranulocytosis, particularly in patients with renal impairment or collagen vascular disease, and that available data are insufficient to show that VASOTEC does not have a similar risk (see WARNINGS, Neutropenia/Agranulocytosis).

In considering use of VASOTEC, it should be noted that in controlled clinical trials ACE inhibitors have an effect on blood pressure that is less in black patients than in non-blacks. In addition, it should be noted that black patients receiving ACE inhibitors have been reported to have a higher incidence of angioedema compared to non-blacks (see WARNINGS, Head and Neck Angioedema).

Especialização do Dr. Reddy

Com sede em Hyderabad, Índia, o Dr. Reddy's Laboratories é um dos principais fornecedores de Ingredientes Farmacêuticos Ativos (API) do mundo. O negócio de API do Dr. Reddy é um parceiro preferencial para empresas farmacêuticas nos EUA, Europa, Brasil, América Latina, Japão, China, Coréia e mercados emergentes.

Os negócios de API do Dr. Reddy prosperam com os profundos pontos fortes técnicos estabelecidos nos últimos 30 anos no desenvolvimento e fabricação de APIs complexas, como esteróides, peptídeos, moléculas complexas de cadeia longa e APIs altamente potentes (HPAPIs / medicamentos para oncologia). Essa experiência é complementada por nossa capacidade em propriedade intelectual e assuntos regulatórios, o que nos ajuda a cumprir e exceder consistentemente os padrões regulatórios. A API do Dr. Reddy Enalaprilat é o resultado de uma extensa experiência em pesquisa e desenvolvimento, PI e regulamentação.

Um componente essencial para ajudar nossos clientes a serem os primeiros no mercado é uma cadeia de suprimentos responsiva. Conseguimos isso garantindo que todas as nossas instalações estejam operando com eficiência e com os mais recentes padrões de qualidade, segurança e produtividade. Uma forte interconexão entre negócios e fábricas permite uma reação rápida às mudanças dinâmicas do mercado, para que possamos evitar escassez e atender a súbitas oscilações na demanda.