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RX BIN: 015558RX PCN: HTGroup ID: DDN6600Card Holder ID: DDN6600
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Enalapril volume of distribution

Distribution of enalapril into human body tissues and fluids has not been fully characterized. Approximately 50-60% of enalaprilat is bound to plasma proteins. Two binding sites have been identified, a low affinity, high capacity site and a high affinity, low capacity site. Drug bound to the latter site may represent enalaprilat bound to circulating serum angiotensin converting enzyme, possibly accounting for the prolonged terminal elimination of the drug. Information on distribution into the CNS is limited, but enalapril appears to cross the blood brain barrier poorly, if at all, and enalaprilat does not appear to distribute into the CNS. The drug did not accumulate in any tissue following multiple dose administration in animals.

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What is Enalapril

Enalapril is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is rapidly metabolized in the liver to enalaprilat following oral administration. Enalaprilat is a potent, competitive inhibitor of ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Enalapril may be used to treat essential or renovascular hypertension and symptomatic congestive heart failure.

Enalapril mechanism of action

There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, which arise from tandem gene duplication. Although the two domains have high sequence similarity, they play distinct physiological roles. The C-domain is predominantly involved in blood pressure regulation while the N-domain plays a role in hematopoietic stem cell differentiation and proliferation. ACE inhibitors bind to and inhibit the activity of both domains, but have much greater affinity for and inhibitory activity against the C-domain. Enalaprilat, the principle active metabolite of enalapril, competes with ATI for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII as described in the Pharmacology section above. Enalapril also causes an increase in plasma renin activity likely due to a loss of feedback inhibition mediated by ATII on the release of renin and/or stimulation of reflex mechanisms via baroreceptors. Enalaprilat’s affinity for ACE is approximately 200,000 times greater than that of ATI and 300-1000 times greater than that enalapril.

Dosage forms of Enalapril

FormRouteStrength
Tabletoral10 mg
Tabletoral2.5 mg
Tabletoral20 mg

Prescription Generics

false

International Brands

Act Enalapril

Synonyms

(S)-1-(N-(1-(Ethoxycarbonyl)-3-phenylpropyl)-L-alanyl)-L-proline (S)-1-{(S)-2-(1-((S)-ethoxycarbonyl)-3-phenyl-propylamino)-propionyl}-pyrrolidine-2-carboxylic acid

Manufacturers

Actavis Pharma Company

CAS number

75847-73-3

UNII

69PN84IO1A

State

solid

Affected organisms

Humans and other mammals

Indication of Enalapril

For the treatment of essential or renovascular hypertension and symptomatic congestive heart failure. It may be used alone or in combination with thiazide diuretics.

Toxicity of Enalapril

Overdosage may result in marked hypotension and stupor. Most common adverse effects include hypotension, headache, dizziness and fatigue.

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