Enalapril resources


DRUG INFO
Enalapril

Drug Name: Enalapril

Indication: For the treatment of hypertension and heart failure. It may be used alone or in combination with thiazide diuretics



Pharmacology: Enalapril, an angiotensin-converting enzyme (ACE) inhibitor, is a prodrug which, when hydrolyzed by estarases to its active Enalaprilat, is used to treat hypertension and heart failure, to reduce proteinuria and renal disease in patients with nephropathies, and to prevent stroke, myocardial infarction, and cardiac death in high-risk patients. Enalapril and Enalaprilat inhibit 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.

Mechanism Of Action: Enalaprilat, the active metabolite of Enalapril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Enalaprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.

Drug Category: Antihypertensive Agents; Angiotensin-converting Enzyme Inhibitors; ATC:C09AA02

Brand Names/Synonyms: Bonuten; Enalapril; Enalapril Bp; Enalapril Maleate; Enalapril Richet; Enalaprila [Inn-Spanish]; Enalaprilat; Enalaprilum [Inn-Latin]; Gadopril; Kinfil; Vaseretic; Vasotec

Dosage Forms: Tablets; IV injection

Absorption: 60%

Interactions: DrugBank: Interactions for Enalapril

Interactions for Enalapril:


Hypotension: Patients on Diuretic Therapy: Patients on diuretics and especially those in whom diuretic therapy was recently instituted, may occasionally experience an excessive reduction of blood pressure after initiation of therapy with enalapril or enalaprilat. The possibility of hypotensive effects with enalapril or enalaprilat can be minimized by either discontinuing the diuretic or increasing the salt intake prior to initiation of treatment with enalapril or enalaprilat. If it is necessary to continue the diuretic, provide close medical supervision after the initial dose for at least two hours and until blood pressure has stabilized for at least an additional hour..

Agents Causing Renin Release: The antihypertensive effect of enalapril and enalapril IV is augmented by antihypertensive agents that cause renin release (e.g., diuretics).

Non-steroidal Anti-inflammatory Agents: In some patients with compromised renal function who are being treated with nonsteroidal anti-inflammatory drugs, the co-administration of enalapril may result in a further deterioration of renal function. These effects are usually reversible.

In a clinical pharmacology study, indomethacin or sulindac was administered to hypertensive patients receiving VASOTEC. In this study there was no evidence of a blunting of the antihypertensive action of VASOTEC. However, reports suggest that NSAIDs may diminish the antihypertensive effect of ACE inhibitors. This interaction should be given consideration in patients taking NSAIDs concomitantly with ACE inhibitors.

Other Cardiovascular Agents: Enalapril and enalapril IV have been used concomitantly with beta adrenergic-blocking agents, methyldopa, nitrates, calcium-blocking agents, hydralazine, prazosin and digoxin without evidence of clinically significant adverse interactions.

Enalapril IV has been used concomitantly with digitalis without evidence of clinically significant adverse reactions.

Agents Increasing Serum Potassium: Enalapril and enalapril IV attenuate potassium loss caused by thiazide-type diuretics. Potassium-sparing diuretics (e.g., spironolactone, triamterene, or amiloride), potassium supplements, or potassium-containing salt substitutes may lead to significant increases in serum potassium. Therefore, if concomitant use of these agents is indicated because of demonstrated hypokalemia, they should be used with caution and with frequent monitoring of serum potassium. Potassium sparing agents should generally not be used in patients with heart failure receiving enalapril.

Lithium: Lithium toxicity has been reported in patients receiving lithium concomitantly with drugs which cause elimination of sodium, including ACE inhibitors. A few cases of lithium toxicity have been reported in patients receiving concomitant enalapril/enalapril IV and lithium and were reversible upon discontinuation of both drugs. It is recommended that serum lithium levels be monitored frequently if enalapril is administered concomitantly with lithium.





Chemical IUPAC Name: 1-[2-(1-ethoxycarbonyl-3-phenyl-propyl)aminopropanoyl]pyrrolidine-2-carboxylic acid

Chemical Formula: C20H28N2O5

Half Life: 11 hours

Drug Type: Approved Drug

# Accession No: APRD00510

CAS Registry Number: 75847-73-3



Enalapril News
(When available)


Trainer Holloway Disqualified Over Drugs  16 Jan 2006
Virtual Form Guide, Both Holloway and Hedges denied giving the six-year-old the substance Acepromazine Maleate, commonly known as Ace, and offered that it could have been done by ...

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PharmaLive.com (press release), ROCKVILLE, Md., Jan. 5, 2006--GlaxoSmithKline and FDA notified healthcare professionals about post-marketing reports of new onset ...

NSW stewards inquiry into tranquiliser find  Jan 13, 2006
ThoroughbredNews.co.nz, 1pm on Monday, 16 January 2006, following the Analyst's report of the presence of a metabolite of the veterinary tranquiliser Acepromazine Maleate being found ...

BioDelivery Sciences Retains The Investor Relations Group of New ...  Jan 13, 2006
Genetic Engineering News, As previously announced, BDSI submitted a New Drug Application (NDA) on Emezine(R), a dissolving buccal tablet formulation of prochlorperazine maleate for the ...

NPPA FIXES/REVISES THE PRICES OF BULK DRUGS AND FORMULATIONS  Dec 27, 2005
Press Information Bureau (press release), Bulk Drugs – The prices of bulk drugs Sodium Penicillin G, Procaine Penicillin G, Benzathine Penicillin G, Phenramine Maleate, Trimethoprim, Pentoxyphylline ...

Bulk drug prices revised  Dec 27, 2005
Business Standard, Authority (NPPA) has revised the prices of some bulk drugs and formulations, including Sodium and Procaine Penicillin G, Phenramine Maleate, Trimethoprim and ...

NPPA revamps bulk drugs/formulation prices  Dec 27, 2005
NewKerala.com, Meanwhile, the prices of bulk drugs Pheniramine Maleate, Trimethoprim, Rifampicin were revised upwards to Rs 1107/kg, Rs 840/kg, Rs 3560/kg from the existing ...

In fine health  Jan 8, 2006
Business Standard, ...companies. The company has also recently received tentative US FDA approval for its anti-diabetic drug, Rosiglitazone Maleate tablets. ...

BioDelivery Sciences Files IND for BEMA(TM) LA, a treatment for ...  Jan 9, 2006
dBusinessNews Triangle (press release), Needless to say, with our existing NDA for Emezine(R) (prochlorperazine maleate) under review at FDA; BEMA(TM) Fentanyl entering Phase III and now with our ...

Drug prices may face a small hike  Dec 28, 2005
Andhra Cafe, Also, prices of other bulk drugs such as pheniramine maleate and timethoprim have been raised by 3.65 and 20 per cent respectively. ...

Easing IBS  Jan 4, 2006
WOWT, Researchers are now testing the use of another drug, tegaserod maleate, can help prevent overgrowth of bacteria for longer periods of time.

Irritable Bowel Syndrome (IBS)  Dec 16, 2005
WSOCtv.com, Tegaserod maleate (Zelnorm®) is approved for women with IBS who have constipation as their main symptom. There aren't any conclusive diagnostic tests for IBS. ...

An Association Between Avandia® and Avandamet® and Vision ...  Dec 23, 2005
DG News MISSISAUGA, ONTARIO, CANADA -- December 23, 2005 -- Avandia(R) (rosiglitazone maleate) tablets and Avandamet(R) (rosiglitazone maleate/metformin hydrochloride ...

Pen G derivatives prices reduced by up to 32%  Dec 27, 2005
Financial Express, The authority also announced hike in prices of bulk pheniramine maleate (3.65%), trimethoprim (20%) and rifampicin (2.3%), citing rise in prices of raw ...

Novartis Remains Committed to Making Zelnorm Available for Women ...  Dec 15, 2005
PharmaLive.com (press release), Novartis markets Zelnorm® (tegaserod maleate) in the US, Canada, Philippines and South Africa; and under the trademark Zelmac® (tegaserod) in Switzerland ...

Sensex snaps 5-day rally; rupee climbs  Dec 14, 2005
Gulf Times, The company won approval to sell 2-milligram, 4-milligram and 8-milligram tablets of rosiglitazone maleate in the US, the drug regulator said in an e-mailed ...

Mother explains horrors of local OTC drug abuse  Dec 15, 2005
Atlanticville, C (CCC), a nickname for the cough medicine Coricidin HBP Cold & Cough, the most popular brand of dextromethorphan (DXM) and chlorpheniramine maleate that is ...

Nursing Homes Confront New Drug Plan's Hurdles  16 Jan 2006
Spartanburg Herald Journal (subscription), Coumadin for blood clots. Motrin for arthritis pain. Serzone for depression. Vasotec for high blood pressure. Aricept for Alzheimer's disease. ...

NURSING HOMES CONFRONT NEW DRUG PLAN'S HURDLES  Jan 15, 2006
Amherst Times.com, Coumadin for blood clots. Motrin for arthritis pain. Serzone for depression. Vasotec for high blood pressure. Aricept for Alzheimer's disease. ...

Rx for seniors: Education  Jan 15, 2006
New York Daily News, ...that seniors who suffer from heart disease, stroke, heart arrhythmia, dementia and cancer, and who take such medications as Coumadin, Vasotec, Zestril, Atenolol ...

Heart drug use has increased, but still suboptimal  Jan 9, 2006
Reuters.uk, In 2002, rates of overall and consistent use of angiotensin-converting enzyme (ACE) inhibitors, such as Accupril and Vasotec, in patients with heart failure ...

Heart patients don't stick to drug programs  Jan 10, 2006
News-Medical.net, In 2002, rates of overall and consistent use of ACE inhibitors, such as Accupril and Vasotec, in patients with heart failure were 51 percent and 39 percent ...


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