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Enalapril maleate

Enalapril maleate structure

CAS No:
76095-16-4
Formula:
C24H32N2O9
Chemical Name:
Enalapril maleate
Synonyms:
1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-prolin(s)-l-prolin(z)-2-bu;1-[n-[1-(ethoxycarbonyl)-3-phenylpropyl]-l-alanyl]-l-prolin(s)-l-prolin(z)-2-but;mk421maleate;n-((s)-1-ethoxycarbonyl-3-phenylpropyl)-l-alanyl-l-proline maleate;ENALAPRIL MALLATE;(S)-1-((S)-2-((S)-1-ETHOXY-1-OXO-4-PHENYLBUTAN-2-YLAMINO)PROPANOYL)PYRROLIDINE-2-CARBOXYLIC ACID MALEATE;Enalapril Maleate　USP24,25,EP2000;Enalapril maleate BP2000/USP25
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Enalapril Maleate, the active metabolite of enalapril, is an angiotensin-converting enzyme (ACE) inhibitor.Target: ACEEnalapril 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 an

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.

White to Off-White Crystalline Powder

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 is11 hours.

Enalapril maleate Basic Attributes

Molecular Weight：

492.52

Exact Mass：

492.210785

EC Number：

278-375-7

Color/Form：

white to off-white

HScode：

29339900

Characteristics

λmax：

208nm(MeOH)(lit.)

PSA：

171

XLogP3：

log Kow = 0.07 at pH 4.9

Appearance：

white to off-white powder

Melting Point：

143-144,5°C

Boiling Point：

0°C

Flash Point：

0°C

Water Solubility：

Soluble in water, methanol, and ethanol.

Storage Conditions：

-20°C Freezer

Vapor Pressure：

1.06X10-12 mm Hg at 25 °C (est)

Toxicity：

LD50 oral in rat: 2973mg/kg

Specific rotation：

D25 -42.2° (c = 1 in methanol)

PKA：

pKa1 3.0; pKa2 (25°) 5.4

Critical Temperature & Pressure：

2-8°C

Safety Information

Transport codes：

3077

wgk germany：

hazard class code：

Xi,Xn

safety instructions：

22-24/25-36/37-26

RTECS Number：

TW3666000

Marks：

Xi,Xn

Stability/Shelf Life：

Stable under recommended storage conditions. /Enalapril maleate/

Precautionary statement(s)：

P281

Hazard Statements：

36/37/38-62-63

RIDADR：

3077

Enalapril maleate Use and Manufacturing

An antihypertensive.An angiotensin-converting enzyme (ACE) inhibitor.

sunscreen

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.

Drug Function and Efficacy

It is hydrolyzed in the liver to enalaprilat, which is a renin angiotensin converting enzyme inhibitor (ACEI), which can reduce the formation of AgII in tissues and plasma, reduce aldosterone secretion, increase plasma potassium concentration, weaken the negative feedback effect of AgII on renin secretion, increase plasma renin activity, and increase the activity of circulating and local kallikrein-kinin systems (also increase the activity of prostaglandin systems). For hypertensive patients, it can reduce supine and standing blood pressure without causing compensatory heart rate acceleration, and significantly reduce peripheral vascular resistance. Usually there is no significant effect on renal blood flow or glomerular filtration rate. The antihypertensive effect appears about 1 hour after taking the medicine, and the peak occurs 4-6 hours after taking the medicine. The maximum antihypertensive effect generally occurs 3-4 weeks after taking the medicine at the prescribed dose. Long-term medication at the recommended dose will continue to have a continuous antihypertensive effect, and short-term discontinuation of the drug will not cause a rebound in blood pressure.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Enalapril Maleate Tablets
Ingredients	Enalapril maleate.
Indication	Other drugs may affect the efficacy and side effects of enalapril maleate. These drugs include other antihypertensive drugs, antipyretic analgesics, diuretics, anesthetics (tell the anesthesiologist if you are using enalapril), antidepressants, anticancer drugs, immunosuppressants, adrenocortical steroids, drugs for gout, drugs for diabetes, adrenergic receptor agonists and thrombolytics. Drinking alcohol while taking medication will increase the effect of alcohol. High-salt foods will reduce the efficacy of enalapril maleate and should be avoided. Please inform your doctor if you are taking other drugs at the same time.
Specifications	5mg/tablet

Enalapril Maleate Tablets
Ingredients	Enalapril maleate.
Indication	Other drugs may affect the efficacy and side effects of enalapril maleate. These drugs include other antihypertensive drugs, antipyretic analgesics, diuretics, anesthetics (tell the anesthesiologist if you are using enalapril), antidepressants, anticancer drugs, immunosuppressants, adrenocortical steroids, drugs for gout, drugs for diabetes, adrenergic receptor agonists and thrombolytics. Drinking alcohol while taking medication will increase the effect of alcohol. High-salt foods will reduce the efficacy of enalapril maleate and should be avoided. Please inform your doctor if you are taking other drugs at the same time.
Specifications	10mg
Manufacturer	Shanghai Shourusong Pharmaceutical Industry Miyang Pharmaceutical Co., Ltd.

Enalapril Maleate Tablets
Ingredients	The main ingredient of this product is enalapril maleate.
Indication	1. Antihypertensive treatment: This product may have an additive effect when used simultaneously with other antihypertensive treatments. 2. Serum potassium 2.1 In clinical trials, serum potassium was generally maintained within the normal range. After 48 weeks of treatment of hypertensive patients with enalapril maleate alone, an average increase in serum potassium of about 0.2 mg equivalent/ml was observed. In patients treated with enalapril maleate plus a thiazide diuretic, the potassium excretion effect of the diuretic is often weakened by the effect of enalapril. 2.2 The use of enalapril maleate and potassium excretion diuretics together can reduce diuretic-induced hypokalemia. 2.3 Risk factors for the development of hyperkalemia include renal insufficiency, diabetes, and the simultaneous use of potassium-storing diuretics (such as spironolactone, triamterene or amiloride), potassium supplements or potassium-containing salt substitutes. 2.4 The use of potassium supplements, potassium-storing diuretics or potassium-containing salt substitutes (especially in patients with renal insufficiency) can cause a significant increase in serum potassium. 2.5 If it is considered appropriate to use the above drugs at the same time, use them with caution and monitor serum potassium frequently. 3. Serum lithium. Like other sodium excretion drugs, lithium clearance may be reduced. Therefore, if lithium salts are taken, serum lithium concentrations should be carefully monitored. 4. Non-steroidal anti-inflammatory drugs. For some patients with renal insufficiency, the combination of angiotensin-converting enzyme inhibitors and non-steroidal anti-inflammatory drugs may lead to further decline in renal function. This effect is usually reversible.
Specifications	10mg
Manufacturer	Huarun Shuanghe Limin Pharmaceutical (Ji'nan) Co., Ltd.

See More Related Drugs

Registered Holders

DR. REDDYS LABORATORIES LTD.

Philippines
Active
MEDICHEM SA

Spain
Active
NEULAND LABORATORIES LTD.

India
Active

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