Chemical Property of CID 6992028
Chemical Property:
- Appearance/Colour:White solid
- Melting Point:106-108 °C
- Boiling Point:616.2 °C at 760 mmHg
- PKA:pKa 3.30±0.01(H2O
t = 25.0
I = 0.15 (KCl)) (Uncertain);5.75±0.00(H2O
t = 25.0
I = 0.15 (KCl)) (Uncertain)
- Flash Point:326.4 °C
- PSA：95.94000
- Density:1.2 g/cm3
- LogP:2.71200
- Storage Temp.:2-8°C
- Solubility.:DMSO: ~18mg/mL
- XLogP3:2.1
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:5
- Rotatable Bond Count:9
- Exact Mass:416.23112213
- Heavy Atom Count:30
- Complexity:613
- Purity/Quality:
-
99%, *data from raw suppliers
Ramipril *data from reagent suppliers
Safty Information:
- Pictogram(s):
Xi
- Hazard Codes:Xi
- Statements:
36/38
- Safety Statements:
26-37/39
- MSDS Files:
-
SDS file from LookChem
Useful:
- Canonical SMILES:CCOC(=O)C(CCC1=CC=CC=C1)[NH2+]C(C)C(=O)N2C3CCCC3CC2C(=O)[O-]
- Isomeric SMILES:CCOC(=O)[C@H](CCC1=CC=CC=C1)[NH2+][C@@H](C)C(=O)N2[C@H]3CCC[C@H]3C[C@H]2C(=O)[O-]
-
Description
Ramipril (brand name: Altace) is a kind of prodrug which is capable of inhibiting the angiotensin-converting enzyme (ACE) which converting angiotensin I to angiotensin II. It is metabolized to ramiprilat in the liver which exerts the effect of ACE inhibition. It is used for the treatment of hypertension, congestive heart failure and nephropathy. It can also be used for the prevention of heart attack, stroke and cardiovascular death. It can also be used for the treatment of kidney damage due to diabetes with protein-containing urine. Ramiprilat, is the competitive inhibitor of ATI for binding to ACE, further inhibiting the enzymatic proteolysis of ATI to ATII, alleviating the effect of ATII on blood pressure. Ramipril, a prodrug of ramiprilat, is a long-acting, tissue-specific and non-sulfhydryl ACE
inhibitor useful in the treatment of mild to moderate hypertension. In animal studies
ramipril exerted cardioprotective effects resembling those of bradykinin in cardiac
reperfusion injuries. Ramipril is also reportedly useful in congestive heart failure.
-
Uses
An antihypertensive. An angiotensin converting enzyme (ACE) inhibitor, converted to active, diacid metabolite An inhibitor of the angiotensin- coverting enzyme (ACE) Angiotensin-converting enzyme (ACE) removes the C-terminal dipeptide from angiotensin I to form angiotensin II, a powerful vasoconstrictor. ACE is a key regulator of the renin-angiotensin system and an important drug target for the treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing renal and retinal complications in diabetes. Ramipril is a second generation ACE inhibitor (IC50 = 4 nM) that acts as a prodrug, which is hydrolyzed in vivo to the active metabolite ramiprilat. The antihypertensive and cardioprotective efficacy of ramipril has been demonstrated in large-scale noncomparative studies and clinical trials.[Cayman Chemical]
-
Clinical Use
Angiotensin-converting enzyme inhibitor:
Hypertension
Secondary prevention of myocardial infarction (MI),
stroke or cardiovascular death
Heart failure
Diabetic nephropathy
-
Drug interactions
Potentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect.
Analgesics: antagonism of hypotensive effect and
increased risk of renal impairment with NSAIDs;
hyperkalaemia with ketorolac and other NSAIDs.
Antihypertensives: increased risk of hyperkalaemia,
hypotension and renal failure with ARB’S and aliskiren.
Bee venom extract: possible severe anaphylactoid
reactions when used together.
Ciclosporin: increased risk of hyperkalaemia and
nephrotoxicity.
Cytotoxics: increased risk of angioedema with
everolimus.
Diuretics: enhanced hypotensive effect;
hyperkalaemia with potassium-sparing diuretics.
ESAs: increased risk of hyperkalaemia; antagonism
of hypotensive effect.
Gold: flushing and hypotension with sodium
aurothiomalate.
Lithium: reduced excretion (possibility of enhanced
lithium toxicity).
Potassium salts: increased risk of hyperkalaemia.
Tacrolimus: increased risk of hyperkalaemia and
nephrotoxicity
