Ramipril

Bezeichnung:Ramipril

CAS-Nr87333-19-5

Englisch Name:Ramipril

CBNumberCB0249104

SummenformelC23H32N2O5

Molgewicht416.51

MOL-Datei87333-19-5.mol

Ramipril physikalisch-chemischer Eigenschaften

Schmelzpunkt	106-108°C
Siedepunkt	616.2±55.0 °C(Predicted)
alpha	D24 +33.2° (c = 1 in 0.1N ethanolic HCl)
Dichte	1.200±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: ~18mg/mL
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)
Aggregatzustand	powder
Farbe	white
BCS Class	1
CAS Datenbank	87333-19-5(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/38
S-Sätze:	26-37/39
WGK Germany	2
RTECS-Nr.	GY5879600
HS Code	2933995300
Giftige Stoffe Daten	87333-19-5(Hazardous Substances Data)
Toxizität	LD50 (14 day) in male, female mice, male, female rats (mg/kg): 1194, 1158, 687, 608 i.v.; 10933, 10048, >10000, >10000 orally (Donaubauer, Mayer)

Gefahreninformationscode (GHS)

Ramipril Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/38:Reizt die Augen und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
Beschreibung
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.
Chemische Eigenschaften
White Solid
Originator
Hoechst AG (W. Germany)
Verwenden
An inhibitor of the angiotensin- coverting enzyme (ACE)
Verwenden
cardiotonic
Verwenden
An antihypertensive. An angiotensin converting enzyme (ACE) inhibitor, converted to active, diacid metabolite
Verwenden
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]
Definition
ChEBI: A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.
Trademarks
Altace (King);Triatec.
Allgemeine Beschreibung
Ramipril, (2S, 3aS, 6aS)-1-[(S)-N-[(S)-1-carboxy-3-phenylpropyl]alanyl]octahydrocyclopenta[b]-pyrrole-2-carboxylic acid 1-ethyl ester (Altace), ishydrolyzed to ramiprilat, its active diacid form, faster thanenalapril is hydrolyzed to its active diacid form. Peak serumconcentrations from a single oral dose are achieved between1.5 and 3 hours. The ramiprilate formed completely suppresses ACE activity for up to 12 hours, with 80% inhibitionof the enzyme still observed after 24 hours.
Biochem/physiol Actions
Angiotensin converting enzyme (ACE) inhibitor.
Clinical Use
Angiotensin-converting enzyme inhibitor:
Hypertension
Secondary prevention of myocardial infarction (MI), stroke or cardiovascular death
Heart failure
Diabetic nephropathy
Veterinary Drugs and Treatments
Ramipril is a long-acting angiotensin converting enzyme (ACE) inhibitor that may be useful in treating heart failure or hypertension in dogs or cats. It is an approved product in the UK for treating heart failure in dogs. In cats, ramipril has been used for treating arterial hypertension. A recent study (MacDonald, Kittleson et al. 2006) did not show any significant benefit using ramipril in treating Maine Coon cats with hypertrophic cardiomyopathy without heart failure.
Like other ACE inhibitors, it may potentially be useful as adjunctive treatment in chronic renal failure and protein losing nephropathies. In dogs with moderate renal impairment (such as might be found with CHF), there is apparently no need to adjust ramipril dosage.
Arzneimittelwechselwirkung
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
Stoffwechsel
Ramipril is metabolised in the liver to its active metabolite, ramiprilat, and other inactive metabolites. It is excreted mainly in the urine, as ramiprilat, other metabolites, and some unchanged drug. About 40% of an oral dose appears in the faeces; this may represent both biliary excretion and unabsorbed drug.
Lager
Store at +4°C

Ramipril Upstream-Materialien And Downstream Produkte

Ramipril Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

87333-19-5, Ramipril Verwandte Suche:

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