Cilazapril Monohydrate
Names
[ CAS No. ]:
92077-78-6
[ Name ]:
Cilazapril Monohydrate
[Synonym ]:
Cilazapril Monohydrate
Cilazapril (monohydrate)
Biological Activity
[Description]:
Cilazapril Monohydrate is a angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.Target: ACECilazapril is a new nonthiol group containing angiotensin converting enzyme (ACE) inhibitor. Cilazapril has been investigated in more than 4000 patients with all degrees of hypertension, as well as in the special patient groups such as the elderly, renally impaired, and patients with concomitant diseases, such as congestive cardiac failure or chronic obstructive pulmonary disease [1]. Cilazapril is a very potent and highly effective converting enzyme inhibitor. Doses well below 5 mg/day will probably suffice for therapeutic efficacy [2].
[Related Catalog]:
[References]
[Related Small Molecules]
Angiotensin I/II (1-7) trifluoroacetate salt
|
Captopril
|
Enalapril maleate
|
Perindopril erbumine
|
Lisinopril diydrate
|
Phosphoramidon disodium salt
|
Trandolapril
|
Fosinopril sodium
|
Quinapril hydrochloride
|
Ramipril
|
Enalaprilat Dihydrate
|
omapatrilat
|
Temocapril (hydrochloride)
|
Cilazapril
|
Hemorphin-7
Chemical & Physical Properties
[ Boiling Point ]:
598.1ºC at 760mmHg
[ Melting Point ]:
98° (dec)
[ Molecular Formula ]:
C22H33N3O6
[ Molecular Weight ]:
435.51400
[ Flash Point ]:
315.5ºC
[ Exact Mass ]:
435.23700
[ PSA ]:
108.41000
[ LogP ]:
1.79790
[ Storage condition ]:
-20℃
Toxicological Information
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- UR6113250
- CHEMICAL NAME :
- 6H-Pyridazino(1,2-a)(1,2)diazepine-1-carboxylic acid, octahydro-9-((1-(ethoxycarbonyl)-3- phenylpropyl)amino)-10-oxo-, hydrate, (1S-(1-alpha,9-alpha(R*)))-
- CAS REGISTRY NUMBER :
- 92077-78-6
- LAST UPDATED :
- 199706
- DATA ITEMS CITED :
- 12
- MOLECULAR FORMULA :
- C22-H31-N3-O5.H2-O
- MOLECULAR WEIGHT :
- 435.58
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 15 mg/kg/22W-I
- TOXIC EFFECTS :
- Skin and Appendages - dermatitis, other (after systemic exposure)
- REFERENCE :
- LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 345,398,1995
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >5 gm/kg
- TOXIC EFFECTS :
- Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - hypermotility, diarrhea
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,1281,1989
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 830 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,1,1990
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >1 gm/kg
- TOXIC EFFECTS :
- Skin and Appendages - dermatitis, other (after systemic exposure) Behavioral - rigidity (including catalepsy)
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,1281,1989
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >30 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,1281,1989
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 5 gm/kg
- TOXIC EFFECTS :
- Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Nutritional and Gross Metabolic - body temperature decrease
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,1281,1989
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 1300 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,1,1990
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- >1 gm/kg
- TOXIC EFFECTS :
- Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,1281,1989
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- >30 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,1281,1989
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Primate - monkey
- DOSE/DURATION :
- >4 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,1,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 22750 mg/kg/13W-I
- TOXIC EFFECTS :
- Cardiac - changes in heart weight Blood - normocytic anemia Nutritional and Gross Metabolic - weight loss or decreased weight gain
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,1295,1989
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Primate - monkey
- DOSE/DURATION :
- 22500 mg/kg/90D-I
- TOXIC EFFECTS :
- Cardiac - changes in heart weight Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Blood - changes in erythrocyte (RBC) count
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,1333,1989
Articles
Cilazapril stability in the presence of hydrochlorothiazide in model mixtures and fixed dose combination.
Acta Pol. Pharm. 70(6) , 1079-85, (2013)
The presented study aimed at the evaluation of hydrochlorothiazide influence on cilazapril stability in model mixture and fixed dose tablet formulation. The degradation of cilazapril in the presence o...
Common medications among dental outpatients: considerations in general dental practice.N. Z. Dent. J. 108(4) , 140-7, (2012)
To provide information about the most common medications listed as being taken by dental patients presenting to an outpatient setting at a tertiary institution and to establish a list of the most comm...
Ultra-thin-layer chromatography mass spectrometry and thin-layer chromatography mass spectrometry of single peptides of angiotensin-converting enzyme inhibitors.J. Chromatogr. A. 1218(20) , 3089-94, (2011)
The separation of structurally related angiotensin-converting enzyme (ACE) inhibitors lisinopril, cilazapril, ramipril and quinapril and their corresponding active diacid forms (prilates) by conventio...