antihypertensive agents ACE inhibitors

1
antihypertensive agents ACE inhibitors
2
115/75 ???? 20 ????????? ?? ???????????? ? 10
????????? ?? ?????????????140-160/90-95 ????,
???????, ?????? 1??? 160/95 ????????????
??????, ?????? 2
3
(No Transcript)
4
????????? ?? ????????
angiotensinogenase
Renin Release ---? Angiotensinogen ---?
Angiotensin I ACE ---? Angiotensin II ---?
Angiotensine III ---? Inactive

Products
5
(No Transcript)
6
2

• Bradykinin ---? Prostaglandin Release ---?
• 
  Vasodilatation

ACE
Inactive Products
---?
7
Captopril
1981 ?

• (S)-(3-????????-2-?????-1-????-
• ??????)-L-??????

(2S)-1-(2S)-2-?????-3-?????????????????????????
?-2-???????????? ????????
Ph Eur
(2S)-1-(2S)-2-Methyl-3-sulphanylpropanoylpyrroli
dine-2-carboxylic acid
Angiotensin-converting enzyme inhibitor
8
(No Transcript)
9
??????????
??????????????? ??????? ? ?????????? ?????? ??
3-?????????-2-?????-??????????? ?-?? ?
?????????? ?? ????. ?????????????????? ??
???????? ???? ????????????????.
10
3-?????????-2-?????-????????? ????????
?????????????? ?? ???????? ?-?? ??? ???????????,
?????? ????????? ?? ???????????.
11
Lisinopril

• (S)-1-N-(1-????????-3
• ???????????)-L-?????-L-??????
• ????????

1-6-a????-2-(1-????????-3-?????-??????)a????- ???
???????????????- 2-???????????? ????????
????????
Ph Eur
Lisinopril Dihydrate
(2S)-1-(2S)-6-amino-2-(1S)-1-carboxy-3- phenylp
ropylaminohexanoylpyrrole-2-carboxylic acid
12
?????????????

• Enalapril

(S)-1-N-1-(??????????????)-3-???????????-L- ???
???-L-??????
1-2-(1-e?????????????-3-?????-??????)a???????????
?? ?????????-2-???????????? ????????
Ph Eur
Enalapril Maleate
(2S)-1-(2S)-2-(1S)-1-(ethoxycarbonyl)-3- phenyl
propylaminopropanoylpyrrolidine- 2-carboxylic
acid (Z)-butenedioate
13
VASOTEC I.V.(Enalaprilat) is a sterile aqueous
solution for intravenous administration.
Enalaprilat is an angiotensin converting enzyme
inhibitor. It is chemically described as
(S)-1-N-(1-carboxy-3-phenylpropyl)- L-alanyl-L-p
roline dihydrate. Its empirical formula is
C18H24N2O52H2O. Enalaprilat is a white to
off-white, crystalline powder with a molecular
weight of 384.43. It is sparingly soluble in
methanol and slightly soluble in water. Each
milliliter of VASOTEC I.V.contains 1.25 mg
enalaprilat (anhydrous equivalent) sodium
chloride to adjust tonicity sodium hydroxide to
adjust pH water for injection, q.s. with
benzyl alcohol, 9 mg, added as a preservative
14
?????????????

• Fosinopril

4-???????????-1-2-?????-1- (1-????????????)
?????????(4-??????????) ????????a?????-L-??????
???????? ???, trans-
4-??????????-1-2-(2-?????-1-?????????????-??????
??)- (4-??????????)????????a?????-?????????-2-??
?????????? ????????
15
(No Transcript)
16
?????????????

• Quinapril

3S-2R(R),3R-2-2-1-(??????????????)- 3-
???????????-????? -1-??????????-1,2,3,4-???????
???-3- ?????????????????????? ????????
???????????
17
?????????????

• Moexipril

3S-2-R(R),3R-2-2-1-(??????????????)-3-
????????????????- 1-??????????-1,2,3,4- ??????
????-6,7-?????????-3-??????????- ????????????
???????? ???????????
18
?????????????

• Perindopril

2S-1-R,(R),2alpha,3a beta,7a
beta-1- 2-1-(??????????????)-??????????-1-
???????????????????-1?-?????-2- ????????????
????????
19
Perindopril Erbumine

• Ph Eur

2-Methylpropan-2-amine (2S,3aS,7aS)-1-(2S)-2- (
1S)-1-(ethoxycarbonyl)butylaminopropanoyloctahy
dro- 1H-indole-2-carboxylate
20
?????????????

• Trandolapril

Ph Eur
(2S,3aR,7aS)-1-(2S)-2-(1S)-1-(Ethoxycarbonyl)-
3- phenylpropylaminopropanoyloctahydro-1H-indol
e-2- carboxylic acid
21
?????????????

• Cilazapril

Ph Eur
(1S,9S)-9-(1S)-1-(ethoxycarbonyl)-3-phenylpropyl
amino- 10-oxooctahydro-6H-pyridazino1,2-a
1,2diazepine-1-carboxylic acid
22
?????????????

• Spirapril

Spirapril Hydrochloride Monohydrate
Ph Eur
(8S)-7-(2S)-2-(1S)-1-(Ethoxycarbonyl)-3-phenylp
ropylaminopropanoyl- 1,4-dithia-7-azaspiro4.4
nonane-8-carboxylic acid hydrochloride monohydrate
23
Ramipril
(2S,3aS,6aS)-1-(S)-2-(S)1-(??????????????)- 3-
???????????a?????????????o??????????????????b
?????- 2-???????????? ????????
Ph Eur
(2S,3aS,6aS)-1-(S)-2-(S)-1-(ethoxycarbonyl)-3-
phenylpropylaminopropanoyloctahydrocyclopentab
pyrrole -2-carboxylic acid
24
???????? ????? ?? L-???????
???? 3-??????????????
???????? ?? ???? ????? ????????? ?-??
(S)-N-(1-??????????????-3- ???????????)-(S)-??????
25
?????????????
angiotensin II receptor (type AT1) antagonist

• Losartan

Non-peptide angiotensin II receptor antagonist
2-?????-4-?????-1-2-(1?-????????-5-??)1,1-???
????-4-?? ?????-1?-????????-5-???????
26
Losartan potassium
27
?????????????

• Valsartan

Nonpeptide angiotensin II AT1 receptorantagonist

N-(1-??????????)-N-2-(1?-????????-5-??)1,1-??
?????- 4-???????-L-?????
28
?????????????

• Telmisartan

4/-(1,4/-???????-2/-??????2,6/-??-1?-???????????
?-1/-??) ?????1,1/--???????-2-????????????
????????
nonpeptide angiotensin II receptor (type AT1)
antagonist.
29
Eprosartan
non-tetrazole angiotensin II receptor (AT1)
antagonist.
Prototype of the imidazoleacrylic acid
angiotensin II receptor antagonists
(?)-alfa-2-?????-1-(4-?????????????)?????- 1?-
????????-5-?????????-2- ???????????????
???????? ?????????????????