?? ????Cholinergic Drugs

1
?????????

• ??
• ????????????????????????,??????????????????
• ??????????????,??????????

2
?? ????Cholinergic Drugs ?? ??????--????? ???
???--??AchE ?.??????? (?)????
To (?)?????? To (?)M?????
To ???????? To (?)?????????? (?)??????????
To
sum
3
1.???? Acetylcholine (CH3)3N-CH2-CH2OCOCH3 ??,???
,????????,????,????,?????,?????????? ????M?N??????
?M????N???,????????????
4
M???-----( M???) 1/ ?? ????????--(??????
????) 2./ ?? ?????????? --(????????) 3/ ???
????????????????? --(??????????????????????) 4/
??? ???????--(??? ???? ???? )
5
N???-----(N???) 1./ N1????(???????) ???????(????
???????)M????1-3--(??? ???? M????1-3) 2./
N2???? ?????? --(??????) Ach ????????,??????? Back
6
2.????(Carbachol) ??????(glaucoma),
0.51.5???? 3.??????????????? 4.?????????????
? ?????Ach,?????M?N??? ?????AchE??,????,??????
????? ????????????????? back
7
(?) M????? ????? (Pilocarpine ,????)
??????,???,?????M??, ???? ????????????? 1.????
1)??(miosis) ??M??(??????) ??????????To 2)???? ???
?????????????????????????????????????? ???glaucom
a ?????????? Pilocarpine ??????????????????????
??????????? ???? ??
8
3)???? Pilocarpine-????????M??????????????????????
????????? ????????????? To 2. ?????
????M???????,????????????
9
???? 1) ??? 1-2 ?? ? ??(20???-75???-??48??)
? ??????????????,?????????????????,??????? ??????
???????????,???????,???????????????
10
2) ?????? ????????,?????(????),???????????
3)?? ???????????? 4)??????? 3.??????,???????
??M??? Back
11
??????? (Anti cholinesterase drugs) ??????? ???
?????????,???????????,???????????? ?????????????
?????????????,???????,??????
12
AchE?Ach?????

• 1.AchE (?????),?????MW8?,???????
• ?????(?????)????????
• ??????N(?????)???OH(?????)??H,??????OH????,??AchE?
  ??C???? pp54?
• 2.AchE??Ach???
• ??AchAchE-- ???
• ???????AchE
• ??????AchE(23??) ??

13
(?)?????????? 1. ????(Neostigmine) ????
?Ach???AChE???,??????????,?Ach????,??????????????
??????N2?????????????????
?? 1)???,??????(???????10?),????BBB???? 2)???????
?????????????? 3)??????????????? 4)??????
14
1/ ???? (1)????? (Myasthenia
gravis,???? ???????????,???0.05,
N2????,??N2?????7090),15min??,??24h? ?????????
??M?N???,?????? ?????????(prednisolone)
??????(????,Azathioprine)?????
15
(2)?????????,???????? (3) ????????????? (4)
????????(????)???? ???? ?????,??????,?????????,?
??????????????????????????
16
2. ???? Physostigmine(eserin???) ???????????,???
?????,?????????,???????????,????????? ?? 1.
??????,???????(0.25),????pilocarpine,??,?????? 2.
????M??N???,??????????
17
(?)?????????? ??????????? ?.????????? ?????E1
059??????????? ???????????? ???? ??? 
18
???? ???????????????,???? ?????-AchE???,
?????(4h ??)?????(??????????? ????AChE)??????,??
??? 1530?
19
(?)???? ???? 1.      ??M??? 2.     
??MN??? 3.      ??MNCNS?? ???(???????????)---
??(????????????????)--?? ???? ??AChE??,?????????
??????
20
?.???????? (?)???? 1?????(????,???????,1????,???
??) 2?????(??,??,????) 3?M???????????Atropine(
??,??,??,??????????????????????)????M???
,N1???CNS?? 4??????AchE??,????N???
21
?)??????? (cholinesterase reactivitor) ????(??PAM
) 1.???? ?? N-OH ????AchE????OH?????,????????
????? ??????????? AchE????? ????????????????AchE?
2. ???? ?????Atropine??,?????????? ????(PAM-
Cl)????,??,?????,???,???,????PAM Back
22

• ??????(Anticholinergic drugs)
• ??
• M??????? To
• N1?????
• N??????? 
• N2?????
• 
  To

23
M?????

• ?????M??(M1?M2?M3)
• ??? ???(?????), ????(?????,????1965?),????(??),??
  ??,???(??????,????1970?)
• ???????

24

• ??     ???(Atropine)
• (?)????
• 1.????????M??
• 2.?????N1??
• 3.?????????
• 4.?????????

25
(?)??????????? 1.???? 1/)?? - ???M????,?1?????????
? ???????(?????1-2?,???Homatropine)??????(??????
) 2) ????-???Pilocarpine??-- ????? 3)
????-?????,?????,?????,?????--?????(?????)
26
2.???? ??????????????????,???? ?????(??????????
) ?????? 3.????? ??????????????????????????????
????????????????????? ?????,????????,?????????
?????? ??????????,????????(?????,???),???????????
?????
27
4.????? 1)?????????(??????M1,?Ach???
????????????)?????????M2 ??,???? ?????????? 2
)????????????????????????????? ????????? 3
)?????????????? ???????,??????????,??????????????
???,??????,?????, ?????????? 5.????????,????? 6.?
???????????
28
(?)????????? 1.????????????????????????? ????????
????? ???????????????????? 2.????(????????????)
????--????? ??Pilocarpine , Neostigmine 3.??
???(??),?????(????),????
29
???M??????? (?Atropine????) ???? ???? ???? ??
?? ????
30
(?)????(Anisodamine , 654-1 ?2)1965???????????????
? ???????? ???????,??????????????????????(
?????1/15),???????? ??????????????????????????
?????????????????????????????????????
31
(?)????(Scopolamine)?????,??????? ????
??????????????????????????????? ?????,?????,????
?,??? ???? 1. ?????(?????,????) 2.
???(????,??????,?????) 3. ????(?????),????,??????
???
32
(?)???????????

• 1??????
• ????(Homatropine)
• --??????,???,?????????????,????????(1-3?)?
• ????(tropicamide)

33
(?)???????????

• 2??????
• ????(Probanthine)
• ??????????????,?????,?????????,????????
• ?? ?????????????(?H2??????????cimetidine????)
  

34
(?)???????????

• 3.???M1?????
• ????(pirenzepine)?????M1?????,???????????,??H2????
  ???????????? ???????? ????
• back

35
N ???????

• N1???????
• ?????Ach????????N1?????,?????????????
• ????
• ???????,??????
• ????,????,?????
• ????????????
• ???(Mecamylamine)

36
N ???????

• N2 ???????,?????(Skeletal muscular
  relaxants)?????????N2???,???????????,???????
• ????
• ?????????,??????
• ??
• 1????????
• 2????????? To com

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N2 ???????

• 1????????
• ??????????N2??,????AchE??,?????Ach?????????,?????
  ??????????????????,?????
• ???????
• ?1? ??????
• ?2? ??????????Ach???

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N2 ???????

• ?????(Suxamethonium,??? Scoline)
• ??AchAch (??????,?????)
• ????
• ????????????????
• ????????????????

39
N2 ???????

• ????
• ?????????????
• iv 1030mg,????????,1min?????(???????,???????
  ,?????),???5min?
• ???? ????,???,???,???????????

40
??????? ?????,???????????(???????,????)?
??????(???,??,???K????,?????,??K) --?????????,??
K??,?????????????? ??????AchE????,???????,????
????Neostigmine??(??!) ????
back
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N2 ???????

• ?????(?????)???
• ????
• ?Ach????????N2??,??Ach?????????????,????
  ????

42
????(d-Tubocurarine)????? ????(pancuronium
bromide),????????5?,???????? ????
23????,??30???,??????-??-??,??????? 3.??
?????????,????????? 4.?? ??????????????????????
???????Neostigmine ??
43
????(????,gallamine triethiodide)
????????1/5,?????1/2 , ?????Atropine???(??????????
???) Back
44
?????????????????????
??????? ????????
????? ?????????
????????? ?????????????????????
??????????? ???????????
???????????? ?????????????
????????????? ????????????
sum
45
To-14
46
To-14
47
???????
48
To-17
49
To-18
50
To-7
51
To-35
52
To-25
53
????
??????qd ??1? bid??2?
tid ??3? qid??4?
on ??1???
q4h
?4??1? ???? im (intra muscular)????
iv (intra venous)????
sc(subcutaneous
injection)???? po
(per oral )???? iv
inf (iv infusion)????
ip (intra peritoneal )????
54

• ???????(Alzheimers disease,AD)
• ?????(???????????????????????),?????????????
• ?????????Ach(AchE inhibitors)
• ???(tacrine)???BBB,??AchE,????M???????????????
• ???(huperzine),????????????????AD??
• ????(galantamine)????tacrine,????????????????
• ????(metrifonate),??Bayer??1952???????(???),80????
  AD?To-20

55
TO-1
56


TO-1
57
TO-9
58
TO-7
59
TO-3
60
vagal system that fosters digestion and responds
to novelty or threat by reducing cardiac output
to protect metabolic resources. Behaviorally,
this is associated with immobilization behaviors
61
Demonstration of local adaptation effects. Note
the close connection of the effects to eye
movements.
62
Atropine, scopolamine are muscarinic ACh receptor
antagonists                                     
                                                 
                          
63
??