Pharmacology

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??? ???????(I) M???????
Cholinoceptor blocking drugs Muscarinic receptor
antagonists
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• Muscarinic receptor antagonists
• (-)
• muscarinic cholinergic receptors at
  neuroeffector
• (-)
• the effects of ACh (smooth muscle, cardiac
  muscle, gland cells, peripheral ganglia and in
  CNS.
• muscarinic receptor antagonists includes
• the naturally occurring alkaloids (atropine,
  scopolamine)
• semisynthetic derivatives of these alkaloids
• synthetic congeners

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1. SOURCE AND CHEMISTRY
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Atropine natural
congeners
????????? tertiary amine alkaloid esters of
tropic acid
Naturally occurring atropine is
Ll(-)-hyoscyamine, but the commercial material is
racemic d,l-hyoscyamine. Scopolamine is d()
isomers.
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Absorptiondistributionmetabolism and excretion
2. ???? (1) Atropine(???),PO???,F
50,??????,?????,????(CNS), ???scopolamine????????
CNS, (2) ???PO??? (3) Atropine PO?1h??????,t1/2
4h,????????72h,????3-4h?
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???(Atropine)
M?????,?????ACh????? M1?M2?M3??????,????N1????????
?????????????????,?????????,???????????,????,??
????????
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6. ?????? 0.5-1 mg ?????????????????() 1-2 mg
??????? 5 mg CNS ?????? 10 mg ??, CNS
???? ????,????,????????????????
6. ??????????
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Adverse Effects
1. ???????,????? ???????????????????????CNS??? 2
.?????????????????????????????????,?????????,??
?80-130 mg,??? 10 mg?
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  3. atropine????? ???? (1)?????,?????? (2)???
? 1-4 mg(??0.5 mg)??i.v,??????(??????),???????????
??,?????? (3)???????????? ?????????(????M??,????)?
???????????? 4. ?????,?????(??????)?
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???? (anisodamine, 654) ?? ????????????,??????
654-2?
??????,????? 1. ???? (1)????????? (2)??????,????
??? (3)????????? 2. ?? (1) ??????? (2) ??????? 3.
????????????

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???? (scopolamine)
??
1. ???? (1)????????????
??????????? (2)????????gt???,?????????? 2.
?????????????????????????(Parkinsons
disease,PD) 3. ????atropine
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??? ???????????????
?? ?????
????(homatropine) ???? (tropicamide) ????
(cyclopentolate) ???? (eucatropine) ????????(0.25
-2d) ????????
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?. ?????

• (?)???
• ?????
• ????M?????,???????????
• ?????(????,propantheline bromide)
• ??????????????????
• ????????????????????????????
• ?????atropine,???????????
• ????????????????????????????????????????,????????
  ?????

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• (?)???
• ?????????????(trihexyphenidyl hydrochloride)
• ??????????????????????
• ????(benactyzine,???)
• ?????,?????????,??????,?????
• ??
• (1) ?????????????
• (2)???????????
• 3. ?????????
• ????????????????????????
• ????,??????????

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?????M???????
????(pirenzepine) ????(telenzepine)

• ?????????,????????
• ?????M1????????????
• ??
• (1)?????????????
• (2)?????????
• ???????

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??? ???????(II) N???????
Cholinoceptor blocking drugs Nicotinic receptor
antagonists
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??? ?????? Ganglionic blocking drugs
?????N??????Ach????????????????,????????? ?9-
1 ?????????????????????? ?? 1.
???????? 2.???????,?????????????????, ?????? ???
?(mecamylamine, ???) ????(trimetaphan camsilate)
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??? ?????? Skeletal muscular relaxants Neuromuscu
lar blocking agents
???????????NM??,??????????
???????(depolarizing muscular relaxants) 2?
????????(nondepolarizing muscular
relaxants)
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?????????

• ???????????N?????ACh???????
• ??????N???????ACh????????
• ????
• I????II???
• ??
• ?????????????????????????????
• ??????????
• ???????????????,??????
• ???????????

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???? (succinylcholine,???,scoline
) ??????????????
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????

• ????
• i.v??????????????????
• ???????????

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???? 1.??????????,??????????AchE??? 2.???? ???
??????????,???3-5?? 3.?????,??K??????? 4.????
????,????,????(?????)?
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?????? 1.????????,?????????? 2.?????????????????
????AChE? ?,?????????? 3.?????????B????????????
,? ????
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??????????
??????? 1. ??????????????? 2. ???????? ???
??????????,?ACh?????????N??,??Ach??????????
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???? (d-tubocuratine)
??
???????????????????,????,?????????????,?????????
????????????????

• ??
• ????????,?????,????????2???,5????,40?????
• 2. AchE????????????????

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5. ????,????????,????,?????? 6.
???? ?????P87,?9-2
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summary

• Cholinoceptor antagonists are divided into
  muscarinic and nicotinic subgroups on the basis
  of their specific receptor affinities.
• Atropine causes reversible blockade of
  cholinomimetic actions at muscarinic receptors.
  It does not distinguish the M1, M2, M3 subgroups
  of muscarinic receptors.
• suppresses secretion of gland
• Eye(dilated pupils,cannot focus for near
  vision)
• relaxes smooth muscle
• Cardiovascular system
• Central nervous system

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3. Anisodamine, scopolamine, homatropine,
propantheline bromide, trihexyphenidyl,
pirenzepine, et al. 4. Antimuscarinic agents
can provide some relief relief in the treatment
of common travelers diarrhea and urinary urgency
caused by minor inflammatory bladder disorders,
Some of them are used in treatment Ophthalmologic
disorders, Parkinsons disease, motion sickness,
shock and cholinergic poisoning.