Download - 心血管药理
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(cardiovascular pharmacology)
[email protected] floorLibrary Building
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24 (drugs acting on ion channels in cardiovascular system )
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permeationselectivitygatingRPAP
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1(voltage gated channels): (ligand gated channels)(mechanically gated ion channels)(nongated background/leak channels2 ionchannelpathies
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(calcium channel blockers,)
()1.2. LTNPQR LT :
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calcium antagonist () Ca2+,Ca2+(calcium channel blocker)()1.WHO(1987) PDC PDC
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2.IUPHAR(1992)L4 a b c d T N P
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()1. (1), (2),, (3)Ca2+2. (1), (2) (3)
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3. (1) (2) (3) (4)(, 4. ,,5. ASVSMC6. ;; 7.;;;
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()1.2.
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()1.(1),(2),(3),(4)(5),,,,,,(6)As2.,
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()
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+++ ++ ++ +++ ++ ++ 0+ 0+ 0 0 0 0 +0
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(drugs acting on potassium channel)
(potassium channel modulators). (potassium channel blockers) : (potassium channel openers) ,
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(drugs acting on sodium channel)
(sodium channel blockers) I
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25 (antiarrhythmic agents)
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1.*2. RPAP AP AP APNa+K+Ca2+3.,,
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1.2.* RPAP AP AP APNa+K+Ca2+3.,,
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1.2. RPAP AP AP APNa+K+Ca2+3.,,*
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1. (1):, (2)2.(afterdepolarization)(triggered activity) AP,TP,,
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: (EAD)AP23* (DAD)AP :K+ ,TP,,Ca2+AP Ca2+Na+Na+TP,
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: (EAD)AP23 (DAD)AP*: K+,TP,, Ca2+AP Ca2+Na+Na+TP,
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: (EAD)AP23 (DAD)AP. : K+,TP,, Ca2+ AP Ca2+Na+Na+TP,
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3. (1):,, AP (2)(reentry) : : ERP *
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reentry
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4.
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RPAP 1. Na+Ca2+K+2. (1) K+
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(2) Na+(Ca2+K+) 3.ERPAPD (1)ERP: Na+Ca2+K+ERP (2)ERP/APD (3)ERP4. ,,
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:Na+ a, b, c::APD():
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pro-arrhythmia
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()a(quinidine)1.Na+,K+,Ca2+ Na+(, ) (1) (2) (3)APDERP (4)
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2.1.,2.,,3.,1.chichonic reaction2.3.:,,,4.
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(procainamide) :1.2.,,,3.,,;4.,,
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() b(lidocaine)K+,Na+,K+ 1.2.ERPAPD,ERP/APD,ERP,*3.
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() B(lidocaine)K+,Na+ 1.2.ERPAPD,ERP/APD,ERP,3.
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(1)(2) (),1.2.
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(phenytoin sodium)1.,;Na+-K+-ATP,2.,ERPAPD,,3.,,4.
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mexiletine
,,,
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()C(propafenone)1.Na+2.APDERP;3.4.
(flecainide),(encainide)
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(,propranolol) CA1Na+Ca2+ ,,ERP(1)()1(2)Na+ : : 1.: 2. 3.ERP
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CA()(1)(2)(3),, (4),;(5)
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APD (amiodarone )T3T41.APDERP2.:,3.4.,,
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,1.2.3.,4.
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sotalol12APDERP
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LERP ,,(verapamil)Ca2+ :1. 2. 3.ERP
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1.2.,3.4. ,;
:P291
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27 [Drugs used in treatment of chronic congestive heart failure(CHF)]
RAAI :,
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1.*2.3.:,,4. (1) (2)ACEI
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1.2.*3.:,,4. (1) (2)ACEI
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1.2.3.:,,4. 507070ACEI8090AVPET
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RAAI: ACEI, AT1, : :,(1)(2)ACEI
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RAAI(renin-angiotensin-aldosterone inhibitor) ACEIAT1
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ACEI 1.12
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2CHF(1)ACE ACEAng Ang NOPGI2
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(2): ACEAng (3) (ventricular re-modeling)4 CA1AC5VEC
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AngACEIAngNOPGI2 3.CHF 4.5. (captopril) (enalapril) (cilazapril) (benazapril)
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AT1(ARB)1.Ang2.CHF( Ang)3. ACEI4.(losartan)(valsartan)(erbesartan)
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(aldosterone antagonists) VSMC PAI (spironolacton) ACEI
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(diuretics) 1VSMC2ACEI CHF CHF CHF3RAASNA
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1. 2.(1) Ang II CACa2+
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CA RAAS (2) (3) (4)3.CHF()CHF,,CHF,
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(carvedilol)()(metoprolol)(bisoprolol)4.(1)ACEI(2)(3) 3(4)(5)
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(cardiotonic agents) 1.,2. (1), (2)1, , (3)PDEPDEcAMP (4)(calcium sensitizer),;PDE-III
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(cardiac glycosides)
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1.(1) :,, :, ,,*(2) , ,
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1.(1) :,, :, ,,(2) , ,
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(3) +(Na+-K+-ATP)Na+K+Na+Na+Na+Ca2+ ,Na+Ca2+Ca2+*2.(1)(2)
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(3) +(Na+-K+-ATP)Na+K+Na+Na+Na+Ca2+ ,Na+Ca2+Ca2+2.(1)(2)
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(3) ,; ;
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3.(1)(2) () (3)
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4. ,5. ERP (1)Na+-K+-ATP(2) ACh,,ERP
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6.P-P,P-R,Q-T,T,S-T,
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NA CNSCTZCHFII
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(1) (2)Na+-K+-ATPNa+
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1.CHF(1), ; ; (2),
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(1)(2)(3)B1,(4),,(5),
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1.2.3.1997
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2.(1) ,(2) ERP, , ,, ,(3)
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(1),(2) ,;K,, , , :,;,,,K , ,,K,,
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1. (1) (2)CNS (3) 2.
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(1),,,,(2), 3. (1) (2) (3) , (4)
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1.+ , ,24h, ,24 , 1.251.5mg 0.1250.5mg2. ,0.25mg/1
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(1)(digitoxin),(2)(digoxin),(3) Clanatoside Ccedilanid) K(strophantin K)
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( receptor agonists) 1. AdNAIP (1) (2) (3)
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2.1,,,,,
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(1) ,,(2)(xamoterol) (3)DA 1 ,1DR 12DR(4):()
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(PDEI) (1)+(2)PDEVSMCcAMP; VSM,,(3)(4),(5)(milrinone),
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calcium sensitizer PDE-III
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(vasodilators) 1. (1)AV , (2)2., 3. (1)
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(2) (3) 4.(1)(2)(3) ;(4)
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4. (1)(nitrovasodilator) (V>A),(A=V) (2)(A>V) (3) (A>V) (4) A>V (5)ACEI
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ACEIACEIACEIACEIACEIACEI(:2002)
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28 (antianginal drugs)
1.2. (1) (2) 3 3.,
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4. , , 5.: (1) (2) (3)4
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(nitrates) (nitroglycerin),,(8%),(80%),
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,VSMNOGCcGMP cGMPPK *1.VSM,AV, V2.., , 3.,, ,,
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,VSMNOGCcGMP cGMPPK 1.VSM,AV, V2.., , 3.,, ,,
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1.: A,V,2., (1)AV (2),,,,,()3. NOPGI2CGRP 4.NO
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1.,,,2.:,3.1.2.VSMC,,
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(receptor blockers) 1. 1,2.(1)1(2)2,3.FFAGS
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1.()2.?3. 4., (1),
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(2) (1),(2)(3)(4)
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(calcium antagonists) (nifedipine)(verapamil)(diltiazem)Ca2+1. ,
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2.(1),(2)3. Ca2+Ca2+4. ,,,
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1.2.3.,4.,,5.,,,,
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/
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29 (anti-atherosclerotic drugs) 1.As2.(1)LDL ; (2)TGVLDL. A 3.
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lipidemic-modulating drugs 1. cholTG cholTGPL HDLLDLIDLVLDLCM2. () (-) (ab) -() -() ()()*
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AS I CM TGTC a LDL TC b VLDLLDL TGTC III IDL TGTC IV VLDL TG V CMVLDL TGTC
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3.(1)(2)(3)LDLVLDLTCTGapo BHDLapo A
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LDL ()HMG CoA(HMG CoA reductase inhibitors)(statins)1.(1)TCLDLVLDLapo B,HDL(2) VSMC As CAs
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2.HMG CoAchol,cholLDLLDLVLDLapo BVLDL3.(ab)4.ALP5.
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(cholestyramine,)(colestipol,)TCLDL(1)chol (2)chola1.2.3.,,,,,
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TGVLDL(nicotinic acid)1.TG,VLDLLDL(TGVLDL)2.HDL3.TXA2PGI2TG B,,1.2.,3.
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fibrates,1.TGVLDLLDLTCHDL2.3.(1)VLDLTG (2),VLDLTG (3)PPAR b,,,III1.2.,,,,
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(probucol)1.1ox-LDL2TCLDLHDL3As2.3.
:E(vitmin E)
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(polyenoic fatty acid)
(unsaturated fatty acids)
:1.TGcholLDLVLDLHDL2.3.4.
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(heparin)AsTCTGLDLVLDLHDLVSMC As
(
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30 (antihypertensive drugshypotensive drugs)
1. ,140/90mmHg2.VECAsAs 3. (1)/ (2)///3/*
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4.
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1.2.- (1)ACEI (2)AT1 (3):3. (1) (2) (3) (4) 4.5. (1):, (2):,*
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(duretics) ,,1. 2. Na+VSMC Na+ Na+-Ca2+Ca2+VSM
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1.,2.3..ACEI (,)Na+()()
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-renin-angiotensin inhibitors ACEI1.10 2.,3.,4.5.6.
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ACE 3,,,,+(),+,+
1.ACE,2.,PGI2NO3.4.5.,6.
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1.:++2.,1.()2.3.4.(captopril)(enalapril)(ramipril)(benazapril)
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ACEI1.2.ACEI3.AT11.AT AT4AT12. AT1AT-II3.:ACEI4.(losartan),(valsartan) (irbesartan)
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(clonidine,)1. (1), (2), (3) 2.,
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1.I12.2,()3.NA2NA
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1. 2.1.2.3.
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1.(1) 2. 3.
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(prazosin)1.(1), (2) (3) (4), (5) 2.3.TGTCLDL-cVLDL-cHDL 1
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1.,2.1.2.
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(propranolol)1.,,2.3.,4.1.12.NA3.24.()5.6.
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1.2. (1) (2) (3),,3.,
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(labetalol,)1.,1212112.,3.
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VSMCCa2+Ca2+VSM
(nifedipine) (nitrendipine) (lacidipine) (amlodipine)
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(nifedipine)1.,2.3.,4.ACEI4.,,5.,,
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(nitrendipine)(lacidipine)(amlodipine)
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1. 2.
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(hydralazine,)1.,2.,,,3.,4.,,Ca2+Ca2+
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1.2.,1.2.3.
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(diazoxide)1.2.,3. VSM4.,5.,,
,
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(sodium nitroprusside)1.,2.3.NOGCcGMP VSM4.,5.,
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1., ACEI ,*
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2. (1) (2)+ (3)++ (4)+++3. (1)-,,ACEI (2)-,, ACEI, (3),,, ACEI, (4),,
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(5), (6) (7) (8) (9)(10)4.5.6.7.ACEIAT18.(ACEI)
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Thanks for your cooperation
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