n

]i.!\-. il \m , V,\/l I

..

............................ 1
..............
1
...................................... 2
...................... 3
.......................... 6
....................:.............. 7
.................................... 9
.................................. 13
.............................. 17
-..... ............... 17
...................... 19
.............................. 21
.............:..............22
............................ 24
...........
25
...............
27
.............................. 28
..............29
...... ....................... 35
...................................... 35

...................... 36
.................................. 37
...................................... 38
..................................41
......................................42
............ 43
.................. 43
M A C ................
44
M A C ...........................46
M A C ............................ 47
.............. 48
............48
........................50
.... .................... 54
............ 57
....................................... 57
> ..................................... 61
......................................66
....................................70
...................................... 72
......................................76
......................................... 80
................. 81
..................................... .
............................... 82
....................................... ..
.......................... 96

________________________________

......................................97
...................................... 107
.................................. .117
..........
124
.............................. 126
. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 128
....................

129

.................................... 129
.................................... 129
.......................... 131
.................................... 132
...... :...................... 133
.......................... 134
........................................ 134
............................ 138
... ................................. 140
........................ 142
.................................. - 144
.................................. 145
_ ..................... 146
..........:........................ 147
...................................148
... ................................. 149
.........
149
.................................... 150
........................... 151
..................................... .
X 3X

...................................... 153
...................................... 154
...................... 155
...................................... 155
....................
157
................................ 158
.... ............................... 158
................................ 158
........................ 160
...................... 163
Cm) ................ 165
............................ 165
........
168
:...................... 171
........................................ 171
........................................ 176
..................... :.......177
# 180
........................ 180
..................... 180
.......................... 181
::..................... 181
.............................. 183
........................ 188
.......................... 189
.................................. 189
.......
X

4X

191

..................................... 199
...................................... 199
.............................. 201

................................ 201

.................................. 202
.............................. 205
n .................................... 207
.................................. 207
.......................
208
..............................208
.................................. 209
..................................209
.................................. 210
.................................... 210
.......................... 210
.................................. 211
............................ 211
.................................. 212
.................................. 213
....................................213
....................................214
.................................... 215
.................................... 216
....................................217
.................................... 218
.................................... 218
......................
220
X 5X

................................. 220
................................. 221
................................. 222
.................................. 222
....................... 223
......................... 226
.............................. 226
.................................. 231
IC U .......................233
...................... 235
......................... 237
........................... 241
..................................... 241
................... 242
............................. 242
................................. 246
......... 247
....................... 247
....................... 255
......................... 258

. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 259

.............................263
........................ ..... 267
............................... 267
...................................... 267
...........................275

.............................. 293
........................................294
.................................... 295
.................................... 300
............. 305
............................ 308
.............................. 317
....................318
........................ 320
............................ 321

X 7X

pharmacology)

pharmacodynaijiics),.
pharmacokinetics) ,

Iinearmammillarymodel)

compartment)

1 ~ 2

 FW

1 - 1 )

1 - 1
X
Xp: X0:
ki2k2i k13k31:
k km :

X 3jX

passive transport)

simple diffusion)

p H Henderson _ Haseelbalch 0

HA= H + + A .

Ka (

log [H + ] =IogKa + log

pH = - log [H + ]
pH = pKa+ l

[HAJ
[A -]

pKa = - IogKa
o

(I )

5 0 %
1 ) pKa = pH .pKa
5 0 % pH

1 )
,nDH.BK, [A ~ l
[]
[HA ] []

(2)

,Q

gK a -P H

"

[BH + ]
[]
[B ] []

(3)

2)
3 ) PH PK a

p H p H
p K a
PK a

pKa ( 6 . 5 ) PH
9 0 % -

- COOH - NH3 COOH - NH3

filtration)

Jt = - kx"

G h
n = 1 = O

M = 1)
4 ) ;/= - AZ

Xt= X
e-h
X0

Xt

(5)

5 )

1
=1gZ- ^ ?

F = a + t o , i
6 = - A/2. 3026,
1A

6)
G Ij

 ~ PW

Iog^ 11 = IogX0 -

IogZl2= IogZ0

:
k =2. 3026

IogXi i - IogZl2

h ~h

k

k

fc
n = ), 4 ) / =
k

Xt=X0- kt
(7)
6 = - A , &
A = (Z q - Z ,) /

firstpasselim_
ination )

bioavailab ility)

F )
- area under the curve, AUC )

AUC ( P M )
X 100%
_ AUC ()

1 apparent volume of distribution. )
Vd) Xq)
C
Vd

(8)

X 9X

Vd V d
PK a
V d
70k g
40 ~46 L 3 - 5 L
13 ~ 16L 25 ~ 28L Vd = 5 L
10 ~20 L
4L 100~200 L
C

the central volume of distributionV c )

PK a
V c V c
V c V c

the peripheral volumes of distribution,

Vp ) : V c V p

(Ieanbodymass) V p
the volume of distribution at steady state,
Vdss) :

 JW

2 .

(1)

V d

9 9 % 9 8 % ,
1 % , 1 1

(2)

C
pKa =7.6,
70ml


awMwwgwnwtmwiwmtiWiniiiiniwniwiiumiiiviwwnwniwiiiiriwip wffiBigwmwww w--

. miiT 1 IOOg M ) lml min_1 IOOg

^ )

redistribution)

p H
7 5 %

(3)

(4 )
PH PH

p H
p H pH ( 7 . 0 )

 SW

pH =7.4 ) ,

_
( PKa =7. 3 ) 2

'(

--------

200
P - 4 5 0
P - 4 5 0
50 ~ 200 3 0
P - 4 5 0 - 2E P

- 4 5 0 - 2 E 1
P - 450 - 2 B
P -450 - 3 A
P - 45 0 6 0 %

enzyme induc
tion)
enzyme inhibition) ,

WM

muiM
B tmMMW-,

BUWIIMII WWWWMW MWWWiMm

N2O

clearance, CL )

systemic clearance, CLs)

$ ml . mhT 1,
CLs = CLw + CLl f + CLj^ ;
C is = h . h CL, = K . &
elimination half - life )
terminal half - life )

(context-sensitive half - time)

5 0 %

5 0 %
200min ,
5 0 % 55min25min

 SW

1 Z
(J)
( 1 ) - g = - kt ,
k : Z ,= Z fje_kt

(9)
( 2 ) - Vd

C1= C0e~h

(10)

1 0 )

IgC1 = IgC0 -^3026*

(11)

C ,- i lgC
- A/2. 3026
( 3 ) h alf - lifetim e T 172) :
f = ?V 2, C , = C
/ 2
7^ 2 =0.693/
:T1/2
1) < = ^ \ /2 A =0.693/7\/2:
Cn/2 = C0 ()" = 1 Cn/2 =0.5 C0; n = 3.32
C3.32r1/2 =
. lC ; w = 5 C5T1IZ2 = 0.03Co; n = 6.64
Q 64n^2 =.i c

2.

(1 ) -
,dXr

(Ki2+ K i0) .Xc

'dXD
^ =k^XC~ hixP

\ M / d,
A12
b

.
(21 ) - B t
a -p
a
Y

^21 )

a p

-C t

( 12 )

 Jii

(2)

-1 2 )

K )
r - X0
- kn )c-O1 X0 (^21 - ^ ) -
Ct~ Vc (a -l3) e + Vc (a -P ) 6

/I3 -V
( }

f i U 3 )

C1^Ae-a,+ B

(14)

C, t
( 3 ) a += 1() + A:12 + A:21; a = i 10 . Ar21;
C0 ( = 4 + B ; Fe ( =

I ;i f f
^

; = +

=JUC = V^ K^

(
= 5^ ;

(.

Tu2,
=

K .k10
/?

1. X )
t )
( 1 ) -/cfe= /?- fee, 7?
A:
X, = lk (1 ' e"fa)

(15)

( 2 ) -1 5 ) R :

(1 - e"b)
(16)
1 6 ) C, t eo
, Css)
Ct =^ h

C j !

Vd

( 1 7 )

1 7 )

&
Css,
1 7 ) 16.)C,= Css

(18)

= r 1/2, 1 8 ) n = l IJ

1 1/2

Q 1/2 = 5 CJS; = 4 , IJ C47v2 =0 93 CSS; n = 5 UC53^2 =

0. 97 C , 5 r 1/2
2

k '
k 21

R
Xc

Y
7S

( 1 ) -:
- K + Ki^p- (^12+^1) Xc
\d X B

\~dT =

- k^xP

:
Xc=

^ lO

10

-a t

(19)

 ~ PW

( 2 ) -1 9 )
K )
-Ak
R0
^lO
e)
( 20 )
Ct
(1 --- e
OL
P
K ^io
-P

R0
" = 55

2 1 ) /?

21 )

( 3 ) -
R0 (k2l - a) (e-aT- l)
R()8 -^ 21) (e
- I)
Ct
Vc ( a - . a
Vc ( a - / 3 ) . P
-1

( 22 )

71: y

Sheiner 1979

5 0 % r i/2^ =0 693/Ae
L

L 4 S C
T1172fc
12 5min

0.691^1^1, r 1/2fc

lm in , 9 0
3 7 % L 0. WmirT 17\/2fc

4 min5 ~ 6 m in
2 0 %

L
L r 1/2fc

(L
. ^ ^ ^ I
/&

TV2fc
4 min,
5 ~ 7 min
L

computer-assisted continuos infusionCACI ) CA C I

closed - loop)
open - loop)

 ~ 5W

C A C I CACI

1968 Kriiger - Thiemer

X
X =Cpss K LBM)
Cpss, & = Z
U 10+ h e +

) C pss LBM
Cpss ,

1985
C A C I
Kriiger - Thiemer C/ws:
U =
. K . LBM ( mg,

C ) = C/m & . Aiq . LBM

( mg/ ml)

F ) = I +
J tI

10

ml )

*2 w p o
h ) = l + _ e - mg/ A t A t = 3 ~ 1 5 s )
10
LBM : (Lean Body Mass
LBM ( =0.407 B W +26.7 -19.2
LBM ( =0.252 B W +47.3//-48.3B W = kg )

\23 O

!! ^)

Kt =Cpss & Kw (1 +

) -C, = Cpss (1 - e

lA C p ss5 Cpss
r 1/2^ > > : r1/2a
Cp ss Kriiger- Thiemer

CACI

the percent performance error, PE% )

3% (50 ~ 60) % PE% =
[( - / ] X 1 0 0 %
TK ( the median absolute value of percent performance error, MAVPE )

I
action)
effect)
A
A

selectivity)

/3,
/S1

a d v e r s e r e a c t i o n )

side reaction) :

residual effect) :

toxic reaction) :

allergic reaction) :

. anaphylactoid reaction) :
#

(C 3,

IgM IgG)

 IW

idiosyncratic reaction) :

S -
-
-

potency) :
0
10 . 5
15 ~ 1 0
IOmg , lOOmg
maximal efficacy) :

slope) : -

variation) : ,

ED5q)
LD5q)
(therapeutic index, TI ) LD5q ED
TI = LD50/
ED5e,

T I LD5
/
ED5c-
-
ED95 LD5, ED95 9 5 %
LD5 5 %
ED9j LD5 = LD5/ ED95

-
a 0

1 .

( receptor)

1906 Langley

receptive substance) ,

1914 Dale Ach )

M) N ) 1913 Clark -

M
( N ( N1
N2
M M1M2M3M4M5

7 0
N 19821992 ~ 1995
8

ligand)

(
P
3
( down regulation) ; (3
up regulation)

P2

a 2
CX2
o r p h a n receptor)

2
IE

( 1 )

 SW

1)

7 - GABAa )
5
2) G G GTP
GTP GTP _

5
G
3)

4)
DNA

( 2 )

1 )
GABAa

G cGTP
C cAMP DAG ) 14 5
IP3) cAMP
cGMPDAG IP3

Na +)
GABAa C r

2)
G

'
G 3
a P 7 a G TP
GTP p 7 G
a G Gs )
A C ) G G i )
A C ,
G 3 a p 7 ),
a G D P a p 7 . GDP
R ) H ) RH ) ,
GDP RH . 7 Mg2+
G TP GDP
R P"/ a G T P
A C cAM P cAMP
cAMP
G
cGMP C
3)

4)
D

 SW

D N A

3 .
( 1 ) 2 0 Clark

2 0
5 0 Ariens

agonist)
antagonist)
partial agonist)
Stephenson

2 0 8 0 inverse agonist)
carboline

( 2 )

competitive antagonist)

PA2
A ) 2

PA2 p A 2
PA2
K 1)
PA2 K 1
noncompetitive antagonist)

PD2'

PA2

1 )
2 )

3 )
4 )

5 )

6 )
7 )

8 )
9 )
1 0 ) 1 1 )
1 2 ) 1 3 )
M ) 15)
1 6 ) 1 7 )

2 - 1
2-1________

74. 1 197.4 165. 0. 184.5 184.5 200

168 44.0

U 34.6

20T
59.'1
kPa
' 442
(
)
20t (kj
27.6
- mol-1)
m m H g

50.2 104.7 56.5

48.5

58.5

23.5 -88.0

32. 1

3.0

23.3

31.8

20.9

89.3

5200

241

22.5

175

240

156.9

670

39000

28.9

33.9

32.3

7.90

18.2

1.45

6.702

g 0.72 1.86 1.43 1.52 1.50 1.25

ml ~ 1)
Antome A
6. 151 5. 892 6.206 6. 112 4.822
(kPa)
B
L109.58 L043.70L336. 58L107. 84536. 46
G
233.2 218.3 213.5 213. 1 HLO

m l
233
(ml)

227

208

198

196

1.92

0.77

0. 16

1.68

1. 15

MAC

1.71

912. 90
285.3

7.25 105.0

1 mole,

6. 023 XIO23 Avogadre

0 1
I mole 22.4 L

22. 4 L/ mole 2 0 Im l
227m l
I x l . 86 g

I. 86

T 97.4

mole

_ I X I .86
293
: 22. 4 X ^ 4 it r e s
= T 97. 4
= 227ml
20)
I.

8 6 197.4

2 - 1, 1. 5 %
2 L/ m in I h 9. I ml

= mL) X
'x min) + m l

2 x 1000 x 0.015 X 60
=0. 09ml
198

IfiI/ / //

Ostwald)

(Henry)
V 38 P

X)
2 - 2

X

2 - 2

/
\
/

37 B

/ / / / / / /

0.45

1.3

18.7

1.4

0.47

I. 1

1.4

0.8

0.65

1.7

55

1.8

1.4

1.6

98

1.8

1.4

2.5

2.0

27

1.2

2.3

1.2

3. 1

48

1.8

1.2

2.9

45

98

2. 1

1.7

36

1.9

224

2. 1

1.2

3.4

51

12

2.0

65

1.9

0.9

1.3

13

1.4

970

2.0

0.9

1.6

38

0. 1

0. 115 0. 13 1.85

1.0

1.

N2O 700
2.

300

\ 39 O

/
0.47)
/ 13),

/2 - 3

2 -3
/
20 ~25 )
/ /
300

6.6

58

74

120

120

190

26

62

110

630

L2

118

3 .
2 - 4 )

/
MAC

^ 40 Jp

/
/

2-4
]
/

IO0C
20C
(% 0C )
(% 0C )

9.3

-4. 18

2108

-4.58

3.4

-3.94

1570

-4.53

7.7

-3.76

881

-4. 54

1.6

-4.01

469

-4.36

1.4

-3.22

180

-3.51

30.5

-4.89

117

-3. 39

0.3

-2. 11

16.7

-2. 18

0.7

-2.33

1.7

-1. 13

1.

2
;

C
1
C

2 - 1 201
Antoine

I o g (P )
A B C C 273. 15 (^

K)

C A B Rodgers
HiIl 1978 Antoine

latent heat of vaporization)

N2O
N2O

36. 5 T ) ,

N2O

minimum alveolar concentration, MAC )

5 0 %
1 MACM A C 4

MAC ; M AC

M AC
- ED5fl

M A C 0 . 5
M AC I .0 MAC
M AC

MAC

MAC/
MAC

M A C
MAC -

X Y Y Z ,
/K

-
m a c
MAC
-
M AC
MACawake5fl) , M AC
5 0 % m a c a&1^95 9 5 %
MACawake =0.4 MAC
MACawake MAC 0 4 MAC EI5fl
5 0 %

MAC EI95
9 5 %
MAC 3 0 % MAC BAR

M A C M ACBAR m
5 0 %

MAC BAR95 9 5 %
M A C 2 - 5 9 5 %
AD95) 9 9 % ED99): M A C
AD95S 9 5 %
095 ED99
AD9^ ED99 I .3 MAC0 65M AC
MAC (SubM AC )
N2O
MAC ( superM AC ) : M A C 2
MAC ,

MAC
MAC
2 -5
MACMACMAC BAR

AD9J

MAC50

1.0 MAC (0.7 0.03%) 1.0 MAC (1.68 0.04%)

MAC EI50

1.3 MAC

1.4 MAC

MAC BAR50

1.5 MAC

1.6 MAC

MAC95

1.2 MAC

I .I MAC

MAC EI95

1.7 MAC

1.9 MAC

MAC BAR95

2. I MAC

2. 6 MAC

M A C A D 9^

2 - 6 5 0 %

M A C awak

0. 37 % ; 0. 84% ; 50 H z 1. 0 3 % ;
1. % ; 1. 16% ; 1. 7 6 %

M A C

2 -6
MACAD9^ MACawik

0.65 MAC LOMAC

MACawake

AD95

2 MAC

0.48

0.75

0. 30

1.00

1.50

1.09

1.68

0. 67

2. 20

3. 36

0.75

1. 16

0.46

1.51

2.32

0. 10

0. 16

0. 06

0. 20

0. 32

65.00

101.00

41.00

131.00

202

I .11

171

0. 68

2. 22

3.42

A C

( ) M A C
(I ) P a C O 2 >90 mmHg P a C O 2 < 10 mmHg (
2)
Pa2 < 4mmHg (
3 )
4)
1 0 % <4.3 m l / d l = (

5 ) 5mmH g
6 ) ;
(7 ),

8 )
9 )
\ 46

( 1 0 ) 1 1 ) 1 2 )
I 3 ) U 4 ) Ct2 -

( M A C
M A C 4 2 M A C

Na +
M AC 3 0 % ~ 5 0 % ;

( M A C

h

PaCO2 10 ~ 90 mmHg PaO2 40 ~ 500 mmHg

M A C
M AC

I .5 ~ 2. 0 MAC ,

MAC'

M AC / X (/g ) MAC
. X (/g ) 2_7 , M AC

2 - 7 MAC

MAC (%)

X (f/g)

MAC \ (/g)

0. 16

970

155

0. 17

394

67

0.75

224

168

1.68

98

165

1.92

65

125

9.2

-11.2

109

71

2.8

199

105

1.4

147

SF6

490

0.29

142

CYP2E 1
CYP2 E 1 P45

+ROH ROR

RH ()

P45q,
P
II (NADPH)

R P45Fe3+ )
- - Fe3+ N AD PIT
P45
NADPH Fe2+;
- -
Fe3+ ; NADPH P45

R0 H , P45

2N2O

4 h

2
2 9 %

3 . 2
A - B A + . B 2
heterolysis)

J
E
E

4 covalent bind
ing)

2 8 15.0% ~ 2 0 . 0 % )

2-8

2. 1 -3.6

15.0-20.0

4.5 -5.0

12. 1-15.4

Br- , Cl
F - )

10. 6 ~ 23. 2

F -

7.4-44.0

F
F -

2.4-2.9

F -F -

0. 17 0.20

F -F -

3.0

F -F -

0. 1

B 12 N2)N2O
N2 N2O
N2O

N2O N2O
Bt2 B

14C

9
~ 1 2

(
12% ~ 2% 2
Cohen

4 % CO2, 11. 6 %
2 9 %

700 ~ 1000
CF3COONa)

(
82. 7 % 2. 4 %
7 h
2.5 % ~ 1 0 %

M A C . h e
2.7 M A C . h
D p o l / L , 9.6 MAC h 34_
]/[

6 0 % ~

K t

8 0 %

1. 2 % 4
h

l A p j n o l / L 2 4 h

h e x a flu o r o is o p r o p y l a l c o h o l ) C O 2
F _

48 h

I h 22. 1 6. O jx m 0I/
L
1/20,

(
i
F -
4 h

a -

( )
1.

2.

4.

5.

HPV)
6.

ICU

5h

(
1 .

M
2

fluothane, halothane) 1951

Suckling1956 Raventos
1956 Johnston

[]
'(

PaCO2 CO2

7
SGOT)


^~(afssws*x.-wtwMwmiWiwmiiwmiWiwih

3
(

(
ADH ACTH

2 .

3 .
(1)
.

B ain F
0 5 % 1% 5 0 % ~ 6 0 %

5 0 % ~ 6 5 %

(2)

enflurane, ethrane. ) TerreIl 1963
Krantz1966 Virtue

3 % ~ 3. 5 %

PaCO2 PaCO2
PaCO2
3 %
PaCO2

3 % 5 0 %

1978 Smith
/
3. 3 ,
3 . 0 )
IM A C
2 M AC
PaCO2 PaCO2

9 0 /
6 5 /

1 1.5M AC
30. 0 % 3. 3 % 38. 3 % 4.0 % , I .5 M AC
2 MAC

1.25M A C
5 0 % 10. Qpg/ kg ,
I . 25M AC 2. l ^ g/ kg
(

1978 Wolfson
/

PaCO2 1966 Virtue

IMAC PaC0 2 S 8.13kPa (61mmHg) ;
1.5M AC 10.13kPa (76mmHg) ; 2 MAC

1. 0 % 8. 3 %
2 % 1 4 %

1978
Stacey

6Om iri
3 7 %
1 4 %

,
1 / 2 5 0 0 0 0
(

2 0 % 25 % 23 % , 2h

22.2jjLmol/ L
50~8( Vmol/ L )

180|xm]/L 2 15|xmol/ L

(
0 5 MAC
1.5MAC
74 %

L 25
M AC

1 /2

(
XtACTH
AD H

1.

2.

PaCO2

3 .
( 1 )

(2)

2
(3)

isoflurane, forane) Terrell 1965
KmntzRudo Dobkin
1975 Dobkin, BylesStevens Eger

Corbett
1978 Eger

(
/1.48,
M AC 31
~55 1. 15% ; 20 ~ 30 1.28% ; 55 1. 0 5 %
7%0 5 0 % 0. 5 6 % 0. 37% .

7 ~ 11 min)
(
IM A C
IM A C
1 .5 M A C 2 M A C
PaCO2
0 . 6 ~ I . I M A C
1 . 6 M AC
PaCO2

5.7,
3.3)
3.0)2 M AC
MAC

1. 5 M AC
5 0 % 3
Homi PaCO2 70 mmHg,

(

PaCO2 PaCO2 Flemming

I . IM AC CO2
8 5 % 6 8 %
\ 67

2 MAC

PaO2
0. IM AC
I . IM AC

SGOTSGP T LDH)
(

2 MAC ED5
1.6mg/ m2,

ED90SSm gZ m 2, 1/3 ~ 1/20

[]
1.

ICU
2.

(
5 ~10 min,
5 0 % ,
2 M A C 5 0 %
7 0 % N2O
1. 1 % 1. 7 % ,
2. 2 % 3. 4 %

1 .3 M A C

nitrous oxide) 1779 Priestley

1779 Davy 1844 W ells

(
3 0 % ~ 5 0 %
8 0 % M AC 105
7 5 %
.5 % ~ 1. 0 %
6 6 %
3.56kPa (26.7 mmHg)

2 % 6 0 % 2
(

a -
(

( )
3 ~ 4

5 0 % 4 8 h
(

3h

Shaffer 3 ~ 5 min (
PaO2
9. 2 kPa ( 6 9 mmHg) 7 . 2 kPa ( 5 4 mmHg) , PaCO2
5 . 6 kPa (42 mmHg)

6 _ 6 7 kPa ( 5 0 mmHg)

5 ~ 10 min

1 .

2 .

3 .

5 0 % ~ 6 6 % , 4 0 % 3 0 %

5 0 %

sevoflurane) 1968 Regan 1971
Wallin 1975
1976 Holaday1984
19861990

[]
FCH2OCH ( CF3)2
- - /
0.63

200. 0 5 , 58. 6 T , 20 T
20.92kPa ( l 56.9mmHg)
1 1 % 1 0 %

P1
P5): P1
P2 P3
P4 P5

40 T P1,

45 t
P3

(
4 % 2 min

1 % IOm in

(
0.9% ~ 7 % ( 0.4 ~ 3. 0 MAC)

2 % ( 1.2MAC) 4 % ( 2.4MAC)
4 % ( 2.4 MAC)
1.5% (2 MAC)
2 % ~ 3 % PaCO2 6.67kPa
(50mmHg) ) 1 1 % 2 % ~ 4%
PaCO2 15% ,
V

3JP

1 0 %
5 % 2 % ~ 3 % PaCO2
6.67kPa (50mmHg) ) , PaCO2
1 . 5 % 2 %

5 % ( 2 MAC)
1.8%~3.15%( 0.8~1.31\^()

9. 7 , 3 4 ,
1.3M AC ADE (arrhythmogenic dose
of epinephrine)
1.25M AC AD E
2 M AC

CO2 PaCO2
1_ IM A C
L 4M A C PaCO2 7.33kPa
(55 mmHg)

GOT
1 2 %
1 0 0 % 88. 5 %
86. 8 % , 1 4 %
95. 7 % 57. 1 % 42. 3 %

ED50, 1.6

> >
>
(

1 % 0 . 5 % 3h
1 . 4 % 4 h
26.3 0.8 11.5 1.8
1/3 ~ 3 / 4
48h 4
Cook
IOh, i ~ 3 h
ADH

1 .

2.

3 .
- - -
10 ~ 2m in

4 5
f

1959 1966 Terrell 7 0 0
635 desflurane)
1

1988 9
1990 Jones

M AC

PaCO2 0 8 M AC I .2 M A C

1 .2 M A C 2 h
4 . 7 3.0 min,
14. 2 8. lm i n 23. 2 7. 6 min,

47. 2 4. 7 min

(
PaCO2

0.83MAC)
1.24 1.66MAC )
L 66M AC
ventricular ejection
fraction)

M AC
1.66 M A C / O2 ,
L 7 4 M A C /
7 h 90 min

PCWP)
(
PaCO2
PaCO2

(
Jones 1 0 3_ 6 % 89 min

4 h M h 72 h 1 9
7 -

(
24h 72h
RBP (Retinil - binding protein) NAG
((3 - N - acetyl - D - glucose - aminidase)
N AG
R B P
(

Koblin

D Jones
1.2MAC
lh , 24h

[]
1 .

2.

3..

6 0 % 4 ~8 mg/k g
4:6 0

3 fjug/ kg , - MAC
2 0 %
0. 05 mg/ k g MAC 6. 0 0. 3 4. 7

_ 3 2. 3 % 3. 0 % 6 0 % O2;

Xenon) 1951 Culen

X e , 131. 2 ,
4 -111. 9 -108.1 T
/0.085 (37 ) ~0. 095 ( 2 5 ) /
0.115/1.8 ~ 1.9 (37T ) ,
MAC 0.71

99. 9 9 5 % 7 0 % 30%'
.5L/ min) 2 h
< 2 0 % , 8 0 %

1864 von Baeyer 1903

Fischer von Mering
diethylbarbituricacid)

1932 Weese
Scharpff sodium hexobarbital)

( sodiumpentothal) 1934 Water Lundy

2 0 5 0

2 0 6 0

propanidid
1956 sodium hydroxybutyrate 1962
1^1^1; 1965 61
111^6 197 2
propofol 1977

1 0

- Jif

1~4
amytal4 ~ 6
luminal 6 ~ 8
4~5
t 1/2)
9 5 %
t 1/26

5 1 2
5

6 % ( W/ W )
\83 O

o .9 % 2. 5 % 2 %
1 %
pH10~ 1 1 ) ,
,

3 0
thiopental,sodium
thiopentone sodium, Pentothal sodium) ,
1 - [ 5 - 1 ^ 1 - 5 - ( 1 methylbutyl) - 2 -thiobarbituricsodiu ],
2.5% ~ 5 %
p H 10.6-10. 8 2. 8 %
CO2
24 ~48 1
pH
(
7 - 7 - aminobutyricacidGABA )
G ABA
5
G A B A
.G A BA

GABA
ligand - gated chloride ion
channels) G A B A
G A B A

 &

G A B A
G A B A
G ABA
(

- 1 0

1 5 5 % (9 0 % ) 6 %
2 8 %
5 % 1 2 %

5 %
1 8 % ,
7 5 % ~ 8 0 % 8 0 %

5 21/1, 3 0
9 6 %

2.5 ~6
8 6 0 %
4 %

477 ~600 mg/ k g

context sensitive half- time, t1/2es) 16 ~ 30
6 ~ 10
7 2 % ~ 8 6 %

sulafurazole)

inwiwiawi iiiiiwwiiWMi_Miiwii a

wan

2 8 %
5 3 % 5 5 %

3
9

5. 9 6. 3 fjLg/ m l
pH
pH
pH

PH7_ 4
6 1 %
pKa7.6 PH

a - W - W - O M w wMtg MmMlWiiiiriiiiwiwinnwwwwMiiiwwiwipwKwn,

0 . 3 % )

0.08 ~. 20,
I .6 ~4. 3ml/ kg/ min
5 ,
thiopental carboxylic acid) ,

1 0 % 1 5 % 11. 6

2
8 2 4
6 7

VdssC l t 1/2

1/2

27. 8
(6. 3
(

'

15 ~30 1 15 ~
2 0 3 ~5
a S 0
4 8
cerebral metabolic rate of oxygen CMRO2)

55% )
4 8 % ,
5 0 %
3 ~7

bispectral index, BIS )

5 5
5 0 %
11. 3 juLg/nd 5 0 %
15.6jjug/ ml5 0 % 33.9pg/ ml,
5 0 % 30. 3 |xg/ ml,
39.
5 0 %
50.
ml

78. S fig/

3 0

 #
bh -JtwwaHwwaiwwaattMBaMgMiwwMiTOMMuimwMi-HwiiiMIIIIiifninioimriiiwn w w iw tw w

ii iM W w

ryanodine)

2 5 %

1.25% ~ 2 %

6 mg/ kg , SmgZkg

5. 6 mg/k g

P - 4 5 0

[]

4 0 %

3 4
2. 5 %

tolazoline) ,

porphyria)

S -
A L A A L A

1 .
- 1

5 ~ 8
2.5 ~ 4. 5mg/kg
5 ~ 6 m&/kg
SlXgZkg,
ED504 mg/ k g 2. 2 mg/ kg ,

2. 5 %
5^n l

2 .

50
~ IOOmg,

3 .

4 .

N O-cGM P system)
40 mg/ kg
30mg/
k g

1 .
2 .
3.
4 . 7 -
5 .
6 .
7.
8 .
9 .

10.

1 9 5 8 Greifenstein
P
p h en cyclid in e),
2 5 %

1962 .Stevens ketamine, 'ketalarKetaje c t ) , 1 9 6 5 Corssen Damino

1 9 7 0

(
2 - - 2 -
238 kd

pH 3.5 ~ 5.5, PKa7. 5 1:10 OOO

benzethonium chloride) 10mg/m l

5 ~ 10
1 5

12% ~ 4 7 % ) ,
6.5:1 (

1 0 7%

45
12
2. 5
2_ 8 VDss) 3. lL / kg
11 ~ 1 6
12 ~
17111/1^1^11 1.4^1^11

P - 4 5 0 N
_ norketamine,. I )

 a x

dehydronorketamine,
n )
I
1/5 ~ 1/3 ; n 1 %
f
5 9 1 % ,
4 % I 1 6 %
3 %

(diazepam)
secobarbitibsodium)
=
I

(SKF525 - A )

2 mg/ kg ,

P K a p H
3 0
1 2 m g/kg
10 ~ 1 5 0.5 mg/
kg lm g / k g 5.7 1.5
mg/kg 9. 1 2 mg/kg 10

15 ~ 3 0
5 ~ 1

.2 ~ 0 4 mg/ kg , 0. ljxg/m l
.2jxg/ml L l fjugAnl

2 mg/kg , 0.7 ~
2.2(xg/ ml, 3. 6|xg/m l

SfJLgAnl,

dissociative anesthesia)

 &

CX
s e

N - - D -
(NMDA) NMDA

S - ( + ) P -

Wide dynamic range neuronal activity)

CMRO2) 0

CO2
PaCO2
1 5
3 0

3.4
1.5

2 0 % ~ 3 0 % 5 ~ 15

_lmg/ k g
3. 3kPa (25mmHg) , 2.13kPa (16mmHg)
0.5mg/ k g
3 ~5

NMDA

e t

1 2
3 ~5
>
^

CO2
PaCO2

carbachol)

e w

5 % ~45%)

5 ~ 1 5

15 ~ 3 0

Iorazepam)

.5~2mg/ kg 4 ~ 6 mg/ kg ,

0.5 ~ lmg/ kg
5 2 0

I mg (0.05 mg
3 ~ 10 mg/ k g 2 0 45
lOmg /k g 87%
25 mg50 mg 25 mg
1 ~ 3 300 mg,

chlorobutanol)

disoprofol, diprivan, propofol) ,

ICU
27

977 K e y Rolly

(
2, 6 -
2 6 - di-isopropyl
phenol)

cremophor
EL ) ,
1 % W/ V )1 0 % W/
V )2. 2 5 % W/ V ) 1 . 2 % W/ V )

0 . 0 0 5 % disodium edetate)
PH7 . 0

5 % 2 5 1

2 mg/ kg 2 ~ 5 | xg/ ml,

2~8
1~3

1 ~ 8 30 ~ 74 ~ 23. 5

.
4 ~ 7 20 ~ 30ml/ kg/min ,

2 0 ~ 4 0 L , VDSS) 2 ~ 1 0 L/kg

context sensitive h alf - time)

8 4 0

5 0 %

t 1/2(3 35 ~ 4 5

9 2
'

3
3

2 2 %

0.1
9 5 %

1 % 2 %

P - 4 5 0

2. 5 tng/ kg ,
1 - 90 ~ 100

2 ~2. 5 mg/ k g 5 ~
1
ED5a) I ~ 1 .5 mg/kg
9 5 % ED95) 2
2.88 mg/ kg 6 0
2 mg/kg , 1 2. 25 mg/ kg 60
I .6 mg/ k g
I. 5 mg/ kg 0

2 mg/ kg/h ^ g A n l

2. 5 mg/ kg , S c t f
7 0
3 - Spg / m l

BIS)
B IS 9 0
B IS
BIS 6 3 5 1 5 % 9 5 %

B IS 7 7 9 5 % B IS
9 5 %

BIS 5 0

BIS
BIS

30 %

30%
~ 5 0 % )

CO2

3 0 % ~ 4 %

SpO2)

25 % ~ 3 0 %
3 0

2
4 5

l
(W k g / m in
2 %4 %
CO2
CO2
PaCO2 PaO2

2 ~2.5 mg/ kg
25 % ~ 4 %

2 % ~ 3 0 % HKVg/ kg/ m in
3 0 %
5 4 108jjLg/ kg/
min

lOS^ g/ kg/ min,

1 0 %

S X

ACTH

[]

IOmg

KKVg
5 mg, 1.5mg/ kg

20 ~40 m g

ethylenediamine.tetraacetic
acid , EDTA )
(

( l ~2.5 mg/ kg
9 5 % ED95) 2.25 ~2.5 mg/kg
6 0
I mg/ kg 1.75 mg/ kg
ED95S 2 3 mg/kg

10 ~ 40 m g
100~20(V g / kg/min,

50~150^
/|{8/11^,
3 pg/kg , 0.2^ g/kg/tnin

I C U
30|x g /k g /m i n

2 4 9 6 ^

1964 e t o m i d a t e , a m i d a t e h y p n o m i d a t e ,
1972

(
R - ( + ) -
- 1 ( 1 - - H - - 5 -
342.36 k d ,
2 4
3 5 %
0 . 2 % l O i n l 2m g /m l
p H 6. 9

[R ( + ) ] [S ( - ) ]
[S ( - ) ]

.3 mg/ kg , ,

2. 7 2 9
2.9 ~ 5. 3 18 ~
25ml/ kg/ min 0.5~0.9

VDss) 2. 2 ~ 4.5L /kg

76. 5 %

R ) - ( + ) - 1 - ( 1 - - I H -
- 5
7

2 % ~3%

 &

8 5 % 1 3 %

'
(

- W/ W
1 2
4 ~ 5

0. 25mg/ kg ,
0.3 mg/ kg 0.1 ~ 0.4
mg/ kg ) 7 M

300 ~50(V g /ml , 150
~30(V g / rnl150~25(V g / ml
G A B A
GABA -
3 4 %
CMRO2) 45 %
/
5 0 %

(X
P S - e 5

0.3mg/ kg

dp/dt max
3

0.3mg/ k g

2% ,

<

4 5
3 0 %

S #

3 0

CO2
CO2
CO2

ICU

11 - P - 11 -
1 7 - Ct-
1 1 - 1 7 -
( A C T H ) 11 - P -
I 7 - a -
P - 4 5 0

( C ) P - 4 5 0
11 - P - 11 -
C ,

0_ 3 mg/ k g
3 0% ~ 6 0 % 5

10% ~65.5%

S # #

~ -menmmemmmiammmnmaminmmmammmmmmimmmmmmmmmmmmmmmmmmmmmmmmmmmmmm

3 0 % ~ 4 0 % ,

10% ~ 50%

.3 m g / k g 1 3 % ,
0. 9mg/kg 37 % 1 4 2 4 %

(
'

0 5
/)526.44.6

0. 2 ~0. 6 mg/ kg
. 3 mg/
kg , 0.1 mg/k g
1006.5 mg/ k g 4
lOjxg/ kg/ min, N2O

.
5~8|xg/kg/min ,

porphyria)
5 -
ALAS )
8 5 % 4 0 %

7 -
7
- 7 -

Laborit 1960

(
7 _.
sodiumhydroxybutyrate) ,
7 - OH ,
2 5 %
pH 8. 5 ~ 9. 5 ,
CH2OH - CH2CH2 - COONa , 129. 06
{
7 - O H 1 5 6 0
80% ~
9 0 % CO2 4 ~ 5
P

S S X

CO2
(
3 ~ 5 1 0 20
~ 3 0 60 ~ 9 0 4
~ 5

7 - OH

CO2

7 - O H

7 - OH
T U
10 ~ 2 0 20 ~ 4 0
6 0

OH

7-1111)505 101118/1^
I 855mg/ kg I 940mg/ kg
601
/1^ 1^5
3%,

(
- O H

5 0 ~ 8 0 mg/ kg lOOmg/ kg
2 ~ 5 g , 2 5 %
1 ~2 I ~ 2 g

(

(hydroxydione)
althesin)
alphaxalone) alphadolone)

minaxolcme,
1 5

(pregnanolone) 2 0 8 0
eltanolone) ,
3a - - 5 p - - 2 0 -
5 P - 1 0 %
pH7_ 5
1 ~ 2
l ~ 3 L/ kg/ h ,

0. 5 ~ I .Omg/ kg
(
propanidid,
polyoxylated castor oil , Cremophor EL )
5

narcotic analgesics, narcotics) ,

opiates)

(opioids)

opium)
1803 Sertume r 1925
Gulland RobinsonE isleb Schailman
19391942

 TO

i n ni
phenanthrene) I
3 6 3
3 6
I

119 1 3 [CH2 CH2 - N ( CH3 ) - ] 7 -

- N -
N

1973 I
opioid receptors)

/f substantia gelatinosa) 1975

P -

(X K
S CT-
T -
JJL2

2 0 9 0 Evans Kieffer
5 K IX
DORK O R MOR

1996IUPHAR)

opioids) OP ; S 1992
OP1, 1993 1995
K k OP2 OP3

solitary tract)
locus coeruleus)

p H
G

1
2

3 .
phenylpiperidine derivatives)
morphinans)
( Ievorphan ) ; benzmorphans )

(pentazocine) ; diphenylmethanes )
(methadone)
(

1 . opioid agonists)

f i -

2 - opioid agonist - antagonits)

K a f i

3 opioid antagonists)
K 5

JJL -

sodium index)

IC5
IC5

5 0 %

0.25% ~ 0 . 5 % )

 W 1|!4 ?

(withdrawal syndrome) ,
-

G cAMP
G - cAM P
G - cAM P
G - cAM P
cAM P PKA )
P K A

anti - opioids).
cholecystokinin)

opioid agonists} Jjtl

morphine)
1 0 %

[]

(euphoria) a

 TO

S
Edinger - Westphal

area postrema)

PaCO2

lmg/ kg )

ADH ) ,
AD H
(

A C T H

15 ~30 45 ~90
4 2 0
3 0 % (23% ~ 3 6 % ) ,
3.2 ~3.7 L/
kg )
0 . 1 % ) -
-

 TO ?

6 0 % - 7 0 %
5 % ~10%6 3
glucuronides) ,
6 M - 6 - G ) 8 0 % ,

7 % ~ 1 0 % 1 0 %
2~4 M .7 ~ 1 8 ml/ (k g . min)

8 ~10 mg

lmg/ kg )

1
.papaveretum)
5 0 % 20m g
13. 3 mg

#
.

pethidine) phenoperidine)
phenylpiperidine)
(Dolantin) , 1 - - 4 - - 4 -
1 - (3 - -3 - 4 - -4 -

1/1050mg 50%;
125mg, , 15m g
1/2 ~ 3/4
50 ~ 10030 ~ 6 0
4 ~ 6

5 ~ 1 5
6 0 % , 3. 8 L/
kg
9 0 %

pH pH
5 % ; PH 5 2 5 %
10. 4 ~ 15. IAnl (kg . min)2. 4 ~ 4. 4
6 ~8
5 0 %

5 0 % 13 0.9ml/ (kg
min)193

I
NLA ) ,

fentanyl) Sublimaze, 1960

75 ~ 125
3 0

5 ~ 10
1 0

9 1 0

20 ~90

C
2 0 2

(LZkg) [ml/ (kg min)]

(%)

30
3.2-3.7
14. 7 ~ 18
2~3

60

3.8

10.4 ~ 15. I

2.4-4

84

4. 1

11. 6 ~ 13.3

4.2

92.5

1.7

12.7

2.5

92

0.86

6.4

1.2-1.5

70

0.39

41.2

9.5min

i f

8 %

n NLA
.

3 ~4

sufentanil) alfentanil)
1974 1976

5 ~ 10
2 1 / 4 ,
1/3

N - O -
1 %

1/10,
'

1 / 4 , 1/3 ~ 1/2
p K a 6. 8 ,
pH , PH7. 4 8 5 %
9 % ) -

1 %
10 ~
2(V g /k g 10~20
Hughes
--- context - sensitive half - time,
t l /2 C - S 5 0 %
4 t 1/2C_s
262. 5 58. 2 33. 9

remifentanil)
GI87084B ,
2 1

P
EC5 P ,
(
50 2.4 0.6 11111
1/[ (
501.8
0.4mn
l/ L ) EC50 20.1
1.2nmol/ L ) , EC500.3 0.09nmol/ L ) o
15 ~ 3 0

MAC 4 0
I .2(xg/L M A C 5 0 % 32^#

3 ~5
2 0 %

.39 L/ kg 4 L 2 ml/ (k g . min)

9. 5
4 t 1/M_s
3. 7

 TO

> 9 8 % )
(GR 929 1 ) , 1 . 1 % ) GR
94219) GR 90291 0. 1 % ~
0 . 3 % i

ED5 0.03|xg/ (kg . min)

ED50 O^ 2 tOjg/ ( k g . min)

5 m g
15mg 5m l

dihydroetorphine) '(oripavine)

[]

6 277 11 488

1 0
29. 2 % 2. Oiy
kg , 75ml/ (kg min) 27. 7

20
410 ~20 jjug15 ~20

5 10
3 ~4

2 ~ 3

( 0.82%) 12.5%
33. 3 %

-
- opioid agonist - antagonists)
<
(T IJL

pentazocine) Talwin) ,
benzmorpaps)
1/4 ~ 1 / 3 , 30 ~
4Omg lOmg2 0 3
(T

2 0 % 1 ~ 3 15 ~ 45
3 5 % ~ 6 4 %
3 L /kg -

5% ~ 2 5 %
2 % 2 3

butorphanol)

20 10 ~ 30 er
4 ~8
30 ~ 4 0
2m g 3 ~ 4
30~6( V g/kg

6 5 % ~
9 0 %
3.817 (k g . min)
2.5 ~ 3. 5
5 % ~ 1 7 %
4 8 % ~ 7 %
-

1530 ~ 6 0 6
481.8

l ~ 2 mgI m g ;

Img
3

nalbuphine)
(oxymorphne)
3
1/4
ceiling
effect) t r

3 0
60 % ~ 7 %

3 ~6
A

buprenorphine ) Temgesic

^
3 0
0.3m g lOmg jx
5 0 (X 7
~ 8 1 8 &

IX

1.5 ~ 2. 8L/kg 9 6 %
1/3
2/3 13
min)3

(kg

0_3m g
6 ~8

nalorphine) N - N - allylnormorphine) , Lorfan, N -
- CH2C H = CH2)

74%, 36%'

ro

Im g 3 ~ 4 mg

1 5 3 0
-9 0
3 ~ 4 1 ~4

IOmg 150|xg/ kg 1 0

JJL
K S

naloxone) N -
N-allyl
- noroxymorphone) Narcan

3 0

-
2 ~34 5
1 0 2. 5 ~3
3 0 -
4. 6
1/10

1.81L /kg 4 6 %

14~30 ml/ (k g _ min ) 30~78

0.3 ~

0.4mg150.6mg5 ^ #
(kg h )

P -
P -

4 ~. 6m g

'naltrexone) Trexan,
N

2 4
1 5 0 %
~ 6 0 % 2 0 % 16.lL /kg

4 ~ 10

7 ~
1

nalmefene) 6

(JLS K 6

1 6
1 2 2 8

.4 m g I .6m g
3 ~ 4

5m g 2 Im g 4 2m g 8

5 000
12 ~24 mg

I ~ 2 mg,

0.9 ~ 2 . 5
8. 2 ~ 8. 9 485
123 L 6 0 ~ 6 5 L /h
7 0 % ,
4% ~ 5 6 %
5 %

0 ZS^ g/kg (0 I pg/k g 2 ~ 5

 ra
-

wwwwri _nw _ w

1KS^ g
.5mg/7 kg 2 ~ 5
lmg/70kg 1.5mg/70kg

tramadol) , Tramal

fJL1/6000, K 8 -
A - 1/25
4 5 %

JJL
5 - 5 - ,
+ ) A

5 -
- )

1/10 20 ~ 3 0
<~6 1 ~2
5 ~ 6

5 0 %

5 ~ 1 0

1/10

9 0 % )
2 6 5 % ~ 6 8 %
9 0 % ~ 1 0 0 %
203L ( ~306 L (
2 0 %
8 5 % N - O O
- (JL
2009 0 %
5 ~6
1 5 0 %

50mg;

lOOmg2 ~3

flupirtine ) Katadolon

IX K S

5 0 %

9 0 %
.
2 0% - 3 6 %
2 ~3

lOOmg3

1884 Koller
Einhom 1905

fast
- track)

( .
- -

R3N ) , R2N ) ,
4 5
0.6 ~0. 9 mm

1 0

Ot - 5 0

(
Takman ( 1 9 7 5 )

B
.axoplasmic)
Q X - 3 14Q X -572Q X - 2 2 2

C
benzocaine) ,
( N - butanol)
D

R = N + H C l- R = NH+

(1)

R = NH +^ R = N h-H +
(

(2)

(
PK a )

,
,

[H
]
Ka =

[]
K a
3 ) :
pKa = pH - log []

[]

4 )
pH = = 1 ,
Iog = O, pKa = pH p H

pKa )
PK a 7.5 ~ 9.0 PH

4 )
log [ I = pKa pH

(5)
[]

5 ) PKa - pH > 0 )

pKa pH < 0 ) ,
p H

pH

CO2 PH

CO2

CO2

A B C A
B C C -
7 5 % ~ 8 0 % 9 5 %
2 ~22
Ranvier)

A
ct
57 S Aot
C
Wildsmith 1985
A B
C

A B C
A
C
C
A C
A
A c

pKa
A
C

P K a

,
Aa I .6mm3. 2mm ~
3.5mm

endoneuri
um),
perineuri
um) 15
> >

perilemma)

30 % ~ 7 5 %

Cm)


TtwmeaaWiiwKwmMWMMwmiMimwiiibiuiiuii

C m )

Cm)
C m
C m

Cm pH : p H
Cm , p H PH7. O
Cm , PH5. O 1/100

Cm

comformationalsteps) ,

flicking block)

(
'

Na + toni<?) phasic)
Na +

.2mmol/ L )
Na +40mmol/
L ) Na +
> 5 HZ (5Pul/ S ) Na +
(

pKa
Na +

1 )

2 )
allosteric antagonisms)
(

benzocaine)

Cm ; Cm

1 / 3 ,

C m

Cm
W innie

Cm
]

5 0 % PH

Cm , Cm ,
C m
Cm ,

Cm ;

1 5

Br0mage
1/4 ~ 1/3
1/4 ~ 1/3

PH4_ 0 ~ 6 . 0 ) ,
pH

pK a pK a 7.4

15 ~ 3 0

1 % 2 %
2 % 1 %
1 %

> >
> > -
400m g 7(JLg/ ml

SfigA n l ,

PH

5
1/3 ~1/2 4 %
8

2. 5 % 2. 5 %
EmIa,

45 ~ 6 0
45 ~ 120
120 ~300

Emla
(

1 5 %
3 0 %

3 3 % ,
2 2 % ,

1:200000
5 jJLg
1:80000,
a -

'
(

C
/

p K a

a -

lpg / m l 7 1 %
2(V g / m l 2 8 %

a -
I/2 0. 2 ~
0 . 4 , 0.5~0.6 0.6~0.70 . 3
0. 4 4 , 1.0-1. 18
1 0
/
(
pH

p H

pH

pH

sodiumpyrosulfate) pH

3 ~6
,
1 .
_44 ~0. 7717kg
-
>
1. 5 70k g lOOrng
2(V g / kg ,
700ml/ kg

2
-

3 . Vdss)
V dss

V dss I .32L/ kg ;
Vds s 0.88iy k g
C

5 0 %
V d ss 91L 133L

JwwaKjaiiMMiwwi
w o w "" Hnwi1IMiiw 1.. ...... ..

72L , Vds s
1


5 - 1 :
5 -1

tMa

t>27
(L)
(min)
(min)
(h)

(iymin)

261

0.5

5.0

1.5

2.84

91

1.0

9.6

1.6

0.95

84

0.7

7.2

1.9

0.78

72

2.7

28.0

3.5

0.47

133

2.2

19.0

2.6

1.22

22 ~ 268 0 61
~ 7 1 138

1. 5
5

=S
. 8mg/kg . h

pH

NADPH

1
PABA) DEAE)
PABA 2/3 DE
AE 1/3

-
MEGX) MEGX
N - MEGX
GX)0 G X
2 MEGX
GX MEGX
G X

PH , PK a
pH
MEGX ( PKa 8 . 1 )

N - MEGX24
3 1 : 1

3 7 ~
3 8 5 8 2 0 1 - 2 2 ,
8 3

ym in )
t 1 / 2 ) 11/2
5 71/2

0.95L/ min, 0.77L/min, 0.76L/

min,
3

2
1 5 jjLg/ ml)

( 4

Na +

Vmax)

use-dependent block)
Na +

P R QRS

C a ++

1 %

(
Cm

2% ~3% 20m l
p H pH3. 12 ~
3 . 1 6 )

(lOmg/kg ) , O -
(Hb ++ ) Hb3+), 3
~ 5 g / d l O2

1 5 mg/ kg )
2 mg/ kg )

50 ~ 100(xg/ m l

I
(

2 % ,

E (IgE ,

5 -

NHK ^ ~ eCK )H E
methylparaben)
phydroxybenzoate)

1 0

0.05ml)

1 5 3 0

(
,

4 - Gpg/ ml,
(

a
0 5

I.
CO2 PaCO2
PaCO2
PaCO2
1 ) CO2

2 ) CO2 pH

3)

itfc,

PaCO2
2. PH
3.

CD 12 (
5 0 %

CC/ CNS)
CC/ C N S 7. I I . 1 7

3. 7 0.55 4.4 0.9;

Vmax)
50 ~ IOObpm lp g / rnl Vmax
K W m l
150bpm
Vmax 5 ~ 6 Vm ax

P R Q R S

4:1) Q R S 1: 1 6 ,
Q R S 16 S A
A - V -

S S R
S R

^
S -
S - R
Na +

Ca2+
S -

bretylimn)

( - )

l ~ 2 mg/kg )

___ ___________________

0 lmg/ k g 5 ~
7 mg0
(

50 ~ IOOmg (2. 5 %
2 ~ 4 ml)
2.5 ~ 5. Omg
lmg/ kg )

(
Procaine, Novocaine, Planocaine )

45 ~ 6 0 PK a

p H

0.25% ~0. 5% ~ 1 . 0 %
1 . 5 % ~2_0%
I g 3% ~ 5 %
15mg,
M 1: 200000 ~ 300000
1. 0 % ~2. 0 %
( Tetracaine Pontocaine PamocineAmethocaineDicaine )

10
~15 3
10 10
2/3

1 %
2 % 0.2% ~

0 . 3 % 40 ~ 6 0 mg
_1% ~.2%
1. % ~ 1. 5 %
IOmg;
1 % Im l , 1:1:1
8 ~ IOmg ( 2.5 ~ 3. Oml),
120 ~ 180
(
2 - Chloroprocaine, 2 Chloroprocaine, Nesacaine)

4 6 ~ 1 2 30 ~ 60

1 %
?800mg
3 0 2 % ~ 3 %

pH =3. 3 ,

( LidocaineLignocaineXylocaine Xylotox)

0 . 5 % 1 %

4 %; 2%1

4 %
2 % 200mg, 5
15 ~ 3 0 0 5 % ~ 1. 0 %
60 ~ 120
1 % ~ 1 . 5 % 10 ~ 2 0 120 ~
2401 % 2 %
5. 0 I .0 16.2 2. 6
90 ~ 1202 % ~ 5 %
40 ~ IOOmg, 60 ~ 9 0

400mg,
500mg400mg
2 ~ 4 8/1111 5^
/1111;
7^ g/m l
( BMepivacaine
Carbocaine)

1 % ~ 6 %
pK a pH

5 0 % /

65 ~0. 7 0 ,

1 % ~ 2 % 1:200000
6. 2 17. 5 ,
2 0 %
( Bupivacaine Marcaine)

pipecolylxylidine, PPX ) , 1/8P P X

t 1/2p ) 8
9
2 ~3 ,
2 5 %

0.25% ~ 0 . 7 5 %
150mg, 225mg JL/ 0.30~0. 44,

0.25% ~ 0 . 5 %

0 . 5 %
1 8 4 0 0 0 . 7 5 %

0.125%

levobupivacaine)
dextrobupivacaine) , S - )

R + )
S R

R EC5d 3 9 %
K d) R S 27. 3
4. I ^ M , R S 7
R Vmax S
R S

981ms:56ms) S Harding
S Vmax
30 jiM Vmax S
5 0 % 4S Vmax
R
5 / 6 A - V
S 4/6 A - V

150mg
24h 400mg
2 0 0 . 5 %
300mg ( > 3 mg kg _1) , 3. 7 (ig .
m r 1 C N S

0 . 7 5 %
20m l

556:506min) ,

355:376min)

( EtidocaineDuranest)

5 0 %
5 0 % 2 ~
3 2 .
4

0 5 % ~ L 0 % L 0 % ~ 1. 5 %
150 ~300 mg

p H
3.0 ~ 4. 5 )
5 ~ 15 170 ~ 147

(
PrilocaineCitanestPropitocaine)

3 %
2% 3 %
0 . 5 % 1 % ~ 3 %
400 mg 600m g

(

Di-

bucaine s Sovcaines Nupercaine^ Percainev Cinchocaine)

I 2 ~ I 5

0.3% ~0. 5 %
0.2% ~0.5%
5.0~7.5 ~10 mg
( RopivacameLEA 103)

S -
> <
> < A S C

5: 1:2;
9:1:2 1 . 0 % 0 . 7 5 %

0.5% ~ 1 . 0 % 20m l
OjSfjog/ ml,

0 . 5 %

5 ~ 1 5
4 ~ 6

5 - 2

5 - 2

(%)

(min') (min)
O g)

(mg/kg)
1, 000
600-800
19.2
100 ~ 150 1 -5 45 -90
600-800
13
60

0.25-1.0

1.5 2_0

3.0-5.0
3.0-4.0
0.5 ~ 1.0
1.0 2.0 40 60

0.2-0.3 50-75

7-10
0.33
0_2 0.3 75-100
0.25 0.5 300 ~500

2.0-4.0
200

400
1.0-1.5

+
2.0-4.0 40-100
L 5 2.0 150 ~400
0.5 -1.0 300-500

LO 1.5 300-400

0 2.0 150 400

1_
0.25 0.5
150

0
.
25
-0.5
200

0.5
15 20
0.25 ~ 0.7537.5 -225
0.5 1.0
300

1,0 1.5 150-300

1.0-2.0

400

1.0 3.0 150 600

1 ~3
15
15
15 -20
1.0
2-5

10-20
2~5
8 12
10-20
5 ~15
15 30
10-20
10-20
5 15
10-20
5-15

60
120 ~ 180 2.5
90 ~ 120
90 180
*
90 120
60
120-240 7.0
90
90 -120
90 ~ 120
180-300 7.0
60 ~ 180
120 - 240 2.0
360 ~720
75 200
180-300
360 720 4.0
170
120 180 8.0

(%)

)0.25 ~ 1.0

0.25 0.5
0.5 ~ 1.0

0.75-1.0
-
h-FFl

0.5 ~ 1.0

(min) (min)

(mg)
(mg/kg)
0.4
5 10
2 4 240 400 3.5
200
180 210
2
10-15
100 ~ 150 5 ~15

1942
(tubocurarine)
metocurine)
alecuronium)
pancuronium ) vecuronium )
(rocuronium) rapacuronium) pipecuronium) atracurium) c i s - atracurium)
mivacurium) doxacurium)
gallamine) fazadinium) suxame
thonium)
imbretil)

d - tubcurarine)

4 2 5 % 8min
8 ~20 m in
20 ~50 min
50m in

IC U

IC U

7 5 %
9 5 %

2 % 8 0 %
ED7

095
095
0 % 1 0 0 % )

ED2flED5ED75ED95

ED8
^

25%
9 5 % 2 5 %
75%

15% ,

O.OZmgkg-1)

V 1)

Vdss)

t1/2a )

t 1/2(3)

2 IOmin2 h ,
70miri,
20min
2 ~

6 0 100 ml/ kg/min

2. 5 min

6 - 1 6 - 2

6 - 1

(ml/kg/min)
(ml/kg)
(min)
(%)
6 ~ 16
200-500
2 8
30

200 ~450

2 4

120-200

40 50

400 -470

1.2-1.3

220-360

35

230

2.7

99

28 34

180-280

5.5 10_ 8

17 ~20

51

110 ~200

4 7

18 27

146 -588 \
26-147 \ 1 ~5 \
~ 123 -338 112 18 79 55 2 8 2. 32
191 -346/
2~5 /
41 200
~

150 ~340

1.0~1.9

100 ~ 132

30

340 425

1.6 3.4

100-215

180 ~250

3.6-5.3

50-53

30 57

170-210

3.4

70 80

25

200 -457

8.5 11.1

72 88

6-2

( % )

1 -2

90%)

40-60
40

10-40 2
-

60 80 10-20 <10%
10 40

60-90%)
-

( % )

y 10 - 15

80%)

95 ~ 99%)

<5

70

30

10% ~ 20%)

70

20

10%)

20-30 70-80
40%)
70

30

<25

10%)

50%)

suxamethoniumsuccinylcholine)

1000

2 % ,

2 % ~ 5 %
ED50 ED95J 0 3mg/kg 0. 5 mg/ kg , 0 5mg/kg ,
60 ~ 90s , 60s
T K p 2 ~ 4 min lmg/ k g
4 5min6 12min
0. 1 % 0. 2 %
50 ~ 100(jLg/kg / min 30 ~ 60m in
1 %
0 . 5 % 0.05% ~
0 . 0 7 %
lmg/ k g 1.5mg/ kg
lOmg/ lm l I .5 ~2. Omg/ kg

I I
3 0 60m in 7 lOmg/ kg
n n 5% n

i g n
.5g n
n
n

n n i ) 4

2 )

3 )
4 )

5min

A
K +
O.5mm
l/ L
,
p
k
5. 5 mmol/ L

1 ~ 2

3 ~ 5 min

.5m g /k g 0. 03m g /k g ,
0. lm g/kg

7m g /k g

C dantrolene)

3 0 % 30% ~
5 0 % ,

1.07kPa (8mmHg)
lm in 2 ~ 4 m in 5 ~ 1 0 m in

PCO2

3.92kPa (40cmH20 )

0.2% ~ 8 9 %

I ~ 2 m in

0.5% ~
1 % 1:12000, 1:
30000

0 . 0 6 %

d - tubocurarine)
pH

.3 ~ 0. 5m g

10 ED95

15mg/70k g

.1 ~
2m g /k g 0 4 ~ 0 5m g/k g
.5~0.6mg/k g

ED 95 0.5m g /k g 6m in 2 5 ~ 35min

9 0 % 7~ 90min
0.1mg/ k g , .5mg/ kg

f
dimethyl tubocurarine.metocurine)
2 ~2. 5

0.44 ~0.5/ kg 90 s
150min ED95
0. 25mg/ kg )
5min 3 0 ~ 4 0 min, 9 0 % 80
~90 min

Pavulonpancuronium)

5
3
4 0 % ~ 5 0 % , n 1/
5

2 ~ 3 ED9J f

2 ED 95 3. 5min 0. 12 ~
0. 2mg/k g 90s SOmin
120minED 95S .07mg/kg 25min 90%
60min

0.015mg/kg .7mg/kg

pipecuronium)

3 40% ~ 5 0 % ,
lOOniin95 0.05~
0.06m g/kg 5 ~ 6 min, 3 0 4
min 9 0 %

80 ~90min 0 lm g/kg, 3 ~ 3. 5m in
7~ IlOmin ,
0. 06mg/kg .
4mg/kg

U 214C

vecuronium)
D
A

P -

1/2 ~ 1/3

i5 0 % ~

6 0 % 1 7 3. 17

15% ~ 25%

ED95S 0. 05 mg/ kg 4 6 min,

3 5 ED95
2_8min l .lm in ,
ED95
1 0 b m in , 9 0 % 3min 0.0 7 ~
0_15mg/ kg .2mg/ kg ,

O.OSmg/kg I ~2|xg/kg . min,

9 0 % 6 0 1
0. lmg/kg

N -

rocuronium )

1/72/3

2 ~ 3

1)95
. 3mg/kg,
3 ~ 4 min, 10 ~ 15min, 9 0 %
30min .60mg/kg , 90s
45 min L 0mg7kg,
60 ~ 90s 75 min
-

rapacuroniumQrg9 4 8 7 )

293ml/ kg 8. 5 ml/ kg/ min

i3
5 0 % , ED90 1.15mg/ kg
I .5 mg/ k g TOF 96s
62s , 60s
20min24m in
2 min TOFR 0. 7
12min 1 2 - ^ pg/ kg/ min
2 ~ 3 mg/kg ,
3mg/ kg
ltxg/ ml2 2 %
3 -
1

doxacurium)

ED95
ED95S 0. 025 ~0. 03mg/ kg 10 ~ 14min
9 0 % 80 ~ lOOmin 0. 05 ~
0.06mg/ kg 90~120 min

.04mg/ kg 0 02 ~ 0. 03mg/ kg
IC U

tracriumatracurium)

1 6
10
Hofmami
Hofmannp a
C - N pH
Hofmann4p H
3 6 0 % 1/3
Hofmann

lmg/ kg )

H1 H2
N
Iaudanosime) N -

N - N
MAC
ED95S 0. 2mg/
kg , 4 ~ 5 min, 1 0 ~ 1 5 min, 9 0 %
30 min

4 ~. 5 mg/ kg 25 ~ 4min

lmk/ kg
.7mg/kg

N -

5
~ 10|jLg/ kg/ min

c i s - atracurium) 10
4
ED 95S 0.05mk/ k g
7.5min 2min 45min , T O FR 0.7
67min .2mk/ k g
2.7min
5ml/ kg/min ,
24min Hofman
N -
N -
N -

8 ED95
4 ED95

mivacurium)
- 3 5% ~
4 0 % ) , -
50% ~ 6 0 % ) , -
4% ~8 % )
2min, 50 ~ 100ml/kg _
min
7% ~ 8 0 % -

1/10,
53min4.6ml/ kg/ min ,

3 0% ~50%,

0 2 mg/ k g 1/3
0.25mg/ kg , 5 0 %

5 0 % ED95 0 08mg/
kg 3 ~ 6 min 2 5 % 15min
6 8min9 0 % 25min 3
_2 2 0 %
. 2mg/
kg , 9 0 15 ~20 min
5 ~ l Ug/kg/ min
5 % 9 5 % 15min,

flaxedilgallamineTrithiodide)

1/6 ~ 1/5

8 0 % ,
5

1/5 ~ 1/2 40m g

80~120 m g 3 ~ 4 mg/ kg
.6mg/kg
0..3mg/kg ED 95S 2.5mg/kg 4 ~ 5 min 25~
40min , 9 0 % 70 ~ 80min

alcuronium)
I ~ 1. 5 ,

3 mg /kg 3
ED950.2 ~
0.25mk/ k g 3 0 % ~
50% 0

fdzddinium)
1/3 1/2

1/2 ~
2/3

1.0 ~
I . 5 mg/ kg 0. 5 ~ I .Omg/ kg

i t

A D
A

H1 - H2 -

. 3 ~0. 4 mg/ kg

.5 mg/ kg 0. 6 mg/k g 0. 8mg/ kg

3 0 % 5 0 % 9 0 %
15s 75 s 0.6mg/ k g

6 mg/ k g 15m in H1
H2
A
A

N -

2 - 3 -

. 6 mg/ k g

6 - 3

6 -3

.
I ~ 2 min
5 ~ 7 min
9 5 %


---iwBteWKawwawMgwiwawawwBBiMWiBwuiiiwu.iiiuiiiMiuwiinmiiBiiiwmiMirjaBua *

1 0
1 0 10

3 %

2 0 95
3 ~ 4 0 95
3 4 0 95
30 ~ 60s

1/10 ~ 1/6
5 /6 9/10

90s

90s

4 ~ 5 min,

0 95
0. 6 mg/ kg ) , 90s

3 ~ 4
95 0. 9 mg/kg ~ I .2 nig/ k g Im in
50 ~150 min

l _5mg/ kg 63 TOFR0 . 7 35min

6
- 4 6 - 5
6 -4

ED95

(mg/kg)
(mg/kg)
0.5
1.0

0.2

4
=

T95%

(min) F25%
min) (min)
1.0
6 ~12
12 15

0.3 -0.4

2 ~3

40 50

50 70

0.05

0.2

2.6-2.1

66-70

83 ~91

0.03

0.05

5 ~7

72 ~83

109 ~ 133

E D 95

<
T 9 5 %

(m in ) D 5 %
m in )
(m in )

(m g /k g )

(m g /k g )

'

0. 08

0.2

2 3

12-15

30

0.3

0.6

3 ~4

90-110

140 160

0. 25

0.3 -0.4

2-4

100 ~ 120 . 180 240

0.05

0-08 0. 1

2 3

90-100

120 150

0. 045

0. 08

2 3

90 120

120 150

0.04

0.08 0. 1

2 3

45 ~60

60 80

0.3

0.6

1.5

23 75

60 70

6 -5

(m g / k g )

(m in )

T 2 5 %

T 9 5 %

(m in )

(m in )

1.5

45 ~ 60s

10 12

15

0.5

45 ~60

60 90

0.4

1.8 2.0

88 ^ 95

115 128

0.08

3 ~5

125 ~ 190

200 230

0. 25

1.5 -2.0

12 -20

34

0.2

1.5 ~2.0

120 ~ 150

180 ~ 300

0. 15

150 200

200 300

0.2

1.5 2

60 80

80 ~ 120

1.2

45 ~ 75s

38 ~ 150

9 5 % 4
T 1 T2T3 T4
8 5 % 4
T 1T2 T3 , T4

PTC P TC O 2

1/5 ~ 1/3
15 ~20 min,
40 ~60 min

a
I I I I I

I I
9 5 % ,
2 5 %

13min5 % 9 5 % 32min

12. 5 min, 2 5 % , 5 % 9 5 %
26. 6 min

2 5 %
5. 7 min , 5 % 9 5 % 13. 6 min
6 - 6
6 - 6

|jig /k g / m in

T 2 5 %

(m in )

95% (m in )

30 ~ 100

15-30

8.3

4. 0-6. 5

13.6-16.6

1 ~2

12-15

30

10

9~17

27-65

7 ~10

12-15

25

1.6

(T 9 5 %
33. 2 I .8m in

IC U
IC U 1 )

2 )

3 )

4)
ICU

IC U

3 -

N 4 9 ~
22mg/ k g N - 4
HjJLgAnl, N - 2
I l
N - 4 6 fjLg/ ml
N - 4

N - 4
8 0 %

I I I

I K

3 % ~ 5 %

(DN) 9 6 %

DN > 70 0. 0 4 %
DN <30
4%
DN 3 0 7

I I

f ,

3 ~4

2 5 % 3 0 %

7 ~
llm in l ~ 2 min 15~20 min

1 2

.
4 mg/ k g 0. 2 mg/k g

5 0 %
7 5 % 7 0 % ,
6 - 7
6 - 7

(m in )
(1/k g ) (m l/ k g /m i n )
(m in )

0.7

9.2

3.4

77 '

1.6

4.8

2.5

181

I .1

8.6

6.7

112

1.0

2. 1

3.9

379

I .1

9.6

7.2

110

0.7

2.7

7.0

206

4 4
1 2 ~3 4
30min10 ~ 12m in 3 ~ 5 min

0.7mg/ kg
0.28mg/k g lmg/ kg

Im in 7 ^ g /k g
0 . 5 ~ l _0mg/kg 2 ~ 3 min
7 jxg/kg
.7mg/kg

4
6-80

6 - 8 4

T O F

(m g / k g i v )

(f x g / k g i v )

<2

0.07

7 15

2 ~3

0.04

7 15

' 0.25 ~ 0.5

0 rg25969,
1:1

IS-

CX-
P -
Ct1 Ct2 P1 P2
1. - Ct1 -
C a , prazosin) Ct2

Ot2
-
yhimbine ) a 2 -

2. p -
P - P2P3

G - cAMP
P1 -
P2 -

P2 -
- A T P

P2 -
-
(3 -
1 5 % P2 - 3 0 % ~ 4 0 %
P2 -
- P2 -

B2 -

cAMP
P2 -
P2 - P3 -

3 .
- I ( D A 1) - 2 ( D A - 2 ) - 1

cAM P
- 1 - A T P
- - 2
- 2
- 2

4_ G - G -

Ct - P -
G - G - a
(3 7 G -
G - GDP)
G -
GDP, GTP) G - a

G - a - GTP p - 7 a GTP a a

P - 7 G -
GTP GDP a p 7 G -

P - G -
cAMP

P -
cAMP4 0 0 cAMP
a 2 -

G -
cAMP G - p
-

Ot1 - G -
C P1P2)

G - G -
Gs) G -

Gi )
G -

P - G -
cAMP
G -
cAMP
G -
G - cAMP
cAMP

5 .
3 -

P - 3 0 p
-
P -

-
|3-
P -

P -
P -
P - P -

1.

M1 - M5), M2 M2
M3
2

a p cts S )

Nmob)
Nrep)

M1 M3
M5) M3
C
M2 M4) G -

3 4

ctp

'

1 .

P - P -
+ 2. 5
2 pg/min (30ng . kg _1 . min - 1 ) Ot1 -

3(xg/min (50n g . kg -1
min - 1 )

4 % ~ 1 6 %

10 ~50 ng kg _1.min-1

5 ~ IOmg10 ~ 15m l
. 25%
10 ~ 1 5
2 .
- N -

a i Ot2

P2) , P 1 -

P2 -
(X1 -

P -

Im g 0.2 mg/ kg ,

0.1~0.2 mg/ kg ) ,

IOml

I ~ 2 jjLg/mi n (32 -
2 ~ K W m in (25 ~ 120ng .
kg ' mirT1) Pl -

HVgAnin ( l M n g . k g 'm i n
1 ) a -
a -

2 0 300900(xg

P2 -

CX1 -

OU

a P -

1

0.5~2.1{8 -1_111;11_1, 0 1

2 H Vg .kg _1.min_1 a |3,

5 . k g -1
-mirT1,
10 ~ 2 0 kg ' min-1
a P 1 - P 1 -

4 .

P 1 - a (32 -

2
2 ~20 (jug . kg -1,min-1

5 .

(3 - P 1 P2
- -

P2 - ,

P2 -

g
P 1 P2 -

n m

5 ~ IO^g

(20 ~ lM ng kg ' rniiT1) ,

6.

a p -

10 ~
30mg

7.

a - Ct-

10 ~ 20m g IOOml

5 0 - IOOtJLg,
8.

a -

a -

5 0 lOOjjug

9.
1962
1972

Ct2:a i 200: 1
a 2 -
a 2

 : ;

2 - P

a 2 -
ACTH P -

5 0 %

9 0
5^ g / kg , MAC

6 0 % 4 0 % ~ 7 4 %
3 4 .

150(xg )

1a -
Ot2 -
Qt1 - -

3 ~ 5
Ot1 -

2
5

1 0 20mg IOOml I ~ 2 mg
P -

2
_
a , - i i
Ct2 -
5 - - I A

3 5 2. 7
8 0 % , 10% ~ 1 5 %

25 mg
.6mg/kg , O j mgZkg ,

.5mg/ k g 4 jjug_ kgM

3.

P 1 -

P2 -

1 2 % ,

1 2 92. 4 L/ h 9 5 %

l ~ 2 mg,
l mg

4.
8 0
P 1 -
a -

5 5 %
2%
9 0.5111
/ 1 ^ 5 0 ~ 300 1^-1
min M 5
10 ~ 2P 1 - 30

0.25 ~ 0.5mg/ kg 50 ~ 3 0 0 . kg
1
.min4 0.25mg/ kg

5 .
P - Ct1:(3
1 : 6 , 2 - ai -
1/10, P 1 P2 -
P 1 -
I/4 , P2 -
1/12,

1 1 0 4 ~
5 i

2. 5 mg, 5

25 ~ 100

glycopyrrolate.)

5 ~ 6

10% ~ 2 5 %
5 0 % , 1.0140
5 0 %
3 0 %

1.6~3.3 1.2~2.7 iy k g
1 %
3 .
( 1 )

100

0.3 ~0.5 mg)

3

(2)

0. I ~0. 2 m g

(3)

(4)

1)

2)

H2

3)

7 ~ 1 4

4)

5^ g/h 72

^262^

 S :

1.

( 1 ) edrophonium, tensilon)

< lm s )
3 0
0.5mg/
kg ) 1 0 4 5 % 2 0
1 5 %
O
(2)

6 5 5 0 %
8 ~ 10

(3)

2 .

5 0 % "75% 7%
3 -
1/102 5 %
3 - - N -
3%

0.7L /kg , 1.117kg

I . lL / kg ; 9. 2 ml.kg
1.miiT 1
8. 6ml.kg ' min_1 9. 6ml.kg ' min-1; t1/2oi
3. 4 6. 7 7. 2
t 1/2P 77 112 110
t,/2p

20 ~30 2

3.0mg/ kg , 15mg/kg
35 mg/kg

0. 8 2.0 7 ~ 1 1 12 ~ 1 6
6 0
9 0

3 .
( 1 )

(2)

2mg1
8mg

1 2 Img

(3)

,
.

5 0

3 0

(
1.

Poiseuille s Law) , <?)

P 1 - P 2) y 4
Z T7
Q. = ( P 1 - P 2) TryA/ S Vl
2
16

2 .

(1)
:

a
(2 )

Minoxidil)

Na + - Ca2+

(3)

CGMP) ,

(
'

= X

-
-

Frank - Starling

(
8 - 1

19691972

. ^
V 9.33k P a (7mmHg) ,

8- 1

1.
2.

(1)

(2)

(1)
3.

(2)

(3)
4.

(4)

(5)

- 2

8 -2

TT

11

--

<

I
I

pH

2 ~2. 4 kPa (15 ~ 18mmHg)

1.32kPa (IOmmHg)

8 - 3

8 - 4 ) :

8 - 5
8 - 3 __________ !___________________

8-4

A )
V )

8 -5

V > A
A
A
A
A
A
A
A

> >V
> >V
> >V
> >V
>V
=V
=V

V > A
V > A

U
I i
i

T T

I l

--

--

--

I i

11

<

<

<

T
T

<~ t

N1

1 .
(1)

(2 )

2
3 .
(1)

hexamethoniumC6)

50~100 mg, 8.0 9.33kPa (60~70 mmHg) ,

30 ~50 min5 ~
3mg, 2 0 ~ 3 0 mg lOOmg

(2)
trimethaphan)

arfcmad)

^ 276


!S

1%

0 . 1 %
250mg

3 0 %
( a
a a

a a
Otl
(terazosin) doxazosin); @ a 2
Ct1 CX2
1 . prazosin)
Ct1
Ct1
(X, (X1
a i

.( Ct1

P
Ct1

P
1~2
3 ~4 9 7 %
t f ,

0.5mg lmg
3 9 mg/
15 ~20 n7g Img,
3 5 mg, 4 ~6

2 urapidil) ebrantil) ,

a 2
5 - I A

2 ~ 5

4 ~6

N - 5 0 % ~70%

Tlt
25 ~50 mg0. 5 %
3 phentolamine, regitine)

Ct2 a i

Ct2

4 0 %
3 0 % ,

0. ImgAnin
0.5111#11^11, 20(^(]^.11^11)

(
1 K +
K +

K +
ATP
K +
K +

K +
Ca2+
nicorandil)
pinacidil) cromakalin)
K +

( 1 ) pinacidil) , pindac,


C 13H19N5245. 3 , K +

K +
1 3
6

8 ~ 1 2


57% ) 3 9 % ~ 6 5 %
1 3 ~ 4
(3

12.5mg/ 2 / 12.5 ~ 2 5 mg/
2 /
P

I
T

(2 ) minoxidil)
minkdyl, prexidil, Ioniten
C 9H15N5O , 209. 3

NO
A T P K +

2. 5 mg/ 2 / 5 ~ IOmg/
2 / 40 mg/

IOmg
T

( 3 ) diazoxide)
eudemine, hyperstat, hypertonalum, proglicem,
proglycem C 8H7ClN2O2S , 230. 77
A T P

t 2 4 8
4 ~ 20
1 3 5

10
~ 1 5 50 ~100 mg

2 .

(felodipine) isradipine) nicardipine)

nifedipine) nisoldipine)

8
- 6 )

Psaty 1995 ; Pahor 1995 )

2 ~ 15mg/ h

8 -6

i
I
I
T

1
Il
I I
T

TI

Tt

1 sodiumnitroprusside, niprode)
(1)
Na2Fe
(CN )5WO J H 2Ot5
50m g 5 %
3 1 0 %
4 8 5 0 %


(2)

NO,
CGMP

0.61 ~3. 87|xg/kg . min min ,

37_ 2 % 3 1 . 1 % ,
8. 8 % 5. 5 % 2
9 0 %
4 0 % ,
1 5 %

16% ~ 2 0 %

( 3 )

5
44% 2 %

5 CN - )
-4

SCN

CN _ ) Fe3+ )
CN -

0 34 mg/ d l ZTfxg/ dl
45 ~ 48

200 ~300mg,
20 ~30 mg

10

2. 9 mg/d l 10 ~ 15mg/
dl 20 mg/ d l
1
25 ~20(V g / min 1
25mg/ 1
200(jig/ min

CN _ ,

'

150mg/ k g 3 ~5
C N -

( 4 )
0 . 0 1 % 0.25 ~ IOfJig ( k g . min) 3
(k g . min) 2 3
4 ~6 i ~
1
8 ~ 16|xg/min 5 ~ 105 ~ IOfJig ,

8kPa (60mmHg)

5(xg/min200 ~ 400|xg/ kg . min, 50 ~

100|Xg/ min
5(V g / mi n

pH
2 nitroglycerin)

( 1 ) prodmg)
NO, N O
N O LNO

GC) , CGMP CGMP
Ca2+

3 1 .88^

(2 )

I f
13 1, 2

SH )

NO2)

(NO3 ,

( 3 ) f
0 . 0 1 % I lXg (kg
min) , 3 ~ 6 kg min)

0.25(xg (k g . min)
Ip g (kg min)

0 3 ~0. 6m g 2 ~3

5 ~30mg) 8 ~ 1 2

(
1. hydralazine) dihydralazine)

4 0 % ; 5 0 % ,

25mg, IOOmg,
3
P

2 I angiotensin converting enzyme inhibitors, ACEI)

- - RAAS)
RAAS
RAAS
mRNA
RAAS,
ACEI
I n

ACEI , captopril) , enalapril) ,

ramipril) , Iysinopril) ,
(perindopril) , benazapril) , cilazapril) ,

fosinopril)
captopril) ,

7 0 % 1 5 1~2 12.5
25mg100~300 mg/

2 % ) 5 ~ 2 0 % )

3. Bindapamide)

3 0
9 3 %

4.

ketanserin, 5-

5 - HT2 Ci1 - H l -
5 - H T
5 - H T

Q - T >500 ms

1 8

-
Ca2+
calcium channel blocker) ,
Ca2+
Ca2+
Ca2+
(calciun entry blocker). calcium antagonist)

receptor operated calcium
channel) voltage dependent calcium chan
nel),
L T N P N P

Ot1a 2P "yS Ct1

6 a i 1 a 2
4 (31 7
T

T Ct116
16p l 3 . 3 ) , 1 7

1987 WHO

6
1.
i n m

2 .
JV V VI
1992

(1 ) 1 L
Ct1 Ct13

I a

I b
I c

(2 ) 2 Ca2+

 !HS

N W - C T X (ea - conotoxins)

P AgelVA
3 non - selective channel modula
tors)

'
1 T
T

(
1 .
(1)

(2 )

0 Vmax) ,

APA ) 4

( 3 )

> >

2 .

8 - 7 )

8 -7

---

+++

++

++

+++

++

, + +

ERP

3 .
(1)

(2)

.

'

4
( 1 )

L
Ca2+

LDL ) LD L
IL- 6

(2 )
-

(
'
8 - 8 ) 31^!1~311

2 0 % ~ 4 0 %
3 ~ 8 L/kg t1/2p 3 ~ 7 h

P4 5 0

6 ~ 9 h

8 - 8

(m g )

80
160/8h

30
120/8h

1040/8h

10
20/8h

70 150 70 150 5 -20

5 20

10
240/24h I 0m g /24h
20/12h

( I^gZ kg )

.k g _
* m in -1)

1 5

1 ~5

>90

>90

(m in )

<30

15

75 -90

(%)

0. 1 0.3 0.5 1.5

>90

.99

2m g / h

80

>90

64

3 ( 20 60 15 30
30 90
20 ( )

210

70~80

40 60

20 40

60

20

24

40 60

30

20

90

89

90

98

98

2. 3 6. 22.9-8.5 0.8
(I ^ k g )

90

5 10 60 65

99

70.6 6. 6 2 6

98

21.0

h)

4 10

2 ~6

3 5

3 5

12

3 35

50-250 100 250 10 ~ 100 5 100

10-30

2.4

10

(n g /m l )

70

35

80

55

85

20

(%)

15

65

20

45

80

(%)

3 ~4

0.2-4

0 1

<0.03

<0. 1

(% )

6 0 % cohort study) 7 1

Braun

8 9)
8-9

1.

2.
3.
4.
.5.
6.
7.
8.
9.

10.
11.
12.
13.
14.

()

WPW

6 0 % 9 0 %
75 ~15(V g/kg
( 5 ~ IOmg) , 3 ~5

WPW

QRS

WPW

P -
(3 -

3mt

n m

0 lm g /k g IOmg
0 . 5 2 mg/kg

Ot2 -

150 ~ 300m g/kg

2~50 m g ljjug/kg . min

IOmg

1 0 ~ l 5 mg/h 25 min, 3 ~ 5 mg/h

.7mg/
k g 10% ~ 2 0 % IOmin,

9.86kPa ( 74m m H g)
1
(kg . m in)
8kPa (60mmHg)5~15m g/k g
0.1 ~ .3mg ( kg . m in )
30min

( .
Ca2+

ATP

200jxg/L

15(V g/kg
50mg

K V g / k g

2 4

L 2 MAC )
40mg (k g . min) 40 min

70~15( V g / k g
lOOmg/ k g 0. 15mg/ kg

-
-
-
-

(

(
isoptin) C27H38N2O4
HCL, 491. 15 % pH 4.5 ~ 6. 5 ,

1 .
(1)

P- R ^

(2)

Ca2+

P
(3)
,

(4 )

2 .
> 9 0 % ) ,
2 0 %
Tpeak 1 ~ 3
2

5
4 ~ 6

8 ~ 10Vd 4 L/kg ,
Vd t1/2p
norverapamil)
2 0 %

7%
4 % P450 3A4
3.

(1)

IOmg;
1 Im g

( 2 ) 40 ~ 120mg 3 ~ 4

P
( 3 )
1
120~240mg
4 .
A

Ct1 Ct2

ct
5

(
C 17H18N2O6
346. 34

>

1.
( 1 )

20mg

5 -

(2)

(3)

(4 )

2.

4 5 % ~ 7 %, 9 0 %
3 2 0 Tpeak
2 0 ~ 3 0 1 ~ 2 6 ~ 8
tl/2(3 4 ~ 1 1 P450 3A4

20~300 ng/ ml tl/2

3.

4.

-
5.

1 7 % ,

4 %, > 1 0 %
4. 7 %

( amlodipine)
Cm H25
CLN2O5, 408. 9 ,

2 4

N O
N O

2.
,
Tpeak 6 ~ I 2 6 0 % ~ 6 5 %

< 1 0 %
Vd 2Iiy k g (i V) PH
'
9 8 % ) t 1/2
3 6 45 ~ 5 0
7 ~ 8

3 .
4.

P -

5
( diltiazem)
C22H26N2O4S
HC1 , 451.0,

1 .
( 1 )

(2)

ST

(3)

2
4 0 %

2 5 % ~ 5 0 % 15~30 Tpeak
3 0 80%, Vd S 5L/kg t1/2
5

.25mg/k g 2 7 5 %
0. bm g/k g
15 0.35mg/k g

4. P -

H2
A 60 ~80 mg/d ,
A A
5 .
4 %

(
n im o d ip in e )
C 21H26N2O7, 418. 4
1

1 0 %

2.

1 3 % 9 5 % 11/2 2 ~ 9

3.

4
4 60mg 2I 2 0
40mg/ 2 ~ 3
4.

21 % 25 % )

(
nicardipine)
k C26
H29N3O6 v HCl, 516.0
179 -185,

1/1 0 ,

DI W
9 2 8 % 1 8 %
2 2 %
2.

30m g 3 5 % 9 7 %

t 1/2 8
3.

5 mg/ h , 1 5
I ~2_ 5 mg, 15mg/h
4.

54% ~ 6 3 % ) ,

< 1 0 %

(
nitrendipine)
C18Hm N2O6,
360.4

1.

20mg, ,

_
2.

10% ~ 20 % 9 8 % t1/2 6 ~ 1 5

3 .
4.

10% ~'20%) 6 % ~ 1 5 % )
5 % ~ 10% ) 0

()

Na +
O
Vmax )

m h
h
Na +

1 K + h ,
Na + Cl

2 d f ,
Ca2+
Ca2+

Ca2+ 2

3 K +

K +3
4
K +4

4 4 Na + 4
Na +
Na +4

1 4

APD )
2

APD ERP ERP

ERP APD ERP A P D
ERP
ERP

A P D

Vaughan Williams
A B C
( I

1 .I A O

APD ERP )

2. IB

3. IC

( n - P -
P -

( m
APD ERP,

( IV
Ca2+

Vaughan Williams
,
Sicilian gambit

( I A
Na +

4 Na + if )
ERP/ APD E R P
K + Ca2+

1 . qiuinidine)
cinchona ledgeriana)
5 ~
11918

( 1 )
Na +

1 )

2 )

3)

E R P APD APD K +
Q - T
E R P
E R P
ERP

4)

a -

(2 ) 2

7 2 % ~ 8 7 % 3~6|jLg/m l ,
6~8| xg/ m l 8 0 % ~90%
1 0 2
4 iy k g
10% ~ 2 % , p H 7 8
5 0 %
(3)

K +

(4 )
1/3

Q - T c
5 0 %

pH K +

( 5 )

c t -

'

2. procainamide)
- CO - NH - )
- C O - O - )

(1)

APD ERP ,

(2)
8 0 % , 1
2 0 % ,

1. 5 ~ 2. 5 L/kg N -
3 0 % ~ 6 0 %
(3)

(4)

1 10% ~
2%
DNA

3 . B disopyramide)

( 1 )

1)

(1.3~5. 6 ng/ ml)

2)

3)

APDERP
ERP
(2)

8 3 % )
2
1 5 % , -N
- 5 ~7

pH
(3)

( 4 ) 10% ~
4 0 %

n n

I
n mQRS Q - T
2 5 %

Q - T Jervell - Lang - Nielsen

.
Q - T

4 . aprindine)

APD ERP,
K +
I A

,( I B
O
4
Na + K +
A P D

1 Iidocaine)

( 1 ) Na +
K +-

1 ) p - SfjLg/ ml)

2 )
- K +

K +

K +
K +
lO ^ g/ ml) O

3 )
APD ERP APD ERP

2 Na +
(2)

1/3
7 0 % ,
3 117kg
t f 1 0 % t 1/2p 2

(3)

K +

Q - T
U

4 ~ 5 mg/k g , 1 5
9 0 I ~ 2mg/k g , 20 ~
50mg/ min 20~40
15 ~ 5 0 kg min ) ,
1

40 ~50(^ (k g min ))

1.5~5 fjLg/ml)
( 4 )

i i n m
2 . phenytoin sodium)
5 0

1958

( 1 ) -

1 )

2)

K +

K +
K +
'.
.
3)
-

(2)

1

9 3 % 0. 5 ~
0.817k g ,
3/4

(3)

(4)
^
50mg )

>2(V g / m l

'

3 . mexilitine)

6 ~8
p H PH5 . 0 )
2. 8
PH8. O) 8. 6

l i
o n - T

4 tocainide)

( I C
0

4 Na +
1 . flecainide )
C 17HmF6N2O3 .
C2H4O2, 474. 4

( 1 )
^331/^

4
(2)
2 ~ 4
12 P450 2 D6
t 1/21 0
17 3 0 % t 1/2

(3)

2
50mg, 2 /
100 ~200 mg2 / 600 mg/d
lmg/ kg , 1 5 0. 5 mg/ kg 2 mg/ kg
(4)

2 . encaninide)

C22H28N2O2 ^ HCL , 388.9,
1~2
tl/2 3

8 0 %
4 % ~ 2 5 %
25mg, 3 / 50mg, 3 /
200mg,

3 . Iorcainide)
C22H27CLN2O HCL , 407.4
1~2

t 1/2 3 0 t 1/2 8
tV2

8 0 % 3 0 % ~ 6 5 %
lOOmg2 / 400mg/
2 mg, 300mg

4 . propafenone)

171 ~ 1 74
(1)

I C

E R P APD P - L

(2 ) 3 0 2 ~3
2 0 % ,
9 0 % P4502D6 5 -
P -
W 502D6 N -

P4502D6

tU2 2.4-11. 8

(3)

150mg, 3 / 3 4 300mg, 2
70mg/ 3 ~5 2 0
1 350mg
(4)

( n
P -
p -

4
P - A P D ERP
A P D

1 - propranolol)

P -
'

(1)

1)

2)
(3-1 0

3)
A P D ERP
APD , IOOlXgAnl
E R P
(2)
9 0 %
1~3
>30 mg)

9 0 % 2 0

(3)

1 )
WPW

2 ) :

0.5
~ I .OgAi)
( 4 ) P
I ) P 1-

P -

(2)

( 3 )

P -
P

2 metoprolol)
P 1

25~1 0 0 mg/ d 2
2 0 0 ~ 450 mg/ d , .15mg/ kg ,

3esmolol)
P

2
8
6 ~ 102
P -
250~500jxg/kg 1
50 ~300(xg (kg . m i n ) ,

( DI---
APD
A P D ERP
1. amiodarone)

2
37. 2 %

(1)

1)

2)

3)

APD E R P W PW

4)

et - Ca2+

(2)
5 0 %
I .2 L/kg 3 0
4 ~ 6
t 1/2p 1 0 ~ 5 0
(3)

(100 ~ 2OOmg/

8 0 %

9 0 % 800 ~
1600mg, 1 ~ 3 2 ~ 4 800mg ,
600m g 4 ~ 8 2~3
400m g 400m g

IOOmg/

1 0 15mg/ min, 6 lmg/ min, 189

0. 5 mg/ min 10150m g
2 ~3
^

800 ~ 2000mg, 2 ~ 3 2 ~ 3|xg/ m l

1 2
( 4 )
1)
.

2)

400m g

25%
S 5 %

5 %

T 3
T4 rT3
2 0 %

5 % ~ 1 5 %

1995


2 . bretylium)
F D A

'
( 1 )
1)

A P D A PD
APD

2)

'

(2)

5 0 % ,

5 ~ 1 0

13. 5
3 0 2
(3)

(4)

2
~ 4
3 sotalol)
C 12Hm
N2O3S H CL 308. 5
( 1 )
Ikr (
A P D ERP ,

P -

(2 )
1 0 0 % ,
V 27 ~18
150ml/ min7 5 %

(3)

,

2 ~ I .5 mg/ kg 1 0

80~160 mg2 / 160~480 mg/
d 2 / 640mg/ d
torsades depointes, Tdp)
(4)
Tdp
Q T Q - T Tdp

Q - T

( IV

1 verapamil)
( 1 )
4
0

(2)

. 10% ~ 2 0 % 2
3 6
1/10,0.5 ~ 1 2 10
1 0 3 0 9%
t1/2p 3 ~ 7 7 5 %
(3)

;
WPW

WPW
a
40 ~8 j0mg3 /
24~32mg/ 480 ~720 mg/
5 ~ IOmg/
(4 )
(3,-

( 5 )

P ,

n ni

2 diltiazem)

P -
30~ 9 0 mg/ 3 / 5 ~ l mg/

3 bepridil)

APD
ERP ,

TdP 300~450m g 1 / 2 ~ 4 mg/kg

(
1 . adenosine)

(1)

0.03~0.3 jjLgmd/ L A
A ,A2a A2bA3
G A ATP

cGMP cGCP cGCP

(2)
,
t,/2 10 ~ 2 0

(3)

3 0 12mg 9 2 %
2. 5 mg

P -

3mg 1
~2 6 mg 1~2

12mg
( 4 )
1

COPD
:

2_ magnesium sulphate)

Na+ - K + ATP

Ig
( 20min
1 2 ~ 3 g/3

[General Inform ation]

=
=
=346
S S =12055332
DX^ =
=2008.4
=

MAC

 MA C
MAC

Cm)

I C U