Manual of Pharmacotherapy 1 (Rx 38)

7/21/2019 Manual of Pharmacotherapy 1 (Rx 38)

1/705


2/705

...

() MUPYRx36& 37

MUPY Rx 38 !"! " # # ! $ "

% &! $ "" 4 ! '

"#"!"## :)

"(..... ( ( )* !+,!

" ! ) -!

"(...... Rx 38 # $# ."/(

! ( # ! )

0#" (+ ")

*). *).

*). + *

"(+


3/705

Table of Contents

Manual of Pharmacotherapy IChapter

Pages


4/705

187 !"!#$"%#&$'

() % *+&, -'()*+,-./012

3456789:;

?

@A

B


5/705


6/705

188 !"!#$"%#&$'

() % *+&, -'()*+,-./012

3456789:;

?

@A

B


7/705

/023/02 5609:;?????????????>>>>@1


8/705

18A !"!#$"%#&$'

() % *+&, -'()*+,-./012

3456789:;

?

@A

B


9/705


10/705

1AB !"!#$"%#&$'

() % *+&, -'()*+,-./012

3456789:;

?

@A

B


11/705

/02 C= ;6D9:9;


12/705

1A1 !"!#$"%#&$'

() % *+&, -'()*+,-./012

3456789:;

?

@A

B


13/705

FEINFECTIOUS DISEASES

B G6;H;>> I11 J9:0;9K

L6;62;;=???????????????>>>

1@A@ CMM0 N=M;09;


14/705

S X5Y3G5/=???????????????????

?> @1I7 LK;>>>> @7A

11 OH0:K> @A1

1@G6;ZKV;6;:=??????????????????> EBE


15/705

ONCOLOGIC DISORDERS

B ]96:0?????????????????

???? E1E1 ]96:0^9;6???????????????????EE8

Manual of Pharmacotherapy IINEUROLOGIC DISORDERS

I888 ZR=;> EIA

I8AB L;209;6

X9W9:Z???????????????>>ESII8A1 /V6;9??????????????

?????>>>> E8E


16/705

I8A@ GK_Z;V0`=/;=9=???????????????>

EA1I8AE /M0==;>>>>>>EA8

I8AF T:Z;_ F1B

I8AI 56= F17I8AS G6U;R???????????????

?????? F@II8A7 aM;KM=R???????????????

?????>> F@AI8A8 ]bT T;VK96

/02=??????????????>> FFE

I8AA cH=;R???????????????????>>>>>>> FFA


17/705

IABB G/X/????????????????????>>>>>> FSI

IAB1 90d;6=>>>F7E

GYNECOLOGIC, OBSTETRIC AND UROLOGIC DISORDERS

@Ee>>>>>>>F81

@F ^ F88@Ia6W FAA


18/705

I888 /R=P6:; IBE

I88A C0;690R56:>>> I1E

I8AB X???????>> I@E

I8A1 c= IIF

I8AE J6;26 ^0 ISBI8AF a0:;K

/R=P6:;> ISA


19/705

DERMATOLOGIC DISORDERS

@Ea6W>IAA

@S Y;09K Td;656P:;>>>>>S@E

@7^909=;

56P:;SEE

@8 G:6?????????????????????? SFA


20/705

@A GK> SIA

EB T6=:06???????????????????>> SSF

Manual of Pharmacotherapy IIIEYE AND EAR DISORDERS

I888 aR/;=> S7@

I88A a90W;=??>> 7BI@F i 717


21/705

I888 c=> 7E1

I88A NZV9>>>>7ES

ENDOCRINOLOGIC DISORDERS

@E OZR0>>> 7FF

@F/;9H;:

LKK;>7I7CAEDIOVASCULAR DISORDERS I

I888 /02 C= ;6

]90W;>> 8BB


22/705

I8AB T> 817

I8A1 ] 8EE

I8A@ G0;9K[;H0;KK9; 8I@

I8AE Y6> 87FI8AI 56P:;\

a6W>> 881

HEMATOLOGIC DISORDERS

@E G6V;9????????????????????>>>> AB@


23/705

@F OZ9K9==V;9??????????????????>>> A@@

@IJK>>>> AEA

@7i3S3

^/????????????????????? AF1

@8]>>

AIBCAEDIOVASCULAR DISORDERS II

I888 XRM06=;>??>>> AIS


24/705

I88A /R=K;M;WV;9??????????????????>> A7I


25/705

Manual of Pharmacotherapy IVGASTROINTESTINAL DISORDERS

@E ^ZR=;>>>>> 1BB1

@F^M;:CK:0???????????????????

1B1I@I /R=MM=;9???????????????????>> 1B@A

@S iaN/ h

jaT??????????????????>>1BE8

@7 500;9HK J 1BSB


26/705

@A /;900Z9???????????????????>>>>>> 1B7S

EBb9=9Y>>1B8@

E1 ^ZR=; 11B8

EEY;09KXM9;;=??????????????????> 1117

EFD;\0

:;00Z 11E1

OTHERS

I888 Y9::;6????????????????????>>> 11FB


27/705

I88A G=ZV9 h ]c^/????????>>????????> 117@

I8AB GW\0= /02 N9:;>???????????? 1@B7

I8A1 J>>>> 1@SE

I8A@ ^Z90V9:;:=?????????????????>>>1@7F

I8AE L96P9:0;62????????????

?????? 1E@1I8AF ^Z90V9:R

D9Q?????????????????>>>1EE7

I8AI ^6V


28/705

I8AS 56k6_9 G lX1b1m???????????????>> 1E7B


29/705

Biopharmaceuticals 1

BIOPHARMACE

UTICALS

Chapt

er

1*). ) % 4903028*). 12 3 4903064*). " (( 4903110

Biopharmaceutics ( )* )

Biopharmace!ic" *1&(")(Ph#"ico$chemica%

Proper!ie") 4+,#))(5 /!"" +# + " / 6.!(#

(Ra!e a' x!e! o *+"orp!io)

Bioa,ai%a+i%i!# !( / -Pharmaco'#amic" *10 -4+,

+ 0 ) * ! *1 0

- "

Pharmaco-ie!ic" *1&+ #!( "#"

Pharmacokinatics " -!

i+era!io "!! $" *+"orp!io "/6 / /i"!ri+!io / i!e o ac!io Me!a+o%i"m ! Ph#"icochemica% proper!# #

&$-

xcre!io ""&

Absorption Process

22 *+"orp!io Proce"" "/6 / n &- ""(

# 0 6 / ! ! 22 )* # %+"! %# - # ! 7 %

)* # "" Bo%" "/6 $

p%o! 8 P%a"ma coce!ra!io " !ime - /!


30/705

MUPY Rx38


31/705

2 Manual of Pharmacotherapy

QQQ>690>:


32/705

*UY P*RM*Y


33/705


22 .*+ coce!ra!io ra'ie!

22 Plasma protein *!"

p%a"mapro!ei ..

#'7(/i"io ra!e)

%6''!" !$ ()!%&'89(ic-;"ir"!%a


34/705

MUPY Rx38


35/705


36/705

Biopharma ceuticals '

! 0"

( " (ph#"icoch emica% proper !ie" o

'r")

p>a .............. 0 io&iA a!io& (&io&iA e' - ....)

1 %& i o&iAe' .!%&

1 %& i o&iAe' .!%&

%ipi' "o%+i%i!# & #- - (mem+rae !" -! )

mo%ec%ar < eih! . - & macro mo%ec%e 0 - -

5888 pro!ei $CCCC........5889 0 (mem +rae perm ea+i%i!#)

" (" capi%%ar# e'o!he%ia% ce%% 6 # $

23 0 ' i%"i'a%

" # %

# 3 %

24 0 ' - - # 0 (B%oo'Brai Barrier)


37/705

MUP Y Rx38


38/705


23 $ (mem+rae !ra"por!er)P$%#copro!ei $# 0 mem+rae

!(-!(reioa% +%oo' Do


39/705

5889 a%pha 1 aci' %#copro!ei (**@)5888 1 +i'i "i!e5889 "" +a"ic 'r

5888 proprao%o%Eami!rip!#%ieE imipramieE

%i'ocaieE meperri'ie5890 %o+%i

*UY P*RM*Y


40/705

Biopharmaceuticals

23%ipopro!ei24RB

!i""e pro!ei +i'i5888 ! 0 :("5888p%a"ma +i'i " !i""e +i'i5889!ra"por! proce"" !i""e 5890+%oo' per"io

5889 0 5888 : ..... #-- / ......

/ #-- "!

5889'ii!oxi....... ("#"" #-

5890 !e!rac#c%ie..... "6! !"6 ....#/

8

ch%oroHie....".0( $# 0$ )

Pharmacokinetic parameter

23 $# +"!!" 24

- !

25 +".- ! -26 ""

(/i"!ri+!io Ra!e o"!a!E) )5888 ! " ".#

""$

"

5889 & .&

5890 ) ! % !

(/i"!ri+!io ha% %ieE !1I2)23 # # /

24 ( )


41/705

25 !00"

MUPY Rx38


42/705


!(o%me o /i"!ri+!io)

*+ (," amount(m-" of +ru- in the .o+yplasma +ru- concentration(m-/," after e0uili.ration

%+''+!+


43/705

,* )!

%+' $

'+"*%&$(omoeo")

,*

%+' )!

2 %+'(o%me o !he e!ra% ompar!me!E

])2 %+'! 1'

(o%me o /i"!ri+!io a! "!ea'# "!a!eE

TT)2 %+'!+%,-

(x!rapo%a!e' o%me o /i"!ri+!ioE a^)

2 !%(o%me o 'i"!ri+!io +# areaEGNaG E)

/ # $

. %#- * ' .%-

*, oa'i 'o"e

:r

=9WR =9,oa+in- +ose #pss *+ H;


44/705

*UY P*RM*Y


45/705


Pharmaco&inetic parameter varia#ility ( ! 0 " )

23 a! "


46/705

cirrho"i" E ephri!ic "#'rome $# G ...... $#

MUPY Rx38


47/705


'ru! interaction

23 pro!ei +i'i " pro!ei / & "- ree (K )

p%a"maK arfarin"

phe#%+!aAoeIa"piri

#iliru#in " "a%ic#%a!e

phe#!oi " ,a%proic aci'22 !i""e K 'i!o*in" Hii'ie

24 ihi+i! P$%#copro!ei ( $ -!# !% " 1 . )K""

cyclosporine "

'a&or+ici&

*")$.!

ritonavir "

"aHi&a,ir0 1

/ %%%$$$ " pro!ei ( ! )

+,- +./+,-

Gaproxe& Phe!oi&

h#roxi&e Propra&o%o%

?arari& o'im ,a%proa!e

/iaAepam

epari&

miprami&e

*mi!rip!#%i&e

@%i+e&c%ami'e


48/705

*UY P*RM*Y


49/705


Metabo$ism Process

5888

(%imia!io J Me!a+o%i"mL xcre!io)

5889 me!a+o%i"m Pro'r ac!i,e me!a+o%i!e

Drug metabolism

5888 Pha"e Reac!io (YP Pha"e )NONO NONO0 Micro"oma%

oxi'a!io 0.0 #'rox#%a!io0.1 xi'a!io

NONO NONO1 Go$Micro"oma% oxi'a!io

1.0 Re'c!io1.1 #'ro%#"i"

5889 Pha"e oxi'a!io NONO NONO0 #!o"o%

eA#me0.0 @%croi'a!io0.1 %a!io0.2 *ce!#%a!io0.3 *mio aci' coa!io

NONO NONO1 Micro"oma%& c#!o"o% eA#me

1.0 Me!h#%a!io1.1 @%!a!hioe coa!io

Metabolite !.%& 4%


50/705

0 i,er +%oo' Do<

1 oac!or0 coac!or 1 a%+mi ree 'r

MUPY Rx38


51/705


0 *e0 @ra#

Ba+# #'rome h%orampheica%

1 eA#me Rea% +%oo' Do<

Me!a+o%i!e

1 /ie! A#me i'cer :

!.oh;"


52/705

*UY P*RM*Y


53/705

Biopharma ceuticals 13

5888 A.i'cer 2 5888 *!o$i'c!io : i'ce e A.*'

-'iaAepam + . %' +!'o"e !!+ i'

ce eA.* +!)$ 6 +!)$ !

5889 ro""$i'c!io : - 'i'ce eA. . %*'

5889 A.ihi+ i!orPharmac okinetic Parameter

x!rac!io Ra!io# ,a%e " 1 0 J 1$High E ( E>0.7)

2!rst " ass metabolism "24clearance "

2#.nitr ogl$cerin%

"ro"anolol% mor"hine &o' E (E

0.)

2!rst " ass metabolism '*

27.the o"h$lline% 'a r*arin% +ia,e" am

24epa!ic c%earace#

Q hepa!ic + %oo'Do #

5 0 /! #"! -

22 0/ ! .0/ ! / !;

22 + 0# !; -

22 )% ! %0%% 0!! 0/ ! / 0 $

# ! "!# ! " # 6 $ # !;

0/ ! ! %".0$ #


83/705

*UY P*RM*Y


84/705

Dru-&Dru- %nteractions 27

5888 " *%+mi 0 Pro!ei +i'i /

?arari ""%! 90F & " *%+mi # $# ree


85/705

MUPY Rx38


86/705


];=9M0;W ]K90;Z0


87/705

*UY P*RM*Y


88/705

Dru-&Dru- %nteractions 31

OZ;


89/705


%ari!hrom#ci

*mio'aroe

%,oxamie

C?P

1

Parace!amo%

/i"%Wram thanol

!hao%

/* preerre'1a' accep!a+%e

@su#stratesor i ,i!ro experime!".X

Therapeutic In'e* " 6 "ru!Interaction

*mio%#co"i'e i'ocaie *#c%o"pori i!him heoph#%%ie

/ioxi Me!ha!rexa!e o%+!ami'e

#'ro%#cemic

ae!"

Phe#!oi ?arari

i'ocaie Procaiami'e

/ "ru!interaction "

0 Garro< herape!ic"1 #!o!oxic ae!"

2 *!iarrh#!hmic"3 ra% co!racep!i,e"4 @%cocor!icoi'"5 erapami%6 e,o'opa

!;

!; $ - + !! -!# - ( & )

(- & - %# 1 # $! "! #


90/705

*UY P*RM*Y


91/705

Dru-&oo+ %nteractions 33

OOu}y |rv}rzF7BEB7S*) . 4903074 # % "! (ora% 'o"ae orm) /6 /

4+, ) . " "! .&//6 /

% %0 " " /6 "! $ # !;

6 0# I .!( / 6 (+ioa,ai%a+i%i!#) -

$ # 0 1 !!- % !; + " &

# pharmaco-ie!ic pharmaco'#amic

%# pharmaco-ie!ic (*/M) 0

0 /6 (a+"orp!io pha"e) 0 %! a%+mi %o+%i ('i"!ri+!io pha"e) 0 $ YP (me!a+o%i"m pha"e) 0 ! ! (excre!io pha"e)

.- n & !; + "# "! " &0 # 0# 1- !+ )

0 Foo'/"ru! interaction " ! #3

1. 0% ('irec! eec!" i!erac!io)! !; % "! 0#+ioa,ai%a+i%i!# 0 1

!; che%a!io !e!rac#c%ie " E me!a% io"

. mae"im !

2. 0 (i'irec! eec!" i!erac!io)$ # !! @c!io $# /6 +ioa,ai%a+i%i!#

! !-!

- !; "

1. 0!! ('i""o%!io) ('i"i!era!io) 6 #/!

. . !6/ & //6 / -%

0


92/705

1.1 $ # ! (# $

- $ # /! .# 0 $ # /6 ~

MUPY Rx38


93/705

Manual of Pharmacotherapy

$ -! $# # 0 # /6 $

#! ( " " $# &/" "0 .& / /6

/ - -

1.2

0 # p

$# # (p !( 1.5$2) 0

$- peici%%i @E ampici%%iE omepraAo%e "

$ ! e!eric$coa!e' # $ - omepraAo%e $# -6 " #& /$ e"!era"e / #/! e"!er(

cepo'oxime proxe!i%%E er#!hrom#ci e"!o%a!eE ceroxime axe!i%%) - &/ -6 e"!era"e $

$ $# (" ! (" !

$# (" ! / #/! ! # /6 . - 0 ./ 6 % #3 &//6 $- .

- / / # 0# - "/( .$

# -! $- .- $ # #/ 6 4+, - " / (

& //6 #$ - .- $# !(&/ / 6 / (*U)

""" ! !"- &&/ /6 - !" 6

!; che%a!io !e!rac#c%ie " E me!a% io"

ph#%a!e /- "& & "" "! /

6 - erro" "%a!e

" "" carrier ( $ ) / %! / "

" %e,o'opa #"" aroma!ic amio aci' !ra"por!er $- .

- / $ 0# (" - #-&//6 / -

" 0 me!a+o%i"m raperi!E ! YP 3*4 ihi+i!or "!

" &/ !)%-6 YP3*4 $# "/ "-6 YP 3*4 $

- raperi! . " YP 3*4 $- $# "& //6 c#c%o"porie

!#ramie ! !"- z " M*" (mooamie oxi'a"e

ihi+i!or") !#ramie &/!!%-6 M* 7 & M* ihi+i!or" /. !#ramie


94/705

*UY P*RM*Y


95/705

Dru-&oo+ %nteractions 3'

( - M*-!! ! !#ramie) 6 !#ramie -!#- G 6 $#

%/7 " $# "!ro-e M !#ramie +roa' +ea"E

ra"p+errie"E a,oca'oE choco%a!eE E - E & E 0 E % E

6& E &

E - E -

!

$ ! E E 0 E > 4+, ?arari

$'opa ( 1 Par-i"o;") " hih pro!ei 'ie! $'opa &//6 %

#e!ra% amio aci' !ra"por!er %! & /6 $'opa .

(# # !; "

+ # "! " # "! $ 3 4+,

# 0/ ! "!#+ " - 0# "#

! $# ! . ! - ## #0 / !

- "!+ ) #

# + "

@ - "#

@ "# @ "#

@ - "#

7 ( # - " -

-AAA

@a"!ric emp!#i !ime: / #-! $- (

- -!&$- )

- # : @a"!ric emp!#i !ime J 0.5$1 % 7

.%,/1 % - !$ - -!. - "

# : @a"!ric emp!#i !ime J 1$2 % # @a"!ric

emp!#i !ime %7 - & -- " " # -

. 1/ % - "

$$ #! -!; "

1.) ( ! !; ) " & -%$ "! "#

1%1 "! .%,/1 % 9 1/ % ( 6 !

- # p # 4


96/705

MUPY Rx38


97/705


. (. )

!% * "() +

"() cap!opri% 1) 30$40 !% *()+!)$ ++2 c#c%o"porie -

- !. * "() /+0 - ciproDoxaci

ca%cim (ciproDoxaci /i,a%e!Iri, a%e! ca!io - M@

E a@

)

$' %3 ciproDo xaci

! -' -' ++ %& #

' .#

)+

$ ()!#"%+%-+( ci"roo/acin Dialent1rialent cation

# %oroHio%oe 7. " ar+ox# !'* 3

" >e!oe ! '* !4 $ $), he%a!io #!% 2 3 +

%& comp%ex !

'. * $+ !#! 2

3 * "()

"%+%-+( etrac$cline Dialent1rialentcation

$e!rac #c%ie ,'++ he%a!io !

#! 2 3. ! , '+%&%!.% -e!oe *%coho%

(eo%iAa!io) ! '* 11 12

$* %&' %oroHio%oe e!rac#c%ie

! % 2 3 %oroHio%oe e

!rac#c%ie %& 2 -!# 3 -!# p 4

-!. er#!h - rom#ci "!eara!eI+a"eE peici%%i @Eampici%%iE aAi!hrom#ci cap"%eE omepraAo%e


98/705

*UY P*RM*Y


99/705

Dru-&oo+ %nteractions 3

**+!'+@ 1$.'+- + , + - %'++'

!+ er#!hrom#ci ' 11.30 . )!+' 12.30. 7+' 11.30

. + '!!)! ciproDoxaci '1%& +' 12.00

. . .. ! +.7'@

''-+ 7+.- er#!hrom#ci "!eara!eI+a"e.

)'+)!1))!-!# er#!hrom#ci ' e"!o%a!e '+!+!"()

* .(e"!era"e *e"!er +o'.1"*


100/705

MUPY Rx38


101/705


'@

$ i!racoaAo%e %& 1""% cap"%e '- )+

'1" "% "o%!io .'3- )+.

!" e"!er orm ()!'* e"!era"e !'

"% e"!er ()!%&"% !"(). - cepo'oxime proxe!i%eE er#!hrom#ci e"!o%a!eE ceroxime

axe!i%eE ce'i!ore pi,oxi%

epo'oxime proxe!i%e %+! )$ 70F2.) ,!%B+++$.1..#%.''# %!.%-!4 !.%8+++

!-+!% raperi! -iceE /+0%& YP3*4

ihi+i!or 7. !1" me!a+o%iAe' 6 YP3*4

%+!!1""()"%+,+ #'+'

3.) -+!+!/+0/r.!$oo'!erac!io *''! i"%i+ 15 0.5 -!# !

/+0

3.2 *' )$%co"i'a"e ihi+i!or" +* !$*.()$%co"i'a"e

% 0.5$1 -!# *

!'4!%

!.

!.(!%&) .+*+ 1$2 -!#

% *

!'-(n!%&) - i!racoaAo%e cap"%e !""% e"!erorm ()!'* e"!era"e !'

"% e"!er ()!" "%!"().- er#!hrom#ci e"!o%a!eE ceroxime axe!i%eE ce'i!ore

pi,oxi%

!/+0!|- G*/"

0eference

+ +E %- '+E C DC. "- *

.+2, %-- *

:+$!

1E2549.


102/705

*UY P*RM*Y


103/705

Dru- use in ,actation 37

yn v}F7BEBF@3


104/705

-!6"* #+,*

(mi%- !o p%a"ma: MIP ra!io) -'*!!62 -$!!%&.%.

!-!)!-+' !"''*%&/+0

MUPY Rx38


105/705


& # !) $ #0 /$ - # ) "

!

$ !#"" "#"!emic ! " # /# "#

$ "!

r#-!

!-!-$# "# (

$ !#6 ! ## #" $ ! # # " ! %

#" " $ # # #

! ( 4V5

# 0! - 6 " " 0

! " 0 ! "0 / /

### ("

! % "! $

(5 ! PP H7

Categori

es

xzrn A


106/705

o&!rai&'ica!

e'

." +' ")

*UY P*RM*Y


107/705

Dru- use in ,actation 1

!.-

*!ire!ro,ira%

"

*!ieop%a"!ic"

*mio'aroe

*"piri

Be!a$+%oc-er"Ben;o'ia;epines

oxi+"

ari"opro'o%

h%orampheic

o%

h%orpropami'

e /ap"oe

r!ot

al&aloi's

Isotretinoin

Pheo!hiaAie"E

*!i'epre""a!" Pro!o Pmp

hi+i!or"

6tatins

%oami'

e" %i'ac

?arari

!-5+' 1% % .

!. !$ *"piri & Paracetamo$$ oxi+" G*/" !-. ' $ /ic%oeac$

Ga+me!o&

e

$ +proe

$%i'ac

'!. $ 'ome!haci

$ Meeamic aci'


108/705

$ Me%oxicam$ Gaproxe$ Piroxicam

Go!e

:

$ Parace!amo% : -.$ '$L

$ G*/" : '-E-.'

MUPY Rx38


109/705


% '-

!. !$ h%orampheico% / Beta/lactams @

mo*icilin$ /ap"oe $ %a,%oa!eE %+ac!am$ amcic%o,ir $ *c#c%o,irE ,a%acic%o,ir$ @ri"eo%,iE !racoaAo%e $ >e!ocoaAo%eE

%coaAo%e$ Me!roi'aAo%e $ %i'am#ci$ %oami'e" $ Macro%i'e"

/ Euinolones

$ e!rac#c%ie"$ Me+e'aAo%e

Go!e : $ '!'- ''-.: Qio%oe"E e!rac#c%ieE >e!ocoaAo%e$ ' '!" a!ia%:- @ri"eo%,iE !racoaAo%e - '

>e!ocoaAo%eE %coaAo%e-. ! ha%Die ! "*

7.

2%

2#.

!. !$ erpie h#'ra!e ( a%coho%

! 0

/ ntihistamine $.

7.e&A. *%coho% $ *ce!#%c#"!eie'eh#'roea"e .!( 1 " ) $ /ex!rome!horpha

$ @aee"i$ Phe%ephri&eE

P"e'oephe'ri&e

4

%

*'

!. !

$ Chlorpropami'e( a% %ie

)

$ @%i+ec%ami'eE @%imeperi'eE

@%ipiAi'e$ Me!ormi


110/705

*UY P*RM*Y


111/705

Dru- Use in Pre-nancy 3

yn v}F7BEBF@3


112/705

2#6+%'+'


113/705


# $ ! /!) #)% !

#) !% -"""

##$ #0#1#) # #

!-!-

# # /0# 1%

# )

! " #) # - " " ! ! /

# )# /!)#) - # #

! " $ ##- "! % # $ 3

# # ) /)# / )# $ " %

! $ ) # / %

) & + ! " %#") # "%

.''$


114/705

*E BE E /

*UY P*RM*Y


115/705

Dru- Use in Pre-nancy '

a!eor# * *1"" "#1 " / # a!eor#* - #

# 0! #) # - - 2# .

0

!

#) # # -

2 3

a!eor# B *1# " / # a!eor#B - #$# 0!

# ) - *1"" "#1

*1# " / # a!eor#B #$# 0!

# ) - "0 *1"" "#1 # - -

2# ! 0!#) # # - 2 3

a!eor# *1# " #/ # a!eor# $# 0!

#) - *1"" "#1 - *1#1 &0

#) / # a!eor# # ! !%

# 0!#)

a!eor# / 2# . / # a!eor#/ # # 0!

# ) -.# # &$- ( # !%

#)- # 1 # #1%6-

!) - # !) - - 0

a!eor# *1# 1 " / # a!eor# $# 0! #) I !"( # #1 " # $# 0! #)

#0! !% - "

# a!eor# # ! # #

)

-. Preac# a!eor# ! /"

# - / " /( "0#) *1 /2


116/705

MUPY Rx38


117/705


!: (5 ! U /*a!eorie" *1# *1#

$*I # #- "*

- "$

!era!oeic$%


118/705

?arari1 - " #6 / # U/*;"Preac# a!eor# / 6

2" 0 #)

*UY P*RM*Y


119/705

Dru- Use in Pre-nancy

nwnrst?: !" U/*;" Preac# a!eor# / ''2

A G:;0;6 GV;


120/705

7 b9HV


121/705


': X "'*

'$


122/705

$ 3 64 + i!eme!ar# a+orma%i!ie"#1


123/705

Dru- Use in Pre-nancy 7

26"5+'$7

*%&'-

!eroi' "ppo"i!or# -!eroi' . !-7 -=! % .

!. !*$ spirin%% 'o"e #- 1 3 (/) & Paracetamo$ 8B;

$ J6I"s C7IBs#-1 3 (/)


124/705

MUPY Rx38


125/705

'6 Manual of Pharmacotherapy

Go!e: $ !-G*/".. %'+7" 'c!"ar!erio"" "

$%9.% 1.%9G*/" .%%9$ $ G*/" 1'$''!"" 7.%

' /* %9'$'"*."6+%'+/* !%9%9.+'

.7 '-" !$ G*/" .%%97%9..

,% '-

!. !*$ Tetracycline (/) '-.' 2 3 & Amo=ici$in 8B;$ Euinolones() %o< ri"-

$ Peici%%i"E epha%o"pori"

(B)

$ 6ulfonami'es() '.-.'!3(/) $ %a,%o&a!eE %+ac!am

(B)$ >e!ocoaAo%eE %coaAo%e()

$ %i&'am#ci& (B) : ram

L

$ %ari!hrom#ci () $ r#!hrom#ci (B)$ *Ai!hrom#ci& (B) :

ram $

$ Me!roi'aAo%e (B)$ %o!rimaAo%e !opica% (B)

Go!e: $ 1 L peici%%i - c%i'am#ci L *Ai!hrom#ci$ %oami'e" - Bac!rim (o$!rimaAo%e) -

.'!3 !"%a.%. ! +i%ir+i a%+mi * +i%ir+i.%!

*+ -eric!er"

: 1!- % &+2' 7 ' 1 . - ' 7'-$ !%&--+

'. "%


126/705

*UY P*RM*Y


127/705

nti.iotics '1

A7TIBIO

TICS

Chapt

er


128/705

h%orampheico%"E !hiampheico%

e!rac#c%ie": ch%or!e!rac#c%ieE !e!rac#c%ieE 'ox#c#c%ieE mioc#c%ie

MUPY Rx38


129/705


Macro%i'e": er#!hrom#ciE roxi!hrom#ciE c%ari!hrom#ciE aAi!hrom#ci

ico"ami'e": %icom#ciE c%i'am#ci

*mio%#co"i'e": "!rep!om#ciE -aam#ciE eom#ciE e!amiciE!o+ram#ciE ami-aci

%oami'e": "%a'iaAieE "%ace!ami'eE "%W"oxaAo%eE "%ame!hoxaAo%eE"%a'oxie

Qio%oe": a%i'ixic aci'E orD%oxaciE oDoxaciE ciproDoxaciE %e,oDoxaci

Po%#pep!i'e": po%#m#xi BE co%i"!iE ,acom#ciE !eicop%aiE ramici'i"E+aci!raci

Gi!rora": i!rora!oiE i!roraAoeE DraAo%i'oe

Riam#ci": riampiE ria+!i

ynznx|znwzr}

Broa spectr"m

4+, " "" ampici%%i

4+, " - # 6 - ch%orampheico%

" %!%6 ric-e!!"ia - !e!rac#c%ie"E ch%orampheico%Eme!roi'aAo%e

Mei"m spectr"m

4+, " """ "%oami'e" -

7arro, spectr"m

4+, " "

4 +, #3 " " peici%%ia"e - $re"i"!a!peici%%i" (oxaci%%iE c%oxaci%%i)E peici%%i @

4 +, #3 " " amio%#co"i'e" -


130/705

#U,RM#Y


131/705

nti.iotics '3

*'/+ 0' -

Bacterici'al '-/+0F*-#!.%./+0'6('

(

Bacteriostatic '-/+0$+5'+#'-$-./+0$

#%'$)'


132/705

' Manual of Pharmacotherapy

*'./+0

./+ 0

1. $6( 1.o"om#ci2.#c%o"erie

3.Baci!raci

4.acom#ci

eicop%ai

5. $%ac!am a!i+io!ic"

2./+0'( po%#m#xi Bco%i"!i

ramici'i"

ampho!erici B

#"!a!i

3.$#%'30 ri+o"ome"+i!

1.*mio%#co"i'e"

2.e!rac#c%ie"

50 ri+o"ome"+i!

1.h%orampheico%"E

2.Macro%i'e"

3.ico"ami'e"

4.$&c%eic aci' Qio%oe"Riampici

Me!roi'aAo%e


133/705

#U,RM#Y


134/705

nti.iotics ''

5. '#. %oami'e"

M3amio"a%ic#%ic aci'

!rime!hoprim

p#rime!hamie

i"oiaAi'

6..!4

I !$ 6(

6( 2 $'

$'!1 ri'ie 'ipho"pha!e$ace!#%mram#%$pe!ape!i'e (U/P$G*M *)E

^90d 6:K

!$6( .fosfomycin9 cycloserin e


135/705

MUPY Rx38


136/705


$'! -!' G*@$G*M* pho"pho%ipi' c#c%e

!$6($'$. #acitracin9

$'!2 cro"" %i- pep!i'o%#ca

!$6($'$. K/lactamanti#iotics9 vancomycin

# 6(

6( 6(

2,6(!'' *! !are! ' pep!i'o%#ca /+0'

%a#er -$pep!i'o%#ca " (? 20

m) %& %ipi' +i%a#er /+0. !

1.% PBP-$pep!i'o%#ca /+0.

%ipi' +i%a#er 2 -$ o!er mem+rae c#!op%a"mic mem+rae

-$pep!i'o%#ca " '(? 2 m )/+0'()6 o!er mem+rae 6 pori .% . )

1PBP -$pep!i'o%#ca ()!%& !are! . * !#

. 6' ' - %+, PBP%+,!

!-$!%ipopo%#"acchari'e !

%& pep!i'o%#ca. - %% G( !%& '*

6!% &- pro!ei

pori - **6 ( pori $


137/705

*UY P*RM*Y


138/705

nti.iotics '

?1 >os-om'cinH H

+!.-$T708M7


139/705

6( #$*

.( 2 -+/$a%aie racema"e /$a%aie %ia"e

MUPY Rx38


140/705


%'+-$1 /$*%a. #%!"% $*%a /$

*%a#- .( /$a%aieracema"e $.( /$a%aie %ia"e

%B+++'/$*%a %& /$*%a$/$*%a ()!*1" .% pep!i'o%#ca

. !$.( /$a%aie racema"e * /$*%a.(#(%& rii' aa%o /$*%a ).( /$a%aie %ia"e

/$*%a$/$*%a * . '+/$*%aie pe!apep!i'e

c#c%o"erie '* --+!B #=2 G

$1""()%'!1)%

6''+() @*B* *'%

)*-=!.''',#'!$

Po$'peptie antibiotics

Bacitracin

.-$ J9:;KK= =H7;KK= %& po%#pep!i'e

a!i+io!ic"omoc#c%ic % CH3 S

ami&o aci' 7 H3C

H NN O

(hep!apep!i'e") 2

L-H! D-A!" L-A!# L-L$%

D-&'$

L-I($ D-O)# L-(*! L-I($ D-G(%

B+)+# A

omo$!#pe %iear"!rc!re

% amio

aci' 5

'(pe!apep!i'e")

zzznwzr}$6( # $i"opre#% p#ropho"pha!e ()!%& carrier

po%#"acchari'e"EII


141/705

pep!i'o%#ca"E %ipopo%#"acchari'e" 6( $

'epho"phor#%a!io ( pho"pha!e rop %ipi' carrier)

rec#c%i (* %ipi' carrier -) pho"pho%ipi' c#c%e

#U,RM#Y


142/705

nti.iotics '7

x|znwzr}

4+, " "% 7 T79MZRK


143/705

!; pep!i'o%#ca " (- ) $# c#!op%a"mic mem+rae

" /3 permea+i%i!# -!

MUPY Rx38


144/705


x|znwzr}

Garro< "pec!rm a!i+io!ic - 0 ram (L) M* MR*E e!erococci ]K


145/705

|wsx|rsxvancom'cin zx teicop$anin

ux} !eicop%ai %ipophi%ic ,acom#ci $# 0 - .

#U,RM#Y


146/705

nti.iotics 91

4 +, !eicop%ai ,acom#ci ! " "4+, -

" !eicop%ai 4 +, ,acom#ci 2$4

#

!eicop%ai 1o@ # ## # "0/ ! -

!eicop%ai # 7- M 6 7 i"io # .

.- ,acom#ci 7 - 7 # (i"io S 1 hr)

4 +,- ! !eicop%ai ephro!oxici!# o!o!oxici!# $

re'$ma] "#'rome ,acom#ci

znw~n|

!erococci ! % /$a%a$/$a%a ! /$a%a$/$%ac ( ! G

! ) - & +- < % " " - 4+,- -

G1 & Lactam Antibiotics

ac!am % ! ami'e $

$ 8 ()) " ()

! $ %$$ " / &/ %# %ac!amri

$ ac!am ! % ! ami'e !" 4 aAe!i'ioe

% $! 4+, (pharmacophore) # % !" $

ac!am ri " " 5 6 ("e' +ic#c%ic he!eroc#c%ic)

6 # " 6 8 6

MUPY Rx38


147/705


Penici$

$ins

1 2 $ 1 2

3. N 8 N

3

/ 5 . /

5

Cepha$os

porins

O 1 2 O 1 2 O 1 2 2 2

N O O. 3 O 2 . N N 3

13

13

1 3 8 8 N 8 N

/ 5 . N 3 / 5 S .

/ . ./ O / SC+)+"$#$ 5

/ 5 O &$#+ 5 5 C+)+$"'$

O+$"'$ C$"'$O+"$#+

%6(

A B A B A B

Po$'saccharie %&6(

%7AC^ G$b$O O

L-A(+ L-A(+ ace!#%%co"amie (*) 7AMA ^b$

D-G(% G(* D-G(% ace!#%mramiic aci' (B)-!'L-L*! N L- L*! N G(*

H O HD-A(+ D-A(+ O

OO

G(* G(*

G(* G(*A B A B A B

O G(* O G(*

Interpeptie brige 8IP; !

"

L-A(+L-A(+ G(*

G(*D- G(% D- G(%

%#cie 5 #'%&'-!'*L-L*! N G(* L-L*! N G(*

# ! cro"" %i- D- A(+ D-A(+

H H

O O

O O

pep!i'o%#ca& % G@

G(* G(*

G(*G(*

G(* G(*

G(*G(*

G(*H G(*H

N O N O

#U,RM#Y


148/705

#" $ 3 -!

*%a $ 4

& -


149/705

nti.iotics 93

,&la & ,&,ys D&la &B # D $lu D la

COOH= @>

$ly $ly $ly $ly $ly (@>2"-!' G

@PA %nterpepti+e&.ri+-e ( %P "

& " /$*%a $ B D&$lu ,& D& D&la# ,la ,ys la C4##$4#

COOH

= NH 4 *%&'3.(

$ly $ly $ly $ly $ly (@> "

A %nterpepti+e&.ri+-e ( %P" 2

./+0 /Dactam nti#iotics

%B+- V%ac!am /+0#$6( ()!%&*5*-+'

+ac!eria#.%$ cro"" %i- !-! pep!i'o%#ca '+

%B+++ ac#%a!io ! .( !ra"pep!i'a"e ()!%& eA#me !*5 cro"" %i-

pep!i'o%#ca %&6

eA#me $.1*!-!'#6(. *7)6(1"

*)$

.(!ra"pep!i'a"e -! peici%%i +i'i pro!ei" (PBP") ()!

"+, c#!op%a"mic mem+rae PBP" %&-+ #'-+!!''

.% V %ac!ama!i+io!ic" ''7/+0' PBP" ''.%

$%ac!am.% .(

!ra"pep!i'a"e %& /$*%a

pe!apep!i'e !ra"pep!i'a"e )

.%* %B+++ *!ra"pep!i'a"e

. 1*! cro"" %i-

6

O COO-

COO-

ONN

R CH2O

H H R

CH2OH

B$+ L++&B&

NH3

&B&

NH3

T)+#!"$"6+!$


150/705

MUPY Rx38


151/705


RH O - D-A(+ CH3

R H OR

H O

N CH3COO

- NO N OH H2N

O

CH2

N I&O O N

H3C H O H3C &B& H3C HO O

CH2OH D-A(+-D-A(+ NH3

C$(( 7+(( !$$# H2NI& CH2OH

&B& O &B&

NH3 NH3

T)+#!"$"6+!$ -

.%'+ cro"" %i- pep!i'o%#ca

,%1 Penicillins

. erme!a!io o^

6;:;KK;V :Z0R=


152/705

%!" car+ox# !2 % & e"!er

#U,RM #Y


153/705

nti.iotics 9'

zzznwzr}

$$ ce%%


154/705

1 !pro+eeci' .%# !r+%ar "ecre!io peici%%i" *

peici%%i" 1"- /+ 02)$

MUPY Rx38


155/705


$

-$ $%ac!ama"e * $%ac!am ri * . '!.%PBP - X>;6k6_9E

T>90=Ea>:


156/705

*UY P*RM*Y


157/705

nti.iotics 9

-! '/+0'-

2 minopenicillins ami&o # 4+,

.)$ '.' peici%%ia"e

Broa' spectrum @

*mpici%%i D;=70;9 V


158/705

MUPY Rx38


159/705


G1?1? 7at"ra$

penici$$ins

$

$

.-'+

'/ +0(arro< "pec!rm) -. -$ T>

90= .6-$"%- +b;==0;9 "pp. +

-T70M> @r. *E^6V


160/705

6 2 -+ o'im

po!a""im "a%! procaie

+eAa!hie "a%! !o"e! 7 )$

/+0

#U,RM #Y


161/705

nti.iotics 97

Penici$$in *

O 1 COOH

CH3O N 23

O / 5 S CH3N H HH

(" Aci stab$e &/"%#

"!

+eA#% rop pheox# rop

$# $ %#- /

6- peici%%i @ & 3&'$#4*$'*("$#((# ! 7

/ #/! po!a""im "a%!

# " UR 0' - # 3G@mg=Dac ?hr G& a'

Penici$$inase&resistant penici$$ins

> !aph#%ococc" Peici%%i"

-6 peici%%ia"e % T79MZ> #

" !rc!re - !

8?; Str"ct"re t'pe iso=a)o$es"bstit"tepenici$$in

- xaci%%iE %oxaci%%iE /ic%oxaci%%i %c%oxaci%%i

C$o=aci$$in an


162/705

# 500 m x 4 ac 5

b


163/705


"harmacokinetic !'ic%oxaci%%i % %& " !5 $! R R*

1 @

%& o$po%ar )"()+. +i'

p%a"ma pro!ei 6 'ic%oxaci%%i " c%oxaci%%i

"harmaco+$namic 'ic%oxaci%%i % !2 ' *

" )+ "!eric hi'race ami'e #on' K/

lactam rin! . %G 1"* `$%ac!ama"e

. c%oxaci%%i ()!%!"

7*acillin9 Jafcillin (Gaci%%i . . # " i"oxaAo%eV"+"!i!!e'Vpeici%%i )

- *-$ "!aph#%ococci "!rep!ococci +*. * + ph%e+i!i"

"#

O 1 COOH+eA#% ri # +eA#%peici%%i phe#%V

i"oxaAo%eR 2 3 ri * # . % & "lanar()! % & steric R O N1 2 CH3

CH3 h$+rol$,e+ #5lactamase/ 5 SN

N

HH H

O $'+"ha%oe!'* or!ho phe#% ri R1= R2= H >

O+((#

6*,'+%& h#'ropho+ic )$ *1""().)$ -R1 = C(, R2= H > C(4+((#R1 = R2= C( > D(4+((# +iclo/acillin "(). clo/acillinR1 = C(, R2= F >

F(%(4+((#

() 6tructure type 'imetho*yLphenylLsu#stitute'Lpenicillin

. MethicillinMethicillin

.' (aci' %a+i%e) )'#=

/+0.'-$ "!rep!ococciE 6.aureus (! peici%%ia"e)E

6.e"i+ermi+is '-=!*%& me!hici%%i *+ i!er"!i!ia%

ephri!i"


164/705

%:-= me!hici%%i -$ 6.aureusE 6.e"i+ermi+is$'$

# %!% PBP" !-$$' me!hici%%i (me!hici%%i$re"i"!a!

!aph#%ococc" are"E MR*) $'!4$ peici%%i" !

cepha%o"pori"

#U,RM#Y


165/705

nti.iotics 1

/%

O 1 COOH

CH3OCH3O

N 23

CH3N / 5 SH H

H

OCH3

M$'((#

$ 3 me!hici%%i 6 +eA#% rop

2E6V 'ime!hox#phe#% !& / h#'ro%#"e' %

`$%ac!ama"e 0 "!eric hi'race " i"oxaAo%e

(c%oxaci%%iE 'ic%oxaci%%i) # !!& /$

ami'e+o' " ( "i'e chai $ 6

i"oxaAo%e !! ami'e +o' `$%ac!am ri

ami'e +o' "i'e chai $ 6 . $ 3 & ami'e+o'

" (&/ $-!. ! 1;6k6_9Ea>:^6V;6k6_9 # ! a>: V;09H;K;=

# 500 m x4 ac 1 hr 5$7

/6 - - $# / #/! pro'r +acampici%%iO 1 C OOH O 1 C OO

C H3N

2

C H3O N 2 O

3 3

C H3 C H3/

5 S/

5 S NN


166/705

H H H HH2NH

HH3NH

H

A"((#

MUPY Rx38


167/705


%: 5*5 ampici%%i sznw~~ n. " .+" "%!

%* "().

COOH H COO - H

COO


168/705

#U,RM#Y


169/705

nti.iotics 3

%& peici%%ia"e "e"i!i,e peici%%i ' "().",! .6'"()

ntipseu'omonal penicillins e*tene'Lspectrum penicillins

Broa' "pec!rm ''/+0)$! amiopeici%%i

'/+0

"!rep!ococciE "!aph#%ococci (T> 90= T> M;W0V;W;= !.(peici%%aa"e6. a!ra% peici%%i" amiopeici%%i" )

+!)$-X> ;6k6_9Ea>:902;6


170/705

%&!Vamio rop

MUPY Rx38


171/705


Carbenici$$in

/#/! 'i"o'im car+ox#%ic rop / 2 /#) !-

h#'rophi%%ic #-0 # riar# !rac! iec!io (U) =>902;6 ;6k6_9 .' $

car+ox#peici%%i"

Averse


172/705

hepa!i!i" #=!* ephri!i" !$5.'

+%ee'i: car+eici%%i

#U,RM#Y


173/705

nti.iotics '

%o""i!i" (+$E %)E "!oma!i!i" * orma% Dora +

* )+'+-$)$.]96W;W99KH;:96 - #

$+)$!-%&4 7 )$.%+ pac#!opeiaE hemo%#!ic aemia 'iarrhea #= ampici%%i amoxici%%i !%& +roa' "pec!rm %=E iDamma!io $ (ph%e+i!i") '!*+

c%oxaci%%i

"periDec!io - '+-$ ]96W;W9 9KH;:96 -%E +


174/705

MUPY Rx38


175/705


-$-+$5$# `V%ac!ama"e **%&' V%ac!ama"e

ihi+i!or -*moxici%%i I %a,%aa!e

7ote

*moxici%%i 1%& 'r o choice UR" #1-$.$ 500m 1b3

m 2b2

#'+-$!+ R !+-$ ^6VM6V90= X> ;6k6_9EL> :97900Z9K;= J> P092;7;=


176/705

* piperaci%%i L !aAo+ac!am (aAoci) 1F p"e'omoa".

(1%& ampici%%i amoxici%%i `$%ac!ama"e ihi+i!or" 7F p"e'omoa"

..)

v}sznwwxwrnn

5.1"* - *mpici%%iE %oxaci%%i /ic%oxaci%%i

'% ''.PeE- *moxici%%i 1%.

#U,RM#Y


177/705

nti.iotics

,% Cephalosporins

#O COOH O COOH O

O

HO2CO N OCH3 NOC( N OCH3

H2NN S H2O H2N S

H H H HC$"'+(4!"4)# C .-A#4$"'+(4!"4)+# +6

@.-ACA

ephem ri .]MZ9K


178/705

MUPY Rx38


179/705


%.

*moxici%%

i

R# !%H$$)4+)*( !% COOH C(C*(4+(;*( !% O

1 R2 CH3O N 2 3

. / 5 CH2

ORN S

HH H

CH2SR

R1

O+$"'$ +#6 H3CC+)+$"'$

N N +%ee'iEB$+-M$'4* 6$)+$A(;4* !% N

O R O$'$) ' !aph#%ococca%

N

A#4 !% NH2COOH 4) H

3C

NN OH a!a+"e$

%i-e.COOR `$%ac!ama"eA*(%)$64 !%9 NH

N

O N O ac!ea%coho%

O N CH3 CH2 N

O

L ,e chare "#COOHY(6$# 6$)+$ e&era!io&

-4+,

" 06 " (Bac!erio"!a!ic eec!) % "" Peici%%i$+i'i Pro!ei" (PBP")

! ime /epe'ec#E # - - 0# -

epha%o"pori" 0 06 - ('ecrea"e p!a-e) !!PBP" $# "" PBP" - (!are! a%!era!io) eA#me `V%ac!ama"e $4+,

# eera!io 2 3 "# 1"

/! # 0 !#pe1`V %ac!ama"e $#

#eera!io 3 # eera!io 4 (eepime) # 0 !#pe 1

" Cephalosporins

1st

!eneration

n

!eneration

2r

!eneration

4th

!eneration

7ral Cephale*i

n

Cefuro*ime

a*etil

]P99V

M;\


180/705

eac%orE e!i+!eE

eo!iam

hexe!i%

e'i!ore

pi,oxi%X

In8ection ]MZ9K


181/705

nti.iotics 7

Ce-a)o$in Ce-"ro=ime ]P


182/705

+ram 6 ve F Peici%%i e"i!i,e . Pemoia (PP) M* .

'.F MR*

+ram ve F P> . '.F P"e'omoa"eE *cie!o+ac!or-

F-$ M*. 1-'+-$6+ $! e%%%i!i"E*+ce""E - ?o'

MUPY Rx38


183/705


"!eom#e%i!i" )!+'+-$ .are" $-$. %G'+-$6'- eaAo%i] !!d (8 -!#) $6'"

-#'+-$+%:omp%ex -+Pharmacokinetic

-+%

' "().+ + epha%exi ephra'ie *"()

- ea'roxi%

Pro!ei Bi'i '*)'$!."62 6..$7'

5.' )*%&'%6"%>.'! -+=

-. M eaAo%i + M !.*% 6*.$

5.'"%+ me!a+o%i!e ( 'e"ace!#% me!a+o%i!e epha%o!hi

ephapiri) eaAo%i .'.-!)1-!'!

6"%>.'!*%&'%

+eneration 3 eac%orE eproAi%E eroximeE eoxi!i

F !aph.'$$).*- !aph '- !rep 6. "neumoniae."

/+0F-$ @ram V ,e )$ H. inuen,a% Enterobacteriaceae% 3eisseriaP (XX*

4%& HE7PE] '.- M* )/+0F-$

+ram 6 ve F Peici%%i e"i!i,e . Pemoia (PP) F M*.''.- '.F!erococci

+ram ve F GP> . '.F Pseu+omonase Anaerobic: eoxi!i F *aero+e.

-

!' !rep )-'+-$!+$

%G'+-$


184/705

#U,RM#Y


185/705

nti.iotics 81

Pharmacokinetic

$EM % $56*.."!*62).- !

eroxime .me!a+o%iAe ).'"%+ *'%6"%>#.'

+eneration 4 XXX

e'iirX eo!aximeX e!riaxo&eX

8e*ta,i+ime

--

8e*o"era,one19albacta

m--

--F-$ Pseu+omonase.

e!i+!e epo'oxime eWxime

e'i!ore&

$!aph . !rep ' " - 6."neumoniae 1%& Pemoia # e!riaxoe eo!axime %!%&+

-e'iir

--$ @ram V ,eE GP> L 6erratiaPharmacokinetic

$ 5 EM (1$2 H 8 hr) #%$ 5 %, 1$2 -!# e!riaxoe ! 8 -!#('o"e 1$2 H 12 hr)

B>I B>I

6*.%'+.'6)$6"%>!

5.' pro+eeci' .%-$ '*" eoperaAoeE - e!riaxoe )

6"%>!*'6+%'+ -$ Ps. aeruginosa-!3 - e!aAi'imeE eoperaAoeE e"%o'i

+eneration D eepimeE epirome

- M*E !aph 7"E @ram V,e 7 .%1) GP> : 6erratia LPseu+omonas

@e 4 /+0 @e 1L3XX')!!''! eoxi!i .- epha%o"pori '%& epham#ci

#' ea%o"pori ()!Ce-o=itin /+0F-$ *aero+ic ,'+-$+

!raa+'omia% iec!io -$ @ram V ,e aaero+ic

Pharmacokinetic


186/705

2,#%&


187/705


$ 2 '1# ME 6$!'4.ha%$%ie2 $2.5 hr .'%&5

-=2#'+-$!$'!3 !4(5

%& '+-$#)

-$ P". aerio"a -ami-aci e%!i%mici

/+0F-$ 0W;4

7Zgen 8e"h

Gram ve F Peici%%i e"i!i,e . Pemoi (PP) '.F M* '

.' Peici%%i !erme'ia!e . pemoia (PP) - e!aAi'imeE e!i+!eE

eWxime

XX/+0@ram L ,e ' e 3E4 e 3 'F PP .''F../+0F @ram L ,e e 4 e 3

Gram L ve F e 1E 2 1)6erratia s"". e!aAi'imeE eoperaAoeE eepime (e 4) F-$ P.aeruginosa


188/705

'1%& 6."neumoniaeE !$' peici%%i .-e!i+!eE eWximeEe!aAi'ime

1%& 6. "neumoniaeE 5eoxi!i e!riaxoe - cepha%o"pori" .F !erococci .%& e.7'

#U,RM#Y


189/705

nti.iotics 83

Pharmacokinetic 8~wv;

5#= M '! P .$','+!.

.ea'roxi%E epha%exiE ephra'ieE eac!or ()!1"().+'* "() ea'roxi% ' @e.!1 2 .16*.


190/705

epha%o"pori !"Me!h#!hio!e!raAo%e (GM)mo%ec%e ('

M$'*('4$)+


191/705


$ R2) i'e eec! GM & /!!! .

#i!. > 10 mI' (5$10 I "$ i!.> $# i!. > $ orma% Dora #$- 6

i!. >


192/705

nti.iotics 8'

G14 Monobactam

A)treonam

GV;W H 902;6!.'.

Averse r"g reaction

hrom+oph%e+i!i" Mac%opap%ar ra"hE Ur!icaria


193/705

$ B%ee'i: !hrom+oc#!opeiaE pro%oe' pro!hrom+i !ime periec!io P"e'omem+rao" co%i!i" (PM) @E @PE a%-a%ie pho"pha!a"eE / ")$ Ga"eaE ,omi!i

MUPY Rx38


194/705


1Carbapenems

'$ !hieam#ciE imipeamE meropeam er!apeem

#'' peici%%i" cepha%o"pori" # W,e mem+ere'ri &/ % 'o+%e +o' $ 2 (me!h#%ee moie!#) 6 !

0#car+apeem ri /#

) peici%%i" $ #ami'e +o' $ac!am ri %-

% .$ # car+apeem" &"" peici%%i +i'i

pro!ei 2

(PBP2) - peici%%i"

cepha%o"pori" # # % -6`$

%ac!ama"e

a+"o%!e "!ereoi"omer #

INEST8T

O 1 COOH2 NH2

NH3C3

/ 5 SOH H H

H

Thienam'cin

COOHO

NH2N

SH

3C

H HOH

T'$#+*#

hieam#ci $ ! / $ 3 ! amiorop 6 ("

! c%eophi%e -! a!!ac- $ac!am ri % #!-# /

+hieam#ci mipeem " #0/! 0 ! "

"" G -

$ "

Imipenem

COOH H3CO NH NH

N H3C S COOHS ON

H3C

H H-

NH2H CO2 N+

OHI"$#$ C(+!+# !46%


195/705

amio rop $ 3 b$ormimimo#% moie!# 6

! c%eophi%e $# imipeem !hieam#ci i!ermo%ec%ar amio%#"i"

$%ac!ama"e - &/$ (h#'ro%#"e) - %-6 'ipep!i'a"e ('eh#'ropep!i'a"e 1

^ (/P$1)) 6! $%ac!ama"e - / # " /P$1ihi+i!or ci%a"!a!i (Primaxi ) #

1:1 # imipeem 4+,-

/o"e : 250$1000 m H 6$8 hr

*UY P*RM*Y


196/705

nti.iotics 8

TM:70V

mipeam %&'- %ac!am !/+0

!+oar' %& "pec!rm a!i+io!ic !- ci%a"!a!i- 2#'+-$+%:

/+0'-$ $!- . - (+ anaero#e

- !aph#%ococciE !rep!ococciE !erococci

- b>2


197/705

mipeem *-.! .% @*B*recep!or

. @*B* ).%@*B* recep!or. . 6

).+)$*-. + me!a+o%i!e imipeem ($%ac!am

ri !1"%9 ).%' +-

MUPY Rx38


198/705


mipeem +-7!%& meii!i"' imipeem *7#+- - meropeem-- !*+-. high. +ose"enicillins% 8e*e"ime mi"enem

MeropenemO COOH

ENH3C F S

H H CH3 CH3

OH N N

CH3

M$)4"$#$ O

"#!he!ic car+apeem

"!5!3 chira% me!h#% rop !4 ()! `$me!h#% rop $*!%G

1" h#'ro%#"e'# /P$1 )1-!4..*%&' i%a"!a!i

'1" *# $%ac!ama"e /+0F

.'' )-%&=(1$2H 8 hr)

rtrapenem

r!apeem

me!h#% rop !4 - Meropeem *$' /P$1 )1!4. . *%&' i%a"!a!i

i'e chai !'*,'+#%'.#%'*!%&

""!ai re%ea"e 4%%' )1$.(1 /)

%& r!apeem !' Meropeem mipeem !' 3$4 $ 5%, 80F .'$"%+ me!a+o%iAe' %, 10F

)'%-6"%>!.'/+0F-$ Car#apenems

-$

-mipeem ! M '* ()!' M*E!rep!ococciE i"!eriaE E.*aecalis


199/705

Meropeem r!apeem /+0 '++.''

*UY P*RM*Y


200/705

nti.iotics 87

-$

-Meropeem r!apeem mipeem'' mipeem Meropeem F Pseu+omonas .'r!apeem

F Pseu+omonas.. .

1F


201/705

MUPY Rx38


202/705


II%/+0'(

Po$'m'=in B Co$istin

8po$'m'=in E;

C4(!# AL-L$%

@L-D+

@ L-D+ D-&'$ D-L$%

L-T') @ L-D+

&4(*# B-L-D+

@L-D+

L-T')

@L-D+

O

%& c#c%ic ca!ioic po%#pep!i'e"

'e!ere!"E M? S 1E000 #%& $

2E4$'iamio+!aric aci' (

hep!apep!i'e !ripep!i'e)#

Po%#mixiB amio aci' %& /$

Phe E o%i"!i * %& /$e

zzznwzr}

,'+ 'e!ere!" /+0#*

%B+++ pho"pho%ipi'"( #

- !%&%L #.%% pho"pha!e rop pho"pho%ipi'" !+,

! ( **(

6+%'+.%

CH3

CH3

/+0*= aero+ic m ($)

-^=> 902;6


203/705

po%#m#xi B ! !oxic " )-%&


204/705

nti.iotics 71

+ramiciins

1 2 3 5 / . 8 9 10 11 12 13 1 15 G(* A(+ L$% A(+ V+( V+( V+( T)" L$% T)" L$% T)" L$% T)"

OH

NH

V+(#$-G)+6# A> = L-V+(#$ HO

I!4($%#$-G)+6# A> = L-I!4($%#$

.-$J9:;KK= H0\;= !*-%&%&% ramici'i" 4 -+6"

zzznwzr}

*permea+i%i!# ce%% mem+rae -$.% ramici'i" '.%"

-$ ce%% mem+rae '(he%ica%) *+2,!%&"(pore)

6ca!io !*%& '*-+'!6(.

'/+0 +aci!raci /+0' m(L) +ac!eria $!-

.-(+(- m ($) ..6)

-=


205/705

MUPY Rx38


206/705


III%$#%'

$#%'2.6ri#osome su#unit

?1 Aminog$'cosies

# amio%#co"i'e" +!#! a%#coe(*

') moo 'i"acchari'e !%&% amio%#co"i'e"

H2N

/

HN1

NH OH2

/H

2N

1HO OH H NH22

H3CHN2

HO N HO NH2 HO/ 1

NHCH3OH3

5 HO HO NH 5 OH

3 5OH

3

S)$"6#$ 2-D$4*!)$"+#$ S"$#+#$

@N,N'-D$'*(-2-$"!)$"+#$

,'+$

5$#%'-$ # 30ri+o"ome "+i! ()!%& +ac!erio"!a!ic eec!

*ce%%

P* (po"! a!i+io!ic eec!) /+0")! '* M

b


207/705

*UY P*RM*Y


208/705

nti.iotics 73

""0 6 - M

a

/" P $ #P

#! /! ! ( !/ ) 0 6permea+i%i!# $ # ! -! $ #6 ("

$ - 0 ce%% 00 -- ! /" ( perip%a"mic "pace " c#!op%a"mic mem+rae

00 #/ ce%% - " e%ec!ro !ra"por! 6

# e%ec!rochemica% ra'ie! 6 0

ce%% #

# ce%% h#'ro%#"i" *P e%ec!rica% po!e!ia% / $

$

b


209/705

MUPY Rx38


210/705


$ +. 3 .

%!% p!a-e%!% +i'i "i!e" ri+o"ome

en;ymes (%& .!! ) %!%# . 3$ace!#%a!e (*$amio%#co"i'e ace!#%a"e)@$pho"phor#%a!e (*P$amio%#co"i'e pho"phor#%a"e)

@$a'e#%a!e (*G$ amio%#co"i'e c%eo!i'e !ra"era"e)# eA. *%B+++ amio%#co"i'e 6 # +%!.% ! %G 7 * /+ 02 (!$G@ *%& ' /+ 0) #.%+%B+

++!'* ' 4"%

OHO-+6$#*(+$

O

N-+$*(+$ 1 N-+$*(+$HO 5

3 2

NH2H2N OH O 1

O 5/ NH2N-+$*(+$ HO

2 1 3 25

O H2NHOHO 3

OH

O-+6$#*(+$ +#+*# A N-+$*(+$

O-&'4!"'4)*(+$

'/+0'

arro< "pec!rm %& +ac!erici'a% !/+076'-$"% %&5 $-+!'-

ox#e -+-ox#e 7(!ac%!a!i,e) 6'-$ !ero+ac!eriaccaeE

P"c'omaa"

"pp. (- Ps.aeruginosa)E aemophi%" "pp. %&' 6'

-+$ 6ta"h aureus(MA6


211/705

*UY P*RM*Y


212/705

nti.iotics 7'

*A!reoam (moo+ac!am)E mipeem (car+apeem")E

x!e'e'$"pec!rm peici%%i"E x!e'e'$"pec!rm

cepha%o"pori"E %oroHio%oe"

*-

- $.62!'-$ T70M7


213/705

MUPY Rx38


214/705


.1"%!%)1"%:()'% 'o"e 6"%>#.') #

6#" "%!.%!% 98V99Frea% c%earace %,

2I3 c%earace 1""(). )!-+'!!!.')

1) 300$700hr".

)!-+'3 *- 4 15V30 .%

* ce%% $ $pha"e ( 'i"!ri+!i,e pha"e) df15 V 30

b


215/705

*UY P*RM*Y


216/705

nti.iotics 7

%+2'" (7toto*ic)

+)$=!%,!9 2()!6' . +'

1* % coch%ear I,e"!i+%ar . #

peri%#mph ch'o%#mph "-$#() " . - 4 ()!1"" ()

" . - +% &+2' ". )$ (6"% >#.')+%&+2'"

. %'+ ) +2'"$. I J %&%'+

+2)$peri%#mph - $ cm%a!i,e 'o"e

Geom#c% +2!()!1*++2. . #+#=6"% > (!

%: ro"emi'e ,acom#c%E E . " '! .+%'+)

'+'6--+ #7,!% &+2' I J % &%'+

+2'' (,e"!i+%ar !oxici!#) =+!%

321V2 '!. +1 %,$2 % '")#

. !'.% oc" )$#"!am" 1'"! )$7

" propriocep!i,e -''=$.%+$#

6" % > . ' 1 +!*+#((' " !

--()!6" % > )$'


217/705

MUPY Rx38


218/705


/+0$!ace!#%cho%ie %%#$6 %%(

6*/+0 ace!#%cho%ie !po"!"#ap!ic recep!or ()!!%/+0

erom"c%ar c!io $eom#c% )/+0$!pre"#ap!ic !

amio%#co"i'e" *++2'$. . #+7'%G. $*.#--4 20V30 . - +/+0$'

$ .*. ca%cim%coa!e

eo"!imie e'rophoim ()!%&!$.( ace!#%cho%ie"!era"e +


219/705

nti.iotics 77

"$- - ! 1 -% & "$ / - - - !"

/$ ! # /-! /$ -

Mai!eace 'o"e "$- &/"-! #3 !(&/ "

+ %"

- - crea!iiec%earace

!" $- % !"# !"## -!

$/ia%#"i" &$" -!- # 0#1

+ # # # "# 1 60

# 1 - P*

# *mio%#co"i'e" " B$%ac!am a!i+io!ic #

chemica% icompa!i+i%i!# 6$# 4 +, #1 2

icompa!i+i%i!#

!;G$ac#%a!io

c

amio%#co"i'e"

"/car+o#%

B$%ac!am ri

1

- 0 2 # .$7 # # "( 7 (# M

" amino!lycosi'es

" /% - 5

!rep!om#ci

>aam#ci - -aam#ci *E -aam#ci BE ami-aciE !o+ram#ci

MUPY Rx38


220/705


& T70M7


221/705

*UY P*RM*Y


222/705

nti.iotics 161

nwn? ~x|znwzr}naminog$'cosies3

Organisms +enera$$' S"sceptib$e to Aminog$'cosies

i09V3M G i bO

G^^ aT]

a60


227/705

]0RM


228/705


GHH0\;9;


229/705

L9=0W ;VVW;9KR M0;


230/705

nti.iotics 16'

4 Doa'in! 'ose9 maintenace 'ose 1"

amino!lycosi'es # #0 / #3 (creatinine clerance

+. )

"ru!a "aily Maintenance"ose

"esire' 6erum Concentrations(u!ml)

Doa'in! "ose Total "ivi'e'

asPea& Trou!

h(m!&!) (m!&!) (m!&!)

@e!amici

2 5.1 1.7 H 8 hr 4$10 1$2

o+ram#ci

2 5.1 1.7 H 8 hr 4$10 1$2

Ge!i%mici

2 6 2 H 8 hr 4$10 1$2

*mi-aci

2 15 7.5 H 8 hr 15$30 5$10

!rep!om#ci

&H

2 15 7.5 H 8 hr 15$30 5$10

*%% 'r"E ic%'i "!rep!om#ciE ca +e i,e im or i,.

Maximm 'ai%# 'oe". 2.0 . ca a'mii"!er 1.0 im (or i,) 'ai%# or

!+erc%o"i"

31 Tetrac'c$ines

"+2 .2 -..

OH O OH O O H10 11 12

OH1 H H O

2 O OO O9 C A NH2

O

D B 3 NH28 OH

. / 5

N

H

OH "+1 298 - 39H3C H3CCH3 OH N H

T$)+*(#$ H3C CH3 "+3 91 - 9.H

"


231/705

%

re'ce' aph!hacee ri

! ampho!eric compo' p>a 3 2.8$3.4E 7.2$7.8E 9.1$9.7

i"oe%ec!ric poi! p 5

0 ! +a"e $4$ $'ime!h#%amio moie!#

6 chira% ce!er 4E 4aE 5E 5aE 6E 12a

MUPY Rx38


232/705


H H HO O O OO

O NH2. / 5

OH

H

R

1 R2R

3 NM$ M$

$ene#%& na'e T#a(e na'e )*1 *" *3

T$)+*(#$ A')4*# H OH CH3 H

S%*#T$)+(+#

D$$(4*(#$ D$(4*# C( OH H H

M#4*(#$ M#4# N@CH32H H H

S+#*(#$ H H H HO*$)+*(#$ T$))+*# H OH CH3

OH

M$'+*(#$ H CH2OH

D4**(#$ V)+*# H H CH3OH

D4)*

% aci'$+a"e

ca!a%#"!X

-

aci'$+a"e ca!a%#"! $# ()

zzznwzr}

aci'$+a"e

ca!a%#"!X

-

'o+%e

+o'

hi+i! pro!ei "#!he"i" %"" 30" ri+o"oma% "+i! 4+, ! +ac!erio"!a!ic "

Mioc#c%ie 6 ! %ipophi%ic -!"$ ce%% mem+rae %ea-

c%eo!i'e"

! +ac!erici'a%

Spectr"m N Inication

Broa' "pec!rmE +ac!erio"!a!icRecomme' # ei!a% iec!io ]ZK9VRW;9 709:Z


233/705

# 1 !ra,e%er;" 'iarrhea a>:


234/705

nti.iotics 16

+- %o< 'o"e - .!6+#$ >9:6l^0#.'.#.'%

Averse


235/705

6'": a !:" 7%&1*'17

8 %K E!e!rac#c%ie 6$+5"


236/705


6''.' !e!rac#c%ie *' +(E E '

-+ !e!rac#c%ie *+ aAo!emia ( 'ox#c#c%ie mioc#c%ie) .%

$ pro!ei*+ amio aci' (.%-) )BUG

)$ prea!


237/705

H9V966;;E !$'e!rac#c%ie

*',er"e eec!" %E .E E %E E '+-$(E

hrom+oc#!opeiaE +! hepa!ic eA#me"E +,!=

%&= '.%! 1*E %E *.E " "erm !4 -!# 100m "i%e 'o"e

*UY P*RM*Y


238/705

nti.iotics 167

- &/ me!a+o%i!e %" " /! $

## e!rac#c%ieE 3 ) E . . E / -

/ #" ;6k6_9) a!i+io!ic"

! - +ac!erio"!a!ic +ac!erici'a% " coc.

# #$ " ,ir"! "! re"er,e $ " %

ir"! choice # 1 !#phoi' a' para!#phoi' e


239/705

ih%# %ipophi%icE ora% B* 90FE 1o@3 hr

MUPY Rx38


240/705


*+"or+e' - # coc. /# G - " (meii!i")

&/ me!a+o%iAe' " %"" %coroa!e pare! 'r

me!a+o%i!e &/" rie (hepa!ic me!a+o%i"m & rea%excre!io)

# %coro#% !ra"era"e & / me!a+o%iAe 0# p%a"ma

coc. @ra# +a+# "#'rome] (a"he ra# c#ao"i"E E

re"pira!or# 'epre""ioE h#po!e"ioE "hoc-) - # # %7

2


241/705

- # /0/ ! /7 1 /

*UY P*RM*Y


242/705

nti.iotics 111

Je 'ru!

Thiamphenicol

%& me!h#%"%o#% aa%oe ch%orampheico%

/+0 ch%orampheico%. * ' . *

ch%orampheico% '!. * +ap%a"!ic aemia

%3- 2' ' +'- 2oorrhea

31Macro$ies

M+)4(6$ )#

O CH3 N@CH32 H3CH C OH

CH3

9 RO HO 3H3C 10 8 CH3 A#4!%+)

O O OHO 11

OHO CH3

12 HO. / O CH3

H C 13 OH 5 H3C CH3CH3

CH3 O OO3 1 H

5C

21 3 O

OCH3 H3CO 2

CH3

C(+6#4!$ ORH3C

NO

O H C OH

OCH33H3C

OCH3 H3C CH3

OH

#

ac!oe ri (Macro%i'e ri) !5 * car+o 14$16 a!om"!4 %ac!oe ri $%#co"i'ic %i-ae c%a'io"e 6 $%#co"i'ic

%i-ae

amio"ar./+0

/+0%& Bac!erio"!a!ic ()!/+0$#%' +ac!eria#

50" ri+o"oma% "+i! -! ,'+F-$%& !ime'epe'i

eec!

'F-$

/+0.6 +ac!eria ram L %&5 -T>90= !rep!ococc" "pp.EM#co+ac!erim

ram $ -+ -b> V6;62;7;= b> 2 :


243/705

MUPY Rx38


244/705


-#'+-$+!1.%(

+..$

%!%#%' 50""+i! *.1..(e"!era"e ()!* %ac!oe ri

ac!i,e ex +!(macroli'es %& 2eera!io

ir"! eera!io - r#!hrom#cieco' eera!io - Roxi!hrom#ciE %ari!hrom#ciE *Ai!hrom#ci

/iri!hrom#ci

%1 rythromycin

OCH3

RON@CH32

9 8

H3C10

CH3HO 11

O OCH312 HO. /

H3C13 OH 5

CH31

H5C2 1 3 O OCH3O 2 CH3

O H3C

OH

OCH3

H

O9

HO. /

OH

O1 2O

O

%& a!ra% pro'c! .T70M7


245/705

-.6 ram L %&5 - !rep!ococc"E !aph#%ococc" ram $ -+ -b> V6;62;7;= b> 2:


246/705

nti.iotics 113

!+ioa,ai%a+i%i!# '*ha%$%ie $)% 4 $I n!

*/R: * +'+- !. *

'(cho%e"!a!ic hepa!i!i")

#="%e"!o%a!e/r i!erac!io: !'$po!e! YP3*4 ihi+i!or *'+!)$

- !heoph#%%ieE car+amaAepieE !erea'ieE 'ioxiE


247/705

MUPY Rx38


248/705


%ari!hrom#ci ! er#!hrom#cio ++

o %2 $Io + 'r i!erac!io %&mi%' YP3*4

ihi+i!or

'/+0

A)ithrom'cin

HH

H3C10

N11

O1

N@CH32 - ''-$- r#!hrom#ci '/+0+!)$

HO '-$-+ M*E-TZ;2KK9 T9KV


249/705

0

O

OH eA#me +e!a$%ac!ama"e .'$ macro%i'e -+!4OCH3 - +ioa,ai%a+i%i!# - ha%$%ie /6

A-#'+-$3#- 1"i%e 'o"e - comp%ica!e'

re!hri!i"E cer,ic!ri!i"E 6+

*Ai!hrom#ci ! r#!hrom#cio '/+0'-$(Broa'er

"pec!rm)o ++

o % 1 $I. YP3*4)+ 'r i!erac!io.


250/705

nti.iotics 11'

znw|wsx

|rsxmacro$ie

r#!hrom#ci

Roxi!hrom#ci

&

%ari!hrom#ci& *Ai!hrom#ci&

Bioa,ai%a+i%i!# $ 72$85 55 37

a%$ie (h) 1.7 10.5 4.7 11$14

"!(I) 4 2 2 1

' .

@ "i'e eec!

"" YP 3*4 - "/r i&!erac!io&

- 0 @(L) 5 @(L) 5 @(L) 5 @(L) 5

X>MRK;6k6_9

X>;6k6_9 L>:97900Z9K;=

L>:97900Z9K;=J>H02W


251/705

me!a+o%iAe' 0 YP3*4 : - YP3*4

!( 50:50 - !" 'o"e #0/ /

0/ ! %" $-

MUPY Rx38


252/705


41Lincosamies

H3C CH3 H3C CH3

N N

NHCH3

NHCH3

O . O .

OH HOH OH C(

H

HO HO

O O

HO RO

S S

CH3 CH3

L#4*# @7R C(#6+*# @7S

R = H C(#6+*#

R = &O3H C(#6+*# "'4!"'+$

'$icom#ci - %i'am#ci

C$inam'cin

%& "emi"#!he!ic 'eri,a!i,e icom#ci # h#'rox#% rop

!7 % .c%i'am#ci #$ 2 '$' peici%%iE

cepha%o"pori =$!Be!a$%ac!am r. 1 -$ 2 '$.

%& amio aci' ' amio "ar%!"'#1""()@)$/+0' +ac!eria *%:-%icom#ci

zzznwzr}

%& +ac!erio"!a!ic$#%'.##(#!50""+i! (! er#!hrom#ciE

ch%orampheico%

=$.- 3 '$$)x|znwzr}

- -.-$ @(L) cocci (!rep!ococc" @r.*E T79MZRK


253/705

*UY P*RM*Y


254/705

nti.iotics 11

Pharmaco&inetics

,'+%& W;-:;K oppor!i"!ic aaero+e(-a!i+io!ic '!) +

P"e'omem+rao" co%i!i" 'iarrhea ( 1+ p"e'omem+rao"

").'

Ga"eaE ,omi!iE cramp"!e,e"$oh"o "#'rome (+)

+ /r i!erac!io" r#!hrom#ci Gerom"c%ar B%oc-i*e!"

!-

)$'*!+'+-$


255/705

/+0'-$ ac!iom#ce!e"E m#cop%a"maE P%a"mo'im "pecie"

MUPY Rx38


256/705


!6+2" )1"*- 7.-6"%>!peici%i" '+-$

$

7e, r"g

Streptogramins

. Qipri"!i L 'a%opri"!i

' 3:7 /+0%& +ac!erici'a%

./+0

Qipri"!i 50" ri+o"oma% "+i! e%oa!io

po%#pep!i'e /aopri"!i !'*4 '*!Qipri"!i #

*%! coorma!io 50" ri+o"oma% "+i! ! -Qipri"!i +i'i "i!e

)$ -2'+-$ R* R (acom#ci$Re"i"!a!

!erococci)

Lin)o$i

/+0'-$ MR*E$-$ R(./+0'-$

P"e'omoa" - !ero+ac!eriaceae)

!6 )*- a!i+io!ic '!-

'+ -$! .''! $%& re"er,ea!i+io!ic]

ora% +ioa,ai%a+i%i!#100F $16"%>)$71%=%&+

. me!a+o%iAe !' '.6 YP450

.'%6""E 6"%>#.'E 6"%>#'

mi%'$!o$mo'era!e

$: % : +oe marro< *7'*!- 2 % )

moi!or '4 !!

,-%&*+ periphera% eropa!h#E op!icer,e 'amae %ac!ic aci'o"i"

. $ ir"! "!ep #%'(ii!ia!io)#%G

' ii!ia!io comp%ex ( %& +ac!erio"!a!ic )

/r i!erac!io


257/705

- M*" (! ieAoi' %&


258/705

nti.iotics

117

IV%

$

nu

cle

ic

aci

'

%"ino$

ones

Qio%oe"

%&

!.

#

'

7$ h%oroHio%oe#

'

7a$ii=ic$

aci()!

#

%& Gaph!h#ri'ie /+0$

-$.

-$

-2'+

-$+%:

'%:-!

4

%

a% %ie $

Pro!ei +i'i "

6

7


259/705

MUPY Rx38


260/705


%+,(+.% .1$*.(. .*.1

%$ . '+!!")$ %!-+6'%


261/705

Ga%i'ixic

aci'

1000 20 $40

1.5 90 3 Rea%

GorDoxaci 400 1.5 3 15 30 Rea% &epa!ic

iproDoxaci&

500 2.5 4 40 20 V 40 Rea% & @

*UY P*RM*Y


262/705

nti.iotics 121

omeDoxaci

400 4.0 8 10 65 Rea%

parDoxaci

&

400 1.3 18 40 10 Rea% &epa!ic

Doxaci 400 4.8 6 40 65 V 80 Rea%

e,oDoxaci

&

500 5.2 7 40 83 Rea%

@a!iDoxaci

&

400 4.0 9 20 74 Rea%

@repaDoxaci

400 1.4 50 8 8 epa!ic

ro,a%oxaci

300 2.5 12 76 6 epa!ic

MoxiDoxaci

&

400 3.1 13 50 19 epa!ic

@emiDoxaci

320 1.2 7 60 27 Rea% & e!c.

Bin' " "JBin' " n;yme

%

Bin' "

n;ymeR 5 O O

+,-a

#

)


263/705

MUPY Rx38


264/705


Ph'siochemica$ properties

COOH !'* !3 ''. 1 g 5.4 $ 6.4 + $+o' >e!o rop !'*

9!4. !Heterocylic ring !'* !7: p>92 g 8.1$9.3 * " "%jQ;770;


265/705

JH39 CH4: Q Pro%oa!io

- /

Potency@ JH3O 7H O

CH4

O H

! #)$" )!-

6"%>!%'+Qpro%oa!io .!+!Q i&!er,

a%

- i"apri'eE

r#!hrom#ciE*mi!rip!#%ie # @repaDoxaci ('*!

5 %& E) *6"%>-+')1"1

**UY P*RM*Y


266/705

nti.iotics 123

0

Fluorine : ')$ $$$$$

.G)$ 6()$

-6-

FluoroquinolonesQ

0 Heterocyclic rin! ,/<

Pipera;ine9 Pyrroli'ine: # G

Piperazine, Pyrrolidine L /

! J

%'+ # @*B* Rc

-!'+Azabicyclic - : %& +' % - ()3

6'.( "

CN toxicity

@ Pipera;ine9 Pyrroli'ine .

6"6 "!O"!

"rin! : $# 4+, $- G*/"

-."" !6(

&//6 &/NA!"s toxicity@ @ Pipera;ine9

Pyrroli'ine

.()$ *)!-+')$ "!O."!

Pipera;ine9 Pyrroli'ine !.1"

!:$

YP1*2 *heoph#%%i&e ")$

%&'. $ aei&e #

+!)$

0 F9 CH47 : " *aero+e" &//6 +%B+++'6+ - 6!

E


267/705

#""-6 0 6 "

!!% omp%ex ' .* "() )

%!.#%++


268/705


.#6" 1 *%& '

Qio%oe" -!# %! 03 H %& " !!"

'* !92 %& !@/+0

1 . '# %& ()!' %, 10 %K #

+, '/+0%&

Euinolones 1!

%: - '/+ 0/+ 0=. !-+

a670


269/705

*UY P*RM*Y


270/705

nti.iotics 12'

-2'+-$::M6V


271/705

MUPY Rx38


272/705


DomeNo*acin

%orie 2 " !'* 6 8 '* !7 %& $me!h#%$

piperaAie * 1"me!a+o%iAe )$ ha% %ie ))$ $

)

- *'+-$!*+)$ = $%G

'+-$ 6 ' +%: o %orie !'* 8 * #+ Pho!o!oxici!#

omeDoxaci

o Bioa,ai%a+i%i!# 95 F

2.4 7No*acin

+! 1E4$oxaAie .%! '* !1 8 * /+0'

)$ 6 $!' 4. )$

o /+0' GorDoxaci ' .

G G

G X

Bioa,ai%a+i%i!# (Bioa,ai%a+i%i!# 95 F)o-2#'+-$+ # %

e,oDoxci " Baci%%i 1 " Doxaci oorrhea E ch%am#'ia

o ''* 3*+ &a&!iomer ()!()$ /+0'.(R)$

1) 8$125 2.5 DevoNo*acin

o '* R7Me!h#% *6 G .o '*!%& hira% car+o Me!h#% ()! po%ariAe %e,o$

o - 2 Re"pira!or# i&ec!io&" *c!e exa cer+a!io&" ochro&ic

+ro&chi!i"E *c!e +ac!eria% "i&"i!i"E comm&i!#$ acHire'

p&emo&iaEo o"ocamia% pemoia

-%G2ra,e%er;" /iarrheao %& *%!era!i,e choice ooococca%

re!hri!i"E roei!a% ch%am#'ia% iec!ioEuinolones 2!


273/705

/+0 " a!#pica% pa!hoe 2 $

/+0.' - cocci -T>M6VMRM;W0V;W; =

T>90=

*UY P*RM*Y


274/705

nti.iotics 12

- 2 12#% -$ .

(commi!# acHire' pemo ia (*P)

.r $ %

='

G G

G

@a!iDoxaci

GatiNo*a cin

Me!hox# !'* 8 3$me!h#%$piperaAie ! '* 7 */+0 ' 6' a!#pica% pa!hoe& 2

3$me!h#%$piperaAi&e !'* 7*a% %ie )$ 9 -!#

o GrepaNo*acin %:1"1'.)%

pro%o Q i!er,a% !"!'* 5 %& me!h#%

Euinolones 4!

/+0 a!#pica% pa!hoe

Qio%oe" 3

/+0 !.-(+.J9:70


275/705

MUPY Rx38


276/705


+emi/o= acin

%&'!4 ()!#%& 1E8$ap!h#ri'ie#

''* 1 %& c#c%opropr#% *%


277/705

*UY P*RM*Y


278/705

Bacterial Menin-itis 127

BACTERIALME7I7+ITIS

*) . !( " + 4703056*) . * 1> 4903117

OUTLI7E

/GGP*PY@YG* PRG*GPY* *MG*G

Bru';ins&iSs si!n

Rerni!Ss si!n

Dum#ar puncture

P*RM*@ R*MG"e*amethasone

mpirical ntimicro#ial Therapy

2r !en Cephalosporins@ Ceftria*one9

Cefota*ime

Vancomycin

Car#apenems

Fluoro=uinolones

Cha

pter

>


279/705

" " - 6 -!

1% "7" (cutepurulent menin!itis)

|Streptococc"s pne"moniae: E1Co$i9Meningococc"s9Haemophi$"s in/"en)atype B

! 6 7 " ! # . %

( !" E /

" E

" ) 0

% 0/ ! /" % / & %

0/ ! %* 1 % ) !

MUPY Rx38


280/705


% "(% (Tu#erculous menin!itis)

(%6 ! % 0

% ! ! 0/ !

$# "- #.0/ #3 /% " # . 1$5 !

2% "- (Viral menin!itis)

/ E a670


281/705

. ("!ie"" o ec-) %! (cha% rii'i!#)

*UY P*RM*Y


282/705


Ph'sica$ e=amination

Bru';ins&iSs si!n # 0(L)

+ : # 0/ ! *1& " 0/ ! - 0 (L)

Rerni!Ss si!n # 0(L)+ : # 0/ ! " 0 / % # %

7"" - # !

# # 0/ ! - - . " - !& & - 0"

XXX$- (Dum#ar puncture9 DP) 6 !

$ #- "+arachoi' "pace 0/ !

# $#$ %m+ar pc!re -

0/ ! .

)/ "

! %""!

oca% ero%oica% 'eWci! (pa%"# o craia% er,e - - ! $ P

Papille'ema

0/ ! 0/ #3

)/ " (E*/"E immo"ppre""i,e ae!"E !ra"p%a!a!io)! %""! :ma"" %e"ioE "!ro-eE oca% iec!ioGe< o"e! o "eiAreoca% ero%oica% 'eWci!*%!ere' co"cio"e""Papille'ema

Papillede$a "

0/ ! # (icrea"e' i!racraia%

pre""re) & $ m+ar pc!re 0 /

+rai heria!io -

! & papi%%e'ema $ P & - papi%%e'ema

$ P - 0/ ! $ P

XXX $$B%oo' c%!re" #/exame!ha"oe L empirica% a!imicro+ia% !herap#

$ "ca *1

0/ ! - $ P B%oo' c%!re" $ P # /exame!ha"oe L empirica%

a!imicro+ia% !herap#


283/705

MUPY Rx;38


284/705


Da#oratory Tests@ $-

: P (ope&i&

pre""re)

: 200$500 mm @

?B : 1000 V 5000 ce%%"ImmE

@%co"e : T 40 mI' ('* 1I3 %co"e)Pro!ei :

Pharmaco$ogic treatment

"e*amethasone /o"e J 0.15 mI- H 6 hr 2$4

Geoa!e" ( 1 ): - $# #'exama!ha"oe -

*1 'exama!ha"oe /#. 1 -

a!" (1 1 !) I hi%'re (1$12 !): & X>;6k6_9!#pe B (m (V) ro') # #'exama!ha"oe

*'%!" (12 ! -!): T>M6V


285/705

mpirical ntimicro#ial Therapy

|r nrstS1pne"moniae *ancom'cin 6 Ce-tria=one 9

Ce-ota=ime

H1in/"en)ae Ce-tria=one 9 Ce-ota=ime

a>:


286/705


- -$! !-

1 T>929K9:7;9 a>:M6VV6;62;7;W;=

'anco$y

cinL e!riaxo&e I

eo!axime

T>929K9: X>;6k a>:V6;62;7;W;=

T>M6VV902;6


287/705

$ ((F-$ #= PRP (Peici%%i$re"i"!a!T708M7


288/705


/ rea%c!io 0/ ! % / crea!iie

c%earace ( & %:0 S 60 m%Imi & !- !"*/R: rea% ai%reE h#po!e"ioE eo"iophi%iaE XXnephroto=icit': ototo=icit':

Re man s'nromeXX

)Re man s'nrome # ,acom#ci .-! %- " ,acom#ci i"io - 6

!! hi"!amie % ea!i,e

io!ropic ,a"o'i%a!a!io 0 hi"!amie

/ i"io -! !( 2$3 .

! Re' ma "#'rome $- % i"io ( 1 %) # a!ihi"!amie

1 Re' ma "#'rome $- %# a!ihi"!amieE cor!ico"!eroi'" Di'

Carbapenems

M*: " +ac!eria% ce%%


289/705

% !Bac!eria% Meii!i" #


290/705

Upper Respiratory


291/705

Common col' ( .)

n|

#+'+-$.!.%3 6-$ rhio,ir" %&'!.

! ()!.$.%'"!!+*+*!()!!

chemica% me'ia!or" !*5 +ra'#-iiE pro"!a%a'iE hi"!amieE i!er%e-iV1 ero%oic reDex

(.E )

MUPY Rx38


292/705


,71 %K!.'*4 *"4.'*"4"" '""

'*#'+,''+-$ 6tre"tococcus grou" :' 1$4 -$.53 -+ *E BE

." 4 4 %!'$ % ! 2$4.%&"

4 . %&"1$4 %''.5.

. .."(25%,/4.

@C) .'*4

4 4 44

%!''4 %!''


293/705

(''EE7) /".

7 .47 .4

#U,RM#Y


294/705

Upper Respiratory $": Bir >$"

$

!% !( ! ! - E ) /

,ir" iDeAae !#pe *E BE !#pe * ! " #!2547 !#pe *

5G1

!-E - ." $ /- ! #. #$" #

# 4V10 ! -! ! $##--# #

2V4 ! 7( & # )

- - " #$ "

! 0 !% 7 ! *#/ I$x - I 0 !

1 #)# 48 %

"e%!amirir 75 m +i'E aamirir 10 m +i' 4+, " eramii'a"e*ma!a'ie 100 m +i'E Rama!a'ie 100 m +i'

!

#"e%!amirirE ama!a'ieE rima!a'ie - 0 70 V 80

#,accie - #3#( - ! -!- + !

""!--

- #3+#..+

,ir" iDeAae (1G1) 1G1 " ! -0 /

( J L/L) & /- - " - "! / ! - !

-7 6 -#3

- -!0 / !#3 1 - 0/! % "

"- o"e%!ami,ir )# 2 ! # 0 10 / ! 0/ ! % %! %# %" 0 / )// // ///////// ( $ 0 65 !) .. (

5 !) 3 ) 0/ )


295/705

MUPY Rx38


296/705


nwznnnznw

1% - - # Parace!amo%E *"piriE +proe # -

Paracetamol !

+proe # 7- / 39 - - parace!amo% - # #. T6 ( ! -

#


297/705

Antihistamine gen&3 $# 0 # - 4+,

! a!icho%ieric !erea'ieE a"!emiAo%e ! "&"

Antihistamine gen&4 - $# 6 0 - 4+, a!icho%ieric %ora!a%ieE

exoea'ie

#U,RM#Y


298/705

Upper Respiratory


299/705

ripro%i'ie (*c!ie'

a+%e! !" ripo%i'ie 2.5mLP"e'oephe'rie 60 m) Preac# a!eor# *DoseB 1 !a+. !i'

MUPY Rx38


300/705


h%orpheiramie: Preac# a!eor# Brompheiramie: Preac# a!eor#

* DoseB 4 mI!a+. 1 .

3

2% " / (Jasal

'econ!estants) /

6 0# "

"$# h#peremia ""& /

-ii me'ia!or" &/ # " "& ! #..$# " # "

"" # $# # ""

## %/ /

" " 4+, -2

*!ihi"!amie"#mpa!homime!ic 'r" 6 " # - ! ra%'ecoe"!a!" opica%

'ecoe"!a!"

" % -

- !ha&o%ami&e $

PiperaAi&e

- !h#%ee'iamie

$Phe&o!haiAi&e

- *%-#%amie $Piperi'ie


301/705

- !her

#U,RM#Y


302/705

Upper Respiratory


303/705

mi'aAo%ie 'eri,a!i,e": GaphaAo%ieE e!rah#'roAo%ieE x#me!aAo%ieE

#%ome!aAo%ie 4+, 4+, $

phe#%e!h#%amie 'eri,a!i,e"

" #

MUPY Rx38


304/705


?1 Topica$ econgestants % ' 5 '1.1 *r#%a%-#%amie"

phe'rie $ %: . +-

Phe#%ephrie $%& !%++


305/705

4.+ reboun+ congestion 4

.

.* reboun+ congestion

(!"+/+0)

#U,RM#Y


306/705

Upper Respiratory common col+.6$opica% ra% 'o"e 6"%> acute rhinosinusitis .6$opica% ra% 'o"e

7.-7'* 2 %K

*-0.9F Ga% "I -.%*-*""-

-6"%># ##+'"!#

?#'.6+%'+ "'" '"#' 6"%>!.

ric#c%ica!i'epre""a! 6"%>"

.- M*$ !*+"$ .-6"!$

**7 2 %K .-

".-+ 3$5 + rhii!i" me'icame!o"a

/ M*"

Documents

Manual of Pharmacotherapy 1 (Rx 38)