KHNG SINH TNG HP

sulfamid khng khun

LCH S TM RA SULFAMID Ngay t nhng nm u th k 20 cc nh khoa hc nhn thy rng cc phm nhum c tc dng khng khun , tuy nhin cc phm nhum thng rt c. Nm 1913 ngi ta tm thy phm azoic cryzoidin c tc dng dit khun v tng i t c.

H2N

N N NH2
Azoic cryzoidin
3

LCH S TM RA SULFAMID Khi c thm nhm - SO2NH2 trong cng thc cc phm nhum thng rt bn v gn cht vo protein. Ngi ta th gn thm vo phn t cryzoidin nhm sulfamido, v thu c mt cht c tc dng chng t cu v lin cu l prontosil

H2N

N N
Azoic cryzoidin

SO2NH2
Prontosil
4

NH2

LCH S TM RA SULFAMID 1935 Bovet v Trefuel pht hin ra rng prontosil khng c tc dng trn in vitro m ch c tc dng trn in vivo

In vitro

In vivo

LCH S TM RA SULFAMID Vo c th prontosil chuyn ha thnh cht khc c tc dng khng khun

Prontosil

LCH S TM RA SULFAMID Nguyn liu u tng hp protosil l p-aminobenzensulfonamid

H2NSO2 NH2 + NaNO2

HCl

H2NSO2

+ H [ N N ] Cl

p - aminobenzensulfonamid (Sulfanilamid)

NH2 H2N
m - phenylendiamin

H2N

N N NH2
Prontosil

SO2NH2
7

LCH S TM RA SULFAMID Khi thay th sulfanilamid bng amin khc cho sn phm khng c tc dng khng khun
NH2
anilin

+ NaNO2

HCl

+ H [ N N ] Cl
NH2

H2N

m - phenylendiamin

H2N

N N NH2
8

LCH S TM RA SULFAMID Khi thay th m - phenylendiamin bng cht khc cho sn phm c tc dng khng khun
H2NSO2
Sulfanilamid

NH2 + NaNO2

HCl

H2NSO2

+ H [ N N ] Cl

OH
phenol

HO

N N NH2

O2SNH2
9

LCH S TM RA SULFAMID
Bovet v Trefuel th v thy sulfanilamid c tc dng khng khun trn c in vitro v trn in vivo. Ngoi ra sn phm acetyl sulfanilamid xut hin trong nc tiu

sulfanilamid

H2NSO2

NH2

CH3COOH

CH3CONH

SO2NH2

10

LCH S TM RA SULFAMID

Sulfanilamid tr thnh sulfamid u tin trong lch s. Vic pht hin ra prontosil v sulfanilamid m ra mt k nguyn mi cho vic ha tr liu cc bnh nhim khun. Da trn cu trc sulfanilamid ngi ta tng hp rt nhiu sulfamid trong khong 40 loi c s dng lm thuc.

11

LIN QUAN GiA CU TRC V TC DNG DC LC

R2NH
Thay i trn N4

SO2NHR1
4 1

N lun lun phi v tr C4 ( para vi SO2NH ) N lun lun phi gn vi nhn thm NHR1

R 1NH R2 NH

R2NHCH2

SO2NHR1

R1NH Sulfamylon

NHR1

12

LIN QUAN GiA CU TRC V TC DNG DC LC

R2NH

SO2NHR1
1

Thay NH2 C4 bng nhm khc u lm mt tc dng nhng nu thay bng NO2 vn cn tc dng nhng c

O 2N

SO2NHR

13

LIN QUAN GiA CU TRC V TC DNG DC LC

Thay i trn N4 N lun lun phi t do

COOH
OH CO HN H2N
S N
Ftalazol

NHSO2

Sulfathiazol

14

LIN QUAN GiA CU TRC V TC DNG DC LC

Thay i trn nhn thm Khi thay th nhn benzen bng cc nhn khc u lm gim hoc mt tc dng nhng c th to ra cc tc ng khc. Mi s th trn nhn u lm gim hoc mt tc dng.

R2NH
R

SO2NHR1
R

15

LIN QUAN GiA CU TRC V TC DNG DC LC

Th nhm sulfamid Khi thay nhm sulfamid bng cc nhm khc u lm gim hay lm mt tc dng. Khi th H bng cc nhm th mch thng ni chung lm gim tc dng tr trng hp sulfaguanidin v sulfacetamid th bng d vng cho tc dng tt. COCH3

NH

H2N
Sulfaguanidin

SO2NH R
N

NH2

Sulfathiazol Sulfacetamid

16

iU CH SULFAMID
i t anilin Bo v nhm amin

NH2

+ (CH3CO)2O +
HCOOH

NHCOCH3
NHCOCH3

NH2

NH2

+ ClCOOC2H5

NH COOC2H5

17

iU CH SULFAMID
clorosulfon ha

H2N

H + HO SO2 Cl

H2N

SO2 Cl

To nhm sulfamoyl nh tc dng ca NH3 hay RNH2

NH3
H2N SO2 Cl
RNH 2

CH3CO NH

SO2NH2

CH3CO NH

SO2NHR

18

iU CH SULFAMID
Thy phn gii phng sulfamid

CH3CO NH

SO2NH2

HCl

NaOH

HCl.NH
NaOH

SO2 NH2

H2N

SO2 NHNa
HCl

H2N

SO2 NH2

H2N

SO2 NH2

19

iU CH SULFAMID
i t clorobenzen

Cl

HOSO2Cl

Cl

NH3

Cl
NH3
200oC

NH2

80 at
SO2NH2

SO2Cl

SO2NH2

20

iU CH SULFAMID
i t cc sulfamid c sn

H2N

SO2NH2

+ H2N C

NH NH2

H2N

SO2 NH-C

NH NH2

Sulfanilamid

Sulfaguanidin

H2N

SO2NH2

(CH3CO)2O

H2N

SO2NHCOCH3

Sulfanilamid

Sulfacetamid

H2N

SO2 NH-C
Sulfaguanidin

NH NH2

HC OHC

H2N

SO2 NH N
Sulfadiazin
21

TNH CHT SULFAMID Tnh cht ha hc Tnh acid

O
H2N SO2NH2

O H2N S=NH ONa

H2N

S=NH OH

Cho ta mui Ag, Cu, Co

Tnh base
HCl

H2N

SO2NH2

HCl. H2N

SO2NH2
22

TNH CHT SULFAMID Nhm amin thm cho phn ng diazo ha thng dng nh tnh v nh lng
H2NSO2
Sulfanilamid
OH

NH2 + NaNO2

HCl

H2NSO2

+ H [ N N ] Cl

H2NSO2

23

TNH CHT SULFAMID Nhn benzen cho cc phn ng th c th p dng nh tnh hay nh lng

SO2NH2

SO2NH2
+

Br2
Br NH2 Br

NH2

24

TNH CHT SULFAMID

Nhm NH2 c th phn ng vi p-aminobenzaldehyd ( PDAB) cho sn phm c mu c th dng nh tnh v nh lng

H2NSO2

NH2

CH3 HOC N CH3

CH3

H2N

N=CH

N CH3

25

KiM NGHIM SULFAMID

nh tnh

cc phn ng mu sc k ph hng ngoi t ngoi

Rf

Th tinh khit Clorid Sulfat Gim khi lng do sy kh Tp cht lin quan

IR

UV

26

KiM NGHIM SULFAMID

nh lng Diazo ha

H2NSO2

NH2 + NaNO2

HCl

H2NSO2

+ H [ N N ] Cl

KI + h tinh bt

Tropeolin OO Chun th

Ch th ngai

Ch th ni

pp dng c

27

KiM NGHIM SULFAMID

Phng php quang

H2NSO2

NH2

CH3 HOC N CH3

CH3

H2N

N=CH
Mu vng

N CH3

Phng php quang

28

KiM NGHIM SULFAMID

nh lng sulfamid bng phng php acid-base NaOH 0,1N sulfadiazin, sulfacetamid ( acid mnh ) Natrimethylat 0,1N xanh thymol (CT) Cc sulfamid ( acid yu ) Chun mi trng khan Chun mi trng nc

dimethylformamid HClO 4 0,1N

Cc sulfamid ( base yu )

Tm tinh th (CT) Acid acetic bng

Chun mi trng khan

29

KiM NGHIM SULFAMID

Phng php kt ta

H2NSO2

NH2

AgNO 3

H2N

SO2NHAg

Cn

30

Lin quan cu trc tc dng: - Nhn thm, nhm sulfamid (-SO2NHR), nhm amin thm t do v tr para vi -SO2NHR - Nhm th cc v tr khc trn nhn thm lm mt tc dng. - R: c th thay i v lm thay i tc dng iu tr, c quan ch. iu ch: - T Anilin - T Clorobenzen. - Bn tng hp t cc sulfamid c sn
31

Tnh cht: - Tnh lng tnh: -NH2 cho tnh base; - SO2NHR cho tnh acid To mui vi KLN - Nhm amin thm bc 1: - Phn ng diazonium - To mu vi TT PDAB - Nhn thm: cho phn ng th vi - Khi t cc sulfamid khc nhau chy cho cn mu khc nhau
32

Kim nghim: - nh tnh - Kim tinh khit - nh lng - PP Diazo ha - PP quang - PP kt ta - PP acid base: - Mi trng thng - Mi trng khan
33

DC NG HC Hp thu Tr mt s sulfamid khng hp thu qua ng tiu ha v c s dng tr nhim khun ng rut nh ftalazon, sulfaguanidin a s cc s sulfamid hp thu nhanh qua ng rut. Khong 70%
H2N SO2 NH-C NH NH2
N H2N SO2 NH N
Sulfadiazin (hp thu tt )
34

Sulfaguanidin ( khng hp thu )

DC NG HC Phn phi - Sulfamid c phn phi khp cc t bo ca c th. - Sulfamid c th nhanh chng i vo mng phi, hot dch mt v cc dch tng t. - Kh nng thm vo mng no thay i ty thuc vo loi sulfamid; mc gn protein; mc acetyl ha v mc tn thng ca mng no. Th d: sulfadiazin vo mng no 17% trn ngi thng nhng trn ngi b vim no c th ti 66%. - Sulfamid thng qua c nhau thai.
35

DC NG HC
Chuyn ha Kh nng acetyl ha sulfamid ty thuc vo c a bnh nhn v loi sulfamid s9a vo c th
H2NSO2 NH2
CH3COOH

CH3CONH

SO2NH2

- Cc dn cht acetyl ha ca sulfamid thng khng c tc dng, tuy nhin mt s cht gy kt tinh thn. - Ngy nay ngi ta to ra nhng loi sulfamid t b acetyl ha hoc c dn xut acetyl ha d tan : - sulfamethoxypiridazin c t l acetyl ha 10% - sulfadiazin c dn cht acetyl ha tng i d tan
36

TAC ONG DC LC Ph khng khun Sulfamid c ph khng khun rng: Gr (+) : t cu, lin cu, ph cu, lu cu Gr (-) : trc khun l, thng hn, E.Coli X khun. Virus mt ht

37

C TNH SULFAMID c tnh trn mu - Ri lon h thng to mu do hin tng mn cm, - Hin tng tan huyt lin quan ti s hot ha glucose- 6 phosphat dehydrogenase. - Phn ng khng ph thuc vo nng sulfamid m vo tng c th v tng sc dn v thng xy ra trong tun u dng thuc. Triu chng c th l - Bun nn, st, chng mt, vng da, xanh xao trong trng hp nng c th l thiu mu bt sn. - Tm ti do to methemoglobin.
38

C TNH SULFAMID c tnh trn thn Sulfamid c th c th kt tinh thn gy tn thng thn, vim thn, si thn i ra mu. Nhc im ny c khc phc dn do tm c nhng sulfamid t acetyl ha, t kt tinh.. Cn ch : Ung nhiu nc Ung dung dch kim Khng dng cho tr em
39

C TNH SULFAMID Phn ng tng nhy cm - Phn ng ny rt khc nhau i vi tng sulfamid v vi tng ngi thng hay xut hin khi dng sulfamid tc ng chm. - Triu chng: c th l ni ban , xut huyt Khi dng ngoi c th gy nm da do kch thch s nhy cm ca da vi tia t ngoi

40

MT S SULFAMID KHNG KHUN CHNH Phn loi Sulfamid tc ng ton thn Hp thu tt qua ng tiu ha v khuch tn tt ti cc t chc trong c th. Nhm c chia ra thnh cc nhm : Sulfamid tc ng nhanh Sulfamid tc ng chm Sulfamid tc ng trung gian

41

MT S SULFAMID KHNG KHUN CHNH Phn loi Sulfamid tc ng ti ch t hp thu vo mu nn ch tc dng ti ch. Nhm ny c chia ra thnh cc nhm: Sulfamid ng rut Sulfamid ng tiu Sulfamid dng ngai

42

SULFAMID TON THN Sulfamid tc dng nhanh hp thu nhanh v thi tr nhanh nn phi ung nhiu ln trong ngy. t lin hp protein Thng l nhng sulfamid th h u D gy kt tinh thn o thi nhanh t tch ly nn tng i t c

43

SULFANILAMID

H2N
Ch nh

SO2 NH2

- y l sulfamid u tin trong lch s trc kia c coi l thn dc v c tc dng trn mng no cu, lin cu. - Hin nay t dng trong iu tr v c tnh tng i cao v b acetyl ha nhiu (80%). - Ngy nay ch yu c dng lm nguyn liu tng hp sulfamid khc.
44

SULFATHIAZOL
H2N SO2 NH N S

Ch nh

- Dng trong iu tr t nm 1940 v l mt trong nhng sulfamid c tc dng tt nht chng t cu, lu cu, mng no cu, ph cu. - t c. - D hp thu t nhanh nng cao trong mu. - T l acetyl ha khong 30%.

45

SULFADIAZIN

N H2N
Ch nh Sulfadiazin l mt trong s t sufamid cn s dng nay. t tan nhng hp thu nhanh v bi tit chm nhanh chng t nng cao trong mu. Trn invitro n tc dng km sulfathiazol nhng invivo mnh hn v t c hn
46

SO2 NH

SULFAMID TC NG CHM - Gm nhng sulfamid hp thu nhanh vo mu nhng tn ti lu trong c th. - C kh nng lin hp vi protein ln nn thi tr chm. - t b acetyl ha (10%) tin cho vic tr liu v ch cn dng mt liu duy nht trong ngy. - Cc sulfamid ny u c cha trong phn t nhm CH3O, mt nhm ny th khng cn tc dng ko di. - Cn thn vi nhng ngi nhy cm v thuc c th tich ly
47

SULFAMETHOXYPYRIDAZIN
H2N SO2 NH OCH3

N N

Ch nh - Hp thu nhanh v thi tr rt chm nn ch cn ung 1g / ngy. - c tnh tng t cc sulfamid khc nhng khi ng c th c im thi tr chm li l im bt li. - Nu th H ca -SO2NH bng -CH3CO ta c acetylsulfamethoxy- pyridazin khng ng thch hp vi tr em.
48

SULFADOXIN
H2N SO2 NH N N OCH3 OCH3

Ch nh Thi tr rt chm ch cn dng 1g / tun. Sulfadoxin + pyrimetamin FANSIDAR tr st rt

49

SULFAMID TC NG TRUNG GIAN - Hp thu nhanh v tc thi tr va phi phn tn u trong c th. - t b acetyl ha thng ung ngy 2 ln. - Cc sulfamid nhm ny thng c d vng 5 cnh. - Hin nay mt s sulfamid nhm ny cn s dng ph bin.

50

SULFAMETHOXAZOL
H2N SO2NH N O CH3

Ch nh

y l sulfamid c dng ph bin hin nay thng dng tr nhim trng ng tiu, nhim trng da. Bactrim c th thay th cloramphenicol chng thng hn BACTRIM Sulfamethoxazol Trimethoprim

800 mg 160 mg
51

SULFAMID TI CH Sulfamid ng tiu Ni chung c th dng nhng sulfamid trn tr nhim khun ng tiu. Ngi ta thng chn nhng sulfamid thi tr nhanh t acetyl ha d tan. Tuy nhin cng c nhng sulfamid chuyn dng tr nhim khun ng tiu. Nhm mch thng Nhm d vng: thng c nhm CH3 v d vng 5 cnh
52

SULFACETAMID
H2N SO2NHCOCH3

Ch nh - D tan trong nc hn nhiu sulfamid khc, nhanh chng t nng cao trong mu, nhng thi tr nhanh, t kt tinh . - Do thi gian tc dng ngn nn t c dng lm thuc khng khun ton thn. - Thng lm thuc khng khun ng tiu v to nng cao trong nc tiu. - Cn c s dng lm thuc nh mt tr mt ht. Mui Na d tan khng gy kch ng nim mc.
53

SULFAMID TI CH Sulfamid ng ruot Cc sulfamid nhm ny khng tan v khng hp thu qua ng tiu ha nn t nng cao rut v c s dng tr cc bnh ng rut nh t,l, vim rut. Trong s ny tr sulfaguanidin chuyn bit tr bnh ng rut, cc sulfamid khc u i t nhng sulfamid thng thng c gn thm nhng nhm chc lm cho cc cht ny khng hp thu qua ng tiu ha v tc ng ti ch.

54

SULFAGUANIDIN
H2N SO2NH C NH2 NH H2O

Ch nh y l sulfamid dng ph bin nc ta. Do t tan trong kim nn khng hp thu rut. t c nn c th dng liu cao . Tuy nhin sulfaguanidin c nh hng ti vi khun ng rut, nn ung thm men tiu ha v ung km B1
55

SULFAMID TI CH Sulfamid dung ngoai Ni chung t s dng cc sulfamid tr nhim khun da do s c mt ca PABA trn cc vt thng v s tng mn cm ca da khi dng sulfamid. Mt s sulfamid c s dng dng ngoi di dng thuc bt hay thuc m nh sulfanilamid, sulfadiazin. Mui bc sulfadiazin c tc dng khng khun rt tt.
N

H2N

SO2NH 2 H2N

SO2 N N Ag
56

SULFAMID TI CH Sulfamid dng ngoi Ngoi cc sulfamid trn c mt sulfamid chuyn s dng ngoi da v khng chu tc ng bi PABA l sulfamilon

NH2 CH2

SO2NH2

57

thuc khng khun nhm quinolon

58

I CNG NHM QUINOLON

Lch s Thuc u tin: acid nalidixic (negram), mt thuc khng khun tng hp tr nhim khun ng tiu bi vi khun Gram (-) t 1964.

59

I CNG NHM QUINOLON

O O O Y N X COOH

Cc quinolon th h I

ten thuoc acid oxolinic cinoxacin mibxacin

X H N H

Y H H H

R C2H5 C2H5 OCH3

60

I CNG NHM QUINOLON Cc quinolon th h I O

.

X R1 Y N R2
ten thuoc X Y N N H
N

COOH

R1

R2 C2H5
NH

acid piromidic N acid pipemidic N resoxacin H

C2H5 C2H5

61

I CNG NHM QUINOLON Cc quinolon th h I

.

- Cc quinolon th h 1 khng cha F (tr flumequin). - Hp thu km v chuyn ha nhiu gan thnh sn phm khng c tc dng. - Ph khng khun hp , ch c tc dng trn mt s vi khun ng rut v ng tiu: E. coli, Proteus, Samonella, Enterobacter, gonorrhea. - khng nhanh do hin nay t c s dng.
62

I CNG NHM QUINOLON

O F N R3 R2 R4 COOH

Cc quinolon th h II

N N R1

ten thuoc Perfloxacin nofloxacin Amifloxacin ofloxacin Ciprofloxacin lomefloxacin Enoxacin

R1 CH3 H CH3 CH3 H H H

R2 H H H H H CH3 H

R3 H H H H F N
O

R4 C2H5 C2H5 NHCH3

CH3

C2H5 C2H5
63

. Cc quinolon mi

I CNG NHM QUINOLON

O
O F N COOH

F N N

COOH

N H2N

O H3C
F

NH2
O F H N O H H3C

Gemifloxacin
COOH

Trovafloxacin
HN

Moxifloxacin

( Avelox)

64

I CNG NHM QUINOLON

Lin quan cu trc v tc ng dc lc

5 6 7 8 O 4 3COOH

2 CH C N2H 35 1

h thng pyridon phi ngng t vi nhn thm. - V tr 1 th alkyl ngn ( methyl, ethyl, cyclopropyl ) tng tc dng khng khun.
65

I CNG NHM QUINOLON

5 N O 4 N

6N 7

3COOH

N
8

N 2
1

- Vic th v tr 2 lm gim hay hy tc dng. - Vic th ng cu in t N cho C v tr 2 (cinnolin), 5 ( 1,5- naphthyridin) , 6 ( 1,6naphthyridin), 8 (1,8- naphthyridin) vn duy tr tc dng khng khun.
66

I CNG NHM QUINOLON

R R F

5 6 7 8

O 4 N

3COOH 2

V tr 3 bt buc phi l COOH V tr 4 Nhm C=O khng c thay i V tr 5,6 khi th lm gim tc dng Th F v tr 6 lm tng tc dng khng khun
67

I CNG NHM QUINOLON

5 6
N H3C N

O 4 N

3COOH 2
CH3

O F

- V tr 7 th lm gim tc dng tr s th nhn pyperazinyl hay d vng. - Thm nhm N-CH3 lm tng thi gian bn hy - V tr 8 c th th bng F cho tc dng tt. - Vng ngng t 1-8 cho tc dng tt
68

I CNG NHM QUINOLON

Ha tnh -Tnh bn: Cc quinolon u khng bn ngoi nh sng. - Phn ng kt ta: Quinolon base cho phn ng kt ta vi cc thuc th chung alkaloid. - Nhm acid c th cho phn ng to ester - Nhm C=O cho phn ng vi Natrinitroprusiat cho mu tm. - Phn ng to phc: Cc quinolon u c th to phc chelat vi cc ion ha tr 2,3 nh Ca2+, Mg2+, Al3+, Fe 3+ . 69

I CNG NHM QUINOLON

Kim nghim nh tnh. 1/ Cc phn ng to ta, phc, mu. 2/ Cc phng php ha l: ph t ngoi, hng ngoi, sc k lp mng, sc k lng hiu nng cao. nh lng Phng php mi trng khan : HClO4 / CH3COOH Tc ng dc lc - Fluoroquinolon c ph khng khun rng c bit c hiu qu cao chng vi khun Gram (-) hiu kh. - Hiu qu trong iu tr Staphylococcus aureus, nhng hin nay c s khng.
70

I CNG NHM QUINOLON

C ch tc ng. c ch hot tnh enzym AND gyrase , ngn cn qu dui xon chui AND, c ch s sao chp AND. T bo ngi khng cha DNA gyrase, nhng cha topoisomerase enzym c chc nng tng t. Fluoroquinolon ch c ch DNA gyrase liu iu tr; nng cao hn gp 100- 1000 ln s c ch topoisomerase.

71

I CNG NHM QUINOLON

Quinolon

AND gyrase 72

I CNG NHM QUINOLON

Phn ng ph - Fluoroquinolon tng i t phn ng ph v t c tnh. - Ri lon tiu ha: bun nn, au bng, kh chu - Ni m ay, d ng - Ri lon th gic - Tng s mn cm da vi nh sng mt tri - Nhng bin chng v sn thy ng vt cha trng thnh khi dng liu ln hn liu cho ngi do c khuyn co nhng thuc ny khng nn dng cho tr em di 16 tui
73

I CNG NHM QUINOLON

Ch nh. - Tr norfloxacin, do kh nngsinh hc km khi ung, nn ch hn ch trong iu tr nhim trng ng tiu nh cc quinolon th h 1. - Cc quinolon cn li s dng trong nhim trng ng tiu, sinh dc, a chy, thng hn, h hp, xng, tin lit, lao

74

CIPROFLOXACIN
O F COOH

N NH
ten khac: C 17H18FO3N3 cipro, ciflox p.t.l 331,35

Ten khoa hoc : acid 1-Cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1piperazinyl)-3-quinolin carboxylic

75

CIPROFLOXACIN Kim nghim. nh tnh Ph hng ngoi Sc k lp mng Phn ng ca ion F Phn ng ca C=O : vi Natri nitroprusiat cho mu tm Th tinh khit Cl-, SO42-, kim loi nng, tro sulfat nh lng Sc k lng cao p Mi trng khan
76

CIPROFLOXACIN Tc dng dc lc - Ciprofloxacin c tc dng trn khun hiu kh Gram(-) gm c thng hn. - Hin xut hin s khng trn chng Pseud. aeruginosa. - Trc y c tc dng trn mt s chng Gr (+), nhng hin nay khng nhiu Cng dng iu tr cc bnh nhim trng h hp, tai, mi, hng, thn, ph khoa, gan mt, tin lit, xng, khp, bnh rut, thng hn, l.
77

CIPROFLOXACIN Tc dng ph - Fluoquinolon c th gy thng tn sn, cn thn cho tr em < 16 tui - Dng km corticoid c th tng nguy c phn ng ph. - Dng cn thn trn bnh nhn b cc bnh v gan, thn. - Ciprofloxacin c th gy phn ng ph h thn kinh trung ng, nh ri lon thn kinh, trm ut, hoa mt, o gic, run, kch ng, lo lng, ng g, au u, mt ng, kh chu, ri lon v m, chng mt,...
78

H1

OFLOXACIN
O F N O CH3 COOH

N N H3C

ten khac : ofloset, Exocin; Flobacin; Floxil; Floxin; Oflocet Oflocin; Ox aldin; C 18H20FO4N3 p.t.l 331,35 Ten khoa hoc: acid (+)-9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1piperazinyl)-7-oxo-7 H- pyrido[1,2,3- d ]-1,4-benzoxazin-6-carboxylic

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Slide 79 H1 H2
Hp, 3/19/2008 Hp, 3/19/2008

OFLOXACIN Tc ng dc lc - Ofloxacin c thi gian bn hy trung bnh - C tc dng trn nhm vi khun Gr (-) nhng yu hn so vi Ciprofloxacin. - Ofloxacin c hiu qu chng lu cu v nhim trng niu o do Chlamydia. - Nhng nghin cu gn y cho thy ofloxacin c trin vng trong ha tr liu ci. Hin ang nm trong chng trnh chng ci ca OMS
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SPARFLOXACIN
NH2 F H3C HN CH3
Ten khac : Spara, Zagam C 19 H 22 F 2 N 4 O 3 p.t.l. 329,41 acid (cis) -5-Amino-1-cyclopropyl-7-(3,5-di methyl-1-piperazinyl)-6,8-difluoro1,4 dihydro-4-oxo-3-quinolin carboxylic

O COOH N

N F

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SPARFLOXACIN

Sparfloxacin l quinolon th h th hai. c FDA cho php 1996 Ch nh Vim phi v nhim khun nng. Vim ph qun mn tnh. Vim xoang.

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MOXIFLOXACIN
O F H HN N O H H3C COOH

( Avelox) Ch nh. Nhim trng ng h hp, nhim trng da

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