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1KHKHNG SINH TNG SINH TNG HNG HPP
2sulfamid khng khun
3Ngay 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.
LCH S TM RA SULFAMID
Nm 1913 ngi ta tm thy phm azoic cryzoidin c tc dng dit khun v tng i t c.
NN
NH2
H2N
Azoic cryzoidin
4NN
NH2
H2N
Azoic cryzoidin
SO2NH2
Prontosil
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
LCH S TM RA SULFAMID
51935 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
6Prontosil ?
Vo c th prontosil chuyn ha thnh cht khc ctc dng khng khun
LCH S TM RA SULFAMID
7NH2 H2NSO2 + NaNO2HCl +H
-Cl]N[NH2NSO2
NH2
H2N
SO2NH2N
NH2
H2N N
(Sulfanilamid)
m - phenylendiamin
p - aminobenzensulfonamid
Nguyn liu u tng hp protosil lp-aminobenzensulfonamid
Prontosil
LCH S TM RA SULFAMID
8Khi thay th sulfanilamid bng amin khc cho sn phm khng c tc dng khng khun
+ NaNO2HCl
NH2
H2N
anilin
+H-Cl]N[NNH2
NN
NH2
H2N
m - phenylendiamin
LCH S TM RA SULFAMID
9NH2 H2NSO2 + NaNO2HCl +H
-Cl]N[NH2NSO2
Sulfanilamid
OH
NN
NH2
HO
Khi thay th m - phenylendiamin bng cht khc cho sn phm c tc dng khng khun
phenol
LCH S TM RA SULFAMID
O2SNH2
10
Bovet v Trefuel th v thy sulfanilamid c tc dng khng khun trn cin vitro v trn in vivo. Ngoi ra sn phm acetyl sulfanilamid xut hin trong nc tiu
sulfanilamid NH2 H2NSO2
CH3COOH
SO2NH2CH3CONH
LCH S TM RA SULFAMID
11
Sulfanilamid tr thnh sulfamid u tin trong lch s. Vic pht hin ra prontosil v sulfanilamid m ra mt knguyn 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.
LCH S TM RA SULFAMID
12
LIN QUAN GiA CU TRC V TC DNG DC LC
14
N lun lun phi v tr C4 ( para vi SO2NH )
R1NH
R1NH
NHR1
NHR1
SO2NHR1
SO2NHR1
R2NH
R2NH
N lun lun phi gn vi nhn thm
R2NHCH2
Sulfamylon
Thay i trn N4
13
14SO2NHR1R2NH
Thay NH2 C4 bng nhm khc u lm mt tc dng nhng nu thay bng NO2 vn cn tc dng nhng c
SO2NHRO2N
LIN QUAN GiA CU TRC V TC DNG DC LC
14
Thay i trn N4
N lun lun phi t do COOH
COOH NHSO2N
SHN H2N
Ftalazol
Sulfathiazol
LIN QUAN GiA CU TRC V TC DNG DC LC
15
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.
SO2NHR1R2NH
R
R
R
R
Thay i trn nhn thm
LIN QUAN GiA CU TRC V TC DNG DC LC
16
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.
H2N SO2NHR C
NH
NH2
Sulfaguanidin
COCH3
Sulfacetamid
N
SSulfathiazol
Th nhm sulfamid
LIN QUAN GiA CU TRC V TC DNG DC LC
17
iU CH SULFAMID
i t anilin
NH2 + (CH3CO)2O NHCOCH3
NH2 + HCOOH NHCOCH3
NH2 + ClCOOC2H5 NH COOC2H5
Bo v nhm amin
18
H2N H ClSO2HO ClH2N SO2+
ClH2N SO2
NH3
2RNH
CH3CO NH2SO2NH
NHRSO2NH CH3CO
clorosulfon ha
To nhm sulfamoyl nh tc dng ca NH3 hay RNH2
iU CH SULFAMID
19
CH3CO NH2SO2NH
Thy phn gii phng sulfamid
SO2NH NH2HCl.
SO2NH2H2N SO2NH2H2N
SO2H2N NHNa
HCl
HClNaOH
NaOH
iU CH SULFAMID
20
i t clorobenzen
ClHOSO2Cl
SO2Cl
ClNH3
SO2NH2
Cl NH3
80 atSO2NH2
NH2
200oC
iU CH SULFAMID
21
i t cc sulfamid c sn
H2N SO2NH2 + CH2NNH2
NH
NH2
NHNH-CH2N SO2
H2N SO2NH2 + (CH3CO)2O NHCOCH3SO2H2N
NH2
NHNH-CH2N SO2 +
HCOHC
C H2N SO2 NHN
N
Sulfanilamid
Sulfanilamid Sulfaguanidin
Sulfacetamid
Sulfaguanidin Sulfadiazin
iU CH SULFAMID
22
TNH CHT SULFAMID
NH2H2N SO2
OH
H2N
O
S=NH
ONa
S=NH
O
H2N
Cho ta mui Ag, Cu, Co
NH2H2N SO2HCl
NH2H2N SO2HCl.
Tnh cht ha hc
Tnh acid
Tnh base
23
NH2 H2NSO2 + NaNO2HCl +H
-Cl]N[NH2NSO2
SulfanilamidOH
NH2NSO2 N
Nhm amin thm cho phn ng diazo ha thng dng nh tnh v nh lng
TNH CHT SULFAMID
24
Nhn benzen cho cc phn ng th c th p dng nh tnh hay nh lng
SO2NH2
NH2
+ Br2
NH2Br Br
SO2NH2
TNH CHT SULFAMID
25
Nhm NH2 c th phn ng vi p-aminobenzaldehyd ( PDAB) cho sn phm c mu c th dng nh tnh v nh lng
+
CN=H2N H N
CH3
CH3
NH2H2NSO2 NHOCCH3
CH3
TNH CHT SULFAMID
26
nh tnh
cc phn ng musc kph hng ngoit ngoiTh tinh khitCloridSulfatGim khi lng do sy khTp cht lin quan
Rf
IR UV
KiM NGHIM SULFAMID
27
KiM NGHIM SULFAMID
nh lng
Diazo ha
NH2 H2NSO2 + NaNO2HCl +H
-Cl]N[NH2NSO2
KI + h tinh bt
Ch th ngai Ch th ni
Tropeolin OO Chun th
pp dng c
28
+
CN=H2N H N
CH3
CH3
NH2H2NSO2 NHOCCH3
CH3
Phng php quang
Mu vng
Phng php quang
KiM NGHIM SULFAMID
29
nh lng sulfamid bng phng php acid-base
NaOH 0,1NChun mi trng nc
sulfadiazin, sulfacetamid( acid mnh )
Cc sulfamid( acid yu )
Natrimethylat 0,1N
xanh thymol (CT)
dimethylformamid
Chun mi trng khan
Cc sulfamid( base yu )
HClO 4 0,1N
Tm tinh th (CT)
Acid acetic bng
Chun mi trng khan
KiM NGHIM SULFAMID
30
Phng php kt ta
NH2 H2NSO2 + AgNO 3 SO2NHH2N Ag
Cn
KiM NGHIM SULFAMID
31
iu ch:- T Anilin- T Clorobenzen.- Bn tng hp t cc sulfamid c sn
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.
32
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
33
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
34
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
N
NNH2
NHNH-CH2N SO2
Sulfaguanidin ( khng hp thu ) Sulfadiazin (hp thu tt )
35
- 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 vmc 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.
Phn phiDC NG HC
36
Chuyn ha
Kh nng acetyl ha sulfamid ty thuc vo c a bnh nhn v loi sulfamid s9a vo c th
SO2NH2CH3CONHNH2 H2NSO2CH3COOH
- Cc dn cht acetyl ha ca sulfamid thng khng ctc 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
DC NG HC
37
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
TAC ONG DC LC
38
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 mvo 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.
39
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 kimKhng dng cho tr em
C TNH SULFAMID
40
- Phn ng ny rt khc nhau i vi tng sulfamid vvi 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
C TNH SULFAMID
Phn ng tng nhy cm
41
MT S SULFAMID KHNG KHUN CHNH
Phn loi
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
Sulfamid tc ng ton thn
42
Sulfamid dng ngai
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 tc ng ti ch
Phn loi
MT S SULFAMID KHNG KHUN CHNH
43
SULFAMID TON THN
Sulfamid tc dng nhanhhp thu nhanh v thi tr nhanh nn phi ung nhiu ln trong ngy.t lin hp proteinThng l nhng sulfamid th h uD gy kt tinh thno thi nhanh t tch ly nn tng i t c
44
SULFANILAMID
Ch nh
- 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.
NH2 SO2H2N
45
SULFATHIAZOL
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%.
H2N SO2NHS
N
46
SULFADIAZIN
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
N
NNHH2N SO2
47
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 trchm. - 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 thtich ly
48
SULFAMETHOXYPYRIDAZIN
OCH3H2N SO2NHN 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.
49
SULFADOXIN
NN
NHH2N SO2
OCH3 OCH3
Ch nh
Thi tr rt chm ch cn dng 1g / tun.
Sulfadoxin + pyrimetamin FANSIDAR tr st rt
50
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.
51
SULFAMETHOXAZOL
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
BACTRIMSulfamethoxazol 800 mgTrimethoprim 160 mg
N O CH3
NHSO2H2N
52
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 thngNhm d vng: thng c nhm CH3 v d vng 5 cnh
53
SULFACETAMID
Ch nh- D tan trong nc hn nhiu sulfamid khc, nhanh chng t nng cao trong mu, nhng thi trnhanh, 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.
NHCOCH3SO2H2N
54
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.
SULFAMID TI CH
55
SULFAGUANIDIN
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
H2ONH
NH2CH2N SO2NH
56
Sulfamid dung ngoaiNi 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.
2H2N SO2NH H2N SO2N
NN
Ag
SULFAMID TI CH
57
Sulfamid dng ngoi
Ngoi cc sulfamid trn c mt sulfamid chuyn sdng ngoi da v khng chu tc ng bi PABA lsulfamilon
CH2NH2 SO2NH2
SULFAMID TI CH
58
thuc khng khun nhm quinolon
59
. I CNG NHM QUINOLON
Lch sThuc u tin: acid nalidixic (negram), mt
thuc khng khun tng hp tr nhim khun ng tiu bi vi khun Gram (-) t 1964.
60
Cc quinolon th h I
YX
NO
O COOH
O
ten thuoc X Y R
acid oxolinic H H C2H5cinoxacin N H C2H5mibxacin H H OCH3
. I CNG NHM QUINOLON
61
X
Y N
COOH
O
R1
R2
ten thuoc X Y R1 R2acid piromidic N N C2H5
acid pipemidic N N C2H5
resoxacin H H C2H5
N
HNN
N
Cc quinolon th h I. I CNG NHM QUINOLON
62
- Cc quinolon th h 1 khng cha F (trflumequin).- 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 sdng.
Cc quinolon th h I. I CNG NHM QUINOLON
63
N
F
O
COOH
NN
R2
R3R1 R4
ten thuoc R1 R2 R3 R4Perfloxacin CH3 H H C2H5nofloxacin H H H C2H5Amifloxacin CH3 H H NHCH3ofloxacin CH3 H
Ciprofloxacin H H H
lomefloxacin H CH3 F C2H5Enoxacin H H N C2H5
OCH3
Cc quinolon th h II
. I CNG NHM QUINOLON
64
Cc quinolon mi
OCOOHF
ON
HN
H
H H3C
Moxifloxacin ( Avelox)
F
N
H2N
N
O
COOH
F
F
Trovafloxacin
O
H3C
N N
COOH
O
F
N
NH2
Gemifloxacin
. I CNG NHM QUINOLON
65
Lin quan cu trc v tc ng dc lc
87
65 4 3
21
N
COOHO
h thng pyridon phi ngng t vi nhn thm. - V tr 1 th alkyl ngn ( methyl, ethyl, cyclopropyl ) tng tc dng khng khun.
C2H5CH3
. I CNG NHM QUINOLON
66
- 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 ( 1,6-naphthyridin), 8 (1,8- naphthyridin) vn duy tr tc dng khng khun.
87
65 4 3
21
N
COOHO
RN
NN
N
. I CNG NHM QUINOLON
67
87
65 4 3
21
N
COOHO
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
R
R
Th F v tr 6 lm tng tc dng khng khun
F
. I CNG NHM QUINOLON
68
- 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
87
65 4 3
21
N
COOHO
NN
H3CF
CH3O
. I CNG NHM QUINOLON
69
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+ .
. I CNG NHM QUINOLON
70
Kim nghimnh 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 lngPhng php mi trng khan : HClO4 / CH3COOH
. I CNG NHM QUINOLON
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.
71
C ch tc ng. c ch hot tnh enzym AND gyrase , ngn cn qudui 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 chtopoisomerase.
. I CNG NHM QUINOLON
72
AND gyrase
Quinolon
. I CNG NHM QUINOLON
73
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
. I CNG NHM QUINOLON
74
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
. I CNG NHM QUINOLON
75
CIPROFLOXACIN
F
O
COOH
NHN
ten khac: cipro, ciflox
C 17H18FO3N3 p.t.l 331,35
Ten khoa hoc : acid 1-Cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolin carboxylic
76
Kim nghim.nh tnh
Ph hng ngoiSc k lp mng Phn ng ca ion FPhn ng ca C=O : vi Natri nitroprusiat cho mu tm
Th tinh khitCl-, SO42-, kim loi nng, tro sulfat
nh lngSc k lng cao p Mi trng khan
CIPROFLOXACIN
77
Tc dng dc lc- Ciprofloxacin c tc dng trn khun hiu khGram(-) 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
CIPROFLOXACIN
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.
78
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,...
CIPROFLOXACIN
79
OFLOXACIN
N
O
COOH
O
F
NN
CH3H3C
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-1-
piperazinyl)-7-oxo-7 H- pyrido[1,2,3- d ]-1,4-benzoxazin-6-carboxylic
H1
Slide 79
H1 Hp, 3/19/2008
H2 Hp, 3/19/2008
80
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 ctrin vng trong ha tr liu ci. Hin ang nm trong chng trnh chng ci ca OMS
OFLOXACIN
81
SPARFLOXACIN
NN
HN
H3C
CH3
F
F
NH2COOH
O
Ten khac : Spara, ZagamC 19 H 22 F 2 N 4 O 3 p.t.l. 329,41acid (cis) -5-Amino-1-cyclopropyl-7-(3,5-di methyl-1-piperazinyl)-6,8-difluoro-1,4 dihydro-4-oxo-3-quinolin carboxylic
82
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.
83
MOXIFLOXACINO
COOHF
ON
HN
H
H H3C
( Avelox)
Ch nh. Nhim trng ng h hp, nhim trng da