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Bng 1-Aminosid/dh

Khng sinh aminoglycosid


(gi tt l Aminosid)
* Cu trc: Heterosid "Genin-O-Ose"
OH

OH
HO

H2N

OH

2
3

HO

HO

OH

OH

Cyclitol
(polyalcol vng)
Genin: L cc diaminocyclitol
1. Dn cht 1,3-diaminocyclitol:
Gm 3 cu trc: streptidin,
streptamin.

H2N

OH

C HN

HO

NH

2
3

NH C

H2N

NH2

streptamin

H2N

deoxy-2

2
3

NH2

OH

HO

OH

OH

Streptidin
Streptamin

OH

NH2

HO

OH

Aminocyclitol

6
5

OH

OH

NH

NH2

6
5

OH

OH

Deoxy-2 streptamin
(dideoxy-1,3
diamino-1,3
cyclitol)

H2N

2
3

Ose O

NH2

H2N

O Ose

2
3

Ose O

NH2

OH
O Ose
5

OH

Dn cht th 4,6
Dn cht th 4,5
c tnh:
Th 4,5

th 4,6
(khng c tim)
(tim c)
2. Dn cht 1,4-diaminocyclytol (fortamin): Cht in hnh
l fortimicin.
CH NH
Me

NH2

O
NH2

OH

OMe

6
4

HO

. 2 H2SO4

Me
CO CH2NH2

Fortimicin A sulfat

Ph tc dng: Tng t gentamicin.


Bng 2 -Aminosiddh
Ose (ng):
+ ng amin 6 cnh:
CH2OH

HO

HO

NH2

OH

H2N

H3C

NH2

HO

NH2
CH
O

OH
NH2

Garosamin
Sisosamin
+ ng 5 cnh:
H3C

OH

OH

D-glucosamin-3

O
OH

OH

H2N

CH2 NH2

HO

OH

D-glucosamin-2
Neosamin C
HO

CH2OH

HO

CH2 NH2
O
OH

NH2

Purpurosamin

HOH2C

OH

OH

CHO
L

streptose

ribose

OH OH

OH OH

* S xp nhm cc aminosid dn cht 1,3-diaminocyclitol

AMINOSID
Streptamin Streptidin

Deoxy-2 streptamin

Genin

Th 4,5

Th 4,6

OH

Aminosid
Kanamycin

Spectinomycin

thin

Neomycin

Streptomycin

Paromomycin

Gentamicin

nhin

Lividomycin

Tobramycin
Ribostamycin
Sisomicin

Aminosid

Dihydrostreptomycin

Amikacin

BTH

Dibecacin
Netilmicin

Bng 3-Aminosid/dh

* Ngun gc:
T mi trng
Streptomyces (S.)

nui

cy

Micromonospora

(M.);

Bng 18. 6. Khng sinh v chng vi sinh


Tn khng sinh
Apramycin
Kanamycin
Lividomycin
Neomycin
Paromomycin

Chng vi sinh sn xut


S. tenebrarius
S. kanamyceticus
S. lividus
S. fradiae v albogriseolus
S.
rimosus
v
chrestomyceticus
Ribostamycin
S. ribosidificus
Spectinomycin
S. spectabilus
Tobramycin
S. tenebrarius
Streptomycin
S. griseus v oliraceus
Sisomicin
M.
inyoensis
v
cyaneogranulata
Gentamicin
M.
purpurea
v
echinospora
Fortimicin
M. olivoasterospora
Butirosin
B. circulans
Ghi ch: S. = Streptomyces; M. = Micromonospora; B. = Bacillus

Ph tc dng: Ch yu trn vi khun gram (-); m rng sang


gram (+).
Mt s c th nhy cm:
+ Streptomycin: Rt nhy cm vi Mycobacterium (lao,
phong).

+ Aminosid th 4,6 v th 4,5-deoxy-2 streptamin:


Tc dng trn hu ht cc chng vi khun gy bnh thuc
c hai gram VK, tr vi lin cu (km penicillin) .
+ Paromomycin: Tc dng trn amip v sn rut (KST).
Hp thu: Khng hp thu qua nim mc ng tiu ha.
Thi tr: 70-90% qua ng thn-nc tiu.
c tnh: Hai tc dng bt li ch yu khi dng ko di:
+ Tc ng xu trn thn kinh thnh gic, gy ic kh hi
phc.
+ Knh ng ng thn, nng gy hoi t.
Tc dng khng mong mun khc: Mn cm thuc, gim th lc...
Dn cht th 4,5-deoxy-2 streptamin c cao nht; chng
ch nh bng ng tim.
* Nguyn tc s dng khng sinh aminosid:
+ Khng dng liu cao.
+ Khng dng lin tc trong thi gian di; phn t 7-10
ngy.
+ Phi hp vi cc thuc cu trc khc cng tc dng.
+ Theo di thnh lc v lng nc tiu trong thi gian tim
aminosid.
+ Khng tim cc aminosid thuc dn cht th 4,5 deoxy-2
streptamin.
* S khng aminosid ca vi khun
+ B khng nhanh (c th ngay t t iu tr u).
+ Khng cho gia cc aminosid xy ra ph bin.
Bng 4-aminosid/dh
Dn cht Streptidin
Streptomycin sulfat
Ngun gc: T mi trng nui cy Streptomyces griseus (1943)

Cng thc:

CH2OH
O
HO
1

,,

NH

H3C
L streptose

CHO
2

OH

,,

OH NHCH3

H2N C HN

NH
NH C NH2

2
1

L glucosamin

OH

OH
OH

. 3 H2SO4

Streptidin
2

c im: C 3 trung tm mang tnh base; mt nhm -CHO; v


tr 1,3 l hai gc guanin.

Tnh cht:
Bt mu trng, v ng, ht m mnh;
D tan trong nc; kh tan trong cc dung mi hu c.
Dung dch nc khng bn (nhanh b kt ta dng base).
Ha tnh-nh tnh:
- un si streptomycin/NaOH: gii phng NH3 (guanin).
- un si vi thuc th Fehling: Cu2O mu nu (tnh
kh).
- un si streptomycin/NaOH cho maltol, to mu tm vi
FeCl3:
H3C

O
CHO

,
OH OR

OR

H3C

OH , t

H3C
+

HO
Maltol O

Fe

3+

Fe 3
O
O

Phc vi st (III)-tm

ng dng: nh tnh v th tinh khit bng o quang, so vi


chun.
- Sc k lp mng;
- Hm lng streptomycin B 3% (HPLC).
nh lng:
+ Phng php vi sinh: Hot lc 720 UI/1mg cht th.
+ Hm lng sulfat: 18,2-21,5% (bng complexon III, qua BaCl 2
chun)
Ch nh: Phi hp iu tr lao: INH + streptomycin +
Rifampicin.
Liu dng: tim bp (IM) 1-2g/24h; chia 2 ln. L bt ch pha khi
dng.
Tc dng khng mong mun: Chung ca aminosid.
Bo qun: Trnh m; nhit thp. Thuc c hn dng.

Bng 5-aminosid/dh
Dn cht th 4,6 ca deoxy-2 streptamin:
Gm: Gentamicin, kanamycin, tobramycin, sisomicin v netilmicin
(BTH).
Gentamicin
Ngun gc: T mi trng nui cy Micromonospora purpurea v M.
khc.
Hn hp cc gentamicin A, B, C1, C1a, C2, C2a, X.

Cng thc chung:


R5

R3

CH R4
O
,
1
R2 ,

H2N

2
1
4

NH2

R1

OH

,,

H3CHN
2

,,

R6
OH

OH

Cc gentamicin khc nhau cc gc R (1...6) (xem bng 4-10


HD II)
Ch phm dc dng: Mui sulfat ca hn hp Gentamicin C 1, C1a,
C2, C2a.
Gi chung l Gentamicin sulfat.
Tnh cht:
Bt kt tinh mu trng. D tan trong nc; kh tan trong
dung mi hu c. []D20 = +107o n +121o (dung dch
10%/nc).
nh tnh:
- Cho mu tm vi ninhydrin (chung ca aminosid).
- Phn ng ca ion SO42- Sc k, so vi gentamicin sulfat chun: t nht c 3 vt
mu.
nh lng:
- Phng php vi sinh: Hot lc 590UI/1mg cht th.
- HPLC.
- Hm lng SO42-: 32-35% (p.p. complexon, thng qua BaCl2
chun).
Ph tc dng:
- Hu ht vi khun gram (-); nhy cm nht nh vi Ps.
aeruginosa.
- VK gram (+): Nhy cm t cu vng.
Khng nhy cm lin cu (thua penicillin G).
Ch nh:
- Cc nhim khun ton thn do vi khun gram (-).
- Thay th/phi hp penicillin khi nhim khun t cu, lu
cu.
- Phng nhim khun hu phu.
Liu dng: Tim IM 0,4-0,8mg/kg/ln 3 ln/24h; t 7-10 ngy.
Tc dng KMM: Chung ca KS aminosid.
Thn trng: Khng phi hp vi cephalosporin hoc cc thuc
c tnh thn.

Bo qun: Trnh m; nhit thp. Thuc c hn dng.


Bng 7-Aminosid/dh
Sisomicin
Ngun gc: T mi trng nui cy Micromonospora inyoensis
Cng thc: Khc gentamicin C1a (4', 5').
Hot tnh khng khun: Tng t gentamicin
c im: + Tc dng vi t cu vng khng methicillin.
+ Trn Ps. aeruginosa: > gentamicin 2-4 ln.
Nhc im: Nhanh b vi khun khng.
S dng: C th dng trc tip; thng lm nguyn liu bn tng
hp Netilmicin.
Netilmicin sulfat
CH2 NH2
O
,
1
2

H2N

2
1
4

NH2

NH C2H5
O

OH

OH

,,

H3CHN
2

CH3

,,

. 5 H2SO4
2

OH

Dng dng: Mui sulfat (C21H41N5O7)2 . 5H2SO4


ptl : 1441,56
Bt mu trng; d tan trong nc.
[]D20 = +88o n +96o (d.d. 30 mg/ml)
1 mg netilmicin sulfat tng ng 595 g netilmicin base.
Ph tc dng: Tng t sisomicin, gentamicin; khng b vi
khun khng.
Ch nh: Tng t gentamicin; c bit TK m xanh (Ps.
aeruginosa).
Liu dng: Ngi ln, tim bp 1,3-2,2 mg/kg/8 h; t 7-10 ngy.
Dn cht th 4,5 ca deoxy-2 streptamin
Neomycin sulfat
CH2 NH2
Ngun gc: T mi trng nui cy Streptomyces
fradiae
(1949)
H
2
NH2
, O
2N
5
1
Cng thc: Hn hp Neomycin A, B v C. ,
Neomycin A

- Neomycin B
R1 = H; R2= -CH2NH2
- Neomycin C

HO

Neosamin

R2
HO

OH ,
2

6
5

NH2

O
O

OH
O

HOH2C
OH D ribose
R1
OH
,, O
5
O
OH

,,

,,

NH2

R1 = -CH2NH2; R2= H

Bng 7-Aminosid/dh
Neomycin-tip
Tnh cht:
Bt mu trng ng, v ng.
D tan trong nc; tan nh trong ethanol; khng tan trong d/m
hu c.
nh tnh:
- Cho mu tm vi ninhydrin.
- Sc k: Sc cho 3 vt tng ng neomycin sulfat
chun.
nh lng:
- Phng php vi sinh: Hot lc 680 UI/1 mg cht th.
- Hm lng SO42-: 27-31%.
Ph tc dng:
+ Trn hu ht VK gram(-), k c Vibrio cholerae (t).
+ Khng tc dng trn TK m xanh.
+ Nhy cm vi khun gram (+), tr hu ht lin cu.
Ch nh:
- Dng ngoi: Thuc m 3-5 mg/g thuc.
Phi hp vi khng sinh polypeptit, nystatin iu tr a
nhim da.
- Ung lm sch rut trc phu thut bng.
c tnh: Chung ca aminosid; c tnh cao khng c tim.
Bo qun: ch mt.
Framycetin: Ch phm thun neomycin B, ngun gc t
Streptomyces decaris.
Ch nh, cch dng: Tng t neomycin.
Aminosid dn cht Streptamin
Spectinomycin hydroclorid
Ngun gc: T mi trng nui cy Streptomyces spectabilis
Cng thc:
OH

Tnh cht:

H3C HN

HO

O
NHCH3

OH

CH3

. 2HCl . 5H2O

Bt kt tinh mu trng, khng bn vi khng kh, nh sng.


D tan trong nc; tan nh trong mt s dung mi hu c.
Ph tc dng:
- Tng t gentamicin, nhng hot lc thp.
- Nhy cm c bit: N. gonorrhoeae (lu cu).
- Khng tc dng trn xon khun giang mai.
Thi hn tc dng: 24 h.
Ch nh: Ch yu iu tr bnh lu do lu cu (thay th lactam).
Ngi ln, tim bp su 2-4 g/ln/24 h. L bt pha tim 2 v 4
g.
c tnh thp do cu trc khng hon ton aminosid.
Bng 8-Aminosid/dh
c thm:
Tobramycin sulfat
Tn khc: Nebcin
Ngun gc: T mi trng nui cy Streptomyces tenebrarius hoc bn
tng hp t kanamycin B.
Cng thc: L dn cht deoxy-3' ca kanamycin B.
CH2NH2
O

NH2

H2N

HO
NH2

OH

D Glucosamin

C18H37N5O9
ptl : 467,5
Tnh cht: Bt kt tinh mu trng. Rt d tan trong nc; kh tan
trong alcol.
nh tnh:
- Dung dch 5 mg tobramycin trong nc, thm ninhydrin 0,1%;
un cch thu: xut hin mu xanh tm.
- Sc k lp mng, so vi tobramycin chun.
nh lng: Bng cc phng php:
- Phng php vi sinh. Hot lc khng thp hn 930 UI/mg.
- HPLC, so vi tobramycin chun.
Ph tc dng:
Tc dng trn hu ht cc vi khun gram (-); trn vi khun gram
(+) rt nhy cm vi t cu vng; vi trc khun m xanh hiu lc cao
hn gentamicin. Khng tc dng trn nhiu chng lin cu.

Ch nh: Tobramicin l thuc la chn iu tr nhim trc khun


m xanh, c dng phng nhim khun phu thut. Cc ch nh
khc tng t gentamicin.
Liu dng: Ngi ln v tr em, tim bp 1-1,7 mg/kg/8 h; t 7-10
ngy.
Thuc tim l dung dch tobramycin thm acid sulfuric n
nh.
Bo qun: nhit di 15o C.
Amikacin sulfat
kanamycin (aminosid

Ngun gc: BTH t


kanamyceticus).
Cng thc:
C22H43N5O13 . 2 H2SO4
Ptl : 781,8

H2N

CH2NH2
HO

O
OH

1"
2"
OH

2
5

NH R
O

OH

1''

CH2OH
2"

OH

OH

Streptomyces

Kanamycin
R=H
Amikacin
OH

NH2

R=

CO C CH2CH2 NH2
H

Dn cht th 4,6- ca deoxy-2 streptamin.


Tnh cht: Bt kt tinh mu trng hoc gn nh trng.
D tan trong nc; khng tan trong alcol, aceton.
Ph tc dng: Tng t gentamycin.
Nhy cm nht nh: Mycobactarium tuberculosis (TK lao).
Khng hu ht enzym phn hy aminosid ca vi khun.
Tuy nhin khng lm dng; vn tun th cc nguyn tc dng
aminosid.
Ch nh:
Thay th gentamycin, tobramycin tr nhim khun nng.
Phi hp tr lao.
Liu dng: Tnh theo amikacin base.
1,3 mg tng ng 1 mg amikacin base.
Ngi ln, tr em c th tim bp 5 mg/kg/8 h; 3 ln/24 h. t 7-10
ngy.
Bo qun: Trnh m.
Fortimicin A sulfat
Tn khc: Astromicin sulphate

Ngun gc: Chit sut t mi trng nui cy chng M.


olivoasterospora. Trong hn hp thu c cn c thnh phn fortimicin B
cng c hot tnh khng khun.
Phn genin l vng cyclitol, trong 2 OH (1,4) thay bng hai
nhm amin.
(Dn cht 1,4-diaminocyclitol).
Cng thc:
H2N

H3C

CH

NH2
O

OH
6

O
NH2

HO

. 2H2SO4

OCH3

CH3
CO CH2 NH2

C17H35N5O6 . 2H2SO4

ptl : 601,70

Tnh cht:
Bt v nh hnh mu trng, b bin mu trong khng kh, nh
sng; nng chy khong 200o C. Tan trong nc; tan nh trong ethanol;
hu nh khng tan trong nhiu dung mi hu c. []D20 khong +87o.
Ph tc dng: Tng t gentamicin; nhy cm t cu vng khng
methicilin.
Ch nh: Tng t gentamicin sulfat.
Liu dng: Tim bp hoc truyn 200 mg/ln 2 ln/24 h.
Bo qun: Trnh m.

Bng 10-Tetra./dh

Khng sinh tetracyclin

Gm cc cht khng sinh l dn cht octahydronaphtacen:

Octahydronaphtacen
* Cu trc chung:

R1
8
9

R6

R3
6

R2 R4
5

10

11

12

OH

OH

H
4a
12 a

OH

N (CH3)2
OH

3
2

CO R5

Cc tetracyclin khc nhau cc nhm th R (1...6)


Bng tng hp cng thc cc tetracyclin
Tn KS

R1

Clotetracyclin( -Cl

R2

R3

R4

R5

R6

-CH3 -OH

-H

-NH2

-H

Pht
hin
1948

-CH3 -OH

-OH

-NH2

-H

1950

-CH3 -OH
-H
-OH

-H
-H

-NH2
-NH2

-H
-H

1953
1957

-H
-OH
-CH3 -H
=CH2
-H
-H
-H
-H
-H
-H
-CH3 -OH
-CH3 -OH
-CH3 -OH
-CH3 -OH

-H
-OH
-OH
-H
-H
-H
-OH
-H
-H
-H

-NH2
-NH2
-NH2
-NH2
-NH2
-NH2
-CH3
-NHX
-NHZ
-NHY

-H
-H
-H
-H
-H
-NH2
-H
-H
-H
-H

1957
1958
1960
1964
1960

*)

Oxytetracyclin -H
(*)

Tetracyclin(*)
-H
Demeclocyclin -Cl
(*)

Demecyclin(*)
Doxycyclin
Methacyclin
Minocyclin
Sancyclin
Amicyclin
Terramycin X(*)
Lymecyclin
Mepicyclin
Rolicyclin

-H
-H
-H
-N(Me)2
-H
-H
-H
-H
-H
-H

1960
1962
1959
1958

Ghi ch: (*) = Cc tetracyclin thin nhin


Phn loi:
1. Theo ngun gc: Thin nhin v bn tng hp
Bng 11-tetra./dh
- Cc tetracyclin thin nhin.
T mi trng nui cy xa. khun (Streptomyces = S.))
- Cc tetracyclin bn tng hp (BTH).
Thay i mt vi nhm th cc tetracyclin thin nhin
ci thin v hiu lc khng khun, dc ng hc, tan trong nc...
2. Theo hiu lc tc dng: Th h I v II

Bng phn loi cc tetracyclin


Tn KS

Chng S.
cho KS

Ngun
gc

Th
h

T1/2
(h)

S.
aureofacien
s
Oxytetracycl S. rimosus

TN

5-6

TN

S.
viridifaciens
Demeclocycl S.
in
aureofacien
s
Demecyclin S.
aureofacien
s

TN

6-9

TN

II

10-17

TN

Doxycyclin
Metacyclin
Minocyclin
Limecyclin
Mepicyclin
Rolitetracycl
in

+
+
+
+
+
+

II
II
II
I
I
I

Clotetracycli
n

in
Tetracyclin

Bn/
H+

15-20

12-20
4-6
4-6
4-6

Tan/H2O

+
+
+

Ghi ch:
- Cc cht c tn chng Streptomyces l KS thin nhin.
- Cc tin tetracyclin: Limecyclin, Mepicyclin, Rolitetracyclin.
Tnh cht dc ng hc, tai bin:
+ Hp thu ng tiu ha:
- Mi cht c mc khc nhau.
- Demecyclin: KS thin nhin; km hp thu khi ung.
+ Thi tr: T l cao qua ng mt-rut; mt phn qua ng
thn-nc tiu.
+ Tai bin:
- i lc cao vi ion Ca++, tp trung xng, rng gy xn
mu, gin xng d gy; nh hng xu ti pht trin xng, rng
(tr em < 7 tui).
- Sn phm chuyn ha anhydrotetracyclin) kch ng, hoi t
ng thn.
- Tc dng trn vi khun rut (gram -): gy ri lon tiu ha.
- Mn cm thuc: Khng xy ra thng xuyn.
Ch nh:

Kh nng cc tetracyclin l khng a tr.


Thc t: Do tai bin, ch nn dng khi cn:
+ Dch hch, bnh than (phng, dp dch);
+ Dng ngoi: tr nhim khun da, mt.
Hn ch dng tr vim ng h hp do c khng sinh
c hiu.
Bng 12-tetra./dh
Ph tc dng:
a. Rt nhy cm (CMI < 1 g/1 ml huyt tng):
- Trn vi khun gram (+)
Streptococcus pyrogens
Lin cu A
"
viridans
Staphylococcus pyrogens
T cu
- Trn vi khun gram (-)
Neisseria gonorrhoeae
Lu cu
"
miningiditis
Mng no cu
Haemophillus influenzae
Bacillus anthracis
TK than
Yersinia pestis
VK dch hch
Clostridium welchii
"
tetani
TK un vn
Corynebacterium diphteriae
TK bch hu
b. Nhy cm (1 g/1 ml < CMI < 10 g/1 ml)
- Trn vi khun gram (+)
Streptococcus faecalis
Lin cu D
- Trn vi khun gram (-)
Escherichia coli
E. coli
Klebsiella pneumoniae
Salmonella
TK thng hn
Shigella
TK l
Brucella
Ghi ch:
CMI = Concentration Minimum Inhibitrice (nng c ch
nh nht).
Nhn xt chung:
-Ph tc dng ca cc tetracyclin trn c hai gram vi khun,
- Nhy cm vi nhiu chng lin cu (Streptococcus).
+ Chng ch nh:
Tr em ang thi k pht trin xng rng (< 7 tui)
Ph n mang thai v thi k cho con b.
Ngi thiu nng gan, thn
Ngi c c a mn cm thuc.
Vi khun khng thuc:

- Xut hin khng sau qa trnh s dng;


- Khng cho gia cc tetracyclin.
c im l-ha tnh:
Cng l dn cht ca octahydronaphtacen nn cc tetracyclin
c nhiu tnh cht l-ha chung:
- Bt mu vng; pht hunh quang vng trong nh sng UV.
- Hp th UV vi nhiu cc i hp th.
Bng 13-tetra./dh
ly-ha tnh (tip)
- Nhm -OH vng D l phenol, cho phc mu vi FeCl 3.
- Tnh kh: B bin mu chm khi tip xc lu vi khng kh,
nh sng; kh thuc th Fehling (cho kt ta Cu2O mu nu).
- Lng tnh: Nhm dimethylamin (4) tnh base; cc nhm -OH
tnh acid.
- To phc bn vi cc ion kim loi a tr: Fe3+, Zn2+, Cu2+...
+ Cc chelat to thnh c mu;
+ V tr lin kt vi ion kim loi thay i theo pH;
+ c bit to mu vi ZnCl2, mi tetracyclin cho mu ring:
clotetracyclin (), oxytetracyclin (tm), tetracyclin (vng)...
C th dng phn ng ny phn bit s b cc
tetracyclin.
- Trong pH acid, nhit phng, xy ra chuyn cu hnh, gi
l "epi ha":
Cc nhm -CH3 v -N(CH3)2 (4) lin kt , hot lc.
Ur, phosphat, citrat, acetat xc tc cho s chuyn ny.
Tuy nhin khi v pH thch hp, cu trc tr v bnh thng,
hot tnh khng sinh tr li:
H
4

N (CH3)2
OH

H+

A
1

OH

A
1

CONH2

OH

N (CH3)2
OH

CONH2

Dng epi (mt hot tnh)


Nh vy cc tetracyclin khng bn trong khng kh, nh sng;
Mt hot tnh mi trng qu kim hoc qu acid.
nh lng: Phng php vi sinh; HPLC.

Cng thc:

Tetracyclin H
hydroclorid
N (CH )
CH3

HO

OH

3 2

OH

OH

OH
CONH2
O

. HCl

Ngun gc: T mi trng nui cy Streptomyces viridifaciens.


Tnh cht:
+ Bt kt tinh mu vng, v ng, khng mi. B bin
mu/khng kh.
+ Tan trong nc, nhng dung dch khng bn; khng tan trong
nhiu dung mi hu c. []D20 = -250o (HCl 0,1 M).
Bng 14-tetra./dh
tetracyclin-tip
nh tnh:
+ Pht hunh quang vng di n UV (tm dung dch ln
giy)
+ Dung dch cho kt ta vi thuc th alcaloid (tnh base)
+ un si dung dch vi thuc th Fehling: kt ta Cu 2O (
nu).
+ To mu vi FeCl3 v H2SO4 m c.
+ Sc k lp mng, so vi chun.
nh lng: Phng php vi sinh hoc HPLC.
Ph tc dng v ch nh: Nh ni phn chung.
Liu dng: Ngi ln, ung 250-500 mg/ln/6-8 h
Tr em > 8 tui ung 5-10 mg/kg/12 h
Dng bo ch: Vin nang; thuc m 1-3% (bi ngoi).
Bo qun: Trnh nh sng.
Doxycyclin hyclat
Bit dc: Umidox-100
Cng thc:
H

H3C

OH

N (CH3)2
OH

. HCl .

OH

OH

OH

1
2

H2O .

1
2

C2H5OH

CONH2
O

Mt phn t doxycyclin ngm 1/2 H2O v 1/2 ethanol.

Ngun gc: Bn tng hp t


methacyclin (cht BTH t
oxytetracyclin).
(Xem HD II)
Tnh cht: Bt kt tinh mu vng, v ng, khng mi; bin
mu / khng kh.
Tan trong nc, ethanol; khng tan trong dng mi hu c.
nh tnh: Sc k, so vi doxycyclin chun.
Tc dng: Tng t tetracyclin hydroclorid; thuc th h II
u im so vi tetracyclin:
Hiu lc khng khun cao hn 2 ln gim liu ung 24 h.
Bn trong pH acid thi hn tc dng ko di (xem t1/2).
Ch nh: Cc ch nh chung nh tetracyclin;
Tr hiu qa nhim khun da do VK cha xc nh (u im
ni bt).
Liu dng: Ngi ln, ung 50-100 mg/12 h.
Dng ngoi: Bi thuc m.
Dng bo ch: Vin nang 100 mg (qui ra doxycyclin base).
Bo qun: Trnh nh sng.
Bng 15-tetra./dh
Minocyclin hydroclorid
Tn khc: Minomycin; Minocin
Cng thc:
N(CH3)2

OH

OH

OH

N (CH3)2
OH
CONH2
O

iu ch: Tetracyclin bn tng hp t demecyclin (Xem HD II).


(Demecyclin chit c t mi trng nui cy S. aureofaciens.
Tc dng ko di, nhng km hp thu ng tiu ha nn khng
s dng).
Tnh cht:
Bt kt tinh mu vng, v ng; b bin mu trong khng
kh, nh sng.
Tan trong nc v ethanol; kh tan trong dung mi hu c.
Tan trong kim (lng tnh).

nh tnh, nh lng: Cc phng php chung vi tetracyclin.


Tc dng:
Tc dng ko di nh demecyclin.
Hp thu hon ton khi ung (demecyclin km hp thu khi
ung).
So vi tetracyclin:
- Hiu lc khng khun cao hn 2-4 ln.
- Vi khun kh khng minocyclin;
- Khng khng cho vi cc tetracyclin khc.
- Thi hn tc dng ko di hn, liu 24 h thp hn.
Ch nh: Thay th tetracyclin.
Liu dng: NL, ung 100-200 mg/12 h.
Tc dng KMM: Chung ca tetracyclin.
Bo qun: Trnh nh sng.