CAC BETA-LACTAMIN

C che tac ong :

Beta-lactamin + PBP

c che s tong hp peptidoglycan

Phan huy thanh vi khuan

Cau truc vach VK va PBPs

NHOM BETA-LACTAMIN

PENAM

(PENICILLIN)

1928

Penicillin G & V

Penicillin A

Penicillin M

Carboxy-Penicillin

Ureido-penicillin

CEPHEM

(CEPHALOSPORIN)

Cephalosporin I

Cephalosporin II

Cephalosporin III

Cephalosporin IV

PENEM

Imipenem

( + cilastatin)

MONOBACTAM Aztreonam

Khang sinh -Lactamin

R

O

N

S

R

COOH

R

O

NH

R

R

O

N

S

COOH

R

O

N

S

COOH

B A

6

Penam ( *O: oxapenam)

- Cc penicillin

Penem (*C: carbapenem)

Monobactam - Aztreonam

Cephem (*O: oxacephem)

- Cc cephalosporin

Cu trc ho hc

C CHE E KHANG BETALACTAMIN CUA VK

S giam tnh tham cua thanh vi khuan

S thay oi iem ch cua khang sinh

Tac ong thuy phan cua cac men

-lactamase do VK tiet ra

Nhom Penam - Pho khang khuan

Peni G & V

Benzathin

Penicillin

Procain Pe

Cau khuan Gram +:

Lien cau, phe cau, tu cau (* ).

Cau khuan Gram -:

Lau cau, mang nao cau khuan.

Trc khuan Gram +:

B.anthrasis, C.diphteria,

L. monocytogenes, Clostridium.

Xoan khuan: Treponema pallidium

Peni A

La pho cua Peni G cong VK Gram -:

-E, Coli, Samonella, Shigella, H. influenza..

+

-

Nhom Penam - Pho khang khuan

Peni M

# Peni G nhng tac ong ac biet tren:

Staphylococcus aureus ( tiet penicillinase)

MSSA.

Carboxy-

penicillin

Pho Peni A cong them:

-Trc khuan mu xanh ( P. aeruginosae)

- Enterobacter

Ureido-

penicillin

Pho Peni A cong them:

- Trc khuan mu xanh

- Enterobacter

- Klebsiella

- Bacteroides

+

-

Nhom Penam

Penicillin G & V & Benzathin Penicillin

Co cung pho tac dung.

Peni G b huy pH acid dd IM/IV ( muoi K,Na)

Phan bo rong dch va mo, kem o LCR, SCN, xng, mat.

T1/2

ngan :# 1/2 h . Thai tr chu yeu qua than.

ket hp + probenecid : trong tr lau cau khuan.

Peni V: ben trong pH acid > Peni G PO.

Benzathin Peni, Procain Peni:

(EXTENCILLIN, BICILLIN) tac dung keo dai, ch IM.

NHOM PENAM

Peni G & V

Nhom Penam

Penicillin G & V

oc tnh :tng oi thap, chu yeu la d ng .

Lieu oc / ngi suy than : co giat. (*)

Khoang an toan rong:

3-6 x106 v/ ngay en 30-40 x10

6 v/ ngay

Ch nh:nhiem trung tai cho/ toan than do

cac VK nhay cam ( NT phoi, mau, mang nao,

noi mac tim, giang mai, lau, than, hoai th..)

Chong ch nh : tien s d ng

Than trong ngi suy than .

Penicillin G & V Tac dung phu - oc tnh

D ng vi nhieu mc o khac nhau, co tnh mien dch.

1-10%: nga,me ay, phat ban, viem troc da, viem mach, au ni chch.

< 1% : hc Stevens-Johnson, viem da hoai t, co that thanh,kh quan, soc phan ve ( co the t vong)

viem than mo ke, thieu mau tieu huyet, co giat,

Benzathin Peni, Procain Peni IM co the rat au va tao ap xe ni tiem.

IV > 10x106 v Peni co the gay tha Na hay K/ huyet nguy hiem ( tim mach, co giat..)

Nhom Penam

Aminopenicillin ( ampicillin, amoxicillin)

Hien b e khang bi nhieu VK Gram + va Gram- ke ca lau cau khuan can kiem tra o

nhay cam khi cho toa.

Ampicillin: PO luc oi ( hap thu 40-50%) , IM , IV

- hieu lc tren Gram am > Peni G,V.

- khong ben vi betalactamase (ket hp+sulbactam)

- TDP: d ng, co the gay xao tron tieu hoa, nam

Candida, au co that bung ..

Nhom Penam

Aminopenicillin

Amoxicillin: dung PO ( hap thu 80-90%), t b anh hng bi thc an.

- Pho kk # ampicillin.

- khong ben vi -lactamase (ket hp +ac clavulanic).

- con dungphoi hp tr H.pylori trong loet da day

- TDP: d ng, co the gay xao tron tieu hoa

( t hn ampicillin do SKD cao ), nam Candida

Nhom Penam

Carboxy-penicillin ( ticarcillin.carbenicillin..)

-Ben vi men cephalosporinase do VK tiet.

- Co hieu lc tren TK mu xanh, Enterobacter,

Citrobacter tiet cephalosporinase.

- Co the gay nhc K/huyet (cha 110-120mgNa/g)

- Dung IV

- Phoi hp vi ac., clavulanic e tang hieu lc.

( CLAVENTIN )

Nhom Penam

Ureido-penicillin : piperacillin,mezlocillin..)

- Ben vi men cephalosporinase & penicillinase (*)

- Pho KK rong

- Ch nh trong nhiem trung nang tai cho/toan than

ac biet vi VK Gram va VK k kh.

- Khang sinh d phong trong SP khoa & tieu hoa

- IV cham/IM/IV.

- Phoi hp + tazobactam= ( TAZOCILLIN).

- Hieu chnh lieu ngui suy than.

NHOM CEPHEM (CEPHALOSPORIN)

Nhom Cephem - Pho khang khuan

CG I

Cefalexin

Cefalothin

Cefaloridin

Cefazolin

Cefedroxil

-Cau khuan Gram + :

Lien cau, phe cau, tu cau meti-S

- Cau khuan Gram : Neisseria

-Trc khuan Gram -:

-H.Influinza. E. Coli, K. pneumonia. P.

-mirabilis

CG II

Cefaclor

Cefuroxim

Cefoxitin

Cefotetan

# CG I nhng hieu lc > v Gram

Tac ong tot tren VK Gram k kh

( cefoxitin, cefotetan)

Nhom Cephem - Pho khang khuan

CG III Cefoperazon

Cefotaxim

Cetriazon

Ceftazidim

Cefpodoxim

Cefixim

Latamoxef

-Pho khang khuan / CG II + :

- Cac VK ho khuan ng ruot.

- Trc khuan mu xanh (Ceftazidim)

(P. aeruginosa)

CG IV

- Pho khang khuan # CG III

- Ben hn vi -lactamase

Nhom Cephem

CG1: cefalexin,cefazolin,cefalotin,cefaloridin..

Hieu lc tot tren tu cau tiet penicillinase (meti-S).

- cefazolin tac dung tren Gram + tot hn cac CG1 khac

thng dung trong d phong phau thuat

Tuy chat, co the dung PO, IM, IV.

Ch nh trong NT ORL,ho hap, tieu, da, ..

TDP: d ng (cheo vi penicillin : 10-15 %) ,

roi loan tieu hoa, xao tron ve mau.

- cefaloridin oc vi than

- cefalotin co the gay viem TM hay viem huyet khoi TM

Nhom Cephem

CG2: cefaclor,cefuroxim,cefoxitin,cefotetan..

Tac dung tren tu cau meti-S yeu > CG1 nhng tot hn tren trc khuan Gram -.

- cefaclor co pho gan CG1 hn cac CG2 khac, hieu qua

tren H. influenza tot > cefalexin.(viem xoang, tai, NT hh

tren)

Ch nh :nhiem trung khang vi CG1, amoxicillin

d phong NT trong phau thuat.

nhiem B.fragilis: cefoxitin, cefotetan

Thng dung IM / IV ; PO : cefaclor, cefuroxim

Nhom Cephem

CG3: ceftriaxon.ceftazidim,cefotaxim,cefixim..

Co hieu lc tot > CG1 & 2 tren nhiem trung

Gram am.

- Ceftazidim co hieu lc tot tren TK mu xanh.

- ceftriazon co T1/2

(8h), co the dung 1lan/ngay

Qua c LCR: dung trong viem mang nao.

Thai chu yeu qua than tr ceftriaxon (40%) va

cefoperazon (80%) qua mat.

Latamoxef, cefoperazon co the gay xao tron

ong mau ( nhom metyl-thio-tetrazol)

Nhom Cephem

CG4: cefepim (MAXIPIM, AXEPIM)

IM/ IV t 2-3 lan/ngay.

Pho tac dung # CG3 nhng cho hieu lc manh

hn tren VK khang thuoc .

Qua hang rao mau nao nh CG3.

Ben vi - lactamase hn CG3 co the do co

them iem gan PBP2 chuyen biet.

Hieu chnh lieu ngi suy than.

NHOM PENEM ( CARBAPENEM)

Imipenem + cilastatin (THIENAM )

Pho khang khuan rong, ben vi nhieu betalactamase.

T1/2

= 1h, 90% vao nc tieu hieu chnh lieu

cho ngi suy than.

C: nhiem trung nang (NTBV, boi nhiem) TDP: d ng, tieu hoa, co giat. IV cham trong 20-30 p ,3-4lan/ ngay. Cam ng manh cephalosporinase can phoi

hp khi ieu tr khuan mu xanh,

NHOM PENEM ( CARBAPENEM)

NHOM MONOBACTAM

ai dien duy nhat : Aztreonam (AZACTAM)

La KS co pho chon loc tren VK Gram am

hieu kh ( nhieu trc khuan & cau khuan).

Khong tac dung tren Gram + va VK k kh.

Ch nh trong nhiem trung Gram nang. IM/IV 3-4 lan /ngay.

TDP : d ng, roi loan tieu hoa.

AZTREONAM

CAC CHAT C CHE - LACTAMASE

Khong /co tnh khang khuan rat yeu

c phoi hp vi 1 beta-lactamin (BL).

Lam tang tac dung cua BL a b e

khang do s tiet betalactamase/VK.

Co 3 chat c dung tren lam sang:

acid clavulanic

sulbactam

tazobactam

Ac clavulanic S tng t ve cau truc

C che tac ong cua Augmentin

ACID CLAVULANIC

Tac ong khang khuan yeu

c che manh cac -lactamase (chu yeu la

cac penicilinase nhom TEM ) thng tiet ra bi

cac vk:

- H. Influenza,, S. aureus, N. gonorrhrea, M.

catarrhalis K. pneumonia , E. Coli. Samonella,

Shigella.. ) B. fragilis , P. vulgaris.

Hieu lc c che penicilinase manh, ch can 1g/ml cho 1 n v enzym.

Ket hp chat c che -lactamase

vi betalactamin :

Acid clavulanic

+ amoxicillin (AUGMENTIN)

+ ticarcillin ( CLAVENTIN )

Sulbactam

+ ampicillin ( UNACYNE )

Tazobactam

+ piperacillin) ( TAZOCILLINE)

Ch nh tr lieu

Viem tai gia cap dai dang hay tai phat

Viem xoang

Nhiem trung ng ho hap tren ( viem xoang, hong) hay ho hap di ( viem

phoi, phe quan)

Nhiem trung ng tieu

Nhiem trung phu khoa

Nhiem trung da va mo mem.

do cac vi khuan e khang mot so KS

va benh tr nen man tnh.