1.

Antimicrobial Drugs

Exercise I1.Beta lactam Drug action

CH,
R--0C-HN-
CH,
A B

N COOH

-D)
A. B.
ua2o die
C. B laetamcse
clavwau acud

1. Name the two rings of the beta lactam nucleus (A) and (B). Mentionthe microbial
enzyme (C) that targets ring (A), inactivating the molecule.
2. Name an agent (D) that inhibits the enzyme (C) and protects the penicillin nucleus.

9. D- plaetanese ui Gitons - clavauc aeidsulbaatau

Auoxlln clauurare aed

JesA Hhe e caey
Aupialin+ Slbaetam Peueilliu
piperaeillin Ta2obaetun

55
 I. Antimicrobial Drugs

EartierPenicillins
Exercise | 2. Plasma concentration time curves of
-m
concentration
cg/ml
10
2 i.m.

3 i.m.
1.0

Plasma
1 oral
4 i.m.

0.1
2 4 6 12 18 24
TI me in hours
1. 2.
Beuzyl pencilun eoJa)
3. 4.
pYocaine Beugaine Rencalli
1. ldentify each of the earlier penicillins indicated as 1, 2, 3 and 4.
2. Comment on the duration of action of each of these penicillin preparations.

Drug Dural oy
Oral 6eulge pen cain Q-6hr

a- 4 6Y

DVbcaiue percin
BenaHiue pencillin

56
 I. Antimicrobial Drugs

Exercise l3. - Sequential Blockade of Bacterial Folate Synthesis

P-amninobenzoic acid +Pteridine
Pteridine
synthetase
Dihydropteroic acid
Dihydrofolate
synthetase
Dihydrofolic acid
Dihydrofolate
reductase
Tetrahydrofolic acid
Thymid ine ’Methionine
Purines
1. 2.
Sulfannethonu2ole im etho prim
1. Identify each of the agents acting at sites 1 and 2. Name the fixed dose drug combination
that manifests this sequential blockade of folate synthesis.
2. Explain how this combination provides optimal synergy for the spectrum and bactericidal
action of the drug.

A- Sulfawethoxa 2o le G- Triunetnopm m
FDC - CotrinoXa2ole

at a conceuwai
op hwal Syuergy u cane f wost orqaisn Is enlhibited ba 3-6bmes
uIc of each Co mponent mag be rodu ced
o£ 10 , the at dose
ui (la plasa when the two a e
The Yaho abtaned
T nethopvin S wove vapialy trprd soluble
Talio o! 5:1 bo cause tthosa2ole ud att ajn
Vd.han Salfa we
eutve any hssues has highey (i
couceulwaian Row auer Tri welhupvig adequatey ross
loawer plas wna
iwethopriwn Ls none
blood Gvau bammer and yoaceuta MoreOveN
apldly absorbedl roun sulfouetha zole
57

657
Pgf of salfaue hoyatole-
 I. Antimicrobial Drugs

Exercise I4. Drugs Inhibiting Folate Synthesis in Different Species

BACTERIA PROTOZOA

PABA 4 PTERIDINE

Dihydro pteroic acid HUMAN BEING

Dihydro folic acid Dietary Folic acid

4)
Tetrahydro folic acid

PURINE -PYRIMIDINE BASES

DN A DN A DN A

1. 2
Sul fadi aine ,Salfanelnoxa20le Sultadox ine
3 4. 5.
Tienehopvim Pyraun e hauine uelhobekate
1. What is the difference between bacteria and human beings in their
acquisition of folic acid?
2. Mention agents that act at each of the sites 1,2,3,4 and 5. State
the enzyme and process that
is blocked. Name the indications of use for each agent.

- baelena syuthes ts thelgn ocn totic aed Rom PABA ptenilane and dutajmic aljd
but hun an regui re eteu al o uvce or oue aerd

Sultaue thoxa 2ole - folate Squa ase 4

S
Sul fadia ine Glale squk Malana
wilh
Triwmetoo prin-
fura aelhewu ne Dihydu tolslereluel ase - Malan a
Metholyen ade Yeuoane~ Auh caucelos
58
 1. Antimicrobial Drugs

EXercise l5. Mechanisms of Action of Some

Antimicrobial Agents
PURINES< TETRAHYDRO-FOLATE -------. --- PABA

DNA
2
m RNA
5 PROTEIN
1

REPLICATION

1. Penallins cephalocpori ns 2.
Cotkimoxi2ole
3
Doxorubian 4 5.
FluvoquinoDon e) Rifarpin Arm nogycos) de
1. Specify one antimicrobial agent acting at the sites 1, 2, 3,
4 and 5. State the mechanism of
action of each of these agents.
2.. Mention two indications for use of each of
these antibiotics.

( Penciln- cell woall synth esis (nhi bt tor G ephdyl hensferane eyme
2- Cotrimoxazale - inhi bit folate Synthe sis by Sequenicl bec ape
3 Huvoquinolanes- tuoibit DNA Syrane thus inhibit DNA Yerlica hoy
4 Aitampicin - nhibt RNA pdly mean e( ord wilo Pr sabamt polymuone)
S. Gentanmiain (nhibitt baotenal rotein Sy nthesis ny binng wiG 30s
of 0iboSOme

Penalli ~ Rheuhmale geves, syphl

Cohonoxawle- UT, RenpiYchy haot nfeai on
fluoswn Jan - Typhod, stDs, Raf ampicin - TB
59 Aentanan-soft bsue infechon
 I. Antimicrobial Drugs

Exercise l6. Spectrum of Antimicrobial Action

Rickettsiae Gram negative Gram positive Chlamydiae
bacteria bacteria
1

(2)

(4
5

1.
penallins, Linazolo1d 2.
(st aen Fluyosno lone
3.
3rd Cen ephaloporin 4. A2ithvo nyan 5
Tetracycine
Doxyscine
1. Name the antimicrobial agent having the spectrum of action indicated by the numbers 1, 2,
3, 4, 5.
2. Mention one organism susceptible to each of tie above antimicrobial agents and
one
infection it causes.

stveptococcuS - yer respiyatoy wast in feehn- penclin

chlamydial nfech ans - Azithio ycn
Ricketsiaa- Tenacycline
Salmo nellat phi- Typhoid fever - Gprofloxain

61
 J.
Chemotherapy of Infections and Neoplastic Diseases
Exercise J2. Action of
Antimalarial Drugs

merozoites RBC
schizont

Tissue
hypnozoitek schizont merozoites

sporozoites

Mosquito

gametocytes

1.
2.
3
primaguine chlovoe, meltos ui'ne
Primasune, 1afinoguine 4. Clsrosuine, quui ne
1. Name one drug in the given boxes. Explain the
actions.
2. Which drug acts wellat sites 1, 3 and 4 but
poorly at site 2? Mention two agents acting at
Site 2, one with a long duration of action and the other
acting for a brief duration.

Name the specific antimalarial drugs A, B and C with the given

actions.

Drug Liver Erythrocyte

Hypnozoites SCHIZONTS GAMETOCYTES Drug Name

A Nil Good
Good action against Avtemi isin
immature gametes
Excellent Poor Good against all species
Good against
Nil Excellent
Plasmodium.vivax chlarosuie
Primagune ti ssue sch 3on hide
chlovoquine -Cvy tvocy ie fch1 3og cid e fast oahng high eytjacoun
Primaquine- hypnozotte
Chlavuguine , Primaque qametou dal
 J. Chemotherapyof Infections and Neoplastic Diseases

Exercise J3. Action of Antitubercular Drugs

5 3
1) &2
Arabinosyl transferaseFatty acid synthase

Yt Translaion

Af Transcription

1. sonia zid pyrauzinanice 3. Ethanbul ol.

4. 5. 6
(NH

1. Name the antitubercular drugs acting at sites 1, 2, 3, 4, 5 and 6.

2. Explain the mechanism of action at each site.

cld, wwch ane

INH- (whbiwon ot Squthesi of uycotie
cell w al
Cbnpon euts of wyo baet enium
faMyacid
ide- iahbit mycolc aad Synthesis bq nterochng orth a
Pyraninan
dirfer ent faty avd synnane Hhan u abrorog
tvans qeYage
uvotad u aabi
Ehanbuto l- tahibtt orabinory taus lewane
tuleteuing tla wyarie aad aud utorpav
jalaelasn syuthera,t e y
wal
aWon tu wycobactexial all
sis PSubunit of
Kitampiçn- lutevept AA Squthesis by btndi s
gtotattevial DADNA clefendent RNA poy mer ae
shepongn- nhioit of ioten Sgnthesis 65