Antibiotics: Classification (Based On Mechanism of Action)

Antibiotics Notes
ANTIBIOTICS
Students are requested to read this topic of antibiotics under following sub headings :
a. Mechanism of action(classification)
b. Pharmacokinetics
c. Pharmacodynamics
d. Resistance mechanisms
e. Side effects
f. Specific indications with spectrum
g. Few special bacterial infection treatment drugs
h. Empirical use of antibiotics
i. Few tables from text book
Classification(Based on Mechanism of action)
1. CELL WALL INHIBITOR
β – Lactam Antibiotics Glycopeptide Ab

MOA Transpeptidase Inhibitor MOA glycosyltransferase
(PBP = Penicillin Binding Protein)
Inhibits CrossLinking b/w NAG and NAM Inhibitor Transfer of D-alanine side chain
Penicillins, Cephalosporins Vancomycin, Teicoplanin
Monobactam, Carbapenems
Misc. Fosfomycin
2. CELL MEMBRANE INHIBITOR
Polypeptide Abs Daptomycin

MOA Inhibit lipid bilayer MOA Inhibit Membrane by
Polymyxin – B Depolarisation
Colistin
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Antibiotics Notes
3. PROTEIN SYNTHESIS INHIBITOR
30s Ribosome 50s Ribosome

Aminoglycosides (16S) Streptogrammins, Macrolides,Lincosamides
Inhibits rRNA chain formation Inhibits A to P translocation
Inhibits mRNA reading
Linezolid, Tedizolid (23S)
Tetracycline Inhibits rRNA chain formation
Inhibits tRNA
Chloramphenicol
Inhibits P to A translocation& peptidyl
transferase enzyme
4. Folic Acid Pathway Inhibitor
PABA + DHA DihydroptericAcid +glutamte Dihydrofolate (DHF)

Pteridinic synthase (DHA) (DHF synthase)
Acid DHF Reductase Trimethoprim
Dapsone
PAS
Sulfonamide Tetrahydrofolate
s
DNA Synthesis
5. Nuclear Material Inhibitor
a) DNA gyrase Inhibitors : Fluroquinolones , Nalidixic Acid

b) RNA polymerase Inhibitor :RiFamycins Fidaxomicin
c) Direct DNA Inhibitor (Free Radicals) : Nitroimidazole Nitrofuranton
d) Anaerobic pathway Inhibitor (PFOR Inhibitor): Nitroimidazole Nitazoxanide
6. Ointments
a) Protein synthesis Inhibitor

Fusidic Acid Elongation Factor – G inhibitor
Mupirocin Isoleucyl tRNA synthase inhibitor
Retapamulin 50s Ribosome inhibitor
Framycetin
Neomycin 30s Ribosome inhibitor
b) Cell wall & Membrane Inhibitor

Bacitracin

Antibiotics Notes
PHARMACOKINETICS
1.Cell Wall Inhibitors
A. β – lactam Antibiotics
 All β – lactam antibiotics are eliminated by kidney except 4 Penicillinsi.eCloxacillin, Oxacillin,
Naficillin, Dicloxacillin& 2 Cephalosporinsi.eCefoperazone& Ceftriaxone.
 Most of β – lactam are Acid sensitive, so can’t be given by oral route except few like Amox,
Ampicillin, Cefixime, Cloxacillin, Dicloxacillin.
 Pen-G (1st antibiotic) also Acid sensitive, so Pen-V was discovered.
 Pen-G is acidic in nature and eliminated by kidney (Tubular Secretion). Probenicid interferes in
that secretion, and hence prolong duration of action of Pen-G.
 Aztreonam is Morcobactam, contains one β – lactam ring in its structure. Other β – lactams have
two rings. So, Metabolite of Aztreonam is different from other β – lactam, can be tried in β –
lactam Hypersensitive patients.
 Imipenem is a Carbapenem, Metabolised by Dehydropeptidase enzyme in kidney. Given along
with Cilastatin to prevent its degradation.
B. Glycopeptide Antibiotics
 All are eliminated by kidney.
 All are peptide in structure, so can’t be given by oral route except Vancomycin which is given by
oral route as a DOC for Pseudomembranous colitis for its direct local effect on Intestinal wall.
 Teicoplanin can be given by I.V. & I.M route both.
 Dalbavancin, oritavancin and telavancin is long acting antibiotic.
2.Cell Membrane Inhibitor

 All drugs eliminated by kidney.
 All drugs given by parentral route. Polypeptides are peptide, can’t be given by oral route.
Daptomycin used for serious infection in unstable patient.
 Daptomycin is sensitive to surfactant present in lungs, so can’t be given for LRTI.
3.Protein Synthesis Inhibitors

3A Aminoglycosides
 Highly lipid insoluble drugs, so can’t cross membranes easily, won’t get absorbed from GIT, so
given only by parentral route.
 All are eliminated by kidney and cause Nephrotoxicity while elimination.
 Require O2 to take entry in bacteria, so can’t be given for Anaerobic Infection.
3B Tetracyclins
 All Tetracyclinis eliminated by kidney except Doxycycline and Tigecycline.
 Tendency to bind with Ca2+ Ion, so can’t be given with dairy products.
 Should not be given to pregnant and children <7-8 years of age, as these Dry Interferes with
Bone and Teeth growth.
 Minocycline stored in glands (salivary) and hence can be given to eradicate
meningococcemia carrier state.
3C Streptogrammins
 Dalfopristin + Quinopristin, two drugs given in combination of 70:30 ratio.
 Metabolized by liver and can inhibit liver enzyme.
3D Macrolids
 Erymromycin Metabolized by liver and also inhibits liver enzyme.

Antibiotics Notes
 Erymromycinestolate salt can cause Cholestatic Jaundice in pregnancy, so avoided. Succinate
salt should be used.
3E Chloramphenicol
 Metabolized by liver glucoronide conjugation. Glucoronidationis Immature in children and
Neonates, so can result in grey baby syndrome.
4.Folic Acid Pathway Inhibitors

 DSP group of Drugs require both liver and kidney for Metabolism and Elimination.
 Metabolized by liver acetylation reaction.
5.Nuclear Pathway Drugs

 All Fluroquinolone eliminated by kidney except PSM (Pefloxacin, Sparfloxacin, Moxifloxacin).
 Levoflox>ofloxacin has almost 100% oral absorption
 FQ absorption is decreased if taken with divalent cations like Fe, Ca tablets or taken with
antacids.
 Fluoroquinolones particularly ciprofloxacin or pefloxacin increase the plasma concentration of
methylxanthines like theophylline and thus enhance their toxicity.
 Rifampicin and MTZ metabolized by liver, where rifampicin is liver enzyme inducer and MTZ is
liver enzyme inhibitor. Interaction with warfarin is common due to this reason.
PHARMACODYNAMICS
1. Bacteriostatic and Bacteriocidal drugs
Bacteriostatic Bacteriocidal
Folic acid pathway inhibitors Cell wall inhibitors
Protein syntheisis inhibitors Cell membrane inhibitors
Exceptions: Exception:
Cotrimoxazole Nitrofurantoin
Aminoglycosides Nalidixic acid
Streptogrammins
2. Pattern of bacterial inhibition:
Time dependent killing(TDK) and Concentration Dependent killing(CDK)
TDK CDK
Beta lactams aminoglycosides
Vancomycin Fluroquinolones
Erythromycin Azithromycin
Tetracyclin Doxycycline
Clindamycin Daptomycin
Most of new antibiotics
3. Post antibiotic effect (PAE):

Persistent suppression of bacterial growth after limited exposure to an antimicrobial agent is known as the
postantibiotic effect (PAE).The PAE reflects the time required for bacteria to return to logarithmic growth.

Antibiotics Notes
In vivo PAEs are usually much longer than in vitro PAEs. This is thought to be due to postantibiotic
leukocyte enhancement(PALE) and exposure of bacteria to subinhibitory antibiotic concentrations. The
efficacy of once-daily dosing regimens is in part due to the PAE. Aminoglycosides and quinolones possess
concentration-dependent PAEs; thus, high doses of aminoglycosides given once daily result in enhanced
bactericidal activity and extended PAEs.
BACTERIAL RESISTANCE MANAGEMENT

1. Beta lactamase producing Staph aureus: Best drugs are Cloxacillin, oxacillin, naficillin and dicloxacillin. One
can also use beta lactam antibiotic with beta lactamase inhibitors.
2. Other beta lactamase producing bacteria : antibitoics are given alongwith beta lactamase inhibitors.
3. MRSA : Methicillin resistance is developed due to the formation of alternative penicillin binding proteins
that have less affinity for the drugs. Organisms resistant to methicillin (MRSA) are resistant to all other beta
lactam drugs. These resistant organisms are treated by vancomycin or teicoplanin. Vancomycin resistant
staphylococcus (VRSA) can be treated by daptomycin (DOC) ,tigecycline or streptogramins.
4. VRE : linezolid, daptomycin, tigecycline and Streptogrammins(only for E. faecium) are useful
Side Effects of Antibiotics
1. Beta lactam antibiotics:
a. Hypersentivity is common with beta lactam antibiotics. In beta lactam hypersensitive patients,
macrolides > cotrimoxazole can be used in stable patients by oral route and vancomycin>sulasoxazole
can be given to unstable patient by parentral route. In patients of syphilis, beta lactams can be replaced
with doxycycline.
b. Secondary infection : Due to their broad spectrum properties, beta lactams are can ihibit gut flora and
lead to secondary infection like pseudomembranous colitis . it is caused by clostridium difficle. Among all
antibiotics , maximum risk of pseudomembranous colitis is with clindamycin followed by broad
spectrum beta lactam like cephalosporins . Management of pseudomembranous colitis is covered in
indication part of antibiotics.
c. Seizures : in patients of kidney failure, beta lactam antibiotics metabolites accumulate in body and can
lead to seizure. Risk is maximum with imipenem.
d. Bleeding and Disulfiram like reaction : Cephalosporins like cefaperazone, cefoxitin containing N-
Thiomethyl Tetrazole nMTT Ring, inhibit the enzyme aldehyde dehydrogenase. In conjunction with
ethanol consumption, use of these medications can cause a disulfiram like reaction. The nMTT side chain
is also associated with hypoprothrombinemia. It is thought that nMTT depletes vitamin K–dependent
clotting factors by inhibition of vitamin K epoxide reductase.
e. Morbiliform rashes: Ampicillin in some patients can lead to morbiliform rashes which resemble
infectious mononucleosis presentation. There is genetic involvement in this.

Antibiotics Notes
2. Glycopeptide antibitics:
a. Red man/neck syndrome : it is due to histamine release associated vasodilation
b. Nephrotoxicity associated with electrolyte imbalance.
c. Neurotoxicity
d. Ototoxicity
3. Cell membrane inhibitors :

Colisitin like vancomycin can result in Nephrotoxicity associated with electrolyte imbalance, Neurotoxicity,
Ototoxicity
Drugs which can cause nephrotoxicity and ototoxicity are:
1. Cisplatin (max nephrotoxicity)

2. Loop diuretics
3. Cyclophosphamide
4. Ifosfamide
5. Amphotericin B
6. Vancomycin
7. Colistin
8. Cyclosporine
9. Aminoglycosides (max ototoxcity)
4. Aminoglycoside antibiotics :
a. Ototoxicity: Drugs directly damage hair cells of inner ear. This adverse effect is more likely with
prolonged use, high serum concentration (especially with renal impairment), hypovolemia , multiple low
dose pattern of drug administration and alongwith other ototoxic medications . Amikacin, kanamycin
and neomycin are more commonly associated with hearing loss whereas streptomycin and gentamicin
cause predominantly vestibular dysfunction. Ototoxicity starts from base of cochlea (high frequency) and
progress to the apex (low frequencies). Netilimicin is least ototoxic aminoglycoside.
b. Nephrotoxicity: It is associated with electrolyte imbalance. Risk factors for nephrotoxicity include
hypokalemia, pre-existing renal disease and concomitant nephrotoxic medications (like Amphotericin B,
vancomycin etc.). Neomycin is most nephrototoxic and is not indicated for systemic use. Among the
systemically used aminoglycosides, gentamicin is most nephrotoxic. Streptomycin is least nephrotoxic.
c. Neuromuscular blockade: It occurs due to inhibition of pre-synaptic release of Ach. Hypocalcemia,

peritoneal administration, use of neuromuscular blocker and pre-existing respiratory depression
constitutes risk factors. This adverse effect can lead to rare but severe respiratory depression .If
respiratory depression occurs, it is reversed by i.v. administration of calcium. Neomycin (not used) and
streptomycin have maximum potency of causing neuromuscular block whereas tobramycin is least
potent in this regard. These drugs are therefore contra-indicated in myasthenia gravis.
d. Teratogenesis: aminoglycosides are contraindicated in pregnancy. Newborn can have defects of inner
ear if mother take these drug during pregnancy.
5. Tetracyclines :
a) Secondary infection and pseudomembranous colitis.
b) Drugs are contra-indicated in pregnancy and young children (< 8 years age) due to the risk of tooth
enamel dysplasia and irregularities in the fetal bone growth. Reason is binding of drugs with calcium.
c) High dose of tetracycline may lead to hepatic necrosis
d) Expired demeclocycline use may lead to Fanconi’s syndrome
e) Demeclocycline can result in photosensitivity and Diabetes insipidus
f) Minocycline may lead to dose dependent vestibular toxicity

Antibiotics Notes
6. Streptogrammins :
a) Venous irritation when given by central line
b) Arthralgia and myalgia
7. Macrolides :
Diarrhea is the most common and important side effects of all macrolides. It is due to the stimulation of
motilin receptors in intestine.
8. Lincosamides (Clindamycin):
Secondary infection : Due to its broad spectrum properties, clindamycin can inhibit gut flora and lead to
secondary infection like pseudomembranous colitis . It is caused by clostridium difficle bacteria. Among all
antibiotics , maximum risk of pseudomembranous colitis is with clindamycin followed by broad spectrum
beta lactam like cephalosporins
9. Linezolid
a. Thrombocytopenia and neutropenia. Blood counts should be monitored if duration of therapy
exceeds one week.
b. It also possesses MAO inhibitory activity and can cause serotonin
c. Optic neuritis
d. Peripheral neuropathy
e. Lactic acidosis
10. Chloramphenicol :
a. Grey baby syndrome
b. Bone marrow suppression( maximum)
c. Secondary infection of GIT
11. Sulfonamides :
a) Hypersensitivity (most common)
b) Aplastic anemia (more common in hiv infected patients).
c) Hemolysis in patients with G-6 PD deficiency.
d) Crystalluria due to deposition in kidney
e) Jaundice or kernictucs by displacing bilirubin from plasma protein binding sites
f) Hepatotoxicity
12. Fluroquinolones:
a) Tendinitis and cartilage development problems, avoided in children less than 18 years old and in
pregnancy..
b) Phototoxicity (maximum with lomefloxacin and sparfloxacnin.)
c) Hypoglycemia ( max with Gatifloxacin systemic use) .
d) Sparfloxacin and gatifloxacin prolong QTc interval (grepafloxacin was withdrawndue to same reason).
e) Trovafloxacin has hepatotoxic potential (withdrawn ).
f) Fluoroquinolones are contra-indicated in epilepay. NSAIDs increase CNS toxicity (seizures) of these
drugs.
g) Peripheral Neuropathy

Antibiotics Notes
Specific Indications
β – Lactams
Penicillins
1. Pen – G
(spectrum g +ve Cocci & Bacilli , g –ve cocci, Anaerobes )

(Not effective g-ve Bacilli, Bacteroids , Fusobacterium, Mycoplasma)
DOC :
Pneumococcus gasgangrene
Actinomycetes leptospirosis
Streptococcus anaerobic Infection(IstLine)
syphillis
Staphylococcus (If sensititve) Spirillum Minor
2. Cloxacillin, Oxacillin, NaFicillin, Dicloxacillin

(spectrum Pen G + β tactamase S.Aureus) DOC
Ist line empirical Drugs for soft tissue infection
3. Extended Spectrum Penicillin

[spectrum Pen – G + g-ve Bacilli]
(given alongwith β – lactamase Inhibitor to cover β – lactamase + Bacteria)
a)Amox, Ampi : All g –ve Bacilli except pseudomonas
Amox + Clav DOC: empirical for Dental Surgery & otitis media(in india due to haemophilus influenza
resistance)
Ampi DOC : Listeria, enterococcus
b) (Anti pseudomonal penicillin)

Carbencillin , Azlocillin, Mezlocillin , Piperacillin, Ticarcillin.
Useful for all g –ve Bacilli including pseudomonas
Cephalosporin
(Not effective against Listeria)
1. gen – I (Mainly against g +ve)

Cephalexin (g +ve& β – lactamase S.Aureus)
st
(I line empirical Dry for soft tissue infection )

Antibiotics Notes
Cefazolin MIC used Ab for Surgical prophylaxis
(Injected just before Incision)
2. gen – II (Few g +ve & Many g –ve) (spectrum Incomplete )

Cefamycin Subgroup
Cefoxitin g –ve &
Cefotetan Anaerobic empirical Ab for serious
Cefmetazole Bacteria Abdominal Infection
3. gen – III(Few g +ve<<<< Almost all g –ve)

Ceftriaxone empirica lIst line Drug for Meningitis, CNS abscess, endocarditis, enteric fever
DOC :enteric fever (unstable & hospitalised) , gonococcus systemic Infection
Cefotaxime
DOC :Meningococcus Meningitis, H.Influenza Meningitis
For prophylaxis Ciplox, Rifampicin
Ceftazidime DOC : pseudomonas
Cefixime 400mg stat for STD by gonococcus
4. gen – IVceph (Broad spectrum)Cefipime, cefipirome

[spectrum All g +ve = g –ve, pseudomonas]
DOC : Class – C resistant β – Lactamase producing bacteria
5.Anti MRSA cephalosporin

Ceftaroline, ceftibiprole
Monobactams (Aztreonam)
 DOC :Class B resistant β – Lactamase producing bacteria
 pseudomonas
 can be given to penicillin allergic patient
Carbapenoms (Broad spectrum)

[spectrum: All g +ve = g –ve bacteria including pseudomonas]
DOC :Class A resistant β – Lactamase producing bacteria (ESBL), Serratia, Acenitobacterium
Also Ist line Drug for Burkholderia Infection
INDICATIONS OF OTHER ANTIBIOTIC GROUPS
1. Glycopeptide Abs
Vancomycin
 MRSA (Doc)
 Pseudo Colitis (Doc)
 1st line empirical drug for endocarditis, meningitis, CNS absence, septic shock

Antibiotics Notes
2. Polypeptide Ab
 Pseudomonas
 Acineto bacterium
3. Aminoglycosides
 Useful mainly against g –ve
 Not useful against anaerobic
 TB—Streptomycin Capreomycin, Amikacin Kanamycin (SACK)
 Pseudomonas—Tobramycin, Amikacin, Gentamycin (TAG)
 Doc Tularemia [strepto]
 Doc Plague [strepto]
 Doc Brucellosis [genta]
4. Tetracycline (Doxy is used)

Rich Ricketssiac (Doc)
Reliance Relapsing fever Borreli
Ricketssia
Brother Brucellosis (Oral first line drug)
Love LGV (Doc)
Cool Cholera (Doc)
Green Granuloma Inguinale (Doc)
Park Prophylaxis (Doc)
Malaria (<6 weeks)
Leptospirosis
Plague
5. Steprogrammins
MRSA, VRSA, VRE Faecium
6. Macrolides
Erythromycin
 Doc Corynbacterium Diphtheria
 Doc Bordetella pertussis
Azithromycin
 Doc Cat Scratch Disease
 Doc Chaneroid (H. Ducreyi)
 Doc Ligonella
 Doc Atypical Pneumonia (Mycoplasma)
 1stline empirical drug for pneumonia
 Doc STD caused by gonococcus
 Doc Campylobacter jejuni
Clarithromycin
First Line Drug
MAC H pylon
(REC Regimen) (Triple Regimen)
RiFabutin +ethambutol +clarithromycin Clarithromycin+MTZ/Amox +PPI

Antibiotics Notes
Spiramycin
--Doc Toxoplasmosis in pregnancy
7. Linezolid
 MRSA
 TB
8. Dapsone
 M. Leprae
 Auto Immune Disease
 Doc Dermatitis Herpetiformis
9. PAS TB
10. Sulfonamides
 Sulfadoxine + pyrimethamine P.Falciparum
 Sulfadiazine + pyrimethamine Toxoplasmosis
 Sulfasalazine
ASA Sulfapyridesic
Anti-inflammatory Immunoruppressive
IBD RA
 Silversulfadiazine
Empirical drug of choice for burn pt.
11. Cotrimoxazole
 Doc P.Carrui
 Doc Nocardiam
 TB
 MRSA
 1st line empirical drug for pneumonia present in <12 years
12. FQ
 Mainly given for g –ve
 Empirical DOC for infective diarrhea & UTI.
 Doc E-coli, shigella, salmonella, proteus
 Ciprofloxacin
Doc Bacillus
Pseudomonas
 Respiratory FQ
Levoflox, Oflox, Gemiflox, Moxiflox
(1st line empirical drug for pneumonia)
 TB
Levoflox, Oflox, Moxiflox
13. Nitroimidazole

Antibiotics Notes
MTZ
Doc Amoebiasis
Doc Gardiasis Anti Protozoal
Doc T. Vaginalis
Doc C. Tetani
Tlt C. difficle Antibiotic against
Doc Bacteroides Anaerobes
Doc Fusobacterium
14. Nitazoxanide
Ab Anti Protozoal Antiviral

C. Difficle Luminal Amoebiasis Herpes, Hepatitis
(P. Colitis)
SPECIFIC BACTERIA
1. Drugs useful for Pseudomonas:
I. β – Lactamase
Penicillin All extended spectrum except Amox, Ampi
Cephalosporin gen – III (cefoperazone ,ceftazidime)

gen – IV (cefipime, cefipirome)
Monobactams Aztreonam
Carbapenems Meropenem, Dorepenem
II. Aminoglycosides
T Tobramycin
A Amikacin
G Gentamycin
III. Fluroquinolones
Ciplox>Levoflox
IV. Polypeptide Ab
Colistin
[TOC Ceftazidime + Aminoglycoside]

Antibiotics Notes
2. Clostridium
1)C.Difficile (pseudomembranous colitis)

(Mild, Mod, Severe, Fulminant)
Adult
Mild to severe oral vanco> Fidaxomicin

Fulminant I.V.MT2 + oral vanco
Children
Mild to Mod. Oral MT2

Severe to Fulminant oral vanco
Recurrent Infection
(>2 episodes)
Ab + Fecal Microbiota Transplantation
Systematic Manifestation
(Toxin B)
Ab + Bezlotoxumab
2) C. Perferinges (gas gangrene) Pen G

3) C. Tetani (Tetanus) MTZ
4) C. Botulinum (Botulism) Antitoxin
3. Syphillis (T.pallidum)
DOC:Pen – G
Pen - G
Aq. Pen G Procaine Pen G Benzathine Pe

Benzyl Pen G
DurationShortest (2 days) Intermediate Longest (21 days)

Onset Fastest Intermediate Slowest
Use Acute Emergency used as Alternative of other two Maintenance t/t

Antibiotics Notes
TABLE5 51-1 Empiric antimicrobial therapy based on microbiologic etiology. (Continued)
Suspected or Proven Disease Drugs of First Choice Alternative Drugs

or Pathogen
Mycobacteria
Mycobacterium tuberculosis Isoniazid + rifampin Streptomycin, moxifloxacin,
+ethambutol + pyrazinamide amikacin, ethionamide,
cycloserin, PAS, linezolid
Mycobacterium leprae
Multibacillary Dapsone + rifampin +
clofazimine
Paucibacillary Dapsone + rifampin
Mycoplasma pneumoniae Tetracycline, erythromycin Azithromycin, clarithromycin,
quinolone
Chlamydia
C trachomatis Tetracycline, azithromycin Clindamycin, ofloxacin
C pneumoniae Tetracycline, erythromycin Clarithromycin, Azithromycin
C psittaci Tetracycline Chloramphenicol
Spirochetes
Borrelia recurrentis Doxycyline Erythromycin,
Chloramphenicol, penicillin
Borrelia burgdorferi
Early Doxycyline, amoxicillin Cefuroxime axetil, penicillin
Late Ceftriaxone
Leptospira species Penicillin Tetracycline
Treponema species Penicillin Tetracycline, Azithromycin,
Ceftriaxone
Fungi
Aspergillus species Voriconazole Amphotericin B, itraconazole,

Antibiotics Notes
caspofungin, isavuconazole
Blastomyces species Amphotericin B Itraconazole, fluconazole
Candida species Amphotericin B, Fluconazole, itraconazole,
echinocandin voriconazole
Cryptococcus neoformans Amphotericin B ± flucytosine Fluconazole, voriconazole
(5-FC)
Coccidiodies immitis Amphotericin B Fluconazole, itraconazole,
voriconazole, posaconazole
Histoplasma capsulatum Amphotericin B Itraconazole
Mucoraceae (Rhizopus, Amphotericin B Posaconazole, isavuconazole
Absidia)
Sporothrix schenchkii Amphotericin B Itraconazole
TABLE 51-2 Empiric antimicrobial therapy based on site of infection.
Presumed Site of Common Pathogens Drugs of First Alternative Drugs

Infection Choice
Bacterial
endocarditis
Acute Staphylococcus Vancomycin + Penicillinase-resistant
aureus ceftriaxone penicillin +
gentamicin
Subacute Viridians Penicillin + Vancomycin +
streptococci, gentamicin gentamicin
entreococci
Septic arthritis
Child Haemophilus Vancomycin + Vancomycin +
influenza, s aureus, β- ceftriaxone ampicillin-sulbactam
hemolytic or ertapenem
streptococci
Adult s aureus, Vancomycin + Vancomycin,
enterobacteriaceae, ceftriaxone ertapenem, or
Neisseria quinolone
gonorrhoeae
Acute otitis media, H influenza, Amoxicillin Amoxicillin-
sinusitis streptococcus clavulanate,
pneumonia, cefuroxime axetil,
Moraxella catarrhalis TMP-SMZ
Cellulitis S aureus,group A Pencillinase-resistant Vancomycin,
streptococcus penicillin, clindamycin,
cephalosporin (first- linezolid, daptomycin
generation)
Meningitis
Neonate Group B Ampicillin + Ampicillin +
streptococcus, cephalosporin (third- aminoglycoside,
Escherichia coli, generation) chloramphenicol,
Listeria meropenem
Child H influenzae, Ceftriaxone or Chloramphenicol,
pneumococcus, cefotaxime ± meropenem

Antibiotics Notes
meningcoccus vancomycin
Adult Pneumococcus, Ceftriaxone, Vancomycin +
meningcoccus cefotaxime Ceftriaxone or
cefotaxime
Peritonitis due to Coliforms, Metronidazole + Carbapenem +
ruptured viscus bacterioides fragilis cephalosporin (third- tigecycline
generation),
piperacillin/tazobacta
m
Pneumonia
Neonate As in neonatal
meningitis
Child Pneumococcus, S Ceftriaxone, Ampicillin-sulbactam
aureus, H influenzae cefuroxime,
cefotaxime
Adult (community- Pneumococcus, Outpatient: Outpatient:
acquired) Mycoplasma, Macrolide, Quinolone
Legionella, H amoxicillin,
influenzae, S aureus, tetracycline
Chlamydophila
pneumonia, coliforms
Impatient: Macrolide Impatient:
+ cefuroxime, Doxycycline +
ceftriaxone, cefotaxime,
ertapenem, or ceftriaxone,
ampicillin ertapenem, or
ampicillin; respiratory
quinolone
Septicemia Any Vancomycin +
cephalosporin (third-
generation) or
piperacillin/tazobacta
m or imipenem or
meropenem
Septicemia with Any Antiseudomonal
granulocytopenia penicillin +
aminoglycoside;
ceftazidime;
cefepime; imipenem
or meropenem;
consider addiction of
systemic antifungal
therapy fever persists
beyond 5 days of
empiric therapy

Antibiotics Notes
TABLE 51-1 Empiric antimicrobial therapy based on microbiologic etiology.
Suspected or Proven Drugs of First Choice Alternative Drugs

Disease or Pathogen
Gram–negative cocci
(aerobic)
Moraxella (Branhamella) TMP-SMZ, cephalosporin Quinolone, macrolide
catarrhalis (second/third-generation)
Neisseria gonorrhoeae Ceftriaxone, cefixime Spectinomycin, azithromycin
Neisseria meningitidis Penicillin G Chloramphenicol, ceftriaxone,
cefotaxime
Gram–negative rods
(aerobic)
E coli, Klebsiella, Proteus Cephalosporin (first/second- Quinolone, aminoglycoside
generation), TMP-SMZ
Enterobacter, Citrobacter, TMP-SMZ, quinolone, Antipseudomonal penicillin,
Serratia carbapenem aminoglycoside, cefepime
Shigella Quinolone TMP-SMZ, ampicillin,
azithromycin, ceftriaxone
Salmonella Quinolone, ceftriaxone Chloramphenicol, ampicillin,
TMP-SMZ
Campylobacter jejuni Erythromycin or azithromycin Tetracycline, quinolone
Brucella species Doxycycline + rifampin or Chloramphenicol +
aminoglycoside aminoglycoside or TMP-SMZ
Helicobacter pylori Proton pump inhibitor + Bismuth + metronidazole +
amoxicillin + clarothrimycin tetracycline + proton pump
Vibrio species Tetracycline Quinolone, TMP-SMZ
Pseudomonas aeruginosa Antipseudomonal penicillin + Antipseudomonal penicillin ±
aminoglycoside quinolone, cefepime,
ceftazidime, antipseudomonal
carbapenem, or aztreonam ±
aminoglycoside
Burkholderia cepacia TMP-SMZ Ceftazidime, chloramphenicol
(formerly Pseudomonas
cepacia)
Stenotrophomonas TMP-SMZ Minocycline, ticatcillin-
maltophilia (formerly clavulanate, tigercycline,
Xanthomonas maltophilia) ceftazidime, quinolone
Legionella species Azithromycin or quinolone Clarothrimycin, erythromycin
Gram-positive cocci
(aerobic)
Streptococcus pneumonia Penicillin Doxycycline, ceftriaxone,
antipneumoccoccal
quinolone, macrolide,
linezolid

Antibiotics Notes
Streptococcus pyogenes Penicillin, clindmaycin Erythromycin, cephalosporin
(group A) (first-generation)
Streptococcus agalactiae Penicillin (±aminoglycoside) vancomycin
(group B)
Viridians Streptococci Penicillin Cephalosporin (first-or-third-
genration),2 vancomycin
Staphylococcus aureus
β-Lactamase negative Penicillin Cephalosporin(first-
genration),2 vancomycin
β-Lactamase positive Penicillin-resistant penicillin As above
Methicillin-resistant Vancomycin TMP-SMZ, minocycline,
linezolid, daptomycin,
tigecycline
Enterococcus species Penicillin + aminoglycoside Vancomycin +
aminoglycoside
Gram-positive rods
(aerobic)
Bacillus species (non- Vancomycin Imipenem, quinolone,
anthracis) clindmaycin
Listeria species Ampicillin (±aminoglycoside) TMP-SMZ
Nocardia species Sulfadiazine, TMP-SMZ Minocycline, imipenem,
amikacin, linezolid
Anaerobic bacteria
Gram-positive (clostridia, Penicillin, clindmaycin Vancomycin, carbapenem,
Peptococcus, Actinomyces, chloramphenicol
Peptostreptococcus)
Clostridium difficile Metronidazole Vancomycin, bacitracin
Bacteroides fragilis Metronidazole Chloramphenicol,
carbapenem, β-lactam----β-
lactamase-inhibitor
combinations, clindmaycin
Fusobacterium, Prevotella, Metronidazole, clindmaycin, As for B fragilis
Porphyromonas penicillin

Antibiotics Notes
TABLE 51-8 Recommendations for nonsurgical antimicrobial prophylaxis.
Infection to be Indication(s) Drug of Choice Efficacy

prevented
Anthrax Suspected exposure Ciprofloxacin or Proposed effective
doxycyclin
Cholera Close contacts of a Tetracycline Proposed effective
case
Diphtheria Unimmunized Penicillin or Proposed effective
contacts erythromycin
Endocarditis Dental, oral or upper Amoxicillin or Proposed effective
respiratory tract clindamycin
procedures in at-risk
patients
Genital herpes Recurrent infection Acyclovir Excellent
simplex (≥4 episodes per
year)
Perinatal herpes Mothers with primary Acyclovir Proposed effective
simplex type 2 HSV or frequent
infection recurrent genital HSV
Group B Mothers with cervical Ampicillin or Excellent
streptococcal (GBS) or vaginal GBS penicillin
infection colonization and their
newborns with one or
more of the
following: (a) onset
of labor or membrane
rupture before 37
weeks’ gestation, (b)
prolonged rupture of
membranes (>12
hours), (c) maternal
intrapartum fever, (d)
history of GBS
bacteriuria during
pregnancy, (e)
mothers who have
given birth to infants
who had early GBS
disease or with a
history of
streptococcal
bacteriuria during
pregnancy
Haemophilus Close contacts of a Rifampin Excellent
influenzae type B case in incompletely
infection immunized children
(>48 months old)
HIV infection Health care workers Tenofovir/emtricitabi Good
exposed to blood ne and raltegravir
after needle-stick
injury

Antibiotics Notes
Pregnant HIV- HAART Excellent
infected women who
are at ≥14 weeks of
gestation; newborns
of HIV-infected
women for the first
time 6 weeks of life,
beginning 8-12 hours
after birth
Influenza A and B Unvaccinated Chloroquine Excellent
geriatric patients,
immunocompromised
hosts, and health care
workers during
outbreaks
Malaria Travelers to areas Chloroquine Excellent
endemic for
chloroquine-
susceptible disease
Travelers to areas Mefloquine, Excellent
endemic for doxycyline or
chloroquine-resistant atovaquone/proguanil
disease
Meningococcal Close contacts of a Rifampin, Excellent
infection case ciprofloxacin or
ceftriaxone
Mycobacterium HIV-infected patients Azithromycin, Excellent
avium complex with CD4 count clarithromycin or
<75/μL rifabutin
Otitis media Recurrent infection Amoxicillin Good
Pertussis Close contacts of a Azithromycin Excellent
case
Plague Close contacts of a Tetracycline Proposed effective
case
Pneumococcemia Children with sickle Penicillin Excellent
cell disease or
asplenia
Pneumocystis jiroveci High-risk patients Trimethorpim- Excellent
pneumonia (PCP) (eg, AIDS, leukemia, sulfamethoxazole,
transplant) dapsone, or
atovaquone
Rheumatic fever History of rheumatic Benzathine penicillin Excellent
fever or known
rheumatic heart
disease
Toxoplasmosis HIV-infected patients Trimethoprim- Good
with lgG antibody to sulfamethoxazole
Toxoplasma and CD4
count <100/μL
Tuberculosis Persons with positive Isoniazid or rifampin Excellent

Antibiotics Notes
tuberculin skin tests or isoniazid +
and one or more of rifapentine
the following: (a)
HIV infection, (b)
close contacts with
newly diagnosed
disease, (c) recent
skin test conversion,
(d) medical
conditions that
increase the risk of
developing
tuberculosis, (e) age
<35 y.
Urinary tract Recurrent infection Trimethoprim- Excellent
infections (UTI) sulfamethoxazole
CLINICAL POSSIBLE TREATMENT COMMENTS

SYNDROME ENTIOLOGIES
Meningococcemia N. meningitdis Penicillin (4 mU q4h) Ceftriaxone
or celtriaxone (2 eradicates
gq12h) nasopharyngeal
carriage of the
organism. Close
contacts require
chemoprophyfaxis
with rifampin (600
mg q12h for 2 days)
or ciprofloxacin (a
single dose, 500 mg).
Rocky mountain Rickettsia rickettsii Doxycycline (100 mg If both
spotted fever (RMSF) bid) meningococcemia
and RMSF are being
considered, use
ceftriaxone (2g q12h)
plus doxycycline (100
mg bid). If RMSF is
diagnosed,
doxycycline is the
proven superior
agent.
Purpura fulminans S. pneumoniae, H. Ceftriaxone (2 gq If a β-lactam-
influenzae, N. 12h) plusvancomycin sensitive strain is
meningitdis (15 mg/kg q12h)b identified,
vancomycin can be
discontinued.
Erythrodema: toxic Group A Vancomycin (15 If a penicillin or
shock syndrome Streptococcus. mg/kg q12h)b plus oxacillin-sensitive
Staphylococcus clindamycin (600 mg strain is isolated,
aureus q8h) these agents are
superior to
vancomycin

Antibiotics Notes
(penicillin, 2 mU q4h;
or oxacillin, 2 g IV
q4h). The site of
toxigenic bacteria
should be debrided; I
V immunoglobulin
can be used in severe
cases.

SYNDROME ETIOLOGIES
Cerebral malaria Plasmodium Artesunate (2.4 mg/kg Do not use
falciparum IV at 0,12 and 24 h; glucocorticoids. Use
then once daily) or IV quindine if IV
quinine (IV loading quinine is not
dose of 20 mg salt/kg; available. During IV
then 10 mg/kg q8h) quinidine treatment,
blood pressure and
cardiac function
should be monitored
continuously and
blood glucose
periodically.
Spinal epidural Staphylococcus spp., Vancomycin (15 Surgical evaluation is
abscess gram-negative bacilli mg/kg q12h) plus essential. If a
either penicillin or oxacillin-
Piperacillin/tazobacta sensitive strain is
m (3.375-4.5 g q6h) isolated, these agents
or cefepime (2 g q8h) are superior to
vancomycin
or oxacillin, 2 g q4h).
Focal Infections
Acute bacterial S. aureus, β- Ceftriaxone (2 g Adjust treatment
endocarditis hemolytic q12h) plus when culture data
streptococci, HACEK vancomycin (15 become available.
group, Neisseria spp., mg/kg q12h) Surgical evaluation is
S.pneumoniae essential.
Empirical Treatment for Common Infectious Disease Emergencies.

SYNDROME ETIOLOGIES
Sepsis without a Clear Focus
Septic shock Pseudomonas spp., Vancomycin (15 Empirical therapy
gram-negative enteric mg/kg q 12h)b plus should be tailored to
bacilli, gentamicin (5 mg/kg local resistance
Staphylococcus spp., per day) plus either patterns. Adjust
Streptococcus spp. Piperacillin/tazobacta treatment when

Antibiotics Notes
m (3.375-4.5 g q6h) culture data become
or cefepime (2 g available.
q8h)c
Overwhelming post- Staphylococcus Ceftriaxone (2 g If a β-lactam-
splenectomy sepsis pneumoniae, q12h) plus sensitive strain is
Haemophilus vancomycin (15 identified,
influenzae, Neisseria mg/kg q12h)b vancomycin can be
meningitidis discontinued.
Babesiosis Babesia microti Clindamycin (600 Atovaquone and
(U.S.), B, divergens mg q8h) plus quinine azithromycin can be
(Europe) (650 mg q8h) used in less severe
disease and are
associated with fewer
side effects.
Treatment with
doxycycline (100 mg
bid) for potential co-
infection with
Borrelia burgdorferi
or Anaplasma spp,
may be prudent.
Sepsis with Skin Findings

SYNDROME ETIOLOGIES
Sepsis with Solt Tissue Findings
Necrotizing fascilitis Group A Vancomycin (15 Urgent surgical
Steptococcus, mixed mg/kg q12h)b plus evaluation is critical.
aerobic/anaerobic clindamycin (600 mg Adjust treatment
flora, CA-MIRSA q8h) plus gentamicin when culture data
(5 mg/kg per day) become available.
Clostridial Clostridium Penicillin (2 mU q4h) Urgent surgical
myonecrosis perfringens plus clindamycin evaluation is critical.
(600 mg q8h)
Neurologic Infections
Bacterial meningitis S. pneumoniae, N. Ceftriaxone (2 g If a β-lactam-sensitive
meningitides q12h) plus strain is identified,
vancomycin (15 vancomycin can be
mg/kg q12h) discontinued. If the
patient is >50 years
old or has comorbid
disease, add
ampicillin (2 g q4h)
for Listeria coverage.
Dexamethasone (10
mg q6h for 4 days)
improves outcome in
adults with
meningitis (especially

Antibiotics Notes
pneumococcal).
Brain abscess, Streptococcus spp., Vancomycin (15 Urgent surgical
suppurative Staphylococcus spp., mg/kg q12h) plus evaluation is critical.
intracranial infections anaerobes, gram- metronidazole (500 If a penicillin-or
negative bacilli mg q8h) plus oxacillin-sensitive
ceftriaxone (2 g q12h) strain is isolated,
these agents are
superior to
vancomycin
or oxacillin, 2 g q4h).
ANTI - CANCER DRUGS

TOTAL 7 GROUPS
GROUP 1 : ALKYLATING AGENTS
MOA
Alkylating Donates Alkyl Binds to DNA of CA cell at Cross linking DNA Replication
Agent Group 7th N2 of Guanine Base pair of DNA Inhibited
(N7 Guanine)
CA cell growth
S/E
: 8 common S/E
2° leukemia
L liver veno occlusive Disease (prevented by Defibrotide)
G GIT Toxicity (Nausea, Vomiting, Diarrhoea ) (M/C S/E)
S Sterility
T Teratogenecity
A Alopecia
H Myelosuppresssion (M/C Dose limiting Toxicity )
P Pulmonary Fibrosis
NOTES :
1. 2° leukemia: Leukemia caused by Drugs. [ M/C AML]

Seen after (1-2 yrs) early leukomegenic drugs

Antibiotics Notes
(3-4 yrs) late leukomegenic drugs
Alkylating agents are late leukomegenic .
2.GIT Toxicity : M/C S/E of any anti cancer drugs

N&V DOC: 5HT3 Inhibitor
Diarrhoea DOC: Loperamide
3. Myelosuppression : M/C Dose limiting toxicity of any anticancer drug except Vincristine &
Bleomycin
T/t : Blood cell growth factor
4. Pulmonary Fibrosis :Long term S/E

Mainly due to destruction of Type I epithelial cells of alveoli & excessive
proliferation of Type II cells.
Important Drugs, their indicators & unique S/E

5 types of Alkylating Agents
Ia
: N2MUSTARDS
DRUGS INDICATIONS S/E
1. Cyclofosfamide Soft tissue CA  Cardiotoxicity
Ifosfamide (more potent) osteosarcoma  SIADH
Breast CA Nephrotoxicity
Active Metabolite : Aldofosfamide Neurotoxicity Prevention
Hmgic cystitis By MESNA
(due to Acrolein Metabolite )
Leads to bladder CA

Antibiotics Notes
2. Mechlorethamine Cut T cell lymphome  Skin ulceration& Blister
3. Chlorambucil CLL -
4. Melphalan Multiple Myelomas -
5. Bendamustine Lymphoma -
Ib
so : NITROSOUREAS
ur
1.eSLomustine CNS tumor due to
Carmustine lipid solubility
Semustine
2. Streptozocin β – cell tumor Fanconi’s AnemiA
Ic
so : THIAZINES
ur
1.eSProcarbazine lukemias & lumphomas Sedation & Drowziness
Dacarbazine Cheese Rxnwith MAOI
Disinfection Rxnwith
ethanol
2. Temozolamide DOC : Glioblastoma
Multiforme -
Id
so : SULFATE
ur
eS Busulfan CML  Adrenal gland suppression
(Addison’s Disease)
 Skin pigmentation
Ie
so : ETHYLAMINES
ur
eS Altretamine
ThioTEPA

Antibiotics Notes
2. ANTI - METABOLITES
MOA  DNA SYNTHESIS INHIBITOR
FA Pathway Inhibitor DNA Polymerase Inhibitor
1.  MTX 3.Purine analogues
2.Pemetrexed 4.Pyrimidine analogues
S/E
6 common S/E : G-STAMP
MIC  GIT Toxity
Dose limiting BM
Important Drugs & their S/E & Indicators
1. MTX
MOA DHFrase Inhibitor  FA synthesis Inhibitor
Indication :
a) Anti Cancer (Given in High Dose )
 DOC: Choriocarcinoma
Brukit’s ymphoma
ALL
Osteosarcoma
Breast CA
b) Immunosuppression (Given in Low Dose)
R.A.
Psoriasis
IBD
 Organ Transplantation

Antibiotics Notes
c) MISC: ectopic pregnancy
MTx
PK a) Lipid Insoluble
Inhibitor BBB Inhibitor Membrane
Given by Intrathecal route for ALL Takes entry in CA cell with help of
During consolidation phase T/t influx pump
b) Acidic in nature Binds to Albumin NSAIDS can displace it from alnumin , & can lead to
toxicity.
c) Action long lastingIt get stored in CA cell with ombination with proteins & keeps on getting
released slowly.
d) Kidney elimination  [Tubular secretion (T.S.) > Filtration ] NSAIDS can inhibit T.S. of MTx
and can lead to it toxicity.
S/E : G-Stamp (common S/E) , seen at dose , particularly for osteosarcoma.

 Liver Fibrosis(LFT required 3 monthly)
CNS Toxicity (particularly given by spinal route) (Max among all anti CA drugs )
Toxicity
: 3 MCQs
1. Prevention  Leucovorin / Folinic Acid
2. T/t Forced alkaline diuresis
3. T/t in CRF pts. Glucarpidase by I.V. Route
Resistance of MTx
:
1. MIC : excessive production of DHFRase enzyme. (gene amplification )
2. Mutation of DHFRase enzyme.

Antibiotics Notes
3. Mutation of influx pump.
4. Induction of efflux pump (p- glycoprotein pump)
p-gp is product of MDR- 1 gene. Once it is induced , CA cell becomes MDR.
p-gp helps in overcoming MDR CA.
2. PEMETREXED
MOA Multiple enzyme inhibitor in F.A. pathway like –
a) Thymidate synthase inhibitor
b) DHFRase enzyme inhibitor
INDICATION NSCC Lung, Mesothelioma.
S/E G- STAMP, Hand & Foot syndrome (Disease of skin ulceration )
TOXICITY prevention  Folic Acid.
3. PURINE ANALOGUES
Structure resembles purine.
All drugs are DNA polymerase inhibitors.
All are competitive inhibitors.
All inhibit enzyme after incorporation in structure of DNA.
PURINE ANALOGUES
DRUG INDICTIONS S/E TOXICITY
a. 6-Mercaptopurine ALL Allopurinol ppt. Toxicity as
6-MP is metabolised by
Xanthine oxidase enzyme.
b. Pentostatin DOC: Hairy cell
Cladribine leukemia
c. Nelarabine
Clofarabine other drugs
6-Thioguanine in this group

Antibiotics Notes
4. PYRIMIDINE ANALOGUES : (Same common pts as purine analogues)

DRUG INDICATIONS S/E TOXICITY
a.5-FU (given by I.V.route) Colorectal CA  Hand & Foot syndrome

(t1/2<<< ) (Anti cancer activity
By Folinic Acid)
b.Capecitabine Colorectal CA  Hand & Foot syndrome

(precursor of 5-FU)
(given by oral route )
c.Gemcitabine Non β – cell tumor of  Flu like symptoms

pancreas
d.Cytarabine ALL  cerebellar toxicity
e.Decitabine other drugs
Azacytidine in group
3. ANTI MITOTIC
MOA  Mitotsis Inhibitor
3a)Vinca Alkaloids (Plants & Trees)
Vincristine, Vinblastine
MOA Spindle formation inhibitor by inhibiting refubular protein
Indication  ALL
S/E  B  BM (rarely seen c vincristine)
R Rashes (HSN RXN) (Alkaloids )
AAlopecia
I Inhibition of spindle (MOA)
N N&V (M/C S/E), Neuropathy (Motor) ( Max : among anti CA drug)

Antibiotics Notes
S S/ADH
3b)Taxane Alkaloids (Plants & Trees)
MOA overstablise the spindle, so cell cycle can’t enter in anaphase stage from metaphase.
Indication Paclitaxel Breast CA , ovarian CA
Docetaxel
Cabazitaxel Prostate CA
S/E BBM
R Rashes (HSN Rxn)
A Alopecia
N N&V, Neuropathy (Motor)
O over stabilisation of spindle (MOA)
3c)IxabepiloreSame as taxane but not an alkaloid. Useful for breast CA.
3d)Estramustine  Contains estrogen. Useful for prostate CA.
4. ANTICANCER ANTIBIOTICS
MOA i) Direct DNA Inhibitors with free radicals. CCNS : Inhibit cell cycle in [except Bleomycin]
ii) Topoisomerase Inhibitor any stage.
S/E i) M/C  N&V&D
ii) Dose limiting  Myelosuppression

iii) In G6PD pts  Hemolysis
iv)Pulmonary Fibroisis
4a) Anthracycline Abs : Doxorubicin, Duanorubicin.
Indication ALL
S/E  Cardiotoxicity (Dilated cardio myopathy )
(prevented by Dexrazoxane)
4b) Mitoxantrone Anthracycline Ab, but no cardiotoxicity.
4c) Actinomycin – D Useful for Ewings’s Sarcoma.

Antibiotics Notes
4d) Bleomycin
Indication Testicular CA
S/E BMsuppression and flagellate hyperpigmentation at back.
4e) Mitomycin –C
Indication 1. Bladder CA
2. Anorectal CA
3. Tracheobronchial Stenosis Given locally for Antifibrotic
4. After Pterygium Sx Property
5. TARGETED CHEMOTHERAPY
(Specific Action ) (less S/E)
5a) abl : bcr Tk Inhibitor T/t : CML
DOC: Imatinib, Dasatinib, Nelotinib, Ponatinib, Bosutinib
5b) HER/ 2Nu Inhibitor T/t : Breast CA
Trastuzumab, Pertuzumab, Lapatinib,
S/E : Cardiotoxicity
5c) EGFR InhibitorT/t : NSCCL
Cituximab, Panitumumab– Also useful for Colon CA& Head and neck Ca
Necitumumab- Pancreatic Ca
erlotinib, geftinib –Also useful for Pancreatic CA
5d) VEGF Inhibitor T/t : Solid Tumors like - Colon CA, Lung CA, RCC, Breast CA
Bevacizumab, Ranibizumab, pegaptanib,Ziv-Aflibercept, Ramucirumab
S/E : dealayed wound healing
5e) Multiple Target Inhibitor
PDGF Inhibitor, VEGF InhibitiorT/t : Solid Tumors
Sorafenib Raf Kinase Inhibitor DOC : HCC
Sunitinib
C- Kit TK Inhibitor  G/ST : T/t
Axitinib
Vandetanib  RET Inhibitor  Medultary CAT/t

Antibiotics Notes
Pazopanib RCC
5f) C- Kit TK Inhibitor T/t : GIST
Sunitinib
Axitinib
Imatinib (DOC)
6. HORMONAL CHEMOTHERAPY
(Covered in Endocrine Drugs)
7. MISCELLANEOUS
7a) Platinum Drugs
Cisplatin, Oxaliplatin, Carboplatin
MOA
(Same as alkylating agents)
COMMON S/E
Cisplatin :
Indications: 1. Germ cell Tumors – Testicular , Ovarian CA
2. Female Reproductive Tract CA–Fallopian tube endometrial Cx CA, Vaginal CA
3. CAlocated above umbilicus – esophageal CA, Head & Neck CA, Breast CA, Lung CA
S/E :
1. M/C N&V (Max among all drugs)
2. 2nd M/C  Nephrotoxicity (Acute Tubular Necrosis)
[prevented by Amifostine/ Mannitol Diuresis ]
3. 3rd M/C  Neurotoxicity
Sensory Neuropathy (max) Ototoxicity
4. Other  L-STAMP

Antibiotics Notes
7b) Asparaginase
T/t : ALL
S/E : 1. Metabolise Asparagine containing molecule
Insulin , Albumin , CF , Anti – CF
2. NH3
3. Pancreatitis
7c) Hydroxyurea
MOA  DNA synthesis Inhibitor
Indication  DOC : Plycythemia vera
DOC : Thrombocytosis Vera
DOC : SCA
S/E BM
7d) Histone Deacetylase Inhibitior
Vorinostat
T/t cut T cell lymphoma
Romidepsin
7e) Protosone Inhibitors
Bortezomib
T/t Multiple Myeloma
Carfilzomib
7f) m- TOR Inhibitor : T/t RCC, CNS Tumor
Temsirolimus, everolimus
7g) ATRA (All Trans Retinoic Acid)
DOC : PML [M3 AML]
7h) Topoisomerase inhibitors:
1. Topoisomerase I inhibitors: Irinotecan, Topotecan.

2. Topoisomerase II inhibitors : Etoposide, teniposide
Irinotecan
a) It is a prodrug , its active metabolite is SN 38 which has cholinergic property and hence
diarrhoea is very common with irinotecan therapy.
b) It is metabolised in liver by UDP glucoronosyl transferase enzyme. In pateints of this
enzyme deficiency, there is risk of toxicity.

Antibiotics Notes
Etoposide is associated with secondary leukemia (early leukomegic drug). It is given for the
treatment of testicular cancer.
7i) Ipilimumab: it binds to cytotoxic T-lymphocyte–associated antigen 4 (CTLA-4), which is

expressed on the surface of activated CD4 and CD8 T-cells. CTLA-4 normally acts as a brake on T-cell
antitumor activity. Binding of ipilimumab results in inhibition of the interaction between CTLA-4 and
its target ligands CD80/CD86 and thus enhances T-cell immune responses, which include T-cell
activation and proliferation.This agent is approved for the treatment of metastatic melanoma
7j) Nivolumab, Atezolizumaband pembrolizumab are IgG4 antibodies that bind to the programmed
death (PD)-1 receptor, which is expressed on T cells, and they inhibit the interaction between the
programmed death ligand 1 (PD-L1) and ligand 2 (PD-L2) and the PD-1 receptor. The PD-1 signaling
pathway mediates an immune escape mechanism, and inhibition of this pathway enhances T-cell
immune response, leading to T cell activation and proliferation. Each of these agents is approved for
unresectable or metastatic melanoma as monotherapy.
7k) Alemtuzumab binds to CD52 found on normal and malignant B and T lymphocytes, NK cells,
monocytes, macrophages, and a small population of granulocytes and approved for the treatment of
B-cell chronic lymphocytic leukemia (CLL).
7l) Rituximab is a chimeric murine-human monoclonal IgG1 (human Fc) that binds to the CD20
molecule on normal and
malignant B lymphocytes and is approved for the therapy of patients with CD20-positive large-B-cell
diffuse non-Hodgkin’s
lymphoma. It is approved for treatment of CLL in combination with chemotherapy. It is also approved
for the treatment of rheumatoid arthritis in combination with methotrexate in patients for whom anti-
TNF- therapy has failed. The most recent indication for rituximab is for the treatment of Wegener’s
granulomatosis and microscopic polyangiitis. Anemia or neutropenia is an important adverse effect,
which can be countered with granulocyte colony-stimulating factor (G-CSF).
Other adverse effects include hypotension, rash, gastrointestinal disturbance, fever, and fatigue.

Antibiotics: Classification (Based On Mechanism of Action)

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Antibiotics Notes

Classification(Based on Mechanism of action)

1. CELL WALL INHIBITOR

β – Lactam Antibiotics Glycopeptide Ab

2. CELL MEMBRANE INHIBITOR

Polypeptide Abs Daptomycin

Email : info@damsdelhi.com | Website : www.damsdelhi.com Page | 1

3. PROTEIN SYNTHESIS INHIBITOR

30s Ribosome 50s Ribosome

4. Folic Acid Pathway Inhibitor

PABA + DHA DihydroptericAcid +glutamte Dihydrofolate (DHF)

5. Nuclear Material Inhibitor

a) DNA gyrase Inhibitors : Fluroquinolones , Nalidixic Acid

a) Protein synthesis Inhibitor

b) Cell wall & Membrane Inhibitor

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2.Cell Membrane Inhibitor

3.Protein Synthesis Inhibitors

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4.Folic Acid Pathway Inhibitors

5.Nuclear Pathway Drugs

2. Pattern of bacterial inhibition:

Time dependent killing(TDK) and Concentration Dependent killing(CDK)

3. Post antibiotic effect (PAE):

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BACTERIAL RESISTANCE MANAGEMENT

Side Effects of Antibiotics

1. Beta lactam antibiotics:

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3. Cell membrane inhibitors :

1. Cisplatin (max nephrotoxicity)

c. Neuromuscular blockade: It occurs due to inhibition of pre-synaptic release of Ach. Hypocalcemia,

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(spectrum g +ve Cocci & Bacilli , g –ve cocci, Anaerobes )

2. Cloxacillin, Oxacillin, NaFicillin, Dicloxacillin

3. Extended Spectrum Penicillin

a)Amox, Ampi : All g –ve Bacilli except pseudomonas

b) (Anti pseudomonal penicillin)

1. gen – I (Mainly against g +ve)

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2. gen – II (Few g +ve & Many g –ve) (spectrum Incomplete )

3. gen – III(Few g +ve<<<< Almost all g –ve)

Ceftazidime DOC : pseudomonas

Cefixime 400mg stat for STD by gonococcus

4. gen – IVceph (Broad spectrum)Cefipime, cefipirome

DOC : Class – C resistant β – Lactamase producing bacteria

5.Anti MRSA cephalosporin

Carbapenoms (Broad spectrum)

INDICATIONS OF OTHER ANTIBIOTIC GROUPS

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4. Tetracycline (Doxy is used)

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Ab Anti Protozoal Antiviral

Penicillin All extended spectrum except Amox, Ampi

Cephalosporin gen – III (cefoperazone ,ceftazidime)

Carbapenems Meropenem, Dorepenem

[TOC Ceftazidime + Aminoglycoside]

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1)C.Difficile (pseudomembranous colitis)

Mild to severe oral vanco> Fidaxomicin

Mild to Mod. Oral MT2