ANTIBIOTICS

Antibiotics are the substances produced by

microorganism which suppress the growth or kill
the microorganism at very low concentration.

• Probiotics are the agents which contains live

yeast and bacteria.
Eg: Lactobacillus Acidophilus.
• Agents which suppress the growth are "Bacteriostatic"
and agents which kill the C are "Bactericidal"
• Based on spectrum of activity antibiotics are classified
into Narrow spectrum and Board spectrum
• Narrow spectrum is effective against either G positive or
G negative microorganisms.
• Board spectrum effective against both G positive and G
negative microorganisms.
 Gram - ve
Cell wall is made up of 2-3 layer of
peptidoglycans
When stained it appears in purple colour
Dye - safranin
H influenza
E. coli (UTI, RTI, GITI)
Neisseria gonorrhea
Bordetella pertussis
Salmonella typhi
Pseudomonas aeruginosa
H. pylori (Peptic Ulcer)
Vibrio cholerae
Yersinia pestis
Chlamydia trachomatis
Gram +ve
Cell wall is made up of 100-300 layers
Peptidoglycans
When stained it appears in pink color
Dye - Crystal violet / Gentian violet
Treponema pallid um(Syphilis)
Staphylococcus aureus
Bacillus anthracis (Anthrax)
Bacillus subtilis
Clostridium botulinum (Food poison)
Clostridium difficile (Super infection)
Streptococcus pyrogens (Fever)
Streptococcus pneumonia
Legionella pneumonia
Streptococcus faecalis
Corynebacterium diphtheriae
Lactobacillus acidophilus (Digestion)
Basic principle of Antimicrobial therapy
Selective toxicity
Selective toxicity means selective destruction of parasite without affecting
the host.

Targets of selective toxicity

Inhibition of enzymes found only in the parasites:

Eg:
Transpeptidase enzyme involved in the synthesis of cell wall in bacteria.
This enzyme is absent in humans.
 Enzyme found in both host and parasite but essential
only for parasites:
C 14 α Demethylase
Eg: Lanosterol Ergosterol [fungal cholesterol]

Enzyme having same function in both host and parasite

differ in sensitivity towards the drugs:

Eg: Dihydrofolate reductase enzyme in the bacteria is more sensitive

when compare to humans.
 Drugs resistance
Mechanism:
Decrease ability of the target (Tolerance to the drug)
Eg:
Pneumococci and Staphylococci organisms develop alternate Penicillin
binding sites which decrease the activity of the drug.

Development of alternate metabolic pathway

Eg:
Organisms which are resistant to Sulfonamides start using folic acid
from humans instead of synthesizing from PABA.
Elaboration of enzyme which inactivate the drug
Eg:
β- lactamase enzyme is released by the bacteria which destroy the β- lactam ring of
Penicillin and Cephalosporins thereby decreasing the activity.

Superinfection/ Suprainfection

• Appearance of a new infection as a result of Antimicrobial therapy

• Some antibiotics destroys the normal microbial growth in GIT, which is
responsible for the proper development and maintenance of GIT
• Broad spectrum antibiotics are most common concerned with
development of super infection.
The major antibiotics producing super infection
Eg:

• Clindamycin [It is the most common Antibiotic producing Super infection]

• Tetracycline
• Chloramphenicol
• Broad spectrum Penicillin
• Cephalosporins from 3rd generation onwards
 Major symptoms of Super infection
• Nausea
• Diarrhea
• Respiratory infection
• UTI

98
The major organisms producing super infection include:

• Clostridium difficile [It is the most common organism producing

Super infection]
• Candida Albicans
• Staphylococci
• Pseudomonas
Clostridium difficile Super infection resulting in Pseudomembranous
colitis [Infection of colon]
The common drugs used in treatment of pseudomembranous colitis
are,
• Vancomycin (Most preferred)
• Metronidazole
 Concentration dependent killing [CDK]
Certain antibiotic produces better action when used is a single large
dose.
Eg:
• Aminoglycosides
• Fluoroquinolones
Time dependent killing [TDK]
They produce better action when given as multiple daily doses over
single dose.
Eg:
• β- lactam antibiotics
• Macrolide antibiotics
 Post Antibiotic effect (PAE)
Certain antibiotics continue produce action even though
they are withdrawn from the therapy for the certain period
of time. This effect is known as PAE.
Eg
• Fluoroquinolones
• Aminoglycosides
• β-lactam antibiotics
CLASSIFICATION OF ANTIBIOTICS BASED ON MECHANISM OF ACTION
INHIBITING CELL WALL SYNTHESIS INHIBITING PROTEIN SYNTHESIS DRUGS AFFECTING NUCLEIC ACID

β- lactam antibiotics Chloramphenicol a. DNA gyrase inhibitor

Bacitracin Tetracycline Fluoroquinolones, Nalidixic acid

b. drugs destroying DNA
Cycloserine Aminoglycosides

Metronidazole
Fosfomycin Lacosamide
c. RNA polymerase inhibitor
Vancomycin Streptogramins

Teicoplanin Linezolid Rifampicin

Drugs affecting cell membrane function
i). Polyene antibiotics
Amphotericin B
Nystatin
Hamycin
Natamycin
ii). Polypeptide antibiotics
Polymyxin B
Colistin
Tyrothricin
iii) Azoles:
• Ketoconazole
• Voriconazole
• Itraconazole
Drugs affecting metabolism
a. Folic acid synthase inhibitors
• Sulphonamides
• Dapsone
• PAS (Para amino salicylic acid)
b. Dihydrofolate reductase inhibitors
• Trimethoprim
• Pyrimethamine
• Methotrexate
• Proguanil
 (II)Based on Type of action
Bacteriostatic Bactericidal
• Tetracyclines • Aminoglycosides
• Chloramphenicol • Streptogramins
• Lincosamide • Fluoroquinolones
• Macrolides • Metronidazole
• Linezolid • Polymyxin B
• Sulphonamides • Colistin
• Dapsone • Amphotericin B
• Trimethoprim • Fosfomycin
• Nitrofurantoin • β Lactam Antibiotics
• Novobiocin • Bacitracin
• Ethambutol [TB] • Cycloserine
• Vancomycin
• Teicoplanin
• Rifampicin, Isoniazid, Pyrazinamide [TB]
Drug inhibiting cell wall synthesis

β lactam Antibiotics
β lactam ring is responsible for medicinal activity of β-lactam
antibiotics
The major β lactam antibiotics include:
• Penicillin
• Cephalosporins
• Monobactams
• Carbapenems
 PENICILLIN
• Discovered by Alexander Fleming in 1928
• Bactericidal
• It inhibit cell wall synthesis by inhibiting Transpeptidase
enzyme
• Penicillin is obtained from fungus moulds like Penicillium
chrysogenum and Penicillium notatum
• First discovered penicillin is Benzyl Penicillin (Penicillin G)
• It is found to be more effective against gram +ve strains
of bacteria like Staphylococcus
 CLASSIFICATION OF PENICILLIN
Natural penicillin
Eg: Penicillin G [Benzyl Penicillin]

• It is not effective orally and given IV or IM routes

• Penicillin G under normal condition does not crosses the blood brain
barrier and it crosses during Meningitis.
• It has short duration of action because rapidly excreted through
kidneys.
• In order to make Penicillin G long acting Procaine and Benzathine is
added, which is administered by IM route.
• IV Penicillin dose = 0.6mcg
 Synthetic Penicillins

a) Acid resistant Penicillin

Eg: Penicillin V (Phenoxy Methyl Penicillin)

It can be given by oral route and it is resistant to

gastric acid.
b) Penicillinase or β-lactamase Resistant Penicillin
Eg:
• Oxacillin
• Cloxacillin [Best Antibiotic for treatment of bone and soft tissue infection]
• Dicloxacillin
• Floxacillin
• Nafcillin
• Methicillin [Effective against almost all type of Gram Positive bacteria]
• The major bacteria producing resistance against Methicillin is Staphylococcus aureus
[MRSA].
• MRSA infection treatment with Vancomycin and Teicoplanin
• VRSA (Vancomycin Resistance) infection is treated with Linezolid, Streptogramins &
Teicoplanin
C) Broad Spectrum Penicillin

Amino Penicillins:
• Amoxicillin (High doses are used ion Otitis media)
• Ampicillin
Carboxy Penicillins:
• Carbenicillin
• Ticarallin
Uridopenicillins:
• Mezlocillin
• Azlocillin
• Piperacillin
Carboxy Penicillins and Urido Penicillins are effective against
Pseudomonas
whereas Amino Penicillin is not effective Pseudomonas infection
β- Lactamase Inhibitors

• β- lactamase enzyme is produced by microorganisms during infection

which will destroy the
• β- lactam ring which is responsible for the activity
• β- lactamase inhibitors can be added with Penicillin, Cephalosporin
Monobactams and Carbapenems
• Augmentin [Amoxicillin + Clavulanic acid], DOC for Otitis media
• Unasyn [Ampicillin + Sulbactam]
• Zosyn [Piperacilline + Tazobactam]

101
Uses
• Treatment of Syphilis (Drug of choice Penicillin G)
• Treatment of Meningitis
• Treatment of leptospirosis (Plaque)
• Treatment of Anthrax Diphtheria
• Treatment of Lyme's disease [Spirochetes infection]
ADR of penicillin
• Hypersensitivity reaction characterized by Rashes and Dermatitis
• Anaphylactic Shock [Treated with Adrenaline]
• Steven Johnson Syndrome
• Pseudomembranous Colitis (Super infection by broad spectrum
Penicillins)
• Neutropenia
• Nausea
• Diarrhea
• Development of Seizures
• Jarisch Herxheimer's reaction (If Penicillin is injected to Syphilis patient, it
produces shivering, fever, myalgia and hypotension due to the sudden
release of antigens from killed bacteria)
Monobactams
Eg:
• Aztreonam
It is the only β- lactam Antibiotic used in patients
having allergy to Penicillin and Cephalosporins.
And it is effective mainly IV route.
 Carbapenems
Eg:
• Imipenem
• Doripenem
• Meropenem
• Ertapenem
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• Imipenem is usually combined with
Cilastatin as it is rapidly inactivated by
Renal Dehydropeptidase enzyme secreted
by kidney.
• Cilastatin inhibit this enzyme and increase
half-life of imipenem
• Others are not metabolites like Imipenem
Cephalosporins
It is obtained from a fungus
Cephalosporium and Acremonium.
 Generations and Spectrum Oral Parenteral
Cefalexin (Ceporex, Keflex)
Cephalothin
Cefadroxil
1st Generation (G +ve only) Cephazolin
Cefaloridine
Cephapirin
Cefradine
Cefuroxime axetil
Cefotetan
Cefmetazole
2nd Generation Cefuroxime axetil (Zinnat) Cefoxitin ( Mefoxin)
(They are active against G +ve & Cefaclor (Ceclor) Cefamandole
slightly against G -ve) Cefprozil (Cefzil) Ceforanide
Cefonicid (Monocid)
Loracarbef
Latamoxef
Cefixime (Suprax)
Cefotaxime( Claforan)
Cefpodoxime
3rd Generation Ceftizoxime
Cefnide
(Good activity against G +ve & Ceftriaxone (Rocephine)
Ceftibuten
increased activity against G -ve) Cefoperazone
Cefetamet Ceftazidime
Cefditoren
 Generations and Spectrum Oral Parenteral
4th Generation Cefepime
(They show excellent Cefpirome
activity Cefclidine
against G+ve and G-ve) Cefluprenam
5th generation:
Ceftobiprole
(The broadest spectrum of
Ceftaroline
Cephalosporins)
USES OF CEPHALOSPORINS

• Treatment of Meningitis [Ceftriaxone, Cefotaxime,

They easily crosses BBB]
• Treatment of Pseudomonas infection [Ceftizoxime]
• Community acquired Pneumonia [Ceftriaxone along
with Azithromycin]
• Treatment of Skin and soft tissue infections
• Treatment of Respiratory tract infection
• Treatment of UTI
• Surgical prophylaxis 103
• Treatment of Uncomplicated Gonorrhea [Ceftriaxone]
• Treatment of Lyme diseases
• Treatment of Impetigo (It is a superficial inflammation of
the skin produced by Staphylococcus bacteria)

Treatment of Impetigo
• First choice Cephalosporins taken orally & Mupirocin
(Bactroban) is applied topically
• Second choice Fusidic acid combined with Steroids.
ADR:
• Anaphylactic Shock
• Urticaria
• Rashes
• Pain at the site of injection
• Super infection
• Produces Disulfiram like reaction
• Neutropenia
• Bone marrow depression
4) VANCOMYCIN
• It is a Glycopeptide and effective against Pseudomonas
and MRSA infection.
• It is used treatment of Pseudomembranous Colitis
(Super infection) caused by Clostridia Difficile
• Rapid IV infusion of Vancomycin results in excessive
release of Histamine commonly known as Redman
syndrome.
5) TEICOPLANIN
• It is a Glycopeptide mainly administered IV or IM
• It does not produce Redman syndrome and used
in the treatment of MRSA & VRSA.
• The uses are limited due to the development of
Skin rashes.
6) FOSPHOMYCIN

• Used in the treatment of UTI

• Not used nowadays due to development of
Resistance and diarrhea.
7) BACITRACIN
• Used only for topical purposes
• Not given in parental route due to Nephrotoxicity

8) CYCLOSERINE
• It is a second line agent in the treatment of TB
ii) DRUG INHIBITING PROTEIN SYNTHESIS
Chloramphenicol
• MOA: It is bacteriostatic in nature and inhibits Protein synthesis by
binding 50S ribosomal subunits.
• Due to the development of high toxicity and drug resistance
Chloramphenicol is not commonly used for systemic purpose.
• They are mainly used for topical infection on eyes, ear, and nose.
ADR:
• Bone marrow depression
• Irreversible myelosuppression
• Aplastic anemia
• Optic neuritis
• Peripheral neuritis
• Grey baby syndrome
GREY BABY SYNDROME:
• In neonates and premature infants there is a deficiency of
Glucoronyl transferase enzyme responsible for decreased
metabolism of Chloramphenicol which is characterized by
destruction of RBC, decrease levels of RBC, development
of Grey color and cardiovascular collapse.
TETRACYCLINES
• MOA: They act by inhibiting protein synthesis by
binding on 30S ribosomal subunits

• Oral absorption of Tetracycline is affected by food and

multivalent cations like Ca2+, Fe2+, Mg2+, and Al3+.
Classification
Group 1 Group 2 Group 3
Short acting / Intermediate acting / Long acting /
6-8 hours 12 hours 16-18 hours

Demeclocycline Doxycycline
Tetracycline
Lymecycline Minocycline
Oxytetracycline
[Renal excretion] [Non-renal excretion]
Chlortetracycline
Safe in liver failure Safe in renal failure
USES OF TETRACYCLINE
• Treatment of Cholera
• Plague prophylaxis
• Treatment of Lyme diseases
• Treatment of Rickettsia infection
• Treatment of Malaria
• Prophylaxis of Malaria
• Treatment of Leprosy 105
• Treatment of Amoebiasis
• Treatment of Peptic ulcer
• Treatment of Periodontitis (Inflammation
of Gingiva, DOC: Doxycycline)
• Treatment of Brucellosis
• (Duration= 6 weeks)
DRUG REGIMEN FOR BRUCELLOSIS
• Doxycycline 100mg PO bid for 6 weeks + Rifampicin
600-900mg/day PO for 6 weeks
• Doxycycline 100mg PO bid for 6 weeks +
Streptomycin 1g/day IM daily for 3 weeks
ADR:
• Pseudomembranous Colitis
• Diarrhea
• GI side effects
• Hepatic necrosis (Seen in pregnant females)
• Photosensitivity reactions
• Vestibular toxicity
• The uses of Tetracyclines are contraindicated in pregnancy
due to increase risk in irregularity in fetal bone, teeth and
enamel growth.
• Increased uses of Tetracyclines in children below 20 years are
contraindicated due to permanent brownish discoloration of
teeth.
• Use of outdated (Expired) Tetracycline leads to Fanconi
syndrome (Renal tubular acidosis)
AMINOGLYCOSIDES
• MOA: It inhibits protein synthesis by binding to 30S and
50S (slightly) ribosomal subunits.
• They produce wide range of action against G+ve and G-
ve organisms (Broad spectrum).
• They primarily excreted by kidney and causes
nephrotoxicity.
• It is bactericidal in nature and they exhibit CDK and PAE.
• They are not used orally except Neomycin.
 AMINOGLYCOSIDES USES
Streptomycin First line drug of TB given by IM
Also given in the treatment of
Brucellosis
Gentamycin, Tobramycin Available as eye drops & effective
against Pseudomonas infection

Kanamycin, Amikacin Second line agents in treatment of TB

Sisomycin, Netilmicin, Framycetin They are not used clinically due to high
toxicity
Neomycin Only aminoglycoside which is taken by
oral route for Gut sterilization in Hepatic
encephalopathy
106
ADR:
• Nephrotoxicity
(Increased level of blood urea nitrogen and creatinine)
• Ototoxicity
(Damage of ear vestibular nerve)
• Neuromuscular blockade
(Contraindicated in Myasthenia Gravis)
Macrolide antibiotics
MOA:
They inhibit protein synthesis by binding to 50S ribosomal nucleus.

Macrolide antibiotics Ketolide antibiotics

Erythromycin Telithromycin
Azithromycin
Clarithromycin
Roxithromycin
ERYTHROMYCIN
• They sire active against G +ve organisms [Narrow
spectrum]
• It is the most preferred drug given alternate to patients
having allergic to Penicillin
Q) Which antibiotic is used for patients having Penicillin
allergy? Erythromycin
Q) Which 3- lactam antibiotic used Penicillin allergy?
Aztreonam or Monobactum
• Erythromycin is not stable under acidic
condition. So they available as enteric coated
tablets
• Food also interferes the absorption of
Erythromycin
• It is and enzyme inhibitor, which increases the
toxicity of other drugs
AZITHROMYCIN, CLARITHROMYCIN, ROXITHROMYCIN

• Effective against G +ve and G-ve [Broad spectrum]

• Uses: Upper & Lower respiratory tract infection, UTI
• Used in eradication of H- pylori infection Peptic ulcer
ADR:
• Gastric pain
• Diarrhea (More common Erythromycin)
• Fever
• Eosinophilia
• Skin rashes
• Jaundice
• Anorexia
Except Azithromycin all others are enzyme inhibitors, which increase
toxicity of other drugs.
 Lincosamides
MOA: It inhibits protein synthesis same as Macrolides
Eg: Clindamycin and lincomycin
uses
• Topical treatment of Acne vulgaris [Systematic use causes
Pseudomembranous Colitis]
• Pneumocystis carinii and Pneumocystis jiroveci
• Pneumocystis carinii is Pneumonia in AIDS patients
• (Rx Lincosamides)
• Toxoplasmosis( Infection by Toxoplasma gonadi parasite, from cat
faeces contamination with food, serious effect in Pregnant and
weakened immune systems
STREPTOGRAMINS
• MOA: They also inhibit 50S ribosomal subunits
• They are bactericidal
• It is a combination of "Quinpristin" and "Dalfopristin"
• They are effective against MRSA and VRSA infection
Oxazolidiones
Eg: Linezolid
• They inhibit both 30S & 50S ribosomal subunits
• They are effective against MRSA and VRSA infection
• Used against G+ve organisms which produce resistance against
other Antibiotics
• They possess 100% bioavailability
ADR:
• Thrombocytopenia
• Optic neuritis
• Lactic acidosis
 ANTIMETABOLITES
SULPHONAMIDES:
MOA: They act by inhibiting folic acid synthase enzyme there
by inhibiting the synthesis of folic acid from PABA bacteria

Para Amino Benzoic acid/ PABA

Folate synthase Sulphonamides, Dapsone, PAS
Dihydro Folic acid [DHFA]
Dihydro Folate Reductase [DHFR] Trimethoprim
Folic acid Methotrexate
[FA] Pyrimethamine
. Proguanil
 CLASSIFICATION
Sulphonamides Examples Uses
1. For systematic use as oral agents
Sulfisoxazole UTI
Sulfamethizole Allergy
a) Short acting Sulfadiazine UTI
[Sulfadiazine + Rx of Toxoplasmosis
Pyrimethamine] Px Pneumocystis carinii
b) Intermediate
Sulfamethoxazole UTI
acting
c) Long acting Sulfadoxine Malaria
Sulfcytine Malaria
 2. For use in GIT Sulfasalazine IBD
Olsalazine IBD
Mesalamine IBD

3. For topical use Sulfacetamide[Ointment] Ocular infection

Silver sulfadiazine Burns

Mafenide acetate Burns
Broad spectrum
4. For use in Epilepsy Zonisamide
antiepileptic drug
ADR:
• Skin rashes
• Granulocytopenia
• Thrombocytopenia
• Aplastic anemia
• Produces Hemolysis in G6PD deficient patient
• Produces drug induced SLE in slow acetylators
• Crystal urea
• Hematorrhea
• Kernicterus [Hyperbilirubinemia]
• Sulfonamides is avoiding during 3rd trimester of pregnancy
 COTRIMOXAZOLE OR BACTRIM
• Combination of Sulfamethoxazole and Trimethoprim
in the ratio of 5:1
• Individually gives drugs are bacteriostatic in nature
but ratio 5:1 they show bactericidal activity.
• They possess 100% oral bioavailability
• Used treatment of UTI & Respiratory tract infection
• Used treatment of Traveler's diarrhea caused by E- coli

109
IV) Drug affecting nucleic acid
Quinolones and Fluoroquinolones:

MOA: They act by inhibiting DNA gyrase and

Topoisomerase 2 enzymes

1- Quinolones
Eg: Nalidixic acid Used as Urinary antiseptic
2- Fluoroquinolones
:

First Second
Third generation Fourth generation
generation generation
Narrow Narrow Good activity
Excellent activity
spectrum spectrum against G+ve and
against G+ve & G-ve
effective effective G-ve (Broad
(Broadest spectrum)
against G-ve against G-ve spectrum)
• Moxifloxacin
• Levofloxacin
• Flerofloxacin
Norfloxacin Ciprofloxacin • Gatifloxacin
• Garenoxacin
Lomefloxacin Ofloxacin • Pefloxacin
• Gemifloxacin
• Sparfloxacin
• Trovafloxacin
USES
• Treatment of UTI (Ciprofloxacin)
• Treatment of Respiratory tract infection (Levofloxacin)
Respiratory Fluoroquinolones: Levofloxacin,
• Gatifloxacin,Gemifloxacin and Moxifloxacin
• Treatment of TB as second line agents
• Treatment Travelers' diarrhea (Ciprofloxacin)
ADR:
• Contraindicated in pregnancy and children due to
increased risk of cartilage erosion.
• Not recommended in adults due to increase risk
tendonitis [Tendon rupture]
• Photo toxicity
• GI upset
• Increase risk of arrhythmia
• Hepatotoxicity
• Development of Seizures
• Hemolytic anemia
• Dizziness
• Headache
 URINARY ANTISEPTICS
These are oral drugs which are rapidly excreted in
urine and suppress the bacterial growth in the urinary
tract. They are more effective in acidic urine
Eg:
 Nalidixic acid
 Nitrofurantoin
 Methenamine Mandelate
• Nalidixic acid and Nitrofurantoin should not be administered
together because of their antagonistic action.
• Methenamine is converted to Formaldehyde at low pH is
responsible for the antibacterial activity. Mandelate is added
to increase the acidity of urine
• It is not effective against Protease infection because it
releases ammonia and alkalizes the urine
• The use of Methenamine is avoided with Sulfonamides due
to formation of insoluble complex between Formaldehyde
and Sulfonamides
Phenazopyridine
It is not a urinary antiseptic, it possess analgesic action and
reducing the burning sensation associated with UTI.
 TUBERCULOSIS
• Tuberculosis produced by Mycobacterium Tuberculosis
• TB affect all organs except nail and hair (dead cells)
• DOTs- Directly Observe Therapy of Short Course: It is
recommended in TB patients to ensure that the patient
is taking proper medication at proper time at proper
dose to reduce the incidence of drug resistant in TB
• Diagnostic test for TB: Mantoux Test
 Drug used in TB
1- First line agents (6-9 months)
• Isoniazid (INH or H)
• Rifampicin (R)
• Pyrazinamide (Z)
• Ethambutol (E)
• Streptomycin (S)
 Isoniazid (INH or H)
• Vitamin B6 / Pyridoxine is added to INH to
prevent Peripheral neuritis
• Produce drug SLE in slow acetylator
• Produce G6PD deficiency
• Produce gynecomastia
• Isoniazid inhibits MAO enzymes, resulting in
Cheese reaction treated with Phentolamine
RIFAMPICIN

• It is an enzyme inducer
• Orange and red coloration of urine
• Increase metabolism of Anticonvulsants, Oral
contraceptives, Anticoagulants and Anti HIV
drugs
PYRAZINAMIDE
• This medication should not be stopped due to
increased risk of drug resistance
• Major ADR is Hyperuricemia [CI in Gout]
• Other ADRs are Hepatic dysfunction and
Photosensitivity
ETHAMBUTOL
• The only first line agent produce bacteriostatic
action
• Mainly produces visual disturbances like optic
neuritis, colour blindness [red & green] and
retinal damage.
STREPTOMYCIN
• Bactericidal in nature and given only
by IM route.
• Contraindicated in pregnancy
2- Second line agent (12-24 months)
Eg:
 Thioacetazone
 Para amino salicylic acid (PAS)
 Ethionamide
 Cycloserine
 Kanamycin
 Amikacin
 Ciprofloxacin
 Ofloxacin
 Linezolid
THIOACETAZONE PAS ETHIONAMIDE

Hepatitis
Kidney, Liver and Hepatitis Optic neuritis
Bone marrow suppression
Thyroid dysfunction Impotence
Steven Johnson syndrome

Also used in the

MOA: Similar to
Bacteriostatic treatment of leprosy
Sulfonamides
Bacteriostatic
 LEPROSY / HANSEN'S DISEASE
Caused by the organism Mycobacterium leprae

DRUGS
1- Dapsone

MOA: Drug inhibiting metabolism (Same as

Sulfonamides) and bacteriostatic in nature
112
ADR:
• Produce drug inducing SLE
• Produce Hemolysis G6PD deficient patient
• GI irritation
• Skin rashes
• Leprae reaction (Acute inflammation of the skin)
• Dapsone syndrome (Accumulation of drug in skin)
2- Clofazimine
Usually give with Dapsone due to anti- inflammatory
property to prevent leprae reactions.
3- Rifampicin

It is only first line agent used in both leprosy and TB

4- Miscellaneous
Eg:
• Ethionamide
• Ofloxacin
• Sparfloxacin
• Minocycline
• Clarithromycin