This document provides information on various antibiotics, with a focus on penicillin. It defines antibiotics and classifies them into different groups. It then discusses beta-lactam antibiotics and their mechanism of inhibiting bacterial cell wall synthesis. The document outlines the timeline of penicillin discovery and development. It describes the mechanism of action of penicillins, including their inhibition of transpeptidase enzyme and weakening of the bacterial cell wall. Finally, it provides details on specific penicillin drugs, their indications, mechanisms, side effects and dosages.

1. ANTIBIOTICS
A PRESENTATION OF
PENICILLIN, POLYPEPTIDE
AND OTHERANTIBIOTICS

2. DEFINITION OF ANTIBIOTIC
A substance of biological, semisynthetic or synthetic
origin of low molecular weight produced by a fungus
or bacterium as secondary metabolites that inhibits
or stop growth of other microorganisms invitro and in
vivo selectively, when it used in low concentration

5. CLASSIFICATION
1. PENICILLINS
2. CEPHALOSPORINS AND OTHER BETA-LACTAMS
3. TETRACYCLINES
4. AMINOGLYCOSIDES
5. MACROLIDES
6. CLINDAMYCIN
7. SOME OTHER ANTIBACTERIALS
8. SULPHONAMIDES AND TRIMETHOPRIM
9. ANTITUBERCULOSIS DRUGS
10. ANTILEPROTIC DRUGS
11. METRONIDAZOLE AND TINIDAZOLE
12. QUINOLONES
13. URINARY-TRACT INFECTIONS

6. Β- LACTAMS: CELL WALL
INHIBITORS

7. PENICILLIN TIMELINE
• 1928- ALEXANDERFLEMING DISCOVEREDTHE PENICILLIN MOLD.
• 1929- FLEMING PUBLISHEDHIS FINDINGS.
• 1939- DOCTORS HOWARDFLOREY ANDNORMAN HEATLEY BEGAN
INTENSIVE RESEARCHON PENICILLIN ANDITS ANTIBACTERIAL
PROPERTIES.
• 1940- FLOREY CONVERTEDPENICILLIN INTO A DRY, STABLE, BROWN
POWDER.
• JULY 9,1941- FLOREY ANDHEATLEY CAME TO THE U.S. WITHA
SMALL SAMPLE OF PENICILLIN TO CONTINUE THEIRRESEARCHAT
PEORIA LABS IN ILLINOIS.
• NOVEMBER26, 1941- ANDREWJ. MOYERSUCCEEDEDIN INCREASING
THE YIELDOF PENICILLIN TEN TIMES.
• 1943- PENICILLIN WAS TESTEDANDPROVEN TOBE THE MOST
EFFECTIVE ANTIBACTERIAL AGENT TO DATE.
• 1946- PENICILLIN BECAME AVAILABLE TO THE GENERAL PUBLIC
FOR55 CENTS A SHOT.

8. PENICILLIN

9. PENICILLINS
• THE PENICILLINS ARE AMONG THE MOST WIDELY EFFECTIVE
ANTIBIOTICS AND ALSO THE LEAST TOXIC DRUGS KNOWN, BUT
INCREASED RESISTANCE HAS LIMITED THEIR USE.
• MEMBERS OF THIS FAMILY DIFFER FROM ONE ANOTHER IN THE R
SUBSTITUENT ATTACHED TO THE 6-AMINOPENICILLANIC ACID
RESIDUE.
• THE NATURE OF THIS SIDE CHAIN AFFECTS THE ANTIMICROBIAL
SPECTRUM, STABILITY TO STOMACH ACID, AND SUSCEPTIBILITY TO
BACTERIAL DEGRADATIVE ENZYMES (Β-LACTAMASES).

10. THE SPORES IN PENICILLIUMOFTEN CONTAIN BLUE
OR GREEN PIGMENTS WHICH GIVE THE COLONIES ON
FOODS AND FEEDS THEIR CHARACTERISTIC COLOUR.
IT IS THE SPORES IN THE BLUE CHEESE THAT GIVE
THE COLOUR TO THE CHEESE.

11. PENICILLIUM
THE NAME PENICILLIUMCOMES FROM PENICILLUS = BRUSH, AND THIS
IS BASED ON THE BRUSH-LIKE APPEARANCE OF THE FRUITING
STRUCTURES

12. Β-LACTAM RING
•The β-lactam ring is a
common structure for:
•Penicillins
•Cephalosporins
•Monobactams
•Carbapenems
• Bacteria will target
this ring to gain
resistance.

15. MECHANISM OF ACTION

17. MECHANISMOF ACTION 1
•Some PBP have
transpeptidase activity.
• Transpeptidase activity
is essential in cell wall
synthesis.
•Beta-lactams bind PBP (Penicillin
Binding Proteins).

18. MECHANISMOF ACTION OF THE
PENICILLINS• PEPTIDO GLYCANIS AHETERO PO LYMER THAT PRO VIDES RIGID MECHANICAL STABILITY TO THE
BACTERIAL CELL WALL BY VIRTUE O F ITS HIG HLY CRO SS-LINKED STRUCTURE. IN GRAM-
PO SITIVE BACTERIA, THE CELL WALL IS 50 – 1 0 0 MO LECULES THICK; IT IS O NLY 1 O R 2
MO LECULES THICK INGRAM-NEGATIVE BACTERIA.
• THE PEPTIDO GLYCANIS CO MPO SED O F G LYCANCHAINS, WHICH ARE LINEAR STRANDS O F TWO
ALTERNATING AMINO SUGARS (N-ACETYLGLUCO SAMINE AND N-ACETYLMURAMIC ACID) CRO SS-
LINKED BY PEPTIDE CHAINS.
• PEPTIDO GLYCAN PRECURSO R FO RMATIO N TAKES PLACE IN THE CYTO PLASM. THE SYNTHESIS
O F UDP– ACETYLMURAMYL-PENTAPEPTIDE IS CO MPLETED WITH THE ADDITIO N O F THE
DIPEPTIDE, D-ALA-D-ALA (FO RMED BY RACEMIZATIO N AND CO NDENSATIO N O F L-ALA). UDP-
ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCO SAMINE ARE LINKED TO FO RM A
LO NG PO LYMER.
• THE CRO SS-LINK IS CO MPLETED BY ATRANSPEPTIDATIO N REACTIO N THAT O CCURS O UTSIDE
THE CELL MEMBRANE. THE B-LACTAMANTIBIO TICS INHIBIT THIS LAST STEP INPEPTIDO GLYCAN
SYNTHESIS, PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIACLEAVAGE O F THE— CO — N
— BO ND O F THE B-LACTAMRING.
• ALTHO UGH INHIBITIO N O F THE TRANSPEPTIDASE IS DEMO NSTRABLY IMPO RTANT, THERE ARE
ADDITIO NAL TARGETS FO R THE ACTIO NS O F PENICILLINS AND CEPHALO SPO RINS; THESE
CO LLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS). THE TRANSPEPTIDASE

19. • Penicillins inhibit a bacterial enzyme called the transpeptidasePenicillins inhibit a bacterial enzyme called the transpeptidase
enzyme which is involved in the synthesis of the bacterial cellenzyme which is involved in the synthesis of the bacterial cell
wallwall
• TheThe ββ-lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibition
• Penicillin becomes covalently linked to the enzyme’s active sitePenicillin becomes covalently linked to the enzyme’s active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formedCovalent bond formed
to transpeptidase enzymeto transpeptidase enzyme
Irreversible inhibitionIrreversible inhibition
N
S Me
Me
H
N
H H
CO2H
O
C
O
R
Nu
Enz
C
H
N
C
CO2H
HH
Me
MeS
HN
O
R
O
Nu-Enz-H
N
S Me
Me
H
N
H H
CO2H
O
C
H
Enz-Nu
O
R
Mechanismof actionMechanismof action

20. • Penicillin inhibits final crosslinking stage of cell wallPenicillin inhibits final crosslinking stage of cell wall
synthesissynthesis
• It reacts with the transpeptidase enzyme to form anIt reacts with the transpeptidase enzyme to form an
irreversible covalent bondirreversible covalent bond
• Inhibition of transpeptidase leads to a weakened cell wallInhibition of transpeptidase leads to a weakened cell wall
• Cells swell due to water entering the cell, then burst (lysis)Cells swell due to water entering the cell, then burst (lysis)
• Penicillin acts as an analogue of the D-Ala-D-Ala portion ofPenicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain.the pentapeptide chain.
Mechanismof action - bacterial cell wall synthesisMechanismof action - bacterial cell wall synthesis

22. MECHANISM OF ACTION
CELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS – GRAM POS.
(cont’d)

23. MECHANISM OF ACTION
CELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS – GRAM NEG.

24. DRUGS OF PENICILLIN
• AMOXICILLIN
• AMPICILLIN
• DICLOXACILLIN
• METHICILLIN
• NAFCILLIN
• FLUCLOXACILLIN
• PENICILLIN V
• PENICILLIN G
• TICARCILLIN

25. LATEST INFORMATION OF PENICILLIN
DRUG
• METHICILLIN
• NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY
BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS.
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO
NEPRITIES

26. AMOXICILLININDICATION:
1. UTI 3. SINUSITIS
2. OTITIS MEDIA 4. ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION:
1.PENICILLIN HYPERSENSITIVITY 2. PORPHYRIA
3. RENAL IMPAIREMENT
SIDE EFFECT:
1. RASHES 2. NAUSEA 3. VOMITING 4. DIARRHOEA
5. ANTIBIOTIC ASSOCIATED COLITIS
DOSE:
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION)
FOR CHILD, UP TO 10 YEARS 125 MG EVERY 8 HOURS
BRANDNAME:
MOXACIL (SQUARE), MOXIN (OPSONIN), TYCIL ( BEXIMCO)

27. AMPICILLIN
INDICATION:
1. UTI 3. LISTERIAL MENINGITIS
2. HAEMOPHILUS INFLUENZAE INFECTION 4. ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION:
1.PENICILLIN HYPERSENSITIVITY 2. PORPHYRIA
3. RENAL IMPAIREMENT
SIDE EFFECT:
1. RAEARLY RASHES (DISCONTINUE TREATMENT)
2. NAUSEA 3. VOMITING 4. DIARRHOEA
5. ANTIBIOTIC ASSOCIATED COLITIS
DOSE:
ADULT: BY MOUTH 0.25 – 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD)
CHILDUNDER 10 YEAR HALF OF ADULT
BRANDNAME: AMPEXIN (OPSONIN), PEN-A (RENETA)

28. DICLOXACILLIN
INDICATION:
1. IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION, WHICHIS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION:
1.PENICILLIN HYPERSENSITIVITY 2. PORPHYRIA
3. RENAL IMPAIREMENT
SIDE EFFECT:
1. URTICARIA 2. FEVER 3. JOINT PAIN 4. RASHES 5. NEUTROPENIA
6. NEPRITIS 7. DIARRHEA
DOSE: FORADULT: 125 TO250 MG EVERY 6 HOURS
FORCHILDREN : 12.5 TO25 MG/KG DAILY INDIVIDEDDOSES
BRANDNAME: DICLOX( NOVARTIS)

29. FLUCLOXACILLIN
INDICATION:
1.BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA
2. ADJUNCT IN PNEUMONIA 3. IMPETIGO 4. OSTEOMYELITIS
SIDE EFFECT:
1. URTICARIA 2. FEVER 3. JOINT PAIN 4. RASHES 5. NEUTROPENIA
6. NEPRITIS 7. DIARRHEA 8. CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION:
PENICILLIN HYPERSENSITIVITY
DOSE:
BY MOUTH, 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD)
CHILDUNDER2 YEARS, QUARTEROF ADULT DOSE; 2-10 YEARS, HALF OF ADULT DOSE
BRANDNAME: FLUBEX( BEXIMCO) , FLUCLOXIN (SK-F), FLUX(OPSONIN)

30. PENICILLIN G OR BENZYL
PENICLLIN
BENZYLPNICILLIN, COMMONLY KNOWN AS PENICILLIN G, IS
THE GOLD STANDARD TYPE OF PENICILLIN. ‘G’ IN THE NAME
‘PENICILLIN G’ REFERS TO ‘GOLD STANDARD’. PENICILLIN G
IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF
ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE
IN THE HCL OF THE STOMACH,BECAUSE THE DRUG IS GIVEN
PARENTERALLY, HIGHER TISSUE CONCENTRATIONS OF
PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH
PHENOXYMETHYLPENICILLIN,THESE HIGHER
CONCENTRATIONS TRANSLATE TO INCREASED
ANTIBACTERIAL ACTIVITY

31. Properties of Penicillin GProperties of Penicillin G
• Active vs. Gram +ve bacilli and some Gram -ve cocciActive vs. Gram +ve bacilli and some Gram -ve cocci
• Non toxicNon toxic
• Limited range of activityLimited range of activity
• Not orally active - must be injectedNot orally active - must be injected
• Sensitive toSensitive to ββ-lactamases-lactamases
(enzymes which hydrolyse the(enzymes which hydrolyse the ββ-lactam ring)-lactam ring)
• Some patients are allergicSome patients are allergic
• Inactive vs.Inactive vs. StaphylococciStaphylococci
Drug DevelopmentDrug Development
AimsAims
• To increase chemical stability for oral administrationTo increase chemical stability for oral administration
• To increase resistance toTo increase resistance to ββ-lactamases-lactamases
• To increase the range of activityTo increase the range of activity

32. Problems with Penicillin GProblems with Penicillin G
• It is sensitive to stomach acidsIt is sensitive to stomach acids
• It is sensitive toIt is sensitive to ββ-lactamases --lactamases -
enzymes which hydrolyse theenzymes which hydrolyse the ββ--
lactam ringlactam ring
• it has a limited range of activityit has a limited range of activity

33. INDICATION OF PENICILLIN G
• CELLULITIS
• INFECTIVE ENDOCARDITIS
• GONORRHEA
• MENINGITIS
• ASPIRATION PNEUMONIA,LUNG ABSCESS
• SYPHILIS
• SEPTIC ARTHRITIS
• GANGRENE

34. CONTRAINDICATION
PENICILLIN SENSITIVITY
ADVERSE EFFECT:
 URTICARIA
JOINT PAINS
 RASHES
ANAPHYLAXIS
LEUCOPENIA
COAGULATION DISORDERS

35. DOSE
ADULT OVER 18 YEARS:
FOR- I/M OR SLOW I/V 1.2G/DAY IN 4 DIVIDED OR 50 MG/ KG
BODY WEIGHT
BRANDNAME:
PEN-G (OPSONIN)
PENICILLIN G SODIUM( RENATA)

36. PHENOXYMETHYL PENICILLIN ORPENICILLIN V
PHENOXYMETHYLPENICILLIN, COMMONLY KNOWN AS
PENICILLIN, IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY
ACTIVE. PHENOXYMETHYLPENICILLIN HAS A RANGE OF
ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE
BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN
AND AND A SIMILAR MODE OF ACTION, BUT IT IS
SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN
AGAINST GRAM-NEGATIVE BACTERIA.

37. INDICATION
TONSILLITIS
PHARYNGITIS
SKIN INGECTIONS
ANTHRAX
LYME DISEASE
 SPLEEN DISORDERS
RHEUMATIC FEVER

38. CONTRAINDICATION
HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT :
 NAUSEA
VOMITING
EPIGASTRIC DISTRESS
DIARRHEA
BLACK HAIRY TONGUE

39. DOSE
ADULT: 500MG/6HR
CHILD: UP TO 1 YEARS 62.5/6HRS AND 1-5 YEARS 125MG/6HRS
BRANDNAME
CRYSTAPEN-V (GSK)
PENVIK( SQUARE)

40. 1. METHICILLIN :
- SENSETIVE TO MOISTURE --- LOSS ½ OF ITS ACTIVITY AFTER 5 DAYS AT
RT .
- SOLUTION FOR PARENTAL AD. MAY KEPT FOR 24 HR ----- [ AT 5
O
C ] .
2. NAFCILLIN , OXACILLIN :
PARENTRAL SOL. STABLE FOR 3 DAYS AT RT. ( 96 HR IF REF. ) .
3. DICLOXCILLIN :
PARENTRAL SOL. STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF. ).
4. CLOXACILLIN :
PARENTRAL SOL. STABLE FOR 14 DAYS ( REF. ) .
5- FLUCLOXACILLIN :
PARENTRAL SOL. STABLE FOR 7 DAYS ( REF. )
STORAGE :
STORE BETWEEN 15 – 30
O
C
Stability

41. POLYPEPTIDE

42. MECHANISM OF ACTION
1.THEY INHIBITS ISOPRENYL PYROPHOSPHATE,A MOLECULE
THAT CARRIES THEE BUILDING BLOCKS OF THE
PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE
INNER MEMBRANE.
2.THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL
OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE. IT
DISPLACES BACTERIAL COUNTER IONS, WHICH
DESTABILIZES OUTER MEMBRANE.THEY ACT LIKE A
DETERGENT AGAINST THE CYTOPLASMIC
MEMBRANE,WHICH ALTERS ITS PERMEABILITY. POLYMYXIN
B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC
SOLUTION.

43. DRUGS OF
POLYPEPTIDES

44. BACITRACIN
INDICATION:
EYE,EAR,OR BLADDER INFECTION
EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLO CO CCAL
BLEPHERO CO NJUNCTIVITIS

45. ADVERSE EFFECT
• KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY
INJECTION)
• IT HAS THE PROPENSITY TO INDUCE ALLERGY

46. DOSE
• EYE DROPS:
INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON. IT VARIES FROM EVERY MIN TO
2-3 TIMES A DAY.
 EYE OINTMENT:
APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE
OINTMENT USED ALONE)

47. BRAND NAME
• NEOBAC (OPSONIN)
• NEBANOL (SQUARE)
• NEOCITIRIN (ACI)

48. POLYMYXINS
• SURFACE ACTIVE AMPHIPATHIC AGENTS.
• INTERACT STRONGLY WITH PHOSPHOLIPIDS AND
DISRUPT THE STRUCTURE OF CELL MEMBRANES.

49. POLYMYXIN B
INDICATION
BACTERICIDAL; EFFECTIVE PARTICULARLY AGAINST GRAM
NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS
(PROTEUS IS RESISTANT). IT CAN’T PENETRATE IN TO THE
EYE.

50. DOSE
• EYE DROPS:
INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON. IT VARIES FROM EVERY MIN TO
2-3 TIMES A DAY.
 EYE OINTMENT:
APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE
OINTMENT USED ALONE)

51. BRAND NAME
• NEOSPORIN (GSK)
• RENAMYCIN (RENATA)

52. OTHERS ANTIBIOTIC

53. FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS
OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS, BUT
MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR
INJECTIONS. THE GLOBAL PROBLEM OF
ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A
RENEWED INTEREST IN ITS USE RECENTLY

54. INDICATION’S
• CERTAIN SKIN DISEASES. IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS, ITCHING, CRUSTING, AND SWELLING OF
THE SKIN SORES
• BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS).
• THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN,
WOUNDS, BLOOD (SEPTICAEMIA), BONE, HEART TISSUE AND LUNGS
(PNEUMONIA). THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE
SWALLOWED.
MECHANISMOF ACTION :
FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM
THE RIBOSOME. FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-
POSITIVE BACTERIA SUCH
AS STAPHYLO CO CCUS SPECIES, STREPTO CO CCUS SPECIES, ANDCO RYNE
BACTERIUM SPECIES. FUSIDIC ACID INHIBITS BACTERIAL REPLICATION
AND DOES NOT KILL THE BACTERIA, AND IS THEREFORE TERMED
"BACTERIOSTATIC".

55. CONTRAINDICATION :
• WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECT:
FUSIDIC ACIDEYE DROPS:
• STINGING OR BURNING FOR A SHORT TIME AFTER USE & ALLERGIC REACTION
(HYPERSENSITIVITY).
FUSIDIC ACIDCREAM:
• RASH
• STINGING AND IRRITATION
• ITCHY RASH AND INFLAMMATION
• FUSIDIC ACIDSUSPENSION:STOMACH UPSETS

56. DOSE:
• ADULTS—500 MG THREE TIMES DAILY
• CHILDREN—UP TO 1 YEAR OF AGE TO 12 YEARS: 20
MILLIGRAMS/KILOGRAM DAILY DIVIDED INTO 3 EQUAL
DOSES, INFUSED OVER AT LEAST 2 HOURS.
BRANDNAMES:
Fusidic plus Beximco
Facid HC Eskayef
Fusiderm Incepta
Fusidate H Aristopharma

57. METRONIDAZOLE
• METRONIDAZOLE IS A
NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED
PARTICULARLY
FOR ANAEROBIC BACTERIA AND PROTOZOA.
METRONIDAZOLE IS
AN ANTIBACTERIAL AGAINST ANAEROBIC
ORGANISMS, AMOEBICIDE ANDANTIPROTOZOAL. IT IS
THE DRUG OF CHOICE FOR FIRST EPISODES OF
MILD-TO-MODERATE CLO STRIDIUM
DIFFICILE INFECTION.

58. INDICATION’S
 ANAEROBIC INFECTION
 ACUTE ULCERATIVE GINGIVITIS & ACUTE DENTAL INFACTION
 SKIN TREATMENT
 INVASIVE INTESTINAL AMOEBIASIS
 UROGENITAL TRICHOMONIASIS
• GIANDAISIES
• ANEROBIC INFECTIONS – BACTERICIDES, CLO STRIDIUM,
• FUSO BACTERIUM, PEPTO CO CCUS, PEPTO SIRGSTO CO CCUS,
• EUBACTERIUM, H. PYLO RIS.
• POLYMICROBIAL INFECTIONS.
• PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
• PSEUDOMEMBRANOUS COLITIS

59. • MECHANISMOF ACTION:
• ENTERS BACTERIA VIA CELL DIFFUSION
• ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS  REACTS WITH NUCLEIC ACID  CELL
DEATH
• SPECTRUMOF ACTIVITY:
• ANAEROBIC BACTERIA
• MICROAEROPHILIC BACTERIA
• PROTOZOA

61. CONTRAINDICATION
• HEPATIC IMPAIRMENT
• HEPATIC ENCEPHALOPATHY
• PREGNANCY AND BREAST FEEDING
• DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTS:
• GI: N, V, EPIGASTRIC DISTRESS
• METALLIC TASTE
• DARKENING OF URINE
• PERIPHERAL NEUROPATHY
• PANCREATITIS
• HEPATITIS
• FEVER
• REVERSIBLE NEUTROPENIA

62. DOSE:
IN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN 400
MG 8 HOURLY FOR 7 DAYS
CHILD: ANY ROUTE-7.5 MG PER KG IN EVERY 8 HOURS
ACUTE ULCERATIVE GINGIVITIS: 200 MG /8 HOUR FOR 3 DAY BY
MOUTH
CHILD:100-150 MG PER 8 HOUR FOR 3 DAYS
ACUTE DENTAL INFECTION: : 200 MG /8 HOUR FOR 3-7 DAY BY
MOUTH

63. BRAND NAMES
Amodis Square
Amotrex ACI
Dirozyl Acme
Filmet-DS Beximco
Flagyl Aventis
Metco Eskayef
Metryl Opsonin
Nidazyl Orion

64. CHLORAMPHENICOL
• CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY
STREPTO MYCES VENEZUELAE AND OTHER SOIL
BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS
NOW EXCLUSIVELY
INDICATION:
 ENTERIC FEVER(আন্ত্রিক জন্ত্র্ক জ্ব্র যাহাSALMO NELLATYPHIদব্ারা সৃিক জষ্ট হয় )
 BACTERIAL MENINGITIS CAUSED BY HAEMO PHILUS
INFLUENZAE(মস্তিক জস্ত্ষ্ক িক জঝিল্লিক জল্ল প্র্দাহ)
 IN MOST ANAEROBIC INFECTIONS RESPOND TO
CHLORAMPHENICOL.SUCH AS RICKETTSIAL DISEASE(িক জরেকটিক জশিয়া উদ্ভূত্
েরাগ) AND BRUCELLOSIS(এটিক জট এটকিক জট েছোঁায়ােচেরেরাগ যা সহেজ্ই গবািক জদপ্শিু েথেকেক
বনয্প্শিু এটমস্তনিক জক মস্তানুেষর মস্তােঝিল্লও সংকর্িক জমস্তত্ হয়)

65. MECHANISMOF ACTION
• CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA
AND, TO A LESSER EXTENT, IN EUKARYOTIC CELLS. THE DRUG
READILY PENETRATES BACTERIAL CELLS, PROBABLY BY
FACILITATED DIFFUSION.
• CHLORAMPHENICOLACTS PRIMARILY BY BINDING REVERSIBLY
TO THE 50 S RIBOSOMAL SUBUNIT. ALTHOUGH BINDING OF TRNA
AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL
SUBUNIT IS THUS UNDISTURBED, THE DRUG APPEARS TO
PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF
THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S
RIBOSOMAL SUBUNIT. THE INTERACTION BETWEEN
PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE
CANNOT OCCUR, AND PEPTIDE BOND FORMATION IS INHIBITED

67. LET’S SEE:
PHARMACOKINETICS
RAPIDLY & COMPLETELY ABSORBED FROM
GIT
30 % PROTEIN BOUND
METABOLIZED BY LIVER –
GLUCURONIDATION
WELL DISTRIBUTED, INCLUDING CNS AND
CSF

68. CONTRAINDICATIONS:
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOL
TRIVIAL INFECTIONS(সামান্য্য সঙ্যক্র্যমণ)
PREGNANCY
HISTORY OF PORPHYRIA(এক্িটি বংশান্ুক্র্যিমক্ যক্ৃত সমব্যন্্যধীয়
োগালযোযাগ)
HISTORY OF BONE MARROW SUPRESSION

69. ADVERSE EFFECTS:
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR
COMPONENTS OF THE BLOOD (RED CELLS, WHITE CELLS, AND
PLATELETS)
SUPER INFECTION
GREY BABY SYNDROME
GASTROINTESTINAL UPSETS
DOSE:
BY MOUTH OR BY IV 50MG/KG DAILY IN FOUR DIVIDED DOSES
INFANT UNDER 2 WEEK 25MG/KG DAILY IN FOUR DIVIDED
DOSES

70. BRAND NAMES
Opsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
Sq.Mycetic Square
Chloram Ibn sina

71. RIFAXIMINE
• RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED
ON RIFAMYCIN. IT HAS POOR ORAL BIOAVAILABILITY,
MEANING THAT VERY LITTLE OF THE DRUG WILL BE
ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN
ORALLY. RIFAXIMIN IS USED IN THE TREATMENT
OF TRAVELER'S DIARRHEA ANDHEPATIC
ENCEPHALOPATHY, FOR WHICH IT RECEIVED ORPHAN
DRUG STATUS FROM THE U.S. FOOD AND DRUG
ADMINISTRATION IN 1998.

72. INDICATION’S
• TRAVELER'S DIARRHEA CAUSED BY E. CO LI
MECHANISMOF ACTION :RIFAXIMIN INTERFERES
WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF
BACTERIAL RNA POLYMERASE. THIS RESULTS IN THE
BLOCKAGE OF THE TRANSLOCATION STEP THAT
NORMALLY FOLLOWS THE FORMATION OF THE FIRST
PHOSPHODIESTER BOND, WHICH OCCURS IN THE
TRANSCRIPTION PROCESS

73. CONTRAINDICATION
• SEVERE LIVER DISEASE,
• CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITIS
• HYPERSENSITIVITY

74. ADVERSE EFFECT
• NAUSEA
• STOMACH PAIN
• DIZZINESS
• EXCESSIVE TIREDNESS
• HEADACHE
• MUSCLE TIGHTENING
• JOINT PAIN

75. DOSE:
FORTRAVELERS' DIARRHEA: 200 MG
TABLET TAKEN ORALLY THREE TIMES A
DAY FOR 3 DAYS.
FORHEPATIC ENCEPHALOPATHY:
550 MG TABLET TAKEN ORALLY TWO TIMES
A DAY
BRANDNAMES:
Hepaximin Aristopharma
Rifamax Incepta

76. TINIDAZOLE
• TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED
AGAINST PROTOZOAN INFECTIONS. IT IS WIDELY KNOWN
THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS
A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC
INFECTIONS. IT WAS DEVELOPED IN 1972.

77. INDICATIONS
• INFECTIONS FROM AMOEBAE, GIARDIA AND
TRICHOMONAS
• TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE
SETTING OF METRONIDAZOLE TOLERANCE
• TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF
OTHER BACTERIAL INFECTIONS(E.G., AS PART OF
COMBINATION THERAPY FOR HELICO BACTER PYLO RI
ERADICATION PROTOCOLS).

78. MECHANISM OF ACTION
• TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO
CYTOTOXIC FORMS IN VIVO. IT HAS A LOW MOLECULAR
WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH
AEROBIC AND ANAEROBIC MICROORGANISMS. AFTER
DIFFUSING INTO THE CELLS OF SUSCEPTIBLE
ORGANISMS, TINIDAZOLE IS REDUCED AT ITS NITRO
GROUP TO SHORT LIVED TOXIC RADICALS BY A
FERRIDOXIN-MEDIATED TRANSPORT SYSTEM. IT IS
THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO
DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY
LEADS TO CELL DEATH.

79. MECHANISM OF ACTION

80. CONTRAINDICATION
 EPILEPTIC SEIZURE,
 NUMBNESS,
 TINGLING OR PAIN OF HANDS OR FEET,
 A MOTHER WHO IS PRODUCING MILK AND
BREASTFEEDING,
 DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD
CELL
 HYPERSENSITIVITY

81. ADVERSE EFFECT
• METALIC TASTE
• NAUSEA
• ANOREXIA
• DYSPEPSIA
• VOMITING
• WEAKNESS
• DIZINESS
• HEADACHE

82. DOSE
ANAEROBIC INFECTION :2G INITIALLY BY MOUTH FOLLOWED
BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS : A SINGLE 2G DOSE BY
MOUTH
BRANDNAME:
Protogyn Renata

83. ANTI-TUBERCULER AGENTS

85. MYCOBACTERIUM TUBERCULOSIS
• SLENDER
• ROD-SHAPED
• ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH
ACIDIFIED ORGANIC SOLVENTS)
• CAUSE LEPROSY AS WELL AS
SEVERAL TUBERCULOSIS-LIKE
HUMAN INFECTIONS
• INFECTIONS ARE INTRACELLULAR
• SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE
FOR MAJOR TISSUE DESTRUCTION
**MYCOBACTERIA ARE INTRINSICALLY
RESISTANT TO MOST ANTIBIOTICS
**THE LIPID-RICH MYCOBACTERIAL
CELL WALL IS IMPERMEABLE TO

86. TRANSMISSION:
• PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY
TRANSMISSION, PATIENTS WITH
THE ACTIVE DISEASE (BACILLI)
EXPEL THEM INTO THE AIR BY:
– COUGHING,
– SNEEZING,
– SHOUTING,
– OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR

88. STRATEGIES FOR ADDRESSING DRUG
RESISTANCE
• MULTIDRUG THERAPY
• BECAUSE,STRAINS OF M. TUBERCULO SIS THAT ARE
RESISTANT TO A PARTICULAR AGENT EMERGE
DURING TREATMENT WITH A SINGLE DRUG

89. NEWERSECONDLINE
DRUGS:
FLOUROQUINOLONES ARE
ACTIVE AGAINST
M.TUBERCULOSIS
CIPROFLAXACIN,
OFLAXACIN,
NEWER MACROLIDES AND
SOME RIFAMPIN
CONGENERS ARE THE
RECENT ADDITIONS.
CLARITHROMYCIN,
AZITHROMYCIN,
RIFABUTIN.
HIGH
EFFICACY
LOW
TOXICITY
LOW
EFFICACY
HIGH
TOXICITY

91. ISONIAZID(INH)
Isoniazid [eye-soe-NYE-a-zid],
the hydrazide of isonicotinic
acid, is a synthetic analog of
pyridoxine.
but is never given as a single
agent in the treatment of
active tuberculosis
It is the most potent of the
antitubercular drugs
Isoniazid is a prodrug

92. MECHANISM OF ACTION
• ISONIAZID INHIBITS SYNTHESIS OF
MYCOLIC ACIDS, WHICH ARE ESSENTIAL
COMPONENTS OF MYCOBACTERIAL CELL
WALLS.
• INHIS A PRODRUG THAT IS ACTIVATED BY
KATG, THE MYCOBACTERIAL CATALASE-
PEROXIDASE.
• THE ACTIVATED FORM OF ISONIAZID
FORMS A COVALENT COMPLEX WITH
ACYL CARRIER PROTEIN (ACPM)
BETA-KETOACYL CARRIER
PROTEIN SYNTHETASE (KASA)
• THIS COMPLEX BLOCKS MYCOLIC ACID
SYNTHESIS AND KILLS THE CELL.
• ISONIAZID INHIBITS SYNTHESIS OF
MYCOLIC ACIDS, WHICH ARE ESSENTIAL
COMPONENTS OF MYCOBACTERIAL CELL
WALLS.
• INHIS A PRODRUG THAT IS ACTIVATED BY
KATG, THE MYCOBACTERIAL CATALASE-
PEROXIDASE.
• THE ACTIVATED FORM OF ISONIAZID
FORMS A COVALENT COMPLEX WITH
ACYL CARRIER PROTEIN (ACPM)
BETA-KETOACYL CARRIER
PROTEIN SYNTHETASE (KASA)
• THIS COMPLEX BLOCKS MYCOLIC ACID
SYNTHESIS AND KILLS THE CELL.

94. INDICATION
TUBERCULOSIS (IN COMBINATION WITH OTHER
DRUGS)
CAUTION:
1. HEPATIC IMPAIRMENT
2. RENAL IMPAIRMENT
3. EPILEPSY
4. BREAST-FEEDING

95. SIDE EFFECT
• NAUSEA
• VOMITING
• PURPURA
• HYPERGLYCAEMIA
• OPTIC NEURITIS

96. DOSE
BY MOUTH, ADULT AND CHILD:
15MG/KG 3 TIMES A WEEK
BRANDNAME:
ISONIAZID(OPSONIN)
SERVIZID( NOVARTIS)

97. 2.RIFAMPIN[R]:
• SEMISYNTH. DERI OF RIFAMYCIN B-
FROM ST.MEDITARRANEI.
• ACTS BOTH EXTRA
&INTRACELLULARLY.
• GOOD STERILISING PROPERTY &
RESISTANCE PREVENTING ACTION.
• BACTERICIDAL EFFICACY ≈ INH
&>ANY OTHER 1ST
LINE
DRUG
• ANALOGUE OF RIFAMPIN IS RIFABUTIN.
OBTAINED FROM RIFAMYCIN S.

98. MECHANISM OF ACTION
D.N.A

RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES)
 DNA DEPENDENT R.N.A.POLYMERASE
R.N.A

PROTEIN SYN.

CELL MULTIPLICATION
RIFAMPIN BIND TO Β S.U OF D.D.R.P

DRUG –ENZ COMPLEX

SUPRESSION OF CHAIN INITIATION

99. INDICATION
• TUBERCULOSIS
• LEPROSY
• PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H.
INFLUENZAINFECTION

100. CAUTION
• HEPATIC IMPAIRMENT
• RENAL IMPAIRMENT
• PREGNANCY
• BREAST-FEEDING

101. CONTRAINDICATION
• HEPATIC FAILURE
• JAUNDICE
SIDE EFFECT
GIT SYMPTOMS
INFLUENZA LIKE SYMPTOMS
SHORTNESS OF BREATH
HAEMOLYTIC ANEMIA

102. • SYNTHETIC ANALOGUE OF NICOTINAMIDE
• HIGHLY EFFECTIVE DURING 1ST
2MONTHS
• ACTIVE BOTH INTRA & EXTRACELLULARLY
• THOUGH WEAKLY TUBERCULOCIDAL

MORE ACTIVE IN ACIDIC MEDIUM

103. MECHANISM OF ACTION
Pyrazinamide
Mycobacterial Pyrazinamidase
Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA

104. INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTION
HEPATIC IMPAIRMENT
RENAL IMPAIRMENT
DIABETES MELLITUS
GOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)

105. CONTRAINDICATION
• LIVER IMPAIRMENT
• PORPHYRIA
SIDE EFFECT
• IMPAIRED LIVER FUNCTIONS
• GI-TRACT UPSET
• ARTHRALGIA

106. BRANDNAME
• PYZIMIDE (JAMS)
• PZA-CIBA (NOVARTIS)

107. 4.ETHAMBUTOL[E]:
• TUBERCULOSTATIC ,ACTIVE AGAINST
M.TB
M.INTRACELLULARAE
• RAPID GROWERS ARE MORE SUSCEPTIBLE.
• HASTENS THE RATE OF SPUTUM CONVERSION.
• PREVENT THE EMERGENCE OF RESISTANT BACILLI.

108. MECHANISM OF ACTION
MYCOBACT. ARABINOSYL
TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF
ARABINOGLYCAN
ESSENTIAL COMPONENT OF

110. PHARMACOKINETICS
P.KProfile/DRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND
CSF
WIDELY BODY FLUID AND CSF BODY TISSUE,
INFLAMMED
MENINGES.
**METABOLISM ACETYLATION IN
LIVER
DEACETYLATION
IN LIVER
LIVER LIVER
EXCRETION URINE(75-95%) BILE,FAECES,
URINE
URINE(50%)
FAECES
URINE
PROTEIN BINDING: Very low (0 to
10%)
High to very high
(89%)
Low (10 to 20%) Low (20 to 30%)
PEAK PLASMA
CONCENTRATION
7 to 9 (mcg/mL) 3 to 7 mcg/mL 19 mcg/mL 2 to 5 mcg/mL
**
• Isoniazid undergoes N-acetylation and hydrolysis,
•resulting in inactive products.
•A bimodal distribution of fast and slow acetylators exists
•It is genetically regulated

111. INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTION
•RENAL IMPAIRMENT
•VISUAL ACUITY

112. CONTRAINDICATION
• OPTIC NEURITIS
• POOR VISION
SIDE EFFECT
• OPTIC NEURITIS
• RED OR GREEN COLOR BLINDNESS
• URTICARIA
• THROMBOCYTOPENIA

113. BRAND NAME
• FIAMBUTOL (FISONS)
• SURAL (AMBEE)

114. ANTI-LEPROTIC DRUG

115. Leprosy :
 Leprosy is a skin disease characterized by sores and boils
caused by Mycobacterium laprae.
 It was discovered in United States, but 70% of all causes are
located in India.
Antileprotic drug :
Drugs which is used in the treatment of Mycobacterium lapper are
called antileprotic drug. The following drugs are used in the treatment
of leprosy :-
 Daps one and other sulfones
 Rifampicin (Rifampin)
 Clofazimine
 Amithiozone

116. Treatment of leprosy :
a) Multi-bacillary form :-
- Daps one - 100 mg/day
- Rimfapicin - 600/once monthly
- Colafazimine – 50mg/day & extra 300 mg
monthly
Duration of treatment : 2 years minimum
b) For paucibacillary form of leprosy :-
- Daps one – 100 mg/day
- Rifampicin – 600 mg once monthly
Why we use the combination of drug?
 Most effective
Drug resistance grow incase of single drug
Lower the duration of treatment
Reduce the risk of adverse reaction
Prevent relafs

117. Dapsone
 Dapsone(diaminodiphenylsulfone) is most
widely used in the long-term treatment of leprosy
 It inhibits folate synthesis
 Dapsone may also be used to prevent and treat
Pneumocystis jiroveci pneumonia in AIDS
patients.

118. Pharmacokinetics :
• Route of administration : Oral
• Absorption : 70-90 %
• Protein binding : 70-80 %
• Metabolism : Hepatic (mostly CYP2E1 mediated)
• Half life : 20-30 hours
• Excretion : Renal

119. Mechanism of action :

120. Contraindication :
 Patient with allergy
 Pregnant women
Adverse effects :
 Haemolytic anaemia
 Sulfhaemoglobinaemia
 GIT intolarance : Nausea, Vomiting, Diarrhoea
 Fever, Pruritus, Rash
 Headache, Nervousness, Insomnia
 Blurring of vision
 Pariparal neuropathy
Dose :
 Adult: 100 mg daily
 Child: Proportionality less depending on weight
Brand Name:
Lepsone (Gaco)

121. Rifampicin :
 Broad spectrum antibiotics
 Bacteriocidal
 Kills both extracellur and intracellular mycobacterium
 Powerful enzyme inducer
Chemistry :
oRifampicin is a naturally made non-peptide
antibiotic
oIt is a derivitive of rifamycin

122. Pharmacokinetics :

123. MECHANISM OF ACTION OF RIFAMPICIN:
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE.

124. CONTRAINDICATION:
•Chronic liver disease
•Old age
•Alchoholism
•Vasculitis
Adverse effects of Rifampicin:
Hepatotoxicity:
 Cholestatic jaundice
 Hepatitis
Hypersensitivity:
 Rash
 Fever
 Nephritis
 Flu like syndrome
GIT upset:
 Naucea
 Vomiting
 Diarrhoea
 Abdominal cramps
Others: Thrombocytpenia, Ataxia, prurities,
Urticaria, renal insufficiency

125. Drug interaction:
Interaction Possible cause
Rifampicin+ Oral
anticoagulents (warferin):
Decrease effectiveness of
warfarin.
Rifampicin is a potent hepatic
enzyme inducer increases
metabolism of warferin.
Rifampicin+ OCP:
Decrease effectiveness of
OCP
Rifampicin increases
metabolism of estrogen of OCP
Rifampicin+ Steroid, digoxin,
Propanplol, Morphine:
Decreased biavailability of
these drugs.
Rifampicin is a potent hepatic
enzyme inducer increases
metabolism of these drugs
Dose:
Parentral: 600mg powder for IV injection
Oral: 150, 300 mg Capsule

126. Clofazimine:
•Is an antileprosy agent
•Available as soft gelatin capsule
•Bacteriostatic and mieldly bactereocidal effect an mycobacterium.
Chemistry:
Clofazimine is a phenazine dye with the following formula.

127. Pharmacokinetics:

128. Mechanism of action of clofazimine :
Clofazimine acts in two mechanisms:-
1)

129. 2)

130. Adverse effect:
Eosinophiolic enteritis
GI irritation
Discoloration of the skin
Depression
Bowel obstruction
Contraindication:
Diarrhoea
Peptic ulcer
Vomiting
steatorrhoea
Dose:
100 mg daily

131. THANKYOU

132. PREPARED BY:
P-121003
P-121007
P-121015
P-121018
P-121024
P-121038
P-121051