antibiotics

1. MACROLIDES AND
CHLORAMPHENICOL
SUBMITTED TO:
Dr.G.Ari hara sivakumar
Head of the department
Department of pharmacology
SUBMITTED BY:
Pavithra.V
M.Pharm-2nd SEM(2018-2019)
Department of pharmacology
KMCH college of pharmacy
SUBMITTED ON:07.02.2019

2. Targeting drugs to the 50s ribosomal subunit
Macrolides
Chloramphenicol
Lincosamides
Streptogramins
Oxazolidinones
pleuromutilins
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KMCH College of pharmacy,Department of
pharmacology

3. MACROLIDES
Macrolides are the large lactone rings
containing the 14 atoms
Bacteriostatic in nature
Macrolides is produced by saccharopolyspora
erythraea (formerly streptomyces erythrus)
Macrolides are bind to the small region of 23S
Rrna, near the peptidyl transferase active
center(translocation step)
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KMCH College of pharmacy,Department of
pharmacology

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KMCH College of pharmacy,Department of
pharmacology

5. MECHANISM
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KMCH College of pharmacy,Department of
pharmacology

6. MACROLIDE DRUGS
 Erythromycin
 Clarithromycin
 Azithromycin semisynthetic derivatives
 Dirithromycin
 Telithromycin
 Oleandomycin
 Tylosin
 spiramycin
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KMCH College of pharmacy,Department of
pharmacology

7. Route of administration
Most of the drugs administered by oral
administration
Topical route of administration-erythromycin
Oral administration of erythromycin-
bioavailability relatively low and variable
Erythromycin short half life than other drugs
Erythromycin gives four times a day
Clarithromycin two times a day
Azithromycin once in a day
Excreted by bile and urine
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KMCH College of pharmacy,Department of
pharmacology

8. SPECTRUM
Macrolides are broad spectrum activity
They are effective against penicillin resistant
strains
Macrolides are effective against most of the
gram (+)ve bacteria,cocci,bacillus
They are activity against gram(-)ve
cocci.especially neisseria spp too.
Macrolides active against
mycoplasma,chlamydia,campylobacterand
legionella in contrast to penicillins
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KMCH College of pharmacy,Department of
pharmacology

9. RESISTANCE
Methylation of guanine residue on ribosomal
RNA leads to lower affinity towards macrolide
An active efflux system
Presence of a plasmid-associated erythromycin
esterase
Clarithromycin and azithromycin show cross-
resistance with erythromycin,but
thelithromycin can be effective against
macrolide-resistant organisms
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KMCH College of pharmacy,Department of
pharmacology

10. RESISTANCE
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KMCH College of pharmacy,Department of
pharmacology

11. COMMON ADVERSE DRUG REACTION
Stomatitis
Heart burn
Nausea
Anorexia
Abdominal discomfort
diarrhoea
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KMCH College of pharmacy,Department of
pharmacology

12. ERYTHROMYCIN
 Active against gram(+)ve
 Acid labile
 Incomplete absorption
 Food delays the absorption
 Inactivated by gastric acid
 Widely distributed
 70-80% protein binding
 Does not cross the BBB
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KMCH College of pharmacy,Department of
pharmacology

13. SENSITIVITY
Highly sensitive:streptococcus
pyogens,streptococcus
pneumoniae,n.gonnorrhoeae,c.diphtheriae,liste
ria,camphylobacter etc..
Moderately sensitive: h.influenzae,
B.pertusis, n.meningitis, rickettsiae
Not sensitive: enterobacteriaceae,B.fragilis
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KMCH College of pharmacy,Department of
pharmacology

14. Binds to the receptor of motilin, a gastric hormone
that activate the duodenal and jejunal receptors
to initiate the peristalisis
Causing the uncoordinated peristalisis leading to
anorexia, vomitting, nausea.
• Azithromycin and clarithromycin less affinity
bind to these receptor
• High IV doses of erythromycin causes
ototoxicity, tinnitus, impaired hearing
• IV route of erythromycin causes the
thrombophelitis
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KMCH College of pharmacy,Department of
pharmacology

15. Uses:
• As an alternative to penicillin
• Streptococcal pharyngitis,
tonsillitis,mastoiditis,community acquired
pneumonia
• Prophylaxis of rheumatoid fever
• Diptheria
• Tetanus
• Syphilis and gonorrhoea
• leptospirosis
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KMCH College of pharmacy,Department of
pharmacology

16. 1st choice in
Atypical pneumonia
Whooping cough
Chancroid
2nd choice in
Campylobacter gastroenteritis
Legionnaires pneumonia
Chlamydia trachomatis
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KMCH College of pharmacy,Department of
pharmacology

17. Interaction
• Erythromycin and clarithromycin inhibit the
CYP3A4:
• theophylline,digoxin
• carbamazepine ,valproic acid
• cyclosporine ,cisapride
• phenytoin ,ergot alkaloids
• warfarin
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KMCH College of pharmacy,Department of
pharmacology

18. Azithromycin
More effective against on gram negative bacteria
Well tolerated,once daily
Mainly used in respiratory infection
Roxithromycin
The highest blood concentration
Long acting and acid stable
Used to treat the respiratory infection and soft
tissue infection
Low adverse effects
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KMCH College of pharmacy,Department of
pharmacology

19. clarithromycin
• Its active metabolite -14 hydroxy
clarithromycin
• Strongest activity against gram positive
bacteria
• In H.pylori infection-
clarithromycin+omeprazole +amoxicillin
• Induced the renal toxicity
• It is the only macrolide partially eliminated by
the kidney
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KMCH College of pharmacy,Department of
pharmacology
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20. NON ANTIBIOTIC APPLICATIONS
OF MACROLIDE
• Anti-inflammatory property
• Motilin receptor agonist
• Diffuse panbronchiolitis
• Cystic fibrosis
• Acute bacterial sinusitis
• Asthma
• Chronic obstructive pulmonary disease
• Bronchiectasis
• Chronic bronchitis
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KMCH College of pharmacy,Department of
pharmacology
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KMCH College of pharmacy,Department of
pharmacology
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KMCH College of pharmacy,Department of
pharmacology
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KMCH College of pharmacy,Department of
pharmacology
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