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Antibiotics
By :

Abdullah Taskin

-4th year med. Student -

BY : Abdullah Taskin 4th y.
• Classified according to their MOA into :

BY : Abdullah Taskin 4th y.
BY : Abdullah Taskin 4th y.
BY : Abdullah Taskin 4th y.
Penicillin's
1.
2.
3.
4.
5.
6.
7.
8.

Benzyl penicillin
Aminopenicillin (ampicillin IV - amoxicillin PO)
Isoxozoyl penicillin (cloxacillin, methicillin, )
Ureidopenicillin ( piperacillin )
Lactamase Inhibitors (Augmentin – tazobactam )
Cephalosporins ( 1 , 2 , 3 & 4 )
Carbapenems (imipenem )
Vancomycin (Vancocin®)
BY : Abdullah Taskin 4th y.
Coverage :
GP except
Staphylococcus,
Enterococcus
Oral anaerobes
(except
Bacteroides,
Treponema)

penicillin
MOA :
Bactericidal:
β-lactam inhibits
(PBP) and
prevents crosslinking of
peptidoglycans

BY : Abdullah Taskin 4th y.

Indications:
actinomycosis,
streptococcal
pharyngitis,
streptococcal
skin and soft
tissue infections,
syphilis
Contraindications:
Hypersensitivity to
penicillin
Coverage :
sam as
B.penicillin

MOA :
sam as
B.penicillin
Contraindications:
Hypersensitivity to
penicillin

Aminopenicillin
( Amoxicillin )

Indications:
bacterial meningitis ,
endocarditis ,
streptococcal ,
part of H. pylori treatment,
UTI

BY : Abdullah Taskin 4th y.
Coverage :
sam as B.penicillin

Isoxozoyl penicillin
(methicillin )

MOA :
sam as B.penicillin
Contraindications:
Hypersensitivity to
Penicillin
&
> Interstitial nephritis

Indications ( only diff. ) :
also cover some staph.a
BY : Abdullah Taskin 4th y.
Coverage :
sam as
B.penicillin

MOA :
sam as
B.penicillin

Ureidopenicillin
(Tazocin®)
Indications :
Same as penicillin &
GN: Pseudomonas
Anaerobes

Contraindications:
Hypersensitivity to
penicillin

Enterococcus
BY : Abdullah Taskin 4th y.
Coverage :
sam as B.penicillin

Lactamase Inhibitors
(Augmentin®)

MOA :
sam as B.penicillin
Contraindications:
Hypersensitivity to
Penicillin
&
jaundice or hepatic
dysfunction

Indications :
Same as penicillin
+/&
Staphylococcus
H. influenzae
Enterococcus

BY : Abdullah Taskin 4th y.
Cephalosporins ( 1 , 2 , 3 & 4 )
widely used

BY : Abdullah Taskin 4th y.
Coverage :
GP except
Enterococcus

Ceph.S. 1st
(cephalexin , cefazolin)

&

GN except
E. coli,
Klebsiella,
Proteus
MOA :
same as penicillin
(B-lactam)

Indications:
GP “more” & GN
Contraindications:
Hypersensitivity to Penicillin or ceha.S.

&
Nephrotoxicity

BY : Abdullah Taskin 4th y.
Coverage :
GP week
&
GN
&
anaerobes

MOA :
same as penicillin
(B-lactam)

Ceph.S. 2nd
(Ceftin®) , Cefprozil (Cefzil®))

Contraindications:
Hypersensitivity to
Penicillin or ceha.S.
BY : Abdullah Taskin 4th y.
Coverage :
GP
Staph & strep.
&

GN
broad
+ pseudomonas
MOA :
same as penicillin
(B-lactam)

Ceph.S. 3rd
(cefixime, ceftriaxone , cefotaxime
& ceftazidime )

Indications:
RTI, gonorrhea (use cefixime),
meningitis, septicemia,
abdominal infections
Contraindications:
Hypersensitivity to
Penicillin or ceha.S.
BY : Abdullah Taskin 4th y.
Coverage :

Ceph.S. 4th
(cefepime)

(good for gram
+ve and –ve)
&
pseudomonas
“penetrates the
CSF”
MOA :
same as penicillin
(B-lactam)

Contraindications:
Hypersensitivity to
Penicillin or ceha.S.
BY : Abdullah Taskin 4th y.
Cephalosporins (β-Lactam) :
a) Renal elimination

b) Ceftriaxone & Cefoperazone biotransformation in the liver.
c) Thrombocytopenia associated with cefamandole and
cefoperazone NOT cefotetan!!
d) Pyrogenic (highest rates of drug induced fever)
BY : Abdullah Taskin 4th y.
Coverage :
GN only
&
work with
aminoglycosides

MOA :
(B-lactam)

Monobactams β-Lactam Aztreonam

Indications:
patients who are allergic to penicillins
or cephalosporins

Contraindications:
Not allergic .
BY : Abdullah Taskin 4th y.
Coverage :
GP except
Enterococcus,
MRSA
GN including
Pseudomonas
+ Enterobacter
Anaerobes
MOA :
(B-lactam)

Carbapenams β-Lactam:
(Imipenam )
Indications:
LARGEST SPECTRUM OF ACTIVITY of any B-lactam
Rx: Septicemia of unknown origin
Major disadvantages:
metabolize by kidney > cause decreased urinary
concentration. SE: seizers ,rash
so IMIPENAM + CILASTATIN (inhibitor of
enzyme) are given
together.
BY : Abdullah Taskin 4th y.
Coverage :
GP except
Enterococcus,
MRSA
GN including
Pseudomonas
+ Enterobacter
Anaerobes

Carbapenams β-Lactam:
(meropenem )

Major disadvantages:
not need CILASTATIN
&
Less seizures

MOA :
(B-lactam)
BY : Abdullah Taskin 4th y.
Coverage :

NON β-Lactam:
( VANCOMYCIN )

GP (strong)

MOA :

Indications:
GP: (RESISTANT to methicillin)
e.g. MRSA & MRSE
must be given IV NO GI

Glycopeptide
stearically
inhibits addition of
peptidoglycan
subunits

Major disadvantages:
Red Man Syndrome
, Nephrotoxicity , Ototoxicity , Neutropenia,
Thrombocytopenia
BY : Abdullah Taskin 4th y.
NON β-Lactam:
(FOSFOMYCIN )

Coverage :
Gram +ve and –
ve spectrum

MOA :

Indications:
SINGLE DOSE Of uncomplicated UTI :
treatment of ONLY IN
FEMALES!!

inhibit cell wall
BY : Abdullah Taskin 4th y.
Contraindicated in pregnancy
1. Aminoglycosides
2. Erythromycin

3. Clarithromycin
4. Tetracyclines
5. Fluoroquinolones
BY : Abdullah Taskin 4th y.
Protein synthesis inhibitors :

BY : Abdullah Taskin 4th y.
50 S
A- Macrolides

Protein synthesis
inhibitors

B- Lincosamides

1) Erythromycin

1) clindamycin

2) clarithromycin

2) Chloramphenico

3) azithromycin

3) linezolid
BY : Abdullah Taskin 4th y.

30 S

1- Aminoglycosides
2- Tetracyclines
Macrolides

Coverage :
GP except
Enterococcus
&
GN
“Atypicals”

MOA :
inhibit 50 S

Indications:
Clarithromycin = H.pyloric
Azithromycin = Co-drug of choice for
Chlamydia & Safe in pregnancy .
Major disadvantages:
GI upset , acute cholestatic hepatitis
Prolonged QT
Hypersensitivity
BY : Abdullah Taskin 4th y.
clindamycin

Coverage :
GP except
Enterococcus
&
Anaerobes

MOA :
inhibit 50 S

clindamycin =Pseudomembranous
colitis
Chloramphenicol= Aplastic anemia &
Grey baby syndrome
linezolid = HTN , myelosuppression
optic neuropathy,
peripheral neuropathy
BY : Abdullah Taskin 4th y.
Aminoglycosides

Coverage :
GN &
psudomonas

MOA :
inhibit 30 S

Indications:
G - & no alternatives .

Major disadvantages:
Nephrotoxicity
Ototoxicity
BY : Abdullah Taskin 4th y.
Coverage :
GP
Anaerobes
Atypicals:
Chlamydophila,
Mycoplasma,
Treponema
prophylaxis
MOA :
inhibit 30 S

Tetracyclines
Indications:
Rickettsial infections,
Chlamydophila, acne
malaria
prophylaxis (doxycycline).
Major disadvantages:
Hepato-renal toxicity, Fanconi’s syndrome,
Photosensitivity, Teratogenic, Yellow teeth and
stunted , Taskin 4th y. growth in children,( not in preg.)
bone
BY : Abdullah
Coverage :
Poor GP activity
GN
Atypicals
FIncludes anaerobes

No Pseudomonas
coverage

TOPOISOMERASE INHIBITORS :
Fluoroquinolones
Indications:
Only use when necessary
to prevent resistance

except : ciprofloxacin

MOA :
Inhibits DNA gyrase
Dysglycemia

Major disadvantages:
Allergy , Seizures , Prolonged QT
BY : Abdullah Taskin 4th y.
Coverage :
GPC
N. meningitidis
H. influenza
Mycobacteria

MOA :
Inhibits RNA
polymerase

TOPOISOMERASE INHIBITORS :
Rifampin
Indications:
TB , latent TB , Endocarditis
& prophlaxis N. meningitides exposure

Major disadvantages:
Hepatic dysfunction, P450, Orange
tears/saliva/urine & Jaundice
BY : Abdullah Taskin 4th y.
Coverage :
Anaerobes
Protozoa

MOA :
Forms toxic
metabolites in
bacterial cell which
damage
microbial DNA

TOPOISOMERASE INHIBITORS :
Metronidazole (Flagyl®)
Indications:
Protozoal infections
(trichomonas, amebiasis,
giardiasis), bacterial
vaginosis, anaerobic bacterial
infections
Major disadvantages:
Seizures
Peripheral neuropathy ,
BY : Abdullah Taskin 4th y.
Coverage :
GP
GN: enteric
Nocardia
Other: Pneumocystis,
Toxoplasmosis

MOA :
Inhibits folic acid
production
(TMP inhibits DHFR and
SMX is a competitive
inhibitor of PABA)

ANTI-METABOLITE:
Trimethoprim- Sulfamethoxazole
(TMP/SMX)
Major disadvantages:
Hepatitis , Stevens Johnson syndrome
TMP:
- Megaloblastic anemia
- Leuko/granulocytopenia
- Hyperkalemia
SMX:
- Hypersensitivity
- Interstitial nephritis
- BM suppression
BY : Abdullah Taskin 4th y.
Remain :
• Antimyobacterial ( rifampicin covered above )

BY : Abdullah Taskin 4th y.
Appendix

BY : Abdullah Taskin 4th y.
Basic : G.ngative vs. G.positive

BY : Abdullah Taskin 4th y.
BY : Abdullah Taskin 4th y.
Properties of penicillin :

• All penicillin has Beta lactam ring .
• Trans-peptidase or (penicillin-binding protein)
• Function : Synthesis of peptidoglycan layer .
• To be effective Penicillin must :

I. Penetrate cell layer
II. Keeps it beta lactam ring intact
III.Bind to Trans-peptidase .
BY : Abdullah Taskin 4th y.
How bacteria defended from penicillin ?
In three ways :
1) G. negatives prevent penetration of
cell layers by
alteration of porins.
2)G. negatives destroy beta-lactam in periplasmic space
.
3) Bacteria inhibit binding of B.lactam
to transpeptidase by altering structure of Trans-peptidase .

BY : Abdullah Taskin 4th y.
References :
• Ananthanarayan & Pinker’s 8th edition .
• Clinical Microbiology Made Ridiculously Simple – 3rd edition

BY : Abdullah Taskin 4th y.
Thank you …
BY : Abdullah Taskin 4th y.
BY : Abdullah Taskin 4th y.

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Antibiotics simplified

  • 1. Antibiotics By : Abdullah Taskin -4th year med. Student - BY : Abdullah Taskin 4th y.
  • 2. • Classified according to their MOA into : BY : Abdullah Taskin 4th y.
  • 3. BY : Abdullah Taskin 4th y.
  • 4. BY : Abdullah Taskin 4th y.
  • 5. Penicillin's 1. 2. 3. 4. 5. 6. 7. 8. Benzyl penicillin Aminopenicillin (ampicillin IV - amoxicillin PO) Isoxozoyl penicillin (cloxacillin, methicillin, ) Ureidopenicillin ( piperacillin ) Lactamase Inhibitors (Augmentin – tazobactam ) Cephalosporins ( 1 , 2 , 3 & 4 ) Carbapenems (imipenem ) Vancomycin (Vancocin®) BY : Abdullah Taskin 4th y.
  • 6. Coverage : GP except Staphylococcus, Enterococcus Oral anaerobes (except Bacteroides, Treponema) penicillin MOA : Bactericidal: β-lactam inhibits (PBP) and prevents crosslinking of peptidoglycans BY : Abdullah Taskin 4th y. Indications: actinomycosis, streptococcal pharyngitis, streptococcal skin and soft tissue infections, syphilis Contraindications: Hypersensitivity to penicillin
  • 7. Coverage : sam as B.penicillin MOA : sam as B.penicillin Contraindications: Hypersensitivity to penicillin Aminopenicillin ( Amoxicillin ) Indications: bacterial meningitis , endocarditis , streptococcal , part of H. pylori treatment, UTI BY : Abdullah Taskin 4th y.
  • 8. Coverage : sam as B.penicillin Isoxozoyl penicillin (methicillin ) MOA : sam as B.penicillin Contraindications: Hypersensitivity to Penicillin & > Interstitial nephritis Indications ( only diff. ) : also cover some staph.a BY : Abdullah Taskin 4th y.
  • 9. Coverage : sam as B.penicillin MOA : sam as B.penicillin Ureidopenicillin (Tazocin®) Indications : Same as penicillin & GN: Pseudomonas Anaerobes Contraindications: Hypersensitivity to penicillin Enterococcus BY : Abdullah Taskin 4th y.
  • 10. Coverage : sam as B.penicillin Lactamase Inhibitors (Augmentin®) MOA : sam as B.penicillin Contraindications: Hypersensitivity to Penicillin & jaundice or hepatic dysfunction Indications : Same as penicillin +/& Staphylococcus H. influenzae Enterococcus BY : Abdullah Taskin 4th y.
  • 11. Cephalosporins ( 1 , 2 , 3 & 4 ) widely used BY : Abdullah Taskin 4th y.
  • 12. Coverage : GP except Enterococcus Ceph.S. 1st (cephalexin , cefazolin) & GN except E. coli, Klebsiella, Proteus MOA : same as penicillin (B-lactam) Indications: GP “more” & GN Contraindications: Hypersensitivity to Penicillin or ceha.S. & Nephrotoxicity BY : Abdullah Taskin 4th y.
  • 13. Coverage : GP week & GN & anaerobes MOA : same as penicillin (B-lactam) Ceph.S. 2nd (Ceftin®) , Cefprozil (Cefzil®)) Contraindications: Hypersensitivity to Penicillin or ceha.S. BY : Abdullah Taskin 4th y.
  • 14. Coverage : GP Staph & strep. & GN broad + pseudomonas MOA : same as penicillin (B-lactam) Ceph.S. 3rd (cefixime, ceftriaxone , cefotaxime & ceftazidime ) Indications: RTI, gonorrhea (use cefixime), meningitis, septicemia, abdominal infections Contraindications: Hypersensitivity to Penicillin or ceha.S. BY : Abdullah Taskin 4th y.
  • 15. Coverage : Ceph.S. 4th (cefepime) (good for gram +ve and –ve) & pseudomonas “penetrates the CSF” MOA : same as penicillin (B-lactam) Contraindications: Hypersensitivity to Penicillin or ceha.S. BY : Abdullah Taskin 4th y.
  • 16. Cephalosporins (β-Lactam) : a) Renal elimination b) Ceftriaxone & Cefoperazone biotransformation in the liver. c) Thrombocytopenia associated with cefamandole and cefoperazone NOT cefotetan!! d) Pyrogenic (highest rates of drug induced fever) BY : Abdullah Taskin 4th y.
  • 17. Coverage : GN only & work with aminoglycosides MOA : (B-lactam) Monobactams β-Lactam Aztreonam Indications: patients who are allergic to penicillins or cephalosporins Contraindications: Not allergic . BY : Abdullah Taskin 4th y.
  • 18. Coverage : GP except Enterococcus, MRSA GN including Pseudomonas + Enterobacter Anaerobes MOA : (B-lactam) Carbapenams β-Lactam: (Imipenam ) Indications: LARGEST SPECTRUM OF ACTIVITY of any B-lactam Rx: Septicemia of unknown origin Major disadvantages: metabolize by kidney > cause decreased urinary concentration. SE: seizers ,rash so IMIPENAM + CILASTATIN (inhibitor of enzyme) are given together. BY : Abdullah Taskin 4th y.
  • 19. Coverage : GP except Enterococcus, MRSA GN including Pseudomonas + Enterobacter Anaerobes Carbapenams β-Lactam: (meropenem ) Major disadvantages: not need CILASTATIN & Less seizures MOA : (B-lactam) BY : Abdullah Taskin 4th y.
  • 20. Coverage : NON β-Lactam: ( VANCOMYCIN ) GP (strong) MOA : Indications: GP: (RESISTANT to methicillin) e.g. MRSA & MRSE must be given IV NO GI Glycopeptide stearically inhibits addition of peptidoglycan subunits Major disadvantages: Red Man Syndrome , Nephrotoxicity , Ototoxicity , Neutropenia, Thrombocytopenia BY : Abdullah Taskin 4th y.
  • 21. NON β-Lactam: (FOSFOMYCIN ) Coverage : Gram +ve and – ve spectrum MOA : Indications: SINGLE DOSE Of uncomplicated UTI : treatment of ONLY IN FEMALES!! inhibit cell wall BY : Abdullah Taskin 4th y.
  • 22. Contraindicated in pregnancy 1. Aminoglycosides 2. Erythromycin 3. Clarithromycin 4. Tetracyclines 5. Fluoroquinolones BY : Abdullah Taskin 4th y.
  • 23. Protein synthesis inhibitors : BY : Abdullah Taskin 4th y.
  • 24. 50 S A- Macrolides Protein synthesis inhibitors B- Lincosamides 1) Erythromycin 1) clindamycin 2) clarithromycin 2) Chloramphenico 3) azithromycin 3) linezolid BY : Abdullah Taskin 4th y. 30 S 1- Aminoglycosides 2- Tetracyclines
  • 25. Macrolides Coverage : GP except Enterococcus & GN “Atypicals” MOA : inhibit 50 S Indications: Clarithromycin = H.pyloric Azithromycin = Co-drug of choice for Chlamydia & Safe in pregnancy . Major disadvantages: GI upset , acute cholestatic hepatitis Prolonged QT Hypersensitivity BY : Abdullah Taskin 4th y.
  • 26. clindamycin Coverage : GP except Enterococcus & Anaerobes MOA : inhibit 50 S clindamycin =Pseudomembranous colitis Chloramphenicol= Aplastic anemia & Grey baby syndrome linezolid = HTN , myelosuppression optic neuropathy, peripheral neuropathy BY : Abdullah Taskin 4th y.
  • 27. Aminoglycosides Coverage : GN & psudomonas MOA : inhibit 30 S Indications: G - & no alternatives . Major disadvantages: Nephrotoxicity Ototoxicity BY : Abdullah Taskin 4th y.
  • 28. Coverage : GP Anaerobes Atypicals: Chlamydophila, Mycoplasma, Treponema prophylaxis MOA : inhibit 30 S Tetracyclines Indications: Rickettsial infections, Chlamydophila, acne malaria prophylaxis (doxycycline). Major disadvantages: Hepato-renal toxicity, Fanconi’s syndrome, Photosensitivity, Teratogenic, Yellow teeth and stunted , Taskin 4th y. growth in children,( not in preg.) bone BY : Abdullah
  • 29. Coverage : Poor GP activity GN Atypicals FIncludes anaerobes No Pseudomonas coverage TOPOISOMERASE INHIBITORS : Fluoroquinolones Indications: Only use when necessary to prevent resistance except : ciprofloxacin MOA : Inhibits DNA gyrase Dysglycemia Major disadvantages: Allergy , Seizures , Prolonged QT BY : Abdullah Taskin 4th y.
  • 30. Coverage : GPC N. meningitidis H. influenza Mycobacteria MOA : Inhibits RNA polymerase TOPOISOMERASE INHIBITORS : Rifampin Indications: TB , latent TB , Endocarditis & prophlaxis N. meningitides exposure Major disadvantages: Hepatic dysfunction, P450, Orange tears/saliva/urine & Jaundice BY : Abdullah Taskin 4th y.
  • 31. Coverage : Anaerobes Protozoa MOA : Forms toxic metabolites in bacterial cell which damage microbial DNA TOPOISOMERASE INHIBITORS : Metronidazole (Flagyl®) Indications: Protozoal infections (trichomonas, amebiasis, giardiasis), bacterial vaginosis, anaerobic bacterial infections Major disadvantages: Seizures Peripheral neuropathy , BY : Abdullah Taskin 4th y.
  • 32. Coverage : GP GN: enteric Nocardia Other: Pneumocystis, Toxoplasmosis MOA : Inhibits folic acid production (TMP inhibits DHFR and SMX is a competitive inhibitor of PABA) ANTI-METABOLITE: Trimethoprim- Sulfamethoxazole (TMP/SMX) Major disadvantages: Hepatitis , Stevens Johnson syndrome TMP: - Megaloblastic anemia - Leuko/granulocytopenia - Hyperkalemia SMX: - Hypersensitivity - Interstitial nephritis - BM suppression BY : Abdullah Taskin 4th y.
  • 33. Remain : • Antimyobacterial ( rifampicin covered above ) BY : Abdullah Taskin 4th y.
  • 34. Appendix BY : Abdullah Taskin 4th y.
  • 35. Basic : G.ngative vs. G.positive BY : Abdullah Taskin 4th y.
  • 36. BY : Abdullah Taskin 4th y.
  • 37. Properties of penicillin : • All penicillin has Beta lactam ring . • Trans-peptidase or (penicillin-binding protein) • Function : Synthesis of peptidoglycan layer . • To be effective Penicillin must : I. Penetrate cell layer II. Keeps it beta lactam ring intact III.Bind to Trans-peptidase . BY : Abdullah Taskin 4th y.
  • 38. How bacteria defended from penicillin ? In three ways : 1) G. negatives prevent penetration of cell layers by alteration of porins. 2)G. negatives destroy beta-lactam in periplasmic space . 3) Bacteria inhibit binding of B.lactam to transpeptidase by altering structure of Trans-peptidase . BY : Abdullah Taskin 4th y.
  • 39. References : • Ananthanarayan & Pinker’s 8th edition . • Clinical Microbiology Made Ridiculously Simple – 3rd edition BY : Abdullah Taskin 4th y.
  • 40. Thank you … BY : Abdullah Taskin 4th y.
  • 41. BY : Abdullah Taskin 4th y.