Contains indication, pharmacokinetics and contraindications of all inhibitors of bacterial wall synthesis especially penicillins

1. Dr. NDAYISABA CORNEILLE
CEO of CHG
MBChB,DCM,BCSIT,CCNA
Supported BY
INHIBITORS OF
BACTERIAL CELL
WALL SYNTHESIS-
PENICILLINS

2. Inhibitors of bacterial cell wall synthesis
1. Beta lactam antibacterial drugs
a. Penicillins *
b. Cephalosporins
c. Carbapenems
d. Monobactams
e. Beta-lactamase inhibitors
2. Non-beta lactam antibacterial drugs
a. Vancomycin
b. Teicoplanin
c. Daptomycin
d.Cycloserine D
e.Bacitracin
f.Fosfomycin
Dr Ndayisaba Corneille

3. PENICILLINS
Dr Ndayisaba Corneille

4. Introduction
 Penicillins;
— Are examples of beta lactam antibacterials bcoz
they contain a beta lactam ring in their structure
— Are either natural & semi synthetic antibacterial
drugs
— Have the same basic structure
— Are usually used in tx of gram +ve bacterial
infections Dr Ndayisaba Corneille

5. — Were the first antibiotic drugs to be effective
against many previously serious diseases
like;
 Syphilis
 Staphylococcus infections
— Are still widely used today but many types
bacteria are currently resistant
— Can be inactivated by bacterial penicillase
enzymes (beta-lactamase enzymes)
Dr Ndayisaba Corneille

6. Mechanism of action of penicillins
— Inhibit bacterial growth by interfering with the
bacterial cell wall synthesis
— This eventually leads to bacterial cell death
— This is by inhibiting transpeptidation reaction
involved in formation of bacterial cell wall
-Penicillins kill bacterial cells only when they are
actively growing & synthesizing cell wall
Dr Ndayisaba Corneille

7. Classification of
Penicillins
Dr Ndayisaba Corneille

8. a) Natural penicillins
b) Repository forms of penicillin G
c) Semi synthetic penicillins
d) Beta-lactamase resistant penicillins
e) Broad spectrum penicillins
f) Antipseudomonal penicillins
g) Penicillins combined with beta-lactamase
inhibitors
Dr Ndayisaba Corneille

9. a) Natural penicillins
 Penicillins obtained from a fungus known as
penicillin notatum
 Are highly active against gram +ve bacteria
 Less active against gram –ve bacteria
 Are inactivated by bacterial beta-lactamase
Example
 Benzyl penicillin (penicillin G)
Dr Ndayisaba Corneille

10. b) Repository forms of penicillin G:
 Penicillin G procaine
 Penicillin G Benzathine
 Procaine penicillin Fortified (PPF)
 Penicillin Aluminium Methysylate - PAM oil
Dr Ndayisaba Corneille

11. c) Semi synthetic penicillins:
 Penicillins produced by modification of
natural penicillins
Examples
 Phenoxymethyl penicillin
Dr Ndayisaba Corneille

12. d) Beta-lactamase resistant penicillins:
 Are penicillins which are resistant to
beta-lactamase enzymes produced by some
bacteria like S.aeurus , E.coli etc
Examples
— Methicillin or Meticillin
— Temocillin
— Nafcillin
Dr Ndayisaba Corneille

13. — Isoxazolyl penicillins like:
 Cloxacillin
 Flucloxacillin
 Dicloxacillin
 Oxacillin
Dr Ndayisaba Corneille

14. e) Broad spectrum penicillins
— Can kill both gram +ve & gram -ve bacteria
Examples
1. Aminopenicillins: contain an amino group
 Ampicillin
 Amoxicillin
 Pavampicillin
 Bacampicillin
Dr Ndayisaba Corneille

15. f) Anti-pseudomonal penicillins
 Penicillins that are usually indicated to tx
pseudomonas aeruginosa infections
 They can also be used to tx other bacteria
infections
Examples
1. Carboxypenicillins:
 Carbenicillin
 Ticarcillin Dr Ndayisaba Corneille

16. 2. Ureidopenicillins:
 Piperacillin
 Azlocillin
 Mezlocillin
Dr Ndayisaba Corneille

17. g) Penicillins combined with beta-lactamase
inhibitors:
 Beta-lactamase inhibitors are agents which
inhibit beta-lactamase enzymes produced by
some bacteria like s.aeurus
 Examples of beta-lactamase inhibitors
 Clavulanic acid
 Sulbactam
 Tozabactam Dr Ndayisaba Corneille

18.  Penicillin + beta-lactamase inhibitors include;
 Clavulanic Acid + Amoxicillin
 Sulbactam + Ampicillin
 Tozabactam + piperacillin
Dr Ndayisaba Corneille

19. Pharmacokinetics of penicillins
 They can be given by;
 Oral route in mild infections
 IM
 Intravenously in severe infections
 Intrathecal x-pen cozes convulsions thus this
route is not recommended
Dr Ndayisaba Corneille

20.  Absorption of oral penicillins is ↓ when taken with
foods like;
 Caffeine -Citrus fruit
 Cola beverages -Fruit juices
 Tomato juice
Dr Ndayisaba Corneille

21.  Penicillins are widely distributed to most body
fluids & parts like;
 Joints
 Pleural cavity
 Pericardial cavity
 Gall bladder
 Saliva & milk
 Across the placenta
Dr Ndayisaba Corneille

22.  Bcoz penicillins are lipid insoluble this means
they;
 They do not enter mammalian cells
 Do not cross the BBB to get to brain unless
the meninges are inflamed like in meningitis
 Elimination of most penicillins is mainly by renal
tubular secretion Dr Ndayisaba Corneille

23. Clinical uses of the penicillins
 Genitourinary infections like cystitis ,pyelonephritis :Amoxiclav
 Severe dental infections like dental abscesses:Amoxiclav
 Cellulitis,Intra-abdominal infections :Amoxiclav
 Ampicillin Combined with flucloxacillin for empirical tx of cellulitis
(co-fluampicil)
 Ampicillin Combined with cloxacillin during tx of pyomyositis &
myositis (ampiclox)
 Ampicillin :Tx of chorioamnionitis in combination with gentamicin
 Ampicillin :Tx of exacerbations of bronchitis
 Ampicillin :Tx of bacterial peritonitis in combination with gentamicin
+ metronidazole
 Ampicillin:Tx of septicaemia in combination with gentamicin
 Ampicillin :Meningitis due to Listeria monocytogenes
 Ampicillin :Invasive salmonellosis
Dr Ndayisaba Corneille

24.  Bacterial meningitis due to Neisseria meningitidis,
Streptococcus pneumoniae: IV benzylpenicillin
 Bone & joint infections due to S. aureus: flucloxacillin
 Skin & soft tissue infections due to Strep pyogenes or S.
aureus ;IV benzylpenicillin or flucloxacillin
 Serious infections due to pseudomonas aeruginosa:
piperacillin.
 Syphilis:procaine benzylpenicillin or benzathine
penicillin
 TX of animal bites: co-amoxiclav
 Pharyngitis due to S. pyogenes: phenoxymethylpenicillin
Dr Ndayisaba Corneille

25.  UTIs due to Escherichia coli: amoxicillin
 Oral infections like dental abscess: amoxicillin
 Used in triple therapy in eradication of helicobacter pylori during tx
of peptic ulcer disease : amoxicillin
 Endocarditis due to S. viridans or Enterococcus faecalis:Amoxillin in
combination with other antibiotics
 Gonorrhea: amoxicillin + probenecid
 Tx of LRTIs like Pneumonia, Bronchitis: amoxicillin,Amoxiclav
 Tx ENT Bacterial Infection such as sinusitis, Otitis media: amoxicillin
 Otitis media due to S. pyogenes, haemophilus influenzae:
amoxicillin
 Tx meningitis due to Listeria monocytogenes:IV amoxicillin
Dr Ndayisaba Corneille

26. Indications of CLOXACILLIN
 Mild to moderate infections due to penicillase producing staph. Aureus
like;
1. Otitis externa
2. Staphylococcal pneumonia when cloxacillin is combined with
gentamicin
3. Impetigo
4. Cellulitis
5. Staphylococcal endocarditis
6. Localized soft tissue/skin infections like boils
7. Septicaemia when its combined with gentamicin
8. Pyogenic arthritis
9. Osteomyelitis
10. Pyomyositis
11. Myositis
Dr Ndayisaba Corneille

27. Indications OF Benzylpenicillin
1. Bacterial meningitis
2. Aspiration pneumonia in combination with fragyl
3. Lung abscess
4. Community-acquired pneumonia
5. Syphilis
6. Gonorrhea
7. Bacterial endocarditis
8. Septicemia in children & adults
9. Septic Arthritis
10. Cellulitis
11. Septic wounds
12. Gangrenous wounds like diabetic foot
13. Bacterial otitis media
14. Given as a prophylactic antibiotic after limb amputation & after major
surgeries
15. Treatment of anthrax
16. Throat infections like tonsillitis ,Pharyngitis
Dr Ndayisaba Corneille

28. S/Es
— Penicillins are remarkably nontoxic
1.Hypersensitivity reactions like
— Anaphylactic shock
— Urticaria
— Fever
— Joint swelling
— Intense pruritus
Dr Ndayisaba Corneille

29. — DIB
— Skin rashes
— Oral ulcerations
— Interstitial nephritis
— Hemolytic anemia
— Vasculitis
— Eosinophilia
— Angioneurotic edema
Dr Ndayisaba Corneille

30. 2. Others less common S/Es
 Seizures esp in pts with RF
 Supra-bacterial infections like vaginal
candidiasis
 N +V & diarrhea with oral penicillins
 Pseudomembranous colitis with ampicillin
 Neutropenia with nafcillin
Dr Ndayisaba Corneille

31.  Hepatitis with Oxacillin
 Non allergic skin rashes with ampicillin &
amoxicillin
Contraindications to penicillins
 Hx of hypersensitivity to penicillins
Dr Ndayisaba Corneille

32. END
BY
DR NDAYISABA CORNEILLE
MBChB,DCM,BCSIT,CCNA,Cyber Security
contact: amentalhealths@gmail.com ,
ndayicoll@gmail.com
whatsaps :+256772497591 /+250788958241
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