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Kenya Medical Training College
Department of Orthopaedic and
Trauma Medicine
PHARMACOLOGY II
Year: 2022 Semester: 2
Session 2
Topic: Classification of Antibiotics
Date: 5th
April 2022
By: Carol Babu
Learning Objectives
By the end of this unit you should be able to:
▪ Classify penicillins
▪ Discuss mode of action of penicillins
▪ Describe Pharmacokinetics of penicillins
▪ Discuss the adverse reactions of penicillins
Classification of antibiotics
1. Beta lactams
• Have a beta lactam ring
• Examples – Penicillins, Cephalosporins,
Monobactam
Cont…
2. Aminoglycosides
• Have an amino acid and a glycoside in their
structures
• Examples – Gentamycin, Kanamycin, Streptomycin,
Amikacin, Tobramycin, vancomycin
3. Sulphonamides
• Are derivatives of sulphanolamide
• Includes sulphamethoxazole and
sulphadimidine
4. Tetracyclines
• Have a 4 ring structure in there make up
• Includes tetracycline, doxycycline,
minocycline, oxytetracycline
5. Macrolides
• Contain a macrocyclic lactone ring in their
structure
• Includes erythromycin, azithromycin,
clarithromycin
6.Polypeptides
• Includes bacitracin, colistin, polymixin B
7. Quinolones
• Includes nalidixic acid, norfloxacin,
ofloxacin,ciprofloxacin, perfloxacin
8. Nitrofurans
• Nitrofurantoin
• Nitrofurazone
• Furazolidine
9. Lincosamides
Lincomycin, clindamycin
10. Others
• Chloramphenicol
Penicillins
Sources
1. Natural penicillins – from a mould called
penicillium
2. Synthetic penicillins – Basic penicillin ring is
created through a fermentation process
• Penicillins produced thru a fermentation
process are called semi-synthetic
Classification of penicillins
A. Synthetic penicillins
1. Beta lactamase resistant penicillins
• Cloxacillin
• Oxaciliin
• Methicillin
• Flucloxacillin
2. Extended (wide) spectrum penicillins
• Amino penicillins such as
✔ Ampicillin
✔ Prodrugs e.g Pivampicillin
✔ Ampicillin analogues e.g Amoxicillin, Amoxicillin/
Clavulinic acid
• Amidino penicillins e.g Pivmecillin, Mecillinan
• Carboxy penicillins e.g Carbenicillin.
• Ureido penicillins e.g Mezlocillin, Azlocillin
B. Natural penicillins
• Benzyl penicillins – Pen G or Crystalline
penicillin
• Phenoxymethyl penicillin – Pen V
Mode of action of penicillins
• Penicillins interfere with cell wall synthesis
• They form cross linkages with the Beta
lactam bonds and cell wall
• Penicillins are bactericidal
• Resistance develops when the bacteria
produce beta lactamase enzyme that
destroys the drug.
Pharmacokinetics
Absorption – variable
• Some penicillins are denatured by acids in the
stomach and can therefore not be given orally e.
g benzyl penicillin
• Pen V is absorbed in the ilium but has a very
short half life
Distribution – Extracellular fluid
Metabolism -Liver
Excretion . Mainly via renals through
active tubular secretion and filtration
• Excretion can be delayed by drugs that
compete for anion transport
mechanisms e.g Probenizid
Adverse reactions of penicillins
• These are the drug unintended effects and
includes:
✔ Allergic reactions- skin rash, urticaria,
angioneurotic edema, anaphylactic shock. Cross
allergies occur with cephalosporins and
monobactams
✔ Diarrhea
✔ Neutropenia
✔ Convulsions and electrolyte imbalance
A). Natural penicillins
Benzyl penicillin
• Usually used when high doses of plasma
concentration of penicillin is needed.
• It is administered parenterally. Half life 30min
• It is highly protein bound and 80 % is excreted
via the kidneys
• Administration – IM with peak plasma conc.
30-60min, IV with peak conc. almost
immediately
Clinical uses
• Gram positive organisms- streptococcus
pneumonia, beta haemolytic streptococcus,
clostridia species, bacillus anthracis,
actinomyces israeli, leptospira
Benzanthine penicillin
• A sustained release preparation
• Gives low plasma concentration that lasts 3-4wks
• Not used for acute infections
• Mainly used for chemoprophylaxis for strep pyogenes
to prevent rheumatic fever
• Dose – 900mg or 1.2mu IM in children
- Adults 2.4mu monthly.
Adverse reaction- Extremely painful, anaphylactic shock
B). Synthetic penicillins
a). Beta lactamase resistant penicillins
• Prevents the beta lactamase from getting to the
beta lactam bond
• Used to treat infections such as Staphylococcus
spp especially the beta lactamase group
• Examples – cloxacillin, flucloxacillin, methicillin,
nafcillin, oxacillin
Cloxacillin
• Half life 30min
• Resist acid degradation
• Food interferes with absorption
• Formulations oral and parenteral
• Dose 500mg 6hrly
Flucloxacillin
• A pro drug of cloxacillin
• Half life 50min
• More fully absorbed than cloxacillin
• Available for oral and parenteral use
b). Extended spectrum penicillins
• Covers both Gram neg as well as Gram positive
organisms
Ampicillin
• Acid stable
• Well absorbed orally
• Can be given orally, IM or IV
• Dose 500mg -2g 6hrly
• Highly concentrated in bile and excreted
unchanged in urine
Amoxicillin/clavulinic acid
• Clavulinic acid is a beta lactam compound
produced from a fungus streptomyces
clavuliginus.
• Clavulinic acid has no antibacterial properties
but protects the penicillin from bacteria that
produces beta lactamase
• Administered orally or IV
• Common side effects include diarrhea and skin
rash resembling measles
NB: Other inhibitors of bacteria enzyme
penicilinase are sulbactam, tazobactum-
piperacillin

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2. PHARMACOLOGY II.pdf

  • 1. Kenya Medical Training College Department of Orthopaedic and Trauma Medicine PHARMACOLOGY II Year: 2022 Semester: 2 Session 2 Topic: Classification of Antibiotics Date: 5th April 2022 By: Carol Babu
  • 2. Learning Objectives By the end of this unit you should be able to: ▪ Classify penicillins ▪ Discuss mode of action of penicillins ▪ Describe Pharmacokinetics of penicillins ▪ Discuss the adverse reactions of penicillins
  • 3. Classification of antibiotics 1. Beta lactams • Have a beta lactam ring • Examples – Penicillins, Cephalosporins, Monobactam
  • 4. Cont… 2. Aminoglycosides • Have an amino acid and a glycoside in their structures • Examples – Gentamycin, Kanamycin, Streptomycin, Amikacin, Tobramycin, vancomycin 3. Sulphonamides • Are derivatives of sulphanolamide • Includes sulphamethoxazole and sulphadimidine
  • 5. 4. Tetracyclines • Have a 4 ring structure in there make up • Includes tetracycline, doxycycline, minocycline, oxytetracycline
  • 6. 5. Macrolides • Contain a macrocyclic lactone ring in their structure • Includes erythromycin, azithromycin, clarithromycin 6.Polypeptides • Includes bacitracin, colistin, polymixin B
  • 7. 7. Quinolones • Includes nalidixic acid, norfloxacin, ofloxacin,ciprofloxacin, perfloxacin 8. Nitrofurans • Nitrofurantoin • Nitrofurazone • Furazolidine
  • 8. 9. Lincosamides Lincomycin, clindamycin 10. Others • Chloramphenicol
  • 9. Penicillins Sources 1. Natural penicillins – from a mould called penicillium 2. Synthetic penicillins – Basic penicillin ring is created through a fermentation process • Penicillins produced thru a fermentation process are called semi-synthetic
  • 10. Classification of penicillins A. Synthetic penicillins 1. Beta lactamase resistant penicillins • Cloxacillin • Oxaciliin • Methicillin • Flucloxacillin
  • 11. 2. Extended (wide) spectrum penicillins • Amino penicillins such as ✔ Ampicillin ✔ Prodrugs e.g Pivampicillin ✔ Ampicillin analogues e.g Amoxicillin, Amoxicillin/ Clavulinic acid
  • 12. • Amidino penicillins e.g Pivmecillin, Mecillinan • Carboxy penicillins e.g Carbenicillin. • Ureido penicillins e.g Mezlocillin, Azlocillin
  • 13. B. Natural penicillins • Benzyl penicillins – Pen G or Crystalline penicillin • Phenoxymethyl penicillin – Pen V
  • 14. Mode of action of penicillins • Penicillins interfere with cell wall synthesis • They form cross linkages with the Beta lactam bonds and cell wall • Penicillins are bactericidal • Resistance develops when the bacteria produce beta lactamase enzyme that destroys the drug.
  • 15. Pharmacokinetics Absorption – variable • Some penicillins are denatured by acids in the stomach and can therefore not be given orally e. g benzyl penicillin • Pen V is absorbed in the ilium but has a very short half life Distribution – Extracellular fluid Metabolism -Liver
  • 16. Excretion . Mainly via renals through active tubular secretion and filtration • Excretion can be delayed by drugs that compete for anion transport mechanisms e.g Probenizid
  • 17. Adverse reactions of penicillins • These are the drug unintended effects and includes: ✔ Allergic reactions- skin rash, urticaria, angioneurotic edema, anaphylactic shock. Cross allergies occur with cephalosporins and monobactams ✔ Diarrhea ✔ Neutropenia ✔ Convulsions and electrolyte imbalance
  • 18. A). Natural penicillins Benzyl penicillin • Usually used when high doses of plasma concentration of penicillin is needed. • It is administered parenterally. Half life 30min • It is highly protein bound and 80 % is excreted via the kidneys • Administration – IM with peak plasma conc. 30-60min, IV with peak conc. almost immediately
  • 19. Clinical uses • Gram positive organisms- streptococcus pneumonia, beta haemolytic streptococcus, clostridia species, bacillus anthracis, actinomyces israeli, leptospira
  • 20. Benzanthine penicillin • A sustained release preparation • Gives low plasma concentration that lasts 3-4wks • Not used for acute infections • Mainly used for chemoprophylaxis for strep pyogenes to prevent rheumatic fever • Dose – 900mg or 1.2mu IM in children - Adults 2.4mu monthly. Adverse reaction- Extremely painful, anaphylactic shock
  • 21. B). Synthetic penicillins a). Beta lactamase resistant penicillins • Prevents the beta lactamase from getting to the beta lactam bond • Used to treat infections such as Staphylococcus spp especially the beta lactamase group • Examples – cloxacillin, flucloxacillin, methicillin, nafcillin, oxacillin
  • 22. Cloxacillin • Half life 30min • Resist acid degradation • Food interferes with absorption • Formulations oral and parenteral • Dose 500mg 6hrly
  • 23. Flucloxacillin • A pro drug of cloxacillin • Half life 50min • More fully absorbed than cloxacillin • Available for oral and parenteral use
  • 24. b). Extended spectrum penicillins • Covers both Gram neg as well as Gram positive organisms Ampicillin • Acid stable • Well absorbed orally • Can be given orally, IM or IV • Dose 500mg -2g 6hrly • Highly concentrated in bile and excreted unchanged in urine
  • 25. Amoxicillin/clavulinic acid • Clavulinic acid is a beta lactam compound produced from a fungus streptomyces clavuliginus.
  • 26. • Clavulinic acid has no antibacterial properties but protects the penicillin from bacteria that produces beta lactamase • Administered orally or IV • Common side effects include diarrhea and skin rash resembling measles NB: Other inhibitors of bacteria enzyme penicilinase are sulbactam, tazobactum- piperacillin