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Clinically useful families of beta- lactam compounds include penicillins , cephalosporins ,

Clinically useful families of beta- lactam compounds include penicillins , cephalosporins , monobactams carbapenems. The Action of Antimicrobial Drugs. The mechanism of action of penicillins and cephalosporins .

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Clinically useful families of beta- lactam compounds include penicillins , cephalosporins ,

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  1. Clinically useful families of beta-lactam compounds include • penicillins, • cephalosporins, • monobactams • carbapenems

  2. The Action of Antimicrobial Drugs

  3. The mechanism of action of penicillins and cephalosporins. β-Lactam antibiotics bind to and competitively inhibiting the transpeptidase enzyme that cross-links PG layers.

  4. Pharmacokinetics • - Orally, IM or IV • - Absorption dependant on stability in acid and absorption to food • - Widely distributed in body fluids • - Lipid insoluble • - Do not cross blood-brain barrier • - Elimination via kidneys • - 90% tubular secretion • - Short plasma half-life • - Intermittent exposure advantageous

  5. Penicillin

  6. Retention of Penicillin G

  7. What are the side-effects of antibiotics? • Most common side-effects of antibiotics: • Diarrhoea • Feeling and being sick • Fungal infections of the mouth, digestive tract and vagina • Rare side-effects of antibiotics: • Formation of kidney stones (when taking sulphonamides) • Abnormal blood clotting (when taking some cephalosporins) • Sensitivity to sun (when taking tetracyclines) • Blood disorders (when taking trimethoprim) • Deafness (when taking erythromycin and the aminoglycosides)

  8. Side Effects and Contraindications • - Hypersensitivity- rashes, fever • - GI disturbances • - Thrush • - Renal Impaired patients

  9. Allergic reactions to antibiotics Some patients may develop an allergic reaction to antibiotics - especially penicillins. Side effects might include a rash, swelling of the tongue and face, and difficulty breathing. Reactions to antibiotics can be very serious, and sometimes fatal - they are called anaphylactic reactions.

  10. Bacterial resistance: It is important to complete the whole course of the medication to prevent the infection from coming back. If you do not complete the course, there is a higher chance the bacteria may become resistant to future treatments - because the ones that survive when you did not complete the course have had some exposure to the antibiotic and may consequently have built up a resistance to it.

  11. Antimicrobial Resistance • Relative or complete lack of effect of antimicrobial against a previously susceptible microbe

  12. Antibiotic Resistance • A variety of mutations can lead to antibiotic resistance • Mechanisms of antibiotic resistance • Enzymatic destruction of drug • Prevention of penetration of drug • Alteration of drug's target site • Rapid ejection of the drug • Resistance genes are often on plasmids or transposons that can be transferred between bacteria.

  13. Resistance to Antibiotics

  14. Penicillin resistancevia penicillinase(βLactamase) Some penicillin resistant organisms produce Penicillinase which degrades penicillin.

  15. Broad vs. narrow spectrum drugs

  16. Antiseptics

  17. Antiseptics • - Anti (against) Septic (putrefactive) • - “substance applied to living tissue to prevent sepsis” • - Disinfectant- “substance applied to non-living materials to prevent microbial growth”

  18. History of Antiseptics • - 1867, Joseph Lister • Common antiseptics used during the last 150 years include alcohol, boric acid, hydrogen peroxide, iodine, carbolic acid and other phenol compounds, chlorohexadine, sodium chloride, sodium hypochlorite and calcium hypochlorite. • - Broad spectrum antimicrobials • - Multiple targets

  19. Chemical structures and uses of biocides in antiseptics and disinfectants

  20. Chemical structures and uses of biocides in antiseptics and disinfectants

  21. Mode of Action

  22. Savlon • Manufactured by Novartis Consumer Health, UK

  23. The active ingredients in Savlon cream • - Cholorohexidinegluconate - Cetrimide

  24. Mode of Action of Chlorhexidine

  25. Mechanism of Action • - Used topically • - Chlorohexidine- Bacteriocidal to Gram positive and Gram negative • - Membrane disrupting • - Cetrimide- cationic surfactant

  26. Side Effects and Contraindications • - Localised sensitivity • - Incompatible with anionic substances • - Nausea/ Vomiting • - Depression of CNS • - No known contraindications

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