Antibiotics-a detailed classification | a detailed pharmacological study

this is a detailed study on classification of all kind of antibiotic drugs .... a detailed pharmacological study
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1. ANTIBIOTICS CLASSI F IC A TION - a detailed study PREPARED BY | MARTIN SHAJI | PHARM D

2. Antibiotics: Sulfonamides Penicillin's Cephalosporin's Tetracycline's Amino glycosides Quinolones Macrolides ANTI-INFECTIVE AGENTS

3. Chemotherapy Refers to treatment of diseases by chemicals Inhibits growth of pathogen (bacteria, viruses) Antibiotics are chemotherapeutics agents that is derived from cells of living organism This term may also refer to antineoplastic Chemotherapy is used in veterinary medicine similar to in human medicine

4. Chemotherapy Potentiating of antibiotics when two drugs are used in combination one may enhances the effect of others e.g. penicillin and streptomycin in the treatment of endocarditis Antibiotics antagonism when use in combination one may reduces the effect of another e.g. penicillin and chlortetracycline in pnemococcal meningitis

5. Chemotherapy contd, Drug resistances is the reduction in effectiveness of a drug " The use and misuse of antimicrobials in human medicine has led to a relentless rise in number and types of microorganisms resistant to these medicines - leading to death, increased suffering and disability, and higher healthcare costs ." - World Health Organisation

6. Chemotherapy contd, E.g. are Penicillinase Acetyltranferase RNA methylase

7. Chemotherapy contd, Mechanism of antibiotics  Inhibition of bacterial cell wall synthesis  Inhibition of cell membrane function  Metabolic antagonism  Inhibition of bacterial protein synthesis  Inhibition of nucleic acid synthesis

8. Antibiotics Medications used to treat bacterial infections Ideally, before beginning antibiotic therapy, the suspected areas of infection should be cultured to identify the causative organism and potential antibiotic susceptibilities.

9. Antibiotics Empiric therapy: treatment of an infection before specific culture information has been reported or obtained Prophylactic therapy: treatment with antibiotics to prevent an infection, as in intra-abdominal surgery

10. Antibiotics Bactericidal: kill bacteria Bacteriostatic: inhibit growth of susceptible bacteria, rather than killing them immediately; will eventually lead to bacterial death

11. Antibiotics: Sulfonamides One of the first groups of antibiotics sulfadiazine sulfamethizole sulfamethoxazole sulfisoxazole

12. Sulfonamides: Mechanism of Action Bacteriostatic action Prevent synthesis of folic acid required for synthesis of purines and nucleic acid Does not affect human cells or certain bacteria—they can use preformed folic acid

13. Sulfonamides: sulfamethoxazole Therapeutic Uses Azo-Gantanol Combined with phenazopyridine (an analgesic-anesthetic that affects the mucosa of the urinary tract). Used to treat urinary tract infections (UTIs) and to reduce the pain associated with UTIs. Bactrim Combined with trimethoprim. Used to treat UTIs, Pneumocystis carinii pneumonia, ear infections, bronchitis, gonorrhea, etc.

14. Sulfonamides: sulfisoxazole Therapeutic Uses Azo-Gantrisin Combined with phenazopyridine Used for UTIs Pediazole Combined with erythromycin Used to treat otitis media

15. Sulfonamides: Side Effects Body System Effect B l oo d Integumentary erm a l Hemolytic and aplastic anemia, thrombocytopenia Photosensitivity, exfoliative dermatitis, Stevens-Johnson syndrome, epid necrolysis

16. Sulfonamides: Side Effects Body System Effect GI diarrhea, Other Nausea, vomiting, pancreatitis Convulsions, crystalluria, toxic nephrosis, headache, peripheral neuritis, urticaria

17. Antibio t ics: Penicillins Natural penicillins Penicillinase-resistant penicillins Aminopenicillins Extended-spectrum penicillins

18. Antibio t ics: Penicillins Natural penicillins penicillin G, penicillin V potassium Penicillinase-resistant penicillins cloxacillin, dicloxacillin, methicillin, nafcillin, oxacillin

19. Antibio t ics: Penicillins Aminopenicillins amoxicillin, ampicillin, bacampicillin Extended-spectrum penicillins piperacillin, ticarcillin, carbenicillin, mezlocillin

20. Antibio t ics: Penicillins First introduced in the 1940s Bactericidal: inhibit cell wall synthesis Kill a wide variety of bacteria Also called “beta-lactams”

21. Antibio t ics: Penicillins Bacteria produce enzymes capable of destroying penicillins. These enzymes are known as beta-lactamases. As a result, the medication is not effective.

22. Antibio t ics: Penicillins Chemicals have been developed to inhibit these enzymes: clavulanic acid tazobactam sulbactam These chemicals bind with beta-lactamase and prevent the enzyme from breaking down the penicillin

23. Antibio t ics: Penicillins Penicillin-beta-lactamase inhibitor combination drugs: ampicillin + sulbactam = Unasyn amoxicillin + clavulanic acid = Augmentin ticarcillin + clavulanic acid = Timentin piperacillin + tazobactam = Zosyn

24. Penicillins: Mechanism of Action Penicillin's enter the bacteria via the cell wall. Inside the cell, they bind to penicillin-binding protein. Once bound, normal cell wall synthesis is disrupted. Result: bacteria cells die from cell lyses. Penicillin's do not kill other cells in the body.

25. Penicillins: Therapeutic Uses Prevention and treatment of infections caused by susceptible bacteria, such as: gram-positive bacteria Streptococcus, Enterococcus, Staphylococcus species

26. Penicillins: Adverse Effects Allergic reactions occur in 0.7% – 8% of treatments urticaria, pruritus, angioedema 10% of allergic reactions are life-threatening and 10% of these are fatal

27. Penicillins: Side Effects Common side effects: nausea, vomiting, diarrhea, abdominal pain Other side effects are less common

28. Antibio t ics: Ce p halos p orins First Generation Second Generation Third Generation Fourth Generation

29. Antibio t ics: Ce p halos p orins Semisynthetic derivatives from a fungus Structurally and pharmacologically related to penicillins Bactericidal action Broad spectrum Divided into groups according to their antimicrobial activity

30. Cephalosporins: First Generation cefadroxil cephalexin cephradine cefazolin cephalothin cephapirin Good gram-positive coverage Poor gram-negative coverage

31. Cephalosporins: First Generation cefazolin (Ancef and Kefzol) IV and PO cephalexin (Keflex and Keftab) PO used for surgical prophylaxis, URIs, otitis media

32. Cephalosporins: Second Generation cefonicid ceforanide cefmetazole cefotetan cefaclor cefprozil cefamandole cefoxitin cefuroxime Good gram-positive coverage Better gram-negative coverage than first generation

33. Cephalosporins: Second Generation cefuroxime (Kefurox and PO Cefoxitin ( Me fo x i n ) Ceftin) IV and IM Used prophylactically for prophylaxis abdominal or colorectal surgeries Also kills anaerobes Surgical Does not kill anaerobes

34. Cephalosporins: Third Generation cefixime cefpodoxime proxetil cefoperazone cefotaxime ceftizoxime ceftriaxone ceftazidime moxalactam Most potent group against gram-negative Less active against gram-positive

35. Cephalosporins: Third Generation cefixime (Suprax) Only oral third-generation agent Best of available oral cephalosporins against gram-negative Tablet and suspension ceftriaxone (Rocephin) IV and IM, long half-life, once-a-day dosing Easily passes meninges and diffused into CSF to treat CNS infections

36. Cephalosporins: Third Generation ceftazidime (Ceptaz, Fortaz, Tazidime, Tazicef) IV and IM Excellent gram-negative coverage Used for difficult-to-treat organisms such as Pseudomonas spp. Eliminated renally instead of biliary route Excellent spectrum of coverage

37. Cephalosporins: Fourth Generation cefepime (Maxipime) Newest cephalosporin agents. Broader spectrum of antibacterial activity than third generation, especially against gram- positive bacteria.

38. Cephalosporins: Side Effects similar to penicillin's

39. Antibiotics: Tetracyclines demeclocycline (Declomycin) oxytetracycline tetracycline doxycycline (Doryx, Doxy-Caps, Vibramycin) minocycline

40. Antibiotics: Tetracyclines Natural and semi-synthetic Obtained from cultures of Streptomyces Bacteriostatic—inhibit bacterial growth Inhibit protein synthesis Stop many essential functions of the bacteria

41. Antibiotics: Tetracyclines Bind to Ca 2+ and Mg 2+ and Al 3+ ions to form insoluble complexes Thus, dairy products, antacids, and iron salts reduce absorption of tetracyclines

42. Tetracyclines: Therapeutic Uses Wide spectrum: gram-negative, gram-positive, protozoa, Mycoplasma, Rickettsia, Chlamydia, syphilis, Lyme disease Demeclocycline is also used to treat SIADH, and pleural and pericardial effusions

43. Tetracyclines: Side Effects Strong affinity for calcium Permanent discoloration of teeth and tooth enamel in fetuses and children May retard fetal skeletal development if taken during pregnancy

44. Tetracyclines: Side Effects Alteration in intestinal flora may result in: Superinfection (overgrowth of nonsusceptible organisms such as Candida) Diarrhea Pseudomembranous colitis

45. Tetracyclines: Side Effects May also cause: Vaginal moniliasis Gastric upset Enterocolitis Maculopapular rash

46. Antibiotics: Aminoglycosides gentamicin (Garamycin) kanamycin neomycin streptomycin tobramycin amikacin (Amikacin) netilmicin

47. A m inoglyc o sides Natural and semi-synthetic Produced from Streptomyces Poor oral absorption; no PO forms Very potent antibiotics with serious toxicities Bactericidal Kill mostly gram-negative; some gram-positive also

48. A m inoglyc o sides Used to kill gram-negative bacteria such as Pseudomonas spp., E. coli, Proteus spp., Klebsiella spp., Serratia spp. Often used in combination with other antibiotics for synergistic effect.

49. A m inoglyc o sides Three most common (systemic): gentamicin, tobramycin, amikacin Cause serious toxicities: Nephrotoxicity (renal failure) Ototoxicity (auditory impairment and vestibular [eighth cranial nerve]) Must monitor drug levels to prevent toxicities

50. Aminoglycosides: Side Effects Ototoxicity and nephrotoxicity are the most significant Headache Paresthesia Neuromuscular blockade Dizziness Vertigo Skin rash Fever Superinfections

51. Antibio t ics: Quinolones ciprofloxacin (Cipro) enoxacin (Penetrex) lomefloxacin (Maxaquin) norfloxacin (Noroxin) ofloxacin (Floxin)

52. Quinolones Excellent oral absorption Absorption reduced by antacids First oral antibiotics effective against gram-negative bacteria

53. Quinolones: Mechanism of Action Bactericidal Effective against gram-negative organisms and some gram-positive organisms Alter DNA of bacteria, causing death Do not affect human DNA

54. Quinolones: Therapeutic Uses Lower respiratory tract infections Bone and joint infections Infectious diarrhea Urinary tract infections Skin infections Sexually transmitted diseases

55. Quinolones: Side Effects B od y Sy ste m Eff e c t s CN S GI headache, dizziness, depression, restlessness, nausea, vomiting, constipation, thrush, increased liver function studies. diarrhea,

56. Quinolones: Side Effects B o d y Sy ste m E ff e c t s Integumentary Ot h e r rash, pruritus, urticaria, flushing, photosensitivity (with lomefloxacin) fever, chills, blurred vision, tinnitus

57. Antibio t ics: Macrolid e s erythromycin azithromycin (Zithromax) clarithromycin (Biaxin) dirithromycin troleandomycin bactericidal action

58. Macrolides: Therapeutic Uses Strep infections Streptococcus pyogenes (group A beta-hemolytic streptococci) Mild to moderate URI Haemophilus influenza Spirochetal infections Syphilis and Lyme disease Gonorrhea, Chlamydia, Mycoplasma

59. Macrolides: Side Effects GI effects, primarily with erythromycin: nausea, vomiting, diarrhea, hepatotoxicity, flatulence, jaundice, anorexia Newer agents, azithromycin and clarithromycin: fewer side effects, longer duration of action, better efficacy, better tissue penetration

60. Thank you…