this is a detailed study on classification of all kind of antibiotic drugs .... a detailed pharmacological study please comment thank you

1. ANTIBIOTICS
CLASSIFICATION-
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
Blood
Integumentary
ermal
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. Antibiotics: Penicillins
•Natural penicillins
•Penicillinase-resistant penicillins
•Aminopenicillins
•Extended-spectrum penicillins

18. Antibiotics: Penicillins
Natural penicillins
•penicillin G, penicillin V potassium
Penicillinase-resistant penicillins
•cloxacillin, dicloxacillin, methicillin, nafcillin, oxacillin

19. Antibiotics: Penicillins
Aminopenicillins
•amoxicillin, ampicillin, bacampicillin
Extended-spectrum penicillins
•piperacillin, ticarcillin, carbenicillin, mezlocillin

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

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

22. Antibiotics: 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. Antibiotics: 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. Antibiotics: Cephalosporins
•First Generation
•Second Generation
•Third Generation
•Fourth Generation

29. Antibiotics: Cephalosporins
•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
(Mefoxin)
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 Ca2+ and Mg2+ and Al3+ 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. Aminoglycosides
•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. Aminoglycosides
•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. Aminoglycosides
•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. Antibiotics: 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
Body System Effects
CNS
GI
headache, dizziness,
depression, restlessness,
nausea, vomiting,
constipation, thrush,
increased liver function
studies. diarrhea,

56. Quinolones: Side Effects
Body System Effects
Integumentary
Other
rash, pruritus, urticaria,
flushing, photosensitivity
(with lomefloxacin)
fever, chills, blurred vision,
tinnitus

57. Antibiotics: Macrolides
•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