Anti Microbial Agents on Beta Lactam Drugs

1. Antimicrobial Drugs
(A.Beta Lactam Drugs)
Dr.Saroj K. suwal

2. Anti bacterial Drugs
 A.Beta Lactam Drugs
 B. Supha Drugs
 C.Aminoglycoside
 D. Tetracycline

3. A.Beta Lactam Antibiotics
 have beta lactam ring nucleus in molecular structure
 Nitrogen is attached to beta carbon relative to carbonyl ring
 Sub classes
 Penicillin
 cephalosporins
 carbapenems
 monobactams
Beta-lactam ring Antibiotics (PCCM)
➢Penicillin
➢Cephalosporins
➢Carbapenems
➢Monobactams

4. Characteristics of Beta lactams
 Same MOA:
 inhibit cell wall synthesis
 Bactericidal
 Short half life
 Primarily renally eliminated
 cross allergenicity

5. General Mechanism of action of beta lactams
Cell Death
interfere with cell wall synthesis
inhibit of peptidoglycan synthesis
binding to penicillin binding proteins ( PBPs)
located in bacterial cell walls

6. Penicillin
 Beta lactam antibiotics
 Used in treatment of bacterial infection caused by staphylococci and
streptococci
 Usually gram positive organism
 Hypersensitivity is the most important adverse effect of the penicillins.

7. Mechanism of actions
 Penicillins are bactericidal antibiotics
 The synthesis of cell wall of bacteria
is completely depended upon an
enzyme named as transpeptidase.
Penicillin
inhibits the cell
wall synthess of
bacteria
Destroy of
bacteria

8. Classification of Penicillin
Penicillin
1. Natural
Penicillin
Benzyl
penicillin
Benzathine
penicillin
phenoxy
methyl
penicillin
procaine
penicillin
2. Semi Synthetic Beta lactamase
resistant Penicillin()
Methicillin
Oxacillin
Cloxacillin
Flucloxacillin
3. Broad Spectrum
Penicillin
Amoxicillin
Amox Clav
Ampicillin
Ampi
sulbactum
4. Extended Penicillin
Piperacillin
Tazobactam
Carbenicillin
Azlocilin
Ticarcillin
Piperacillin

9. 1. Natural Penicillin
 Active against gram positive cocci
 But ineffective against staphylococcus aureus
 Drugs:
 Benzathine penicillin (injection)
 injection,6,00000 IU, 1.2 million units and 2.4 million units per vail
 Penicillin G potassium (injection)
 injections, 1,2,3,5 million per vail
 Penicillin G Procaine (injection)
 injection, 600000, 1.2 million, 2.4 million units
 Penicillin V (tablet)
 tablets/suspension→250mg, 500mg, 125mg/5ml, 250mg/5ml

10. 2. Penicillinase Resistant penicillin
 Effective against penicillinase producing staphylococcus aureus
 Less effective against gram positive cocci than natural penicillin
 E.g.
 Cloxacillin, Dicloxacillin, Flucloxacillin, Nafcillin, Oxacillin
 Cloxacillin→
 capsule, injection →250mg, 500mg,
 Suspension →125mg/5ml
 Are in capsule, suspension, injection form

11. 3. Broad Spectrum Penicillin
 effective against gram positive cocci and some gram negative
bacteria
 Drugs
 Amoxicillin→ tablet, capsule, suspension, injection
 Amoxicillin and clavulanate → tablet, suspension, injection
 Ampicillin→tablet, suspension, injection
 Ampicilin + Sulbactam→injection, tablet

12. 4. Extended spectrum Penicillin
 Effective against Pseudomonas aeruginosa,
Enterobacter, proteus species
 Drugs
 Carbenicillin→tablet, 382 mg
 Piperacillin/Tazobactam→injection 2.25gm,
3.375gm, 4.5 gm
 Ticaracillin or plus clavulanate→injection->1,3,5
gm per vail

13. Benzyl Penicillin ( Penicillin-G)
 Oldest narrow spectrum antibiotics
 Gram positive bacterial coverage
 Comes in powder for injections in vail
 IV or IM
 Penicillin G injection
 300,600 mg x 6 Hrly
 Or 5 00000, or 100000 units or 5000000 units
 600mg➔1000000 units
 Penicillin G potassium Tablets→2 , 4,8 lack

14. indications
 Streptococcal, meningococcal and
gonococcal infection
 Otitis media, pneumonia, Diphtheria
 Clostridium prefinges, tonsillitis
 Rehumatic Fever prohylaxis

15. Usual dose
 2.4- 4.8 gm( 4to 8 lac units) per day in 4 divided dose
 IM or IV ( slow infusion)
 Child →100mg /kg/day in 4 divided dose
 Contraindication
 Hypersensitivity
 Sever anaphylaxis can occur so give after skin test

16. Adverse effect
 Hypersensitivity including anaphylaxis
 Diarrhea after oral use
 Local site pain
 Erythema at injections site

17. Nursing Management
 Access history of drug allergy
 Skin test should be done before systematic
administration
 Hyperkalemia or hyper natremia if high dose to
renal disease patient
 So, RFT regularly monitered

18. Benzathine Penicillin(Pendura)
 Long acting
 Not soluble so, must given by
intramuscular route only
 600000 units, 1.2 million, 2.4
million units per vail

19. Indications
 Streptococcal and post streptococcal infection(pharyngitis,
tonsillitis)
 Prophylaxis for prevention of rheumatic heart disease
 Upper and lower respiratory tract infection
 Acute Rheumatic Fever
 Diptheria
 Tetanus
 Rheumatic arthritis
 Syphillis

20. Dose
 For streptococcal → 12 lack I/M single dose
 Rhumatic fever prophylaxis→ 12 lac I/M
every 3 weekly
 Syphilis→ sing dose 24 lac I/M

21. Nursing management
 Should be skin test before administration
 Should be given deep I/M in large gluteal
muscle
 Need ready for the emergency resuscitation
equipments to manage possible prophylaxis

22. Penicillin V
 Pheno oxymethyl penicillin
 Better for oral use
 Use for gram positive bacteria
 Dose
 250-500mg QID for 7 days
 Prophylaxis for rheumatic heart disease→ 250mg BD for long period( 6
months about)
 Child → 25-50 mg per kg per day QID

23. Indications
 Mild to mod. Respiratory tract
streptococcal infections , pneumococcal
infection
 Otitis media, oropharynx infections,
 Prophylaxis for recurrent rheumatic fever

24. Adverse effect
 GIT→diarrohea, nausea, vomiting,
Pseudomembranous colitis
 Blood→ hemolytic anemia
 Convulsion, fever, skin rash, super
infections

25. Nursing Management
 Neomycin and Penicillin V shouldn’t be give at some
time
 Coz can cause malabsorption of pen V. occur
 Store in refrigerator
 Discard unused portion after 14 days
 Other same as benzathine penicillin

26. Amoxicillin
 For gram positive and less gram negative
 TID given
 Has less incidence of diarrhea
MOA
 Inhibit cell wall synthesis

27. Indications
 Sinusitis
 Otitis media
 Chronic bronchitis
 Pneumonia
 Peptic ulcer
 UTI
 Gonorrhea
 Typhoid fever
 Prophylaxis of endocarditis
 Listeria meningitis

28. Dose
 Tab. Amoxacillin 250-500 mg PO x
TDS
 Inj. Amoxacillin 500mg IV QID for
severe infections
 Child upt ot 12 yrs→20-40mg/lg/day
x TDS

29. Adverse effect
 Dizziness, lethargy, diarrhea, nausea,
abdominal pain, skin rash
 Steven johson syndrome
 Super infections

30. Nursing Management
 Keep suspension at room temperature
stable for 2 weeks at 2-8 deg. Cetigrate
 Pediatric drops directly on children Tongue
for swallowing
 Can be added in milk , water, fruit juice

31. Ampicillin
 Broad spectrum antibiotics
 Similar to amoxycillin but highly effective against H.influenza and shigella bacteria
 Bioavibility less than amoxycillin so need to give QID
 Indications→ same as amoxycillin but has broad coverages
 Dose→250,500 mg in capsule
 100mg 250mg , 500mg in IV/IM x 6 hrly
 For meningitis→ combined with other antibiotics
 Child → 100-200mg /kg/day

32. Adverse effet
 Same as others
 Perioral edema

33. Cloxacillin
 Highly penicillinase as well as acid resistant so can be given orally
 For
 Infections caused by penicillinase producing staphylococci, pneumococci,
group A beta hemolytic streptococci
 Dose
 250-500 mng POxQID
 Child→ 50-100mg/kg/day x QID(IV,IM,PO)

34. Flucloxacillin
 Used for infections due to beta lactamase producing
staphylococci in
 Otitis media , pneumonia, impetigo , cellulitis,
osteomyelitis , staphylococcal endocarditis
 Dose
 250-500 mg xqid at least 30 mins before food
 IV/IM/PO

35. Side effect
 Same to benzyl penicillin
 GI disturbance
 Very rarely hepatitis and cholestatic
jaundice on prolonged used

36. Penicillin combined with beta lactamase inhibitor
 Beta lactamase inhibitor
 resemble beta lactamase antibiotic structure
 bind to beta lactamase and protect antibiotic from destruction
 most successful when they bind beta lactamase
 Three important in medicine
 clavulanice acid
 sulbactum
 tazobactam
Penicillin + beta lactamase inhibitors
• Amoxacillin + Clavunic Acid(
• Ampicillin + Salbactum
• Piperracilin + Tazobactam
• Ticaracillin + Clavunic acid

37. Amoxicillin + potassium clavulanate
 Augmentin, CLAVAM,INDICLAV, MOXICLAV
 Amoxicillin against gram positive
 Clavulanate establish the activity of amoxicillin against
beta lactamase production resistant bacteria
 staphylococcus aureus ,
 H. influenza,
 N. gonorrhea,
 E.coli, Proteus, Klebsiella, salmonella

38. Mechanism of actions( amoxiclav)
 Amoxicillin is bactericidal
 clavulanic → protect from enzymatic degradation
Clavulanate
inhibit beta
lactamase
protect
amoxicillin
from
enzymatic
degradation

39. Uses
 Infections due to Beta lactamase
organism
 RTI
 Genitourinary Infections
 Abdominal infections
 Cellulitis
 Dental infections

40. Prepration,Dose, s/E , CI
Prepration
 Tab: 357mg( amox/clavunate→250/125mg), 625mg(500/125)
 Injction : 500/100( amox 500 as sodium salt and clavunic acid 100mg as potassium), 1.2
gm vail
Dose
 Amox 250-500 mg /clavunate 375-625mg PO/IV TDS
 IV 1.2 gm
 Side effects
 Hepatis, cholestatic jaundice, Steven Jonson syndrome, dizziness, exfoliative
dermatitis
 C/I
 Hypersensitive

41. Cephalosporin
 Semi Synthetic Antibiotics
 are similar to Beta lactam antibiotics
 From fungus Acremonium
 Are effective against bacteria which are resistant to
ampicillin like pseudomonas
 V Generations

42. Cephalosporin
First Generations
(moderate
Spectrum)
Cephalexin ,
Cephadroxil,
Cephazolin
Second Generation
(moderate
Spectrum)
Cefuroxime,
Cefmetazole,
Ceforanide
Third Generation
(Broad Spectrum)
Cefotaxime,
Ceftriaxone,
Ceftazidime,
Cefeperazone,
Cefixime
Fourth Generation
(Broad Spectrum)
Cefepime,
Cefpodoxime
Each newer
generation has
increased
activity
against
G-ve rods
and
decreased
activity
against G+ve
cocci

44. Mechanism of Action
 All are Bactericidal ( same as Penicillin)
 Peptidoglycan layer is important for cell wall
structural integrity
 The final step in synthesis of
peptidoglycan(Transpeptidation) is facilitated by
transpeptidases(penicillin binding proteins)
 Cephalosporins competitively inhibit PBP and
disrupt synthesis of peptidoglycan
 Inhibit bacterial cell wall synthesis

45. THERAPEUTIC USES
 Pharyngitis
 Tonsillitis
 Bronchitis
 Pneumonia
 UTI
 Skin and bone
infections(cefazolin and
ceftriaxone have good
penetration into bone)
 Meningitis( 3rd generation
cephalosporins)
 Surgical prophylaxis

46. Adverse Effect
 Diarrhea, nausea, vomiting
 Pain and inflammation at injection site
 Pseudomembranous colitis
 Allergic reactions
 Bleeding(cefamandole, cefeperazone,
ceftriaxone) ->anti vit-k effect)

47. Parental and Oral Preparations
 Crosses placenta and secreted in breast milk
 Elimination occurs through tubular
secretion/glomerular filtration
 Cefeperazone and ceftriaxone are excreted through
bile (can be administered in renal insufficiency)

48. First Generations
 Cefadroxil, Cefazolin, Cephalexin,
Cephradine
 Strongly for G+Cocci, strep. pneumonia,,
S.pyogenes
 Moderately active against a few G-
ve:E.coli,P.mirabilis,K.pneumonia
 No activity against: Enterococci , MRSA and
B.fragilis

49. Cefazolin
 Mainly used for Skin Infections
 Narrow spectrum but Good Gram Positive
Coverage
 Used for Moderate to severe bacterial
infections of lungs, bone, joint, stomach,
blood , valve and urinary tract

50. Preparations and Dose
 IM and IV preparations
 Powder for Injection:125 mg, 250 mg, 500mg, 1gm in vail
 Adult → 250-500mg TDS
 Child over month→25-50 mg/Kg in TDS or QID
 Perioperative Prophylaxis→
 1gm single dose half an hour before surgery
 If surgery is prolonged more than 2 hour→ 500 to 1 gm every 6-8 hours

51. Adverse Effect
 High does in renal patient may have extreme
confusion
 Tonic colonic seizure
 Increase risk of bleeding when used with
anticoagulants

52. Cefadroxil
 Active against beta lactamase producing bacteria
 E.Coli and Streptococci
 Well absorbed in GI tract
 Crosses placenta and appears in breast milk
 Indications:
 UTI by E.coli, Klebsiella
 Skin and skin structure infection due to staph or strep cocci
 Phyrangitis, tonsillitis due to group A beta hemolytic streptococci

53. Preprations and dose
 Capsule →500mg and 1gm
 Dispersible tablet→ 125mg, 250mg
 Oral Suspension→ 5m=125 and 250mg
Dose
 Adult→ 1-2 gram in single or divided dose
 Children below one yr→30mg /body weight
 1-6 yrs→ 250mg BD
 Overr 6 Years→ 500mg BD

54. Cephalexin
 Oral administrations
 RTI due to strep Pneumonia ,Group A beta Hemolytic streptococci
 Otitis Media
 GU and Bone infections
 Skin Infections
Prepratons:
• Capsule→ 250mg, 500mg
• Dispersible Tablet→125mg
• Suspension→125mg/5ml, 250mg/5ml
• Dose
• 250-500mg QID
• Child→ 75-100mg/kg/day in QID

55. Second Generation
 Effective against Gram Positive proteus, H.
Influenzas, gram negative Enterobacter,
Klebsiella

56. Cefuroxime axetil
 Oral and injection form
 URTI (Pharyngitis, tonsillitis, otitis media, sinusitis
 LRTI( bronchitis, Pneumonia)
 Uncomplicated UTI
 Uncomplicated gonorrhea
 Skin infections

57. Preparations and Dose
 Tablet→ 125mg, 250mg, 500mg
 Suspension→ 125mg/5ml, 250mg/5ml,
 Injection→250mg/50ml
 Powder for injection→ 750mg, 1.5 mg
Dose
 Adult/children/over 18→125-250mg BD for 7-10 days
 Children→ 20mg/kg/day BD for 10 days

58. Nursing Management
 SHAKE WELL BEFORE USE if suspension
 If I/M→ choose large muscle mass → watch for pain
 Dissolve medicine with sterile water or Nacl solution and Shake well until it
dissolves
 For I/V→Dissolve in 5 ml minimum and give slowly over 3-5 mins to prevent
vein irritation
 Discard reconstituted medicine after 24 hours room temp and after 96 hrs
when refrigeration

59. Third Generation Cephalosporin
 Extended or Broad Spectrum
 Inferior activity to gram + cocci
 Enhanced activity against
 gram –ve organism Including N.Gonorrhea Enterobacter E.Coli
K.Pneumonia And Pseudomonas aeruginosa

60. Cefixime
 Bactericidal
Effective against
 Ecoli, H. Influenza, S. Pyrogenes, Strep
pneumonia, beta lactamase positive and
negative strains
 Tablet→200mg, 400mg
 Power for injection→100mg/5ml
Dose
 Adult → 200mg BD or 400 mg Once
 Child→ 8mg/kg OD or 4mg/kg BD
 For uncomplicated gonorrhea→ 400mg
OD
 Adult dose for children above 12 years
and more than 50 kg
Indications:
 Uncomplicated UTI cause by E.coli
 Otitis media
 Phyrangitis and tonsillitis
 Acute and chronic bronchitis
 Uncomplicated cervical and urethral
gonorrhea

61. Nursing Management
 Ask for cephalosporin and penicillin hypersensitivity
reaction before starting medicine
 OD should take at same time to maintain
bioavailability
 W/F GI upset eps diarrhea
 Once reconstituted → keep in room temp

62. Cefotaxim
 Active against beta lactamase production Bactria and gram positive
 IV route especially in Life threating infections,
 post surgery,
 trauma patients,
 malignancy,
 diabetes,
 shock
Indications
• GI Infections
• Lower RTI
• Skin infections
• Bone and Joint infection
• Meningitis and other CNS infections
• Intra-abdominal infection (peritonitis)
• Gynecological infection(endrometrosis,PID)
• Septicimia, bacterima
• Prohylaxis in Surgery

63. Preparations and dose
 Powder for injection→25omg, 500 mg, 1gm, 2gm
Dose
 Adult→ 1gm BD for moderated infection and TDS for severe
infection
 For life threatening→ 2gm TDS
 For renal dose→ dose halved.
 Child→ neonates→ 50mg/kg BD or TDS

64. Nursing Mgmt.
 Discontinue other iv during cefotaxim
 Don’t mix with other drugs especially with
aminoglycosides→ give separately
 IM→ deeply in Muscle
 When High dose like 2gm→ give alternate site
 Give mixing with 10 ml sterile water for injection and
shake well
 Administer slowly→ 3-5 mins
 If particle present or discoloration→ don’t administer
 Record I/O , if decrease→ Infrom ASAP, and diarrohea
 Avoid with alcohol→ disulfiram type reaction

65. Ceftriaxone
 Active against b-lactamase producing bacteria
 IV use only no oral
 Streptococci Pneumoniae, Staphylococcus aureus, H. Influenza para
influenza, Klebsiella, E coli, Proteus Mirabilis, S. pyogenes,
Enterobacter, pseudomonas
Indications
• LRTI, Skin infections
• Uncomplicated cerival/Urethral and rectal gonorrhea
• Bacterial septicemia
• Bone and joint infections
• Intraabdominal infections
• Surgical prohylaxis
• Meningitis

66. Preparations
 Ceftriaxone sodium injections: 250mg, 500mg, 1gm,
2gm in vail
 Dose
 Adult→1-2 gm single dose or BD
 Child→ 100mg/kg day not exceed 4gm daily , BD or OD
 Preoperative→1-2 gm single dose half an hour before
surgery

67. Nursing managements
 Same as before

68. Fourth Generation
 modified form of third generation
 Effective against Styph and strep bacteria
 Extended spectrum

69. Cefepime
 Gram negative and positive spectrum
 Including those resistant to other b-lactam
antibiotics
 injections powder
 250,500mg,1,2gm
Indications
• Uncomplicated UTIs
• Skin infection by staphylococcus aureus or pyogenes
• Moderate to severe pneumonia
• Complicated intraabdominal infection due to E-coli,
streptococci, Enterobacter species
• Mono therapy for empiric treatment for Febrile
neutropenia