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Dr. Lokesh
Garg
M.B.B.S. M.D.
 One of the most commonly used group of drugs.
 A medical doctor has to know the definite clinical pharmacology
of antibiotics, how to select & use them rationally.
- Avoid adverse effects on the patient
- Avoid emergence of antibiotic resistance
- Avoid unnecessary increases in the cost of health care
 Definition
Antibiotics are substances that kill or inhibit the growth
of micro-organisms.
 Bacteriostatic
Bactericidal
Based on their mechanism of
action, antibiotics can be divided
into the following classes:
 Inhibitors of Cell Wall synthesis
 Inhibitors of Protein synthesis
 Inhibitors of Nucleic Acid synthesis
This class includes:
 Penicillin
 Cephalosporin
 Carbapenems
 Monobactams
 Vancomycin
 Beta lactamase inhibitors
B – lactam
antibiotics
Category Parenteral Agents Oral Agents
Natural Penicillins Penicillin G Penicillin V
Antistaphylococcal
penicillins
Nafcillin, oxacillin Dicloxacillin
Aminopenicillins Ampicillin Amoxicillin and
Ampicillin
Aminopenicillin + β-
lactamase inhibitor
Ampicillin-sulbactam Amoxicillin-
clavulanate
Extended-spectrum
penicillin
Piperacillin, ticaricillin Carbenicillin
Extended-spectrum
penicillin + β-lactamase
inhibitor
Piperacillin-tazobactam,
ticaricillin-clavulanate
THE PENICILLINS
Class Examples Routes of
administration
First generation Cephalexin/cefadroxil
Cefazolin
Oral
i.v.
Second
generation
Cefuroxime
Cefoxitin
Oral/ i.v.
Third generation Cefixime
Ceftriaxone/cefotaxim
Ceftazidime
Oral
i.v.
i.v.
Fourth
generation
Cefipime i.v.
 Adverse Effects
 Allergic reactions: itch, rash,
fever, angioedema, rarely
anaphylactic reaction
 GI upset and diarrhoea
 Interstitial nephritis and
increased renal damage in
combination with
aminoglycosides
Pharmacokinetics
 Bactericidal
 Safe in pregnancy
 Dosage needs to be
reduced in cases of
impaired renal function.
This class includes:-
 Macrolides- erythromycin, clarithromycin, azithromycin
 Lincosamides- clindamycin
 Aminoglycosides- gentamicin, tobramycin, amikacin,
netilmicin,neomycin, streptomycin.
 Tetracyclines- tetracycline, doxycycline,minocycline
 Chloramphenicol
Pharmacokinetics:
 Bacteriostatic
 Dose adjustment in renal
failure is not necessary
Adverse Effects :
 GI upset
 Cholestatic jaundice
 Prolongation of QT interval
(erythromycin)
 Theophylline, oral anticoagulants
cannot be administered
simultaneously
PharmacokineticsPharmacokinetics
 Bectericidal
 Negligible oral absorption
 Dose adjustment is
critical in renal
impairment
Adverse Effects
 Ototoxic (permanent)
Avoid concurrent use of
other ototoxics drugs for eg.
Lasix , minocycline
 Nephrotoxic ( reversible):
use cautiously with other
nephrotoxic drugs
Pharmacokinetics
Bacteriostatic
Best oral absorption in fasting
state
 Adverse Effects
 Contraindicated in renal failure
(except doxycycline and minocycline)
 Nausea, diarrhoea
 Binds to metallic ions in bones and teeth (to
be avoided in children and
in pregnancy)
 Phototoxic skin reactions
This group includesThis group includes ::
 Sulphonamides: Sulfamethoxazole, sulfadoxine
 Trimethoprim
 Quinolones: Ciprofloxacin, levofloxacin, pefloxacin, ofloxacin, norfloxacin,
gatifloxacin, moxifloxacin, sparfloxacin
 Rifampicin
Azoles: This group includes-
 Antibacterial- Metronidazole, secnidazole, tinidazole,
 Antihelminth- Albendazole, Mebendazole, thiabendazole
Pharmacokinetics
 Bactericidal
 Well absorbed orally with
good bioavailability
 Dose reduction necessary in
renal failure
Adverse Effects
 Fatal marrow dysplasia and
haemolysis in G6PD
deficiency
 Skin and mucocutaneous
reactions: Stevens- Johnson
syndrome
 Contraindicated in
pregnancy
Pharmacokinetics
 Bectericidal
 Well absorbed after oral
administration
 Dose adjustment required
in renal impairment
(except moxifloxacin and trovafloxacin)
 These two drugs are
contraindicated in hepatic
Adverse Effects
 GI side effects
 CNS effects such as restlessness,
headache, insomnia, confusion and
seizures in the elderly
 Rare skin reactions
 Should be avoided in pregnancy
 Not routinely recommended for use in
patients under 18 years
of age
Pharmacokinetics
 Almost completely
absorbed after oral
administration (60% after
rectal administration).
Adverse Effects
 Metallic taste
 Severe vomiting if taken with
alcohol (disulfiram like
syndrome )
 CNS: Meningitis, brain abscess etc
 Respiratory: URTI, Pneumonia, Lung abscess, Bronchiectasis
 CVS: Acute rheumatic fever, Infective endocarditis
 GIT and HBS: Cholera, Bacillary dysentery, Enteric fever,
gastroenteritis, peritonitis,liver abscess
 Genitourinary: UTI, pyelonephritis, STDs
 Skin : Cellulitis necrotizing fascitis
 Musculoskeletal: Osteomyelitis, Septic arthritis
 Mycobacterial Infections: Tuberculosis, Leprosy
 Chlamydial Infections
 Systemic Infections: Sepsis syndrome
 62 year old male presents to your clinic with c/o: Cough with
expectoration x 4days
◦ Intermittent fever, measured to 100.8
◦ Chest pain – Rt side
 PMHx
◦ Healthy
o No H/O hospitalization in recent past
o not on any medication
 Drink socially , non smoker
 Exam
VS – temp 100.3, P 92, RR 18, Spo2 - 96% on room air, BP
123/75
HEENT – normal
Neck – normal w/o palpable LN or TMG
Lungs – Bronchial breath sound in I/S , I/A on Rt side, clear at
bases,
CV – normal
Legs – no edema
Case 1
 Community –acquired Pneumonia (CAP)
 Recent onset of
- Fever
- Productive cough
- TLC
- CXR
 Why CAP
- Healthy adult with no H/O hospitalization in recent past
& was not taking any antibiotics
Common Outpatient Bacterial Etiologies
AntibioticsAntibiotics
 Oral macrolide
 Erythromycin
 Azithromycin
 Clarithromycin
This patient’s pneumonia is mild
Previously healthy
No antibiotics in past 3 months
 In patients who are older, have comorbid illnesses
Levofloxacin Moxifloxacin
 In patients treated with antibiotics within the last 90 days.
 Respiratory quinolones
Moxifloxacin
Levofloxacin
Gemifloxacin
or
 B- lactam
Amoxicillin + Clavunate
Cefuroxime
 Beta-lactam + macrolide
Ceftriaxone or cefotaxime
Erythromycin, azithromycin, or clarithromycin
OR
 Fluoroquinolone with antistreptococcal activity
Levofloxacin or moxifloxacin
Trimethoprim/sulfamethoxizole x 3 days
women with risk factors, complicated UTI
Fluoroquinolone x 3 days:
 Ciprofloxacin
 Norfloxacin
 Ofloxacin
Nitrofurantoin x 7 days
 Initial drug selections:
Fluoroquinolones
Ciprofloxacin
Levofloxacin
Cephalosorin

Ceftriaxone

Cefotaxime
+ Amikacin
 57 years male painful rash on his right leg. 5 days
ago he developed a blister on his foot after wearing a
new pair of shoes.
c/o fever with chills
 PMHx – COPD, high cholesterol
Social – stopped tobacco two years ago.
 Exam
 Temp 101.2 otherwise stable , APPP
 Exam unremarkable except for
 Lungs – few inspiratory rales
 Right leg …
 Outpatient Treatment: non-MRSA
Antistaphylococcal penicillin
Dicloxacillin
First-generation cephalosporin

Cephalexin
 Inpatient Treatment: non-MRSA
 Amoxicillin + Clavunate
 Clindamycin is a good alternate with penicillin allergy
 Surgical opinion
 A 43 year old male presents with 10 days of purulent
rhinorrhea, subjective fevers, and facial headaches.
 PMHx – HTN, high cholesterol
 Meds – lisinopril/HCTZ
 FamHx – noncontributory
Exam
 HEENT – VS normal tenderness over right maxillary sinus
 Exam otherwise unremarkable
 Diagnosis?
 Sinusitis
Mild Acute Bacterial Sinusitis (ABS)
Amoxicillin
Amoxicillin/clavulanate
Cefuroxime axetil
Cefpodoxime
Or
antistrep. fluoroquinolones:
Levofloxacin
Moxifloxacin
 Drug option in the case of allergies to penicillin
and cephalosporin with Mild ABS:
◦ Doxycycline
◦ Trimethoprim/sulfamethoxizole
◦ Azithromycin
◦ Clarithromycin
 Drug option in the case of allergies to penicillin and
cephalosporin with Moderate to Severe ABS:
◦ Antipneumococcal fluoroquinolone:
 Levofloxacin
 Moxifloxacin
42 years male with 5 days of progressive diffuse
headache, mildly stiff neck,fever vomiting, confusion.
PMHx – none known
PSHx - none
Exam
 VS: T 100.9, Pulse 96, RR 16, BP 138/82
 Gen: mildly ill appearing
 Mental status: orientation to place & person not time
 HEENT: mild photophobia
 Neck: mild pain with flexion (kernig sign +ve )
 Skin: no rash

 Lab.-
 TLC - 16000
 DLC - N80 L18
 CECT Head - normal study
 CSF - TLC – 412
DLC – N 96 L4
protein – 110mg/dl
suger - 23 mg/dl
 Adults(<55years) and children>3 months old:
 High dose ceftriaxone or cefotaxime
+
 Vancomycin 1gm IV BD
 Adults > 55years of age , patient with alcoholism
or other debilitating illness
 High dose ceftriaxone /cefotaxime
+ Vancomycin 1gm IV BD
+ Ampicillin 2gm/ 4horly
2gm IV BD
Cholera:
Tetracycline 250 mg 6-hourly for 3 days,
Doxycycline 300 mg single dose or Ciprofloxacin 1
g in adults
Bacillary Dysentery:
Ciprofloxacin 500 mg 12-hourly for 3 days
Helicobacter pylori Infection:
Two antibiotics (from amoxicillin, clarithromycin
and metronidazole) for 7 days
Aetiology: Salmonella typhi and Salmonella paratyphi A and B
Ciprofloxacin 500 mg 12-hourly
Ofloxacin 400 mg every 12 hourly
Ceftriaxone 2gm IV BD
Azithromycin 1gm once daily x 5 days
Treatment should be continued for minimum 10 days.
Or
5 days after resolution of fever
 Aetiology (pyogenic): E.coli, various streptococci
(amoebic): Entamoeba histolytica
 Management:
o Pyogenic: Combination of antibiotics e.g3rd gen
cephalosporin, gentamicin and metronidazole
o Amoebic: Metronidazole (800 mg 8-hourly for 10 days)
or tinidazole (2 g daily for 3 days)
Luminal amoebicide-diloxanide furoate (500 mg 8-
hourly for 10 days)
Gastro-Intestinal:

Ancylostoma, Ascaris:
Albendazole 400 mg single dose or Mebendazole 100
mg 12 hourly for 3 days
Tissue parasite:

Filariasis: Caused by Wuchereria bancrofti
 Treatment: Diethylcarbamazine 6 mg/kg body wt.
orally in 3 divided doses for 12 days.
 Avoid tetracycline
 Staining of teeth and bones in babies
 Acute yellow atrophy of lever , pancreatitis in mother
 Avoid sulfa drugs in the third trimester
 May be associated with kernicterus
 Avoid aminoglycosides
 Kidney toxicities
 Can cause foetal ear damage
 Fluoroquinolones
Concerns about cartilage development
 Treat the Mother first and the baby will appreciate it 
 Penicillins and cephalosporins are generally safe in
pregnancy.
 Macrolides are generally safe
- They may increase nausea early on
Is antibiotic necessary
What is the most
appropriate antibiotic
H/O
Allergy
Pregnancy
Renal dysfunction
Liver Disease
Dose/Frequency/Route/Duration
Monitor side effects
Antibiotics basics for clinicians

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Antibiotics basics for clinicians

  • 2.  One of the most commonly used group of drugs.  A medical doctor has to know the definite clinical pharmacology of antibiotics, how to select & use them rationally. - Avoid adverse effects on the patient - Avoid emergence of antibiotic resistance - Avoid unnecessary increases in the cost of health care
  • 3.  Definition Antibiotics are substances that kill or inhibit the growth of micro-organisms.  Bacteriostatic Bactericidal
  • 4. Based on their mechanism of action, antibiotics can be divided into the following classes:  Inhibitors of Cell Wall synthesis  Inhibitors of Protein synthesis  Inhibitors of Nucleic Acid synthesis
  • 5. This class includes:  Penicillin  Cephalosporin  Carbapenems  Monobactams  Vancomycin  Beta lactamase inhibitors B – lactam antibiotics
  • 6. Category Parenteral Agents Oral Agents Natural Penicillins Penicillin G Penicillin V Antistaphylococcal penicillins Nafcillin, oxacillin Dicloxacillin Aminopenicillins Ampicillin Amoxicillin and Ampicillin Aminopenicillin + β- lactamase inhibitor Ampicillin-sulbactam Amoxicillin- clavulanate Extended-spectrum penicillin Piperacillin, ticaricillin Carbenicillin Extended-spectrum penicillin + β-lactamase inhibitor Piperacillin-tazobactam, ticaricillin-clavulanate THE PENICILLINS
  • 7. Class Examples Routes of administration First generation Cephalexin/cefadroxil Cefazolin Oral i.v. Second generation Cefuroxime Cefoxitin Oral/ i.v. Third generation Cefixime Ceftriaxone/cefotaxim Ceftazidime Oral i.v. i.v. Fourth generation Cefipime i.v.
  • 8.  Adverse Effects  Allergic reactions: itch, rash, fever, angioedema, rarely anaphylactic reaction  GI upset and diarrhoea  Interstitial nephritis and increased renal damage in combination with aminoglycosides Pharmacokinetics  Bactericidal  Safe in pregnancy  Dosage needs to be reduced in cases of impaired renal function.
  • 9. This class includes:-  Macrolides- erythromycin, clarithromycin, azithromycin  Lincosamides- clindamycin  Aminoglycosides- gentamicin, tobramycin, amikacin, netilmicin,neomycin, streptomycin.  Tetracyclines- tetracycline, doxycycline,minocycline  Chloramphenicol
  • 10. Pharmacokinetics:  Bacteriostatic  Dose adjustment in renal failure is not necessary Adverse Effects :  GI upset  Cholestatic jaundice  Prolongation of QT interval (erythromycin)  Theophylline, oral anticoagulants cannot be administered simultaneously
  • 11. PharmacokineticsPharmacokinetics  Bectericidal  Negligible oral absorption  Dose adjustment is critical in renal impairment Adverse Effects  Ototoxic (permanent) Avoid concurrent use of other ototoxics drugs for eg. Lasix , minocycline  Nephrotoxic ( reversible): use cautiously with other nephrotoxic drugs
  • 12. Pharmacokinetics Bacteriostatic Best oral absorption in fasting state  Adverse Effects  Contraindicated in renal failure (except doxycycline and minocycline)  Nausea, diarrhoea  Binds to metallic ions in bones and teeth (to be avoided in children and in pregnancy)  Phototoxic skin reactions
  • 13. This group includesThis group includes ::  Sulphonamides: Sulfamethoxazole, sulfadoxine  Trimethoprim  Quinolones: Ciprofloxacin, levofloxacin, pefloxacin, ofloxacin, norfloxacin, gatifloxacin, moxifloxacin, sparfloxacin  Rifampicin Azoles: This group includes-  Antibacterial- Metronidazole, secnidazole, tinidazole,  Antihelminth- Albendazole, Mebendazole, thiabendazole
  • 14. Pharmacokinetics  Bactericidal  Well absorbed orally with good bioavailability  Dose reduction necessary in renal failure Adverse Effects  Fatal marrow dysplasia and haemolysis in G6PD deficiency  Skin and mucocutaneous reactions: Stevens- Johnson syndrome  Contraindicated in pregnancy
  • 15. Pharmacokinetics  Bectericidal  Well absorbed after oral administration  Dose adjustment required in renal impairment (except moxifloxacin and trovafloxacin)  These two drugs are contraindicated in hepatic Adverse Effects  GI side effects  CNS effects such as restlessness, headache, insomnia, confusion and seizures in the elderly  Rare skin reactions  Should be avoided in pregnancy  Not routinely recommended for use in patients under 18 years of age
  • 16. Pharmacokinetics  Almost completely absorbed after oral administration (60% after rectal administration). Adverse Effects  Metallic taste  Severe vomiting if taken with alcohol (disulfiram like syndrome )
  • 17.
  • 18.
  • 19.  CNS: Meningitis, brain abscess etc  Respiratory: URTI, Pneumonia, Lung abscess, Bronchiectasis  CVS: Acute rheumatic fever, Infective endocarditis  GIT and HBS: Cholera, Bacillary dysentery, Enteric fever, gastroenteritis, peritonitis,liver abscess  Genitourinary: UTI, pyelonephritis, STDs  Skin : Cellulitis necrotizing fascitis  Musculoskeletal: Osteomyelitis, Septic arthritis  Mycobacterial Infections: Tuberculosis, Leprosy  Chlamydial Infections  Systemic Infections: Sepsis syndrome
  • 20.
  • 21.  62 year old male presents to your clinic with c/o: Cough with expectoration x 4days ◦ Intermittent fever, measured to 100.8 ◦ Chest pain – Rt side  PMHx ◦ Healthy o No H/O hospitalization in recent past o not on any medication  Drink socially , non smoker
  • 22.  Exam VS – temp 100.3, P 92, RR 18, Spo2 - 96% on room air, BP 123/75 HEENT – normal Neck – normal w/o palpable LN or TMG Lungs – Bronchial breath sound in I/S , I/A on Rt side, clear at bases, CV – normal Legs – no edema
  • 23.
  • 24.
  • 26.  Community –acquired Pneumonia (CAP)  Recent onset of - Fever - Productive cough - TLC - CXR  Why CAP - Healthy adult with no H/O hospitalization in recent past & was not taking any antibiotics
  • 27.
  • 29.
  • 30. AntibioticsAntibiotics  Oral macrolide  Erythromycin  Azithromycin  Clarithromycin This patient’s pneumonia is mild Previously healthy No antibiotics in past 3 months
  • 31.  In patients who are older, have comorbid illnesses Levofloxacin Moxifloxacin  In patients treated with antibiotics within the last 90 days.  Respiratory quinolones Moxifloxacin Levofloxacin Gemifloxacin or  B- lactam Amoxicillin + Clavunate Cefuroxime
  • 32.
  • 33.  Beta-lactam + macrolide Ceftriaxone or cefotaxime Erythromycin, azithromycin, or clarithromycin OR  Fluoroquinolone with antistreptococcal activity Levofloxacin or moxifloxacin
  • 34.
  • 35.
  • 36.
  • 37.
  • 38.
  • 39.
  • 40. Trimethoprim/sulfamethoxizole x 3 days women with risk factors, complicated UTI Fluoroquinolone x 3 days:  Ciprofloxacin  Norfloxacin  Ofloxacin Nitrofurantoin x 7 days
  • 41.  Initial drug selections: Fluoroquinolones Ciprofloxacin Levofloxacin Cephalosorin  Ceftriaxone  Cefotaxime + Amikacin
  • 42.  57 years male painful rash on his right leg. 5 days ago he developed a blister on his foot after wearing a new pair of shoes. c/o fever with chills  PMHx – COPD, high cholesterol Social – stopped tobacco two years ago.
  • 43.  Exam  Temp 101.2 otherwise stable , APPP  Exam unremarkable except for  Lungs – few inspiratory rales  Right leg …
  • 44.
  • 45.
  • 46.
  • 47.  Outpatient Treatment: non-MRSA Antistaphylococcal penicillin Dicloxacillin First-generation cephalosporin  Cephalexin  Inpatient Treatment: non-MRSA  Amoxicillin + Clavunate  Clindamycin is a good alternate with penicillin allergy  Surgical opinion
  • 48.  A 43 year old male presents with 10 days of purulent rhinorrhea, subjective fevers, and facial headaches.  PMHx – HTN, high cholesterol  Meds – lisinopril/HCTZ  FamHx – noncontributory
  • 49. Exam  HEENT – VS normal tenderness over right maxillary sinus  Exam otherwise unremarkable  Diagnosis?  Sinusitis
  • 50.
  • 51. Mild Acute Bacterial Sinusitis (ABS) Amoxicillin Amoxicillin/clavulanate Cefuroxime axetil Cefpodoxime Or antistrep. fluoroquinolones: Levofloxacin Moxifloxacin
  • 52.  Drug option in the case of allergies to penicillin and cephalosporin with Mild ABS: ◦ Doxycycline ◦ Trimethoprim/sulfamethoxizole ◦ Azithromycin ◦ Clarithromycin
  • 53.  Drug option in the case of allergies to penicillin and cephalosporin with Moderate to Severe ABS: ◦ Antipneumococcal fluoroquinolone:  Levofloxacin  Moxifloxacin
  • 54.
  • 55. 42 years male with 5 days of progressive diffuse headache, mildly stiff neck,fever vomiting, confusion. PMHx – none known PSHx - none
  • 56. Exam  VS: T 100.9, Pulse 96, RR 16, BP 138/82  Gen: mildly ill appearing  Mental status: orientation to place & person not time  HEENT: mild photophobia  Neck: mild pain with flexion (kernig sign +ve )  Skin: no rash 
  • 57.  Lab.-  TLC - 16000  DLC - N80 L18  CECT Head - normal study  CSF - TLC – 412 DLC – N 96 L4 protein – 110mg/dl suger - 23 mg/dl
  • 58.
  • 59.
  • 60.  Adults(<55years) and children>3 months old:  High dose ceftriaxone or cefotaxime +  Vancomycin 1gm IV BD  Adults > 55years of age , patient with alcoholism or other debilitating illness  High dose ceftriaxone /cefotaxime + Vancomycin 1gm IV BD + Ampicillin 2gm/ 4horly 2gm IV BD
  • 61. Cholera: Tetracycline 250 mg 6-hourly for 3 days, Doxycycline 300 mg single dose or Ciprofloxacin 1 g in adults Bacillary Dysentery: Ciprofloxacin 500 mg 12-hourly for 3 days Helicobacter pylori Infection: Two antibiotics (from amoxicillin, clarithromycin and metronidazole) for 7 days
  • 62. Aetiology: Salmonella typhi and Salmonella paratyphi A and B Ciprofloxacin 500 mg 12-hourly Ofloxacin 400 mg every 12 hourly Ceftriaxone 2gm IV BD Azithromycin 1gm once daily x 5 days Treatment should be continued for minimum 10 days. Or 5 days after resolution of fever
  • 63.  Aetiology (pyogenic): E.coli, various streptococci (amoebic): Entamoeba histolytica  Management: o Pyogenic: Combination of antibiotics e.g3rd gen cephalosporin, gentamicin and metronidazole o Amoebic: Metronidazole (800 mg 8-hourly for 10 days) or tinidazole (2 g daily for 3 days) Luminal amoebicide-diloxanide furoate (500 mg 8- hourly for 10 days)
  • 64. Gastro-Intestinal:  Ancylostoma, Ascaris: Albendazole 400 mg single dose or Mebendazole 100 mg 12 hourly for 3 days Tissue parasite:  Filariasis: Caused by Wuchereria bancrofti  Treatment: Diethylcarbamazine 6 mg/kg body wt. orally in 3 divided doses for 12 days.
  • 65.  Avoid tetracycline  Staining of teeth and bones in babies  Acute yellow atrophy of lever , pancreatitis in mother  Avoid sulfa drugs in the third trimester  May be associated with kernicterus  Avoid aminoglycosides  Kidney toxicities  Can cause foetal ear damage  Fluoroquinolones Concerns about cartilage development
  • 66.  Treat the Mother first and the baby will appreciate it   Penicillins and cephalosporins are generally safe in pregnancy.  Macrolides are generally safe - They may increase nausea early on
  • 67. Is antibiotic necessary What is the most appropriate antibiotic H/O Allergy Pregnancy Renal dysfunction Liver Disease Dose/Frequency/Route/Duration Monitor side effects