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Medicine 2A
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Drugs against pathogenic microorganisms
without affecting the host cell
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Spectrum of bacterial activity
Narrow: (Selective, gm + or gm -)
PCN
Aminoglycoside
Macrolides
Broad: (All)
Chloramphenicol
Tetracycline
Quinolone
Effect on Microorganisms
Cidal: Kills pathogenic microorganism
Static: Inhibits growth and multiplication of pathogenic microorganism
Examples:
Vermicidal – Kills the intestinal border
Vermifuge – paralyze the parasite
Source
From living source - Antibiotics
Non living source – Chemotherapetic agents (Sulfur, INH, minerals)
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1. Interference with wall synthesis
2. Altering the permeability of the cell membrane
3. Interference with CHON synthesis
4. Interference with nucleic acid and metabolism
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Bacitracin
Cephalosporin – A B lactam antibiotic
Cycloserine
Penicillin – A B lactam antibiotic
Resticetin
Vancomycin – Not an aminoglycoside
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Amphoterecin B – anti fungal
Colistin
Imidazole – anti fungal
Nystatin
Polymyxin
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Aminoglycoside
Chloramphenicol – original
Bactericidal / static to a few organisms
Lincomycin (Clindamycin) – for anaerobic
microorganisms
Macrolides (Thromycin)
Original: Erythromycin
Static, but with max. dose can be cidal
Latest: Claricid (Expensive cidal drug)
Claricin: SARS
Tetracycyline - static
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Chloramphenicol
Lincomycin Act on 50s sub unit of bacterial
ribosomes
Macrolides
Aminoglycoside
Act on 30s sub unit of bacterial
Tetracycline ribosomes
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Clofazimine - cidal
Griseofulvin
Metronidazole – cidal, anerobic
Nalidixic acid
Novobiocin
Pyrimethamine
Quinolone – cidal, acts on DNA gyrase enzyme
Rifampin – RNA acting, cidal, anti TB, meningococcemia
prophylactic agent
Sulfonamides – a chemotherapeutic agent
Sulfamethoxazole + Trimethoprim = Cidal effect
Sulfadoxine + Pyrimethamine (Fancidar) = For malaria, cidal
Trimethoprim
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Identify the causative organism
Choose the best, the most appropriate drug use
if only when necessary
Consider the nature of illness and health status
of patient
Given an adequate dose so that blood level
shall either be cidal or static
Evaluate the clinical response and maintain
blood level for sometime even after s/sx have
disappeared
Have an adequate knowledge of the drug to
use
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To provide broad coverage (In mixed bacterial
infections)
For initial (Blind) therapy when patient is
seriously ill and results of culture are pending
To provide synergism when organisms are not
eradicated with any single agent
To prevent the emergence of resistance – Multi
drug therapy
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Cidal + Static = Antagonism
1+1 = 0
Cidal acts on rapidly multiplying bacteria while
static prevents multiplication
Static + Static = Additive or same
1+1 = 1
Cidal + Cidal = Synergism
1+1=3
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Microorganisms produce enzymes that destroy
the active drug
Microorganism develop and altered enzyme
that can still perform its metabolic function but
less affected by the drugs
Microorganism changes their permeability to
the drug
Microorganism develop an altered structural
target for the drug
Microorganism develop and altered pathway
that bypasses the reaction inhibited by the drug
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MIC (Minimum Inhibitory Concentration) –
Lowest concentration of drug that inhibits visible
growth after an overnight concentration
MBC (Minimum bactericidal concentration) –
Lowest concentration of drug that kills at least
99.9% of the original bacterial inoculum
Bacteriostatic – MBC > MIC
Bactericidal – MBC = MIC
PAE (Post antibiotic effect) – Time period after an
exposure to and removal of an antimicrobial agent
during which inhibition of bacterial growth 14
Inhibits Nucleic Acid Synthesis (Quinolone)
Inhibitors of CHON synthesis
(Aminoglycosides)
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Natural Penicillin
Penicillinase resistant
Aminopenicillins
Extended spectrum
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Penicillin V (Phenoxymethyl Penicillin)
Narrow spectrum
Acid stable
Penicillinase sensitive
Give PO since
Penicillin G (Benzylpenicillin)
Narrow spectrum
Acid labile (Sensitive to HCl)
Penicillinase sensitive
Parenteral (IM, IV, intrathecal)
Vial
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Methcillin (Staphcilin)
Acid labile with narrow spectrum
Isoxazolyl
Drugs:
Cloxacillin (Tegopen)
Dicloxacillin
Flucloxacillin – A staphlotoxin, can also be parenteral / capsule
Oxacillin (Bactocill)
Narrow spectrum, acid stable, Highly protein bound:
90-97% (High protein bound = Reduced frequent
administration)
Nafcillin (Uripin)
Penicillinase resistant
Narrow spectrum, poorly absorbed 88% protein bound
only 18
Drugs
Ampicillin
The parent compound
Less absorbed
Amoxicillin – q8o, most widely used
Better penetration even with purulent sputum, can be taken with
food, and also parenteral
Bacampicillin – a prodrug in the liver
Epicillin
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Due to penicilloic acid – antigenic substance
from penicillin, common in expired products
There is a release of Ag-Ab reaction
Drug Organism
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Type Incidence Ab Time after
PCN
exposure
Immediate 0.02-0.2% IgE 0-30 mins
(Anaphylactic)
R—C—NH— CH – CH C—CH3
B A
O=C N CH—COOH
D C
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A = Thiazolidine ring
B = B lactam ring
(B lactamase enzyme, destruction site by
penicillinase, cephalosporins)
C = Site of salt formation
D = Site of penicillinase action
R = Side chain
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Drug Preparation Duration
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S
H2N—CH—HC CH2 5 O
2
6 C N C—CH2—O—C
3
O C CH3
COOH
4
#1 and #7 I cannot find
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1 = Dihydrothiazine
2 = B lactam
3 = Site of action of Cephalosporins
4 = Site of salt action
5 and 6 = Site of substitution
7 = Aminocephalosporanic acid
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1st generation drugs
Cefa: LZ
loridine
zoline
Cepha: DLLP
drine
lexin
lothin
pirin
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2nd generation: AAAMOOOOOU
Cef:
aclor
amandole
amezole
minox
onicid
oramide
otetan
otiam
oxitine
uroxime
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3rd generation DIOOOTTTT
Cef:
diner
ixime
odizime
operazone
otaxime
tazidime
tibuten
tizoxime
triaxone
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Fourth generation
Drugs
Cefditoren
Cefepime
Cefpirome
Has more anaerobic activity
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1st gen 2nd gen 3rd gen 4th gen
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Suspected bacteremia (Most likely the gm --)
especially in debilitated and
immunosuppressed patients. Usually given
with an aminoglycosides
Surgical prophylaxis: Given 2-6hrs before and
12-24hrs after a surgical procedure having
more than 5% risk of infection
Mixed infections especially those including
anaerobes involving chest, abdomen, or pelvis
Penicillinase producing N. gonorrhea
Gm (--) rod bacterial meningitis – 3rd gen is
DOC 34
Monobactam
Aztreonam (Azactam)
Active against Gm (--) aerobes only
No activity against gm (+) organisms and anaerobes
Ex:
E. coli
K. pneumoniae
H. influenza
N. meningitides
N. gonorrhea
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Carbapenens
Imipenem (Primaxin) – Widest spectrum B lactam
antibiotic
Cilastatin – Given in combination with imipenem
A potent selective enzyme inhibitor
Ensures urinary antibiotic concentration
Nephroprotective effect
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- Drugs in combination of PCN and B lactamase
inhibitors
- Drugs:
1. Clavulanic acid
From Strep. clavuligerus
2. Sulbactam
1. Semi synthetic copound derived from 6-APA
2. By forming a complex with the B-lactamase, they
render the enzyme inactive so that a B lactam
antibiotic can destroy the organism
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Amoxicillin + Clavulanic acid (Augmentin) =
PO
Ticarcillin + Clavulanic acid (Timentin) = IV
For gm (--)
Ampicillin + Sulbactam (Uripin) = IV
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THE END
God bless you
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