Summary Pharmacology Summaries - A comprehensive look at Antibiotics, specifically "Cell Wall synthesis Inhibitors", "Nucleic Acid synthesis Inhibitors" and "Protein synthesis inhibitors".
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Course
Pharmacology (SCMD)
Institution
University Of The Witwatersrand (wits)
Pharmacology Summaries - A comprehensive look at Antibiotics, specifically:
"Cell Wall synthesis Inhibitors",
"Nucleic Acid synthesis Inhibitors" and
"Protein synthesis inhibitors".
It includes 3 pages of mind map summaries, one for each drug group to help you memorise, followed by table summar...
Agents affecting bacterial cell wall synthesis
B-lactamase Inhibitors
N.B * these are not antibiotics
B-lactams Other
clavulanic acid (co-amoxiclav)
Other peptides fosfomycin
Penicillins transpeptidase Oral, N.B
cephalosporin
before food
*inactivated by B-lactamase s inhibitors
*transpeptidase
ANTIPSEUDOMONAL PENICILLINS cataylses pentaglycine
bridge formation
Bacitracin Glycopeptide
Narrow spectrum Wider spectrum Piperacillin + s
tazobactam (β-
lactamase
inhibitor) IV
carbapenams monbactams
B-lactamase sens. B-lactamase res. B-lactamase sens. B-lactamase res. Imipenem + cilastatin (enzyme Aztreonam
inhibitor that blocks renal
metabolism) *can use in pen
Cloxacillin AMINOPENICILLIN amoxicillin + * not an antibiotic or B-lactamase I allergic patients Vancomycin
Flucloxacillin 1st line agents clavulanic acid (co- oral teicoplanin
Natural penicllins
amoxiclav) Meropenem *can use in pen
Oral, IM, IV Amoxicillin
Ampicillin allergic patients IV infusion once
ampicillin + Ertapenem → narrower spectrum
oral Oral, IM, IV daily (longer t1/2
cloxacillin in
combination IV than vancomycin)
oral
Penicillin G Penicillin V
Benzylpenicillin Phenoxymethylpenicillin
Slow IV
IV/IM (depot) Oral infusion
(empty
stomach)
4th generation
1st generation
2nd generation 3rd generation IV, IM
Cefepime,
Cefalexin,
Cefpirome
Cefadroxil Oral, IV, IM Cefuroxime, Cefotaxime, IV
Ceftriaxone Cefamandole, Ceftriaxone
oral IV, IM Cefoxitin
IV, IM
More spectrum, oral to more IV, IM
, Antibacterial Drugs - Inhibitors of cell wall synthesis
β-lactams – have a β-lactam ring (4 membered ring); thialzolidine ring = 6 membered.
Penicillin’s Name Spectrum M.O’s MOA Resistance Pharma-kinetics Side-effects Drug-interactions C/I and
affected Cautions
Natural Penicillin G Narrow. Gram +’ve cocci Bactericidal 1.Absence of Extend the action of Hypersensitivity Probenecid 1.Elderly
penicillin’s Benzylpenicillin + anaerobes, Cell wall synthesis a cell wall & penicillin G: reactions
Prophylaxis of in the bacterium is metabolically •Probenecid Must not combine 2.Neonates
β-Lactamase sensitive
streptococcal infxns, Enterococci less disrupted. inactive (competes with pen G Low WBC count aminoglycosides (extended dose
rheumatic fever recurrence, susceptible (add Trans-peptidase bacteria for excretion in (Neutropenia & and penicillin’s in intervals)
surgical/dental procedures aminoglycoside) enzyme (catalyses kidneys). agranulocytosis same syringe or
on patients with valvular . penta-glycine 2.Permeabilit •Depot formulation described) infusion, or same IV (cautioned not
heart disease. bridge formation) y barrier (e.g. via IM injection line C/I - need good
Initial therapy for SERIOUS is inhibited Gram neg. (procaine and Reduce efficacy (inactivate each kidney function)
infxns + syphilis (depot Causing cell wall to bacteria) benzathine) of combined oral other)
prep). rupture. contraceptive 3.C/I when
Penicillin V Narrow 3.β-lactamase •Inflammation - ↑ (kills gut flora Allopuranol – anti- allergic
LESS SERIOUS infections - Acid labile production Penetration into CSF that normally gout (skin rash).
Phenoxymethyl
streptococcal tonsillitis or (unstable). (penicillinase) and synovial fluid make the pill 4.Flucloxacillin –
penicillin pharyngitis. Do not cross BBB more Combined oral porphyria
Follow up treatment after Penicillin V is 2-4 ** won’t work easily. hydrophobic – contraceptive pill.
serious infection. times less active. in B- pill not 5. Patients with
β-Lactamase resistant Cloxacillin Narrow > 90% lactamase Small amount of reabsorbed) cardiac
Not as potent. Staphylococcus resistant metabolism, greater disease/renal
Flucloxacillin Treatment of mild β-lactamase aureus isolates. penicillins. amount excreted Possible disease can lead
positive staphylococcal unchanged in the bleeding → ↓ to fluid
infections. urine. platelet retention and
Aminopenicllins Amoxicillin Extended spectrum Gram pos. aggregation. hypokalaemia.
β-lactamase sensitive penicillins. ↑ activity Short t1/2. (dep. On arrhythmias.
against patient). Cross-sensitivity,
(resistance develops Prophylaxis to prevent enterococci and if allergic to 1
against it much infective endocarditis Listeria. pen allergic to all
easier) Gram neg. of them.
(easier
1st line agents. penetration due Neurotoxic
to hydrophilic (seizures) at high
amino side- doses.
chain), resistant
organisms. Broad spectrum
Ampicillin Extended spectrum Gram pos. kill a lot of
penicillins. bacteria + H. bacteria can
influenza
, β-Lactamase resistant amoxicillin + Extended spectrum cause
1st line agents. clavulanic acid penicillins. superinfections
Makes amoxillin resistant (candida and
(coamoxiclav) to breakdown by enzyme. pseudomembran
ampicillin + Additive effect. ous colitis –
Cover those that use B- clostridium
cloxacillin in
lactamase and those that difficle – toxin
combination dont release that
Antipseudomonal Piperacillin + Gram neg. bacteria shows Pseudomonas causes
high resistance aeruginosa inflammation in
penicillin tazobactam
the colon –
(βlactamase Acts synergistically with leading to
inhibitor) aminoglycosides for empiric bloody diarrhoea
treatment of serious – occurs mainly
Pseudomonas infections. with ampicillin –
WHY? Ampicillin
not as well
absorbed as
amoxicillin).
Amoxicillin:
If patient suffers
from glandular
fever or
(The Epstein–
Barr virus (EBV),
formally called
Human
gammaherpesvir
us 4) – increased
risk of a rash.
[not an allergic
reaction]
Pen G and
piperacillin
(increased risk of
bleeding). –
potent IV –
decreases
platelet
aggregation.
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