Pharm antibiotics Part 1 Flashcards
Antibiotics that taget the cell wall and membrane?
- Beta Lactams
* Pen, Ceph, Carb, Mono - Glycopeptides
* Vancomycin - Cyclic lipopeptide
* Daptomycin
types of beta lactams
- Penicillins
- Cephalosporins
- Carbapenems
- Monobactams
Fxn of beta lactam ab
ALL HAVE BETA LACTAM RING
Fxn: inhibit bacterial cell wall synth
Penicillin fxn
inhibit cell wall synthesis
structural analogs of PBP binding site- PBP enzyme that facilitates cross linking and stability
Penicillin subgroups
- Natural penicillins (Narrow spectrum)
- Aminopenicillins (broad)
- Penicillinase resistant penicillins
- Anti-pseudomonal penicillins (broad)
- Penicillin/Beta lactamase inhibitors
Categorizes of penicillins
- Narrow spectrum penicillins
Natural penicillins= PENICILLIN V AND PENICILLIN G - Broad spectrum penicillins
Amino penicillins-> AMOXICILLIN AND AMPICILLIN
Amino w/beta lactamase inhib-> AMOXICILLIN/CLAVULANATE, AMPICILLIN/SULBACTAM
Antipseudomonal penicillin-> PIPERCILLIN/TAZOBACTAM
Natural Penicillins
ALL NARROW SPEC
1.PENICILLIN V-> greatest non bLactamase producing Gram positive ONLY SOME GRAM - FOR NEISSERIA
low systemic levels
2. PENICILLIN G->greatest non bLactamase producing Gram positive ONLY SOME
* Procaine penicillin G-> rapid acting
* Benzathine Penicillin G->long acting RHEUMATIC FEVER PROPHYLAXIS
* Combined repository (CR)-> combo of both
Rheumatic Fever prophylaxis + duration
Prophylaxis: Benzathine Penicillin G once a month-> for 5 years or till 21-> life long if valvular disease
Duration:
RF with Carditis + Residual heart disease= 10 yrs or 40 yo (which ever is longer)
RF with carditis NO residual= 10 yrs or 21 yo
RF w/out carditis= 5 yrs or until 21 yo
Treponema pallidum info and tx
TP= SYPHILIS (primary, secondary, tertiary)
Testing: Rapid plasma regain (RPR), Flouro trep ab absorp (FTA)
TX: NO KNOWN PCN RESISTANCE= Benzathine PCN for each
has neurosymptoms= Aquaeous Crystalline Penicillin G
Neisseria Meningitidis
Meningococcus
MOA: Gram Negative with endotoxin liberated from cell wall
TX:* High dose Penicillin G*
Empirically: if unsure use Ceftriaxone
Secondary contacts: rifampin or Ceftriaxone if prego
Vacc: Menactra and Bexero
Presentations: sudden fever, headache, stiff neck, N/V, sens to light
Children: inactivity, irritability, vomiting, poor reflexes
Penicillinase resistant penicillins
Anti-staphylococcal Penicillins
1.Oxacillin - for serious staph- endocarditis
2.Nafcillin- for serious staph- endocarditis
3.Dicloxacillin- skin and soft tissue infections- mild/mod
* Penicillinase producing staphylococci and streptococci
NOT MRSA
MRSA
NOT bETA LACTIMASE ISSUE
MUTATION W/ PENICILLIN BINDING PROTEIN
Tx: Vancomycin, Daptomycin
Methicillin Resistant Staphylococcus Aureus- specific to Staph
E
S
K
A
P
E
BUGS CAN BE HARD TO TREAT
E- Enteroccoccus faecium or E. coli idk
S- Staphylococcus aureus
K-Klebsiella pneumoniae
A- Acinetobacter baumannii
P-Pseudomonas aeruginosa
E-Enterobacter supp.
Impetigo
Cause: Staphylococcus Aureus or Streptococcus pyogenes
Tx depends on number of lesions: TRY TO COVER FOR BOTH BUGS
* Dicloxacillin
* Cephalexin
* narrow spec pen or ceph
Amino penicillins
- Amoxicillin- better oral than amp-> AOM, Lower resp tract inf-> PREFERRED FOR PNEUMOCOCCI
- Ampicillin-> h. pylori-> group B step sepsis in Neonates
Overall: effective againts GRAM + AND GRAM - BUT NOT PENICILLINASE RESISTANT
Aminopenicillin/Beta lactamase inhib
- Amoxicillin/Clavulanate-> COVER GRAM NEG -> ACUTE BACTERIAL SINUSITIS
- Ampicillin/Sulbactam-> PROPHYLAXIS FOR POST OPP INF IN APPENDICITIS
Streptococcus Pneumoniae
Pneumococcus
Gram + diplocci
diseases involved:
* Pneumonia-> Amox
* AOM-> Amox
* Acute bacterial sinusitis-> Augmentin
* Meningitis-> Penicillin G
Antipseudomonal Penicillin
4th gen-> Ureidopenicillin
Piperacillin/Tazobactam
* piper only combined with tazo
* GRAM + COVERAGE WITH PIPER
* GRAM NEG-> pseudomonas, E. Coli, Klebsiella
Indications: PNA- pulm nodular amyloidosis, appendicitis or peritonitis, skin infections
Range from narrow to broad
General points with penicillin: MOA
drug resistance
PAPI
4 basic mech
1. Beta lactamase- MC- penicillinase
2. Alteration of PBPs- methicillin resistance- altered pbps
3. Impaired penetration-> Gram Neg only due to impermeable outer mem of cell wall- beta lactamase can enter Gram Neg via porins
4. Active pumping- efflux pump in gram neg
DRUG RESISTANCE
Beta lactamases
100s of them
- Produced by: staphylococcus aureus, H. flu, Escherichia coli
- Extended spectrum B lactamases: AmpC B-lactamase PRODUCED BY PSEUDOMONAS AERUGINOSA AND ENTERO-> HYDROLYZES CEPHALO AND PENICILL
- Carbapenems->mostly res to penicillinases and cephlasporinases-> can hydrolyze metallo-beta lactamases and carbapenemases
typically prefer penicillins to ceph
Pharmacokinetics for Penicillins
- Oral Pen (not amox) = 1-2 hours after eating-> amox doesnt matter
- Serum conc rapidly equilibrate to most tissues EXCEPT EYE, PROSTATE, CNS
- Rapidly exreted by kidneys-> tubular secretions
* Nafcillin = exc hepatic
* Oxacillin, cloxacillin dicloxacillin- renal/hepatic
Pharmacokinetics for Penicillins
- Oral Pen (not amox) = 1-2 hours after eating-> amox doesnt matter
- Serum conc rapidly equilibrate to most tissues EXCEPT EYE, PROSTATE, CNS
- Rapidly exreted by kidneys-> tubular secretions
* Nafcillin = exc hepatic
* Oxacillin, cloxacillin dicloxacillin- renal/hepatic
AE Penicillins
- very safe
- non specific maculopapular rashes
- GI upset in large doses= N/V, Diarr
- Seizures in renal failure= high dose
- TYPE 1 HYPERSENS IS MOST SERIOUS
- Specific:
- Nafcillin= NEUTROPENIA
- Oxacillin, Nafcillin- hepatitis
- Clavulanate- GI symp elderly, hepatitis, cholestasis
Parenteral Penicillins AE
aqueous
Hemolytic anemia
leukopenia
thrombocytopenia/neutropenia
neuropathy
nephropathy
Toxic epidermal necrolysis (TEN)
True Type 1 Hypersensitivity reactions= IgE mediated
Pruritis, Urticaria, Angioedema
N/V, flushing, wheezing, hypotension, anaphylaxis