NR566-Advanced Pharmacology for Care of
the Family.
β-lactam antibiotic MOA - ANS >> All antibiotics in class share the same mechanism of action: disruption
v v v v v v v v v v v v v v v v
of the bacterial cell wall.
v v v v v
Inhibition of cell wall synthesis
v v v v
Empiric Therapy - ANS >> start treatment without cultures or prior to receiving the results of a culture
v v v v v v v v v v v v v v v v v
immediate empiric antibiotics - ANS >> Critically ill patients receive (Fill in the Answer) after the first set
v v v v v v v v v v v v v v v v v
vof cultures obtained; do not wait for results.
v v v v v v v
Bactericidal antibiotics - ANS >> Directly kill bacteria: Agents include aminoglycosides, beta-lactams,
v v v v v v v v v v v
fluoroquinolones, metronidazole, most antimycobacterial agents, streptogramins, and vancomycin.
v v v v v v v v
preferred for immunocompromised patients such as those with diabetes, HIV, or cancer and for those
v v v v v v v v v v v v v v
who have overwhelming infections
v v v v
Bacteriostatic agents - ANS >> inhibit bacterial proliferation while the host's immune system does the
v v v v v v v v v v v v v v
killing. Agents include clindamycin, macrolides, sulfonamides, and tetracyclines
v v v v v v v v
β-lactam Antibiotics - ANS >> Penicillins, Cephalosporins, Carbapenems, Monobactams
v v v v v v v v
Penicillins MOA - ANS >> Weaken bacterial cell wall by two actions:
v v v v v v v v v v v v
(1) inhibition of transpeptidases
v v v
(2) disinhibition (activation) of autolysins.
v v v v
PBPs (Penicillin Binding Proteins) - ANS >> Transpeptidases, Autolysins, and other bacterial enzymes are
v v v v v v v v v v v v v
collectively named as because antibiotic class must bind to them to produce antibacterial effects.
v v v v v v v v v v v v v v
gram-positive bacteria - ANS >> two layers: the cytoplasmic membrane and a relatively thick cell wall;
v v v v v v v v v v v v v v v
penicillins are generally very active against these organisms.
v v v v v v v v
,gram-negative bacteria - ANS >> three layers: the cytoplasmic membrane, a relatively thin cell wall, and
v v v v v v v v v v v v v v v
an additional outer membrane; only certain penicillins (e.g., ampicillin) are able to cross and reach
v v v v v v v v v v v v v v v
penicillin binding proteins (PBPs)
v v v v
Four Major Groups of Penicillins - ANS >> (1) narrow-spectrum penicillins that are penicillinase sensitive
v v v v v v v v v v v v v v
(2) narrow-spectrum penicillins that are penicillinase resistant (antistaphylococcal penicillins)
v v v v v v v v
(3) broad-spectrum penicillins (aminopenicillins)
v v v
(4) extended-spectrum penicillins (antipseudomonal penicillins).
v v v v
narrow-spectrum penicillins: Penicillinase sensitive penicillins - ANS >> Penicillin G, Penicillin V
v v v v v v v v v v v
narrow-spectrum penicillinase sensitive susceptible pathogens - ANS >> Streptococci, Neisseria,
v v v v v v v v v
anaerobes
v
very narrow antimicrobial spectrum and are used only against penicillinase-producing strains of
v v v v v v v v v v v
staphylococci (S. aureus and S. epidermidis). - ANS >> narrow-spectrum penicillins: penicillinase
v v v v v v v v v v v v
resistant penicillins
v v
narrow-spectrum penicillins: penicillinase resistant penicillins - ANS >> Nafcillin, Oxacillin, Dicloxacillin
v v v v v v v v v v
narrow-spectrum- penicillinase resistant susceptible pathogens - ANS >> S. Aureus, S. Epidermidis
v v v v v v v v v v v
Drugs of choice for most staphylococcal infections - ANS >> penicillinase-resistant penicillins (Nafcillin,
v v v v v v v v v v v v
Oxacillin, Dicloxacillin)
v v
Broad spectrum Penicillin: Aminopenicillins - ANS >> Ampicillin, Amoxicillin
v v v v v v v v
Broad spectrum Aminopenicillin susceptible pathogens - ANS >> Haemophilus influenzae, Escherichia
v v v v v v v v v v
coli, Proteus mirabilis, enterococci, Neisseria gonorrhoeae
v v v v v v
Extended spectrum penicillins (antipseudomonal penicillin) - ANS >> Piperacillin
v v v v v v v v
Has the same antimicrobial spectrum as penicillin G, plus increased activity against certain gram-
v v v v v v v v v v v v v
negative bacilli, including Haemophilus influenzae, Escherichia coli, and Salmonella and Shigella - ANS
v v v v v v v v v v v v
>> Broad spectrum Penicillin: Aminopenicillins
v v v v v
First line for acute otitis media and sinusitis - ANS >> Amoxicillin
v v v v v v v v v v v
,Extended spectrum penicillins suceptible pathogens - ANS >> Haemophilus influenzae, Escherichia coli,
v v v v v v v v v v v
Proteus mirabilis, enterococci, Neisseria gonorrhoeae, pseudomonas, enterobactor, klebsiella
v v v v v v v v
Principle pathogenic target of Piperacillin - ANS >> Pseudomonas aeruginosa
v v v v v v v v v
beta-lactamase inhibitors to broaden penicillin spectrum - ANS >> clavulanate, sulbactam, tazobactam
v v v v v v v v v v v
Penicillin/Beta-Lactamase Combinations - ANS >> Ampicillin/sulbactam (Unasyn) v v v v v v v
Amoxicillin/clavulanate (Augmentin) v
Piperacillin/tazobactam (Zosyn) v
MRSA Drug of Choice - ANS >> Vancomycin
v v v v v v v
Most Important AE of Penicillins - ANS >> Hypersensitivity Reaction
v v v v v v v v v
Drug of choice when history of anaphylaxis or some other severe allergic reaction to penicillins - ANS >>
v v v v v v v v v v v v v v v v v
Avoid cephalosporin;
v v v
Vancomycin, erythromycin, and clindamycin are effective and safe alternatives for patients with
v v v v v v v v v v v
penicillin allergy.
v v
Common drug used to treat bacterial infections in children. - ANS >> Penicillins
v v v v v v v v v v v v
First line treatment for infection following animal or human bites - ANS >> Amoxicillin/clavulanate
v v v v v v v v v v v v v
(Augmentin)
v
Medication common for streptococcal pharyngitis - ANS >> Penicillin
v v v v v v v v
Penicillin Risk in Pregnancy - ANS >> evidence suggests there is no second or third trimester fetal risk
v v v v v v v v v v v v v v v v v
Penicillin Risk in Infants - ANS >> Used safely in infants with bacterial infections, including syphilis,
v v v v v v v v v v v v v v v
meningitis, and group A streptococcus.
v v v v v
Amoxicillin - ANS >> Safe use during breastfeeding
v v v v v v v
Penicillin Use in Older Adults - ANS >> Doses should be adjusted in older adults with renal dysfunction.
v v v v v v v v v v v v v v v v v
Cephalosporins - ANS >> β-lactam antibiotics similar in structure and actions to the penicillins.
v v v v v v v v v v v v v v
Are bactericidal, often resistant to β-lactamases, and active against a broad spectrum of pathogens.
v v v v v v v v v v v v v
Useful alternative with mild penicillin allergy
v v v v v
Cephalosporins MOA - ANS >> Bactericidal drug similar to penicillins that bind to penicillin-binding
v v v v v v v v v v v v v
proteins (PBPs):
v v
(1) disrupt cell wall synthesis
v v v v v
, (2) activate autolysins (enzymes that cleave bonds in the cell wall). The resultant damage to the cell
v v v v v v v v v v v v v v v v
vwall causes death by lysis. Most effective against cells undergoing active growth and division.
v v v v v v v v v v v v v
Ceftriaxone (Rocephin) - ANS >> Cephalosporin eliminated largely by the liver.
v v v v v v v v v v v
Dosage reduction is not necessary in patients with renal impairment.
v v v v v v v v v
Cephalosporin Administration - ANS >> poor absorption from the gastrointestinal (GI) tract, many drugs
v v v v v v v v v v v v v
in this class must be administered parenterally (by the intramuscular [IM] or intravenous [IV] route).
v v v v v v v v v v v v v v v
Cephalosporin Elimination - ANS >> Practically all drugs in this class are eliminated by the kidneys;
v v v v v v v v v v v v v v v
patients with renal insufficiency, dosages of drugs must be reduced (to prevent accumulation to toxic
v v v v v v v v v v v v v v v
levels).
v
Cephalosporin Monitoring - ANS >> Check renal function if prolonged therapy
v v v v v v v v v v
Cephalosporin Main Adverse Event - ANS >> Hypersensitivity reactions are the most frequent adverse
v v v v v v v v v v v v v
events.
v
Cephalosporins — Cefazolin, Cefotetan - ANS >> can induce a state of alcohol intolerance (the
v v v v v v v v v v v v v v
disulfiram effect) if to ingest alcohol while taking drugs
v v v v v v v v v
Cephalosporins - Cefotetan, Cefazolin, Ceftriaxone - ANS >> can promote bleeding as they contain a side
v v v v v v v v v v v v v v v
chain that interferes with Vitamin K metabolism which can inhibit the formation of clotting factors;
v v v v v v v v v v v v v v v
Caution if combines with other agents that promote bleeding
v v v v v v v v v
First generation cephalosporins indication - ANS >> Narrow Spectrum
v v v v v v v v
Gram+
Streptococci, Staphylococci, E.coli, K. Pneumoniae v v v v
Use in mild penicillin allergy
v v v v
strep pharyngitis, skin infections, surgical prophylaxis
v v v v v
First generation cephalosporin examples - ANS >> Cephazolin; Cephelexin (Keflex)
v v v v v v v v v
Second generation cephalosporins indication - ANS >> -Gram +/-
v v v v v v v v
-H. influenzae, Klebsiella, pneumococci, staphylococci
v v v v
-Otitis, sinusitis, respiratory tract infection
v v v v
-More broad than first generation
v v v v
Second generation cephalosporins examples - ANS >> ceFAclor, CeFOXitin, CeFURoxime (FAkeFOXFUR)
v v v v v v v v v v
Third generation cephalosporin indication - ANS >> -Serious Gram (-) bacteria
v v v v v v v v v v
the Family.
β-lactam antibiotic MOA - ANS >> All antibiotics in class share the same mechanism of action: disruption
v v v v v v v v v v v v v v v v
of the bacterial cell wall.
v v v v v
Inhibition of cell wall synthesis
v v v v
Empiric Therapy - ANS >> start treatment without cultures or prior to receiving the results of a culture
v v v v v v v v v v v v v v v v v
immediate empiric antibiotics - ANS >> Critically ill patients receive (Fill in the Answer) after the first set
v v v v v v v v v v v v v v v v v
vof cultures obtained; do not wait for results.
v v v v v v v
Bactericidal antibiotics - ANS >> Directly kill bacteria: Agents include aminoglycosides, beta-lactams,
v v v v v v v v v v v
fluoroquinolones, metronidazole, most antimycobacterial agents, streptogramins, and vancomycin.
v v v v v v v v
preferred for immunocompromised patients such as those with diabetes, HIV, or cancer and for those
v v v v v v v v v v v v v v
who have overwhelming infections
v v v v
Bacteriostatic agents - ANS >> inhibit bacterial proliferation while the host's immune system does the
v v v v v v v v v v v v v v
killing. Agents include clindamycin, macrolides, sulfonamides, and tetracyclines
v v v v v v v v
β-lactam Antibiotics - ANS >> Penicillins, Cephalosporins, Carbapenems, Monobactams
v v v v v v v v
Penicillins MOA - ANS >> Weaken bacterial cell wall by two actions:
v v v v v v v v v v v v
(1) inhibition of transpeptidases
v v v
(2) disinhibition (activation) of autolysins.
v v v v
PBPs (Penicillin Binding Proteins) - ANS >> Transpeptidases, Autolysins, and other bacterial enzymes are
v v v v v v v v v v v v v
collectively named as because antibiotic class must bind to them to produce antibacterial effects.
v v v v v v v v v v v v v v
gram-positive bacteria - ANS >> two layers: the cytoplasmic membrane and a relatively thick cell wall;
v v v v v v v v v v v v v v v
penicillins are generally very active against these organisms.
v v v v v v v v
,gram-negative bacteria - ANS >> three layers: the cytoplasmic membrane, a relatively thin cell wall, and
v v v v v v v v v v v v v v v
an additional outer membrane; only certain penicillins (e.g., ampicillin) are able to cross and reach
v v v v v v v v v v v v v v v
penicillin binding proteins (PBPs)
v v v v
Four Major Groups of Penicillins - ANS >> (1) narrow-spectrum penicillins that are penicillinase sensitive
v v v v v v v v v v v v v v
(2) narrow-spectrum penicillins that are penicillinase resistant (antistaphylococcal penicillins)
v v v v v v v v
(3) broad-spectrum penicillins (aminopenicillins)
v v v
(4) extended-spectrum penicillins (antipseudomonal penicillins).
v v v v
narrow-spectrum penicillins: Penicillinase sensitive penicillins - ANS >> Penicillin G, Penicillin V
v v v v v v v v v v v
narrow-spectrum penicillinase sensitive susceptible pathogens - ANS >> Streptococci, Neisseria,
v v v v v v v v v
anaerobes
v
very narrow antimicrobial spectrum and are used only against penicillinase-producing strains of
v v v v v v v v v v v
staphylococci (S. aureus and S. epidermidis). - ANS >> narrow-spectrum penicillins: penicillinase
v v v v v v v v v v v v
resistant penicillins
v v
narrow-spectrum penicillins: penicillinase resistant penicillins - ANS >> Nafcillin, Oxacillin, Dicloxacillin
v v v v v v v v v v
narrow-spectrum- penicillinase resistant susceptible pathogens - ANS >> S. Aureus, S. Epidermidis
v v v v v v v v v v v
Drugs of choice for most staphylococcal infections - ANS >> penicillinase-resistant penicillins (Nafcillin,
v v v v v v v v v v v v
Oxacillin, Dicloxacillin)
v v
Broad spectrum Penicillin: Aminopenicillins - ANS >> Ampicillin, Amoxicillin
v v v v v v v v
Broad spectrum Aminopenicillin susceptible pathogens - ANS >> Haemophilus influenzae, Escherichia
v v v v v v v v v v
coli, Proteus mirabilis, enterococci, Neisseria gonorrhoeae
v v v v v v
Extended spectrum penicillins (antipseudomonal penicillin) - ANS >> Piperacillin
v v v v v v v v
Has the same antimicrobial spectrum as penicillin G, plus increased activity against certain gram-
v v v v v v v v v v v v v
negative bacilli, including Haemophilus influenzae, Escherichia coli, and Salmonella and Shigella - ANS
v v v v v v v v v v v v
>> Broad spectrum Penicillin: Aminopenicillins
v v v v v
First line for acute otitis media and sinusitis - ANS >> Amoxicillin
v v v v v v v v v v v
,Extended spectrum penicillins suceptible pathogens - ANS >> Haemophilus influenzae, Escherichia coli,
v v v v v v v v v v v
Proteus mirabilis, enterococci, Neisseria gonorrhoeae, pseudomonas, enterobactor, klebsiella
v v v v v v v v
Principle pathogenic target of Piperacillin - ANS >> Pseudomonas aeruginosa
v v v v v v v v v
beta-lactamase inhibitors to broaden penicillin spectrum - ANS >> clavulanate, sulbactam, tazobactam
v v v v v v v v v v v
Penicillin/Beta-Lactamase Combinations - ANS >> Ampicillin/sulbactam (Unasyn) v v v v v v v
Amoxicillin/clavulanate (Augmentin) v
Piperacillin/tazobactam (Zosyn) v
MRSA Drug of Choice - ANS >> Vancomycin
v v v v v v v
Most Important AE of Penicillins - ANS >> Hypersensitivity Reaction
v v v v v v v v v
Drug of choice when history of anaphylaxis or some other severe allergic reaction to penicillins - ANS >>
v v v v v v v v v v v v v v v v v
Avoid cephalosporin;
v v v
Vancomycin, erythromycin, and clindamycin are effective and safe alternatives for patients with
v v v v v v v v v v v
penicillin allergy.
v v
Common drug used to treat bacterial infections in children. - ANS >> Penicillins
v v v v v v v v v v v v
First line treatment for infection following animal or human bites - ANS >> Amoxicillin/clavulanate
v v v v v v v v v v v v v
(Augmentin)
v
Medication common for streptococcal pharyngitis - ANS >> Penicillin
v v v v v v v v
Penicillin Risk in Pregnancy - ANS >> evidence suggests there is no second or third trimester fetal risk
v v v v v v v v v v v v v v v v v
Penicillin Risk in Infants - ANS >> Used safely in infants with bacterial infections, including syphilis,
v v v v v v v v v v v v v v v
meningitis, and group A streptococcus.
v v v v v
Amoxicillin - ANS >> Safe use during breastfeeding
v v v v v v v
Penicillin Use in Older Adults - ANS >> Doses should be adjusted in older adults with renal dysfunction.
v v v v v v v v v v v v v v v v v
Cephalosporins - ANS >> β-lactam antibiotics similar in structure and actions to the penicillins.
v v v v v v v v v v v v v v
Are bactericidal, often resistant to β-lactamases, and active against a broad spectrum of pathogens.
v v v v v v v v v v v v v
Useful alternative with mild penicillin allergy
v v v v v
Cephalosporins MOA - ANS >> Bactericidal drug similar to penicillins that bind to penicillin-binding
v v v v v v v v v v v v v
proteins (PBPs):
v v
(1) disrupt cell wall synthesis
v v v v v
, (2) activate autolysins (enzymes that cleave bonds in the cell wall). The resultant damage to the cell
v v v v v v v v v v v v v v v v
vwall causes death by lysis. Most effective against cells undergoing active growth and division.
v v v v v v v v v v v v v
Ceftriaxone (Rocephin) - ANS >> Cephalosporin eliminated largely by the liver.
v v v v v v v v v v v
Dosage reduction is not necessary in patients with renal impairment.
v v v v v v v v v
Cephalosporin Administration - ANS >> poor absorption from the gastrointestinal (GI) tract, many drugs
v v v v v v v v v v v v v
in this class must be administered parenterally (by the intramuscular [IM] or intravenous [IV] route).
v v v v v v v v v v v v v v v
Cephalosporin Elimination - ANS >> Practically all drugs in this class are eliminated by the kidneys;
v v v v v v v v v v v v v v v
patients with renal insufficiency, dosages of drugs must be reduced (to prevent accumulation to toxic
v v v v v v v v v v v v v v v
levels).
v
Cephalosporin Monitoring - ANS >> Check renal function if prolonged therapy
v v v v v v v v v v
Cephalosporin Main Adverse Event - ANS >> Hypersensitivity reactions are the most frequent adverse
v v v v v v v v v v v v v
events.
v
Cephalosporins — Cefazolin, Cefotetan - ANS >> can induce a state of alcohol intolerance (the
v v v v v v v v v v v v v v
disulfiram effect) if to ingest alcohol while taking drugs
v v v v v v v v v
Cephalosporins - Cefotetan, Cefazolin, Ceftriaxone - ANS >> can promote bleeding as they contain a side
v v v v v v v v v v v v v v v
chain that interferes with Vitamin K metabolism which can inhibit the formation of clotting factors;
v v v v v v v v v v v v v v v
Caution if combines with other agents that promote bleeding
v v v v v v v v v
First generation cephalosporins indication - ANS >> Narrow Spectrum
v v v v v v v v
Gram+
Streptococci, Staphylococci, E.coli, K. Pneumoniae v v v v
Use in mild penicillin allergy
v v v v
strep pharyngitis, skin infections, surgical prophylaxis
v v v v v
First generation cephalosporin examples - ANS >> Cephazolin; Cephelexin (Keflex)
v v v v v v v v v
Second generation cephalosporins indication - ANS >> -Gram +/-
v v v v v v v v
-H. influenzae, Klebsiella, pneumococci, staphylococci
v v v v
-Otitis, sinusitis, respiratory tract infection
v v v v
-More broad than first generation
v v v v
Second generation cephalosporins examples - ANS >> ceFAclor, CeFOXitin, CeFURoxime (FAkeFOXFUR)
v v v v v v v v v v
Third generation cephalosporin indication - ANS >> -Serious Gram (-) bacteria
v v v v v v v v v v