D2 prework Flashcards
What is the class of Penicillin?
B-lactam
What is the cellular target of B-Lactam?
Penicillin-binding proteins (PBPS) - transpeptidase.
What cell structure is affected by B-Lactam?
Cell wall synthesis
What are some of the toxicities of B-Lactam?
Hypersensitivity, anaphylaxis (Except Aztreonam), seizure, CDAD
What are all the medications in Penicillin?
Penicillin G/VK,
(Anti-staphylococcal) Oxacillin/nafcillin/dicloxacillin,
ampicillin/amoxicillin and Ampicillin+sulbactam/amoxicillin+clavunate,
Ticarcillin+clavunate, PIP+TAZ
What bacterias are covered by PenG?
Staph (Except SA), Strep/Pneumonia, Oral anaerobes, syphilis.
What bacterias are covered by Pen VK?
Staph (Except SA), Strep/Pneumonia, oral anaerobes
What bacterias are covered by Group 3 B-Lactam?
Staph/MSSA, Step/pneumo
What bacterias are covered by Ampicillin/amoxicillin?
Strep/Pneumo, +VRE, PEK, Some PIDDLY, Oral anaerobes.
What bacterias are covered by PIP+TAZ?
Staph/MSSA, Strep/Pneumonia, Enterococcus/VRE, PEK, PIDDLY, SPACE, Anaerobes
What is the MOA of Penicillins?
Inhibition of cross linked peptidoglycan formation
What are the 4 Stages of NAG-NAM polymer formation?
Stage 1: NAG-NAM
Stage 2: Monomer Export
Stage 3: Transglycosylation
Stage 4: Transpeptidase
Explain the Stage 1 of NAM polymer.
NAG-NAM synthesis: NAG-NAM monomers are assembled and NAG is converted into pentapeptide
Explain the Stage 2 of NAM polymer.
Monomer Export: Bactoprenol (BP) carrier transports and release the NAG-NAM monomer outside the cell
Explain the Stage 3 of NAM polymer.
Transglycosylation: Transglycosylase catalyzes the transfer of the NAG-NAM monomer to the end of the growing peptidoglycan strand
Explain the Stage 4 of NAM polymer.
Transpeptidation is cross linking step between petidoglycan strands. Enzymes that form peptide bonds between the a side chains of NAM are called Transpeptidase (PBPs).
What is the purpose of B-Lactam ring?
The hydrolytic site in the PBP makes it more prone to by hydrolyzed
How is Penicillin G pen formulated?
Na+ and K+ (Pfirzerpen)
Benzathine, or procain salts
What are the type of bacteria that Penicillin G is effective against?
Non B-lactamase producing cocci, syphilis. most oral anaerobes.
What makes Penicillin unstable to stomach acid?
IV (Na+/K+ salt) or IM (Procain/benzathine salt) injection
How do you formulate Penicillin G to last longer and decrease the local pain?
IM injections of low H2O salt forms of PEN are used with Procain and benzathine Base
(T/F) You can take long acting PEN by IV
False (can be fatal)
How do penicillin cause anemia
The medication may react with proteins on the surface of RBC which can be read by immune system and it starts to destroy cells.
What are some of the adv rx of Penicillins?
Immediate IgE-mediated anaphylaxis (type 1 hypersensitivity), Later allergic reaction (type IV) and CDAD
What are some drug interactions of Penicillin?
No CYP450 interactions, can be placed form serum proteins by other drugs (Warfarin)
Probenecid (for gout) could increase the time B-Lactam drugs stay in the system.
B-lactamase could interfere with enterohepatic circulation of oral estrogens causing low levels of estrogen.
What penicillin do we use instead of PEN G for oral use?
Penicillin VK is more acid-stable
What bacteria are covered by Penicillin VK?
it is a narrow spectrum drug that covers Staph/strep and oral anaerobes
How are Penicillin group 3 more stable?
Due to the presence of C-6 side chains.
What are some of the examples of Penicillin group 3?
Methicillin, Oxacillin, Dicloxacillin, Nafcillin
How to increase the Short half-life of Oxacillin?
Blood levels may be prolonged by concurrent administration of probenecid which blocks the renal tubular secretion of penicillin
How is Dicloxacilin excreted?
POO POO
Which group 3 member of penicillin have erratic absorption?
Dicloxacillin (Dynapen) MOTHA FUKA
What are some of the adverse reaction of Dicloxacillin?
Metallic taste and belching may cause poorly tolerated drug FOKA MOTHA
How is Nafcillin excreted?
Through feces
Why shouldn’t you give Group 4 penicillins by itself?
It is unstable to B-lactamase, (must be given with B-Lactamase inhibitor for MSSA and B. Fragilis
What is a risk that is associated with Ampicillin?
higher risk of rash in patients with mononucleosis and diarrhea
Which group IV have better Bioavailability than ampicillin?
Amoxicilin (Also causes less diarrhea)
Adverse reaction of AMP?
Rashes occur more often with AMP and AMX than with other penicillins
What are some of the examples of Group V penicillin?
Ticarcillin, Piperacillin
Who should be cautious while taking Ticarcillin?
pts with restricted Na intake. Disodium formulated
Is ticarcillin weak to B-lactamase?
Yes which is why it is dispensed with Clavulanic acid (Timentin)
What is the administration requirement of Pipercillin?
admin with B-Lactamase inhibitor (tazobactam) Zosyn
What is the MOA of B-lactamase inhibitor?
the inhibitors bind irreversibly to the B-lactation allowing B-al tam antibiotics to reach the PBPs unhindered
Why are majority of of B-lactamase inhibitors require another antibiotic to go along with it?
Most B-lactamases inhibitors do not bind PBPs and most have no antibiotic effects alone.
Which Antibiotic would go with Clavulanic acid (CA)?
Amoxicillin (Augmentin)
Ticarcillin (Timentin)
Which Antibiotic would go with Sulbactam (SUL)?
Ampicillin (Unasyn)
Which Antibiotic would go with Tazobactam (TAZ)
Piperacillin (Zosyn)
Ceftolozane (Zerbaxa)
Which Antibiotic would go with Avibactam (AVI)?
Ceftazidime (Avycaz)
Which Antibiotic would go with Vaborbactam (VAB)?
Meropenem (Vabomere)
Both Gram (+) and Gram (-) may produce _________.
Penicillinase
only in Gram (-) bacteria can produce __________ and _________.
Cephalosporinases (TEM) and Carbapenemases (KPC)
Which antibiotic is the only one that is not effected by Extended Spectrum B-Lactamases (ESBL) in PEK and SPACE?
Carbapenamase
Cephalosporinases is the most common ESBL form in Gram (-) and can be inhibited by:
Clavulanic acid
Sulbactam
Tazobactam
ALl ESBLs are inhibited by:
Avibactam
Vaborbactam
Klebsiella pneumoniae carbapenemase is inhibited by
Avibactam
Vaborbactam
