D4 Flashcards
What are representative members of Lipoglycoprotien?
Oritavacin, Dalbavancin, Telavancin
What is the cellular target of Lipoglycoprotien?
BP-NAG-NAM Monomers
What cell structure if affected by lipoglycoprotien?
Cell wall synthesis
what is the cellular target for Lipopeptide?
Pospholipids
What are the representative members of Lipopeptide?
Daptomycin, Polymyxins, Colistin
What is the cell structure affected by Lipopeptide?
Plasma membrane
What are toxicities associated with Lipopeptide?
Myopathy, eosinophilic pneumonia, Nephrotoxicity, Neurotoxicity.
What is the representative members of rifamycin?
Rifampicin
What is the cellular target of Rifampicin?
RNA Polymerase
what is the cellular affect on Rifamycin?
RNA synthesis
What is the toxicity related to Rifamycins?
Hepatotoxicity = CYP inducer, reddish body secretions
What is the cellular target of Fidaxomycin?
RNA Polymerase
What is the toxicity of Fidaxomicin?
Not well tolerated (Not absorbed)
What is the cellular affect by Fiaxomicin?
RNA synthesis
What are the representative members of Macrolid?
Erythromycin, Clarithromycin, Azithromycin
What is the cellular target of Macrolid?
50S Ribosome
What is the Macrolid’s cell affect?
Protein Synthesis
What is the cellular target of Chloramphenicol?
50S ribosome
What are the toxicology associated with Macrolid?
QT prolongation, hepatotoxicity = CYP Inhibitors
What are the members of Chloramphenicol?
Chloramphenicol
What is the cellular Affect of Chloramphenicol?
Protein synthesis
What are some of the toxicologies associated with Chloramphenicol?
Bone marrow suppression, gray baby syndrome
What bacteria groups are covered by Daptomycin?
MRSA, Step/Pneumo, Enterococcus/VRE
What is brand name for Daptomycin?
Cubicin
What are the bacterial groups covered by Polymixin, Colistin?
Gram (-) only (PEK, PIDDLY, SPACE)
What is fidaxomycin used for?
C.Diff only
What is the brand name for Fidaxomycin?
Difficid
What is the brand name of Rifampicin?
Rifampin
What is rifamycins used for? (Rifampicin, Rifapentine, Rifabutin)
Mycobacteria, Adjunct Abx (biofilms)
What is rifamycins used for? (Rifaximin)
GI E.coli only (Travelers diarrhea)
What is a warning about chloramphenicol
Its toxic and only should be used for last resort meningitis
What bacteria are treated by Chloramphenicol?
- Last stage Meningitis
- MRSA
- Strep
- PEK
- PIDDLY
- SACE
What are macrolids used for?
atypicals, M.Cat., H. flu, Chlamydia, Strep/Pneumo (resistance increasing), Infectious diarrhea
What is clindamycin used for?
Staph/MRSA, Strep/Pneumo, Oral anaerobes
(T/F) Lipoglycopeptide is Bactericidal
True
What is the mechanism of action for Lipoglycopeptide?
Interferes with transglycosylation
List 3 FDA approved Lipoglycopeptide
Dalbavancin,
Oritavancin
Telavancin
Lipoglycopeptides are _________ spectrum with ___________ glycopeptides
Narrow; Hydrophobic
Dalbavancin is good against?
MRSA
What is the pharmacokinetic facts about Dalbavancin?
Long plasma half life allows for once weekly dosing
What is a warning against Dalbavancin?
Hepatotoxicity
Dalbavancin Brand name
Dalvance
Oritavancin MOA?
Inhibits transglycosylation
How often is Oritavancin is dosed?
Long plasma life allows for a single dose treatment
What is a warning against Oritavancin?
Osteomyelitis
Oritavancin Brand name?
Orbactive
Toxicities related to Telavancin?
Nephrotoxicity due to Cyclodextrin vehicle
Telavancin brand name?
Vibativ
What is the MOA for Daptomycin?
Destabilizes plasma membrane integrity causing them to be leaky
Is Daptomycin good in lungs? Why
It is not used for respiratory infections (Pneumonia) because human lung surfactants bind and inactive daptomycin in lungs
Pharmacokinetic fact about Daptomycin?
Long half life (Once daily dose)
What are some of the toxicities related to daptomycin?
Neuropathy, Skeletal Myopathy. Eosinophilic pneumonia
Daptomycin brand name?
Cubicin
What bacteria are treated by Polymyxins?
only gram-negative bacteria susceptible
What is the MOA of Polymyxins?
It is a mixture of lipopeptide that destabilizes plasma membrane integrity causing them to be leaky
What are some toxicities for polymyxins?
Nephrotoxicity, neurotoxicity
Where is Polymyxin B used mainly?
OTC product, used for topical wound infections
What is Polymyxin indicated for
Bladder irrigation, and gut decontamination
What all drugs are in Neosporin?
Polymyxin B + Bacitracin Zinc + Neomycin
Colistin is a sulfate form of what?
Polymyxin E
What are some of the toxicities of Colistin?
Nephrotoxicity and Neurotoxicity (Should only be used as last resort antibiotic for MDR Gram (-) infections
Colistin Brands
Colistimethate
What Type of bacteria are susceptible to Bacitracin?
Gram (+)
How is Bacitracin used?
Topically
Bacitracin MOA?
Inhibitor of cell wall synthesis. Bacitracin binds to bactoprenol (BP)
How do “Inhibitors of Bacterial RNA synthesis” drugs work? (4 steps)
- Chains of RNAs are used to encode peptides and protien via ribosomes in cells
- RNA polymerase reads the DNA template to synthesize RNA strands by a process called transcription
- RNA polymerase and ribosomes (organelles that orchestrate protein synthesis = Translation)
- The most prominent antibacterial agents that inhibit RNA polymerase are the rifamycins that are predominantly used as adjuvant antibiotic in biofilm and mycobacterium infections
What is fidaxomycin used for?
treats C. Diff associated Diarrhea (CDAD), a bowel infection that arises during prolonged antibiotic use and can be fatal if left untreated
Where are C. Diff infections mainly come from?
obtained in hospitals and long term treatment facilities by spore ingestion
Fidaxomycin MOA
Interferes with RNA synthesis by inhibiting bacterial RNA polymerase
Fidaxomycin Phamacokinetics
- Like oral vancomycin, not absorbed in GI tract
- Eliminated by feces
Fidaxomyxin Brand
Dificid
Rifamycins MOA
Inhibitor of mycobacteria RNA polymerase
How is Rifamycin excreted?
Eliminated in feces
What are some of the Adverse rx of Rifamycins?
Hepatotoxcity (cause Orange-discoloration of urine/tears/sweat)
What are some of the drug interactions of Rifamycin?
activates CYP enzymes which can reduce the effectiveness of other drugs
(T/F) Rifamycin a CYP inducer.
True (decreased half life of drug)
What are all the oral Rifamycins?
Rifampin/Rifampicin, Rifabutin and rifapentin and Rifaximin
What is done for Rifamycins to get over its resistance development?
It is always used in combination with other antibiotics (adjuvants)
What are Oral Rifamycins used for?
- Mycobacterium infections (TB)
- Infections due to biofilm-forming bacteria (Staphylococcus)
(T/F) there are many uses for Rifaximin and do not have many ADRs
False however only used for Travelrs diarrhea
How do inhibitors of bacterial protein synthesis work?
- RNA synthesized from DNA by RNA polymerase are translated into peptides/proteins by 70S bacterial ribosomes
- Ribosomes are organelles consisting of 30S and 50S subunits
