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Western U GI

Terms

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Ciprofloxacin
Indications:
Infectious diarrhea:
Salmonellosis (nontyphoidal and typhoid fever)
Shigellosis
Campylobacteriosis
E. coli (except Shiga toxin-producing strains)
Cholera
Yersiniosis
Intra-abdominal infections:
SBP prophylaxis
Community-acquired complicated extra-biliary infections of any severity (with metronidazole)
High risk or severe complicated community-acquired acute cholecystitis/cholangitis with severe physiologic disturbance, advanced age, or immunocompromised state (with metronidazole)
(N.B. Quinolone-resistant E. coli have become common in some communities, and quinolones should not be used unless hospital surveys indicate >90% susceptibility of E. coli to quinolones)











Moxifloxacin (indications)
Mild-to-moderate severity complicated community-acquired intra-abdominal extra-biliary infections
Ceftriaxone (Indications)

Indications:
Infectious diarrhea:
Salmonellosis (typhoid fever)
Severe yersiniosis
Intra-abdominal infections:
SBP
Community-acquired acute cholecystitis of mild-to-moderate severity
Extra-biliary mild-to-moderate complicated community-acquired intra-abdominal infections (with metronidazole)






Ceftriaxone (Rxns)
Hypersensitivity
Biliary stasis (prolonged use)
Bone marrow suppression (rare)
Pseudomembranous colitis


Cefepime (Indications)
Indications: Community-acquired intra-abdominal biliary and extra-biliary infections with high risk or severity (with metronidazole) Healthcare-associated complicated intra-abdominal infections where
Cefepime (MOA)
MOA: bactericidal against actively growing bacteria; bind and inhibit penicillin-binding proteins to inhibit cell wall synthesis
Azithromycin (Indications)
Indications:
Infectious diarrhea:
Salmonellosis (typhoid fever)
Campylobacteriosis
E. coli (except Shiga toxin-producing strains)
Cholera




Azithromycin (MOA)
MOA: bacteriostatic; inhibit protein synthesis by binding reversibly to 50S ribosomal subunits of sensitive microorganisms
Trimethoprim-sulfamethoxazole
(TMP-SMX)
(Indications)

1. Infectious diarrhea:
a. Shigellosis
b. Isosporiasis
c. Severe yersiniosis
2. Intra-abdominal infections:
a. SBP prophylaxis




Trimethoprim-sulfamethoxazole (TMP-SMX)

(MOA)

synergistic bactericidal; sequential blockade of enzymatic pathway for synthesis of tetrahydrofolic acid
Doxycycline
Infectious diarrhea:
Cholera
Yersiniosis (with gentamicin)

Doxycycline (MOA)
bacteriostatic; inhibit bacterial protein synthesis by binding to the 30S bacterial ribosome and preventing access of aminoacyl tRNA to the acceptor site on the mRNA-ribosome complex
Tigecycline
(Indications)
Indications:
Mild-moderate severity community-acquired complicated intra-abdominal extra-biliary infections
Tigecycline (MOA)
MOA: similar to tetracycline but avoids efflux pumps of Enterobacteriaceae, staphylococci, and Acinetobacter



Metronidazole/tinidazole (5-nitroimidazoles)
(Indications)
Indications: Infectious diarrhea: Antibiotic-associated (C. difficile) Intestinal amebiasis (trophozoites) Giardiasis Intra-abdominal infections: Amebic liver abscess Community-acquired complicated extra-biliary infections (with ceftriaxone, aztreonam, or ciprofloxacin) Community-acquired complicated biliary infection (with cefepime or ciprofloxacin) Healthcare-associated complicated intra-abdominal infections where
Metronidazole/tinidazole (5-nitroimidazoles)
(MOA)
MOA: electron acceptor that results in toxic free radicals that damage anaerobic and microaerophilic microbial DNA and other vital biomolecules
Nitazoxanide (Indications)
Infectious diarrhea:
Cryptosporidiosis
Antibiotic-associated (C. difficile)
Giardiasis


Nitazoxanide (MOA)
MOA: exact mechanisms remain unclear but appears to interfere with the PFOR enzyme-dependent electron-transfer reaction
Vancomycin (Indications)
Indications:
Infectious diarrhea:
Severe antibiotic-associated (C. difficile)

Paromomycin (Indications)
Indications:
Infectious diarrhea:
Intestinal amebiasis (cysts only)
Giardiasis






Paromomycin (MOA)
MOA: binding to the 30S ribosomal subunit
Piperacillin-tazobactam
(Indications)
Indications:
Community-acquired intra-abdominal biliary and extra-biliary infections with high risk or severity (severe physiologic disturbance, advanced age, or immunocompromised state)
Healthcare-associated biliary infection of any severity





Piperacillin-tazobactam
(MOA)
MOA: bactericidal against actively growing bacteria; bind and inhibit penicillin-binding proteins to inhibit cell wall synthesis



Cefoxitin (Indications)
Mild-moderate severity community-acquired intra-abdominal extra-biliary infections



Cefoxitin
(MOA)
MOA: bactericidal against actively growing bacteria; bind and inhibit penicillin-binding proteins to inhibit cell wall synthesis
(second gen. Cephlasporin)
Aztreonam (Indications)
Indications:
Intra-abdominal infections:
Secondary peritonitis (with metronidazole and agent effective against Gram-positive cocci)
Pyogenic liver abscess (with metronidazole and agent effective against Gram-positive cocci)
Cholecystitis/cholangitis (with metronidazole and agent effective against Gram-positive cocci)
Pancreatic abscess (with metronidazole and agent effective against Gram-positive cocci)

NO ACTIVITY AGAINST GRAM-POS. BACTERIA






Aztreonam (MOA)
MOA: interacts with penicillin-binding proteins and induces formation of long filamentous bacterial structures. It is resistant to many of the β-lactamases produced by most gram-negative bacteria; activity differs from other β-lactam antibiotics and more closely resembles that of an aminoglycoside; has activity only against aerobic gram-negative bacteria



Gentamicin (Indications)
Indications:
Healthcare-associated intra-abdominal infections where suspicion for ESBL-producing Enterobacteriaceae and/or >20% prevalence of ceftazidime-resistant Pseudomonas (combined with metronidazole and β-lactam)




Gentamicin
MOA: rapidly bactericidal; concentration-dependent; post-antibiotic effect; inhibit protein synthesis and decrease ribosomal mRNA but precise mechanism causing rapid killing is unknown; diffuse through outer membrane aqueous porin channels of gram-negative bacteria to enter the periplasmic space. Transport of aminoglycosides across the cytoplasmic (inner) membrane (energy-dependent phase I, or EDP1). Depends on electron transport in part because of a requirement for a membrane electrical potential (interior negative) to drive permeation. It is rate-limiting and can be blocked or inhibited by divalent cations (e.g., Ca2+ and Mg2+), hyperosmolarity, a reduction in pH, and anaerobic conditions. Acidic and anaerobic conditions impair the ability of the bacteria to maintain the membrane potential. Thus, aminoglycoside activity is markedly reduced within an abscess and hyperosmolar acidic urine. Intracellularly, aminoglycosides bind to polysomes and interfere with protein synthesis by causing misreading and premature termination of mRNA translation. Aberrant proteins insert into the cell membrane and promote enhanced permeability and aminoglycoside transport (termed energy-dependent phase II, or EDP2), which may explain why aminoglycosides are bactericidal



What is the indication for the carbapenem drug ertapenem?
Mild-moderate severity community-acquired intra-abdominal infections: ertapenem
What are the indications for the following carbapenems: doripenem, meropenem, cilastatin-Imipenem?
High risk or severe complicated community-acquired and healthcare-associated intra-abdominal infections: imipenem-cilastatin, meropenem, doripenem
What is the MOA of the carbapenems?
(Imipenem-cilastatin, meropenem, doripenem, ertapenem?
MOA: Inhibits bacterial cell wall synthesis by binding to several of the penicillin-binding proteins, which in turn inhibits the final transpeptidation step of peptidoglycan synthesis; bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.



Lamivudine (indications)
HBV
Tenofovir (Indications)
HBV
Tenofovir
MOA: Tenofovir disoproxil fumarate is hydrolyzed rapidly to tenofovir (a nucleotide monophosphate analog that requires two additional phosphorylations by cellular kinases to the active metabolite, tenofovir diphosphate (actually a “triphosphate”). The intracellular diphosphate is a competitive inhibitor of viral reverse transcriptases. Although tenofovir diphosphate has broad-spectrum activity against viral DNA polymerases, it has low affinity for human DNA polymerases-α, -β, and -γ, which is the basis for its selective toxicity.



Entecavir
Indications: HBV
Adefovir (Indication)
Indications: HBV
Adefovir (MOA)
MOA: enters cells and is deesterified to adefovir. Adefovir is converted by cellular enzymes to the diphosphate, which acts as a competitive inhibitor of viral DNA polymerases and reverse transcriptases with respect to deoxyadenosine triphosphate and also serves as a chain terminator of viral DNA synthesis



Ribavirin (Indications)
HBV, HCV
Interferon-alpha (Indications)
HBV, HCV
Albendazole (Indications)
Indications:
Nematodes:
“Geohelminths”
Ascariasis
Visceral larva migrans (T. canis)
Trichuriasis
Hookworms (Necator americanus, Ancylostoma duodenale)
Enterobiasis
Trichinosis
Cestodes:
Echinococcosis
Cysticercosis (Taenia solium)














Albendazole (MOA) and Mebendazole (MOA)
inhibit microtubule polymerization by binding to β-tubulin
Mebendazole (Indications)
Indications:
Nematodes:
“Geohelminths”
Ascariasis
Trichuriasis
Hookworms (Necator americanus, Ancylostoma duodenale)
Enterobiasis
Trichinosis










Pyrantel pamoate (Indications)
Indications:
Nematodes:
“Geohelminths”
Ascariasis
Hookworms (Necator americanus, Ancylostoma duodenale)
Enterobiasis




Pyrantel pamoate
MOA: depolarizing neuromuscular blocking agent; opens nonselective cation channels and induces persistent activation of nicotinic acetylcholine receptors causing spastic paralysis; also inhibits cholinesterases causing a slowly developing muscle contracture



Ivermectin (Indications)
Nematodes:
“Geohelminths”
Strongyloidiasis

Ivermectin (MOA)
MOA: binds to glutamate-activated chloride channels found in nematode nerve or muscle cells, which causes hyperpolarization by increasing permeability of chloride ions through the cell membrane resulting in paralysis of the parasite
Praziquantel (Indications)
Indications:
Cestodes:
Intestinal form of Taenia solium (pork tapeworm)
Taenia saginata (beef tapeworm)
Diphyllobothrium latum (fish tapeworm)
Hymenolepis nana (dwarf tapeworm)
Trematodes:
Schistosomiasis (blood flukes)
Clonorchis sinensis, Opisthorchis viverrini, O. felineus (Chinese liver flukes)
Fasciolopsis buski, Heterophyes heterophyes, Metagonimus yokogawai, Nanophyetus salmincola












Praziquantel
MOA: 2 major effects on adult schistosomes: 1) at lowest concentrations, increased muscular activity is followed by contraction and spastic paralysis. Worms detach from blood vessel walls and shift from mesenteric veins to the liver; 2) at higher concentrations, tegumental damage exposes antigens; clinical efficacy drug correlates better with tegumental action. The tegument is primary site of action. The drug causes an influx of Ca2+ across the tegument, and the effect is blocked in Ca2+-free medium.
Triclabendazole (Indications)
Trematodes:
Fasciola hepatica (liver fluke)
Paragonimus westermani (lung fluke)

Triclabendazole (MOA)
MOA: active sulfoxide metabolite binds to fluke tubulin by assuming a unique nonplanar configuration and disrupts microtubule-based processes.

Deck Info

51

RaguSiv

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