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86 Cards in this Set

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What are the three Beta-lactamase resistant penicillins?
Methicillin (no longer used), Nafcillin (use Naf for Staph), and Oxacillin (oral); (MNO)
Name the penicillins that targets Pseudomona aeruginosa and other gram-negative aerobes.
Ticarcillin, Carbenicillin, and Piperacillin (Takes Care of Pseudomonas)
Amoxicillin (oral) and Ampicillin HELPS
Haemophilus, E. coli, Listeria, Proteus, Salmonella
What is the molecule found in the cell wall of bacteria that is triggered by penicillins that aid in the destruction of the bacterium through the formation of a spheroplast?
peptidoglycan hydrolase
What medication (used as a uricosouric) is used to increase the half life of penicillin by blocking the excretion of penicillin in the PCT of the kidney?
Probenecid
What multiple of the MIC of penicillin is used for a systemic infection? How about a CNS infection?
4, 10
What is the indications for Penicillin G?
Streptococcus infections, Syphilis (Benzathine Penicillin G), Neisseria meningitidis, anaerobes (e.g. Clostridium perfringens)
How does a penicillin become resistant to a penicillinase?
Either through addition of clavulinic acid or through increasing the -R group of the penicillin molecule
What happens when you increase the size of the -R group, when you are trying to make a penicillinase-resistant penicillin?
The penicillin becomes less potent, so you must increase the dose.
What are the penicillinase-resistant penicillins generally good for?
Skin infections (Methicillin/Nafcillin IV; Oxacillin oral)
Name five general penicillins that are targeted to Gram negatives.
Ampicillin, Amoxacillin, Ticarcillin, Carbenicillin, and Pipercillin
What is special about the amino groups on the R-groups of the aminopenicillins (e.g. ampicillin and amoxacillin)
They increase the penetration of the Gram negative's outer membrane
Which two antibiotics do you often see a skin rash with?
Aminopenicillins (amoxicillin and ampicillin) and sulfamethoxazole
Which form of antibiotics are more likely to cause diarrhea: oral or IV/IM?
Oral (amoxicillin vs. ampicillin)
Name two antibiotics that are most associated with pseudomembraneous colitis.
Amoxicillin and clindamycin
Is ticarcillin and pipercillin effective against Pseudomonas? Bacteroides fragilis (Gram negative anaerobe)?
Yes, yes
Name three bacteria that pipercillin is more affective against versus ticarcillin.
Pseudomonas, Proteus, Klebsiella (PiPerKillin)
What is the Gold Standard for treating Gram negative aerobes?
Aminoglycosides (GNATS: Gentamycin, Neomycin, Amakacin, Tobramycin, Streptomycin)
What is an excellent synergistic combination of antibiotics against Pseudomonas?
Aminoglycosides and Ticarcillin/Carbenicillin/Pipercillin
What is a potential side effect of having to use such a high dose of anti-pseudomonas penicillinases (low potency due to large R-group)?
Sodium salt overload; bad for hypertension
What is the main structural difference between penicillins and cephalosporins?
Cephalosporins have two R-groups, whereas penicillins have one R-group
Will the cephalosporins resist the Staph penicillinase?
The first (Cephalexin and Cefazolin) and fourth (cepepime) generations will, but not the second (cefotetan, cefoxitin, and cefuroxime) and third (ceftriaxone, cefotaxime, and ceftazadime) generations.
Which cephalosporin is highly effective against anaerobes (especially Bacteroides fragilis)?
Cefoxitin (Second generation; send the fox down the pipe to get the B. fragilis).
Which generation(s) of cephalosporin is effective against Pseudomonas?
Third and fourth
What percent of patients having an allergic reaction to penicillins will have an allergic reaction to cephalosporins? Is it worth risking?
10%; probably not
What is the broadest spectrum Beta-lactam? What does it cover?
imipenem. Aerobe/anaerobe Gram positive/negative
What must you watch about using imipenem?
Imipenem should not be used first because the bacteria will secrete massive amounts of lactamase because imipenem won't even bind the lactamase.
What compound must you take with imipenem in order to prevent the kidney's breakdown of imipenem by a dipeptidase?
Cilastatin; the kill is LASTIN with CiLASTATIN.
Aztreonam (aka Monobactam): spectrum and MOA
Gram negative aerobes; MOA similar to Pen G
Mupirocin: use? MOA?
Impetigo cause by Staph and Strep (even lactamase-secreting Staph); Bacterial protein and RNA synthesis are inhibited
Vancomycin: MOA; Use; toxicities
inhibits bacterial cell wall synthesis; MRSA, Enterococcus faecalis/faecium, C. difficile (should use metronidazole though); NOT (nephrotoxicity, ototoxicity, thrombophlebitis (Red Man Syndrome (histamine release; take with aspirin and give slower))
Explain the Davis model as to why aminoglycosides are bacteriocidal.
When a [small] of aminoglycosides gets inside the bacterial cell, it causes an altered protein product, which implants within the bacterial membrane and serves as a pore. Through this pore flows additional aminoglycosides that serve to finish off the bacterial cell.
Name the members of the aminoglycoside family.
GNATS: Gentamycin, Neomycin, Amikacin, Tobramycin, and Streptomycin
What feature of aminoglycosides make them similar to vancomycin, as far as oral dosing remaining within the GI tract?
All the amino groups pick up positive charges, and cannot cross membranes very well (vancomycin is just so damn big)
What is a downstream consequence of the amino groups on the aminoglycosides (think kidney)?
These molecules are mistaken as amino acids in the PCT of the kidney, where 35% of the dose is accumulated, leading to inhibition of lysosomal enzymes, leading to lysosomal burst and renal toxicity
What are the three main toxicities of aminoglycosides?
NON or amiNOglycosides: Nephrotoxicity, Ototoxicity, and neuromuscular block (treat with neostigmine; usually follows bowel rupture)
Name three mechanisms for resistance to aminoglycosides.
1) ribosomal resistance, 2) decreased drug uptake, and 3) aminoglycoside modifying enzymes
What distinguishes the newer Amikacin from the older kanamycin aminoglycosides?
Amikacin has a larger R-group that inhibits many modifying enzymes
What is the main use for aminoglycosides?
Combo therapy with a beta-lactam to treat Gram negative infections or sometimes Staph/Strep infections (aminoglycosides are exclusively targeted against aerobes)
How well do aminoglycosides enter the CNS?
None, due to amino groups
Must you monitor serum drug concentrations and kidney functions when administering aminoglycosides?
YES
What are the indications for aminoglycoside use?
Serious aerobic gram-negative infections, including Pseudomonas aeruginosa
What is unique about the newer tetracyclines doxycycline and minocycline?
They are more lipophilic, have higher protein binding, lower renal excretion, higher half life, and very little renal excretion (doxycycline can be used in renal failure patients).
Which tetracycline can be used in renal failure patients?
Doxycycline (higher lipophilicity with excretion in fecal matter and bile)
Which two antibiotics must you not take with food, milk, other dairy products, and antacids?
Tetracyclines and Floroquinolones (both like bone/cartilage)
What is a negative side effect of tetracycline dosing in children younger than 12?
Gray/brown stained teeth.
How does tetracycline gain access to the bacterial cell?
It is actively pumped in (it is confused with a natural nutrient).
Which antibiotic is known for producing a blistering rash?
Tetracyclines
What are the indications for tetracyclines?
Pulmonary infections (Mycobacterium pneumoniae, Haemophilus influenzae, Streptococcus pneumoniae), Chlamydia (DOC), Rickettsia (DOC), and Lyme disease (DOC)
What antibiotic spectrum does Chloramphenicol have in common?
Tetracyclines
Which side effect of Chloramphenicol put this antibiotic off the market, and how common is it?
Aplastic anemia, which is idiosyncratic, occurs in 1/30000 patients
Name the Macrolides
ACE: Azithromycin, Clarithromycin, and Erythromycin.
What is the DOC for Legionella?
Erythromycin
What are the indications for Marcrolides (ACE)?
UPS: URI:Gram positive (Staph and Strep), Staph aureus (resistant to penicillinases); Pneumonia: Mycoplasma pneumoniae, Haemophilus influenzae; STD: Chlamydia
What are macrolides known for?
Their ability to penetrate tissues well (ears, lungs).
What is the most common side effect associated with Macrolides (ACE)?
GI disturbances (erythromycin causes a motilin-like activity).
Linezolid: uses, price, interaction, and SEs
VRE, MRSA; $45/pill; inhibits MAO; causes BM suppression
Name the antibiotic with an activity similar to vancomycin, without resistance, used to treat nasty Gram positive organisms like VRE and MRSA.
Daptomycin
Clindamycin has activity similar to which antibiotic? If you have resistance to clindamycin, which other antibiotic will you most likely also have resistance to?
Erythromycin, erythromycin
What is the indications for Clindamycin?
Anaerobic infections (e.g. Bacteroides fragilis); but also covers Staph aureus, Strep pyogenes and Strep pneumoniae
What is the most common side effect of Clindamycin?
SPECTACULAR DIARRHEA often (20% of time) leading to pseudomembranous colitis (do NOT treat diarrhea with kaopectate or loperamide)
What is the treatment of choice for Clostridium difficile
Vancomycin, or metronidazole
Metronidazole: things to know
GET GAP (Giardia, Entameba, Trichomonas, Gardnerella, Anaerobes, H. pylori); don't drink (disulfiram like reaction); alters DNA helical coiling
Sulfamethoxazole: MOA; main SOA; Resistance; Toxicity
Inhibits DHF synthetase; UTI; increase PABA or salvage of aas/purines/pyrimidines from environment (this is why you can't use sulfamethoxazole on an abscess); skin rashes and displaces bilirubin from albumin
Trimethoprim: MOA
DHF reductase
TMP-SMX indications
the Super Sport for UTIs and URIs:

Salmonella, Shigella
UTI: E. coli
URI: Strep pneumo, H. influenzae, S. aureus, PCP!
Quinolones: MOA; specialty; indications
Inhibits DNA gyrase (topoisomerase II); oral antibiotics for gram negative infections (including P. aeruginosa)

Indications: Ciprofloxacin (not for respiratory bugs, just gram -s)
Levofloxacin (gram negative bugs plus Staph/Strept)
Moxifloxacin (gram negative bugs, Staph/Strep, anaerobes)
What is the main toxicity associated with quinolones?
Cartilage and tendon damage
Best antibiotic for the following combo of bugs: Neisseria, Bacteroides fragilis, and E. coli
Cefoxitin
Name two polyenes, and their MOA (antifungals)
Nystatin and Amphotericin B; irreversibly binds ergosterol
What is the MOA of the azoles (antifungals)?
Interfere with the biosynthesis of ergosterol by inhibiting 14 alpha-sterol demethylase
Name an azole that is used as a losenge for the treatment of oral candidiasis.
Clotrimazole
What is so special about Griseofulvin? MOA? Indications?
Oral pill for topical infections; Inhibits microtubule formation; surface fungal infections
Terbinafine: MOA? Indications?
Inhibits ergosterol formation by inhibiting squalene monooxygenase; Indicated for onychomycosis (3 month treatment)
Caspofungin: MOA? Indications?
Inhibits formation of Beta-Glucan in cell wall; Used for systemic candida infections ("Ca"spofungin for "Ca"ndida)
Which antifungal is most commonly used to treat Cryptococcus?
Fluconazole
Acyclovir and Gancyclovir: MOA? Indications?
Phosphorylated by viral Tyrosine Kinase and cellular kinases, where they inhibit DNA polymerase; Herpes, and CMV
How do you deal with the short half life of acyclovir?
Add a valine to it, producing valacyclovir!
Amantadine and Rimatadine: MOA? Indications?
Inhibit M2 protein, inhibiting viral uncoating; use as prophylaxis for Influenza A (90% are resistant now)
Zanamivir and Oseltamivir: MOA? Indications?
Inhibits neuraminidase; prophylaxis of Influenza (Oseltamivir decreases mortality associated with H5N1 bird flu and H1N1 swine flu)
Name four Nucleoside Reverse Transcriptase Inhibitors (NRTI) for HIV treatment.
LADZ: Lamivudine (pancreatitis), Abacavir (newer, less SEs), Didanosine (peripheral neuropathy and pancreatitis), and Zidovudine (anemia and granulocytopenia)
What is the MOA of HIV NRTI?
Inhibits the RNA-dependent DNA polymerase (reverse transcriptase). The NRTIs are lacking the 3'OH.
Name the suffix for protease inhibitors. MOA?
(Navir TEASE a proTEASE) -navir (e.g. saquinavir); inhibit maturation of HIV viral proteins.
Name three NNRTI for HIV treatment. MOA?
NED: Neviripine, Efavirenz, Delavirdine; inhibits Reverse Transcriptase.
What is the MOA for Enfuvirtide? What is the drug?
HIV drug; inhibits viral attachment and entry of the HIV virus, through blocking CD41 molecule folding.
Name four drugs used for tuberculosis treatment, along with their toxicities.
RIPE for treatment;
Rifampin (turns excretions red/orange, Red Lobster Man),
Isoniazide (DOC; hepatitis and peripheral neuropathy, supplement with vitamin B6)
Pyrazinamide (hepatitis)
Ethambutol (retrobulbar neuritis, leading to blurry vision and red/green color blindness)

Need 6 months of treatment