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Mechanism of penicillin
Inhibits transpeptidase cross-linking of bacterial cell wall
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Name 3 penicillinase-resistant penicillins
What is their clinical use?
- Methicillin
- Nafcillin
- Oxacillin
Use for staph aureus (except for MRSA)
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Two extended spectrum penicillins
-what needs to be added to treatment plan?
- Ampicillin and amoxicillin
- Use with clavulanic acid or sulbactam to protect against penicillinase
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Treatment of choice for listeria and e. coli
Ampicillin or amoxicillin
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Three anti-pseudomonal penicillins
Ticarcillin, piperacillin, carbenicillin + clavulanic acid, sulbactam, or tazobactam
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Two first generation cephalosporins and their main clinical use
- Cefazolin, cephalexin
- Use for surgical prophylaxis, due to their long half lives
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Three third generation cephalosporins and their major clinical uses
- Cefotaxime, ceftazidime, ceftriaxone
- Use to treat gonorrhea, sepsis, and meningitis (can cross the BBB)
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Name four bacteria that third generation cephalosporins do not work on
- Listeria--penicillin
- Atypicals--macrolides
- MRSA--vancomycin
- Enterococci--amoxicillin
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Mechanism and clinical use of aztreonam
- Inhibits cell wall synthesis
- Synergistic with aminoglycosides
- No cross-allergenicity with penicillin--can be used as an alternative in patients with penicillin allergy
- ONLY works on gram negative rods
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What needs to be administered with imipenem?
Cilastatin, to inhibit renal inactivation
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Major side effect of imipenem
Seizures
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Mechanism and clinical use of vancomycin
- Inhibits D-ala D-ala in bacterial cell walls
- Use for bad gram positives (S. aureus, clostridium)
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Why can't furosemide or gentamycin be used with vancomycin?
Risk of ototoxicity
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Drug that causes red man syndrome, due to hypersensitivity reaction
Vancomycin
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Name five aminoglycosides, and their mechanism of action
Gentamycin, neomycin, amikacin, tobramycin, streptomycin
- Inhibit formation of the initiation complex, block mRNA translation
- Require oxygen for uptake, so don't work against anaerobes
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Side effects of aminoglycosides
- Nephrotoxicity
- Ototoxicity (especially when used with furosemide)
- Teratogenic
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Antibiotic that acts like the botulinum toxin, and causes neuromuscular blockade
Aminoglycosides (streptomycin, neomycin, amikacin, gentamycin, tobramycin)
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Mechanism of tetracycline
Binds to 30S subunit, blocks binding of aminoacyl-tRNA
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Why can't tetracycline be taken with antacids or milk products?
- Tetracycline binds to divalent cations in the gut, which inhibits its absorption (and absorption of the cations)
- Inhibition of Ca absorption can cause dysplastic changes to teeth and bones
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Drug of choice for lyme disease
Doxycycline
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Demeclocycline
A tetracycline that acts as an ADH antagonist. Used to treat SIADH, not used as an antibiotic
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Mechanism and use of macrolides
- Bind to 50S subunit, block translocation
- (names all end in ...thromycin)
- Use for atypicals (mycoplasma, legionella, chlamydia, MAC)
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Side effects of macrolides
- Prolongation of QT interval
- GI discomfort, due to activation of motilin receptors
- Acute cholestatic hepatitis
- Increased concentration of oral anticoagulants
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Drug that causes aplastic anemia and gray baby syndrome
Chloramphenicol
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Drug of choice for gram positive osteomyelitis
Clindamycin--good for osteomyelitis because has good penetrance into bone, but DOES NOT WORK against gram negative osteomyelitis (i.e. salmonella)
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Drug of choice for macrolide-resistant pneumonia
Telithromycin
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Drugs for VRE
- Quinupristin, dalfopristin--bind to 50S ribosomal subunit
- Linezolid--blocks initiation complex formation
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Enzyme inhibited by TMP-SMX
Dihydropteroate synthetase
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Drug of choice for PCP
TMP-SMX
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Drug of choice for Chagas disease
Nifurtimox (arsenic)
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Antibiotics that cause tendonitis
Fluoroquinolones
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Triple therapy
- Bismuth
- Metronidazole
- Amoxicillin/tetracycline
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Side effect of metronidazole
Disulfiram like reaction with alcohol
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Anti-TB drug that exacerbates gout
Pyrazinamide
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Drug that causes red-green color blindness
Ethambutol
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Drug of choice for P. vivax and P. ovale
Primaquine
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Side effects of isoniazid
- Neurotoxicity, due to similarity with B6, and impaired B6 absorption
- B3, niacin, deficiency, since B6 is needed to make B3
- Hepatotoxicity
- DI lupus
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Mechanism and clinical use of AMB
- Binds to ergosterol, causes pores to form in cell membrane
- Use for systemic mycoses (coccidioidomycosis, blastomycosis, aspergillosis, candida, mucor)
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Mechanism and use of nystatin
- Binds to ergosterol, disrupts fungal membranes
- Use for oral candida (too toxic for systemic use)
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Mechanism and use of azoles
- Inhibit P450 14alpha demethylase, block sterol synthesis
- Use for systemic mycoses
- (Drug of choice in invasive aspergillosis)
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Drug of choice for pinworm infections
Mebendazole (disrupts glucose uptake and microtubule structure)
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Mechanism of praziquantel
Opens Ca channels in helminth cell membranes
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Mechanism of flucytosine
- Inhibits RNA synthesis by conversion to 5-FU and incorporation into RNA change, inhibits DNA synthesis by inhibition of thymidine synthase
- Use of systemic fungal infections
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Mechanism of caspofungin
Inhibits synthesis of beta glucans, blocks cell wall formation
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Mechanism and clinical use of terbinafine
- Inhibits squalene epoxidase
- Use to treat dermatophytoses
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Mechanism and clinical use of griseofulvin
- Deposits in keratin-rich tissues, inhibits microtubule function
- Use for dermatophyte infection
- Disulfiram-like reaction
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Mechanism and clinical use (2) of amantadine
- Blocks viral penetration and uncoating
- Causes release of DA from nerve terminals
- Used to treat influenza A and Parkinson's
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Mechanism and use of zanamivir and oseltamivir
- Inhibits influenza neuraminidase
- Side effects are flu-like symptoms. Heehee.
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Mechanism and clinical use of ribivarin
- Inhibits IMP dehydrogenase, blocks synthesis of gaunine nucleotides.
- Use to treat CMV and chronic hep C, in combo with alpha interferons
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Side effect of ribivarin
Hemolytic anemia
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Mechanism and clinical use of acyclovir
- A prodrug that is activated by bacterial thymidine kinase and causes chain termination.
- Use for HSV, VZV, and EBV
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Mechanism and clinical use of gancyclovir
- A prodrug that is activated by human cellular kinases and inhibits viral DNA polymerase
- First line treatment for CMV
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Dose limiting side effect of gancyclovir
BMS
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Mechanism and clinical use of foscarnet
- Inhibits viral DNA polymerase. Not a prodrug.
- Use to treat CMV retinitis when gancyclovir doesn't work
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Side effects of foscarnet
- Nephrotoxicity
- Hypocalcemia, due to Ca chelation--can be life threatening if patient is also on pentamidine, for PCP
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Names and side effects of protease inhibitors
- Squinavir, indinavir, ritonavir
- Ritonavir has lots of interactions with other drugs
- All protease inhibitors cause insulin resistance and lipodystrophy (buffalo hump, central obesity)
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Advantage of atazanavir
Causes less hyperglycemia and lypodystrophy than most protease inhibitors
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Non-nucleoside reverse transcriptase inhibitors (3)
- Nevirapine
- Efavirenz
- Delaviridine
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Side effect of efavirenz
Insomnia, nightmares
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Class and side effect of abacivir
- NRTI
- Severe allergic reactions
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Drug that blocks GP-41 and sterically inhibits HIV fusion with host cell
Enfuvirtide
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Drug that binds to CCR4
Maraviroc
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HIV integrase inhibitor
Raltegravir
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