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GER MS2 UNIT 6 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

BAL

A
  • chelator; solubilized in peanut oil
  • give IM
  • Tx: prior to CaNa2EDTA in treatment of Pb encephalopathy (prevent redistribution of Pb t brain); inorganic Hg and Ag toxicity
  • must alkalinize urine to prevent acidic urine destabilization that leads to decreased renal excretion and metal-induced renal toxicity
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2
Q

succimer/ DMSA

A
  • chelator; MC used
  • only approved oral chelating agent
  • Tx: Pb, Ar, Hg, Cd
  • generally well tolerated; mild transient AST/ALT elevation
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3
Q

CaNa2EDTA

A
  • chelator
  • Tx: Pb; +BAL for severe poisoning/ encephalopathy
  • SE: monitor renal function (nephrotoxic due to Pb chelate)
  • do not confuse with NA2EDTA (severe hypoCa)
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4
Q

Prussian Blue

A
  • chelator; stays in gut, not absorbed until it grabs metal
  • Tx: thallium and Ce
  • well tolerated, not systemically absorbed
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5
Q

Deferoxamine/ DFO

A
  • chelator; free Fe and Fe transported between transferrin and ferritin (mobilizes intracellular Fe from spleen, liver, BM)
  • SE: intrinsic toxicity (acute lung injury)
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6
Q

Antacids

A

-Tx: ulcers, GERD
calcium carbonate
-sodium bicarbonate: rarely used due to systemic alkalosis
-Mg hydroxide/carbonate: liquid based (acts fast); diarrhea; Mg toxicity in presence of renal disease
-Al hydroxide: constipation; safe for use in renal failure (helps elimate PO4)

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7
Q

Atropine sulfate
Propantheline
Metantheline Br

A
  • anticholinergic; reduces acid secretion and spasm (relaxes bowel SM)
  • Tx: ulcers, IBS
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8
Q

H2 receptor blockers

A
  • inhibits 50-80% of 24hr acid production
  • Tx: ulcers; prophylatic for stress ulcers, GERD
  • rebound acidity if stopped suddenly
  • cimetidine, ranitidine: interferes with P450
  • famotidine, nizatidine
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9
Q

misoprostol

A
  • PGE analog; decrease acid production, increase mucous and HCO3 secretion
  • Tx: ulcers when PG production decreased (RA patients taking NSAIDs)
  • not very effective
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10
Q

H/K/ATPase Inhibitors

A
  • inhibit >90% of 24hr acid secretion (better than H2 antagonists), require acidic environment to activate
  • Tx: ulcers
  • SE: P450 interference
  • omeprazole, lansoprazole, dexlansoprazole: also treats H. pylori, GERD
  • rabeprazole, pantoprazole (IV, no P450), esomeprazole
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11
Q

sucralfate

bismuth salts

A
  • mechanical protectors; coat ulcer crater, increase mucosal resistance
  • Tx: ulcers, H. pylori
  • SE: Al toxicity possible in renal failure; bismuth turns BMs black
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12
Q

metochlopramide

A
  • promotility agent; increases motor tone in LES (prevent reflex) and stomach (esp. antrum, improves gastric emptying); peripheral and CNS DA antagonist (CRTZ)
  • Tx: GERD, antiemetic, gastroparesis
  • 1/day for good effects
  • SE: hand tremor, extra pyramidal symptoms
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13
Q

cisapride

A
  • promotility agent; DA antagonist increases motor tone in LES and stomach
  • Tx: GERD, gastroparesis
  • SE: sudden cardiac death (restricted use)
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14
Q

dompareidone

A
  • promotility agent; improves gastric tone

- Tx: gastroparesis

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15
Q

acute IBD and UC treatments

A
  • sulfasalazine, olsalazine, mesalamine
  • -anti-inflammatory agents; work from lumen to reduce inflammation
  • SE: toxicity from systemic absorption of sulfapyridine (sulfasalazine most toxic)
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16
Q

prednisone for IBD treatment

A

acute and chronic therapy for IBD; can be given systemically or as enema

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17
Q

immunosuppressors for chronic IBD

A
  • azathioprine: purine antimetabolite
  • cyclosporine: suppresses T helper and T suppressor lymphocytes
    methotrexate: decreased synthesis of inflammatory mediators
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18
Q

biologics for chronic IBD: TNFa binders/neutralizers

A
  • infliximab
  • adalimumab
  • certolizumab
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19
Q

biologics for chronic IBD: a4 integrin binders

A
  • prevents immune cells from invading tissue
  • natalizumab
  • vedolizumab
  • ustekinumab
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20
Q

prochlorperazine

A
  • phenothiazine (neuroleptic); CNS DA antagonist (reduction of CRTZ stimulation)
  • Tx: anti-emetic
  • SE: extrapyramidal (torticollis)
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21
Q

promethazine

A
  • phenothiazine (neuroleptic); antiH1 receptor, anticholinergic
  • Tx: anti-emetic
  • SE: somnolence (esp in elderly)
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22
Q

trimethobenzamide

A
  • unknown effect on CRTX
  • Tx: anti-emetic
  • low side effect profile; ok for kids
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23
Q

THC

A
  • suppresses CRTZ, probably anticholinergic
  • Tx: anti-emetic
  • often administered in pill form
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24
Q

serotonin (5HT3) receptor antagonists

A
  • odansetron: v. safe for vomiting of any type (including drug-induced); 6mo +
  • granesitron
  • golasetron
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25
Q

loperamide
diphenoxylate
codeine sulfate

A
  • opiod agonist; less penetration to CNS; stimulates mu receptors in GI, increased rectal tone leading to segmentation of colon and disruption of peristalsis leading to increased absorption time
  • loperamide: IBS-D; can use in kids
  • diphenoxylate, codeine: contraindicated in kids (respiratory suppression)
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26
Q

metamucil

A
  • colloid; absorbs water

- Tx: constipation

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27
Q

bismuth subsalicylate

A
  • pectin, absorbs water

- Tx: diarrhea

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28
Q

irritant laxatives

A
  • irritate lumen of colon, cause peristaltic contractions

- castor oil, cascara sagrada, senna, bisacodyl, phenolphthalein

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29
Q

osmotic laxatives

A
  • draw water into colon

- Mg citrate/ sulfate, sodium sulfate, milk of magnesia

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30
Q

bulk forming laxatives

A

psyllium seed, methylcellulose, sodium carbomethylcellulose

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31
Q

lubricant and fecal softeners

A

mineral oil, dioctyl sodium sulfo-succinate, poloxalkol

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32
Q

receptor active agents for constipation

A
  • lubiprostone: PG analog; activates Cl channel on intestinal epithelial cells
  • linaclotide: peptide agonist of cGMP leads to Cl and HCO3 secretion
  • naloxegol: mu opiod receptor antagonist (opiod induced constipation)
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33
Q

dicyclomine HCll

hyoscyamine sulfate

A

-anticholinergic; reduces spasm in IBS

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34
Q

alosetron

A
  • serotonergic antagonist
  • Tx: IBS-D
  • SE: ischemic bowel, constipation
35
Q

tegaserod maleate

A
  • serotonergic agonist

- Tx: IBS-C

36
Q

natural PCNs (PCN G and V)

A
  • form complex with PBP, prevent extracellular transpeptidase activity
  • Tx: mainly gram + aerobes; DOC syphilis, strep, poor staph
  • HSRs; Sz at high dose
  • not effective against B-lactamase-producers
37
Q

penicillinase-resistance PCNs (oxacillin, nafcillin, diclozacillin)

A
  • PCN with bulky side group to stop penicillinases
  • Tx: MSSA (superior to vanc)
  • HSRs
  • oxacillin: hepatotoxicity, neutropenia
  • nafcillin: neutropenia, thrombophlebitis
38
Q

aminoPCNs (ampicillin, amoxicillin)

A
  • semisynthetic PCNs with special side group allows improved pentration into gram - membrane
  • Tx: strep (DOC enterococcus); listeria (gram +; empirical for high risk patients)
  • HSRs (non IgE rash)
  • amox better absorbed than amp PO
  • not effective against penicillinsdr-producing staph
39
Q

ES-PCNs (piperacillin, ticarcillan)

A
  • extended aminoPCN spectrum

- Tx: aminoPCN + proteus, klebsiella, serratia, enterobacter, pseudomonas

40
Q

zosyn (piperacillin + tazobactam); augmentin (amonxicillin + clavulanate)

A
  • suicide inhibitors; retention of PCN spectrum with increased activity against B-lactamase organisms (s. aureus, gut anaerobes, haemophilus, e. coli)
  • augmentin: diarrhea; not effective against pseudomonas
41
Q

1st gen cephalosporins (cefazolin, cephalexin)

A
  • complex with PBP, prevent extracelluar transpeptidase activity
  • Tx: broader spectrum than PCNs; PEcK (proteus, e. coli, klebsiella); MSSA (good choice for non severe PCN allergy)
  • cefazolin: DOC surgical prophylaxis
42
Q

2nd gen cephalosporins (cefuroxime, cefoxitin, cefotetan)

A

-1st gen + haemophilus; anaerobic activity

43
Q

3rd gen cephalosporins (ceftazadime, cefpodoxime, ceftriaxone)

A
  • ceftaz: pseudomonas; post neurosurg meningitis prophylaxis
  • ceftriax: strep, enhanced gram - coverage, CAP, complex UTI, CSF lyme; causes biliary sludging, neonates: precipitation with Ca containing solutions–> kernicterus
  • *higher assoc w/ C. diff than other classes
44
Q

4th gen cephalosporins (cefepime)

A
  • 3rd gen + pseudomonas
  • SE: akinetic Szs
  • crosses BBB (zwitterion)
45
Q

5th gen cephalosporin (ceftaroline)

A
  • has side chain that acts as trojan horse (looks like cell wall), allows acces to PBP2a
  • Tx: gram+ (MRSA, MSSA); gram - similar to ceftriaxone
46
Q

ceftazidime/avibactam

A
  • ES-cephalosporin/b-lactamase inhibitor

- Tx: MDRgram -; reserve for dire circumstances

47
Q

ceftolozane/tazobactam

A

-increased activity against pseudomonas, ESBLs

48
Q

carbapenams (imipenem, meropenem, ertapenem, doripenem)

A
  • broad spectrum (MRSA)
  • ertepenem: not effectiv against pseudomonas
  • imipenem: do not use for meningitis; risk of szs if dose not adjusted for renal failure
  • significant reduction in valproate levels (esp. meropenem)
  • low cross reactivity with PCN
49
Q

aztreonam

A

Tx: gram - aerobic bacilli including pseudomonas

50
Q

vancomycin

A
  • binds rapidly/irreversibly to DalaDala on peptide side chain of membrane bound precursor
  • Tx: G+s; PO for C. diff
  • SE: IgE HSRs, red man syndrome, dose dependent nephrotox, immune mediated thrombocytopenia
51
Q

lipoglycopeptides (dalbavancin, telavancin, oritavancin)

A
  • vanc analogs, inhibit transglycosylation
  • vanc + VRE and more anaerobes
  • SE: metallic taste, nausea, teratogen
52
Q

daptomycin

A
  • penetrates bacterial cell wall, forms channel for subsequent leakage of intracellular ions
  • inactivated by surfactant (no pneumonia)
  • Tx: G+ cocci; VRE, VRSA
  • SE: myalgia, rhabdo (monitor CK), eosinophilic pneumonia
53
Q

colistin

A
  • penetrates bacterial cell wall, forms channel for subsequent leakage of intracellular ions
  • Tx: G- only; reserved for resistant pseudomonas
54
Q

1st gen fluoroquinolone (cipro)

A
  • inhibits DNA gyrase at low concentrations
  • Tx: enterobactericeae, atypical UTIs
  • SE: GI, AMS, long QT, tendon rupture
55
Q

2nd gen fluoroquinolone (levo, moxi)

A
  • inhibits DNA gyrase at low concentrations, inhibits topoisomerase IV at high concentrations
  • Tx: adds pneumococcus
  • levo: pseudomonas
  • moxi: anaerobes (GI and abdomenal infections), no pseudomonas
  • SE: long QT (moxi>levo>cipro)
56
Q

metronidazole

A
  • nucleic acid synthesis inhibitor; use below diaphragm
  • reduced to active free radical under anaerobic conditions, damages bacterial and protozoal DNA
  • Tx: anaerobes (not actinomyces and peptostrepto); DOC c. Diff, H. pylori
  • SE: metallic taste, disulfram-like rxn (blocks aldehyde dehydrogenase); CNS tox szs, neuropathy with LT/high dose
57
Q

rifampin

A
  • nucleic acid synthesis inhibitor; inhibits DNA dependent RNA pol (stops RNA transcription)
  • potent CYP 450 inducer
  • Tx: TB, S. aureus
  • SE: serious flu-like HSR (fever, myalgia, interstitial nephritis, thrombocytopenia, hemolytic anemia
  • NEVER as monotherapy (risk of resistance)
58
Q

anti TB drugs

A
  • rifampin: inhibits DNA dependent RNA pol (stops RNA transcription)
  • isoniazid: inhibits mycolic acid synthesis; hepatitis (monitor LFTs), neurotox, memory loss, psychosis (use pyroxidine)
  • pyrazinamide: unknown mechanism; N/V, hepatotoxicity
  • ethambutol: inhibits arabinosyl transferase involved in cell wall synthesis; neuropathy, optic neuritis
59
Q

aminoglycosides (gentamicin, tobramycin)

A
  • inhibits 30S ribosome (produces inactive proteins; bactericidal)
  • O2 dependent uptake (no anaerobic coverage)
  • synergistic with cell wall active agents for enterococcus
  • Tx: gram - rods
  • SE: oto/nephrotoxicity
60
Q

tetracyclines (doxy, mino)

A
  • inhibits 30S ribosome; blocks access of tRNA anticodon
  • resistance with efflux pump
  • Tx: gram + (s. pneumo, MRSA), intracellular pathogens (mycoplasma, chlamydia, legionella, rickettsia), lyme
  • SE: GI, photosensitivity, hyperpigmentation, Fanconi-like syndrome if expired, pill esophagitis, discolors teeth of kids, avoid in pregnancy
61
Q

tigecycline

A
  • glycylcyline; inhibits 30S ribosome; prevents efflux out of cell
  • Tx: reserve for carbapenem resistant enterobac
  • SE: N/V/D, backbox increase all cause mortality
62
Q

clindamycin

A
  • binds 50S ribosome at A site blocking peptide bond formation
  • Tx: use above diaphragm; CA-MRSA/MSSA, strep; no gram -
  • SE: antibiotic associated diarrhea, c. diff
63
Q

azithromycin

A
  • macrolide; binds 50S and blocks translocation by interference with tRNA release following peptide bond formation
  • Tx: uncomplicated URI/LRI; intracellular pathogens (mycoplasma, chlamydia, legionella)
  • SE: GI distress PO (similar to motilin); TdP
  • long t1/2, v. high tissue distribution
64
Q

linezolid

tedizolid

A
  • bind 50S ribosome, inhibits peptidyl transferase
  • Tx: gram+ (MRSA, MSSA), enterococcus including VRE
  • SE: BM suppression, thrombocytopenia, mitochondrial toxin (lactic acidosis, optic neuritis, peripheral neuropathy)
  • irreversibly inhibits MOA (risk for serotonin syndrome)
65
Q

bactrim (trimethoprim + sulfamethoxazole)

A

-trimetho: DHFR inhibitor; hyperK in severe renal insufficiency
-sulfametho: dihydropterate synthase inhibitor
Tx: empiric pneumocystis pneumonia and toxo in immunocomp; listeria

66
Q

acyclovir
pencyclovir (poor bioavailability)
valacyclovir
famciclovir

A
  • purine analogs; phosphorylated to cause viral DNA chain termination
  • vala and fam: prodrugs with better bioavailability
  • Tx: HSV, VZV (higher dose required, MIC doubles for VZV)
  • SE: CNS changes
67
Q

ganciclovir

A
  • purine analog; phosphorylated to cause viral DNA chain termination
  • Tx: CMV tx and prophylaxis
  • SE: neutropenia, thrombocytopenia
68
Q

foscarnet

A
  • pyrophosphate congener; directly inhibits HSV DNS pol or HIV RT
  • Tx: broad spectrum (HSV/VZV/CMV and RNA viruses including HIV)
69
Q

oseltamivir (MC)
zamamivir
peramivir (IV use only for critically ill)

A
  • neuraminidase inhibitor; prevents viral release from host cells
  • Tx: influenza A and B (within 1-2 days of symptoms)
  • SE: neuropsych toxicity, bronchospasm with zanamivir (inhaled)
70
Q

nonnucleoside RT inhibitors (NRTIs)

A
  • HIV: zidovudine (use in pregnancy; macrocytic anemia), abacavir (HLA assoc HSR)
  • HIV+HBV: lamivudine, emtricitabine, tenofovir (MC; nephrotoxicity)
71
Q

NNRTIs (efavirenz MC, nevirapine, rilpivirine, etravirine)

A
  • inhibit RT through direct enzyme inhibition
  • Tx: HIV
  • SE: CNS tox, vivid dreams, efavirenz is teratogenic
  • affects P450 metabolism
72
Q

HIV protease inhibitors (ritonavir, fosamprenavir, atazanavir, darunavir, lopinavir)

A
  • prevent cleavage of protein chain into functional subunits
  • *ritonavir: one of the most potent CYP 450 inhibitors known; PI + ritonavir boosts blood levels of PI
  • SE: lipdystrophy syndrome
73
Q

NS3/4A PIs (semiprevir, bocepravir, telapravir)

A
  • prevents viral maturation through inhibition of protein synthesis
  • Tx: HCV
74
Q

HCV NS5A inhibitor (ledipasvir, daclatasvir, ombitasvir)

A
  • inhibit NS5A protein required for viral replication
  • Tx: HCV
  • few side effects
75
Q

enfuvitide

maraviroc

A
  • CCR5 antagonist (targets host cell), prevents viral entry
  • Tx: HIV
  • use when patient has developed resistance
76
Q

HIV integrase inhibitors (raltegravir, elvitegravir, dolutegravir)

A
  • binds HIV integrase (necessary for insertion of viral DNA into human genome)
  • first line HIV therapy
  • very safe
77
Q

NS5B polymerase inhibitor (sofosbuvir, paritaprevir)

A
  • compete with viral nucleotide to cause viral chain termination of RNA pol
  • Tx: HCV
  • few side effects
78
Q

ribavirin

A
  • nucleoside analog
  • Tx: HCV
  • SE: hemolytic anemia, teratogenic
79
Q

interferon

A
  • induce interferon-stimulating genes to establish antiviral state within cells
  • Tx: HCV and others
  • SE: flu-like symptoms
80
Q

polyenes (amphoB, nystatin)

A
  • forms pores in cell membrane, allows K and Mg leak
  • Tx: broad antifungal spectrum; nystatin topically
  • SE: NEPHROTOXIC; infusion syndrome with AmphoB
  • better SE when solubilized in lipid but $$$
81
Q

triazoles

A
  • inhibit ergosterol synthesis (cell membrane)
  • SE: hepatotoxicity, **CYP 450 inhibition
  • posaconazole: broadest spectrum; prophylaxis in immunocomp
  • voriconazole (MC): aspergillus, candida
  • itraconazole: histoplasmosis, candida
  • fluconazole: severe thrush/ esophageal candida;
82
Q

topical azoles

A
  • inhibit ergosterol synthesis (cell membrane)
  • efinazonazole: candida, tinea
  • tolnaftate, terbinafine: topical dermatophytes (limited against candida)
83
Q

echinocandin

A
  • capsofungin, micofungin, anidulafungin
  • inhibit synthesis ß1,3Dglucan (component of cell wall)
  • Tx: candida
  • only IV (big molecule)
  • low side effect profile
84
Q

flucytosine

A

-nucleic acid synthesis inhibitor
-prodrug (only PO)
+amphoB: DOC for crypto meningitis; candida
-SE: BM tox (like chemotherapy)

GER MS2 UNIT 6 (1 decks)

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