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
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
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)
4
Q
Prussian Blue
A
- chelator; stays in gut, not absorbed until it grabs metal
- Tx: thallium and Ce
- well tolerated, not systemically absorbed
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)
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)
7
Q
Atropine sulfate
Propantheline
Metantheline Br
A
- anticholinergic; reduces acid secretion and spasm (relaxes bowel SM)
- Tx: ulcers, IBS
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
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
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
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
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
13
Q
cisapride
A
- promotility agent; DA antagonist increases motor tone in LES and stomach
- Tx: GERD, gastroparesis
- SE: sudden cardiac death (restricted use)
14
Q
dompareidone
A
- promotility agent; improves gastric tone
- Tx: gastroparesis
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)
16
Q
prednisone for IBD treatment
A
acute and chronic therapy for IBD; can be given systemically or as enema
17
Q
immunosuppressors for chronic IBD
A
- azathioprine: purine antimetabolite
- cyclosporine: suppresses T helper and T suppressor lymphocytes
methotrexate: decreased synthesis of inflammatory mediators
18
Q
biologics for chronic IBD: TNFa binders/neutralizers
A
- infliximab
- adalimumab
- certolizumab
19
Q
biologics for chronic IBD: a4 integrin binders
A
- prevents immune cells from invading tissue
- natalizumab
- vedolizumab
- ustekinumab
20
Q
prochlorperazine
A
- phenothiazine (neuroleptic); CNS DA antagonist (reduction of CRTZ stimulation)
- Tx: anti-emetic
- SE: extrapyramidal (torticollis)
21
Q
promethazine
A
- phenothiazine (neuroleptic); antiH1 receptor, anticholinergic
- Tx: anti-emetic
- SE: somnolence (esp in elderly)
22
Q
trimethobenzamide
A
- unknown effect on CRTX
- Tx: anti-emetic
- low side effect profile; ok for kids
23
Q
THC
A
- suppresses CRTZ, probably anticholinergic
- Tx: anti-emetic
- often administered in pill form
24
Q
serotonin (5HT3) receptor antagonists
A
- odansetron: v. safe for vomiting of any type (including drug-induced); 6mo +
- granesitron
- golasetron
25
loperamide
diphenoxylate
codeine sulfate
- 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)
26
metamucil
- colloid; absorbs water
| - Tx: constipation
27
bismuth subsalicylate
- pectin, absorbs water
| - Tx: diarrhea
28
irritant laxatives
- irritate lumen of colon, cause peristaltic contractions
| - castor oil, cascara sagrada, senna, bisacodyl, phenolphthalein
29
osmotic laxatives
- draw water into colon
| - Mg citrate/ sulfate, sodium sulfate, milk of magnesia
30
bulk forming laxatives
psyllium seed, methylcellulose, sodium carbomethylcellulose
31
lubricant and fecal softeners
mineral oil, dioctyl sodium sulfo-succinate, poloxalkol
32
receptor active agents for constipation
- 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)
33
dicyclomine HCll
| hyoscyamine sulfate
-anticholinergic; reduces spasm in IBS
34
alosetron
- serotonergic antagonist
- Tx: IBS-D
- SE: ischemic bowel, constipation
35
tegaserod maleate
- serotonergic agonist
| - Tx: IBS-C
36
natural PCNs (PCN G and V)
- 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
penicillinase-resistance PCNs (oxacillin, nafcillin, diclozacillin)
- PCN with bulky side group to stop penicillinases
- Tx: MSSA (superior to vanc)
- HSRs
- oxacillin: hepatotoxicity, neutropenia
- nafcillin: neutropenia, thrombophlebitis
38
aminoPCNs (ampicillin, amoxicillin)
- 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
ES-PCNs (piperacillin, ticarcillan)
- extended aminoPCN spectrum
| - Tx: aminoPCN + proteus, klebsiella, serratia, enterobacter, pseudomonas
40
zosyn (piperacillin + tazobactam); augmentin (amonxicillin + clavulanate)
- 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
1st gen cephalosporins (cefazolin, cephalexin)
- 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
2nd gen cephalosporins (cefuroxime, cefoxitin, cefotetan)
-1st gen + haemophilus; anaerobic activity
43
3rd gen cephalosporins (ceftazadime, cefpodoxime, ceftriaxone)
- 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
4th gen cephalosporins (cefepime)
- 3rd gen + pseudomonas
- SE: akinetic Szs
- crosses BBB (zwitterion)
45
5th gen cephalosporin (ceftaroline)
- 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
ceftazidime/avibactam
- ES-cephalosporin/b-lactamase inhibitor
| - Tx: MDRgram -; reserve for dire circumstances
47
ceftolozane/tazobactam
-increased activity against pseudomonas, ESBLs
48
carbapenams (imipenem, meropenem, ertapenem, doripenem)
- 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
aztreonam
Tx: gram - aerobic bacilli including pseudomonas
50
vancomycin
- 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
lipoglycopeptides (dalbavancin, telavancin, oritavancin)
- vanc analogs, inhibit transglycosylation
- vanc + VRE and more anaerobes
- SE: metallic taste, nausea, *teratogen*
52
daptomycin
- 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
colistin
- penetrates bacterial cell wall, forms channel for subsequent leakage of intracellular ions
- Tx: G- only; reserved for resistant pseudomonas
54
1st gen fluoroquinolone (cipro)
- inhibits DNA gyrase at low concentrations
- Tx: enterobactericeae, atypical UTIs
- SE: GI, AMS, long QT, tendon rupture
55
2nd gen fluoroquinolone (levo, moxi)
- 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
metronidazole
- 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
rifampin
- 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
anti TB drugs
- 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
aminoglycosides (gentamicin, tobramycin)
- 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
tetracyclines (doxy, mino)
- 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
tigecycline
- 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
clindamycin
- 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
azithromycin
- 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
linezolid
| tedizolid
- 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
bactrim (trimethoprim + sulfamethoxazole)
-trimetho: DHFR inhibitor; hyperK in severe renal insufficiency
-sulfametho: dihydropterate synthase inhibitor
Tx: empiric pneumocystis pneumonia and toxo in immunocomp; listeria
66
acyclovir
pencyclovir (poor bioavailability)
valacyclovir
famciclovir
- 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
ganciclovir
- purine analog; phosphorylated to cause viral DNA chain termination
- Tx: CMV tx and prophylaxis
- SE: neutropenia, thrombocytopenia
68
foscarnet
- pyrophosphate congener; directly inhibits HSV DNS pol or HIV RT
- Tx: broad spectrum (HSV/VZV/CMV and RNA viruses including HIV)
69
oseltamivir (MC)
zamamivir
peramivir (IV use only for critically ill)
- 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
nonnucleoside RT inhibitors (NRTIs)
- HIV: zidovudine (use in pregnancy; macrocytic anemia), abacavir (HLA assoc HSR)
- HIV+HBV: lamivudine, emtricitabine, tenofovir (MC; nephrotoxicity)
71
NNRTIs (efavirenz MC, nevirapine, rilpivirine, etravirine)
- inhibit RT through direct enzyme inhibition
- Tx: HIV
- SE: CNS tox, vivid dreams, efavirenz is teratogenic
- affects P450 metabolism
72
HIV protease inhibitors (ritonavir, fosamprenavir, atazanavir, darunavir, lopinavir)
- 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
NS3/4A PIs (semiprevir, bocepravir, telapravir)
- prevents viral maturation through inhibition of protein synthesis
- Tx: HCV
74
HCV NS5A inhibitor (ledipasvir, daclatasvir, ombitasvir)
- inhibit NS5A protein required for viral replication
- Tx: HCV
- few side effects
75
enfuvitide
| maraviroc
- CCR5 antagonist (targets host cell), prevents viral entry
- Tx: HIV
- use when patient has developed resistance
76
HIV integrase inhibitors (raltegravir, elvitegravir, dolutegravir)
- binds HIV integrase (necessary for insertion of viral DNA into human genome)
- first line HIV therapy
- very safe
77
NS5B polymerase inhibitor (sofosbuvir, paritaprevir)
- compete with viral nucleotide to cause viral chain termination of RNA pol
- Tx: HCV
- few side effects
78
ribavirin
- nucleoside analog
- Tx: HCV
- SE: hemolytic anemia, teratogenic
79
interferon
- induce interferon-stimulating genes to establish antiviral state within cells
- Tx: HCV and others
- SE: flu-like symptoms
80
polyenes (amphoB, nystatin)
- 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
triazoles
- 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
topical azoles
- inhibit ergosterol synthesis (cell membrane)
- efinazonazole: candida, tinea
- tolnaftate, terbinafine: topical dermatophytes (limited against candida)
83
echinocandin
- capsofungin, micofungin, anidulafungin
- inhibit synthesis ß1,3Dglucan (component of cell wall)
- Tx: candida
- only IV (big molecule)
- low side effect profile
84
flucytosine
-nucleic acid synthesis inhibitor
-prodrug (only PO)
+amphoB: DOC for crypto meningitis; candida
-SE: BM tox (like chemotherapy)
