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Drugs are bad, m'kay.... Flashcards

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1
Q

proton pump inhibitors (PPI)

A

oral once a day
IV: GI ulcer bleeding (not FDA approved)
SUPERIOR to H2 blockers
-prazole
irreversible inhibition of H/K ATPase
acid labile: ENTERIC COATING: erratic absorption
taken up by parietal cells and protonated to trap there: short T1/2 but effect lasts longer
metabolized by CYP2C19, 3A4
most effective for basal and food stimulated acid
take BEFORE FOOD
NO tolerance develops
Tx: hyperacidity: GERD, PUD, ulcer bleeding (not approved)
AE: slight increase in enteric infections, possible rebound acid secretion on withdrawal, possible increase risk of fractures
may be CI in Vit. B def. due to reduced absorption

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2
Q

H2 blocker

A

-tidine
competitive antagonists
take before bed: most effective for basal/overnight acid (doesn’t help for mealtime acid)
MODEST inhibition of gastric secretion from parietal cells
TOLERANCE within days
Tx: hyperacidity: GERD (only in mild cases), PUD (no longer recommended since PPI is superior and H. pylori assoc.); basically just for mild intermittent heartburn

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3
Q

ranitidine

A

H2 antagonist

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4
Q

cimetidine

A

H2 blocker
CYP inhibitor
drug interactions: phenytoin, warfarin, theophylline

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5
Q

nizatidine

A

H2 blocker

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6
Q

famotidine

A

H2 blocker

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7
Q

esomeprazole

A

PPI

drug interaction: possibly clopidogrel

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8
Q

lansoprazole

A

PPI

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9
Q

omeprazole

A

PPI
nasogastric or orogastric tube: in formulation with NaHCO3 for accelerated absorption rather than enteric coating: only PPI approved for upper GI bleed
also oral enteric coat form
CYP inhibitor
drug interactions: phenytoin, warfarin, diazepam, possibly clopidogrel

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10
Q

rabeprazole

A

PPI

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11
Q

mesalamine

A

5-aminosalicylic acid
Tx: ulcerative colitis (orally and rectally)
continue rectal until bleeding stops
stay on oral

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12
Q

bulk-forming laxatives

A

hydrophilic: form mass when mixed with water
in lumen: absorb and retain water and increase bulk in GI: stimulate stretch receptors to peristalsis
Tx: constipation

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13
Q

carboxymethylcellulose (Citrucel)

A

bulk-forming laxative: colloid mass
digestible
AE: impedes concurrent drug absorption
OFF LABEL: IBS-C

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14
Q

metamucil (Psyllium)

A 
bulk-forming laxative: gelatinous mass
absorb water
Tx: constipation, diarrhea
AE: flatulence, esophageal obstruction, choking, allergic rxn
may inhibit warfarin absorption
OFF LABEL: IBS-C
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15
Q

polycarbophils (Mitrolan)

A

bulk-forming laxative: polyacrylic resins
absorb 60-100x their weight in water
Tx: IBS-C
CI: Ca2+ release may chelate tetracyclines

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16
Q

osmotic (saline) laxative

A

Mg cations or other non absorbable molecules (Phosphate)
osmotic: retain water in lumen of GI tract: stimulate stretch receptors in increase cholinergic activity in ENS
Ex: Mg sulfate, hydroxide, citrate (citrate is cathartic); Pi containing given as enema or tablet
CKK release: increase intestinal motility and secretion
Tx: constipation

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17
Q

lactulose

A

osmotic laxative
non-absrobable disaccharide
fecal acidifier: metabolized to organic acids: lactic, acetic, formic: traps ammonia in ammonium form (slows diffusion into blood)
decreases glutamine and NH3 absorption
Tx: constipation; portal-systemic encephalopathy (adjunct to protein restriction and supportive Tx)

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18
Q

polyethylene glycol (PEG; Golytely)

A

osmotic laxative
dissolve in 4 L water
Use: bowel prep for colonoscopy, constipation, IBS-C
CI: bowel obstruction (nausea, vomiting, abdominal pain or distention) or perforation

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19
Q

docusate sodium (Colace)

A

anionic surfactant laxative
stool softener: reduce strain of defecation
NO direct stimulatory effect on peristalsis
Tx: constipation
CI: abdominal pain, vomiting
AE: irritate intestinal mucosa, increase absorption of other drugs
SHORT TERM use

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20
Q

chloride channel activators

A

laxative
increase volume and hydration of stool: stretch recpetors cause peristalsis
Tx: constipation, IBS-C
AE: abdominal distention and pain, diarrhea, flatulence

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21
Q

linaclotide

A

chloride channel activator: increase intestinal secretion and motility
CFTR
agonist of GC (guanylate cyclase) C2; cGMP; PKG: INDIRECT activation of chloride channel
Tx: constipation (idiopathic and IBS-C)
CI: in children less than 6 yrs

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22
Q

lubiprostone

A 
PGE1: chloride channel activator: increase intestinal secretion and motility
DIRECT: CLC channel
PKA INDEPENDENT
Tx: constipation (IBS-C)
AE: nausea
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23
Q

loperamide

A

opiate agonist
binds calmodulin
chloride secretion blocker and enteric neural blocker: direct action on sm. muscle to slow motility
Tx: diarrhea
AE: hyperglycemia, GI pain (N/V); somnolence
OFF LABEL: IBS-D

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24
Q

opiate antagonist

A

Tx: opiate induced constipation

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25
methylnaltrexone
opiate antagonist | AE: abdominal pain, flatulence, nausea, GI perforation (increased risk with compromised structural integrity)
26
naltrexone
opiate antagonist | AE: reverses analgesia (cautious in pain patients)
27
opiate agonist | What do you add and why?
1. decrease secretions and motility 2. increase muscle tone of sphincters 3. anti-spasmodics: decrease cramps Tx: diarrhea add ATROPINE: prevent opioid abuse
28
paregoric
opiate agonist add atropine Tx: diarrhea
29
diphenoxylate
opiate agonist add atropine Tx: diarrhea
30
stimulant laxatives
most potent laxatives act on large bowel 1. increase permeability of intestinal mucosa: increase back diffusion of water and electrolytes into lumen 2. increase contractility by stimulating myenteric plexus 3. stimulate PGs: increase secretions Tx: constipation
31
senna (anthraquinone)
stimulant laxative natural derivative: more gentle Use: bowel prep for colonoscopy AE: finger clubbing (with abuse), electrolyte imbalance and nephritis (excessive use); dark pigmentation of colonic mucosa, pink urine
32
bisacodyl (diphenylmethane; dulcolax)
stimulant (ENS) laxative prodrug: converted to desacetyl by bacteria enteric coat local axon and segmental reflexes stimulated: produces widespread peristalsis effective in SPINAL CORD INJURY AE: excessive fluid and electrolyte loss leading to colonic inflammatory response
33
castor oil
surfactant laxative rapid irritates mucosa: cathartic effect AE: colic, dehydration, electrolyte imbalance, uterine contraction
34
mineral oil
stool softener mixture of hydrocarbons Tx: constipation AE: anal irritation, fecal incontinence
35
poloxamer 188
``` non-ionic surfactant stool softener Tx: constipation AE: diarrhea CI: GI pain or N/V (promotes diarrhea) ```
36
anticholinergics | regular vs. quaternary
reduce vagal stimulation; anti-spasmodic Tx: diarrhea often combined with: benzodiazepine sedative REGULAR use: IBS diarrhea AE: indiscriminate anti-muscarinc activity QUATERNARY do NOT cross BBB: no CNS activity use: antispasmodic (alleviate cramps), antidiarrheal AE: xerostomia, vision change, bradycardia followed by tachycardia, impotence, bladder, flushing, annhidrosis
37
atropine
anticholinergic Tx: IBS use: combine with opioids to prevent abuse
38
dicyclomine
anticholinergic quaternary amine Tx: diarrhea, IBS more suited to alleviate cramps
39
glycopyrrolate
anticholinergic | OFF LABEL: IBS
40
propantheline
anticholinergic quaternary amine Tx: diarrhea more suited for urinary retention
41
bismuth subsalicylate
antidiarrheal, antiinflammatory 1. stimulates fluid/electrolyte absorption across the intestinal wall (antisecretory action) 2. inhibits PG synthesis (reduces intestinal inflammation and hyper motility) 3. binds toxins produced by E. coli use: H. pylori quadruple therapy, prevent traveler's diarrhea
42
methysergide
serotonin inhibitor Tx: carcinoid tumor inhibits serotonin induced diarrhea
43
serotonin antagonist
-setron: 5HT3 blockers | Tx: diarrhea or emesis
44
alosetron
serotonin (5HT3) antagonist little affinity for dompaminergic or other serotonin receptors Tx: IBS-diarrhea AE: COLITIS and SEVERE CONSTIPATION (BBW), arrhythmia, obstruction, perforation, toxic megacolon physician must enroll in PRESCRIBING PROGRAM use in combo with corticosteroids with/out benzodiazepines
45
amoxicillin
penicillin: binds PBP use: H. pylori triple therapy resistance does not develop AE: diarrhea
46
clarithromycin
``` macrolide use: H. pylori triple therapy low order of toxicity RESISTANCE: do NOT use more than once in H. pylori AE: taste disturbance, diarrhea ```
47
metronidazole
oral IV: complicated C. diff disease use: C. difficile (mild-mod), H. pylori triple therapy if allergic to penicillin RESISTANCE can develop: change dose if use again in H. pylori CI: PREGNANCY, BREAST FEEDING AE: peripheral neuropathy, disulfarim effects, diarrhea
48
tetracycline
Tx: H. pylori quadruple therapy resistance does not develop AE: diarrhea, teratogen
49
fidaxomicin
macrolide: inhibits bacterial RNA polymerases remains in GI: little systemization Tx: C. difficile (not recommended yet) SUPERIOR response (and less recurrence) in high risk C. diff to vanc AE: GI (N/V; abdominal pain, bleed) EXPENSIVE
50
stool transplant
colonoscopy (seems to be best way): blended with saline and filtered through gauze gastroscopy NG tube microbiome replacement recipient: STOP antibiotics 203 days before; colonoscopy prep to reduce stool; loperamide after transplant donor: no recent antibiotics; screen for pathogens; test for Hep. A/B/C, syphilis, HIV; milk of magnesia as softener Tx: C. difficile
51
vacomycin
oral IV: complicated C. diff disease rectal: ileus, distention, anatomic/surgical abnormalities pts (when oral can't reach colon) extended Tx with oral: 2nd recurrence cell wall synthesis inhibitor: binds D-ala, D-ala Tx: C. diff (severe, pregnant/lactating women) AE: hypokalemia, abdominal pain, diarrhea, N/V
52
aluminum hydroxide
antacids | AE: constipation
53
magnesium carbonate
antacids | AE: diarrhea
54
antacids
``` weak bases: neutralize acid most non-absorbable: Mg, Al, Ca avoid: absorbable/systemic agents (NaHCO3) rapid onset, short duration Tx: heartburn AE: Al or Ca based: constipation, Mg based: diarrhea; hypophosphatemia absorbable: alkalosis, Na overload Combo balances AE? ```
55
methylprednisolone
corticosterone use: adjunctive antiemetic for chemo used in combination with serotonin (5HT3) antagonist +/- benzodiazepine
56
misoprostol
PGE1 analogue use: protection against NSAID ulcers not used much: multiple doses and AE AE: abortifacient, diarrhea
57
octreotide
inhibits: serotonin, gastrin, VIP, secretin, motilin, pancreatic polypeptide use: GI carcinoid tumor AE: bradycardia, arrhythmia, gallstones monitor: blood glucose, thyroid function
58
aprepitant
antiemetic NK-1 antagonist use: adjunctive antiemetic for chemo metabolized by: CYP3A4
59
droperidol
post-synaptic GABA binder use: antiemetic: PONV selectively blocked postsynaptic alpha adrenergic receptors AE: vasodilation, hypotension
60
metoclopramide
antiemetic, gastric motility potentiator Tx: paralytic ileus AE: tardive dyskinesia (often irreversible movement disorder)
61
sucralfate
oral adherent proteinaceous exudate: coat over ulcer (about as useful as H2 blocker) can bind bile salts and other drugs (delay drug absorption) Tx: peptic ulcer (not really anymore); bile reflux into stomach (lacks evidence) AE: hyperglycemia in diabetics, use caution in impaired swallowing, constipation (has Al) CI: PPI, H2 blockers (sucralfate needs acidic pH to work)
62
sulfasalazine
anti-inflammatory immunomodulator Tx: ulcerative colitis AE: dizziness, male impotence, blood dyscrasia
63
protease inhibitors
-previr PO: possible interactions Tx: hepatitis C
64
simeprevir
2nd gen: protease inhibitor: NS3/4A Tx: chronic hepatitis C resistance develops more genotypes, once daily dose, fewer AE
65
sofosbuvir
``` CATALYTIC inhibitor: NS5B nucleotide/nucleoside inhibitor Tx: chronic hepatitis C AE: exacerbates IFN induced anemia PANGENOTYPIC ACTIVATION req: phosphorylation: delay in onset resistance uncommon P-gp ```
66
telaprevir
``` oral (multiple dose) 1st gen: protease inhibitor: NS3/4A resistance develops AE: RASH CI: teratogen (male/female) ```
67
boceprevir
oral 1st gen: protease inhibitor: NS3/4A resistance develops CI: teratogen (male/female)
68
ribavirin
inhibition of RNA dependent RNA polymerase enhance: T cell immune clearance inhibition of IMPDH (inosine monophosphate dehydrogenase) increase bioavailability: high fat meal Tx: chronic Hep. C AE: HEMOLYTIC ANEMIA, TERATOGEN (male and female), embryocidal CYP monitor: hematocrit synergism with IFN NO CYP
69
interferon- pegylated
IM or SC upregulates immune system: binds receptor: activate TK endoribonuclease: cleave ss RNA inhibitory effect on darn inhibition of viral penetration and uncoating and/or assembly and release enhanced lytic effects of cytotoxic T lymphocytes Tx: Hep. B and C AE: neuropsychiatric BBW (depression, seizure, confusion), thyrotoxicosis (in susceptible pts), flu like; BLOOD DYSCRASIA, LIVER can develop neutralizing Ab: lose responsiveness monitor: LFTs, TGs
70
adefovir
``` reverse transcriptase inhibitor 2P form produces chain termination prodrug: adefovir dipivoxil Tx: chronic Hep. B resistance develops cross-resistance: tenofovir monitor: LFT ```
71
reverse transcriptase inhibitors
``` oral false building blocks: nucleoside analogs inhibit DNA pol req. 3P for activity Tx: chronic Hep. B monitor: Cr/BUN, phosphate resistance develops NO CYP activity reduce dose in renal dysfunction AE: LIVER (lactic acidosis, steatosis) ```
72
emtricitabine
reverse transcriptase inhibitor | if HIV: give with tenofovir
73
entecavir
``` PREFERRED reverse transcriptase inhibitor food delays absorption long half life monitor: LFT ```
74
lamivudine
reverse transcriptase inhibitor cross-resistance: telbivudine short half life
75
telbivudine
reverse transcriptase inhibitor cross-resistance: lamivudine monitor: LFT
76
tenofovir
``` PREFERRED reverse transcriptase inhibitor: chain termination prodrug form: tenofovir disoproxil high fat meal: increase bioavailability AE: acute RENAL failure, BONE pain and fractures CI: NSAIDs, other nephrotoxic drugs give CALCIUM and VIT. D cross-resistance: adefovir if HIV: give with emtricitabine ```
77
infliximab
TNF-alpha antibody Tx: inflammatory bowel disease AE: immunosuppression (reactivation of latent TB, increased susceptibility to infection)
78
etanercept
soluble TNF receptor antagonist Tx: pancreatic CA AE: GI, prolonged bleeding, elevated LFTs, ocular
79
amifostine
IV cytoprotective agent: free radical scavenger use: radiation induced salivary gland damage AE: hypotension, diarrhea, N/V ORPHAN DRUG
80
TNF antagonists
?
81
cevimeline
parasympathomimetic: M3 (lacrimal and salivary) greater than M1 (CNS) CYP Tx: xerostomia
82
pilocarpine
parasympathomimetic: all M receptors (greater CNS activity) Tx: Sjogren's syndrome, xerostomia caution: psychosis
83
parasympathomimetics
oral Tx: xerostomia CI: asthma, closed angle glaucoma caution: angina, breastfeeding, arrhythmia, cardiac disease, kids, cholelithiasis, COPD, bronchitis, operating machinery, geriatric, MI, nephrolithiasis, pregnancy
84
rifaximin
oral rifampin analog: inhibits bacterial DNA dependent RNA pol GI confined Tx: portal systemic encephalopathy AE: peripheral edema, ascites, dizziness, nausea; fecal urgency and constipation; GI OFF LABEL: IBS-D
85
bevacizumab
anti-VEGF mAB Tx: colorectal CA AE: GI perforation, dehiscence, bleeding
86
EGFR inhibitors
AE: rash
87
cetuximab
anti-EGFR mAB | Tx: colorectal CA
88
erlotinib
EGFR TKI Tx: pancreatic CA AE: edema, increased LFTs
89
glutamic acid
counterbalances HCl deficiency in stomach | Tx: gastric CA
90
imatinib, STI-571
bcr-abl TKI Tx: GIST (gastrointestinal stromal tumor) AE: GI dysfunction, fluid retention, edema
91
sorafenib
multi-kinase inhibitor Tx: liver CA AE: hand-foot syndrome
92
sunitinib
multi targeting TKI Tx: GIST AE: thrombocytopenia, QT prolongation, GI perforation
93
trastuzumab
HER2 monoclonal Ab Tx: gastric CA AE: LVEF dysfunction, cardiomyopathy
94
tricyclic antidepressants
Tx IBS pain
95
hyoscyamine
Tx IBS pain
96
H. pylori triple therapy
complex: poor patient adherence 1. PPI 2. clarithromycin and amoxicillin (metronidazole if allergic)
97
H. pylori quadruple therapy
complex: poor patient adherence 1. PPI or H2 blocker 2. bismuth 3. metronidazole and tetracycline
98
wheat dextrin (Benefiber)
isolated, non-digestible carbs MoA: increase delivery of water to colon, increase bulk, reduce pressure in sigmoid colon results in more formed stools Tx: constipation
99
glycerin
osmotic and lubricant laxative suppository Tx: constipation
100
General AE of laxatives
overuse leads to constipation that takes days to accumulate bulk lag in defection interpreted as continued constipation take more laxatives can make BOWEL UNRESPONSIVE
101
octreotide (somatostatin)
``` decreases vasodilators (like Glucagon) Tx: varices due to portal HTN, hepatorenal syndrome ```
102
vasopressin
Tx: varices due to portal HTN
103
diuretics
Tx: ascites due to portal HTN
104
pentoxifylline
TNFa inhibitor | Tx: ALD
105
desferoxamine
IV Fe chelator Tx: hemochromatosis
106
deferasirox
oral Fe chelator Tx: hemochromatosis use when patient has low hemoglobin (thalassemia, sickle cell)
107
penicillamine
Cu chelator Tx: Wilson's AE: lupus, hepatotoxicity, neuropathy, GI
108
trientene
Cu chelator Tx: Wilson's AE: sideroblastic anemia
109
tetrathiomolybdate
Cu chelator | Tx: Wilson's
110
zinc
Cu chelator, cofactor in NH3 metabolism Tx: Wilson's, hepatic encephalopathy AE: GI
111
N-acetylcysteine
give no matter how late they present and even in low acetaminophen levels Tx: acetaminophen overdose, or regular dose in alcoholic
112
What is the goal for making drugs to Tx Hep C?
increase compliance once daily dosing: combination pills and take fewer times a day also to Tx DIFFERENT GENOTYPES downside: expensive
113
dasabuvir
``` inhibitor: NS5B ALLOSTERIC: non-nucleotide/side Tx: chronic hepatitis C CYP2C8, P-gp AE: well tolerated, dermal, GI ```
114
paritaprevir
2nd gen: protease inhibitor: NS3/4A Tx: chronic hepatitis C resistance develops more genotypes, once daily dose, fewer AE
115
ledipasavir
inhibitor: NS5A Tx: chronic hepatitis C
116
ombitasvir
inhibitor: NS5A Tx: chronic hepatitis C
117
daclatasvir
inhibitor: NS5A Tx: chronic hepatitis C
118
-previr
NS3/4A inhibitor protease inhibitor Tx: Hep C
119
-asvir
``` NS5A inhibitor: prevents replication unknown function PANGENOTYPIC action: highly conserved site Tx: Hep C CYP interactions ```
120
-buvir
``` NS5B inhibitor polymerase inhibitor Tx: Hep C CYP interactions req. ACTIVATION: phosphorylation ```
121
Why would you give combination drugs for chronic HBV?
diminish resistance
122
Hep C drugs in general interaction
CYP
123
Initial approach to IBS Tx
lifestyle and dietary modification | reserve drugs for mod. to severe
124
TCA
CNS reduce repute of NE and serotonin some have anticholinergic activity Tx: IBS-D
125
SSRI
CNS selective serotonin reuptake inhibitor Tx: IBS-D
126
probiotics
Tx: IBS | small benefit; not routinely recommended
127
Drugs that cause xerostomia
1. antihistamines 2. decongestants 3. antidepressants 4. antipsychotics 5. antihypertensives 6. anticholinergics
128
saliva substitutes
Tx: xerostomia | no strong evidence but might as well
129
Drugs to Tx Sialorrhea 1. label 2. off label
1. glycopyrrolate | 2. botulinum toxin, scopolamine
130
For some drugs like Fosamax/alendronate why are there such specific instructions for taking the pill?
can get irritation and bleeding ulcers if it gets stuck
131
pop-bottle method
tablet: sinks fill bottle, put tablet on tongue and close lips around bottle, take drink and purse lips (sucking), swallow bottle will squeeze (don't get air in)
132
lean-forward technique
capsule: floats | put capsule on tongue, take sip of water, bend head forward then swallow

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