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

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

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
Q

methylnaltrexone

A

opiate antagonist

AE: abdominal pain, flatulence, nausea, GI perforation (increased risk with compromised structural integrity)

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26
Q

naltrexone

A

opiate antagonist

AE: reverses analgesia (cautious in pain patients)

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27
Q

opiate agonist

What do you add and why?

A
  1. decrease secretions and motility
  2. increase muscle tone of sphincters
  3. anti-spasmodics: decrease cramps
    Tx: diarrhea
    add ATROPINE: prevent opioid abuse
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28
Q

paregoric

A

opiate agonist
add atropine
Tx: diarrhea

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29
Q

diphenoxylate

A

opiate agonist
add atropine
Tx: diarrhea

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30
Q

stimulant laxatives

A

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

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31
Q

senna (anthraquinone)

A

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

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32
Q

bisacodyl (diphenylmethane; dulcolax)

A

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

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33
Q

castor oil

A

surfactant laxative
rapid
irritates mucosa: cathartic effect
AE: colic, dehydration, electrolyte imbalance, uterine contraction

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34
Q

mineral oil

A

stool softener
mixture of hydrocarbons
Tx: constipation
AE: anal irritation, fecal incontinence

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35
Q

poloxamer 188

A 
non-ionic surfactant
stool softener
Tx: constipation 
AE: diarrhea
CI: GI pain or N/V (promotes diarrhea)
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36
Q

anticholinergics

regular vs. quaternary

A

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

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37
Q

atropine

A

anticholinergic
Tx: IBS
use: combine with opioids to prevent abuse

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38
Q

dicyclomine

A

anticholinergic
quaternary amine
Tx: diarrhea, IBS
more suited to alleviate cramps

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39
Q

glycopyrrolate

A

anticholinergic

OFF LABEL: IBS

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40
Q

propantheline

A

anticholinergic
quaternary amine
Tx: diarrhea
more suited for urinary retention

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41
Q

bismuth subsalicylate

A

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
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42
Q

methysergide

A

serotonin inhibitor
Tx: carcinoid tumor
inhibits serotonin induced diarrhea

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43
Q

serotonin antagonist

A

-setron: 5HT3 blockers

Tx: diarrhea or emesis

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44
Q

alosetron

A

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

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45
Q

amoxicillin

A

penicillin: binds PBP
use: H. pylori triple therapy
resistance does not develop
AE: diarrhea

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46
Q

clarithromycin

A 
macrolide
use: H. pylori triple therapy
low order of toxicity
RESISTANCE: do NOT use more than once in H. pylori
AE: taste disturbance, diarrhea
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47
Q

metronidazole

A

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

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48
Q

tetracycline

A

Tx: H. pylori quadruple therapy
resistance does not develop
AE: diarrhea, teratogen

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49
Q

fidaxomicin

A

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

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50
Q

stool transplant

A

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

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51
Q

vacomycin

A

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

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52
Q

aluminum hydroxide

A

antacids

AE: constipation

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53
Q

magnesium carbonate

A

antacids

AE: diarrhea

54
Q

antacids

A 
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
Q

methylprednisolone

A

corticosterone
use: adjunctive antiemetic for chemo
used in combination with serotonin (5HT3) antagonist +/- benzodiazepine

56
Q

misoprostol

A

PGE1 analogue
use: protection against NSAID ulcers
not used much: multiple doses and AE
AE: abortifacient, diarrhea

57
Q

octreotide

A

inhibits: serotonin, gastrin, VIP, secretin, motilin, pancreatic polypeptide
use: GI carcinoid tumor
AE: bradycardia, arrhythmia, gallstones
monitor: blood glucose, thyroid function

58
Q

aprepitant

A

antiemetic NK-1 antagonist
use: adjunctive antiemetic for chemo
metabolized by: CYP3A4

59
Q

droperidol

A

post-synaptic GABA binder
use: antiemetic: PONV
selectively blocked postsynaptic alpha adrenergic receptors
AE: vasodilation, hypotension

60
Q

metoclopramide

A

antiemetic, gastric motility potentiator
Tx: paralytic ileus
AE: tardive dyskinesia (often irreversible movement disorder)

61
Q

sucralfate

A

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
Q

sulfasalazine

A

anti-inflammatory immunomodulator
Tx: ulcerative colitis
AE: dizziness, male impotence, blood dyscrasia

63
Q

protease inhibitors

A

-previr
PO: possible interactions
Tx: hepatitis C

64
Q

simeprevir

A

2nd gen: protease inhibitor: NS3/4A
Tx: chronic hepatitis C
resistance develops
more genotypes, once daily dose, fewer AE

65
Q

sofosbuvir

A 
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
Q

telaprevir

A 
oral (multiple dose)
1st gen: protease inhibitor: NS3/4A
resistance develops
AE: RASH
CI: teratogen (male/female)
67
Q

boceprevir

A

oral
1st gen: protease inhibitor: NS3/4A
resistance develops
CI: teratogen (male/female)

68
Q

ribavirin

A

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
Q

interferon- pegylated

A

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
Q

adefovir

A 
reverse transcriptase inhibitor
2P form produces chain termination
prodrug: adefovir dipivoxil
Tx: chronic Hep. B
resistance develops
cross-resistance: tenofovir
monitor: LFT
71
Q

reverse transcriptase inhibitors

A 
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
Q

emtricitabine

A

reverse transcriptase inhibitor

if HIV: give with tenofovir

73
Q

entecavir

A 
PREFERRED
reverse transcriptase inhibitor
food delays absorption 
long half life
monitor: LFT
74
Q

lamivudine

A

reverse transcriptase inhibitor
cross-resistance: telbivudine
short half life

75
Q

telbivudine

A

reverse transcriptase inhibitor
cross-resistance: lamivudine
monitor: LFT

76
Q

tenofovir

A 
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
Q

infliximab

A

TNF-alpha antibody
Tx: inflammatory bowel disease
AE: immunosuppression (reactivation of latent TB, increased susceptibility to infection)

78
Q

etanercept

A

soluble TNF receptor antagonist
Tx: pancreatic CA
AE: GI, prolonged bleeding, elevated LFTs, ocular

79
Q

amifostine

A

IV
cytoprotective agent: free radical scavenger
use: radiation induced salivary gland damage
AE: hypotension, diarrhea, N/V
ORPHAN DRUG

80
Q

TNF antagonists

A

?

81
Q

cevimeline

A

parasympathomimetic: M3 (lacrimal and salivary) greater than M1 (CNS)
CYP
Tx: xerostomia

82
Q

pilocarpine

A

parasympathomimetic: all M receptors (greater CNS activity)
Tx: Sjogren’s syndrome, xerostomia
caution: psychosis

83
Q

parasympathomimetics

A

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
Q

rifaximin

A

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
Q

bevacizumab

A

anti-VEGF mAB
Tx: colorectal CA
AE: GI perforation, dehiscence, bleeding

86
Q

EGFR inhibitors

A

AE: rash

87
Q

cetuximab

A

anti-EGFR mAB

Tx: colorectal CA

88
Q

erlotinib

A

EGFR TKI
Tx: pancreatic CA
AE: edema, increased LFTs

89
Q

glutamic acid

A

counterbalances HCl deficiency in stomach

Tx: gastric CA

90
Q

imatinib, STI-571

A

bcr-abl TKI
Tx: GIST (gastrointestinal stromal tumor)
AE: GI dysfunction, fluid retention, edema

91
Q

sorafenib

A

multi-kinase inhibitor
Tx: liver CA
AE: hand-foot syndrome

92
Q

sunitinib

A

multi targeting TKI
Tx: GIST
AE: thrombocytopenia, QT prolongation, GI perforation

93
Q

trastuzumab

A

HER2 monoclonal Ab
Tx: gastric CA
AE: LVEF dysfunction, cardiomyopathy

94
Q

tricyclic antidepressants

A

Tx IBS pain

95
Q

hyoscyamine

A

Tx IBS pain

96
Q

H. pylori triple therapy

A

complex: poor patient adherence
1. PPI
2. clarithromycin and amoxicillin (metronidazole if allergic)

97
Q

H. pylori quadruple therapy

A

complex: poor patient adherence
1. PPI or H2 blocker
2. bismuth
3. metronidazole and tetracycline

98
Q

wheat dextrin (Benefiber)

A

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
Q

glycerin

A

osmotic and lubricant laxative
suppository
Tx: constipation

100
Q

General AE of laxatives

A

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
Q

octreotide (somatostatin)

A 
decreases vasodilators (like Glucagon)
Tx: varices due to portal HTN, hepatorenal syndrome
102
Q

vasopressin

A

Tx: varices due to portal HTN

103
Q

diuretics

A

Tx: ascites due to portal HTN

104
Q

pentoxifylline

A

TNFa inhibitor

Tx: ALD

105
Q

desferoxamine

A

IV
Fe chelator
Tx: hemochromatosis

106
Q

deferasirox

A

oral
Fe chelator
Tx: hemochromatosis
use when patient has low hemoglobin (thalassemia, sickle cell)

107
Q

penicillamine

A

Cu chelator
Tx: Wilson’s
AE: lupus, hepatotoxicity, neuropathy, GI

108
Q

trientene

A

Cu chelator
Tx: Wilson’s
AE: sideroblastic anemia

109
Q

tetrathiomolybdate

A

Cu chelator

Tx: Wilson’s

110
Q

zinc

A

Cu chelator, cofactor in NH3 metabolism
Tx: Wilson’s, hepatic encephalopathy
AE: GI

111
Q

N-acetylcysteine

A

give no matter how late they present and even in low acetaminophen levels
Tx: acetaminophen overdose, or regular dose in alcoholic

112
Q

What is the goal for making drugs to Tx Hep C?

A

increase compliance
once daily dosing: combination pills and take fewer times a day
also to Tx DIFFERENT GENOTYPES
downside: expensive

113
Q

dasabuvir

A 
inhibitor: NS5B
ALLOSTERIC: non-nucleotide/side
Tx: chronic hepatitis C
CYP2C8, P-gp
AE: well tolerated, dermal, GI
114
Q

paritaprevir

A

2nd gen: protease inhibitor: NS3/4A
Tx: chronic hepatitis C
resistance develops
more genotypes, once daily dose, fewer AE

115
Q

ledipasavir

A

inhibitor: NS5A
Tx: chronic hepatitis C

116
Q

ombitasvir

A

inhibitor: NS5A
Tx: chronic hepatitis C

117
Q

daclatasvir

A

inhibitor: NS5A
Tx: chronic hepatitis C

118
Q

-previr

A

NS3/4A inhibitor
protease inhibitor
Tx: Hep C

119
Q

-asvir

A 
NS5A inhibitor: prevents replication
unknown function
PANGENOTYPIC action: highly conserved site
Tx: Hep C
CYP interactions
120
Q

-buvir

A 
NS5B inhibitor
polymerase inhibitor 
Tx: Hep C
CYP interactions
req. ACTIVATION: phosphorylation
121
Q

Why would you give combination drugs for chronic HBV?

A

diminish resistance

122
Q

Hep C drugs in general interaction

A

CYP

123
Q

Initial approach to IBS Tx

A

lifestyle and dietary modification

reserve drugs for mod. to severe

124
Q

TCA

A

CNS
reduce repute of NE and serotonin
some have anticholinergic activity
Tx: IBS-D

125
Q

SSRI

A

CNS
selective serotonin reuptake inhibitor
Tx: IBS-D

126
Q

probiotics

A

Tx: IBS

small benefit; not routinely recommended

127
Q

Drugs that cause xerostomia

A
  1. antihistamines
  2. decongestants
  3. antidepressants
  4. antipsychotics
  5. antihypertensives
  6. anticholinergics
128
Q

saliva substitutes

A

Tx: xerostomia

no strong evidence but might as well

129
Q

Drugs to Tx Sialorrhea

  1. label
  2. off label
A
  1. glycopyrrolate

2. botulinum toxin, scopolamine

130
Q

For some drugs like Fosamax/alendronate why are there such specific instructions for taking the pill?

A

can get irritation and bleeding ulcers if it gets stuck

131
Q

pop-bottle method

A

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
Q

lean-forward technique

A

capsule: floats

put capsule on tongue, take sip of water, bend head forward then swallow

GI (12 decks)

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