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Therapeutic Drugs > GI > Flashcards

GI Flashcards

1
Q

Acid Reducing Drugs

A 
Antacids
- Mg and Al hydroxide
- CaCO3
- NaHCO3
H2 Antagonists
- Ranitidine
- Cimetidine
- Famotidine
- Nizatidine
Proton Pump Inhibitors
- Omeprazole
- Esomeprazole
- Lansoprazole
- Dexlansoprazole
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2
Q

Antacids

A 
Mechanism:
- chemically neutralize acid that is present
Short lived
Use:
- occasional GERD or dyspesia
- discriminate chest pain MI vs acid reflux
Drugs:
MgOH
- diarrhea
- hyperMg in renal pts
AlOH 
- constipation
- hypophosphatemia
- decrease drug adsorption
CaCO3 - produce CO2 - belching/bloating
- constipation
- hyperCa
- kidney stones
- acid rebound
NaHCO3 - produce CO2 - belching/bloating
- systemic alkalosis in renal pts
- fluid retention - Na
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3
Q

H2 antagonists

A

Mechanism:
- prevent histamine induced activation of H release - block histamine binding H2 receptors on parietal cells, no cAMP production
- decrease proton and pepsin secretion in dose dependent manner
Use:
- heartburn and dyspesia, GERD
- added to PPI for nocturnal breakthrough
- stress ulcer prophylaxis
- peptic ulcer healing and zollinger-ellison syndrome, but prefer PPIs
Tachyphylaxis
Drugs:
Cimetidine
- large doses: inhibits cyp450
- antiandrogenic - gynecomastia and galactorrhea
- cardiovascular problems
- confusion in elderly
Ranitidine
Famotidine
Nizatidine

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4
Q

Proton Pump Inhibitors

A

Mechanism:
- directly block parietal H-K ATPase to decrease H secretion into lumen, irreversible block
- needs conversion to sulfenamide via acid
Most effective when parietal cells create the most acid - take before meal, preferably before 1st meal of day
Don’t take with H2 blockers cuz need the acid
Use:
- peptic ulcer disease, GERD, reflux esophagitis
- H pylori with abx
- Zollinger Ellison syndrome
- IV form used for upper GI bleed to reduce need for intervention and reduce risk of rebleeding after intervention
Drugs:
Omeprazole
Lansoprazole
Dexlansoprazole
Pantoprazole
Esomeprazole
Adverse events:
- common: headache, abdominal pain, nausea, diarrhea, flatulence
- p450 metabolism so drug interactions (clopidogrel be aware)
- increased risk of GI infxns - check for C diff if pt has diarrhea
- increase risk of fracture
- increased risk of pneumonia
- risk of hypomagnesemia - check Mg levels

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5
Q

Mucosal Protectants

A

Bismuth Salts
Sucralfate
Misoprostol

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6
Q

Bismuth Salts

A 
Action:
- coats ulcers and inflamed areas
Use:
- gastroenteritis - symptoms of nausea, dyspepsia, diarrhea
- traveler's diarrhea prophylaxis
Side effects:
- black tongue and feces
- interactions with anticoagulants
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7
Q

Sucralfate

A

Action:
- forms temporary coating on ulcers, protects them from acid and digestive enzymes
Take before meals
Use:
- stress ulcer prophylaxis (not much anymore)
- bile reflux gastritis and esophageal ulcers post variceal banding

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8
Q

Misoprostol

A 
Prostaglandin E1 analog
Action:
- stimulates mucous production
- decreases acid secretion
Uses:
- induces labor
- use in pts with chronic NSAID use cuz of ulcer risk with reduced PGE1
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9
Q

GI motility agents

A 
Erythromycin - Abx
Cholinomimetics
- bethanechol, neostigmine
Dopamine receptor antagonists
- metoclopramide, domperidone
Serotonin - metoclopramide
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10
Q

Erythromycin

A 
Macrolide abx
Action:
- activates motilin receptors on smooth muscle of antrum and small intestine
Use:
- diabetic gastroperesis
Adverese events:
- tachyphylaxis
- QT prolongation
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11
Q

Cholinomimetics

A 
Neostigmine, Bethanechol
- increase GI motility big time
Use:
- Ogilive syndrome (IV)
Side effects:
- cholinergic
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12
Q

Metoclopramide, Domperidone

A

Dopamine receptor antagonists - pre and post synaptic
Action:
- promote gastric/intestinal motility through Ach release
- increase gastric tone
- improve antroduodenal coordination
- accelerate gastric emptying
Side effects of metoclopramide:
- reversible: somnolence, feeling jittery, headache, diarrhea
- serious side effects: tardive dyskinesia, dystonia, neuroleptic malignant syndrome

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13
Q

Laxatives

A 
Bulk forming 
- Fiber - psyllium
Osmotic Agents
- Magnesium salts
- polyethylene glycol
- Lactulose
- PED
- milk of magnesia
Stimulants
- Bisocodyl
- Senna
- Castor oil
- Cascara
Stool Softeners
- Docusate
- Mineral Oil
Cl channel secretion 
- Lubiprostone
GC-C agonist
- Linaclotide
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14
Q

Psyllium, Polycarbophil

A 
Fiber laxative
- Bulk laxatives
Action:
- form gels in the colon causing water retention and distention
- increase peristalsis
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15
Q

Polyethylene glycol, Mg salts, milk of magnesia

A

Osmotic laxative
Action:
- draw H2O into intestinal lumen via osmosis resulting in softer/liquid stools and distension induced peristalsis

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16
Q

Bisacodyl/Dulcolax, Senna

A

Stimulant laxative
Action:
- stimulates colonic smooth muscle and causes H2O accumulation in lumen

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17
Q

Docusate

A

Surfactant
Stool softener - laxative
Action:
- causes fat/H2O to mix

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18
Q

Mineral oil

A

Lubrictant
Stool softener - laxative
Action:
- prevents H2O absorption by coating stool
Can inhibit absorption of fat-soluble vitamins

19
Q

Lubiprostone

A

Cl channel secretion laxative
Action:
- activates ClC-2 chloride channels, chloride secretion, Na follows and water follows

20
Q

Linaclotide

A

GC-C agonist laxative
Action:
- binds GC-C receptor, increases cGMP, increases Cl and bicarbonate secretion, therefore water
- activates CFTR

21
Q

Anti-diarrheal

A 
Do not use if GI infxn or inflammation is present
- toxic megacolon
Antimotility
- Loperamide
- Diphenoxylate-atropine
- Tincture of opium
Absorbents
- Bismuth subsalicylate
- Fiber
- Bile acid binding resins - cholestryramine, colestipol
Antisecretory
- Octreotide
- Somatostatin
22
Q

Loperamide, Diphenoxylate/atropine, Tincture of Opium

A

Anti-diarrhea
Antimotility agents - opiates
Action:
- act on opioid receptor in gut
- act directly on circular and longitudinal intestinal muscles
- inhibit peristalsis and prolong transit time of material within gut
- increases viscosity since more time for contact
- diminishes fluid and electrolyte loss
- increases anal sphincter tone
Caution:
- do not combine loperamide and tincutre of opium with other CNS depressants cuz sedation and respiratory depression

23
Q

Bismuth busalicyclate

A 
Anti-diarrhea
Absorbent
- anti-secretory
- anti-microbial
- anti-inflammatory
Caution:
- salicylate, so do not use with aspirin or anticoagulants cuz of blood thinning effect
- reye syndrome - do not use with viral infxn in children
24
Q

Fiber

A

Anti-diarrhea
Bulking agent - stool regulator
Action:
- absorbs intraluminla water and improves consistency of diarrhea

25
Q

Cholestryramine, Colestipol

A

Anti-diarrhea
Bile acid binding resins
Action:
- form non-absorbable complex with bile acids
- bile acids stimulate colonic secretion, causing secretory diarrhea
- bile acids absorbed in terminal ileum
Caution:
- seperate from other meds by 2 hrs cuz binds them

26
Q

Ocreotide/somatostatin

A

Anti-diarrhea
Antisecretory agent
Action:
- reduces fluid and electrolyte secretion by stomach and pancreas
- mild antimolity effect
- promotes intestinal electrolyte absorption
- suppresses neuroendocrine tumor release of peptides that cause intestinal hypersecretion of electrolytes and water

27
Q

Anti-nausea and emesis

A 
Anticholinergic
- scopolamine
Antihistamine
- meclizine, dimenhydrinate
DA antagonist
- prochlorperazine, promethazine
5HT antagonist 
- ondansetron, dolasetron, granisetron
Cannabinoid
- dronabinol
Neurokinin antagonist
- aprepitant
28
Q

Scopolamine

A 
Antiemetic
Anticholinergic
Action:
- blocks Ach at M1 receptor
Use:
- prevents motion sickness
- prevents chemo induced nausea
Side effects:
- anticholinergic: dry mouth, sedation, blurred vision, confusion, urinary retention
29
Q

Meclizine, Dimenhydrinate

A

Antiemetic
Antihistamine
Action:
- block H1 and has anticholinergic effects
Use:
- tx motion sickness
- hyperemesis gravidarum
Side effects:
- sedating; meclizine less than dimenhydrinate
- anticholinergic: dry mouth, sedation, blurred vision, confusion, urinary retention

30
Q

Promethazine, Prochlorperazine

A 
Antiemetic
DA antagonist
Action:
- D2 receptor blocker, some anticholinergic effects
Use:
- prophylaxis preop; postop
- motion sickness
- toxic and metabolic induced nausea
- migraine related nausea
- hyperemesis gravidarum
Side effects:
- anticholinergic: dry mouth, sedation, blurred vision, confusion, urinary retention
- sedation
- extrapyramidal - tardive dyskinesia, pseudo-parkinsonism, acute dystonia
- QT prolongation
31
Q

Ondansetron, Dolasetron, Granisetron

A 
Antiemetic
5HT antagonist
Action:
- act on vagal nerve terminals and chemoreceptor trigger zone, antagonize serotonin receptors
Use:
- multiple settings for antiemesis
- chemotherapy induced nausea/vomit
- migraine related nausea
- postop nausea/vomit
- hyperemesis gravidarum
Side effects:
- QT prolongation
32
Q

Dronabinol (delta 9 THC)

A 
Antiemetic 
Cannabinoid
Action:
- agonize CB1 receptor
Use:
- chemo induced nausea vomit
- appetite stimulant in AIDS/HIV
Side effects:
- euphoria, paranoia, CNS depression, abuse potential
33
Q

Aprepitant, Fosaprepitant

A 
Antiemtic
NK antagonist
Action:
- substance P/neurokinin I receptor antagonist
Use:
- prevention of acute and delayed chemo induced and post-op nausea/vomit
- give before chemo or anesthesia
Adverse events:
- hiccups
- fatigue
- increased risk of infxn
34
Q

Anti-inflammatories

A

Aminosalicylates
- sulfasalazine, mesalamine, balsalazide, olsalazine
Glucocorticoids
- prednisone, methylprednisolone, budesonide
Immunomodulators
- methotrexate, 6MP/azathioprine
Biologics
- infliximab, adalimumab, certolizumab, natalizumab

35
Q

Mesalamine, Balsalazide, Olsalazine

A 
5-Aminosalicylates
Anti-inflammatory
Active in colon
5-ASA is active component
Use: UC and Crohn's
Adverse events:
- mild GI and headache occasionally 
- hypersensitivity rxns - pancreatitis, pneumonitis
- paradoxical worsening of disease
- chronic interstitial nephritis
36
Q

Sulfasalazine

A 
Aminosalicylate
Anti-inflammatory
Prodrug release in colon
Use: UC and Crohn's
Adverse events:
- frequent GI (N/V), CNS and hematologic side effects - megaloblastic anemia, leukopenia
- agranulocytosis - monitor for this
- decreased folic acid absorption - treat with folic acid
37
Q

Prednisone, methylprednisolone

A 
Glucocorticoid
Use: 
- induce remission in both UC and Crohn's
- not maintenance
- must be tapered off
Adverse events:
- muscle wasting
- lipodystrophy - buffalo hump, abdominal fat
- thinning of skin
- moon facies
- HTN
- poor wound healing
- osteoporosis
- hyperglycemia
- increased suspectibility to infxn
38
Q

Budesonide

A 
Non-systemic glucocorticoid
- controlled ileal or colonic release
High first pass metabolism in liver
Use:
- induction for Crohn's and UC
- requires taper
Smaller pts get more systemic effects
Adverse events:
- muscle wasting
- lipodystrophy - buffalo hump, abdominal fat
- thinning of skin
- moon facies
- HTN
- poor wound healing
- osteoporosis
- hyperglycemia
- increased suspectibility to infxn
39
Q

6-MP, Azathiopurine

A

Purine antimetabolites
- 6MP metabolized by TPMT, HPRT, and xanthine oxidase
- HPRT to 6TGN - active metabolite
- TPMT to 6-MMP - inactive metabolite
Action:
- inhibits nucleotide synthesis, decreases lymphocytes, decreases pro-inflammatory cytokine production
Use:
- maintenance of remssion in UC and Crohn’s; 3 mo to reach therapeutic levels
Adverse events:
- leukopenia, thrombocytopenia from 6-TGN
- hepatotoxicity from 6-MMP
- infxn risk increased
- increased risk of malignancy
- avoid use with allopurinol

40
Q

Methotrexate

A 
Immunomodulator
- folate anti-metabolite
- inhibits dihydrofolate reductase
- results in apoptosis of T cells
Use:
- maintenance of remission in Crohn's
Adverse events:
- hepatotoxicity
- myelosuppression
- interstitial lung disease
- mucositis
- teratogenic
Give folic acid to all pts
41
Q

anti-TNFa

A 
mAb against TNF-a
Use:
- induction and maintenance of remission in Crohn's and UC
Infliximab - UC and CD
Adalimumab - UC and CD
Certolizumab - CD only
Adverse events:
- infxn - screen for latent TB and hepatitis B
- myelosuppression
- increased risk of malignancy
- psoriasis
- drug induced lupus
- dymyelination syndrome
42
Q

Natalizumab

A

Anti-integrin
- blocks leukocyte migration from blood vessels to sites of inflammation
Adverse events:
- Progressive multifocal leukoencephalopathy

43
Q

Vedolizumab

A

Anti-integrin

  • gut specific
  • blocks leukocyte migration from blood vessels to sites of inflammation

Therapeutic Drugs (7 decks)

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