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ABBEY MSII U6 > Pharm GI drugs 2 > Flashcards

Pharm GI drugs 2 Flashcards

1
Q

GERD pathophys

A
  • lower esophageal sphincter disorder (inappropriate relaxation, low resting tone, anatomical alteration)
  • acid hyper secretion (esp after meals)
  • decreased acid clearance due to impaired peristalsis or abnormal saliva production
  • delayed gastric emptying and/or duodenogastric reflux of bile salts and pancreatic enzymes
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2
Q

lifestyle measures for treatment of GERD

A
  • elevation of the head of the bed
  • avoidance of food or liquids 2-3 hr before bed
  • avoidance of fatty or spicy food, cigarettes, alcohol
  • weight loss
  • liquid antacid
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3
Q

what is used to treat persistent symptoms of GERD?

A
  • alginic acid antacids
  • promotility drugs (cisapride or metoclopramide)
  • H2 receptor blockers (-tidines)
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4
Q

what is used to treat non response or relapse or barrett’s?

A
  • H2 receptor blocker - regular or double dose
  • H2 receptor blocker + promotility agent
  • proton pump inhibitors (-prazole)
  • antireflux surgery
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5
Q

what are the promotility drugs?

A
  • metochlopramide (peripheral dopamine antagonist)
  • cisapride (dopamine antagonist)
  • domperidone
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6
Q

metochlopramide mechanism, treats, SE

A
  • increases motor tone in lower esophageal sphincter and stomach - also peripheral and CNS (vomiting) dopamine antagonist
  • treats: GERD, anti-emetic, gastroparesis
  • SE: hand tremor, possible extra-pyramidal
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7
Q

cisapride mechanism, treats, SE

A
  • mechanism: increases motor tone in lower esophageal sphincter and stomach
  • treats: GERD, gastroparesis
  • SE: sudden cardiac death
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8
Q

domperidone mechanism, treats, SE

A
  • mechanism: improves gastric tone
  • treats: gastroparesis
  • SE: none listed
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9
Q

pathophys of vomiting

A
  • mediated by chemo receptor Trigger Zone (CRTZ) and vomiting center in the medulla
  • stimulated by: local irritation of stomach (drugs, alcohol, infection), CNS stimulation (infection, inflammation, mass effects, headache and drugs), pain
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10
Q

what are the metabolic consequences of vomiting?

A

dehydration, electrolyte disturbances

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11
Q

what is used for treatment of vomiting?

A

antiemetics (central actions of CRTZ)

  1. phenothiazines
  2. benzamide derivatives
  3. tetrahydro cannabinol
  4. serotonin receptor antagonists
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12
Q

what are the phenothiazines?

A
  1. prochlorperazine

2. prometazine

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13
Q

prochlorperazine mechanism

A

probable CNS interaction with dopaminergic receptor-antagonist (leading to reduction of stimulation in the CRTZ in the medulla)
ANTI-EMETIC - phenothiazine

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14
Q

prochlorperazine SE

A

extra pyramidal (torticollis - the neck muscles contract, causing the head to twist to one side.)

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15
Q

promethazine mechanism

A

(antihistaminic H1 receptor) - anticholinergic

ANTI-EMETIC - phenothiazine

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16
Q

what are the benzamide derivatives? what are their SE?

A
  1. trimethobenzamide
  2. metochlopramide
    SE: extra pyramidal symptoms
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17
Q

trimethobenzamide mechanism

A

unknown effect on CRTZ

ANTI-EMETIC - benzamide derivative

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18
Q

trimethobenzamide SE

A

low-side effect profile; possible extra-pyramidal symptoms

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19
Q

metochlopramide mechanism

A

CNS and peripheral dopaminergic receptor antagonism

ANTI-EMETIC, GERD, gastroparesis use

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20
Q

tetrahydro cannabinol mechanism

A

THC - suppress the CRTZ by probable anticholinergic mechanism
ANTI-EMETIC

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21
Q

what are the serotonin receptor antagonists?

A

-SETRON!!!
1. ondansetron
2. granesitron
3. dolasetron
used as anti-emetics

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22
Q

serotonin receptor antagonists SE

A

headache, dizziness, somnolence

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23
Q

what is gastroparesis?

A

outlet obstruction and/or loss of gastric tone (e.g. DM)

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24
Q

what is used in treatment of gastroparesis?

A

promotility drugs (metochlopramide, cisapride, domperidone)

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25
Q

what are the 5 types of diarrhea?

A
  1. acute diarrhea
  2. traveler’s diarrhea
  3. chronic and recurrent diarrhea
  4. chronic diarrhea of unknown origin
  5. incontinence
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26
Q

what are the causes of acute diarrhea?

A
  1. viral, bacterial, parasitic infection
  2. food poisoning
  3. drugs (acute or chronic)
  4. fecal impaction
  5. heavy metal poisoning (acute or chronic)
27
Q

what are the causes of traveler’s diarrhea?

A
  1. bacterial infections (enterotoxins, invasion of mucosa and inflammation)
  2. viral and parasitic infections
28
Q

what is the mechanism of toxin mediated diarrhea?

A

increased production of cAMP = more Cl in lumen = osmotic diarrhea

29
Q

what are the causes of chronic and recurrent diarrhea?

A
  1. irritable bowel syndrome
  2. inflammatory bowel disease
  3. parasitic infections
  4. malabsorption syndromes, lactase deficiency
  5. drugs (acute or chronic)
  6. heavy metal poisoning (acute or chronic)
30
Q

what are the causes of chronic diarrhea of unknown origin ?

A
  1. surreptitious laxative abuse
  2. irritable bowel syndrome
  3. unrecognized inflammatory bowel disease
  4. bile acid malabsorption
31
Q

what are the causes of incontinence?

A
  1. sphincter dysfunction (anal surgery, episiotomy or tear during childbirth, anal crohn’s, diabetic enuropathy, idiopathic)
32
Q

what are the goals of diarrhea treatment?

A

decrease GI secretion - present less fluid to colon

and decrease GI motility - more time for reabsorption of water and decrease cramps

33
Q

what drug classes are used for treatment of diarrhea?

A
  1. anticholinergics
  2. opioid agonists
  3. colloids and pectins
  4. antibiotics
34
Q

anticholinergic drugs and mechanism for treatment of diarrhea

A

atropine sulfate

-relax all bowel smoothe uscle

35
Q

opioid agonists drugs and mechanism for treatment of diarrhea

A

loperamide, diphenoxylate, codeine sulfate

-these drugs have less penetration to CNS - interact with mu or sigma receptors in GI tract

36
Q

difference between loperamide and diphenoxylate / codeine sulfate

A

diphenoxylate and codeine sulfate combined with atropine which relaxes bowel smooth muscle

37
Q

what is the contraindication for diphenoxylate and codeine sulfate?

A

children (respiratory suppression)

38
Q

colloids and pectins: drugs and mechanism for treatment of diarrhea

A

metamucil (colloid) and kaopectate (pectin)

-absorb water but don’t prevent potential dehydration

39
Q

risk of metamucil and kaopectate (colloid and pectin)

A

doesn’t prevent potential dehydration

40
Q

what is used for treatment of constipation?

A
  1. irritants/stimulants
  2. osmotic cathartics
  3. bulk-forming (hydrophilic colloids)
  4. lubricant and fecal softeners
  5. receptor active agents
41
Q

what are the irritants/stimulants used for constipation?

A
  1. castor oil
  2. cascara sagrada
  3. senna extract
  4. bisacodyl
  5. phenolphthalein
42
Q

what are the osmotic cathartics used for constipation?

A
  1. magnesium citrate
  2. magnesium sulfate (epsom salt)
  3. sodium sulfate
  4. milk of magnesia
43
Q

what are the bulk-forming hydrophilic colloids?

A
  1. psyllium seed
  2. methylcellulose
  3. sodium carboxymethylcellulose
44
Q

what are the lubricants and fecal softeners used for constipation?

A
  1. mineral oil
  2. dioctyl sodium sulfo-succinate
  3. poloxalkol
45
Q

what are the receptor active agents? what are their mechanisms?

A
  1. lubiprostone (chloride channel activator - osmotic)
  2. linaclotide (stimulates cGMP resulting in chloride and bicarb secretion)
  3. naloxegol (mu opioid receptor antagonist)
46
Q

when is naloxegol used?

A

for people on chronic opioids (mu opioid receptor antagonist)

47
Q

inflammatory bowel disease pathophys

A

all are idiopathic (probably autoimmune)

48
Q

crohn’s disease

A

inflammatory bowel of the small bowel, especially ileum

49
Q

ulcerative colitis

A

inflammatory bowel of large bowel

50
Q

granulomatous (crohn’s) colitis

A

inflammatory bowel large bowel

51
Q

acute therapy for inflammatory bowel disease

A
  1. anti-inflammatories
  2. corticosteroids
  3. antibiotics
52
Q

what are the anti-inflammatories used in inflammatory bowel disease?

A
  1. mesalamine (delayed release -used for terminal ileum)
  2. sulfasalazine (toxicity from systemic absorption of sulfapyridine)
  3. olsalazine (less toxic than sulfasalazine)
53
Q

which corticosteroid is used in inflammatory bowel disease?

A

prednisone (systemically or as enema)

54
Q

what are the immunosuppressive agents used for chronic therapy of inflammatory bowel disease?

A
  1. azathioprine (purine antimetabolite)
  2. corticosteroids (prednisone, decadron)
  3. methotrexate
  4. anti TNFa antibodies
  5. anti-integrin antibodies
  6. cyclosporine (suppresses T helper and T suppressor lymphocytes)
55
Q

what is used for chronic therapy of inflammatory bowel disease?

A

immunosuppressive agents

56
Q

what are the anti TNFa antibodies?

A

infliximab, adalimumab, certolizumab

57
Q

what are the anti-integrin antibodies?

A

natalizumab, vedolizumab, ustekinumab

58
Q

what are the contributing causes of irritable bowel syndrome?

A

psychosocial factors, altered motility, and altered sensation

59
Q

what are the drug classes used to treat irritable bowel syndrome?

A
  1. anticholinergics (antispasmodic)
  2. serotonergic antagonist
  3. serotonergic agonist
60
Q

what are the anticholinergics used to treat irritable bowel syndrome?

A
  1. dicyclomine HCl

2. hyoscyamine sulfate

61
Q

what is the serotonergic antagonist used to treat irritable bowel syndrome? what does it block?

A

alosetron - blocks 5HT3

62
Q

side effect of alosetron

A

ischemic bowel and constipation (no longer used)

63
Q

what is the serotonergic agonist used to treat irritable bowel syndrome? what does it hit?

A

tegaserod maleate - hits 5HT4

ABBEY MSII U6 (18 decks)

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