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Pharmacology > GI Drugs > Flashcards

GI Drugs Flashcards

1
Q

Antacids moa

A

Weak bases that act locally in the stomach by neutralizing gastric acidity

Stimulates PG production

Binds bile salts

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2
Q

Antacid DOA
Fasting:
W/ meals:

A

Fasting: 30 mins

W/ meals: 2-3 hours

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3
Q

Antacid prescription

A

Given 1 and 3 hours after meals and at bedtime

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4
Q

Antacid preparations

Scam

A

Sodium bicarbonate
Calcium bicarbonate
Aluminum hydroxide
Magnesium hydroxide

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5
Q

NAHCO3 adverse effects

A

Fluid retention

Metabolic alkalosis

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6
Q

CaCO3 adverse effect

A

Hypercalcemia

Nephrolithiasis

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7
Q

Aluminum Hydroxide adverse fx

A

Osteoporosis

Hypophosphatemimilk-alkali syndrome(inc Ca, MA, RI)

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8
Q

MgOH adverse fx

A

Osmotic diarrhea

Hypermagnesemia

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9
Q

[PUD]

Drugs that reduce intragastric acidity (AHP)

A

Antacids
H2 receptor Atagonists
Proton pump inhibitors

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10
Q

Antacids drug interaction

A

It should be taken 2 hrs before or after taking other drugs

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11
Q

H2Receptor Antagonist Drugs

A

Cimetidine
Ranitidine
Famotidine
Nizatidine

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12
Q

H2RA Pk

A

Rapidly absorbed
Not affected by food
Cross bbb and placenta
First pass metab

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13
Q

Moa of H2RA

A

Competitive inhibitors of histamine at H2 receptors in parietal cells

Suppress basal and meal-induced acid secretion

Decrease volume of gastrin secretion and concentration of pepsin

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14
Q

H2RA clinical uses

A

GERD
PUD
NUD
Stress-related gastritis or bleeding

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15
Q

H2RA adverse fx in CNS

A

Altered mental status like headache hallucinations confusion delirium

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16
Q

Endocrine fx of H2RA
Cardiac
Pregnancy
Rare

A 
Men: gynecomastia and impotence
Women: galactorrhea
Bradycardia
No teratogenic fx
Blood dyscrasia
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17
Q

PPI DRUGS

A

Omeprazole

Esomeprarazole

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18
Q

PPI Pk (6)

A 
Highly protein bound
F decreased by 50 pc bc of food
Rapidly absorbed
Acid-labile
All are inactive prodrugs that require activation in an acid environment
Rapid first pass
Rebal clearance
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19
Q

PPI MOA

A

Inhibit fasting and meal-stimulated acid secretion

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20
Q

PPI CLINICAL USES

A 
GERD
PUD
NUD
stress-related gastric bleeding
Gastrinoma and other hypersecretory conditions
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21
Q

PPI ADVERSE FX

A 
Nausea
Abdominal pain
Constipation
Diarrhea
Skin rashes
No teratogenicity
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22
Q

Nutritional fx of ppi

A

Affect absorption of vit b12 and fe ca zinc esp in prolonged use

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23
Q

Respi and enteric infections of ppi

A

Increase in gastric bacterial concentration-> increase risk for HAP CAP and clostridium difficile

Inc gastrin levels- ECL hyperplasia
Gastric carcinoid tumors

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24
Q

[PUD]

Agents that promote mucosal protection

A

Sucralfate
Prostaglandin analogs
Colloidal Bismuth Conpounds

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25
Q

MOA SUCRALFATE

A

Polymerization and selective binding to necrotic ulcer tissue to act as a barrier against pepsin gastrin and bile for up to six hrs after a single doe

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26
Q

AE OF SUCRALFATE

A

Nausea and constipation

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27
Q

Colloidal Bismuth Compounds MOA

A

Selectively binds to ulcer coating it and protecting it from gastin and pepsin

Other: inhibit pepsjn activity, stimulate mucus production and increase prostaglandin secretion

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28
Q

Prostaglandin analogs

A

Misoprostol and rebamipide

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29
Q

Misoprostol moa

A

Both acid inhibitory and mucosal protective properties

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30
Q

Rebamipide moa

A

PG synthesis and scavenging ros

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31
Q

Pg analog fx

A

Reduce incidence of nsaid-induced ulcer and ulcer complication
Stimulate uterine contractions

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32
Q

Agents used to eradicate H. Pylori

Clinical use

A

Ppi in triple therapy (with antibiotics)

To prevent ulcer recurrence

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33
Q

Prokinetic agents moa

A

Selectively stimulate gut motor function

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34
Q

Prokinetic agents

A

Cholinomimetic agents
Dopamine receptor antagonist
Macrolides
5-HT4 agonist

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35
Q

Cholinomimetic agents

A

Bethanecol

Neostigmine

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36
Q

Bethanecol
Moa
Clinical use

A

Stimulate M3 receptors

gerd

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37
Q

Neostigmine
Moa
Clinical uses

A

Acetylcholinesterase inhibitor
Enhance gastric, si, and colonic emptying
Ogilvie’s syndrome

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38
Q

Cholinomimetic agents effects

A

Excessive salivation, nausea, vomiting diarrhea bradycardia

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39
Q

Dopamine receptor antagonists

A

Domperidone

Metoclopromide

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40
Q

DRA MOA

A

Blocks the inhibitory effect of dopamine receptors-> increase esophageal peristaltic amplitude, increase LES pressure, enhance gastric emptying, no fx on si and colonic motility

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41
Q

DRA MOA

A

Also block D2 receptors in the chemoteceptor trigger zone of tbe medulla -> antinausea and antiemetic action

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42
Q

DRA CLINICAL USES

A 
GERD
postsurgical and diabetic gastroparesis
Prevention and treatment for vomiting
NUD
Promote postpartum lactation (domperidone)
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43
Q

Metoclopromide CNS AE

Extrapyramidal effects

A

Insomnia, anxiety, agitation
Dystonias akathisia parkinsonian features
Tardive diskinesia

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44
Q

Metoclopromide and domperidone

AE

A 
Prolactenemia
Galactorrhea
Gynecomastia
Impotence
Menstrual disorders
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45
Q

Macrolides moa

Exaple and use

A

Stimulate motilin receptors on GI smooth muscle and promote MMC

Erythromycin: gastroparesis

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46
Q

Laxatives classification

A

Stimulants or irritants
Luminally active agents
Prokinetic agents

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47
Q

Bulk forming agents examples

AE

A

Bran, psylliumbloating flatus

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48
Q

Osmotic laxatives moa

Clinical use

A

Soluble but nonabsorbable cmpds-> increase stool liquidity due to an obligate increase in fecal fluid
Use: treatment of acute constipation or prevention of chronic constipation

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49
Q

Osmotic laxatives
Example
Subexample with AE

A

Nonabsorbable sugars or salts: lead to intravascular volume depletion and intravascular volume depletion

  • milk of magnesia: hypermagnesemia
  • mg citrate and na phosphate:
  • Sorbitol and lactulose: severe flatulose and cramps
  • Polyethylene glycol
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50
Q

Stool softeners
Examples
Use

A

Mineral oil and docusate glycerin supository

Prevent constipation and prevent straining

51
Q

Stimulant lacatives moa

A

Induce bowel movement thru direct stimulation of ens and colonic electrolyte and fluid secretion

52
Q

Stinulant laxatives examples

A

Anthraquinones- cascara and aloe::melanosis coli
Diphenylmethane derivatives- bisacodyl
Castor oil

53
Q

Chloride channel activator moa

A

Stimulation kf chloride channel openjng in the SI increases Cl- rich fluid secretion into the intestine and shortens intestinal transit time

54
Q

Cl channel activator uses

Example

A

Chronic constipaion and IBS-C
Lubiprostone
Linaclotide

55
Q

Opioid receptor antagonist
Moa
Example and uses
Ae

A

Inhibit peripheral mu-opioid receptors
Methylnaltrexone- treatment of opioid induced constipation
Alvimopan- postoperative ileus
Cardiovascular toxicity

56
Q 
Serotonin 5-HT4 receptor agonist
Moa
Example
Use
AE
A

Stimulates second order enteric neurons to promote peristaltic reflex
Chronic constipation and IBS constipation
Cardiovascular due to QT prolongation of tegaserod
Tegaserod and prucalopride

57
Q

Antidiarrheal agents

A

Fluid and electrolyte therapy
Antidiarrheal agents
Treat the underlying cause

58
Q

Fluid and electrolyte therapy

A

Oral rehydration solution

Parenteral ivf

59
Q

Antidiarrheal agents

Examples

A

Opioid agonists
Bile salt binding resin
Somatistatin/octreotide

60
Q

Opioid agonist

Effect

A

Loperamide- dies not cross bbb not analgesic no ptential for addiction
Diphenoxylate
Increase colonic transit time and fecal water absorption
Decrease mass colonic movement and gastrocolic reflex

61
Q

Bile salt binding resins
Example
Ae

A

Cholestyramine and colestipol- decrease diarrhea caused by excess fecal bile acids
Bloating flatulence

62
Q

Somatostatin/Octreotide effects

A

Somatostatin- inhibit secretion of hormones, reduce intestinal fluid secretion and pancreatic secretion, slows gi motility (kulang)
Octreo same

63
Q

S/O uses

A

Gi neuroendocrine tumors pancreatic fistula, GI bleeding

64
Q

S/O ae

A

Bradycardia, steatorrhea, hypothyroidism

65
Q

Treat the underlying cause

A

Antimicrobials

Dietary modif

66
Q

Drugs for IBS

A

Serotonin 5-HT3 receptor antagonists
Antispasmodics
Clrode channel activator

67
Q

Antispasmodics
Ex
Moa
Ae

A

Dicyclomine & hyocyamine
Inhibit muscariniv cholinergic receptors jn the enteric plexus and on sm: for abdominal pakn and disconfort
Dry mouth visual disturbancesconstipation

68
Q

Prokinetic agents moa

A

Selectively stimulate gut motor function

69
Q

Prokinetic agents

A

Cholinomimetic agents
Dopamine receptor antagonist
Macrolides
5-HT4 agonist

70
Q

Cholinomimetic agents

A

Bethanecol

Neostigmine

71
Q

Bethanecol
Moa
Clinical use

A

Stimulate M3 receptors

gerd

72
Q

Neostigmine
Moa
Clinical uses

A

Acetylcholinesterase inhibitor
Enhance gastric, si, and colonic emptying
Ogilvie’s syndrome

73
Q

Antispasmodics
Ex
Moa
Ae

A

Dicyclomine & hyocyamine
Inhibit muscariniv cholinergic receptors jn the enteric plexus and on sm: for abdominal pakn and disconfort
Dry mouth visual disturbancesconstipation

74
Q

Drugs for IBS

A

Serotonin 5-HT3 receptor antagonists
Antispasmodics
Clrode channel activator

75
Q

Treat the underlying cause

A

Antimicrobials

Dietary modif

76
Q

S/O ae

A

Bradycardia, steatorrhea, hypothyroidism

77
Q

S/O uses

A

Gi neuroendocrine tumors pancreatic fistula, GI bleeding

78
Q

Somatostatin/Octreotide effects

A

Somatostatin- inhibit secretion of hormones, reduce intestinal fluid secretion and pancreatic secretion, slows gi motility (kulang)
Octreo same

79
Q

Bile salt binding resins
Example
Ae

A

Cholestyramine and colestipol- decrease diarrhea caused by excess fecal bile acids
Bloating flatulence

80
Q

Opioid agonist

Effect

A

Loperamide- dies not cross bbb not analgesic no ptential for addiction
Diphenoxylate
Increase colonic transit time and fecal water absorption
Decrease mass colonic movement and gastrocolic reflex

81
Q

Antidiarrheal agents

Examples

A

Opioid agonists
Bile salt binding resin
Somatistatin/octreotide

82
Q

Fluid and electrolyte therapy

A

Oral rehydration solution

Parenteral ivf

83
Q

Antidiarrheal agents

A

Fluid and electrolyte therapy
Antidiarrheal agents
Treat the underlying cause

84
Q 
Serotonin 5-HT4 receptor agonist
Moa
Example
Use
AE
A

Stimulates second order enteric neurons to promote peristaltic reflex
Chronic constipation and IBS constipation
Cardiovascular due to QT prolongation of tegaserod
Tegaserod and prucalopride

85
Q

Opioid receptor antagonist
Moa
Example and uses
Ae

A

Inhibit peripheral mu-opioid receptors
Methylnaltrexone- treatment of opioid induced constipation
Alvimopan- postoperative ileus
Cardiovascular toxicity

86
Q

Cl channel activator uses

Example

A

Chronic constipaion and IBS-C
Lubiprostone
Linaclotide

87
Q

Chloride channel activator moa

A

Stimulation kf chloride channel openjng in the SI increases Cl- rich fluid secretion into the intestine and shortens intestinal transit time

88
Q

Stinulant laxatives examples

A

Anthraquinones- cascara and aloe::melanosis coli
Diphenylmethane derivatives- bisacodyl
Castor oil

89
Q

Stimulant lacatives moa

A

Induce bowel movement thru direct stimulation of ens and colonic electrolyte and fluid secretion

90
Q

Stool softeners
Examples
Use

A

Mineral oil and docusate glycerin supository

Prevent constipation and prevent straining

91
Q

Osmotic laxatives
Example
Subexample with AE

A

Nonabsorbable sugars or salts: lead to intravascular volume depletion and intravascular volume depletion

  • milk of magnesia: hypermagnesemia
  • mg citrate and na phosphate:
  • Sorbitol and lactulose: severe flatulose and cramps
  • Polyethylene glycol
92
Q

Osmotic laxatives moa

Clinical use

A

Soluble but nonabsorbable cmpds-> increase stool liquidity due to an obligate increase in fecal fluid
Use: treatment of acute constipation or prevention of chronic constipation

93
Q

Bulk forming agents examples

AE

A

Bran, psylliumbloating flatus

94
Q

Laxatives classification

A

Stimulants or irritants
Luminally active agents
Prokinetic agents

95
Q

Macrolides moa

Exaple and use

A

Stimulate motilin receptors on GI smooth muscle and promote MMC

Erythromycin: gastroparesis

96
Q

Metoclopromide and domperidone

AE

A 
Prolactenemia
Galactorrhea
Gynecomastia
Impotence
Menstrual disorders
97
Q

Metoclopromide CNS AE

Extrapyramidal effects

A

Insomnia, anxiety, agitation
Dystonias akathisia parkinsonian features
Tardive diskinesia

98
Q

Serotonin 5-HT3 receptor antagonist
Moa
Ex use
Ae

A

Inhibit colonic motility esp in left colon inc total colonic transit time
Alosetron- IBS with diarrhea
Constipation

99
Q

Antiemetics

A 
Serotonin 5-HT3 antagonists
Corticosteroids
Neurokinin receptor antagonists
Phenothiazined and butyrophenones
Substituted benzamides
H1 antihistamines and anticholinergics
Benzodiazepines
Cannabinoids
100
Q 
[antiemetics]
Serotonin 5-HT3 antagonists
Moa
Examples
Ae
A

Block receptors in the vomiting center and CTZ and peripheral receptors kn extrinsic intestinal vagal anf soinal sfferent nerves
Ondansetron
Headachedizzines constipation prolong qt interval

101
Q

Corticosteroids
Ex
Moa

A

Dexamethadone and methylprednisolone

Enhance efficacy of 5-HT3 receptor antagonists for prevention of comit due to chemo

102
Q

Neurokinin receptor antagonist
Moa
Ex- characteristics

A

Central blockage in the area postrema

Aprepitant- highly selective NK1 receptor antagonist crosses bbb

103
Q

Phenothiazines
Moa
Ex

A

Inhibit dopamine and muscarinic receptors

Prochlorperazine

104
Q

Butyrophenones

A

Central dopaminergic blockade

105
Q

Substituted benzamines
Ex
Moa
Ae

A

Metoclopromide
Dopamine receptor blockade
Extrapyramidal effect: restlessness parkinsonian symptoms

106
Q

H1 antihistamines and anticholinergics
Ae
Use
Ex- use

A

Treatment of motion sickness
Dizziness sedation
Diphenhydramine- sedating
Meclizine- less sedation; motion sickness and vertigo due to labyrinth dys
Huoscine(scopolamine)- muscarinic receptor antagonist; motion sickness

107
Q

Benzodiazepines

A

Lorazepam or diazepam- used prior to chemo to reduce vomiting/ vomiting due to anciety

108
Q

Cannabinoids
Ex- use
Ae

A

Drinabinol-as appetite stimulant and antiemetic
- euphoria sedation hallucination
Nabiline- thc analog

109
Q

Drugs used tn treat inflammatory bowel disease

A

Azo cmpds- sulfasalazine

Mesalamine cmpds- rowasa

110
Q

[IBD]

Immunosuppressive agents

A 
Glucocorticoids
Purjne analogs
Methotrexate
AntiTNF therapy
Anti-integrin therapy
111
Q

[IBD]
Immunosuppressive agents
GLUCOCORTICOIDS EX
Mode

A

Prednisone prednisolone

Rectal

112
Q 
[IBD]
Immunosuppressive agents
PURJNE ANALOGS
Ex
Use
Ae
A

Azathioprine and 6- mercaptopurine
For jnduction and maintenance of remission of ulcrrative colitis and Chron’s disease
Nausea vomiting

113
Q 
[IBD]
Immunosuppressive agents
Methotrexate
Moa
Use
Ae
A

Inhibit dihydrofolate reductase; interfere with inflamm action of Il-1
Induce and maintain remission in Chron’s
Bone mattoe duppression alopecia

114
Q

AntitNF therapy
Ex
Use
Ae

A

Infliximab adalimimab golimumab certolizumab
Acute and chronic treatment of Uc and Cron’s
Infection lymphoma

115
Q

Bile acid therapy for gall stones
Moa
Use

A

Ursodiol
Expands bile acid pool
Dec cholesterol content of bile bunreducing hepatic cholesterol secretion

116
Q

Drugs used for upper Gi bleeding
Ex
Moa
Use

A

Somatostatin/Octreotide
Reduce portal bf and varice pressures
Initial hemostasid from bleeding esophageal varices

117
Q

Drugs used for upper Gi bleeding
Ex
Moa
Use

A

Vasopressin ang terlipressin
Causes splanchnic arterial vasoconstriction leading yo reduced splanchnic perfusion and loerred portal venous pressure
Ae: MI HPN

118
Q

Drugs used for upper Gi bleeding
Ex
Moa
Use

A

Beta receptor blocking agents
Reduce portal venous pressure via a decrease in portal venous pressure via a decrease ib portal venous inflow due to decrease in CO (B1 blovkade) and splanchnic vasoconstriction (B2 blockade)

To reduce incidence of initial bleeding anf reduce rate of recurrent bleeding

119
Q

DRA CLINICAL USES

A 
GERD
postsurgical and diabetic gastroparesis
Prevention and treatment for vomiting
NUD
Promote postpartum lactation (domperidone)
120
Q

DRA MOA

A

Also block D2 receptors in the chemoteceptor trigger zone of tbe medulla -> antinausea and antiemetic action

121
Q

DRA MOA

A

Blocks the inhibitory effect of dopamine receptors-> increase esophageal peristaltic amplitude, increase LES pressure, enhance gastric emptying, no fx on si and colonic motility

122
Q

Dopamine receptor antagonists

A

Domperidone

Metoclopromide

123
Q

Cholinomimetic agents effects

A

Excessive salivation, nausea, vomiting diarrhea bradycardia

Pharmacology (2 decks)

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