GI drugs Flashcards

1
Q

Disorder involving erosion or ulceration of mucosal lining of GI tract

A

Acid Peptic Disease

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2
Q

Drug that reduces nausea and vomiting

A

Anti emetics

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3
Q

Esophageal irritation or inflammation due to reflux of stomach acid

A

GERD

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4
Q

Paralysis of muscle of stomach and GI due to nerve or muscle damage

Common in DM and PD

A

Gastroparesis

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5
Q

Inflammatory disease involving irritation and ulceration of COLON and RECTUM

A

Ulcerative colitis

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6
Q

Inflammatory disorder involving colon plus proximal parts of GI tract

A

Crohn’s dse

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7
Q

Disease of unknown origin manifesting as episodes of abdominal discomfort and abnormal bowel dysfunction

A

Irritable bowel syndrome

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8
Q

Drug that promotes GI motility

A

Prokinetic

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9
Q

Uses energy of ATP to secrete protons into stomach

Common target of drugs that suppress acid secretion

A

Proton Pump H/K ATPase in Parietal Cell

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10
Q

Weak bases that neutralize stomach acid by reacting with protons in the lumen

A

Antacids

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11
Q

PROTECTIVE FUNCTION of gastric mucosa

A

Antacids

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12
Q

Difference in antacids

A

Absorption and stool consistency

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13
Q

Aluminum hydroxide causes

A

Constipation

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14
Q

Magnesium hydroxide causes

A

Diarrhea

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15
Q

Less commonly used bec are completely absorbed and with more SE

A

Sodium bicarbonate Calcium carbonate

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16
Q

Two classes of GI drugs

A

1 reduce intragastric acidity

2 promote mucosal defense

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17
Q

Inhibit basal acid production by parietal cells

Inhibits binding of histamine at H2 receptor and preventing HKATPase pump

A

H2 antagonist

Cimetidine
Ranitidine
Famotidine
Nizatidine

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18
Q

Inhibit prandial acid release

A

H2 agonist

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19
Q

Cimetidine

A

1st H2 blocker
CYP450 inhibitor (inc Warfarin effect)
Inc metabolism of estrodiol - gynecomastia

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20
Q

Cimetidine endocrine effects (4)

A

Alopecia
Loss of libido
Impotence
Irregular menstruation

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21
Q

Most used H2 receptor blocker

A

Ranitidine

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22
Q

H2 receptor blocker other SE

A

Abdominal discomfort
NDV
Give BID PO

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23
Q

Proton Pump Inhibitors are Lipophilic weak bases that irreversibly inactivate the final common pathway of H secretion

A

H+/K+ ATPase

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24
Q

PPIs are metabolized in the

And have a half life of

A

Liver

1-2h

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25
PPIs have a duration of action of and Require days of treatment to achieve effectiveness
24 h 3-4 days of treatmenr
26
Most bioavailable of PPIs
Lansoprazole
27
Lansoprazole is excreted via the rest are via renal
biliary tract
28
PPIs can inhibit percentage of 24h acid secretion SE
90-98% ``` C difficile Pneumonia Dec absorption of Ca, Mg and Fe cations Osteoporosis (dec Ca absorption) Hypomagnesemia ```
29
Least bioavailable PPI
Omeprazole
30
PGE analog increasing mucus and bicarbonate
Misoprostol
31
Misoprostol increases and inhibits
mucosal protection acid secretion
32
Misoprostol CI
pregnant
33
Sucrose complex with sulfatef aluminum hydroxide
Sucralfate
34
Sucralfate MOA
polymerizes in acid environment of stomach
35
Sucralfate SE
constipation
36
Reduces stool frequency and liquidity in infectious diarrhea
Bismuth salt
37
Bismuth SE
stool and tongue blackening
38
Bismuth toxicity (5)
``` Encephalopathy Ataxia Headache Confusion Seizure ```
39
D2 antagonist that can cross BBB and has antiemetic effect at CTZ
Metaclopromide
40
Metaclopromide SE
EPS and endocrine
41
Does not cross BBB, not anti enetic but for stimulation of Post Partum Lactation
Domperidone
42
Macrolide that promotes Motilin release
Erythromycin Parenteral
43
Erythromycin se
Diarrhea
44
Used in constipation, prevention of straining, preparation of diagnostic examination, removal of poison or toxin, antihelminth
Laxative
45
Laxatives are CI in
Appendicitis Diverticulitis Ulcerative colitis
46
Laxative SE
``` Diarrhea Abdominal cramping Nausea Fluid and electrolyte imbalance Sympathetic reactions CATHARTIC dependence ```
47
Surfactant which facilitate mixing of water and oily material
Stool softeners/Emollients
48
Drugs with 5 aminisalicylic acid (5-ASA) for topical therapy in IBD These inhibit synthesis of prostaglandin and inflammatory leukotrienes hence no cytokines
Aminosalicylate
49
Inhibits cAMP and blocks cytosol Ca Inhibits GH, glucagon, insulin, gastrin Used in treatment of esophageal varices, acromegaly, carcinoid, glucagonoma, gastrinoma)
Somatostatin
50
Long acting somatostatin synthetic analog Acromegaly, carcinoid, gastrinoma, glucagonoma
Ocreotide
51
Ocreotide side effects
GI gallstones Bradycardia, conduction anomaly
52
Agonist at V1 and V2 ADH Activates insertion of aquaporin in water channels in collecting tubule Decreases water excretion Vasoconstriction Used for varices, pituitary diabetes insipidus
Desmopressin | Vasopressin
53
Desmopressin Vasopressin side effect
Hyponatremia | Hypertension
54
Promotility agents
Erythromycin 250 Metaclopromide D2 antagonist 10 Domperidone D2 antagonist
55
D2 dompamine receptor antagonist against area postrema but Prokinetic promoting upper GI intestinal motility D2 receptor blocking action in the area postrema of value in preventing emesis after surgical anesthesia and cancer chemotherapeutic drugs
Metaclopromide | Domperidone
56
Metaclopromide SE
``` Parkinsonism EPS Tardive dyskinesia Hyperprolactinemia Upper GI prokinetic Diarrhea because of D2 receptor blockade Drowsiness Depression Neuroleptic malignant syndrome bec of D2 blockade (fever, rigidity, msc, autonomic instability, rhabdomyolysis) QT prolongation Torsade de pointes ```
57
D2 antagonist that does not cross BBB so less CNS
Domperidone
58
Promotes motility by stimulating motilin receptors
Erythromycin
59
Interferes with activity of T lymphocytes , decreased inflammation Metabolized to sulfapyridine and 5 ASA Compete with p-aminobenzoic acid (PABA) Inhibits dihydropteroate synthase
Sulfasalazine
60
Calcineurin inhibitor Inhibits trascription of IL - 2 and cytokines involved in T cell activation Used in severe UC refractory to IV corticosteroids
Cyclosporine
61
Activates u opiod receptor and slows motility with negligible CNS effects
Loperamide Similar: Diphenoxylate greater CNS opiod
62
5HT3 receptor antagonist of high potency and duration of binding Reduces smooth muscle activity in GI tract Severe diarrhea predominant IBS in women
Alosetron
63
Alosetrone 5HT3 antagonist SE
ischemic colitis bowel infarct constipation
64
Chloride channel activator useful in constipation-predominant IBS
Lubiprostone
65
Selective 5HT3 receptor block on vagal afferents of GI and CNS Prevention of chemotherapy-induced and postoperative nausea and vomiting May slow colonic transit constipation
Ondansetron similar: Dolasetron Granisetron Palonosetron
66
GI irritation due to infection, chemotherapy and distention cause release of
serotonin activating 5HT3 receptors of vagus nerve relaying impulse at vomiting centers hence emesis
67
Vestibular system also communicates directly to vomiting center hence
vestibular nausea
68
5HT3 antagonists like ondansentron alarming SE
``` Prolong QT interval Torsade Serotonin syndrome (rigidity, tremor, hyperthermia and confusion) ```
69
Vestibular system receptors for vomiting and emesis
H1 histamine receptor coupled to Gq | M1 muscarinic receptors
70
Treat vestibular nausea and motion sickness
1st gen antihistamine receptors Diphenhydramine Meclizine SE: sedation, antimuscarinic
71
Muscarinic agonist that treats motion sickness (M1 blockade)
Scopolamine
72
Area postrema receptors
D2 receptors | Neurokinin NK1 receptors activated by Substance P
73
Metaclopromide CI
Small bowel obstruction
74
Antagonizes NK1 receptors in area postrema Treats chemotherapy induced vomiting No effect on serotonin, dopamine and muscarinic receptors Limited adverse effects
Aprepitant
75
Inhibits both gastrin and histamine by ECL cells Tones down gastric acid production even on gastrinomas
Somatostatin Ocreotide long acting SST analog useful on Zollinger Ellison