GI Drugs Flashcards

1
Q

Name the major receptors involved in nausea/vomiting. (7)

A

H1, M1, chemoreceptors, D2, NK1, 5-HT3, mechanoreceptors

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2
Q

Scopolomine’s best application for N/V?

A

Prophylactic

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3
Q

What antihistamine is often used for Meniere’s Disease?

A

Meclizine (Antivert)

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4
Q

Name 2 highly emetogenic chemotherapeutic drugs.

A

Cisplatin, Cyclophosphamide

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5
Q

What drug class is the “biggest player” in an antiemetic regimen for chemotherapy-induced N/V? What can you add for higher levels of N/V?

A

5HT3 antagonist; corticosteroid and Aprepitant (NK1 antag)

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6
Q

What drug class is the cornerstone of chemotherapy anti-emesis regimens?

A

5-HT3 antagonists

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7
Q

Which 5-HT2 Antagonist has a half-life of 40 hours and is effective for delayed emsis?

A

Palonosetron

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8
Q

What antiemetic class can have major P450 enzyme interactions?

A

Neurokinin Receptor-1 antagonists

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9
Q

Name 2 NK-1 antagonists

A

Aprepitant

Netupitant

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10
Q

What is the advantage of CINVANTI over fosaprepitant?

A

It is a lipid emulsion of aprepitant rather than a prodrug like fosaprepitant and can be given by IV push rather than as a 30 minute infusion

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11
Q

What is Akynzeo?

A

A combination of (fos)netupitant (NK-1 antag) and palonosetron (5-HT3 antag); both drugs have a longer half-life; this prep can be given IV or PO

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12
Q

Name some D2 dopamine receptor antagonists used as antiemetics.

A

Benadryl
Phenergan
Benzos
Reglan

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13
Q

What are 2 contraindications for the use of laxatives?

A

Fecal impaction

Bowel obstruction

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14
Q

Name some bulk-forming laxatives.

A

Methylcellulose, Psyllium (Metamucil, Citrucel)

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15
Q

What drug class is the agent of choice for relief of temporary constipation?

A

Bulk-forming laxatives; safest class

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16
Q

Name some surfactant laxatives

A

Docusate salts, colace

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17
Q

Describe the MOA of surfactant laxatives

A

Anionic surfactant (soap-like) allows oil and water to penetrate stool

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18
Q

What is the most abused class of laxatives?

A

Stimulant laxatives; eating disorders

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19
Q

Name some stimulant laxatives

A

Bisacodyl (Dulcolax, Correctol), Senna (Ex-Lax, Senokot), Castor Oil

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20
Q

What mechanism of stimulant laxatives can lead to a common side effect?

A

Direct stimulation of GI motility can lead to severe stomach cramping

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21
Q

What class of laxatives is used for bowel prep?

A

Osmotic laxatives

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22
Q

Name some subclasses and drugs of osmotic laxatives.

A
Magnesium Salts (Milk of Magnesia)
Polyethylene Glycol/PEG (Miralax, GoLytely)
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23
Q

What is a concern with osmotic laxatives for older and renal-impaired patients?

A

Hypermagnesemia with Mg2+ salts

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24
Q

What are 3 characteristics of the antimotility/antisecretory agent Bismuth (Pepto-Bismol)?

A

Antimotility
Anti-inflammatory
Antimicrobial

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25
Q

What formulation of diphenoxylate (chemically related to meperidine) decreases its abuse potential?

A

Combination with atropine

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26
Q

What antimotility/antisecretory agent similar to diphenoxylate has NO abuse potential?

A

Loperamide

27
Q

Name two common demographics that experience IBS.

A

Onset younger than 35 years old and female

28
Q

What tricyclic antidepressant is most commonly used at subtherapeutic doses for IBS-D?

A

Amitriptyline

29
Q

What is an advantage of lubiprostone, a prostaglandin analog, used for IBS-C?

A

Very low systemic absorption

30
Q

Name an NHE3 inhibitor used for IBS-C.

A

Tenapanor (IBSRELA)

31
Q

What is the MOA of tenapanor?

A

An NHE3 inhibitor; inhibits sodium reabsorption in the SI and colon, resulting in increased water secretion

32
Q

What opioid is used for IBS-D and associated with gallbladder issues?

A

Eluxadoline

33
Q

What antibiotic-derived drug is the first-line treatment for IBS-D?

A

Rifaximin (works against anaerobic and gram-negative bacteria including C. diff)

34
Q

What drug class for inflammatory bowel disease exists mainly as prodrugs which are activated in the colon by bacteria?

A

5-Amino Salicylic Acid (5-ASA)

35
Q

Name 3 5-ASA prodrugs which are activated in the late SI/colon.

A

Sulfasalazine, Olsalazine, Balsalazide, Mesalamine (if given as a delayed-release formulation)

36
Q

What is the primary mechanism of 5-ASA drugs?

A

Inhibit cyclooxygenase 1 and 2 (topically, not systemically) and reduce production of inflammatory prostaglandins and cytokines in intestines

37
Q

What glucocorticoid is used for IBD?

A

Budesonide

38
Q

What is the MAJOR aggressive factor leading to PUD?

A

H. pylori

39
Q

What is the major goal of PUD therapy?

A

Eradicate H. pylori

40
Q

What receptors on the gastric parietal cells lead to increased acid production?

A

ACh (with vagal stimulation)
Histamine
Gastrin

41
Q

What is the role of pepsin in PUD?

A

Pepsin is a proteolytic enzyme most active at a pH around 2; when the mucosal barrier is compromised, pepsin will digest the gastric tissue and degrade fibrin clots, promoting GI bleeding

42
Q

What are the first line antibiotics used to eradicate H. pylori?

A

Amoxicillin and clarithromycin

43
Q

What are the 3 steps in PUD therapy?

A

Eradicate H. pylori
Suppress acid production/activity
Enhance mucosal defenses

44
Q

What is the most commonly used H2 receptor antagonist?

A

Famotidine

45
Q

What is the MOA of H2 receptor antagonists?

A

Competitively antagonize H2 receptor on gastric parietal cell causing a modest reduction in acid production

46
Q

What is the H2 receptor antagonist application in anesthesia?

A

Use of H2 receptor antagonists can raise the pH of gastric secretions such that bacteria that would normally be killed at a lower pH can cause pneumonia with aspiration

47
Q

In what population should H2 receptor agonist doses be reduced?

A

Renal insufficiency

48
Q

For what drugs can H2RAs decrease absorption due to higher pH?

A

Itraconazole

Iron

49
Q

What antacid drug can cause a harmless increase in serum creatinine?

A

H2RAs

50
Q

What drug class is more effective than H2RAs in reducing acid secretion?

A

PPIs

51
Q

What is the mechanism of many drug interactions with PPIs?

A

Some PPIs are CYP2C19 substrates and inhibitors

52
Q

What is a major DDI for PPIs?

A

Plavix (clopidogrel), a prodrug, can fail to activate since PPIs may inhibit CYP2C19 of which Plavix is a substrate.

53
Q

What is given in PUD “Triple Based Therapy”?

A

PPI + 2 ABs

54
Q

What 2 ABs are usually given in PUD therapy?

A

Clarithromycin and amoxicillin

55
Q

What can be substituted for amoxicillin in PUD therapy with a PCN allergy?

A

Metronidazole

56
Q

What is added to “Triple Therapy” for PUD in “Quadruple Therapy”?

A

Bismuth 525 mg PO QID

57
Q

What is the major DDI with sucralfate?

A

Sucralfate can decrease the absorption of quinolone ABs (ex., ciprofloxacin) due to chelation by aluminum (component of sucralfate)
DO NOT administer these ABs within 2 hours of sucralfate

58
Q

What is a teaching point for patients taking bismuth?

A

May cause discoloration of mucus membranes and darkening of stool which could be confused for GI bleed

59
Q

What is the major CI for mistoprosol?

A

Pregnancy Category X - abortifacient!!!!

60
Q

What is mistoprosol?

A

A PGE analog

61
Q

What is the pegylated version of naloxone used to decrease GI motility?

A

Naloxegol oxalate

62
Q

Why is naloxegol oxalate pegylated?

A

Adds a positive charge to the molecule, making it unlikely to cross the BBB, decreasing potential for abuse

63
Q

What is another property of naloxegol oxalate which makes it unlikely to penetrate the CNS (besides PEGylation)

A

Pgp substrate

64
Q

What is the anesthetic/analgesic implication of a patient taking a Pgp inhibitor with naloxegol oxalate?

A

A Pgp inhibitor will allow naloxegol oxalate into the brain so it may prevent the analgesic effects of a drug such as morphine