Pharm Flashcards

1
Q

What is the MOA of and indication for loperamide?

A
  • Binds Mu opioid receptors in the gut wall.
  • Also reduces ACh/prostaglandin release.
  • Both actions decrease GI motility.
    Used to treat common diarrhea.
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2
Q

What are some AE of loperamide?

A

QT prolongation/Torsade’s

Constipation, dizziness, nausea

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3
Q

What is the MOA of and indication for bismuth-subsalicylate?

A
  • Stimulates absorption of water from the LI.
  • Forms a protective lining in the intestines
  • Believed to have some antimicrobial properties

Used to treat common diarrhea and H. pylori infections. (Pepto-Bismol)

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4
Q

What are some AEs of bismuth-subsalicylate?

A

Dark stools
Dark tongue
**AVOID USE in patients with renal dysfunction: bismuth can accumulate and cause CNS effects, though this is rare

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5
Q

What is the MOA of and indication for diphenoxylate/atropine?

A

Diphenoxylate/atropine is an opioid analgesic.

  • Binds mu opioid receptors in the GI tract (decreases motility and secretions).
  • Atropine reduces risk of abuse

Diphenoxylate/atropine is used to treat common diarrhea. It is not used frequently, as loperamide is equally effective.

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6
Q

What are some AEs of diphenoxylate/atropine?

A

Well, it’s an opioid.
N/V, respiratory depression, sedation, miosis, confusion

Anticholinergic effects can also occur (anti-SLUD effects).

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7
Q

What is the MOA of and indication for opium tinctures?

A

Opium tinctures bind mu opioid receptors in the GI tract, decreasing peristalsis and secretions.

It is (rarely) used for severe diarrhea; sometimes used in HIV patients with crypto.

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8
Q

What are some AEs of opium tinctures?

A

It’s opium?

N/V, respiratory depression, sedation, miosis, confusion, addiction.

Schedule II drug.

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9
Q

Name four therapies for common diarrhea that we discussed.

A
  • Loperamide (OTC)
  • Bismuth-subsalicylate (OTC)
  • Diphenoxylate/atropine (Rx)
  • Opium tincture (Rx)
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10
Q

What are nine drug classes we discussed for treatment of IBS with constipation?

A
  • Bulk-forming laxatives
  • Osmotic laxatives
  • Stool softeners
  • Lubricants/emollients
  • Stimulants
  • Prostaglandin derivatives
  • Guanylate cyclase-C receptor agonists
  • Na+/H+ exchanger inhibitors
  • 5-HT4 agonists
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11
Q

What is the MOA of and indication for psyllium (or methylcellulose, or fiber)?

A

These are examples of bulk forming laxatives.
They hold water content in the intestine, forming a softer/bulkier stool that is easier to pass.

They are used to treat constipation.

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12
Q

What are some examples of osmotic laxatives? What is their MOA?

A

Lactulose, macrogol, and magnesium are examples of osmotic laxatives. They are non-absorbable and create a hypertonic environment inside of the colon, drawing water in, “flushing” out the colon.

They are used to treat constipation.

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13
Q

What kind of drug is lubiprostone? What is its MOA and indication?

A

Lubiprostone is a prostaglandin derivative used to treat constipation.
It activates Cl- channels in the GI tract, stimulating intestinal fluid secretion.

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14
Q

What is the MOA of and indication for linaclotide?

A

Linaclotide is used to treat IBS-C in adults. It works by targeting guanylate cyclase-C receptors, increasing concentrations of cGMP. cGMP then activates CF-regulated ion channels, increasing GI motility and secretions.

Plecanatide is a similar drug.

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15
Q

What is the MOA of and indication for plecanatide?

A

Plecanatide is used to treat IBS-C in adults, as long as there is no GI obstruction.

It works by targeting guanylate cyclase-C receptors, increasing concentrations of cGMP. cGMP then activates CF-regulated ion channels, increasing GI motility and secretions.

Linaclotide is a similar drug.

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16
Q

What is the MOA of and indication for tenapanor?

A

Tenapanor is used to treat IBS-C in adults. It may also be used to treat hyperphosphatemia in CKD patients.

It works by inhibiting Na+/H+ exchanger 3. Inhibition of sodium absorption results in decreased water absorption, decreasing transit time.

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17
Q

What is the MOA of and indication for tegaserod?

A

Tegaserod is used to treat IBS-C in women <65 YO without cardiovascular risk.

It works via agonism of 5-HT4 receptors: these stimulate GI secretions and speeds transit.

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18
Q

Name 3 agents that directly increase intestinal peristalsis.

A

Cascara sagrada
Bisacodyl (dulcolax)
Senna

(^Stimulants are often abused by patients with eating disorders, and should not be prescribed for chronic use.)

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19
Q

What are some AE associated with bulk-forming laxatives?

A

Flatulence
Bloating
Must take with adequate hydration or intestinal blockage can occur

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20
Q

What are some AE associated with osmotic laxatives?

A

Generally well-tolerated
Diarrhea
Mg can accumulate in patients with renal impairment

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21
Q

What are some AE associated with lubiprostone?

A

Diarrhea
Nausea
Dyspnea
Must adjust dose in patients with hepatic impairment

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22
Q

What are some AE associated with guanylate-cyclase agonists?

A
(Linaclotide, plecanatide)
Diarrhea (can be severe)
Flatulence
Abdominal pain
Abdominal distention
Serious dehydration can occur (BBW for patients <18YO)
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23
Q

What are some AE associated with tenapanor?

A
Diarrhea
Flatulence
Abdominal distention
Dizziness
Serious dehydration (BBW for patients <18YO)
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24
Q

What are some AE associated with tegaserod?

A
Diarrhea
Flatulence
Dizziness
Dyspepsia
Abdominal pain
HA
Rare reports of suicidal ideation

Contraindications: hx of MI, stroke, TIA, angina, ischemic colitis, renal impairment, hepatic impairment

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25
Q

What are 7 drug classes commonly used to treat IBS-D?

A
  • Anti-diarrheals (loperamide)
  • Antispasmodics
  • Antidepressants
  • Antibiotics (rifaximin specifically)
  • Bile acid sequestrants
  • Opioid receptor agents
  • 5-HT3 receptor antagonists
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26
Q

What is the MOA of and indication for hyoscyamine?

A

Hyoscyamine is an antispasmodic used in the treatment of IBD-D. Often used PRN or before meals.

It relaxes intestinal smooth muscle (directly and via anticholinergic mechanisms).

Dicyclomine is a drug in the same class.

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27
Q

What is the MOA of and indication for dicyclomine?

A

Dicyclomine is an antispasmodic used in the treatment of IBD-D. Often used PRN or before meals.

It relaxes intestinal smooth muscle (directly and via anticholinergic mechanisms).
Hyoscyamine is a drug in the same class.

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28
Q

What are some AE associated with dicyclomine and hyoscyamine?

A

Anticholinergic effects:

  • Anti-SLUD (salivation, lacrimation, urination, defecation)
  • Drowsiness*
  • Dizziness
  • Confusion
  • Palpitations
  • Visual disturbance
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29
Q

What is the MOA of and indication for amitriptyline?

A

Amitriptyline is a tricyclic antidepressant used in the treatment of moderate to severe IBD-D, especially if there is an anxious/depressive element to their disease.

It works via anticholinergic effects to reduce abdominal pain and alter GI transit time.

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30
Q

What are some AE associated with amitriptyline?

A

Anticholinergic effects:

  • Anti-SLUD (salivation, lacrimation, urination, defecation all dry up)
  • Drowsiness*
  • Dizziness
  • Confusion
  • Palpitations
  • Visual disturbance
  • Overdose is quite dangerous; can cause cardiac arrhythmias
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31
Q

What is the MOA of and indication for Rifaximin?

A

Rifaximin is an antibiotic that is often used to treat IBD-D. It is often used in patients with hepatic encephalopathy.

It is thought to alter gut microbiota. Specifically, it reduces population of bacteria that absorb nitrogen.

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32
Q

What are some AE associated with rifaximin?

A
  • Antibiotic resistance and associated C. diff
  • Nausea
  • Myalgia
  • Elevated ALT
  • Elevated creatinine kinase
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33
Q

What is the MOA of and indication for cholestyramine?

A

Cholestyramine is a bile acid sequestrant. It decreases absorption of triglycerides and cholesterol. It is used off-label to improve IBS-D symptoms and slow motility. Data are limited.

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34
Q

What is the MOA of and indication for colestipol?

A

Colestipol is a bile acid sequestrant. It decreases absorption of triglycerides and cholesterol. It is used off-label to improve IBS-D symptoms and slow motility. Data are limited.

35
Q

What are some AE associated with cholesytramine and colestipol?

A
  • Constipation

- Possible reduced absorption of other medications

36
Q

What is the MOA of and indication for eluxadoline?

A

Eluxadoline is a newer medication used to treat IBS-D.

It is a mu-opioid receptor agonist: decreases GI motility and secretions.

It is also a delta-opioid receptor antagonist: helps reduce drug-induced constipation and abdominal pain.

$$$

37
Q

What are some AE associated with eluxadoline?

A
  • Constipation
  • Nausea
  • Abdominal pain
  • GI obstruction
  • Euphoria/feeling of drunkenness

Contraindications:

  • Do not use in patients with hx of cholecystectomy, biliary/pancreatic duct obstruction or dysfunction
  • Do not use with anticholinergics
38
Q

What is the MOA of and indications for alosetron?

A

Alosetron is a 5HT-3 antagonist. It is used in the treatment of IBD-D.

39
Q

What are some AE associated with alosetron?

A
BBW: 
- Constipation
- Ischemic colitis
Other AE:
QT prolongation
40
Q

Name 9 classes of drugs that can be used as antiemetics.

A
  • Dopamine receptor antagonists
  • Serotonin receptor antagonists
  • Anticholinergics
  • Antihistamines
  • Neurokinin receptor antagonists
  • Glucocorticoids
  • Benzodiazepines
  • Atypical antipsychotics
  • Cannabinoids
41
Q

To what drug class does prochlorperazine belong, and what is its indication?

A

Dopamine receptor antagonist.

Used to treat nausea/vomiting; often used in the ER and to treat hyperemesis gravidarum.

42
Q

To what drug class does metoclopramide belong, and what is its indication?

A

Dopamine receptor antagonist (also some serotonin blocking).

Used to treat nausea/vomiting; also used in gastroparesis as its prokinetic effects increase peristalsis.

43
Q

To what drug class does domperidone belong, and what is its indication?

A

Dopamine receptor antagonist

He did not emphasize this drug

44
Q

In what area of the brain do dopamine receptor antagonists enact their antiemetic effects?

A

D2 receptors in the area postrema

45
Q

What are some of the important AEs of dopamine receptor antagonist drugs?

A

Lots of CNS effects:

  • Drowsiness
  • Weird dreams
    • Prokinetic effects: movement disorders!!
    • QT Prolongation!!
46
Q

Your patient, who is on metoclopramide, presents with torticolis. What is this condition and what is the treatment?

A

Metoclopramide is a dopamine receptor antagonist that has prokinetic effects. Torticolis is a painful contortion/twisting of the neck and is an AE of metoclopramide. It can be treated by administering an anticholinergic such as diphenhydramine.

47
Q

To what drug class does droperidol belong, and what is its indication?

A

Dopamine receptor antagonist.

Used to treat nausea and vomiting, often used post-procedure. Can also be used as a sedative/tranquilizer.

48
Q

Drugs that end in the suffix “-setron” belong to which class?

A

5HT-3 antagonists

Dolasetron, granisetron, palonosetron, ondansetron

49
Q

Serotonin antagonists provide antiemetic relief in two ways. Which two areas of the CNS are affected to give this effect?

A

Centeral effects: area postrema

Peripheral effect: inhibition of the vagus nerve

50
Q

Which classed of drugs are most commonly added to traditional antiemetics to treat chemotherapy-induced nausea/vomiting?

A
  • 5-HT3 antagonists
  • Neurokinin receptor blockers
  • Glucocorticoids
  • Benzos
  • Atypical antipsychotics
  • Cannabinoids
51
Q

What are some AEs of 5-HT3 antagonists?

A
  • Constipation
  • HA
  • *QT prolongation
  • Increased liver enzymes
  • Serotonin syndrome (overdose or used with other 5-HT3 blockers)
52
Q

To what class of drugs does scopolamine belong, and what is its indication?

A

Scopolamine is an anticholinergic agent, used for the treatment of motion sickness (vestibular-induced nausea) and vomiting.

53
Q

How does scopolamine work?

A

Scopolamine is an anticholinergic/ non-specific muscarininc antagonist, which works in three areas:

  • Area postrema (centrally)
  • Vestibular system (centrally)
  • Vagus nerve inhibition (peripherally)
54
Q

What are some AE of scopolamine?

A

Anticholinergic effects:

  • Anti-SLUD (salivation, lacrimation, urination, defecation all dry up)
  • Tachycardia (inhibition of PNS)
  • Effects can be treated with physostigmine, a cholinesterase inhibitor
55
Q

Name the antiemetics that fall in the antihistamine class:

A
Meclizine
Promethazine
Dimenhydrinate
Diphenhydramine
Doxylamine
56
Q

What is the MOA of meclizine?

A

Antihistamine (H1 blocker)
Has two central effects to provide antiemetic relief:
1.) Area postrema
2.) Vestibular system

57
Q

What is the MOA of promethazine?

A

Antihistamine (H1 blocker)
Has two central effects to provide antiemetic relief:
1.) Area postrema
2.) Vestibular system

58
Q

What is the MOA of dimenhydrinate?

A

Antihistamine (H1 blocker)
Has two central effects to provide antiemetic relief:
1.) Area postrema
2.) Vestibular system

59
Q

What is the MOA of diphenhydramine?

A

Antihistamine (H1 blocker)
Has two central effects to provide antiemetic relief:
1.) Area postrema
2.) Vestibular system

60
Q

What is the MOA of doxylamine?

A

Antihistamine (H1 blocker)
Has two central effects to provide antiemetic relief:
1.) Area postrema
2.) Vestibular system

61
Q

What are some indications for use of antihistamines?

A
  • Nausea/vomiting from vestibular causes
  • Hyperemesis gravidarum
  • Can be used for sedative effect
62
Q

What are some AE of antihistamines?

A

Drowsiness, confusion
Anti-SLUD effects (salivation, lacrimation, urination, defecation all dry up. Can give physostigmine, a cholinesterase inhibitor, to correct)

63
Q

Drugs with the suffix “-prepitant” belong to which class?

A

Neurokinin receptor antagonists

64
Q

What is the MOA of and indication for aprepitant and fosaprepitant?

A

These are neurokinin receptor antagonists used to treat CINV. **Only approved for n/v in cancer patients; used prophylactically.

They inhibit NK1 receptors in solitary nucleus to provide antiemetic effects.

65
Q

What are some AE associated with aprepitant and fosaprepitant?

A
  • Hypersensitivity reactions
  • Infusion site reactions
  • CYP3A4 enzyme inhibition can cause increased levels of other drugs metabolized by the same enzyme
  • He emphasized that these are NOT associated with QT prolongation
66
Q

What classes of drugs are sometimes added onto antiemetic treatment regimens, especially in cancer patients?

A
  • Glucocorticoids (dexamethasone, metylprednisone)
  • Benzodiazapines (lorazepam)
  • Atypical antipsychotics (olanzapine)
  • Cannabinoids (dronabinol, nabilone)
67
Q

What is the MOA of lorazepam?

A

Lorazepam is a benzodiazepine, and its antiemetic effects are likely due to GABA inhibition in the chemo-trigger zone

68
Q

What is the MOA of olanzapine?

A

Olanzapine is an atypical antipsychotic, and its antiemetic effects are due to inhibition of multiple neurotransmitters (dopamine, serotonin, histamine)

69
Q

What are some AE of olanzapine?

A
  • *QT prolongation
  • Sedation
  • Weight gain
  • Iatogenic diabetes, hypertriglyceridemia, hypercholesterolemia
  • Extrapyramidal AEs
70
Q

What are some AEs of cannabinoids?

A
  • Ataxia/Dizziness
  • Dry mouth
  • Eu/dysphoria
  • Paranoia
  • Hallucinations
  • Abdominal pain
  • Paradoxical n/v
71
Q

What is a major difference between the treatment strategies when treating ulcerative colitis vs. Crohn’s disease?

A
  • UC affects the colon only, and almost always includes the rectum.
  • Crohn’s can affect any part of the GI tract from mouth to anus.

It is important to know where we are treating; administration routes may vary depending on location.

72
Q

What would an appropriate treatment for mild ulcerative colitis include?

A
  • Enema of corticosteroid or 5-ASA compound
73
Q

What is a major difference between older and newer 5-ASA-containing drugs used to treat UC and CD?

A
  • Older agents used sulfa to carry the 5-ASA to the gut. Many patients had intolerable AE associated with the sulfa.
  • Newer agents are encapsulated and do not use sulfa, avoiding the associated AE.
74
Q

To what class do mesalamine, olsalazine, balsalazide, and sulfasalazine belong? What is their indication?

A

These are 5-ASA compounds.
The first 3 are newer drugs which avoid use of sulfa.

They are used for the treatment of ulcerative colitis and Crohn’s disease, and can be administered orally or topically (as suppositories, foams, or enemas).

75
Q

When would use of a corticosteroid be appropriate in an ulcerative colitis or Crohn’s patient?

A

When 5-ASA treatments are ineffective, and only for acute bouts.

76
Q

What is the first line treatment for maintenance in ulcerative colitis and Crohn’s disease?

A

Oral 5-ASA agents, such as mesalamine

77
Q

Biologics such as infliximab, adalimumab, etc are indicated for what use?

A

Can be used for Crohn’s disease, both in active disease and maintenance.

  • Use caution and education when treating young patients with these drugs.
  • High risk of opportunistic infections.
78
Q

When should antibiotics definitely be given to a patient with Crohn’s disease?

A

Presence of fistula or when patient is infectious.

Be sure to cover Gram (-) and anaerobes. Consider cipro + metronidazole.

79
Q

What is a rare AE associated with natalizumab?

A

Leukoencephalopathy (mad cow disease). BBW for this.

80
Q

What is the MOA of methotrexate and what is the indication we discussed this module?

A

Methotrexate is an immunomodulator: it blocks DNA synthesis, causing cell death.

It can be considered for use in moderate-severe Crohn’s disease who have failed glucocorticoids.

81
Q

What is the MOA of cyclosporine, and what is the indication we discussed this module?

A

Cyclosporine is has immunosuppressive effects through its antimetabolite actions. Its most common use is post-transplant, but low doses may be used in severe ulcerative colitis when glucocorticoids have failed.

82
Q

What is a steroid-sparing agent that can be added to maintenance therapy for UC and CD?

A

Azathioprine and mercaptopurine (both are immunosuppreants/chemo drugs).
Low doses are used. Lots of labs need to be monitored and cannot be given in pregnancy.

83
Q

Why can’t we just take aspirin for ulcerative colitis?

A

5-ASA has a different structure from aspirin that allows it to work topically rather than via absorption. It is paired with other agents to promote topical delivery and prevent absorption.