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DERS Pharm > GI Drugs 2 > Flashcards

GI Drugs 2 Flashcards

1
Q

Examples of laxatives

A
  • Bulk Forming Laxatives
  • Cathartics (Stimulant Laxatives)
  • Stool Softeners
  • Lubricant Laxatives
  • Osmotic Laxatives
  • Selective Mu-Opioid Receptor Antagonists
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2
Q

These drugs are Non-digestible colloids which absorb water to form a bulky, soft jelly that distends the colon to promote peristalsis

A

Bulk-Forming Laxatives:

Methylcellulose
Psyllium
Bran

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3
Q

When are Methylcellulose, Psyllium and Bran contraindicated?

A

in patients who are immobile or in long-term opioid therapy as intestinal obstruction may result

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4
Q

Examples of Cathartics (Stimulant laxatives)

A

Bisacodyl
Senna
Caster oil

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5
Q

This laxative acts on nerve fibers in the mucosa of the colon and causes minimal systemic absorption

A

Bisacodyl

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6
Q

This laxative causes water and electrolyte secretion into the bowel; chronic use may lead to melanosis coli

A

Senna

melanosis coli: a harmless brown pigmentation of the colonic mucosa unrelated to colon cancer risk

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7
Q

This laxative is broken down into ricinoleic acid in the small intestine and is contraindicated in pregnancy as this may cause uterine contractions

A

Castor oil

  • Required on a long-term basis for patients who are neurologically impaired and in bed bound patients
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8
Q

Who are the stool softeners

A

Docusate and Glycerin

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9
Q

Function of lubricant laxatives such as mineral oil

A

coats fecal material preventing water reabsorption

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10
Q

What should not be given with mineral oil

A

Docusate

- the mineral oil will be absorbed into the stool thereby negating its laxative effects

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11
Q

Non-absorbable sugars or salts which exert an osmotic pull to retain water in the intestinal lumen

A

Osmotic laxatives

- lactulose, magnesium salts, polyethylene glycol

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12
Q

This drug is metabolized by colonic bacteria and can lead to severe flatus with abdominal cramping

A

Lactulose

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13
Q

This drug should not be used for prolonged periods in persons with renal insufficiency as they may cause hypermagnesemia

A

Magnesium salts

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14
Q

This drug is commonly used for complete bowel preparation before gastrointestinal endoscopic procedures and does not produce significant flats or cramping

A

Polyethylene glycol (PEG)

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15
Q

This drug stimulates the type 2 chloride channels of the small intestine and increases secretion of chloride-rich fluid which stimulates intestinal motility

A

Lubiprostone

- Indicated for chronic constipation and IBS with predominant constipation

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16
Q

Adverse effects of lubiprostone

A
  • Diarrhea (most common)

* Contraindicated in children

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17
Q

Who are the Selective Mu-Opioid Receptor Antagonists?

A

Alvimopan
Methylnaltrexone

  • Act at the level of the gut to maintain normal motility
  • Do not cross the blood-brain barrier and thus do not negate the analgesic effect of opiods
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18
Q

Analogs of the opioid meperidine which activates presynaptic mu- opioid receptors in the enteric nervous system to inhibit ACh release and decrease gut peristalsis

A

Opioid agonists
- loperamide and diphenoxylate

Both drugs are contraindicated in children and patients with severe colitis

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19
Q

This opioid agonist does not cross blood brain barrier and has no analgesic properties or potential for addiction

A

Loperamide

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20
Q

This opioid agonist at higher doses can have CNS effects and with prolonged use that leads to opioid dependence

A

Diphenoxylate

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21
Q

synthetic octapeptide with 30x the serum half-life of somatostatin

A

Octreotide

Somatostatin analog

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22
Q

When do you use octreotide ?

A
  • Secretory diarrhea due to neuroendocrine tumors such as carcinoid and VIPoma
  • Diarrhea caused by vagotomy, dumping syndrome, short bowel syndrome and AIDS
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23
Q

Adverse effects of octreotide

A

• Decrease pancreatic exocrine function
- resultant steatorrhea —> deficiency of fat-soluble vitamins
• Inhibition of gallbladder contractility leads to formation of biliary sludge which may precipitate gallstones

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24
Q

Which drug controls traveller’s diarrhea by decreasing fluid secretion in the enteric tract

A

Bismuth subsalicylate (Pepto-Bismol)

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25
Q

First line strategy to treat irritable bowel syndrome

A

1) Exclusion of gas-producing foods
2) Diet low in fermentable oligo-, di-, and monosaccharides and polyols (FODMAPs)
3) Lactose and/or gluten omission

Moderate to severe symptoms that impair quality of life qualify for pharmacologic intervention

26
Q

Drugs to treat constipation predominant IBS

A
  • Psyllium
  • Lubiprostone
  • Polyethylene Glycol
  • Docusate
27
Q

Drugs used to treat diarrhea predominant IBS

A
  • Loperamide (opioid agonist)
  • Alosetron ( 5-HT3 antagonist )- reduce nausea and vomiting
  • Anticholinergics (Hyoscyamine, Dicyclomine, Glycopyrrolate, Methscopolamine)
28
Q

Mild IBD is characterized by

A
  • Ambulatory
  • Tolerating orally
  • < 10% weightloss
  • No symptoms of systemic disease or bowel obstruction
29
Q

Moderate to severe IBD IS CHARACTERIZED By

A
  • Failed treatment for mild to moderate disease
  • Intermittent nausea or vomiting
  • > 10% weightloss
  • Fever
  • Abdominal pain
  • Anemia
30
Q

Severe to fulminant IBD is characterized by

A
  • High fevers
  • Persistant vomiting
  • Intestinal obstruction
  • Peritoneal signs
  • Cachexia
31
Q

Treatment for mild IBD

A

Tropical corticosteroids
Budesonide
Antibiotics
5-ASA

32
Q

Treatment for moderate IBD

A

Oral corticosteroids
TNF Antagonists
Methotrexate
Azathioprine

33
Q

Treatment for severe IBD

A 
IV Corticosteroids 
TNF Antagonists 
Cyclosporine 
Natalizumab
Surgery
34
Q

Drugs used for long term maintenance of IBD remission

A

Aminosalicylates: Active group is 5-aminosalicylic acid (5-ASA)

Sulfasalazine
Balsalazide
Mesalamine

35
Q

MOA of Aminosalicylates

A
  • Inhibition of the activity of nuclear factor-κB (NF- κB): an important transcription factor for proinflammatory cytokines
  • Inhibition of cellular immunity mechanisms
  • Modulation of both cyclooxygenase and lipoxygenase pathways
36
Q

Clinical efficacy of 5ASA

A

Needs to achieve high concentrations at the target sites
• given orally- completely absorbed by the jejunum
• No therapeutic effect in the more distal ileum, colon and rectum would be obtained
• Suppository or enema if isolated sigmoid colon or rectal disease

37
Q

Composition of sulfasalazine

A

5ASA linked to sulfapyridine by an Azo bond

38
Q

sulfasalazine is reduced by coli form bacterial enzyme called_______ to sulfapyridine and 5ASA

A

Azoreductase

5 ASA may backwash into the terminal ileum to act there

39
Q

Adverse effects of Aminosalicylates

A
  • Nausea
  • GI upset
  • Headaches
  • Arthralgias
  • Myalgias
  • Bone marrow suppression
  • Hypersensitivity reactions
40
Q

This drug involves 5-ASA linked to an inert, unabsorbed carrier molecule that allows maximal amounts of 5-ASA to be delivered to the colon

A

Balsalazide

41
Q

This drug involves Physically packaged 5-ASA in extended release or pH sensitive microgranules that release the active drug into the desired specific portion of the gut actively affected by IBD

A

Mesalamine

42
Q

List the glucocorticoids used in IBD

A

Prednisone
Prednisolone
Budesonide

43
Q

How do glucocorticoids work

A
  • Inhibition of phospholipase A2 and cyclooxygenase

- Inhibition of nuclear factor-κB

44
Q

Glucocorticoids of choice for oral therapy

A

Prednisone and prednisolone

45
Q

_________is administered via enema for sigmoid and rectal IBD flares

A

Hydrocortisone

46
Q

Adverse effects of glucocorticoids

A
  • Adrenal suppression - Immunosuppression - Hyperglycemia - Osteoporosis
47
Q

This drug treats

  • Topical effects on the luminal surface of the inflamed bowel
  • Following enteric absorption, undergoes rapid first-pass metabolism thus has low systemic bioavailability
  • Significantly decreased rate of systemic adverse effects a compared to prednisone
A

Budesonide

48
Q
  • Immunosuppressive purine analogs
  • Indicated for induction and maintenance of IBD remission
  • Steroid-sparing effect
A 
Immunosuppressants: 
Mercaptopurine (6-MP) 
Azathioprine
Methotrexate
Cyclosporine
49
Q

Adverse effects of immunosuppressants

A
  • Nausea
  • Vomiting
  • Bone marrow depression
  • Hepatotoxicity
50
Q

Allopurinol reduces _______ activity which can increase serum concentration of 6-thioguanine nucleotides to precipitate life-threatening leucopenia

A

Xanthine oxidase

• Use allopurinol with caution in patients taking 6-MP or azathioprine

51
Q
  • Inhibits dihydrofolate reductase, an enzyme important in the production of thymidine and purines
  • Reduces the inflammatory actions of Interleukin-1
  • Stimulates increase release of adenosine
A

Methotrexate

52
Q

Adverse effects of methotrexate

A
  • Bone marrow depression • Megaloblastic anemia

* Mucositis

53
Q

Explain the relationship between cyclosporine and calcineurin

A

Calcineurin activates NFAT which is required for induction of cytokine genes

Cyclosporine forms a complex with cyclophilin—>
immunophilin

This complex inhibits calcineurin

54
Q

Adverse facets of cyclosporine

A
  • Nephrotoxicity
  • Neurotoxicity
  • Hypertension
  • Hyperkalemia
  • GI complaints
  • Hyperglycemia
55
Q

Anti – TNF - α Drugs for IBD

A

Infliximab: for moderate to severe colitis which is not responsive to mesalamine or corticosteroids

Adalimumab

56
Q

Function of Anti – TNF - α Drugs

A

Bind and inactivate human Tumor Necrosis Factor (TNF): • TNF is a key mediator of:

  • Release of proinflammatory cytokines
  • Stimulation of hepatic acute phase reactants
  • Upregulation of endothelial adhesion molecules promoting leukocyte migration
57
Q

Adverse effects of Anti – TNF - α Drugs

A

• Suppression of Th1 activity:
- fungal disease
- Reactivation of latent tuberculosis
• Antibodies may develop against these biologics:
- Elimination of clinical response to therapy
- Acute or delayed infusion reactions
• Increased risks of lymphoma, acute hepatic failure and congestive heart failure have also been reported

58
Q
  • Humanized monoclonal antibody targeting several integrins on circulating inflammatory cells
  • Disruption of leukocyte vascular wall adhesion and subsequent tissue migration
  • Indicated in moderate to severe, unresponsive Crohn’s disease
A

Anti- Integrins

- natalizumab

59
Q

Adverse effects of natalizumab

A
  • Infusion reactions
  • Opportunistic infections
  • Reactivation of the human polyomavirus (JC virus) resulting in progressive multifocal leukoencephalopathy
60
Q

Causes of exocrine pancreatic insufficiency ( when secretion of pancreatic enzymes fall below 10% of normal)

A

Cystic fibrosis
Chronic pancreatitis
Pancreatic resection

Presents with stentorian, ADEK vitamin malabsorption, weight loss

61
Q

Pancrelipase

A
  • Combination of amylase, lipase and proteases which are rapidly degraded by gastric acids
  • Enteric-coated formulations should be used or non-coated forms given with acid suppression therapy
  • Given by mouth with each meal
62
Q

Adverse effects of pancrelipase

A

• Diarrhea
• Abdominal pain
Rare: hyperuricosuria, renal stones, colonic strictures

DERS Pharm (9 decks)

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