Gastrointestinal Drugs II Flashcards

1
Q

Causes of gastroesophageal reflux

A
  • Lower esophageal sphincter - inappropriate relaxation, low resting tone, anatomical alteration
  • Acid hypersecretion
  • Decreased acid clearance due to impaired peristalsis or abnormal saliva production
  • Delayed gastric emptying and/or duodenogastric reflux of bilee salts and pancreatic enzymes
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2
Q

GERD lifestyle Tx

A
  • Elevate head of bed
  • Avoid food/liquid 2-3 hrs before bedtime
  • Avoidance of fatty or spicy food
  • Avoidance of cigs/alcohol
  • Weight loss
  • Liquid antacid
  • Pregnancy
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3
Q

Tx of GERD in patients w/o Esophagitis

A
  • Alginic acid antacids
  • Promotility drugs - cisapride, metoclopramide
  • H2 blockers - cimetidine, ranitidine, famotidine, nizatidine
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4
Q

Tx of GERD of patients w/ esophagitis

A
  • H2 blockers
  • OR
  • H2 recceptor blockers + promotility agent
  • OR
  • PPI
  • OR
  • Anti-reflux surgery
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5
Q

MOA of promotility drugs to treat GERD?

A

Promotility drugs prevent acid from sitting in stomach too long

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6
Q

What are the promotility drugs?

A

Metochlopramide, cisapride

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7
Q

SE of promotility drugs?

A

Tremor

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8
Q

What is vomiting mediated by?

A

Chemoreceptor Trigger Zone and Vomiting Center in the Medulla

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9
Q

What is vomiting stimulated by?

A

Local irritation or CNS stimulation

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10
Q

Metabolic consequences of vomiting?

A
  • Dehydration
  • Hypochloremic metabolic alkalosis
  • Hypokalemia (Kidney reuptake of acid results in K+ loss)
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11
Q

What are the classes of antiemetics?

A
  • Phenothiazines
  • Benzamide
  • Tetrahydrocannabinol
  • Serotonin (5HT3) receptor antagonists
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12
Q

What are the phenothiazines?

A

The neuroleptic class

  • Prochlorperazine
  • Promethazine
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13
Q

MOA of Phenothiazine? Promethazine?

A
  • Prochlorperazine - Dopaminergic receptor antagonist
  • Promethazine - H1 anticholinergic
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14
Q

SE of prochlorazine and promethazine?

A
  1. Prochlorperazine - Torticollis
  2. Promethazine - Somnolence
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15
Q

Adverse effects of Benzamide derivatives?

A

Extrapyramidal Syx (but ont as severe phenothiazines)

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16
Q

What are the Benzamide derivatives?

A
  • Trimethobenzamide
  • Metochlopramide
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17
Q

MOA of Trimethobenzamide and Metochlopramide?

A
  • Trimethobenzamide - unknown effects on CRTZ
  • Metochlopramide - CNS and peripheral dopaminergic receptor antagonism
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18
Q

MOA of THC?

A

Suppress the CRTZ by probable anticholinergic mechanism

19
Q

What are the 5HT3 blockers?

A

Ondansetron, Granesitron, Dolasetron

20
Q

Adverse SE of 5HT3 antagonists?

A

Headache, dizziness, somnolence

21
Q

Tx strategy for gastroparesis?

A

Metochlopramide, cisapride, domperidone

22
Q

5 Types of diarrhea?

A
  1. Secretory - Na and Cl secretion/decreased reabs
  2. Osmotic - Nonabs molecules in gut lumen
  3. Inflammatory absorptive surface - Destruction of mucosa, impaired abs, outpouring of blood, mucus
  4. Decreased abs - impaired reabs of electrolytes
  5. Motility disorder - Increased motility/decreasd motility with bacterial growth
23
Q

What are the goals to treat diarrhea?

A

Decrease GI secretion and decrease GI motility

24
Q

What are the classes for diarrhea Tx?

A
  • Anticholinergics
  • Opioid Agonists
  • Colloids
  • Pectins
25
Q

Anticholinergic drugs to treat diarrhea?

A

Atropine sulfate

26
Q

MOA of loperamide?

A

Immodium! increase rectal tone and disrupt peristalsis via mu receptor

27
Q

MOA of diphenoxylate and codeine sulfate?

A

Mu-R agonist causing contraction of circular muscle “segmentation”

28
Q

What are the colloids and pectins and what is their MOA?

A
  • Colloid - Metamucil
  • Pectin - Kaopectate

Bulk up stool

29
Q

What is the treatment for constipation?

A

Laxatives or cathartics

30
Q

What are the classes of treatments for constipation?

A
  • Irritants/Stimulants
  • Osmotic cathartics
  • Bluk-forming (hydrophilic colloids)
  • Lubricants and fecal softeners
31
Q

What are the irritants/stimulants?

A

Castor oil, cascara sagrada/aromatic fluid extract, senne extract, bisacodyl, phenolphthalein

32
Q

What are the osmotic cathartics?

A

Magnesium citrate solution, magnesium sulfate, sodium sulfate, milk of magnesia, sodium phosphate, lactulose

33
Q

What are the bulk forming colloids?

A

psyllium seed (metamucil), methycellulose, sodium carboxymethylcellulose

34
Q

What are the lubricant and fecal softeners?

A

Mineral oil, dioctyl sodium sulfo-succinate, poloxalkol

35
Q

What is the likely the etiology of the inflammatory bowel diseases?

A

Likely autoimmune

36
Q

What are the acute treatments for inflammatory bowel diseases?

A
  1. Anti-inflammatories
  2. Cortiocsteroids
  3. Antibiotics
37
Q

What are the antiinflammatory drugs, and what do they target?

A
  1. Mesalamine - delayed release for terminal ileum, colon
  2. Sulfasalazine - ulcerative colitis (colon)
  3. Olsalazine - ulcerative colitis
38
Q

What is the mechanism of sulfasalazine? What causes its SEs?

A

Sulfasalazine is hydrolyzed into 5-ASA (mesalamine - active drug) and sulfapyridine. Sulfapyridine causes side effects

39
Q

What makes olsalazine so special?

A

It is a dimer of mesalamine and has few side effects!

40
Q

What are the drugs used to treat ulcerative colitis and chron’s disease (chronic Tx)?

A

Immunosuppressive agents:

  1. Azathiprine - purine antimetabolite that interferes with DNA synth
  2. Corticosteroids
  3. Infliximab - binds to and neutralizes TNFalpha
  4. Cyclosporine - suppresses T helper and T suppressor lymphocytes
41
Q

What are the drugs used to treat Irritable Bowel syndrome?

A
  1. Bulking agents (metamucil)
  2. Opioids - loperamide
  3. Anticholinergics - antispasmodics - Dicyclomine hydrochloride, hyoscyamine sulfate
  4. Antidepressants
42
Q

What antidepressant is used for diarrhea predominant irritable bowel syndrome? Constipation predominant?

A
  • Alosetron for diarrhea predominant (5HT3 antagonist)
  • Tegaserod maleate for constipation predominant (5HT4 agonist)
43
Q

What conditions affect the large bowel? Small bowel?

A
  • Large - Ulcerative colitis, granulomatous (Chron’s) colitis
  • Small - Chron’s disease