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GI Mike Rose > Drugs Week 4 > Flashcards

Drugs Week 4 Flashcards

1
Q

Aprepitant

A

Chemotherapy antiemetic

Substance P receptor antagonist especially of central “high order center” NK1 centers. Involved in central and peripheral vomiting pathway.

Oral (vs. Fosaprepitant)

Given w/ 5HT3 antagonists and Dexamethasone

A.E. Generally well tolerated; fatigue, dizziness, diarrhea

Metabolized by CYP3A4 –> drug interactions w/ cancer drugs –> worry about bone marrow suppression.

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2
Q

Fosaprepitant

A

Chemotherapy antiemetic

Substance P receptor antagonist especially of central “high order center” NK1 centers. Involved in central and peripheral vomiting pathway.

IV (vs. Aprepitant)

Given w/ 5HT3 antagonists and Dexamethasone

A.E. Generally well tolerated; fatigue, dizziness, diarrhea

Metabolized by CYP3A4 –> drug interactions w/ cancer drugs –> worry about bone marrow suppression.

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3
Q

Diphydrinate

A

Antihistamine (anticholinergic)

Antiemetic

A.E. Anitcholinergic (confusion, dry mouth, etc.) ; Drug interactions w/ some abx;

Don’t use w/ morning sickness

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4
Q

Diphenhydramine

A

Antihistamine (anticholinergic)

Antiemetic

A.E. Anitcholinergic (confusion, dry mouth, etc.) ; Drug interactions w/ some abx;

Don’t use w/ morning sickness

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5
Q

Meclizine

A

Antihistamine (anticholinergic)

Antiemetic

A.E. Anitcholinergic (confusion, dry mouth, etc.) ; Drug interactions w/ some abx;

Don’t use w/ morning sickness

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6
Q

Dronibinol

A

Cannabinoid

Act on central cannabinoid receptors. Unknown mechanism, sedation?

Better agents now available, often give w/ phenothiazine –> synergistic

Side effects: sedation, hallucinations, euphoria, dry mouth, and increased appetite (good).

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7
Q

Nabilone

A

Cannabinoid

Act on central cannabinoid receptors. Unknown mechanism, sedation?

Better agents now available, often give w/ phenothiazine –> synergistic

Side effects: sedation, hallucinations, euphoria, dry mouth, and increased appetite (good).

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8
Q

Dexamethasone/Methylprednisolone

A

Unkown MOA

Often given w/ 5HT antagonists and NK1 antagonists.

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9
Q

Balsalazide

A

X-ASA. X group block cox absorbtion in stomach –> bacteria remove X and allow Cox inhibition in colon.

Specific action at colon

First line treatment in mild/moderate UC. Not effective in Crohn’s due to disease severity/inability to get concentrated enough drug.

Minimal A.E.’s.

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10
Q

Mesalamine

A

X-ASA. X group block cox absorbtion in stomach –> bacteria remove X and allow Cox inhibition in colon.

First drug in class; not specific action at colon. Can be used as suppository (rectum only then).

First line treatment in mild/moderate UC. Not effective in Crohn’s due to disease severity/inability to get concentrated enough drug.

Minimal A.E.’s.

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11
Q

Olsalazine

A

X-ASA. X group block cox absorbtion in stomach –> bacteria remove X and allow Cox inhibition in colon.

Specific action at colon

First line treatment in mild/moderate UC. Not effective in Crohn’s due to disease severity/inability to get concentrated enough drug.

Minimal A.E.’s.

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12
Q

Sulfasalazine

A

X-ASA. X group block cox absorbtion in stomach –> bacteria remove X and allow Cox inhibition in colon.

Specific action at colon

First line treatment in mild/moderate UC. Not effective in Crohn’s due to disease severity/inability to get concentrated enough drug.

A.E. Sulfa drug –> hypersensitiivty, decreased folate absorbtion.

40% have severe GI upset, Nausea, headache, arthralgias, and bone marrow suppression.

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13
Q

Budesonide

A

Specific corticosteoid to think of when treating Crohn’s.

Subject to extensive first pass metabolism –> local rather than systemic effects.

Used in mild to moderate Crohn’s disease involving the ileum and proximal colon.

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14
Q

Infliximab

A

TNF-a MAB. Activates compliment.

1/3 of patient’s will become refractory –> will develop antibodies vs. antibodies.

Symptomatic improvement in 60% and remission in 30%

A.E. *infections (TB!) , infusion reactions), severe hepatic problems, possibly increased risk of lymphoma (cause vs. exacerbation debate).

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15
Q

Activated Charcoal

A

Toxin Binding drug used in GI contimination due to its large surface area.

Must be given in at least 10:1 ratio.

Doesn’t bind iron, lithium, or potassium. Binds EtOH and cyanide poorly.

Note useful in cases of poisoning due to corrosive mineral acids or alkalis

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16
Q

Polyethylene Glycol

A

Hastens removal of toxins and reduce absorbtion

Whole bowel irrigation can enhance decontamination following ingestion of iron tablets, enteric coated medicines, illicit drug filled packets, and foreign bodies.

Used before endoscopic procedures

Also used as an osmotic cathartic.

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17
Q

Ipecac

A

Use is controversial, especially if treatment is initiated more than 1 hour after ingestion of poison.

Parents should avoid

Local irritant effect as well as acting on CTZ

Emesis may not occur if stomach is empty

Oral dose –> 15-30 minutes

Used to be OTC. Common in medicine cabinets.

Dangerous if corrosive, a petroleum distillate, or a rapidly-acting convulsant is the toxic substance.

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18
Q

-setrons

A

MOA: Serotonin 5HT3 Antagonists. Blockade of peripheral 5HT3 receptors in GI. Also receptors in CMZ and vomiting centers.

Therapeutic uses: Best for chemo. Prevention (best) and treatment. Useful for ACUTE phase nausea. Also given post op and post radiation. Not good for motion sickness.

Adverse effects: well tolerated; excellent safety profile (esp. compared to alosetron which is used in IBS). MC is constipation, dizziness, mild headach. Small QT elongation (small risk)

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19
Q

Scopolamine

A

Muscarinic and dopaminergic receptor antagonist in cerebellum. Widely distributed in CNS.

Most effective agent for motion sickness.

Given in transdermal patch to decrease side effects.

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20
Q

Droperidol

A

Dopamine (D2) Receptor antagonist

MOA: Antagonist at D2 receptors in CTZ. Resetting GI motility and sedation.

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21
Q

Metocloprimide

A

Dopamine (D2) Receptor antagonist

MOA: Antagonist at D2 receptors in CTZ. Resetting GI motility and sedation. Also decrease DA inhibition of Ach in gut –> increasing motility of entire gut (prokinetic)

Use: Antiemetic, hiccups, and increased gut motility post surgery, vagotomy, gastroparesis, etc.

AE: somnolence, nervousness, agiation, anxiety. Dystonia, parkinsonism, tardive dyskinesia (permanent). Increased prolactin release (impotence, menstral probs, and galactorrhea)

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22
Q

Prochlorperazine

A

Dopamine (D2) Receptor antagonist

MOA: Antagonist at D2 receptors in CTZ. Resetting GI motility and sedation.

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23
Q

Promethazine

A

Dopamine (D2) Receptor antagonist

MOA: Antagonist at D2 receptors in CTZ. Resetting GI motility and sedation.

24
Q

Thiethylperazine

A

Dopamine (D2) Receptor antagonist

MOA: Antagonist at D2 receptors in CTZ. Resetting GI motility and sedation.

25
Q

Azathioprine

A

MOA: Prodrug –> mercaptopurine –> decreased purine synthesis –> decreased DNA synthesis –> decreased B and T cell production.

Given in low doses for the induction and maintenance of remission of UC and Crohn’s. Allow elimination of steroids.

26
Q

6-mercaptopurine

A

MOA: Decreased purine synthesis –> decreased DNA synthesis –> decreased B and T cell production.

Given in low doses for the induction and maintenance of remission of UC and Crohn’s. Allow elimination of steroids.

27
Q

MTX

A

MOA: DHFR blocker –> decreased DNA synthesis –> decreased B and T cell production.

Given in low doses for the induction and maintenance of remission of UC and Crohn’s. Allow elimination of steroids.

28
Q

SSRIs

A

Used in constipation variant IBS.

Increase 5HT in afferent –> increased peristalsis.

29
Q

Methylecellulose

A

Bulk laxative

Increase distension –> increase 5HT afferent –> increased peristalsis

Can act as stool stabilizers –> help both diarrhea and constipation.

Use limited by neurons being present and knowing the cause of constipation.

A.E. Allergies, increased flatulence, increase obstruction.

30
Q

Polycarbophil

A

Bulk laxative

Increase distension –> increase 5HT afferent –> increased peristalsis

Can act as stool stabilizers –> help both diarrhea and constipation.

Use limited by neurons being present and knowing the cause of constipation.

A.E. Allergies, increased flatulence, increase obstruction.

31
Q

Psyllium

A

Bulk laxative

Increase distension –> increase 5HT afferent –> increased peristalsis

Can act as stool stabilizers –> help both diarrhea and constipation.

Use limited by neurons being present and knowing the cause of constipation.

A.E. Allergies, increased flatulence, increase obstruction.

32
Q

Anthraquinone

A

Contact Cathartic

Act on large intestine and is less potent.

MOA: Irritation of mucosa? Unknown.

Side effects: Dependency, destroy myenteric plexus w/ long term use. Melanosis coli.

33
Q

Bisacodyl

A

Contact Cathartic

Act on large intestine and is less potent.

MOA: Irritation of mucosa? Unknown.

Side effects: Dependency, destroy myenteric plexus w/ long term use. Melanosis coli.

34
Q

Castor oil

A

Contact Cathartic (prokinetic)

Act on small and large intestine and is more potent.

MOA: Irritation of mucosa? Unknown.

Side effects: Dependency, destroy myenteric plexus w/ long term use. Melanosis coli.

Castor oil - dehydration, electrolyte imbalance, uterine contraction

35
Q

Alosetron

A

MOA: 5HT3 antagonist that causes constipation (doesn’t work as an antiemetic like other -setron’s

Used in dirrhea dominant IBS as last effort. Compassionate use only.

Side effects: 30% have constipation –> 10% must stop due to this –> 0.1% will require hospitalization. 0.3% develop ischemic colitis. Increased side effects w/ inhibitors of CYP1A2 (antidepressants)

36
Q

Cisapride

A

MOA: 5HT4 (and some 5HT3) receptor agonist –> increased release of NT from afferent –> increased peristalsis.

Therapeutic use: Use when no other options. Diabetic constipation.

AE - CV toxicity (esp. long QT) –> 85% had preexisting long QT and/or concomitant admin of cyp3A4 inhibitors.

37
Q

Tegaserod

A

MOA: 5HT4 receptor agonist –> increased release of NT from afferent –> increased peristalsis.

Therapeutic use: Use when no other options. Constipation dependent IBS.

AE - CV toxicity (esp. long QT) –> 85% had preexisting long QT and/or concomitant admin of cyp3A4 inhibitors.

38
Q

Loperamide

A

MOA: Stimulation of enkephalin interneuron (normally inhibited by 5HT) which inhibits peristalsis. Doesn’t cross BBB –> no addictive/euphoric properties (except w/ blockers of p glycoprotein. I.e. Ca blockers or PPIs)

Therapeutic Use: Diarrhea

AE: Abdominal cramps. Toxic megacolon (esp. if pt has UC).

Strongest antidiarrheal and better if diarrhea has started.

39
Q

Diphenoxylate

A

MOA: Stimulation of enkephalin interneuron (normally inhibited by 5HT) which inhibits peristalsis. Some can cross BBB –> give w/ atropine for synergy and AEs at euphoric dosese

Therapeutic Use: Diarrhea

AE: Abdominal cramps. Toxic megacolon (esp. if pt has UC). Euphoria and physical dependence.

Strongest antidiarrheal and better if diarrhea has started.

40
Q

Alvimpopan

A

MOA: mu receptor antagonists –> block opiate induced constipation.

Use: Short term hosptial patients

AE: MI risk.

41
Q

Methylnaloxone

A

MOA: mu receptor antagonists –> block opiate induced constipation

Use: long term use in chronic pain pts/palliative care.

42
Q

Domperidone

A

Dopamine (D2) Receptor antagonist

MOA: Decrease DA inhibition of Ach in gut –> increasing motility of entire gut (prokinetic)

Use: Compassionate use only. Esp gastroparesis.

AE: somnolence, nervousness, agiation, anxiety. Dystonia, parkinsonism, tardive dyskinesia (permanent). Increased prolactin release (impotence, menstral probs, and galactorrhea)

43
Q

TCAs

A

MOA:

  1. )Decrease reuptake of NE from postganglionic symp neurons –> increase activation of alpha-2 presynaptic terminals of Ach postganglionic parasympathetic nerves –> decreased Ach release –> decreased motility
  2. ) Decrease reuptake of DA –> increase actiavtion of D2 –> decrease Ach and motility
44
Q

Atropine

A

MOA: Antimuscarinic. Decreased peristalsis (given w/ diphenxolate for synergism and antiabuse)

45
Q

Macrolides

A

Stimulate motilin receptors at subclinical doses.

AE: increase resistance to gut flora to macrolides

Goal is to get motilin receptor agonist w/o ABX properties.

46
Q

Lubriprostone

A

MOA: CIC-2 stimulant. Increased Cl- secretion.

Use: Chronic constipation; constipation predominant IBS

AE: Very little absorbtion –> minimal. Diarrhea, Nausea, headache; fetal loss in animals

47
Q

Linaclotide

A

MOA: Activates guanyl cyclase c –> activates CFTR –> increase Cl- secretion.

Therapeutic uses: Constipation; IBS

AE: Diarrhea; maternal death; increase in juvenile mortality

48
Q

Crofelemer

A

MOA: Voltage independent inhibition of CFTR.

Use: HIV diarrhea due to NRTI and proteases.

AE: Little systemic absorbtion

49
Q

Octreotide

A

MOA: Somatostatin analog w/ long half life (6-12hrs.). Decreases fluid secretion. Low doses increase motility and high doses inhibit motility.

Use: Off label for severe diarrhea due to dumping syndrome, short bowel syndrome, vagotomoy, AIDS

AE:

  • Impaired pancreatic secretion (steatorrhea and poor fat absorbtion)
  • Decreased GI motility (Nausea, abd. pain, flatulence)
  • Decreased gallbladder activity (stones)
  • Poor release of insulin/glucagon
  • Hypothyroidism
  • Bradycardia
50
Q

Bismuth Subsalicylate

A

MOA: Salicylate decreases PG and Cl- secretion in LI. Antimicrobial; binds enterotoxins.

Use: Prevention of traveler’s diarrhea.

Not as effective as loperamide once diarrhea has started.

AE: blackening of stool/tongue. Salicylate tox at high doses.

51
Q

Lactulose

A

Osmotic cathartic

MOA: Not absorbed –> osmosis

Use: Constipation esp. when enteric nervous system is disrupted. Decreases plasma ammonia by increasing growth of bacteria that make NH4+ –> hepatic encephalopathy.

AE: Bacterial overgrowth –> flatulence/abdominal discomfort

If systemically absorbed –> intravascular volume depletion and electrolyte imbalances. Safe in most patients, but dangerous in frail, elderly, renal insuf, cardiac disease.

52
Q

Magnesium hydroxide

A

Osmotic cathartic

MOA: Not absorbed –> osmosis

Use: Constipation esp. when enteric nervous system is disrupted.

AE: High magnesium in renal failure pts.

If systemically absorbed –> intravascular volume depletion and electrolyte imbalances. Safe in most patients, but dangerous in frail, elderly, renal insuf, cardiac disease.

53
Q

Sodium phosphate

A

Osmotic cathartic

MOA: Not absorbed –> osmosis

Use: Constipation esp. when enteric nervous system is disrupted. Decreases plasma ammonia by increasing growth of bacteria that make NH4+ –> hepatic encephalopathy.

AE: If systemically absorbed –> intravascular volume depletion and electrolyte imbalances. Safe in most patients, but dangerous in frail, elderly, renal insuf, cardiac disease.

54
Q

Cholestyramine

A

MOA: Decrease reabsorbtion of bile salts. In secretory diarrhea (crohn’s or ileal resection) they bind unabsorbed bile salts to decrease H20 secretion

AE: GI bloating, flatulence, constipation, fecal impact ion. Impaired absorbtion of other drugs and ADEK

55
Q

Colestipol

A

MOA: Decrease reabsorbtion of bile salts. In secretory diarrhea (crohn’s or ileal resection) they bind unabsorbed bile salts to decrease H20 secretion

AE: GI bloating, flatulence, constipation, fecal impact ion. Impaired absorbtion of other drugs and ADEK

56
Q

Docusate

A

MOA: Surfactant that lubricates stool

Use: widespread; ? effectiveness

Few AEs

57
Q

Mineral Oil

A

MOA: Lubricates stool

Use: widespread; ? effectiveness

AE: Severe lipid pneumonitis if aspirated. Decreased absorbtion of ADEK

GI Mike Rose (6 decks)

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