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Pharmacology > Exam 4 GI + Pain > Flashcards

Exam 4 GI + Pain Flashcards

1
Q

Nociceptive pain

A

Nerve receptor stimulation following tissue injury, disease or inflammation

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2
Q

Neuropathic pain

A

Abnormal signal processes in the CNS, perceived as burning, tingling, shooting

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3
Q

Neurotransmitters involved in pain

A

Prostaglandins, histamine, bradykinin, serotonin

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4
Q

Main inhibitory neurotransmitters

A

Serotonin and norepinephrine

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5
Q

Acetaminophen

A

Prostaglandin inhibitor in CNS and COX3
No anti-inflammatory, platelet or GI effects
Decreases opioid requirements by 30%

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6
Q

Aspirin

A

Effective as APAP
Very effective in pain associated with inflammation
GI side effects
Irreversible inactivation of COX1 and COX2

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7
Q

COX1 inhibition

A

Leads to decreased blood flow to kidney, GI tract tissues and decreases platelet aggregation

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8
Q

COX2 inhibition

A

Decreases inflammation

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9
Q

Misoprostol (Cytotec)

A

Can decrease NSAID induced bleeding
Synthetic prostaglandin E analog parent drug rapidly de-esterified to misoprostol acid and replaces protective prostaglandins
Inhibits gastic acid secretions and protects gastric mucosa
Pregnancy category X
SE: diarrhea, abdominal pain, HA

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10
Q

Ketorolac (Toradol)

A

First parenteral NSAID available

Use limited to <5 day due to SE profile

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11
Q

Effects of opioids

A

Analgesia, respiratory depression, sedation, confusion, N/V, pruritus, miosis, constipation, urinary retention

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12
Q

Opioid DOC in renal or liver failure

A

Fentanyl

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13
Q

Fentanyl forms

A

Injectable, buccal, long acting transdermal patch (duration of 72 hours)
Causes less histamine release than other opioids

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14
Q

Tramadol

A

Centrally acting weak mu receptor agonist; also inhibits NE reuptake and increases serotonin release
Less respiratory depression
May increase risk of seizures

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15
Q

Methadone

A

Used to treat opioid substance abuse
Mu receptor agonist and NMDA receptor antagonist
8-12 hours duration if used chronically
Cheap and good for refractory pain

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16
Q

Naloxone

A

pure opioid antagonists
Used for opioid induced respiratory depression
Lasts 45 minutes
SE: tachycardia, htn, V Fib, cardiac arrest, seizures

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17
Q

Opioid treatments of constipation

A

Methylnaltrexone or naloxegel

Mu antagonism in gut only

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18
Q

Withdrawal symptoms of opioid use

A

Tremors, sweating, fever, flu like symptoms, increased RR, perspiration, lacrimation, mydriasis, anorexia

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19
Q

Co-analgesics

A

Antidepressents, anticonvulsants, sodium channel blockers, antispasmodics, antispastics

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20
Q

Antidepressants for pain relief

A

TCAs and SNRI

Good for neuropathic pain

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21
Q

Anticonvulsants for pain relief

A

Gabapentin, pregabalin, carbamezapine usually
Decrease activation of second order neurons responsible for pain transmission
Good for neuropathic pain

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22
Q

Sodium channel blockers

A

Act as local anesthetics
Block Na channels, slowing pain transmission and lowering firing threshold of second order neurons
Topical lidocaine patches indicated for postherpetic neuralgia

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23
Q

Ketamine

A

NMDA antagonist
Lower doses for analgesia, higher doses for anesthesia
Decreases sensitivity to pain impulses
SE: vivid dreams, sedation, delirium, hallucinations

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24
Q

Cyclobenzapine

A

Antispasmodic skeletal muscle relaxant
Mostly used for lower back pain
Has anticholinergic SE

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25
Q

Baclofen

A

Antispastic agent

Used for MS and spinal cord injuries

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26
Q

Hydromorphone

A

Dilaudid
More potent than morphine, safer in renal failure, more soluble
Good choice for opioid tolerant patients or cachectic patients

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27
Q

Codeine

A

Weak opioid activity by itself; usually combine with APAP
Metabolized to morphine by the liver
Ceiling effect on analgesia but not side effects

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28
Q

Meperidine

A 
Demerol
Not first line
Short duration of action
Low potency 
Very long half life 
Avoid in renal dysfunction or hx of seizures
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29
Q

Steroids useful for what type of pain

A

Bone pain and nerve compression

Dexamethasone and prednisone

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30
Q

Herb-drug interactions

A
  • Taking Senna can affect drug transit time and reduce absorption of prescription medicines
  • Zinc lozenges decrease levels of antibiotics
  • High doses of vitamin E may increase anticoagulant effect of warfarin
  • Taking ephedra with caffeine can cause death
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31
Q

Dronabinol + Nabilone

A

Both synthetic THC approved for treatment of N/V associated with cancer chemotherapy
SE: dry mouth, sedation, orthostatic hypotension, ataxia, dizziness, anxiety, tachycardia, agitation, confusion

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32
Q

Neurotransmitters involved with the vomiting center

A

Dopamine, histamine, serotonin, ACh

Antiemetic effects occur when these neurotransmitters are blocked

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33
Q

Phenothiazines

  • MOA
  • SE
  • Uses
A

Prochlorperazine + Promethazine
Dopamine receptor blockade in chemo trigger zone
Has anticholinergic activity also
SE: drowsiness, sedation, increased EPS, CNS depression
Preg Category C
Monotherapy for mild-moderate N/V or long term therapy

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34
Q

Antihistamines

  • MOA
  • SE
  • Uses
A

Hydroxyzine, meclizine, dimenhydrinate (dramamine), scopolamine
Interrupts visceal afferent pathways responsible for N/V
Can be used in pregnancy but not BF
Used for mild nausea such as motion sickness
SE: sedation, drowsiness, confusion, anticholinergic effects
CI: asthma, glaucoma, GI/urinary obstruction

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35
Q

Benzodiazepines for N/V

  • MOA
  • SE
  • Uses
A

Lorazepam (ativan) most frequently used
Prevent/treat emesis as well as anxiolysis and amnesia
Helpful for anticipatory nausea/vomiting with chemo
SE: CNS depression, memory impairment, constipation, headache, change in appetite
CI: hepatic or renal failure
Pregnancy D

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36
Q

Serotonin antagonists

  • MOA
  • SE
  • Uses
A

Ondansetron (Zofran), Granisetron, Palonestetron, Dolasetron
Antagonize 5HT3 receptors centrally in CTZ and peripherally at vagal and splanchnic afferent fibers
Used for chemo N/V or hyperemesis gravidarum primarily
SE: mild to moderate HA, diarrhea, increase in liver enzymes
CI in lactation
Does not cause EPS symptoms

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37
Q

Metoclopramide (Reglan)

  • MOA
  • SE
  • Uses
A

Used for N/V related to diabetic gastric stasis, post surgical gastric stasis, GERD, migraine HA
Increases motility and gastric emptying
Dopamine receptor inhibition in CTZ
Sensitizes tissues to Ach
SE: EPS, diarrhea
Hypertensive crisis can occur when used with MAOI
Preg Cat B

38
Q

Steroids for N/V

  • MOA
  • SE
  • Uses
A

Reserved for chemo induced N/V
Dexamethasone + methylprednisolone most used
SE: mental disturbances, headaches, insomnia, restlessness, increase in glucose levels, immunosuppression, osteoporosis

39
Q

Dronabinol

  • MOA
  • SE
  • Uses
A

Cannibinoid
Administer 6-12 hours prior to chemo
SE: sedation, ataxia, dysphoria, orthostatic hypotension, blurred vision, tachycardia, appetite stimulation

40
Q

Antacids

  • MOA
  • SE
  • Uses
A

Mg, Al or Ca salts
Coat stomach with a neutralizing substance
For mild N/V
By increasing pH, pepsin is inhibited

41
Q

1st line for non-chemo N/V

A

Ondansentron
Phenothiazine
Promethazine

42
Q

2nd line for non-chemo N/V

A

Antihistamine/anticholinergic

43
Q

1st line for acute emesis in chemo N/V

A

Combo of serotonin antagonist and steroids minutes before chemo

44
Q

What is responsible for gastric mucosal damage

A

HCl and pepsin

45
Q

What stimulates parietal cells to release acid

A

Histamine, ACh, gastrin

46
Q

What decreases gastric acid production

A

Prostaglandins and bicarbonate

-H Pylori and NSAIDs impede these defenses

47
Q

Effect of H Pylori

A

Increases acid production, gastric secretions and secretes noxious enzymes and toxins

48
Q

H2 receptor antagonists

A

Cimetidine (tagamet), famotidine (pepcid), nizatidine, ranitidine (zantac)
Effective in mild GERD, ulcer healing, H Pylori eradication
Reversibly inhibits H2 on gastric pariertal cells, decreasing acid secretion and pepsin activation

49
Q

Proton pump inhibitor

A

Omeprazole (Prilosec), Pantoprazole (Protonix)
Most potent acid-suppressing agent
Binds to H+/K+ ATPase in gastric parietal cells–causes decrease basal and stimulated acid secretion
Moderate to severe GERD, revention of NSAID induced ulcer, ulcer healing
Irreversibly inhibits gastric proton pumps
Category C pregnancy, CI in BF
SE: HA, N/V, abdominal pain, flatulence

50
Q

Antibiotics used in H Pylori eradication

A

Amoxicillin, Clarithromycin, Metronidazole, Tetracycline, Misoprostol

51
Q

Tx of NSAID induced ulcer

A

PPI for 4 weeks and D/C NSAID

52
Q

Triple therapy for H Pylori

A

PPI, amoxicillin and clarithromycin for 7-10 days
OR
PPI, metronidazole and clarithromycin 10-14 days

53
Q

2 step therapy for H Pylori

A

PPI and amoxicillin for 5 days followed by PPI, clarithromycin and metronidazole for 5 days

54
Q

Bulk forming laxatives

  • Examples
  • MOA
  • SE
  • CI
A

Methylcellulose, psyllium (metamucil), polycarbopil, malt soup extract, wheat dextin
Non-digestible and non-absorbable
Binds to fecal contents and pulls water into stool–softens and lubricates stool
Take with plenty of water
Not systemically absorbed
SE: increased gas and bloating
CI: strictures of esophagus, GI ulcerations, stenosis

55
Q

Hyperosmotic laxatives

  • Examples
  • MOA
  • SE
  • CI
A

Lactulose, sorbitol, polyethylene glycol (Miralax)/electrolyte solution, polyethyle glycol, magnesium hydroxide, magnesium citrate
Increases concentration of solutes, creating osmotic pressure by drawing more fluid into GI tract
Glycerine safest–use in children
SE: abdominal cramping and nausea
CI: diabetic patients and appendicities, fecal impaction or intestinal obstruction

56
Q

Saline laxatives

  • Examples
  • MOA
  • SE
  • CI
A

MgOH, Mg Citrate, Mg Sulfate, Na phosphate
Draw water into intestines through osmosis
May cause dehydration

57
Q

Stimulant laxatives

  • Examples
  • MOA
  • SE
  • CI
A

Bisacodyl (dulcolax) + Senna concentrates
Increases peristalsis through direct effects on smooth muscle of intestine and promotes fluid accumulation in colon
Avoid long term
SE: N/V, Cramping

58
Q

Surfactant laxatives

  • Examples
  • MOA
  • SE
  • CI
A

Ducosate Sodium (colace)
Stool softeners–decrease surface tension of liquid contents of bowel by promoting additional lipid into the stool
Inhibits fluid and electrolyte reabsorption
DOC for patients who should not strain
Take with plenty of water

59
Q

Lubricant laxatives

  • Examples
  • MOA
  • SE
  • CI
A

Mineral Oil, Castor oil
Oil coats and softens the stool and prevents reabsorption of water from stool by the colon
Prevents straining
SE: can impair absorption of fat soluble vitamins and unpleasant taste

60
Q

Secreatagogues

  • Examples
  • MOA
  • SE
  • CI
A

Lubiprostone
Derivative of prostaglandin–increases chloride rich intestinal fluid without altering serum sodium and potassium
Acts locally on intestines
SE: nausea
CI: mechanical obstruction, severe diarrhea

61
Q

Naloxegol

A

Peripherally acting mu-opioid receptor antagonists
May cause opioid withdrawal
SE: abdominal pain, diarrhea, nausea, flatulence, vomiting, headache, hyperidrosis

62
Q

First line therapy for constipation

A

Bulk forming laxative

Then stool softener

63
Q

1st line for avoiding straining

A

Stool softener

64
Q

2nd line therapy for constipation

A

Milk of magnesia, lactulose, sorbitol (hyperosmotic laxatives)

65
Q

Medications that can cause diarrhea

A

Antacids, antibiotics, SSRIs, cholinergic agents, colchicine, digoxin, metoclopramide, laxatives, metformin, prostaglandins, quinidine

66
Q

Prophylactic agent for travelers diarrhea

A

Bismuth subsalicylates (Pepto bismol), quinolone antibiotic or tifaximin

67
Q

Loperamide

A

Immodium
Opioid receptor agonist acting on mu receptors of large intestine
Avoid with infectious diarrhea–fever, blood in stool, fecal leukocytes SS
SE: dry mouth, abdominal discomfort, constipation, drowsiness

68
Q

Diphenoxylate

A

Similar to loperamide but does cross BBB

69
Q

Bismuth subsalicylates

A

Pepto Bismol
Stimulates prostalandin, mucus and bicarb secretion in stomach and inhibits prostaglandin and chloride secretion in large intestine
Caution if taking aspirin
SE: black stools, darkening of tongue, tinnitus

70
Q

Kaolinide

A

Absorbs water along with bacteria and toxins as well as helps solidify stools
SE: constipation and feeling ful, bloating, gas
Works locally not systemically

71
Q

Rifaximin

A

Semisynthetic antibiotic similar to rifampin
Only effective against noninvasive strains of E Coli
Use for travelers diarrhea
SE: peripheral edema, nausea, dizziness, fatigue, muscle spasms

72
Q

1st line for diarrhea

A

Loperamide or rifaximin

73
Q

2nd line for diarrhea

A

Adsorbents

74
Q

Antispasmodics for IBS

  • Examples
  • MOA
  • SE
  • CI
A

Dicyclomine (Bentyl) and Hyosycamine
Blocks effects of ACh at muscarinic cholinergic receptors–has anticholinergic effects
Direct relaxation of smooth muscle component of GI tract
SE: dry mouth, vomiting, dysphagia, urinary retention
CI: glaucoma, stenosing peptic ulcer, COPD, cardiac arrhythmias, impaired liver or kidney, MG
Pregnancy category B, CI in lactation

75
Q

Alosetron

A

Serotonin 3 receptor antagonist
Decreases abdominal pain, slows colonic transit time, increases stool consistency
Used for severe diarrhea IBS

76
Q

1st line tx for IBS

A 
Tx Should only be used in exacerbations
Contipation: Osmotic laxative 
Diarrhea: loperamide
Bloating and pain: Dicyclomine 
Psychological symptoms: SSRI
77
Q

Treatments for inflammatory bowel disease

A

Aminosalicylates, corticosteroids, immunosuppresive agents, antibiotics, biologic agents

78
Q

Aminosalicylates

A

Sulfasalazine, mesalamine, olsalazine, balsalazide
Gold standard for tx of UC or CD
Decrease inflammation of GI tract by inhibiting prostaglandin synthesis
May improve symptoms within 1 week
CI in aspirin allergy
May need to take long term

79
Q

Corticosteroids for inflammatory bowel disease

A

Prednisone, methylprednisone, hydrocortisone, dexamethasone, budesonide
Used for acute IBD exacerbations only
Causes immunosuppression and prostaglandin inhibition when UC/CD fails to respond to aminosalicylates

80
Q

Immunosuppresive agents for inflammatory bowel disease

A

Azathioprine, 6-mercaptopurne, methotrexate, cyclosporine

Used as adjunct therapy to induce and maintain remission

81
Q

Abx for inflammatory bowel disease

A

Metronidazole or ciprofloxacin

Must be active against G- and mycobacterium

82
Q

1st line tx for CD

A

Mild to moderate: aminosalicylate alone or in combo with antibiootic or budesonide monotherapy oral
Moderate to severe: combo of aminosalicylates .+ steroids

83
Q

Aminosalicylate of choice

A

Mesalamine

6-16 pills per day

84
Q

Acute diarrhea

A

48 hours or less
Nonpharmacologic measures and adequate hydration; avoid anti diarrheals if possible
If using an anti-diarrheal, adsorbents are best

85
Q

Aminosalicylates

A

Sulfasalazine, mesalamine, olsalazine, balsalazide
Gold standard for tx of UC or CD
Decrease inflammation of GI tract by inhibiting prostaglandin synthesis
May improve symptoms within 1 week
CI in aspirin allergy

86
Q

Corticosteroids for inflammatory bowel disease

A

Prednisone, methylprednisone, hydrocortisone, dexamethasone, budesonide
Used for acute IBD exacerbations only
Causes immunosuppression and prostaglandin inhibition when UC/CD fails to respond to aminosalicylates

87
Q

Immunosuppresive agents for inflammatory bowel disease

A

Azathioprine, 6-mercaptopurne, methotrexate, cyclosporine

Used as adjunct therapy to induce and maintain remission

88
Q

Abx for inflammatory bowel disease

A

Metronidazole or ciprofloxacin

89
Q

1st line tx for CD

A

Mild to moderate: aminosalicylate alone or in combo with antibiootic or budesonide monotherapy oral
Moderate to severe: combo of aminosalicylates .+ steroids

90
Q

Aminosalicylate of choice

A

Mesalamine

6-16 pills per day

91
Q

Acute diarrhea

A

48 hours or less

Nonpharmacologic measures and adequate hydration; avoid anti diarrheals if possible

92
Q

Chronic diarrhea

A

10 days

Opiates and opioid derivatives best

Pharmacology (56 decks)

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