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Gastroenterology > Gastro Pharm 2 > Flashcards

Gastro Pharm 2 Flashcards

1
Q

Bulk forming laxatives

  1. hydrophilic muciloid that forms gelatinous mass when mixed with water; allergic rxns, flatulence, borborygmi, intestinal obstruction, may inhibit coumarin absorption
  2. hydrophilic, digestible, colloid mass w/ water, may bind/ impede Rx absorption
  3. hydrophilic, polyacrylic resin, absorbs 60-10x their weight in water, Ca+ polycarbophils release calcium that is contra-indicated w/ tetracycline
A
  1. Psyllium husk
  2. methyl cellulose
  3. polycarbophils
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2
Q

Surfactant laxatives (stool softeners to reduce strain of defecation)

  1. anionic surfactant, weakly active, stool softener to reduce strain of defecation, no effect on intestinal peristalsis; not for use during abdominal pain, N/V, can irritate the intestinal mucosa, & increase absorption of other Rx, short-term use
  2. non-ionic surfactant, stool softener, can cause diarrhea, not for use during abdominal pain, N/V
  3. rapid acting, anionic surfactant that produces catharsis – complete evacuation of the bowels, stimulates intestinal peristalsis; can cause colic, dehydration, electrolyte imbalance, can induce uterine contractions in pregnant women
A
  1. Docusates
  2. Poloxamers
  3. Caster oil
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3
Q

Stimulant laxatives: act on the large bowel, increase the permeability of intestinal mucosa, increase back diffusion of water & electrolytes, stimulate mucosal mycenteric plexus, stimulate prostaglandin synthesis & increase intestinal secretions, most potent class of laxatives

  1. prodrug, converted by enteric bacteria to the desacetyl active form; enteric coated; OD can cause excessive fluid loss  colonic inflammatory response (synthetic)
  2. natural derivatives of Lilliaceae plants (senna, cascara)- more gentle than synthetic drugs, work by promoting colonic motility; OD – abdominal pain, nephritis, melanotic pigmentation of colon, abnormal urine color
A
  1. Diphenylmethanes - Bisacodyl (swallow hole! would cause cramps in stomach/ SI)
  2. Anthraquinones - Senokot
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4
Q

Saline/ Osmotic Laxatives – osmotic effect retains water in the lumen of the GI; Mg produce laxation by osmotic effect thru release of CCK, which increases intestinal motility and secretion

  1. Epson salt
  2. Milk of magnesia
  3. Cathartic
A

Magnesium sulfate
Magnesium hydroxide
Magnesium citrate

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5
Q

Osmotic Laxative given as a fleet enema

A

Buffered phosphate

now have sodium phosphate tablets

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6
Q

Osmotic Laxative
semisynthetic disaccharide that is not absorbed, produces an osmotic laxative effect; metabolized by enteric bacteria to organic acids such as lactic, formic, acetic acid – fecal acidifier; acidification traps ammonia in the ammonium form which is not toxic

A

Lactulose

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7
Q

Osmotic laxative

suppository – osmotic/ lubricant effects

A

Glycerine

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8
Q

Osmotic laxative

dissolved into 4 L and ingested 8 Oz ~ 10 min for colonoscopy where complete evacuation is needed

A

Polyethylene glycol electrolyte solutuion

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9
Q

Osmotic laxative

mixture of hydrocarbons that penetrates & softens the stool

A

Mineral Oil

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10
Q

Laxatives for IBS

  1. activates intestinal chloride channels, in a PKA independent fashion; increases intestinal secretions and motility for chronic idiopathic constipation
  2. peptide agonist of guanylate cyclase 2C that acts on intestinal cells to indirectly activate the chloride channel
A
  1. Lubiprostone

2. Linaclotide

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11
Q

Anti-diarrheal - Absorb etiological factors in the lumen

absorb harmful bacteria, viruses, toxins; tx of traveler’s diarrhea & H pylori

A

Bismuth sulfate & charcoal

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12
Q

Anti-diarrheal - Absorb water

A

Cellulose derivatives, semisynthetic polysaccharides: Metamucil

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13
Q

Anti-diarrheal: Opiates & Anti-cholinergics
Opiates
-decrease salivary, gastric, intestinal secretions
-decrease motility of stomach & intestines, -increase muscle tone
-increase tone of sphincters including external anal sphincter – reduces urgency; anti-spasmodics, -decrease cramps
-increases the contact times between the ingested matter & reabsorptive epithelium

  1. 0.04% morphine in benzoic acid, camphor, anise oil tincture
  2. merperidine congener that has effect similar to opiates (atropine reduces dose & abuse - anti-cholinergic that crosses BBB)
  3. (Imodium) – interacts w/ intestinal opiod receptor & inhibits calmodulin
A
  1. Paregoric
  2. Diphenoxylate w/ atropine
  3. Loperamide
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14
Q

Anticholinergics – reduce vagal stimulation, anti-spasmodic
Quaternary ammonium derivatives of atropine; do not cross BBB, anti-spasmotic & alleviate cramps

  1. used for urinary frequency – causes retention
  2. more suited to alleviate cramps
    Combined w/ benzodiazapines
A
  1. Propantheline

2. Dicyclomine

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15
Q

Motion sickness: Anticholinergics

prophylactic only for motion sickness; cochlear sensation of motion is projected via cholinergic fibers of the auditory nerve to CTZ; blocks M receptor activation by acetyl choline (transderm patch placed behind the ear), sedation, extrapyramidal drowsiness, dry mouth

A

Scopolamine

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16
Q

H1 antihistamines – older antihistamines exhibit anti-cholinergic effects in addition to anti-histamine H1 effects

A

Dimenydrinate (Dramamine) – OTC for prophylaxis of MS, 30-60 min prior, will last 4-6 hours

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17
Q

Piperazines - MS

A

Cyclizines – OTC for MS

Meclizines - depresses hyperstimulation of labyrinthine function; vestibular disturbances

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18
Q

Anti-Dopaminergics/ Anti-emetics – block the dopamine receptors in the chemoreceptor trigger zone (CTZ)
used for management of N/V; Sedation

A

-Phenothiazine: Promethazine – used for management of N/V; Sedation

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19
Q

Anti-emetic Serotonin Antagonists – Serotonin (5-HT) block 5-HT3 receptors in the stomach & small intestine, these organs transmit stimuli thru vagal and SNS afferents to the CTZ and to the VC thru the solitary tract nucleus; they also block 5HT3 receptors that stimulate the VC to produce emesis; most effective to date; can be used alone or in combination w/ GC & benzodiazapines
1. more potent than odansetron

  1. longer half-life
  2. given IV
A
  1. Granisetron - more potent
  2. Dolesetron - longer half-life
  3. Palonosetron - IV
20
Q

one of the major substances in marijuana that acts by stimulating the CB-1 subtype of cannabinoid receptors; only in cancer tx when patients have failed to respond to other emetics

A

Dronabinol

21
Q

have anti-emetic effects: enhance overall antiemetic effect; MOA is to prevent production of prostaglandins a/w with chemo/radiation

A

Corticocteroids (Dexamethazone, Methylprednisolone)

22
Q

P/neurokinin 1 (NK1) receptor antagonist, used as an adjunct to prevent emesis induced by cytotoxic agents; crosses the BBB and inhibits emesis via central actions; oral, CYP3A4 metabolism

A

Aprepitant

23
Q

used as an adjuct to other antiemetic regiments; effective in patience w/ anticipatory vomiting because they cause somnolence & amnesia; given prior to chemo;

A

Benzodiazapine – Lorazepam & Alprazolam

24
Q

centrally acting anticholinergic/ antidopaminergic, N/V, intractable hiccoughs

A

Chlorpromazine

25
Q

poor antipsychotic, but highly useful antiemetic

A

Prochlorperazine

26
Q

inhibits CTZ and VC

A

Thiethylperazine

27
Q

blocks dopaminergic receptors in the CTZ, post-op for N/V

A

Butryrophenones: Droperidol

28
Q

DA receptor antagonist that blocks chemotherapy induced activation of D2 receptors, stimulates gastric emptying; given prophylactically prior to chemo, prevent post-op N/V

A

Benzamine: metoclopramide

29
Q

Trimethobenzamide AE

A

extrapyramidal side effects

30
Q

Tx carcinoid tumors

A

interferon alpha

ocreotide

31
Q

liver cancer 3 drugs

A

doxorubicin, 5FU, sorafinib

32
Q

first line for GIST

A

imatinib

ocreotide

33
Q

rash is common w/ this mAB to EGFR

A

Cetuximab

34
Q

DPD def (familial pyrimidemia) enhances the neurotoxicity of this Rx

A

5FU

+Leucovorin

35
Q

gastric acidifier to counterbalance the deficiencies of gastric juice in gastric cancer ; nutritional supplement

A

Glutamic acid

36
Q

HER2 mutations in — GI cx?

A

gastric, trastuzumab

37
Q

C diff
macrolide; bactericidal – including hypervirulent strains; inhibits bacterial RNA polymerases, no activity against gram-neg, facultative aerobes, enterobacteriaceae, limited effect on normal fecal flora; no cross-resistance w/ other antimicrobials, including rifamycin (different site of action on RNA polymerases), minimal systemization after oral administration (side effect profile comparable to oral vancomycin) – costs more than vancomycin, but may decrease recurrence

A

Fidaxomicin

38
Q

C diff
for mild/ moderate, oral; 10% of patients suffer from nausea & metallic taste; readily crosses placenta; long term use is associated w/ peripheral neuropathy of extremities (least expensive)

A

Metronidazole

39
Q

Hep B
acyclic phosphonates
nucleotide analog of adenosine-5-monophosphatel; disphosphate that inhibits polymerase and terminates chain; preferred; should be taken w/ a high fat meal to increase bioavailability; could be lipid solubility, stays in the stomach longer; higher incidence of bone turnover & bone fractures; active against HIV and HBV; ARF – monitor Creatinine & BUN

A

Tenofovir

40
Q

Hep B

acyclic phosphonates; diphosphate, chain termination

A

Adefovir

41
Q

Hep B

Acyclic phosphonates, diphosphonate, chain termination

A

Tenofovir

Adefovir

42
Q

Hep B
preferred; d-cyclopentane, guanosine analog; weakly active against HIV; triphosphate inhibits polymerase; food delays absorption

A

Entecavir

43
Q

Hep B L nucelosides

A

Telbivudine

Lamivudine

44
Q

approved for HIV, good for co-infection w/ HBV; L-isomer of cytosine, triphosphate that inhibits polyermase

A

Emtricitabine

45
Q

Hep C
NS3/NS4 serine protease inhibitors; BBW for rash – pruritis – half of patients:
DRESS (Drug Rash w/ Eosinophilia & Systemic Symptoms), SJS, high fat food
Inhibitor for CYP3A4 and P-gp

A

Telaprevir

46
Q

Hep C

NS3/NS4 serine protease inhibitors take with food, no rash

A

Boceprevir

47
Q

Hep C
high fat meal is beneficial for distribution; enhanced host T cell function, inhibition of host inodine monophosphate dehydrogenase (IMPDH) w/ depletion of guanosine triphosphate, essential for viral RNA synthesis; direct inhibition of RNA-dep RNA polymerase, may only transiently reduce HCV RNA but will normalize ALT; synergistic w/ interferon
Primary toxicity: hemolytic anemia

A

Ribivirin

Gastroenterology (5 decks)

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