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23 spring: pharm > Test 2: lecture 29 +30 GI part 2 > Flashcards

Test 2: lecture 29 +30 GI part 2 Flashcards

1
Q

sucralfate (sucramal) causes what things

A
  • forms paste to protect gastic epithelial cells
  • binds and inactivates bile salts and pepsin
  • Stimulates prostaglandin synthesis
  • increases Mucosal blood flow

chemical diffusion barriers:
sucralfate (sucramal)
Bismuth subsalicylate (pepto-bismol)
montmorillonite (diarsanyl)

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2
Q

montmorillonite (diarsanyl)

A

smectite clay forms protective layer in stomach

absorbs toxins, bacteria, viruses, enzymes and free radicals

used for diarrhea in dogs and cats by coating intestinal mucosa

chemical diffusion barriers:
sucralfate (sucramal)
Bismuth subsalicylate (pepto-bismol)
montmorillonite (diarsanyl)

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3
Q

— is a chemical diffusion barrier drug that is used to treat diarrhea in dogs

A

montmorillonite (diarsanyl)

smectite clay forms protective layer

absorb toxins, bacteria, viruses, enzymes and free radicals

chemical diffusion barriers:
sucralfate (sucramal)
Bismuth subsalicylate (pepto-bismol)
montmorillonite (diarsanyl)

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4
Q

how does bismuth subsalicylate (Pepto-Bismol) work

A

Bismuth:
* Coats ulcerated mucosal surfaces
* Absorbs toxins
* Mild antibacterial action (H pylori)

Salicylate (aspirin)
* Anti-inflammatory action

can’t be metabolized by cat

chemical diffusion barriers:
sucralfate (sucramal)
Bismuth subsalicylate (pepto-bismol)
montmorillonite (diarsanyl)

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5
Q

GI is under — control what happens when you give atropine?

A

PARA

blocks ACh (muscarinic) receptors

cause dry, mouth, tachycardia, decrease secretions, bronchioconstriction, large pupils ect.

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6
Q

pirenzepine

A

M1-selective blocker

but causes decreased gastric acid somehow even though there are M3 receptors on parietal cells?

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7
Q

H1 receptors

A

Located on smooth muscle and endothelium and in CNS and promotes vasodilation, bronchoconstriction, smooth muscle activation, and CNS activation

make you sleepy

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8
Q

H2 receptors are found where and cause what?

A

Located on parietal cells and regulates histamine-mediated gastric acid secretion

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9
Q

what are the H2 receptor blockers

A

cimetidine (Tagamet)
ranitidine (Zantac)
famotidine (Pepcid)
Pepcid Complete (Life cycle management)
nizatidine (Axid)

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10
Q

cimetidine (Tagamet)

A

1st gen H2 blocker

decreases gastric acid without causing sleepiness (H1 blockage)

  • inhibits CYP → toxic levels of drugs from decreased metabolism
  • many drug interactions
  • decreases liver blood flow→ decreased clearance of propranolol and lidocaine

H2 receptor blockers:
cimetidine (Tagamet)
ranitidine (Zantac)
famotidine (Pepcid)
Pepcid Complete (Life cycle management)
nizatidine (Axid)

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11
Q

ranitidine (Zantac)

A

2nd gen H2 blocker

fewer side effects that cimetidine → less drug interactions, less CYP inhibition

longer lasting
10x more potent

H2 receptor blockers:
cimetidine (Tagamet)
ranitidine (Zantac)
famotidine (Pepcid)
Pepcid Complete (Life cycle management)
nizatidine (Axid)

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12
Q

famotidine (Pepcid)

A

3rd gen H2 receptor blocker

poor bioavilability
30x more potent than cimetidine
no CYP inhibition
increases motility of stomach

H2 receptor blockers:
cimetidine (Tagamet)
ranitidine (Zantac)
famotidine (Pepcid)
Pepcid Complete (Life cycle management)
nizatidine (Axid)

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13
Q

Pepcid Complete (Life cycle management) is a combo of what drugs

A

famotidine H2 antagonist (10 mg)
calcium carbonate antacid (800 mg) (constipation)
magnesium hydroxide antacid (165 mg) (diarrhea)

Ca and Mg balance each other out
Antacids act quickly and H2 blocker act slowly

H2 receptor blockers:
cimetidine (Tagamet)
ranitidine (Zantac)
famotidine (Pepcid)
Pepcid Complete (Life cycle management)
nizatidine (Axid)

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14
Q

nizatidine (Axid)

A

H2 receptor blocker

no CYP inhibition
excreted unchanged in urine
increases motility of stomach

H2 receptor blockers:
cimetidine (Tagamet)
ranitidine (Zantac)
famotidine (Pepcid)
Pepcid Complete (Life cycle management)
nizatidine (Axid)

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15
Q

which H2 blockers do not cause CYP inhibition

A

famotidine (pepcid)
nizatidine (axid)

H2 receptor blockers:
cimetidine (Tagamet)
ranitidine (Zantac)
famotidine (Pepcid)
Pepcid Complete (Life cycle management)
nizatidine (Axid)

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16
Q

— is an experimental gastrin blocker

A

netazepide (YF476)

CCKB receptor blocker

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17
Q

— are proton pump inhibitors

A

omeprazole (Prilosec)
lansoprazole (Prevacid)
esomeprazole (Nexium)
rabeprazole (Aciphex)

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18
Q

how does omeprazole (Prilosec) work

A

weak base that is absorbed and then protonated

will irreversibly covalently bind and inhibit proton pump inhibitors

lasts 2-3 days

proton pump inhibitors:
omeprazole (Prilosec)
lansoprazole (Prevacid)
esomeprazole (Nexium)
rabeprazole (Aciphex)

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19
Q

— covalently and irreversibly binds and blocks proton pumps

A

omeprazole (prilosec)
lasts 2-3 days

proton pump inhibitors:
omeprazole (Prilosec)
lansoprazole (Prevacid)
esomeprazole (Nexium)
rabeprazole (Aciphex)

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20
Q

what happens with prolonged use of omeprazole (prilosec)

A

Prolonged decrease in gastric acid production will cause increase in stomach pH

this can cause bacterial overgrowth → pneumonia

stomach will try to bring pH back to 4 by increasing acid → increased gastrin levels and parietal cell hyperplasia

omeprazole: irreversibly and covalently bind to proton pump

proton pump inhibitors:
omeprazole (Prilosec)
lansoprazole (Prevacid)
esomeprazole (Nexium)
rabeprazole (Aciphex)

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21
Q

how does prostaglandin help with gastric mucosal integrity

A

(1) Inhibit gastric acid secretion
(2) Stimulate bicarb secretion
(3) Stimulate mucous secretion
(4) Increase mucosal blood flow
(5) anti-inflammatory

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22
Q

how does misoprostol (Cytotec) work

A

prostaglandin

Binds to Prostaglandin receptor on parietal cell and ↓ intracellular cAMP levels leading to a ↓ in proton pump activity

(1) Increase mucous production in gastric ulcers
(2) Co-administered with NSAIDs to prevent ulceration

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23
Q

off label uses of misoprostol (Cytotec)

A

prostaglandin

Primary Indications:
* Increase mucous production in gastric ulcers
* Co-administered with NSAIDs to prevent ulceration

Off label Uses:
* induce labor by causing smooth muscle contraction
* Abortion in conjunction with RU-486
* Erectile dysfunction

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24
Q

the — plexus of the ENS controls gut motility

A

myenteric

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25
the --- plexus of the ENS controls secretions and absorption
Submucosal plexus
26
Promote elimination of soft formed stools
laxatives
27
Result in elimination of more liquid stools
cathartics
28
bisacodyl (Correctol, Fleet)
Stimulant Laxative ↑ water and electrolytes in colon lumen and/or stimulate intestinal muscle motility slow onset of action (6 hrs)
29
docusate
Surfactant Laxative **detergent-like action** that act as stool-wetting and stool softening agents allowing the efficient mixing of water ↑ intestinal water secretion to soften stools
30
mineral oil
soften and lubricate fecal mass make it easier to expel Indigestible, takes 2-3 days to soften stools **Anal leakage** and irritation can be a problem and chronic use can also lead to **malabsorption of fat soluble vitamins and drugs**
31
dietary fiber
bulk forming laxative Material absorbs water and **increases bulk** which **stimulates bowl peristalsis**
32
Concentration of solute in the medication is GREATER than in intestinal cells
hypertonic causes water to come toward it
33
Concentration of solute in the medication is THE SAME as in intestinal cells
isotonic water does NOT move
34
what is osmosis
Movement of water across a semi permeable membrane from an area of low concentration of solute to an area of high concentration of solute
35
hypertonic laxatives such as --- will cause water to ---
Solutions of Mg2+, tartrate, Na+ salts, or solutions of lactulose, glycerin, sorbitol, mannitol, or polyethylene glycol **(miralax)** pulls water from intestinal cells into poop Need to be **careful to avoid dehydration** due to movement of water into colon
36
--- is used to clean out colon before a colonoscopy
**isotonic agent (cathartics)** colyte no movement of water- does NOT cause dehydration
37
loperamide (Imodium)
opioid agonist→ antidiarrheal acts on μ and δ opioid receptors in the myenteric plexus decreasing motility of the large intestine. This permits more time for water resorption. Also increases anal sphincter tone muscarinic antagonist is added to prevent abuse/addiction to this drug ## Footnote loperamide (Imodium) diphenoxylate (Lomotil)
38
Kaolin-pectin Suspensions (Kao-Pec)
antidiarrheal Kaolinite is a clay mineral → **absorbs water** in the intestine to decrease fluidity of fecal material DOES NOT decrease diarrhea-induced water loss
39
Why can't you give cat pepto bismol (bismuth subsalicylate)
salicylates (aspirin) is toxic in cats cant break it down
40
what are some humorally mediated causes of emesis
Kidney failure Liver Disease Endotoxinemia apomorphine digoxin toxicity ## Footnote humorally = blood bourne
41
what are some neurally mediated causes of emesis
* Gastrointestinal infection * Gastrointestinal toxicity * Gastrointestinal inflammation * Malignancy
42
emetic center receives input from what 4 sources
(1) Chemotrigger zone (CRTZ) (2) Vestibular system (ear) (3) Peripheral sensory receptors (stomach, intestine) (4) Higher central nervous system (CNS) centers
43
what happens with excessive vomiting
dehydration low potassium, chlorine, sodium high blood pH
44
chlorpromazine and acepromazine work on what receptor
* α2/1 adrenergic blocker * Weak dopamine, histamine and cholinergic receptor blocker Blocks vomiting reflex at **Emetic Center and CRTZ** cause mild sedation from H1 block and hypotension from ⍺1 block
45
chlorpromazine and acepromazine will block vomiting by ---
Blocks vomiting reflex at **Emetic Center** (⍺2) **CRTZ** (D2, H1, M1) ## Footnote will cause hypotension(⍺1 block) and mild sedation (H1 block)
46
metoclopramide (Reglan)
**D2 Dopamine Antagonists** **Anti-emetic** action due to blockade of D2 dopamine receptors in the CRTZ high dose can block serotonin 5-HT3 receptor increases peristalsis in jejunum and duodenum from some muscarinic activity, D2 antagonism, and 5-HT4 receptor agonism side effects: hyperactivity, tremors and constipation
47
what are some side effects of metoclopramide (reglan)
D2 Dopamine Antagonists **hyperactivity, tremors and constipation** Anti-emetic → blocks D2 dopamine receptors in the CRTZ and at high dose→ blocks serotonin 3 receptor increases peristalsis in jejunum and duodenum) due to some muscarinic activity, D2 antagonism, and 5-HT4 receptor agonism
48
ondansteron (Zofran)
**5-HT3 Serotonin Antagonists** **Anti-emetic** action due to blockade of 5-HT3 serotonin receptors in the **CRTZ and in the gastrointestinal tract** Side effects include transient headache, constipation and dizziness ## Footnote ondansteron (Zofran) granisteron (Kytril)
49
butorphanol (Torbugesic)
**Opioid Antagonists** **Anti-emetic** activity due to blockade of opiate receptors in the **emetic center and higher CNS centers** Sedation is a common side effect
50
butorphanol (Torbugesic) **Opioid Antagonists** **Anti-emetic** activity due to blockade of opiate receptors in the **emetic center and higher CNS centers** Sedation is a common side effect
51
**5-HT3 Serotonin Antagonists** ondansteron (Zofran) granisteron (Kytril) **Anti-emetic** action due to blockade of 5-HT3 serotonin receptors in the **CRTZ and in the gastrointestinal tract** Side effects include transient headache, constipation and dizziness
52
D2 Dopamine Antagonists **metoclopramide (Reglan)** **Anti-emetic** action due to blockade of D2 dopamine receptors in the **CRTZ** At higher doses it blocks 5-HT3 receptors which also may contribute to its anti-emetic properties increases peristalsis in jejunum and duodenum) due to some muscarinic activity, D2 antagonism, and 5-HT4 receptor agonism Side effects include hyperactivity, tremors and constipation
53
**α2 Adrenrgic Antagonists** acepromazine chlorpromazine also blocks dopamine, histamine and ACh receptors **Blocks vomiting** reflex at **Emetic Center and CRTZ ** Side effects include mild sedation due to histamine receptor blockade and hypotension due to α1 receptor blockade
54
dimenhydrinate (Gravol, Dramamine)
Antihistamines **block motion sickness** Anti-emetic activity due to blockade of H1 Histamine receptors in **CRTZ** by diphenhydramine sedation →H1 receptors in CNS
55
why doesn't dimenhydrinate (Gravol, Dramamine) stop motion sickness in cats
dramamine works on **H1 receptors in the CRTZ** **anti-motion sickness** cats: Vestibular nucleus impulses pass directly to the emetic center dogs: Vestibular nucleus impulses pass through CRTZ to the emetic center
56
anti-emesis antihistamine **dimenhydrinate (Gravol, Dramamine)** **anti motion sickness** in dogs by H1 receptor in CRTZ not in cats which vestibular skips the CRTZ and goes right to emetic center
57
meclizine (Dramamine II)
**Anti-emetic** activity due to blockade of **H1** histamine receptors in **CRTZ** less sedation then dramanine cause less BBB cross ? Used to treat vertigo as a result of inner ear infections
58
**Anticholinergics Anti-Emetics** scopolamine (Hyoscine) propantheline isopropamide darbazine
59
scopolamine (Hyoscine)
Anticholinergics- **anti-emetics** blockade of muscarinic receptors in **Emetic Center** Blocks muscarinic receptor activation in the emetic center activated by vagal afferent pathways from stomach and gut use for travel sickness
60
propantheline isopropamide
Anticholinergics anti- emetic not as effective alone, should be combined with other meds Anticholinergics combined with phenothiazines ## Footnote Anti- ACh Anti- vomiting: scopolamine (Hyoscine) propantheline isopropamide darbazine
61
darbazine
anti- ACh anti-vomiting **Side Effects**: due **antimuscarinic** effects Tachycardia, loss of visual accommodation, urine retention, constipation, xerostomia
62
maropitant (Cerenia)
Neurokinin1 (NK-1) Antagonists anti-vomiting and motion sickness Blockade of NK-1 activation in **CRTZ** reduces vomiting
63
THC
Cannabinoids anti-vomiting Binds to CB1 and CB2 (GPCR) receptors in many areas of CNS
64
centrally acting emetics
apomorphine xylazine
65
apomorphine
Nonselective dopamine AGONIST Stimulates CRTZ ## Footnote centrally acting emetics: apomorphine xylazine
66
xyalzine
centrally acting emetic α2 adrenergic AGONIST induces vomiting in cats then **mild sedation.** ## Footnote centrally acting emetic: apomorphine xylazine
67
peripherally acting emetics
Sodium Chloride Hydrogen Peroxide (H2O2) Syrup of Ipecac Ayahuasca (a-ya-wa-ska)

23 spring: pharm (46 decks)

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