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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
Q

the — plexus of the ENS controls secretions and absorption

A

Submucosal plexus

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26
Q

Promote elimination of soft formed stools

A

laxatives

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27
Q

Result in elimination of more liquid stools

A

cathartics

28
Q

bisacodyl (Correctol, Fleet)

A

Stimulant Laxative

↑ water and electrolytes in colon lumen and/or stimulate intestinal muscle motility

slow onset of action (6 hrs)

29
Q

docusate

A

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
Q

mineral oil

A

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
Q

dietary fiber

A

bulk forming laxative

Material absorbs water and increases bulk which stimulates bowl peristalsis

32
Q

Concentration of solute in the medication is GREATER than in intestinal cells

A

hypertonic

causes water to come toward it

33
Q

Concentration of solute in the medication is THE SAME as in intestinal cells

A

isotonic

water does NOT move

34
Q

what is osmosis

A

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
Q

hypertonic laxatives such as — will cause water to —

A

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
Q

— is used to clean out colon before a colonoscopy

A

isotonic agent (cathartics)

colyte

no movement of water- does NOT cause dehydration

37
Q

loperamide (Imodium)

A

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

loperamide (Imodium)
diphenoxylate (Lomotil)

38
Q

Kaolin-pectin Suspensions (Kao-Pec)

A

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
Q

Why can’t you give cat pepto bismol (bismuth subsalicylate)

A

salicylates (aspirin) is toxic in cats

cant break it down

40
Q

what are some humorally mediated causes of emesis

A

Kidney failure
Liver Disease
Endotoxinemia
apomorphine
digoxin toxicity

humorally = blood bourne

41
Q

what are some neurally mediated causes of emesis

A
  • Gastrointestinal infection
  • Gastrointestinal toxicity
  • Gastrointestinal inflammation
  • Malignancy
42
Q

emetic center receives input from what 4 sources

A

(1) Chemotrigger zone (CRTZ)
(2) Vestibular system (ear)
(3) Peripheral sensory receptors (stomach, intestine)
(4) Higher central nervous system (CNS) centers

43
Q

what happens with excessive vomiting

A

dehydration

low potassium, chlorine, sodium

high blood pH

44
Q

chlorpromazine and acepromazine work on what receptor

A
  • 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
Q

chlorpromazine and acepromazine will block vomiting by —

A

Blocks vomiting reflex at Emetic Center (⍺2)
CRTZ (D2, H1, M1)

will cause hypotension(⍺1 block) and mild sedation (H1 block)

46
Q

metoclopramide (Reglan)

A

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
Q

what are some side effects of metoclopramide (reglan)

A

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
Q

ondansteron (Zofran)

A

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

ondansteron (Zofran)
granisteron (Kytril)

49
Q

butorphanol (Torbugesic)

A

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
Q
A

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
Q
A

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
Q
A

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
Q
A

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
Q

dimenhydrinate (Gravol, Dramamine)

A

Antihistamines
block motion sickness

Anti-emetic activity due to blockade of H1 Histamine receptors in CRTZ by diphenhydramine

sedation →H1 receptors in CNS

55
Q

why doesn’t dimenhydrinate (Gravol, Dramamine) stop motion sickness in cats

A

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
Q
A

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
Q

meclizine (Dramamine II)

A

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
Q
A

Anticholinergics Anti-Emetics

scopolamine (Hyoscine)
propantheline isopropamide
darbazine

59
Q

scopolamine (Hyoscine)

A

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
Q

propantheline isopropamide

A

Anticholinergics

anti- emetic

not as effective alone, should be combined with other meds

Anticholinergics combined with phenothiazines

Anti- ACh Anti- vomiting:
scopolamine (Hyoscine)
propantheline
isopropamide
darbazine

61
Q

darbazine

A

anti- ACh
anti-vomiting

Side Effects: due antimuscarinic effects Tachycardia, loss of visual accommodation, urine retention, constipation, xerostomia

62
Q

maropitant (Cerenia)

A

Neurokinin1 (NK-1) Antagonists

anti-vomiting and motion sickness

Blockade of NK-1 activation in CRTZ reduces vomiting

63
Q

THC

A

Cannabinoids

anti-vomiting

Binds to CB1 and CB2 (GPCR) receptors in many areas of CNS

64
Q

centrally acting emetics

A

apomorphine

xylazine

65
Q

apomorphine

A

Nonselective dopamine AGONIST

Stimulates CRTZ

centrally acting emetics:
apomorphine
xylazine

66
Q

xyalzine

A

centrally acting emetic

α2 adrenergic AGONIST induces vomiting in cats then mild sedation.

centrally acting emetic:
apomorphine
xylazine

67
Q

peripherally acting emetics

A

Sodium Chloride
Hydrogen Peroxide (H2O2)
Syrup of Ipecac
Ayahuasca (a-ya-wa-ska)

23 spring: pharm (46 decks)

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