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Pcol2 > GIT (Drugs For Motility Disorders and Irritable Syndrome) > Flashcards

GIT (Drugs For Motility Disorders and Irritable Syndrome) Flashcards

1
Q

Drugs that can selectively stimulate gut motor function
(prokinetic)

A

DRUGS FOR MOTILITY DISORDER

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2
Q

drugs that increases ____________ pressure may be
useful for GERD

A

lower esophageal sphincter pressure

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3
Q

Increase lower esophageal sphincter pressure may be
useful for

A

GERD

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4
Q

Improves gastric emptying may be helpful for ________ and ________

A

gastroparesis; post surgical gastric emptying delay

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5
Q

CHOLINOMIMETICS will reduce ________

A

LES sphincter tone

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6
Q

Stimulate muscarinic M3 receptor on muscle cell and at
myenteric plexus synapse

A

BETANECHOL

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7
Q

BETANECHOL is used in the past for the treatment of _______ and
____________

A

GERD and gastroparesis

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8
Q

Used in the past for the treatment of GERD and
gastroparesis

A

BETANECHOL

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9
Q

T/F: Betanechol is no longer used due to toxic effect

A

T

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10
Q

Motility Disorder Drugs that is also an Acetylcholinesterase inhibitor

A

NEOSTIGMINE

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11
Q

what does NEOSTIGMINE inhibits

A

Acetylcholinesterase

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12
Q

Can enhance gastric and small intestine and colonic
emptying

A

NEOSTIGMINE

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13
Q

Administration of ______ of Neostigmine may lead to evacuation of the feces

A

2mg

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14
Q

Side Effects of Neostigmine

A

○ Excessive salivation
○ Bradycardia
○ Nausea
○ Vomitting
○ Diarrhea

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15
Q

Used in hospitals for acute bowel distention

A

NEOSTIGMINE

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16
Q

Activation of dopamine receptor inhibits ________________ therefore its blockade is
believed to be the primary prokinetic mechanism

A

cholinergic
smooth muscle stimulation

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17
Q

primary prokinetic mechanism

A

blockade of cholinergic smooth muscle stimulation caused by the activation of dopamine receptor

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18
Q

Movement in the GI is faster if _________ is blocked

A

dopamine

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19
Q

D2 blockade causes (increase/decrease) bowel transit

A

increased

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20
Q

METOCLOPROMIDE (can/cannot) cross the blood brain barrier (BBB)

A

can

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21
Q

Blocks D2 receptor in the chemoreceptor trigger zone
(CTZ) of the medulla, resulting in potent antinausea and
antiemetic action

A

METOCLOPROMIDE

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22
Q

METOCLOPROMIDE blocks D2 receptor in the chemoreceptor trigger zone
(CTZ) of the medulla, resulting in potent _______ and ________ action

A

potent antinausea and
antiemetic action

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23
Q

Metoclopromide blocks D2 receptor in the _______________ of the medulla, resulting in potent antinausea and
antiemetic action

A

chemoreceptor trigger zone
(CTZ)

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24
Q

May also cause parkinsonian symptoms (dystonia,
akathisia, parkinsonian)

A

METOCLOPROMIDE

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25
Q

D2 Antagonist that does not cross the blood-brain barrier; less likely to cause
CNS effects

A

DOMPERIDONE

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26
Q

T/F: Domperidone does not have anti-emetic property

A

T

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27
Q

only improves motility → transit of the bowel

A

DOMPERIDONE

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28
Q

MOTILIN RECEPTOR AGONISTs

A

Erythromycin

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29
Q

Erythromycin is classified under ________ antibiotics

A

macrolides

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30
Q

Stimulates the motilin receptors on gastrointestinal
smooth muscle and promote the onset of a migrating motor
complex

A

Motilin Receptor Agonist (Erythromycin)

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31
Q

Motilin Receptor Agonist stimulates the motilin receptors on gastrointestinal
smooth muscle and promote the onset of a _______________

A

migrating motor
complex

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32
Q

form and dose of erythromycin that is beneficial in some patients
with gastroparesis

A

IV erythromycin (3 mg/kg)

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33
Q

Used in patients with acute upper gastrointestinal
hemorrhage to promote gastric emptying of blood before
endoscopy

A

Motilin Receptor Agonist (Erythromycin)

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34
Q

ADRs of Motilin Receptor Agonist (Erythromycin)

A

Diarrhea
Gastroparesis

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35
Q

T/F: Tolerance can be rapidly developed in Erythromycin

A

T

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36
Q

LAXATIVES

A

BULK FORMING LAXATIVE
STOOL SURFACTANT AGENTS (SOFTENER)
OSMOTIC LAXATIVE
BALANCED POLYETHYLENE GLYCOL
STIMULANT LAXATIVE
DIPHENYLMETHANE DERIVATIVE

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37
Q

BULK FORMING LAXATIVEs

A

Psyllium, Methylcellulose, Polycarbophil

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38
Q

Indigestible, hydrophilic colloids that absorb water,
forming bulky, emollient get that distends the colon and
prompt peristalsis

A

BULK FORMING LAXATIVE (Psyllium, Methylcellulose, Polycarbophil)

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39
Q

STOOL SURFACTANT AGENTS (SOFTENER)

A

Docusate, glycerin and mineral oil

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40
Q

Soften stool material, permitting water and lipids to
penetrate

A

STOOL SURFACTANT AGENTS (Docusate, glycerin and mineral oil)

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41
Q

STOOL SURFACTANT AGENTS May be administered _________ or ________

A

orally or rectally

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42
Q

lubricates fecal material, retarding water
absorption from the stool

A

Mineral oil

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43
Q

Used to prevent the impaction of the fecal matters

A

Mineral oil

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44
Q

Long term use impairs absorption particularly insoluble
vitamins (Vit. A, D, E, K

A

STOOL SURFACTANT AGENTS (Docusate, glycerin and mineral oil)

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45
Q

Soluble but nonabsorbable compound (sugar) that result
in increased stool liquidity due to an obligate increase in
fecal flui

A

OSMOTIC LAXATIVE

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46
Q

Nonabsorbable sugar or salt (Osmotic Laxative) is used for the treatment of ________ or the prevention of ________

A

acute constipation or the
prevention of chronic constipation

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47
Q

Commonly used osmotic laxative

A

Magnesium hydroxide (Milk of Magnesia)

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48
Q

Magnesium hydroxide should not be used for prolonged period in
patients with _______________ due to the risk of
hypermagnesemia

A

renal insufficiency

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49
Q

Nonabsorbable sugar that can be used to prevent
or treat chronic constipation

A

Sorbitol and Lactulose

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50
Q

Sorbitol and Lactulose are metabolized by ____________
producing severe flatulence and cramps

A

colonic bacteria

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51
Q

These sugar are metabolized by colonic bacteria
producing severe flatulence and cramps

A

Sorbitol and Lactulose

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52
Q

High doses of osmotically active agents produces
prompt bowel evacuation within

A

1 to 3 hours

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53
Q

May be used for the treatment of acute constipation or
to cleanse the bowel prior to medical procedure

A

OSMOTIC LAXATIVE

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54
Q

infrequently used osmotic laxative due to the
risk of hyperphosphatemia

A

Sodium phosphate

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55
Q

Osmotic Laxatives

A
  • Absorbable sugars
  • Nonabsorbable sugars:
    * Magnesium hydroxide (Milk of Magnesia)
    * Sorbitol and Lactulose
    * Sodium phosphate
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56
Q

Used for complete colonic cleansing before
gastrointestinal endoscopic procedure

A

BALANCED POLYETHYLENE GLYCOL

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57
Q

Inert, nonabsorbable, osmotically active sugar (PEG) with
sodium sulfate, sodium chloride, sodium bicarbonate and
potassium chloride

A

BALANCED POLYETHYLENE GLYCOL

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58
Q

Designed so that no IV fluid and electrolyte shift will occur

A

BALANCED POLYETHYLENE GLYCO

59
Q

For opitmal bowel cleansing ____ to ______ liters of BALANCED POLYETHYLENE GLYCOL solution should be ingested rapidly (over 1 to 2 hours) on the evening before
the procedure and again in ___ to ___ hours before the
procedure.

A

1 to 2 L; 4 to 6 hours

60
Q

For treatment or prevention of chronic constipation,
smaller doses of _____________ may be mixed with water or
juice (17 g/8 oz)

A

PEG powder

61
Q

Induce bowel movements through a number of poorly
understood mechanisms

A

STIMULANT LAXATIVE

62
Q

Direct stimulation of the enteric nervous system and
colonic electrolyte and fluid secretion

A

STIMULANT LAXATIVE

63
Q

Anthraquinone Derivative

A

STIMULANT LAXATIVE

64
Q

Anthraquinone Derivative (plants)

A

Aloe, senna, cascara sagrada

65
Q

Poorly absorbed and after hydrolysis in the colon,
produce a bowel movement in 6 to 12 hours when given
orally and within 2 hours when given rectall

A

Anthraquinone Derivative

66
Q

Chronic use of Anthraquinone Derivative causes __________

A

melanosis coli

67
Q

Carcinogenic

A

Anthraquinone Derivative

68
Q

DIPHENYLMETHANE DERIVATIVEs

A

Bisacodyl (Dulcolax)

69
Q

Bisacodyl is used for the treatment of ________ and ________

A

acute and chronic constipation

70
Q

Used in conjunction with PEG solution for colonic cleansing
prior to colonoscopy

A

DIPHENYLMETHANE DERIVATIVE (Bisacodyl)

71
Q

Bisacodyl Induces bowel movement within ______ to _______ hours when given
orally and ______ to ______ minutes when taken rectally

A

6 to 10 hours orally; 30 to 60 rectally

72
Q

CHLORIDE CHANNEL ACTIVATORs

A

LUBIPROSTONE
LINACLOTIDE

73
Q

Prostanoic acid derivative labeled for use in chronic
constipation and irritable bowel syndrome (IBS)

A

LUBIPROSTONE

74
Q

Stimulating the type 2 chloride channel (CIC-2) in the
small intestine

A

LUBIPROSTONE

75
Q

LUBIPROSTONE stimulates the _________ in the
small intestine

A

type 2 chloride channel (CIC-2)

76
Q

Increases the chloride rich fluid secretion into the intestine,
which stimulate intestinal motility and shortens intestinal
transit time

A

LUBIPROSTONE

77
Q

LUBIPROSTONE increases the _______ rich fluid secretion into the intestine,
which stimulate intestinal motility and (shortens/lengthens) intestinal
transit time

A

chloride; shortens

78
Q

_________ mcg of LUBIPROSTONE orally ______ daily is recommended dose for
treatment of chronic constipation

A

24; twice

79
Q

T/F: There is no loss of efficacy if Lubiprostone is taken as long term therapy

A

T

80
Q

Minimally absorbed Chloride Channel Activator

A

LINACLOTIDE

81
Q

14 amino acid peptide that stimulates intestinal chloride
secretion through a different mechanism

A

LINACLOTIDE

82
Q

LINACLOTIDE is approved for the treatment of chronic constipation
and _____________

A

IBS with predominant constipation

83
Q

Binds to and activates guanylyl cyclase-C on the luminal
intestinal epithelial surface, resulting in increased
intracellular and extracellular cGMP that leads To
activation of the cystic fibrosis transmembrane
conductance regulator (CFTR) leading to increased
chloride rich secretion and acceleration of intestinal transit

A

LINACLOTIDE

84
Q

LINACLOTIDE binds to and activates guanylyl cyclase-C on the ____________, resulting in ______(increased/decreased)
intracellular and extracellular cGMP that leads To
activation of the ________________leading to increased
chloride rich secretion and acceleration of intestinal transit

A

luminal
intestinal epithelial surface; increased; cystic fibrosis transmembrane
conductance regulator (CFTR)

85
Q

OPIOID RECEPTOR ANTAGONIST

A

METHYLNALTREXONE BROMIDE AND ALVIMOPAN

86
Q

Acute and chronic therapy with opioids may cause
___________ by decreasing intestinal motility, which
results in _________ transit time and _________ absorption of
fecal water

A

constipation; prolongs; increased

87
Q

METHYLNALTREXONE BROMIDE AND ALVIMOPAN (Do not readily cross/ Readily cross) the blood-brain barrier

A

Do not readily cross the blood-brain barrier

88
Q

inhibit peripheral µ-opioid receptor without
impacting analgesic effects within the CNS

A

METHYLNALTREXONE BROMIDE AND ALVIMOPAN

89
Q

METHYLNALTREXONE BROMIDE AND ALVIMOPAN inhibit peripheral µ-opioid receptor _____(with/without)
impacting analgesic effects within the CNS

A

without

90
Q

Treatment of opioid induced
constipation; administered SQ (0.15 mg/kg) every 2 days.

A

Methylnaltrexone

91
Q

Short term used to shorten the period of
postoperative ileus in hospitalized.

A

Alvimopan

92
Q

Opiod antagonist that have cardiotoxic effect

A

Alvimopan

93
Q

Opiod antagonist that doesnt have pschological/CNS effects

A

Methylnaltrexone

94
Q

SEROTONIN 5-HT4 RECEPTOR AGONISTs

A

TEGASEROD
PRUCALOPRIDE

95
Q

Stimulation of ____________ on the presynaptic terminal
of submucosal intrinsic primary afferent nerves enhances
the release of their neurotransmitters, including __________, which stimulates second order enteric
neurons to promote the__________

A

5-HT4 receptor; gene
related peptide; peristaltic reflex

96
Q

Serotonin 5-HT4 partial agonist that has high affinity for
5-HT4 receptor but no appreciable binding 5-HT3 or
dopamine receptor

A

TEGASEROD

97
Q

TEGASEROD is approved for the treatment of patients with chronic
constipation and ______________

A

IBS with predominant constipation

98
Q

High affinity 5-HT4 agonist available in Europe

A

PRUCALOPRIDE

99
Q

PRUCALOPRIDE is used as treatment for chronic constipation in ______

A

women

100
Q

ANTIDIARRHEAL treats _______

A

Mild to moderate diarrhea

101
Q

Can Antidiarrheals be used for patients with bloody diarrhea, high fever and systemic toxicity?

A

No, If given, it can worsen underlying conditions becase it increases the colonic phasic activity inhibiting the
stimulation of the GI

102
Q

OPIOID AGONISTs

A

Loperamide
Diphenoxylate
Kaolin
Pectin
Combined: Kaolin-Pectin

103
Q

Increase colonic phasic segmenting activity through
inhibition of presynaptic cholinergic nerve in the
submucosal and myenteric plexuses and lead to increased
colonic transit time and fecal water absorption.

A

OPIOID AGONIST

104
Q

Opioid agonist that does not cross the blood-brain
barrier

A

Loperamide

105
Q

Opioid agonist that has no analgesic properties or potential addiction

A

Loperamide

106
Q

Prescription opioid agonist that has no analgesic
properties in standard doses

A

Diphenoxylate

107
Q

Higher doses have CNS effect, and prolonged use can
lead to opioid dependence

A

Diphenoxylate

108
Q

Naturally hydrated magnesium aluminum silicate

A

Kaolin

109
Q

Indigestible carbohydrate from apple

A

Pectin

110
Q

Absorbs bacterial toxin and fluids

A

Pectin

111
Q

T/F: Combined: Kaolin-Pectin may interfere with the absorption of other drugs

A

T

112
Q

T/F: Combined: Kaolin-Pectin can cause constipation

A

T

113
Q

Conjugated bile salt normally absorbed in the terminal
ileum

A

BILE SALT BINDING RESIN

114
Q

BILE SALT BINDING RESINs

A

Cholestryramine, Colestipol and Colesevelam

115
Q

BILE SALT BINDING RESIN is normally absorbed in the

A

terminal
ileum

116
Q

May decrease diarrhea caused by excess fecal bile acid

A

BILE SALT BINDING RESIN

117
Q

BILE SALT BINDING RESIN ADRs

A

○ Bloating
○ Flatulence
○ Constipation
○ Fecal impaction

118
Q

OCTREOTIDEs

A

SOMATOSTATIN

119
Q

T/F: Somatostatin is not a statin

A

T

120
Q

14 amino acid peptide that released in the gastrointestinal
tract and pancreas from paracrine cell, D cells and enteric
nerve as well as from hypothalamus

A

SOMATOSTATIN

121
Q

nhibits the secretion of numerous hormones and
transmitter including gastrin, cholestykinin, growth
hormones

A

SOMATOSTATIN

122
Q

SOMATOSTATIN inhibits the secretion of numerous hormones and
transmitter including ______, __________, ____________

A

gastrin, cholestykinin, growth
hormones

123
Q

Reduces intestinal fluid secretion and pancreatic secretion

A

SOMATOSTATIN

124
Q

Slows gastrointestinal motility and inhibits gallbladder
contraction

A

SOMATOSTATIN

125
Q

Reduces portal and splanchnic blood flow

A

SOMATOSTATIN

126
Q

Inhibits secretion of some anterior pituitary hormone

A

SOMATOSTATIN

127
Q

Clinical usefulness of somatostatin is limited by its ________( short/long)
half-life in the circulation

A

short

128
Q

Somatostatin can inhibit _________ and reduce __________:

Inhibits:
-secretion of numerous hormones and
transmitter including ___________________
secretion of _________________

Reduces
- _____________ secretion and ________ secretion
- _________ and _________ blood flow

A

Inhibits:
-secretion of numerous hormones and
transmitter including gastrin, cholestykinin, growth
hormones
-secretion of some anterior pituitary hormone

Reduces
- intestinal fluid secretion and pancreatic secretion
- portal and splanchnic blood flow

129
Q

an idiopathic chronic, relapsing disorder
characterized by abdominal discomfort (pain, bloating,
distention or cramps) in association with alterations in
bowel habits (diarrhea, constipation

A

IBS

130
Q

Pharmacologic therapy for IBS are directed at __________ and __________

A

relieving
abdominal pain and discomfort and improving bowel
function

131
Q

ANTISPASMODIC (ANTICHOLINERGIC) Drugs

A

Dicyclomine and Hyoscyamine

132
Q

Works primarily through anticholinergic activities

A

ANTISPASMODIC (ANTICHOLINERGIC)

133
Q

Inhibits muscarinic cholinergic receptor in the enteric
plexus and on smooth muscle

A

Dicyclomine and Hyoscyamine

134
Q

Used to relieve abdominal pain

A

Dicyclomine and Hyoscyamine

135
Q

At lower dose, Dicyclomine and Hyoscyamine exhibits

A

minimal autonomic effect

136
Q

At a higher dose, Dicyclomine and Hyoscyamine exhibits

A

significant anticholinergic effect

137
Q

activate
visceral afferent pain sensation via extrinsic sensory
neurons from the gut to the spinal cord and central
nervous system

A

5-HT3 receptor

138
Q

Inhibition of afferent gastrointestinal 5-HT3 receptor may
_____(increase/reduce) unpleasant visceral afferent sensation, including
nausea, bloating and pain

A

reduce

139
Q

Highly potent and selective antagonist of the 5-HT3
receptor

A

Alosterin

140
Q

Alosterin is rapidly absorbed from the gastrointestinal tract with a
bioavailability of 50 to 60%, and has a plasma half-life of
____________ but a much longer duration of effect

A

1.5 hours

141
Q

Alosterin undergoes extensive _____________ with renal excretion of most metabolite

A

hepatic cytochrome P450
metabolism

142
Q

Alosterin binds with ________ affinity and dissociates _________ from
5-HT3 which accounts for its long duration of action

A

higher; more slowly

143
Q

Alosterin is approved for the treatment of women with __________ in
whom diarrhea is the predominant symptoms

A

severe IBS

144
Q

Drugs that are approved for the treatment of chronic constipation
and IBS with predominant constipation

A

LINACLOTIDE
TEGASEROD
Alosterin (for women)

Pcol2 (20 decks)

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