GIT (Drugs For Motility Disorders and Irritable Syndrome) Flashcards by Kim Grace

Drugs that can selectively stimulate gut motor function
(prokinetic)

DRUGS FOR MOTILITY DISORDER

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drugs that increases ____________ pressure may be
useful for GERD

lower esophageal sphincter pressure

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Increase lower esophageal sphincter pressure may be
useful for

GERD

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Improves gastric emptying may be helpful for ________ and ________

gastroparesis; post surgical gastric emptying delay

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CHOLINOMIMETICS will reduce ________

LES sphincter tone

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

BETANECHOL

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

GERD and gastroparesis

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Used in the past for the treatment of GERD and
gastroparesis

BETANECHOL

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

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Motility Disorder Drugs that is also an Acetylcholinesterase inhibitor

NEOSTIGMINE

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what does NEOSTIGMINE inhibits

Acetylcholinesterase

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Can enhance gastric and small intestine and colonic
emptying

NEOSTIGMINE

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

2mg

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Side Effects of Neostigmine

○ Excessive salivation
○ Bradycardia
○ Nausea
○ Vomitting
○ Diarrhea

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Used in hospitals for acute bowel distention

NEOSTIGMINE

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

cholinergic
smooth muscle stimulation

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primary prokinetic mechanism

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

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Movement in the GI is faster if _________ is blocked

dopamine

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D2 blockade causes (increase/decrease) bowel transit

increased

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

can

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

METOCLOPROMIDE

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

potent antinausea and
antiemetic action

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

chemoreceptor trigger zone
(CTZ)

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

METOCLOPROMIDE

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

DOMPERIDONE

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

only improves motility → transit of the bowel

DOMPERIDONE

MOTILIN RECEPTOR AGONISTs

Erythromycin

Erythromycin is classified under ________ antibiotics

macrolides

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

Motilin Receptor Agonist (Erythromycin)

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

migrating motor complex

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

IV erythromycin (3 mg/kg)

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

Motilin Receptor Agonist (Erythromycin)

ADRs of Motilin Receptor Agonist (Erythromycin)

Diarrhea Gastroparesis

T/F: Tolerance can be rapidly developed in Erythromycin

LAXATIVES

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

BULK FORMING LAXATIVEs

Psyllium, Methylcellulose, Polycarbophil

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

BULK FORMING LAXATIVE (Psyllium, Methylcellulose, Polycarbophil)

STOOL SURFACTANT AGENTS (SOFTENER)

Docusate, glycerin and mineral oil

Soften stool material, permitting water and lipids to penetrate

STOOL SURFACTANT AGENTS (Docusate, glycerin and mineral oil)

STOOL SURFACTANT AGENTS May be administered _________ or ________

orally or rectally

lubricates fecal material, retarding water absorption from the stool

Mineral oil

Used to prevent the impaction of the fecal matters

Mineral oil

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

STOOL SURFACTANT AGENTS (Docusate, glycerin and mineral oil)

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

OSMOTIC LAXATIVE

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

acute constipation or the prevention of chronic constipation

Commonly used osmotic laxative

Magnesium hydroxide (Milk of Magnesia)

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

renal insufficiency

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

Sorbitol and Lactulose

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

colonic bacteria

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

Sorbitol and Lactulose

High doses of osmotically active agents produces prompt bowel evacuation within

1 to 3 hours

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

OSMOTIC LAXATIVE

infrequently used osmotic laxative due to the risk of hyperphosphatemia

Sodium phosphate

Osmotic Laxatives

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

Used for complete colonic cleansing before gastrointestinal endoscopic procedure

BALANCED POLYETHYLENE GLYCOL

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

BALANCED POLYETHYLENE GLYCOL

Designed so that no IV fluid and electrolyte shift will occur

BALANCED POLYETHYLENE GLYCO

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.

1 to 2 L; 4 to 6 hours

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

PEG powder

Induce bowel movements through a number of poorly understood mechanisms

STIMULANT LAXATIVE

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

STIMULANT LAXATIVE

Anthraquinone Derivative

STIMULANT LAXATIVE

Anthraquinone Derivative (plants)

Aloe, senna, cascara sagrada

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

Anthraquinone Derivative

Chronic use of Anthraquinone Derivative causes __________

melanosis coli

Carcinogenic

Anthraquinone Derivative

DIPHENYLMETHANE DERIVATIVEs

Bisacodyl (Dulcolax)

Bisacodyl is used for the treatment of ________ and ________

acute and chronic constipation

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

DIPHENYLMETHANE DERIVATIVE (Bisacodyl)

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

6 to 10 hours orally; 30 to 60 rectally

CHLORIDE CHANNEL ACTIVATORs

LUBIPROSTONE LINACLOTIDE

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

LUBIPROSTONE

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

LUBIPROSTONE

LUBIPROSTONE stimulates the _________ in the small intestine

type 2 chloride channel (CIC-2)

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

LUBIPROSTONE

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

chloride; shortens

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

24; twice

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

Minimally absorbed Chloride Channel Activator

LINACLOTIDE

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

LINACLOTIDE

LINACLOTIDE is approved for the treatment of chronic constipation and _____________

IBS with predominant constipation

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

LINACLOTIDE

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

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

OPIOID RECEPTOR ANTAGONIST

METHYLNALTREXONE BROMIDE AND ALVIMOPAN

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

constipation; prolongs; increased

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

Do not readily cross the blood-brain barrier

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

METHYLNALTREXONE BROMIDE AND ALVIMOPAN

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

without

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

Methylnaltrexone

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

Alvimopan

Opiod antagonist that have cardiotoxic effect

Alvimopan

Opiod antagonist that doesnt have pschological/CNS effects

Methylnaltrexone

SEROTONIN 5-HT4 RECEPTOR AGONISTs

TEGASEROD PRUCALOPRIDE

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__________

5-HT4 receptor; gene related peptide; peristaltic reflex

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

TEGASEROD

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

IBS with predominant constipation

High affinity 5-HT4 agonist available in Europe

PRUCALOPRIDE

PRUCALOPRIDE is used as treatment for chronic constipation in ______

women

ANTIDIARRHEAL treats _______

Mild to moderate diarrhea

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

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

OPIOID AGONISTs

Loperamide Diphenoxylate Kaolin Pectin Combined: Kaolin-Pectin

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.

OPIOID AGONIST

Opioid agonist that does not cross the blood-brain barrier

Loperamide

Opioid agonist that has no analgesic properties or potential addiction

Loperamide

Prescription opioid agonist that has no analgesic properties in standard doses

Diphenoxylate

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

Diphenoxylate

Naturally hydrated magnesium aluminum silicate

Kaolin

Indigestible carbohydrate from apple

Pectin

Absorbs bacterial toxin and fluids

Pectin

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

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

Conjugated bile salt normally absorbed in the terminal ileum

BILE SALT BINDING RESIN

BILE SALT BINDING RESINs

Cholestryramine, Colestipol and Colesevelam

BILE SALT BINDING RESIN is normally absorbed in the

terminal ileum

May decrease diarrhea caused by excess fecal bile acid

BILE SALT BINDING RESIN

BILE SALT BINDING RESIN ADRs

○ Bloating ○ Flatulence ○ Constipation ○ Fecal impaction

OCTREOTIDEs

SOMATOSTATIN

T/F: Somatostatin is not a statin

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

SOMATOSTATIN

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

SOMATOSTATIN

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

gastrin, cholestykinin, growth hormones

Reduces intestinal fluid secretion and pancreatic secretion

SOMATOSTATIN

Slows gastrointestinal motility and inhibits gallbladder contraction

SOMATOSTATIN

Reduces portal and splanchnic blood flow

SOMATOSTATIN

Inhibits secretion of some anterior pituitary hormone

SOMATOSTATIN

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

short

Somatostatin can inhibit _________ and reduce __________: Inhibits: -secretion of numerous hormones and transmitter including ___________________ secretion of _________________ Reduces - _____________ secretion and ________ secretion - _________ and _________ blood flow

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

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

IBS

Pharmacologic therapy for IBS are directed at __________ and __________

relieving abdominal pain and discomfort and improving bowel function

ANTISPASMODIC (ANTICHOLINERGIC) Drugs

Dicyclomine and Hyoscyamine

Works primarily through anticholinergic activities

ANTISPASMODIC (ANTICHOLINERGIC)

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

Dicyclomine and Hyoscyamine

Used to relieve abdominal pain

Dicyclomine and Hyoscyamine

At lower dose, Dicyclomine and Hyoscyamine exhibits

minimal autonomic effect

At a higher dose, Dicyclomine and Hyoscyamine exhibits

significant anticholinergic effect

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

5-HT3 receptor

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

reduce

Highly potent and selective antagonist of the 5-HT3 receptor

Alosterin

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

1.5 hours

Alosterin undergoes extensive _____________ with renal excretion of most metabolite

hepatic cytochrome P450 metabolism

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

higher; more slowly

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

severe IBS

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

LINACLOTIDE TEGASEROD Alosterin (for women)

GIT (Drugs For Motility Disorders and Irritable Syndrome) Flashcards

(144 cards)