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63 Cards in this Set
- Front
- Back
What are prokinetic agents?
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Drugs that increase contractile force and accelerate intraluminal transit, thus enhancing coordinated GI motility.
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What are the receptors that ACh binds to on GI smooth muscle, stimulating propulsion?
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M2 (more abundant)
M3 (more important) |
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Bethanecol: MOA
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"Call Beth if you want to stimulate your bowels and bladder"
cholinergic agonist: selectively stimulates muscarinic receptors without any effect on nicotinic receptors. Longer duration than Ach. |
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Neostigmine: MOA
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AChE inhibitor.
Allows accumulation of ACh at sites of release. Does not stimulate muscle directly. |
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Metoclopramide: MOA
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Dopamine receptor antagonist.
DA inhibits motility, mostly in upper GI. Inhibition of D2 receptors can enhance prokinetic actiity. |
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What is metoclopramide used for?
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Mostly used to lessen N/V caused by GI dysmotility syndromes.
1) GERD: increases LES tone 2) Gastric stasis: stimulates gastric motility 3) Diabetic gastroparesis: stimulates antral motility 4) Decreases small intestinal transit time by stimulating peristalsis |
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What is tegaserod maleate?
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Partial 5HT4 agonist.
Accelerates GI transit. Efficacy shown mainly in female patients with constipation-predominant IBS. |
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Important side fx of tegaserod maleate
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CV adverse events, including angina, heart attacks, stroke.
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Macrolides and Erythromycin work how?
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Motilin agonists.
Motilin is a potent contractile agent. |
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What are luminally active laxatives?
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They increase retention of intraluminal fluid by hydrophilic or osmotic mech, decrease net absorption of fluid by effecting electrolyte transport, and alter motility by inhibition of segmental contractions and enhance peristaltic contractions.
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What are bulk producing laxatives?
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psyllium and bran fiber that undergo bacterial fermation to make short chain fatty acids.
These are trophic to colonic epithelium, stimulate an increase in bacterial mass to increase stool volume. They attract water to increase stool bulk. |
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What are osmotically active laxatives?
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Non-absorbable inorganic salts or sugars. Exert effect by osmotically mediated water retention which then stimulates peristalsis.
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impaired relaxation of the LES with defective peristalsis
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achalasia
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metoclopramide: adverse fx
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Extrapyrimidal effects and parkinsonian like symptoms. Increase serum prolactin.
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Heterogenous disorder characterized by difficulty in passage of stools and infrequent defecation pattern.
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constipation
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What are saline laxatines? How do they work?
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Contain Mg or Phosphate. Laxative effect is from osmotically mediated water retention in lumen that stimulates peristalsis.
These include Mg salts |
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Glycerin and lactulose are what type of laxative?
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Non-digestible alcohols and sugars
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Hygroscopic agent and lubricant
Only administered rectally by suppository or applicator |
Glycerin
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What laxative is also used to treat hepatic encephalopathy and why?
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Lactulose.
Patients with severe liver disease have Impaired capacity to detoxify ammonia from the colon: SCFA from lactulose – Traps ammonia by converting to ammonium ion |
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What are the polyethylene glycol electrolyte solutions?
What are they used for primarily? |
Long chain PEGs that are poorly absorbed and caused retention of water by high osmotic effect.
They're used to cleanse the bowel prior to GI exam. |
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What are the stool-wetting agents and emollients?
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Anionic surfactants that lower surface tension of stool and allow mixing of aqueous and fatty substances. Softens the stool and permits easier defecation.
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What is docusate sodium?
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Stool softener - anionic surfactant.
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T/F Mineral oil (indigestible mix of aliphatic hydrocarbons that penetrates and softens the stools) is widely used yet only marginally effective.
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T
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Stimulant/Irritant Laxatives: How do they work?
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Probably induce low grade inflammation that promotes accumulation of water and electrolytes and stimulate intestinal motility. Includes activation of cAMP and cGMP pathways.
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Bisacodyl: what class of laxative?
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stimulant/irritatve.
OD leads to fluid and electrolyte deficit. |
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Anthraquinone: what class of laxative?
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stimulant, irritative.
Produce giant migrating colonic contracts, induce water and electrolyte secretion. |
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Lubiprostone : What is it?
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Laxative that works as a chloride channel activator, stimulating fluid secretion and enhances mobility.
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Lubiprostone : what is it approved to treat?
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chronic idiopathic constipation and in a lower dose for women with IBS with constipation.
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What are two drugs to treat opioid-associated constipation?
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methylnaltrexone; alvimopan
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Consequences of chronic untreated diarrhea
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1. Electrolyte imbalances—esp. Na+, K+, Mg++
2. Dehydration 3. Inadequate absorption of nutrients |
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What are indications for use of anti-diarrheal drugs?
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1) Acute self-limited diarrhea
2) Symptomatic tx of chronic diarrhea until underlying cause can be found and cured |
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Bismuth Subsalicylate : MOA
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bulk-forming and hydroscopic agents.
Bismuth may have direct antibacterial effect. |
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Diphenoxylate with Atropine : MOA
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Opiate with atropine added to discourage abuse.
Used as anti-diarrheal. |
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Loperamide: effects
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opiate that doesn't cross bbb.
Slows intestinal motility by direct inhibition of circular and longitudinal SM. |
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In severe cases of diarrhea, ___ and ____ are the principle
risk in infants, children and frail elderly patients. |
dehydration and electrolyte imbalances
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Treatment of Diarrhea due to cases of E. coli, shigella or salmonella
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Antibiotics: specifically trimethoprim and sulfamethoxazole
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used to prevent “Travelers Diarrhea” commonly
caused by enterotoxigenic E. coli. |
doxycycline
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Recurrent abdominal pain associated with altered bowel movements.
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Irritable bowel syndrome
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Patients with mild IBS symptoms are usually started on what med?
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fiber supplements
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Alosetron: MOA and use
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antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract. Slows movement of fecal material thru colon.
Only used in women with severe diarrhea-predominant IBS. |
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What are hyosyamine and methscopolamine?
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Anticholinergics used to tx diarrhea predominant IBS
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Tricyclic antidepressants: nortryptiline - also used for what?
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Diarrhea-predominant IBS
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Mixture of beneficial lyophilized bacteria given orally
Enhance barrier function, modulation of the mucosal immune system, alteration of intestinal microflora |
probiotics
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First line therapy for IBD (crohn's and UC)
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Aminosalicylates
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What is the active ingredient that is desirable to be delivered to colon?
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5-ASA (mesalamine)
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Prototypical aminosalicylate
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sulphasalazine
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What do the aminosalicyclates end in?
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-salazine
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What MUST be ruled out before treating for IBD?
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C. difficile pseudomembranous colitis.
This is because the presentation for IBD and C difficile is similar, but the treatment is exactly the opposite (immunosuppression vs ABX). |
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Second line therapy for IBD
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Corticosteroids - Budesonide
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Budesonide: what is it and what is it used for?
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It's a corticosteroid used to treat IBD
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MOA of aminosalicylates (mostly 5-ASA) in IBD
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Acts locally in colon to decrease the inflammatory response and systemically inhibits prostaglandin and leukotriene synthesis.
Inhibits 5-lipoxygenase pathways of arachidonic acid metabolism 1. Reduces LTB4 and 5-HETE levels (assoc. with chemotaxis) 2. Reduces neutrophil, macrophage and lymphocyte chemotaxis |
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Side effects of aminosalicylates
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Side effects mainly by sulfapyridine include fever, dizziness, headache, rash, itching, nausea, vomiting (10-45% of pts). Many pts are on the newer agents
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What is used as remission maintenance therapy in IBD?
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Mesalamine
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T/F Corticosteroids are used as remission maintenance therapy in IBD.
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F. They have many adverse effects if use is prolonged.
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Methylprednisolone : MOA
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Decreases inflammation by suppressing migration of polymorphonuclear leukocytes and reversing increased capillary permeability.
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When are corticosteroids best used?
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During a major flare up, acute exacerbations, severe disease, etc. NOT good for remission therapy.
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Why are short-acting corticosteroids preferred?
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They depress cortisol much less than long acting corticosteroids and thus some side effects can be prevented/minimized.
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3 short acting corticosteroids
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budesonide
beclomethasone fluticasone |
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Azathioprine (prodrug converted to 6-Mercaptopurine): MOA
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1) Inhibits nucleic acid synthesis
2) Suppresses lymphocyte proliferation 3) Anti-inflam effects 4) Suppression of NK cell cytotoxicity |
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Azathioprine (prodrug converted to 6-Mercaptopurine): indications
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severe refractory IBD. Used for long-term treatment or for patients who do not respond to 5-aminosalicylate or corticosteroids.
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Infliximab : MOA
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MAB that neutralizes TNFα, thus Reduces infiltration of inflammatory cells, reduces proportion of
mononuclear cells from the lamina propia able to express TNF and interferon. |
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When are ABX used in IBD?
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Are usually administered on an empirical basis in patients with severe colitis in addition to steroids.
Antibiotics help treat complications (e.g., abscesses and fistulas) caused by bacteria that leak from the intestine. Broad-spectrum antibiotics are often used in hospitalized patients with extremely active IBD, especially if a fever is present. |
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Two common ABX used in IBD
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metronidazole, ciprofloxacin
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