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Pharm, Ass9
GI Drugs
69
Pharmacology
Graduate
11/10/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
Methyl psyllium
Definition

(Metamucil) Bulk-forming laxative;

Dissolves in water to form a gel; Swell as the compartment accumulates water;

 

SE - allergic rxns, gas, intestinal obstruction, inhibits coumarin absorption

Term
Methyl cellulose
Definition

Bulk-forming laxative;

Dissolves in water to form a gel; Swells as the compound accumulates water;

 

SE - ↓ absorption of other drugs/nutrients

Term
Polycarbophil
Definition

Bulk-forming laxative;

Hydrophillic polyacrylic resin, absorbs 60-100X its weight in water;

 

SE - Ca release

CI - tetracycline

Term
Docusates
Definition

Anionic Surfactant laxative - stool softener;

↓ water tension between stool and GI tract, allows for easier stool passage;

 

CI - long term use (mucosal irritation) and in pt presenting with abdominal pain, N/V

Term
Poloxamer 188
Definition

NON-ionic Surfactant laxative - stool softener;

↓ water tension between stool and GI tract, allows for easier stool passage;

 

CI - In pt presenting with abdominal pain, N/V

Term
Castor oil
Definition

Anionic Surfactant laxative - stool softener + stimulates peristalsis @ myenteric plexus;

Prodrug - converted to active ricinoleic acid*;

↓ water tension between stool and GI tract, allows for easier stool passage; 

CATHARTIC (induces complete bowel evacuation);

 

SE - induces uterine contraction, dehydration, electrolyte imbalance

Term
Bisacodyl
Definition

(Modane, Dulcolax)

Stimulant laxative - MOST POTENT;

Enteric-coated tablet, Prodrug (converted to desacetyl);

 

[3 MOAs @ colon]

(1) ↑ permiability of intestinal mucosa for back diffusion, (2)stimulate myenteric plexus to ↑ peristalsis, (3) ↑ PG synthesis and intestinal secretion; 

 

SE - dehydration, electrocyte loss, enterocyte damage

Term
Senna
Definition

Stimulant laxative - MOST POTENT;

Natural product, gentle;

 

[3 MOAs @ colon]

(1) ↑ permiability of intestinal mucosa for back diffusion, (2) Stimulate myenteric plexus to↑ peristalsis, (3) ↑ PG synthesis and intestinal secretion; 

 

SE - abdominal pain, nephritis, pigmentation of colon, pink urine

Term
Magnesium sulfate
Definition

(Epsom Salt)

Osmotic laxative +Magnesium;

 

Non-absorble w/ osmotic activity, triggers the release of CCK → ↑ intestinal motility and secretion.

Term
Magnesium hydroxide
Definition

(Milk of Magnesia)

Osmotic laxative +Magnesium;

 

Non-absorble w/ osmotic activity, triggers the release of CCK → ↑ intestinal motility and secretion.

Term
Magnesium citrate
Definition

Osmotic laxative +Magnesium;

 

Non-absorble w/ osmotic activity, triggers the release of CCK → ↑ intestinal motility and secretion+

 CATHARTIC

Term
Fleet enema
Definition
Osmotic laxative +Phosphate; Cathartic
Term
Lactulose
Definition

Osmotic laxative;

Osmotic activity, non-absorbed;

 

Conversion to organic acids make it a fecal acidifier (In hepatic failure - ↑ ammonia clearance by ↓ absorption in colon);

 

Prevents/tx encephalopathy in portal HTN

Term
Glycerine
Definition
Osmotic laxative; Osmotic and lubricant effects; Suppository
Term
Polyethylene glycol
Definition
Osmotic laxative; Mass evac for colonoscopy pre-op; Dissolve into 4L and chug
Term
Mineral oil
Definition

Laxative/stool softner;

Hydrocarbon mixture that penetrates and softens stool

Term
Lubiprostone
Definition

Laxative;

↑ secretions by activating Cl- channels in a PK-A-independant manner which ↑ interstitial fluid secretion and ↑ motility;

 

Tx chronic idiopathic constipation

Term
Naloxone
Definition
T-Sweat: "opiate antagonists are used off label to treat opiate-induced constipation or constipation associated with irritable bowel syndrome"
Term
Noltrexone
Definition
T-Sweat: "opiate antagonists are used off label to treat opiate-induced constipation or constipation associated with irritable bowel syndrome"
Term
Bismuth subsalicylate
Definition

Anti-Diarrheal and cytoprotective agent;

Absorbs harmful bacteria, viruses, toxins;

↑ secretion of mucous and HCO3, inhibits Pepsin activation, chelates proteins at base of ulcer forming protective barrier, and inhibits H. pylori colonization;

 

Tx travellers diarrhea and H. Pylori infection

Term
Charcoal
Definition
Anti-Diarrheal;
Absorbs harmful bacteria, viruses or toxins
Term
Attapulgite, Magnesium aluminum disilicate
Definition
(Diasorb)
Not in notes (?)
Anti-Diarrheal: Binds to acids, toxins, bacteria in the GI;
(previously included in Kaopectate)
Term
Paregoric
Definition

Opiate Anti-diarrheal;

Morpine in benzoic acid;

 

↓ secretions, ↑ muscle tone (anti-spasmotic) including tone of sphincters (↓ urgency @external anal sph), ↓ motility, ↑ contact time.

Term
Diphenoxylate + atropine
Definition

Opiate Anti-diarrheal;

 

↓ secretions, ↑ muscle tone (anti-spasmotic) including tone of sphincters (↓ urgency @external anal sph), ↓ motility, ↑ contact time;

 

 Atropine added to thwart abuse.

Term
Loperamide
Definition

(Imodium)

Opiate Anti-diarrheal;

 

↓ secretions, ↑ muscle tone (anti-spasmotic) including tone of sphincters (↓ urgency @external anal sph), ↓ motility, ↑ contact time;

Binds calmodulin and inhbitis its calcium-binding actions.

Term
Propantheline
Definition

Anti-cholinergic as Anti-Diarrheal;

Blocks vagal tone to the GI (Ach) to ↓ GI motility and secretions;

Anti-spasmodic for cramps;

Also tx urinary incontinence

Term
Dicyclomine
Definition

Anti-cholinergic as Anti-Diarrheal;

Blocks vagal tone (Ach) to the GI to ↓ GI motility and secretions;

Anti-spasmodic to tx CRAMPS.

Term
Scopolamine
Definition

Anti-cholinergic, Anti-emetic;

Blocks muscarinic receptors on CN VIII (vestibular afferents);

Transdermal patch behind ear;

Tx: prophylaxis for motion sickness;

 

SE - sedation, drowsiness, dry mouth

Term
Dimenhydrinate
Definition
(Dramamine);
Anti-Emetic - anti-histamine;
Remember anti-cholinergic action of first Gen H1 blockers;
OTC prophylaxis for motion sickness
Term
Cyclizine
Definition
Anti-Emetic - anti-histamine;
Remember anti-cholinergic action of first Gen H1 blockers;
OTC prophylaxis for motion sickness
Term
Meclizine
Definition
(Antivert)
Anti-Emetic - anti-histamine;
Remember anti-cholinergic action of first Gen H1 blockers;
Prescription Rx for Vertigo and Meniere's dz, depressant effect in ear labyrinth
Term
Promethazine
Definition

(Phenergan);

Potent Anti-Histamine (H1 blocker) and Anti-Emetic; Remember anti-cholinergic action of first Gen H1 blockers;

 

Tx severe N/V, can be used pre-op;

 

SE - Sedation

Term
Chlorpromazine
Definition
Anti-emetic - anti-dopaminergic;
Also has anti-cholinergic functions;
Tx N/V and intractable hiccups
Term
Prochlorperazine
Definition
Anti-emetic - anti-dopaminergic;
Also has anti-cholinergic functions;
Tx N/V and intractable hiccups;
Poor antipsychotic, useful antiemetic
Term
Thiethylperazine
Definition

Anti-emetic - anti-dopaminergic; Also has anti-cholinergic functions;

IV - useful in hospital setting;

 

Tx N/V and intractable hiccups;

Inhibits CTZ & VC

Term
Droperidol
Definition

Anti-emetic - anti-dopaminergic;

Binds D2 receptors in CTZ;

Tx post-op N/V

Term
Metoclopramide
Definition

Anti-emetic - anti-dopaminergic, Prokinetic;

Blocks D2 receptors, ↑ ACH - ↑ gastric emptying; ↑ LES tone, ↑ esophageal peristalsis;

Tx chemo-induced and post-op N/V, GERD, given prophylactically;

 

SE - tardive dyskinesia*

Term
Trimethobenzamide
Definition

Anti-emetic - anti-dopaminergic, Prokinetic;

Blocks D2 receptors, ↑ ACH - ↑ gastric emptying; ↑ LES tone, ↑ esophageal peristalsis;

Tx chemo-induced and post-op N/V;

 

SE - extrapyramidal, use short term only*

Term
Ondansetron
Definition

(Zofran)

Anti-emetic - Serotonin antagonist;

IV or Oral;

Blocks receptors in GI (↓ vagal afferents), blocks receptors in CTZ;

MOST Effective class of Anti-Emetics - use for chemo tox; 

↑ potency w/ dexamethasone.

Term
Granisetron
Definition

Anti-emetic - Serotonin antagonist;

Oral;

Blocks receptors in GI (↓ vagal afferents), blocks receptors in CTZ;

MOST Effective class of Anti-Emetics - use for chemo tox; 

↑ potency w/ dexamethasone.

Term
Dolasetron
Definition

Anti-emetic - Serotonin antagonist;

IV or Oral; Long t 1/2*;

Blocks receptors in GI (↓ vagal afferents), blocks receptors in CTZ;

MOST Effective class of Anti-Emetics - use for chemo tox; 

↑ potency w/ dexamethasone.

Term
Palonosetron
Definition

Anti-emetic - Serotonin antagonist;

IV;

Blocks receptors in GI (↓ vagal afferents), blocks receptors in CTZ;

MOST Effective class of Anti-Emetics - use for chemo tox; 

↑ potency w/ dexamethasone.

Term
Aprepitant
Definition

Anti-emetic adjuvant;

Substance P and neurokinin 1 (NK-1) antagonist;

Crosses BBB to act on CTZ;

 

Tx: N/V from cytotoxic chemo therapy.

Term
Dronabinol Delta 9-tetrahydro cannabinol
Definition

Anti-emetic adjuvant;

Marijuana derivative;

 

Tx intractable N/V in chemo pts;

 

SE - psychomimetic reactions

Term
Dexamethasone
Definition

Anti-emetic corticosteroid (in this case);

 

Reduces SE of other drugs due to ↓ prostaglandins,

↑ effectiveness of serotonin antagonists.

Term
Methylprednisolone
Definition

Anti-emetic (in this case) corticosteroid;

Reduces SE of other drugs by reducing prostaglandin synthesis.

Term
Calcium carbonate
Definition

(Tums)

Antacid;

Weak base neutralizes HCl, prevents pepsin activation;

 

Tx: gas, PUD, acid (↑ pH);

 

SE - ↓ absorption of other drugs

Term
Magnesium-aluminum hydroxide
Definition

(Maalox)

Antacid;

Weak base neutralizes HCl, prevents pepsin activation;

 

Tx gas, PUD, acid (↑ pH);

 

SE - ↓ absorption of other drugs

Term
Mg-Al hydroxide Alginic acid
Definition

Antacid;

Weak base neutralizes HCl, prevents pepsin activation;

 

Tx gas, PUD, acid (↑ pH);

 

SE - ↓ absorption of other drugs

 

Algenic acid is a floating gel to dec reflux, regurg;

Term
Cimetidine
Definition

(Tagamet)

H2 antagonist;

 Competitively inhibits H2 receptors in stomach which ↓ acid secretion;

Least potent in this class of anti-emetics, short half life;

 

Tx: PUD, GERD;

SE - @CYP450; avoid by using other drugs

Term
Ranitidine
Definition

(Zantac)

H2 antagonist;

 Competitively inhibits H2 receptors in stomach which ↓ acid secretion;

Medium potentcy in this class of anti-emetics;

 

Tx: PUD, GERD;

Term
Nizatidine
Definition

 

H2 antagonist;

 Competitively inhibits H2 receptors in stomach which ↓ acid secretion;

Least potent in class of anti-emetics;

 

Tx: PUD, GERD;

Term
Famotidine
Definition

(Pepcid AC) 

H2 antagonist;

 

Most potent and longest half life of any agent in this class*;

 

 Competitively inhibits H2 receptors in stomach which ↓ acid secretion;

 

Tx: PUD, GERD;

Term
Omeprazole
Definition

(Prilosec)

PPI;

Irreversibly modifies the H/K-ATPase which traps the drug at its site of action;

Requires acidic pH for activation*;

Oral, long 1/2 life; More powerful than H2 blocker in inhibiting HCl production;

 

Tx:  PUD, GERD and Z-E syndrome, refractory ulcers;

Term
Esomeprazole
Definition

(Nexium)

PPI;

Irreversibly modifies the H/K-ATPase which traps the drug at its site of action;

Requires acidic pH for activation*;

Oral, long 1/2 life; More powerful than H2 blocker in inhibiting HCl production;

 

Tx:  PUD, GERD and Z-E syndrome, refractory ulcers;

Term
Lansoprazole
Definition

(Prevacid)

PPI;

Irreversibly modifies the H/K-ATPase which traps the drug at its site of action;

Requires acidic pH for activation*;

 

More powerful than H2 blocker in inhibiting HCl production but less effective than other members of the PPI group*

 

Tx:  PUD, GERD and Z-E syndrome, refractory ulcers;

 

Term
Rebeprazole
Definition

PPI;

Irreversibly modifies the H/K-ATPase which traps the drug at its site of action;

Requires acidic pH for activation*;

 More powerful than H2 blocker in inhibiting HCl production;

Less CYP450 metabolism - longer lasting;

 

Tx:  PUD, GERD and Z-E syndrome, refractory ulcers;

Term
Sucralfate
Definition

Cytoprotective agent;

Forms sticky gel at base of ulcer, adheres to epithelium; Requires acidic pH to work*, give before meal;

 

Tx: H2-blocker or PPI-induced pneumonia, DoC in bed ridden patients (alklinization of the stomach has adverse effects in these pt and this drug works at acidic pH)*

Term
Misoprostol
Definition

Cytoprotective agent - PGE1 analog;

 

↑ secretion of mucous and HCO3;

 

SE - dose-limiting diarrhea; Used only in pts that require NSAID use

Term
Clarithromycin
Definition

Macrolide Antibiotic;

 Inhibits microbe protein synthesis;

Tx: H.pylori infection;

 

Resistance: Rare

Term
Amoxicillin
Definition

Antibiotic effective against G(-) bacilli

Tx: H.pylori infection;

 

CI - penicillin allergy

 

Resistance: rare

Term
Tetracycline
Definition

Antibiotic;

Tx: H.pylori infection; 2nd line, use if penicillin allergy, stagger dosing;

 

SE - teeth discoloration;

 

CI: Kids under 8 yrs

Term
Metronidazole
Definition

Synthetic Antibiotic - effective against obligate anaerobes;

Tx: H.pylori infection;

 

Common RESISTANCE*

Often have to switch to Furazolidine*

Term
Furazolidone
Definition

Antibiotic and Anti-protozoal agent

Tx: H.pylori infection; 

 

Used in the case of Metronidazole (common) and/or Clarithromycin (rare) resistance.

Term
Sulfasalazine
Definition

Anti-inflammatory agent;

Enteric coated tablet; Prodrug broken down to 5-ASA (the anti-infalmmatory/active compnent) and sulfapyridine (the component that causes SEs);

 

Tx: IBD;

 

SE - anemia, rash, Impotence

Term
Dimer-ASA
Definition

Anti-inflammatory agent;

Enteric coated tablet; Prodrug: broken into 2 molecules of 5-ASA;

 

Tx: IBD;

 

SE - less impotence but is Weaker as an anti-inflamm

Term
Infliximab
Definition

Monoclonal Ab, Anti-TNF;

Antibody binds TNF-alpha, ↓ inflammation;

 

Tx: IBD when Used w/ other immunosuppression

Term
Etanercept
Definition

(Enbrel)

Monoclonal Ab, Anti-TNF;

Soluble TNF-alpha receptor, binds it; Does not require concomitant immunosuppression;

 

Tx: IBD.

Term
Neomycin
Definition

Antibiotic;

Give enema to ↓ colonic bacteria;

 

Tx - portal HTN, portal systemic encephalopathy

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