Choi Flashcards
Antacid that causes CO2 gas, metabolic alkalosis, and Na-fluid retention
sodium bicarbonate
antacid that causes CO2 gas, metabolic alkalosis, and milk-alkali syndrome
calcium carbonate
antacid that causes osmotic diarrhea
magnesium hydroxide
antacid that causes constipation
aluminum hydroxide
Pts with *** insufficiency should not take antacids long term
renal
Antacids should not be given within 2 hours of doses of tetracyclines, fluoroquinolones, itraconazole, and iron because
- reduced absorption
- affected dissolution or solubility
inhibits both meal stimulated and nocturnal secretion of acid
PPI
inhibits nocturnal acid secretion only
H2 blocker
Explain why you should take PPIs 1 hour before meals (2)
1 - PPI is an uncharged prodrug which is capable of crossing the plasma membrane of parietal cells. It is activated by H+, which adds a charge to the PPI. If you take it after a meal, it is activated in the stomach lumen, and will A) not be effective and B) be unable to cross PM.
2 - Parietal cell needs to be in active (stimulated) form in order for PPI to inhibit PP. PPIs have short half life, so it is important to activate parietal cell while PPI is IN the cell and capable of action.
PPIs have a very short half life but a long duration of action. Why?
Irreversible inhibitor, .:. in order to regain H+ secretion, you need to produce and insert a new PP into the PM
PPIs take a few days to produce full effect. Why?
Because not all proton pumps are available to be inhibited. Takes multiple cycles to hit hte critical # of PPs
H. pylori triple therapy
- PPI (omexazaprole, lansoprazole, etc)
- Clarythromycin
- Metronidazole OR amoxicilline OR tetracycline
H. pylori quadruple therapy
- PPI OR H2 antagonist
- metronidazole
- tetracycline
- bismuth
H2 antagonist that can cause gynecomastia, impotence, galactorrhea
Cimetidine
Black box warning on PPIs
Life-threatening hypomagnesia with secondary hypocalcemia
For Acid - Peptic DZ: salt of sucrose complexed to sulfated aluminum hydroxide
Sucralfate
For Acid - Peptic DZ: MOA of sucralfate
polymerizes in stomach and forms a wall; stimulates mucosal protaglandin and bicarb secretion
For Acid - Peptic DZ: Used for prevention of stress related bleeding in critically ill pts
sucralfate
Adverse effects of sucralfate
constipation (aluminum)
Do not use for prolonged periods with renal insufficiency
For Acid - Peptic DZ: methyl analog of PGE1
Misoprostol
For Acid - Peptic DZ: Pros and Cons of misoprostol
Pro: better bioavailability than PGE1
Con: need to take qid (4Xday)
For Acid - Peptic DZ: Con of PGE1
v. unstable. only lasts for minutes
C/I for misoprostol; Why?
pregnant or fertile female; stimulate uterine contractions.
For Acid - Peptic DZ: Creates a protective layer, may stimulate PG, mucus, bicarb secretion; has direct antimicrobial effects and binds enterotoxins
Bismuth compounds
Adverse effects of bismuth compounds (4)
1 - Weird blackness everywhere (stool, tongue)
2 - Avoid with renal insufficiency
3 - Prolonged use can lead to bismuth tox .:. encephalopathy
4 - High dose can lead to salicylate tox
3 classes of prokinetic drugs
1 - cholinomimetics (bethanechol, neostigmine)
2 - D2 antagonists (metoclopramide, domperidone)
3 - Macrolides (erythromycin)
Prokinetics: stimulates M3 receptors; used in the past to tx gastroparesis
bethanecol
Prokinetics: AChE inhibitor; Given IV to hospitalized pts with acute large bowel distention
neostigmine
Prokinetic class with SE of excessive salivation, nausea, vomiting, diarrhea, bradycardia
cholinomimetics (bethanecol, neostigmine)
Prokinetic class with SE of restlessness, drowsiness, insomnia, anciety, agitation, extrapyramidal effects, tardive dyskinesia, elevated prolactin
D2 receptor antagonist (metoclopramide, domperidone)
Prokinetic that can cause galactorrhea, gynecomastia, impotence, and menstrual disorders
D2 receptor antagonist (metoclopramide, domperidone)
D2 receptor antagonist that does not readily cross the bbb and .:. has fewer neuropsyciatric and extrapyramidal SE
domperidone
Prokinetic that directly stimulates motilin receptors on GI smooth muscle and promotes the onset of an MMC
erythromycin
prokinetic that is given IV for gastroparesis OR prior to endoscopy after an acute upper GI bleed
erythromycin
Action/Class: Psyllium
Laxative
Bulk-forming
Action/Class: methylcellulose
Laxative
Bulk-forming
Action/Class: polycarbophil
Laxative
Bulk-forming
Action/Class: docusate
Laxative
stool surfactant agents
Action/Class: glycerine suppository
Laxative
stool surfactant agents
Action/Class: magnesium hydroxide
Osmotic Laxative
Action/Class: sorbitol
Osmotic Laxative
Action/Class: lactulose
Osmotic Laxative
Action/Class: magnesium citrate
Osmotic Laxative
Action/Class: sodium phosphate
Osmotic Laxative
Action/Class: balanced polyethylene glycol
Osmotic Laxative
Action/Class: Aloe
Laxative
Stimulant
Action/Class: Senna
Laxative
Stimulant
Action/Class: Cascara
Laxative
Stimulant
Action/Class: bisacodyl
Laxative
Stimulant
Action/Class: Lubiprostone
Laxative
Chloride channel activator
Action/Class: Methylnaltrexone
Laxative
opioid receptor antagonist
** highlighted in PPT
Action/Class: alvimopan
Laxative
opioid receptor antagonist
** highlighted in PPT
Action/Class: Tegaserod
Laxative
5 HT4 agonist
Action/Class: Cisapride
Laxative
5 HT4 agonist
** highlighted in PPT
Action/Class: Prucalopride
Laxative
5 HT4 agonist
Action/Class: Linaclotide
Laxative
Guanylate cyclase C agonist (i.e. CFTR activator)
Laxative with potential side effect of long QT
cisapride
To treat opiod induced constipation
methylnaltrexone
Action/Class: Loperamide
Anti-diarrheal
Opioid agonist
Action/Class: Diphenoxylate
Antidiarrheal
Opioid agonist
Non-Rx Opioid Agnoist for tx of diarrhea
loperamide
What do you mix with Diphenoxylate to minimize dependence?
atropine
To treat diarrhea caused by excess fecal bile acids
Bile salt-binding resins (cholestyramine, colestipol, colesevelam)
To treat effects of endcrine tumor (carcinoid, VIPoma)
Octreotide
synthetic somatostatin
octreotide
To tx IBS with constipation
Lubiprostone (Cl channel activator)
To tx IBS with diarrhea
Alosertron (5HT3 antagonist)
How often are anticholinergics used for IBS? MOA? Give two examples
infrequently
antispasmodic
dicyclomine
Hyoscyamine
Action/Class: ONdansetron; granisetron; dolasetron; palonosetron
Antiemetic
5HT3 blocker
Action/Class: dexamethasone
Antiemetic
corticosteroid
Action/Class: aprepitant; fosaprepitant
Antiemetic
neurokinin receptor antagonist
Action/Class: metoclopramide
Antiemetic (also prokinetic)
D2 blocker
Action/Class: droperidol
Antiemetic
D2 blocker
Action/Class: promethazine
Antiemetic
D2 blocker
Action/Class: diphenhydramine
Antiemetic (esp for motion sickness)
H1 blocker
Action/Class: meclizine
Antiemetic
H1 blocker
Action/Class: Dronabinol
Antiemetic
cannabinoid
Action/Class: nabilone
Antiemetic
cannabinoid
Class profile
Indication: chemotherapy induced nausea and vomiting, postop and post radiation nausea and vomiting
AE: headache, dizziness, constipation, prolongation of QT
5 HT3 blockers
ONdansetron; granisetron; dolasetron; palonosetron
Class Profile
antiemetic with unknown MOA
Enhances 5HT3 receptor antagonists
prevention of acute and delayed nausea and vomiting in pts receiving moderate to high emetogenic chemotherapy regimens
corticosteroids
Class profile
antiemetic; May inhibit the metabolism of other drugs metabolized by the CYP3A4 (docetaxel, paclitaxel, etoposide, irinotecan, imatinib, vinblastine, vincristine)
Decreases the INR in patients taking warfarin
Neurokinin receptor antagonist (Aprepitant)
Action/Class: aprepitant
anti-emetic
Neurikinin receptor antagonist
Class Profile: Potent antiemetic and sedative properties
Inhibition of dopamine and muscarinic receptors (antiemetic)
Antihistamine (sedation)
Phenothiazines
(Prochlorperazine, thethylperazine, Promethazine**)
**highlighted in PPT
Action/Class:Promethazine
antiemetic
phenothiazine
**highlighted in PPT
Class Profile: Central dopaminergic blockade
Post-operative nausea and vomiting, in conjunction with opiates and benzodiazepines for sedation for surgical and endoscopic procedures, for neuroleptanalgesia, for induction and maintenance of general anesthesia
AE - extrapyramidal effects, hypotension, may prolong QT interval
Butyrophenone
Droperidol
Action/Class: Droperidol
Antiemetic
Butyrophenone
Action/Class:Metoclopramide, trimethobenzamide
antiemetic
substituted benzamide
Action/Class: Prochlorperazine, thethylperazine
antiemetic
phenothiazine
Class Profile:Central dopaminergic blockade
nausea and vomiting from highly emetogenic chemotherapeutic regimen
AE - extrapyramidal effects (restlessness, dystonias, parkinsonian symptoms)
substituted benzamide
Metoclopramide, trimethobenzamide
Class Profile: Weak antiemetic activity
Particularly useful for the prevention or treatment of motion sickness
AE – sedation, dizziness, confusion, dry mouth, cycloplegia, urinary retention
H1 antihistamines and anticholinergic drugs
Diphenhydramine, dimenhydrinate, Meclizine, Hyoscine (aka scopolamine)
Antiemetic: antihistamine with minimal anticholinergic, less sedation, prevention of motion sickness and treatment of vertigo due to labyrinth dysfunction
Meclizine
Antiemetic: antimuscarinic to prevent motion sickness
Hyoscine (aka scopolamine)
antihistamine and anticholinergic, used in conjunction with other antiemetics for treatment of emesis due to chemotherapy
diphenhydramine, dimenhydrinate
Antiemetic: Before the initiation of chemotherapy to reduce anticipatory vomiting or vomiting caused by anxiety
Benzodiazepines
Lorazepam, diazepam
Action/Class: Dronabinol
Anti-emetic and appetite stimulant
Cannabinoid
Action/Class: Nabilone
Anti-emetic
Cannabinoid
Therapy for severe IBD
TNF antagonists (Infliximab, Adalimumab, Certolizumab)
IV corticosteroids
Therapy for moderate IBD
TNF antagonists (Infliximab, Adalimumab, Certolizumab)
oral corticosteroids
Methotrexate
Azathioprine/6 MP
Therapy for mold IBD
Budesonide
Topical corticosteroids
Antibiotics
5-Aminosalicylates
Action/Class: Sulfasalazine, balsalazide, olsalazine
IBD Therapy (mild) Aminosalicylates
Class Profile:
- First-line agent for treatment of mild to moderate active ulcerative colitis and Crohn’s disease
- Slow acetylators have more frequent and more severe adverse effects
- Oligospermia
- Impairs folate absorption and processing (dietary supplementation is recommended)
Sulfasalazine
Name 3 anti-TNF antibodies for IBD
Infliximab
Adalimumab
Certolizumab
Which anti-TNF Ab is fully humanized?
Adalimumab
Certolizumab (s chimeric, so… whatever. Note the U before the MAB, and that means humanized apparently)
Which anti-TNF Ab is chimeric?
Infliximab
the I before the MAB signifies chimeric.
Blocks alcohol dehydrogenase for
- excess alcohol consumption
- tx of ethylene glycol ingestion
- tx of methanol ingestion
fomepizole
Blocks aldehyde dehydrogenase to act as a deterrent for alcohol consumption. Poor rates of compliance.
Disulfiram
For alcohol dependence
Nonselective competitive antagonist of opioid receptors
Reduced risk of relapse
Naltrexone
For alcohol dependence
NMDA antagonist & GABAA agonist
Reduced risk of relapse
Acamprosate