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what are the pharmacologic options for GERD?
antacids +/- alginic acid
H2-receptor antagonists
PPI
prokinetics
mucosal protectants
which drugs can cause GERD?
1. anticholinergics
2. narcotics
3. CCB
4. nitrates
5. theophylline
6. quinidine
7. bisphosphonates
8. potassium/iron salts
9. aspirin and NSAIDs
which drugs neutralize acid directly in the stomach?
antacids
sodium bicarb
calcium carbonate (tums)
aluminum hydroxide
magnesium hydroxide
what are the effects of sodium bicarb?
- fluid retention (Na retained→ consider this in Cardio/preg patients)
- produce gas
- increased pH increases gastrin release
which antacids can cause increased kidney pH and kidney stones?
calcium carbonate (tums)
which antacid is contraindicated in appendicitis?
aluminum hydroxide (amphagel)
and milk of magnesia
which antacids are constipating?
calcium carbonate (tums)
aluminum hydroxide (amphagel)
what is the MOA of amphagel?
decreases phosphate absorption
which antacid has drug interactions d/t chelation?
aluminum hydroxide (amphagel)
which antacid causes diarrhea?
magnesium hydroxide (milk of magnesia)
which antacid is contraindicated in renal failure, appendicitis, and intestinal obstruction?
milk of magnesia
why are aluminum hydroxide and magnesium hydroxide commonly used together?
amphagel causes constipation, milk of magnesia causes diarrhea
combo drugs = mylanta and maalox
why should you avoid sodium bicarb in pregnant patients?
edema risk
which drug reacts with Na bicarb and saliva to form a viscous solution?
alginic acid
which drugs reduce gastric acid secretion?
H2 receptor antagonists (-tidine)
why should you not use cimetidine?
strong CYP3A4 inhibition
why may H2RA and PPIs be used IV?
to reduce stress ulcers from overproduction of cortisol
should you adjust dose of H2RA in renal impairment
yes
Can H2RAs be used in pregnancy?
yes, cat B
which drugs irreversibly inhibit the proton pump?
PPIs (-prazole)
what are the adverse effects of PPIs?
- hyperplasia of parietal cells
- elevated stomach pH
- bacterial infections
- hypergastrinemia
- decreases calcium absorption (bc calcium likes to be absorbed in acidic environment)
which drugs are better at healing severe esophagitis and providing sx relief?
PPIs
why should PPIs not be chewed or crushed?
they are not stable in acidic environment → meant to be absorbed in intestine
which drug is a gastrin inhibitor?
Octreotide (Sandostatin) → parenteral only
which drugs are mucosal-protecting agents?
pepto-bismol
sucralfate (carafate)
misoprostol
which drug imparts a black color to oral cavity and feces?
pepto bismol
which drug should you not use in children <16 with fever d/t presence of salicylates?
pepto bismol
What is the MOA of misoprostol?
Prostaglandin E1 analog that increases mucus secretions, reducing acid secretions → used in ulcers caused by nsaids
can misoprostol be used in pregnancy?
NO → used for chemical abortion
what is the MOA of pepto-bismol?
enhances cytoprotective factors, inhibits pepsin activity
what are the causes of PUD?
H. pylori
NSAIDs-induced ulcers
stress-related damage (cortisol)
what are the available treatments for PUD?
PPIs
H2RAs
sucralfate
antacids
drugs to eliminate H. pylori
depends on the cause of the ulcer
what are the non-pharm therapies for PUD?
- eliminate or reduce stress
- avoid trigger foods and eat smaller meals
- avoid NSAIDs, Decrease dose of NSAIDs, switch agent
- EtOH/smoking cessation
what agents are used to tx H. pylori?
- abx → clarithro, amox, flagyl, tetracycline
- BSS (bismuth subsalicylate)
- H2RA
- PPI
which one would be most sufficient to treat a pt with H. pylori-induced ulcer?
*** potential test q
Pt on omeprazole, nizatidine, clarithro/amox, why is this incorrect for tx of H. pylori induced ulcer?
PPI + H2RA
4 drug regimen= want bismuth
what is the MOA of bismuth?
local gastroprotection via stimulation of endogenous PGs also suppress H. pylori
what treatment regimens are preferred for H. pylori ulcers?
4 drug regimen is preferred → bismuth, flagyl, tetra, PPI
could do 3 drug regimen → clarithro, amox, PPI
what regimen is used for failure of H. pylori treatment?
omeprazole
amox
metronidazole (flagyl)
what are the risk factors fo NSAID-induced ulcers?
- age >60
- hx of PUD or GI bleed
- concurrent use of corticosteroids
- high dose and multiple NSAID use
- concurrent use of anticoag
- chronic major organ impairment
what is the pathophys for NSAID-induced ulcers?
direct topical irriration of gastric epithelium
inhibition of COX-1 → prevents synthesis of GI mucosal PG
what are the tx options for NSAID-induced ulcers?
- stop NSAID
- eval for H. pylori
- H2RAs/PPIs/sucralfate (PPI preferred)
what agents are used for prevention of NSAID-induced ulcers?
misoprostol
PPIs
H2RAs
what is the MOA for misoprostol?
synthetic PgE1 analog which provided mucosal PGs
pregnancy category X!
when can misoprostol be used for maintenance of healed ulcers?
if NSAIDs are continued
could also use PPI in this circumstance
which anti-emetic has only antimuscarinic actions?
scopolamine
benefit = not sedating
what are the side effects of scopolamine?
dry mouth
blurred vision
urinary retention
which anti-emetics are anti-muscarinic and anti-histaminic?
- dramamine
- meclizine
- hydroxyzine
- benadryl
- glycopyrrolate
- hyoscyamine
ADR = sedation, anti-muscarinic effects
which anti-emetic would be best for someone going on a cruise?
scopolamine
bc only anti-muscarinic = no sedation
which anti-emetics have anti-serotinergic actions?
- zofran
- dolasetron
- granisetron
- 5-HT3 RA
what are the adverse reactions for anti-serotonergic anti-emetics?
HA
diarrhea
constipation
QT prolongation
which anti-emetic is good for chronic drooling?
glycopyrrolate
which anti-emetic is good for abdominal cramping?
hyoscyamine (levsin)
which anti-emetics are useful in chemotherapy?
anti-serotonergics
which anti-emetics are anti-dopaminergic?
- metoclopramide
- phenothiazines → compazine, haldol, Phenergan
what are the adverse reactions of anti-dopaminergic anti-emetics?
- dizziness, fatigue
- seizures
- sedation
- increased prolactin
- neuroleptic malignant syndrome
which anti-dopaminergic is more likely to cause neuroleptic malignant syndrome?
haldol
which cannabinoids are used for anti-emetic effects?
dronabinol (marinol)
nabilone (Cesamet)
Delta 9 oral formulation
which drugs can be used to treat n/v from chemo when other agents fail?
cannabinoids → central action on vomiting center
also useful for appetite stimulation!
what are the adverse reactions of cannabinoids?
confusion
euphoria
dizziness
incoordination
hallucinations
mood change
orthostatic hypotension
increased appetite
which substance P antagonists may be used for anti-emetic effects?
aprepitant (emend) → used for vomiting d/t cisplatin (chemo) in acute AND delayed phase
which drug helps treat N/V in the delayed phase of emesis d/t cisplatin?
aprepitant
CYP3A4 inhibitor!
which corticosteroids are used in chemo-induced N/V?
dexamethasone
prednisone
which drugs are useful as anxiolytics prior to anticipatory N/V?
benzos → ativan and xanax
which route should you consider for anti-emetics?
sublingual
IV
rectal
prob avoid PO
which drugs are prokinetics?
reglan
erythro
increase gastric emptying
which drugs may induce constipation?
opioids
anticholinergics
antacids
iron
CCBs
what are the indications for laxatives?
1. prepare for bowel surgery
2. hasten bowel excretions of toxins
3. post-operative stimulation
4. minimizing straining in pt with CV dz
5. relief of temporary constipation
in which dx is laxative use contraindicated?
underlying bowel disease
what are the general side effects of laxitives?
acute → N, abd cramp, Diarrhea
chronic → mucosal inflammation, atrophy of outer muscle layers, damage to nerve plexus, malabsorption, dehydration, protein loss, disruption of intestinal flora
what are the 3 categories of laxatives?
1. soften in 1-3 days (bulk-forming agents, emollients, osmotic agents)
2. soft/semi-fluid stools in 6-12 hrs (stimulants)
3. watery evacuation in 1-6 hrs (osmotic laxatives, enemas, bowel clean outs)
which laxatives are bulk-forming?
- psyllium (metamucil)
- methylcellulose (citrucel)
non-digestible fiber→ increase bulk and water content of stool → increase motility
which laxatives are stool softeners?
Docusate sodium (Colace)
mineral oil
glycerin
emulsified with stool → increase water content and lubricate
which laxatives are stimulants/irritants?
- castor oil → increase motility and water/electrolyte secretion
- senna → increase colonic motility
- bisacodyl (dulcolax) → increase colonic motility
what are the side effects of stimulant laxatives?
Abdominal cramps, weakness,
diarrhea
which laxatives are osmotic agents?
- mag sulfate
- mag hydroxide
- lactulose, mannitol
- sodium phosphate (fleet enema)
- polyethylene glycol (miralax)
increase water content and motility
what may be a cause of fatality in pts using osmotic laxatives?
use of electrolytes in young/old patients → fatalities due to hyperphosphatemia
(particularly sodium phosphate enemas)
why should you not rectally administer drugs to neutropenic patients?
risk of microtears → infection
which opioids are used as anti-diarrheals?
diphenoxylate (Lomotil)
loperamide (imodium)
which anti-diarrheal is used for infectious diarrhea?
pepto-bismol
which drugs are aminosalicylates?
sulfasalazine (Azulfidine)
Mesalamine (5-ASA)
what is the MOA for sulfasalazine?
prodrug of sulfapyridine and 5-ASA (mesalamine) → reduced inflam through inhibition of COX and lipoxygenaase
what may be a CI for sulfasalazine?
sulfa drugs
use mesalamine instead!
which form of 5-ASA would be used for proctitis?
canasa
which form of 5-ASA would be best for left-sided disease?
rowasa
what is the MOA of mesalamine?
reduces inflam through inhibition of COX, lipoxygenase and other possible mechanisms
less adverse effects than sulfasalzine
which form of 5-ASA would be best for proximal disease?
oral → pentasa, lialda, asacol
which corticosteroid has the least systemic effects?
budesonide → extensive 1st pass effect
which immunosuppressants can be used for treatment of IBD?
thiopurines
cyclosporine
methotrexate
what are the adverse reactions of corticosteroids?
weight gain
diarrhea
nausea
glucose intolerance
osteoporosis
cushing's disease
which corticosteroids are used for IBD?
oral → budesonide, prednisone, methylprednisone
topical → colocort, anusol-HC, cortifoam
IV → hydrocortisone, prednisolone, methylprednisolone
know risk of anaphylaxis with MAbs
!!!
which monoclonal abs are used for IBD?
infliximab (remicade)
adalimumab (humira)
which immunosuppressant has risk of nephrotoxicity, HTN, infection, and hirsutism?
cyclosporine (Neoral)
which immunosuppressant has risk of myelosuppression, hepatotoxitiy, infectionss, and dermatologic reactions?
methotrexate
which treatments are used for IBS-C?
- bulk-forming laxatives
- osmotic laxative
- lubiprostone
- TCA/SSRI
- 5HT4 partial agonist (tegaserold)
which treatments are used for IBS-U?
probiotics
TCA/SSRI
antispasmodic
which treatments are used for IBS-D?
- bulk-forming laxatives
- loperamide /cholestyramine
- TCA/SSRI
- 5HT3 antagonist (alosetron)
which drug is used to treat SIBO?
rifaximin
what is the MOA of lubiprostone (Amitzia)?
PGE1 derivative that increases intestinal secretion secondary to Cl channel activation
