Test 4: Arrhythmias, Immune, GI Flashcards
What is the MOA of H2 Blockers?
Reversibly block Histamine H2 receptors, decreasing basal secretion of H+ by parietal cells
Take H2 blockers before you “dine”. Think: “table for 2” to remember H2
What is the suffix of H2 Blockers?
–tidine
Cimetidine
Ranitidine
Famotidine
Take H2 blockers before you “-dine”. Think: “table for 2” to remember H2
What are the therapeutic uses of H2 Blockers?
- Ulcers
- GERD
**Not as effective as proton pump inhibitors
What side effects are associated with H2 Blockers?
All:
- Tolerance in 3 days
- Loss of effectiveness
- May cause hypergastrinemia
Very High Doses (OTC)
- (-) Testosterone
- gynecomastia
- Thrombocytopenia
Cimetidine
- Inhibits CYP enzymes of liver
What side effect is unique to Cimetidine within the H2 Blocker family?
It inhibits CYP liver enzymes
What is the MOA of proton pump inhibitors?
- Reacts covalently and irreversibly with the H+/K+ ATPase
- Long-acting
- Most potent suppressors of gastric acid secretion
What is the suffix of proton pump inhibitors?
-prazole
(Think pretzel)
Ex: Omeprazole
How does food affect bioavailability of proton pump inhibitors?
It decreases it by 50%
What are the therapeutic uses of proton pump inhibitors?
- Ulcers
- GERD
- erosive esophagitis
- Zollinger-Ellison syndrome (hypergastrinemia)
- NSAID-associated gastric ulcers
Which proton pump inhibitor is indicated for use in children?
Omeprazole
What side effects are associated with proton pump inhibitors?
- Hip fracture
- inhibit osteoclastic activity
- Bone loss
- Magnesium depletion
- Hypergastrinemia
- rebound hyperacidity and tumors
What is the MOA of Sucralfate?
- It is an aluminum polysaccharide
- At pH<4, undergoes cross-linking, creates polymer that sticks to epithelial cells and ulcerations
- provide physical protection
- (Don’t take w/antiacids or things that increase stomach pH)
What are the therapeutic uses of sucralfate?
- Mucosal inflammation and ulceration
- oral mucositis/proctitis from radiation
- bile reflux
- Not used for peptic acid disease
What side effects are associated with sucralfate?
- Constipation
- can also be used to treat traveller’s diarrhea (FA)
- CON: Renal failure
- aluminum overload
WHat is the MOA of Misoprostol?
- Prostaglandin analog (PGE1)
- stimulates mucin production
- inhibits cAMP in parietal cells => inhibits H+ secretion and acid formation
What side effects are associated with Misoprostol?
- abortifacient
- CON: pregnant women
- Diarrhea
- CON: IBS (irritable bowel syndrome)
What are the therapeutic uses of Misoprostol?
NSAID-induced mucosal injury
Mg2+ antacids
- Benefit
- Side effects
- Rapidly acting
- SE:
- Diarrhea
- Mg = Must Go to the bathroom
- Chelates drugs
- Diarrhea
Al3+ antacids
- Benefit
- Side Effects
- Slowly-reacting (long-term relief but not immediate)
- SE:
- Constipation
- Aluminimum amount of feces
- Chelates drugs
- Constipation
What are the negative effects associated with CaCO3 antacids?
- CO2
- cause belching, nausea, flatulence
- Ca2+
- rebound acid secretion
Simethicone
- MOA
Surfactant that may decrease foaming and esophageal reflux
Bismuth
- MOA
- Indication
- SE
- MOA
- physical protection by binding ulcer
- promote mucin and HCO3- secretion
- Antibacterial against H. pylori
- Indication (not as important)
- H. pylori ulcers
- nausea
- diarrhea
- gastroenteritis
Neostigmine methylsulfate
- MOA
- IND
- SE
Last ditch effort
- MOA
- AChE inhibitor
- IND (off label)
- Colonic pseudo obstruction
- Paralytic ileus
- SE
- Severe Bradycardia
Metoclopramide
- MOA
- Indications
- Side effects
- MOA
- D2 receptor antagonist
- stimulate ACh release from myenteric motor neurons
- acts on upper digestive tract
- Indications
- Gastroparesis
- anti-emetic (dismotility or chemo)
- Side effects
- Extrapyramidal symptoms
- parkinson-like
- dystonia
- tardive dyskinesia
- Galactorrhea
- increased Prolactin
- Pituitary hypertrophy possible
- Extrapyramidal symptoms
What side effects are associated with Metoclopramide?
- Extrapyramidal symptoms
- parkinson-like
- dystonia
- tardive dyskinesia
- Galactorrhea
- increased Prolactin
- Pituitary hypertrophy possible
What is the MOA of metoclopramide?
- D2 receptor antagonist
- increases ACh release from myenteric motor neurons
- acts on upper digestive tract
What are the therapeutic uses of metoclopramide?
- gastroparesis
- anti-emetic (w/dismotility or chemo)
What is the MOA of serotonin receptor agonists on the GI tract?
- stimulate nausea, vomiting, abdominal pain
- Peristaltic reflex
Tegaserod
- MOA
- Indications
- Side effects
- MOA
- Serotonin receptor agonist
- Stimulates motility
- Indications
- constipation-predominant irritable bowel syndrome
- Side effects
- Diarrhea
- Headache
What is the MOA of Cisapride? Why is it no longer used?
- MOA:
- serotonin receptor agonist
- stimulate gastric motility
- IND:
- GERD
- Gastroparesis
- SE: arrhythmias
- V-tach
- V-Fib
- torsade de pointes
Macrolides
- MOA
- Indications
- Ex: erythromycin and other -mycins
- MOA
- motilin mimetic
- used to stimulate motility of upper GI and “sweep the bowel clean”
- Increased LES presure
- Indications
- Diabetic gastroparesis
- Dumping effect (ultrastrong contractions to clear undigestible residue)
What is the effect of botulinum toxin in the GI tract?
paralyzes LES and improves esophageal clearance
Used for esophageal spasms
Which types of laxatives are the mildest with regard to symptoms and used for mild discomfort?
- Bulk-forming laxatives
- ex: dietary fiber and supplements
- Surfactant laxatives
Which type of laxatives are of intermediate action, turning stools soft/semi-fluid and work in 6-8 hours?
Stimulant laxatives
Which types of laxatives are used for watery evacuation in 1-3 hours?
Osmotic laxatives (high dose)
(low dose used for laxative effect)
Which type of laxative is used when non-pharmacological measures are unrealistic (elderly, infirmity)?
- Bulk-forming
- Osmotic (low dose)
What are the effects of long-term use of stimulant laxatives?
- habit
- loss of excess water and electrolytes
- possible secondary aldosteronism
What are contraindications for bulk-forming laxatives?
- Megacolon
- Obstruction
What is the MOA of osmotic laxatives?
osmotically-mediated water retention, which stimulates peristalsis
What are the therapeutic uses of Bile Acid Sequestrants in GI dysfunction?
Treat bile salt-induced diarrhea from resection of the distal ileum
(normal site of bile acid reabsorption)
Loperamide
- MOA
- Indications
- Side effects
- aka imodium
- MOA
- binds to opioid receptors in the GI tract
- Indications
- traveller’s diarrhea
- Side effects
- mild, cannot penetrate CNS
Ondansetron
- MOA
- Indications
- MOA
- serotonin receptor antagonist
- Indications
- chemo-induced emesis
- most powerful and safe
- chemo-induced emesis
Diphenhydramine
- MOA
- Indications
- MOA
- Histamine H1 receptor antagonist
- Indications
- Motion sickness
Aprepitant
- MOA
- Indications
- MOA
- Neurokinin receptor antagonist
- Indications
- chemo-induced emesis
- delayed vomiting, often associated with Cisplatin