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
Dronabinol
- MOA
- Indications
- MOA
- Cannabinoid receptor agonist
- Indications
- chemo-induced emesis
Azathioprine
- MOA
- Indications
- Side effects
- MOA
- Prodrug of purine analog 6-mercaptopurine
- inhibits DNA replication
- Inhibits B and T cell proliferation
- Indications
- Organ rejection, RA, SLE (FA 215/403)
- Side effects
- Bone marrow suppression
Hyoscine
- MOA
- Indications
- MOA
- Muscarinic receptor antagonist
- Indications
- motion sickness
Glucocorticoids
- MOA (in immunosuppression)
- Indications
- MOA
- NF-KB inhibitor, triggering apoptosis (FA 215/406)
- Indications
- Transplate rejection
- Graft vs Host disease
- Autoimmune
Methylprednisolone
- Belongs to which Drug class?
- Indications
- Glucocorticoids
- Acute transplant rejection
Antithymocyte Globulin (ATG)
- MOA
- Indications
- Side effects
- MOA
- Ab to T-cell ag
- depletes circulating lymphocytes
- Indications
- Acute renal rejection
- Immunosuppression
- Withdrawal of calcineurin inhibitors
- Side effects
- Cytokine release syndrome
- T cells are active before being destroyed
- Cytokine release syndrome
Cyclosporin
- MOA
- Indications
- Side effects
- MOA
- binds cyclophilin
- blocks dephosphorylation of NFAT by calcineurin, can’t enter nucleus
- Blocks IL-2 production
- Indications
- Organ transplants
- RA
- Side effects
- Nephrotoxicity
- HTN
- Hirsutism
- gum hyperplasia
What is the MOA of cyclosporine?
binds cyclophilin
blocks dephosphorylation of NFAT by calcineurin, can’t enter nucleus
Blocks IL-2 production

What are the therapeutic uses of cyclosporine?
- Organ transplants
- RA
What side effects are associated with cyclosporine?
- Nephrotoxicity
- HTN
- Hirsutism
- Gum hyperplasia
Both calcineurin inhibitors are highly nephrotoxic. (tacrolimus and cyclosporine)
Tacrolimus
- MOA
- Indications
- Side effects
- MOA
- binds FKBP
- Prevents dephosphorylation of NFAT by calcineurin
- inhibits IL-2 production
- Indications
- Transplantation and rescue w/rejection
- Side effects
- Nephrotoxicity
- Neurotoxicity
What is the MOA of Tacrolimus?
- binds FKBP
- Prevents dephosphorylation of NFAT by calcineurin
- inhibits IL-2 production

What are the therapeutic uses of tacrolimus?
- Transplantation
- rescue therapy w/ rejection
What side effects are associated with Tacrolimus?
- Nephrotoxicity
- Neurotoxicity
Both calcineurin inhibitors are highly nephrotoxic. (tacrolimus and cyclosporine)
Sirolimus (Rapamycin)
- MOA
- Indications
- Side effects
- MOA
- Binds FKBP (like tacolimus)
- blocks mTOR to inhibit intracellular IL-2 receptor signaling
- Indications
- Prophylaxis in organ transplants
- Side effects
- Hyperlipidemia
- Leukopenia
- Thrombocytopenia
- The kidney “Sir-vives”
What is the MOA of Sirolimus (Rapamycin)?
- Binds FKBP (like tacolimus)
- blocks mTOR to inhibit intracellular IL-2 receptor signaling

What are the therapeutic uses of Sirolimus?
Prophylaxis in organ transplantation
esp in patients with liver disease
What side effects are associated with Sirolimus?
- Hyperlipidemia
- Leukopenia
- Thrombocytopenia
Mycophenolic Acid and Mycophenolate Mofetil
- MOA
- Indications
- Side effects
- MOA
- inhibits inosine monophosphate dehydrogenase (IMPDH)
- rate-limiting in guanosine formation
- Preferentially affects lymphocytes
- depend solely on IMPDH for purine synthesis
- Drug prefers Type II IMPDH, highly expressed in lymphocytes
- inhibits inosine monophosphate dehydrogenase (IMPDH)
- Indications
- Transplant rejection
- Side effects
- leukopenia
What is the MOA for Mycophenolic Acid and Mycophenolate Mofentil?
- inhibits inosine monophosphate dehydorgenase (IMPDH)
- rate-limiting in guanosine formation
- Preferentially affects lymphocytes
- depend solely on IMPDH for purine synthesis
- Drug prefers Type II IMPDH, highly expressed in lymphocytes
Muromonab - CD-3
- MOA
- Indications
- Side effects
- MOA
- Ab against CD3
- depletes T-cells
- Indications
- organ transplant rejection
- Side effects
- Cytokine release syndrome
- pulm edema
- CV collapse and arrythmia
Daclizumab
- MOA
- Indications
- Side effects
- MOA
- anti-CD25
- binds IL-2 receptor on activated T cells
- Indications
- Renal transplants (prophylactic)
- Side effects
- Anaphylaxis
Lenalidomide
- MOA
- Side effects
- MOA
- tumor cell apoptosis
- Side effects
- teratogen (related to thalidomide)
Thalidomide
- Indications
- Side effects
- Indications
- multiple myeloma
- leprosy
- Side effects
- teratogen
Rh0(D) Immune Globulin
- MOA
- Indications
- MOA
- IgG Ab
- Indications
- Rhesus disease
- defend Rh (+) baby against Rh (-) mom’s immune system
Mitotane
- Action
- Indication
- Action
- Toxic to adrenocortical cells
- Inhibits P450
- Indication
- Adrenal tumor
Aminoglutethimide
- MOA
- Indications
- Side effects
- MOA
- blocks cholesterol side-chain cleavage
- (No pregnenolone)
- inhibits P450
- Indications
- breast cancer
- prostate cancer
- Side effects
- Adrenal insufficiency (not enough hormone produced)
- GI/Neuro issues
- rash
Ketoconazole
- MOA
- Indications
- Side effects
- MOA
- inhibits 17-alpha-hydroxylase
- excess mineralocorticoids
- decreased glucocorticoids
- inhibits P450
- inhibits 17-alpha-hydroxylase
- Indications
- Antifungal
- Cushing’s (second line)
- Side effects
- hepatotoxicity
Metyrapone
- MOA
- Indications
- MOA
- inhibits 11ß-hydroxylase
- Indications
- hypercorticism (cushing’s) resulting from neoplasm
What is the MOA of glucocorticoid use and the effects?
- MOA
- binds type II glucocorticoid receptor
- Binds GRE (response elements) which change gene expression
- Physiology
- increased glucose (SE=diabetes)
- Increased aa (muscle catabolism)
- Increased triglycerides
- decrease inflammation
What are the therapeutic uses of glucocorticoids?
- Adrenal insufficiency (ex; Addison’s disease)
- Anti-inflammatory/ immune suppression
- asthma
- RA
- Crohn’s
- Psoriasis
- dermatitis
- arthritis
What are the side effects associated with glucocorticoids?
- Diabetes
- Cushing’s
- Osteoporosis
- Impaired vertical bone growth in children
- Secondary hyperparathyroidism
- Steroid psychosis
Fludrocortisone
- Indications
Hypoaldosteronism
Presents with dehydration, hypotension, possibly hyperkalemia
Spironolactone
- MOA
- Indications
- MOA
- minerolocorticoid receptor antagonist
- Indications
- hyperaldosteronism
- edema, HTN, hypokalemia
- hyperaldosteronism
Eplerenone
- MOA
- Indications
- MOA
- minerolocorticoid receptor antagonist
- Indications
- hyperaldosteronism
- edema, HTN, hypokalemia
- hyperaldosteronism
ß2 agonists
- MOA
- Indications
- Side effects
- MOA
- increase cAMP
- relax bronchial smooth mm
- Indications
- asthma
- Side effects
- tachycardia
- hypotension
Albuterol, terbutaline, pirbuterol, salmeterol
Ipratropium
- MOA
- Indications
- MOA
- muscarinic receptor antagonist
- Indications
- asthma and COPD in patients who can’t take ß2 agonists
- taking MAOI
- arrhythmia or angina
- asthma and COPD in patients who can’t take ß2 agonists
Tiotropium
- MOA
- Indications
- MOA
- muscarinic receptor antagonist
- Indications
- asthma and COPD in patients who can’t take ß2 agonists
- taking MAOIs
- arrhythmia or angina
- asthma and COPD in patients who can’t take ß2 agonists
Beclomethasone
- MOA
- Indications
- Side effects
- MOA
- glucocorticoid
- suppresses inflammation
- Indications
- severe asthma attacks
- Side effects
- hoarse voice
- oral candidiasis
Fluticasone
- MOA
- Indications
- Side effects
- MOA
- glucocorticoid
- Indications
- severe asthma attacks
- Side effects
- hoarse voice
- oral candidiasis
Cromolyn
- MOA
- Indications
- Side effects
- MOA
- inhibits mast cell degranulation
- reduce airway reactivity
- Indications
- moderate/severe asthma
- Side effects = mild
- cough
- wheezing
- bronchospasm
- bad taste
Montelukast
- MOA
- Indications
- Side effects
- MOA
- Leudotriene receptor antagonist (C4, D4, E4)
- same with zafirlukast
- Indications
- prophylactic, mild asthma
- Side effects = rare
- pulm. inflitrates
- neuropathy
- skin rash
- vasculitis
-Lukast = Leukotriene receptor antagonist

Zileuton
- MOA
- Indications
- Side effects
- MOA
- 5-lipoxygenase inhibitor
- Indications
- prophylactic for mild asthma
- Side effects
- (slight elevation of liver enzymes)

Omalizumab
- MOA
- Indications
- MOA
- IgG Ab that binds free IgE
- blocks release of histamine and leukotrienes
- decreased airway responsiveness
- Indications
- asthma
Combivent (Ipratropium/Albuterol)
- Indication
- Contraindication
- Indication: COPD
- CON: soy allergy
First Generation H1 receptor antagonists
- Indications
- Side effects
Diphenhydramine, Promethazine, Hydroxaline
- en/ine or -en/ate
- Enter CNS
- Indications
- Allergic reaction
- Side effects
- Sedation
- Anti-muscarinic effects
Second Generation H1 Receptor Antagonists
- Indications
- Side effects
Loratadine, Fexofenadine
-adine
- MOA
- does not cross into CNS
- Indications
- Allergic reaction
- Side effects
- minimal
Diphenhydramine
- MOA
- Indications
- Side effects
- MOA
- first gen H1 histamine receptor blocker
- Indications
- allergies
- motion sickness
- reduces early Parkinson’s symptoms
- Side effects
- Sedation
- anti-cholinergic effects
Promethazine
- MOA
- Indications
- Side effects
- MOA
- first gen H1 histamine receptor blocker
- Indications
- allergies
- motion sickness
- Side effects
- Sedation
- anti-cholinergic effects
Triptans
- MOA
- Indications
- Side Effects
- Types: Sumatriptan, Zolmitriptan
- MOA
- 5HT1 receptor agonist
- 1B and 1D (vasoconstriction)
- 5HT1 receptor agonist
- Indications
- Acute migraine
- Side Effects
- Dry mouth
- Paresthesia
- Coronary artery spasm
- arrythmia
Ergot Alkaloids
- MOA
- Indications
- Side Effects/CON
- Types: Methysergide, Ergotamine
- MOA
- 5HT agonists
- Indications
- migraine
- Side Effects/CON
- CON: Pregnancy
- stimulates uterus, decrease blood flow
- CON: coronary or peripheral artery disease
- CONLiver or renal disease
- CON: Pregnancy
Methylsergide
- MOA
- Indications
- Side Effects
- MOA
- 5HT receptor agonist
- Indications
- migraine prophylaxis
- Side Effects
- Same as ergot alkaloids
- develop lung/heart fibrosis
- shouldn’t be administered more than 6 mo.
What is the difference in the MOA between acetylsalicylic acid and acetaminophen?
- acetylsalicylic acid
- irreversible inhibition of COX 1 & 2
- Acts peripherally so anti-inflammatory
- Acetaminophen
- reversible
- only acts on CNS (inactivated peripherally)
What are side effects of acetylsalicylic acid?
- Ulcers
- Increased bleeding
- Reyes (children with viral infection)
- Hep tox
- Tinnitis with toxicity
When is acetaminophen preferred over acetylsalicylic acid?
Patients with:
- ulcers
- anticoag meds/clotting disorder
- gout
- children with viral infection
Celecoxib
- MOA
- Indications
- Side effects
- MOA
- irreversibly inhibits COX-2
- thought to be upregulated at sites of inflammation only, protecting normal PG function
- irreversibly inhibits COX-2
- Indications
- Rheumatoid arthritis
- Osteoarthritis
- Side effects
- Allergic rxn to Sulfa
What drugs are used for the treatment of Rheumatoid arthritis?
- Anti-neoplastic drugs
- Etanercept (false TNF-alpha receptor)
- TNF-alpha Ab
- Infliximab
- Adalimumab
- Gold compounds
- Celecoxib (inhibits COX-2 only)
Etanercept
- MOA
- Indications
- Side effects
- MOA
- false receptor for TNF-alpha
- anti-inflammatory
- Indications
- Rheumatoid arthritis
- autoimmune disease
- Side effects
- Injection site rxn
Infliximab
- MOA
- Indications
- Side effects
- MOA
- TNF-alpha Ab
- inhibit inflammation
- Indications
- Autoimmune disease
- RA
- Inflammatory bowel disease
- Side effects
- Infection
- Anaphylaxis/hypotension (rare)
- Lupus-like syndrome (rare)
Gold compounds in treatment of RA
- Action
- Indication
- Side effects
- Action
- relieve pain/stiffness
- may prevent further joint degeneration
- Indication
- progressive RA
- Side Effects
- metallic taste
- GI problems
- dermatitis
- blood component disorders
What agents are used to treat gout?
- NSAIDS
- Glucocorticoids
- Colchicine
- Probenecid
- Allopurinol
- Rasburicase
Colchicine
- MOA
- Indications
- Side effects
- MOA
- inhibits migration of granulocytes to inflammed area (MT depolarization)
- Indications
- Acute attacks of gout
- Side effects
- Diarrhea
- Blood dyscrasia
Probenecid
- MOA
- Indications
- Side effects
- MOA
- decrease reabsorption of uric acid (increased excretion)
- Indications
- prevent further attacks of gout
- Side effects
- decreased renal function
Allopurinol
- MOA
- Indications
- MOA
- decreased production of uric acid
- inhibit xanthine oxidase (purine metabolism)
- Indications
- Prevent attacks of gout
Rasburicase
- MOA
- Indications
- Side effects
- MOA
- recombinant version of urate oxidase
- catalyze conversion of uric acid to allantoin
- increased excretion
- recombinant version of urate oxidase
- Indications
- Gout
Febuxostat
- MOA
- Indications
- Side effects
- MOA
- decreased production of uric acid
- inhibit xanthine oxidase (purine metabolism)
- Indications
- Prevent attacks of gout
MOA of drugs in treatment of Gout:
- Allopurinol
- Febuxostat
- Probenacid
- Diuretics