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Pharmacology > Test 4: Arrhythmias, Immune, GI > Flashcards

Test 4: Arrhythmias, Immune, GI Flashcards

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1
Q

What is the MOA of H2 Blockers?

A

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

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2
Q

What is the suffix of H2 Blockers?

A

–tidine

Cimetidine

Ranitidine

Famotidine

Take H2 blockers before you “-dine”. Think: “table for 2” to remember H2

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3
Q

What are the therapeutic uses of H2 Blockers?

A
  1. Ulcers
  2. GERD

**Not as effective as proton pump inhibitors

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4
Q

What side effects are associated with H2 Blockers?

A

All:

  • Tolerance in 3 days
    • Loss of effectiveness
    • May cause hypergastrinemia

Very High Doses (OTC)

  • (-) Testosterone
    • gynecomastia
  • Thrombocytopenia

Cimetidine

  • Inhibits CYP enzymes of liver
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5
Q

What side effect is unique to Cimetidine within the H2 Blocker family?

A

It inhibits CYP liver enzymes

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6
Q

What is the MOA of proton pump inhibitors?

A
  • Reacts covalently and irreversibly with the H+/K+ ATPase
    • Long-acting
  • Most potent suppressors of gastric acid secretion
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7
Q

What is the suffix of proton pump inhibitors?

A

-prazole

(Think pretzel)

Ex: Omeprazole

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8
Q

How does food affect bioavailability of proton pump inhibitors?

A

It decreases it by 50%

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9
Q

What are the therapeutic uses of proton pump inhibitors?

A
  1. Ulcers
  2. GERD
  3. erosive esophagitis
  4. Zollinger-Ellison syndrome (hypergastrinemia)
  5. NSAID-associated gastric ulcers
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10
Q

Which proton pump inhibitor is indicated for use in children?

A

Omeprazole

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11
Q

What side effects are associated with proton pump inhibitors?

A
  1. Hip fracture
    • inhibit osteoclastic activity
    • Bone loss
  2. Magnesium depletion
  3. Hypergastrinemia
    • rebound hyperacidity and tumors
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12
Q

What is the MOA of Sucralfate?

A
  • 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)
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13
Q

What are the therapeutic uses of sucralfate?

A
  • Mucosal inflammation and ulceration
    • oral mucositis/proctitis from radiation
    • bile reflux
  • Not used for peptic acid disease
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14
Q

What side effects are associated with sucralfate?

A
  • Constipation
    • can also be used to treat traveller’s diarrhea (FA)
  • CON: Renal failure
    • aluminum overload
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15
Q

WHat is the MOA of Misoprostol?

A
  • Prostaglandin analog (PGE1)
  • stimulates mucin production
  • inhibits cAMP in parietal cells => inhibits H+ secretion and acid formation
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16
Q

What side effects are associated with Misoprostol?

A
  • abortifacient
    • CON: pregnant women
  • Diarrhea
    • CON: IBS (irritable bowel syndrome)
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17
Q

What are the therapeutic uses of Misoprostol?

A

NSAID-induced mucosal injury

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18
Q

Mg2+ antacids

  • Benefit
  • Side effects
A
  • Rapidly acting
  • SE:
    • Diarrhea
      • Mg = Must Go to the bathroom
    • Chelates drugs
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19
Q

Al3+ antacids

  • Benefit
  • Side Effects
A
  • Slowly-reacting (long-term relief but not immediate)
  • SE:
    • Constipation
      • Aluminimum amount of feces
    • Chelates drugs
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20
Q

What are the negative effects associated with CaCO3 antacids?

A
  • CO2
    • cause belching, nausea, flatulence
  • Ca2+
    • rebound acid secretion
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21
Q

Simethicone

  • MOA
A

Surfactant that may decrease foaming and esophageal reflux

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22
Q

Bismuth

  • MOA
  • Indication
  • SE
A
  • 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
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23
Q

Neostigmine methylsulfate

  • MOA
  • IND
  • SE
A

Last ditch effort

  • MOA
    • AChE inhibitor
  • IND (off label)
    • Colonic pseudo obstruction
    • Paralytic ileus
  • SE
    • Severe Bradycardia
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24
Q

Metoclopramide

  • MOA
  • Indications
  • Side effects
A
  • 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
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25
What side effects are associated with Metoclopramide?
* Extrapyramidal symptoms * parkinson-like * dystonia * tardive dyskinesia * Galactorrhea * increased Prolactin * Pituitary hypertrophy possible
26
What is the MOA of metoclopramide?
* D2 receptor antagonist * increases ACh release from myenteric motor neurons * acts on upper digestive tract
27
What are the therapeutic uses of metoclopramide?
1. gastroparesis 2. anti-emetic (w/dismotility or chemo)
28
What is the MOA of serotonin receptor agonists on the GI tract?
* stimulate nausea, vomiting, abdominal pain * Peristaltic reflex
29
Tegaserod * MOA * Indications * Side effects
* MOA * Serotonin receptor agonist * Stimulates motility * Indications * constipation-predominant irritable bowel syndrome * Side effects * Diarrhea * Headache
30
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
31
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)
32
What is the effect of botulinum toxin in the GI tract?
paralyzes LES and improves esophageal clearance Used for esophageal spasms
33
Which types of laxatives are the mildest with regard to symptoms and used for mild discomfort?
1. Bulk-forming laxatives * ex: dietary fiber and supplements 2. Surfactant laxatives
34
Which type of laxatives are of intermediate action, turning stools soft/semi-fluid and work in 6-8 hours?
Stimulant laxatives
35
Which types of laxatives are used for watery evacuation in 1-3 hours?
Osmotic laxatives (high dose) | (low dose used for laxative effect)
36
Which type of laxative is used when non-pharmacological measures are unrealistic (elderly, infirmity)?
1. Bulk-forming 2. Osmotic (low dose)
37
What are the effects of long-term use of stimulant laxatives?
1. habit 2. loss of excess water and electrolytes 3. possible secondary aldosteronism
38
What are contraindications for bulk-forming laxatives?
1. Megacolon 2. Obstruction
39
What is the MOA of osmotic laxatives?
osmotically-mediated water retention, which stimulates peristalsis
40
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)
41
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
42
Ondansetron * MOA * Indications
* MOA * serotonin receptor antagonist * Indications * chemo-induced emesis * most powerful and safe
43
Diphenhydramine * MOA * Indications
* MOA * Histamine H1 receptor antagonist * Indications * Motion sickness
44
Aprepitant * MOA * Indications
* MOA * Neurokinin receptor antagonist * Indications * chemo-induced emesis * delayed vomiting, often associated with Cisplatin
45
Dronabinol * MOA * Indications
* MOA * Cannabinoid receptor agonist * Indications * chemo-induced emesis
46
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
47
Hyoscine * MOA * Indications
* MOA * Muscarinic receptor antagonist * Indications * motion sickness
48
Glucocorticoids * MOA (in immunosuppression) * Indications
* MOA * NF-KB inhibitor, triggering apoptosis (FA 215/406) * Indications * Transplate rejection * Graft vs Host disease * Autoimmune
49
Methylprednisolone * Belongs to which Drug class? * Indications
* Glucocorticoids * Acute transplant rejection
50
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
51
Cyclosporin * MOA * Indications * Side effects
* MOA * binds **cyclo**philin * 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
52
What is the MOA of cyclosporine?
binds cyclophilin blocks dephosphorylation of NFAT by calcineurin, can't enter nucleus Blocks IL-2 production
53
What are the therapeutic uses of cyclosporine?
1. Organ transplants 2. RA
54
What side effects are associated with cyclosporine?
1. Nephrotoxicity 2. HTN 3. Hirsutism 4. Gum hyperplasia Both calcineurin inhibitors are highly nephrotoxic. (tacrolimus and cyclosporine)
55
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
56
What is the MOA of Tacrolimus?
* binds **FKBP** * Prevents dephosphorylation of NFAT by calcineurin * inhibits IL-2 production
57
What are the therapeutic uses of tacrolimus?
1. Transplantation 2. rescue therapy w/ rejection
58
What side effects are associated with Tacrolimus?
1. Nephrotoxicity 2. Neurotoxicity Both calcineurin inhibitors are highly nephrotoxic. (tacrolimus and cyclosporine)
59
**Sir**olimus (**R**apamycin) * MOA * Indications * Side effects
* MOA * Binds FKBP (like tacolimus) * blocks mTO**R** to inhibit intracellular IL-2 receptor signaling * Indications * Prophylaxis in organ transplants * Side effects * Hyperlipidemia * Leukopenia * Thrombocytopenia * The kidney "**Sir**-vives"
60
What is the MOA of Sirolimus (Rapamycin)?
* Binds FKBP (like tacolimus) * blocks mTOR to inhibit intracellular IL-2 receptor signaling
61
What are the therapeutic uses of Sirolimus?
Prophylaxis in organ transplantation esp in patients with liver disease
62
What side effects are associated with Sirolimus?
1. Hyperlipidemia 2. Leukopenia 3. Thrombocytopenia
63
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 * Indications * Transplant rejection * Side effects * leukopenia
64
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
65
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
66
Daclizumab * MOA * Indications * Side effects
* MOA * anti-CD25 * binds IL-2 receptor on activated T cells * Indications * Renal transplants (prophylactic) * Side effects * Anaphylaxis
67
Lenalidomide * MOA * Side effects
* MOA * tumor cell apoptosis * Side effects * teratogen (related to thalidomide)
68
Thalidomide * Indications * Side effects
* Indications * ​multiple myeloma * leprosy * Side effects * teratogen
69
Rh0(D) Immune Globulin * MOA * Indications
* MOA * IgG Ab * Indications * Rhesus disease * defend Rh (+) baby against Rh (-) mom's immune system
70
Mitotane * Action * Indication
* Action * Toxic to adrenocortical cells * Inhibits P450 * Indication * Adrenal tumor
71
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
72
Ketoconazole * MOA * Indications * Side effects
* MOA * inhibits 17-alpha-hydroxylase * excess mineralocorticoids * decreased glucocorticoids * inhibits P450 * Indications * Antifungal * Cushing's (second line) * Side effects * hepatotoxicity
73
Metyrapone * MOA * Indications
* MOA * inhibits 11ß-hydroxylase * Indications * hypercorticism (cushing's) resulting from neoplasm
74
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
75
What are the therapeutic uses of glucocorticoids?
1. Adrenal insufficiency (ex; Addison's disease) 2. Anti-inflammatory/ immune suppression * asthma * RA * Crohn's * Psoriasis * dermatitis * arthritis
76
What are the side effects associated with glucocorticoids?
1. Diabetes 2. Cushing's 3. Osteoporosis 4. Impaired vertical bone growth in children 5. Secondary hyperparathyroidism 6. Steroid psychosis
77
Fludrocortisone * Indications
Hypoaldosteronism Presents with dehydration, hypotension, possibly hyperkalemia
78
Spironolactone * MOA * Indications
* MOA * minerolocorticoid receptor antagonist * Indications * hyperaldosteronism * edema, HTN, hypokalemia
79
Eplerenone * MOA * Indications
* MOA * minerolocorticoid receptor antagonist * Indications * hyperaldosteronism * edema, HTN, hypokalemia
80
ß2 agonists * MOA * Indications * Side effects
* MOA * increase cAMP * relax bronchial smooth mm * Indications * asthma * Side effects * tachycardia * hypotension Albuterol, terbutaline, pirbuterol, salmeterol
81
Ipratropium * MOA * Indications
* MOA * muscarinic receptor antagonist * Indications * asthma and COPD in patients who can't take ß2 agonists * taking MAOI * arrhythmia or angina
82
Tiotropium * MOA * Indications
* MOA * muscarinic receptor antagonist * Indications * asthma and COPD in patients who can't take ß2 agonists * taking MAOIs * arrhythmia or angina
83
Beclomethasone * MOA * Indications * Side effects
* MOA * glucocorticoid * suppresses inflammation * Indications * severe asthma attacks * Side effects * hoarse voice * oral candidiasis
84
Fluticasone * MOA * Indications * Side effects
* MOA * glucocorticoid * Indications * severe asthma attacks * Side effects * hoarse voice * oral candidiasis
85
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
86
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
87
Zileuton * MOA * Indications * Side effects
* MOA * 5-lipoxygenase inhibitor * Indications * prophylactic for mild asthma * Side effects * (slight elevation of liver enzymes)
88
Omalizumab * MOA * Indications
* MOA * IgG Ab that binds free IgE * blocks release of histamine and leukotrienes * decreased airway responsiveness * Indications * asthma
89
Combivent (Ipratropium/Albuterol) * Indication * Contraindication
* Indication: COPD * CON: soy allergy
90
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
91
Second Generation H1 Receptor Antagonists * Indications * Side effects
Loratadine, **Fexofenadine** **-adine** * MOA * does not cross into CNS * Indications * ​Allergic reaction * Side effects * minimal
92
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
93
Promethazine * MOA * Indications * Side effects
* MOA * first gen H1 histamine receptor blocker * Indications * allergies * motion sickness * Side effects * Sedation * anti-cholinergic effects
94
Triptans * MOA * Indications * Side Effects
* Types: Sumatriptan, Zolmitriptan * MOA * 5HT1 receptor agonist * 1B and 1D (vasoconstriction) * Indications * Acute migraine * Side Effects * Dry mouth * Paresthesia * Coronary artery spasm * arrythmia
95
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
96
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.
97
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)
98
What are side effects of acetylsalicylic acid?
1. Ulcers 2. Increased bleeding 3. Reyes (children with viral infection) 4. Hep tox 5. Tinnitis with toxicity
99
When is acetaminophen preferred over acetylsalicylic acid?
Patients with: 1. ulcers 2. anticoag meds/clotting disorder 3. gout 4. children with viral infection
100
Celecoxib * MOA * Indications * Side effects
* MOA * irreversibly inhibits COX-2 * thought to be upregulated at sites of inflammation only, protecting normal PG function * Indications * Rheumatoid arthritis * Osteoarthritis * Side effects * Allergic rxn to Sulfa
101
What drugs are used for the treatment of Rheumatoid arthritis?
1. Anti-neoplastic drugs 2. Etanercept (false TNF-alpha receptor) 3. TNF-alpha Ab * Infliximab * Adalimumab 4. Gold compounds 5. Celecoxib (inhibits COX-2 only)
102
Etanercept * MOA * Indications * Side effects
* MOA * false receptor for TNF-alpha * anti-inflammatory * Indications * Rheumatoid arthritis * autoimmune disease * Side effects * Injection site rxn
103
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)
104
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
105
What agents are used to treat gout?
1. NSAIDS 2. Glucocorticoids 3. Colchicine 4. Probenecid 5. Allopurinol 6. Rasburicase
106
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
107
Probenecid * MOA * Indications * Side effects
* MOA * decrease reabsorption of uric acid (increased excretion) * Indications * prevent further attacks of gout * Side effects * decreased renal function
108
Allopurinol * MOA * Indications
* MOA * decreased production of uric acid * inhibit xanthine oxidase (purine metabolism) * Indications * Prevent attacks of gout
109
Rasburicase * MOA * Indications * Side effects
* MOA * recombinant version of urate oxidase * catalyze conversion of uric acid to allantoin * increased excretion * Indications * Gout
110
Febuxostat * MOA * Indications * Side effects
* MOA * decreased production of uric acid * inhibit xanthine oxidase (purine metabolism) * Indications * Prevent attacks of gout
111
MOA of drugs in treatment of Gout: 1. Allopurinol 2. Febuxostat 3. Probenacid 4. Diuretics

Pharmacology (12 decks)

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