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What are examples of inhaled Short-acting Beta Agonists? (SABAs) - correct answer Albuterol and levabuterol
What is the MOA of inhaled beta agonists? - correct answer To relax airway smooth muscle by increasing cyclic cAMP; dilation and opening of airway
What is the use of inhaled beta agonists? - correct answer Used in bronchospasm associated with: asthma, bronchitis, and COPD
When are SABAs used (albuterol and levabuterol)? - correct answer For relief of ACUTE asthma attacks
Is albuterol approved in children under 4? - correct answer Yes.
How do beta-2 agonists affect calcium? - correct answer They open large conductions in calcium activated potassium channels = hyperpolarized airway smooth muscle cells
- decreased intracellular calcium
- increased potassium concentration
- decreased myocleynase activity = smooth muscle relaxation and bronchodilation
What are examples of long-acting beta agonists (LABAs)? - correct answer salmetrol and formoterol
What are LABAs (salmeterol and formoterol) used for? - correct answer Used for PREVENTION or long term treatment of asthma
NOT for acute attacks; not first line treatment
CANNOT be used alone
What population should LABAs NOT be prescribed in? - correct answer African Americans
What is special about the beta 2 adrenergic receptor gene? - correct answer This gene causes LABAs to worsen asthma control
Who is more likely to have the beta 2 adrenergic receptor gene? - correct answer African Americans; this genotype is present in 1/6th of the U.S. population
How does the beta 2 adrenergic receptor gene cause worsening asthma control when LABAs are taken? - correct answer Asthmatics with this gene are at risk for decreased airflow and worsening asthma control
What are adverse effects of inhaled beta agonists? - correct answer Tachycardia and tremors
What is the absorption of inhaled beta agonists? - correct answer Very little systemic absorption
What are examples of anticholinergics/antimuscarinics in maintenance therapy of COPD? - correct answer ipatroprium (Atrovent) and tiotroprium (Spiriva)
What is the MOA of anticholinergics (ipatroprium and tiotroprium)? - correct answer They block muscarinic receptors decreasing the formation of cAMP
CAUSES BRONCHODILATION BY:
- decreasing smooth muscle contraction of lungs (mainly on M3 receptors)
- decreases mucous secretion
What are ipatroprium and tiotroprium used for? - correct answer Maintenance of COPD
What is tiotroprium (Spiriva)? - correct answer LONG-ACTING bronchodilator for COPD; better absorbed from lung than ipatroprium (Atrovent)
What is ipotroprium (Atrovent)? - correct answer SHORT-ACTING bronchodilator for COPD
What bronchodilator is the best choice in patients taking propranolol? - correct answer Ipatroprium (Atrovent)
Should be taken twice a day, every day
What is the correct order of use of corticosteroid and bronchodilator? - correct answer BRONCHODILATOR should be used FIRST then inhaled corticosteroid
What are examples of mast cell stabilizers (inhaled anti-inflammatory agents)? - correct answer Cromolyn, nedocromil
What is the MOA of mast cell stabilizers? - correct answer Inhibits mast cell degranulation = prevents histamine release
=inhibits cough, decreases inflammatory process in lungs
Mast cell stabilizers do NOT have bronchodilator, antihistamine, or vasoconstrictor activity
What is mast cell stabilizers used for? - correct answer Long term control for asthma prophylaxis (not used much anymore)
What are examples of xanthine derivatives? - correct answer Theophylline, aminophylline, caffeine
What is xanthine derivatives used for? - correct answer Treatment of asthma
What is the MOA of xanthine derivatives? - correct answer Produces and increase in cAMP
= bronchial smooth muscle and pulmonary RELAXATION
What are side effects of xanthine derivatives? - correct answer Insomnia, excitability, increased heart rate, GI upset
What is special to know about xanthine derivatives? - correct answer They affect all body systems and theophylline lab values are necessary
(especially in patients with nausea, vomiting, and HA)
What are examples of leukotriene modifiers (leukotriene receptor antagonists)? - correct answer montelukast (Singulair), zafirlukast (Accolate)
What is the MOA of leukotriene antagonists? - correct answer Leukotrienes BLOCK the leukotrienes that have an important role in the inflammatory process (leukotrienes cause smooth muscle contraction, neutrophil aggregation, and chemotaxis)
What are adverse effects and patient education for leukotriene antagonists? - correct answer 1. Anxiety
- Depression
- Agression
- Suicidal thoughts
What is an example of a monoclonal antibody drug? - correct answer omalizumab (Zolair)
What is the use of omalizumab (Zolair)? - correct answer Used in moderate to severe asthma (subQ injection)
What is the MOA of omalizumab (Zolair) (monoclonal antibody)? - correct answer Limits the binding of IgE to receptors on the surface of mast cells and basophils
What are examples of intranasal corticosteroids? - correct answer mometasone (Nasonex), fluticasone (Flonase)
What is the use of intranasal corticosteroids? - correct answer Drug of choice in treatment of allergic rhinitis
Also used in asthma
What is the MOA of intranasal corticosteroids? - correct answer Anti- inflammatory -- they interrupt inflammation by inhibiting the synthesis of mediators
When are intranasal corticosteroids contraindicated? - correct answer Acute asthma attacks because there is NO relief of acute bronchospasm
- Well tolerated by GI
Much less SE than 1st generation
What is another name for antihistamines? - correct answer H1 antagonists
What is the use of H1 antagonists? - correct answer Allergic rhinitis, pruritus, urticaria, insomnia, N/V, cold symptoms
What is the MOA of H1 antagonists? - correct answer BLOCKS the action of HISTAMINE by binding to histamine receptors
How are H1 antagonists absorbed? - correct answer Well absorbed orally by CYP450 system
What should H1 antagonists not be used with? - correct answer other CNS depressants
How does diphenhydramine (Benadryl) affect children? - correct answer Paradoxical reactions found in children in which the drug has opposite effect causing excitation instead of sedation
What is the Pregnancy Category of diphenhydramine (Benadryl)? - correct answer Pregnancy Category B -- excreted in breastmilk
At what age is Benadryl not recommended? - correct answer In patients over 60 and under 6
On the BEERS list because of anticholinergic effects; treat those patients with 2nd generation antihistamine instead
What medications are to be avoided in men with BPH? - correct answer Meds for cold and allergies that contain decongestants (like Sudafed)
Watch urinary retention; antihistamines slow the flow of urine by preventing muscles in the bladder neck and prostate from relaxing
What are examples of oral and intranasal decongestants? - correct answer Oral - pseudoephedrine (Sudafed), phenylephrine
Nasal - oxymetazoline (Afrin)
What is the use of decongestants? - correct answer To relieve nasal congestion and improve Eustachian tube function (congestion in ears, not infection)
What is the MOA of decongestants? - correct answer Work by stimulating alpha receptors of vascular smooth muscle
= constricts dilated arterioles within nasal mucosa = decreased swelling and inflammation
mild CNS effects
What is the pharmacokinetics of decongestants? - correct answer Well absorbed and widely distributed = side effects
At what age should decongestants not be used? - correct answer In children under 4 (hydration and rest instead)
What should be used in patients with high BP and congestion instead of decongestants? - correct answer OTC chlorpheniramine or coricidin
What is an example of expectorants? - correct answer guafenesin (Robitussin, Mucinex)
What is the use of expectorants? - correct answer Management of COUGH associated with bronchitis, colds, and sinusitis
What is the MOA of expectorants? - correct answer Increases the output of the respiratory tract by decreasing adhesiveness and surface tension =
=changes a dry, non-productive cough into a productive cough (helps to remove phlegm from the lungs)
What are side effects of expectorants? - correct answer GI effects, HA
When should digoxin levels be monitored? - correct answer In patients taking albuterol
What is the Black Box Warning with LABAs? - correct answer Increased risk of asthma related deaths
How do diuretics work in HTN? - correct answer They act by diminishing sodium reabsorption at different sites in the nephron
= increased urinary sodium and water losses (to decrease BP)
What lab values should be checked when using diuretics? - correct answer KIDNEY FUNCTION should be assessed
What labs should be monitored with thiazide diuretics? - correct answer Must have GFR > mid 40mL/min and check BUN and creatinine
When and why are diuretics helpful? - correct answer Useful in edematous states and HTN because they induce negative fluid balance
What are example of Loop diuretics? - correct answer bumetanide (Bumex), furosemide (Lasix)
What is the site of action for loop diuretics? - correct answer Loop of Henle (Ascending limb)
What is the MOA of loop diuretics? - correct answer INHIBITS SODIUM REABSORPTION (doesn't let the sodium stay in the body)
=excretion of water and urine (pees out sodium and water bc water follow sodium)
How do loop diuretics affect electrolytes? - correct answer 1. Causes potassium loss
- Causes calcium loss (increased calcium excretion) -- can lead to risk of decreased bone density
Are loop diuretics potassium-sparing? - correct answer NO. Loop diuretics cause potassium loss into the urine
What are examples of thiazide diuretics? - correct answer chlorthalidone, hydrochlorithiazide, indapamide, metolazone
What is the site of action of thiazide diuretics? - correct answer Early distal convoluted tubule
What is the MOA of thiazide diuretics? - correct answer Inhibits the NaCl symporter
=retention of water and frequent urination is due to the increased loss of water (urine) that has not been retained by the body
What is the use of thiazide diuretics? - correct answer 1. Long term antihypertensive action by decreasing preload and blood pressure
- Short term effect - unknown vasodilator effect that decreases BP
How do thiazide diuretics affect electrolytes? - correct answer 1. Causes potassium loss
- Causes gain of calcium (increased calcium reabsorption)
Are thiazide diuretics potassium-sparing? - correct answer No. They cause potassium to be loss into the urine
What are examples of potassium-sparing diuretics? - correct answer spironolactone, eplerenone, amiloride
What is the site of action of potassium-sparing diuretics? - correct answer Late distal tubule collecting duct
What is special about potassium-sparing diuretics? - correct answer Potassium is RETAINED and not lost in the urine like other diuretics
What are examples of carbonic anhydrase inhibitors? - correct answer acetazolamide, methazolamide
When using mannitol (osmotic diuretic), what may increase blood glucose and urinatioN? - correct answer Use of stimulants
What is the MOA of carbonic anhydrase inhibitors? - correct answer inhibits the enzyme carbonic anhydrase which is found in the proximal convoluted tubules
causes bicarbonate accumulation in the urine and decreased sodium absorption
What is the use of carbonic anhydrase inhibitors? - correct answer Used in patients with edema and metabolic alkalosis who need to lose excess bicarbonate in the urine
What are examples of non-systemic antacids? - correct answer aluminum hydroxide, magnesium hydroxide, calcium carbonate (TUMS)
What is the use of antacids? - correct answer Treat symptoms of heartburn/acid reflux
What are antacids? - correct answer They are weak bases that react with hydrochloride to form salt and water
What is the MOA of antacids? - correct answer 1. Neutralize gastric acid
- Increase pH of stomach
- inhibits proteolytic activity of pepsin
- increase LES tone
What is a side effect of aluminum and calcium based antacids? - correct answer Diarrhea
What is a side effect of magnesium based antacids? - correct answer Constipation
What should you not take antacids with? - correct answer Food containing phosphorus (dairy)
How do antacids react with other drugs? - correct answer They react with many other drugs and can cause chelation
Take antacids two hours after other meds
ex: antibiotics
What can antacids cause? - correct answer Kidney stones (calcium)
What are examples of proton pump inhibitors? - correct answer omeprazole (Prilosec), esomeprazole (Nexium), iansoproazole (Prevacid 24hr)
What is the use of PPIs? - correct answer Treat hyperacidity: GERD, esophagitis, PUD, gastritis
What is the MOA of PPIs? - correct answer They are a prodrug
- decreases blood flow to stomach
- decreases pepsin secretion
- increases serum pepsinogen
decreased acid in the stomach aids in healing of ulcers and reduces pain from indigestion and heartburn
What does too little acid causes? - correct answer hypocholorida
What are stomach acids needed for? - correct answer To digest proteins, vitamin B12, calcium, and other nutrients
Why is the proton pump an ideal target for inhibiting acid secretion? - correct answer It is the terminal stage in gastric acid secretion being responsible for secreting hydrogen ions
Why are PPIs significantly more effective than H2 antagonists? - correct answer They reduce gastric acid secretion by up to 99%
=decreased total pepsin output
What is the doses of H2RAs? - correct answer 1. famitodine (Pecid): 40mg -- less active ingredient
- ranitidine (Zantac): 150mg -- better absorbed than famitodine, but requires more time to exert action
What is the metabolism of H2RAs? - correct answer Undergoes extensive first- pass metabolism
Why is cimetidine (Tagamet) much less used than the other H2RAs? - correct answer It inhibits CYP450 so it has a lot of drug interactions
When is the Step Down Approach for GERD used? - correct answer For rapid symptom relief for frequent or severe symptoms
What is the Step Down Approach for GERD? - correct answer 1. Begin with standard dose of PPI for 8 weeks
----if sx not resolved, PPI dose is doubled for another 4-8 weeks
- After 4 weeks, a lower dose of PPI is tried
- If no relief after 8 weeks of twice daily PPI, then refer to GI
What is the Goal of the Step Down Approach to GERD? - correct answer Step DOWN to the lowest PPI dose or transition to an H2RA if symptoms are not relieved
When is the Step Up Approach for GERD used? - correct answer Used for occasional symptoms or mild disease
What is the Step Up Approach to GERD? - correct answer 1. Begins with lifestyle changes and OTC antacids -- followed by H2RAs and PPIs
- If symptoms refractory after 4-8 weeks of treatment or if endoscopy shows erosive disease, then PPIs become central management
- PPI treatment: start as once daily and if symptoms continue, twice daily
What is an example of a pro kinetic drug (antiemetic)? - correct answer metoclopramide (Reglan)
What is the use of metoclopramide (Reglan)? - correct answer Management of GERD, diabetic gastroparesis, post-op and chemotherapy induced N/V
What is the MOA of metoclopramide (Reglan)? - correct answer Antiemetic activity due to its blocking action at the D2 receptors and chemoreceptor trigger zone in the CNS
=prevention of N/V triggered by most stimuli
What do higher doses of metoclopramide (Reglan) cause? - correct answer The 5HT3 antagonist may also contribute to antiemetic effects:
- Increased LES and force of gastric contractions
- Improves coordination of contractions
- Enhances gastric emptying
D2 receptor is a dopamine receptor
5HT3 is a serotonin receptor
What is an example of a Prostaglandin Antiulcerant? - correct answer misoprostol (Cytotec)
What is the use of misoprostol (Cytotec)? - correct answer Used to treat stomach ulcers
What is the MOA of sucralfate (Carafate)? - correct answer Binds electrostatic ally to positively charged proteins within the ulcer to form a BARRIER
Only 5% is absorbed systemically
What are drug interactions with sucralfate (Carafate)? - correct answer Chelates with other medications, like antacids
What is Triple Therapy for positive H. pylori PUD treatment? - correct answer 1. PPI twice daily
- Amoxicillin 1gram twice daily
- clarithromycin 500mg twice daily
treatment of all for 10-14 days (abx)
If there is a PCN allergy, can use metronidazole
How long should the PPI be used for positive H. pylori treatment? - correct answer Continue for 8-12 weeks until healing is complete
What is quadruple therapy for positive H. pylori PUD treatment? - correct answer 2nd line for patients who fail initial tx:
- PPI twice daily
- Metronidazole
- Tetracycline
- Bismuth subsalicylate for 14 days (Pepto-Bismal)
What antibiotics may show resistance of H. pylori eradication, especially in women? - correct answer Metronidazole and clarithromycin
What is the resistance related to clarithromycin? - correct answer 1. Highest in mid Atlantic and NE of US - 13%
- Older age
- Presence of inactive ulcer disease
What type of laxative is the safest? - correct answer Bulk-forming laxatives
What are examples of bulk-forming laxatives? - correct answer methylcellulose (Citrucel), psyllium (Metamucil)
What is the use of bulk-forming laxatives? - correct answer LONG-TERM management of chronic constipation and chronic watery diarrhea
What is the MOA of bulk-forming laxatives? - correct answer Produces peristalsis by producing mechanical DISTENTION, reduces transit time
What is the onset of action of bulk-forming laxatives? - correct answer 12 hours; NOT absorbed by GI tract
What are side effects of bulk-forming laxatives? - correct answer bloating and flatulence
What are drug interactions with bulk-forming laxatives? - correct answer DECREASES absorption of warfarin, ASA, and digoxin
When should you NOT use bulk-forming laxatives? - correct answer With impaction
What is another word for a surfactant? - correct answer Stool softener
What are examples of surfactants (stool softeners)? - correct answer docusate sodium (Colace, Correctol), docusate calcium, docusate potassium
What is the use of surfactants? - correct answer PREVENTS constipation
What is the MOA of surfactants? - correct answer Brings water and lipids INTO the stool
= decreased surface tension = softens stool
