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Pharm Sci Exam 2

Terms in this set (139)

Seasonal "Hay Fever" causes.
Pollen from trees, grasses, and weeds
Persistent "Hay Fever" causes
Mold, dust mites, and animal dander
Comorbid disorders from "Hay Fever",
Asthma, rhinosinusitis, allergic conjunctivitis, and sleep apnea
Histamine release process. (4 steps)
1. Exposure to antigen.
2. B-cells synthesize IgE which binds to Fce receptors on mast cells.
3. Second exposure to antigen causes cross-linking of IgE, triggering degranulation
4.Histamine releases, producing inflammation
What are the four classes of medication used to treat inflammation?
1. Antihistamines
2. Intranasal steroids
3. Leukotreine receptor antagonists
4. Mast cell degranulation inhibitors
Histamine (agonist) has preferential activity for the ______ site.
active
Inverse agonists (antihistamine has preferential activity for the ________ site.
inactive
What are the signaling mechanisms for the H1 receptor?
Gq, increased IP3, and DAG
What are the signaling mechanisms for the H2 receptor?
Gs, and increased cAMP
What are the signaling mechanisms for the H3 receptor?
Gi, and decreased cAMP
What are the signaling mechanisms for the H4 receptor?
Gi, and decreased cAMP
H1 receptors are expressed in what tissues?
Smooth muscle, endothelium, and the brain
H2 receptors are expressed in what tissues?
Gastric mucosa, cardiac muscle, mast cells, and the brain
H3 receptors are expressed in what tissues?
Presynaptic autoreceptors and heteroreceptors: brain, myenteric plexus, and other neurons
H4 receptors are expressed in what tissues?
Eosinophils, neutrophils, mast cells, CD4 T cells
What is the clinical response of the H1 receptor?
Pain, itching, tachycardia, hives, etc.
What is the clinical response of the H2 receptor?
Gastric acid secretion.
What is the clinical response of the H3 receptor?
Wakefulness
What is the recently approved H3-antagonist indicated for narcolepsy?
Pitolisant (Wakix)
What are the three enthanolamine antihistamines?
1. Carbinoxamine (Clistin) - Slight to moderate sedation
2. Dimenhydrinate (Dramamine) - Strong sedation; anti-motion sickness activity
3. Diphenhydramine (Benadryl) - Strong sedation; anti-motion sickness activity
What are the three piperazine derivative antihistamines?
1. Hydroxyzine (Atarax) - Strong sedation
2. Cyclizine (Marezine) - Slight sedation; anti-motion sickness activity
3. Meclizine (Bonine) - Slight sedation; anti-motion sickness
What are the two alkylamine antihistamines?
1. Brompheniramine (Dimetane, etc.) - Slight sedation
2. Chlorpheniramine (Chlor-Trimeton, etc.) - Slight sedation
What is the phenothiazine derivative antihistamine?
Promethazine (Phenergan) - Strong sedation; antiemetic
What is the miscellaneous antihistamine?
Cyproheptadine (Periactin, etc) - Moderate sedation
What is the piperidine 2nd generation antihistamine?
Fexofenadine (Allegra)
What are the two miscellaneous 2nd generation antihistamines?
1. Loratadine (Claritin)
2. Cetirizine (Zyrtec)
Dimenhydrinate (Dramamine) and diphenhydramine (Benadryl) both have significant _______________ activity.
anticholinergic
Cyclizine (Marezine) and meclizine (Bonine) act on _________ receptors.
histamine
Promethazine (Phenergan) exerts its antiemetic activity by action on ________ and __________ receptors.
dopamine; muscarinic
What is the primary indication of brompheniramine (Dimetane) and chlorpheniramine(Chlor-Trimeton)?
Allergic reactions ( allergic rhinitis/hay fever)
What is the primary indication of the second generation H1 "antagonists"?
Chronic urticaria (hives)
What is the primary indication of dimenhydrinate(Dramamine) and promethazine(Phenergan)?
Motion sickness (promethazine is also indicated for allergic treatment and sedation)
What are common adverse effects of H1 antagonists?
Sedation, anticholinergic effects (dry mouth, constipation, urinary retention, etc.)
T/F. Antihistamines have excellent oral bioavailability.
True
T/F. Antihistamines have a relatively slow absorption. (long half-life)
False
T/F. Second generation antihistamine typically have longer half-lives then the first generation antihistamines.
True
Second generation antihistamines do not enter the CNS, mainly because they are substrates for the _-____________ transporter in the BBB.
p-glycoprotein
T/F. Wakix (pitolisant), an H3 antagonist that was recently approved for daytime sleepiness associated with narcolepsy, has a very high abuse potential.
False
What are three condition that lead to acid-peptic disease?
1. Gastroesophageal reflux
2. Peptic ulcer
3. Stress-related mucosal injury
What are the two therapeutic approaches to treating gastrointestinal diseases?
1. Drugs that reduce intragastric acidity
2. Drugs that promote mucosal defense
What are six steps leading to acid release mediated by histamine?
1. ECL cells are stimulated to release histamine by gastrin and acetylcholine
2. Histamine binds to H2 receptors on the parietal cell
3. Adenylyl cyclase is activated
4. cAMP increases
5. Protein kinase is activated
6. Acid secretion is stimulated by the H+/K+-ATPase
What are the four H2 blockers?
1. Cimetidine (Tagamet)
2. Famotidine (Pepcid)
3. Nizatidine (Axid)
4. Ranitidine (Zantac) - recalled due to impurity
T/F. The H2 blockers are rapidly absorbed.
True
T/F. H2 blocker dose does not have to be reduced in patients with renal dysfunction.
False
In patients taking multiple medication, cimetidine (Tagamet) should not be prescribed because it is a ____ enzyme inhibitor.
P450
What are some adverse effects of H2 blockers?
1. Diarrhea, headaches, fatigue, constipation.
2. Nosocomial pneumonia in critically ill patients
T/F. H2 blockers are safe to use in women who are pregnant or breastfeeding.
False
What are the two classes of medications that can relax bronchiole smooth muscle?
1. Beta-2 agonists
2. Muscarinic antagonists (M3)
Regarding the stepwise approach for management of asthma, what medication(s) is preferred for step 1 of treatment?
PRN SaBa
Regarding the stepwise approach for management of asthma, what medication(s) is preferred for step 2 of treatment?
1. Daily low-dose ICS and PRN SaBa
or
2. PRN concomitant ICS and SaBa
Regarding the stepwise approach for management of asthma, what medication(s) is preferred for step 3 of treatment?
Daily and PRN combination low-dose ICS-formoterol
Regarding the stepwise approach for management of asthma, what medication(s) is preferred for step 4 of treatment?
Daily and PRN combination medium-dose ICS-formoterol
Regarding the stepwise approach for management of asthma, what medication(s) is preferred for step 5 of treatment?
Daily medium-high dose ICS-LaBa + LaMa and PRN SaBa
Regarding the stepwise approach for management of asthma, what medication(s) is preferred for step 6 of treatment?
Daily high-dose ICS-LaBa + oral systematic corticosteroids + PRN SaBa
Regarding the stepwise approach for management of asthma, what are the ALTERNATIVE medications for step 2 of treatment? (2)
1. Daily LTRA and PRN SaBa
2. Nedocromil or Zileuton and PRN SaBa
Regarding the stepwise approach for management of asthma, what are the ALTERNATIVE medications for step 3 of treatment? (3)
1. Daily medium-dose ICS and PRN SaBa
2. Daily low-dose ICS-LaBa, or daily low-dose ICS + LaMa, or daily low-dose ICS + LTRA, and PRN SaBa
3. Daily low-dose ICS + theophylline (Theo-24) or Zileuton and PRN SaBa
Regarding the stepwise approach for management of asthma, what are the ALTERNATIVE medications for step 4 of treatment? (2)
1. Daily medium-dose ICS-LaBa or daily medium-dose ICS + LaMa, and PRN SaBa
2. Daily medium-dose ICS + LTRA, or daily medium-dose ICS + theophylline (Theo-24), or daily medium-dose ICS + Zileuton, and PRN SaBa
Regarding the stepwise approach for management of asthma, what are the ALTERNATIVE medications for step 5 of treatment? (1)
Daily medium-high dose ICS-LaBa or daily high-dose ICS + LTRA, and PRN SaBa
What are the short-acting beta-agonists (SaBa)? (2)
1. (Lev)Albuterol
2. Terbutaline
What are the long-acting beta-agonists (LaBa)? (5)
1. (Ar)formoterol
2. Salmeterol
3. Indacaterol
4. Vilanterol
5. Olodaterol
What are the glucocorticoids? (6)
1. Beclomethasone
2. Triamcinolone
3. Fluticasone
4. Mometasone
5. Budesonide
6. Flunisolide
What are the leukotriene agents? (3)
1. Montelukast
2. Zafirlukast
3. Zileuton
What are the anti-cholinergics/LAMAs? (5)
1. Ipratropoium
2. Tiotropium
3. Umeclidinium
4. Aclidinium
5. Glycopyrrolate
Regarding beta-2 agonists, what is beneficial about newer agonists?
They are 200x-400x more selective for beta-2 vs beta-1 receptors. (reducing cardiac events)
Beta-2 agonists work by causing relaxation of the ___________ smooth muscle.
bronchiolar
Beta-2 agonists _________(increase/decrease) mast cell degranulation and _________(increase/decrease) release of inflammatory cytokines.
decrease; decrease
What class of medications are mostly used for "rescue" inhalers?
SaBas (albuterol and levalbuterol)
LaBas are recommended to be taken with what class of medication to reduce asthma-related deaths?
inhaled corticosteroids (ICS)
What are some adverse effects of beta-2 agonists? (3)
1. Tremor
2. Tachycardia
3. Cardiac arrythmias
T/F. Zileuton (Zyflo) requires liver function tests due to its hepatotoxicity.
True
What two leukotriene pathway inhibitors are dosed twice daily?
1. Zileuton
2. Zafirlukast
Which leukotriene pathway inhibitor has a response rate of only 40-60%
Montelukast
How does anti-IgE monoclonal antibody omalizumab (Xolair) work?
It binds the FceR1 binding domain of the IgE, preventing IgE from binding to mast cells and antigen presenting cells.
What is normal dose of omalizumab (Xolair)?
300mg SC injection every 2 to 4 weeks
What is IL-5?
IL-5 is an inflammatory cytokine that is released from mast cells and promotes eosinophil migration to the site of inflammation.
What are the dosages of the three anti-IL-5 drugs, mepolizumab (Nucala), reslizumab (Cinquair), and beneralizumab (Fasenra)?
1. Mepolizumab - 100mg SC every 4 weeks
2. Reslizumab - 3mg/kg IV infusions every 4 weeks
Beneralizumab - 30mg/dose SQ every 4 weeks, then once every 8 weeks.
What is the anti-IL-4 drug and what is it's dosage?
Dupilumab (Dupixent) - 400mg-600mg initially, then 200mg-300mg SQ every other week; patient can learn to administer themselves
What about their structure, compared to other anticholinergics, makes ipratropium and tiotropium better treatments for COPD and asthma?
They have a quaternary amine which allows for trapping in the lungs.
What are the four strategies to treat peptic ulcer?
1. Promoting healing
2. Reducing acid secretion
3. Enhancing the mucosal defense
4. Neutralizing gastric acid
What are some of the commonly prescribed medication to treat peptic ulcers associated with H. pylori?
1. Amoxicillin or metronidazole
2. Clarithromycin or tetracycline
3. Bismuth (optional)
4. PPI or H2RA
What is the mechanism of action for PPIs?
PPIs are activated by acid and then bind irreversibly to the H+/K+ATPase on the gastric lumen side of the parietal cell. These agents stay bound until new enzyme is made by the parietal cell.
What are three reasons that PPIs are sometimes referred to as "ideal drugs"?
1. Short half-life but long duration of action
2. Very selective for the proton pump
3. Concentrated at site of action
Why should PPIs be administered 1 hour before food?
Food decreases bioavailability of PPIs by about 50%.
What are some adverse events associated with long-term PPI use?
1. Vitamin B12 deficiency which can lead to pernicious anemia
2. Decreased calcium absorption which can lead to osteoporosis-related fractures
3. Atrophic gastritis, a precursor to gastric cancer
What are the three agents used to enhance mucosal defense for use in treating diseases associated with gastric acid hypersecretion?
1.Misoprostol (Cytotec)
2. Bismuth compounds (Kaopectate, Pepto)
3. Sucralfate (Carafate)
What are three ways prostaglandins enhance mucosal defense?
1. Increasing blood flow to the area. which reduces the acidity
2. Enhancing mucous and bicarbonate production
3. Reducing acid secretion
Which prostaglandin is indicated for NSAID-induced ulcer prophylaxis?
Misoprstol
What is the major implication of aluminum-containing antacids?
Constipation
What is the major implication of magnesium-containing antacids?
Laxative
What is the major implication of calcium-containing antacids?
May cause acid rebound
What is the major implication of carbonate-containing antacids?
Releases CO2 which can lead to bloating, belching, and flatulence
What is the mechanism of action of the D2 antagonist, metoclopramide?
It blocks D2 receptors in the chemoreceptor trigger zone to relieve N/V. Increases lower esophageal sphincter tone and enhances gastric emptying.
What is the Rome IV diagnostic criteria for IBS?
Recurrent abdominal pain, on average, at least 1 day/week in the last 3 months, associated with two or more of the following criteria:
1. Related to defecation
2. Associated with a change in frequency of stool
3. Associated with a change in form (appearance) of stool
What are four treatments for IBS-D?
1. Anti-diarrheals
2. Anticholinergics
3. Tricyclic antidepressants
4. Antibiotics (Rifaximin)
What are three opioid agents used for diarrhea?
1. Loperamide (Imodium)
2. Diphenoxylate/atropine (Lomotil)
3. Eluxadoline (Viberzi)
Loperamide (Imodium) is an agonist at __ ______ receptors.
mu opiate
T/F. Loperamide (Imodium) may act directly on GI smooth muscle to decrease longitudinal and circular muscle tone and decrease propulsive movements.
True
What is the life-threatening condition associated with Imodium overuse in patients with ulcerative colitis (UC)?
Toxic megacolon
T/F. Eluxadoline (Viberzi) is indicated for IBS-D as well as common diarrhea
False, Viberzi is indicated for IBS-D only
What are the primary muscarinic receptor antagonists? (3)
1. Dicyclomine
2. L-hyoscyamine
3. Glycopyrrolate
What is the major difference between the two muscarinic receptor antagonists, l-hyoscyamine and dicyclomine?
Onset of action
L-hyoscyamine onset of action: 5-20 minutes
Dicyclomine onset of action: 60-90 minutes
T/F. The antibiotic commonly prescribed for traveler's diarrhea and IBS-D, rifaximin (Xifaxan), may reduce small intestine bacterial overgrowth (SIBO).
True
Vomiting is a complex behavior that consists of what three things?
1. Pre-ejection phase
2. Retching
3. Ejection
The vomiting center receives input from what 4 regions of the brain?
1. Chemoreceptor Trigger Zone (CTZ)
2. Vestibular System (inner ear)
3. Vagal afferents from GI tract to CTZ and vomiting center
4. Descending tracts from the CNS
Benzodiazepines are useful for treating ____________ vomiting or vomiting caused by _______.
anticipatory; anxiety
What are the four 5-HT3 receptor antagonists?
1.Ondansetron
2.Dolasetron
3.Graniseton
4.Palonosetron
What is the 5-HT3 receptor?
The 5-HT3 receptor is a ligand-gated channel that is found on extrinsic peripheral vagal afferent neurons in the GI tract; they also play a role in GI motility.
What are the indications of 5-HT3 receptor antagonists?
1. Ondansetron- chemo-induced N/V, postoperative N/V, and radiotherapy-associated N/V
2. Palonosetron- Chemo-induced N/V, and postoperative N/V
3. Granisetron- Prevention of chemo-induced N/V
4. Dolasetron- Prevention of chemo-induced N/V
What rare but serious adverse effects is associated with 5-HT3 receptor antagonist use?
QT prolongation
What 5-HT3 receptor antagonist requires dosing adjustment in liver disease?
Ondansetron
What are the three common NK-1 receptor antagonists?
1. Aprepitant
2. Rolapitant
3. Netupitant
What are the two cannabinoids used for N/V?
1. Dronaninol (Marinol)
2. Nabilone (Cesamet)
Lubiprostone, linaclotide, and plecanatide are _________ agents.
secretory
What are the indications for lubiprostone, linaclotide, and plecanatide?
1. Luibiprostone(Amitiza)- IBS-C(women only) and chronic idiopathic constipation(CIC)
2. Linaclotide(Linzess)- IBS-C and CIC
3. Plecanatide(Trulance)- IBS-C and CIC
What is the mechanism of action of prucalopride(Motegrity)?
Prucalopride is a selective 5HT4 receptor agonist that can activate 5-HT4 receptors that reside on IPAN cells that release Ach onto enteric nerves. Enteric nerve activation elevates GI motility throughout the GI tract.
What are the three peripherally acting mu receptor antagonists (PAMORAs) used in opioid-induced constipation?
1. Methylnaltrexone
2. Bromide
3. Naloxegol
What would be the best choice of H2 antagonist for an 85 year-old patient suffering from GERD?
Famotidine (Pepcid) or nizatidine (Axid) are suitable for use in older patients.
What are the roles of acetylcholine and gastrin in the release of histamine from ECL cells?
Gastrin and Ach stimulates ECL cells stimulates the release of histamine.
What is an off-label use of diphenhydramine(Benadryl) and promethazine(Phenergan)?
Diphenhydramine and promethazine are also sodium channel blockers and can function as local anasthetics.
Which of the following agents, famotidine, calcium carbonate, or omeprazole, would be most likely to increase a patients' risk for opportunistic infections such as pneumonia?
Omeprazole has the greatest effect on gastric pH leading to the greatest chance for bacteria to grow.
What pharmacokinetic features of montelukast make it more desirable than either zileuton or zafirlukast?
It can be taken once daily as well as less drug-drug interactions.
What class of drugs might provide the most benefit in aspirin-sensitivity asthma (ASA)?
Leukotriene pathway inhibitors
What agent is particularly beneficial in patients with IBS that have associated small intestine bacterial overgrowth?
Rifaximin will reduce small intestine bacterial overgrowth.
What drug is safer to take for a women who is pregnant or lactating, lubiprostone or misoprostol?
Lubiprostone is a safer choice because it has very little systematic absorption. Misoprostol is systematically absorbed and is considered an abortifacient.
Which nausea agents are available is a transdermal patch?
Granisetron (Sancuso)
What shuts off gastrin release?
Somatostatin
What signs/symptoms do you look for when considering peptic ulcer disease?
1. Abdominal pain
2. Burning pain
3. Heartburn
What are some risk factors for peptic ulcer disease?
1. NSAID use
2. Alcohol use
3. Smoking
4. PMH of ulcers
When the protective role of prostaglandins is lost, what will happen to the stomach lining?
Stomach ulcers
Why are PPIs formulated in acid resistant enteric coated capsules if they work in the stomach?
We want them to reach the blood, not break down in the GI tract.
What is the only PPI approved for stress-related gastritis?
Omeprazole immediate release with NaHCO3 (Zegerid)
Why is omeprazole formulated with NaHCO3 (Zegerid)?
The NaHCO3 neutralizes stomach acid which increases absorption of omeprazole.
In what patients should you use Zegerid (omeprazole w/ NaCHO3) with caution?
CKD patients as well as patients with HF/HTN
What is a potential problem of ingesting bismuth salicylates with a bleeding ulcer?
They can have an anti-inflammatory/blood-thinning effect which will increase bleeding.
Do subcitrate or salicylate salts have more adverse effects?
Salicylate salts
T/F. Sucralfate is often prescribed as monotherapy.
False
What antacids often cause costipation?
1. Aluminum hydroxide
2. Calcium carbonate
Why is promoting motility important in GERD?
The longer food stays in your stomach, the more acid is produced.
What effects do acetylcholine mediate in the GI tract?
Acetylcholine increase lower esophageal tone by hitting D2 receptors.
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