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E2- Summary Flashcards

1
Q

What are the physiological effects of stimulation of the H1 receptor?

A 
Allergic response
Releases NO causing vasodilation
Wakefulness
Inhibits appetite
*Acts through Gq
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2
Q

What are the physiological effects of stimulation of the H2 receptor?

A

Gastric acid secretion
Vasodilation
*Acts through Gs, increases cAMP

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3
Q

What are the effects of histamine on the cardiovascular system?

A

Vasodilation, decreased BP, reflex tachycardia, increased capillary permeability, edema, swelling, hives

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4
Q

What are the effects of histamine on the lungs?

A

Bronchospasm (problematic in asthmatics)

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5
Q

What are the 1st generation antihistamines?

A

Diphenhydramine (Benadryl)
Dimenhydrinate (Dramamine)
Promethazine (Phenergan)

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6
Q

Do 1st generation or 2nd generation antihistamines enter the brain?

A

1st generation (main SE is sedation)

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7
Q

Which antihistamine is best used for sedation?

A

Diphenhydramine (Benadryl)

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8
Q

Which antihistamines are best used for motion sickness?

A

Diphenhydramine (Benadryl)

Dimenhydrinate (Dramamine)

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9
Q

What antihistamine is best used as an antiemetic?

A

Promethazine (Phenergan)

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10
Q

What are the SE of 1st generation antihistamines?

A 
Sedation 
Anticholinergic (dry mouth)
Decreased seizure threshold
GI
Possibly teratogenic
Allergic rxn (topical)
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11
Q

What type of drugs should you not combine with 1st generation antihistamines?

A

CNS depressants (alcohol, BZs)

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12
Q

What are the effects of 1st generation antihistamine OD?

A 
Sedation
Anticholinergic (fever, dry mouth, blurred vision, urinary retention, constipation, flushed, delusion)
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13
Q

What are the 2nd generation antihistamines?

A

Fexofenadine (Allegra)
Loratadine (Claritin)
Cetirizine (Zyrtec)

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14
Q

Which 2nd generation antihistamine is excreted by the kidneys?

A

Cetirizine (Zyrtec)

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15
Q

Which antihistamines are used for allergic rhinitis?

A 
Fexofenadine (Allegra)
Loratadine (Claritin)
Cetirizine (Zyrtec)
Azelastine
*Best when used prophylactically
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16
Q

What are SE of 2nd generation antihistamines?

A

GI
Possibly teratogenic
Allergic rxn (topical)

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17
Q

What inhibits the metabolism of 2nd generation antihistamines?

A

Cimetidine
Erythromycin
Ketoconazole
Grapefruit juice

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18
Q

What are the effects of 2st generation antihistamine OD?

A

Arrhythmias

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19
Q

Which antihistamine is a noncompetitive nasal H1 antagonist?

A

Azelastine

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20
Q

What 5 properties affect the pharmacokinetics of placenta exchange?

A 
Lipid solubility
Molecular size and pH
Placental transporters
Protein binding
Placental and fetal drug metabolism
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21
Q

Do non-ionized or ionized drugs cross the placenta more easily?

A

Non-ionized

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22
Q

What drug should always be given in pregnancy? Why?

A

Folic acid (Cat A) to prevent neural tube defects

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23
Q

Is any amount of alcohol safe in pregnany?

A

NO known level of alcohol is safe!

Leading preventable cause of intellectual disability

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24
Q

If a pregnant women requires anticoagulation therapy, should you give Warfarin or Heparin?

A

Heparin (does not cross the placenta-ionized)

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25
What drug may be used to tx nausea in pregnant women, but can cause damage to DNA through oxidative stress and cause limb deformities?
Thalidomide
26
What type of acne medication is strictly contraindicated in pregnancy and pts to enter iPLEDGE program, a negative pregnancy test, and 2 forms of BC before beginning therapy?
Isotretinoin
27
Which anticonvulsants are the best choice for pregancy?
Levetiracetam | Lamotrigine
28
Which anticonvulsant should NEVER be given in pregnancy?
Valproate
29
Which drug has associated male and female teratogenicity and occupation exposure risk due to aerosolized exposure?
Ribavirin
30
What is the MOA of Albuterol and Levalbuterol?
Short-acting B2 agonist (SABA)
31
What is DOC for stopping an asthma attack in progress?
Albuterol Levalbuterol *SABAs act immediately
32
What drugs are long-acting B2 agonist (LABA)?
Salmeterol/fluticasone Formoterol/momestasone Vilanterol/fluticasone *20 min for effect
33
What asthma drugs are used for prophylaxis and are supplied with a steroid?
LABAs Salmeterol/fluticasone Formoterol/momestasone Vilanterol/fluticasone
34
What are the SE of SABAs and LABAs?
``` Tachycardia Nervousness Dizziness Tremor *short-lived and tolerance devleops ```
35
What is the Blackbox warning associated with LABAs?
Increased risk of asthma-related death
36
What is the MOA of Ipratropium and Tiotropium?
Muscarinic antagonist
37
What are the uses for Ipratropium and Tiotropium?
COPD Used in combo with B2 agonist Used in pts intolerant of B2 agonist
38
What is the main SE of Ipratropium and Tiotropium?
Dry mouth
39
What is the main difference b/w Ipratropium and Tiotropium?
Tiotropium has a longer duration of action (only needs 1/day dosing)
40
What is the MOA of Theophylline (oral)?
Blocks adenosine receptors Increases cAMP Inhibits phosphodiesterase
41
What is Theophylline used for?
Asthma or COPD NOT controlled by B2 agonist or muscarinic antagonist *rarely used due to toxicities and low therapeutic index
42
What are SE of Theophylline? What can OD cause?
Nervousness Insomnia Decrease diaphragm fatigue OD = Fatal arrhythmias
43
What increases the clearance of Theophylline?
Phenytoin Smoking Rifampin Oral contraceptives
44
What decreases the clearance of Theophylline?
Cimetidine
45
What inhaled corticosteroid are used for the tx of asthma?
Fluticasone Beclomethasone Flunisolide
46
What are the effects of inhaled corticosteroids?
Decrease inflammation Reduced bronchial reactivity Improve response to B2 agonsit
47
What are SE of inhaled corticosteroids?
``` Oral candidiasis (thrush) Hoarseness ```
48
What is the MOA of Montelukast?
Leukotriene inhibitor
49
Which drug is used in the tx of asthma, especially due to exercise and/or cold air triggers?
Montelukast
50
What are SE of Montelukast?
URI Sore throat Sleepiness
51
What is the MOA of Omalizumab?
Monoclonal antibody to IgE
52
What is the use of Omalizumab?
mod/severe allergic asthma
53
What are SE of Omalizumab?
Rash | Injection site reaction
54
Which asthma drugs can decrease the need for steroids?
Montelukast | Omalizumab
55
What is the MOA of Cromolyn sodium?
Inhibits the release of histamine from mast cells (NOT a bronchodilator)
56
What is the use of Cromolyn sodium?
Asthma prophylaxis esp. in children | *Must be used several times a day chronically
57
What is the SE of Cromolyn sodium?
Bad taste
58
What is the MOA of Magnesium hydroxide and | Aluminum hydroxide? Why are they often combined?
Neutralize acid by directly binding to HCl Magnesium- diarrhea Aluminum- constipation
59
What is the MOA of Cimetidine and Ranitidine?
H2 Histamine Antagonist (decrease GI acid)
60
What are the uses of Cimetidine and Ranitidine?
Ulcers GERD adjunct Pre-anesthesia Severe allergic reaction (w/ H1 antagonist)
61
What are SE of Cimetidine?
Anti-testosterone effect Gynecomastia Loss of libido Impotence
62
What are drug interactions of Cimetidine?
Warfarin, phenytoin, theophylline, digoxin | Inhibits CYP3A4
63
What is the MOA of Omeprazole and Esomeprazole?
PPI | Activated in gastric parietal cells, irreversibly block acid formation
64
What is the DOC for GERD?
Omeprazole | Esomeprazole
65
What are SE of Omeprazole and Esomeprazole?
↓ Ca2+, Mg2+, Vit B absorption (risk of osteoporosis) Pneumonia C. diff
66
What is a drug interaction of Omeprazole?
Clopidogrel | Inhibits CYPC19
67
How should you take H2 receptor blockers? | How should you take PPIs?
H2 receptor blockers = night | PPIs = empty stomach
68
What is the MOA of Misoprostol? What is its major CI?
Prostaglandin E1 analogue | Pregnancy
69
What is the use of Misoprostol?
Prevention of NSAID-induced ulcers
70
What is the MOA of Metoclopramide?
D2 antagonist | increases ACh release
71
What is the main SE and CI of Metoclopramide?
SE: Parkinson's-like sx CI: pregnancy
72
What are the uses of Metoclopramide?
Gastric hypomotility | Antiemetic
73
What is the MOA of Bethanechol? | What are its SE?
Muscarinic agonist | GI cramping, diarrhea, salivation, sweating
74
What are the uses of Bethanechol?
Post-op ileus | ↑ LES tone
75
What can be used to tx diabetic gastroparesis?
Erythromycin (macrolide that stimulates motilin receptors)
76
What is the MOA of Dicyclomine? | What are its SE?
Muscarinic antagonist Dry mouth Sedation Constipation
77
What is Dicyclomine used for?
Intestinal overactivity, cramping, spasms
78
What is the MOA of Amitriptyline? | What are its SE?
Muscarinic antagonist and ↑ NE release Dry mouth Sedation Constipation
79
What are the uses of Amitriptyline?
IBS w/ diarrhea | Decreases pain
80
What is the MOA of Ondansetron?
Serotonin (5-HT3) antagonist
81
What drugs are classified as "anti-emetics?" (5)
``` Ondansetron Prochlorperazine Promethazine Dronabinol Aprepitant ```
82
What is the MOA of Prochlorperazine and | Promethazine?
Block DA, muscarinic, and H1 receptors
83
Which anti-emetics can also be used to tx motion sickness? | What is the their main SE?
Prochlorperazine and Promethazine Highly sedating
84
What is the MOA of Aprepitant?
NK1 antagonist
85
What osmotic laxative can be used for bowel prep or OTC occasional constipation?
Polyethylene glycol
86
What is the use of Lactulose?
Cirrhosis to ↓ ammonia levels | *can be used chronically
87
Which drugs can be used chronically for the tx of constipation?
Lubiprostone | Linaclotide
88
What is the MOA of Lubiprostone?
PG E1 analogue | Activates CIC-2 Cl- channels in luminal cells to ↑ fluid secretion
89
What is the MOA of Linaclotide?
Activates guanylate cyclase C in lumen | ↑ cGMP activates CFT, ↑ Cl- and fluid into the lumen
90
What is used to treat IBS with constipation?
Linaclotide
91
What is an opioid analogue that decreases peristalsis used to tx diarrhea?
Loperamide
92
What are the CI to Loperamide?
Infections Ulcerative colitis Recovering addicts
93
What is used to tx Ulcerative colitis?
Sulfasalazine
94
What is used to tx bloating and flatulence?
Simethicone (anti-inflammatory)
95
What is the CI to Sulfasalazine?
Children (Reyes)
96
Prostaglandins are synthesized from ___ through the ___ pathway?
Arachidonic acid Cyclooxygenase pathway
97
What are the effects of COX-1?
Activates thromboxane which is a vasoconstrictor and promoter of platelet aggregation
98
What are the effects of COX-2?
Activates prostacyclin which is a vasodilator and inhibitor of platelet aggregation
99
What is the MOA of Acetylsalicylic acid/ASA/Aspirin?
Nonselective, irreversible inhibitor of COX-1 and COX-2
100
What is the pharmacokinetics of Acetylsalicylic acid/ASA/Aspirin elimination?
Low doses = 1st order kinetics | High doses = zero order kinetics
101
How is Acetylsalicylic acid/ASA/Aspirin excreted?
Renal excretion (alk of urine promotes excretion- absorption ↓ by antacids)
102
How does Acetylsalicylic acid/ASA/Aspirin effect uric acid excretion?
Low doses = ↓ uric acid excretion | High doses = ↑ uric acid excretion
103
How does Acetylsalicylic acid/ASA/Aspirin effect the respiratory system?
Low doses = respiratory alkalosis | High hoses = metabolic and respiratory acidosis
104
What are the indications for Acetylsalicylic acid/ASA/Aspirin?
Anti-inflammatory Analgesic Antipyretic Anti-platelet
105
What are SE of Acetylsalicylic acid/ASA/Aspirin?
GI upset, gastritis, ulcer, bleeding Renal damage ↑ bleeding time Aspirin asthma (↑ leukotrienes)
106
What are CI of Acetylsalicylic acid/ASA/Aspirin?
``` Children Gastric ulcer Bleeding disorders Vitamin K deficiency Severe hepatic damage Hypersensitivity to ASA or salicylates Gout ```
107
Why is Acetylsalicylic acid/ASA/Aspirin CI in children? | How do you treat this SE?
Reye’s Syndrome | DOC = acetaminophen
108
What are the indications for NSAIDs?
Analgesia Antipyretic Anti-inflammatory
109
What is the MOA of Celecoxib?
Specific reversible inhibitor of COX-2
110
What is a benefit of Celecoxib? What is a risk?
Benefit- less GI effects than other NSAIDs | Risk- increased risk of CV disease
111
What drugs are classified as nonspecific reversible inhibitors of COX-1 and COX-2?
``` Indomethacin Diclofenac Ketorolac Ibuprofen Naproxen Piroxicam/Meloxicam ```
112
What can be used to tx patent ductus arteriosus?
Indomethacin
113
What drug can be combined with misoprostol to decrease GI SE?
Diclofenac
114
What drug can be used as an analgesic for post surgical pain? What is the caveat?
Ketorolac | Must be d/c after 5 days due to GI SE
115
What is the 1st line choice of NSAID?
Ibuprofen (lower incidence of SE)
116
Which NSAID has the longest half-life? | What are its associated drug interactions?
Naproxen | Anticoagulants, hypoglycemics
117
What are SE of NSAIDs?
``` GI (pain, bleeding, ulcers, pancreatitis, diarrhea) HA, dizziness, confusion, depression Bronchoconstriction Agranulocytosis, aplastic anemia Nephrotoxicity/Hepatotoxicity Hypersensitivity reactions ```
118
Which NSAID is the worst but most potent?
Indomethacin
119
What are indications for acetaminophen?
Analgesia | Antipyretic
120
What is the effect of acetaminophen OD?
Fetal hepatic necrosis, encephalopathy, coma, death
121
What is the pathophysiology of acetaminophen OD?
Dose dependent free radical production exceeds the available reduced glutathione
122
What can increase acetaminophen toxicity?
Chronic alcohol consumption
123
How do you tx acetaminophen toxicity?
IV N-acetylcysteine
124
If pt has no hx of PUD, what analgesics can they use?
Any NSAID
125
If pt has PUD hx, but no active PUD, what analgesics can they use?
Celecoxib +/- antacids | NSAIDs + misoprostol or PPIs (“-prazols”)
126
If pt has active PUD, what analgesics can they use?
Acetaminophen
127
What are the uses of Penicillamine?
RA | Wilson’s disease
128
What are SE of Hydroxychloroquine sulfate?
Hemolysis (G6PD def), ototoxicity, retinopathy
129
What DMARD is just as effective as Penicillamine but better tolerated?
Sulfasalazine
130
What are SE of Sulfasalazine?
GI disturbances, hepatitis, blood dyscrasias | monitor for hepatitis and marrow suppression
131
What is the MOA of Infliximab?
Chimeric IgG1k monoclonal antibody targeting TNFα
132
What are the uses of Infliximab?
RA | Crohn's disease
133
What is the MOA of Adalimumab?
100% human IgG1 monoclonal antibody targeting TNFα
134
What is the use of Adalimumab?
RA (monotherapy)
135
What is the MOA of Certolizumab pegol and Golimumab?
Bumanized antibody targeting TNFα
136
What is the MOA of Etanercept?
Dimeric fusion protein that inhibits TNFα
137
What are CI of Etanercept? (7)
``` Bone marrow suppression Breastfeeding Children DM Infection/sepsis Vaccination Varicella ```
138
What is the MOA of Rituximab?
Blocks B-cells differentiation
139
What are the uses of Rituximab?
RA | Non-Hodgkin Lymphoma
140
What is the MOA of Abatacept?
Blocks T-cell activation
141
What is the MOA of Leflunomide?
Inhibits DHODH, pyrimidine synthesis, and COX-2 | inhibits nucleic acid syn
142
What are CI of Leflunomide?
Pregnancy Breastfeeding Hepatic/renal failure
143
What is the MOA of Micophenolate mofetil?
Inhibits purine synthesis by blocking the enzyme IMPDH (inhibits nucleic acid syn)
144
What is the MOA of Anakinra?
Human interleukin-1 receptor antagonist (IL-1Ra)
145
What is the MOA of Tocilizumab?
Human interleukin-6 receptor antagonist (IL-6)
146
What is the MOA of Tofacitinib?
Inhibits JAK1 and JAK3
147
What us the use of Tofacitinib?
Mod/severe RA with inadequate response/intolerance to Methotrexate
148
What are SE of Tofacitinib?
Serious infections and malignancy
149
What is the MOA of Baricitinib?
Inhibits JAK1 and JAK2
150
What are the uses of Baricitinib?
Mod/severe RA (mono therapy or combo with Methotrexate)
151
What can be used in for acute gout management?
Indomethacin, Naproxen, or Celecoxib | Colchicine
152
What is the MOA of Colchicine?
Binds to tubulin inhibiting the assembly of microtubules
153
What is the effect of Colchicine?
Anti-inflammatory (inhibit leukocyte migration and phagocytosis)
154
What is the main SE of Colchicine?
Diarrhea
155
Which analgesics are contraindicated in the tx of gout?
ASA, salicylates (↓ urate excretion)
156
Which drugs can be used in chronic gout management?
Probenecid Allopurinol/Febuxostat Rasburicase/Regloticase Lesinurad
157
What is the MOA of Probenecid?
Increase excretion of uric acid by blocking the reabsorption of uric acid in the PT
158
Which drugs used in the chronic management of gout should always initially be given with Colchicine to prevent a gouty attack?
Probenecid | Allopurinol/Febuxostat
159
What is a drug interaction of Probenecid?
Penicillin
160
What is the MAO of a Allopurinol and Febuxostat?
Inhibit synthesis of uric acid by inhibiting xanthine oxidase
161
What are drug interactions of Allopurinol and Febuxostat?
Mercaptopurines (increases effects/toxicity) | Fluorouracil (inhibits effect)
162
What is the MAO of Rasburicase and Pegloticase?
Recombinant form of urate oxidase, catalyzes oxidation of uric acid into to allantoin (readily excreted metabolite)
163
What are SE of Rasburicase and Pegloticase?
Bypersensitivity rxn, anaphylactic shock (non-endogenous in humans)
164
What is the MOA of Lesinurad?
URAT inhibitor
165
What is the blackbox warning associated with Lesinurad?
Risk of acute renal failure = should always be used in combo with xanthine oxidase inhibitor (Allopurinol, Febuxostat)
166
What can be used in the symptomatic tx of migraines?
Sumatriptan Ergotamine Dihydroergotamine (IV) Aspirin, Acetaminophen, Naproxen, Propoxyphene
167
What is the MOA of Sumatriptan?
5-HT1D agonist on intracranial vessels (vasoconstriction)
168
What are SE of Sumatriptan?
``` Cardiac (arrhythmias, angina, MI, cardiac arrest, stroke) Hemorrhage Seizures PVD GI ```
169
What is the MOA of Ergotamine?
5-HT agonist (less specific than Sumatriptan, more extensive SE)
170
What is unique about the pharmacokinetics of Ergotamine?
Best if taken early in migraine onset | Caffeine increases absorption
171
What is used to treat migraine pain?
Aspirin, Acetaminophen, Naproxen, Propoxyphene
172
What can be used as prophylactic tx of migraines?
``` Propranolol (B-blocker) Verapamil (CCB) Amitriptyline, Fluoxetine (Antidepressants) Clonidine Valproate, Topiramate (Anticonvulsants) Botulinum Toxin ACE-I, ARBs Erenumab ```
173
What is the MOA of Erenumab?
IgG2 monoclonal antibody that binds CGRP

Pharmacology 3 (10 decks)

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