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Pharmacology 3 > E2- Summary > Flashcards

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
Q

What drug may be used to tx nausea in pregnant women, but can cause damage to DNA through oxidative stress and cause limb deformities?

A

Thalidomide

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26
Q

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?

A

Isotretinoin

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27
Q

Which anticonvulsants are the best choice for pregancy?

A

Levetiracetam

Lamotrigine

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28
Q

Which anticonvulsant should NEVER be given in pregnancy?

A

Valproate

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29
Q

Which drug has associated male and female teratogenicity and occupation exposure risk due to aerosolized exposure?

A

Ribavirin

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30
Q

What is the MOA of Albuterol and Levalbuterol?

A

Short-acting B2 agonist (SABA)

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31
Q

What is DOC for stopping an asthma attack in progress?

A

Albuterol
Levalbuterol
*SABAs act immediately

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32
Q

What drugs are long-acting B2 agonist (LABA)?

A

Salmeterol/fluticasone
Formoterol/momestasone
Vilanterol/fluticasone
*20 min for effect

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33
Q

What asthma drugs are used for prophylaxis and are supplied with a steroid?

A

LABAs
Salmeterol/fluticasone
Formoterol/momestasone
Vilanterol/fluticasone

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34
Q

What are the SE of SABAs and LABAs?

A 
Tachycardia
Nervousness
Dizziness
Tremor
*short-lived and tolerance devleops
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35
Q

What is the Blackbox warning associated with LABAs?

A

Increased risk of asthma-related death

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36
Q

What is the MOA of Ipratropium and Tiotropium?

A

Muscarinic antagonist

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37
Q

What are the uses for Ipratropium and Tiotropium?

A

COPD
Used in combo with B2 agonist
Used in pts intolerant of B2 agonist

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38
Q

What is the main SE of Ipratropium and Tiotropium?

A

Dry mouth

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39
Q

What is the main difference b/w Ipratropium and Tiotropium?

A

Tiotropium has a longer duration of action (only needs 1/day dosing)

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40
Q

What is the MOA of Theophylline (oral)?

A

Blocks adenosine receptors
Increases cAMP
Inhibits phosphodiesterase

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41
Q

What is Theophylline used for?

A

Asthma or COPD NOT controlled by B2 agonist or muscarinic antagonist
*rarely used due to toxicities and low therapeutic index

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42
Q

What are SE of Theophylline? What can OD cause?

A

Nervousness
Insomnia
Decrease diaphragm fatigue
OD = Fatal arrhythmias

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43
Q

What increases the clearance of Theophylline?

A

Phenytoin
Smoking
Rifampin
Oral contraceptives

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44
Q

What decreases the clearance of Theophylline?

A

Cimetidine

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45
Q

What inhaled corticosteroid are used for the tx of asthma?

A

Fluticasone
Beclomethasone
Flunisolide

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46
Q

What are the effects of inhaled corticosteroids?

A

Decrease inflammation
Reduced bronchial reactivity
Improve response to B2 agonsit

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47
Q

What are SE of inhaled corticosteroids?

A 
Oral candidiasis (thrush)
Hoarseness
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48
Q

What is the MOA of Montelukast?

A

Leukotriene inhibitor

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49
Q

Which drug is used in the tx of asthma, especially due to exercise and/or cold air triggers?

A

Montelukast

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50
Q

What are SE of Montelukast?

A

URI
Sore throat
Sleepiness

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51
Q

What is the MOA of Omalizumab?

A

Monoclonal antibody to IgE

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52
Q

What is the use of Omalizumab?

A

mod/severe allergic asthma

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53
Q

What are SE of Omalizumab?

A

Rash

Injection site reaction

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54
Q

Which asthma drugs can decrease the need for steroids?

A

Montelukast

Omalizumab

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55
Q

What is the MOA of Cromolyn sodium?

A

Inhibits the release of histamine from mast cells (NOT a bronchodilator)

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56
Q

What is the use of Cromolyn sodium?

A

Asthma prophylaxis esp. in children

*Must be used several times a day chronically

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57
Q

What is the SE of Cromolyn sodium?

A

Bad taste

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58
Q

What is the MOA of Magnesium hydroxide and

Aluminum hydroxide? Why are they often combined?

A

Neutralize acid by directly binding to HCl
Magnesium- diarrhea
Aluminum- constipation

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59
Q

What is the MOA of Cimetidine and Ranitidine?

A

H2 Histamine Antagonist (decrease GI acid)

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60
Q

What are the uses of Cimetidine and Ranitidine?

A

Ulcers
GERD adjunct
Pre-anesthesia
Severe allergic reaction (w/ H1 antagonist)

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61
Q

What are SE of Cimetidine?

A

Anti-testosterone effect
Gynecomastia
Loss of libido
Impotence

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62
Q

What are drug interactions of Cimetidine?

A

Warfarin, phenytoin, theophylline, digoxin

Inhibits CYP3A4

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63
Q

What is the MOA of Omeprazole and Esomeprazole?

A

PPI

Activated in gastric parietal cells, irreversibly block acid formation

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64
Q

What is the DOC for GERD?

A

Omeprazole

Esomeprazole

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65
Q

What are SE of Omeprazole and Esomeprazole?

A

↓ Ca2+, Mg2+, Vit B absorption (risk of osteoporosis)
Pneumonia
C. diff

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66
Q

What is a drug interaction of Omeprazole?

A

Clopidogrel

Inhibits CYPC19

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67
Q

How should you take H2 receptor blockers?

How should you take PPIs?

A

H2 receptor blockers = night

PPIs = empty stomach

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68
Q

What is the MOA of Misoprostol? What is its major CI?

A

Prostaglandin E1 analogue

Pregnancy

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69
Q

What is the use of Misoprostol?

A

Prevention of NSAID-induced ulcers

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70
Q

What is the MOA of Metoclopramide?

A

D2 antagonist

increases ACh release

71
Q

What is the main SE and CI of Metoclopramide?

A

SE: Parkinson’s-like sx
CI: pregnancy

72
Q

What are the uses of Metoclopramide?

A

Gastric hypomotility

Antiemetic

73
Q

What is the MOA of Bethanechol?

What are its SE?

A

Muscarinic agonist

GI cramping, diarrhea, salivation, sweating

74
Q

What are the uses of Bethanechol?

A

Post-op ileus

↑ LES tone

75
Q

What can be used to tx diabetic gastroparesis?

A

Erythromycin (macrolide that stimulates motilin receptors)

76
Q

What is the MOA of Dicyclomine?

What are its SE?

A

Muscarinic antagonist
Dry mouth
Sedation
Constipation

77
Q

What is Dicyclomine used for?

A

Intestinal overactivity, cramping, spasms

78
Q

What is the MOA of Amitriptyline?

What are its SE?

A

Muscarinic antagonist and ↑ NE release
Dry mouth
Sedation
Constipation

79
Q

What are the uses of Amitriptyline?

A

IBS w/ diarrhea

Decreases pain

80
Q

What is the MOA of Ondansetron?

A

Serotonin (5-HT3) antagonist

81
Q

What drugs are classified as “anti-emetics?” (5)

A 
Ondansetron
Prochlorperazine
Promethazine
Dronabinol
Aprepitant
82
Q

What is the MOA of Prochlorperazine and

Promethazine?

A

Block DA, muscarinic, and H1 receptors

83
Q

Which anti-emetics can also be used to tx motion sickness?

What is the their main SE?

A

Prochlorperazine and
Promethazine
Highly sedating

84
Q

What is the MOA of Aprepitant?

A

NK1 antagonist

85
Q

What osmotic laxative can be used for bowel prep or OTC occasional constipation?

A

Polyethylene glycol

86
Q

What is the use of Lactulose?

A

Cirrhosis to ↓ ammonia levels

*can be used chronically

87
Q

Which drugs can be used chronically for the tx of constipation?

A

Lubiprostone

Linaclotide

88
Q

What is the MOA of Lubiprostone?

A

PG E1 analogue

Activates CIC-2 Cl- channels in luminal cells to ↑ fluid secretion

89
Q

What is the MOA of Linaclotide?

A

Activates guanylate cyclase C in lumen

↑ cGMP activates CFT, ↑ Cl- and fluid into the lumen

90
Q

What is used to treat IBS with constipation?

A

Linaclotide

91
Q

What is an opioid analogue that decreases peristalsis used to tx diarrhea?

A

Loperamide

92
Q

What are the CI to Loperamide?

A

Infections
Ulcerative colitis
Recovering addicts

93
Q

What is used to tx Ulcerative colitis?

A

Sulfasalazine

94
Q

What is used to tx bloating and flatulence?

A

Simethicone (anti-inflammatory)

95
Q

What is the CI to Sulfasalazine?

A

Children (Reyes)

96
Q

Prostaglandins are synthesized from ___ through the ___ pathway?

A

Arachidonic acid Cyclooxygenase pathway

97
Q

What are the effects of COX-1?

A

Activates thromboxane which is a vasoconstrictor and promoter of platelet aggregation

98
Q

What are the effects of COX-2?

A

Activates prostacyclin which is a vasodilator and inhibitor of platelet aggregation

99
Q

What is the MOA of Acetylsalicylic acid/ASA/Aspirin?

A

Nonselective, irreversible inhibitor of COX-1 and COX-2

100
Q

What is the pharmacokinetics of Acetylsalicylic acid/ASA/Aspirin elimination?

A

Low doses = 1st order kinetics

High doses = zero order kinetics

101
Q

How is Acetylsalicylic acid/ASA/Aspirin excreted?

A

Renal excretion (alk of urine promotes excretion- absorption ↓ by antacids)

102
Q

How does Acetylsalicylic acid/ASA/Aspirin effect uric acid excretion?

A

Low doses = ↓ uric acid excretion

High doses = ↑ uric acid excretion

103
Q

How does Acetylsalicylic acid/ASA/Aspirin effect the respiratory system?

A

Low doses = respiratory alkalosis

High hoses = metabolic and respiratory acidosis

104
Q

What are the indications for Acetylsalicylic acid/ASA/Aspirin?

A

Anti-inflammatory
Analgesic
Antipyretic
Anti-platelet

105
Q

What are SE of Acetylsalicylic acid/ASA/Aspirin?

A

GI upset, gastritis, ulcer, bleeding
Renal damage
↑ bleeding time
Aspirin asthma (↑ leukotrienes)

106
Q

What are CI of Acetylsalicylic acid/ASA/Aspirin?

A 
Children
Gastric ulcer
Bleeding disorders
Vitamin K deficiency
Severe hepatic damage 
Hypersensitivity to ASA or salicylates
Gout
107
Q

Why is Acetylsalicylic acid/ASA/Aspirin CI in children?

How do you treat this SE?

A

Reye’s Syndrome

DOC = acetaminophen

108
Q

What are the indications for NSAIDs?

A

Analgesia
Antipyretic
Anti-inflammatory

109
Q

What is the MOA of Celecoxib?

A

Specific reversible inhibitor of COX-2

110
Q

What is a benefit of Celecoxib? What is a risk?

A

Benefit- less GI effects than other NSAIDs

Risk- increased risk of CV disease

111
Q

What drugs are classified as nonspecific reversible inhibitors of COX-1 and COX-2?

A 
Indomethacin
Diclofenac
Ketorolac
Ibuprofen
Naproxen
Piroxicam/Meloxicam
112
Q

What can be used to tx patent ductus arteriosus?

A

Indomethacin

113
Q

What drug can be combined with misoprostol to decrease GI SE?

A

Diclofenac

114
Q

What drug can be used as an analgesic for post surgical pain?
What is the caveat?

A

Ketorolac

Must be d/c after 5 days due to GI SE

115
Q

What is the 1st line choice of NSAID?

A

Ibuprofen (lower incidence of SE)

116
Q

Which NSAID has the longest half-life?

What are its associated drug interactions?

A

Naproxen

Anticoagulants, hypoglycemics

117
Q

What are SE of NSAIDs?

A 
GI  (pain, bleeding, ulcers, pancreatitis, diarrhea)
HA, dizziness, confusion, depression
Bronchoconstriction
Agranulocytosis, aplastic anemia
Nephrotoxicity/Hepatotoxicity
Hypersensitivity reactions
118
Q

Which NSAID is the worst but most potent?

A

Indomethacin

119
Q

What are indications for acetaminophen?

A

Analgesia

Antipyretic

120
Q

What is the effect of acetaminophen OD?

A

Fetal hepatic necrosis, encephalopathy, coma, death

121
Q

What is the pathophysiology of acetaminophen OD?

A

Dose dependent free radical production exceeds the available reduced glutathione

122
Q

What can increase acetaminophen toxicity?

A

Chronic alcohol consumption

123
Q

How do you tx acetaminophen toxicity?

A

IV N-acetylcysteine

124
Q

If pt has no hx of PUD, what analgesics can they use?

A

Any NSAID

125
Q

If pt has PUD hx, but no active PUD, what analgesics can they use?

A

Celecoxib +/- antacids

NSAIDs + misoprostol or PPIs (“-prazols”)

126
Q

If pt has active PUD, what analgesics can they use?

A

Acetaminophen

127
Q

What are the uses of Penicillamine?

A

RA

Wilson’s disease

128
Q

What are SE of Hydroxychloroquine sulfate?

A

Hemolysis (G6PD def), ototoxicity, retinopathy

129
Q

What DMARD is just as effective as Penicillamine but better tolerated?

A

Sulfasalazine

130
Q

What are SE of Sulfasalazine?

A

GI disturbances, hepatitis, blood dyscrasias

monitor for hepatitis and marrow suppression

131
Q

What is the MOA of Infliximab?

A

Chimeric IgG1k monoclonal antibody targeting TNFα

132
Q

What are the uses of Infliximab?

A

RA

Crohn’s disease

133
Q

What is the MOA of Adalimumab?

A

100% human IgG1 monoclonal antibody targeting TNFα

134
Q

What is the use of Adalimumab?

A

RA (monotherapy)

135
Q

What is the MOA of Certolizumab pegol and Golimumab?

A

Bumanized antibody targeting TNFα

136
Q

What is the MOA of Etanercept?

A

Dimeric fusion protein that inhibits TNFα

137
Q

What are CI of Etanercept? (7)

A 
Bone marrow suppression
Breastfeeding
Children
DM
Infection/sepsis
Vaccination
Varicella
138
Q

What is the MOA of Rituximab?

A

Blocks B-cells differentiation

139
Q

What are the uses of Rituximab?

A

RA

Non-Hodgkin Lymphoma

140
Q

What is the MOA of Abatacept?

A

Blocks T-cell activation

141
Q

What is the MOA of Leflunomide?

A

Inhibits DHODH, pyrimidine synthesis, and COX-2

inhibits nucleic acid syn

142
Q

What are CI of Leflunomide?

A

Pregnancy
Breastfeeding
Hepatic/renal failure

143
Q

What is the MOA of Micophenolate mofetil?

A

Inhibits purine synthesis by blocking the enzyme IMPDH (inhibits nucleic acid syn)

144
Q

What is the MOA of Anakinra?

A

Human interleukin-1 receptor antagonist (IL-1Ra)

145
Q

What is the MOA of Tocilizumab?

A

Human interleukin-6 receptor antagonist (IL-6)

146
Q

What is the MOA of Tofacitinib?

A

Inhibits JAK1 and JAK3

147
Q

What us the use of Tofacitinib?

A

Mod/severe RA with inadequate response/intolerance to Methotrexate

148
Q

What are SE of Tofacitinib?

A

Serious infections and malignancy

149
Q

What is the MOA of Baricitinib?

A

Inhibits JAK1 and JAK2

150
Q

What are the uses of Baricitinib?

A

Mod/severe RA (mono therapy or combo with Methotrexate)

151
Q

What can be used in for acute gout management?

A

Indomethacin, Naproxen, or Celecoxib

Colchicine

152
Q

What is the MOA of Colchicine?

A

Binds to tubulin inhibiting the assembly of microtubules

153
Q

What is the effect of Colchicine?

A

Anti-inflammatory (inhibit leukocyte migration and phagocytosis)

154
Q

What is the main SE of Colchicine?

A

Diarrhea

155
Q

Which analgesics are contraindicated in the tx of gout?

A

ASA, salicylates (↓ urate excretion)

156
Q

Which drugs can be used in chronic gout management?

A

Probenecid
Allopurinol/Febuxostat
Rasburicase/Regloticase
Lesinurad

157
Q

What is the MOA of Probenecid?

A

Increase excretion of uric acid by blocking the reabsorption of uric acid in the PT

158
Q

Which drugs used in the chronic management of gout should always initially be given with Colchicine to prevent a gouty attack?

A

Probenecid

Allopurinol/Febuxostat

159
Q

What is a drug interaction of Probenecid?

A

Penicillin

160
Q

What is the MAO of a Allopurinol and Febuxostat?

A

Inhibit synthesis of uric acid by inhibiting xanthine oxidase

161
Q

What are drug interactions of Allopurinol and Febuxostat?

A

Mercaptopurines (increases effects/toxicity)

Fluorouracil (inhibits effect)

162
Q

What is the MAO of Rasburicase and Pegloticase?

A

Recombinant form of urate oxidase, catalyzes oxidation of uric acid into to allantoin (readily excreted metabolite)

163
Q

What are SE of Rasburicase and Pegloticase?

A

Bypersensitivity rxn, anaphylactic shock (non-endogenous in humans)

164
Q

What is the MOA of Lesinurad?

A

URAT inhibitor

165
Q

What is the blackbox warning associated with Lesinurad?

A

Risk of acute renal failure = should always be used in combo with xanthine oxidase inhibitor (Allopurinol, Febuxostat)

166
Q

What can be used in the symptomatic tx of migraines?

A

Sumatriptan
Ergotamine
Dihydroergotamine (IV)
Aspirin, Acetaminophen, Naproxen, Propoxyphene

167
Q

What is the MOA of Sumatriptan?

A

5-HT1D agonist on intracranial vessels (vasoconstriction)

168
Q

What are SE of Sumatriptan?

A 
Cardiac (arrhythmias, angina, MI, cardiac arrest, stroke)
Hemorrhage
Seizures
PVD
GI
169
Q

What is the MOA of Ergotamine?

A

5-HT agonist (less specific than Sumatriptan, more extensive SE)

170
Q

What is unique about the pharmacokinetics of Ergotamine?

A

Best if taken early in migraine onset

Caffeine increases absorption

171
Q

What is used to treat migraine pain?

A

Aspirin, Acetaminophen, Naproxen, Propoxyphene

172
Q

What can be used as prophylactic tx of migraines?

A 
Propranolol (B-blocker) 
Verapamil (CCB)
Amitriptyline, Fluoxetine (Antidepressants)
Clonidine
Valproate, Topiramate (Anticonvulsants)
Botulinum Toxin
ACE-I, ARBs
Erenumab
173
Q

What is the MOA of Erenumab?

A

IgG2 monoclonal antibody that binds CGRP

Pharmacology 3 (10 decks)

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