Pulmonary Pharmacology Hit List Flashcards Preview

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Flashcards in Pulmonary Pharmacology Hit List Deck (295):
1

Asthma & COPD
Epinephrine
Class

Bronchodilators

2

Asthma & COPD
Epinephrine
Mechanism

Adrenergic agonists – Non-specific
Increase cAMP, some inhibitory effect on mast cells, some inhibitory effect on microvascular permeability, promote a small degree of mucociliary transport

3

Asthma & COPD
Epinephrine
Route/Time

30-90 min duration; mist form

4

Asthma & COPD
Epinephrine
Adverse Rxns:

N/V, headache, fall in BP, increase HR, cardiac arrhythmias, PaO2 may decrease, CNS toxicities

5

Asthma & COPD
Albuterol
Class

Bronchodilators

6

Asthma & COPD
Albuterol
Mechanism

Adrenergic agonists – B2 specific, quick onset, short acting.
Rescue medication

7

Asthma & COPD
Albuterol
Route/Time

Quick onset, 3-6 hour duration

8

Asthma & COPD
Salmeterol
Class

Bronchodilators

9

Asthma & COPD
Salmeterol
Mechanism

Adrenergic agonists – B2 specific, slow onset, long-acting.

10

Asthma & COPD
Salmeterol
Route/Time

Long-acting used in combination w/ corticosteroids
12+ hour duration

11

Asthma & COPD
Formoterol
Class

Bronchodilators

12

Asthma & COPD
Formoterol
Mechanism

Adrenergic agonists – B2 specific, slow onset, long-acting

13

Asthma & COPD
Formoterol
Route/Time

Long-acting used in combination w/ corticosteroids
12+ hour duration

14

Asthma & COPD
Ipratropium
Class

Bronchodilators

15

Asthma & COPD
Ipratropium
Mechanism

Cholinergic Antagonists / Anti-muscarinics
Reduces airway constriction, decrease in mucous secretion, enhance B2 mediated dilation, can cause pupillary dilation and cycloplegia on contact

16

Asthma & COPD
Theophylline
Class

Bronchodilators & Anti-Inflammatory

17

Asthma & COPD
Theophylline
Mechanism

Methlxanthines (related to caffeine)
Increases cAMP, blocks muscle adenosine receptors, causes bronchodilation, anti-inflammatory; increases CNS activity, increases gastric acid secretion, has a weak diuretic effect

18

Asthma & COPD
Theophylline
Adverse Rxns:
Dose: 5-10ug/m

5-10ug/ml can cause N/V, nervousness, headache, insomnia

19

Asthma & COPD
Theophylline
Adverse Rxns:
Dose: greater than 20 ug/mL

Serum levels greater than 20 ug/mL cause vomiting, hypokalemia, hyperglycemia, tachycardia, cardiac arrhythmias, tremor, neuromuscular irritability, seizures

20

Asthma & COPD
Cromolyn sodium
Class

Anti-inflammatory

21

Asthma & COPD
Cromolyn sodium
Mechanism

May alter the activity of chloride channels, inhibit degranulation of mast cells in the lung, inhibit inflammatory response by acting on eosinophils, inhibit cough by action on airway nerve, reduce bronchial hyperactivity associated w/ exercise and antigen-inhaled asthma

22

Asthma & COPD
Cromolyn sodium
Adverse Rxns:

Unpleasant taste, no systemic toxicity, irritation of trachea, rarely – chest pain, restlessness, hypotension, arrhythmias, NV, CNS depression, seizures, anorexia

23

Asthma & COPD
Beclomethasone
Class

Corticosteroid

24

Asthma & COPD
Prednisolone
Class

Corticosteroid

25

Asthma & COPD
Monteleukast
Class

Leukotriene Receptor Blocker – Anti-inflammatory

26

Asthma & COPD
Monteleukast
Mechanism

LTD4 activation  bronchial hyper-reactivity, bronchoconstriction, mucosal edema, increased mucus secretion

27

Asthma & COPD
Monteleukast
Effective in some patients

To reduce aspirin-related asthma

28

Asthma & COPD
Monteleukast
Adverse Rxns:

GIT, laryngitis, pharyngitis, nausea, otitis, sinusitis, viral infections

29

Asthma & COPD
Monteleukast
Unusual Adverse Rxn:

Possible association w/ suicide ideation
High doses tumorigenic in rodents

30

Asthma & COPD
Zileuton
Class

Leukotriene Synthesis Blocker – Anti-inflammatory

31

Asthma & COPD
Zileuton
Mechanism

Inhibits leukotriene formation, decreases smooth muscle contraction and blood vessel permeability, reduces leukocytes migration to damaged areas.

32

Asthma & COPD
Zileuton
Adverse Rxn:

Causes hepatic enzyme elevation – LFTs required

33

Asthma & COPD
Zileuton
Interactions:

CYP1A2 interaction w/ theophylline; evaluation for other inflammation-related diseases

34

Asthma & COPD
Omalizumab
Class

Anti-IgE antibody

35

Asthma & COPD
Omalizumab
Mechanism

Binds to IgE and prevents release of inflammatory mediators  decreases allergic response
Reduces the frequency & severity of asthma attacks

36

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Cyclophosphamide
Class

Alkylating agent

37

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Cyclophosphamide
Mechanism

Produces B & T cell lymphopenia, suppression of B cell activity and decreased Ig secretion; associated with neutron- thrombocytopenia, bladder cancer, myeloproliferative malignancie s

38

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Cyclophosphamide
Adverse Rxn:

Hemorrhagic cystitis is a frequent complication, but this is prevented by adequate fluid intake and mesna.
Can cause diarrhea.

39

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Ambrisentan
Class

Endothlin-1 Receptor Antagonist

40

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Ambrisentan
Mechanism

Blocks smooth muscle proliferation and pulmonary artery vasoconstriction by binding to endothliun-1 type A (smooth muscle) and type B (endothelial cells)

41

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Ambrisentan
Route

Orally active

42

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Ambrisentan
Black Box Warning

Teratogenic (category X)

43

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Beractant
Class

Exogenous surfactant

44

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Beractant
Mechanism/Target

Administered to preterm (<30 weeks) infants to reduce pulmonary surface tension; purified animal-derived products rich in surfactant proteins B, and C, neutral lipids, surface active PLs, and DPPC (primary surface active component)

45

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Epoprostenol
Class

Prostanoid for PAH

46

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Epoprostenol
Mechanism

Prostanoids induce pulmonary artery vasodilation, retard smooth muscle growth and disrupt platelet aggregation.

47

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Epoprostenol
Route/Time

Half life of 3-5 minutes, requires continuous IV infusion

48

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Epoprostenol
Dose limiting

Hypotension, muscle pains, headache, flushing

49

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Tadalafil
Class

Phosphodieterase type 5 inhibitors

50

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Tadalafil
Treatment

Tx of benign prostatic hypertension and erectile dysfunction

51

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Tadalafil
Side effect

Headache is most common side effect

52

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Tadalafil
Time

Halflife 17 hours

53

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Tadalafil
Unusual Adverse Rxn

Change in color vision due to non-arteritic anterior ischemic optic neuropathy (NAION)

54

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Methotrexate
Class

Immunosuppressent

55

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Methotrexate
Mechanism

DHFR inhibition, additional actions that increase adenosine-mediated immunosuppression (increase in cAMP)

56

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Methotrexate
Treatment

Tx for sarcoidosis (non-caseating granulomas)

57

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Methotrexate
Significant side effects

– NOT a front-line therapy
High-dose intravenous methotrexate chemotherapy acute kidney failure and severe and life-threatening CNS toxicity.

58

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Iloprost
Class

Prostanoid for PAH

59

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Iloprost
Mechanism

Prostanoids induce pulmonary artery vasodilation, retard smooth muscle growth and disrupt platelet aggregation

60


Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Iloprost
Time

Halflife of 25 minutes, requires 6-9 inhaled doses/ day (10 min per dose)

61

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Iloprost
Side effects

Cough, flushing, headache are common, hypotension, muscle cramps, bleeding, reports of hemoptysis

62

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Diltiazem
Class

Calcium Channel Blocker (CCB)

63

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Diltiazem
Mechanism

CCB – prevent membrane depolarization, block the key mediator of smooth muscle contraction allowing vasodilation to endure; not all patients respond to these drugs, some develop hemodynamic decompensation

64

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Diltiazem
Time/Route

Halflife 3-6 h, PO TID

65

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Diltiazem
Side effects

CYP3A4
Bradycardia, headache, edema, hypotension

66

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Rituximab
Class

mAb against CD20 on B cells

67

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Rituximab
Mechanism

mAb that binds CD20 on M cell precursors and mature B cells) Depletion lasts 6-9 months (depletion via 2 mechanisms: ACDC, complement mediated  MAC, induction of apoptosis)

68

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Rituximab
Can cause

HTN, asthenia, pruritis, urticarial, rhinitis, arthralgia

69

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Rituximab
Treatment

tx for Wegener’s granulomatosis

70

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Treprostinil
Class

Prostanoid for PAH

71

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Treprostinil
Mechanism

Prostanoids induce pulmonary artery vasodilation, retard smooth muscle growth and disrupt platelet aggregation

72

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Treprostinil
Route/Time

Halflife of 4 hours, continuous SC or IV infusion

73

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Treprostinil
Injection site rxns;

Headache, nausea, diarrhea, vasodilation, jaw pain,

74

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Treprostinil
Monitor

monitor for bleeding, decreased clearance w/ gemfibrozil

75

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Azathioprine
Class

Facilitates apoptosis of T cell populations

76

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Azathioprine
Mechanism

DNA, RNA synthesis inhibitor

77

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Azathioprine
Associated

associated w/ neoplastic, mutagenic, and leukopenic & thrombocytopenic toxicity; increases the risk of infection

78

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Bosentan
Class

Endothlin-1 Receptor Antagonist

79

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Bosentan
Mechanism

Blocks smooth muscle proliferation and pulmonary artery vasoconstriction by binding to endothliun-1 type A (smooth muscle) and type B (endothelial cells)

80

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Bosentan
Route/Time

Orally active
5-8 hours; PO BID

81

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Bosentan
BBW/Side effects

Teratogenic (category X)
Liver and blood toxicities
Significantly elevated LFTs, anemia, naopharyngitis, interactions w/ CYP2C9 and 3A4 substrates; leading cause of drug-drug interactions

82

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Amlodipine
Class

Calcium Channel Blockers (CCB)

83

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Amlodipine
Mechanism

CCB – prevent membrane depolarization, block the key mediator of smooth muscle contraction allowing vasodilation to endure;

84

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Amlodipine
Time

Halflife 35-50 hours

85

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Amlodipine
Adverse Rxn

Not all patients respond to these drugs, some develop hemodynamic decompensation

86

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Amlodipine
Side effects

CYP3A4
Edema, fatigue, hypotension

87

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Verapamil
Class

Calcium Channel Blockers (CCB)

88

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Verapamil
Mechanism

CCB – prevent membrane depolarization, block the key mediator of smooth muscle contraction allowing vasodilation to endure

89

Drugs for Restrictive Lung Diseases
& Pulmonary Artery Hypertension
Verapamil
Side effects

Headaches, facial flushing, dizziness, lightheadedness, swelling, increased urination, fatigue, nausea, ecchymosis, galactorrhea, and constipation

90

Diphenhydramine
Class

Antihistamines
1st generation
Antitussive
Ether/ Ethanolamine derivative

91

Diphenhydramine
Mechanism

Based on structure of histamine – short lived, multiple dosing, H1 blockade.
Antihistamine-H1 antagonist, suppresses cough by action on the respiratory center due to its anticholinergic effect

92

Diphenhydramine
Side effects

Side Effects – drowsiness, respiratory distress, blurred vision, dry mouth, urinary retention

93

Diphenhydramine
Time

Duration 4-6 hours

94

Dimenhydrinate
Class

Antihistamines
1st generation
Ether/ Ethanolamine derivative

95

Dimenhydrinate
Mechanism

Based on structure of histamine – short lived, multiple dosing, H1 blockade

96

Dimenhydrinate
Side effects

Highly sedative, anticholinergic side effects
Sedative
Anticholinergic
GI
Can potentiate nasal congestion

97

Dimenhydrinate
Time

Duration 4-6 hours

98

Chlorpheniramine
Class

Antihistamines
1st generation
Alklamine

99

Chlorpheniramine
Mechanism

Based on structure of histamine – short lived, multiple dosing, H1 blockade

100

Chlorpheniramine
Side effects

Highly sedative, anticholinergic side effects
Sedative
Anticholinergic
GI
Can potentiate nasal congestion

101

Chlorpheniramine
Time

Duration 4-6 hours

102

Hydroxyzine
Class

Antihistamines
1st generation
Piperzine derivative – much longer duration: 4-24 hours

103

Hydroxyzine
Mechanism

Based on structure of histamine – short lived, multiple dosing, H1 blockade

104

Hydroxyzine
Side effects

Highly sedative, anticholinergic side effects
Sedative
Anticholinergic
GI
Can potentiate nasal congestion

105

Hydroxyzine
Time

Much longer duration: 4-24 hours

106

Fexofenadine
Class

Antihistamines
2nd generation

107

Fexofenadine
Mechanism

Divergent structures, different from histamine, longer therapeutic doses,interactions H1 blockade
Anti-asthmatic

108

Fexofenadine
Side effects

Limited or nonsedating, enhanced safety profiles (cardiac arrhythmias, drug-drug
Has only mild cognitive disturbances
-adine
-stine

109

Fexofenadine
Time

Duration 8-24 hours

110


Desloratadine
Class

Antihistamines
2nd generation

111

Desloratadine
Mechanism

14-7x greater binding to H1 receptors than loratadine
15-50 fold lower affinity for muscarinic receptors compared w/ H1 receptors

112

Desloratadine
Side effects

Limited or nonsedating, enhanced safety profiles (cardiac arrhythmias, drug-drug
Has only mild cognitive disturbances
-adine
-stine

113

Desloratadine
Time

Long elimination halflife = 27 hours

114

Cetirizine
Class

Antihistamines
2nd generation

115

Cetirizine
Mechanism

Divergent structures, different from histamine, longer therapeutic doses,interactions H1 blockade
Anti-asthmatic

116

Cetirizine
Side effects

Limited or nonsedating, enhanced safety profiles (cardiac arrhythmias, drug-drug
Has only mild cognitive disturbances
-adine
-stine

117

Cetirizine
Time

Duration 8-24 hours

118

Azelastine
Class

Antihistamines
2nd generation

119

Azelastine
Mechanism

Divergent structures, different from histamine, longer therapeutic doses,interactions H1 blockade
Anti-asthmatic

120

Azelastine
Side effects

Limited or nonsedating, enhanced safety profiles (cardiac arrhythmias, drug-drug
Has only mild cognitive disturbances
-adine
-stine

121

Azelastine
Time

Duration 8-24 hours

122

Cough Suppressants, Degongestants
& Mucolytics
Acetaminophen
Class

Mild analgesic

123

Cough Suppressants, Degongestants
& Mucolytics
Acetaminophen
Mechanism

Inhibition of cyclooxygenase (COX), and recent findings suggest that it is highly selective for COX-2.

124

Cough Suppressants, Degongestants
& Mucolytics
Acetaminophen
Treatment

Fever, pain, myalgia, and headache.

125

Cough Suppressants, Degongestants
& Mucolytics
Acetaminophen
Adverse Rxns:

Metabolized by the liver and is hepatotoxic; side effects are multiplied when combined with alcoholic drinks.

126

Cough Suppressants, Degongestants
& Mucolytics
Acetaminophen
Time

The onset of analgesia is approximately 11–29.5 minutes after oral administration and its half-life is 1–4 hours.

127

Diphenhydramine
Contraindicated

Prostate hypertrophy, urinary obstruction, asthma, COPD, peptic ulcer, MAOIs

128

Cough Suppressants, Degongestants
& Mucolytics
Dextromethorphan
Class

Antitussive

129

Cough Suppressants, Degongestants
& Mucolytics
Dextromethorphan
Mechanism

Suppresses cough reflex via direct action on the cough center in the medulla of the brain. Metabolized by CYP2D6 into active metabolite dextrorphan

130

Cough Suppressants, Degongestants
& Mucolytics
Dextromethorphan
Contraindications:

MAOIs, antidepressants, respiratory insufficiency, HS White margin of safety (12-75x of TD to produce halllucinations.

131

Cough Suppressants, Degongestants
& Mucolytics
Dextromethorphan
Time

Onset: 15-30 min, duration 3-6 hours

132

Cough Suppressants, Degongestants
& Mucolytics
Codeine
Class

Opoid analgesic, Antitussive
(3-methylmorphine)

133

Cough Suppressants, Degongestants
& Mucolytics
Codeine
Mechanism

Suppresses cough by action on the respiratory center
10% is converted to morphine

134

Cough Suppressants, Degongestants
& Mucolytics
Codeine
Side effects

Constipation, sedation, histamine release, vasodilation, orthostatic hypotension, dizziness

135

Cough Suppressants, Degongestants
& Mucolytics
Camphor
Class

Topical Agent = ointment, lozenges, inhalation

136

Cough Suppressants, Degongestants
& Mucolytics
Camphor
Mechanism

Rub on throat and chest as a thick later, not used in nostrils or mouth

137

Cough Suppressants, Degongestants
& Mucolytics
Menthol
Class

Topical Agent= ointment, lozenges, inhalation

138

Cough Suppressants, Degongestants
& Mucolytics
Menthol
Mechanism

Rub on throat and chest as a thick later, not used in nostrils or mouth

139

Cough Suppressants, Degongestants
& Mucolytics
Pseudoephedrine
Class

Nasal decongestant

140

Cough Suppressants, Degongestants
& Mucolytics
Pseudoephedrine
Mechanism

Vasoconstricive drug that reduces nasal congestion, does not affect the release of histamine or other mediators in the allergic reaction, commonly formulated with antihistamines
Alpha-adrenergic agonist
Acts primarily by releasing NE from adrenergic nerves

141

Cough Suppressants, Degongestants
& Mucolytics
Pseudoephedrine
Metabolized

Metabolized to a minor extent, 88% excreted unchanged in the urine

142

Cough Suppressants, Degongestants
& Mucolytics
Pseudoephedrine
Time

Better bioavailability – but both have a short half-life, with a peak at 0.5-2 hours

143

Cough Suppressants, Degongestants
& Mucolytics
Pseudoephedrine
Side effects:

Side effects: CV stimulation, CNS stimulation, rebound congestion (ischemic as a result of vasoconstriction of the drug or local irritation of the drug)
Behind the Counter OTC product to reduce use in meth

144

Cough Suppressants, Degongestants
& Mucolytics
Phenylephrine
Class

Nasal decongestant

145

Cough Suppressants, Degongestants
& Mucolytics
Phenylephrine
Mechanism

Acts by directly stimulating adrenergic receptors on postsynaptic sites

146

Cough Suppressants, Degongestants
& Mucolytics
Phenylephrine
Metabolized

Rapidly metabolized by MOA and COMT in the GI mucosa, liver, and other tissues

147

Cough Suppressants, Degongestants
& Mucolytics
Oxymetazoline
Class

Topical nasal decongestant

148

Cough Suppressants, Degongestants
& Mucolytics
Oxymetazoline
Adverse Rxn

Do not use for more than 3-5 days because it can cause rhinitis medicamentosa

149

Cough Suppressants, Degongestants
& Mucolytics
Oxymetazoline
Preferred Treatment

Preferred agent during pregnancy

150

Cough Suppressants, Degongestants
& Mucolytics
Guaifenasin
Class

Expectorants
(Mucinex)

151

Cough Suppressants, Degongestants
& Mucolytics
Guaifenasin
Mechanism

Symptomatic relief of ineffective productive coughs, not used for chronic coughs, loosens and thins lower respiratory tract secretions by increasing volume and reducing volume of secretions.

152

Cough Suppressants, Degongestants
& Mucolytics
Guaifenasin
Trivia

In veterinary medicine, used to induce and maintain anesthesia in horses

153

Cough Suppressants, Degongestants
& Mucolytics
Acetyl cysteine
Class

Mucolytic

154

Cough Suppressants, Degongestants
& Mucolytics
Acetyl cysteine
Mechanism

Use in diseases with increased mucus production – cystic fibrosis, COPD, Bronchiectasis, Respiratory infections, TB.
Break H bonds by substituting a sulfhydryl radical-HS

155

Cough Suppressants, Degongestants
& Mucolytics
Acetyl cysteine
Route

Given aerosol or by direct instillation into the ET tube

156


Cough Suppressants, Degongestants
& Mucolytics
Acetyl cysteine
Unique Treatment

Given orally to reduce liver injury w/ acetoaminophen (Tylenol) overdose

157

Cough Suppressants, Degongestants
& Mucolytics
Acetyl cysteine
Side effects

Side effects – bronchospasm (asthma) – if used with asthma, use 10% with bronchodilator
Side Effects – increase mucus production (be prepared to suction a patient who cannot cough), do not mix with antibiotics in the same nebulizer, disagreeable odor due to the hydrogen sulfide, N/V

158

Cough Suppressants, Degongestants
& Mucolytics
Amiloride
Class

Aersolized Diuretic/ sodium channel blocker

159

Cough Suppressants, Degongestants
& Mucolytics
Amiloride
Mechanism

Diuretic that can be given by aerosol to patients w/ CF, sodium channel blocker.
In CF, sodium is absorbed into the epithelium along with water, leaving the mucus thick and dehydrated – but by blocking the absorption, dehydration of the mucus is prevented

160

Cough Suppressants, Degongestants
& Mucolytics
Amiloride
Route

The drug is dissolved in 0.3% NaCl solution and nebulized

161

Treatment of Tuberculosis
Rifampin
Class

RIF

162

Treatment of Tuberculosis
Rifampin
Mechanism

Inhibition of RNA synthesis, binds the beta subunits of RNA polymerase
Bactericidal for IC and EC bacteria
Resistance – DNA dependent RNA polymerase does not bind drug
Never given as a single agent due to resistance

163

Treatment of Tuberculosis
Rifampin
Route/Time

Abs – oral, impaired by food & para-aminosalicylic acid (admin 8-12 hours apart)

164

Treatment of Tuberculosis
Rifampin
Tissues/Metabolized

Penetrates all tissues well including CSF (meningitis)
Metabolized – de-acetylated in liver (halflife increased by hepatic dysfunction/ de-acetylated rifampin still has full antibacterial activity but is not resorbed
Excreted primarily in bile, small amount renal tubular secretion, but no adjustment w/ renal failure

165

Treatment of Tuberculosis
Rifampin
Adverse effects

Discolors body fluids – orange/red tears, urine, saliva), GI disturbances, CND complains, Hepatotoxic (more relevant in slow acetylators);

166

Treatment of Tuberculosis
Rifampin
Drug interactions

Induces P450 (within 2 weeks of drug use), reduces the halflife of prednisone, BBs, suldonamides, dapsone, NNRTIs
Probenecid increases serum levels of rifampin
Rifabutin has less effect on the metabolism of HIV protease inhibitors

167

Treatment of Tuberculosis
Rifampin
Other indications:

MRSA, MRSE, prophylaxis of household members exposed to memingococci or H. influenza, eradication of staph in nasal carriers

168

Treatment of Tuberculosis
Isoniazid
Class

INH

169

Treatment of Tuberculosis
Isoniazid
Mechanism

Interferes w/ mycolic acid synthesis – disrupts cell wall synthesis; cidal for rapidly dividing bacilli; extracellular cavitary lesions; static for slowly growing lesions; penetrates host cells – effective for intracellular bacilli

170

Treatment of Tuberculosis
Isoniazid
Resistance

Inability to take up the drug, alteration of target enzyme, overproduction of target enzyme, emerges rapidly (INH is never used as a single agent in active infections) – 1/10^6 will develop resistance, and the average cavitary lesion has 100 million bacteria

171

Treatment of Tuberculosis
Isoniazid
Absorbed/Distributed

Absorbed rapidly from the GI tract with oral dose or can be given IM.
Distributed to all tissues/ fluids (including placenta, meninges in meningitis, breast milk)

172

Treatment of Tuberculosis
Isoniazid
Metabolism

Acetylated via N-acetyl transferase (some people are fast metabolizers, some are slow – slow metabolizers have levels 2-3 times higher)- determines halflife of 1-5 hours

173

Treatment of Tuberculosis
Isoniazid
Excretion

Drug and inactive metabolites excreted in the urine (~75%) – no adjustment w/ renal failure

174

Treatment of Tuberculosis
Isoniazid
Adverse effects

Peripheral neuropathy due to competition w/ pyridoxical phosphate (corrected w/ B6 admin) – more frequent in malnourishment
Hepatotoxic (2% major toxic rxn to metabolite)

175

Treatment of Tuberculosis
Isoniazid
Interactions w/:

Antacids w/ Al3+ salts decrease absorption; administer 1h before any antacids
Corticosteroids decrease efficacy
Inhibits P450 that metabolizes phenytoin, diazepam, fluoxentine, nelfinavir

176

Treatment of Tuberculosis
Pyrazinamide
Class

PZA

177

Treatment of Tuberculosis
Pyrazinamide
Mechanism

Bacilli convert pyrazinamide to pyrazinoic acid, decreasing pH and inhibiting growth; resistant strains may lack pyrazinamidase/ cidal or static depending onconcentration in infected site

178

Treatment of Tuberculosis
Pyrazinamide
Active against

Active against tubercle bacilli in acid environment of lysosome & macrophage (most significant effect at intracellular sites where MTB replicates slowly)

179

Treatment of Tuberculosis
Pyrazinamide
Route/Time

Well/ rapidly absorbed within 2 hours & widely distributed- including to CSF

180

Treatment of Tuberculosis
Pyrazinamide
Metabolized

Metabolized in liver, excreted in urine via glomerular filtration

181

Treatment of Tuberculosis
Pyrazinamide
Adverse effects

Dose related hepatotoxicity (most severe rxn), mild non gouty arthalgias, hyperuricemia is usually asymptomatic

182

Treatment of Tuberculosis
Ethambutol
Class

EMB

183

Treatment of Tuberculosis
Ethambutol
Mechanism

Inhibition of RNA synthesis. Disrupts cell wall synthesis – inhibits arabinosyl transferase, necessary for peptidoglycan units of cell wall resulting in increased cell wall permeability
Static, possibly cidal at high levels
Bacilli must be actively dividing

184

Treatment of Tuberculosis
Ethambutol
Esistance

Slow development of resistance
No cross resistance

185

Treatment of Tuberculosis
Ethambutol
Absorption/Elimination

Absorption of 75% dose, concentrates in kidneys, lungs, saliva, therapeutic levels in CSF with inflamed meninges , placenta, breast milk.
Elimination – partly metabolized in the liver, excreted in the urine, T1/2 of 3.5 hours

186

Treatment of Tuberculosis
Ethambutol
Adverse Rxn:

Optic neuritis, dose related, decreased visual acuity, loss of color discrimination – monthly visual exams- reversible weeks to months after therapy, can cause allergic rxns, hyperuricemia, drug interactions (Al3+ containing antacids reduce absorption

187

Treatment of Tuberculosis
Cycloserine
Class

Antiobiotic Second line drub TB

188

Treatment of Tuberculosis
Cycloserine
Mechanism

Blocks cell wall synthesis; structural analog of D-alaninel can block enzymes, L-alanine racemase & D-alanine synthetase/ enzymes for D-alanine incorporation into pentapeptide or peptidoglycan strands
Depending on conc – cidal or static

189

Treatment of Tuberculosis
Cycloserine
Effective

Effective in resistant organisms – no cross-resistance
Broad spectrum, second-line agent, active against pulmonary and extra-pulmonary TB

190

Treatment of Tuberculosis
Cycloserine
Treatment

Only used when other treatments fail – MDR-TB (INH, RIF-R)
Used against mycobacterium avium
Used to treat UTIs

191

Treatment of Tuberculosis
Cycloserine
Route

Administered orally w/ good absorption (70-90%)
Distributed widely & not protein bound
Lungs, pleura, synovial fluid, CSF more when inflamed/ excreted unchanged –renal – dose adjustment in renal failure

192

Treatment of Tuberculosis
Cycloserine
Adverse effects

Adverse effects – involve CNS – reversible when therapy is discontinued- Headache, tremor, vertigo, confusion, psychotic states w/ suicidal tendencies, paranoia, seizures (not for use in epileptic pts) – risk of suicide increased w/ depression / manifest within first 2 weeks

193

Treatment of Bacterial Infections
Amoxicillin
Class

Aminopenicillins
(Cell wall)

194

Treatment of Bacterial Infections
Amoxicillin
Route/Dose considerations

Can be taken with food unlike other penicillins
=dose is affected by the state of the kidneys or admin of other organic acids

195

Treatment of Bacterial Infections
Amoxicillin-clavulanate=Augmentin
Class

Aminopenicillins
(Cell wall)

196

Treatment of Bacterial Infections
Amoxicillin-clavulanate=Augmentin
Treatment/Side effects

MSSA, anaerobes
Can cause N/V in children

197

Treatment of Bacterial Infections
Ampicillin-sulbactam=Unasyn
Class

Aminopenicillins
(Cell wall)

198

Treatment of Bacterial Infections
Ampicillin-sulbactam=Unasyn
Treatment

Amp-R H influenza, mixed gram positive and anaerobic infections (CAP)

199

Treatment of Bacterial Infections
Carbapenem
Class

B-lactam
Cell wall

200

Treatment of Bacterial Infections
Carbapenem
Mechanism

Small hydroxyethyl side chain makes it easier for B lactam to move through complex outer membrane of GN bacteria.

201

Treatment of Bacterial Infections
Carbapenem
Resistance/Spectrum

High resistance to beta-lactamases
Broadest spectrum of the B-lactams

202

Treatment of Bacterial Infections
Carbapenem
Route/Metabolized

Give IV
Excreted by glomerular filtration and secretion
Drug formulated w/ cilastatin to inhibit hydrolysis in brush border

203

Treatment of Bacterial Infections
Carbapenem
Treatment

Active against GN and GP, not as a monotherapy for P aeruginosa/ resistant nosocomial gram-negative (Enterobacter) /
Combine w/ aminoglycoside to tx actinobacter

204

Treatment of Bacterial Infections
Carbapenem
Contra-indicated

Contra-indicated in patients w/ CNS seizures/ expensive

205

Treatment of Bacterial Infections
Ceftriaxone
Class

(Cell wall)
B-lactam
3rd generation cephalopsporin

206

Treatment of Bacterial Infections
Ceftriaxone
Mechanism

Same 4 membered B-lactam ring as penicillins w/ a 6 membered dihydrothizide ring – more chemical binding sites
More resistant to B-lactamases
Broader spectrum

207

Treatment of Bacterial Infections
Ceftriaxone
Penicillin Allergies

Effective in pts allergic to penicillin

208

Treatment of Bacterial Infections
Ceftriaxone
3rd Generation Benifits

1st  3rd = greater GN less GP / more resistance to B-lactamases / increased ability to enter CSF

209

Treatment of Bacterial Infections
Ceftriaxone
Treatment

Used for active infections – bacteremia, severe pulmonary infections use w/ aminoglycosidases, do not work against enterococci

210

Treatment of Bacterial Infections
Ceftriaxone
Route/Metabolized

Mostly IV/ IM (can be oral)
Renal Excretion

211

Treatment of Bacterial Infections
Clarithromycin
Class

Macrolide

212

Treatment of Bacterial Infections
Clarithromycin
Mechanism

Binds to 50S ribosomal subunit / Static

213

Treatment of Bacterial Infections
Clarithromycin
Route/Metabolized

More acid stable, rapid first pass metabolism (primary metabolite is still active), eliminated by kidney & liver
Absorption increases w/ food
Inhibits CYP P450 but not as much as erythromycin

214

Treatment of Bacterial Infections
Clarithromycin

Legionnaire’s disease
Mycoplasma pneumonia
Chlamydia pneumonia
H influenza
Strep pneumo & GAS
Moraxella

215

Treatment of Bacterial Infections
Doxycycline
Class

Tetracycline
30S – protein synthesis

216

Treatment of Bacterial Infections
Doxycycline
Mechanism

First broad spectrum (GN & GP)
Bacteriostatic – binding to the ribosome 30s is reversible
Enters cell through porin channels

217

Treatment of Bacterial Infections
Doxycycline
Resistance

Resistance occurs slowly – can develop if the efflux pump is induced
Inhibited by di & tri-valent cations

218

Treatment of Bacterial Infections
Doxycycline
Route/Metabolized

Best absorbed in acidic conditions of the stomach
Hepatic elimination

219

Treatment of Bacterial Infections
Doxycycline
Adverse effects

Adverse – N/V – less w/ doxy
Superinfections, chelation of calcium (teeth discoloration/ depression of bone growth)
Some vestibular toxicity (minoclycine), photosensitivity (doxy)

220

Treatment of Bacterial Infections
Doxycycline
Treatment

Used for Atypical pneumonia (Mycoplasma, Legionells, Chlamydia), Lyme disease, acne, periodontal disease

221

Treatment of Bacterial Infections
Erythromycin
Class

Macrolide

222

Treatment of Bacterial Infections
Erythromycin
Mechanism

Binds to 50S ribosomal subunit / Static
Narrow spectrum

223

Treatment of Bacterial Infections
Erythromycin
Route/Metabolized

Admin orally, but increased acidity may inactivate
Well –distributed but not to CSF
Concentrates in liver (check liver functions)
Excreted in bile/ feces
Placenta/ breast milk

224

Treatment of Bacterial Infections
Erythromycin
One of few drugs that can?
Also crosses into?

One of few drugs to cross into prostatic fluid and accumulates in macrophages

225

Treatment of Bacterial Infections
Erythromycin
Treatment

Legionnaire’s disease
Mycoplasma pneumonia
Chlamydia pneumonia
GP & GN atypical organisms
Can be used to eliminate the carrier state w/ corynebacterium diphtheria

226

Treatment of Bacterial Infections
Erythromycin
Side effects

Epigastric distress is the most common side effect
Transient deafness
Big time inhibitor of CYP P450
Cholestatic hepatitis

227

Treatment of Bacterial Infections
Imipenem
Class

B-lactam
Cell wall

228

Treatment of Bacterial Infections
Imipenem
Contrindication
Advantage

Not used in patients w/ seizures
Does not need co-admin of cilastatin

229

Treatment of Bacterial Infections
Imipenem
Treatment

Best outcomes for Extended Spectrum Beta-lactam (ESBL) E coli & Klebsiella

230

Treatment of Bacterial Infections
Levofloxacin
Class

Newer Fluoroquinolone

231

Treatment of Bacterial Infections
Levofloxacin
Mechanism

Analog of quinolone nalidixic acid
Inhibition of bacterial DNA gyrase
Bactericidal

232

Treatment of Bacterial Infections
Levofloxacin
Resistance

Resistance via alterations in DNA gyrase enzyme (increases in SA and PA) = quinolone resistance-determining region (QRDR)
Resistance – not plasmid mediated – decreased porins, energy-dependent efflux

233

Treatment of Bacterial Infections
Levofloxacin
Route/Metabolized

Good oral absorption, wide distribution, decreased abs w/ antacids, poor CSF penetration, renal & liver excretion

234

Treatment of Bacterial Infections
Levofloxacin

Strep pneumo, Legionella, GN coverage similar to aminoglycosides – synergism w/ B-lactams

235

Treatment of Bacterial Infections
Meropenem
Class

(Cell wall)
B-lactam

236

Treatment of Bacterial Infections
Meropenem
Activity

Does not need co-admin of cilastatin
Less G+ activity
Less CNS px

237

Treatment of Bacterial Infections
Meropenem
Treatment

Best outcomes for Extended Spectrum Beta-lactam (ESBL) E coli & Klebsiella

238

Treatment of Bacterial Infections
Moxifloxicin
Class

Newer Fluoroquinolone

239

Treatment of Bacterial Infections
Moxifloxicin
Mechanism

Analog of quinolone nalidixic acid
Inhibition of bacterial DNA gyrase
Bactericidal

240

Treatment of Bacterial Infections
Moxifloxicin
Metabolism

Mostly hepatic clearance
Not used for UTIs
Hepatic elimination

241

Treatment of Bacterial Infections
Penicillin
Class

(Cell wall)
B-lactam

242

Treatment of Bacterial Infections
Penicillin
Metabolism

An acid administered as a salt w/ high doses – evaluate pt w/ HTN CHF exists as a non-absorble anion, K+ moves into the tubule in exchange for H+  hypokalemic alkylosis

243

Treatment of Bacterial Infections
Penicillin
Adverse Rxns

Can cause HS rxns, delayed allergic rxns, >2 days rash, more common with ampicillin & amoxicillin
Hives/ uticaria
Most life-threatening responses are caused by peritoneal drug admin

244

Drugs to Treat Lung Cancer
Bevacizumab
Treatment

Adenocarcinoma
Non-squamous NSCLC

245

Drugs to Treat Lung Cancer
Bevacizumab
Mechanism

Humanized antibody, binds VEGF, given IV
Inhibition promotes non-physiologic apoptosis of endothelial cells and decreases deposition of subendothelial matric making the vasculature more susceptible to severe bleeding

246

Drugs to Treat Lung Cancer
Bevacizumab
Contraindicated/Side effect

Risk of bleeding in squamous lung cancers – not approved
Can cause HTN

247

Drugs to Treat Lung Cancer
Carboplatin
Treatment

SCLC

248

Drugs to Treat Lung Cancer
Carboplatin
Mechanism

Forms DNA intra-strand cross-links and adducts

249

Drugs to Treat Lung Cancer
Carboplatin
Adverse Rxns

Allergic (platinum rxns)
Dose-related myelosuppression; cumulative anemia
Dose-related N/V
Blood chemistry dyscrasia, increase in hepatic enzymes, BUN & creatinine

250

Drugs to Treat Lung Cancer
Cisplatin
Treatment

SCLC/ NSCLC

251

Drugs to Treat Lung Cancer
Cisplatin
Mechanism

Forms DNA intra-strand cross-links and adducts

252

Drugs to Treat Lung Cancer
Cisplatin
Adverse Rxns

Dose-related severe nephrotoxicity, myelosuppression, N/V
Significant ototoxicity

253

Drugs to Treat Lung Cancer
Crizotinib
Treatment

Adenocarcinoma

254

Drugs to Treat Lung Cancer
Crizotinib
Mechanism

Reversible multi-kinase inhibitor, ALK
CYP3A4 inhibitor

255

Drugs to Treat Lung Cancer
Crizotinib
Route

Oral on empty stomach

256

Drugs to Treat Lung Cancer
Crizotinib
Adverse Rxn

Visual disorders are common

257

Drugs to Treat Lung Cancer
Cyclophosphamide
Treatment

SCLC

258

Drugs to Treat Lung Cancer
Cyclophosphamide
Mechanism

Pro-drug of active alkylating moiety

259

Drugs to Treat Lung Cancer
Cyclophosphamid
Adverse Rxns

Blood dyscrasias  anemia
Hemorrhagic cystitis (mesna)
Infertility
Monitor for 2ndary malignancies
Pulmonary fibrosis

260

Drugs to Treat Lung Cancer
Doxorubicin
Treatment

SCLC

261

Drugs to Treat Lung Cancer
Doxorubicin
Mechanism

Intercalator, free radical generator, topo II inhibitor (DNA STRUCTURE)

262

Drugs to Treat Lung Cancer
Doxorubicin
Adverse Rxns

Myelosuppresion,
Cumulative dose cause CHF
Hepatic disease
2ndary malignancies
Extravasational necrosis
N/V

263

Drugs to Treat Lung Cancer
Erlotinib
Treatment

Adenocarcinoma

264

Drugs to Treat Lung Cancer
Erlotinib
Mechanism/Epidemiology

EGFR kinase inhibition
(lung cx) – most never smokers
Mutations high in Asian populations

265

Drugs to Treat Lung Cancer
Erlotinib
Route/Side effects

Oral, few side effects

266

Drugs to Treat Lung Cancer
Etoposide
Treatment

SCLC

267

Drugs to Treat Lung Cancer
Etoposide
Mechanism

DNA-topo II complex stabilizer

268

Drugs to Treat Lung Cancer
Etoposide
Side effects

Myelosuppression, infection
N/V
Diarrhea, alopecia

269

Drugs to Treat Lung Cancer
Gemcitabine
Treatment

NSCLC

270

Drugs to Treat Lung Cancer
Gemcitabine
Mechanism

DNA polymerase inhibitor via incorpotation of triphosphate form during DNA synthesis (DNA SYNTHESIS)

271

Drugs to Treat Lung Cancer
Gemcitabine
Adverse Rxns

Myelosuppression, arthralgia, sensory peripheral neuropathy

272

Drugs to Treat Lung Cancer
Ifosfamide
Treatment

SCLC

273

Drugs to Treat Lung Cancer
Ifosfamide
Mechanism

Intra- and Inter- strand cross-linker

274

Drugs to Treat Lung Cancer
Ifosfamide
Side effcts

Alopecia, N/V, blood dyscrasia  infection

275

Drugs to Treat Lung Cancer
Ifosfamide
Adverse Rxn

Hemorrhagic cystitis is rare when ifosfamide is given together with mesna.
Dose-limiting side effect is encephalopathy

276

Drugs to Treat Lung Cancer
Irinotecan
Treatment

SCLC Myelosuppression and GI toxicity
Elevated liver functions and serum creatinine

277

Drugs to Treat Lung Cancer
Irinotecan
Mechanism

Prevents DNA from unwinding by inhibition of topoisomerase 1.

278

Drugs to Treat Lung Cancer
Irinotecan
Side effects

Myelosuppression and GI toxicity
Elevated liver functions and serum creatinine

279

Drugs to Treat Lung Cancer
Methotrexate
Treatment

SCLC

280

Drugs to Treat Lung Cancer
Methotrexate
Mechanism

Folic Acid analog
Dihydrofolate reductase inhibition (universal)
Folic acid essential dietary factor
Polyglutamation (which traps drug) also inhibits thymidylate synthase (TS) and 2 early enzymes in purine biosynthesis
Rescue other cells with Leucovorin

281

Drugs to Treat Lung Cancer
Methotrexate
Toxicity

Methotrexate is a highly teratogenic drug and categorized in pregnancy category X

282

Drugs to Treat Lung Cancer
Paclitaxel
Treatment

NSCLC

283

Drugs to Treat Lung Cancer
Paclitaxel
Mechanism

Micro tubule (MT) stabilizer inhibiting depolymerization (MT)

284

Drugs to Treat Lung Cancer
Pemetrexed
Treatment

NSCLC

285

Drugs to Treat Lung Cancer
Pemetrexed
Mechanism

Inhibiting dihydrofolate reductase (DHFR)
DHFR inhibitor (DNA SYNTHESIS)

286

Drugs to Treat Lung Cancer
Pemetrexed
Dose limiting toxicity

Low blood cell counts, as measured by a Complete Blood Count. This is a dose-limiting toxicity.

287

Drugs to Treat Lung Cancer
Topotecan
Treatment

SCLC

288

Drugs to Treat Lung Cancer
Topotecan
Mechanism

DNA topo I complex stabilizer

289

Drugs to Treat Lung Cancer
Topotecan
Side effects

Myelosuppression and GI toxicity
Hyperbilirubinemia

290

Drugs to Treat Lung Cancer
Vincristine
Treatment

SCLC

291

Drugs to Treat Lung Cancer
Vincristine
Mechanism

MT inhibitor, tubules disintegrate into spiral aggregates/ protofilaments

292

Drugs to Treat Lung Cancer
Vincristine
Side effects

Peripheral neuropathy, hyponatremia, constipation, and hair loss.
First symptoms of peripheral neuropathy is foot drop:

293

Drugs to Treat Lung Cancer
Vinorelbine
Treatment

NSCLC

294

Drugs to Treat Lung Cancer
Vinorelbine
Mechanism

MT inhibitor, tubules disintegrate into spiral aggregates/ protofilaments

295

Drugs to Treat Lung Cancer
Vinorelbine
Side effects

Neutropenia, (peripheral neuropathy)