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Pulmonary Block > Pharmacology Asthma/COPD/Mucus/TB > Flashcards

Pharmacology Asthma/COPD/Mucus/TB Flashcards

1
Q

Non-specific adrengergic agonists

A

Bronchodilators; Epinephrine, Ephedrine, Isoproterenol

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2
Q

B2 Specific agonists with quick onset and short duration

A

Bronchodilators; Albuterol, Terbutaline

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3
Q

B2 specific agonists with slow onset and long duration

A

Bronchodilators; Salmeterol, Formoterol (used with steroids)

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4
Q

Cholinergic antagonists

A

Bronchodilators; Atropine, Ipratropium

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5
Q

Methylxanthines

A

Bronchodilators and anti-inflammatory; aminophylline, theophylline

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6
Q

Cromolyns

A

Anti-inflammatory; cromolyn sodium

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7
Q

Corticosteroids

A

Anti-inflammatory; budesonide, fluticasone, fluticasone (w/ Salmeterol), budesonide (w/ formoterol), Mometasone, Beclomethasone, Ciclesonide, Prednisone (oral), Prednisolone, Methylprednisolone, Dexamethasone (oral or IV)

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8
Q

Leukotriene Receptor Blockers

A

Anti-inflammatory; Monteleukast, Zafirlukast

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9
Q

Leukotriene Synthesis Inhibitors

A

Anti-inflammatory; Zileuton

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10
Q

Anti IgE Antibody

A

Omalizumab

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11
Q

Sympathomimetics MOA

A

increase levels of cAMP; some inhibition on the release of mediators from mast cells; some inhibition on microvascular permeability; promote to a small degree mucocilliary transport

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12
Q

Sympathomimetics Adverse Effects

A

N/V, HA, fall in BP, increase Heart Rate, Cardiac Arrhythmias, PaO2 decrease, CNS toxic effects (agitation, convulsions, coma, respiratory and vasomotor collapse)

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13
Q

AntiMuscarinics MOA

A

Competitive Ach-muscarinic blockade, reduce airway smooth muscle constriction, enhance B2 mediated bronchodilation

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14
Q

AntiMuscarinics Adverse Effects

A

Pupillary dilation and cycloplegia

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15
Q

Ipratropium

A

A antimuscarinic that is poorly absorbed with no significant systemic effects

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16
Q

Combivent

A

Combined anti-cholinergic and B2 agonist that is more effective at producing improved lung function than either alone; it is indicated for COPD

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17
Q

Methylxanthines Effects

A

increase cAMP, block muscular adenosine receptors, decrease release of mediators; bronchodilation, anti-inflammatory effect, positive isotropic and chronotropic effects, increased CNS activity, increased gastric acid secretion, weak diuretic effect, increased skeletal muscle strength (diaphragm)

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18
Q

Methylxanthines Adverse Reactions

A

N/V, nervousness, HA, insomnia, hypokalemia, hyperglycemia, tachycardia, cardiac arrhythmias, tremor, neuromuscular irritability and seizures

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19
Q

Cromolyn Sodium Effects

A

alters the activity of chloride channels, inhibits degranulation of mast cells in the lung, inhibit the inflammatory response by acting on eosinophils, inhibits cough by action on airway nerves, reduces bronchial hyperactivity associated with exercise and antigen inhaled asthma

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20
Q

Cromolyns Adverse Effects

A

No systemic toxicity; unpleasant taste, irritation of trachea leading to cough and bronchospasm

Rare: chest pain, restlessness, hypotension, arrhythmias, nausea, vomiting, CNS depression, seizures, anorexia

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21
Q

Glucocorticoid Effects

A

decreases production of inflammatory cytokines, reduces mucus secretions, reduces bronchial hyperactivity, enhance the effect of B2 agonists

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22
Q

Glucocorticoid MOA

A

binds to glucocorticoid receptor cause decreased mRNA stability through effect on tristetraprolin leading to decreased TNF, IL6, GM-CSF, COX2; decreases inflammatory genes; increases anti-inflammatory genes (SLPI, MKP-1, GILZ); decreases TH2 by blocking GATA3

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23
Q

Inhaled Glucocorticoid Adverse Effects

A

oropharyngeal candidiasis, hoarseness, dry mouth; decreased bone mineral density in premensopausal women; decrease growth rate of children

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24
Q

Oral glucocorticoids Adverse Effects (prolonged use)

A

Cushing syndrome, glucose intolerance, increased blood pressure and weight, bone demineralization, cataracts, immunosupression, retarded growth in children

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25
Q

Cushing Syndrome

A

Caused by glucocorticoids - weight gain in abdomen, face (moon face), neck, buffalo hump; thin skin with easy bruising stretch marks; increased acne, facial hair; scalp hair loss; ruddy complexion of face and neck; acanthuses (neck darkening); child obesity and poor growth in height; high BP

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26
Q

Steroids primary target

A

Phospholipase A2 (stops conversion of Membrane phospholipids to Arachidonic Acid)

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27
Q

Nedocromil primary target

A

COX1/2 (stops conversion of Arachidonic Acid to PGG2)

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28
Q

Zileuton primary target

A

5-LO (stops conversion of arachidonic acid to LTA4)

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29
Q

Zafirlukast primary target

A

Block Leukotriene receptor

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30
Q

Seatrodast primary target

A

blocks thromboxane A2 receptor

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31
Q

LTB4 role

A

Neutrophil chemoattractant

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32
Q

LTC4 and LTD4 role

A

mimic many symptoms of asthma - bronchial hyper reactivity, bronchoconstriction, mucosal edema, increased mucus secretion

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33
Q

Zafirlukast and Monteleukast Role

A

Block LTD4 receptors, decrease bronchial reactivity and bronchoconstriction, decrease mucosal hyper secretion and mucosal edema, decrease airway inflammation

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34
Q

Zafirlukast Adverse Effects

A

G.I.T. disturbances, mild HA and elevation of liver enzymes in some patients; high doses in rodents have caused hepatic and bladder cancer and histolytic carcinoma

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35
Q

Monteleukast Adverse Effects

A

G.I.T. disorders, laryngitis, pharyngitis, nausea, otitis, sinusitis, viral infections; suicidal ideation possible

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36
Q

Zileuton Affects

A

inhibits leukotriene formation - decreases smooth muscle contraction and blood vessel permeability and reduces leukocyte movement to damaged area

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37
Q

Zileuton Adverse Effects

A

Causes hepatic enzyme elevation - LFTs required; other effects mild and self limited

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38
Q

Zileuton Interactions

A

CYP1A2 substrate and inhibitor - interaction with theophylline and others

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39
Q

Omalizumab Effects

A

binds to IgE, preventing IgE release of inflammatory mediators, leading to decreased allergic response; it reduces severity/frequency of asthma attacks, requires inhaled steroid with it; improves long term asthma control

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40
Q

Omalizumab Adverse Effects

A

anaphylaxis, redness, bruising, warmth, buring, pain, inflammation at injections site, sore throat, cold symptoms, increase in CV complications, no known drug interactions

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41
Q

COPD Treatment Options

A

Smoking cessation with nicotine replacement or Bupropion; bronchodilator SABA or LABA; Antmuscarinics; Theophylline and derivatives; combo therapy; steroids, guafensesin, N-acetylcystine; supplemental O2; surgery, lung volume reduction, transplants

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42
Q

Contraindicated drugs in airway disease

A

sedatives, beta blockers, aspirin and other COX inhibitors, ACE inhibitors, Local anesthetics containing epinephrine

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43
Q

Doxapram

A

Respirayoty stimulant used for drug induced respiratory depression, acute hypercapnia in COPD; has narrow margin of safety; short acting and given by infusion

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44
Q

Doxapram MOA

A

activates peripheral carotid receptors

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45
Q

Locations of Cough Receptors and Nerves Involved

A

airway bifurcations, distal esophagus - link to cough centers via vagus and superior laryngeal nerves

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46
Q

Location of cough control

A

Medulla

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47
Q

Acute cough

A

a cough lasting less than three weeks

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48
Q

Subacute cough

A

cough lasting three to eight weeks

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49
Q

Chronic cough

A

cough lasting greater than eight weeks

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50
Q

Cough with clear secretions

A

bronchitis

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51
Q

Cough with purulent secretions

A

bronchial infections

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52
Q

cough with yellow secretions

A

inflammatory disorders

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53
Q

cough with malodorous secretions

A

anaerobic infection

54
Q

Non productive cough

A

viral illness, bronchospasm, allergies, airway obstruction, GERD

55
Q

Complications of cough

A

Exhaustion, urinary incontinence, pain, insomnia, syncope, stroke, rib fractures

56
Q

Nonpharmacological treatment for cough

A

Elimate irritants, hard candies, lozenges, humidifiers, vaporizers, hydration

57
Q

Dextromethorphan (DM Drugs) Effects

A

antitussive; suppresses the cough reflex by direct action on the cough center; nonopiod but equal potency to codeine; quick onset with 3-6hr duration; wide margin of safety

58
Q

Dextromethorphan metabolism

A

metabolized by CYP2D6 to active metabolite dextrorphan

59
Q

Dextromethorphan Side Effects

A

Dizziness, drowsiness, N/V, diarrhea, irritability, excitability, light headedness, trouble sleeping

60
Q

Dextromethorphan Contra

A

Concurrent use of MAOI antidepressants; advanced respiratory insufficiency; hepatic disease; hypersensitivity to any ingredients

61
Q

Diphenhydramine (benadryl) effects

A

antihistamine - H1 receptor antagonist; suppresses cough reflex by direct effect on cough center; 15 min onset; 4-6hr duration; indicated for nonproductive cough caused by irritation

62
Q

Diphenhydramine Adverse Effects

A

Drowsiness, respiratory depression, blurred vision, dry mouth, urinary retention, constipation

63
Q

Diphenhydramine Contra

A

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

64
Q

Codeine effects

A

opioid analgesic that acts on mu receptors but has lower affinity than morphine; depresses cough reflex by direct effects on cough control center; 10-30 min onset; 4-6hr duration

65
Q

Codeine Adverse Effects

A

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

66
Q

Codeine Contras

A

Hypersensitivity, labor of premature birth, preganany, prostatic hypertrophy, individs on sedatives, patients with acute respiratory depression, asthma, COPD

67
Q

Topical cough relievers

A

Camphor and menthol and eucalyptus

68
Q

Guaifenesin effects

A

symptomatic relief of ineffective productive cough w/ chest congestion; not for chronic cough; loosens and thins lower respiratory tract secretions by increasing the volume and reducing the viscosity of secretions

69
Q

Guaifenesin Adverse effects

A

Dizziness, dry mouth, rash, diarrhea, drowsiness, N/V, stomach pain, diarrhea, uric acid nephrolithiasis (large doses)

70
Q

Nasal decongestants MOA

A

Alpha adrenergic agonist (sympathomimetic) causing constriction of blood vessels throughout the body, reducing blood supply to nose, decreasing amount of blood in sinusoid vessels, decreasing mucosal edema.

71
Q

Nasal Decongestant Drugs

A

Pseudoephedrine (oral, systemic) - releases norepi from adrenergic nerves, phenylephrine (oral, systemic) - directly stimulates adrenergic receptors on postsynaptic sites; both have short half life

72
Q

Pseudoephedrine metabolism

A

metabolized to only a minor extant by N-demthylation to norpseudoephedrine

73
Q

Phenylephrine metabolism

A

rapid metabolism by MOA and COMT in GI mucosa, liver and other tissues

74
Q

Systemic Decongestants Adverse Effects

A

CV stimulation, CNS stimulation - more likely with children/elderly; causes rebound congestion due to ischemia

75
Q

Systemic decongestant Contras

A

hyperthyroidism, bradycardia, partial heart block, uncontrolled HTN, V Tach

76
Q

Oxymetazoline

A

Afrin; topical nasal spray; do not use for more than 3-5 days; preferred topical agent in pregnancy

77
Q

Levamfetamine

A

Inhaled decongestant - does not cause nasal rebound for 7 days

78
Q

Propylhexadrine

A

inhaled decongestant that is often abused via cotton plug ingestion or injection

79
Q

Mucolytics MOA

A

promote breakdown of mucus by breaking physical bonds within mucus

80
Q

Mucolytic uses

A

diseases with excessive production of mucus; cystic fibrosis, COPD, Bronchiectasis, Respiratory infections (TB)

81
Q

Facilitation of Mucus Clearance

A

Provide adequate hydration, remove causative factors, optimize tracheobronchial clearance, reduce inflammation

82
Q

Bromohexine

A

Secretolytic, increases the production of serous mucus in the respiratory tract and decreases the viscosity of phlegum

83
Q

Mucolytics - N-Acetyl Cysteine, Acetadote, Erdosteine, Carbocysteine MOA

A

break the bonds by substituting sulfhydryl radical thus breaking disulfide bonds within mucus; given by aerosol into ET tube; can be given orally to reduce liver injury due to Tylenol overdose

84
Q

Mucolytic Adverse Effects

A

Bronchospasm, increased mucus production, incompatible with antibiotics in nebulizer, N/V, bad odor due to hydrogen sulfide, must be used within 96 hrs.

85
Q

Sodium Bicarbonate

A

Used to increase the pH of mucus by weakening carbohydrate side chains, thus weaking polysaccharide chains; can be injected directly into the trachea

86
Q

Dornase Alfa (Pulmozyme)

A

clone of the natural human pancreatic DNase enzyme which digests extracellular DNA; it reduces the viscosity of secretions during an infection.

87
Q

Dornase Alfa Indications

A

Cystic fibrosis, chronic bronchitis, bronchiectasis - has no effect on non-infected sputum

88
Q

Dornase Alfa (pulmozyme) adverse effects

A

voice alteration, pharyngitis/laryngitis, rash, chest pain, conjuctivitis

89
Q

Pulmozyme Contras

A

patients hypersensitive to Chinese Hamster Ovary cell products

90
Q

Amiloride

A

diuretic that can be given by aerosol for pts with CF; Na channel blocker, preventing dehydration of the mucus

91
Q

Denufosol Tetrasodium

A

Enhances mucosal hydration and mucus clearance by activating Cl- secretion and inhibition ENa transport via activation of P2Y2 receptors; Fast track treatment for CF

92
Q

Barriers to TB treatment

A

slow growth, intracellular location, development of resistance, noncompliance, drug toxicity and interactions

93
Q

TB first line therapy

A

Isoniazide + Rifampin + Pyrazinamide + Ethambutol/Streptomycin

94
Q

M. Avium first line therapy

A

Clarithromycin + Ethambutol or Clofazimine or Ciprofloxacin or Amikacin

95
Q

Latent TB treatment schedule

A

Isoniazid for 9 months; Isoniazid for 6 months; Isoniazid and Rifapentine for 3 months once weekly (highest compliance); Rifampin daily for 4 months

96
Q

Patients who can’t have Isoniazid and Rifapentine

A

kids under 2; HIV infected pts because of drug interaction possibility; pregnant women; patients with presumed resistance to either drug

97
Q

Initial phase Active TB treatment

A

isoniazid, rifampin, pyrazinamide, and ethambutol for 8wks

98
Q

Continuation phase Active TB treatment

A

Daily or twice weekly isoniazid and Rifampin for 18 weeks; can drop Ethambutol once susceptibility to primary drugs is known

99
Q

Isoniazid MOA

A

inhibits cell wall synthesis by interfering with mycolic acid synthesis; tidal to rapidly dividing bacilli; static for slowing growing; penetrates host cells

100
Q

Ethambutol MOA

A

Disrupts cell wall synthesis by inhibiting arabinosyl transferase, disrupting arabinogalactan synthesis, leading to increased cell wall permeability; static effect, must have actively dividing bacilli, slow development of resistance, no cross resistance

101
Q

Pyrazinamide MOA

A

exact target unknown but disrupts plasma membrane and disrupts energy metabolism; converted to active agent by bacilli; decrease pH below threshold for bacterial growth; tidal/static concentration dependent; active against TB in acid environment of lysosome and macrophage

102
Q

Rifampin MOA

A

inhibits RNA synthesis by binding beta subunit of RNA polymerase; bacerticidal for intra or extra cellular mycobateria

103
Q

Isoniazid resistance

A

inability to take up the drug; alteration in target enzyme; overproduction of target enzyme; emerges rapidly when used alone so never use alone

104
Q

Isoniazid absorption,

A

rapidly absorbed from GI tract with oral dose; can also be given IM; half life of 1-4hrs

105
Q

Isoniazid distribution

A

all tissues and fluid; with inflamed meninges get therapeutic levels in CSF; crosses placenta and breast milk

106
Q

Isoniazid Metabolism

A

acetylated via N-acetyl transferase - fast/slow acetylators affect therapy; chronic liver disease will decrease metabolism; excreted in urine as drug and inactive metabolites

107
Q

Isoniazid Adverse Effects

A

Peripheral neuropathy (correct with Vit B6 supplement), Hepatotoxicity (dose related)

108
Q

Isoniazid Drug interactions

A

Antacids with Al3+ salts decrease absorption (split dosing), corticosteroids decrease efficacy, inhibits P450 isozyme that metabolizes phenytoin, diazepam, fluoxetine, nelfinavir, etc.

109
Q

Rifampin Resistance

A

lack of binding due to beta subunit alteration; never given alone due to rapid resistance

110
Q

Rifampin absorption

A

Well absorbed orally; impaired by food or para-aminosalicyclic acid

111
Q

Rifampin distribution

A

penetrates all tissues including CSF; 75-85% protein bound

112
Q

Rifampin Metabolism

A

Deacetylated in liver; excreted mainly in bile, small amount in renal tubules - no adjustment with renal insufficiency

113
Q

Rifampin Adverse Effects

A

Discolors body fluid (turns tears orange-red), GI disturbances and nervous system complaints, fever, chills, aches; Hepatotoxicity (jaundice with liver disease, especially slow acetylators)

114
Q

Rifampin Interactions

A

Induction of CYP450 - reduces half life of drugs metabolized by this system (prednisone, Propanodol, sulfamides, dapsone, ketoconazole, HIV protease inhibitors, NNRTIS, etc); makes anticoagulants and oral contraceptives less effective; Probenecid increases serum levels of Rifampin when taken concurrently

115
Q

Rifampin Uses

A

first line TB treatment; MRSA w/ Vancomycin; prophylaxis for people exposed meningococci or H flu.; most active antileprosy drug

116
Q

Ethambutol Absorption and Distribution

A

Absorbed orally; distributed widely with concentrated areas in kidneys, lungs, saliva; therapeutic levels in CSF, crosses placenta, distribute in breast milk;

117
Q

Ethambutol Elimination

A

Partially metabolized in liver; excreted in urine; half like of 3.5hr that extends up to 15hr with renal disease so reduce dose if renal dysfunction

118
Q

Ethambutol Adverse Effects

A

Optic neuritis (decreased visual acuity and color discrimination, constriction of visual fields) - dose related and reversible, allergic reactions, increase in serum irate (hyperuricemia - may be increased by INH and Pyridoxine)

119
Q

Ethambutol Interactions

A

Al3+ containing antacids reduce absorption (split dose timing)

120
Q

Pyrazinamide Distribution and Metabolism

A

Absorbed rapidly from GI tract; distributed widely including CSF and breast milk (undocumented about placenta); eliminated after being hydrolyzed by liver active metabolite

121
Q

Pyrazinamide Adverse Effects

A

Dose related hepatoxicity; mild non gout related arthralgias; hyperuricemia due to inhibition of irate excretion - usually asymptomatic

122
Q

Multidrug resistant TB (MDR TB)

A

TB that is resistant to Isoniazid and Rifampin

123
Q

Cycloserine

A

used for MDR TB for active TB, Mycobacterium avium, and UTIs

124
Q

Cycloserine MOA

A

blocks cell wall synthesis, structural analog to D-alanine so blocks enzymes required for D alanine incorporation into pentapeptide of peptidoglycan strands; cidal/static conc dependent; effective in resistant organisms; shows no cross resistance

125
Q

Cycloserine Absorption, Distribution and Excretion

A

Absorbed orally; distributed widely not protein bound to lung, pleural/synovial fluids, CSF, placenta, breast milk; excreted unchanged renal mech - requires dose adjustment with renal issues

126
Q

Cycloserine Adverse Effects

A

CNS issues that are reversible with discontinuation of medication; HA, tremor, vertigo, confusion, psychosis with suicidal ideation, paranoia, seizures (increase with alcohol use)

127
Q

Cycloserine Contras

A

History of epilepsy

128
Q

Ethionamide

A

inhibits peptide synthesis (similar to Isoniazid with different MOA), oral drug, widely distributed, hepatic metabolism, conc dependent static/cidal, last line therapy due to GI, neuro, Hepto toxicity; resistance develops when used alone; Pyridoxine relieves neuro issues

129
Q

Extensive Drug Resistant TB (XDRTB)

A

does not respond to INH, RIF, and the second line drugs; requires 2 years of extensive drug treatment

130
Q

Capreomycin

A

unknown MOA, bacteriostatic, IM administration; nephrotoxic (proteinuria, cylinduria, nitrogen retention), ototoxic (hearing loss, tinnitus, vestibular disturbances); resistance when used alone; effective in MDRTB; last resort drug

Pulmonary Block (8 decks)

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