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Pharmacology Exam III > Medications Individual > Flashcards

Medications Individual Flashcards

1
Q

Albuterol

A

Short Acting Beta Agonist (SABA) - bronchodilator

MOA: relax airway smooth muscle by direct stimulation of B2 receptors in airway; increase clearance and transport of mucus in airways; stabilize mast cell membranes

AE: tachycardia, tremor, hypokalemia, palpitations, sleep disturbances (more likely in high dose LABAs)

  • most effective agent for reversing acute airway obstruction caused by bronchoconstriction
  • best at bronchodilating
  • 1st line for acute asthma, chronic asthma symptoms, and preventing exercise induced bronchospasm
  • used for rescue prn use in COPD
  • onset 5 min
  • dosed 1-2 puffs per 4-6 hrs
  • delivery: inhaler or nebulizer
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2
Q

Lebalbuterol

A

Short Acting Beta Agonist (SABA) - bronchodilator

  • marketed as having fewer side effects as and being more effective than Albuterol, but they are equal
  • R-enantiomer of albuterol

MOA: relax airway smooth muscle by direct stimulation of B2 receptors in airway; increase clearance and transport of mucus in airways; stabilize mast cell membranes

AE: tachycardia, tremor, hypokalemia, palpitations, sleep disturbances (more likely in high dose LABAs)

  • most effective agent for reversing acute airway obstruction caused by bronchoconstriction
  • best at bronchodilating
  • 1st line for acute asthma, chronic asthma symptoms, and preventing exercise induced bronchospasm
  • used for rescue prn use in COPD
  • onset 5 min
  • dosed 1-2 puffs per 4-6 hrs
  • delivery: inhaler or nebulizer
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3
Q

Terbutaline

A

Short Acting Beta Agonist (SABA) - bronchodilator

MOA: relax airway smooth muscle by direct stimulation of B2 receptors in airway; increase clearance and transport of mucus in airways; stabilize mast cell membranes

AE: tachycardia, tremor, hypokalemia, palpitations, sleep disturbances (more likely in high dose LABAs)

  • most effective agent for reversing acute airway obstruction caused by bronchoconstriction
  • best at bronchodilating
  • 1st line for acute asthma, chronic asthma symptoms, and preventing exercise induced bronchospasm
  • used for rescue prn use in COPD
  • onset 5 min
  • dosed 1-2 puffs per 4-6 hrs
  • delivery: inhaler or nebulizer
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4
Q

Salmeterol

A

Long Acting Beta Agonist (LABA) - bronchodilator

MOA: relax airway smooth muscle by direct stimulation of B2 receptors in airway; increase clearance and transport of mucus in airways; stabilize mast cell membranes

AE: tachycardia, tremor, hypokalemia, palpitations, sleep disturbances (more likely in high dose LABAs)

  • NOT FOR MONOTHERAPY IN CHRONIC ASTHMA- increased risk of severe exacerbation and death
  • many in combination with ICS
  • 12-24 hr duration; decrease to 5 hr in chronic use
  • Onset: salmeterol – 30 min
  • delivery: inhaler (alone or w/ ICS) or nebulizer
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5
Q

Formeterol

A

Long Acting Beta Agonist (LABA) - bronchodilator

MOA: relax airway smooth muscle by direct stimulation of B2 receptors in airway; increase clearance and transport of mucus in airways; stabilize mast cell membranes

AE: tachycardia, tremor, hypokalemia, palpitations, sleep disturbances (more likely in high dose LABAs)

  • NOT FOR MONOTHERAPY IN CHRONIC ASTHMA- increased risk of severe exacerbation and death
  • many in combination with ICS
  • 12-24 hr duration; decrease to 5 hr in chronic use
  • Onset:formoterol – 5 min (not approved for SABA)
  • delivery: inhaler (alone or w/ ICS) or neb
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6
Q

Indacaterol

A

Long Acting Beta Agonist (LABA) - bronchodilator

MOA: relax airway smooth muscle by direct stimulation of B2 receptors in airway; increase clearance and transport of mucus in airways; stabilize mast cell membranes

AE: tachycardia, tremor, hypokalemia, palpitations, sleep disturbances (more likely in high dose LABAs)

  • NOT FOR MONOTHERAPY IN CHRONIC ASTHMA- increased risk of severe exacerbation and death
  • longer lasting
  • many in combination with ICS
  • 12-24 hr duration; decrease to 5 hr in chronic use
  • delivery: inhaler (alone or w/ ICS) or nebulizer
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7
Q

Olodaterol

A

Long Acting Beta Agonist (LABA) - bronchodilator

MOA: relax airway smooth muscle by direct stimulation of B2 receptors in airway; increase clearance and transport of mucus in airways; stabilize mast cell membranes

AE: tachycardia, tremor, hypokalemia, palpitations, sleep disturbances (more likely in high dose LABAs)

  • NOT FOR MONOTHERAPY IN CHRONIC ASTHMA- increased risk of severe exacerbation and death
  • longer lasting
  • many in combination with ICS
  • 12-24 hr duration; decrease to 5 hr in chronic use
  • delivery: inhaler (alone or w/ ICS) or nebulizer
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8
Q

Vilanterol

A

Long Acting Beta Agonist (LABA) - bronchodilator

MOA: relax airway smooth muscle by direct stimulation of B2 receptors in airway; increase clearance and transport of mucus in airways; stabilize mast cell membranes

AE: tachycardia, tremor, hypokalemia, palpitations, sleep disturbances (more likely in high dose LABAs)

  • NOT FOR MONOTHERAPY IN CHRONIC ASTHMA- increased risk of severe exacerbation and death
  • longer lasting
  • many in combination with ICS
  • 12-24 hr duration; decrease to 5 hr in chronic use
  • delivery: inhaler (alone or w/ ICS) or nebulizer
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9
Q

Arformoterol

A

Long Acting Beta Agonist (LABA) - bronchodilator

MOA: relax airway smooth muscle by direct stimulation of B2 receptors in airway; increase clearance and transport of mucus in airways; stabilize mast cell membranes

AE: tachycardia, tremor, hypokalemia, palpitations, sleep disturbances (more likely in high dose LABAs)

  • NOT FOR MONOTHERAPY IN CHRONIC ASTHMA- increased risk of severe exacerbation and death
  • longer lasting
  • many in combination with ICS
  • 12-24 hr duration; decrease to 5 hr in chronic use
  • delivery: inhaler (alone or w/ ICS) or nebulizer
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10
Q

Ipratropium bromide

A

Inhaled Anticholinergics

MOA: anti-inflammatory; inhibit the effects of acetylcholine on muscarinic receptors in airways = causes bronchodilation; protect against cholinergic-mediated bronchoconstriction; may decrease mucus secretion

AE: dry mouth; blurred vision, urinary retention, metallic taste, constipation, tachycardia, precipitation of narrow-angle glaucoma, urinary retention, increased CV events

CI: cardiovascular disease

  • delivery: inhaler and nebulizer (ipratropium)
  • onset: ipratropium – 15 min (too slow for rescue med; tiotropium – 30 min; aclidinium < 30 min
  • duration: ipratropium 4-8 hrs
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11
Q

Tiotropium bromide

A

Inhaled Anticholinergics

MOA: anti-inflammatory; inhibit the effects of acetylcholine on muscarinic receptors in airways = causes bronchodilation; protect against cholinergic-mediated bronchoconstriction; may decrease mucus secretion

AE: dry mouth; blurred vision, urinary retention, metallic taste (ipratropium), constipation, tachycardia, precipitation of narrow-angle glaucoma, urinary retention

CI: cardiovascular disease

    • longer lasting
  • delivery: inhaler
  • onset: tiotropium – 30 min
  • duration: tiotropium > 24 hr
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12
Q

Aclidinium bromide

A

Inhaled Anticholinergics

MOA: anti-inflammatory; inhibit the effects of acetylcholine on muscarinic receptors in airways = causes bronchodilation; protect against cholinergic-mediated bronchoconstriction; may decrease mucus secretion

AE: dry mouth; blurred vision, urinary retention, constipation, tachycardia, precipitation of narrow-angle glaucoma, urinary retention, increased CV events

CI: cardiovascular disease

  • delivery: inhaler
  • onset: aclidinium < 30 min
  • duration: aclidinium < 24 hrs
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13
Q

Umeclidinium bromide

A

Inhaled Anticholinergics

MOA: anti-inflammatory; inhibit the effects of acetylcholine on muscarinic receptors in airways = causes bronchodilation; protect against cholinergic-mediated bronchoconstriction; may decrease mucus secretion

AE: dry mouth; blurred vision, urinary retention, constipation, tachycardia, precipitation of narrow-angle glaucoma, urinary retention, increased CV events

CI: cardiovascular disease

    • longer lasting
  • delivery: inhaler
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14
Q

Glycopyrrolate

A

Inhaled Anticholinergics

MOA: anti-inflammatory; inhibit the effects of acetylcholine on muscarinic receptors in airways = causes bronchodilation; protect against cholinergic-mediated bronchoconstriction; may decrease mucus secretion

AE: dry mouth; blurred vision, urinary retention, constipation, tachycardia, precipitation of narrow-angle glaucoma, urinary retention, increased CV events

CI: cardiovascular disease

  • delivery: inhaler
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15
Q

Theophyline

A

Methylxanthines

MOA: anti-inflammatory and causes bronchodilation by inhibiting phosphodiesterase and antagonizing adenosine; act as a bronchodilator at high concentrations; anti-inflammatory effect at low concentrations

AE: heartburn, restlessness, insomnia, irritability, tachycardia, tremor; with increased dose: nausea, vomiting, seizures, arrhythmias

Target Serum Concentration: 5-15 mg/L
<10 little bronchodilation (more anti-inflammatory)
10-20 bronchodilation
> 15 increased adverse effects (headache, nausea, vomiting, insomnia)
> 20 more serious AE (cardiac arrhythmias, seizures)

CI: many drug interactions (metabolized by CYP1A2, CYP2W1, and CYP3A4) – alcohol, ciprofloxacin, diltiazem, erythromycin, oral contraceptives, phenytoin, propranolol, verapamil

  • narrow therapeutic index; life-threatening toxicity
  • only for pts who cannot use inhaled meds or if symptomatic despite appropriate use of inhaled meds
  • non-linear pharmacokinetics: drug changes, drug interactions, hepatic function, tobacco increases clearance (smokers need higher dose)
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16
Q

Beclomethasone

A

Inhaled Corticosteroids

MOA: decrease airway inflammation, attenuate airway hyperresponsiveness, minimize mucus production/secretion, improve response to beta 2 agonists

AE: local: oralpharyngeal candidiasis (thrush); cough; dysphonia (hoarse voice; decreases with decreased dose); systemic: reduced linear growth (1/2 cm per year), increased pneumonia

CI: potent CYP34A inhibitors (ritonavir, itraconazole, ketoconazole, etc) + high doses of ICS causes Cushing syndrome and adrenal insufficiency

  • smoking decrease response – need higher dose
  • onset: 12 hours; 2+ weeks for max effect
  • many used in combination with LABAs
  • variability in response: age, genetics, smoking (need higher dose), race
  • abrupt discontinuation leads to exacerbations
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17
Q

Budesonide

A

Inhaled Corticosteroids

MOA: decrease airway inflammation, attenuate airway hyperresponsiveness, minimize mucus production/secretion, improve response to beta 2 agonists

AE: local: oralpharyngeal candidiasis (thrush); cough; dysphonia (hoarse voice; decreases with decreased dose); systemic: reduced linear growth (1/2 cm per year), increased pneumonia

CI: potent CYP34A inhibitors (ritonavir, itraconazole, ketoconazole, etc) + high doses of ICS causes Cushing syndrome and adrenal insufficiency

  • smoking decrease response – need higher dose
  • onset: 12 hours; 2+ weeks for max effect
  • many used in combination with LABAs
  • variability in response: age, genetics, smoking (need higher dose), race
  • abrupt discontinuation leads to exacerbations
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18
Q

Ciclesonide

A

Inhaled Corticosteroids

MOA: decrease airway inflammation, attenuate airway hyperresponsiveness, minimize mucus production/secretion, improve response to beta 2 agonists

AE: local: oralpharyngeal candidiasis (thrush); cough; dysphonia (hoarse voice; decreases with decreased dose); systemic: reduced linear growth (1/2 cm per year), increased pneumonia

CI: potent CYP34A inhibitors (ritonavir, itraconazole, ketoconazole, etc) + high doses of ICS causes Cushing syndrome and adrenal insufficiency

  • smoking decrease response – need higher dose
  • onset: 12 hours; 2+ weeks for max effect
  • many used in combination with LABAs
  • variability in response: age, genetics, smoking (need higher dose), race
  • abrupt discontinuation leads to exacerbations
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19
Q

Flunisolide

A

Inhaled Corticosteroids

MOA: decrease airway inflammation, attenuate airway hyperresponsiveness, minimize mucus production/secretion, improve response to beta 2 agonists

AE: local: oralpharyngeal candidiasis (thrush); cough; dysphonia (hoarse voice; decreases with decreased dose); systemic: reduced linear growth (1/2 cm per year), increased pneumonia

CI: potent CYP34A inhibitors (ritonavir, itraconazole, ketoconazole, etc) + high doses of ICS causes Cushing syndrome and adrenal insufficiency

  • smoking decrease response – need higher dose
  • onset: 12 hours; 2+ weeks for max effect
  • many used in combination with LABAs
  • variability in response: age, genetics, smoking (need higher dose), race
  • abrupt discontinuation leads to exacerbations
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20
Q

Fluticasone

A

Inhaled Corticosteroids

MOA: decrease airway inflammation, attenuate airway hyperresponsiveness, minimize mucus production/secretion, improve response to beta 2 agonists

AE: local: oralpharyngeal candidiasis (thrush); cough; dysphonia (hoarse voice; decreases with decreased dose); systemic: reduced linear growth (1/2 cm per year), increased pneumonia

CI: potent CYP34A inhibitors (ritonavir, itraconazole, ketoconazole, etc) + high doses of ICS causes Cushing syndrome and adrenal insufficiency

  • smoking decrease response – need higher dose
  • onset: 12 hours; 2+ weeks for max effect
  • many used in combination with LABAs
  • variability in response: age, genetics, smoking (need higher dose), race
  • abrupt discontinuation leads to exacerbations
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21
Q

Mometasone

A

Inhaled Corticosteroids

MOA: decrease airway inflammation, attenuate airway hyperresponsiveness, minimize mucus production/secretion, improve response to beta 2 agonists

AE: local: oralpharyngeal candidiasis (thrush); cough; dysphonia (hoarse voice; decreases with decreased dose); systemic: reduced linear growth (1/2 cm per year), increased pneumonia

CI: potent CYP34A inhibitors (ritonavir, itraconazole, ketoconazole, etc) + high doses of ICS causes Cushing syndrome and adrenal insufficiency

  • smoking decrease response – need higher dose
  • onset: 12 hours; 2+ weeks for max effect
  • many used in combination with LABAs
  • variability in response: age, genetics, smoking (need higher dose), race
  • abrupt discontinuation leads to exacerbations
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22
Q

Prednisone

A

Systemic (oral) Corticosteroids

MOA: decrease airway inflammation, attenuate airway hyperresponsiveness, minimize mucus production/secretion, improve response to beta 2 agonists

AE: adrenal suppression, decreased bone mineral density, skin thinning, cataracts, easy bruising, steroid myopathy, insomnia, increased appetite, agitation/ irritation; weight gain (longer term)

  • used in acute exacerbation of asthma of asthma or COPD; only used longer-term in serious cases
  • onset: 4-12 hours; start early in exacerbation, continue for 3-10 days
  • taper only necessary if used long-term
  • avoid long-term use
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23
Q

Prednisolone

A

Systemic (oral) Corticosteroids

MOA: decrease airway inflammation, attenuate airway hyperresponsiveness, minimize mucus production/secretion, improve response to beta 2 agonists

AE: adrenal suppression, decreased bone mineral density, skin thinning, cataracts, easy bruising, steroid myopathy, insomnia, increased appetite, agitation/ irritation; weight gain (longer term)

  • used in acute exacerbation of asthma of asthma or COPD; only used longer-term in serious cases
  • onset: 4-12 hours; start early in exacerbation, continue for 3-10 days
  • taper only necessary if used long-term
  • avoid long-term use
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24
Q

Methyprednisolone

A

Systemic (oral) Corticosteroids

MOA: decrease airway inflammation, attenuate airway hyperresponsiveness, minimize mucus production/secretion, improve response to beta 2 agonists

AE: adrenal suppression, decreased bone mineral density, skin thinning, cataracts, easy bruising, steroid myopathy, insomnia, increased appetite, agitation/ irritation; weight gain (longer term)

  • used in acute exacerbation of asthma of asthma or COPD; only used longer-term in serious cases
  • onset: 4-12 hours; start early in exacerbation, continue for 3-10 days
  • taper only necessary if used long-term
  • avoid long-term use
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25
Q

Montelukast

A

Leukotriene Receptor Antagonist

MOA: anti-inflammatory; act to antagonize the leukotriene receptor; improve FEV1, decrease asthma symptoms, decreased SABA use, decrease asthma exacerbations, steroid sparing

AE: - generally few (esp. Montelukast); sleep disorders, aggressive behavior, suicidal thoughts, eosinophilic granulomatosis with polyangiitis (rare), angioedema, urticartia

CI: CYP2C9 drugs

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26
Q

Zileuton

A

Leukotriene Receptor Antagonist

Expensive!

MOA: anti-inflammatory; act to antagonize the leukotriene receptor; improve FEV1, decrease asthma symptoms, decreased SABA use, decrease asthma exacerbations, steroid sparing

AE: - generally few; hepatotoxicity, sleep disorders, aggressive behavior, suicidal thoughts, eosinophilic granulomatosis with polyangiitis (rare), angioedema, urticartia

CI: CYP2C9 drugs (significant)

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27
Q

Zafirlukast

A

Leukotriene Receptor Antagonist

MOA: anti-inflammatory; act to antagonize the leukotriene receptor; improve FEV1, decrease asthma symptoms, decreased SABA use, decrease asthma exacerbations, steroid sparing

AE: - generally few; hepatotoxicity, sleep disorders, aggressive behavior, suicidal thoughts, eosinophilic granulomatosis with polyangiitis (rare), angioedema, urticartia

CI: CYP2C9 drugs (significant)

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28
Q

Omalizumab

A

Immunomodulator

MOA: anti-inflammatory; inhibits binding of IgE to receptors on mast cells and basophils; results in inhibition of inflammatory mediator release/attenuation of early and late phase allergic response

AE: injection site reactions: bruising, redness, pain, stinging, itching, burning; anaphylactic reactions (monitor after injection; give epinephrine prescription); increased risk of CV events and cancer?

  • subcutaneous q2-4 weeks in office/clinic
  • expensive
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29
Q

Roflumilast

A

Phosphodiesterase-4 Inhibitor

MOA: reduce inflammation by inhibiting breakdown of cAMP - do not cause direct bronchodilation; used for preventing COPD exacerbations or for select chronic bronchitis patients

AE: much more likely than other meds; diarrhea, weight loss, nausea, headache, insomnia, decreased appetite, abdominal pain, anxiety, depression, increased suicidality

Interaction: theophylline (both inhibit PDE-4)

  • very expensive
  • little effect on symptoms and quality of life
    modest benefit in lung function and preventing exacerbations
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30
Q

Cromolyn

A

broncodilator

MOA: decrease bronchospasm through anti-inflammatory effect

  • not much benefit over placebo
  • less effective and less cost effective than ICS
  • reserved for pts who cannot tolerate ICS
  • 2nd line therapy for exercise induced asthma
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31
Q

Nicotine Gum

A

Nicotine Replacement Product

  • provides nicotine at a fixed dose; used prn for cravings

AE: irritation in the mouth, sore jaw, hiccups, stomach discomfort

Avoid with Dentures

  • OTC
  • chew gum until it tingles; park it in the cheek until tingling subsides, repeat until gum no longer tingles
  • do not eat or drink 30 min after use
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32
Q

Nicotine Inhaler

A

Nicotine Replacement Product

AE: irritation of mouth and throat, mild coughing, stomach discomfort

  • prescription/expensive
33
Q

Nicotine Lozenge

A

Nicotine Replacement Product

AE: irritation of mouth and throat, sore throat, stomach discomfort

  • OTC
  • dissolve in mouth, do not eat or drink 30 minutes after use
  • contains 25% more nicotine than gum
34
Q

Nicotine Nasal Spray

A

Nicotine Replacement Product

AE: irritation in the nasal passages and throat, runny nose

  • prescription/expensive
35
Q

Nicotine Patch

A

Nicotine Replacement Product

AE: rash where the patch is placed, trouble sleeping

  • can be worn 24 hrs per day; reduces cravings, but doesn’t take them away; can be used in combination with prn nicotine replacement
  • OTC and prescription
  • 8-week treatment; longer has no added benefit
  • change patch q24 hrs
  • remove patch at night if insomnia or weird dreams
36
Q

Bupropion SR

A

Smoking Cessation Medication

MOA: antidepressant; blocks reuptake of dopamine and NE

AE: dry mouth, insomnia, lowers seizure threshold, may increase suicidality, esp. in adolescents/young adults

  • cardiotoxic at high doses; widens QRS complex (caution with CVD)

CI: history of seizures or eating disorders (reduces appetite), use of monoamine oxidase within 14 days (risk hypertensive reactions)

DI: MAO-Is; drugs that lower seizure threshold (antipsychotics, antidepressants, theophylline, systemic corticosteroids)

  • can combine with NRT
  • may benefit in pts w/ history of depression
  • not 1st line for adolescents
  • doubles odds of smoking cessation compared to placebo
  • caution with CVD with immediate post MI or with serious symptoms or worsening angina
37
Q

Varenicline

A

Smoking Cessation Medication

MOA: nicotinic receptor partial agonist and antagonist; reduces cravings/withdrawal and blocks effects of smoked nicotine

AE: - insomnia, nausea, increased risk of CV events; neuropsychiatric symptoms: changes in behavior, hostility, agitation, depressed mood, suicidal thoughts and behavior, attempted suicide (MONITOR)

  • monotherapy; DO NOT combine with NRT or bupropion
  • works better than bupropion
  • begin 1 week before quit date and continue for 12-24 wks
  • caution with CVD with immediate post MI or with serious symptoms or worsening angina
38
Q

Methotrexate

A

Conventional Disease Modifying Antirheumatic Drugs

MOA: inhibits dihydrofolate reductase, which causes inhibition of inflammatory factors

AE: nausea, diarrhea, hepatotoxicity, alopecia (hair loss), new onset cough or SOB, myelosuppression

Methotrexate Toxicity (reduced folic acid) – dihydrofolate reductase coverts FH2 to active FH4; methotrexate prevents active folic acid; supplement with 1 gram folic acid; Leucovorin rescue for cancer treatment pts; signs: stomatitis, diarrhea, nausea, alopecia, myelosuppression, elevations in LFTs

CI: hepatic impairment, alcohol (increased liver damage risk), pregnancy (even if intended, men and women)

  • adjust dose in renal impairment
  • pregnancy – spontaneous abortion, myelosuppression, limb defects, CNS abnormalities); discontinue 3 months before trying to get pregnant
  • first-line RA treatment
  • must give folic acid supplements to prevent toxicity
  • IM, po, or subcutaneously
  • monitor: CBC, creatine, LFTs ever 6-8 weeks, signs of infection
39
Q

Hydroxychloroquine

A

Conventional Disease Modifying Antirheumatic Drugs

MOA: unknown; modify disease process and prevent/reduce joint damage

AE: - nausea, diarrhea, headache, vision changes (monitor yearly eye exam), skin pigmentation

  • OKAY TO USE WITH: renal, hepatic, or bone marrow suppression
  • slow onset; must use for 6 mo before determining if effective
  • can combine with either or both methotrexate for RA
  • oral
40
Q

Sulfasalazine

A

Conventional Disease Modifying Antirheumatic Drugs

MOA: unknown; modify disease process and prevent/reduce joint damage

AE: - nausea, abdominal discomfort, diarrhea (start low, go slow); leukopenia/ myelosuppression (routine blood work); rash, yellow-orange discoloration, photosensitivity (use sunscreen)

CI: sulfa-allergy

  • avoid: hepatic impairment
  • adjust dose in renal impairment
  • monitor: CBC every 2-4 wks for 3 months, then every 3 months
  • slow onset; must use for 6 mo before determining if effective
  • can combine with either or both methotrexate for RA
  • oral
  • drug of choice for pregnancy
41
Q

Leflunomide

A

Conventional Disease Modifying Antirheumatic Drugs

MOA: inhibits t-lymphocyte response which halts inflammatory cascade

AE: hepatotoxicity (higher risk if used in combo with methotrexate)

  • if need abrupt d/c (pregnancy or toxicity), use cholestyramine to speed removal from body
  • similar efficacy to moderate methotrexate or sulfasalazine doses
  • long half- life: start with loading dose and follow with maintenance dose
  • can use with methotrexate
42
Q

Infliximab

A

Brand Name: Remicade

TNF Antagonists (Biological DMARDs)

MOA: prevent action of TNF, causing a reduction in inflammation

AE: mouse antibody – infusion related reaction (monitor); rash, urticaria, flushing, headache, fever, chills, nausea; temporarily d/c, slow infusion rate; pre-treat with corticosteroids/
antihistamines if reactions are common

  • also used in Crone’s, ulcerative colitis, ankylosing spondylitis
  • screen for TB; could reactivate
  • screen for hepatitis
  • avoid in pts with serious infections, demyelinating disorders, hepatitis, and heart failure
  • ONLY IV
43
Q

Adalimumab

A

Brand Name: Humira

TNF Antagonists (Biological DMARDs)

MOA: prevent action of TNF, causing a reduction in inflammation

AE: injection site reaction (rotate sites, topical corticosteroids, antipruritics, analgesics, rotate site)

  • monitor signs of infection
  • give subcutaneously or IV
  • screen for TB and hepatitis; could reactivate
  • avoid in pts with serious infections, demyelinating disorders, hepatitis, and heart failure
44
Q

Golimumab

A

Brand Name: Simponi

TNF Antagonists (Biological DMARDs)

MOA: prevent action of TNF, causing a reduction in inflammation

AE: injection site reaction (rotate sites, topical corticosteroids, antipruritics, analgesics, rotate site); IV infusion reaction
- monitor signs of infection

  • give subcutaneously or IV
  • screen for TB; could reactivate
  • screen for hepatitis
  • avoid in pts with serious infections, demyelinating disorders, hepatitis, and heart failure
45
Q

Etanercept

A

Brand Name: Enbrel

TNF Antagonists (Biological DMARDs)

MOA: prevent action of TNF, causing a reduction in inflammation

  • screen for TB; could reactivate
  • screen for hepatitis
  • avoid in pts with serious infections, demyelinating disorders, hepatitis, and heart failure
  • SubQ or IV
46
Q

Certolizumab

A

Brand Name: Cimzia

TNF Antagonists (Biological DMARDs)

MOA: prevent action of TNF, causing a reduction in inflammation

  • screen for TB; could reactivate
  • screen for hepatitis
  • avoid in pts with serious infections, demyelinating disorders, hepatitis, and heart failure
  • SubQ or IV
47
Q

Abatacept

A

Brand Name: Orencia

Costimulation Modulator (Biological DMARD)

MOA: blocks T cell signaling and activation (prevents inflammatory response)

AE: headache, infection, infusion reaction, injection site reaction

  • IV or subcutaneous
  • monitor infection
  • monotherapy or combo therapy after inadequate response of methotrexate and/or anti- TNF
  • avoid in pts with serious infections, demyelinating disorders, and hepatitis
48
Q

Rituximab

A

Brand Name: Rituxan

Anti-CD20 Monoclonal Antibody (Biological DMARD)

MOA: causes B lymphocyte depletion in bone marrow and synovial tissue

AE: Black Box – fatal infusion reactions, severe mucocutaneous reactions; injection adverse reactions

  • better response if rheumatoid factor positive RA
  • also used in non-RA conditions
  • IV
  • monitor infection
  • avoid in pts with serious infections, demyelinating disorders, and hepatitis
49
Q

Tocilizumab

A

Brand Name: Actemra

Anti-interleukin-6 Receptor Antibody (Biological DMARD)

MOA: blocks interleukin-6, which is implicated in joint damage and disease activity in anemia

AE: elevated LFTs, cholesterol, triglycerides, HDL; nasopharyngitis, infection

  • monitor infection, LFTs
  • IV, subcutaneous
50
Q

Tofacitinib

A

Brand Name: Xeljanz

Targeted Synthetic DMARD

MOA: inhibits specific kinases

AE: infection, headache, hypertension, elevated LFTs, diarrhea, worsening lipids

  • adjust dose if renal or hepatic impairment
  • oral; good choice for patients who prefer oral meds
  • monitor CBC, hemoglobin, lipids, LFTs, infection
51
Q

Acetaminophen

A
  • used for pain and fever

MOA: centrally acting analgesic and antipyretic with minimal anti-inflammatory properties

  • generally well tolerated
  • renal toxicity (may worsen kidney function), hepatic toxicity, GI upset)
  • caution with stable chronic liver disease (monitor)
  • Acetaminophen Toxicity – leading cause of acute liver injury; be cautious of meds that have APAP combo
  • Signs of Acute APAP OD (200 mg/kg or 10 g): abdominal pain, elevation of ALT and AST about 24 hr after ingestion (peak 2-3 days after), liver failure, renal injury, coma, hyperglycemia, lactic acidosis, death (if serum conc of APA > 500 mcg/mL)
  • Signs of Chronic Supratherapeutic OD (over 4 g/day): ALT elevation, malaise, N/V, abdominal pain, hepatotoxicity, jaundice, hypoglycemia, coagulopathy, renal failure, fulminant hepatic failure, encephalopathy, death
  • Mild/moderate toxicity: obtain APAP conc, start acetylcysteine if risk of hepatic injury (>200 mg/kg ingested, > 10g ingested, if conc can’t be measured, or >150 mcg/mL 4 hrs post ingestion)
  • Severe toxicity: if pt presents >36 hours after ingestion (greater injury/failure), proved emergency care prn (intubation, fresh frozen plasma, vasopressors, dialysis, airway management, fluid resuscitation); acetylcysteine if hepatic injury
  • avoid alcohol
  • use for mild-to-moderate pain in general
  • can be combined with NSADS
  • effective, inexpensive, favorable risk-benefit profile
  • same efficacy as NSAIDs
  • OTC, generally taken prn, but can be scheduled
  • max daily dose 4000mg per day or less; max dose 1000mg or less – toxicity (know)
  • onset within 1 hour
  • one of the safest analgesics; preferred for patients with hypertension of kidney failure
52
Q

Aspirin

A

NSAID - Nonselective

MOA: has analgesic (aspirin not advised for pain) and antipyretic activities by blocking COX1 and COX2, which causes inhibition of prostaglandins

  • COX1 = gastric mucosa (increase mucus, bicarb), kidney (dilate afferent arteriole), platelets (promote normal function)
  • COX 2 – normally undetectable, but increases at sites of inflammation and local tissue injury

AE:
- Salicylism: toxic syndrome that occurs due to excessive doses of aspirin, salicylic acid, or consumption of oil of wintergreen (5mL); mixed respiratory alkalosis and metabolic acidosis (anion gap); can occur due to acute overdose or chronic overdose; signs: severe headache, nausea, vomiting, tinnitus, confusion, increased pulse, increased respiratory rate; can progress to seizures, coma, cerebral/pulmonary edema, death; treatment: urine alkalization (sodium bicarb), hemodialysis, emergency care prn

  • GI (COX1 related; add gastroprotection to nonselective NSAID or use lower GI risk NSAID: celecoxib), renal insufficiency (drink water), hepatic dysfunction, increased cardiovascular risk (COX2 related), CNS effects, increased blood pressure, fluid retention, rarely cause tubulointerstitial nephropathy renal papillary necrosis
  • COX 1 related: adverse effects on gastric mucosa – asymptomatic gastric and duodenal mucosal ulceration (15-45%); direct irritant effect on GI (10-60%) – nausea, dyspepsia, anorexia, abdominal pain, flatulence, diarrhea; perforation, gastric outlet obstruction, GI bleeding (1.5-4%)
  • COX2 related: degree of COX2 selectivity dictates CV risk; celecoxib (selective COX2 inhibitor) has strongest association with CV events; diclofenac and ibuprofen have strong association with CV events

CI:
- at risk/current peptic ulcers or GI risk; bleeding risk; renal insufficiency, uncontrolled hypertension, heart failure, caution if NSAID/aspirin sensitive asthma

  • caution women of childbearing age/pregnant women: risk of fetal bleeding; possible CI – some potential association with miscarriage in 1st trimester; CI after 30 wks (3rd trimester); may promote premature closure of ductus arteriosus in fetus
  • renal insufficiency; esp in chronic renal insufficiency, LV dysfunction, elderly, diuretics, RAAS drugs; causes decreased glomerular filtration, hyperkalemia, sodium/water retention
  • interaction: aspirin, warfarin, oral hypoglycemic, antihypertensives, lithium, other drugs that bind to proteins, drugs that affect renal efficiency, drugs that have antiplatelet activity (monitor efficacy and AE)
  • use for mild-moderate pain in general
  • can be combined with APAP
  • OTC
  • oral
  • similar APAP efficacy
  • onset of pain relief = 1 hr
  • onset of inflammatory response = 2-3 wks of continuous therapy
53
Q

Solsalate

A

NSAID - Nonselective

54
Q

Etodolac

A

NSAID - Nonselective

55
Q

Diclofenac

A

NSAID - Nonselective

topical; minimizes systemic exposure; only for superficial joints (dosing depends on joint); gel solution or patch

AE – NSAID specific AE are low; application site dermatitis, pruritus, phototoxicity

high association with CV events

56
Q

Indomethacin

A

NSAID - Nonselective

57
Q

Nabumetone

A

NSAID - Nonselective

58
Q

Ibuprofen

A

NSAID - Nonselective

59
Q

Naproxen

A

NSAID - Nonselective

OTC

lowest CV risk and low GI risk

60
Q

Meloxicam

A

NSAID - Nonselective

61
Q

Prioxicam

A

NSAID - Nonselective

62
Q

Sulindac

A

NSAID - Nonselective

63
Q

Kerorolac

A

NSAID - Nonselective

-strong NSAID

CI: CV disease, GI risk, peptic ulcer risk, advanced renal impairment, high bleeding risk, contaminant NSAIDs; short term only (max 5 days); only for adults; initiate in office with IM or IV

  • significant risk of potentially fatal GI adverse events, CV events, acute renal insufficiency; not common for OA (osteoarthritis)
64
Q

Celecoxib

A

NSAID - Selective COX2 Inhibitor

for pts with high risk for GI complications and low risk for CV events

  • COX2 related: degree of COX2 selectivity dictates CV risk; celecoxib (selective COX2 inhibitor) has strongest association with CV events; diclofenac and ibuprofen have strong association with CV events
65
Q

Colchicine

A

Gout Treatment

MOA: anti-inflammatory; interferes with migration of neutrophils to sites of inflammation that have been induced by deposits of monosodium urate crystals in synovial fluid; NOT analgesic or uricosuric

AE:

  • common: nausea, vomiting, diarrhea, abdominal pain
  • more serious: myopathy, bone marrow suppression (neutropenia)
  • caution: toxicity more likely if renal insufficiency (adjust dose)
  • low therapeutic index
  • interactions: p-glycoprotein or strong CYP3A4 inhibitors: clarithromycin, verapamil, ritonavir, cyclopsporine, ranolazine
  • used to stop attack; do not used for acute attack if already on or if have used colchicine in the last 14 days
  • only works if given right away (<36 hours); 2/3 of people respond if given within 24 hrs of attack
  • used to be generic; now only brand name – more expensive, proper labeling and safety data, FDA approved, dosing changed (less used now, just as effective)
66
Q

Allopurinol

A

Urate Lowering Therapy

First Line

MOA: both drug and primary metabolite (oxypurinol) reduce uric acid concentrations by inhibiting xanthine oxidase (preventing production of uric acid)

  • adjust dose based on renal function (cleared by kidneys)
  • interactions: theophylline (may lower T dose); warfarin (may need to lower W dose); azathioprine (muse reduce Az dose); ampicillin (increased risk of skin rash)
  • AE: generally well tolerated, nausea, diarrhea
  • Stevens-Johnson Syndrome: can be caused by a variety of meds; characterized by severe expression of erythema multiforme, top layer of affected skin dies and sheds off, often hospitalized in burn unit, potential for severe morbidity or death, may occur 1-2 weeks after initiation; do not take med again!
    Allopurinol Hypersensitivity Syndrome: presents as sever desquamating skin lesions, high fever (>39*C), hepatic dysfunction, leukocytosis with predominant eosinophils, renal failure; highest risk in first months; rare (20-25% mortality); screen: HLA BS801 for pts at elevated risk – Koreans with stage 3+ CKD, Han Chinese or Thai descent; do not give allopurinol if AHS history
  • commonly used
  • generally effective when titrated properly
  • oral
  • half-life: allopurinol – 2-3 hrs; oxypurinol 24 hrs (once daily dosing)
  • important to give anti-inflammatory (low dose colchicine or NSAID) if initiated during acute attack – rapid uric acid concentration changes can cause crystals, so it is important to prevent inflammation and therefore crystals
  • dosing: decrease dose if renal impairment, start with low dose, increase 2-5 wks prn and tolerated, titrate dose to reach goal uric acid level (<6mg/dL) or max dose (800 mg daily)
  • monitor serum uric acid levels (2-5 wks during titration, 6 mo after target is achieved)
67
Q

Febuxotat

A

Urate Lowering Therapy

First Line

MOA: xanthine oxidase inhibitor that acts to decrease uric acid; structurally different than allopurinol

CI: CrCL <30 – can cause kidney stones

AE: nausea arthralgias, rash, transient elevation of hepatic transaminases

Monitor: liver function tests (baseline, 2mo, 4mo, periodically)

  • important to give anti-inflammatory (low dose colchicine or NSAID) during initiation and titration to prevent gout attack
  • expensive – only use if allopurinol is not tolerated or if additional therapy is needed to reach uric acid goal
68
Q

Probenecid

A

Urate Lowering Therapy

Alternate

MOA: uricosuric; blocks reabsorption of uric acid, increasing its excretion

CI: history of urolithiasis or urate nephropathy

AE: nausea, fever, rash, hepatic toxicity

  • less effective as renal function declines; avoid if CrCl <50
  • counsel pts to drink a lot of water – reduces risk of stone formation
  • not recommended for urate overproducers
69
Q

Pegloticase

A

Urate Lowering Therapy

Refractory

IV

MOA: recombinant form of uricase, an enzyme that exists in nonprimates to convert uric acid into soluble product that is easily excreted

AE: gout flares, infusion reactions, anaphylaxis (5%)

CI: G6PD deficiency (due to risk of hemolysis and methemoglobinemia; screen for this)

  • use when other
    therapies don’t work
  • reserve for sever gout with tophi or nephropathy that is refractory
  • $$$
70
Q

Oxycodone

A

Opioid

Use: last resort for OA pain relief

AE:

  • MAJOR ADDICTION POTENTIAL
  • nausea, constipation, sedation, addiction
  • respiratory depression/arrest esp at high dose, in combo with other opioids, in combo with alcohol
  • do not drive
  • start with low doses and use lowest possible dose for shortest duration possible
  • APAP combos reduce opioid need (oxy-APAP; hydrocodone-APAP)
  • reserve for special patients: those who have severe pain; if other options are inadequate; if other conditions make other meds CI (like NSAIDS and renal failure, heart failure, anticoagulation, etc.)
71
Q

Hydrocodone

A

Opioid

Use: last resort for OA pain relief

AE:

  • MAJOR ADDICTION POTENTIAL
  • nausea, constipation, sedation, addiction
  • respiratory depression/arrest esp at high dose, in combo with other opioids, in combo with alcohol
  • do not drive
  • start with low doses and use lowest possible dose for shortest duration possible
  • APAP combos reduce opioid need (oxy-APAP; hydrocodone-APAP)
  • reserve for special patients: those who have severe pain; if other options are inadequate; if other conditions make other meds CI (like NSAIDS and renal failure, heart failure, anticoagulation, etc.)
72
Q

Methadone

A

Opioid

Use: last resort for OA pain relief

AE:

  • MAJOR ADDICTION POTENTIAL
  • nausea, constipation, sedation, addiction
  • respiratory depression/arrest esp at high dose, in combo with other opioids, in combo with alcohol
  • do not drive
  • start with low doses and use lowest possible dose for shortest duration possible
  • APAP combos reduce opioid need (oxy-APAP; hydrocodone-APAP)
  • reserve for special patients: those who have severe pain; if other options are inadequate; if other conditions make other meds CI (like NSAIDS and renal failure, heart failure, anticoagulation, etc.)
73
Q

Hydromorphone

A

Opioid

Use: last resort for OA pain relief

AE:

  • MAJOR ADDICTION POTENTIAL
  • nausea, constipation, sedation, addiction
  • respiratory depression/arrest esp at high dose, in combo with other opioids, in combo with alcohol
  • do not drive
  • start with low doses and use lowest possible dose for shortest duration possible
  • APAP combos reduce opioid need (oxy-APAP; hydrocodone-APAP)
  • reserve for special patients: those who have severe pain; if other options are inadequate; if other conditions make other meds CI (like NSAIDS and renal failure, heart failure, anticoagulation, etc.)
74
Q

Fentanyl

A

Opioid

Use: last resort for OA pain relief

AE:

  • MAJOR ADDICTION POTENTIAL
  • nausea, constipation, sedation, addiction
  • respiratory depression/arrest esp at high dose, in combo with other opioids, in combo with alcohol
  • do not drive
  • start with low doses and use lowest possible dose for shortest duration possible
  • APAP combos reduce opioid need (oxy-APAP; hydrocodone-APAP)
  • reserve for special patients: those who have severe pain; if other options are inadequate; if other conditions make other meds CI (like NSAIDS and renal failure, heart failure, anticoagulation, etc.)
75
Q

Tramadol

A

Opioid

Use: last resort for OA pain relief

AE:

  • MAJOR ADDICTION POTENTIAL
  • nausea, constipation, sedation, addiction
  • respiratory depression/arrest esp at high dose, in combo with other opioids, in combo with alcohol
  • do not drive
  • start with low doses and use lowest possible dose for shortest duration possible
  • APAP combos reduce opioid need (oxy-APAP; hydrocodone-APAP)
  • reserve for special patients: those who have severe pain; if other options are inadequate; if other conditions make other meds CI (like NSAIDS and renal failure, heart failure, anticoagulation, etc.)
76
Q

Codeine

A

Opioid

Use: last resort for OA pain relief

AE:

  • MAJOR ADDICTION POTENTIAL
  • nausea, constipation, sedation, addiction
  • respiratory depression/arrest esp at high dose, in combo with other opioids, in combo with alcohol
  • do not drive
  • start with low doses and use lowest possible dose for shortest duration possible
  • APAP combos reduce opioid need (oxy-APAP; hydrocodone-APAP)
  • reserve for special patients: those who have severe pain; if other options are inadequate; if other conditions make other meds CI (like NSAIDS and renal failure, heart failure, anticoagulation, etc.)
77
Q

Duloxetine

A

Anti-depressant

Use: pain relief in OA

78
Q

Capsaicin

A

Topical Pain Relief

MOA: stimulates the release of a compound believed to be involved in communicating pain between the nerves in the spinal cord and other parts of the body

  • element of hot pepper
  • may increase pain during first application before relieving it

Pharmacology Exam III (3 decks)

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