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Pharmacology Exam III > Medications Grouped > Flashcards

Medications Grouped Flashcards

1
Q

Short Acting Beta Agonists (SABAs)

A

Albuterol
Levalbuterol
Terbutaline

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

Long Acting Beta Agonists (LABAs)

A 
Salmeterol
Formoterol
Arformoterol
Inadacaterol*
Olodaterol*
Vilanterol*

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
  • Onset: salmeterol – 30 min; formoterol – 5 min (not approved for SABA)
  • delivery: inhaler (alone or w/ ICS) or nebulizer
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3
Q

Inhaled Anticholinergics

A 
Ipratropium bromide
Tiotropium bromide*
Aclidinium bromide
Umeclidinium bromide*
Glycopyrrolate

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, increased CV events (ipratropium; not tiotropium)

CI: cardiovascular disease

    • longer lasting
  • 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; tiotropium > 24 hrs; aclidinium < 24 hrs
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4
Q

Methylxanthines

A

Theophyline

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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5
Q

Inhaled Corticosteroids

A 
Beclomethasone
Budesonide
Ciclesonide
Flunisolide
Fluticasone
Mometasone

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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6
Q

Systemic (oral) Corticosteroids

A

Prednisone
Prednisolone
Methyprednisolone

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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7
Q

Leukotriene Receptor Antagonists

A

Montelukast
Zileuton
Zafirlukast

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); hepatotoxicity (zileuton and zafirlukast), sleep disorders, aggressive behavior, suicidal thoughts, eosinophilic granulomatosis with polyangiitis (rare), angioedema, urticartia

CI: CYP2C9 drugs (significant with zileuton and zafirlukast)

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8
Q

Immunomodulator

A

Omalizumab

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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9
Q

Phosphodiesterase- 4 Inhibitor

A

Roflumilast

also used as antidepressant

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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10
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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11
Q

Nicotine Replacement Products

A 
Nicotine Gum
Nicotine Inhaler
Nicotine Lozenge
Nicotine Nasal Spray
Nicotine Patch
  • increases chances of quitting by 50-70%
  • dosing/strength based on # of cigarettes per day and if pt smokes immediately upon waking
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12
Q

Smoking Cessation Medications

A

Bupropion SR - antidepressant; blocks reuptake of dopamine and NE

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

  • caution with CVD with immediate post MI or with serious symptoms or worsening angina
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13
Q

Conventional Disease Modifying Antirheumatic Drugs

A

Used in RA

Methotrexate
Hydroxychloroquine
Sulfasalazine
Leflunomide

  • mainstay treatment for RA: modify disease process and prevent/reduce joint damage
  • choose based on safety/efficacy, disease severity, patient characteristics, cost, and experience
  • methotrexate is first-line, but comes with risk of methotrexate toxicity
  • suflasalazine is the drug of choice for pregnant patients
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14
Q

TNF Antagonists

A

2nd line for RA
(Biological DMARDs)

Infliximab (Remicade)
Adolimumab (Humira)
Golimumbab (Simponi)
Etanercept (Enbrel)
Certolizumab (Cimzia)

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

  • injection site reaction (rotate sites, topical corticosteroids, antipruritics, analgesics, rotate site)
  • IV infusion reaction
  • monitor for infection
  • screen for TB; could reactivate
  • screen for hepatitis
  • avoid in pts with serious infections, demyelinating disorders, hepatitis, and heart failure
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15
Q

Costimulation Modulator (Biological DMARD)

A

Abatacept (Orencia)

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
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16
Q

Anti-CD20 Monoclonal Antibody (Biological DMARD)

A

Rituximab (Rituxan)

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
17
Q

Anti-interleukin-6 Receptor Antibody (Biological DMARD)

A

Tocilizumab (Actemra)

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
  • avoid in pts with serious infections, demyelinating disorders, and hepatitis
18
Q

Targeted Synthetic DMARD

A

Tofacitinib (Xeljanz)

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
19
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
20
Q

Nonsteroidal Anti-Inflammatory Drugs

A

Nonselective:

Asprin
Solsalate
Etodolac
Diclofenac
Indomethacin
Nabumetone
Ibuprofen
Naproxen
Meloxicam
Prioxicam
Sulindac
Kerorolac

Selective COX2 Inhibitor
Celecoxib

MOA: have analgesic 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 (aspirin or naproxen); others are Rx
  • oral or topical
  • similar APAP efficacy
  • onset of pain relief = 1 hr
  • onset of inflammatory response = 2-3 wks of continuous therapy
  • choose based on patient preference, previous response, tolerability, dosing frequency, cost, GI and CV risk
  • if one doesn’t work, try another
21
Q

Gout Treatment

A

Colchicine

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)
22
Q

Urate Lowering Therapy

A

Allopurinol
Feuxotat
Probenecid
Pegloticase

  • designed to either decrease uric acid production or increase uric acid secretion; goal is to decrease uric acid levels significantly and prevent crystal formation
  • used to prevent attacks
  • continue urate lowering therapy even during acute flares
23
Q

Opiods

A 
Oxycodone
Hydrocodone
Methadone
Hydromorphone
Fentanyl
Tramadol
Codeine

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.)
24
Q

Duloxetine

A

Anti-depressant

Use: pain relief in OA

25
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
26
Q

Rarely Used RA Options

A

Azathioprine
D-penicillamine
Gold Salts
Anakinra

Pharmacology Exam III (3 decks)

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