Medications Grouped Flashcards
Short Acting Beta Agonists (SABAs)
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
Long Acting Beta Agonists (LABAs)
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
Inhaled Anticholinergics
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
Methylxanthines
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)
Inhaled Corticosteroids
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
Systemic (oral) Corticosteroids
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
Leukotriene Receptor Antagonists
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)
Immunomodulator
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
Phosphodiesterase- 4 Inhibitor
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
Cromolyn
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
Nicotine Replacement Products
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
Smoking Cessation Medications
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
Conventional Disease Modifying Antirheumatic Drugs
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
TNF Antagonists
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
Costimulation Modulator (Biological DMARD)
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
Anti-CD20 Monoclonal Antibody (Biological DMARD)
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
Anti-interleukin-6 Receptor Antibody (Biological DMARD)
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
Targeted Synthetic DMARD
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
Acetaminophen
- 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
Nonsteroidal Anti-Inflammatory Drugs
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
Gout Treatment
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)
Urate Lowering Therapy
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
Opiods
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.)
Duloxetine
Anti-depressant
Use: pain relief in OA
Capsaicin
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
Rarely Used RA Options
Azathioprine
D-penicillamine
Gold Salts
Anakinra
