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NSAID inhibit COX, CYP3A or CYP2C metabolism
Aspirin/Salicylates can cross BBB and placenta -low doses is analgesia -high doses is anti-inflammatory
Aspirn weak organic acid
Aspirin irreversible inhibits both COX
Diflunisal NSAID
Diflunisal weal organic acid
Diflunisal reversibly inhibits both COX
Diflunisal used by dentists
Olsalazine pro-drug
Olsalizine NSAID
Olsalazine metabolized to 5-aminosalicylic acid
Olsalazine retained in colon for ulcerative colitis
Proprionic Acid Derivatives Profens & Naproxen
Proprionic Acid derivatives reversible inhibitor of both COXs -inhibit PG synthesis but not leukotrienes
Proprionic acid side effect tinnitus
Naproxen better tolerated than aspirin
Indolacetic acids Indomethacin, Sulindac, Etodlac
Indomethacin more potent; inhibits both COX, can have anti-inflammatory effects at normal doses
Indomethacin usually prescribed for gout or premature labor - suppresses uterine contractions
Sulindac less potent than indomethacin
Sulindac Sulfoxide prodrug
Etodlac safer than Indomethacin & sulindac
Etodlac may increase blood levels and toxicity of digoxin, lithium, methotrexate and cyclosporine
Fenamate mefenamic acid and meclofenamate have no real avantage over other NSAIDS
Fenamate side effect diarrhea, hemolytic anemia
Fenamate used for menstrual cramps
Diclofenac accumulates in synovial fluid; safe and effective
Ketorolac given IM for post-op pain
Ketorolac never be used for more than 5 days in outpatient; go into renal failure
Piroxicam & Meloxicam NSAID good for compliance
Acetaminophen inhibits PG synthesis, less effect on COX
Acetaminophen used in pt with gastric probs, drug of choice for children, gestational
Anti-arthritic Celecoxib
Anti-arthritic Hydroxychloroquin
Anti-arthritic Leflunomide
Anti-arthritic Sulfasalazine
Anti-arthritic Gold Salts
Celecoxib selective for COX2, metabolized by CYP2C, doesnt inhibit platelets
Celecoxib contraindicated in pt allergic to sulfa
Celecoxib interacts with flucanazole, beta blockers, antidepressents
Hydroxychloroquin selective for COX2
Hydroxychloroquin side effects decreased accomodation, hemolysis in GCPD deficient pts
Hydroxychloroquin 1st line for rheumatoid arthritis
Leflunomide prodrug
leflunomide not for renal impaired or gestational
Sulfasalazine contraindicated in urinary or GI obstruction
Gold Salts side effets bone marrow depression, diarrhea, ulcers, jaundice
Gold Salts indicated in active rheumatoid arthritis unresponsive to NSAIDS
Narcartic Opiods hydromorphone, oxycodone, hydrocodone, levorphanol, oxymorphone
Opiods -Morphone, -Codone
Morphine Opiate, inhibits pain nerve cells
Morphine side effects pinpoint pupils, antitussive, parasympathetic like
Drug of choice for severe pain MI Morphine
Morphine contraindicated in head/brain trauma
Opiod less potent than morphine; mod to severe pain, better absorbed orally than morphine, useful in outpatient
Meperidine synthetic opiod for acute pain
Meperidine contraindicated for cough/diarrhea
Meperidine overdose causes convulsions due to metabolite normeperidine
Mepereidine doesent cause pinpoint pupils but dilates due to atropine-like activity
Meperidine interacts with MAO inhibitors causeing severe CNS excitation, resp depression, hypotension
Methadone full morphine like actions, weaker sedative, less euphoria
methadone treat morphine addiction due to lower euphoria therefore develop less psych dependence
Phenylpiperidines fentanyl, sufentanil, alfentanil
fentanyl more potent than morphine; preop use in anesthesia, no tolerance/dependence
fentanyl transdermal or transmucosal (child w/cancer)
sufentanil more potent than fentanyl
alfentanil less potent than fentanyl
Phenanthrenes codeine or buprenorphine
Opiod phenanthrene codeine
mixed agonist-antagonist phenanthrene buprenorphine
Codiene prodrug converted to morphine
codeine higher oral efficacy than morphine; good antitussive
mixed agonist-antagonists pentazocine and buprenorphine
pentazocine moderate pain; may be used prep; mixed with naloxone
buprenorphine new drug to treat opiod addiction
drugs to treat opiod addiction methadone, buprenorphine**
buprenorphine works like morphine in naive pt
Tramadol non-opiate synthetic analgesic
tramadol reduces uptake of norepi and serotonin
tramadol less resp depression than opiates and less platelet toxicity than NSAIDS
tramadol induced miosis limits pupil exam in trauma pt
tramadol class II controlled substance
pure antagonists naloxone and naltrexone
naloxone blocks opiod receptors; no effect in narcotic free pts
naloxone given IV, short half life
Naltrexone given orally, longer duration, can block effects for up to 48 hrs
naltrexone indicated in tx of alcoholism
Migraine drugs sumatriptan
sumatriptan serotonin agonist
sumatriptan causes vasoconstriction of cranial arteries; not given IV
butalbital used before triptans
butalbital short acting barbiturate with anticonvulsant and sedative properties
butalbital indicated for tension headache
isometheptene controlled substance
Migraine drug butalbital
migraine drug isometheptene
isometheptene indicated for tension headache
isometheptene contraindicated in glaucoma, severe renal, cardiace, HTN or hepatic disease
Acute gout cholchicine to decrease movement of granulocytes into effected area and NSAIDS to decrease pain and inflammation
cholchicine anti-inflammatory
cholchicine alleviates pain of gout within 12 hrs; may be combined with probenecid
cholchicine side effects diarrhea*** 1st sign to stop
chronic gout allopurinol, probenecid
allopurinol reduces production of uric acid
allopurinol inhibits xanthine oxidase
allopurinol low incidence of side effects but may exacerbate gout attacks, cause GI upset, rash and Stevens-Johnson syndrome
Probenecid uricosuric that blocks proximal tubular reabsorption of uric acid
Probenecid side effects may exacerbate gout attacks, accumulate with repeated dose, cause headache, dizziness, sore gums***
Asthma Beta-adrenergic agonists
beta-adrenergic agonists mild asthma
short-acting beta adrenergic agonist albuterol
short-acting beta pirbuterol
short acting beta terbutaline
short-acting beta adrenergic agonists rescue agents, no anti-inflammatory, never used alone
long-acting beta salmetrol xinaoate
long-acting beta formoterol fumarate
long0acting beta levalbuterol
salmeterol xinaoate chemical analog of albuterol; long duration
salmeterol xinaoate slow onset of action, never used in acute attacks
formoterol fumerate maintenance of asthma and prevention of bronchospasm in reversible obstructive airway disease
levalbuterol single isomer albuterol; preservative free for children
corticosteroids mod to severe asthma who require inhaled beta 2 agonists more than once daily
severe asthma systemic glucocorticoids for short term
oral inhaled steroids -IDE or -ASONE
oral inhaled steroids flunisolide, mometasone, fluticasone, budesonide, beclomethasone
most popular corticosteroid fluticasone bc beta 2 and steroid
corticosteroids decrease inflammation, reduce cytokine production, dont relax airways, reduces hyperresponsiveness to triggers
corticosteroid side effects thrus, osteoporosis, cataracts, headache, pharyngitis
Mast cell inhibitors inhibit release histamine
mast cell inhibitors prophylactic anti-inflammatory, prevention
mast cell inhibitors not useful in acute attack bc not direct bronchodilators
mast cell inhibitor cromolyn
cromolyn fine powder inhalation or aerosolized solution
cromolyn anti-inflammatory; pretreatment blocks allergen & exercise induced bronchoconstriction
cromolyn side effects poorly absorbed so minimal side effects but caution in pregnancy
cholinergic antagonists reduce secretions, also used for pt who cannot tolerate beta 2 agonist
cholinergic antagonists -IUM or theophylline
cholinergic antagonist ipratropium
cholinergic antagonist tiotropium
cholinergic antagonist theophylline
ipratropium derivative of atropine
ipratropium most popular; minimal side effects
ipratropium not used in children, caution in preg and glaucoma
tiotropium long term maintenance of bronchospasm due to chronic bronchitis and emphysema
tiotropium inhaler or dry poweder caplets to be inhaled
tiotropium not used in children or acute attacks; caution in pregnancy and glaucoma
theophylline direct bronchodilator with some anti-inflammatory activity
theophylline well absorbed in GI tract *****pill*****
theophylline side effects constriction of cerebral vessels
theophylline narrow therapeutic index; toxicity may cause seizures or fatal arrythmias; caution in pregnancy and glaucoma
anti-leukotriene drugs new, reversible inhibitors of the cysteinyl leukotriene 1 receptor thus blocking effects of cysteinyl leukotrienes
anti-leukotriene drugs prophylactic tx of asthma
anti-leukotriene drugs -KAST
anti-leukotriene zafirlukast
anti-leukotriene montelukast
zafirlukast inhibit CYP-450 thus increase serum warfarin levels; too many drug interactions
montelukast dont inhibit CYP-450
zafirlukast & montelukast in addition to low dose inhaled steroids/cromolyn in mild persistant asthma
zafirlukast & montelukast orally active, highly protein bound & drug interactions
Allergic rhinitis 1st line agents are antihistamines and decongestants
antihistamines h1 receptor blockers
h1 receptor blockers diphenhydramine, chlorpheniramine, cetirizine, clemastine, azelastine
non-sedating h1 receptor blockers loratidine & fexofenadine
alpha-adrenergic agonists phenylephrine & oxymetazoline
phenylephrine & oxymetazoline constrict arterioles in nasal mucosa & reduce airway resistance
pehnylephrine & oxymetazoline normally in aerosol form and have rapid onset of action; not used in long term therapy due to rebound nasal congestion after discontinuance
corticosteroid nasal sprays full effects may not be evident for 1-2 weeks; -IDE or -ASONE
anticholinergic nasal sprays ipratropium
ipratropium dries nasal secretions; use caution in glaucoma and pregnancy
mast cell stabilizers cromolyn
cromolyn nasal spray stops hypersensitivity reactions; caution in pregnancy & nursing
antitussives not indicated for productive coughs
most efficacious class of antitussives codeine & hydrocodone
OTC antitussive dextromethorpan
dextromethorpan no potential for dependence, no side effects
expectorants increase bronchial secretions, reduce thickness/viscosity
expectorants guaifenesin
mucolytics acetylcysteine
acetylcysteine via inhalation
acetylcysteine used to directly loosen thick, viscous bronchial secretions as in cystic fibrosis
acetylcysteine antidote for acetaminophen
rapid acting insulin preparations insulin glulisine
rapid acting insulin prep lispro
rapid acting insulin prep insulin aspart
insulin glulisine 15 min before or within 20 min of starting meal; peak 60 min
lispro not normally used alone
lispro 15 min before meal; onset 15 min later; peak 60 min; duration: 3-4 hrs
insulin aspart s. cerevisiae
insulin aspart onset: 15 min, peak 1-3hrs, duration 3-5 hrs
short insulin prep regular insulin
regular insulin/short acting novalin R
regular insulin/short acting Humulin R
Humulin/Novalin R soluble, crystalline zinc
Humulin/Novalin R peak 50-120 min; duration 4-5 hrs
humulin/novalin R given SC but may be given IV (only one)
humulin/novalin R safely used in pregnancy
intermediate-acting insulin NPH, Humulin, Novalin N
Humulin/novalin N absorption and onset delayed by combining appropriate amounts of insulin and protamine
humulin/novalin N onset 2-5 hrs, duration 4-12 hrs; crystals release insulin slower
prolonged acting insulin insulin glargine
prolonged acting insulin insulin detemir
two insulins not with E.colie Insulin aspart (rapid) and insulin detemir (prolonged)
insulin glargine new, peakless, used for background
insulin glargine onset: 1 hr, no peak, duration 24 hrs
insulin detemir s. cervisiae
insulin detemir onset 1 hr, no peak duration 24 hrs
insulin secretagogue sulfonylurea
insulin secretagogue repaglinide, nateglinide
sulfonylureas stimulate insulin release
sulfonylureas glyburide & glipizide
sulfonylureas glimepiride
glyburide & glipizide bind to serum proteins, metabolized by liver
gestational diabetes insulin regular only
glyburide & glipizide contraindicated in pt w/hepatorenal insufficiency; pregnancy
glimepiride new 2nd generation sulfonylurea - 1st to be approved for concurrent use w/insulin
sulfonylurea oral hypoglycemic agents
repaglinide binds to ATP-sensitive K channels of beta cells causing release of insulin
nateglinide works well with metformin
biguanides metformin
metformin 1st line agent
metformin not bound to serum proteins and is not metabolized
metformin inhibits gluconeogenesis; less risk of hypoglycemia
alpha-glucosidase inhibitors acarbose
acarbose inhibits alpha-glucosidase in intestines thus decreases absorption of starch and disaccharides
acarbose used as adjunct
thiazolidinediones -LITAZONES
thiazolidinediones pioglitazone & rosiglitazone
pioglitazone & rosiglitazone insulin sensitizers; counteract insuin resistance
pioglitazone & rosiglitazone side effects URI,MI
Dipeptidyl peptidase-4 inhibitors -GLIPTINS
dipeptidyl peptidase 4 inhibitor sitagliptin
dipeptidyl peptidase 4 inhibitor saxagliptin
dipeptidy peptidase 4 inhibitor linagiptin
sitagliptin bioavailability over 85%
sitagliptin peak 1-4hrs, half life 12 hrs
sitagliptin if used with sulfonylureas may need to adjust dose downward to prevent hypoglycemia
sitagliptin side effects URI
saxagliptin given orally
saxagliptin peak 2-4 hrs, half life 2.5 hrs
saxagliptin hypoglycemia if used with sulfonylureas
saxagliptin side effects URI
saxagliptin peripheral edema if used with thiazolidinediones
Created by: jjohrden16