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drugs for osteoarthritis, ra, and gout
pharmacology module 4
82
Medical
Graduate
07/17/2009

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Term
To what category does asa belong?
Definition
salicylates
Term
To what category do the following belong: Magnesium choline salicylate (Trilisate)
Salsalate (Disalcid)
Diflunisal (Dolobid)?
Definition
nonacetylated salicylates
Term
What is A weak acid rapidly absorbed from stomach and small intestine
Leads to damage of gastric mucosal barrier?
Definition
asa
Term
Acetylsalicylic acid is hydrolyzed to what compound, which is the active form of aspirin?
Definition
salicylic a
Term
What medication is Highly protein bound and is
Conjugated and renally eliminated by 1st order kinetics with therapeutic doses < 650mg?
Definition
asa
Term
Regarding asa, Metabolic pathway saturated when what level of doses given? this leads to what order kinetics, long half-life (15 hrs), and toxic serum levels?
Definition
high doses, zero order kinetics
Term
What med is a Nonselective inhibitor of cyclooxygenase (COX) enzymes 1 and 2 that has the following properties:
Anti-inflammatory
Analgesic
Antipyretic?
Definition
asa
Term
Does asa inhibit platelet function reversibly or irreversibly?
Definition
irreversible inhibition
Term
What medication involves Inhibition of COX-1 prevents synthesis of thromboxane A2 by platelets, preventing clot formation?
Single dose effect lasts 8-10 day life of platelet.
Definition
asa
Term
Do Nonacetylated salicylates and nonselective NSAIDs have reversible or irreversible effects?
Definition
reversible
Term
What med involves the following ade: Gastritis and gastric bleeding,
Increase in bleeding time,

Airway hypersensitivity
(10% of asthmatics have history;
Cross reactivity with other NSAIDs)
Definition
asa
Term
Do Nonacetylated salicylates have an irreversible effect on platelets?
Definition
no
Term
What type of poisoning involves Tinnitis, nausea and vomiting, hyperventilation, hypokalemia, metabolic acidosis, dizziness, agitation, hallucinations?
Definition
Salicylism (salicylate poisoning)
Term
Salicylism, bleeding, and reye's syndrome are involved w/what med?
Definition
asa
Term
What syndrome involves: Hepatic encephalopathy and liver failure in young children;
Associated with aspirin use to treat febrile viral infection?
Definition
reye's syndrome
Term
What nsaid should not be given to children for fevers due to chicken pox or uri's?
Definition
asa
Term
What med is Rarely used for arthritis or pain and is Primarily for prophylaxis (prevention) of myocardial infarction or stroke?
Definition
asa
Term
What med in a Low dose of 81mg irreversibly inhibits platelets and in
Higher doses only increase risk of GI bleeding?
Definition
asa: Primarily for prophylaxis (prevention) of myocardial infarction or stroke
Term
What drug involves Adverse effects higher than OTC NSAIDs and
Risk of accumulation and salicylate toxicity?
Definition
asa: rarely used for arthritis or pain
Term
What are the 2 major classes of NSAIDS?
Definition
Nonselective (traditional) NSAIDs.
Selective COX-2 inhibitors
Term
What drug class involves the following MOA: Inhibition of COX-1 and/or COX-2 enzymes to prevent prostaglandin synthesis?
Definition
nsaids
Term
Is COX 1 or 2 Continuously expressed (constitutive) and widely distributed in most organ systems including GI tract and
Needed for production of thromboxanes for clotting
Definition
cox-1
Term
is cox 1 or 2 Primarily induced at sites of inflammation and neoplasms and
Continuously active in kidney, intestine, uterus, brain?
Definition
cox-2
Term
Which drug class involves adverse effects of Dyspepsia,
Ulceration, bleeding, perforation?
Risk increases with dose and duration of treatment, alcohol use, steroid use.
Definition
gi effects of nsaids
Term
What drug class involves adverse effects including Sodium and water retention
(Can exacerbate heart failure and hypertension),
Acute tubular necrosis,
Prostaglandins necessary for autonomic control of blood flow to glomerulus,
Risk with dehydration, hypovolemia, ACE inhibitors and ARBs?
Definition
renal adr of nsaid
Term
what is the most common adr of nsaids?
Definition
gi effects
Term
What drug class involves the following adr's: Reversible platelet inhibition;
CNS: dizziness, drowsiness, confusion;
Thrombosis associated with COX-2 selective agents
[Rofecoxib (Vioxx) and valdecoxib (Bextra) removed from market recently]
Definition
nsaids
Term
How high is the risk of gi toxicity with Ibuprofen (Motrin, Advil, etc),
Naproxen (Alleve, Naprosyn), and
Ketaprofen (Orudis)?
Definition
low to moderate risk
Term
How high is the risk for gi toxicity with Diclofenac (Voltaren)?
Definition
low to moderate risk
Term
How high is the risk of gi toxicity w/Nabumetone (Relafen)?
Definition
low to moderate risk
Term
How high is the risk of gi toxicity w/
Meloxicam (Mobic)?
Definition
low to moderate risk
Term
How high is the risk of gi toxicity w/
Celecoxib (Celebrex)?
Definition
low to moderate risk
Term
How high is the risk of gi toxicity w/
Salsalate (Disalcid)?
Definition
low to moderate risk
Term
How high is the risk of gi toxicity w/Indomethacin (Indocin)?
Definition
high risk
Term
How high is the risk of gi toxicity w/
Piroxicam (Feldene)?
Definition
high risk
Term
How high is the risk of gi toxicity w/
Flurbiprofen (Ansaid)?
Definition
high risk
Term
How high is the risk of gi toxicity w/
Fenoprofen (Nalfon)?
Definition
high risk
Term
How high is the risk of gi toxicity w/
Oxaproxin (Daypro)?
Definition
high risk
Term
What adr is reduced when you Add H2 antagonists (ie ranitidine) or proton pump inhibitors (ie omeprazole) to NSAID therapy?
Definition
gi toxicity; 80% with ulcers are healed with PPI versus 60% with H2 blocker
Term
What adr is reduced by substitutin celecoxib (celebrex) ( but should avoid pt w/cardiovascular disease)?
Definition
reduce gi toxicity secondary to nsaids
Term
What adr is reduced when you Add misoprostol (Cytotec), a prostaglandin analog that helps protect gastric mucosa?
Definition
reduce gi toxicity- Arthrotec = diclofenac + misoprostol,
Poor tolerance due to diarrhea and cramping,
Contraindicated in pregnancy
Term
What drug interactions occur w/nsaids?
Definition
ibuprofen.
Celecoxib. other antiplatelet drugs. diuretics. ace inhibitors. angiotensin receptor blockers. methotrexate.
Term
what nsaids drug interaction involves inhibition of antiplatelet effect?
Definition
ibuprofen
Term
What drug interaction w/nsaids involves loss of potential gi protective effect?
Definition
celecoxib
Term
What increases risk of bleeding w/nsaids?
Definition
other antiplatelet drugs such as clopidogrel (plavix)
Term
nsaids antagonizes diuresis and Na+ loss of what drug?
Definition
diuretics
Term
nsaids antagonizeds renal effects of what drug?
Definition
ace inhibitors
Term
nsaids antagonizes renal effects of what drug?
Definition
angiotensin receptor blockers
Term
nsaids may increase serum concentration and toxicity of what drug?
Definition
nsaid
Term
what are 4 uses for nsaids?
Definition
pain relief, incl ha. fever, inflammatory conditions such as arthritis. primary dysmenorrhea.
Term
what dose of nsaids are comparable to 650 mg of T for pain?
Definition
low doses (ibuprofen 200 mg; naproxen 250 mg)
Term
what doses of nsaids are comparable to acetaminophen/codeine combinations for pain?
Definition
moderate doses (OTC: Ibuprofen 400mg, naproxen 500mg)
Term
What doses of nsaids are used for for anti-inflammatory effect?
Definition
high doses (OTC: ibuprofen 1800-2400 mg/day, naproxen 1000 mg/day)
Term
OTC only for what dose of ibuprofen and naproxen?
Definition
ibuprofen: 200 mg; naproxen 250 mg strengths
Term
What is the Only parenteral NSAID – given IV or IM?
Definition
ketorolac (toradol)
Term
What nsaid is indicated for pain relief; Higher dose (30mg) comparable to morphine?
Definition
ketorolac (toradol)
Term
For how many days can you use ketorolac (toradol)?
Definition
Cannot use > 5 days: GI ulceration and bleeding
Term
In what dosage is ketorolac (toradol) indicated for osteoarthritis or RA?
Definition
Not indicated for osteoarthritis or rheumatoid arthritis
Term
What drug for OA relieves mild pain, but inferior to NSAIDs for moderate to severe pain?
Definition
T
Term
What drug for OA may be as effective as oral NSAIDs and avoids systemic toxicity?
Definition
topical nsaids- Ibuprofen 10% or ketoprofen 5% compounded by pharmacist.
Diclofenac 1% topical gel (Voltaren Gel)
Term
What drug for oa relieves pain by inhibiting substance P – 50% experience local burning sensation which diminishes over time?
Definition
topical capsaicin cream (otc); 50% experience local burning sensation which diminishes over time
Term
What drug for oa results of trials still controversial – overall appears to reduce pain with chronic use with little adverse reaction?
Definition
Glucosamine sulfate +/- chondroitin
Term
What tx option for oa is combined w/local anesthetic and injected into affected jts?
Definition
glucocorticoid injections
Term
What injections for oa are common, though probably noet effective?
Definition
hyaluronic acid injections
Term
Tramadol (ultram) adn opioids are other tx options for what disorder?
Definition
oa
Term
What are 4 non-drug tx for ra?
Definition
jt protection. energy conservation. passive exercise. heat.
Term
What is short-term drug tx for ra?
Definition
nsaids (no disease modifying activity), and corticosteroids (local injections, low-dose systemic therapy (predinsone 10mg))
Term
Do DMARDS have slow or rapid onset?
Definition
slow onset of effect (3-6 mos)
Term
Why might pts on dmards require regular evaluation?
Definition
for adrs
Term
What are 2 drugs for *mild* arthritis?
Definition
hydroxychloroquine (plaquenil) adn sulfasalazine (azulfidine)
Term
What is the least toxic of all dmards?
Definition
hydroxychloroquine (plaquenil)
Term
Which dmards involves hemolytic anemia if g6pd deficiency?
Definition
hydroxychloroquine (plaquenil), sulfasalazine (azulfidine)
Term
What non-biologic dmard involves potential retinal damage in the elderly?
Definition
hydroxychloroquine (plaquenil)
Term
What are adr's of sulfasalazine (azulfidine)?
Definition
nausea, rash, hemolytic anemia if g6pd deficiency, rare-leukopenia, hepatitis
Term
What is teh DMARD of choice by most rheumatologists?
Definition
methotrexate
Term
Is the response rate to methotrexate fast or slow? high or low?
Definition
rapid and high response rate
Term
How is methotrexate administered?
Definition
low oral doses once weekly
Term
The following are adr's of what dmard: Elevated liver enzymes in 15% (discontinue if 2x normal upper limit), nausea, vomiting?
Definition
methotrexate
Term
The following are adrs of what dmard: Dose-related toxicity: bone marrow suppression and stomatitis?
Definition
methotrexate
Term
The following are adrs of what dmard: teratogenic: pregnancy category x?
Definition
methotrexate
Term
How is methotrexate excreted?
Definition
renally- avoid if clcr<30 ml/min
Term
What supplement might be necessary for dmard?
Definition
folic acid supplement
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