NSAIDS, DMARDS, Non-opioid Analgesics Flashcards
Which of the following is not used to treat inter-critical gouty arthritis?
A. Uricase
B. Probenecid
C. Allopurinol
D. Colchicine
E. Sulfinpyrazone
D. Colchicine is used as first-line drug for ACUTE gouty attack
For inter0critical gouty arthritis, we provide Urate lowering therapy via:
- Xanthine Oxidase inhibitors (Purine analogues such as allopurinol, oxypurinol, and tisopurine. Others include febuxostat, topiroxostat, and inositols (phytic acid and myo-inositol)
- Uricosurics (Probenecid, Sulfinpyrazone and Lesinurad)
- Uricase (Pegloticase and Rasburicase)
The only non-acid NSAID current in use
Nabumetone
- ketone prodrug
- Nabumetone itself is non-acidic and, following absorption, it undergoes extensive first-pass metabolism to form the main circulating active metabolite (6-MNA) which is a much more potent inhibitor of preferentially cyclo-oxygenase (COX)-2.
Which of the following is not true of NSAIDs?
A. They are well absorbed, and food does not substantially change their bioavailability
B. They are highly metabolized
C. Their metabolism proceeds, in large part, by way of the CYP3A or CYP1A families of P450 enzymes in the liver
D. Renal excretion is the most important route of final elimination
E. Most are highly protein-bound (~98%), usually to albumin
C. CYP3A and CYP2C
Which products of the LOX and COX pathway result to the alteration of vascular permeability, bronchial constriction, and increased secretion?
Leukotrienes (LOX: LTC4, LTD4, LTE4)
Prostaglandin and Thromboxane (COX)
- hence, causing bronchospasm, congestion, mucous plugging
Which anti-gout agent is used to treat inflammation induced by phagocyte attraction and activation by LTB4?
Colchicine
Which group of NSAIDs do not inhibit platelet aggregation?
Cox-2 selective inhibitors and Non-acetylated salicylates
COX-2-selective inhibitors have increased incidence of the following, EXCEPT:
A. Edema
B. GI ulcers
C. Hypertension
D. MI
B. low effect on GI
DOC NSAIDs for patients with renal insufficiency
Non-acetylated salicylates
Which of the following is NOT an adverse effect of NSAIDs?
A. Aseptic meningitis
B. Dyspepsia
C. Neutropenia
D. Pruritus
E. Hypokalemia
E should be Hyperkalemia due to renal insufficiency
This is responsible for the anti-inflammatory action of aspirin
Salicylic acid
Which of the following is the effect of aspirin at lower dose (80mg)?
A. Anti-pyretic
B. Anti-platelet
C. Anti-inflammatory
D. Analgesic
B. Anti-platelet at 80mg, Anti-inflammatory at 325mg (higher dose)
Which of the following is NOT true of aspirin?
A. Rapidly hydrolyzed (serum half-life 15 minutes) to acetic acid and salicylate
B. Irreversibly inhibits platelet COX so that aspirin’s antiplatelet effect lasts 8–10 days
C. Long-term use is associated with higher incidence of colon cancer
D. May be valuable in treating preeclampsia-eclampsia
C.
long-term use of aspirin at low dosage is associated with a lower incidence of colon cancer
Which of the following is NOT true of aspirin?
A. Rapidly hydrolyzed (serum half-life 15 minutes) to acetic acid and salicylate
B. Irreversibly inhibits platelet COX so that aspirin’s antiplatelet effect lasts 8–10 days
C. Long-term use is associated with higher incidence of colon cancer
D. May be valuable in treating preeclampsia-eclampsia
C.
long-term use of aspirin at low dosage is associated with a lower incidence of colon cancer
Which of the following is NOT true of aspirin?
A. Rapidly hydrolyzed (serum half-life 15 minutes) to acetic acid and salicylate
B. Irreversibly inhibits platelet COX so that aspirin’s antiplatelet effect lasts 8–10 days
C. Long-term use is associated with higher incidence of colon cancer
D. May be valuable in treating preeclampsia-eclampsia
C.
long-term use of aspirin at low dosage is associated with a lower incidence of colon cancer
What are the main adverse effects of aspirin at anti-thrombotic doses?
Gastric upset (intolerance) and Gastric bleeding
Which of the following is not true of Non-acetylated Salicylates?
A. All nonacetylated salicylates are effective anti-inflammatory drugs
B. They inhibit platelet aggregation
C. They may be preferable when COX inhibition is undesirable such as in patients with asthma and/or renal insufficiencies
D. They are administered in doses up to 3–4 g per day
B. DO NOT inhibit platelet aggregation (may be used in patients with bleeding tendencies)
Aspirin should not be used in children and adolescents for viral infections (with or without fever) because of an increased risk of ___________, a rare and potentially fatal pediatric illness defined as acute noninflammatory encephalopathy with fatty liver failure.
Reye’s syndrome
Which arachidonic acid isozyme is inducible by cytokines and Growth factors for the pathologic prostaglandin production?
COX-2
Which of the following is FALSE of COX-2 isozyme?
A. Has profound impact on platelet aggregation
B. Its selective inhibitors inhibit prostacyclin synthesis in the vascular endothelium
C. Inhibitors of it do not offer cardioprotective effect
D. Causes inflammation, pain, and fever
A. NO impact on platelets
Which Selective COX-2 inhibitor can cause rashes brought by its sulfonamide ring?
Celecoxib
Celecoxib interacts occasionally with which anticoagulant?
Warfarin since they are metabolized via CYP2C9
Which of the following is NOT true of Meloxicam?
A. Given to patients with SEVERE pain
B. Inhibit synthesis of TXA2 at supratherapeutic doses
C. It is an enol carboxamide related to piroxicam
D. Only preferentially selective
E. Associated with fewer GI sx compared to piroxicam
A. Mild to moderate pain only
Which Selective COX-2 inhibitors are associated with increased cardiovascular thrombotic events?
Valdecoxib and Rofecoxib
This Selective COX-2 inhibitor is used to relieve moderate post-surgical dental pain, but should only be used for a maximum of 8 days for treatment of inflammatory and painful symptoms
Etoricoxib (Arcoxia)
This is the first parenteral COX-2 selective inhibitor to be developed for the management of pain, is a prodrug that is rapidly hydrolyzed in vivo to its active form, valdecoxib, which is approximately 28,000-fold more potent against COX-2 than COX-1.
Parecoxib
Which of the following is not a Non-selective NSAID?
A. Diclofenac
B. Nimesulide
C. Diflunisal
D. Etodolac
E. Flurbiprofen
A. Nimesulide is a relatively selective COX-2 inhibitor
Which of the following is FALSE of Diclofenac?
A. Results to less GI ulceration
B. A phenylacetic acid derivative that is relatively
nonselective as a COX inhibitor
C. Combination with Misoprostol may result in Constipation
D. Elevation of serum aminotransferases
occurs more commonly with this drug than with
other NSAIDs
E. Used for prevention of postoperative ophthalmic inflammation, and solar keratosis
C. should be diarrhea
if with Omeprazole = Renal adverse effect
Which of the following is FALSE of Diflunisal?
A. Derived from Salicylic Acid but not metabolized to salicylic acid or salicylate
B. It has anti-pyretic effect
C. It is subject to capacity-limited metabolism
D. It undergoes an enterohepatic cycle with reabsorption of its glucuronide metabolite followed by cleavage of the glucuronide to again release the active moiety.
E. Does not cross the BBB
B. Largely devoid of antipyretic effects
Non-selective NSAIS that is a racemic acetic acid derivative with an intermediate half-life of 6.5 hours
Etodolac
What is the recommended dose of Etodolac in OA and RA?
300 mg twice or three times a day up to 500 mg twice a day initially followed by a maintenance of 600 mg/d
Which of the following is not a propionic acid derivative NSAID?
A. Flurbiprofen
B. Ibuprofen
C. Ketoprofen
D. Naproxen
E. Ketorolac
E. Ketorolac is a synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic, and antipyretic activities.
NSAID available in a topical ophthalmic formulation for inhibition of intraoperative miosis
Flurbiprofen
NSAID available intravenously, effective for perioperative analgesia in minor ear, neck, and nose surgery, and in lozenge form for sore throat.
Flurbiprofen
Which of the following is not true of Flurbiprofen?
A. Has been shown in rat tissue to also affect tumor necrosis factor α (TNF-α) and nitric oxide synthesis.
B. Rarely causes cogwheel rigidity, ataxia, tremor, and myoclonus
C. Hepatic metabolism is extensive
D. Its (R)(+) and (S)(–) enantiomers are metabolized differently, and it does not undergo chiral conversion
E. NOTA
E. NOTA
Which of the following is not true of Ibuprofen?
A. Oral doses of <1600 is given for anti-inflammation
B. In doses of about 2400 mg daily, ibuprofen is equivalent to 4 g of aspirin in anti-inflammatory effect
C. Ibuprofen oral and IV is effective in closing patent ductus arteriosus in preterm infants
D. In comparison with indomethacin, ibuprofen decreases urine output less and also causes less fluid retention
E. Antagonizes irreversible platelet inhibition induced by aspirin
A. Oral ibuprofen is often prescribed in lower doses (<1600 mg/d), at which it is analgesic but not anti inflammatory. It is available over the counter in low-dose forms.
Ibuprofen is relatively contraindicated in individuals with the following except:
A. Nasal polyps
B. Angioedema
C. Bronchospastic reactivity to aspirin
D. Dysmenorrhea
D. an indication
Ibuprofen in combination with __ may be an alternative to codeine-based analog
paracetamol
T/F: Common rare hematologic effects of ibuprofen include agranulocytosis and aplastic anemia.
T
A potent non-selective COX-2 inhibitor that can be given for gout and ankylosing spondylitis
Indomethacin
Epidural injections of Indomethacin produce a degree of pain relief similar to that achieved with ___________ in post-laminectomy syndrome.
methyl prednisolone
The GI adverse effect related to Indomethacin
Pancreatitis
This propionic acid derivative that inhibits both COX
(nonselectively) and lipoxygenase
Ketoprofen
T/F: Ketoprofen is superior to other NSAIDs in efficacy
F
This medication for arthritis prolongs the half-life of Indomethacin and Ketoprofen
Probenecid
The major adverse effects of Ketoprofen are on the:
GI tract and the central nervous system
This NS-NSAID decreases opioid requirement by 25-50%
*NS: Non-selective
Ketorolac
For seasonal allergic conjunctivitis
Ketorolac
Ketorolac is an effective analgesic and has been used successfully to replace ___________ in some situations involving mild to moderate postsurgical pain
morphine
Which patient below may take Dolfenal for pain relief?
A. Post-CABG patient
B. 5-year-old with Colles fracture
C. Breastfeeding mother
D. Patient under dialysis
E. 37-week pregnant patient
C. Mefenamic acid does not pass in the breast milk
Which NS-NSAID can only be given to patients aged 14 year old and above?
Mefenamic acid = MeFourteenamic acid
Renal impairment results in a doubling of this NSAID half-life and a 30% increase in the area under the curve.
Nabumetone
Pseudo porphyria and Photosensitivity as adverse effects
Nabumetone
Indicated for tumor fever
Naproxen
___ is a naphthylpropionic acid derivative. It is the only
NSAID presently marketed as a single enantiomer, its free fraction is significantly higher in women than in men, but half-life is similar in both sexes
Naproxen
Its adverse effects include rare cases of allergic pneumonitis, leukocytoclastic vasculitis, and pseudoporphyria
Naproxen
Drug combined with naproxen to reduce gastric acid production and protect the mucosal lining of the stomach
Esomeprazole
A propionic acid derivative NSAID that has a very long half-life (50–60 hours) but DOES NOT undergo enterohepatic circulation.
Oxaprozin
Non-selective NSAID with mild uricosuric effect
Oxaprozin
Which of the following does not describe peroxicam
A. It’s a nonselective COX inhibitor
B. At high concentrations, it inhibits polymorphonuclear leukocyte migration
C. Can decreases oxygen radical production, and inhibit lymphocyte function
D. Has long-half life
E. Do not cause peptic ulcer and bleeding even with high dose
E. When piroxicam is used in dosages higher than 20 mg/d, an increased incidence of peptic ulcer and bleeding (relative risk up to 9.5) is encountered
Which of the following is not an indication for Sulindac?
A. Rheumatic disease
B. Nephrotic syndrome
C. Familial intestinal Polyposis
D. Breast and prostate cancer prevention
B. Its an adverse effect
Which NS-NSAID is known to cause Stevens Johnson Epidermal Necrolysis Syndrome?
Sulindac
Which of the following is the side effect of Phenacetin?
A. Aplastic anemia
B. Agranulocytosis
C. Nephrotoxicity
D. Cardiovascular disease
C.
Phenacetin - nephrotoxic: papillary necrosis and acute tubular necrosis
Phenylbutazone - aplastic anemia and agranulocytosis
Rofecoxib and Valdecoxib - cardiovascular thrombotic
events
Which NSAID are ineffective for gout?
Aspirin, Salicylates, and Tolmetin
NSAIDs associated with the greatest toxicity
Indomethacin and Tolmetin
Least toxic NSAIDs
Ibuprofen, Salsalate, and Aspirin
Drugs associated with more liver function test abnormalities than other NSAIDs
Diclofenac and Sulindac
The safest NSAID for patients with high risk for GI bleeding
Celecoxib