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)