Analgesics 5 Flashcards
Enumerate the uses of indomethacin?
- Articular inflammatory conditions: as rheumatoid arthritis, osteoarthritis, ankylosing
spondylitis and acute gouty arthritis. - Anti-pyretic in refractory cases of fever (Hodgkin’s fever).
- To induce closure of Patent ductus arterious in early infancy.
- Batter’s syndrome (syndrome in children with juxtaglomerular hyperplasia, high renin, Ald., normotension)
- Delay premature labor (Tocolytic, suppress uterine contraction).
Mention the prodrug that changed to active sulfide in the body => less GIT toxicity?
Sulindac
Drug associated with hepatic abnormalities (elevation of transaminase)?
Diclofenac
Drug used as short term analgesic for post -operative pain and Its analgesic effect is equivalent to morphine?
Ketorolac
Drug Long t ½ (50 h.), so can be used once /day (due to enterohepatic circulation)?
Piroxicam
Oxicam undergo complete absorption after oral administration?
Piroxicam
Oxicam show some cox-II selectivity and cause Less gastric ulceration/ less adverse effect on the kidney
Meloxicam
Prodrug Its half-life of more than 24 hours and used once-daily and its the only nonacid NSAID?
Nabumetone
All the following true about Selective Cox-2 inhibitors (Coxibs) except?
A. Has no antiplatelet or cardio-protective effect
B. Enhance the effect of ADH
C. Vasoconstriction occurs reducing the glomerular filtration rate (GFR) which may result in acute renal failure
D. Associated with high gastric ulceration
D / Associated with little or no gastric ulceration
T OR F/ Selective Cox-2 inhibitors, inhibit COX-2-mediated prostacyclin synthesis in the vascular endothelium result in the risk of cardiovascular adverse effects as heart attacks, thrombosis and stroke
T
Two drugs have CVS side effects which are removed from the market?
Rofecoxib and valdecoxib
Selective Cox-2 inhibitors has a sulfur atom and may cause problem in patients with allergies to sulfonamides?
Celcoxib
All the following are true about Paracetamol except?
A. Well and complete absorption after oral administration
B. Cross placental barrier and cause teratogenic effect during pregnancy
C. Inactivated in the liver by conjugation with glucuronic acid and sulfuric acid
D. Inhibit PGs synthesis centrally only
B / Cross placental barrier and safe during pregnancy (non-teratogenic)
Mention the pharmacological actions of Paracetamol?
analgesic, anti-pyretic action only
Enumerate the adverse effect of Paracetamol?
- Allergic reactions such as skin rash
- Acute paracetamol toxicity lead to fatal hepatic necrosis
- Chronic use of paracetamol may lead to nephrotoxicity in susceptible individuals