10. Analgesics Flashcards
Arachidonic acid is derived from
phospholipids in membranes. Enzyme phospholipase
Arachidonic acid can be broken down into two different pathways, what are they
cyclooxygenase and lipoxygenase pathway
What are the products of the cyclooxygenase pathway
-Prostaglandins and thromboxane
What are the products of the lipoxygenase pathway
-5-HETE and leukotrienes
What are the different peripheral analgesics
- Acetaminophen
- NSAIDs
MOA of acetaminophen
-Inhibition of cyclooxygenase in different manner from NSAID
Clinical activities of acetaminophen
- Analgesia
- Antipyretic
- No anti-inflammatory effects
- No inhibition of platelet aggregation
- No inhibition of platelet aggregation
- no gastric irritation
T/F Acetaminophen crosses the placenta
t
Describe the toxicity of acetaminophen
- Acute toxicity with as little as 6 g taken within a short period
- Metabolite NAPQI binds to liver proteins injuring hepatocytes
- Hepatotoxicity
How is hepatotoxicity induced by acetaminophen treated
gastric lavage
What is the daily max dose for Acetaminophen for adults
4 gm
Mechanisms of analgesia for NSAIDs
- inactivation of cyclooxygenase
- Inhibition of bradykinin synthesis
Anti-inflammatory mechanism of NASIADs
- Inactivation of cyclooxygenase
- Inhibition of WBC migration
- Inhibition of WBC lysosomal enzyme release
- Inhibition of phosphodiesterase
Anti-pyretic mechanism of NSAIDs
-Inhibition of prostaglandin synthetase in hypothalamus
T/F NSAIDs don’t have a ceiling effect
f
Adverse effects of NSAIDs are
- Allergy
- Anemia
- Bronchospasm
- Increased risk of coronary and cerebrovascular thrombotic events
- GI irritation/bleeding
- Inhibits platelet aggregation
- Hepatotoxic
- Renal toxicity (renal papillary necrosis)
- Mutagenic
- Carcinogenic (leukemia possible with indomethacin, phenylbutazone)
- Fetotoxicity
- Reye’s syndrome (kids)
Describe the fetotoxic effects of NSAIDs in 1st, 2nd and 3rd trimesters
1st
-Teratogenic effects
2nd and 3rd
- Premature closure of ductus arteriosis
- Fetal pulmonary hypertension
- Prolonged gestation
- Decreased uterine contractions
- Bleeding at delivery
NSAID drug interactions
- Anticoagulations
- Triamterene
- Lithium
- Phenytoin
- Valproic acid
- Digitalis
- Cyclosporine
- Fluoroquinolones
- Imidazole antifungals
T/F NSAIDs should be taken on an empty stomach
f
Mixture of NSAIDs with _ increases risk of gastritis
alcohol
Contraindications for NSAIDs
- Allergy
- Alcoholism
- Asthma
- Gastritis/ peptic ulcers
- Pregnant
- Blood dyscrasia
- Renal function impairment
- Psychiatric illness
- Recent coronary artery bypass graft (CABG)
Indomethacin belongs to what drug category
NSAIDs (Indoleacetic acid)
Incidactions for indomethacin
- Osteoarthritis
- Rheumatoid arthritis
Indomethacin shouldn’t be used in what populations
pediatric and geriatric and pregnant
Indomethacin may worsen what diseases
CNS diseases such as epilepsy and risk of leukemia
What drug class does Nabumetone belong to
NSAIDs (Naphthylakanones)
Nabumetone is primarily used for
osteoarthritis and rheumatoid arthritis and TMJ
Nabumetone is FDA class _
C