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
Other names for indomethacin and Nabumetone are
indocin and relafen
Primary in dication for piroxicam are
- OA
- RA
- Gout
Piroxicam may produce what types of symptoms
flu like
Diclofenac is indicated for
primarily arthritis but good for acute dental pain
T/F diclofenac has minimal effect on platelets
t
What risk does diclofenac have
risk of bone marrow suppression
Diclodenac is FDA class
B
What drug category does piroxicam fall under
NSAID (oxicam)
What drug class does diclofenac belong to
NSAID (phenylacetic acids)
What are the different NSAID propionic acids
- Ibuprofen
- Fenoprofen
- Fluribiprofen
- Ketoprofen
- Naproxen
- Oxaprozin
Propionic acids are good for treating what kinds of pain
acute pain
Other names for ibuprofen are
motrin and advil
Indications for ibuprofen
mild to moderate pain
What are the doses for ibuprofen for analgesia and inflammation
- Analgesia= 200-400 mg 6hrs
- Anti-inflammation= 600-800mg 6hrs
T/F Ibuprofen has been associated with sedation
t
Other name for fluribprofen is
ansaid
Issues with flurbiprofen
- *not indicated for routine analgesic use
- Potentially fetotoxic and embryotoxic
Other names for naproxen
aleve and anaprox
Indications for naproxen
mild to moderate dental pain
Naproxen is associated with _ in young kids
rash
Avoid what form of naproxen in the elderly
Na+ salt form
What form of naproxen should be avoided for initial therapy
delayed release
Etodoloc belongs to what family of NSAIDs
pyranocarboxylic acid
Other name for etodoloc is .
lodine
Indications for Etodoloc
Mild to moderate pain
Etodoloc is associated with abnormal
fetal limb development and decreased fertility, testicular atrophy
Another name for aspirin is
acetylsalicylic acid
Other Salicylates are
Aspirin and diflunisal
All salicylates are associated with _ syndrome
reyes
Salicylates should be avoided in what population
children (avoid in treating fever due to viral illness –> reyes)
Diflunisal has a (greater/lesser) effect on platelets compared to ASA
lesser
Diflunisal shouldn’t be used in combo with
acetaminophen
Celecoxib is what class of NSAID
COX2 inhibitor
Celecoxib is indicated for
RA and OA ONLY
Celecoxib has a (higer/lower) incidence of gi effects
lower
T/F Celecoxib is indicated for odontogenic pain
f
Celecoxib puts patients at (increased/decreased) risk of CV events, MI, storke, etc.
increased
T/F There is cross reactivity between celecoxib and other NSAIDs
t
FDA classification of celecoxib
C
Avoid celecoxib in patients with
- CVD
- daily aspirin use
- Hypersensitivity
- Asthmatics
- Pregnant
Metabolize of celecoxib is antagonized by
fluconazole and other agents metabolized via cytochrome p450 2C9
Prostaglandins are involved in
GI mucosal protection (mediate pain, fever and inflammation)
Thromboxanes are involved in
hemostasis
