analgesics Flashcards
NSAIDS AND OPIODS
2 types of analgesics
important inflammatory mediators that are produced locally and dont circulate to any significant degree
prostaglandin
sensitizes nerve endings to the action of bradykinin, histamine, and other chemical mediators
PGE2
act by inhibiting the synthesis of prostaglandins
NSAID function
binds to cyclooxygenase, irreversible –> cant be reproduced
*if NSAID binds to cyclooxygenase –> platelet does not work
prostaglandin 2 synthase –> acts at final inflammatory level
platelets are fragments of thrombocytes (anuclear) –> no capacity to regenerate
SSRI –> will interfere with seratonin pathway –> inhibits platelet aggregation
thromboxane A 2 –> mediator of platelet aggregation
NSAID random facts about blood
acetaminophen (tylenol)
ibuprofen (advil)
celecoxib (celebrex)
3 popular nsaid drugs
acetaminophen (tylenol)
ibuprofen (advil)
celecoxib (celebrex)
3 popular nsaid drugs
indication: pain (mild), fever
dose: 325-1000 mg; 1 tab q4-6h
acetaminophen
– Act by inhibiting COX and enhancing 5-HT release (attenuates pain mediator generaIon)
– Regulates body temperature by acIng centrally at the hypothalamus; PG synthetase inhibition
acetaminophen moa
– Anti-inflammatory
– Anti-platelet
– Anti-pyretic
– Central
ASA (aspirin) distinctions
No inflammatory control i.e. not an NSAID – No platelet inhibition – Anti-pyretic – Central pain relief only – No GI effects – Safe in pregnancy
acetaminophen distinctions
ADVERSE EFFECTS
• Common: nausea, rash, headache
SERIOUS ADVERSE EFFECTS
• Hepatic: acute hepatotoxicity usually w/ doses >4g/d
• Renal: acute renal tubular necrosis, chronic analgesic nephropathy
acetaminophen effects
NT that we see as a target NT in nausea pathway
seratonin
why do people over use acetaminophen?
acute hepatotoxicity –> causes death
*therefore dont use with people who have liver disease
why do people over use acetaminophen?
acute hepatotoxicity –> causes death
*therefore dont use with people who have liver disease
classic sign of liver disease
jaundice, yellow sclera
- Acetaminophen/Antihistaminic Combos (additive hepatotoxicity)
- ASA (additive nephropathy)
- Lidocaine Topical (additive methemoglobinemia)
acetaminophen drug interactions
• INDICATION
• Mild to Moderate Pain, Primary
Dysmenorrhea, Fever
• DOSING [100-800mg] • 400mg q4-6h
ibuprofen indication
• CLINICAL PHARMACOLOGY – NSAID Analgesic
• Mechanism of Action
– Inhibits COX, reducing PG and TXA2 synthesis
ibuprofen
ADVERSE EFFECTS
• Common: headache, fluid retention, ecchymosis, photosensitivity
NOTABLE ADVERSE EFFECTS
• Neuro: tinnitus
• Renal: acute renal tubular necrosis, chronic analgesic nephropathy
ibuprofen adverse effects
• DRUG INTERACTIONS
• ASA NSAIDs, Acetaminophen (addiIve
hemorrhagic risk)
• Acetaminophen, Cyclosporine (addiIve nephrotoxicity)
ibuprofen drug interactions
• INDICATION
• ArthriIs, Ankylosing SpondyliIs,
Dysmenorrhea, Acute Pain
• DOSING [50-400mg] • 200 mg qd-bid
celecoxib
• INDICATION
• ArthriIs, Ankylosing SpondyliIs,
Dysmenorrhea, Acute Pain
• DOSING [50-400mg] • 200 mg qd-bid
celecoxib indication
• INDICATION
• ArthriIs, Ankylosing SpondyliIs,
Dysmenorrhea, Acute Pain
• DOSING [50-400mg] • 200 mg qd-bid
celecoxib indication
• INDICATION
• ArthriIs, Ankylosing SpondyliIs,
Dysmenorrhea, Acute Pain
• DOSING [50-400mg] • 200 mg qd-bid
celecoxib indication
• CLINICAL PHARMACOLOGY – NSAID Analgesic
• Mechanism of AcIon
– SelecIvely inhibits COX-2 and reduces PG synthesis
celecoxib moa
ADVERSE EFFECTS • Common: headache BLACK BOX WARNINGS • CV: Stroke, CHF, MI • GI: Bleed, ulceraIon/perforaIon
celecoxib adverse effects