Pain Drugs (Wolff) Flashcards
What are the 4 NSAIDs used to treat mild to moderate and moderate to severe nociceptive pain?
aspirin
ibuprofen
naproxen (long half-life)
celecoxib
Nociceptive pain
perception of input from a nociceptor
if somatic - injury to body tissues: well localized and sharp
if visceral - viscera stretch receptor: poorly localized, deep, dull and cramping
Neuropathic pain
abnormal neural activity secondary to disease, injury or dysfunction of the nervous system
aspirin
irreversibly inhibits COX-1 and 2; NSAID used for nociceptive pain; toxicities - ulcer, increased risk of bleeding, increased risk of Reye syndrome
Reye syndrome
A rare but serious condition that causes confusion, swelling in the brain, and liver damage (kids); can be triggered by aspirin
Which agent used to treat pain can trigger Reye syndrome?
aspirin
ibuprofen
non-aspirin NSAID; reversibly inhibits COX-1 and 2; management of pain; increased risk for MI and stroke (contraindicated in CABG); increased risk of GI bleed and not recommended around 20 weeks gestation or later in pregnancy (fetal renal dysfunction)
What is a feared complication of non-aspirin NSAIDs in pregnancy
20 weeks gestation of later due to potential to cause fetal renal dysfunction leading to oligohydramnios
Celecoxib
non-aspirin NSAID; reversible inhibits COX-2 (not COX-1); does NOT inhibit platelet aggregation (no risk of bleeding); increased risk of MI and stroke
According to the American Heart Association, what is the NSAID of choice?
naproxen (longer half-life); use the lowest effective dosage for the shortest possible time
acetaminophen
agent used to treat minor aches, pains and headache and moderate to severs pain (does NOT suppress inflammation); MOA not fully known; toxic metabolite when glutathione is depleted; risk of medication errors can cause overdosage and hepatotoxicity with acute liver failure and death
agent used in acetaminophen toxicity?
N-acetylcysteine
Treatment for nociceptive pain?
NSAIDS and acetominophen
The 3 first line treatments for neuropathic pain?
Antidepressants: 1. SNRI-duloxetine or 2. TCA-amitriptyline
or 3. Ca2+ ch alpha 2 delta inhibitors - pregabalin or gabapentin
SNRI
serotonin-NE reuptake inhibitor; anti-depressant; duloxetine
duloxetine
anti-depressant serotonin-NE reuptake inhibitor (SNRI); used for fibromyalgia and neuropathic pain; increased risk of suicidal thoughts and behaviors
TCA
tricyclic antidepressants; amitriptyline - used to treat neuropathic pain
amitriptyline
tricyclic antidepressants used to treat neuropathic pain and chronic fatigue syndrome; increased risk of suicidal thoughts and behaviors, anticholinergic effects, serotonin withdrawal and withdrawal syndrome
CNS alpha-2-delta Ca2+ channel blockers
pregabalin and gabapentin - does NOT bind GABA receptors!
Pregabalin
CNS alpha-2-delta Ca2+ channel blocker (does NOT bind GABA receptors!); first-line agent used in neuropathic pain, fibromyalgia, diabetic neuropathy, seizures; pain benefits evident in 1st week; depression and suicidal ideation
Second line treatments for neuropathic pain?
antidepressant + u agonist - Tramadol and Tapentadol
antidepressant + u agonist
Tramadol (partial u agonist - weak) and Tapentadol (u against - strong)
Tramadol
Second line treatments for (severe) neuropathic pain; antidepressant + partial u agonist; multiple back box warnings - risk of errors/ingestion by children - OD and death (respiratory depression); addiction, abuse and misuse; withdrawal syndrome; risk of respiratory depression
Third line treatments for neuropathic pain?
NMDA antagonists - Ketamine
Selective alpha 2 agonists - Dexmedetomidine and Clonidine
Ketamine
noncompetitive NMDA receptor antagonist; blocks glutamate; can go into a cataleptic-like state (dissociation from surrounding environment); used for acute and chronic pain and indicated in general anesthesia; requires careful monitoring
Which neuropathic agent can cause a patient to go into a cataleptic-like state?
Ketamine; noncompetitive NMDA receptor antagonist; blocks glutamate; dissociation from surrounding environment; used for acute and chronic pain and indicated in general anesthesia; requires careful monitoring
Dexmedetomidine
Selective alpha 2 agonists in the brainstem; a potent anxiolytic used in postoperative pain management; can cause significant harm when used in error
Clonidine
Selective alpha 2 agonists in the brainstem; used for hypertension and as epidural pain relief; administered by continuous infusion through an epidural catheter
Fourth line treatments for neuropathic pain?
Botulinum toxin injections or intrathecal ziconotide
Ziconotide
N-type VG Ca2+ channel blockers on afferent nerves of the dorsal horn; 4th line treatment in neuropathic pain (severe chronic pain); VERY expensive - intrathecal route; severe psychiatric symptoms and neurological impairment
Botulinum Toxin
decreases the release of acetylcholine at 4 sites: NMJ, autonomic ganglia, postganglionic parasympathetic nerve endings and postganglionic sympathetic nerve endings that release Ach
What are the two anti-migraine medications?
Sumatriptans (triptans) and dihydroergotamine
dihydroergotamine
late treatment option for migraines; can cause “St. Anthony’s fire” - behavioral disturbances and pain and distal gangrene in fingers, nose, penis and toes
