Opioids Flashcards
rx length
Up to 3 days for most things; up to 7d max
MOA
Most bind to and stimulate the Mu opioid receptors (agonists). Inhibit neurotransmitter (substance P, glutamate, CGRP) release AND reduce transmission of pain signals. Hyperpolarise postysynaptic cell, so less likely to generate any further pain sensations. Raise the pain threshold at the spinal cord level (dorsal horn). Alter the brain’s perception of pain. The stronger the agonist, the greater the effect
opioid contras
Use in Head Injuries (can increase intracranial pressure), Use in Pregnancy (stick to short term use), Impaired Pulmonary Function, Impaired Hepatic or Renal Function, Endocrine Disease, Undiagnosed abdominal pain
AEs
nausea, constipation, respiratory depression. flushing, pruritis, hypotension from release of histamine. Pinpoint pupils that do not respond to light.
overdose symptoms and treatment
Overdose: CNS depression (coma), resp depression (apnea or bradypnea), miosis. Give Narcan (opioid receptor antagonist) IV, IN, IM, or SC, onset in 2-3 min and give 2nd dose at 3 min if still not awake; effect lasts 2 hrs, so pts should be monitored for 4-6 hrs after Narcan; induces opioid withdrawal (agitation, anxiety, confusion, tachycardia, HTN.
interactions
“Sedative-Hypnotics: Benzodiazepines, Diphenhydramine, Soma, tramadol
Alcohol
Antipsychotics
MOAIs”
pt counseling - 4
“PO initial onset in 20 min, full benefit at 1hr.
take antinausea 20 min before
Let pt know when using combo w/ acetaminophen - caution against taking too much aceta otherwise
Avoid alcohol. don’t take benzodiazepines or diphenhydramine at same time; space out 2-4 hrs if you really need it due to extra sedative effect”
co-prescribe
Co-prescribe antiemetic (Zofran) and senna + bisacodyl; also naloxone if risk factors (prior OD, substance abuse, doses >120MME/d, concomitant benzo)
weakest agonist
codeine
codeine contras
Absolute: <12 y/o, <18 y/o after tonsillectomy / adenoidectomy. Avoid in <18 y/o
most constipating opioid
codeine
MOA: mild-mod agonist. Targets the mu-receptor and inhibits reuptake serotonin and norepinephrine
tramadol
tramadol contras
Caution in pts w/ seizure hz or those on TCAs or serotonergic agents
which opioids are only partially antagonised by naloxone
tramadol, Tapentadol (Nucynta)
tramadol dose adjustment for whom?
CrCl <30 or severe hepatic impairment, dose Q12 hours
indications: “ped surgery/ED
extended release: neuropathic pain”
Tapentadol (Nucynta) PO, IV
AEs: Low GI effects, but risk of seizures, risk of serotonin syndrome when combined with SSRIs. Partially antagonised by Naloxone
Tapentadol (Nucynta) PO, IV
order of strength of the mild-mod agonists
oxycodone > hydrocodone > tramadol > codeine
morphine contra
avoid in kidney dz
AEs: Thought to cause more pruritus, nausea, and sedation than hydromorphone (Dilaudid) or fentanyl
morphine
interactions: Tapentadol (Nucynta) PO, IV
SSRIs
switch morphine non-responders to
oxy
MOA: strong agonist. Synthetic - More potent than Morphine (~50-100x). Rapid onset of action: IV formulation has peak effect on average in 10 minutes.Very short acting. secreted in the stomach and reabsorbed, creating a second peak
fentanyl
fentanyl dosed in
micrograms
change fentanyl transdermal patch Q
Q72 hrs
indication for fentanyl transdermal patch
chronic pain once stable
fentanyl contras
Avoid in patients with obesity hypoventilation syndrome, liver failure
pt counseling for transdermal patch
Patch: proper disposal in sharps container necessary to protect kids/pets
methadone contras
Avoid use in older adults for pain, or older adults w/ delirium or at risk
when is the peak of opioid withdrawal symptoms?
72 hrs after last pill
do hospital providers need a x waiver to give buprenorphine to a pt in withdrawal?
no
when is x waiver needed?
Rx for buprenorphine outside of hospital
x waiver allows rx for how many pts
up to 30
MOA: strong agonist. suppress craving and withdrawal symptoms and block the acute effects of other opioids
methadone
indications: Opioid dependence. Chronic, severe pain. Neonatal withdrawal. Postanesthesia shivering,and blood product-induced rigors. IV: adjunctive sedative for procedures (less common).
methadone
AEs: Risk for seizure, serotonin syndrome. at common doses, not an effective pain medication, may cause neurotoxicity including delirium, and safer analgesics are available. Prolongs QT interval, constipation, mild drowsiness, ED, low libido
methadone
MOA: Mixed agonist-antagonist (partial agonist). Long-acting, partial mu agonist, delta and kappa antagonist
Buprenorphine (Butrans®)
indications: “OUD / opioid withdrawal (flu-like sx, n/v/d, abd pain, HTN, mydriasis, tachycardia, hyperreflexia, insomnia, irritability, anxiety, depression).
Acute pain in opioid naïve pts IM/IV”
Buprenorphine (Butrans®)
MOA: opioid receptor blockade secondarily diminishes dopamine activity that is otherwise enhanced by alcohol. Mu, Kappa, Delta Antagonist
Naltrexone (Vivitrol) PO or long-acting IM
indications: alcohol and opioid dependence - Maintenance treatment to prevent relapse
Naltrexone (Vivitrol) PO or long-acting IM
