Analgesics: Narcotics Flashcards
What is the MOA of narcotics?
Act as mu-opioid receptor agonists
-alter the perception and response to pain centrally and peripherally
Which narcotics also inhibit reuptake of norepinephrine?
Modifies the ascending pain pathway
-also are mu- agonists
Tramadol
Tapentadol
Which narcotic is a mu-agonist with weak kappa-antagonist activity?
Buprenorphine
Which narcotics are partial agonists of mu- and kappa-receptors?
- butorphanol
- nalbuphine
What are contraindications of narcotics?
Severe respiratory disease / depression, including:
-acute asthma (unless patient is mechanically ventilated)
Paralytic ileus
What are black box warnings of narcotics?
Serious life-threatening / fatal respiratory depression may occur
-monitor closely for respiratory depression
—especially during initiation / dose escalation
Opioids expose patients to risks of addiction, abuse, and misuse
- potentially leading to overdose / death
- assess each patient’s risk prior to prescribing
- monitor all patients regularly for developing of these behaviors / conditions
Accidental ingestion can result in fatal overdose
- even one dose of an opioid
- especially in children
What is the black box warning for opioid use in pregnancy?
Prolonged use during pregnancy can result in neonatal withdrawal syndrome
-may be life threatening if not recognized and treated according to protocols developed by neonatology experts
What are common members of the narcotics class?
- buprenorphine
- fentanyl
- hydromorphone
- methadone
- hydro/oxycodone
- tramadol
- tapentadol
What are uncommon members of the narcotics class?
- alfentanil
- butorphanol
- codeine
- levorphanol
- meperidine
- nalbuphine
- opium tincture
- oxymorphone
- pentazocine
- remifentanil
- sufentanil
What are brand names of buprenorphine?
- Buprenex
- Belbuca
- Probuphine
- Butrans
- Subutex
What are the dosage forms of buprenorphine?
- injection
- TD patch
- buccal film
- SC implant
- SL tablet
What is buprenorphine used for?
- management of pain severe enough to require ATC, long term opioid treatment and for which alternative treatment options are inadequate
- opioid dependence
- opioid withdrawal in heroin-dependent hospitalized patients
What pregnancy category is buprenorphine?
C
What is buprenorphine dosing for pediatric acute pain (moderate-severe) for children 2-12 years?
IM, slow IV: 2-6 mcg/kg every 4-6 hours
What is buprenorphine dosing for adults, usual dose?
0.15-0.6mg every 4-8 hours PRN
What is buprenorphine dosing for adults, acute pain?
0.3mg IM/IV every 6-8 hours PRN
What is buprenorphine dosing for adults with chronic pain, TD patch, opioid-naive?
Initial: 5mcg/hour applied once every 7 days
-max patch dose of 20mcg/hour/7days
What is buprenorphine dosing for adults with chronic pain, TD patch, receiving daily dose of 30-80mg oral morphine equivalent
10mcg/hour/7days
What is buprenorphine dosing for adults with chronic pain, buccal film, opioid-naive?
Initial: 75mcg once daily
What is buprenorphine dosing for adults with chronic pain, buccal film, receiving daily dose of 30-89mg oral morphine equivalents?
Initial: 150mcg every 12 hours
What is buprenorphine dosing for adults with chronic pain, buccal film, receiving daily dose of 90-160mg oral morphine equivalents?
Initial: 300mcg every 12 hours
What is buprenorphine dosing for adults with opioid dependence, SL tablets?
Day 1: 8mg PO
Usual range: 12-16mg/day during induction
Target dose: 16mg/day maintenance
What is buprenorphine dosing for adults with opioid withdrawal in heroin dependent hospitalized patients (unlabeled use), IV?
0.3-0.9mg every 6-12 hours
How is buprenorphine dosing affected by hepatic impairment, buccal film / SL tablet?
For severe impairment (Child-Pugh class C):
-reduce starting dose and titration dose by 50%
What are the most common adverse reactions of buprenorphine?
- sedation
- hypotension
- dizziness
- nausea
- vomiting
- headache
- respiratory depression
- constipation
- application site rash (patch, implant)
What are rare / severe / important adverse reactions of buprenorphine?
- respiratory depression
- QTc prolongation
- hepatotoxicity
- severe allergic reactions
What are major drug interactions that affect buprenorphine?
CNS depressants and alcohol
-increased sedation / dizziness
CYP 3A4 inhibitors / inducers
-alter its metabolism
QTc prolonging drugs
-may increaserisk of arrhythmias
MAO-I inhibitors
-may increased sedation
What are contraindications of the buprenorphine TD patch?
- management of mild / acute / intermittent pain
- management of pain requiring short-term opioid analgesia
- management of postoperative pain
What are essential monitoring parameters of buprenorphine?
-CNS depression
-BP
—for hypotension
-liver enzymes
What are counseling points for buprenorphine?
-avoid excessive alcohol
-may cause drowsiness
—impair ability to operate machinery
- may cause constipation requiring laxatives
- may cause physical / psychological dependence with prolonged use
- notify healthcare provider if pain unrelieved
- do not place direct heat (heating pads) on patch
- report any allergic reactions
- never cut the TD patches
-rotate patch sites on arms, chest, and back
—apply to hairless / dry area
-keep any used / unused patches away from children
What are black box warnings of buprenorphine?
Misuse / abuse by chewing / swallowing / snorting / injecting drug extracted from buccal film / TD system will result in:
- uncontrolled delivery of buprenorphine
- significant risk of overdose / death
Concomitant use of BDZ / alcohol / other opioids / other CNS depressants may result in:
- profound sedation
- respiratory depression
- coma
- death
Insertion / removal of implant are associated with risk of:
- implant migration
- protrusion
- expulsion
What are rare but serious complications that may result from improper insertion of buprenorphine implant in upper arm?
-nerve damage
-migration
—resulting in embolism and death
What is preferred over buprenorphine monotherapy for maintenance of opioid dependence?
Combination of buprenorphine and naloxone
-naloxone is a non-absorbed opiate antagonist that blocks effects of buprenorphine if snorted / injected
—makes the combo an abuse-deterrent
What patch dose of buprenorphine is associated with an increased risk of QT interval prolongation?
20mcg/hour
What neurological disorder can buprenorphine exacerbate?
Cause seizures in patients at risk
-can lower seizure threshold
What do prescribers have to be certified in to prescribe buprenorphine tablets and TD patch?
REMS program
What are brand names of fentanyl?
- Abstral
- Actiq
- Duragesic
- Fentora
- Sublimaze
- Lazanda
- Subsys
What are the dosage forms of fentanyl?
- TD patch
- TD device
- buccal tablets
- buccal lozenge
- nasal spray
- SL spray
- SL tablet
- injection
What is fentanyl injection used for?
- relief of perioperative pain
- adjunct to general / regional anesthesia
What is fentanyl TD patch used for?
-management of pain in opioid-tolerant patients
—severe enough to require:
—
What is fentanyl transmucosal lozenge, buccal tablet, NS, SL tablet / spray used for?
-management of breakthrough cancer pain in opioid-tolerant patients who are:
—already receiving and tolerant to ATC opioid therapy for their underlying persistent cancer pain
What pregnancy category is fentanyl?
C
