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Pharm Exam 2 > Opioid > Flashcards

Opioid Flashcards

1
Q

Opioids vs Opiates

A

Opioid

  • Medication that work at the opioid receptor
  • Narcotics: Used to describe sleep agents, now for addictive drugs
  • Associated with pain relief, diarrhea treatment and euphoria

Opiates

  • Natural plant
  • Active compounds: morphine, codeine
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2
Q

Opioids MOA

A

Opioid receptor agonist; block release of pain neurotransmitters from the nociceptive fibers; activate presynaptic receptors on GABA neurons (inhibit GABA release)

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3
Q

Opioid Receptors

A

Mu (Morphone= Mu agnoist): found in the brainstem and medial thalamus; responsible for analgesia, respiratory depression, euphoria, sedation, decreased GI motility and physical dependence

  • Mu1: analgesia, euphoria and serenity
  • Mu2 (OP3 or MOR– morphine opioid receptors): respiratory depression, pruritus, prolactin release, dependence, anorexia, and sedation

Kappa (OP2 or KOR– kappa opioid receptors): limbic and other diencephalic areas, brainstem, and spinal cord; responsible for analgesia, sedation, dyspena, dependence, dysphoria, and respiratory depression

Delta: located largely in the brain; effects are not well studies (may be psychomimetic and dysphoric effects)

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4
Q

Opioid Agonist

A

Full agonist (complete response)

  • Morphine
  • Fentanyl
  • Hydromorphone
  • Codeine
  • Oxycodone
  • Methadone
  • Heroin
Partial agonist (partial response or antagonist) 
- Analgesic ceiling effect: Buprenorphine (kappa receptor), Butorphanol

Antagonist (block response)
- Naloxone, Naltrexone

  • Suboxone (buprenorphine + naloxone)
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5
Q

Short Acting Opioids

  • Codeine
  • Hydrocodone
  • Hydromorphone (Dilaudid)
  • Morphine (MSIR, Raxanol)
  • Oxycodone
  • Oxymorphone (Opana)
  • Fentanyl (Actiq)
A

USE

  • Acute pain
  • Incident pain
  • Breakthrough pain
  • For activity: post op, physical therapy, travel
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6
Q

Long Acting Opioids

  • Fentanyl (transdermal)
  • Levorphanol
  • Methadone
  • Morphine (MS Contin, Kadian, Azinza)
  • Oxycodone (Oxycontin)
  • Oxymorphone (Opana ER)
A

Use

  • Chronic pain
  • Moderate to severe pain
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7
Q

Opioid ADR

A
  • Sedation, lethargy
  • Constipation
  • Respiratory depression
  • N/V
  • Pruritus/urticaria (direct histamine response, can also cause bronchospasm)
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8
Q

Opioid Overdose

A

Triad

  • Miosis
  • Loss of consciousness
  • Respiratory depression
  • Much worse with other CNS depressant (EtOH)
  • Antidote: Naloxone (Narcan)
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9
Q

Morphine

A
  • Crosses BBB
  • ADR: direct histamine release; respiratory depression; orthostasis; constipation; N/V
  • Drug interactions rare
  • t1/2= 2hrs
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10
Q

Codeine

A
  • MOA: weak mu agnoist
  • Metabolized to morphine (50% potency of morphine)
  • t1/2= 2.5-3hrs
  • CYP 2D6 substrate: inhibited by bupropion, cimetidine, celecoxib, cocaine; warning for ultra-rapid metabolizers– lots of codeine!!!! (nursing infants, baby might be ultra rapid metabolizers)
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11
Q

Oxycodone (Oxycontin, Percocet)

A
  • Activity at mu and kappa receptors
  • High potency analgesia
  • t1/2= 2.5-3 hrs
  • Metabolized by CYP 2D6 to oxymorphone
  • Combo products: oxycodone/acetaminophen (percocet)
  • highly abused
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12
Q

Hydocodone

A
  • Most commonly used opioid
  • Weak activity at mu receptor
  • t1/2= 4hrs
  • Metabolized by CYP 2D6 to hydromorphone
  • Combo products: hydrocodone/acetaminophen (Vicodin); hydrocodone/ibuprofen (Vicoprofen)
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13
Q

Hydromorphone (Dilaudid)

A
  • Activity at mu and delta receptors
  • More potent than morphine
  • t1/2= 4 hrs
  • Metabolized by glucuronidation
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14
Q

Oxymorphone (Opana)

A
  • 10x more potent than morphine

- No P450 interactions

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15
Q

Fentanyl (Actiq)

A
  • Strong mu agonist (80x more potent than morphine)
  • CYP 3A4 metabolism
  • Transdermal: Long acting (steady state 3-6 days); clearance up to 24 hrs; dose dumping with heat; Don’t cut the patch!!!
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16
Q

Codeine allergy

A

Can take fentanyl due to different compound and structure

17
Q

Meperidine (Demerol)

A
  • Weak mu agonist (10% morphine potency)
  • Anticholinergic properties (recommended to avoid elderly)
  • Avoid with MAOIs (Respiratory depression)
  • Neurotoxic metabolite (anxiety, tremors, seizures; not reversible with naloxone)
18
Q

Propoxyphene (Darvon, Darvocet)

A
  • Weak mu agonist, NMDA antagonist
  • CYP 3A4 inhibitor
  • CNS effects: dizziness, sedation, weakness, falls, agitation, insomnia
  • Recommended to avoid in elderly
  • Neurotoxic: seizures, reversible with naloxone
  • Cardiotoxicity
19
Q

Methadone

  • Often used to help get ppl off heroin
  • Helps pt ease through withdrawal
A
  • High affinity mu agonist (Analgesic effect)
  • NMDA antagonist (Neuropathic pain)
  • Serotonin-norepinephrine reuptake inhibitor (SNRI)
  • Analgesic effect 4-8 hrs
  • Metabolized by CYP 3A4 and 2D6: initially induces 3A4 metabolism, then levels out; titrate slowly
  • t1/2= 12-150hrs (highly lipophilic)
  • Cardiotoxicity (Torsades)
20
Q

Buprenorphine

A
  • Mu receptor partial agonist (ceiling effect)
  • Kappa receptor antagonist
  • Used for opioid/heroin addiction
  • 3A4 metabolism
  • ADR: sedation; N/V; dizziness, HA; respiratory depression
21
Q

Butorphanol (Stadol)

Levorphanol

A
  • Partial Mu agonist
  • USE: moderate to severe pain
  • ADR: respiratory depression, euphoria, typical opioids ADRs
22
Q

Naloxone (Narcan)

A
  • Mu receptor antagonist
  • USE: reversal agent for opioid OD
  • Reverses respiratory depression, sedation, hypotension (works in 2-5 mins, Lazarus effects)
  • IM, subQ, IV, intranasal
23
Q

How to give nasal spray naloxone

A
  1. pull or pry off yellow caps
  2. pry off red cap
  3. grip clear plastic wings
  4. gently screw capsule of naloxone into barrel of syringe
  5. insert white cone into nostril, GIVE A SHORT, VIGOROUS PUSH on end of capsule to spray naloxone into nose; ONE HALF OF THE CAPSULE INTO EACH NOSTRIL
  6. if no reaction in 2-5 mins, give the second dose
24
Q

Naltrexone (Vivitrol)

A
  • Opioid receptor antagonist
  • USE: opioid and alcohol addiction (MOA in EtOH abuse unknown)
  • Contraindicated in pts using opioids
  • Well tolerated: some associated with N, HA, dizziness, nervousness, fatigue
25
Q

Tramadol

A
  • Synthetic codeine analog; weak Mu receptor agonist; inhibits NE and 5HT uptake (SNRI)
  • As effective as morphine for mild to moderate pain, labor pain
  • Less effective for severe or chronic pain
  • Warning for seizure risk at recommended and increased doses (higher incidence with SSRIs, TCAs, opioids, MAOI)
  • Suicide risk
  • Serotonin syndrome risk
  • ADR: dizziness, vertigo, N/V/C, HA, somnolence, pruritis
  • DRUG INTERACTIONS: CYP 2D6 and 3A4 inhibitors, serotonergic drugs, carbamazepine
26
Q

Tapentadol (Nucynta)

A
  • Mu opioid agonist, NE reuptake inhibitor
  • 1st opioids specifically approved for diabetic neuropathy
  • Stronger than tramadol
  • No P450 metabolism
  • Potentially fatal if taken with EtOH
  • CII
  • Same drowsiness/ dizziness as oxycodone with less N/V/C
27
Q

Opioid Conversions

A
  • Calculate 24 hr total dose
  • Dividing by dosing schedule
  • Reduce dose by 30-50%
  • Titrate to goal
28
Q

Opioid Drug Interaction

A
  • Erythromycin
  • Phenytoin
  • Phenobarbital
  • CY2D6 inhibitors (increase tramadol levels)
  • CYP3A4 inhibitors (increase methadone levels)
29
Q

Opioid withdrawal

A

Signs and symptoms

  • mood lability (irritability, anxiety, restlessness)
  • chills, sweating
  • abd pain/N/D
  • sneezing, rhinorrhea, dilated pupils
  • muscle weakness, pains
  • insomnia
  • Begin 8-16 hrs following last dose, peak 2-4 days
  • extremely unpleasant but not life threatening
  • resolve 7-14 days
30
Q

Opioid Dependence Treatment

A

Detoxification

  • Necessary step for long term abstinence
  • Slow taper: tapering of opioids through prescription of methadone
  • Rapid: reversal med or d/c of opioids–Naltrexone or buprenorphine; other meds (clonidine– help with noradrenergic hyperactivity; antidiarrheal meds, NSAIDs, muscle relaxants)

Goals

  • prevent or reduce withdrawal sx
  • prevent or reduce cravings
  • avoid relapse
  • restore normal physiological functions caused by opioid dependence
  • improve impairments created by opioid dependence

Non-pharmacological treatments: support groups, psychotherapy, pain contracts, family counseling

Pharmacological treatments

  • Methadone
  • Buprenorphine
  • Naltrexone
31
Q

CDC Chronic Pain Guidelines

A
  • Pain lasting > 1 yr

12 recommendations

  • nonopioid and nonpharm treatments preferred (consider opioids when benefits outweigh risks)
  • establish treatment goals before starting opioid therapy
  • discuss risks and realistic benefits
  • start with IR opioids
  • start with lowest effective dosage
  • for acute pain, lowest effective dose at limited duration (3-7 days)
  • evaluate treatment q1-4 wks after starting or increasing dose; if dosing stable, evaluate q 3months (if harm> benefit, taper and d/c)
  • evaluate risk for harms (sleep disorders, pregnancy, renal/liver insufficiency, >65 yrs old)
  • review history of controlled substance prescriptions
  • urine drug testing prior to initiation and annually thereafter
  • avoid concomitant use of BZDs
  • arrange treatment for opioid use disorders

Pharm Exam 2 (7 decks)

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