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845 > Opioid Analgesics Part III (Other Drugs) > Flashcards

Opioid Analgesics Part III (Other Drugs) Flashcards

1
Q

Mepergan

A
  • Meperidine + Promethazine
  • Analgesia, sefation, and anti-nausea effects
  • Used as a preanesthetic medication
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2
Q

Meperidine

A
  • Demerol
  • Moderate to severe pain
  • Less smooth muscle spasm, constipation, and depresssion of cough reflex
  • Equianalgesic to morphine
  • NO MIOSIS
  • SE: Tachycardia
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3
Q

Meperidine Toxicity

A
  • CNS excitation
  • Increased seizure risk (normeperidine especially due to long half life)
  • Metabolite is excreted by kidney, don’t use with renal insufficiency
  • Naloxone doesn’t inhibit seizures and could worsen the sedative effects
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4
Q

Hydromorphone

A
  • Dilaudid
  • Management of pain
  • HP = high potency, Exalgo = ER
  • WARNING: high potential for abuse and risk of respiratory depression that could result in death
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5
Q

Oxymorphone

A
  • Numorphan
  • Suppository for moderate to severe pain
  • Parenteral administration for moderate to severe pain, support of anesthesia, and relief of anxiety in patients with dyspnea
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6
Q

Opana

A
  • Oxymorphone
  • Oral
  • Black box warning for abuse potential
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7
Q

Fentanyl

A
  • Actiz
  • Pain management
  • Use IV, epidural
  • 100x potency of morphine
  • Lipid soluble, terminated by redistribution after IV administration
  • Has other preparations like tozenge, film, tablets, patches
  • Lazanda Nasal spray only for persistent cancer pain
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8
Q

Carfentanil

A
  • Synthetic opioid
  • 10,000x more potent than morphine and 100x more potent than fentanyl
  • Used to tranquilize large animals
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9
Q

Fentanyl Black Box Warnings

A
  • Abuse potential
  • Repiratory depression
  • CYP450 3A4 interactions, don’t use with 3A4 inducers since it can increase fentanyl concentration
  • Risk of use in combination with benzos and CNS depressants which can cause profound sedation, respiratory depression, coma, and death
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10
Q

Remifentanil

A
  • Ultiva
  • Similar to fentanyl in action and use
  • Metabolized by plasma esterases and is eliminated in minutes
  • Minute-to-minute control of analgesia
  • Can intensify muscle tone causing truncal rigidity when given quickly via IV which can interfere with ventilation
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11
Q

Heroin

A
  • Diacetylmorphine
  • No clinical use in USA
  • Crosses BBB rapidly due to high lipid solubility
  • Metabolized to monoacetylmorphine and morphine
  • Morphine is responsible for the effects of heroin (same SE)
  • Schedule 1
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12
Q

Heroin Addictive Theory

A
  • Ventral tegmental area (DA neurons) prohects to the nucleus accumbens as part of the mesolimbic system
  • Most addictive substances affect this area as a final common path
  • Faster a drug of abuse gets to this area the more addictive the substance tends to be
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13
Q

Methadone

A
  • Dolophine
  • Orally active
  • 15-40 hour half life
  • Mu agonist
  • Risk of QT prolongation, safe during pregnancy
  • Uses: chronic pain, treat narcotic abstinence syndrome, maintenance of opioid use disorder
  • Special license to prescribe for methadone maintenance
  • Potential for diversion and abuse
  • Satisfies cravings and allows a person to function in society
  • Recommended minimum 12 mo treatment
  • Prolongs QT interval
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14
Q

Codeine

A
  • Antitussive, analgesic + ASA/APAP
  • 10% is metabolized to morphine by CYP2D6
  • Limited by low potency (don’t use for severe pain), low affinity for receptor, and frequent N/V
  • Prodrug of morphine with limited oral availability
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15
Q

Codeine Black Box Warning

A
  • Respiratory depression and death in children with CYP2D6 polymorphism that makes them ultra-rapid metabolizers
  • Tramadol may have a similar problem
  • Alternatives: NSAIDs and APAP, lowest effective weight-based dose used PRN only, CYP3A4 metabolized drugs
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16
Q

Oxycodone

A
  • Oxaydo, Oxecta
  • Opioid agonist for mild to severe pain
  • Used in combination with ASA, APAP, and ibuprofen
  • Targiniq ER = Oxycodone and naloxone
17
Q

Apomorphine

A
  • Apokyn
  • Little analgesic activity may dperess respiration
  • D2 receptor agonist - induces vomiting by directly acting on CTZ
18
Q

Hydrocodone

A
  • Antitussive and pain relief

- Used for nail congestion and moderate pain as well

19
Q

Brands of Hydrocodone

A
  • Histinex HC (Hydrocodone, phenylephrine) - nasal congestion
  • Hycodan (Hydrocodone, homatropine) - prevent abuse
  • Hycotuss (Hydrocodone and guaifenesin) - expectorant
  • Tussionex (Hydrocodone and chlorpheniramine) - antihistamine
  • Vicodin (hydrocodone + APAP) - pain relief
  • Apadaz (Benzhydrocodone _ APAP) - acute pain, gi metabolism to hydrocodone
20
Q

Zohydro ER

A
  • ER hydrocodone without APAP
  • Can be crushed and abused
  • Box warning: addiction, abuse, misuse, life threatening respiratory depression
21
Q

Pentazocine

A
  • Talwin
  • Oral
  • Analgesic for mild to moderate pain
  • Weak mu antagonist or partial agonist
  • Blocks morphine analgesia and induces opioid withdrawal in the dependent
  • DOESN’T block morphine respiratory depression
  • Kappa agonist effects are blocked by naloxone
22
Q

Pentazocine Effects

A

only has limited respiratory depression risk

  • Agonist at kappa and sigma receptors
  • Withdrawal has mild morphine like syndrome
  • Dysphoria and uncontrolled, strange thoughts occur with repeated high doses
23
Q

Butorphanol

A
  • Stadol
  • Parenteral supplement to balanced anesthesia for pre/post-operative analgesia
  • Stadol NS (nasal spray) used to manage pain
  • Mu antagonist (induces abstinence syndrome in dependent) and kappa agonist (analgesic activity)
  • SE: limited respiratory depression, lower incidence of psychotomimetic effects, mild abstinence syndrome
24
Q

Buprenorphine

A
  • Buprenex
  • CIII
  • Analgesic for moderate to severe pain
  • Partial agonist at mu receptors (high affinity, low dissociation)
  • Repiratory depression is less than other mu agonist, euphoria, and mild morphine type abstinence syndrome
  • Replacement for methadone as a maintenance drug for opioid use disorder
  • Displaces opioid and causes withdrawal, used for opioid maintenance and detoxification
25
Q

Suboxone

A
  • Buprenorphine + Naloxone
  • Comes in film versions too, some for pain therapy
  • Can be given every 6-8 hours instead of once daily
  • Analgesic effect wears off faster
26
Q

Tramadol

A
  • Ultram
  • 30% affinity for mu receptors but also blocks 5HT and NE reuptake
  • Partially reversed by naloxone
  • Can cause seizures and increase seizure risk
  • Possible serotonin syndrome risk as well
27
Q

Ultracet

A
  • Tramadol + APAP
  • Hepatotoxicity blcok box warning, monitor APAP intake
  • Converted to active metabolism by CYP2D6, avoid tramadol use in kids
28
Q

Tapentadol

A
  • Nucynta
  • Oral analgesic for moderate to moderately severe pain
  • For neuropathic pain
  • Mu opioid agonist and inhibition of NE reuptake
  • CII
  • Warnings about serotonin risk and risk for seizures
29
Q

Dextromethorphan

A
  • OTC cough suppressant that is considered safe at therapeutic doses
  • D-isomer of opiate agonist levorphanol
  • No analgesic or addictive effects
  • Doses 5-10 times the normal produce euphoria possible, PCP like effect?
30
Q

Diphenoxylate

A
  • Lomotil
  • For antidiarrhea effects
  • CV
  • Diphenoxylate has abuse potential so it is combined with atropine to make lomotil
  • Atropine produces undesirable anticholinergic effects when taken more than therapeutic dose
31
Q

Loperamide

A
  • Imodium
  • OTC for diarrhea
  • As effective as diphenoxylate
  • Poorly absorbed after oral administration
  • Acts directly on intestinal musculature to inhibit motility
32
Q

Analgesia in Pregnant/Lactation

A

Pregnancy

  • Use APAP
  • Avoid NSAIDs, codeine, hydrocodone, and tramadol

Lactation

  • Use smallest doses for shortest durations
  • Ibuprofen is NSAID of choice for breastfeeding mothers
33
Q

Opioid Overdose

A

-Triad of symptoms
1. Depressed respiration
2. Pinpoint pupils, hypoxia may cause pupils to dilate however
3, Coma - additive or synergistic effects to produce CNS and/or respiratory depression
-Treat by restoring respiration by administering naloxone

34
Q

Naloxone

A
  • Evzio (injection), Narcan (nasal spray)
  • May precipitate an opioid withdrawal syndrome
  • Watch patient, usually only lasts 1-1.5 hours, could start another overdose after that time
  • Usually patients recover enough to survive
35
Q

Pure Competitive Opioid Antagonists

A
  • Naloxone, nalmefene, and naltrexone (ordered by increases in half life and duration)
  • At all opioid receptors with no opioid agonist activity
  • No effect when used without narcotics
  • Can enhance pain in those with pain
  • Withdrawal includes rhinorrhea, yawning, chills, piloerection, hyperventilation, muscular aches, vomiting, diarrhea
  • Naltrexone used for treatment of opioid and alcohol dependence while others are used for suspected/known overdoses
36
Q

Naltrexone

A
  • Vivitrol (ER injectable suspension)
  • Oral, high dropout rates
  • Long acting opioid receptor antagonist
  • Overcomes problems of agonists like social resistance and no diversion of maintenance drug
  • Treats alcohol and opioid dependence
  • May be vulnerable to precipitation of withdrawal symptoms if transitioning from methadone or buprenorphine

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