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Anesthesia Pharmacology Medications > Week 7: Opiates > Flashcards

Week 7: Opiates Flashcards

1
Q

Morphine

  1. Mechanism of Action
  2. Unionized %, Lipid solubility, Onset
  3. T1/2 and Duration
A
  1. Mu opioid receptor agonist
  2. 23%, 1.4, -> slow onset
  3. 2-3 hours, 4-6 hours
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2
Q

Hydromorphone

  1. Synthetic or nonsynthetic?
  2. Potency related to morphine
  3. IV onset and peak
  4. Oral onset and peak
A
  1. Non-synthetic morphine derivative
  2. 5-10x more potent than morphine
  3. Onset 5 minutes, peak 10-20 minutes
  4. Onset 20-40 minutes, peak 1.5 hours
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3
Q

Codeine

  1. Mechanism of action
  2. Synthetic or nonsynthetic?
  3. Other effects
A
  1. Has a low affinity for opioid receptors, so analgesic effects are due to about 10% conversion to morphine which causes analgesia
  2. Non-synthetic morphine derivative
  3. Very good anti-tussive agent
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4
Q

Oxycodone

  1. Comparison to morphine
  2. Synthetic or nonsynthetic?
  3. Dose
A
  1. Less 1st pass metabolism than morphine
  2. Nonsynthetic morphine derivative
  3. Adults: 5-15mg every 6 hrs (oral) and Peds: .05-.15mg/kg every 4-6 hours (oral)
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5
Q

Oxycontin

  1. Synthetic or nonsynthetic?
  2. Dose
  3. Why abuse potential?
A
  1. Nonsynthetic morphine derivative
  2. 10-20 mg q 12 hrs… up to 80-160 mg for opioid tolerant patients
  3. Get high when crushed or chewed… the sustained release is only when taken whole
    * *Generally only used for chronic pain patients
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6
Q

Naloxone

  1. Mechanism of action
  2. Route and dosage
  3. Metabolism
  4. What to watch for?
A
  1. Competitive antagonist at Mu, K, Delta receptors
  2. IV, IN, or SQ -> .4 mg, peak effect 1-2 minutes
  3. Glucuronidation in the liver, excreted in the urine (1/2 life 65 minutes in adults, 3 hrs in neonates)
  4. Know half life of opioid you want to reverse to make sure effect outlasts them, watch for withdrawal symptoms such as HTN, Tachycardia, pulmonary edema, and NV
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7
Q

Naltrexone

  1. Mechanism of action
  2. Use
A
  1. Long action oral opioid antagonist
  2. Opioid and alcohol dependent addiction
    * *Antabuse
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8
Q

Nalmefene

  1. Dose
  2. Use
A
  1. Equipotent to naloxone: 15-25mcg every 5 min IV
  2. Longer duration than naloxone so more useful with ventilatory depression
    * *Very expensive
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9
Q

Meperidine

  1. Synthetic or nonsynthetic?
  2. Comparison to morphine
  3. Uses
  4. SE
A
  1. Synthetic Opioid
  2. 1/10 the potency of morphine with higher lipid solubility (faster onset) and less bradycardia and respiratory depression
    * *actually INCREASES HR
  3. Spinal anesthetic: has some LA activity due to sodium channel block, postoperative shivering (K and a2 effect)
  4. Can cause N/V, active metabolite -> leads to seizures and delirium, dysphoric and psychomimetic effect (K effect)
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10
Q

Serotonin Syndrome

  1. What opiates can trigger this? What makes them more susceptible?
  2. Signs and Symptoms
A
  1. Meperidine inhibits reuptake of serotonin, so when given with concurrently with MAOIs or SSRIs can cause serotonin syndrome
  2. Delirium, Fever, Convulsions

**Does not occur with meperidine derivatives (fentanyls)

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11
Q

Fentanyl

  1. Mechanism of Action
  2. Comparison to morphine
  3. Onset
  4. Important pharmacokinetics
A
  1. Almost completely a Mu receptor agonist
  2. 50-100x more potent than morphine
  3. 3-5 minutes
  4. Lipid solubility of 816 -> rapid onset due to rapid distribution to VRG; Larger Vd -> longer elimination half life -> leaves VRG slowly (As an infusion….half life makes it long acting)
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12
Q

Fentanyl

  1. Metabolites and Metabolism
  2. Context sensitive half life on length of administration
  3. Dosage for Infusion
A
  1. 100% hepatic metabolism to INACTIVE metabolites (clearance is directly related to liver blood flow and is decreased with P450 inhibitors)
  2. 1 minute infusion: T1/2 5 minutes, 1 hour: 20 min, 8 hours: 250 minutes
  3. Loading dose: 8-12 mcg/kg; Maintenance dose: 1-2 mcg/kg/hr
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13
Q

Alfentanil

  1. Mechanism of action and comparison to morphine
  2. Onset, why?
  3. Metabolism and metabolites
  4. Dose
A
  1. Almost completely Mu receptor agonist; 10x as potent as morphine
  2. 1-2 minutes, 90% unbound is unionized so rapidly crosses BBB
  3. 30-50% hepatic metabolism to INACTIVE metabolites
  4. Loading: 35-70mcg/kg; Maintenance: .25-.50 mcg/kg/min
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14
Q

Remifentanil

  1. Mechanism of action and comparison to morphine
  2. Onset, Offset
  3. Metabolism and pharmacokinetics
  4. Dose
A
    1. Almost completely a Mu receptor agonist; 50-100x more potent than morphine (equipotent to fentanyl)
  2. 1 minute; 6-9 minutes
  3. Non-specific plasma esterases (NOT pseudocholinesterase) -> CONSTANT clearance, not affected by liver flow, renal failure, or length of infusion
  4. Loading: 1-2mcg/kg, Infusion: .05-.25 mcg/kg/min
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15
Q

Opioid Tolerance

  1. Mechanism
  2. Treatment
A
  1. Alteration of NMDA receptors and its second messenger system
  2. NMDA antagonists like ketamine and magnesium
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16
Q

Butrophanol

  1. Mechanism of action and affinity for receptors
  2. Advantages
  3. Disadvantages
A
  1. Mixed agonist/antagonist: low mu antagonism, moderate agonism of K, low sigma affinity
  2. Limited ventilatory depression, low potential for physical dependence
  3. Hard to then use opioid agonists if needed, have ceiling effect (increase dose does not increase response)
17
Q

Buprenorphine

  1. Mechanism of action and affinity for receptors
  2. Use
  3. Advantages
  4. Disadvantages
A
  1. Mixed agonist/antagonist: Minimal actual antagonism, but has the ability to displace agonist from the mu receptor
  2. Postoperatively and in epidural space
  3. Great analgesic potency (.3mg =10mg MOS4), limited ventilatory depression or physical dependence
  4. Hard to then use opioid agonists if needed, have ceiling effect (increase dose does not increase response)
18
Q

Tramadol

1. Metabolism

A
  1. CYP 2D6 -> active metabolite of transmethyltramadol
19
Q

Sufentanil

  1. Relative potency to morphine
  2. Lipid solubility, nonionized fraction, protein binding
  3. Metabolism and excretion (t1/2)
A
  1. 500-1000x
  2. 1778, 20%, 93%
  3. Hepatic metabolism, renal excretion -> 1-2 hour T1/2

Anesthesia Pharmacology Medications (9 decks)

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