3 - Opioids Flashcards by mike smith

What are Mu1 receptors responsible for:

Analgesia

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What are Mu2 receptors responsible for:

Respiratory depression, miosis, reduced gastric motility, sedation, euphoria, pruritis, urinary retention, PHYSICAL DEPENDENCE

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What are Kappa receptors responsible for?

Contribute to analgesic properties (but Mu1 is responsible for most of the analgesia)

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What is the Delta receptor responsible for?

Located in the periphery and selective for enkephalins

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Which is more hydrophilic - morphine or fentanyl?

Morphine

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Which is more lipophilic - morphine or fentanyl?

Fentanyl

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What causes tolerance?

Down-regulation of opioid receptors

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What is opioid-induced hyperalgia?

Increased pain or pain sensitivity without a change in medical condition

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Desensitization is the result of:

Down-regulation

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Which opioid is associated with the greatest histamine release and thus “itching” sensation?

Morphine

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Morphine - MOA?

High affinity for Mu1 and Mu2

Weak affinity for Delta/Kappa

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Morphine - pharmacokinetics:

Significant first pass effect if oral

Least lipophilic - only a small amount crosses BBB -> less euphoria than fentanyl or heroin

Will cross placenta

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Heroin is __ times more potent than morphine

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Presence of morphine in urine could indicate exposure to:

Morphine
Heroin
Codeine

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Morphine - AE’s?

Increases ICP (caution in head injury)

Respiratory depression

N/V

Pruritus

HOTN

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Hydromorphone (Dilaudid) - MOA:

Mu receptor agonist

Metabolite of morphine

More lipophilic than morphine

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Hydromorphone (Dilaudid) - note on extended release form:

Requires provider training q 2 yrs - Risk Evaluation and Mitigation Strategy (REMS) drug

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Hydrocodone ER (Zohydro ER) - MOA:

Less binding affinity than morphine

Metabolizes to hydromorphone

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Oxycodone (OxyContin) - MOA:

Mu receptor agonist - low binding affinity

Metabolizes to noroxycodone and oxymorphone (active metabolites)

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Oxymorphone (Numorphan) - MOA:

Semi-synthetic Mu receptor agonist

Greater analgesic profile than morphine

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Codeine - MOA:

PRODRUG (no analgesic activity)

Metabolized to morphine

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Codeine - clinical use:

Mild to moderate pain

Antitussive

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Codeine - box warning:

Death delated to ultra-rapid metabolism of codeine to morphine

Not recommended for peds <12

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What is the CYP enzyme responsible for converting codeine to morphine?

CYP2D6

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If Codeine is single ingredient, what schedule?

If codeine combined with another analgesic (i.e. APAP), what schedule?

III

If Codeine combined with Guaifenesin (cough medicine), what schedule?

Buprenorphine (Buprenex) C-III - MOA:

Mixed agonist/antagonist Partial Mu agonist and Kappa ANTagonist

Buprenorphine (Buprenex) - clinical use?

Opioid detoxification As effective as methadone Resistant to naloxone d/t long duration of action

Butorphanol (Stadol) C-IV - MOA?

Partial Mu and Kappa agonist

Butorphanol (Stadol) C-IV - clinical use:

Pain management Pain during labor (if epidural is not possible)

Butorphanol (Stadol) C-IV - AE’s?

Can produce unwanted dysphoria

Nalbuphine (Nubain) - MOA:

Not controlled Partial Mu antagonist Strong Kappa agonist

Nalbuphine (Nubain) - clinical use:

Sedation with minimal respiratory depression Used to reverse ventilatory depression in opioid overdose WHILE MAINTAINING some alalgesia Think “Nubain” is the kinder Narcan

Meperidine (Demerol) C-II - MOA:

Strong Mu and Kappa agonist Anticholinergic effects

Meperidine (Demerol) C-II - clinical use:

ACUTE DOSING ONLY Relief of moderate to severe pain SHIVERING AND RIGORS USE NOT GENERALLY RECOMMENDED

Meperidine (Demerol) C-II - CI’s?

Renal impairment MAOI’s Hepatic impairment Elderly (caution)

Meperidine (Demerol) C-II - AE’s?

Anticholinergic effects (can cause tachycardia and mydriasis) HOTN, delirium, seizures Severe withdrawal GENERALLY - AVOID THIS DRUG

Fentanyl C-II - MOA:

Mu receptor agonist Synthetic 75 to 125 time more potent than morphine More lipophilic (easily crosses BBB leading to more euphoria) Rapid onset/shorter duration than morphine

Fentanyl - pharmacokinetics:

Renal excretion Easy distribution in tissues due to high lipohilicity

Fentanyl - clinical use?

Moderate to severe pain (acute) Moderate to severe pain (chronic)(patches)

Fentanyl - transdermal onset of action:

12 to 24 hours

What is the TIRF REMS program?

Transmucosal Immediate Release Fentanyl Risk Evaluation and Mitigation Strategy Mitigate the misuse, addiction, overdose, and serious complications due to medication errors with the use of TIRF medicines

Which Fentanyl derivative has the fastest peak effect, duration and elimination?

Remifentanil (think “r” revved up)

What do Alfentanil, Sufentanil, and Remifentanil all have in common?

They don’t accumulate when infused

Methadone - MOA:

Potent agonist of Mu, Kappa, Delta Antagonist of NMDA receptor Inhibits serotonin and norepi reuptake

Methadone - clinical use:

Chronic pain syndrome (CA, non-CA, neuropathic) Detoxification of opioid addiction

Methadone half-life?

Unpredictable - 8 to 59 hours Difficult to titrate Analgesia duration is SHORTER than t1/2, toxicity d/t accumulation can occur

Methadone - cardiac AE’s?

Arrhythmias can occur - prolonged QT interval

Pentazocine (Talwin) C-IV - MOA:

Partial Mu agonist Full kappa agonist

Pentazocine (Talwin) C-IV - clinical use:

Moderate to severe pain Labor when epidural is not possible

Pentazocine (Talwin) C-IV - AE’s:

``` HTN Hallucinations Dysphoria Dizziness Tachycardia ```

Tramadol (Utlram) C-IV: MOA:

Partial Mu receptor agonist Serotonin and norepinephrine reuptake inhibitor

Tramadol (Ultram) - metabolism:

Majority of therapeutic activity depends on metabolism Ultra-rapid metabolizers -> significant respiratory depression

Tramadol (Ultram) C-IV- AE’s:

SEROTONIN SYNDROME Seizures reported at recommended doses

Tapentadol (Nucynta) C-II - MOA:

Chemically similar to tramadol Mu agonist, norepi reuptake inhibitor

Tapentadol (Nucynta) C-II - clinical use?

Diabetic peripheral neuropathy (ONLY OPIOID WITH THIS INDICATION)

What is the only indication for oral Naloxone?

Opioid-induced constipation

Naltrexone - MOA:

Mu receptor competitive antagonist Competes but does not displace opioids

Naltrexone - clinical use:

Longer duration of action (10 hrs) Tx of ETOH and opioid dependence

Naltrexone can be combined with ___ for weight management:

Bupropion

Nalaxone (Narcan) - MOA:

Competitive antagonist of Mu receptors - displaces opioids

Nalaxone (Narcan) - clinical use:

Reversal of opiate overdose

Naloxone can be given every ___ to ___ minutes:

2 to 5

When tapering off opioids, what percentage deduction in amount of drug (for non-addicted patients):

20 to 50 percent (of original dose) per week