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Pharm Exam 2 > Bannon: Opiod Drugs > Flashcards

Bannon: Opiod Drugs Flashcards

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1
Q

Hydromorphone (Dilaudid)

A

Older semi-synthetic morphine derivative used as painkiller

More potent than morphine; equivalent efficacy

Oft-requested in ER
Was used primarily as immediate release, but now other formulations (extended-release in ‘11)

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2
Q

Opiate Receptors:

A

Mu
Kappa
Delta

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3
Q

Mu:

Encoded by:

A

Mu: for morphine (endogenous ligands are beta-endorphin and more recently recognized endomorphins)

  • Encoded by MOP gene
  • Many opioid agonists and antagonists show preference here
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4
Q

Kappa:
Encoded by:
What is relatively strong here?
In some cases, have actions opposite to:

A

Kappa: for ketoclazocine (endogenous ligand is dynorphin)

  • Encoded by KOP gene
  • Partial agonists relatively strong here
  • May have more importance in spinal anesthesia
  • In some cases, have actions opposite to mu receptors
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5
Q

Delta:
Encoded by:
Morphine and other opioid drugs:

A

Delta: for vas deferens (endogenous ligand is enkephalin)

  • Encoded by DOP gene
  • Morphine and other opioid drugs weaker here
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6
Q

Opioid-Like Receptor NOP:

Insensitive to:
Elicits : (2)

A

Opioid-Like Receptor NOP: nociceptin/orphanin FQ peptide receptor
o Insensitive to classical opioid antagonists
o Elicits hyperalgesia (increased sensitivity to pain) and anti-opiod effects suprasinally
o Elicits antinociceptive spinal effects

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7
Q

Single Gene Results in Several Receptor Subtypes Seen Pharmacologically
Example:

A

Single Gene Results in Several Receptor Subtypes Seen Pharmacologically:

Example: MOP gene elicits μ1, μ2, and μ3

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8
Q

Single Gene Results in Several Receptor Subtypes Seen Pharmacologically

Possible Explanations: (3)

A

Alternative splicing of common gene products (really not important)

Receptor dimerization to give different subtypes (may be important)*

Interaction of common gene product with signaling proteins (may be important)*
- For example, drug dependent activation of signaling pathways (which pathway gets activated depends on which drug bind)

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9
Q

Morphine (Gold Standard)

Absorption:
Metabolism:

A

Absorption: well absorbed by multiple routes of administration (oral, IM, IV, subQ, rectal, epidural or intrathecal)

Metabolism: extensive first-pass metabolism limits oral use (~35% bioavailability)

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10
Q

Morphine (Gold Standard)

Excretion:

A

Polar metabolites excreted in the urine

  • After chronic use, polar metabolite morphine-6-glucuronide is responsible for analgesic effects
  • Therefore, toxicity may result in renal insufficiency due to decreased clearance of this active metabolite (confusion, agitation)
  • Morphine-3-glucuronide is another minor metabolite that may be proconvulsant (CNS excitatory properties; again, take care with renal insufficiency)

Glucoronide conjugates also secreted in bile

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11
Q

Morphine (Gold Standard)

Formulations: (4)

A

Long-Acting SR Beads
Morphine SR + Naltrexone (Embeda)
Post-Surgical Formulations (DepoDur)
Infumorph/Astromorph/Duramorph

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12
Q

Morphine

Long-Acting SR Beads:

A

Long-Acting SR Beads: to be swallowed; if chewed or combined with alcohol, can cause release of too much morphine

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13
Q

Morphine

Morphine SR + Naltrexone (Embeda):

A

Morphine SR + Naltrexone (Embeda): for continual use with decreased risk of abuse (if crushed, opioid antagonist naltrexone will be freed)

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14
Q

Morphine

Post-Surgical Formulations (DepoDur):

A

Post-Surgical Formulations (DepoDur): single liposomal injection (last 48 hours)

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15
Q

Morphine

Infumorph/Astromorph/Duramorph:

A

Infumorph/Astromorph/Duramorph: continual epidural or intrathecal infusion formulations

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16
Q

Uses/Effects of Morphine:
Analgesia
Basics:

A

Basics:

  • Pain relief without general sensory loss or loss of consciousness
  • Pain reported as present but no longer bothers the patient
  • Better against continuous dull pain than sharp, intermittent pain
  • Multiple supraspinal (ie. brain) and spinal sites of action
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17
Q

Uses/Effects of Morphine:
Analgesia
Issues: (2)

A

SIGNIFICANT tolerance to this effect (as well as most others)

Paradoxical hyperalgesia may occur (MOA unclear- possibly increased glutamate transmission in the dorsal horn)

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18
Q

Uses/Effects of Morphine:
Analgesia
Use:

A

Use: surgical anesthesia (in combination with other drugs- multimodal anesthesia)

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19
Q

Uses/Effects of Morphine
Mood and Cognitive Effects
Basics:

In normal (Pain-Free) Individuals:

A

Basics: cause euphoria and tranquility

Normal (Pain-Free) Individuals: often unpleasant
o Dysphoria (intense feelings of depression or discontent)
o Difficulty thinking
o Drowsiness
o Nausea

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20
Q

Uses/Effects of Morphine
Mood and Cognitive Effects

Site of Action:
Side Effects:
Use in Combat Injured Subjects:

A

Site of Action: unclear (locus ceruleus, mesolimbic DA, nucleus accumbens all possible)

Side Effects: confusion and sedation (especially in the elderly)

Use in Combat Injured Subjects: prompt administration of morphine reduced risk for PTSD

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21
Q

Uses/Effects of Morphine
Miosis

Cause:
Sign of Toxicity/Abuse:

A

Cause: excitation of the PS innervation to the pupil

Sign of Toxicity/Abuse: little/no tolerance to this effect with chronic use

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22
Q

Uses/Effects of Morphine
Cough Inhibition

Mechanism:

A

Mechanism: depression of cough reflex mediated by medullary cough center (can administer a dose that easily provides cough suppression without respiratory depression)

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23
Q

Uses/Effects of Morphine
Respiratory Depression

Mechanism:
Importance:

A

Mechanism: dose-related depression mediated via brainstem centers

  • Decreased response to CO2
  • Synergistic depression seen with many other CNS drugs

Importance: especially of concern in patients with COPD and pain

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24
Q

Uses/Effects of Morphine
Increased Intracranial Pressure

Mechanism:
Importance:

A

Mechanism: due to increased pCO2 (causes cerebrovascular dilation)

Importance: needs to be taken into consideration with head trauma

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25
Uses/Effects of Morphine Nausea/Emesis Mechanism:
Mechanism: mediated by area postrema chemoreceptor trigger zone - Relatively uncommon in supine patients but common in ambulatory patients (hints at possible vestibular component to mechanism) - Tolerance to this effect develops rapidly
26
Uses/Effects of Morphine Cardiovascular Effects: Mechanism:
Effects: peripheral vasodilation (reduced peripheral resistance) and inhibition of baroreceptor reflex - Not evident in supine patient, however, orthostatic hypotension and fainting can be seen upon standing Mechanism: may be due in part to histamine release
27
Uses/Effects of Morphine Cardiovascular Use:
Use: IV morphine used for immediate relief of dyspnea from acute pulmonary edema associated with left ventricular failure - Decreases anxiety, venous tone and peripheral resistance
28
Uses/Effects of Morphine GI Effects:
Effects: decreased propulsive contractions (leads to increased water absorption and constipation) - Little tolerance to this effect and therefore can be a problem with chronic use
29
Uses/Effects of Morphine Ureter: Uterus: Itching:
Ureter: increase sphincter tone to decrease urinary output (especially in the elderly) Uterus: leads to prolongation of labor (also need to worry about fetal effects) Itching: due to effects on CNS and peripheral nerves - Mechanism: probably substance P and/or histamine related
30
Morphine Toxicity Causes:
Causes: clinical overuse, renal insufficiency, accidental OD or suicide attempt
31
Morphine Toxicity Key Signs:
Key Signs: coma, respiratory depression and pinpoint pupils
32
Heroin
Potent and fast-acting (“heroic”) Converted to morphine by deacetylation in vivo
33
Oxycodone Use: Cancer patients: with aspirin: acetaminophen: ibuprofen:
Use: painkiller (has a morphine backbone) for the short-term relief of moderate pain - Cancer patients (ER release form) - In combination with aspirin (Percodan) - In combination with acetaminophen (Percocet) - In combination with ibuprofen (Combunox)
34
Oxycodone Absorption: Efficacy:
Absorption: more orally active than morphine Efficacy: roughly equivalent maximal efficacy to oral morphine
35
Oxycodone: Acurox:
Popular Drug of Abuse: possibly lethal Acurox: recently FDA approved drug used as a deterrent for abuse - Combination of niacin (unpleasant effects) and inactive ingredients that convert to a gel upon attempted extraction - Unfortunately, has driven up abuse of other opiates
36
Meperidine | Use:
Use: painkiller whose use is now limited to acute pain management (ie. post-surgical) - Rapid onset and short duration of action - Irritating to tissue if given IM
37
Meperidine | Unique Toxicity:
Unique Toxicity: - Seizures, twitching, delirium and psychiatric changes - Due to accumulation of a long-lived metabolite
38
Codeine | MOA:
MOA: weak full agonist with modest analgesic activity after deacetylation to morphine - However, 10% of the population lack the enzyme for conversion
39
Codeine | Pharmacokinetics; (3)
Absorption: good oral absorption Highly protected from first pass glucuronidation High oral:parenteral potency ratio
40
Codeine | Use:
- Most often given in combination formulations (ie. Tylenol 3) - Also a sustained release formulation - Antitussive effects (possibly through distinct receptors; efficacy questioned for this use)
41
Fentanyl Pharmacokinetics Potency: Duration of Action:
Potency: 80-100x more potent than morphine (effective but potentially dangerous) Duration of Action: short (with no active metabolites)
42
Fentanyl | Use: (2)
- IV use for surgical anesthesia (often with droperidol) | - Acute post-op pain (patient controlled analgesia by transdermal iontophoresis)
43
Fentanyl | Other unique delivery routes for pain in opioid-tolerant patients:
Transdermal patch (change every 48-72 hours) o Be careful of exposure of patch to heat o Be careful with concurrent use of CYP3A4 inhibitors (ie. clarithromycin, ketoconazole) Effervescent buccal tablet, buccal film or lonzenge on a stick (for breakthrough pain)
44
Propoxyphene (Darvon) MOA: Efficacy: Safety:
MOA: partial agonist painkiller Efficacy: very low Safety: low therapeutic index (not very safe)
45
Propoxyphene (Darvon) Formulations: Toxicity:
Formulations: - Combinations with aspirin/caffeine (Darvon compound) - Combinations with acetaminophen (Darvocet) Toxicity: accumulation of a toxic metabolite can lead to a variety of effects - Cardiotoxicity, convulsions, OD (being pulled from the market!)*
46
Nalbuphine/Butophanol/Pentazocine MOA: Side Effects:
MOA: kappa agonists and weak mu mixed agonists or antagonists Side Effects: - More adverse behavioral symptoms (psychomimetic effects/Salvinorin-A like effects)
47
Nalbuphine/Butophanol/Pentazocine | Effects: (4)
Effects: - Less analgesia - Less respiratory depression - Less tolerance - Less naloxone reversibility*
48
Tramadol Structure: MOA: Use:
Structure: synthetic codeine derivative MOA: active metabolite is a weak mu agonist - Also blocks 5HT and NE uptake - Some GABA mechanisms also suspected Use: should be limited to chronic neuropathic pain (due to need for slow titration); however, being seen more and more for use in acute pain
49
Tramadol Formulations:
- Extended release | - In combination with acetaminophen (Ultracet)
50
Tramadol Side Effects: (3)
- Reports of increased frequency of seizures - Esp. in patients with seizure history or on antidepressant medications - DDIs may lead to serotonin syndrome (buildup of serotonin)
51
Tapentadol Structure: MOA: Risks:
Structure: tramadol-like compound MOA: weak mu agonist (also a NE reuptake inhibitor; NOT 5HT) Risks: risk of abuse and serotonine syndrome unclear at this point
52
Methadone MOA: Pharmacokinetics: Half-life:
MOA: full agonist Pharmacokinetics: - Long Half-Life: slow metabolism in most people and high fat solubility - Need careful initial titration - Hepatic metabolism: no active metabolites, and therefore safe in patients with renal problems
53
Methadone | Use:
Chronic pain (esp. in patients with renal issues) Addict detoxification or maintenance
54
Buprenorphine MOA: Pharmacokinetics: Duration:
MOA: partial agonist at mu receptor (but more potent than full agonist methadone) Pharmacokinetics: - Long Duration of Action: very slow dissociation from receptor (resistance to naloxone receptor)
55
Buprenorphine Use: Formulations: (3)
Use: - Opiate dependence (can be prescribed in office setting) Formulations: - Sublingual formulation - Combination with naloxone (Suboxone) to prevent abuse - Sustained release formulation (once a month dosing) currently being tested
56
Naloxone and Naltrexone | MOA:
MOA: opiate receptor antagonists (mu > kappa and delta)
57
Naloxone:
ER form for opiate OD Blocks antidiarrheal, antitussive and analgesic effects of opioids
58
Naltrexone:
Oral form used for prevention of relapse to heavy drinking - Poor compliance - Hepatotoxicity if taken at 3-4x the recommended dose Recently approved injectable ER formulation (once a month) to maintain alcohol abstinence
59
Naltrexone SR + Buprenorphine SR (Contrave):
Naltrexone SR + Buprenorphine SR (Contrave): recently approved for obesity treatment - Modestly effective - Concerns about cognitive and CV side effects
60
Methylnaltrexone MOA: Administration: Use:
MOA: opiate antagonist that does NOT cross BBB (therefore, will not affect analgesia) Administration: injectable Use: approved recently for opioid-induced constipation in terminal patients under palliative care
61
Diphenoxylate/Loperamide MOA: Action:
MOA: mu receptor agonists Action: meperidine congeners that have very poor absorption from the gut (exclusive use in diarrhea)
62
Diphenoxylate/Loperamide | Formulations: (2)
Diphenoxylate + Atropine (Lomotil) | Loperamide (Immodium)
63
Dextromethorphan Structure: MOA:
Structure: D isomer of methylated levorphanol (does not have typical opioid effects) MOA: NMDA receptor antagonist and sigma receptor agonist
64
Dextromethorphan Use: (2)
Antitussive (MOA unclear, efficacy questioned but seems to work) Abuse potential now evidence
65
Dextromethorphan | Contraindications:
Contraindications: young children; also discouraging use of combination products (ie. with antihistamines etc.)
66
Nalfurafine MOA: Use:
MOA: new kappa opioid receptor agonist (no action at mu receptors) Use: relief of itching - However, taking a kappa agonist should be VERY unpleasant (recall psychomimetic effects)
67
Current Investigative Uses of Opioid Drugs: (3)
- Antidepressants - Anti-addiction - Cardioprotection .
68
General Principles of Therapeutic Use of Opioids: (2)
Only symptomatic relief: do not treat underlying disease Tolerance: repeated administration can lead to tolerance and physical dependence; however, important to note that most people that are using prescribed opioids do NOT become addicts

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