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Pharmacology Winter Exam 2 > L16-17: Opioids & Antagonists Lecture > Flashcards

L16-17: Opioids & Antagonists Lecture Flashcards

1
Q

What are the three types of opioid receptors?

A

Mu (µ), Kappa (κ), Delta (δ)

Sigma (σ) is not an opioid receptor but may play a role in CNS effects.

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2
Q

What is the primary action of Mu (µ) receptors?

A

Analgesia, euphoria, sedation, side effects

Stimulation of these receptors decreases pain transmission.

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3
Q

What is the definition of ‘opioid’?

A

Having properties similar to drugs derived from opium.

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4
Q

What are endogenous opioid peptides?

A

Enkephalins, beta-endorphin, dynorphin

Released in response to pain and decrease responsiveness to pain.

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5
Q

What effect does nociceptin have?

A

Antagonizes analgesia by µ receptor and may inhibit the reward system.

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6
Q

Fill in the blank: Opioids decrease the release of _______ in the dorsal horn.

A

excitatory transmitters

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7
Q

True or False: Tolerance develops to all effects of opioids.

A

False

There is no tolerance to miosis, constipation, or seizures.

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8
Q

What are common adverse effects of opioids?

A

Nausea, vomiting, constipation, urinary retention, respiratory depression

Adverse effects can be dose dependent.

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9
Q

What mechanism do all opioid receptors share?

A

Coupled to G i/o proteins.

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10
Q

What is one of the effects of opioids on the gastrointestinal system?

A

Decreased gastric motility, leading to constipation.

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11
Q

What is the role of dynorphin A?

A

May increase sensitivity to pain in the spinal cord.

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12
Q

What is the effect of opioids on respiratory function?

A

Decreases response of brain stem to elevated CO2.

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13
Q

What happens to body temperature with opioid use?

A

Decreased due to dysregulation in the hypothalamus.

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14
Q

What is the relationship between opioids and euphoria?

A

Opioids increase firing in the reward system, leading to euphoria.

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15
Q

Fill in the blank: Opioids can produce histamine release, causing _______.

A

flushing, itching, sweating

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16
Q

What effect do opioids have on the urinary system?

A

Decreases urine output and increases sphincter tone.

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17
Q

What is the consequence of opioid overdose on mental state?

A

Can cause graded depression of cortical function, leading to coma or death.

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18
Q

What is the effect of opioids on the cardiovascular system?

A

Decreased blood pressure common; bradycardia may occur.

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19
Q

What is one of the primary therapeutic uses of opioids?

A

Analgesia, to decrease sensation and reaction to pain.

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20
Q

What is the impact of opioids on the release of GABA?

A

Opioids decrease the release of GABA, allowing activation of pain modulation pathways.

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21
Q

True or False: Opioid abuse and addiction has decreased in recent years.

A

False

Opioid abuse and addiction has become a major health problem.

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22
Q

What is a common misconception about opioid allergies?

A

People often claim they are allergic to opioids due to histamine reactions, but true allergies are very rare.

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23
Q

What is one possible consequence of long-term opioid use?

A

Hyperalgesia may occur, making pain transmission more effective.

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24
Q

What occurs in anyone who uses opioids chronically, for any reason?

A

Tolerance and physical dependence

This is a common consequence of chronic opioid use.

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25
Q

When is addiction most common with opioid use?

A

When opioids are used for euphoric effect

Addiction can also occur with medical use of opioids.

26
Q

What happens if a patient develops severe pain and is relieved by an opioid?

A

This provides reinforcement

The reward pathway is activated.

27
Q

What is advised to patients regarding pain management?

A

Tell patients to STAY AHEAD OF THE PAIN!!

This emphasizes proactive pain management.

28
Q

What are common symptoms of opioid withdrawal?

A
  • Dysphoria
  • Anxiety
  • Insomnia
  • Anorexia
  • Yawning
  • Chills
  • Goose bumps (piloerection)
  • Vomiting
  • Diarrhea
  • Rhinorrhea
  • Lacrimation
  • Increased blood pressure
  • Increased heart rate
  • Increased temperature
  • Muscle aches
  • Muscle twitches

Symptoms can be reduced by clonidine or another opioid like methadone.

29
Q

What are the signs of an opioid overdose?

A
  • CNS depression
  • Respiratory depression
  • Pinpoint pupils
  • May dilate if severely hypoxic

Treatment involves supporting respiration and using opioid antagonists like naloxone.

30
Q

What are some routes of administration for opioids?

A
  • Patient controlled analgesia
  • Transdermal patch
  • Intranasal spray
  • Buccal-lollipop
  • Sublingual

These methods can vary in their effectiveness and ease of use.

31
Q

What are the clinical uses of opioids?

A
  • Analgesia for acute pain
  • Trauma
  • Cancer and terminal pain
  • Chronic non-terminal pain
  • Sedation

Tolerance to sedation occurs with repeated use.

32
Q

What should be done to manage pain effectively with opioids?

A

Combine with non-opioids when possible

This maximizes effectiveness and reduces the required dose of opioids.

33
Q

What is the mechanism of action for morphine?

A

Stimulates all opioid receptors

It is a strong agonist useful in severe pain.

34
Q

What is the standard therapeutic dose of morphine?

A

10 mg SC or IM

This dose is used as a comparison for all other analgesic drugs.

35
Q

What is the primary metabolic pathway for morphine?

A

Metabolized in liver by CYP2D6

It is conjugated to glucuronide compounds.

36
Q

What are the potential adverse effects of morphine’s major metabolite?

A

Morphine-3-glucuronide may cause adverse effects if it accumulates

This can lead to increased side effects like itching or vomiting.

37
Q

What is the duration of analgesia after parenteral administration of morphine?

A

Approximately 4-6 hours

The peak analgesic action occurs within one hour of injection.

38
Q

What is hydromorphone used for?

A

Very effective for moderate to severe pain

It is more potent than morphine and has less likelihood of causing histamine release.

39
Q

What is methadone traditionally used for?

A

Maintenance treatment of addicts

It is also effective in long-term control of chronic pain.

40
Q

What is a significant risk associated with meperidine?

A

Can cause seizures due to the accumulation of normeperidine

It should not be used for more than 48 hours or in high doses.

41
Q

What is a characteristic of fentanyl?

A

Very lipid soluble and highly potent

It has a short duration of action and high abuse potential.

42
Q

What is the metabolism characteristic of hydrocodone?

A

Conversion by CYP2D6 is needed for some analgesic effect

It is often combined with acetaminophen.

43
Q

What is the significance of codeine’s metabolism?

A

Must be metabolized to morphine by CYP2D6 to be active

It doesn’t work effectively in patients on fluoxetine or paroxetine.

44
Q

What is the abuse potential of oxycodone?

A

Schedule II, often abused

It may be combined with naloxone or sequestered naltrexone to decrease abuse potential.

45
Q

What is the role of CYP2D6 in drug metabolism?

A

CYP2D6 metabolizes codeine, oxycodone, and hydrocodone to active compounds

Inhibition of CYP2D6 leads to less pain relief.

46
Q

What can happen if CYP2D6 is inhibited in extensive metabolizers?

A

Codeine may become toxic

A nursing baby died due to maternal ultrarapid metabolism of codeine.

47
Q

What are the characteristics of Pentazocine?

A
  • Kappa receptor agonist
  • Mu receptor partial agonist
  • Used for moderate pain
  • May be less sedating than other opioids
  • Schedule IV drug
48
Q

What is Buprenorphine used for?

A

Maintenance treatment of opioid addiction, decreases craving for drugs

It can be injected, sublingual, or intranasal.

49
Q

What is the effect of naloxone when combined with buprenorphine?

A

Naloxone blocks the effect of buprenorphine if injected

Naloxone is not absorbed sublingually.

50
Q

What are the potential effects of Nalbuphine?

A
  • Kappa agonist
  • Mu antagonist or partial agonist
  • Analgesia similar to pentazocine
51
Q

What is Tramadol primarily used for?

A

Mild to moderate pain

It is a weak mu agonist and inhibits NE/5-HT reuptake.

52
Q

What are common side effects of Tramadol?

A
  • Dizziness
  • Sedation
  • Constipation
  • Nausea
53
Q

True or False: Dextromethorphan is an analgesic.

A

False

It is primarily a cough suppressant.

54
Q

What is the primary function of opioid antagonists?

A

Bind to opioid receptors and prevent agonists from acting

Mixed agonists/antagonists may cause withdrawal in opioid-dependent individuals.

55
Q

What is Naloxone used for?

A

Drug of choice for opioid overdose

It can reverse respiratory depression and requires repeated dosing.

56
Q

What is the duration of action of Naltrexone?

A

24 hours

It is effective orally and used in treating opioid addiction.

57
Q

What impact did opioid overdoses have on US life expectancy?

A

Contributed to a decrease in life expectancy

This occurred alongside the COVID-19 pandemic.

58
Q

What are the prescribing guidelines for acute pain management?

A
  • Use non-opioid treatments when possible
  • Prescribe opioids only for severe pain
  • Re-evaluate if pain persists
59
Q

What should be done to manage opioid withdrawal symptoms?

A

Taper off drugs if possible; clonidine may help

Long-term options include methadone or buprenorphine/naloxone.

60
Q

What is the role of behavioral therapy in addiction treatment?

A

Part of integrated pain management and treatment programs

61
Q

What are the adverse effects of opioids?

A
  • Tolerance
  • Dependence
  • Respiratory depression
62
Q

What criminal complaints did Purdue Pharma plead guilty to?

A

Related to their role in the opioid epidemic

They were fined for their actions.

Pharmacology Winter Exam 2 (4 decks)

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