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Pharmacology I > Exam 3 - L22-24 - Opioids > Flashcards

Exam 3 - L22-24 - Opioids Flashcards

1
Q

3 types of opioid recptors

A

Mew, Kappa, Delta (dont worry about delta)

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2
Q

describe the characteristics of Mu receptor

A

1) mu receptor mediates pain relief
mu agonist have the best efficacy but also have potential to be overused
2) effects include:
euphoria, respiratory depression, sedation, tolerance, and dependence
3) located in brainstem, spinal chord

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3
Q

What receptors do Strong Analgesics interact with

A

Mu Receptors

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4
Q

List the Partial Agonist and Mixed Agonist/Antagonist

A

Pentazocine (Mixed Agonist )
Buprenorphine (partial agonist)
Tramadol (Partial agonist)
Trapentoadal (partial agonist)
Butorphanol (partial agonist)

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5
Q

Opioid Antagonist drugs

A

Naloxone, Naltrexone, Methylnatrexone, Naloxegol

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6
Q

Opiate

A

Derrived from opium

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7
Q

Opioid/ How it relieves pain

A

Properties similar to drugs derrived from opium
(synthetic)

  • Opiods inhibit surges of Ca+ ultimately preventing release of neurotransmitters to block
    Pain signals
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8
Q

Narcotic

A

Sleep inducing

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9
Q

What drugs have peptides that act as agonists on mew receptors

A

Opioid drugs

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10
Q

Opioid function

A

Uncouple the physical pain sensation by blocking substance P from conscious awareness and emotional response to pain

  • Reduces conscious response
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11
Q

Substance P

A

NT which Crosses synaptic cleft and sends an action potential to the CNS inducing a pain feeling

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12
Q

A systemically administered opioid acts on what levels
(possible question)

A

Supraspinal levels

Mechanism: Acts as agonist at receptors for endorphins and enkephalins

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13
Q

Which receptors are linked with with some spinal and supraspinal analgesia, miosis, sedation, and dysphoria.

A

Kappa receptors

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14
Q
A
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15
Q

Which receptor is mainly envolved in the limbic system and is known to cause euphoria

A

Mu receptor

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16
Q

Activation of what receptor causes nausea in opioids

A

(CRTZ)hemoreceptor trigger zone in the medulla. (May also be some vestibular involvement)
** If a patient had heart surgery you would most likely not want to give them opioid due to the possible vomiting and nausea

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17
Q

What is the most common cause of death in opioid overdose

A

Depression of respiration (Mu receptor agonism)

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18
Q

At which dose of morphine can a patient not be aroused

A

When a patient has a overdose of morphine

*leads to mental clouding and sedation and death

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19
Q

in what cases does depression of respiration play a beneficial role

A

in cases of pulmonary edema small doses of morphine can be given to patient with pulmonary edema to reduce patient distress relaxing them improving cardiovascular function
(aka Compassionate Care Pack)

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20
Q

Dysphoria

A

Panic attacks and halucenations

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21
Q

Main sign of opioid overdose

A

Miosis (Pin-point pupils)

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22
Q

If a patient experiences a dysphoric response to morphine what drug could be used instead

A

ketoralac

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23
Q

Antitussive opiods effect/side effect:
1) Major drug + (mentioned another analogue)
2) H-1 affect / aggravation of asthma/ COPD (mentioned on this slide)
3) H-1 affect alleviation

A

1) Main drug at hand is Codeine ( he did also mention Hydrocodone analogue)
2) H-1 affect is when opiods literally move into MAST cells and displace the Histamine inside them. It occurs especially in IV admin causes itching.
3) Diphenhydramine (Benadryl) relieves itching

** Think bout tweakers or rappers like Yeat said the perc got him itching

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24
Q

Morphine therapuetic dose

A

10 milligrams with IV administration, subcutaneous, and intramuscular (injection)

(gold standard)

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25
Q

Chronic oral dose of morphine

A

10-30 mg

26
Q

When dealing with patients who have a history of reoccurring seizure such as Epileptic patients the doctor:

A

Should be carful when administering opioids as they lower seizure threshold
This does not mean that the patient cannot take them at all.

27
Q

What smooth muscle adverse effects are present in opioids

A

increased tone of circular smooth muscle and decrease in propulsive movement of longitudinal muscle

  1. Decreased intestinal motility (constipation peristalsis decreased)
  2. Urine retention
  3. Broncho constriction
  4. Increased biliary pressure due to constriction of Bile duct
28
Q

What cardiovascular adverse effects

A
  1. Postural (orthostatic hypotension – going from laying to standing
  2. Cutaneous vasodilation
  3. increased CSF pressure
29
Q

Skeletal Muscle Rigidity:
Problems which may occur during surgical anethesia with the use of opiods

A

A technique called Balanced Analgesia is used in surgeries where Anesthesia is used to KO person and the opioid is used to manage the pain during the operation:

  • opioids increase skeletal tone -> patient is given neuromuscular blocker ( acts on Nicotinic)
30
Q

In chronic use of opioids what adverse effect may arise

A

changes in endocrine function and immunosuppression
** affect females menstrual cycles

31
Q

As tolerance to opioids develop the severity to most adverse effects lessen. Which two adverse effects don’t get better as tolerance is developed

A

Miosis and constipation

32
Q

How much of morphine metabolized in first pass?

A

75% is metabolized in first pass.

33
Q

half life of opioids is and is primarily excreted in

A

half like is 2-3 hours it is primarily excreted in the urine

34
Q

Major drug interactions of opiods, antidepressents, and an example of a drug mixture tweakers use

A

-additive effects like drinking with a benzo, antipsychotics

-“speedball” addy + coke kinda lit (idk how this is related to content but he said to know in lecture)

-Duloxotene SNRI antidepressent effects which enhance analgesic effects of opiods by inhibiting synaptic reuptake of serotonin and dopamine

35
Q

Combining NSAID and Acetaminophen with opioids

A

enhance analgesic effect

36
Q

Treatment for overdose

A

Support respiration and NARCAN (naloxone)

37
Q

Codeine properties and uses

A

Given orally
1/12 the potency of morphine common doses are 30-60 orally

Metabolized to morphine (CYP2D6) Under metabolizers may not be effective
over metabolizers may be fatal

mild pain

38
Q

Hydromorphone

A

10x more potent then morphine
- Strong Mu agonism
-same use as morphine in pain relief
-

39
Q

Oxycodone

A

50% more potent then morphine used orally for mild moderate pain 0

Oxycotin in sustain release oral pill

40
Q

Hydrocodone

A

*similar to morphine and codeine used as an antitussive
*oral use for mild moderate pain
*widely used in combination with NSAIDS + Acetominophen

41
Q

Meperidine

A

Synthetic drug given orally

1/10 potency of morphine
Weaker smooth muscle effect then morphine
Used in obstetrics

Short acting 1-3 hours NOT GOOD CHRONIC PAIN
can cause SEIZURES In long term use

42
Q

Heroin

A

1)More potent and more euphoric than morphine
2) Heroin is an attractive substance for abuse due to it’s ability to pass through the BBB easily giving intense high (Acetal side chain)

last 4-6 hours

SCHEDUALE 1

injection and snorting or smoking is method used to take drug

43
Q

Methadone

A

Can be used as an Analgesic and to treat opioid addiction (not common)
*Methadone clinic stigma
Less euphoric than Morphine

when used in opioid addiction (Methadone maintenance treatment) lasts long time (12-24 hours)

For analgesic use last 4-6 hours
used for severe pain

44
Q

Fentanyl

A

Synthetic potent mu receptor agonist
100x more potent then morphine

Administered during surgical anesthesia

also given in a Transdermal preparation

Can be found in street drugs to make them more potent

45
Q

In opioid Combination Preparations what drugs are usually used? Why do these drugs exist? Why cant they be used in high doses for severe pain?

A
  1. These drugs either have acetaminophen, Aspirin or ibuprofen in combination with an opioid. Opioids used (Codeine, hydrocodone, oxycodone, or propoxyphene
  2. allow for the less than 10mg of morphine equivalent to be used while still providing sufficient analgesia. Used for moderate pain
  3. When used in high doses Acetaminophen and NSAID toxic metabolites can build up. (Renal/Liver damage)
    NOT recommended for severe pain
46
Q

Mixed agonist/antagonist drugs

A

Pentazocine, Buprenorphine, Butorphenol,Tramadol, Tapentadol

47
Q

Pentazocine

A

A mixed Agonist-Antagonist:
1) Partial agonist at LOW doses=weak effect on Mu receptors.

2) At the same time its Antagonist traits in HIGH doses.

3) Less effective than morphine, but less sedation and respiratory depression.

4) Acts agonistically on Kappa receptors causing dysphoric effects
+ Increased CNS stim and hallucinations.

5)Less risk for physical dependence than morphine. Can precipitate withdrawal syndrome in opioid addicts.

48
Q

Buprenorphine

A

Partial Agonist at mu and kappa.

Less analgesic effect than morphine, but less potential for abuse.

Reduces drug craving, so used to treat opioid addiction.

  • Has a plateau effect which decreases overdose likelihood
  • Office based treatment

*more accesible than methadone (forgot why, someone add…
it could be related to stigma of methadone clinics)

49
Q

what does a presense of naloxone in oral drugs provide?

A

naloxone will be metabolized if taken orally if addicts were to try to administer a drug intravenously naloxone would prevent overdose.
* Therefore detering addicts

50
Q

Tramadol

A

Newer drug for mild/moderate pain.

Weak mu agonist and inhibits reuptake of norepinephrine and serotonin.

Good analgesic with minimal side effects.

Lower abuse potential.

51
Q

Tapentadol

A

Similar to tramadol, but a stronger agonist of mu receptors.

Inhibits reuptake of NE and serotonin

More effective than tramadol, but greater abuse potential.

Beneficial for neuropathic pain

52
Q

Naloxone

A

Treats opioid poisoning

Given parenterally in ED or intranasally by EMTs

Short acting (1-2 hours) after levels will begin to increase again

Patient goes right into withdrawal

(ex: Heroin has a 6 hour 1/2 life)

53
Q

Naltrexone

A

Treatment of alcohol poisoning by reducing cravings

Risk of hepatotoxicity and poor patient compliance

Patient must be entirely detoxified before naltrexone can be initiated.

54
Q

Physical drug dependence

A

Patient tolerent to drug

upon stopping you see withdrawl

55
Q

Main characteristic of withdrawl

A

Dialated pupils, drug craving, GI hypermotility, sweating, yawning,

patient has turkey/chicken skin (Opposite effects of what opiods do)

56
Q

clonidine

A

Tones down CNS and treats withdrawal symptoms like sweating and hypertension

57
Q

Naloxegol

A

-Approved for opioid induced constipation
-Taken orally, so has few systemic effects
-Useful for out patients

58
Q

Duration and Intensity of Acute Withdrawal

A

Short acting drug: intense symptoms for 2-3 days
Long acting drug: moderate symptoms for 4-7 days.
Acute withdrawal is followed by prolonged symptoms including anxiety, sleep disturbances, and autonomic excitability.

59
Q

Spinal Morphine

A
  • just remember that inhibits the release of substance P (NT) to shutoff pain impulses and given often post operatively
60
Q

Methylnaltrexone

A

Analog of Naloxone approved to treat constipation
Must be given parenterally
Only used for severe symptoms caused by potent opioids

Pharmacology I (12 decks)

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