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Apex > Opioids And Non-opioid Analgesics > Flashcards

Opioids And Non-opioid Analgesics Flashcards

1
Q

What are the 4 steps in the pain pathway?

A

Transduction
Transmission
Modulation
Perception

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2
Q

Which step converts a chemical soup signal into an action potential?

A

Transduction

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3
Q

What drugs target transduction?

A

NSAIDS
Local anesthetics
Steroids
Antihistamines
Opioids

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4
Q

What step allows a pain signal to be relayed through the three-neuron afferent pathway along the spinothalamic tract?

A

Transmission

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5
Q

Where are first order pain neurons?

A

Periphery to dorsal horn

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6
Q

Where are second order neurons?

A

Dorsal horn to thalamus

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7
Q

Where are third order neurons?

A

Thalamus to the cerebral cortex

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8
Q

What drugs target transmission?

A

Local anesthetics

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9
Q

Which section of the pain pathway allows a signal to be modified (inhibited or augmented)?

A

Modulation

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10
Q

Where is the most important site of modulation?

A

Substantia gelatinosa in the dorsal horn (rexed Lamina 2 and 3)

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11
Q

What drugs target modulation?

A

Neuraxial opioids
NMDA antagonists
Alpha 2 agonists
AchE inhibitors
SSRIs
SNRIs

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12
Q

What aspect of the pain pathway describes the processing of the afferent pain signals ~ how we “feel” about pain?

A

Perception

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13
Q

What drugs target perception?

A

Opioids
General anesthetics
Alpha 2 agonists

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14
Q

What are the endogenous ligand for the opioids receptors?

A

Endorphins = Mu
Enkephalins = Delta
Dynorphins = Kappa
Nociceptin = NOP

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15
Q

How does opioid stimulation affect the presynaptic neuron

A

Decreased cAMP
Reduces calcium conductance —> reducing neurotransmitter release

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16
Q

How does opioid receptor stimulation affect the post synaptic neuron?

A

Increase potassium conductance —> hyperpolarizes the cell

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17
Q

What are some aspects about the Mu receptor?

A

Resp: depression
Cardio: bradycardia
CNS: sedation, euphoria, hypothermia
Pupil: miosis
GU: urinary retention
GI: N/V, decrease peristalsis, and ^ biliary
Pruritus: yes
Antishivering: 0

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18
Q

What are some aspects about the delta receptor?

A

Resp: depression
Cardio: 0
CNS: 0
Pupil: 0
GU: urinary retention
GI: 0
Pruritus: yes
Antishivering: 0

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19
Q

What are some aspects about the kappa receptor?

A

Resp: depression??
Cardio: 0
CNS: sedation, dysphoria, hallucinations
Pupil: miosis
GU: 0
Pruritus: 0
Antishivering: yes

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20
Q

What do opioids do to the CO2 response curve?

A

Right —> this reduces ventilatory response to CO2

Reduces RR increase TV

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21
Q

What aspect of the pupil do opioids stimulate?

A

Edinger Westphal nucleus —> pupil constriction

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22
Q

How do opioids affect biliary pressure? How do you relieve this?

A

Contraction of the sphincter of Oddi —> increases biliary pressure

Tx: glucagon and naloxone

23
Q

What are naturally occurring opioids?

A

Phenantherene derivatives:

Morphine
Codiene

24
Q

What are some semisynthetic opioids?

A

Morphine derivatives:

Hydromorphone, heroin, naloxone, naltrexone

Thebaine derivatives: oxycodone

25
Q

What are some synthetic opioids?

A

Piperidines: meperidine

Phenylpiperidines: fent, sufentanil, Remi, alfentanil

Diphenylpropylamines: methadone

26
Q

What is the relative potency for all the opioids? And their potency compared to 10 mg morphine

A

Sufentanil (1000) > Fentanyl (100) > Remifentanil (100) > alfentanil (10) > hydromorphone (7) > Morphine (standard) > meperidine (0.1)

27
Q

What occurs when a person taking a drug goes through withdrawals upon discontinuation?

A

Dependence

28
Q

What occurs when a patient requires higher doses of a drug to achieve a given effect?

A

Tolerance

29
Q

What occurs when tolerance to one drug produces tolerance to another drug that has similar effects?

A

Cross-tolerance

30
Q

What is considered a disease state where a person cannot stop using a drug despite negative consequences?

A

Addiction

31
Q

What are the two exceptions to tolerance?

A

Miosis
Constipation

32
Q

What would be the peak hours of withdrawal for a patient addicted to fent/meperidine?

A

6-12 hours

33
Q

What would be the peak hours of withdrawal for a patient addicted to morphine/heroin?

A

36-72 hrs

34
Q

What would be the peak hours of withdrawal for a patient addicted to methdone?

A

3-21 days

35
Q

Which opioids have an active metabolite?

A

Morphine (morphine-3-glucuronide) AND (morphine-6-glucuronide)
Meperidine (normeperidine)

36
Q

Why is normeperidine so bad?

A

Reduces seizure threshold
Increase CNS excitability

Avoid in renal patients and Elderly

37
Q

What is Remifentanil dosed at?

A

Lean body weight.

38
Q

What drugs must you avoid with Meperidine for risk of serotonin syndrome?

A

Demerol is a weak serotonin reuptake inhibitor

Avoid in MOAS (phenelzine, isocarboxazid, tranylcypromine)

39
Q

Why does Meperidine exhibit anticholinergic effects?

A

Structurally related to atropine (has atropine-like ring)

Tachycardia, mydriasis, dry mouth

40
Q

Which opioid has the fastest onset of action?

A

Alfentanil

This is due to its low pKa (more of the drug is in an unionized form)

41
Q

What type of procedures is alfentanil beneficial in?

A

Tracheal intubation
Retrobulbar block

42
Q

What is the maintenance infusion of Remifentanil?

A

0.1-1.0 mcg/kg/min

43
Q

What can Remifentanil cause following discontinuation?

A

Hyperalgesia

This can be attenuated by ketamine and magnesium

44
Q

What are the three MOAs of methadone?

A

Mu agonism
NMDA antagonism
MOA reuptake inhibition

45
Q

How does methdone affect the heart?

A

It can increase QT interval ~ this can lead to Torsades

46
Q

What is Oliceridine?

A

IV opioid analgesic that primary selects Mu receptor. Indicated for adults with acute pain or where alternative treatments fail

Loading dose: 1-2 mg
Supplemental doses: 1-3 mg q 1-3 hours

*** should not be used in patients with acute or severe asthma in an unmonitored setting

47
Q

What can rapid administration of opioids cause?

A

Skeletal muscle rigidity

More common with sufentanil, fentanyl, Remi, and alfentanil

48
Q

What is the treatment for opioid-induced skeletal rigidity

A

Paralysis and intubation

Also naloxone, but nobody wants that. Haha

49
Q

What are some complications of stiff chest?

A

Resp: (hypoxia, hypercapnia, ^ O2 consumption, decrease compliance, decreases FRC)

Card: ^ CVP, PAP, PVR

50
Q

What are some partial opioid agonists?

A

Buprenorphine (high affinity Mu agonist)

Nalbuphine (kappa agonist, Mu antagonist)

Butorphanol (kappa agonist, Mu antagonist ~ weak)

51
Q

What is the dose for Nalxone?

A

Dose: 1-4 mcg/kg ~ try 20 to 40 mcg at a time

Duration: 30-45 mins (** it may be necessary to repeat dose)

Metabolism: liver

52
Q

Which opiate reversal agent doesn’t cross the BBB thus making it beneficial for opioid induced bowel dysfunction?

A

Methylnaltrexone

53
Q

What is considered the “gold standard” for postoperative opioid delivery?

A

IV PCA

54
Q

What are the programmable components to IV PCA

A

Initial loading dose
Demand dose
Lockout interval
Basal infusion rate

Apex (47 decks)

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