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PHRM 845 > Exam 5: Psych, Pain, SUD > Flashcards

Exam 5: Psych, Pain, SUD Flashcards

1
Q

Comorbidities of Bipolar Disorder

A
  • alcohol and substance use common (50-60%)
  • anxiety disorders are common and can significantly impact remission of mood episodes if left untreated or inadequately treated
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2
Q

What mood pole is experienced most often in bipolar disorder and can lead to misdiagnoses?

A

Depression

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3
Q

DSM-5 Classification of Bipolar I Disorder

A

≥ 1 manic episodes, depressive or hypomanic may have occurred

episodes generally last ≥ 1 week

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4
Q

DSM-5 Classification of Bipolar II Disorder

A

major depressive and hypomanic episodes

hypomanic episodes generally lasts ≥ 4 days

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5
Q

Target Symptoms of BPD: Mood

A
  • euphoria, elation, happiness
  • depression
  • lability
  • irritability
  • hostility
  • dissatisfaction
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6
Q

Target Symptoms of BPD: Cognitive/Perceptual

A
  • flight of ideas
  • racing thoughts
  • grandiosity
  • delusions
  • hallucinations
  • ideas of reference
  • fragmented thoughts
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7
Q

Target Symptoms of BPD: Activity/Behavior

A
  • pressured speech
  • impulsivity
  • insomnia
  • aggression, outbursts, violence
  • increased sexual dysfunction
  • panic
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8
Q

Pharmacotherapy Overview for BPD

A
  • mood stabilizers are the foundation of acute and maintenance treatment
  • 1st line: usually lithium or valproic acid
  • atypical antipsychotics can also be used 1st line as monotherapy or in combination with lithium or valproic acid
  • many patients will take polytherapy with mood stabilizers
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9
Q

What is lithium associated with a decrease in?

A
  • suicidality, especially in BPD
  • narrow therapeutic index, evaluate if patient has a plan, and if it does involve overdose via pill ingestion
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10
Q

Lithium Dosage Forms

A

some difference in lithium content, but use 1:1 conversion

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11
Q

Therapeutic Level of Lithium for Acute Treatment

A

0.9-1.2 mEq/L

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12
Q

Therapeutic Level of Lithium for Maintenance

A

0.6-0.9 mEq/L

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13
Q

Therapeutic Level of Lithium for Toxicity

A

1.5 - >3.0 mEq/L

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14
Q

When should you draw lithium levels?

A

draw trough serum concentration 72 hours after dose initiation, 12 hours after last dose

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15
Q

Toxicities of Lithium

A
  • GI
  • ataxia
  • coarse hand tremor
  • AMS
  • seizure
  • lethargy
  • confusion
  • agitation
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16
Q

Side Effects of Lithium

A
  • fine hand tremor
  • hypothyroidism
  • polyuria
  • polydipsia
  • acne (upper body, chest)
  • dry mouth
  • weight gain
  • ECG changes
  • diabetes insipidous
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17
Q

Teratogenic Effects of Lithium

A
  • cardiac structural abnormality that requires surgery
  • avoid in 1st trimester, use with caution in 2nd and 3rd trimester
  • BPD gets worse in pregnancy, might need to increase dose
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18
Q

Lithium Lab Monitoring

A
  • SCr, BUN (almost entirely renally excreted)
  • urine specific gravity
  • Na, K, Ca
  • ECG (especailly if age > 40 or cardiac risk factors)
  • Thyroid Function (TSH, T4)
  • Parathyroid hormone
  • CBC w/ differential
  • Weight
  • Pregnancy Test
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19
Q

How is lithium metabolized?

A

Mostly renally excreted

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20
Q

Decreased Li Renal Clearance Causes

A

due to ACEi, ARBs, thiazides, NSAIDs, dehydration

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21
Q

Increased Li Renal Clearance

A

lower Li levels
- caffeine
- osmotic diuretics
- loop diuretics

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22
Q

Increased Li Excretion Causes

A
  • lower Li levels
  • sodium bicarb
  • high sodium intake
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23
Q

Toxicity Related to Na Depletion with Lithium

A
  • thiazide diuretics
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24
Q

Valproate Dosage Forms: ER

A
  • ER dosage form is ~ 10-15% less bioavailable than delayed release dosage from
  • 1:1 converstion, expect lower serum concentration with the ER dosage form, usually not clinically significant
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25
Q

Valproic Acid Syrup and Capsule Sprinkle Form

A

higher risk for GI ulcerations (usually esophageal)

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26
Q

Serum Levels for Efficacy w/ Valproate

A
  • 80-125 mcg/mL associated with most efficacy in mania
  • obtain level at least 96 hours (4 days) after first dose or dose increase
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27
Q

Valproic Acid in Pregnancy

A
  • unsafe in any trimester of pregnancy
  • obtain baseline pregnancy test
  • use contraceptive
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28
Q

Valproic Acid and PCOS

A
  • PCOS occurs in up to 50% of women
  • may treat with metformin
  • refer to endocrinologist
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29
Q

Valproic Acid Side Effects

A
  • GI: anorexia, N/V/D, dyspepsia, ulceration
  • throbocytopenia, platelet dysfunction
  • teratogenic neural tube defects, enduring negative effects on IQ of offspring
  • increased appetite, weight gain (~6-8 kg)
  • hyperammonemia
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30
Q

Valproate Lab Monitoring

A

Baseline
- pregnancy test
- LFTs
- CBC w/differential

  • Serum Ammonia if suspected hyperammonemia
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31
Q

Drug Interactions with Valproic Acid

A
  • signficant concern with combo use with lamotrigine (increased lamotrigine serum concentration and increased risk of SJS
  • drug dosing cut in half
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32
Q

Carbamazepine in BPD

A
  • thrombocytopenia/hematologic effects
  • induce nearly all CYP450 enzymes
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33
Q

Oxcarbazepine in BPD

A
  • CYP450 3A4 inducer
  • associated with hyponatremia
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34
Q

Lamotrigine in BPD

A
  • not useful for acute treatment or for manic episodes
  • 1st line treatment for DEPRESSIVE symptoms
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35
Q

Topiramate in BPD

A
  • may cause weight loss
  • heat intolerance/hypohidrosis
  • metabolic acidosis and kidney stones
  • possible teratogen
  • DRESS
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36
Q

Antipsychotics in BPD

A
  • atypicals (except brexpiprazole, clozapine, iloperidone, and paliperidone) are FDA approved for acute and/or maintenance treatment (manic/mixed episodes) with and without psychosis
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37
Q

Seroquel in BPD

A
  • FDA approved for bipolar depression
  • dose at least 300 mg/day
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38
Q

Abilifiy/Brexpiprazole in BPD

A
  • FDA-approved for adjunctive treatment in depression in combination with antidepressants treatment
  • may see increased use for bipolar disorder
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39
Q

Symbyax for BPD

A
  • olanzapine/fluoxetine
  • FDA-approved for bipolar depression and treatment-resistant depression
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40
Q

Latuda in BPD

A
  • FDA approved for bipolar depression
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41
Q

Clinical Pearls: Antipsychotics in BPD

A
  • atypical antipsychs may be used as monotherapy or can be used combo with other mood stabilizers (VA or Li)
  • all monitoring parameters for metabolic syndrome and movement side effects apply when used for BPD
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42
Q

Treatment Considerations of BPD

A
  • mood stabilizers treatment is long-term and considered to be maintenance treatment to reduce time to subsequent mood episodes
  • suicide attempt risk is high in both poles of bipolar disorder, monitor closely, use lithium cautiously
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43
Q

Treatment in Pregnancy: BPD

A
  • lithium, VA, carbamazepine and topiramate are known or possible teratogens
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44
Q

Antidepressants in Bipolar Disorder

A
  • need to have maintenance mood stabilizer therapy in combo with antidepressant therapy
  • will use serotenergic antidepressants to treat anxiety
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45
Q

Functions of Pain

A
  • warning system (avoid injury)
  • aid in repair (hypersensitivity)
  • can be maladaptive (irreversible neuropathy)
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46
Q

Temporal Features of Pain

A
  • onset
  • duration
  • course
  • pattern
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47
Q

Intensity of Pain

A
  • average
  • least
  • worst
  • current pain
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48
Q

Location of Pain

A
  • focal
  • multifocal
  • generalized
  • referred
  • superficial
  • deep
  • opioid induced hyperalgesia (generalized)
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49
Q

Quality of Pain

A
  • inflammatory: throbbing, pulsating
  • neuropathic pain: stabbing, shooting, burning
  • visceral: squeezing
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50
Q

Pain Transmission

A
  • trauma in the periphery will transmit signal to spinal cord (activation of PNS)
  • activation of CNS at spinal cord
  • spinal cord sends input to the brain
  • processed in the brain
  • descending modulation to the spinal cord
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51
Q

Temperature Sensitive Receptors and Channels (in the skin)

A
  • transient receptor potential cation channel (TRP
  • TRPV (vanniloid) = heat
  • TRPM (melastatin) = cold
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52
Q

Acid Sensitive Ion Channel

A

ASIC activated by H+ and conducted by Na+

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53
Q

Chemical Irritant Sensitive Receptors and Channels involved in Pain Signaling

A

histamine
bradykinin

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54
Q

Reflex Upon Painful Stimuli

A
  • bypasses CNS, goes right back toward the muscle
  • transmission via afferent nerve to the spinal cord
  • modulation back to muscle via efferent nerve
  • does not go to brain!
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55
Q

Sodium Channels responsible for conduction of pain signal that are non-opioid

A

Nav1.1, Nav1.6, Nav1.7, Nav1.8

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56
Q

Neurotransmitter released at the end of afferent neuron

A

glutamate (conduction of pain in spinal cord)

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57
Q

A-beta fibers

A
  • non-noxious (touch, pressure)
  • innervate the skin (thicker myelin)
  • faster (35-75 m/s)
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58
Q

A-gamma fibers

A
  • pain, cold
  • myelinated
  • fast (2-35 m/s)
  • first pain, reflex arc
  • sharp prickly pain
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59
Q

C fibers

A
  • pain, temp, touch, pressure, itch (polymodal)
  • unmyelinated
  • slow (0.5-2 m/s)
  • second pain
  • dull aching
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60
Q

Substance P’s Role in Pain

A
  • repeated stimuli reduces firing threshold
  • increase expression of pain receptors via sensitization
  • sunburn is a good example
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61
Q

Substance P MOA

A
  • injury occurs at periphery
  • substance P is released
  • stimulates areas of the blood to degranulate mast cells
  • vasodilation and release of bradykinin, prostaglandins, histamines (inflammatory markers)
  • increase in receptors in the periphery to send more signals into the spinal cord
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62
Q

Neuropathic Pain Sensitization

A
  • spontaneous afferent activity: possibly enhanced expression of sodium channel subtypes contributing to enhanced cellular excitability and generation of ectopic action potentials
  • spinal sensitization leading to increased AMPA and NMDA expression and sensitivity
  • A-beta afferent fibers that cause light touches to hurt due to cord sensitization
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63
Q

Neurotransmitters released in neuropathic pain signalling

A
  • neuropeptides
  • CGRP
  • Substance P
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64
Q

_____ expression of opioid receptors in the brain stem along the _______ pathway

A

high, descending

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65
Q

Mu Opioid Expression Effects on Brain

A
  • alter mood
  • produce sedation
  • reduce emotional reaction
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66
Q

Mu Opioid Receptor Expression on Brainstem

A
  • increase activity of descending fibers
  • decrease activity of input in ascending pathway via afferent neuron
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67
Q

Mu Opioid Receptor Expression on Spinal Cord

A
  • inhibit vesicle release
  • hyper-polarize post-synaptic membrane
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68
Q

Mu Opioid Receptor Expression on Periphery

A
  • reduce activation of primary afferent
  • modulate immune activity
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69
Q

What do Mu opioid receptors do?

A

influence ascending pathway and perceivement of pain

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70
Q

Amygdala and Pain

A

anticipates pain and reacts to perceived threats

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71
Q

Somatosensory Cortex and Pain

A
  • registers which body part is in pain and the intensity of that pain
  • less activity here when patients focus their attention away from their pain
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72
Q

Prefrontal Cortex and Pain

A
  • processes pain signals rationally and plans action
  • active when trying to consciously reduce pain
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73
Q

Right Lateral Orbitofrontal Cortex

A
  • evaluates sensory stimuli and decides on response, particularly if fear is involved
  • mindfulness meditation calms down this response
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74
Q

Opium contains which two types of Alkaloids

A
  • phenanthrenes
  • benzylisoquinolines
  • opiates are only those opioids that are naturally occuring
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75
Q

Codeine SAR

A

3 position substitutions ether or ester produces decreased potency

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76
Q

Hydromorphone or Hydrocodone SAR

A

6 position increases activity

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77
Q

Oxycodone SAR

A

14 position OH has increased potency

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78
Q

Naloxone or Naltrexone SAR

A

N-allyl gives antagonists

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79
Q

Opioid SAR Overview

A
  • 3 ring structure
  • 3, 6, N position
  • bulky group on N decreases potency
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80
Q

Where are peptides active?

A

endogenously

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81
Q

What are cleaved into more opioid subtype selective peptides?

A

large precursor proteins

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82
Q

Pro-opiomelanocortin (POMC)

A

cleaves beta-endorphin to Mu opioid

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83
Q

Preproenkephalin

A
  • Leu-enkephalin –> delta opioid
  • met-enkaphalin = mu and delta opioid
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84
Q

Preprodynorphin

A
  • dynorphin –> kappa opioid
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85
Q

G protein coupled opioid receptor

A
  • Family A peptide receptors
  • Gi/o- coupled inhibition of cAMP production
  • open GIRK potassium channels
  • close calcium channels
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86
Q

Mu Opioid Receptors

A
  • morphine
  • endogenous opioid = endorphin
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87
Q

Kappa Opoid Receptors

A
  • endogenous opioid = dynorphin
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88
Q

Delta Opioid Receptors

A

endogenous opioid = enkephalin

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89
Q

Nociceptin/Orphanin FQ Receptor

A

endogenous opioid = nociceptin

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90
Q

Sigma Receptors

A

not an opioid receptor

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91
Q

Opioid Receptor Signal Transduction

A
  • presynaptic = inhibit calcium channel (Gi) decrease in neurotransmitter release
  • postsynaptic = activate GIRK channel, efflux of K+ –> hyperpolarization
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92
Q

Endogenous peptides associated with Mu receptor

A
  • beta-endorphins via POMC (endogenous morphine)
  • component of runners high
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93
Q

Therapeutic Use of Mu

A
  • analgesia (cancer pain, palliative, PCA)
  • sedation
  • antitussive (suppression of cough center in the medulla oblongata)
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94
Q

Opioid Induced Side Effects are mostly what?

A

on-target effects

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95
Q

Opioid Induced Side Effects

A
  • respiratory depression in brain stem and pre-botzinger complex in the ventrolateral medulla
  • constipation (GI tract)
  • pruritus (itch) which is a side effect, not allergic response
  • addiction
  • urinary retention (opioid-induced ADH release)
  • Nausea/Vomiting via chemoreceptor trigger zone in medulla
  • miosis in oculomotor nerve (PAG)
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96
Q

Kappa opioid receptor endogenous peptide

A
  • dynorphins natural ligand
  • preprodynorphin
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97
Q

Kappa opioid receptor activation

A
  • dysphoric
  • aversive
  • potential use for treatment of addiction by reducing dopamine release
  • counterbalance mu opioid receptor effects
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98
Q

Delta opioid receptor endogenous ligand

A
  • enkephalins
  • proproenkephalin
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99
Q

Delta opioid receptor expression

A
  • more dynamic expression
  • intracellular
  • externalized upon chronic stimuli
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100
Q

Role of Delta Opioid Receptor

A
  • hypoxia/ischemia/stroke
  • hibernation release of enkephalin like opioid
  • reduce anxiety
  • reduce depression
  • treat alcoholism
  • relief hyperalgesia, chronic pain
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101
Q

Side effect of delta opioid receptor

A

seizures

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102
Q

FDA approved delta opioids

A

None available

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103
Q

Opioid Site of Action

A

Ventral Tegmental Area and Nucleus Accumbens

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104
Q

Depressants can cause what neurotransmitter release

A
  • dopamine release
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105
Q

Opioid MOA

A
  • binds to mu receptor
  • Gi signaling inhibits neurotransmitter release
  • less GABA to activate GABAa
  • less inhibition of dopamine neuron activity
  • increase dopamine release
  • increased activation of dopamine receptors in nucelus accubens
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106
Q

oral administration of opioids pk

A
  • slow rise, long duration
  • does not reach side effect region
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107
Q

Where is morphine absorbed?

A
  • readily absorbed in GI
  • first pass metabolism
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108
Q

Metabolism of Morphine/Phenanthrenes

A
  • CYPD 2D6 and 3A4
  • elimination T1/2 increased with liver disease
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109
Q

Morphine and Phenanthrenes undergo what type of metabolism?

A
  • glucuronidation at 3’ and 6’ position
  • morphine 6 glucuronide is still potent
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110
Q

Excretion of Morphine/PHenanthrenes

A
  • glomerular filtration (renal)
  • 90% excreted in 24h
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111
Q

Opioids that are prodrugs

A
  • heroin
  • codeine
  • tramadol
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112
Q

CYP3A4 impact on opioid metabolism

A
  • responsible for converting opioids to “nor” metabolites
  • makes them less active
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113
Q

CYP 2D6 impact on opioid metabolism

A
  • converts prodrug to active metabolite (morphine, hydromorphone, oxymorphone)
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114
Q

Which phenotype of 2D6 metabolizers is of high relevance

A

UM
- up to 50% higher plasma concentrations of morphine than EM when given codeine
- frequency 40% in North Africa

PM
- more common in caucasians
- no therapeutic effect from codeine
- same incidence of adverse effects

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115
Q

Use of Fentanyl

A
  • 100x potent over morphine
  • 50x potent over heroin
  • used for palliative care breakthrough pain
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116
Q

Sufentanil, Remifentanil, Alfentainil

A
  • agnoists
  • anesthesia/sedation
  • breakdown by plasma esterases due to ester linkage
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117
Q

Fentanyl Dosage Froms

A
  • iv
  • patch
  • lollipop
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118
Q

Hydromorphone and Oxymorphone active metabolites

A
  • no opioid active metabolites
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119
Q

Morphine use

A
  • covered by medicare –> preferred over oxycontin
  • extended release (MScontin)
  • long acting, lower rush, M6G contribution to pain relief. risk for abuse if IV injected at once
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120
Q

Non-phenanthrene opioids

A
  • tramadol
  • meperidine
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121
Q

Tramadol use

A
  • mild opiate anelgesic
  • has SNRI properties (5HT/NE reuptake inhibitor, stimulates 5HT release)
  • management of mild neuropathic pain
  • painkiller used when you dont want to prescribe a stronger opioid
  • schedule IV
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122
Q

Meperidine Use

A
  • used to treat rigors (shivering)
  • has toxic metabolite normeperidine (3A4)
  • metabolite is devoid of analgesic activity
  • neurotoxic causing nervousness, tremors, muscle twitches, and seizures
  • renally excreted, do not use in patients with decreased renal function
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123
Q

Methadone MOA

A

block NMDA receptors

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124
Q

Methadone use

A
  • primarily used for opioid dependence
  • prolonged QTc
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125
Q

Opioids for Cough

A
  • usually codeine
  • DM has limited opioid activity (not scheduled)
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126
Q

Opioids for Diarrhea

A
  • dephenoxylate with atropine
  • Loperamide is strong pgp substrate (low BBB penetration)
  • eluxadoline for IBS with diarrhea, mu/kappa agonist and delta antagonist
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127
Q

Pentazocine and Butorphanol

A
  • k agonist
  • partial agonist/antagonism at mu
  • parenterally administered
  • side effects include less dysphoria, hallucinations, increase in BP, HR
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128
Q

Nalbuphine

A
  • full agonist at K
  • antagonist at mu
  • antagonism produces withdrawal
  • parenterally administered
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129
Q

Buprenorphine

A
  • partial mu agonist
  • weak k agonist and gamma antagonist
  • primary use in opioid replacement therapy
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130
Q

Prevention of constipation due to opioid use

A

Senna
- irritates colon
- cause fluid secretion/colonic contraction

Miralax
- stool softner via osmotic increase in GI water content

Docusate
- stool softener

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131
Q

opioid tolerance

A
  • analgesic effects
  • nausea
  • urinary retention
  • respiratory depression (biggest risk of death in withdrawn patients/users)
  • euphoria
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132
Q

limited/no tolerance of opioid

A
  • constipation
  • itch
  • miosis
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133
Q

Treatment for Opioid Dependence: Methadone

A
  • full mu opioid receptor agonist (cross tolerance)
  • provide relief from withdrawal
  • slow acting (2-4 hours)
  • accumulates with repeated dose
    • NDMA antagonist racemic mixture
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134
Q

Treatment for Opioid Dependance: Buprenorphine

A
  • mu opioid receptor partial agonist
    -blocks full agonist effect of heroin, oxycodone (antagonist)
  • provides some activation (agonist) with less withdrawal
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135
Q

Subutex clinical pearl

A

abuse potential

136
Q

suboxone clinical pearl

A
  • partial blocks agonist effects when taken i.v.
  • 4:1 bup:nx
137
Q

Treatment for Opioid Dependance: Naltrexone

A
  • intramuscular injection
  • extended release
  • once monthly
  • decent oral bioavailability
  • medium half life (4 hours)
  • will cause withdrawal
  • works better if patient has been drug free for 1 month or more
138
Q

Naloxone and Naltrexone

A
  • not interchangable
  • naloxone: limited oral bioavailability/short half life
  • naltrexone: PO
139
Q

Treatment for Opioid Dependance: Narcan

A
  • limited oral bioavailability
  • rapid onset
  • short half-life
  • repeat every 2-5 minutes if not conscious
  • one does is not enough
  • presence of fentanyl and other opioids means even more doses
  • causes strong withdrawal
140
Q

Neonatal Abstinence Syndrome

A
  • drug dependent
  • causes serious withdrawal in the baby
  • seizures may occur
  • opioids can also be present in breast milk
  • symptoms may begin 24-48 hours after birth or as late as 5 to 10 days
141
Q

Nonpharmacological Treatment for Neonatal Abstinence Syndrome

A
  • swaddling
  • hypercaloric formula
  • frequent feedings
  • observations
  • rehydration
142
Q

pharmacological treatment of neonatal abstinence syndrome

A
  • morphine diluted to 0.4 mg/mL
  • sublingual buprenorphine
  • methadone 0.05 to 1 mg/kg/dose every 6 hours
  • morphine and buprenorphine linked with shorter hospital stay than methadone
  • clonidine could be useful
143
Q

Therapeutic Applications of NSAIDs

A

Analgesic
- chronic postsurgical pain
- potentailly inhibit bone healing
- myalgias
- inflammatory pain
- dysmenorrhea

Anti-inflammatory
- gout and hyeruricemia
- RA
- OA
- tendonitis and bursitis

Antipyretic
- feber

Prophylactic to reduce risk of MI
- aspirin

144
Q

Three Phases of Inflammation

A

acute
- vasodilation leads to increased permeability

Subacute
- infiltration

chronic
- proliferation

145
Q

Recruitment of Eicosanoids

A
  • arachiodonic acid metabolites produce prostaglandins
  • prostaglandins = heat, pain, reddness
  • thromboxanes
  • leukotrienes (swellign)
  • cytokines (pain)
146
Q

Aspirin

A
  • irreversibly inhibits COX 1/2 by acetylation of COX
  • frequently used as prophylactic for anti-coag
  • no tolerance development to analgesic efffects
  • reyes syndrome
147
Q

Other NSAIDs

A
  • competitive (reversible) inhibitors of COX 1/2
148
Q

PK Properties of Aspirin/Salicylates

A
  • rapidly absorbed
  • delayed by presence of food
  • distribution throughout most tissues and fluids and competes for protein binding sites
  • salicylate half-life is 6-20 hours
  • increased excretion with increased urinary pH (iv bicarb; pH trapping of aspirin in the urine)
149
Q

Clinical Features of Salicylism/Aspirin Poisoning

A
  • vertigo, tinnitus
  • respiratory alkalosis caused by hyperventilation (moderate, adults)
  • metabolic acidosis leading to lowering of blood pH (high dose or kids)
150
Q

Treatment of Salicylism/Aspirin Poisoning

A
  • reduce salicylate load by increasing urinary excretion (dextrose, sodium bicarb)
  • trap in urine pKa of salicylate at 3.0
  • correct metabolic imbalance
151
Q

Arylpropionic Acids

A
  • ibuprofen, naproxen
  • Half life: Ibuprofen = 2 hr, naproxen = 14 hr
  • better tolerated than aspirin
152
Q

Diclofenac Therapeutic Use

A
  • available as gel
  • excellent alternative to ibuprofen and naproxen
  • increased risk of peptic ulcer and renal dysfunction
  • combined with misoprostol for chronic use
153
Q

Indomethacin Therapeutic Use

A
  • most potent reversible inhibitors of PG biosynthesis
  • high incidence and severity of side effects long term
  • acute gouty arthritis
154
Q

Sulindac

A
  • less toxic derivative of indomethacin
  • still significant side effects
  • RA
155
Q

Enolic Acid NSAIDs

A
  • use to treat arthritis
  • great joint penetration
  • least GI side effects
  • at low doses, meloxicam is cox-2 selective
  • long half life (20 hours meloxicam, 57 hours piroxicam)
156
Q

Adverse Effects of NSAIDs

A
  • inhibition of renal PGE2 synthesis can lead to increased sodium reabsorption, causing peripheral edema
  • increased risk of bleeding due to transient inhibition of platelet aggregation
  • inhibition of uterine motility (delaying preterm labor)
  • GI distress/ulceration
157
Q

Therapeutic Use of Acetaminophen

A
  • highly effective as analgesic and antipyretic
  • limited anti-inflammatory activity
  • no GI toxicity
  • acute overdose may lead to fatal hepatic necrosis
158
Q

Adverse Effects of Acetaminophen

A
  • more renal toxicity than aspirin and NSAIDS due to vasoconstriction by inhibition of PGE2
  • dose dependent hepatic necrosis (limit 4 g/day)
  • increase in toxic acetaminophen metabolites (NAPQI)
  • treat with n-acetylcystemine to detoxify NAPQI
159
Q

MOA of acetaminophen overdose

A
  • APAP metabolized via glucuronidation and sulfation
  • if those two pathways are overwhelmed, apap will. be metabolized by a third pathway via n-hydroxylation and rearrangement (cyp mediated)
  • this creates NAPQI which has toxic reactions with proteins and nucleic acids
160
Q

Side Effect Profile of Nonselective COX inhibitors

A
  • reduce ulcers and GI bleeds
  • withdrawn due to high chance of blood clots, stroke, and heart-attacks
  • inhibition of cox-2 decreases PGI2, which increases platelet aggregation
161
Q

NSAID contraindications

A
  • chronic kidney disease
  • peptic ulcer disease
  • history of GI bleed
  • CV risk (lowest risk is naproxen, highest is diclofenac)
  • interfere with bone healing
  • asthma exacerbations (cox 2 specific less likely)
162
Q

Sodium Channel Blockers for local Pain

A
  • lidocaine
  • bupivacaine
  • benzocaine
163
Q

Lidocaine pearls

A
  • local analgesia (dentistry)
  • itch, burn
  • 15 min onset, lasts 30-120 minutes
164
Q

Bupivocaine pearls

A
  • longer lasting (3.5 hour)
  • epidural
165
Q

Benzocaine pearls

A
  • otc use
  • oral ulcers
  • ear pain
  • esters have higher allergy risk
166
Q

NaV1.7 Target

A
  • severe neuropathic pain (GOF mutation)
  • congenital insensitive to pain (LOF mutation)
  • expressed in peripheral neurons (high in nociceptive neurons, low in cardiac muscles or CNS)
167
Q

Psychiatric Drugs as Sodium Channel Blockers for Pain

A
  • lamotrigine off label for peripheral neuropathy, migraine
  • carbamazepine for tregminal neuralgia
  • tricyclic antidepressants like amitriptyline
168
Q

SNRI impact on pain

A
  • increase NE levels
  • can act on alpha 2 adrenergic receptors in the spinal cord (reflex arc)
  • provide analgesia
169
Q

Duloxetine use in pain

A
  • diabetic pain
  • fibromyalgia
  • peripheral neuropathy
170
Q

Venlafaxine use in pain

A
  • off label diabetic neuropathic pain
  • non-selective opioid effects
  • naloxone reversible analgesia
  • cardiac toxicity (NaV channels)
171
Q

SNRIs lacking Sodium Channel Functionality

A

milancipran, tapentadol

172
Q

CCBs as possible analgesics

A
  • heart rate, blood pressure decrease
  • diabetic neuralgia
  • fibromyalgia, neuropathic pain
173
Q

Gabapentin and Pregabalin use as CCBs

A
  • alpha 2 gamma - CaV1, 2 selective blocking
  • not metabolized
  • no drug-drug interactions
  • affect the Agamma/C fiber afferent neuron
  • decrease glutamate, decreasing pain firing
174
Q

Schedule 1

A
  • no medical use
  • high abuse potential
  • safety not guaranteed
175
Q

Schedule 1 drugs

A
  • heroin
  • marijuana
  • THC
  • LSD
  • GHB
  • psilocybin
  • MDMA
176
Q

Schedule II

A
  • medical use
  • high abuse potential
  • large risk of dependence
177
Q

Schedule II drugs

A
  • cocaine
  • Ritalin
  • PCP
  • morphine
  • fentanyl
  • oxycodone
  • hydromorphone
178
Q

Schedule III

A
  • medical use
  • moderate abuse and dependence
179
Q

Schedule III drugs

A
  • ketamine
  • buprenorphine
  • marinol
180
Q

Schedule IV

A
  • medical use,
  • low abuse and dependence
181
Q

Schedule IV drugs

182
Q

Opioids receptor target

183
Q

LSD, mushrooms receptor target

A

serotonin receptor (2A, 2C)

184
Q

marijuana, K2, spice receptor target

A

cannabinoid receptors (CB1)

185
Q

GHB receptor target

186
Q

Caffeine receptor target

A

adenosine receptors

187
Q

Substances that act indirectly on G protein coupled receptors

A
  • cocaine
  • amphetamine
  • mdma/ecstasy
  • alcohol
188
Q

Cocaine/Amphetamine MOA

A
  • dopamine transporter
  • noradrenaline, serotonin transporters
  • release dopamine, serotonin, noradrenaline –> GPCRs
189
Q

MDMA/Ecstasy MOA

A

monoamine transporters (dopamine, serotonin)

190
Q

Alcohol MOA

A
  • GABA channels
  • 5HT3 channels
  • NMDAR, nAchR, Kir3
  • causes releaase of endogenous opioids
191
Q

Substances of abuse that act on ion channels

A
  • nicotine
  • PCP, ketamine
  • benzos, barbiturates
192
Q

Nicotine MOA

A
  • ionotropic acetylcholine receptors (Na)
  • agonist
193
Q

PCP/Ketamine MOA

A
  • ionotropic NMDA receptor (Ca, Na - K)
  • antagonist
194
Q

Benzos/BBTs MOA

A
  • ionotropic GABAa recpetors (Cl-)
  • positive allosteric modulators
195
Q

Frontal Cortex

A

decision making impulsivity

196
Q

Striatum/SA

A

reward/value

197
Q

Nucleus Accumbens

A

pleasure valuation

198
Q

VTA

A

source of dopamine

199
Q

Hippocampus

A

Memory/Learning

200
Q

Dopamine hypothesis of addiction

A
  • pleasurable events release dopamine
  • PD only develop addiction during treatment
  • DA important for assigning value to reward prediction error
  • value provides the drug with an incentive salience
201
Q

Limits of Dopamine Hypothesis

A
  • dopamine not required for reward learning
  • dissociation between liking and wanting
  • tolerance to pleasurable effect, enhanced effect
  • dopamine does not encode liking, but involved in making reward predictions and learning from the outcome/error
202
Q

Glutamate Hypothesis of Addiction

A
  • glutamate can increase dopamine activity in NAcc
  • glutamate projects to the VTA
  • destruction of this pathway reduces cocaine/morphine reward
  • mGluR5 KO mice show reduced cocaine reward
  • NMDA antagonist blocks acquisition of reinforcement learning
  • intraNAcc AMPA injection causes relapse
  • dopamine controls glutamate activity in amygdala
203
Q

How does drug use impact neuronal plasticity

A
  • long term potentiation
  • persistent increase in synaptic strength following intense stimulation
  • rewarding substances cause relative increase in glutamatergic AMPA receptors
204
Q

Drug abuse defination

A

the use of a drug for a nontherapeutic effect

205
Q

drug misuse defination

A

inappropriate, illegal, or excessive use of prescription or nonprescription drug

206
Q

Substance use disorder criteria

A
  • mild (2-3), moderate (4-5), severe (>6)
  • cravings
  • distracted
  • causing problems in relationships
  • giving up on activities
  • tolerance
  • withdrawal
207
Q

physical dependence

A
  • body needs more drug (tolerance)
  • cellular adaptations upon repeated activation of receptors
  • body withdraws without the drug
208
Q

Dangerous Withdrawal Symptoms

A
  • alcohol and tranquilizers
  • grand mal seizures (also tramadol)
  • hallucinations
  • delirium tremens
209
Q

psychological dependence

A
  • addiction
  • mental urge to take drug to function
  • compulsive need/craving
  • even in absence of withdrawal
210
Q

drug is rewarding or produces positive reinforcement when:

A

the user feels pleasure/satisfaction

211
Q

negative reinforcement

A
  • reward by escaping negative/painful stimulus or event
  • not same as punishment
212
Q

respiratory depression

A

opioids, alcohol

213
Q

cardiac arrhythmias, brain hemorage, stroke

A

stimulants

214
Q

fatal seizures

A

withdrawal, choke on own vomit

215
Q

PQRSTU

A
  • palliative or precipitating factors
  • quality of pain
  • region of pain
  • severity
  • time related nature of pain
  • impact of pain on you
216
Q

objective assessment of pain

A
  • dilated pupils
  • paleness
  • sweating
  • tachycardia
  • tachypnea
217
Q

Acute pain

A
  • < 3 months
  • nociceptive (tissue)
218
Q

chronic pain

A
  • > 3 months
  • neuropathic (nerve)
219
Q

goals of therapy for non-malignant pain

A
  • correct underlying cause of pain if possible
  • minimize pain and symptoms for pain/injury
  • improve QOL and activities of daily living
  • limit pharmacotherapy side effects
220
Q

non-pharm therapy for pain

A
  • can be used in combination with analgesics
  • correct the underlying cause
  • exercise
  • acupuncture
  • massage
  • heat or ice
  • physical manipulation
221
Q

WHO analgesic ladder: step 1

A
  • non-opioid +/- adjuvant analgesic
222
Q

WHO analgesic ladder: step 2

A
  • opioid for mild-moderate pain
    • non-opioid
  • +/- adjuvant analgesic
223
Q

WHO analgesic ladder: step 3

A
  • opioid for mod-severe pain
    • non-opioid
  • +/- adjuvant analgesic
224
Q

Non-opioid analgesics

A
  • acetaminophen
  • NSAIDS
225
Q

adjuvant therapies

A
  • gabapentinoids
  • SNRIs
  • TCAs
  • muscle relaxants
  • antiepileptics
  • topical agents
226
Q

Acetaminophen Uses

A

analgesics and antipyretic

227
Q

Acetaminophen formulations

A
  • tablet
  • capsule
  • chewable tablet
  • liquid/gel
  • IV solution
  • suppository
228
Q

Acetaminophen: Non-PO options?

A

YES
- suppository
- IV

229
Q

Acetaminophen Dosing Adult

A
  • 325 - 1000 mg PO Q4-6H PRN
  • in liver disease, decrease max ≤ 2 g/day
230
Q

Acetaminophen Dosing Children

A
  • 10-15 mg/kg PO Q4H PRN
  • max dose: 75 mg/kg/day or ≤ 3-4 g/day
231
Q

Side Effects: APAP

A
  • hepatotoxicity (acute liver liver failure most likely with ≥ 10 g dose)
232
Q

APAP clinical pearls

A
  • gold standard for OA due to fewer side effects in geriatric patients than NSAIDs
  • education patients about max daily doses, including combo products
  • injection is expensive
233
Q

NSAIDs uses

A

analgesic, antipyretic, anti-inflammatory

234
Q

NSAIDs side effects

A
  • GI bleeding
  • nephrotoxicity
  • fluid retention
  • increase CV events
235
Q

NSAIDs clinical pearls

A
  • take with food
  • caution use in geriatric patients due to increased side effects (beers list)
  • avoid systemic NSAIDs in patients with cardiac history (can use topical NSAIDs)
  • avoid in severe liver disease or CKD
236
Q

Aspirin Formulations

A
  • chewable tablet
  • tablet
  • EC tablet
  • capsule
  • ER capsule
  • suppository
237
Q

Aspirin: Non-PO options

A

YES
- suppository

238
Q

aspirin recommended dosing

A
  • 325-1000 mg PO q4-6h prn (max 4 g/day)
239
Q

aspirin clinical pearls

A
  • avoid use for pain in patients taking blood thinners or anti-platelets
  • some formulations available OTC
240
Q

Reye’s Syndrome association

A

associated with teens/children using aspirin when they have viral infections such as flu or chickenpox (with or without fever)

241
Q

Ibuprofen available formulations

A
  • capsule
  • tablet
  • chewable tablet
  • suspension
  • IV solution
242
Q

Ibuprofen: Non-PO options?

A

YES
- IV solution

243
Q

ibuprofen recommended dosing adult

A

200-800 mg PO q6-8h PRN (max 3200 mg/day)

244
Q

ibuprofen recommended dosing pediatrics

A
  • > 6months
  • 5-10 mg/kg PO q4-6h prn
  • max 40 mg/kg/day or 2400 mg, whichever is less
245
Q

Diclofenac available formulations

A
  • capsules
  • tablet
  • IV solution
  • suppository
246
Q

Diclofenac: Non-PO options?

A

YES
- topical gel
- suppository
- topical solution
- ophthalmic solution
- patch

247
Q

Diclofenac recommended dosing

A
  • 50 mg PO q8h or 2-4 g applied topically 4 times/day
248
Q

diclofenac clinical pearls

A
  • minimal systemic side effects with topical gel
249
Q

Naproxen available formulations

A
  • capsule
  • tablet
  • DR/ER tablet
  • suspension
250
Q

naproxen: Non-PO options?

251
Q

naproxen recommended dosing adults

A

220 mg - 500 mg po q6-12h (max 1000 mg/day)

252
Q

Ketorolac available formulations

A
  • tablet
  • IV/IM solution
  • nasal spray
  • ophthalmic solution
253
Q

ketorolac: Non-PO options?

A

YES
- IV/IM solution
- nasal spray
- ophthalmic solution

254
Q

Ketorolac recommended dosing adult

A

15-30 mg IV q6h prn or 10 mg po q6h prn

255
Q

ketorolac recommended dosing pediatric

A

0.5 mg/kg/dose IM/IV q6h prn

256
Q

ketorolac clinical pearls

A
  • max duration is 5 days
  • increased risk of gi bleed when used longer
    oral dosing is inteded as a continuation of IM or IV therapy
257
Q

celebrex available formulation

A
  • capsule
  • oral solution
258
Q

celebrex: Non-PO options?

259
Q

celebrex recommended dosing

A
  • 200 mg po bid
260
Q

gabapentinoids uses

A
  • fibromyalgia
  • neuropathies
  • post op pain
261
Q

gabapentinoids available formulations

A
  • tablets/capsule
  • ER tablet
  • liquid solution
262
Q

gabapentinoids: Non-PO options?

263
Q

recommended dosing: gabapentin

A

100-300 mg po TID (max 3600 mg/day)

264
Q

recommended dosing: pregabalin

A

75 mg po bid (max 600 mg/day)

265
Q

side effects of gabapentinoids

A
  • sedation
  • dizziness
  • peripheral edema
266
Q

gabapentinoids clinical pearls

A
  • really dose adjusted
  • titrate up dose to limit sedation
  • use in combo to decrease requirements of other analgesics
  • pregabalin is schedule V
267
Q

SNRI uses

A
  • fibromyalgia
  • neuropathy
268
Q

SNRI available formulatiosn

A
  • capsule/tablet and in ER formulation
269
Q

SNRI: Non-PO options?

270
Q

recommended dosing venlafaxine

A
  • 37.5-75 mg po daily (max 225 mg/day)
271
Q

recommended dosing duloxetine

A

30 mg po daily x 1 week, then increase to 60 mg po daily (max 60 mg/day)

272
Q

Side Effects of SNRIs

A
  • nausea
  • headache
  • hypertension
  • sedation
  • weakness
273
Q

SNRI clinical pearls

A
  • start low dose and titrate up to minimize side effects
  • renally dose adjust venlafaxine
  • avoid duloxetine for CrCl < 30 mL/min
274
Q

TCA uses

A
  • all off label
  • fibromyalgia
  • neuropathy
  • migraine prophylaxis
275
Q

TCA available formulations

A
  • tablet (amitriptyline)
  • capsule (nortriptyline)
  • oral solution (nortriptyline)
276
Q

TCA: Non-PO options?

277
Q

recommended dosing: TCA

A
  • 10 mg po qhs (max 150 mg/day)
278
Q

Side Effects: TCA

A
  • anticholinergic side effects
  • sedation
279
Q

Clinical Pearls: TCA

A
  • last line option for neuropathy and fibromyalgia due to side effects
280
Q

Muscle Relaxants available formulations

A
  • tablet/capsule (IR/XR)
  • oral suspension (baclofen)
  • parenteral solution (methocarbamol, baclofen)
281
Q

muscle relaxants: Non-PO options?

A

YES
- parenteral solution for methocarbamol and baclofen

282
Q

Side Effects: muscle relaxants

A
  • sedation/drowsiness
  • dizziness
  • dry mouth
  • vision changes
283
Q

Muscle relaxants clinical pearls

A
  • short term use (< 3 weeks)
  • carisoprodol is schedule IV due to abuse potential
284
Q

carbamazepine available formulations

A
  • tablet
  • ER capsule/tablet
  • chewable tablet
  • suspension
285
Q

carbamazepine: Non-PO options?

286
Q

recommended dosing of carbamazepine

A
  • 200-400 mg PO daily in 2-4 divided doses (max 1200 mg/day)
287
Q

Carbamazepine clinical pearls

A
  • increased risk of hypersensitivity reaction in patient with HLA-B*1502
  • auto induction of hepatic enzymes (levels will fall over first few weeks of use)
288
Q

Lidocaine available formulations

A
  • patch
  • injection
  • topical
289
Q

recommended dosing: lidocaine

A
  • apply 1 patch to affected area daily and remove 12 hours later (can vary by manufacturer)
290
Q

side effects: lidocaine

A
  • hypotension
  • arrhythmia (minimal risk with patch)
291
Q

lidocaine clinical pearls

A
  • tachyphylaxis with continuous use
  • 12 hour break between patches
  • local effect, apply to site of pain
292
Q

Capsacian available formulations

A
  • cream, gel, lotion: apply 3-4 times per day
  • patch: apply 1 patch to affected area daily and remove 8 hours later
293
Q

capsacian side effects

A
  • skin irritation and pain
294
Q

capsacian clinical pearls

A
  • do not get medicine into eyes (burning)
  • wash hands after applying
  • some formulations available OTC
295
Q

Recommendations for Older Adults: Nonselective COX-2 NSAIDs, aspirin > 325 mg/day

A
  • increased risk of GI bleeding or PUD
  • can increase blood pressure and induce kidney injury
  • use of ppi or misoprostol reduces but does not eliminate risk
  • avoid short term scheduled use in combo with oral or parenteral steroids, anticoagulants, or antiplatelet agents unless other alternatives are not effective and patient can take a gi protective agent
296
Q

Recommendations for Older Adults: Indomethacin and ketorolac

A
  • increased risk of GI bleeding/PUD/AKI in older adults
  • indomethacin has the most adverse effects, higher CNS effects
  • avoid
297
Q

Recommendations for Older Adults: Skeletal muscle relaxants

A
  • poorly tolerated by older adults because some have anticholinergic adverse effects, sedation, and increased risk of fractures
  • effectiveness at dosages toleraged by older adults is questionable
  • this does not include baclofen or tizanidine
  • avoid
298
Q

Recommendations for Older Adults: SNRIs/TCAs/Carbamezpine

A
  • may exacerbate or cause SIADH or hyponatremia
  • monitor sodium levels closely when starting or changing dosages in older adults
  • use with caution
299
Q

Recommendations for Older Adults: opioids + benzo combo

A
  • increased risk of overdose and adverse effect
  • avoid
300
Q

Recommendations for Older Adults: opioids + gabapentinoids combo

A
  • increased risk of severe sedation related adverse events older adults including respiratory depression and death
  • avoid
  • except transitioning from opioid to gabapentinoid or using gabapentinoid to reduce opioid dose
301
Q

Recommendations for Older Adults: anticholinergic and anticholinergic

A
  • increased risk of cognitive decline, delirium, and falls or fractures
  • TCA or muscle relaxant and other anticholinergic medication)
  • avoid, minimize the number of anticholinergic drugs
302
Q

Recommendations for Older Adults: antiepileptics, antidepressants, antipsychotics, benzos, z drugs, opioids, skeletal muscle relaxant combos

A
  • increased risk of falls and fracture with concurrant use of three or more CNS active agents
  • avoid concurrent use of three or more CNS active drugs
303
Q

Naloxone (narcan) treatment of overdose

A
  • opioid antagonist
  • IV: 0.4-2 mg q2-3 min
  • Nasal spray: 4 mg q2-3 minute alternate nostrils
  • can precipitate withdrawal
304
Q

Opioid Withdrawal onset

A
  • Short acting (heroin): 8-24 hours after last use; duration 4-10 days
  • long acting (methadone): 12-48 hours after last use; duration 10-20 days
305
Q

opioid withdrawal treatment

A
  • clonidine
  • buprenorphine
  • methadone
306
Q

Side effects of opioids

A
  • antitusive
  • constipation
  • n/v
  • itching
  • orthostatic hypotension
  • urinary retention
  • sedation
  • respiratory depression
307
Q

Codeine available formulations

A
  • tablet
  • cough syrup
308
Q

Codeine metabolism

A
  • CYP 2D6
  • poor metabolizers will get no effect from codeine
  • ultra rapid metabolizers can experience overdose, resulting in respiratory depression and death in children
  • not recommended in breastfeeding mothers or children<12
309
Q

Tramadol available formulations

A
  • capsule ER 24 hr
  • tablet IR and ER 24 hr
  • oral solution
  • combo products
310
Q

tramadol clinical pearls

A
  • risk of serotonin syndrome
  • renally dose adjusted
  • Use of CYP 3A4 inducers/inhibitors and 2D6 inhibitors with tramadol requires careful consideration of the effects on parent drug and metabolite
311
Q

Morphine Available Formulations

A
  • capsule ER 24 hr
  • tablet IR and 12 ER
  • oral solution
  • solution for injection
  • suppository
312
Q

Morphine: non-PO option?

313
Q

Morphine clinical pearls

A
  • itching more prominent compared to other opioids
  • morphine and its metabolites are renally excreted and accumulate in renal dysfunction
  • avoid in patients with ESRD or AKI
  • boxed warning: avoid alcohol while taking ER capsules
  • leads to increased morphine plasma levels and potentially fatal overdose
314
Q

Hydromorphone available formulations

A
  • IR and ER tablets
  • oral solutions
  • solutions for injection
  • suppository
315
Q

hydromorphone: non-PO available?

A

YES
- solution for injection
- suppositiory

316
Q

hydromorphone clinical pearls

A
  • US boxed warning about dosing errors when prescribing, dispensing
  • oral solution: do not confuse mg and mL
  • IV: do not confuse high potency (10 mg/mL) with other solutions
317
Q

hydrocodone+apap available formulations

A
  • oral solution
  • ER tablet
  • tablet
318
Q

hydrocodone+apap clinical pearls

A
  • counsel patients
  • use with cyp 3A4 inhibitors may increase hydrocodone plasma concentrations
319
Q

oxycodone available formulations

A
  • tablet
  • capsule
  • oral solution
320
Q

oxycodone clinical pearls

A
  • counsel patients on apap use with combination
  • ER capsule/tablets are abuse deterrent
  • CYP 3A4 inhibitors may increase plasma concentrations
321
Q

fentanyl available formulations

A
  • buccal tablet
  • sublingual liquid
  • lozenge
  • injectable solution
  • patch
322
Q

fentanyl: non-PO formulations?

A

YES
- IV
- Patch

323
Q

fentanyl: clinical pearls

A
  • Monitor patients receiving CYP 3A3 inhibitors or inducers
  • can use in renal impairment
  • less hypotension than morphine or hydromorphone at similar doses
  • non-injectable forms are only indicated for patients who are opioid tolerant
  • opioid tolerant is defined as taking morphine 60 mg per day (or equivalent) for at least 1 week
  • doses are not converted from one fentanyl product to another on a mcg-per-mcg basis
324
Q

fentanyl patch counseling

A
  • apply one patch every 72 hours
  • apply the patch tot he chest, back, flank, or upper arm
  • do not cut the patches or use a patch that is torn or damage
  • do not use the patch over broken skin
  • do not let the patch get too warm while wearing
  • your body will absorb too much medicine
325
Q

methadone use

A
  • last line treatment of chronic pain
  • opioid detoxification
326
Q

methadone available formulations

A
  • oral solution
  • injectable solution
  • tablet
327
Q

methadone clinical pearls

A
  • US boxed warning: QTc prolongation
  • US boxed warning: monitor patients receiving CYP 3A4 inhibitors or inducers
  • long half life (8-59 hours)
328
Q

meperidine available formulations

A
  • injectable solution
  • oral solution
  • tablet
329
Q

meperidine clinical pearls

A
  • avoid in elderly, avoid in renal impairment, caution use in hepatic impairment
  • monitor patients receiving cyp 3a4 inhibitors or inducers
  • do not use within 14 days of MAOi
  • metabolized by the liver into an active metabolite (accumulation of active metabolite can cause delirium and seizures)
  • not commonly used due to adverse effects
330
Q

potential side effects of opioid

A
  • lower seizure threshold
  • cause serotonon syndrome when used with other agents with serotonergic activity
  • tramadol
331
Q

Allergic Cross Reaction: Natural Opiates

A
  • morphine and codeine
  • YES, avoid in patients with allergy to other natural opiates and semi synthetic opioids
332
Q

Allergic Cross Reaction: Semi Synthetic Opiates

A
  • hydromorphone, oxycodone, oxymorphone, hydrocodone, buprenorphine
  • YES, avoid in patients with allergy to other semi synthetic opioids and natural opiates
333
Q

Allergic Cross Reaction: Synthetic Opioids

A
  • fentanyl, methadone, meperidine, tramadol
  • NO, can be used if patient has an allergy to another synthetic opioid, semi synthetic opioid, or natural opiate
334
Q

Switching between opioids

A
  • calculate daily consumption for each opioid
  • convert each opioid to oral morphine
  • add morphine doses together to get total daily oral morphine dose
  • reduce the equal analgesic by 25-50%
  • split total daily dose into appropriate dosing interval based on opioid selected (duration of action)

PHRM 845 (14 decks)

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