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IPT: MS > Block 1 > Flashcards

Block 1 Flashcards

1
Q

What is the most common systemic inflammatory disease?

A

Rheumatoid arthritis

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2
Q

When does rheumatoid arthritis occur?

A

At any age

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3
Q

Rheumatoid arthritis occurs more frequently in (men/women)

A

Women

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4
Q

Are genetics a risk factor for rheumatoid arthritis?

A

Yes, especially rheumatoid factor as it is the most important factor

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5
Q

In RA, (osteoblasts/osteoclasts) are promoted

A

Osteoclasts; breaks down bones

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6
Q

Signs of RA

Joint involvement is (asymmetrical/symmetrical)

A

Symmetrical

whereas osteoarthritis it is asymmetrical

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7
Q

What is the most important risk factor in gout or hyperuricemia?

A

Elevated serum urate levels

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8
Q

Gout/hyperuricemia occurs more frequently in (men/women)

A

Men

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9
Q

What is hyperuricemia?

A

Accumulation of uric acid in blood (≥6.8)

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10
Q

Gout and hyperuricemia are inflammatory joint diseases due to what?

A

Deposition of monosodium urate crystals

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11
Q

Solubility limit of serum urate?

A

Anything >7 exceeds the solubility limit

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12
Q

What are some production sources of uric acid?

A

Dietary purines (beef, liver, alcohol)

Converted via 2 enzymes

De novo synthesis of purine bases

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13
Q

How is uric acid excreted?

A

Urine (66%) or GI tract

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14
Q

Which enzymes can cause a build up of uric acid?

A

PRPPase can increase the levels and a deficiency of HGPRTase can also increase it

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15
Q

Which drugs can induce hyperuricemia and gout?

A

Diuretics

Salicylates (<2g) **do not stop drug to prevent gout if they have a heart issue, risk

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16
Q

Which joint is the most commonly affect in gout?

A

Big toe

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17
Q

Do NSAIDs alter the course of RA or prevent joint destruction?

A

No, it just helps with inflammation

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18
Q

Methotrexate targets what?

A

DHFR

Inhibits PURINE synthesis

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19
Q

MTX metabolism, excretion, and AE?

A 
Metabolism = liver
Excretion = urine
AE = liver damage
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20
Q

MTX interaction?

A

PCN

Cyclosporine

NSAIDs

Probenecid

Cola

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21
Q

CI of MTX?

A

Liver disease or Immunodeficiency

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22
Q

Active form of leflunomide?

A

Teriflunomide

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23
Q

Target of leflunomide?

A

DHODH

Inhibits PYRIMIDINE synthesis

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24
Q

Leflunomide vs MTX, which one has a half life of 14-18 days?

A

Leflunomide

MTX is like 8hrs

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25
Q

Leflunomide metabolism? AE?

A

Prodrug, metabolized in GI and liver

AE = infection and liver toxicity

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26
Q

Interaction of leflunomide?

A

Live vaccines

Warfarin

Diabetic drugs or rosuvastatin

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27
Q

What can be used as a binding agent when used with leflunomide?

A

Cholestyramine; use if serious toxicities occur or if pt wishes to become pregnant

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28
Q

Metabolism and excretion of hydroxychloroquine?

A

Rapid GI absorption and excreted by kidney

Half life = 30-50 days

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29
Q

Hydroxychloroquine AE?

A

Ocular toxicity

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30
Q

CI of Hydroxychloroquine?

A

Hypersensitive to 4-aminoquinoline or any retinal field changes

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31
Q

Rituximab MOA?

A

Targets CD20 protein on B cells

Different from the other biological DMARDs as they are TNF alpha inhibitors

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32
Q

Which biological DMARDs contains mouse proteins?

A

Infliximab

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33
Q

Which biological DMARDs contains murine proteins?

A

Rituximab

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34
Q

TNF alpha blocker AE and interactions?

A

AE = inj. site reaction (etanercept only) + infections

Interaction = anakira + live vaccines

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35
Q

What effect does colchicine have on serum uric acid levels?

A

No effect

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36
Q

Colchicine MOA?

A

Inhibits microtubules (for gout)

Prevents activation, degranulation and migration of neutrophiles

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37
Q

Colchicine metabolism?

A

CYP3A4

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38
Q

Colchicine interaction?

A

P-gp and CYP3A4 inhibitors

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39
Q
  • Enhance uric acid degradation
  • Increase uric acid excretion
  • Reduce uric acid production

Pegloticase
Uricosuric rx
Xanthine oxidase inhibitors

A

Xanthine - reduce production

Uricosuric - increase excretion

Pegloticase - enhance degradation

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40
Q

Can you use urate-reducing drug therapy in acute gout attack?

A

No, may prolong it by changing equilibrium of body rate

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41
Q

What are the xanthine oxidase inhibitors?

A

Allopurinol + Febuxostat

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42
Q

What are the uricosuric drugs?

A

Probenecid (targets URAT1)

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43
Q

Pegloticase targets what?

A

Uric acid; converts uric acid to allantoin (more excretable metabolite)

Used in refractory pts

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44
Q

Allopurinol AE? Interaction?

A

Allopurinol hypersensitivity syndrome

DDI with azathioprine and didanosine

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45
Q

Structurally, what’s different about febuxostat vs allopurinol? Interactions?

A

Febuxostat is NOT purine like; it’s a thiazole carboxylic acid derivative. Does NOT have hypersensitivity syndrome

DDI with azathioprine, mercaptopurine, theophylline

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46
Q

Probenecid AE and DDI?

A

GI issues, hypersensitivity

DDI with ASA

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47
Q

Pegloticase AE, DDI, CI?

A

Chest pain, nasopharyngitis, anaphylaxis

DDI - Probenecid, sulfinpyrazone, allopurinol

CI - G6PD deficiency

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48
Q

Can you use NSAIDs as monotherapy for RA?

A

No

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49
Q

Special AE/allergy of selective COX inhibitors?

A

BP increases due to sodium and fluid retention

Sulfa allergy

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50
Q

Can you use corticosteroids as monotherapy for RA?

A

No

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51
Q

To reduce systemic AE of corticosteroids, how can you give them?

A

Intra-articularly

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52
Q

Short and long term AE of corticosteroids?

A

Short term - insomnia/mood swings, BG/Wt gain, HTN

Long term - Cushings, Osteoporosis, infection

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53
Q

Methotrexate dose for RA?

A

7.5mg ONCE WEEKLY

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54
Q

Methotrexate CI

A

Pregnancy, Liver issues, alcoholism

Causes liver issues

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55
Q

What is the initial therapy + their considerations for RA?

A

Methotrexate

Premedicate w/ folic acid (5mg/week)

Dose adjustments for renal/hepatic impairment

Use contraception for at least 3 months after d/c

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56
Q

Leflunomide dose for RA?

A

LD = 100mg PO daily x3days

Then 20mg PO daily

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57
Q

Leflunomide considerations for RA?

A

Take Cholestyramine 8g TID for 11 days (overdose)

Contraception is still needed for a few months after d/c

Dont take live vaccine

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58
Q

Hydroxychloroquine considerations for RA?

A

Can be used as monotherapy for MILD disease if MTX is CI

Retinal damage

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59
Q

Sulfasalazine consideration for RA?

A

Dont take w/ Sulfa or salicylate allergy

Yellow-orange urine/skin discoloration

Abx and iron can decrease absorption

Affects warfarin

Premedicate with antihistamine or steroids to prevent serum sickness

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60
Q

What are the JAK inhibitors?

A

”..inib”

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61
Q

What is the dose of Tofacitinib for RA?

A

5mg PO BID (IR) or 11mg QD (ER)

Reduce to 5mg QD (IR) in renal or hepatic impairment

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62
Q

Tofacitinib CI and considerations?

A

Avoid in severe impairment, lymph count <500, ANC <1000 or hgb<9

DI w/ 3A4 inhibitors

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63
Q

Baricitinib dose for RA?

A

2mg PO BID

Dont use if GFR<60

Used if pt failed ≥1 TNF blockers

**pretty much same CI and consideration w/ Tofacitinib

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64
Q

Which JAKi can be used as monotherapy?

A

Upadacitinib

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65
Q

Which JAKi should be used cautiously with history of thrombosis or latent TB?

A

Upadacitinib + Baricitinib

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66
Q

Upadacitinib dosing for RA?

A

15mg PO QD

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67
Q

Which JAKi should you not take w/ biological DMARDs or strong immunosuppressants?

A

Upadacitinib + Baricitinib

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68
Q 
Adalimumab
Etanercept
Infliximab
Golimumab
Certolizumab

Which one must be taken w/ith MTX?

A

Infliximab + Golimumab

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69
Q 
Adalimumab
Etanercept
Infliximab
Golimumab
Certolizumab

Which one has a CI of sepsis?

A

Etanercept

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70
Q 
Adalimumab
Etanercept
Infliximab
Golimumab
Certolizumab

Which one is dosed at 40mg SQ q14 days?

A

Adalimumab

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71
Q 
Adalimumab
Etanercept
Infliximab
Golimumab
Certolizumab

Which one has a CI of doses >5mg/kg in CHF?

A

Infliximab

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72
Q 
Adalimumab
Etanercept
Infliximab
Golimumab
Certolizumab

Which one is dosed at 50mg SQ weekly for 25mg SQ twice weekly?

A

Etanercept

73
Q 
Adalimumab
Etanercept
Infliximab
Golimumab
Certolizumab

Which one has murine proteins?

A

Infliximab

74
Q 
Adalimumab
Etanercept
Infliximab
Golimumab
Certolizumab

Which one is dosed at 50mg SQ monthly?

A

Golimumab

75
Q 
Adalimumab
Etanercept
Infliximab
Golimumab
Certolizumab

Which one is dosed as an IV infusion?

A

Infliximab

76
Q 
Adalimumab
Etanercept
Infliximab
Golimumab
Certolizumab

Which one is dosed at 400mg SQ at 0,2,4 weeks then 200mg q14 days?

A

Certolizumab

77
Q

Abatacept (orencia) dosing?

A

IV based on weight

<60kg - 500mg

60-100kg - 750mg

> 100kg - 1000mg

78
Q

Abatacept considerations and monitoring?

A

Dont give w/ TNF alpha inhibitors

Screen for TB and Hep B

79
Q

Rituximab consideration and monitoring?

A

Give w/ MTX

Premedicate w/ benadryl, steroid, APAP

TB and Hep B screen

80
Q

Tocilizumab consideration and monitoring?

A

Elevated lipids, transaminitis

Dont give w/ combo DMARDs

TB screening

81
Q

Abatacept
Rituximab
Tocilizumab

Humanized, inhibits IL-6

A

Tocilizumab

82
Q

Abatacept
Rituximab
Tocilizumab

Binds to CD20, depletes B cells

A

Rituximab

83
Q

Abatacept
Rituximab
Tocilizumab

Binds to CD80/86, prevents interaction of MPC and T cells

A

Abatacept

84
Q

Early RA management

A

<6months

Low activity - DMART mono then to combo

Moderate/high - straight to combo

No JAKi, only used in established RA

85
Q

Established RA management

A

> 6months

Low activity - DMART mono then to combo

Moderate/high - straight to combo

CAN use JAKi, then start to switch to another class. Cant cure RA

If in remission, consider tapering but never d/c

86
Q

What are the killed vaccines?

A

Pneumococcal, IM flu, hep B, HPV

87
Q

What is the most common symptoms of gout/uricemia?

A

“Joint on fire”

88
Q

How is acute gouty arthritis classified?

A

Intensity

Mild = ≤4
Moderate = 5-6
Severe = 7-10

Duration

Early <12hrs
Well established 12-36hrs
Late >36hrs

89
Q

What is the goal urate target?

A

<6

90
Q

Which NSAIDs are approved for tx of gout? When should they be initiated?

A

Indomethacin, naproxen, and sulindac

ASAP or within 24 hrs

91
Q

Colchicine MOA?

A

Antimitotic agent

Prevents migration of neutrophils

No analgesic property

92
Q

Colchicine dosing?

A

LD = 1.2mg PO then 0.6mg one hr later on day one, Then 0.6 1-2 times a day

Max of 1.8mg in acute tx or 1.2mg in prophylaxis

Beneficial to use within 36 hrs after onset of attack

93
Q

Colchicine CI and AE?

A

CI = using P-gp or 3A4 inhibitors

AE = diarrhea

94
Q

Treatment guideline for gout with NSAIDs, Colchicine, or systemic corticosteroid based on mild, moderate, severe pain

A

Mild/moderate = monotherapy, if inadequate switch to another mono or just add another drug on top

Severe = combo

Combo is NEVER NSAIDs + oral corticosteroids

95
Q

What are some indications for pharmacologic ULT for chronic management?

A

Diagnosis of gouty arthritis AND one of the following:

2+ gout attacks / year

Presence of 1+ tophus

Evidence of radiographic damage

96
Q

Which ULT for chronic management should NOT be initiated during a flare up?

A

Probenecid, wait until its over

97
Q

Allopurinol doisng?

A

100mg daily and titrate every 2-4 or 5 weeks.

There is renal dosing

98
Q

Allopurinol AE and considerations?

A

Dont take with HLA-B*5801 allele (asians)

Maculopapular eruption

DRESS, SJS, TEN

99
Q

Febuxostat AE and consideration?

A

Transaminitis

FDA warning for increased death in pt with CV issues

Should only be prescribed if they cant take allopurinol or failed it.

100
Q

Probenecid AE and considerations?

A

AE of Urolithiasis

Initiate after gout attack but if attack occurs, just continue

Avoid in CrCl<30

101
Q

Lesinurad CI and AE?

A

CI: CrCl <30

AE: nephrolithiasis and renal failure

Must take with food and water in combo with XOI

102
Q

Pegloticase consideration?

A

d/c all oral urate-lowering rx prior to initiation

CI in G6PD deficiency

Premedication with antihistamine and corticosteroid

103
Q

Nerve fibers in conduction

A-delta vs C-polymodal

A

A-delta = large, myelinated, localized pain

C = small, unmyelinated, poorly localized pain

Both use voltage gated sodium channels

104
Q

Acute pain lasts how long?

A

<30 days

> 30 is chronic

105
Q

Goal of Acute vs Chronic Pain?

A

Acute - treat it

Chronic - functionality

106
Q

Which drug was more lipophilic and had superior CNS penetration vs morphine?

A

Heroin

107
Q

Morphine derivative opioids produce their analgesic effects through which receptor?

A

Agonism of mu-opioid receptors

108
Q

Oxymorphone
Nalbuphine
Butorphanol
Buprenorphine

mu (+/-)
kappa (+/-(

A

Oxymorphone; mu +

Nalbuphine and butorphanol; mu - and kappa +

Buprenorphine; partial mu +

109
Q

Pharmacophore of general morphine derivatives?

A

4-Phenylpiperidine; 3 rings with a nitrogen

110
Q

Oxymorphone
Nalbuphine
Naloxone
Naltrexone

Differences in R1 group?

A

Oxymorphone = 1C

Nalbuphine = 5C

Naloxone/Naltrexone = 3-4 C

111
Q

Morphine + Codeine

Differences in R2 group?

A

Codeine = Methoxy group

Morphine = Hydroxyl group

112
Q

What group is associated w/ histamine release in morphine derivatives?

A

C6-OH

113
Q

What must be active to contribute to analgesic activity of codeine/morphine?

A

Morphine-6-glucuronide + O-demethylation

114
Q

Oral bioavailability of codeine vs morphine is enhanced due to….

A

methyl esters

115
Q

Hydromorphone/oxymorphone have (more/less) DDI vs morphine/codeine

A

Less cause CYP450 play less of a role

116
Q

What kind of metabolizers are a concern with codeine?

A

UR CYP2D6 metabolizers, especially in poor renal function

117
Q

For naloxne and naltrexone vs mu opioid receptor agonist, what do they replace the N methyl group with?

A

Allyl or cyclopropylmethyl groups

118
Q

Special info on methylnaltrexone?

A

AKA relistor

Quaternary amine and peripherally restricted

Used in opioid induced constipation

119
Q

Special info on Buprenorphine?

A

Even tho it has the cyclopropylmethyl group, its NOT a mu opioid antagonist, but rather an agonist lol

25-50x more potent than morphine

120
Q

Kappa vs Mu agonists, what are some benefits?

A

Kappa agonists have less respiratory depression, constipation, potential for addiction

However, sedation and dysphoria are the biggies

121
Q

Fentanyl structure?

A

Non-morphne derivative

Has a N-phenethyl group

Increased lipophilicity, fast onset, short duration

122
Q

Which analgesic is CI w/ MAOIs?

A

Meperidine

123
Q

Normeperidine AE?

A

Neurological issues

124
Q

Fentanyl DI?

A

Interacts w/ CYP3A4 inducers/inhibitors

125
Q

Analgesic effects of methadone are due to (R/S) enantiomer

A

R

126
Q

Methadone info on metabolites?

A

Metabolized in liver and produces 2 metabolites that inhibit CYP2C19

127
Q

Which analgesic carries a risk of serotonin syndrome?

A

Tramadol

128
Q

Which metabolite of Tramadol exerts the analgesic effect?

A

Both enantiomer and its metabolite do

129
Q

All opioid receptors (mu, delta, and kappa) are ________ receptors

A

G-protein coupled

130
Q

Match plz

Dynorphins
Endorphins
Enkephalins

Delta
Kappa
Mu

A

Kappa - Dynorphins

Delta - Enkephalins

Mu - Endorphins

131
Q

When a G-protein coupled receptor is activated, what happens to Calcium and Potassium channels?

A

Inactivates Calcium and activates Potassium

Inhibits adenylyl cyclase

Activates phospholipase C

132
Q

Delta
Kappa
Mu

Which one produces respiratory depression?

A

Mu + Delta

133
Q

Delta
Kappa
Mu

Which one produces euphoria?

A

Mu + Delta

134
Q

Delta
Kappa
Mu

Which one produces constipation?

A

Mu + Kappa

135
Q

Delta
Kappa
Mu

Which one produces dysphoria?

A

Kappa

136
Q

Delta
Kappa
Mu

Which one produces pinpoint pupils?

A

Mu + Kappa

137
Q

Delta
Kappa
Mu

Which one produces constipation?

A

Mu + Kappa

138
Q

Delta
Kappa
Mu

Which one produces psychotomimetic effects?

A

Kappa

139
Q

Analgesia emerges from what steps in the message to brain/spinal cord?

A

Blocks ascending message

Inhibits pain fibers in dorsal horn

140
Q

Opioids increase the pain threshold at the spinal cord by….?

A

Inhibit release of substance P, makes it harder to get message to second order neurons

141
Q

Pain is better controlled (before/during/after) drug effects are gone

A

Give drug BEFORE last dose wears off

142
Q

(Neuropathic/Nociceptive) pain is relieved better

A

Nociceptive

Dull > Sharp

143
Q

Delta
Kappa
Mu

Which one produces a sense of tranquility and rewarding properities?

A

Mu + Delta

144
Q

How are opioids linked to seizures?

A

Mu + Delta can inhibit GABA release, hyperpolarizes cell

145
Q

What is the primary cause of morbidity related to opioid therapy?

A

Respiratory depression (use cautiously in asthma, COPD, other respiratory conditions)

146
Q

Which analgesic have antitussive properties?

A

Morphine + codeine (depresses cough reflex) by affected the medulla

147
Q

If you see pupils dilating (mydriasis) in analgesic therapy, whats going on?

A

Onset of asphyxia

148
Q

Opioid agonists produce N/V by affecting what?

A

Chemoreceptor zone in area postrema

149
Q

Absorption and Distribution of Morphine?

A

Slow GI; significant first pass

Enters all tissues including fetuses

150
Q

When is fentanyl indicated?

A

Breakthrough pain in cancer pt who are tolerant to opioids

Chronic pain in opioid tolerant pt

151
Q

Compared to morphine, how does methadone stack up in potency, euphoria, and duration?

A

Equipotent

Less euphoria

Longer duration

152
Q

Additional MOA of methadone?

A

NMDA antagonist + SNRI

153
Q

Which analgesic is more likely to produce delirium?

A

Meperidine; only used for short term acute pain

154
Q

Which analgesic can lower seizure threshold?

A

Tramadol

155
Q

Compared to morphine, how does tramadol affect respiratory suppression?

A

Less suppression vs morphine

156
Q

Which analgesic is used for rapid detoxification?

A

Naltrexone

157
Q

If you notice a pt is using their PRN meds for pain frequently, what should you do?

A

Switch to scheduled

158
Q

IV OPIOID NAIVE pt

If continuous infusion is desired, when can it be set?

A

After 4-8hrs

159
Q

IV OPIOID NAIVE pt

How do you calculate their dose?

A

Add up PRN dose in 24hrs and take 50% of it.

10-15% of total infusion can be PRN q2-3hrs

Example: Morphine 2mg q2h = 24*0.5 = 12mg/24hrs

+

12*0.1 = 1.2 or 1mg PRN for breakthrough pain

160
Q

What is a reasonable regimen to decrease dose when tapering opioids?

A

10% reduction /week or month

161
Q

How do you go from PRN to scheduled opioid use?

A

Take total amount / 24 hrs period and divide by their dosing interval + PRN dose (10%)

Examples: 12mg / 24hrs, they take it every 4hrs

12/6doses = 2mg q4h

+ 12*0.1 = 1.2mg PRN

162
Q

How do you calculate a continuous infusion for opioid use?

A

Take total dose in 24hrs and divide by 50% and then by 24hrs for hourly rate + 10% for PRN

  1. 5mg q2h = 120.5 = 6/2 = 3mg/24 = 0.125mg/hr + 30.1 = 0.3mg PRN
  2. 125mg/hr + 0.3 PRN
163
Q

How do you calculate opioid dose for CHRONIC pain?

A

Start with short-acting PRN, then add long acting opioid (50-75% of PRN)

Titrate PRN to be 10% of TDD

164
Q

What are some nonpharmacologic Tx that are considered somewhat beneficial or have limited evidence?

A

Somewhat - spinal cord stimulation

Limited - TENS and lumbar support

165
Q

Which Rx is the first line for osteoarthritis pain?

A

APAP

166
Q

What are the first line tx for neuropathic pain?

A

Amitriptyline

Duloxetine

Pregabalin

Gabapentin

+ Tramadol for breakthrough pain PRN

167
Q

Naturally occuring agents
Semi-synthetic agents
Synthetic agents

Which one has the most/least histamine release?

A

Most - natural (morphine, codeine)

Least - synthetic

168
Q

Which opioid should NOT be used in children or if breastfeeding?

A

Codeine (mothers were UR metabolizers)

BBW: respiratory depression and death in children following tonsillectomy in UR metabolizers

169
Q

Fentanyl patch info?

A

NEVER for acute pain, do NOT titrate up for acute pain

170
Q

Which opioid has interactions with MAOIs?

A

Fentanyl + Meperidine

However less blood pressure effects of fentanyl vs other opioids

171
Q

When checking for tolerance, how much do you reduce the dose by?

A

25-50%

172
Q

Risk factors for Fibromyalgia?

A

Females

FH

Physical trauma, infections, stress, cold weather

173
Q

Clinical presentation of fibromyalgia?

A

Pain all over the body + fatigue

174
Q

Drug induced fibromyalgia caused by…?

A

Statins or aromatase inhibitors (anastrozole, letrozole)

175
Q

How would you diagnose fibromyalgia?

A

Pain present for most of the day for at least 3 months that cant be attributed to another cause

176
Q

What are the FDA indicated drugs and what should you just avoid?

A

Indicated - duloxetine, milnacipran, pregabalin

AVOID - opioids

No cure

177
Q

Pregabalin AE?

A

Somnolence, wt gain, fatigue

178
Q

If someone has fibromyalgia and has fatigue, what do you use? No fatigue, but has depression?

A

Fatigue, use pregabalin

Depressed, use duloxetine

IPT: MS (3 decks)

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