OA/RA/AD Pharmco Flashcards

1
Q

Aspirin

A
  • Non-selective COX Inhibitor
  • pseudo- irreversible
  • Uncouples mitochondrial oxidative phosphorylation
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2
Q

Aspirin ADR

A
  • NVD
  • GI upset + Bleed
  • heartburn
  • tachycardia
  • Asthma
  • Blood in vomit and stool
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3
Q

Which PG gives GI protection?

A

COX-1: PGE2

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4
Q

What happens when you inhibit PGE2?

A

GI Bleeding + peptic ulcer

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5
Q

Which COX and PGs are important for cardio?

A

COX-1 and COX 2
PGI2 and TxA2

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6
Q

Which NSAIDs are NON-selective but has more COX-2 activity?

A
  • Diclofenac
  • Etodolac
  • Ketorolac
  • Meloxicam
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7
Q

NSAID Prodrugs?

A
  • Diclofenac
  • Nabumetone
  • Sulindac
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8
Q

NSAID Therapeutic use

A
  • Headache
  • Fever
  • Pain
  • RA/OA
  • Dysmenorrhea
  • Bursitis, tendonitis
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9
Q

What occurs when you take Aspirin with another NSAID?

A

You lose antiplatelet effect

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10
Q

NSAID ADR

A
  • NVD
    -Ulcers
  • Neutropenia
  • Aplastic or Hemolytic Anemia
  • Eosinophilia
  • Hypersensitivity
  • decrease in GFR
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11
Q

NSAID is associated with?

A
  • Nephrotoxicity
  • hematuria
  • fluid retention
  • colitis
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12
Q

COX-2 Inhibitors

A
  • Celecoxib
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13
Q

Celecoxib Use

A
  • OA/ RA
  • Pain
  • Dysmenorrhea
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14
Q

Celecoxib DI

A
  • Fluconazole
  • Lithium
  • Loop diuretic
  • Warfarin
  • Rifampin
  • MTX
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15
Q

Acetaminophen

A

Cox-3 inhibitor
Analgesic
Antipyretic
(Not anti-inflammatory)
High activity when Low ROS

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16
Q

APAP ADR

A
  • Hematological effects
  • CNS depression
  • GI irritation + bleeding
  • Metabolic acidosis
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17
Q

Arthritis treatment

A
  • anti-inflammatory drugs
  • Steroids
  • Immunosuppressants
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18
Q

Other drugs for Arthritis

A
  • capsaicin
  • tramadol
  • opioids
  • duloxetine
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19
Q

Capsaicin

A

Desensitizes TRPV
Depletes Substance P

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20
Q

Tramadol

A
  • opioid
  • mu receptor agonist
  • Suppresses 5-HT and NE- mediated nociceptors
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21
Q

Duloxetine

A
  • SNRI
  • 5-HT2A agonist
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22
Q

Anti-inflammatory Corticosteroid Class

A

Class 1 - Most potent
Class 7 - Least Potent

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23
Q

Corticosteroid MOA

A

Stimulate the synthesis of lipocortin which inhibits PLA1 from synthesizing AA

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24
Q

Corticosteroid effects

A
  • Anti-inflammatory
  • anti-mitotic
  • immunosuppressant
  • vasoconstriction
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25
Q

Corticosteroid ADR (short-term)

A
  • GI issues
  • Fluid retention
  • insomnia
  • agitation
  • concentration difficulties
  • irregular menses / vaginal yeast infection
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26
Q

Corticosteroid ADR (rare)

A
  • psychosis
  • diabetes
  • Aseptic necrosis (skeletal)
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27
Q

Corticosteroid ADR (long-term)

A
  • myopathy
  • fragile skin
  • osteoporosis
  • lipodystrophy
  • hair loss or facial hair
  • cataracts
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28
Q

What are DMARDs?

A

Disease Modifying Anti-rheumatic Drugs
- immunosuppressants
- Stop underlying progression (without analgesic and inflammatory effects)

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29
Q

DMARD drugs

A
  • hydroxychloroquine
  • leflunomide
  • methotrexate
  • sulfasalazine
  • tofacitinib
  • baricitinib
  • upadacitinib
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30
Q

Biologics are DMARDs

A
  • TNF-inhibitor
  • IL-1 Inhibitor
  • IL-6 inhibitor
  • T-cell inhibitor
  • AntiCD20 Antibody
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31
Q

Anakinra
(Biologic)

A
  • IL-1 inhibitor
  • immunosuppressant
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32
Q

Anakinra ADR

A
  • Immunosuppression
  • Inj Site rxn
  • Upper respiratory infection
  • NVD
  • Allergic rxn
  • autoantibody dyscrasias
33
Q

Methotrexate

A
  • Inhibits Dihydrofolate reductase (DHFR)
  • inhibit the synthesis of polyamine
  • Anti-folate properties
34
Q

Methotrexate ADR

A
  • NVD
  • Hepatic/renal Failure
  • anemia
  • rigidity
  • GI issues
  • CNS toxicity
  • pharyngitis
  • cirrhosis
  • portal vein fibrosis
35
Q

Methotrexate Contraindication

A

Do NOT take with NSAIDs
- NSAID compete with MTX which causes toxic levels of mtx in the blood

36
Q

Leflunomide

A
  • antirheumatic, immunosuppressant, immunomodulator
  • Inhibits DHODH and pyrimidine synthesis (t-cell)
  • analgesic, anti-pyretic, histamine-blocking
37
Q

Leflunomide ADR Common

A
  • alopecia
  • Diarrhea
  • increased LFTs
  • rash
38
Q

Leflunomide ADR serious

A
  • bronchitis
  • HTN
  • Respiratory infection
  • Hepatotoxicity
  • SJS
39
Q

Apazone + Nimesulide

A
  • weak COX inhibitors
  • inhibits interleukin and leukocytes
40
Q

Tumor Necrosis Factor inhibitor

A
  • blocks signals from macrophage to Helper T-cells (TNF-alpha)
  • for severe RA
  • May be toxic, but for QoL
41
Q

What receptors are on the Osteocyte surface?

A

IL-1 receptor
IL-6 receptor
TNF receptor

42
Q

TNF Inhibitor (drug names)

A
  • adalimumab
  • certolizumab
  • etanercept **
  • golimumab
  • infliximab **
43
Q

IL-6 Inhibitor Drugs

A
  • Tocilizumab
  • Sarilumab
44
Q

B-cell Inhibitor (Anti- CD20)

A

Rituximab

45
Q

CD80 and CD86 inhibitor

A

Abatacept

46
Q

Infliximab
(biologic)

A

TNF-alpha NEUTRALIZER
- chimeric antibody
- reduces synovial inflammation, bone resorption, cartilage degradation
- binds to both transmembrane and soluble form of TNF

47
Q

Infliximab ADR

A

(common) Abdominal pain, NVD
Serious
- delayed hypersensitive rxn
- infusion rxn
- an invasive fungal infection
- tuberculosis
- epilepsy
- worsening of CHF

48
Q

Etanercept
(biologic)

A
  • TNF-alpha BINDER
    recombinant DNA technology
49
Q

Etanercept ADR COMMON

A
  • GI effects
  • NVD
  • Inj site rxn
  • respiratory symptoms
  • exacerbation of CNS disorders
50
Q

Etanercept Serious ADR

A
  • allergic rxn
  • anemia
  • leukopenia
  • neutropenia
  • pancytopenia
  • thrombocytopenia
  • sepsis
  • optic neuritis (permanent )
51
Q

Abatacept
(biologic)

A
  • T-cell co-stimulatory inhibitor
  • blocks release of co-stimulatory factors from APCs (prevent activation of T cells)
  • binds to B7 protein
52
Q

Abatacept ADR

A
  • NVD. fever, chill flu-like symptoms, weight loss
  • trouble breathing, chest pain, wheezing, painful urination
  • skin infection
  • stomach pain, indigestion, back pain
53
Q

Tocilizumab
IL-6 inhibitor

A
  • reduce pain + inflammation
  • blocks metalloproteases
54
Q

Tocilizumab ADR

A
  • NVD
  • Flu-like symptoms
  • trouble breathing, chest pain, phlegm, painful urination
  • Skin infection
  • blistering rash
  • bruising, tarry stool, coffee ground vomit
  • stomach pain, indigestion, back pain
55
Q

Sarilumab
IL-6 Inhibitor

A
  • Human monoclonal AB
  • IL-6 receptor inhibitor
  • reduces pain and inflammation
  • slows/ prevents joint dmg
56
Q

Rituximab
(biologic)

A
  • B-cell CD20 inhibitor
  • B-cell lysis
57
Q

Rituximab ADR

A
  • NVD
  • CV
  • inj site rxn
  • allergic rxn
  • abdominal pain
  • flu, bronchitis
  • vertigo
  • Heart failure
58
Q

Tofacitinib

A
  • JAK 1/3 inhibitor
  • blocks STAT activity, affecting gene expression
  • reduction in t- and b- lymphocytes
59
Q

Tofacitinib ADR

A
  • Systemic infection (nose, throat, UTI)
  • NVD, headache
  • increase in TG/ cholesterol
60
Q

Upadacitinib

A

JAK 1 inhibitor

61
Q

Baricitinib

A

Oral
JAK 1 AND 2 inhibitor

62
Q

Baricitinib ADR

A
  • IMMUNOSUPPRESSION
  • Flu-like symptoms
  • increased urination + pain (?)
  • stomach pain
  • diarrhea
  • SoB
  • pink/ red mucus
63
Q

Cutaneous Drug Reaction

A
  • can be mildly discomforting or life-threatening
  • often associated with anti-infective and anti-convulsant medications
64
Q

Major classes that Cause cutaneous rxn

A
  • NNRTI
  • Anticonvulsant
  • sulfonamides
  • antibiotics
  • NSAID (oxicams)
  • Antifungal
  • Antimalarial
  • allopurinol
65
Q

(Main) 4 drugs Cutaneous Rxn

A
  • sulfamethoxazole-trimethoprim
  • sulfasalazine
  • phenytoin
  • carbamazepine
66
Q

Exfoliative Dermatitis

A
  • aka erthema multiforme
  • mainly seen on extensor surface
  • may be associated with herpes, systemic infection, Disease-drug rxn
  • sudden onset with history of occurrance
67
Q

Erythema multiform MAJOR (SJS)

A
  • more than 50% of skin has fallen off
  • erosive involving 2 or more mucosal surface
  • commonly: coral, conjunctiva
68
Q

Drug-Induced EM
Toxic Epidermal Necrolysis

A
  • most severe vesiculobullous disease on this spectrum
  • more than 20% BSA in 24 hrs
  • Skin peels in large sheets
  • accompanied by: constitutional (flu-like) symptoms
69
Q

SJS Treatment

A
  • supportive
  • fluid balance; acid-base
  • pain management
  • prednisone
  • Cyclosporine or azathioprine
  • IgG
  • Biologics (infliximab)

loss of skin - loss of protein

70
Q

Low dose Aspirin Inhibits?

A

COX-1

71
Q

Heteroaryl propionic acid

A
  • contains heteroaryl ring
  • more cox-2 than cox-1
  • this selectivity lowers GI risks
72
Q

Oxicams
Tautomer B is more potent than Tautomer A.
Why?

A

In Tautomer A, there is NH which allows the H to constantly travel. In tautomer B, Instead of NH, it’s a N= which stops the movement of H

72
Q

COX-1 enzymes

A
  • constitutive
  • Produces TxA2
72
Q

COX-2 enzymes

A
  • Induced by cytokines and GFs to produce PG
  • Produces PGI2
72
Q

PGI2 (prostacyclin)

A
  • vasodilator
  • anti-platelet
72
Q

Phospholipase A2

A

Cleaves AA from cell membrane phospholipids

72
Q

Misoprostol

A
  • Semi-synthetic derivative of PGE1 (prodrug)
  • reduced gastric ACID secretion
  • stimulates gastric MUCUS secretion
  • Vasodilation (increased blood flow)
73
Q

TxA2 (thromboxane)

A
  • vasoconstriction
  • platelet aggregation
74
Q

Antidote to APAP?

A

N-Acetyl Cysteine