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Pharmacology > NSAIDs & DMARDs > Flashcards

NSAIDs & DMARDs Flashcards

1
Q

All side effects

Neural, Heart, GI, blood, liver, lungs, skin, kidneys

A
  1. Vertigo, tinnitus, headache
  2. HTN, retention & edema
  3. common stuff
  4. Thrombocytopenia, Neutropenia
  5. Liver failure
  6. Asthma
  7. Itching
  8. Kidney failure, Hyperkalemia, Proteinuria
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2
Q

Aspirin

Mechanism, half life, pharmacokinetic, clearance

A
  • COX, irreversible, no platelet adhesion
  • 8-10d effect, life of platelets
  • Good oral absorption
  • Acidic, for clearance we can alkalise urine
  • Low dose half life: 3-5h
  • High dose (anti-inflamatory) half life: zero degree kinetics , so side effects
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3
Q

Aspirin clinical use

A
  • Transient ischemic attacks
  • Prevention of angina
  • Coronary thrombosis prevention
  • Thrombosis preventin in bypass
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4
Q

Aspirin side effects

A
  • All side effects, GI more
  • In type II patients: GI bleed
  • Contraindication in hemophilia
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4
Q

Aspirin side effects

A
  • All side effects, GI more
  • In type II patients: GI bleed
  • Contraindication in hemophilia
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5
Q

COX II selective inhibitors

A
  • Celecoxib
  • Etodolac
  • Meloxicam
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5
Q

COX II selective inhibitors

A
  • Celecoxib
  • Etodolac
  • Meloxicam
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6
Q

Celecoxib

Mechanism, use

A
  1. 10-20 times stronger
  2. Only prostacyclins (in heart endothelium)
  3. Osteoarthritis, RA, JRA, 100-200mg BID
  4. 400mg daily in schizophrenia
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7
Q

Celecoxib side effects

A
  1. GI bleed
  2. Little effect on platelets
  3. Toxicity w/ lithium, fluconazol
  4. Interaction w/ warfarin
  5. Rash
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7
Q

Celecoxib side effects

A
  1. GI bleed
  2. Little effect on platelets
  3. Toxicity w/ lithium, fluconazol
  4. Interaction w/ warfarin
  5. Rash
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8
Q

Etodolac

A
  • Racemic
  • Oral
  • Medium half life, glucuronidation clearance
  • OA, RA, JRA 300-500mg BID/TID
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9
Q

Meloxicam

Mechanism, use

A
  • Not selective, but COX II more
  • Inhibit thromboxan A2 synthesis
  • OA, RA, JRA 7.5 - 15mg
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10
Q

Non-selective COX inhibitors

A
  1. Diclofenac
  2. Flurbiprofen
  3. Ibuprofen
  4. Indomethacin
  5. Ketoprofen
  6. Nabumetone
  7. Naproxen
  8. Piroxicam
  9. Sulindac
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11
Q

Diclofenac

Salts, forms, use, side effects

A
  • Na, K, Epolamin
  • Ophth, gel, supp, oral, IM
  • for less GI: Omeprazole
  • More kidney problems, less GI
  • OA, RA, JRA
  • Increase serum aminotransferase
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12
Q

Flurbiprofen

Form, use, mechanism, side effects

A
  • Oral, ophth, IV
  • Myosis prevention
  • Pain management in ENT surgeries
  • in RA, OA
  • Racemic
  • S enantiomer: TNF-a & Nitric oxide synthesis inhibition
    Side effects:
  • Ataxia
  • Tremor
  • Myoclonus & shaking
  • Rigidity
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13
Q

Ibuprofen

A
  • IV, topical, patch
  • in RA, PDA (indomethacin more)
  • 400-600 mg < Analgesic < 1600mg/d
  • Decrease TNF-α, IL-1
14
Q

Ibuprofen side effects & contraindications

A
  • Less urinary output & water retention
  • Can negate aspirin, so not together
    Contraindications:
  • Nose polyp
  • Angioedema
  • Bronch constriction reaction to aspirin
  • SLE (can cause meningitis)
  • Agranolocytosis & Aplastic anemia
15
Q

Indomethacin

A
  • Better in kids
  • Inhibit A&C phospholipase, neutrophil migration, B&T-cell proliferation
  • RA, OA, AS, Tendonitis, Muscular pain, Gout (Naproxen better)
  • Surgical pain like Laminectomy
    Side effects:
  • GI
  • Pancreatitis, Ulcerative colitis
  • most important Headache
  • Depression, parkinson, epilepsy
  • Eye problems
15
Q

Indomethacin

A
  • Better in kids
  • Inhibit A&C phospholipase, neutrophil migration, B&T-cell proliferation
  • RA, OA, AS, Tendonitis, Muscular pain, Gout (Naproxen better)
  • Surgical pain like Laminectomy
    Side effects:
  • GI
  • Pancreatitis, Ulcerative colitis
  • most important Headache
  • Depression, parkinson, epilepsy
  • Eye problems
16
Q

Ketoprofen

A
  • COX & LOX
  • +Probenacid: More half life & concentration, less urine clearance
  • RA, OA
  • w/ Tramadol & Dexketoprofen: Better analgesic effect in dental surgeries
  • NOT > 300mg/d
17
Q

Nabumetone

A
  • NOT acidic, is a pro-drug
  • 35% works in active form & is like naproxen
  • 24h half life
  • NOT enterohepatic
    Side effects:
  • Diarrhea
  • Stomach pain
18
Q

Naproxen

side effects too

A
  • Single enantiomer
  • More free fraction in women
  • OA, RA, Gout, Tendonitis, AS
  • w/ sumatriptan for migraine
    Side effects:
  • Nausea
  • Drowsiness
  • Tiredness
  • GI bleed
  • More cardiovascular risk than profen
  • Vasculitis & Porphyria
  • Allergic pneumonia
  • Contraindication in liver problems
19
Q

Piroxicam

A
  • High concentration: Inhibits PMN migration, Inhibit lymphocyte actions
  • 57h
  • Oral, inj, topical
    Side effects:
  • if > 25mg/d: GI bleed
  • Most GI bleeding
20
Q

Sulindac

A
  • Pro-drug
  • Bile, enterohepatic
  • 12-16h
  • Rheumatic diseases
  • Hereditary intestine polyps
  • Colon, prostate, breast cancer
    Side effects:
  • Thrombocytopenia
  • Agranolocytosis
  • Nephrotic syndrome
  • Liver problems
  • Pancreatitis
  • if w/ DMSO, Peripheral neuropathy
21
Q

NSAIDs without CYP450 metabolism

A
  • Diflunisal
  • Etodolac
  • Ketoprofen
  • Oxaprozin
  • Tolmetin
22
Q

DMARDs

Definition, duration, types

A
  • Disease Modifying AntiRheumatic Drugs
  • 2w-6m
  • Synthetic (csDMARDs) / Biologic (bDMARDs)
23
Q

csDMARDs

A
  • Cyclophosphamide
  • [Hydroxy]Chloroquine
  • Azathioprine
  • Methotrexate (*)
  • Sulfasalazine
  • Mycophenolatemofetil
  • Leflunomide
  • Cyclosporine
24
Q

bDMARDs

A
  1. T-cell modulatory (Abatacept)
  2. B-cell (Rituximab)
  3. ILs, IL-6 (Tocilizumab)
  4. IL-1 (Anakinra, Rilonacept, Canakinumab)
25
Q

bDMARDs

A
  1. T-cell modulatory (Abatacept)
  2. B-cell (Rituximab)
  3. ILs, IL-6 (Tocilizumab)
  4. IL-1 (Anakinra, Rilonacept, Canakinumab)
  5. TNF-α
26
Q

Azathioprine

A
  • Cancers, Autoimmune, RA, SLE, Psoriasis, Vasculitis, Behcet
  • 6-MP then 6TG
  • T&B-cell, Igs, IL-2 inhibition
  • in RA 2mg/kg/day
    Side effects:
  • Bone marrow suppression
  • GI
  • Carcinogen
  • Immune system suppression
  • Leukopenia in NVDT15
27
Q

Calcineurin inhibitors

A

Cyclosporine
Tacrolimus

Pharmacology (6 decks)

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