NSAIDs & DMARDs Flashcards
All side effects
Neural, Heart, GI, blood, liver, lungs, skin, kidneys
- Vertigo, tinnitus, headache
- HTN, retention & edema
- common stuff
- Thrombocytopenia, Neutropenia
- Liver failure
- Asthma
- Itching
- Kidney failure, Hyperkalemia, Proteinuria
Aspirin
Mechanism, half life, pharmacokinetic, clearance
- 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
Aspirin clinical use
- Transient ischemic attacks
- Prevention of angina
- Coronary thrombosis prevention
- Thrombosis preventin in bypass
Aspirin side effects
- All side effects, GI more
- In type II patients: GI bleed
- Contraindication in hemophilia
Aspirin side effects
- All side effects, GI more
- In type II patients: GI bleed
- Contraindication in hemophilia
COX II selective inhibitors
- Celecoxib
- Etodolac
- Meloxicam
COX II selective inhibitors
- Celecoxib
- Etodolac
- Meloxicam
Celecoxib
Mechanism, use
- 10-20 times stronger
- Only prostacyclins (in heart endothelium)
- Osteoarthritis, RA, JRA, 100-200mg BID
- 400mg daily in schizophrenia
Celecoxib side effects
- GI bleed
- Little effect on platelets
- Toxicity w/ lithium, fluconazol
- Interaction w/ warfarin
- Rash
Celecoxib side effects
- GI bleed
- Little effect on platelets
- Toxicity w/ lithium, fluconazol
- Interaction w/ warfarin
- Rash
Etodolac
- Racemic
- Oral
- Medium half life, glucuronidation clearance
- OA, RA, JRA 300-500mg BID/TID
Meloxicam
Mechanism, use
- Not selective, but COX II more
- Inhibit thromboxan A2 synthesis
- OA, RA, JRA 7.5 - 15mg
Non-selective COX inhibitors
- Diclofenac
- Flurbiprofen
- Ibuprofen
- Indomethacin
- Ketoprofen
- Nabumetone
- Naproxen
- Piroxicam
- Sulindac
Diclofenac
Salts, forms, use, side effects
- Na, K, Epolamin
- Ophth, gel, supp, oral, IM
- for less GI: Omeprazole
- More kidney problems, less GI
- OA, RA, JRA
- Increase serum aminotransferase
Flurbiprofen
Form, use, mechanism, side effects
- 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
Ibuprofen
- IV, topical, patch
- in RA, PDA (indomethacin more)
- 400-600 mg < Analgesic < 1600mg/d
- Decrease TNF-α, IL-1
Ibuprofen side effects & contraindications
- 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
Indomethacin
- 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
Indomethacin
- 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
Ketoprofen
- COX & LOX
- +Probenacid: More half life & concentration, less urine clearance
- RA, OA
- w/ Tramadol & Dexketoprofen: Better analgesic effect in dental surgeries
- NOT > 300mg/d
Nabumetone
- NOT acidic, is a pro-drug
- 35% works in active form & is like naproxen
- 24h half life
- NOT enterohepatic
Side effects: - Diarrhea
- Stomach pain
Naproxen
side effects too
- 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
Piroxicam
- High concentration: Inhibits PMN migration, Inhibit lymphocyte actions
- 57h
- Oral, inj, topical
Side effects: - if > 25mg/d: GI bleed
- Most GI bleeding
Sulindac
- 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
NSAIDs without CYP450 metabolism
- Diflunisal
- Etodolac
- Ketoprofen
- Oxaprozin
- Tolmetin
DMARDs
Definition, duration, types
- Disease Modifying AntiRheumatic Drugs
- 2w-6m
- Synthetic (csDMARDs) / Biologic (bDMARDs)
csDMARDs
- Cyclophosphamide
- [Hydroxy]Chloroquine
- Azathioprine
- Methotrexate (*)
- Sulfasalazine
- Mycophenolatemofetil
- Leflunomide
- Cyclosporine
bDMARDs
- T-cell modulatory (Abatacept)
- B-cell (Rituximab)
- ILs, IL-6 (Tocilizumab)
- IL-1 (Anakinra, Rilonacept, Canakinumab)
bDMARDs
- T-cell modulatory (Abatacept)
- B-cell (Rituximab)
- ILs, IL-6 (Tocilizumab)
- IL-1 (Anakinra, Rilonacept, Canakinumab)
- TNF-α
Azathioprine
- 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
Calcineurin inhibitors
Cyclosporine
Tacrolimus