OA/RA/AD Pharmco Flashcards
Aspirin
- Non-selective COX Inhibitor
- pseudo- irreversible
- Uncouples mitochondrial oxidative phosphorylation
Aspirin ADR
- NVD
- GI upset + Bleed
- heartburn
- tachycardia
- Asthma
- Blood in vomit and stool
Which PG gives GI protection?
COX-1: PGE2
What happens when you inhibit PGE2?
GI Bleeding + peptic ulcer
Which COX and PGs are important for cardio?
COX-1 and COX 2
PGI2 and TxA2
Which NSAIDs are NON-selective but has more COX-2 activity?
- Diclofenac
- Etodolac
- Ketorolac
- Meloxicam
NSAID Prodrugs?
- Diclofenac
- Nabumetone
- Sulindac
NSAID Therapeutic use
- Headache
- Fever
- Pain
- RA/OA
- Dysmenorrhea
- Bursitis, tendonitis
What occurs when you take Aspirin with another NSAID?
You lose antiplatelet effect
NSAID ADR
- NVD
-Ulcers - Neutropenia
- Aplastic or Hemolytic Anemia
- Eosinophilia
- Hypersensitivity
- decrease in GFR
NSAID is associated with?
- Nephrotoxicity
- hematuria
- fluid retention
- colitis
COX-2 Inhibitors
- Celecoxib
Celecoxib Use
- OA/ RA
- Pain
- Dysmenorrhea
Celecoxib DI
- Fluconazole
- Lithium
- Loop diuretic
- Warfarin
- Rifampin
- MTX
Acetaminophen
Cox-3 inhibitor
Analgesic
Antipyretic
(Not anti-inflammatory)
High activity when Low ROS
APAP ADR
- Hematological effects
- CNS depression
- GI irritation + bleeding
- Metabolic acidosis
Arthritis treatment
- anti-inflammatory drugs
- Steroids
- Immunosuppressants
Other drugs for Arthritis
- capsaicin
- tramadol
- opioids
- duloxetine
Capsaicin
Desensitizes TRPV
Depletes Substance P
Tramadol
- opioid
- mu receptor agonist
- Suppresses 5-HT and NE- mediated nociceptors
Duloxetine
- SNRI
- 5-HT2A agonist
Anti-inflammatory Corticosteroid Class
Class 1 - Most potent
Class 7 - Least Potent
Corticosteroid MOA
Stimulate the synthesis of lipocortin which inhibits PLA1 from synthesizing AA
Corticosteroid effects
- Anti-inflammatory
- anti-mitotic
- immunosuppressant
- vasoconstriction
Corticosteroid ADR (short-term)
- GI issues
- Fluid retention
- insomnia
- agitation
- concentration difficulties
- irregular menses / vaginal yeast infection
Corticosteroid ADR (rare)
- psychosis
- diabetes
- Aseptic necrosis (skeletal)
Corticosteroid ADR (long-term)
- myopathy
- fragile skin
- osteoporosis
- lipodystrophy
- hair loss or facial hair
- cataracts
What are DMARDs?
Disease Modifying Anti-rheumatic Drugs
- immunosuppressants
- Stop underlying progression (without analgesic and inflammatory effects)
DMARD drugs
- hydroxychloroquine
- leflunomide
- methotrexate
- sulfasalazine
- tofacitinib
- baricitinib
- upadacitinib
Biologics are DMARDs
- TNF-inhibitor
- IL-1 Inhibitor
- IL-6 inhibitor
- T-cell inhibitor
- AntiCD20 Antibody
Anakinra
(Biologic)
- IL-1 inhibitor
- immunosuppressant