NSAIDs Flashcards
Acetylsalicylic acid
AKA aspirin
Non-opioid analgesics
Anti-fever, and anti-inflammatory drug (we dont use it as an anti-inflammatory drug!)
Irreversible COX inhibitor, COX-1> COX-2
Therapeutic effects:
1. Inhibition of platelet aggregation (80-300 mg/day) for preventing/treating arterial thrombosis
2. Analgesic (500mg/day)
3. Antipyretic- reduces fever (500mg/day)
4. Anti-inflammatory (4-5 g/day) - we dont use it for this indication
Special adverse effects:
1. Bleeding
2. Hepatic effects - asymptomatic hepatitis, Reyes syndrome
3. Hypersensitive reactions in the CNS - tinnitus, vertigo, decrease of hearing, hyperventilation (stimulates the respiratory center, inhibits oxidative phosphorylation)
4. Hyperglycemia (with large doses)
5. Hyperuricemia (contraindicated in gout)
INTOXICATION: metabolic acidosis, respiratory depression, hyperpyrexia, coma
LETHAL DOSE: 10-30 mg
Therapy - sodium bicarbonate i.v + symptomatic
Naproxen
Non-opioid analgesics
Proprionic acid
Relatively selective COX1 inhibitors
Long duration of action (more than 10 hours) - half life is 14 hours
It inhibits the migration of neutrophils
Commonly used to mediate inflammation, pain and fever
Dex-ibuprofen
Non-opioid analgesics
Proprionic acid
Used for the management of patent ductus arteriosus
First line druge
COX-1=COX-2
Dex-ketoprofen
Non-opioid analgesics
Proprionic acid
Ketoprofen - topical
Dex-ketoprofen - oral
It has some lipoxygenase inhibition too
Inhibits COX enzymes (which we know decreases production of prostoglandins - compounds that mediate pain and inflammation
Relatively selective COX-1 inhibitor
Indomethacin
Non-opioid analgesics
Hematologic effects - aplastic anaemia, agranulocytosis
Relatively selective COX-1 inhibitors
Short duration of action (less than 10 hours)
Acetic acid derivative
COX-1>COX-2 +inhibition of cell migration and lymphocyte proliferation, anti-inflammatory and anti-gout effect
SPECIAL INDICATIONS: hodgkin disorder as antipyretic
Management of patent ductus arteriosus (second line)
SEVERE ADVERSE EFFECTS: GI irritation, CNS (severe headache, depression, psychosis), hematologic reactions (aplastic anemia, thrombocytopenia), renal side effects
Diclofenac
Non-opioid analgesics
Inhibitors showing weak selectivity towards COX-2
Short duration of action (less than 10 hours)
Acetic acid derivatives
Anti-inflammatory (Accumulates in synovial fluid)
Analgesic, antipyretic
SIDE EFFECTS: enhancement of the transaminase level, significant fluid retention, precaution is cardiovascular diseases
Meloxicam
Non-opioid analgesics
Inhibitors showing medium selectivity towards COX-2
Long duration of action (more than 10 hours)
Enol acid derivative (OXICAMS)
Higher affinity towards COX-2
Half life is about 20 hours
Causes edema especially in elderly patients
Celecoxib
Non-opiod analgesic
Inhibitors showing medium selectivity towards COX-2
Used mainly as anti-inflammatory drugs
It contains a sulfonamide group - potential concern for individuals with sulfonamide allergies
Phenylbutazone
Non-opioid analgesic
Pyrazolone derivative
Anti-inflammatory, analgesic, antipyretic
SEVERE SIDE EFFECTS: used only in severe inflammation, maximum for 1 week (in Bechterew disease sometimes longer)
It is also used topically (thrombophlebitis)
Metamizole
Non-opioid analgesic
– CHAT GPT
Pain relief and fever reduction
It also has spasmolytic properties
SIDE EFFECTS: risk of agranulocytosis (decrease in WBCs), allergic reactions (including skin rashes and anaphylaxis)
BANNED/ RESTRICTED IN SOME COUNTRIES LIKE USA BUT STILL USED IN EUROPEAN COUNTRIES
Paracetamol
COX inhibitors but not anti-inflammatory
-COX inhibition in the brain COX-3
- It inhibits the peroxidase activity of COX enzymes, but not the endoperoxide synthase (cyclooxygenase) activity
Short duration of action
In case of not too high doses its safe
Can be administered to children/ pregnancy
SIDE EFFECTS: acute hepatic necrosis (might be fatal) - dose dependent (adult: 10-15g and children: 6-8g)
Alcoholics and children are more sensitive
