NSAIDs Flashcards
2 negative effects of prostaglandin (an eicosanoid) synthesis inhibition?
Kidneys: Fluid retention ^Na+
Stomach: ^Acid, ¥Mucous –> Mucousal irritation
Prostaglandins:
^Renal blood flow
Inhibition of PG’s lead to?
** Renal failure in Compromised patients & Athletes
- DECREASE GFR
- ^ BP (fluid & Na+ retention)
- ^ K+ (heart arrhythmias)
- Oedema
1) NSAIDs: MOA?
2) How do NSAIDs work?
1) Inhibit CYCLOOXYGENASE (COX)
2) Inhibit formation of eicosanoids
(e. g Prostaglandins)
NSAIDs:
1) Adverse effects from?
2) 3 most common ADR?
1) Inhibition of COX-1 & COX-2 synthesis (non-selective) 2) (peptic ulcer, nausea, & vomiting) - Epigastric distress - Microscopic bleeding (~ALL w/ aspirin) - Renal Impairment
1) COX-1 located? Inhibition causes?
2) COX-2 located? Inhibition causes?
1) COX-1 present in most tissues Inhibition causes ADVERSE EFFECTS 2) COX-2 @ site of inflammation Inhibition: Analgesic & Anti-inflam. effects (NSAIDs --> COX -//-> Prostanoids)
Selective COX-2 inhibitor ISSUES:
Coxibs: Patients can develop?
^Risk heart attack
Healing peptic ulcers?
- SIGNIFICANT GASTRO
Duodenal ulcer & Bleeding - Decrease PGF2 –> Decrease protective anticoagulative effect
- Slowed down
1) NSAIDs: 3 common therapeutic properties? (Vary in strength of effects)
2) NSAIDs most effective when?
1) Analgesia / Anti-inflammatory / Anti-pyretic
2) Presence of inflammatory component
(Arthritis, muscle pain)
1) Antipyretic action: NSAIDs inhibit what?
2) NSAIDs do not decrease temp in what?
1) PGE production
2) Heat stroke
1) Aspirin: Action?
2) Used after ____ to prevent ____.
3) 2 other actions besides antiplatelet?
Treatment in?
1) PLATELET AGGREGATION - ANTIPLATELET [˅ thromboxane (TXA2) synthesis] 2) MI ; Transient ischaemic attack (minor stroke) 3) Analgesic & Antipyretic --> Rheumatic fever & RA
1) Aspirin side effect?
2) Aspirin before surgery?
3) If taking salicylates (e.g. Aspirin)?
1) ^ Bleeding time
2) Do not take aspirin AT LEAST 1 WEEK before surgery.
3) DECREASE Anticoagulant dosage
(Salicylates inhibit PG synthesis)
Aspirin:
1) For ____, but ^____ effects.
2) How to minimise GI disturbances?
3) ADR common in?
1) Mild pain; ^ GI effects
2) Take w/ Food & ^Fluids
3) Elderly & chronic users
Aspirin causes IRREVERSIBLE inhibition by +Acetyl group (Acetylating; covalent bonding) to?
COX @ SERINE 530 (amino acid)
1) How is low dosage aspirin eliminated?
2) How is anti-inflammatory dosages of Aspirin eliminated?
1) <600mg/day (low dosage)
First-order kinetics
2) 4g/day (anti-inflammatory dosage)
Zero-order kinetics
Aspirin, ibuprofen, paracetamol: reversible/irreversible inhibition?
Irreversible: Aspirin
Reversible: Ibuprofen, Paracetamol
1) Ibuprofen: well tolerated & effective pain relief e.g.?
2) Drug of choice for _____ because?
1) Dysmenorrhoea
(excessive menstrual pain)
2) INFLAMMATORY joint disease ;
Low incidence side effects
Paracetamol:
1) Used as?
2) Toxic?
3) Treatment?
1) Antipyretic & Analgesia ONLY
2) FATAL HEPATOTXICITY >2-3 X Therapeutic dose
3) N-acetyl cysteine
PIROXICAM: (potent drug)
1) Used for?
2) Dose?
3) Adverse?
1) Chronic inflammatory conditions
(arthritis, gout, ankylosing sponditis)
2) 20mg PO ONCE DAILY (T1/2 50hrs)
3) ^ GI Problems
1) Actions on GIT:
Aspirin causes decrease PG’s resulting in?
Which causes what?
2) Stop use of Aspirin when?
In stomach:
^ Gastric acid secretion; ˅ Mucus levels
= MUCOSAL IRRITATION
2) Signs of RENAL IMPAIRMENT
(can cause Acute reversible renal impairment)
Aspirin Hypersensitivity: S/S:
- Bronchoconstriction
1) Urticaria (wheals)?
2) Angiooedema?
3) Fatal anaphylactic shock?
1) Red elevated patches (wheals) w/ severe itching
2) Acute swelling (subcut oedema): Face, neck, larynx, viscera (soft internal organs of the body)
3) Rare
REYE’S SYNDROME:
1) Associated with?
2) Occurs in?
3) Often fatal. S/S?
1) Aspirin given during viral infections
2) CHILDREN, young teens
(treat w/ Paracetamol Not aspirin)
3) Sudden severe HEPATITIS (liver inflam)
Cerebral oedema (Brain swelling); Confusion; Coma
