Drugs Used in Pain and Inflammation Flashcards
Corticosteroids
Fludrocortisone
Hydrocortisone
Fludrocortisone - MOA
Mineralocorticoid.
Acts on electrolyte + H2O metabolism.
Fludrocortisone - Administration
Oral
Fludrocortisone - Therapeutic Use
Replaces aldosterone in adrenal insufficiency
Congenital adrenal hyperplasia
Fludrocortisone - Adverse Effects
Na+ & H2O retention Hypertension Oedema Headache Hypokalemia Muscle weakness & fatigue, Immunosuppression Depression Weight gain
Hydrocortisone - MOA
Glucocorticoid.
Anti-inflammatory & immunosuppressant. Metabolic effects [↑ gluconeogenesis, glycogen deposition, & protein / lipid / Ca2+ metabolism]
Hydrocortisone - Administration
Oral
IV
Topical
Hydrocortisone - Therapeutic Use
Severe allergic reactions
Eczema
Gout
Hydrocortisone - Adverse Effects
Dryness
Itching
Leukotrine Antagonists
Zileuton
Mintelukast
Zileuton - MOA
Active inhibitor of 5-LOX enzyme. Results in inhibition of: 1. LTB4 2.LTC4 3. LTD4 4. LTE4
Zileuton - Administration
Oral
Zileuton - Therapeutic Use
Asthma
Allergies (allergic rhinitis)
Zileuton - Adverse Effects
Sinusitis
Nausea
Mintelukast - MOA
Leukotriene receptor antagonist
Mintelukast - Administration
Oral
Mintelukast - Therapeutic Use
Asthma
Allergies (allergic rhinitis)
Mintelukast - Adverse Effects
GIT disturbances Headaches, Hypersensitivity Sleep disorders ↑ bleeding
Non Steroidal Anti-Inflammatories
Aspirin Diclophenac Indomethacin Piroxicam Ibuprofen Naproxen Mefenamic Acid
Non Steroidal Anti-Inflammatories - MOA
Competitive, reversible COX I + II inhibition.
Inhibits thromboxane production
Non Steroidal Anti-Inflammatories - Kinetics
Oral
Rectal
IV
IM
Non Steroidal Anti-Inflammatories - Therapeutic Use
Analgesic
Anti-inflammatory
Anti-pyretic
Non Steroidal Anti-Inflammatories - Adverse Effects
Related to PG Inhibition:
- GIT effects (ulceration, perforation, bleeding),
- Inhibit platelet aggregation resulting in ↑ bleeding time
- Renal vasoconstriction leading to ischemia (nephrotoxicity)
- Prolonged gestation/bleeding in pregnancy
Unrelated to PG inhibition:
- Tinnitus
- Hypersensitivity (rash, bronchospasm)
Non Steroidal Anti-Inflammatories - D/I
Anti-coagulants
Anti-hypertensives
Lithium.
Aspirin - MOA
Irreversibly acetylates COX I and II
Aspirin - Kinetics
Absorption: Rapid - stomach & small intestine
Biotransformation: Liver (glycine conjugation)
Excreted: Urine (alkalinity increases)
Aspirin - Therapeutic Use
Analgesic
Anti-inflammatory
Anti-pyretic
In v. low doses: prevent MI/Strokes etc
Aspirin - Adverse Effects
GIT distress
Renal dysfunction
Aspirin - C/I
Children
Pregnancy
Paracetamol - MOA
Reversible, non-competitive inhibition of COX I + II (in brain)
Paracetamol - Kinetics
Rapid absorption
Hepatic conjugation
Paracetamol - Therapeutic Use
Analgesic
Antipyretic
Paracetamol - Adverse Effects
Mild to non-existent.
Skin rash
Allergic reactions.
Acute overdose - hepatic necrosis
Paracetamol - C/I
Hepatic damage
Paracetamol - Administration
Oral
IV
Rectal