Block 12 Pharmacology Flashcards
Azathioprine
Purine metabolism antagonist (Immunosuppresive drug)
Uses: Autoimmune conditions (RA, SLE, Chrohn’s, Ulcerative colitis) and to prevent transplant rejection
MOA: Inhibits purine synthesis -> inhibits DNA/RNA synthesis -> inhibits CELL PROLIFERATION
S/E: bone marrow suppression (need monitoring for myelosuppresion)
Diclofenac
NSAID
Analgesic and Anti-pyretic with some anti-inflammatory efffect
Uses: Pain, dysmenorrhea and ocular inflammation (miosis)
MOA: Inhibition of COX1 and COX2 -> inhibition of prostaglandin synthesis
Celecoxib
NSAID
Uses: RA and osteoarthritis and FAP
MOA: COX2 SPECIFIC inhibitor -> inhibition of prostaglandin synthesis
note: only targeting COX2 means no anti-platelet effect (like aspirin) -> cannot be used as substitute
Cyclophosphamide
Alkylating agent
Uses: Chemotherapy drug (leukaemias and myelomas)
MOA: • Attach alkyl groups to DNA bases OR
• Form cross-bridges between base pairs in DNA OR
• Cause the mispairing of the nucleotides leading to mutations
Vitamin D (Cholecalciferol)
Fat soluble coenzyme
Uses: Rickets, osteoporosis and vit. D deficiency -> increases Ca absorption from intestines and decrease PTH which decreases resorption of calcium from bones
MOA: • It’s a prodrug, becomes hormonally active once metabolised in liver and kidney
• In the liver cholecalciferol -> 25-hydroxycholecalciferol
• In the kidney 25-hydroxycholecalciferol -> 1,25-dihydroxycholecalciferol.
Ciclosporin
Immunosupressive agent
Uses: To prevent raft rejection in organ and tissue transplantation.
MOA: Binds to cyclophilin -> this inhibits calcineurin -> decreased transcription of IL-2.
This causes reversible inhibition of T cells (TH1) in the G0/ G1 cell cycle phase.
Aurothiomalate
DMARD A gold based anti-inflammatory/immunosuppressive agent
Uses: Rheumatoid arthritis
MOA: Unknown - possible inhibition of prostaglandins
Chloroquine
Anti-malarial (Shizonticidal)
Uses: to treat infections caused by chloroquine-resistant P.falciparun malaria or acute attacks of malignant malaria (P. falciparum)
MOA: Inhibit heme breakdown used for digestion -> lack of breakdown = parasite starves and toxic levels hemoglobin builds up -> PARASITIC death
Same MOA as quinine
Sulfasalazine
DMARD
Uses: IBD (Crohn’s, UC) and RA
MOA: Unknown. Thought to be anti-inflammatory
Calcitonin/Salcatonin
Hormone produced by thyroid parafollicular cells
Uses: Hypercalcemia
MOA: Reduces Serum Ca levels (opposes action of PTH which increases concentrations) -> binds GCPR receptors in osteoclasts and increased bone deposition
Prednisolone
Glucocorticoid receptor agonist (Corticosteroid)
Uses: Anti-inflammatory and immunomodulatory -> RA, SLE, leukemias, lymphomas etc
MOA: Binds nuclear glucocorticoid receptor -> inhibit expression of prostaglandins, kinins, histamine and other inflammatory mediators
Raloxifene
Selective oestrogen receptor modulator
Uses: Slows the rate of bone loss and used as treatment of post-menopausal symptoms
MOA: Binds to oestrogen receptors in bone -> reduces bone resorption and increases bone mineral density in post-menopausal women. Also antagonises effects of oestrogen on mammary and uterine tissues.
Alendronic acid
Bisphosphonate
Uses: to treat osteoporosis (especially in PM women), Paget’s disease and hypercalcemia
MOA: inhibits osteoclast activity and reduces bone resorption and turnover (via inhibition of FPP synthase)
Digoxin
Cardiac glycoside (Na/K ATPase inhibitor)
Uses: Heart failure, supraventricular arrhythmias, and AF
MOA: Inhibits the Na/K ATPase which increasing intracellular Na -> This in turn causes the Na-Ca exchanger to extrude sodium out and pump in more calcium -> increases contractility of heart muscle cells.
Betaxolol
Cardioselective B1 adrenoceptor antagonist
Uses: Ischaemic heart disease (note: bisoprolol is more commonly used)
MOA: Inhibits B1 receptors are found in heart -> reduction of heart rate, cardiac output, systolic and diastolic blood pressure
