Block 12-Week 3 Flashcards
Diclofenac
Cox inhibitor
NSAID also anti pyretic
Used for :
Pain , ocular inflammation
Dysmenorrhea
Celebcoxib
COX-2 specific inhibitor
Reducing production of PGs
Used to treat rhemutoid arthritis , osteoarthritis , FAP
Cyclophosphamide
An alkylating agent
Antineoplastic , anti immunosuppressive agent activated by P450 in liver
Used to read cancers such as myelomas and leukaemias
Non cell cycle specific , all induce cell death
Attaches alkyl groups to DNA bases resulting in DNA being fragmented by repair enzymes stopping DNA synthesis and RNA transcription from damaged DNA , cross linking of DNA to prevent DNA transcription
Induction of DNA mis pairing leading to mutations
Vitamin D : A coenzyme
Metabolised to 1,25-dihydroxycholecalciferol - activated then bind to receptors and form a complex with retinoic-X receptor then modulate gene expression as complex acts as a transcription factor
Ciclosporin
Immunosuppressive agent
Used for prophylaxis of graft rejection in organ and tissue transplantation
Inhibits T lymphocytes - T helper cell main target - inhibits immunocompetent lymphocytes
Aurothiomalate
Gold based anti inflammatory - cytokine inhibitor
Given as an intramuscular injection
Not widely used as superceded by other DMARDs and biological treatments
Chloroquine
Anti inflammatory - DNA/RNA synthesis inhibitor
Anti malarial drug - inhibit parasitic enzyme heme polymerase causing a build up of toxic Heme within the parasite
Treats rheumatoid arthritis (DMARDs)
Thought to reduced inflammatory agents IL-6 TNFa . IL-1 b.
Methotrexate
Folate antagonist
Anti-metabolite synthetic versions of purines and pyrimidines - building blocks of DNA prevent purines and pyrimidines being incorporated into DNA during S phase of cycle stopping normal development and cell division.
Inhibits Folic acid reductase which converts folic acid to tetrahydrofolic acid which is required for purine and pyrimidines biosynthesis . - stopping DNA synthesis
Used at low dose in management of severe or definite RA
Sulfasalazine
Anti immunomodulatory agent
Anti inflammatory agent - used to treat ulcerative colitis and RA
Replaced by Mesalazinr - Dosent contain sulphur so better tolerated by some patients
Calcitonin /Salcatonin
Hormone produced by thyroid gland agonist
Controls Ca conc in blood
Antagonise parathyroid hormone
Calcitonin binds to calcitonin receptor in osteoclasts (GPCR receptor) activating cAMP and calcium signalling pathways leading to increased production of vitamin D producing enzymes , greater calcium retention and enhanced bone density
Not commonly used as treatment
Prednisolone
Glucocorticoid receptor agonist - corticosteroid - binds to receptor and leads to changes in DNA transcription reducing production of inflammatory proteins - affect cell membrane altering ion permeability and neuro hormone production
Raloxifene
Selective oestrogen receptor modulator
In bones , binds to receptor reducing bone resorption and Increasing bone mineral density in post menopausal women slowing rate of bone loss
Alendronic acid
Nitrogen containing Second generation biphosphonate
Strengthens bone hence used in corticosteroid induced osteoporosis in post menopausal women
Inhibits FPP inhibition of this enzyme in osteoclasts prevents the post translational farnesylation and geranylgeranylation of small GTPase signalling proteins causing a reduction in osteoclasts activity reducing bone resorption and turnover
Digoxin
Cardiac glycoside
Sodium potassium ATPase inhibitor
Used in AF
