Pharmacology Flashcards
What is the mode of action of bisphosphonates?
Bind to hydroxyapatite in bone
Taken up by osteoclasts during bone resorption
Lead to apoptosis of osteoclasts - reduce bone resorption
What is the side effect of bisphosphonates?
Oesophagitis Esophageal ulcers Gastric irritation Osteonecrosis of the jaw Osteonecrosis of auditory ear canal Increased risk of atypical stress fracture Hypocalcaemia
What is the mode of action of Denosumab?
Binds to RANKL to inhibit activation and maturation of osteoclasts to limit bone breakdown
S/E: diarrhoea, dyspnoea, hypocalcaemia, URTI
What is the mode of action of NSAIDs?
Inhibiting the activity of cyclooxygenase enzymes (COX-1 and/or COX-2) in the arachidonic pathway, thus reducing the production of key mediators involved in inflammation such as prostaglandins, leukotrienes.
What is the mode of action for the oral contraceptive pill?
Synthetic oestrogens inhibit FSH release by negative feedback, suppressing follicular development.
Synthetic progesterone like compounds (progestins) block the oestrogen-mediated positive feedback surge in LH release, preventing ovulation, also change the properties of cervical mucous so that it is hostile to sperm.
Endometrial development is scant and not favourable for implantation.
What is the mode of action of paracetamol?
Paracetamol is a COX enzyme inhibitor.
Selective for COX-3.
COX enzymes stimulate the production of prostaglandins. Paracetamol helps to prevent PGE2 synthesis which is the main compound that alters the homeostatic temperature set point in the hypothalamic neurons that regulate body temperature.
In fever, the temperature set point is elevated by the production of PGE2.
PGE2 production is stimulated by cytokines (IL-1, TNF alpha), which are produced by the action of bacteria/viruses on the immune system. By blocking PGE2 production, paracetamol brings down the temperature set point to normal
What are side effects of glucocorticoids?
Osteoporosis Retardation of growth Immunosuppression Cataracts and glaucoma Psychosis Diabetes Stomach ulcers Thinning of skin, bruising, delayed wound healing Cushings - Moon face, Buffalo hump
What is the mode of action of azathioprine?
Prodrug of mercaptopurine
Inhibits purine synthesis
Need to test for TPMT first to ensure have enzymes to convert to prodrug
What are the side effects of azathioprine?
Bone marrow suppression
Nausea/vomiting
Pancreatitis
Interaction with allopurinol
What is the mode of action of methotrexate?
Antimetabolite that inhibits dihydrofolate reductase, an enzyme essential for the synthesis of purines and pyrimidines
What are side effects of methotrexate?
Myelosuppression - pantocytopenia Pneumonitis Pulmonary fibrosis Liver fibrosis Hepatotoxicity
What are side effects of NSAIDs?
Peptic ulceration
Exacerbation of asthma
Kidney failure
Heart failure
What is the monoclonal antibody against CD20 on B cells?
Rituximab
What are the monoclonal antibody against TNF-alpha?
Infliximab
Adalimumab
Etanercept
What is the monoclonal antibody against HER2?
Trastuzumab