Block 5 Pharmacology Flashcards
Alendronic acid - class?
Nitrogen containing bisphosphonate
Alendronic acid - MoA?
Inhibits farnesyl pyrophosphate (FPP) synthase.
Inhibits osteoclastic activity so reduced bone resorption.
Alendronic acid - uses?
Osteoporosis
Paget’s disease
Calciferol - class?
Vitamin D agonist
Calciferol - MoA?
Increases mobilisation of Ca2+ in bones.
Prevents maturation of osteoclasts.
Calciferol - uses?
Vitamin D deficiency
Calcitonin - class?
Thyroid hormone
Calcitonin - target?
Calcitonin receptor (GPCR) on osteoclasts
Calcitonin - MoA?
Enhances production of vitamin D producing enzymes.
Improves Ca2+ retention.
Increases bone density.
Calcitonin - uses?
Post-menopausal osteoporosis
Hormone Replacement Therapy - class?
Sex hormones
HRT - target?
Osteoblasts
HRT - MoA?
Stimulates osteoblastic activity -> more bone deposition.
Raloxifene - class?
Selective estrogen receptor modulator (SERM)
Raloxifene - target?
Oestrogen receptors
Raloxifene - MoA?
Reduces bone resorption
Increases bone density
Inhibits proliferation of preosteoclastic cells
Codeine - class?
Opioid receptor agonist
Codeine - target?
Mu opioid receptors
Codeine - MoA?
Decrease intracellular cAMP -> inhibition of nociceptive neurotransmitters.
Close N-type Ca2+ channels and open Ca2+ dependent K+ channels -> hyper-repolarisation.
Codeine - uses?
Analgesic
Cough suppressant
Pethidine - class
Opioid receptor agonist (kappa receptors)
Pethidine - MoA
Decrease intracellular cAMP -> inhibition of nociceptive NTs.
Hyper-repolarisation.
Pethidine - uses
Severe pain management
Lidocaine - class
Na+ channel blocker - local anaethetic
Lidocaine - MoA
Block voltage-gated Na+ channels so prevents initiation and transmission of APs.
Blocks the channels during phase 0 of cardiac AP.
Lidocaine - uses
Local anaethetic
Peripheral nerve block
Ventricular tachyarrthymias
Tramadol - class
Opioid receptor agonist (O-desmethyl M1)
Tramadol - MoA
Decrease intracellular cAMP -> inhibits nociceptive NTs.
Hyper-repolarisation
Tramadol - uses
Post-operative pain
Dobutamine - class
Beta adrenoceptor agonist (B1)
Dobutamine - MoA
Binds B1 in heart -> increases contractility, stroke volume and cardiac output.
Isoprenaline - class
Beta adrenoceptor agonist (B1 and B2)
Isoprenaline - MoA
Increases intracellular cAMP -> relaxation of bronchial smooth muscle (bronchodilator).
Isoprenaline - uses
Mild asthma
COPD
Heart block
Salbutamol - class
Beta adrenoceptor agonist (B2)
Salbutamol - MoA
Binds B2 in lungs -> smooth muscle relaxation (increased cAMP) and inhibits mediators of mast cells.
Bronchodilator
Salbutamol - uses
Bronchospasm relief e.g. asthma, COPD