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
Salmeterol - class
Beta adrenoceptor agonist (B2)
Salmeterol - MoA
Lung smooth muscle relaxation -> bronchodilator.
Longer lasting than salbutamol.
Noradrenaline - class
Alpha adrenoceptor agonist
Noradrenaline - MoA
Peripheral vasoconstriction and inotropic stimulator
Noradrenaline - uses
Vasodilatory shock treatment
Phenoxybenzamine - class
Alpha adrenoceptor antagonist
Phenoxybenzamine - MoA
Blocks alpha receptors -> muscle relaxation and vasodilation.
Lowers BP
Phenoxybenzamine - uses
Pheochromocytoma
Hypertension
Prazosin - class
Alpha adrenoceptor antagonist (A1)
Prazosin - MoA
Inhibits vasoconstrictor effects -> lowers BP.
Prazosin - uses
Hypertension
Severe congestive heart failure
Muscarine - class
Muscarinic cholinergic receptor agonist
Muscarinic - MoA
Mimics ACh
Pilocarpine - class
Muscarinic cholinergic receptor agonist
Pilocarpine - MoA
Contraction of ciliary muscles
Pilocarpine - uses
Glaucoma
Atracurium - class
Nicotinic cholinergic receptor agonist
Atracurium - MoA
Competitively binds nicotinic receptors on motor end plates -> muscle relaxant.
Botulinum A toxin - class
ACh release inhibitor
Botulinum A toxin - MoA
Inhibits release of ACh from presynaptic terminal.
Causes parasympathetic paralysis.
Botulinum A toxin - uses
Cervical dystonia
Prevent hypersalivation and spasticity
Cocaine - class
Na+ channel blocker / NA reuptake inhibitor
Cocaine - MoA
Inhibits excitation of nerve endings and blocks conduction in peripheral nerves. Inactivates Na+ channels -> local anaesthesia. Vasoconstrictor.
Cocaine - uses
Local anaesthesia to nasal, oral and laryngeal cavities.
Dexamphetamine - class
NA releaser
Dexamphetamine - MoA
Stimulates release of NA
Dexamphetamine - uses
ADHD
Narcolepsy
Dopamine - class
Neurotransmitter
Dopamine - MoA
Produces coordinated movement.
Positive chronotropic and inotropic effects.
Dopamine - uses
Parkinson’s
Fluoxetine - class
SSRI
Fluoxetine - MoA
Blocks uptake transporters of serotonin so more available.
Fluoxetine - uses
Major depressive disorder
Anxiety
Hemicholinium - class
Choline reuptake inhibitor
Hemicholinium - MoA
Blocks transport of choline back into nerve terminal -> no ACh made.
Imipramine - class
Tricyclic antidepressant
Imipramine - MoA
Prevents reuptake of serotonin and NA
Imipramine - uses
Depression
ADHD
L-DOPA - class
Dopamine precursor
L-DOPA - MoA
Increases dopamine in substantia nigra
L-DOPA - uses
Parkinson’s
Nicotine - class
Nicotinic cholinergic receptor agonist
Nicotine - MoA
Stimulant of limbic system, releases dopamine and indirect release of adrenaline.
Raises BP and HR.
Nicotine - uses
Aids smoking cessation
Phenelzine - class
MAO inhibitor
Phenelzine - MoA
Irreversible non-selective inhibitor of MAO
Phenelzine - uses
Depression
Pralidoxime - class
Cholinesterase reactivator
Pralidoxime - MoA
Cleaves phosphate-ester bond between AChE and toxin.
Pralidoxime - uses
Sarin poisoning
Sarin - class
Anticholinesterase
Sarin - MoA
Irreversibly binds to AChE on active site.
Sarin - uses
Chemical weapon
Tropicamide - class
Muscarinic cholinergic receptor antagonist
Tropicamide - MoA
Blocks muscarinic receptors (M4) in eye -> pupil dilation and relaxation of lens.
Tropicamide - uses
Diagnostic optician procedures