Principles of Pharmacodynamics

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Anonymous
ID:
108126
Filename:
Principles of Pharmacodynamics
Updated:
2011-10-11 17:05:11
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Pharmacodynamics
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Description:
How drugs work
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  1. Sequence of effects following drug administration
    • 1. Medicines administered
    • 2. Drug binding to a target site
    • 3. Changes in ion permeability, enzyme activities, the levels if biochemical mediators or changes in the receptor proteins or other proteins that serve as mediators of cellular processes
    • 4. Change in physiological function of target site tissues
  2. Nerve membrane sodium ion (Na+) channel
    • Nerve membrane sodium ion (Na+) channel that controls Na+ influx into cell
    • e.g. nicotinic AcCh receptor in CNS activated by nicotine, changes Na+ ion movement in and out of nerve cells
  3. Nerve membrane chloride ion Cl- channel
    • Nerve membrane chloride ion Cl- channel
    • Receptor for neurotransmitter GABA is coupled to a Cl- channel, this receptor is the target site for alcohol and diazepam (anti-anxiety drug, VALIUMR)
  4. Diazepam
    • Anti-anxiety drug
    • e.g. VALIUMR
  5. Blood vessel membrane calcium ion Ca+ channel
    • Blood vessel membrane calcium ion Ca+ channel
    • Verapamil (ISOPTINR) is a calcium channel blocker (antagonist) used for angina and hypertension.
    • Similar receptors are found on a variety of smooth muscle membranes
  6. Verapamil
    • Calcium channel blocker
    • e.g. ISOPTINR
  7. Membrane ATP-dependent ion transport systems
    • Membrane ATP-dependent ion transport systems
    • Digoxin (LANOXINR) binds to Na/K ATPase which causes Na+ transport out of cells to slow and cardiac function to improve
  8. Digoxin
    • From Digitalis flower
    • Often used after a heart attack to increase contractile activity of the heart
    • Overdose can cause overcontraction which can be fatal
    • Binds to Na/K ATPase causing slower release of Na+ from cell
    • e.g. LANOXINR
  9. Nerve synaptic membrane neurotransmitter transport proteins
    • Nerve synaptic membrane neurotransmitter transport proteins
    • Fluoxetine blocks serotonin reuptake (e.g. PROZACR)
    • Trimipramine blocks reuptake of neurotransmitter norepinephrine
  10. Fluoxetine
    • Example of an SSRI
    • Blocks serotonin reuptake through a nerve synaptic membrane neurotransmitter transport protein
    • e.g. PROZACR
  11. Trimipramine
    • Example of a TCAD
    • Blocks reuptake of norepinephrine through a nerve synaptic membrane neurotransmitter transport protein
  12. Epithelial membrane transport for metabolites
    Probenecid blocks uric acid transport by inhibiting a uric acid transporting protein in the kidneys so stops uric acid retention by body (i.e. gout)
  13. Probenecid
    Affects epithelial membrane transport for metabolites, i.e. inhibits a uric acid transporting protein in the kidneys so stops uric acid retention by body (i.e. gout)
  14. Special membrane-associated transduction (G) proteins and ion channel activity
    • AcCh receptor-active drugs such as tubocurarine (curare) or atropine which are both muscle relaxants
    • Membrane receptors for insulin (drugs can increase glucose uptake into cells and tissues)
  15. Enzyme activity as part of a transduction mechanism
    • Phenylephrine (NEO-SYNEPHRINE) binds to alpha1 receptors normally activated by epinephrine (agonist). The drug binding is coupled to the enzyme adenylate cyclase and indirectly controls Ca+ ion influx into smooth muscle cells (can contract muscles in iris causing dilation of the pupil)
    • Salbutamol (VENTOLIN) binds to the beta2 receptors (agonist), so acts selectively on bronchial smooth muscles (dilates bronchioles for pxs with asthma)
  16. Phenylephrine
    • Binds to alpha1 receptors (agonist) normally activated by epinephrine. The drug binding is coupled to the enzyme adenylate cyclase and indirectly controls Ca+ ion influx into smooth muscle cells (can contract muscles in iris causing dilation of the pupil)
    • e.g. NEO-SYNEPHRINE
  17. Salbutamol
    • Binds to the beta2 receptors (agonist), so acts selectively on bronchial smooth muscles (dilates bronchioles for pxs with asthma)
    • e.g. VENTOLIN
  18. Gene activation (or supression) to change RNA dependent synthesis of an enzyme
    Corticosteroids such as dexamethasone (MAXITROL) increase RNA polymerase activity to indirectly elevate levels of lipocortins (which then inhibit an enzyme called phospholipase A2)
  19. Dexamethasone
    • Example of a corticosteroid
    • Increases polymerase activity to indirectly elevate levels of lipocortins (which then inhibit an enzyme called phospholipase A2)
    • e.g. MAXITROL
  20. Tubocurarine
    • AKA curare
    • Coupled to membrane-associated transduction (G) proteins and ion channel activity
    • AcCh receptor active drug
    • Used as a muscle relaxant
  21. Atropine
    • Coupled to membrane-associated transduction (G) proteins and ion channel activityAcCh receptor active drug
    • Used as a muscle relaxant

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