Mechanism of Action.ppt - PHARMACODYNAMICS What the Drug does to the Body DRUG ACTIONS OR EFFECTS MECHANISM OF ACTION Kibuule's Pharmacology 2006 1

Mechanism of Action.ppt - PHARMACODYNAMICS What the Drug...

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Kibuule's Pharmacology 2006 1 PHARMACODYNAMICS What the Drug does to the Body DRUG ACTIONS OR EFFECTS & MECHANISM OF ACTION
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Kibuule's Pharmacology 2006 2 Mechanisms of drug Action Receptor mediated Lock & key mechanism On cell membrane, Cell cytoplasm, nucleic receptors Non receptor Mediated Action on enzymes (biological catalysts) Changing physical properties: Mannitol - Osmolarity Changing cell membrane permeability Combining with other chemicals Antimetabolites
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Kibuule's Pharmacology 2006 3 Drug Receptors Mechanisms Definition of a receptor A macromolecular component of a cell with which a drug interacts to produce a response Usually a protein Binds with endogenous substances like Hormones, neurotransmitters ( Ligands) Drugs are also Ligands to receptors
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Kibuule's Pharmacology 2006 4 Drug Receptors Mechanisms Most drugs act (bind) on receptors In or on cells ( membrane, cytoplasm, Nuclear) Form tight bonds with the ligand Exacting requirements (size, shape, stereo specificity ) Can be agonists (salbutamol), or antagonists (propranolol) Receptors have signal transduction methods
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Kibuule's Pharmacology 2006 5 Types of Protein receptors Regulatory Change the activity of cellular enzymes Enzymes May be inhibited or activated Transport e.g. Na + /K + ATP’ase Structural These form cell parts
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Kibuule's Pharmacology 2006 6 Receptors Sites Cell wall receptors in microorganisms Cell membrane receptors Cytoplasmic components: Proteins (in patient, or microbes) Genome (Cyclophosphamide) Microtubules (vincristine) Enzymes Ribibosomes
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Kibuule's Pharmacology 2006 7 Signal Transduction Enzyme Linked ( Multiple actions) Ion Channel Linked ( speedy) G protein linked ( Amplifier) Nuclear Gene linked ( Long standing)
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Kibuule's Pharmacology 2006 8 Signal transduction
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Kibuule's Pharmacology 2006 9 G protein-linked receptors Structure: Single polypeptide chain threaded back and forth resulting in 7 transmembrane å helices There’s a G protein attached to the cytoplasmic side of the membrane (functions as a switch)
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Kibuule's Pharmacology 2006 10 G protein-linked receptors
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Kibuule's Pharmacology 2006 12
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Kibuule's Pharmacology 2006 13 Enzyme linked Receptors Tyrosine-kinase receptors Structure: Receptors exist as individual polypeptides Each has an extracellular signal-binding site An intracellular tail with a number of tyrosines and a single å helix spanning the membrane
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Kibuule's Pharmacology 2006 14
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Kibuule's Pharmacology 2006 16 Ion channel linked Receptors Structure: Protein pores in the plasma membrane
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Kibuule's Pharmacology 2006 18 Intracellular Receptors
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