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Theme One (Pharmacodynamics (Receptors (Enzyme linked receptors
Tyrosine…
Theme One
Pharmacodynamics
Receptors
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G protein coupled receptors
- amplifies signals via 2nd messengers
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Agonists
Full agonist: maximal effect
Partial agonist: no max effect
Inverse agonist: eliminates basal activity
Antagonists
Competitive antagonists:
- potency reduced (shifts drug to the right)
Irreversible antagonists:
- reduction in efficacy
Allosteric antagonists:
- reduction in max
Cholinergic receptors
- binds ACh
- when it binds, opens channels
Muscarinic
- G-protein coupled receptor
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Adrenergic Receptors
Alpha receptors
Alpha 1
- Stimulatory response
- Eyes
- Vasoconstriction
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1. Absorption
2. Distribution
3. Metabolism
4. Elimination
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Zero order kinetics:
Rate of elimination = constant
- E.g. aspirin
- saturation of enzymes
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Volume of distribution = (amount of drug in body)/
(conc. drug in blood plasma)
- Passive diffusion
- Facilitated diffusion
- Active transport
- Endocytosis
Factors:
- Blood flow (high in brain)
- Lipid solubility
- Capillary permeability
- Binding to plasma protein and tissues (Albumin)
- etc.
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Endogenous Mediators
5-HT
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Removal
- Serotonin uptake transporter (SERT)
- Active
E.g. Prozac (antidepressant)
- Increases 5-HT through selective
serotonin re-uptake inhibitors (SSRIs)
- Found in GI tract (increases gut motility)
- In the brain (sleep, appetite)
- Promotes vomiting
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Prostogalndins
- Inflammatory response
- Pain relief
- NSAIDS (e.g. ibuprofen) can cause gastric ulcers
- NSAIDs are non-inflammatory
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Autonomic Nervous System
SNS
- Short pre-ganglionic
- Long post ganglionic
- Dilation of pupils
- Inhibition of salivation
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PNS
- Releases ACh
- Long pre-ganglionic neurons
- Short post-ganglionic
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Disease
Dopamine
Parkinson's disease
- decreased stimulation of DA receptors
- Levodopa = increased DA synthesis
Schizophrenia
- Excessive DA activity in the brain
Pharmacokinetics
-The movement of the drug in the body
- What the body does to a drug
Pharmacodynamics
- Drug on the body
- onto the receptors
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