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49 Cards in this Set
- Front
- Back
Dose-response curve
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the magnitude of an effect of a drug as a function of how much administered. higher the dose, the greater the effect, UNTILL the point of maximum effect
morphine ex- has two effects- stops pain and depresses. a low does relieves pain, a high dose causes depressant and the dif between these is the 'margin of safety' |
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why do drugs vary in efficacy?
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1) different sites of action (direct to cns is best)
2) They have different affinities for the molecules to which they attach. a drug with a high affinity will produce an effect on a very low dose. A drug may have a high affinity at one site of action and low at another. |
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sensitization vs tolerance
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1) tolerance- drugs effects diminish because of repeated use, it is the bodes attempt to compensate for drugs effect
2) Sensitization- drug becomes more and more effective through repeated use. is barbiturates have sedative and depressive effects and the sedative effect shows tolerance while depressive does not. |
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direct vs indirect agonist/antagonist
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direct agonist/ antagonist= competitive binding - mimics neurotrans, attaches to binding site of neurotrans causing ion channels to open (agonist) or close (antagonist)
indirect= incompetitive binding - attaches to site other than that of neurotrans. and cause the ion channels to open/close |
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cocaine, meth
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catecholamine agonist that is highly addictive and increases dopamine and norepinephrine activity by blocking reuptake
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benzodiazepines
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acts as GABA agonist BUT doesn't mimic the action of GABA (don't bind to same site), reduces anxiety, induces sleep
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botox
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nicotinic antagonist which blocks acetylcholoine release
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curare
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cholinergic receptor, paralyzes because blocks muscarinic receptors of ACh
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routes of administration (10)
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intraperitoneal (stomach), IV (vein), intramuscular (slow), oral, sublingual, interectal, inhalation, topical, intracerebral (brain), intracerebroventivular (into cerebral ventricle)
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this type of drug easily passes through blood brain barrier:
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lipid soluble
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therapeutic index
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the margin of safety. for example 5.0 means the toxic dose is five times higher than that go the desired effects
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pharmacokinetics
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process by which drugs are absorbed and distributed in body
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Botulinium toxin (AChl)
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produced by a bacteria that can grow in improperly canned food- inhibits ACh!
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Black widow spider venom
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stimulates ACh release
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neostigmine (ACh)
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drug which inhibits Acetylcholinesterase (thus gives more ACh) often for muscular dystrophy patients
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Atrophine (ACh)
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blocks muscarinic receptors of ACh
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the Monoamines, which are catecholaminases?
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Dopamine, Epinephrin and norepinephrine (cate)
serotonin, histamine |
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What are the three Dopaminergic areas?
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NIGROSTRATAL SYSTEM (in substantia nigra and project to Striatum), MESOLIMBIC SYSTEM (in tegmentum and go to limbic system), MESOCORTIAL SYSTEM ( also in tegmentum but project to prefrontal cortex)
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Dopamine is made from___, serotonin from___
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tyrosine; tryptophan hydroxylase
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reserpine (monoamines)
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drug that interferes with storage of monamines in vesicles
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types of dopamine receptors, which are most common?
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most common D1, D2 ; D3 and D4 are less common
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Apomorphine (dopamine)
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blocks dopamine autoreceptors at low doses and at higher doses blocks postsynaptic, too
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methlphenidate (dopamine)
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inhibits reuptake of dopamine
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Two types of ACh receptors
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A) Metatrophic (Muscarinic)
B) Ionotrophic (Nicotinic) (on muscle fibres) |
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MOA; Deprenly
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destroy monoamines; blocks MOAs
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Chloropromazine (dopamine)
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reduces schizophrenia by blocking dopamine D2 receptors
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Fusaric Acid (nor.)
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inhibits production of norepin.
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Mocluobemide
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blocks MOA-A (destroys specifically norepinephrine)
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Axonal varicosity
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enlarged part of axon that contains vesticles and releases a neurotrans.
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idoazoxan ( nor.)
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facilitates release of norepinephrine
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serotonin also called...
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5- HT
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PCPA blocks...
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tryptophan hydroxylase thus is an serotonergenic antagonist
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Fluoxetine (prozac) and Fenflramine
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SSRI to treat depression
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MDMA and LSD are...
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seretonergenic agonists
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What are the 4 glutamate receptors?
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NMDAm(controls na and ca channel), AMPA (controls na) ,= most common, ionotrophoc receptor
Kainate= ionotropic receptor metabotropic glutamate = metabotropic (clearly) |
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PCP binds with...
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the PCP binding site of the NMDA receptor
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AP5 blocks...
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the glutamate binding site on NMDA
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GABA is made from
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GAD enzyme
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allyglycine (GABA)
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inhibits GAD and synthesis of GABA
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What are the 2 receptors of GABA?
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GAGAa and GABAb
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Benzodiazepines like Valium bind with...
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GABAa receptor and incude sleep or reduce seizures
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Anxiolytic means
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anxiety-reducing effect
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see chart ' neurotransmitters and drugs '
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see notes
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what are the types of norepinephrine receptors?
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alpha 1, alpha 2
beta 1, beta 2 adrenergenic receptors |
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histamine receptors, what is histamine involved in?
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H1, H2, H3- sleep, itching
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what are the serotonin receptors? (9)
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5-HT 1A, 1B, 1D, 1E, 1F
5-HT 2A, 2B, 2C 5- HT 3 |
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Autoreceptors vs heteroreceptors?
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auto- preynaptic, sensitive to only the neruotrans from its neuron
hetero- presynaptic also but sensitive only to neurotrans other than its own |
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Why does caffeine have the effect that it does?
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Adenosine is an inhibitor nerurotransmitter in CNS and caffeine acts as an antagonist for it, causing stimulation
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Why do people form dependence on nicotine?
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imitates ACh and binds to its nicotinic receptor. Some of these are located in the tegmentum where dopaminergic areas are. So dopamine is released when these areas are stimulated and = rush. This shows tolerance and the rush reduces with chronic smoking. In chronic smokers, the nicotine causes a desensitization of the nicotinic receptor chronically. When they stop smoking overnight for example, this regains sensitivity and much ACh is there, causing agitation and discomfort.
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