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60 Cards in this Set
- Front
- Back
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Alpha-1
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1. NE
2. q 3. Inc IP3, Inc Ca,Inc DAG Inc PKC 4. Inc vascular smooth muscle contraction |
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M3
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1. ACh
2. q 3. Inc IP3, Inc Ca,Inc DAG Inc PKC 4. Inc exocrine gland secreations and smooth muscle motility |
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H2
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1. His
2. s 3. Inc cAMP, Inc PKA 4. Inc gastric acid secretion |
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Beta 2
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1. NE
2. s 3. Inc cAMP, Inc PKA 4. Vasodilation, bronchodilation Inc glucagon release |
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Alpha 2
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1. NE
2. i 3. Dec cAMP, Dec PKA 4. dec sympathetic outflow, dec insulin release |
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M2
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1. ACh
2. i 3. Dec cAMP, Dec PKA 4. dec heart rate |
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Beta 1
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1. NE
2. s 3. Inc cAMP, Inc PKA 4. Inc HR, contractility, renin release, lipolysis, aqueous humor formation |
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M1
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1. ACh
2. q 3. Inc IP3, Inc Ca,Inc DAG Inc PKC 4. CNS stimulation |
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What do Alpha 1 agonists do to the following
Vascular smooth muscle |
Vasoconstrict
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Pupils
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Mydriasis (dilation)
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Genitourinary smooth muscle
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Inc sphincter tone
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Liver
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Glycogenolysis, gluconeogesesis
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What do B1 agonist do to the following
Heart rate |
Inc
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Contractility
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Inc
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Kidney
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Inc renin
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Fat
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Lipolysis
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What do B2 agonists do to the following
Bronchial smooth muscle |
bronchodilation
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Vascular smooth muscle
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vasodilation
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uterine smooth muscle
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relaxation
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liver
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glycogenelisis and gluconeogenesis
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Are there any drugs that are seletive to a given muscarinic receptor
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no, but potency at each can vary
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What do cholinergic agonists do at the following places and via what receptor
CNS |
stimulation- M1
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Heart Rate
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Decrease M2
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Eye
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pupillary constriction (miosis), ciliary contraction (glaucoma treatment) M3
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GI, GU tract
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Inc motility, secretions, bladder constriction, sphincter relaxation M3
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Lung
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Bronchoconstriction and Inc secreations- M3
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Where are nicotinic receptors located
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autonomic ganglia of sympathetic and parasympathtic systems, as well as at the adrenal medulla
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What is the neurotrasmitter
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ACh
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What drug blocs nicotinic receptor
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Hexamethonium
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What does botulinum toxin do
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Block ACh relases for pre-synaptic neuron
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What do AChesterase do
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breaks ACh into choline and acetate so that choline can be reuptaken by presynaptic neuron
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What does cocaine do
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Blocks reuptake of NE into presynaptic neuron
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amount of drug in body/_______ = Vd
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plasma drug concentration (note: Vd is Volume of Distribution)
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rate of elimination of drug/[plasma drug] = ?
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CL (Clearance)
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(.7)(Vd)/CL = ?
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T 1/2
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A drug infused at a constant rate reaches about 94% of steady state after _______ t 1/2s.
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4
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A loading dose is calculated using this formula.
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(Cp)(Vd)/F (note: Cp = target plasma concentration, and F = bioavailability)
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A maintenance dose is calculated using this formula.
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(Cp)(CL)/F
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Rate of elimination is proportional to _______ ______ in 1st order elimination.
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drug concentration
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In the case of EtOH, which is elimated by _____ order elimination, a constant amount of drug is eliminated per unit time.
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zero
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Phase ____ (I or II) reactions yield slightly polar metabolites that are often _____ (active or inactive)
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I, active
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Phase ____ (I or II) reactions yield very polar metabolites that are often _____ (active or inactive) and are excreted by the _______.
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II, inactive, kidney
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Phase II reactions are often of this type.
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conjugation
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Cytochrome P-450 is involved in _____ phase (I or II) reactions.
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I
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A patent lasts for _____ years after filing for application.
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20
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How many phases are there in drug development?
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4
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Drugs are first tested in patients in phase _____ of clinical testing, pharmacokinetic safety is determined in phase ______ of clinical testing, double blind tests are done in phase ____ and post-market surveillance is done in phase _____.
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2,1,3,4
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In a dose response curve, a competitive antagonist shifts the curve _____, while a non-competitive antagonist shifts the curve ______.
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right, down
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What pharmacologic relationship would determine the existence of spare receptors?
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EC50 < Kd
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What does it mean if EC50 and Kd are equal?
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The system does not have spare receptors
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A partial agonist acts on the same receptor system as a full agonist? T/F
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TRUE
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What's the main difference between a partial agonist and a full agonist?
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A partial agonist has a lower maximal efficacy.
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Is a partial agonist less potent than a full agonist?
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Not necessarily. It can be less, more or equally potent as a full agonist.
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Parasympathetic preganglionic neurons release the neurotransmitter -------- which act on -------- receptors.
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Ach, nicotinic.
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Sympathetic preganglionic neurons to sweat glands release the neurotransmitter ------- which act on ------- receptors.
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Ach, nicotinic.
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Ach is synthesized from acetyl-CoA and choline by the enzyme ---------.
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Choline acetyltransferase.
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In the noradrenergic nerve terminal, tyrosine is hydroxylated to -------, which is decarboxylated to --------, which is finally hydroxylated to NE.
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DOPA, dopamine.
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The action of NE and DA is terminated by --------- and ----------.
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Reuptake, diffusion (different than for Ach).
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The drugs --------- and ---------- inhibit the reuptake of NE.
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Cocaine, TCA.
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Ach inhibits the release of NE from the noradrenergic nerve terminal by binding to --------- receptors.
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M1.
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