Pharm- Drug Effectors and Intracellular Messengers.txt

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Mawad
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300805
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Pharm- Drug Effectors and Intracellular Messengers.txt
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2015-04-14 16:48:52
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  1. Vegetative nervous system; rest and digest.
    parasympathetic nervous system
  2. Fight or flight.
    sympathetic nervous system
  3. The primary site for studying many drug mechanisms.
    peripheral nervous system, particularly the autonomic nervous system
  4. What part of the nervous system is the major control of heart rate, GI, and eye.
    parasympathetic nervous system
  5. What are the 5 steps of neurotransmission for cholinergic and adrenergic nerves?
    • 1. synthesis of neurotransmitter
    • 2. storage of neurotransmitter
    • 3. release of neurotransmitter
    • 4. activation of the postsynaptic receptor
    • 5. removal of neurotrasmitter
  6. In the cholinergic synapse, ____________ is synthesized by choline acetyl transferase; it is released and combines with __________ receptors in ___(2)___ or ____________ receptors in ___(2)____.
    acetylcholine; nicotinic; ganglia or neuromuscular junctions; muscarinic; neuroeffector junctions such as the SA node of the heart
  7. Removal of acetylcholine at a cholinergic synapse is by _________________.
    acetylcholinesterase
  8. In an adrenergic synapse, ______________ is synthesized via...
    norepinephrine (NE); tyrosine --> dopa --> dopamine --> NE
  9. What is the rate-limiting step of the synthesis of norepinephrine?
    tyrosine --> dopa by the enzyme tyrosine hydroxylase
  10. In the adrenal medulla, the enzyme __________ converts NE to epinephrine.
    phenylethanolamine-N-methyl transferase (PMNT)
  11. When sympathetic nerves are stimulated, released ________ combines postsynaptically with ________ receptors in blood vessels of the viscera and skin, ________ receptors of the heart, or __________ in certain tissues.
    NE; alpha1; beta1; beta2
  12. Alpha2 receptors on on the presynaptic terminal provide ___________ of __________, and beta2 receptors facilitate _______________ in response to ____________.
    feedback regulation; NE release; NE release; epinephrine
  13. In adrenergic synapses, removal of NE is primarily through _________, which is...
    Uptake I; re-uptake into the presynaptic terminal, where it is stored in vesicles or exposed to monamine oxidase (MAO) and inactivated.
  14. With adrenergic synapses, an alternate method of removal of NE is by NE being taken up into ______________, called ________, where it is inactivated by the enzyme _________________.
    extraneuronal sites; Uptake II; catechol-O-methyltransferase (COMT)
  15. What are the components of the peripheral nervous system?
    somatic nervous system, autonomic nervous system
  16. The somatic nervous system is comprised on...
    motor and sensory neurons communicating with muscle, skin, and sensory organs
  17. The autonomic nervous system is comprised of...
    parasympathetic and sympathetic nervous systems communicating with organs and glands
  18. The autonomic nervous system is ____________.
    involuntary
  19. Cholinergic drugs mimic ____________ at ____________ and ____________ sites; cholinergic receptor activating drugs are ________________; cholinesterase inhibiting drugs are ________________; cholinergic receptor blocking drugs are ____________.
    acetylcholine; nicotinic; muscarinic; direct-acting agonists; indirect-acting agonists; antagonists
  20. Parasympathomimetic drugs are __________ at ____________; parasympatholytic drugs are ___________ at _____________, which are _______________.
    direct or indirect agonists; muscarinic sites; antagonists; muscarinic; antimuscarinic drugs
  21. Sympathomimetic drugs are _____________ and _____________ sites; they can be... (2)
    agonists; α and β; direct and indirect adrenergic agonists.
  22. Sympatholytic drugs are ____________ at ____________ sites; they are _______________.
    antagonists; α and β; anti-adrenergic drugs
  23. Most drugs that act at cholinergic synapses produce their effects ____________; adrenergic drugs act ______________.
    postsynaptically; pre- and postsynaptically
  24. Cardiovascular function is primarily by __________ control of the _________ and _________; the __________ is dominant in controlling heart rate; the ________ controls vasculature.
    autonomic; heart; blood vessels; parasympathetic nervous system; sympathetic nervous system
  25. Variations in blood pressure (BP) are directed by the ___________ and relayed to the __________.
    carotid sinus; medulla;
  26. Increases in BP result in reflex slowing of the heart via ______ release of ________ at _________ receptors in the _________ of the heart; also, the ______________ decreases outflow, causing diminished release of ________ at _______ receptors, which lowers BP.
    vagal; Ach; muscarinic; SA node; vasomotor center; NE; alpha1
  27. Decreases in BP result in speeding of HR due to diminished release of ________; also, through the release of _______ at _______ receptors, which further increases the firing at the __________. Vasomotor outflow increases to cause release of _______ at _______ receptors to bring BP back to normal.
    Ach; NE; beta1; SA node; NE; alpha1
  28. When the activity of the cardiovascular system increases due to fight or flight, discharge at ___________ neurons increases, as well as the release of __________ in the medulla.
    sympathetic; eppinephrine
  29. Circulating epinephrine acts to... (3)
    speed the heart, constrict blood vessels in the viscera and skin through alpha1 receptors, and dilate vessels to skeletal muscles through beta2 receptors
  30. With increased circulating epinephrine due to fight or flight, blood flow is redirected to __________.
    skeletal muscle
  31. What are the differences between epinephrine and norepinephrine?
    epinephrine is localized to the adrenal medulla, NE is localized to sympathetic neuroeffector junctions; epinephrine is an agonist at alpha and beta1 and beta2 receptors, NE acts at alpha and beta1 receptors only
  32. Isoproterenol acts only at _______ receptors.
    beta
  33. Phenylephrine acts only at _________ receptors.
    alpha
  34. Describe the effectiveness of epinephrine, NE, isoproterenol, and phenylephrine at alpha receptors.
    phenylephrine > NE > epinephrine > isoproterenol
  35. Describe the effectiveness of epinephrine, NE, isoproterenol, and phenylephrine at beta receptors.
    isoproterenol > epinephrine > NE > phenylephrine
  36. Phentolamine is an ________________.
    alpha receptor antagonist
  37. Receptors present in vascular smooth muscle that cause contraction and increase in BP.
    alpha1 receptors
  38. 3 agonists of alpha1 receptors.
    epinephrine, norepinephrine, phenylephrine
  39. 1 antagonist of alpha1 receptors.
    phentolmine
  40. Receptors that provide pre-synaptic negative feedback of norepinephrine release.
    alpha 2 receptors
  41. 1 agonist of alpha 2 receptors.
    xylazine
  42. 1 antagonist of alpha2 receptors.
    yohimbine
  43. Receptors present in the heart that increase the rate and force of contraction.
    beta1 receptors
  44. 3 agonists of beta1 receptors.
    epinephrine, norepinephrine, isoprentol
  45. 1 antagonist of beta1 receptors.
    propanolol
  46. Receptors present in vascular smooth muscles that cause relaxation of vessels and skeletal pre-synaptic negative feedback of norepinephrine release; decrease BP.
    beta2 receptors
  47. 2 agonists of beta2 receptors.
    epinephrine and isoproternol
  48. 1 antagonist of beta2 receptors.
    propanolol
  49. Anticholinesterase is an indirect agonist because...
    its action depends on the release of Ach.
  50. Muscarinic receptors are ____________; nictoinic receptors are associated with __________.
    cardioinhibitory; ganglia
  51. The control of pupillary diameter in dominated by the __________ through the _______.
    parasympathetic NS; CN III
  52. The pupillary light reflex responds to increases in light by...
    actively constricting the constrictor pupillae (circular) muscle
  53. Decreases in light intensity cause...
    the dominant parasympathetic fibers to reduce their rate of firing and allow passive relaxation to dilate the pupil.
  54. ______________ controls the contractility of the dilator pupillae (radial) muscle; pair or fear trigger a ____________ response and cause _________ of the pupil.
    Sympathetic innervation; sympathetic; active dilation
  55. The sympathetic innervation to the pupil is ____________.
    norepinephrine alpha
  56. Contraction of the sphincter m. causes ____________; contraction of the radial muscle causes ___________.
    miosis; mydriasis
  57. Physostigmine is a reversible blocker of ______________; it is a(n) _____________ on the __________ muscle, which is __________ in nature.
    acetylcholinesterase; indirect agonist; sphincter; parasympathetic
  58. Amphetamine causes the displacement and release of ________ from the __________; it is a(n) _____________ of the ________ muscle, which is __________ in nature.
    NE; pre-synaptic terminal; indirect agonist; radial; sympathetic
  59. Cocaine blocks the __________ of __________; it is a(n) _____________ of the __________ muscle, which is ___________ in nature.
    re-uptake; NE; indirect agonist; radial; sympathetic
  60. With Horner's syndrome, the use of _____________ in the affected eye can help to...
    sympathomimetic drugs; localize the lesion to pre-ganglionic or post-ganglionic nerve
  61. [Eye] If the lesion is post-ganglionic to the sympathetic nerve, indirect acting drugs will not produce ___________ because they are dependent upon ______________.
    mydriasis; NE in an intact synaptic terminal
  62. [Eye] If the lesion is post-ganglionic in the sympathetic nerve, direct-acting epinephrine will produce __________ because when degeneration of this fiber occurs, the _______________ for the ______________ is lost.
    mydriasis; pre-synaptic re-uptake mechanism; removal of NE and ephinephrine
  63. [Eye] If the lesion is pre-ganglionic to the sympathetic nerve, cocaine has _______ effect because...
    no; no impulses reach the eye to release NE.
  64. A drug which elicits no response by itself but enhances the response of another drug.
    potentiation
  65. The action of cocaine is ____________ because it has no ____________ qualities, and it ___________ the action of _________.
    potentiation; alpha agonistic; potentiates; released NE
  66. The response elicited by a combination of two drugs is equal to the combined responses of the individual drugs.
    Addition
  67. The response elicited by a combination of two is greater than the combined response of the individual drugs.
    synergism
  68. A drug which elicits no response by itself but inhibits the response of another drug.
    antagonistm
  69. [Eye] Pre-ganglionic AND post-ganglionic lesion of parasympathetic nerve leads to loss of impulses to ________ and up-regulation of ____________, ultimately ____________; there is no effect from __(2)__; there is loss of _______________.
    sphincter muscle; muscarinic receptor; supersensitivity; indirect agonists, antagonists; physiologic antagonism to radial muscle
  70. [Eye] Pre-synaptic lesion of sympathetic nerve leads to loss of impulses to ___________ and up-regulation of ___________, ultimately ___________; there is no effect from ___(2)___; there is loss of _______________.
    radial muscle; adrenergic receptor; supersensitivity; cocaine, antagonists; physiologic antagonist to sphincter muscle.
  71. [Eye] Post-synaptic lesion of sympathetic nerve leads to loss of impulses to ___________ and up-regulation of ___________, ultimately ___________; there is also degeneration of the ___________ at the __________ and loss of __________; there is no effect from ___(3)___; there is loss of _______________.
    radial muscle; adrenergic receptors; supersensitivity; pre-synaptic terminal; radial muscle; uptake; cocaine, amphetamine, antagonists; physiologic antagonist to sphincter muscle
  72. Acetylcholine is a(n) ___________ to the __________.
    direct agonist; sphincter muscle
  73. Norepinephrine is a(n) _____________ to the ____________.
    direct agonist; radial muscle
  74. Atropine is a(n) __________ to the ___________.
    antagonist; sphincter muscle
  75. Phentolamine is a(n) _____________ to the _________.
    antagonist; radial muscle

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