Pharmacology Exam 3

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Rx2013
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43763
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Pharmacology Exam 3
Updated:
2010-10-20 15:31:14
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Adrenergic Agonist Antagonists
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Adrenergic Agonist/Antagonists
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  1. Types of Adrenergic receptors
    • alpha 1
    • alpha 2
    • beta
  2. Targets of Norepinephrine
    • mono-amine oxidase
    • COMT
    • post synaptic membrane
  3. Alpha 1 Adrenergic receptor signaling
    • GPCR reactions
    • smooth muscle contraction
  4. Alpha 2 adrenergic signaling
    • GPCR
    • inhibition of transmitter release
    • smooth muscle contraction
  5. Beta adrenergic receptor signaling
    • heart muscle contration
    • smooth muscle relaxation
    • glycogenolysis
  6. Roles of alpha 1 receptors
    • most vascular smooth muscle
    • pupillary dialator muscle
    • pilomotor smooth muscle contraction
    • prostate contraction
    • heart contraction
  7. Role of alpha 2 receptors
    • platelet aggregation
    • inhibition of neurotransmitters at adr/chol nerve terminals
    • some vascular smooth muscle contraction
    • inhibition of lipolysis
    • inhibition of insulin release
  8. Role of B1 receptors
    • heart muscle contraction
    • renin secretion
    • ghrelin secretion
  9. Role of B2 receptor
    • smooth muscle relaxation
    • lipolysis
    • renin secretion
    • dialate arteries
    • relaxation of non-pregnant uterus
  10. B3 role
    lipolysis
  11. increase in number of carbons on the amino terminus
    increase B (especially B2) selectivity
  12. Addition of OH group on substrates
    • increases potency (faster metabolism by COMT)
    • decreases bioavailability
  13. Alpha 1 agonsits
    • phenylephrine
    • pupil dilation
    • increased BP
  14. Alpha 2 agonists
    • clonidine
    • treatment of hypertension
    • neuropathy
    • sleep disorders
  15. B agonsists
    • Dobutamine
    • - heart failure
    • Terbutaline
    • - delay premature labor
  16. What is the common funciton of all types of adrenergic receptors?
    Muscle contraction
  17. Phenylephrine
    potent alpha 1 agonist
  18. administration of phenylephrine
    • parenteral
    • oral
    • local
  19. uses of phenylephrine
    • dilate pupil
    • nasal decongestant
  20. Norepinephrine
    potent alpha and beta1 receptor agonist
  21. Administration of NE
    parenteral
  22. Uses of NE
    • Used as a pressor
    • (constricts arteriols to increase BP)
  23. Epinephrine
    potent alpha, B1 and B2 agonist
  24. administration of epinephrine
    parenteral
  25. uses of epinephrine
    • anaphylaxis
    • glaucoma
    • in combination with local anesthetics
  26. Isoproterenol
    • non-selective B agonist
    • bronchodilation
    • increased cardiac output
  27. administration of isoproterenol
    • oral
    • parenteral
    • local (inhaled)
  28. Uses of isoproterenol
    • asthma
    • COPD
    • cardiostimulant
  29. Which of the following adrenergic agonists are selective to alpha adrenergic receptors?
    phenylephrine
  30. competitive antagonist
    EC50 decreased but efficacy not changed
  31. Irreversible antagonist
    decrease in efficacy because receptor is destroyed
  32. Yohimbine
    • alpha 2 selective antagonist
    • aphrodisiac
  33. potential uses of yohimbine
    • male impotence
    • depression
    • obesity
    • non-insulin dependant DM
    • same side effects as antidepressants
  34. Yohimbine is metabolized by
    CYP3A4 and 2D6
  35. ADR of yohimbine
    • narrow therapeutic window
    • anxiety
    • high BP
    • rapid HR
    • hallucination
    • seizure
    • renal failure
  36. prazosin decreases the effects of epinephrine mediated action of adrenergic receptors by:
    decreasing potency of epinephrine
  37. Phenoxybenzamine (Dibenzyline)
    • Irreversible antagonist of a1 > a2
    • higher effect when sympathetic tone is high (upright)
    • metabolized by 3A4
  38. Uses of phenoxybenzamine
    • last resort for uncontrolled BP
    • pheochromocytoma
    • low bioavailability
  39. Adverse reactions with phenoxybenzamine
    • postural hypotention
    • reflex tachycardia
    • CNS issues
    • Ejaculation inhibition
    • Nasal congestion
    • Miosis (pupil constriction)
  40. Phentolamine (Regitine)
    • competitive blocker of a1 and a2
    • medium bioavailability
  41. uses for phentoalmine
    • extravasation of NE or DA
    • emergency hypertention (cocain or pheochromocytoma)
    • shock
    • pulmonary edema
    • ED
    • regional pain syndrome
  42. ADR of phentolamine
    • Cardiac and CNS related
    • tachycardia
    • arrhythmias
    • mycocardial ischemia
  43. Prazosin (minipres)
    • alpha 1 selective antagonist
    • low bioavailabilty due to p-gp efflux
    • CYP3A4
  44. uses of prazosin
    • hypertension
    • BPH
    • scorpion stings
    • severe nightmares in children
  45. ADR of prazosin
    • orthostatic hypotension
    • loss of consiusness (syncope)
    • nasal congestion
    • priapism
  46. Tamsulosin
    • alpha 1a selective blocker (prostate)
    • BPH treatment
    • ADR: retrograde ejaculation
    • high bioavailability
    • CYP3A4 and 2D6
  47. What is the last resort for uncontrolled BP?
    A. Prazosin
    B. tamsulosin
    C. phentolamine
    D. Phenoxybenzamine
    D. Phenoxybenzamine
    (this multiple choice question has been scrambled)
  48. uses of beta blockers in heart issues
    • coronary artery disease
    • hypertension/arrhythmia
    • CHF
    • cardiomyopathy
  49. uses of beta blockers other than the heart
    • pheochromocytoma
    • hyperthyroidism
    • migraine
    • tremor
    • anxiety
    • glaucoma
  50. properties of beta blockers
    • L-isomer is more potent
    • B1 (cardiovascular) selectivity
    • partial agonist activity
  51. Pharmacokinetics of B-blockers
    • lipid soluble (high bioavailablity)
    • metabolized in liver
    • enter the CNS
    • shorter elimination half lives (fast abs.)
  52. Adverse reactions to beta blockers
    • cardiac
    • decresed vascular perfusion
    • bronchoconstriction
    • diabetes mellitus
    • depression, nightmares
    • withdrawl
  53. Optimal clearance time to decrease ADR of beta blockers
    3-4 hours
  54. Pindolol
    easily absorbed but not easily metabolized
  55. B-Blockers that have B1=B2 selectivity
    • propranolol
    • pindolol
  56. B-Blockers with B1>B2 selectivity
    • metoprolol
    • esmolol
  57. Propranolol uses
    • cardiovascular
    • migrane
    • post traumatic stress
    • glaucoma
  58. Inhibitors of CYP3A4 and CYP2D6
    • clonidine
    • quinidine
    • cimetidine
  59. Induceers of CYP3A4 and 2D6
    • Phenobarbital
    • Rifampicin
  60. Propranolol given with inhibior would:
    increase efficacy
  61. Propranolol given with an inducer would:
    increase efficacy
  62. Metoprolol
    many more side effects
  63. serious side effects of metoprolol
    • very slow HR
    • cyanosis/tingling of extremities
    • hair loss
    • sexual dysfunction
    • mood change
    • trouble breathing/cough

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