Pharm L19, T2 Adrenergic agents.txt

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kepling
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104897
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Pharm L19, T2 Adrenergic agents.txt
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2011-10-11 21:57:22
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Pharm L19 T2 Adrenergic agents
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Pharm L19, T2 Adrenergic agents
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  1. NE release and receptor binding?
    • release: sympathetic nerve terminals
    • receptors: alpha and Beta 1
  2. Epi release and receptor binding?
    • release: adrenal medulla
    • receptors: alpha, Beta 1 & 2
  3. 2 Direct acting effects of denervation or reserpine?
    • 1) No affect
    • 2) increase response to drug
  4. indirect effect of amphetamine & tyramine?
    increase release of NE
  5. indirect effect of cocaine & TCA's
    inhibit NET so NE is not recycled into cleft
  6. Indirect effect of MAOIs
    inhibit degradation of NE
  7. Indirect effect of reserpine (or denervation)
    No packaging into vesicle = no response
  8. Mixed effect of ephedrine
    • some direct receptor activity
    • some indirect action
  9. Mixed effect of denervation
    blunt but not eliminate effect
  10. Adrenergic receptors on synaptic button, platelets, Smooth mm, and heart?
    • button: Alpha 2
    • platelets: alpha 2 & Beta 2
    • Smooth mm: alpha 1 & Beta 2
    • Heart: Beta 1
  11. Alpha 1 function
    excitatory
  12. Alpha 2 function
    inhibitory
  13. Main alpha 1 agonist?
    Phenylephrine
  14. Main Alpha 2 agonist?
    Clonidine
  15. Epi, noradernaline & isoproterenol effectivity on alpha receptors?
    Epi > noradrenaline >> isoproterenol
  16. Isoproterenol, epi & NE strengths on B1, B2 & B3 receptors?
    • B1: Iso > Epi=NE
    • B2: Iso > Epi >> NE
    • B3: Iso=NE > Epi
  17. Dobutamine receptor and effect
    • receptor: B1
    • effect: increase heart rate & contractility, increase renin
  18. Albuterol receptor and effect
    • receptor: B2
    • effect:
    • same as B1 on heart + relaxed bronchial, uterus, bladder, GI, muscle blood vessels
    • Increase K uptake into muscles
    • Glycogenolysis/gluconeogenesis
    • B3 = fat lipolysis
  19. DA receptor effect on blood vessels
    • Dilate renal vessels, increse flow
    • Dilate coronary vessels
  20. Two molecules that metabolize NE & Epi
    MAO and COMT
  21. Alpha1 receptor effect on Cardiovascular system
    • Vasoconstrict
    • some increase in contraction
    • increased BP (stimulate baroreceptor, slow Heart)
    • Atherosclerosis = baroreceptor response decreased
  22. Alpha receptor effect on eye
    • contract radial pupillary = mydriasis
    • no accomodation effect
    • increase aqueous humor outflow (1 & 2)
    • treat glaucoma
  23. Alpha receptor effect on respiration
    • A1 constrict nasal & upper airway vessels
    • decongestants
  24. Alpha receptor effect on GI
    • A1 = relax GI
    • A2 = inhibit Ach release = less motility
  25. Alpha receptors on genitourinary
    • A1 increase continence, constrict sphincters
    • ejaculation
  26. Alpha receptor effects on metabolism
    • A1 increase glycogenolysis / gluconeogenesis
    • A2 inhibit lipolysis, inhibit insulin secretion, decrease renin
  27. Beta receptor effects on Cardio
    Increase everything (dilation, blood flow, contraction, O2 consumption, etc..)
  28. B receptor effects in eye
    B2 increase aqeous humor secretion, increase intraocular pressure
  29. B receptor effect on respiration
    B2 relax bronchial Sm mm
  30. B receptor effect on Genitourinary
    B2 relax uterus (pregnant) and relax bladder wall
  31. B receptor effect on metabolism
    • B1 increase renin = increased BP
    • B2 stimulate glycogenolysis, increase K uptake, increse insulin secretion
    • B3 = stimulate lipolysis
  32. What happens to Pulse Pressure when B1 and alpha are activated w/ NE?
    unchanged
  33. Alpha receptor effect on BP?
    Increased if alpha 1
  34. What receptors does NE activate
    Alpha and B1
  35. What receptors does Epi activate
    Alpha, Beta 1 & 2
  36. Cardiac effects of NE
    • A = B1 >> B2
    • Inc peripheral resistance (A)
    • Inc. BP
    • PP unchanged
    • HR inc then baroreceptors activate to slow
  37. Cardiac effects of Epi @ low dose
    • A, B1 & B2 (more effect than alphas @ low dose)
    • A = vasoconstriction
    • B1 = inc HR & contraction (systolic)
    • B2 = dilate Sk BV (dec. diastolic)
    • BP unchanged or slight inc
    • Inc PP & inc HR
  38. Effects of high dose/low dose Epi on HR, BP
    • high dose epi: HR inc, BP inc.
    • low dose epi: HR inc, BP dec. (due to more B2 stim.)
  39. What does Ephedrine release and what are its effects?
    • release: NE to stimulate A & B
    • effects: similar to EP
    • longer duration
    • bronchodilator
    • CNS stimulant
  40. function and cautions of Phenylephrine/Pseudoephedrine?
    • function
    • decongestant
    • may increase BP
    • Pseudoephedrine = more effective
    • Caution
    • Rebound Effect
  41. Methoxamine function
    IV for HTN
  42. Midrodrine function
    postural HTN
  43. Xylometazoline / Oxymetazoline function
    • Function
    • alpha agonist
    • Caution
    • rebound effet = receptor down-regulation
    • narrow angle glaucoma or HTN
  44. Clonidine function
    • A2 agonist
    • brain = inhibit NE release
    • decrease SNS output from CNS
    • decrease PR & BP
    • decrease craving for addicts
    • Caution
    • sever HTN of withdrawn abruptly
  45. Isoproterenol function
    • B >> A
    • inc contration
    • vasodilation Sk mm vessels
    • dec BP
    • inc CO
  46. Dobutamine function
    • B1 agonist
    • inc contraction
    • little effect on PR or HR
    • inc CO in heart failure/shock
    • short duration
    • Stress test
  47. Ritrodine receptor, function and side effect
    • B2
    • - relax uterus for premature labor
    • - side effect = headache
  48. Albuterol function & side effect
    • function
    • asthma treatment
    • tremor, tachycardia, palpitations
    • side effect
    • headache
  49. Along w/ albuterol, what other 4 drugs are commonly used for Asthma
    • Terbutaline
    • Pirbuterol
    • Bitolterol
    • Salmeterol
  50. Dopamine receptor, function
    • D1
    • vasodilate renal beds
    • treat cardiac schock
    • inc BF & CO w/o vasoconstriction
    • high doses = B1 stim, NE release and inc BP
  51. Fenoldopam function
    • more selective D1 agonist
    • dec BP
  52. Amphetamine function
    NE release in brain

    • side effects
    • HTN
    • psychosis
    • alert, aware, euphoria
    • headache
    • hemorrhage, convulsions, coma
  53. Methylphenidate (ritalin) function
    decrease ADHD
  54. Cocaine function and side effects
    • function
    • inhibit NE & DA reuptake
    • side effects
    • HTN
    • psychosis
    • tachycardia
  55. Tyramine function and side effects
    • function
    • inc NE releae from nerve terminals
    • side effects
    • tachyphylaxis
    • Sever HTN if MAO blocked = from sever NE release

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