autonomic/cns

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Author:
ekdldksk
ID:
112041
Filename:
autonomic/cns
Updated:
2011-10-25 11:45:57
Tags:
autonomic cns
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Description:
autonomic/cns drugs and concepts
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  1. Adrenergic receptors = GPCRs
    1. Types
    2. Endogenous ligands
    • 1. Types:
    • - a1-gq coupled: increases IP3 & Ca --> contracts arterioles

    - a2-gi coupled: inhibits AC --> dec cAMP --> inc heart contraction

    - b1/b2-gs coupled: activate AC --> inc cAMP --> relax bronchiole SM

    - b2 more sensitive to E than to NE (higher affinity for E)

    2. Endogenous ligands: E & NE
  2. a-adrenergic Rs
    1. general fcn
    2. types and fcn
    1. vasoconstrict arteries to heart, veins, & dec motility of GI SM

    2. a1: SM contraction; a2: inhibit insulin release, activate sphinctors, activate thrombocyte agg.
  3. b-adrenergic Rs
    -types and fcn of each
    - b1: inc HR/CO, inc contraction, inc renin secretion

    - b2: SM relax, dilation (dec bp), inhibit His release from mast cells

    - b3: inc lipolysis in adipose tissue
  4. Adrenergic agonists
    1. 2 categories
    2. Drugs from each category (4 each)
    1. Catecholamines, Non-catecholamines

    • 2.
    • Catecholamines:
    • - clonidine (a2 agonist)
    • - dobutamine (b1 agonist)
    • - isoproterenol (b2 agonist)
    • - E & NE (non-selective)

    • Non-catecholamines:
    • - tetrahydrozoline / visine (a agonist)
    • - phenylephrine (a1 agonist)
    • - pseudoephedrine (a1 agonist)
    • - albuterol (b2 agonist)
  5. B antagonists (autonomic) - 2
    • 1. propanolol (dec HR, bp)
    • 2. labetalol (also a1 antagonist)
  6. Neostigmine
    • AChE inhibitor
    • competitive antagonist
  7. Treatments for Parkinson's disease (3)
    • bromocriptine
    • amantadine
    • L-DOPA + carbidopa = Sinemet
  8. clonidine (CNS)
    • a2 agonist
    • catecholamine
  9. isoproterenol (CNS)
    • b agonist
    • catecholamine
  10. ephinephrine/NE (CNS)
    • non-selective agonist
    • catecholamines
  11. dobutamine (CNS)
    • b1 agonist
    • catecholamine
  12. tetrahydrozoline (CNS)
    • visine
    • non-catecholamine
    • a agonist --> constrict bvs to dec red eye
  13. phenylephrine, pseudoephedrine (CNS)
    • a1 agonists
    • non-catecholamines
    • decongestant (vasoconstrictor --> dec perfusion rate)
  14. albuterol (CNS)
    • b2 agonist
    • non-catecholamine
    • treatment for asthma
  15. bromocriptine
    • DA agonist
    • parkinson's disease treatment
    • longer 1/2 life but less effective than LDOPA
  16. amantadine
    • inc DA release
    • parkinson's disease treatment
  17. Sinemet (L-DOPA + carbidopa)
    • parkinson's treatment
    • allows L-DOPA to cross BBB without being metabolized by AAAD (carbidopa inhibits AAAD enzyme)

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