Difference between revisions of "Adrenergic Pharmacology"
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! Receptor !! Binding Affinity !! Effects !! Mechanism !! Agonists !! Antagonists | ! Receptor !! Binding Affinity !! Effects !! Mechanism !! Agonists !! Antagonists | ||
|- | |- | ||
− | | α1 || NE > Epi >> Iso | | + | | α1 || NE > Epi >> Iso |
+ | | | ||
+ | *Smooth muscle contraction, ↑SVR, ↑MAP | ||
+ | *Mydriasis, urethral sphincter contraction | ||
+ | | | ||
+ | G<sub>q</sub> → PLC → IP<sub>3</sub>/DAG → [Ca<sup>2+</sup>]<sub>i</sub> | ||
| | | | ||
*NE | *NE | ||
− | *Phenylephrine | + | *Phenylephrine (pure α1) |
*Midodrine | *Midodrine | ||
| | | | ||
Line 14: | Line 19: | ||
*Tamsulosin | *Tamsulosin | ||
|- | |- | ||
− | | α2 || Epi = NE >> Iso || | + | | α2 || Epi = NE >> Iso |
+ | | | ||
+ | *↑SVR, ↑MAP | ||
+ | *Decreased insulin release, inhibits lipolysis, decreases aqueous humor production | ||
+ | | | ||
+ | presynaptic G<sub>i</sub> → ↓AC → ↓cAMP → inhibition of NT release, sympatholytic effects | ||
| | | | ||
*Dexmedetomidine | *Dexmedetomidine | ||
Line 24: | Line 34: | ||
*Trazodone | *Trazodone | ||
|- | |- | ||
− | | β1 || Iso > NE > Epi | | + | | β1 || Iso > NE > Epi |
+ | | | ||
+ | *↑Chronotropy (myocytes), ↑Inotropy (SA node) →↑CO | ||
+ | *↑Renin release/↑volume (JGA) | ||
+ | *Amylase secretion | ||
+ | | | ||
+ | G<sub>s</sub> → ↑AC → ↑cAMP | ||
| | | | ||
*Dobutamine | *Dobutamine |
Revision as of 06:07, 4 February 2023
Receptor | Binding Affinity | Effects | Mechanism | Agonists | Antagonists |
---|---|---|---|---|---|
α1 | NE > Epi >> Iso |
|
Gq → PLC → IP3/DAG → [Ca2+]i |
|
α1 selective:
|
α2 | Epi = NE >> Iso |
|
presynaptic Gi → ↓AC → ↓cAMP → inhibition of NT release, sympatholytic effects |
|
Non-selective:
|
β1 | Iso > NE > Epi |
|
Gs → ↑AC → ↑cAMP |
|
Cardiac Selective:
|
β2 | Iso > Epi > NE | Smooth muscle relaxation | Gs, cAMP up |
|
Non-Selective:
|
β3 | Iso > Epi = NE | Lipolysis, bladder detrusor relaxation | Gs, cAMP up |
|
|