Difference between revisions of "Adrenergic Pharmacology"

Latest revision as of 06:17, 4 February 2023

Adrenergic Receptors
Receptor	Binding Affinity	Effects	Mechanism	Agonists	Antagonists
α1	NE > Epi >> Iso	Smooth muscle contraction, ↑SVR, ↑MAP Mydriasis, urethral sphincter contraction	G_q → PLC → IP₃/DAG → [Ca²⁺]_i	NE Phenylephrine (pure α1) Midodrine	α1 selective: Prazosin Tamsulosin
α2	Epi = NE >> Iso	↑SVR, ↑MAP ↓insulin release, ↓lipolysis, ↓aqueous humor production	presynaptic G_i → ↓AC → ↓cAMP → ↓NT release	Dexmedetomidine Clonidine	Non-selective: Phenoxybenzamine Phentolamine Trazodone
β1	Iso > NE > Epi	↑Chronotropy (myocytes), ↑Inotropy (SA node), ↑SBP ↑Renin release/↑volume (JGA) Amylase secretion	G_s → ↑AC → ↑cAMP	Dobutamine Isoprenaline Norepi	Cardiac Selective: Metoprolol Atenolol Esmolol
β2	Iso > Epi > NE	Smooth muscle relaxation, ↓SVR, ↓DBP, ↓MAP Bronchodilation ↑Lipolysis, ↑Insulin release Relax uterine smooth muscle ↑aqueous humor production	G_s → ↑AC → ↑cAMP → ↑PKA	Albuterol Formoterol Isoprenaline Salmeterol Terbutaline Ritodrine	Non-Selective: Propranolol Nadolol Pindolol Timolol Carvedilol (anti-α1) Labetalol (anti-α1)
β3	Iso > Epi = NE	Lipolysis Bladder detrusor relaxation	G_s → ↑AC → ↑cAMP → ↑PKA	Mirabegron	SR 59230A

@@ Line 22: / Line 22: @@
 |
 *&uarr;SVR, &uarr;MAP
-*Decreased insulin release, inhibits lipolysis, decreases aqueous humor production
+*&darr;insulin release, &darr;lipolysis, &darr;aqueous humor production
 |
-presynaptic G<sub>i</sub> &rarr; &darr;AC &rarr; &darr;cAMP &rarr; inhibition of NT release, sympatholytic effects
+presynaptic G<sub>i</sub> &rarr; &darr;AC &rarr; &darr;cAMP &rarr; &darr;NT release
 |
 *Dexmedetomidine
@@ Line 36: / Line 36: @@
 | &beta;1 || Iso > NE > Epi
 |
-*&uarr;Chronotropy (myocytes), &uarr;Inotropy (SA node) &rarr;&uarr;CO
+*&uarr;Chronotropy (myocytes), &uarr;Inotropy (SA node), &uarr;SBP
 *&uarr;Renin release/&uarr;volume (JGA)
 *Amylase secretion
@@ Line 51: / Line 51: @@
 *Esmolol
 |-
-| &beta;2 || Iso > Epi > NE || Smooth muscle relaxation || Gs, cAMP up
+| &beta;2 || Iso > Epi > NE
+|
+*Smooth muscle relaxation, &darr;SVR, &darr;DBP, &darr;MAP
+*Bronchodilation
+*&uarr;Lipolysis, &uarr;Insulin release
+*Relax uterine smooth muscle
+*&uarr;aqueous humor production
+|
+G<sub>s</sub> &rarr; &uarr;AC &rarr; &uarr;cAMP &rarr; &uarr;PKA
 |
 *Albuterol
@@ Line 68: / Line 76: @@
 *Labet'''alol''' (anti-&alpha;1)
 |-
-| &beta;3 || Iso > Epi = NE || Lipolysis, bladder detrusor relaxation || Gs, cAMP up
+| &beta;3 || Iso > Epi = NE
+|
+*Lipolysis
+*Bladder detrusor relaxation
+|
+G<sub>s</sub> &rarr; &uarr;AC &rarr; &uarr;cAMP &rarr; &uarr;PKA
 |
 *Mirabegron