Adrenergic Receptor Agonists/Antagonists Flashcards
Pre-ganglionic cells
Ach
Post-ganglionic parasympathetic release
Ach
Post-ganglionic sympathetic release
NE
EXCEPTION: Sweat glands and some skeletal/vascular smooth muscle release Ach
Adrenal gland releases
Epi and NE
Miosis
Pupillary CONSTRICTION
Mydriasis
Pupillary DILATION
Alpha 1
Vasoconstriction via PLC (DAG and IP3)
Contracts: Vascular smooth muscle, pupillary dilator muscle
Alpha 2
Inhibits NT release via Gi and inhibition of AC (no cAMP)
Vascoconstriction via inhibition of AC and PKA, increased affinity of MLCK to myosin light chain
Inhibtion of NT release, contracts some vascular smooth muscle
B1
Gs increases AC which phosphorylates Ca channels in pacemaker cells and myocytes
Stimulates rate and force of heart
Stimulates renin relase of juxtaglomerular cells
B2
Vasodilation via cAMP and PKA which phosphorylates MLCK to decrease its activity and inhibits myosin light chain
Relaxes respiratory, uterine, and vascular smooth muscle
Can cause tremor in voluntary muscle
Catecholamine receptor affinity
a1
Epi > NE»_space;> Iso
Catecholamine receptor affinity
a2
Epi > NE»_space;> Iso
Catecholamine receptor affinity
B1
Iso > Epi = NE
Catecholamine receptor affinity
B2
Iso > Epi»_space; NE (not a full agonist)
Direct acting alpha agonist
Nonselective
Epi
Ne
Dopamine
Direct acting alpha agonist
a1 selective
Phenylephrine
Direct acting alpha agonist
a2 selective
Clonidine
Direct acting beta agonist
Nonselective
Epi
Isoproterenol
Direct acting beta agonist
B1 selective
Ne
Dopamine
Dobutamine
Direct acting beta agonist
B2 selective
Terbutaline
Albuterol
Indirect acting agonist
Releasers and reuptake inhibitors
Amphetamine Methamphetamine Methyphenidate Ephedrine Pseudoephedrine Tyramine
Adrenergic alpha antagonist
Nonselective
Phentolamine (reversible)
Phenoxybenzamine (irreversible)
Adrenergic alpha antagonist
a1 selective
Prazosin
Dozazosin
Terazosin
Adrenergic beta antagonists
Nonselective
Propanolol
Timolol
Nadolol
Adrenergic beta antagonists
B1 selective
Atenolol
Metoprolol
Adrenergic beta antagonists
Parial B1 and B2 agonist
Pindolol