summary of classification of adrenoceptors

· alpha1, alpha 2
· alpha1 activates phospholipase C
· alpha 2 inhibits adenylyl cyclase
· all beta receptors stimulate adenylyl cyclase
alpha1 cause vasoconstriction, relaxation of GIT
smooth muscles, salivary secretion and hepatic
glycogenolysis
alpha 2 inhibits neurotransmitter release, cause
platelet aggregation, contraction of vascular smooth
muscles and inhibition of insulin release
beta 1 cause increased cardiac rate and force,
delayed cardiac hypertrophy
beta 2 cause bronchodilation, vasodilation,
relaxation of visceral smooth muscle , hepatic
glycogenolysis and muscle tremors
beta 3 cause lipolysis
ACTIONS OF ADRENOCEPTOR
 AGONIST
Alpha 1
phenylephrine,oxymetazoline, methoxamine(non
selective)
Nasal decongestion
Hypertension(vasoconstriction), reflex
bradycardia( baro receptors, medullary vasomotor
centre, M2 decrease HR)
Alpha 2
clonidine (non selective partial agonist),
guanfacine, guanabenz,alpha methyl dopa
hypertension , migraine
drowsiness ( alpha2 on presynaptic neuron in CNS,
PNS)(nucleus coeruleus maintains arousal states via
NE), orthostatic hypotension( gravitational venous
pooling), oedema, weight gain, rebound
hypertension(upregulation of adrenoceptors)
Alpha 1 beta 1
Nor epinephrine
hypertension ( vasoconstriction alpha 1), tachycardia
(beta 1), reflex bradycardia, ventricular
dysrhythmias
Alpha 1 , beta 1, beta 2
epinephrine
Asthma (beta 2 bronchodilation)
anaphylactic shock(improves blood pressure through
alpha 1 and heart function via beta 1,improve
respiration via beta bronchodilation, decreases
inflamatory mediators through beta 2 action on mast
cells), cardiac arrest ( beta 1), adjuvant to anesthesia
(alpha 1vasoconstriction),
same as NE
Beta 1
Dobutamine
cardiogenic shock ( insufficient pumping to meet
bodys need)
dysrhythmias
Dopamine
low dose treats acute tubular necrosis via dilation at
dopamine receptor
physiological dose (moderate dose) improves CO via
beta 1
high dose alpha activity, renal vasoconstriction)
infusion rate must be well controlled

Beta 2
salbutamol,terbutaline
asthma(salmeterol), delay parturition(ritodrine)
( beta 2 on uterus cause smooth muscle relaxation)
clenbuterol
anabolic action on muscles increase strength via
beta 2
tachy cardia
Beta 1 beta 2
isoprenaline(isoproterenol)
asthma
tachycardia
ACTIONS OF ADRENOCEPTOR
ANTAGONIST
Non selective alpha antagonist
phenoxybenzamine (phaeochromocytoma)
postural hypotension, tachycardia, nasal congestion
alpha 1
prazosin
hypertension
tamsulosin(uroselective)
Benign prostatic hyperplasia (BPH) ( Alpha 1
receptor cause muscle proliferation
Beta non selective
propranolol, timolol, alprenolol(partial agonist),
oxprenolol, pindolol
angina, hypertension, cardiac dysrhythmias, anxiety,
tremor, glaucoma(topical, reduce IOP by blocking
sympathetic nerve ending in ciliary epithelium
causing fall in aqueous humour production)
bronchoconstriction(Beta 2 block), cardiac
failure(beta1 block), cold extremities(decreased
blood supply to fingers and toes), fatigue(decreased
heart rate and amount of blood pump), depression ,
hypoglycaemia (inhibit glycogenolysis,
gluconeogenesis)
Beta 1
metoprolol
angina, hypertension, dysrhythmias
as propranolol except bronchoconstriction
nebivolol (also enhance nitric oxide mediated
transmission)
hypertension
fatigue(decreased cardiac output, decreased muscle
perfusion), headache
Beta 2 selective
Butoxamine(weak alpha agonist)
no clinical use
Mixed alpha/beta antagonist
labetalol
hypertension in pregnancy
postural hypertension, bronchoconstriction
carvedilol
heart failure