Adenergic receptors Flashcards
α1(Target action)
- Vascular, genitourinary smooth muscle contraction
- Intestinal smooth muscle relaxation
- Liver: glycogenolysis, gluconeogenesis
- Salivary secretion
α2(target action)
- Panreas: decrease insulin secretion
- Nerve terminals: Decrease NE release
- CNS: decrease sympathetic tone
- Platelet aggregation
β1(Target action)
- Heart: Increase force(+ionotropic), Increase rate(+ chronotropic) Increase AV conduction velocity
- Kidney: increase renin release
β2(Target action)
- Smooth muscle relaxation
- Skeletal muscle glycogenolysis
- Liver: glycogenolysis, Gluconeogenesis
D1(Target action)
Dilates renal vasculature
Direct acting sympathomimetic drugs
Clonidine Albuterol Norepinephrine Phenylephrine Isoproterenol Epinephrine
Indirect acting sympathomimetic drugs
Mao inhibitors Tyramine Ephedrine Amphetamine Cocaine Tricyclic antidepressants
Epinephrine(selectivity)
α, β nonselective
Norepinephrine(selectivity)
α, β1 > β2
Isoproterenol(selectivity)
β
Phenylephrine(selectivity)
α1
Albuterol(selectivity)
β2
Clonidine(selectivity)
α2(centrally active)
Therapeutic uses of adrenergic agonists and target
- Nasal decongestants(α1)
- Slow absorption of local anesthetics(α1)
- Antihypertensive(α2)
- Treatment of shock(β1, dopamine)
- Cardiopulmonary resuscitation( α1 epi)
- Asthma(β2, airway smooth muscle)
- Anaphylactic reactions(mast cells β2; α1 resistance vessels)
- Mydriasis (radial muscle α1)
- Wide angle glaucoma(α1 for vasoconstriction: α2 for reduced secretion)
- Delay premature labor( uterine β2)
Toxicity & side effects of adrenergic agonist
- Hypertensive reactions– cerebral hemorrhage( α1)
- Cardiac ventricular arrhythmias
- Myocardial ischemia
- Vasoconstriction, ischemia
- CNS Stimulation-Rebound nasal congestion
- withdrawal syndrome from α2 agonists
Therapeutic uses of adrenergic antagonists( α-antagonist)
- Hypertension
- Management of pheochromocytoma
- Raynaud’s disease
- Congestive heart failure
- Benign prostatic hyperplasia
Therapeutic uses of adrenergic antagonists(β-antagonist)
- Hypertension
- Angina
- Cardiac arrhythmias
- Reducing mortality after myocardial infarction
- Hyperthyroidism
- anxiety states
- open-angle glaucoma
- migraine(prophylaxis)
Toxicity of adrenergic α-antagonist
- Postural hypotension
- reflex tachycardia
- myocardial ischemia
- Salt and water retention
- Peripheral edema
- GI stimulation
- inhibition of ejaculation
Toxicity of adrenergic β-antagonist
- Bronchoconstriction
- Bradycardia
- Precipitation of CHF
- exacerbation of angina and increased risk of death after abrupt withdrawal
- fatigue
- cold extremeties
β receptor order of selectivity for phenylephrine, isoproterenol, and epinephrine
Isoproterenol > Epi»_space; Phenylephrine
α receptor order of selectivity for phenylephrine, isoproterenol, and epinephrine
Epi > phenylephrine»_space; Isoproterenol
How many subtypes of α1 and α2 receptors are there?
At least 3 subtypes of each
How is Epi made(step by step chemicals)
Tyrosine–> L-DOPA –> Dopamine –> Norepi –> Epi