B4-005 Autonomic Drugs Flashcards
what adrenoreceptors:
* peripheral vasculature
* contraction of smooth muscle
* increase BP
alpha 1
what adrenoreceptor:
* presynaptic autoregulation of neurotransmitter release
alpha 2
what adrenoreceptor:
* approx equal affinity for Epi and NE
beta 1
what adrenoreceptor:
* higher affinity for Epi than NE
beta 2
densensitization of adrenoreceptors may limit
therapeutic response
denervation supersensitivity of adrenoreceptors may
exacerbate side effects
catecholamines
- epinephrine
- norepinephrine
- isoproternol
- dobutamine
- very potent vasoconstrictor & cardiac stimulant
- positive inotropic and chronotropic actions on heart
- also activates beta2 receptors
epinephrine
similar potency at beta 1 receptors, but relatively little effect on beta 2
norepinephrine
- compensatory vagal reflexes over come direct positive chronotropy
- at high doses, may indirectly increase heart rate
norepinephrine
- potent nonselective beta-receptor agonist
- positive chronotropic and inotropic actions
- decreases both diastolic and mean arterial pressure
isoproterenol
- relatively beta 1 selective synthetic catecholamine
- also activates alpha 1 receptors
dobutamine
- prototypic alpha1 agonist
- not a chatechol derivative
- not inactivated by COMT
- longer duration of action than catecholamines
- mydriatic and decongestant
- can raise blood pressure
phenylephrine
first orally active sympathomimetic drug
ephedrine
- widely available OTC decongestant
- also have indirect effects of releasing endogenous NE
psuedoephedrine
- direct alpha 1 agonists
- used as topical decongestants
2
- oxymetazoline
- xylometazoline
- alpha 2 selective agonists
- used (poorly) as antihypertensives
- dimish SNS outflow
2
- clonidine
- methyldopa
- beta 1 selective agonist
- increases cardiac output with less reflex tachycardia
- lack of beta 2 stimulated venous dilation
dobutamine
- beta 2 selective agonists
- treatment of asthma
2
- albuterol
- salmeterol
- beta 2 selective agonist
- treatment of premature labor
ritodrine
- indirect sympathomimetics
- marked stimulant effects on mood and alertness
- depressant effect on appetite
- amphetamine
- methamphetamine
- local anesthetic
- sympathomimetic due to blockade of uptake 1
cocaine
- releases stored catecholamines
- found in high concentrations in fermented foods (cheese)
- MOA inhibitors potentiate effects and can produce hypertension
tyramine
- prototypic alpha antagonist
- nonselective between alpha1 and alpha2
- competitive blockade of receptors
- reduces TPR, MAP
- produces reflex tachycardia (SNA reflex)
phentolamine
- irreversible-binds covalently to alpha receptors
- postural hypotension and tachycardia limit use
phenoxybenzamine
- alpha receptor antagonists
- selective for alpha 1 receptors
3
- prazosin
- terazosin
- doxazosin
- alpha2 selective antagonist
- no established clinical role
yohimbine
- block effects of catecholamines at beta receptors
- varied affinity for beta1 vs. beta2 receptors
- selectivity has important clinical implications
- non are absolutel specific for beta1 receptors
beta receptor antagonists
- lower blood pressure in patients with hypertension
- negative inotropic and chronotropic effects
- reduce oxygen demand of myocardium
beta receptor antagonists
clinically useful for:
* hypertension
* ischemic heart disease
* cardiac arrhythmias
* glaucoma
* hyperthyroidism
beta blockers
- prototypical beta-blocking drug
- nonselective
propranolol
beta-1 selective beta blockers
2
metoprolol
atenolol
beta blockers with a very long duration of action
2
nadolol and timolol
- reversible alpha1 antagonist
- also nonselective beta antagonist
- hypotension with less tachycardia than alpha blockers
labetalol
- beta blocker
- selective for beta2 receptors
- no obvious clinical application
butoxamine
name the adrenoreceptor:
sympathetic activity contracts the radial muscle of the iris
a1
name the adrenoreceptor:
parasympathetic activity contracts the circular muscle of the iris
M3
name the adrenoreceptor:
sympathetic activity relaxes ciliary muscle of eye
beta