adrenergic drugs (agonists and antagonists) Flashcards
Direct sympathomimetics - drugs and mechanism of action
- albuterol - β2 more than β1
- salmoterol - β2 more than β1
- dobutamine - β1 more than β2, α
- dopamine - D1=D2 more than β, and β more than α
- epinephrine - β more than α (but α predominate at high doses)
- fenodlopam - D1
- isoproterenol - β1 = β2
- midodrine - a1
- norepinephrine - a1 more than α2 more than β1
- phenylephrine - α1 more than α2
Albuterol, slameterol - mechanism of action and clinical use
β2 more than β1
albuterol for acute asthma or COPD
salmeterol for long term asthma or COPD control
dobutamine - mechanism of action and clinical use
β1 more than β2, α
- HF (inotropic more than chronotropic)
- cardiac stress testing
epinephrine - mechanism of action and clinical use
β more than α (but α predominate at high doses)
1. anaphylaxis 2. asthma 3. open-angle glaucoma
dopamine - mechanism of action and clinical use
D1=D2 more than β, and β more than α
1. unstable bradycardia
2. HF 3. shock
β predominates at lower doses, α at higher
fenoldopam - mechanism of action and clinical use
D1 1. postoperative hypertension 2. hypertensive crisis 3. vasodilatero (coronary, peripheral, renal, splachinc) 4. promotes natriureis
fenoldopam - side effects
can cause hypotension and tachycardia
isoproterenol - mechanism of action and clinical use
β1=β2
electrophysiologuc evaluation of tachyarrhythimas
isoproterenol - side effects
can worsen ischemia
Milodrine - mechanism of action and clinical use
α1
autonomic insifficiency and postural hypotension
Milodrine - side effects
may exacerbate supine hypertension
norepinephrine - mechanism of action and clinical use
a1 more than α2 more than β1
hypotension
spetic shock
phenylephrine - mechanism of action and clinical use
α1 more than α2
hypotension (vasoconstriction), ocular procedures (mydriatic), rhinitis (decongestant)
Indirect sympathomimetics - drugs
- amphetamines
- cocaine
- ephedrine
amphetamine - mechanism of action
- indirect general agonist
- reuptake inhibitor
- releases stored catecholamines
cocaine - mechanism of action
- indirect general agonist
2. reuptake inhibitor
ephedrine - mechanism of action
- indirect general agonist
2. releases stored catecholamines
amphetamine - clinical use
- Narcolepsy
- obesity
- ADHD
ephedrine - clinical use
- Nasal congestion
- urinary incontinence
- hypotension
cocaine - clinical use
vasoconstriction and local anesthesia
cocaine - β blockers
never give β-blockers if cocaine intoxication is suspected –> it can lead to unopposed α1 activation –> extreme hypertension
epinephrine vs norepinephrine according to effects at β2 receptors
epinephrine has significantly stronger effect at β2 receptor than norepinephrine
norepinephrine effects on cardiovascular system
increases systolic and diastolic pressures (α1 mediated) –> increases MAP
isoproterenol effects on cardiovascular system
causes β2 mediated vasodilation resulting in decreased MAP and increaed heart rate through β1 and reflex activity
norepinephrine vs epinephrine vs isoproterenol according to HR
norepinephrine –> reflex bradycardia
epinephrine –> β1 mediated tachycardia
isoproterenol –> β1 and refelx mediated tachycardia (higher than epinephrine)
norepinephrine vs epinephrine vs isoproterenol according to BP
norepinephrine –> increases systolic, diastolic, and MAP
epinephrine –> increases systolic (a1) and decreases diastolic (β2) (slightly increased MAP)
isoproterenol –> increases systolic (heart) and decreases diastolic (more than epinephrine), (slightly decreased MAP)
norepinephrine vs epinephrine vs isoproterenol according to peripheral resistance
norepinephrine –> increased (unopposed α1)
epinephrine –> decreased (β2>a1)
isoproterenol –> more decreased (unopposed β2)
norepinephrine vs epinephrine vs isoproterenol according to cardiac output
norepinephrine –> unchanged
epinephrine –> increased
isoproterenol –> more increased
norepinephrine vs epinephrine vs isoproterenol according to pulse pressure
norepinephrine –> increased
epinephrine –> increased
isoproterenol –> more increased
sympatholytics - mechanism of action
α2 agonists
sympatholytics (α2 agonists) drugs
- clonidine
- guanfacine
- α-methyldopa
- Brimonidine
clonidine - clinical use
- hypertensive urgency (limited situations)
- ADHD
- Tourette syndrome
clonidine - side effects
- CNS depression
- bradycardia
- hypotension
- respiratory depression
- miosis
α-methyldopa - clinical use
hypertension in pregnancy
α-methyldopa - side effects
- direct coomps + hemolysis
2. SLE-like syndrome
guanfacine - clinical use
- hypertensive urgency (limited situations)
- ADHD
- Tourette syndrome
guanfacine - side effects
- CNS depression
- bradycardia
- hypotension
- respiratory depression
- miosis
Brimonidine - clinical use
Glaucoma