Ch 15 Flashcards
Class of drugs who produce their effects by activating adrenergic receptors
Adrenergic Agonists aka sympathomimetics
Drugs can activate adrenergic receptors by what 4 basic mechanisms
1) direct receptor binding!!!!!
2) promotion of Norepinephrine (NE)
3) blockade of NE reuptake
4) inhibition of NE inactivation
what are the two major classes of adrenergic agonists
catecholamines
noncatecholamines
What 3 things do catecholamines have in common
cannot be used orally
brief duration of action
cannot cross BBB
what are the two enzymes responsible for the brief duration of action and not being able to take catecholamines orally
MAO
COMT
Where does MAO and COMT (enzymes) live
liver and intestinal wall
Can you give catacholamines orally? why/why not
no, because MAO and COMT inactivate them before reaching systemic circulation
Which catecholamines are only effective if given by continuous infusion
NE
dopamine
dobutamine
NE or dopamine that has turned from colorless to pink or brown. Is this normal?
no, the pigmentation is caused by oxidation and should be discarded
Dobutamine that has turned pink or brown. Is this normal?
Dobutamine can be used up to 24 hours after solution was made even if discoloration appears
ephedrine
albuterol
phenylephrine
are what?
noncatecholamines
3 differences of noncatechlamines
longer half-lives
can be given orally
more able to cross the BBB
what receptors does albuterol activate
highly selective for B2
what receptors for isoproterenol
less selective, B1, B2
What receptors for Epinephrine
even less selective, A1, A2, B1, B2
At low doses, selectivity is
maximal
as doses increased, selectivity
declines
What drugs are capable of activating A1 receptors
epinephrine NE phenylephrine ephedrine dopamine
Theraeputic application of A1 activation
vasoconstriction -blood vessels of skin, viscera, mucous membranes
mydriasis
uses
hemostasis (Epi)
nasal decongestants
adjunct to local anesthetics (lido with epi)
Elevation of BP
Mydriasis (dilate pupil for eye exams or surgery)
adverse effects of A1 activation
Hypertension (widespread vasoconstriction)
Necrosis (IV extravates - surrounding tissue tissue)
Bradycardia (A1 agonists can cause reflex slowing of the heart. Vasoconstriction elevates BP which triggers baroreceptor reflex which leads to bradycardia
if extravation of a A1 agonists, what should the area be infiltrated with?
A1 blocking agent
phentolamine
2 effects of Central A2 agonists
1) reduction of sympathetic outflow to heart and blood vessels
2) relief of severe pain
catecholamines that work on A2
epinephrine
norepinephrine
noncatecholamine that works on A2
Ephedrine
Drugs that work on B1 receptors
Epi NE isoproterenol dopamine dobutamine epinephrine
Therapeutic applications of B1 application
Heart failure - positive inotropic effects
Shock - increase HR and force of contraction - which increases Cardiac output and tissue perfusion
AV heart block - enhance impulse conduction
Cardiac arrest
Adverse Effects B1 Activation
tachycardia
dysrhythmias
angina
B2 activation is limited to
lungs and uterus
Drugs used for B2 activating
Epi
isoproterenol
albuterol