Sympathomimetics Flashcards
a1 potency
epi>Ne»ISO
A2 potency
Epi>NE»ISO
B1 potency
Iso>Epi=NE
B2 potency
Iso>Epi»NE
Epinephrine Pharmocologcial effects
Increase HR
increased contractility
increased conduction velocity in the heart
increased oxygen consumption and work done by the heart
greater affinity for B2 so at low doses–>decreased BP, but at higher doses it binds to a1–>vasoconstriction
Epi and coronary vessels
vasodilation B2
epi and kidney, mucosa and skin
vasoconstriction a1
epi and pulmonary vasculature
vasoconstriction a1
Clinical uses for epi
1) Asthma: bronchodilation (B2) and vasoconstriction (a1)
2) anaphylactic shock: immediate SC injection: bronchodilation, decreased edema (VC), decreased histamine, alleviates Hypotension
3) cardiac resuscitation
4) topical hemostatic
5) Infiltration with local anesthetics (keeps them local)
Epinephrine adverse effects
arrhythmias (esp when dosed with gas anesthetics)
cerebral hemorrhage
necrosis at injection site
CNS: fear , anxiety, HA
epinephrine contraindications
HTN shock hyperthyroidism (can increase arrhythmias) angina asthmatics with CVD
NE pharmacology
a1 and B1 agonist (NO B2)
positive inotropic effects (B1), negative chronotropic effects (REFLEX)
vasoconstriction (a1)= always increased HR
NE uses, s/e
IV to manage hypotension during spinal anesthesia
anxiety, slow forceful heartbeat, HA
same contraindications as Epi
Dopamine pharmacology and function
B1 and D1 agonist, a1 at high concentrations
renal vasodilators
used for cardiogenic shock, increased CO and increases Kidney excretion
Dobutamine
B1 selective agonist
positive inotropy and chronotropy = increased CO
used fro MI, CHF, cardiogenic shock
Phenylephrine pharm
a1 agonist (non-catecholamine)= longer lasting and can be PO
Vasoconstriction
increased TPR, increased BP
Reflex bradycardia
Phenylephrine clinical uses
1) Maintain BP in hypotensive states (spinal anesthesia)
2) paroxysmal atrial tachycardia (reflex brady)
3) nasal decongestant
4) Glaucoma
5) infiltration with anesthetics
Albuterol
relatively selective B2 agonist (10x vs B1)
bronchodilation used for asthma
aerosolized decreases systemic effects (PO sometimes used)
desensitization may occur
Salmeterol
long active selective B2 agonist
better for nighttime asthma or prophylaxis tx
Formoterol does same thing
Tyramine
Displaces NE from nerve terminal
normally degraded by MAO in gut
found in high levels in foods, so pt on MAOI can get hypertensive crisis
reuptake also inhibited by cocaine
Cocaine
competitively block the reuptake of NE into nerve terminal, NE levels in the synapse are higher for longer
also block tyramine uptake
amphetamines
cause release of NE from adrenergic nerve endings ( indirect)
increase alertness, fatigue, mood, increased HR etc.
relatively hydrophobic and enter CNS
e.g. adderall
Ephedrine
mixed acting agonist
Direct: B receptor agonist
Indirect: releases NE
not metabolized by COMT or MAO (long lasting)
CV: increased HR and VC
bronchodilation
used as a pressor, nasal decongestant