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Glossary of Adrenomimetics

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What is adrenomimetic drugs?
Also known as sympathomimetics; mimics stimulation of sympathetic ANS "fight/flight"
Direct acting adrenomimetic agents
Dopamine
Dipivefrin (dont worry about this drug)
Direct acting adrenomimetics

Alpha 1 selective agonists
Phenylephrine
Methoxamine
Metaraminol
Xylometazoline
Oxymetazoline
Midodrine
Direct acting adrenomimetics

Alpha 2 selective agonist
Brimonidine
Apraclonidine
Direct acting adrenomimetics

Non-selective B agonists
Isoproterenol
Direct acting adrenomimetics

B1 selective agonists
Dobutamine
Direct acting adrenomimetics

B2 selective agonists
Metaproterenol
albuterol
Bitolterol
Pirbuterol
Salmeterol
Formoterol
Terbutaline
Ritodrine
**most will end in "ol"
Direct acting adrenomimetics

Mechanism of action
Directly activate adrenergic receptors--alpha, beta, or both
Direct acting adrenomimetics

Therapeutic Uses
Open angle glaucoma
Direct acting adrenomimetics

What would be the advantage of vasoconstricting blood vessels in the area where a local anesthetic is applied?
Keeps local anesthetic local

Reduces bleeding
Direct acting adrenomimetics

Nasal Decongestant Agents Used
Phenylephrine
Xylometazoline
Oxymetazoline
Phenylephrine
Short duration of action
Xylometazoline
Oxymetazoline
Long duration of action
What is the problem with chronic use of nasal decongestants?
Rebound nasal congestion
Effect of EPI on angioedema?
A1 --> constrict capillary beds --> counteracts dilation and increased vascular permeability of capillaries
Effect of EPI on bronchoconstriction?
B2 --> bronchodilation
Effect of EPI on Pruritis/urticaria?
B --> suppress release of mediators from mast cells
Why is NE not the drug of choice to treat anaphylaxis?
Low affinity for B2 receptors
How would you treat hypovolemic shock?
Volume replacement, Dopamine
How would you treat cardiogenic/septic shock?
Dopamine, Dobutamine, NE
Effect of low dose Dopamine?
Dopaminergic receptors on renal vasculature --> vasodilation --> increased renal blood flow
Higer dose of Dopamine _________?
B1 receptors (heart) --> increased CO and BP
Even higher dose of Dopamine _________?
A1 --> increased PVR, CO, BP
Drugs to treat heart block
EPI, Isoproterenol
Drug of choice for V Fib/Pulseless V Tach?
EPI
Drug of choice for CHF?
B1 --> increase force of contraction
Dobutamine, Dopamine
Short acting drugs of choice for asthma/COPD
Metaproterenol
Albuterol
Bitolterol
Pirbuterol
Terbutaline
"Four ols and a line"
Long acting drugs of choice for asthma/COPD?
Salmeterol
Formoterol
"For sal for long time"
How does Albuterol work for asthma/COPD?
Albuterol --> B2 --> relax bronchial smooth muscle --> bronchodilation --> open airways
What is the advantage of giving albuterol vs epinephrine/isoproterenol to treat asthma?
Less B1 side effects.
What direct acting adrenomimetic drug is used for premature labor?
Terbutaline
How does Terbutaline workon premature labor?
Activation of B2 receptors cause uterine smooth muscle relaxation --> stop uterine contractions.
What direct acting adrenomimetic dilates the pupil?
Phenylephrine
How does Phenylephrine dilate the eye?
PE --> A1 --> iris radial smooth muscle --> pupil dilation without cycloplegia.
What is cycloplegia?
Ciliary muscle paralysis with blurred vision.
What direct acting adrenomimetics are used for OAG?
Epinephrine--A and B

Brimonidine--A2
Apraclonidine--A2
Direct acting adrenomimetics

Adverse Effects--alpha adrenergic activation
A1 receptors on blood vessels
What are the alpha adrenergic adverse effects on blood vessels?
Reduce peripheral blood flow
Marked elevation in BP --> increase cardiac work --> precipitate cardiac ischemia, MI, HF
Direct acting adrenomimetics

Adverse Effects--alpha adrenergic
Mydriasis --> photophobia, may precipitate attack of NAG
Direct acting adrenomimetics

Adverse Effects--beta adrenergic
Tremor
B2 --> skeletal muscle --> tremor
Direct acting adrenomimetics

Contraindications
Cardiovascular Disease
Hyperthyroidism
Diabetes
Indirect Acting Adrenomimetic Agents
Tyramine
Amphetamine
Methylphenidate
Atomoxetine
What indirect acting adrenomimetic agents are CNS stimulants and/or used for ADHD?
Amphetamine
Methylphenidate
Atomoxetine
What is Tyramine's mechanism of action?
--Not a drug
--Comes from gut bacteria and fermented food.
--Metabolized by MAO
Promotes release of NE from the sympathetic nerve terminal.
What happens if Tyramine is not metabolized by the liver?
HTN crisis.
What may happen if a person is taking a drug that inhibits the activity of MAO and eats a lot of cheese and drinks a lot of beer?
Hypertensive crisis
Mixed Acting Adrenomimetic Agents
Ephedrine
Pseudoephredrine
What does Ephedrine do?
Releases NE from nerve terminals.

Activates A and B receptors
What is Ephedrine approved to be used for?
Asthma/COPD
Nasal congestion
How would ephedrine be useful for treating nasal congestion?
Ephedrine --> Release NE --> A1 in blood vessels of nasal mucosa --> decrease nasal congestion
What other class of drugs is used for nasal congestion?
alpha agonists
How would ephedrine be useful for treating asthma?
Ephedrine --> B2 on bronchiol smooth muscle --> bronchodilation
Ephedrine is seldom used to treat asthma. Why?
Side effects and development of B2 agonists (fewer SE)
What are adverse effects of Ephedrine?
Cardiovascular
--excessive stimulation of heart (B1) --> stroke, MI, sudden death
What are the CNS side effects of Ephedrine
Insomnia
Nervousness
Anxiety
What does psuedoephedrine activate?
Directly activates alpha, and to a lesser extent, B; and releases NE from nerve terminal
What is psuedoephedrine used for?
Nasal decongestant and has fewer CNS side effects than ephedrine.
What is the big problem with pseudoephedrine?
Difficult to find due to the manufacture of meth.
Phenylpropanolamine does what?
Releases NE from nerver terminal and is used as a nasal decongestant and weight reduction (Dexatrim)

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