Adrenergic Direct Agonist Flashcards
Cardiovascular system (B1)
-Positive Chronotropic effect
-Positive inotropic effect
Vascular Smooth Muscle (alpha 1 and Beta 2)
-Alpha 1: Vasoconstriction
-Beta 2: Vasodilation
Respiratory Tract (Beta 2)
Bronchodilation
Urinary Tract (Alpha 1 and Beta 3)
-Relaxes Bladder
-Constrict Sphincter
GI tract (Alpha 1 and Beta 2)
-Decrease GI motility
-Constrict Sphincter
Glands (M3)
Stimulation secretion (sweat glands)
Kidney (Beta 1)
Increase Renin secreation
Adipocytes (Beta 3)
Increase Lipolysis
Which have the strongest response to alpha agonist?
Epinephrine > Norepinephrine»_space; Isoproterenol
Which have the strongest response to Beta agonist?
Isoproterenol > Epinephrine > Norepinephrine
Alpha 1 (Gq)
-Vascular s. Muscle: Vasoconstriction
-GI and bladder sphincter: Constriction
Alpha 2 (Gi)
Suppression of release of Norepinephrine by negative feedback.
Which is one of the most potent vasopressor drugs known?
Epinephrine
-Low dose: predominantly B1 and B2
-High dose: prefers a1 than B2
What can given to treat necrosis cause by epinephrine at the site of infection?
Phentolamine antagonista competitivo de alpha
What drug is a prodrug that administer norepinephrine and to treat orthostatic hypotension?
Droxidopa
The effect of dopamine at different concentrations.
-Low dose act on D1 causing vasodilation increasing renal blood flow and urine output.
-Intermediate dose acts on D1 and B1 increasing HR and cardiac contractibility
-High dose acts on alpha 1 increasing blood pressure and risk of arrhythmias.
Why is Fenoldopam a preferred treatment to control severe hypertension?
It only acts as an agonist on D1 peripheral receptors.
Which drugs were regulated since they are potent CNS stimulants thar are precursors of methamphetamine?
Ephedrine, Phenylpropanolamine, and Pseudoephedrine (relief nasal congestion).
Phenylephrine
Alpha 1 selective agonist
Treatment for hypotension, vasoconstriction in regional analgesia and open-angle glaucoma.
Metaraminol
Alpha 1 selective agonist
Indirectly increase release of norepinephrine. To treat hypotensive states in surgical procedures.
Midodrine
Alpha 1 selective agonist
Prodrug with active metabolite, desglymidodrine. Treat orthostatic hypotension
Midodrine, not droxidopa, increases the risk of supine hypertension.
What is the primarily treatment of Alpha 2 selective agonist?
To treat hypertension.
Clonidine
Alpha 2 Selective agonist
Lowers blood pressure even applied topically in the eye. However, it increases BP if administered IV. Can be used as a patch for a long period of time.
True or False: Clonidine can be used as diagnosis of hypertension or pheochromocytoma.
True
Most common symptoms of pheochromocytoma (PHE). Palpitations, Headaches, Episodic sweating (diaphoresis)
True or False: All drugs that activate Alpha 2 receptors can cause Xerostomia, Badycardia, and Sedation.
True
Apraclonidine
Alpha 2 selective agonist
Decrease intraocular pressure
Brimonidine
Alpha 2 selective agonist
Crosses the BBB and can produce hypotension and sedation
Guanfacine
Alpha 2 selective agonist
More selective for alpha 2 than Clonidine. To treat ADHD.
What is the first line of treatment to treat hypertension during pregnancy?
Methyldopa: a prodrug to alpha methylnorepinephrine
Tizanidine
Centrally acting alpha 2 agonist. Relaja músculos.
Dexmedetomidine
Centrally acting alpha 2 agonist. Used for sedation and cause no respiratory depression.
What are the therapeutic applications of Isoproterenol?
-asthma inhibits antigen-induced release of histamine
-Emergency stimulation of the heart
What are the effects of the two stereoisomers of Dobutamine?
- (-) isomer acts as an alpha 1 agonist and a weak beta 1 agonist (inotropism)
- (+) isomer acts as an alpha 1 antagonist and a potent beta 1 agonist.
What is the treatment and adverse effect of Beta 2 selective agonist?
To treat asthma and COPD but it can cause tachycardia since can stimulate B1 in the heart.
How to diagnose asthma?
Methacoline challenge
Metaproterenol
Short-acting Beta 2 selective agonist
To treat long term COPD, asthma, and acute bronchospasm. Less selective than albuterol or terbutaline, more prone to cause cardiac stimulation.
What drug has fewer side effects than albuterol and is an R-enantiomer of Albuterol?
Levalbuterol Like Albuterol, is a short-acting beta 2 selective agonist
Pirbuterol
Short acting beta 2 selective agonist
Menos potente que albuterol pero más selectivo a los pulmones
What is the difference between Salmeterol and formoterol? (Both are long acting beta 2 selective agonist)
Are agents of choice for nocturnal asthma but Salmeterol last more than 12 hours and take 30 minutes to see the effect and Formeterol last 12 hours but less time to see the effect.
Arformeterol is only for treating COPD not asthma.
What three drugs are very long acting beta 2 selective agonist?
Indacaterol, Olodaterol, and Vilanterol.
What are two Beta 3 selective agonist drugs?
Mirabegron and Vibegron.
Evita que vaya al baño.
