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What nervous system do adrenergic agonist drugs mimic?
How are adrenergic receptors on cells activated? (direct vs indirect)
SNS.
- Direct: drug binds w/ receptor on cell
- Indirect: Promotes cell to release noreepinephrine (NE) --> activates adrenergic receptor.
- Blocks NE reuptake
- Inhibit inactivation of NE
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Categories of adrenergic agonist drugs:
Catecholamines (epinephrine)
-Why can one not take orally?
-Does it cross the BBB?
-Short/long duration?
NO oral admin b/c: rapid inactivation is caused by liver enzymes and intestine.
No, b/c it contains POLAR ions.
Short duration
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Categories of adrenergic agonist drugs:
Non-Catecholamines (albuteral)
-Why can one take orally?
-shorter or long duration?
Orally is OK b/c it is NOT inactivated by liver & GI enzymes.
-Longer duration
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What are the 4 adrenergic agonist receptors and what do they control?
- 1) alpha 1: BV, eyes, heart
- 2) alpha 2: CNS, & PNS
- 3) beta 1: heart
- 4) beta 2: lungs, uterus
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Alpha adrenergic receptors.
Alpha 1: where are receptors located & how does it function?
Adverse effects due to vasoconstriction?
Receptors in SMOOTH MUSCLE (opens ion channels & allows Ca to enter).
Vasoconstriction --> INcreased BP --> slows absorption of local anesthetic --> DEcreases nasal constriction --> dilates pupils.
Adverse effects: necrosis, HTN -->barrel receptor activation --> bradycardia.
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Alpha adrenergic receptors.
Alpha 2: where receptors located & function?
IN CNS, what does receptor activation cause?
Located in BV & NS. In PNS, located in peripheral to prevent NE release.
In CNS, DEcrease in SNS action on heart and BV --> DEcrease activity --> DEcrease pain.
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Beta adrenergic receptors.
Beta 1:
location&function?
Benefits? (5)
Adverse effects? (3)
- Location: receptors in cardiac muscles.
- Function: INcreases contraction, INcreases HR, INcrease speed of electrical conduction, INcrease renin production, INcrease BP --> INcrease cardiac output.
Benefits: cardiac function, HR, shock, AV heart block, cardiac arrest.
Adverse effects: tachycardia, dysrhythmia, angina in Pt w/ CAD.
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Beta adrenergic receptors.
Beta 2: functions? (3)
Relaxes? (3)
*Beta 3: No drug association, NO receptors.
- 1) Bronchodilation
- 2) Vasodilation
- 3) INc. glycogenolysis & gluconeogenisis in liver & DEcreases pancreatic insulin secretion.
- Relaxes:
- 1) Smooth muscle in uterus.
- 2) urinary bladder
- 3) GI tract
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Adrenergic drugs.
*Can be selective OR non-selective in which receptors are stimulated.
Is epinephrine sel/non-sel?
-Acts on which adrenergic receptors? (3)
Is albuterol sel/non-sel?
-Acts on which adrenergic receptors? (1)
- Epi. is NON-selective.
- Acts on alpha & beta, and beta 2 receptors.
- Alubuterol is Selective.
- Acts on beta 2 receptors.
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