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Glossary of Adrenolytic Agents

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What are adrenolytic agents?
Alpha or Beta blockers
What are the alpha 1 selective, reversible agents?
The 5 member "zosin" family and their "zole" friend.
Prazosin
Terasozin
Doxasozin
Tamsulosin
Alfuzosin
Dapiprazole
What is the alpha,non-selective, reversible agent?
Phentolamine
What is the alpha non-selective, and IRREVERSIBLE agent?
Phenoxybenzamine
What is the MOA of alpha antagonists (blockers)?
Block the alpha receptor, thereby preventing the binding of NE or EPI
How does an alpha blocker work on vascular smooth muscle cells?
BLocks alpha 1 --> no A1 activity --> vasodilation
Alpha antagonists

Therapeutic Uses
Orthostatic hypotension
What alpha antagonists are used to treat HTN?
Prazosin
Terazosin
Doxazosin
What alpha antagonist agents are not indicated for tx of HTN?
Tamsulosin and Alfuzosin
What alpha antagonists are used to treat Pheochromocytoma?
The "PH" drugs
Phentolamine
Phenoxybenzamine
What alpha blockers are used to treat BPH?
Terazosin
Doxasozin
Tamsulosin
Alfuzosin
How does an alpha blocker help BPH?
Prostate --> blocking alpha 1 --> relaxes smooth muscle in base of bladder and prostate --> improved urine flow
What is the advantage of using Tamsulosin for the treatment of BPH?
Less hypotension and has greater affinity for alpha 1A receptors than other subtypes.
What alpha blocker is used to treat Raynaud's disease?
Prazosin
Why is constriction of the veins so important?
Returns blood to the heart
Why does alpha blockers cause orthostatic hypotension?
Standup --> decreased BP --> baroreceptor --> CNS --> block alpha 1 --> no vasoconstriction --> blood pools in veins --> doesnt return to heart --> Orthostatic hypotension and syncope
Alpha antagonists

Adverse effects?
Reflex tachycardia
Nasal congestion
Salt and water retention
Inhibition of ejaculation
headache, weakness, dizziness
How does alpha blockers cause reflex tachycardia?
Block alpha 1 --> decreased BP --> baroreceptor --> reflex tachycardia
How does alpha blockers cause nasal congestion?
Blocks alpha 1 in the nasal mucosa --> nasal congestion
How does alpha blockers cause inhibition of ejaculation?
Block alpha 1 on the smooth muscle of the prostate, seminal vesicles, and vas deferens
Beta antagonist agents

Non-selective, competetive, and reversible
The "olol's are beta blockers"
Propranolol
Nadolol
Timolol
Pindolol
Carteolol
Levobunolol
Beta antagonist agents

Beta 1 selective, competetive, and reversible
There is a "BEAM" of B1 selective agents.
Metaprolol
Atenolol
Acebutolol
Betaxolol
Levobetaxolol
Bisoprolol
Esmolol
Beta antagonist MOA
Bind to, but do not activate, beta adrenergic receptors
Beta antagonist

Therapeutic Uses
Cardiovascular diseases
--HTN
--Ischemia
--Arrhythmias
--MI
--HF
Beta blockers

Therapeutic Uses
Pheochromocytoma--in conjunction with an alpha blocker
What may happen if you administer propranolol without an alpha blocker in treating pheochromocytoma?
Unopposed vasoconstriction and increased BP
Beta blockers

Therapeutic Uses?
OAG
Migraine
Essential tremor
How are beta blockers useful in treating migraines?
--Prophylactic treatment
--Reduce frequency, severity, and duration of migraine attacks
Precise mechanism unknown
Beta blockers

Cardiac adverse effects?
Block Beta 1 --> bradycardia, AV block, decrease contractile force --> hypotension --> heart failure
Beta blockers

CNS adverse effects?
Nightmares, lassitude, mental depression, insomnia
WIth lipid soluable agents (Propranolol, metoprolol)
Beta blockers

Adverse effects?
NVD
Sexual dysfunction
Increased trigylercides, decreased HDL-C
Bronchospasm
Unopposed vasoconstriction
Rebound hypertension
Both non-selective and beta 1 selective blockers are contraindicated in asthma. Why?
The selectivity of beta 1 selective blockers may be lost at higher doses
How can beta blockers cause rebound hyptertension?
Chronic therapy up regulates beta 1 receptors --> abrupt withdrawl from beta blocker --> rebound hyptertension, nervousness, tachycardia, angina

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