press above to
begin the lecture
and
install current free versions of Quicktime,
if needed, to support lecture series audio!
return to Pharmacology Table
of Contents
Table
of Contents
-
ß2 selective adrenergic
agonists
-
a-Selective
Adrenergic Agonists
-
a2
Selective
Adrenergic Agonists
-
Introduction
-
Clonidine
(Catapres)
-
Guanfacine
(Tenex)
-
Guanabenz
(Wytensin)
-
a-methyl DOPA
(Aldomet)
-
Miscellaneous
Amphetamine
-
Clinical Use of Sympathomimetic
Agents
|
-
Amphetamines
-
Adrenergic
Neuronal Blocking Drugs
-
Classification of
adrenoceptors (
a1, a2,ß1,
ß2
and D1), molecular consequences of their
activation, and their important locations.
-
Catecholamine
Metabolic Transformations
-
Pulmonary
Uptake
-
Adrenergic
and Cholinergic Effects on End Organs
-
Clinical
Uses: Sympathomimetic Drugs: a/b Adrenergic Agonists
-
Therapeutic
Uses of Indirect-Acting Adrenergic Agonists
-
Adverse
Effects: b Adrenergic Antagonists
-
a-Adrenergic
Antagonists
-
Introduction
-
a1-adrenergic
receptor antagonists
-
a2-adrenergic receptor antagonists
-
Phenoxybenzamine
(Dibenzyline)
-
Phentolamine(Regitine)
and tolazoline (Priscoline)
-
Prazosin
(Minipress) and Terazosin (Hytrin)
-
Others
-
b Adrenergic
Antagonists
-
Introduction
-
ß receptor blockers: Effects
on the heart
-
ß receptor blockers:
Antihypertensive
Effects
-
Pulmonary
Effects
-
Metabolic
Actions
-
Nonselective-ß adrenergic
receptor antagonists
-
propranolol
-
nadolol
-
timolol
-
labetalol
-
Cardioselective ß1 adrenergic
receptor antagonists
-
metoprolol
-
esmolol
-
atenolol
-
Adverse Effects of ß
adrenergic
receptor antagonists
-
Therapeutic
Uses
|
Introduction
-
Distribution of adrenergic receptor
subtypes and adrenergic receptor number are
important factors in organ or cellular responses
to adrenergic input.
-
Physiological
effects caused by sympathomimetcs are due not only to
direct effects, but also to indirect or reflex
effects.
-
Alpha receptor agonist
causes an increase in blood pressure.
-
Carotid/aortic baroreceptors
activations initiates a compensatory
reflex.
-
Sympathetic tone is
reduced (decreases heart rate)
-
Parasympathetic tone is
increased (decreases heart rate)
-
Blood pressure tends to
return to lower levels
Adrenergic
Agonists
Comparative Sympathomimetic Pharmacology
Drug
|
alpha
|
beta1
|
beta2
|
Mechanism of action
|
Peripheral resistance
|
Renal blood
flow
|
Mean arterial pressure
|
CNS stimulation
|
Epinephrine
|
|
|
|
Direct
|
+/-
|
|
|
Yes
|
Norepinephrine
(Levophed)
|
|
|
0
|
Direct
|
|
|
|
No
|
Dopamine
(Intropin)
|
|
|
|
Direct
|
|
|
|
No
|
Isoproterenol
(Isuprel)
|
0
|
|
|
Direct
|
|
|
+/-
|
Yes
|
Dobutamine
(Dobutrex)
|
0
|
|
0
|
Direct
|
NC
|
|
|
|
Ephedrine
|
|
|
|
Direct+Indirect
|
|
|
|
Yes
|
Mephentermine
(Wyamine)
|
|
|
|
Direct+Indirect
|
|
|
|
Yes
|
Amphetamines
|
|
|
|
Indirect
|
|
|
|
Yes
|
Metaraminol
(Aramine)
|
|
|
|
Indirect+direct
|
|
|
|
No
|
Phenylephrine
(Neo-Synephrine) methoxamine
(Vasoxyl)
|
|
0
|
0
|
Direct
|
|
|
|
No
|
--increased
effect; --decreased
effect
adapted from: Table 12-1
Stoelting, R.K., "Pharmacokinetics and
Pharmacodynamics of Injected and Inhaled Drugs", in
Pharmacology and Physiology in Anesthetic Practice, Lippincott-Raven Publishers, 1999, p.
260;
Hoffman, B.B and Lefkowitz, R.J,
Catecholamines, Sympathomimetic Drugs, and Adrenergic
Receptor Antagonists, In, Goodman and Gillman's The
Pharmacologial Basis of Therapeutics,(Hardman, J.G, Limbird, L.E,
Molinoff, P.B., Ruddon, R.W, and Gilman, A.G.,eds) TheMcGraw-Hill Companies, Inc.,1996, pp.199-242
Categories
of Action
Smooth Muscle Effects
-
Smooth muscle activation,
including activation of blood vessel vasculature
(skin, kidney).
-
Activation of glands
(salivary and sweat).
-
Smooth muscle inhibition,
including inhibition of smooth muscle of the gut,
bronchioles, and skeletal muscle vascular smooth
muscle.
Cardiac Effects
Metabolic Effects
Endocrine
Central
Nervous System Effects
-
Respiratory stimulation
-
CNS stimulation
-
Appetite attenuation
Presynaptic Effects
Hoffman, B.B and Lefkowitz, R.J,
Catecholamines, Sympathomimetic Drugs, and Adrenergic
Receptor Antagonists, In, Goodman and Gillman's The
Pharmacologial Basis of Therapeutics,(Hardman, J.G, Limbird, L.E,
Molinoff, P.B., Ruddon, R.W, and Gilman, A.G.,eds) TheMcGraw-Hill Companies, Inc.,1996, pp.199-242
return to Table of
Contents
press the purple
arrow below (right) to go to the next page
|