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Transcript
Neurotransmitters

Pharm Pearl:
The peripheral nervous system (PNS) employs
3 neurotransmitters
• Acetylcholine
• Norepinephrine
• Epinephrine
Any given junction in the PNS
uses only ONE of these substances
2
Transmitter Recap

Acetycholine – employed at most junctions of the PNS
• All preganglion neurons of PNS
• All preganglion neurons of the SNS
• All postganglionic neurons of PNS
• All motor neurons to skeletal muscles
• Most postganglionic neurons of the SNS that
go to sweat glands
3
Transmitter Recap

Norepinephrine – released by practically all
postganglionic neurons of the SNS (exception –
sweat glands)
Epinephrine – major neurotransmitter released by the
adrenal medulla. The adrenal medulla also releases
some norepinephrine.
4
Adrenergic Agonists

* Produce their effects by activating adrenergic
receptors
* Sympathomimetic
* Broad spectrum of applications
• CHF
• Asthma
• Preterm labor
Mechanisms of Adrenergic
Receptor Activation

* Direct receptor binding
* Promotion of norepinephrine (NE) release
* Inhibition of NE reuptake
* Inhibition of NE inactivation
Overview of
Adrenergic Agonists

* Therapeutic applications and adverse effects
of adrenergic receptor activation
* Properties of representative adrenergic
agonists
* Discussion of adrenergic agonists in other
chapters
Overview of the
Adrenergic Agonists

Catecholamines
Noncatecholamines
• Cannot be used orally
• Brief duration of action
• Cannot cross the BBB
(polar molecules)
• Can be given orally
• Metabolized slowly by MAO –
longer half-life
• More able to cross the BBB
Mort & Merv:
the story of selectivity
Receptor
specificity
• Most drugs in chapter
• Peripherally acting
sympathomimetic
• Direct receptor activation
• Amphetamine, cocaine
• Indirect acting sympathomimetic
• Ephedrine
• Direct receptor activation and
promotion of NE release
Receptor Specificity
Terbutaline
(Bricanyl)
Isoproterenol
(Isuprel)
Epinephrine
• Beta2 only
•Beta1 and beta2
•Alpha1 and alpha2
•Beta1 and beta2
Therapeutic Applications
Adrenergic Agonists

Clinical applications of alpha1
Two responses for therapeutic use
•
Vasoconstriction (most common use)
•
•
•
•
Blood vessels
Skin
Viscera
Mucous membranes
 Mydriasis
Therapeutic Applications and Adverse
Effects of Adrenergic Receptor Activation

* Drugs capable of activating alpha1 receptors
•
•
•
•
•
Epinephrine
Norepinephrine (Levophed)
Phenylephrine (Neosynephrine)
Ephedrine
Dopamine
Therapeutic Applications and Adverse
Effects of Adrenergic Receptor Activation

Therapeutic applications of alpha1 activation
* Hemostasis
•
Arrest bleeding via vasoconstriction
* Nasal decongestion
•
Mucosal vasoconstriction
* Adjunct to local anesthesia
•
Delays absorption of local anesthetic
* Elevation of blood pressure
•
Vasoconstriction
 Mydriasis
•
Radial muscle of the iris
Therapeutic Applications and Adverse
Effects of Adrenergic Receptor Activation

Adverse effects of alpha1 activation
* Hypertension
•
Widespread vasoconstriction
* Necrosis
•
Treatment with alpha1 blocking agent
 Bradycardia
•
Response to vasoconstriction and elevated BP
Clinical Consequences of Alpha2
Activation

* Alpha2 receptors in periphery
• Located presynaptically
• Regulate transmitter release
• Activation inhibits NE release
* Alpha2 in CNS
• Reduction of sympathetic outflow to heart and
blood vessels
• Relief of severe pain
Clinical Consequences of Beta1 Activation

Therapeutic applications of beta1 activation
* Cardiac arrest
• Not preferred drug of choice
* Heart failure
• Positive inotropic effect
* Shock
• Positive inotropic effect; increases heart rate
Atrioventricular heart block
• Enhances impulse conduction through AV
Clinical Consequences of Beta1
Activation

* Adverse effects of beta1 activation
• Altered heart rate or rhythm
- Tachycardias or dysrhythmias
• Angina pectoris
- Increased cardiac oxygen demand
Clinical Consequences of Beta2 Activation

* Therapeutic applications of beta2 activation
• Asthma
• Delay of preterm labor
* Adverse effects of beta2 activation
• Hyperglycemia
• Tremor
Clinical Consequences of
Dopamine Receptor Activation

* Activation of peripheral dopamine receptors causes
dilation of the vasculature of the kidneys
Multiple Receptor Activation:
Treatment of Anaphylactic Shock

* Pathophysiology of anaphylaxis
• Severe allergic response
• Hypotension, bronchoconstriction, edema of the glottis
* Treatment
• Epinephrine, injected IM, is the treatment of choice for
anaphylactic shock
Adrenergic Agonists

*
*
*
*
*
*
*
*
Epinephrine
Norepinephrine
Isoproterenol
Dopamine
Dobutamine
Phenylephrine (Neo-synephrine)
Terbutaline
Ephedrine
Epinephrine

* Therapeutic uses
•
•
•
•
•
•
•
•
Delay absorption of local anesthetic
Control superficial bleeding
Elevate blood pressure
Mydriasis during ophthalmologic procedures
Overcome AV block
Restore cardiac function in arrest
Bronchial dilation in asthma
Treatment of choice for anaphylactic shock
Epinephrine

* Pharmacokinetics
• Absorption
• Inactivation
* Adverse effects
•
•
•
•
•
Hypertensive crisis
Dysrhythmias
Angina pectoris
Necrosis following extravasation
Hyperglycemia
Epinephrine

* Drug interactions
•
•
•
•
•
MAO inhibitors
Tricyclic antidepressants
General anesthetics
Alpha-adrenergic blocking agents
Beta-adrenergic blocking agents
Epinephrine

* Preparations, dosage, & administration








EpiPen (1:1000 or 1:2000)
IV (monitor closely) (1:10,000)
IM
SubQ
Intracardiac
Intraspinal
Inhalation
Topical
Norepinephrine

* Receptor specificity
• Alpha1
• Alpha2
• Beta1
* Chemical classification
• Catecholamine
* Therapeutic uses
• Hypotensive states
• Cardiac arrest
Norepinephrine

* Differs from epinephrine – does not activate
beta2 receptors
• Does not promote hyperglycemia
* Cannot be given orally (MAO and COMT)
* Necrosis with extravasation
* Drug interactions
• MAOI, TCA, general anesthetics, adrenergic
blocking agents
Isoproterenol

* Receptor specificity: beta1 and beta2
* Chemical classification: catecholamine
* Therapeutic uses
• Cardiovascular
- AV heart block, arrest
• Asthma
- Bronchodilation – not used anymore
• Bronchospasm
- During anesthesia
Isoproterenol

* Adverse effects
• Fewer than those of NE or epinephrine (doesn’t
activate alpha-adrenergic receptors)
• Tachydysrhythmias and angina pectoris
• Hyperglycemia in diabetes patients
* Drug interactions
• MAOI, TCA, beta-adrenergic blockers
* Preparations and administration
• IV, IM, and intracardiac injections
Dopamine

* Receptor specificity
• Low therapeutic dose – dopamine
• Moderate therapeutic dose – dopamine and beta1
• Very high dose – apha1, beta1, and dopamine
Dopamine

Therapeutic uses
* Shock
•
•
Increases cardiac output
Increases renal perfusion
* Heart failure
•
Increases myocardial contractility
* Acute renal failure
•
•
Was used to preserve renal function with ARF
Early ARF – failed to protect renal function, shorten
stays, or reduce need for renal transplant
Dopamine

* Adverse effects
• Tachycardia, dysrhythmias, anginal pain
• Necrosis with extravasation
* Drug interactions
• MAOI, TCA, certain general anesthetics, diuretics
* Preparations, dosage, and administration
• Preparations: dispensed in aqueous solutions
• Dosage: must be diluted
• Administration: administered by IV
Dobutamine

Receptor specificity: beta
*
1
* Chemical classification: catecholamine
* Actions and uses
• CHF
* Adverse effects
• Tachycardia
* Drug interactions
• MAOI, TCA, certain general anesthetics
* Preparations, dosage, and administration
• Continuous IV infusion
Phenylephrine

* Receptor specificity
• Alpha1
* Chemical classification
 Noncatecholamine
* Therapeutic uses
•
•
•
•
Reduce nasal congestion (locally)
Elevate blood pressure (parenterally)
Dilate pupils (eye drops)
Local anesthetic (delay absorption)
Terbutaline

* Receptor specificity: beta2
* Chemical classification: noncatecholamine
* Therapeutic uses
• Asthma (selective for beta2)
- Replaced isoproterenol in treatment
• Delay of preterm labor
- Relaxes uterine smooth muscle
- Another drug (ritodrine) now preferred
* Adverse effects
- Minimal at therapeutic doses
- Tremor most common; also tachycardia
What’s he got to
do with Pharm?

Anybody ever taken ephedrine?

Are you sure?

Ephedrine

* Receptor specificity: alpha1, alpha2, beta2
* Chemical classification: noncatecholamine
* Therapeutic uses
• Nasal congestion
• Other uses
* Adverse effects
• HTN, dysrhythmias, angina, hyperglycemia, insomnia
(crosses BBB)
Good thing gone bad…

Questions
