Pharmacology Exam 1---Adrenergic Pharmacology

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Sympathomimetics-- Catecholamines

Back 1

Epinephrine (inhibits effects of alpha and beta)
Norephrine
Dopamine

Front 2

Non-catecholamine ALPHA-AGONISTS

Back 2

Amphetamine
Methamphetamine
Ephedrine
Phenylephrine
Clonidine

Front 3

Non-catecholamine-- Beta-adrenoceptor agonists

Back 3

Terbutaline
Albuterol
Salmeterol
Dobutamine

Front 4

Inhibitors of reuptake

Back 4

Cocaine
Tricyclic antidepressants

Front 5

Adrenergic receptor anatagonist ALPHA BLOCKERS

Back 5

Prazosin
Doxazosin
Terazosin

Front 6

Adrenergic receptor anatagonist-- BETA BLOCKER

Back 6

Propranolol
Metoprolol
Atenolol
Esmolol

Front 7

Alpha and Beta antagonist

Back 7

Labetalol
Carvedilol

Front 8

Adrenergic Transmission

Back 8

regulate function of heart and blood vessels and play a role in normal functioning of visceral smooth muscle and grandular tissue.
synthesize, store, and release catecholamines

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Catecholamine

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chemical classification of amine molecules containing a benzene ring of OH substitution at 3 and 4 positions.

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Norepinephrine

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peripheral nervous system
released from post-ganglionic sympathetic nerve fibers
negative feedback -- acts on presynaptic alpha 2 receptor (more relaxed, react) shut down production

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Epinephrine Release Location

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released from chromaffin cells of the adrenal medulla but NOT peripheral nerve endings
released from neurons and act as neurotransmitters (like dopamine)

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Synthesis of Catecholamines

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Derived frim tyrosine
tyrosine converted by enzymes to DOPA and then to dopamime
Dopamine is then converted to norepinephrine
in the granule -- NE AND ATP AND CHROMOGRAIN
in the adrenal gland and CNS -- NE convert to epinephrine

increase neuronal activity increases hydroxylase
increased adrenal gland cortical hormones increase hydroxylase and EPI concentration in medullary cells

NE and EPI synthesis is END PRODUCT INHIBITION. Negative feedback.

Front 13

Fate of transmitter

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activate a1, a2, or b1 adrenoceptor. Synaptic NE stimulates presynaptic a2 and act as negative feedback to inhibit release of transmitter

60-90% is taken back to the presynaptic terminal

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Adrenal Receptors

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a1
a2
b1
b2
b3

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a1-Adrenoceptors

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located postjunctionally at most neuroeffector synapse.
creates an excitatory response and some inhihition on gi and urinary smooth muscles

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a2-- Adrenoceptor

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found om postjunctional membrane of many autonomic end organs and is identical to a1.
also fround on prejunctional membrane and act a negative feedback to prevent excessive release of NE

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B1 -- Adrenoceptor

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found at heart and juxtaglomerular apparatus of kidney
stimulated by NE
Responsible for increasing heart rate, conduction, and crontractile force and release of renin from JG cells
innervated!!!

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b2-- Adrenoceptor

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vascular vasodilation and consequent reduction of blood pressure, relaxation of smooth muscle of bronchial tree, inhibition of GI and urinary tract smooth muscle, and relaxation of gravid uterus

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b3-- Adrenoceptor

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found on fat cells amd contribute to metabolic control mechanisms

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Epinephrine

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acts on ALL a- and b-adrenoceptors.
primary catecholamine
given parentarelly or by inhalation

increases heart rate ad contractility (b1)
relax bronchial smooth muscle for asthma and bronchospasm during anaphylaftic shock (b2)

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Epinephrine for metabolic effects

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1) increases plasma glucose by breakdown of liver glycogen
2) inhibits synthesis of glycogen
3) stimulates gluconeogensis
4) breaks down fats to fatty acids

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Norepinephrine

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acts on all a- and b-adrenoceptors
parenterally given
bolus injection -- increase blood pressure from vasoconstriction and increased cardio output

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Dopamine

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in peripheral nervous system-- metabolic precursor in form of NE and EPI
in CNS-- important neurotransmitter (extrapyramidal motoro system)
CNS defect in dopaminergic mechaniss --- Parkinson disease

renal vasodilation in kidney
can increase blood pressure and cardiac output

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Amphetamine and Methamphetamine

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temporary elevation of mood appetite suppression
Highly toxic and can be lethal
ED50 increases but LD50 remains the same
Paranoid Schizophrenia
intense vasoconstriction of CNS vessels.

can be used to treat hyperkinetics in children and narcolepsy

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Methylphenidate

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mild CNS stimulant related to amphetamine.
in large doses-- CNS excitation and convulsions

Primary use-- ADHD

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Ephedrine

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oldest drug known to man
half action to receptors and half action to release NE from neuronal stores

treatment for Bronchial asthma, ear and nasal decongestion.
short lasting mydriasis w/o cycloplegia

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Clonidine

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causes neurons postsynaptic alpha 2 receptor to to stop firing-- lower blood pressure, decrease pain, muscle relaxation

Front 28

Terbutaline

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b2 agnostic
prevents premature child birth
modification of metaproterenol (higher incidence of cardiac effects)

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Albuterol

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treatment of asthma with indications similar to Terbutaline but is long acting with fewer cardiac effects

Front 30

Salmeterol

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long acting b2, treats bronchial asthma

Front 31

Ritodrine

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relax smooth muscle of uterus and delay premature labor
possible cardiac effects
orally is the preferred route but is mainly given via IV

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Dobutamine

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B1 AGONISTC (does not stimulate dopamine receptors)
increases cardiac output w/o vasoconstriction
used for organic heart hpdiseasr or cardiac surgery

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Cocaine

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local anesthetic and potent inhibitor of NE reuptake 1.

Front 34

Tricyclic antidepressants

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potental inhibitors of catecholamine reuptake into adrenergic nerve terminals
treats pathological depression

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alpha--Adrenoceptor Blockers

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reduction of systemic blood pressure
side effects: postural hypotension, reflex tachycardia, nasal congestion, and failure of ejaculation

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Beta1-adrenoceptor blockade

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affect innervation to heart and sympathetic control of renin release from JG apparatus of kidney

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Prazosin

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a1-Adrenoreceptor
does not produce large reflex tachycardia seen with other alpha - Adrenoceptor antagonist.

treatment for hypertensive patients
should be slowly administered

Front 38

Terazosin and Doxazosin

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prazosin like drug with longer life which permits once a day dosing.
treats benign prostatic hypertrophy

Front 39

Propranolol

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blocks both b1 and b2
NONSELECTIVE
used to treat cardiac arrhythmias
effective antihypertensive drug

Front 40

Metoprolol

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primarily b-adrenoceptors antagonist
CARDIOSELECTIVE
reduces plasma renin (b1), has less metabolic and bronchial effect

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Atenolol

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similar to Metoprolol
longer half-life and adminstered less frequently
less CNS side effects
should not5 be given to patients with renal disease

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Esmolol

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CARDIOSELECTIVE
short half-life given intravenously
used for acute emergency control of ventricular heart rate in patients with atrial fibrillation or atrial flutter

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Labetalol

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selective alpha blocker and nonselective b-antagonist
effective antihypertensive agent that decreases total peripheral resistance with little reflex on heart rate or cardiac output

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Carvedilol

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similar to labetalol
FREE RADICAL SCAVENGER
protect heart cells from damage
treats congestive heart failure

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Reasons to use Sympathomimetics

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Hemostasis
Nasal decongedtion
Use with local anesthetics
Hyper- and hypotension
Cardiac Stimulation
Bronchodilation
Allergic reaction
Narcolepsy
Behavioral Disorders
Uterine Motility
Opioid withdrawal

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Reasons to use Adrenergic Blockers

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Hypertension
Glaucoma
Angina
Post-infarction prophylaxis
Congestivrpe heart failure
Migraine
Stage fright
Cardiac Arrhythmias
Essential tremor
Pheochromocytoma
Benign prostatic hypertrophy
Hyperthyroidism