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68 Cards in this Set

  • Front
  • Back

Endogenous adrenergic neurotrasmitters belong to this chemical group

Catecholamines

How does termination of the action of NE happen

1. Diffusion into the circulation


2. Enzymatic biotransformation


3. Re-uptake into the varicosities

Enzymatic biotransformation involves the action of

Monoamine oxidase


Catechol-amine methyl transferase

Is a mitochondrial enzyme

Monoamine oxidase

Found in soluble fraction of thr cells

Cathechol-amine amine methyl transferase

A prototype sdrenergic stimulant

Epinephrine

5 major effects of epinephrine

Peripheral excitatory effects - alpha


Peripheral inhibitory - beta


Cardioexcitatory effect - beta


Metabolic effects - alpha and beta


CNS effects

What are the peripheral excitatory effects

Vasoconstriction


Mydriasis


Mucoid and thick salivation

What are the peripheral inhibitory effects

Vasodilation


Relaxation of gut smooth muscles


Bronchodilation

What are the cardioexcitatory effects

Increased heart rate


Increased myocardial contraction

What are the metabolic effects

Hyperglycemia


Hyperlipidemia


Increased blood lactic acid

What are the CNS effects

Transient respiratory stimulation


Wakefulness


Anxiety

B receptors chiefly in the heart

B1

B receptors in blood vessels, liver, bronchi

B2

Alpha receptors present in post synaptic fibers

A1

Alpha receptors present in both pre and post synaptic fibers

A2

Have purely direct action or mixed action on the adrenergic system

Sympathomimetic agents

Give examples of endogenous catecholamines

Epinephrine


Norepinephrine

Stimulates both alpha and beta receptors

Epinephrine

Mainly an alpha stimulant

Noepinephrine

Pure alpha stimulants

Phenylephrine


Methoxamine


Phenylpropanolamine

Specific a2 adrenergic stimulants

Clonidine


Oxymethazoline


Xylazine


Mecetomidine


Detomidine

Pure beta stimulants

Isoproterenol


Methoxyphenamine

Specific b2 adrenergic stimulants

Clenbuterol


Salbutamol


Metaproterenol


Albuterol


Terbulatine

Act selectively on b1 receptors, used for cardiac stimulation

Dobutamine

Acts directly on b1 receptors in the heart and on specific dopamine receptors in the CNS

Dopamine

Examples of other directly acting sympathomimetics

Propylhexedrine


Tuaminoheptane


Naphazolene


Tetrahydrozoline


Phenylpropanolamine

Used in nasal inhalers

Propylhexedrine


Tuaminoheptane

Equal in potency to ephedrine but with less CNS action


Used as oral treatment for nasal and sinus congestion

Phenylpropanolamine

Produce their effects by increasing the discharge of NE from varicosities of nerve terminals

Indirectly acting adrenergic agents

Readily enters the CNS and stimulates mood and alertness


Eefects can be mediated by release of catecholamines


Large doses can induce hallucination

Amphetamine

Large doses of amphetamine can cause

Hallucination


Violent behaviour


Psychoses in man

Similar to amphetamine but with greater central than peripheral effects

Metamphetamine

Has an action resembling that of ephedrine but lacks CNS stimulant activity


Used to treat hypotensive state but principally used as mydriatic

Hydroxyamphetamine

Replace NE from the vesicles and at the same time stimulate adrenergic receptors directly

Dual acting adrenergic stimulants

Occurs naturally in plants but is now synthetically produced


Resistant to effect of MAO and COMT


enters the brain


Affects alpha and beta receptors


Commonly used as bronchodilator

Ephedrine

Stereoisomer of ephedrine

Pseudoephedrine

Has both direct and indirect actions


Overall effect is similar to norepi but much less potent


Principal use is to treat hypotensive state in human

Metaraminol

Pharmacological effects of sympathomimetic agents to vascular smooth muscles

Vasoconstriction due to alpha receptor stimulation


Vasodilation due to beta receptor stimulation


Pharmacological effects of sympathomimetic agents to heart

Increased force of myocardial contraction


Increased heart rate


Excessive stimulation that lead to arrythmia

Pharmacological effects of sympathomimetic agents to blood pressure

Decrease or increase of bp

Pharmacological effects of sympathomimetic agents to bronchioles

Bronchodilation


Pharmacological effects of sympathomimetic agents to spleen

Contraction of splenic capsule


Extrusion of blood

Pharmacological effects of sympathomimetic agents to gut

Inhibition of motility


Increased sphincter tone

Pharmacological effects of sympathomimetic agents to urinary bladder

Mild relaxation

Pharmacological effects of sympathomimetic agents to uterus

Cat - relaxation in non gravid uterus but contraction in gravid uterus

When b2 agonists are used to relax gravid uterus in cows it is called

Tocolytics

Pharmacological effects of sympathomimetic agents to eyes

Mydriasis

Pharmacological effects of sympathomimetic agents to exocrine glands

Secretion of thick mucoid saliva


Sweating in horse with adrenaline

Clinical uses of sympathomimetic agents

1. Adjunct to local anesthesia


2. As hemostatic


3. As mydriatic


4. In anaphylactic reactions


5. As bronchodilator


6. Treatment of local skin allergy


7. As decongestant


8. For diagnosis of COPD in horses


9. Treatment of cardiac arrest


10. Treatment of hypertensive conditions

It causes vasoconstriction and prolongs the effect of local anesthetic

Epinephrine

Drug of choice for anaphylactic reactions because it counteracts hypotension and bronchospasm

Epinephrine

Best treatment for bronchial asthma

Specific b2 adrenergic agonist

Treatment for COPD

Isoproterenol (IV)

When infused slowly it causes vasodilation

Dopamine

Alpha adrenergic blockers

Phenoxybezamine


Dibenamine


Phentolamine


Prazosin


Ergot alkaloids


Phenothiazine, butyrophenone tranquilizer


Idazoxan, tolazoline, atipamezole, yohimbine

Pharmacological effects of alpha adrenergic blockers

1. Little effect on resting blood pressure


2. Tendency for postural hypotension


3. Little effect on GIT

Clinical uses of alpha adrenergic blockers

1. Used in reversing compensatory vasoconstriction


2. Used to overcome effect of excessive epinephrine


Treatment best for shock

Corticosteroids

Used to produce sedation in domestic animal

Xylazine


Medetomidine

Pharmacological effect of beta-blockers

1. Cause cardiac depression


2. Cause bronchoconstriction


Beta adrenergic blocking agents

Dichloroisoproterenol


Propanolol


Timolol


Alprenollol


Pindolol


Nadalol


Sutatol


Metoprolol


Butoxamine

Clinical uses of beta blockers

1. Treatment of hypertension


2. Reversing digitalis induced cardiac arrythmias


3. Treat obstructive cardiomyopathy


4. Block effect of excessive epinephrine

Interference with NE release from vesicles by blocking of nerve action by

Bretylium


Guanethidine

Interference with NE re-uptake into varicosities by

Imipramine


Cocaine

Interference with NE re-uptake into the dense core vesicles by

Reserpine


Guanithidine

Synthesis of false transmitter by ____ & ________ cause hypotension

a-methyl-DOPA


octamine

Destruction of adrenergic fibers by _______ produces decreased sympathetic functiom

6-hydroxydopamine