Reasons to put vasoconstrictors in LA agents

By neutralizing the vasodilatation effect of LA agents

1. to slow absorption & reduce toxicity
2. it reduces amount of LA required
3. to prolong duration of action
4. it increase the efficiency of anaesthetic solution (profound anaesthesia)
5. to reduce bleeding

Vasoconstrictor most commonly used in dentistry can be divided into

(1) Pyrocatechin derivative
adrenaline & noradrenaline
(2) Benzol derivative
Levonordefrin
(3) Phenol derivative
Phenyl ephrine
(4) Octapeptide derivative
Fellypressin

ADENALINE
Tartrate synthetic
HCl animal origin
Site of action : Act on adrenergic (Sympathetic) receptor ()
The most potent vasoconstrictor,commonly used vasoconstrictor agent add to dental LA
cartridges.
concentration from 1:50,000 - 1:250,000
(1) concentration greater than 1:50,000 unnecessary
(2) optimal concentration 1:200,000
(3) dental use 1:50,000, 1:80,000, 1:100,000
It is probabaly unwise to use 0.5 mg at one time.
General effects similar to those resulting from stimulation of adrenergic nerve endings
but ultimate action is chiefly on effector cells.
Stimulates both & receptors. Greater affinity with receptors.
Blood vessels - principally present in vessels supplying (skin, mucous membrane,
kindney). Stimulation of receptor causes vasoconstriction of these blood vessels. Then
decrease epinephrine in the site previously stimulated ( receptors) will lead to secondary
vasodilation due to 2 receptor present. (rebound effect- vasodilatation)

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CVS
Main effect is to increase the stroke volume, rate and cardiac output.
It increase the incidence of dysrhythmias - through 1 stimulation increase the risk of
premature venticular contraction & various teachycardia.
Increase systolic BP but diastolic BP still remain in position or decrease.
cerebral & pulmonary arteries constricted, BP in coronary arteries rises, therefore Angina
pectoris may be precipitated in patient with coronary dis: because of augmentation of cardiac
work or on top of narrow vessels.

Respiration System
Bronchi are relaxed (2) vasodilator of smooth muscle of bronchioles.
Depth of respiration slightly increased irregular breathing sometimes seen.

Renal Blood Flow

Decreases because of constriction of renal vessel.
Urine excretion decreases

CNS
Not a stimulant, anxiety, restlessness from mild cerebral stimulation.
Excess dose - toxicity - CNS effect ---> throbbing headache, palpitation.

Miscelleneous effect
blood sugar increase - due to
1. glycogenolysis in liver & muscle (skeletal)
2. anti-insulin effect
3. lipolysis
rise in metabolic rate
dilatation of pupil

Metabolism

Degradation :
mostly conjugation with glycuronic + sulpuric acid & excreted in urine.
smaller portion is oxidized by monoamine oxidase + inactivated by d-methyl transferase.

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Dosage
First dose- adrenaline should not exceed 0.5 mg (0.5 ml of 1:1000 solution)

Dental Use
0.2 mg safe maximum dose for healthy patient
0.04 mg for patient who have organic heart disease

1:200,000 = 0.005 mg/ml - 5 g/ml

1:100,000 = 0.01 mg/ml - 10 g/ml
1:80,000 = 0.0125 mg/ml - 12.5 g/ml
1:50,000 = 0.02 mg/ml - 20 g/ml

Cautions

Adverse reactions are most likely to occur follwing IV injection especially in patient with:
1. diabetes,
2. heart disease
3. thyrotoxicosis
4. epilepsy
5. those receiving halogenated anesthetics :
cyclopropane
halothane
trilene
chloroform
6. drug therapy involving tricyclics or adrenargic neurone blockers.

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Affinity with receptors with receptor
Adrenalins 1/2 +++ +++
Noradrenaline 1 +++ /2 + ++

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