Dr.

Sarah Adil

lecture 2.............................................................................................Clinical pharmacology

Vasoconstrictors Of Local Anaesthetics
Definition:
❖ Vasoconstrictors: are the chemical agents or adjuncts added to local anaesthetic
solutions to a. oppose vasodilatation caused by these agents b. achieve homeostasis.
❖ The combination of LA with vasoconstrictor should not be applied to the end organs
such as the fingers, nose and toes, because it may cause severe vasoconstriction and
cut the blood supply which will lead to gangrene of the finger.
Actions
The addition of a vasoconstrictor to a LA agent causes constriction of blood vessels and
thereby controls tissue perfusion.
The net effects caused by addition of vasoconstrictors to local anesthetic agents are:
1. It decreases the blood flow to the site of injection, because of vasoconstriction.
2. It decreases the rate of absorption of LA agent into cardiovascular system.
3. . It lowers the plasma level of local anesthetic agent decreasing the risk of
systemic toxicity of LA agent.
4. Higher volumes of LA agent remain in and around the nerve for longer periods
increasing the duration of action of most LA agents
5. It decreases bleeding at the site of injection because of decreased perfusion. This is
useful when increased bleeding is expected during a surgical procedure

Classification
• Several types of vasoconstrictors are existing for clinical use in dentistry today.
• All of them except felypressin are Sympathomimetics amines, that stimulate or exert
their action directly on the adrenergic receptors.
• Example of vasoconstrictors

1. Adrenaline = Epinephrine 2. Noradrenalin = Norepinephrine 3. Felypressin

Adrenergic receptors
1. α receptors
Activation of receptors results in vasoconstriction of smooth muscle.
2. β Receptors
β receptors are subcategorized further into β1, β2 and β3 receptors.

a. β1 receptors are found in the heart and small intestine; and are responsible for:

i. cardiac stimulation: HR and the strength of contraction

ii. renin release.
 Dr. Sarah Adil

lecture 2.............................................................................................Clinical pharmacology

b. β2 receptors are found in bronchi, vascular beds, and uterus; and responsible for:
i. Relaxation of bronchial muscles resulting in bronchodililation
ii. Relaxation of muscles in the walls of blood vessels, resulting in vasodilatation,
iii. Relaxation of uterus.
c. β3 receptors are found in adipose tissue responsible for lipolysis.

Epinephrine/adrenaline
• remains the most effective and the most commonly used vasoconstrictor in medicine
and dentistry.
• Source: It is secreted primarily by the adrenal medulla and is also available as a
synthetic.
• Mode of action: It acts directly on both α and β adrenergic receptors, but β effects are
predominant.
Systemic Actions of Adrenaline

Myocardium:

adrenaline stimulates β1 receptors of myocardium. The resultant events are:

i. A positive inotropic effect (increases force of contraction)

ii. A positive chronotropic effect (increases rate of contraction).

Pacemaker Cells

It stimulates β1 receptors and increases the irritability of pacemaker cells, leading to a

greater incidence of dysrhythmias.

Coronary Arteries

It produces dilatation of coronary arteries, resulting in an increased coronary artery blood

flow.

Blood Pressure

a. Systolic BP is increased,

b. Diastolic BP:

1. It is decreased in small doses; because of greater sensitivity to epinephrine of β2

receptors than α receptors present in blood vessels.
2. It is increased in larger doses; because of constriction of blood vessels produced by
stimulation of α receptors.
 Dr. Sarah Adil

lecture 2.............................................................................................Clinical pharmacology

Blood Vessels

✓ The primary action of epinephrine is on microcirculation (small arterioles and

precapillary sphincters).

✓ The blood vessels which supply skin, mucous membranes and kidneys contain primarily
α receptors. Epinephrine produces constriction of these blood vessels.

✓ The blood vessels supplying skeletal muscles contain both α and β2 receptors, with β2
receptors predominating.

✓ β2 receptors are more sensitive to epinephrine than α receptors, so epinephrine in small

doses produces dilatation of these vessels because of stimulation of β2. while at large
doses, epinephrine produce vasoconstriction because of stimulation of α receptors.

Respiratory System: Epinephrine is a potent dilator (β2 effect) of bronchiole smooth

muscle.

Central Nervous System

In therapeutic doses, epinephrine does not stimulate the central nervous system. It
stimulates the central nervous system only if excessive doses are administered.

2. Norepinephrine: (Nor-adrenaline) It is no longer used as a vasoconstrictor in dentistry.

3. Felypressin: It is a synthetic analogue of vasopressin (antidiuretic hormone).

❑ It is available as a vasoconstrictor, in combination with prilocaine, in dental local

anaesthetic cartridges
❑ Mode of action: It acts by directly stimulating the vascular smooth muscle. It has
little or no direct effect on the heart or adrenergic nerve transmission.
❑ Its actions are more pronounced on venous rather than on arteriolar microcirculation
❑ It may be safely used in patients with medical problems such as (i) mild to moderate
cardiovascular diseases, including hypertension, and (ii) other non-cardiovascular
diseases; such as hyperthyroidism.
❑ felypressin also can be used in patients who are on antidepressant drugs such as
tricyclic antidepressants or monoamine oxidase inhibitors.
❑ Local anaesthetic containing felypressin is not recommended for use when
homeostasis is required because of their predominant effect on venous rather than
arteriolar circulation
❑ also, it is not recommended to use LA + felypressin during pregnancy because of its
oxytocic action.