VASOCONSTRICTORS

ANGRY DOCTORS' TEAM

-1-
ALL L.A ARE VASODILATORS EXCEPT > COCAINE

cocaine > very potent vasoconstrictor > may cause hard palate necrosis

CLINICAL BENEFITS OF V.C :

-decreases absorption of L.A into C.V.S

-more profound L.A effect

-increases duration of L.A action

-decreases possibility of L.A toxicity

-decreases blood flow at the site of injection (hemostasis)

-hemostatic effect is inadequate with nerve block technique >

hence L.A must be injected as infiltration

-CHEMICAL STRUCTURE OF V.C :

mostly they are sympathomimetics > hence enhance effect of sympathatic action

> they are either catecholamines / non-catecholamines

-functions of adrenergic receptors :

alpha receptors > responsible for blood vessels

beta receptors > responsible for lung and heart

alpha 1 receptors > responsible for the effect of the V.C on B.V and smooth
muscles

> so the desired V.C is one that acts mainly on alpha receptors and minimum
effect on beta receptors
-2-
-MOST V.C HAVE EFFECT ON BOTH ALPHA AND BETA RECEPTORS ,

but it depends on the dose ,

if the dose is large , then action is mainly that of alpha receptors

if dose is small , then action is mainly that of beta receptors ( as the beta receptors
are more sensitive to V.C )

> rebound vasodilatation :

happens after about 30 mins of injection

> manifests as increased pain sensation ( due to decrease action of L.A due to
decrease in amount of L.A with time )

+ increased bleeding ( due to rebound V.D > with the decrease in amount of L.A >
action on alpha receptors is decreased and action on beta2 receptors prevails >
leading to V.D)

> prevention > increase the dose every 30 mins

-CATEGORIES OF SYMPATHOMIMETICS AMINES :

> direct acting > acts directly on receptors

> indirect acting > stimulates secretion of epinephrine and norepinephrine

> mixed > have both actions

>> all V.C are direct acting , only some are mixed

-3-
-CARPULE HAS 2 NUMBERS WRITTEN ON IT :

1- eg. 1:100 000 > this expresses V.C to solution ratio

2- eg. 3% > this expresses the effective dose of the L.A agent

TO CALCULATE THE ALLOWED NUMBER OF CARPULES FOR THE PATIENT :

> know the maximum V.C mass allowed for the patient

> calculate the mass of V.C per carpule

- TO CALCULATE THE MASS OF V.C PER CARPULE :

1- transform the written number to be expressed in mg : ml

2- determine the volume of the solution , eg. 1.8 ml

3- cross multiply to figure out the V.C mass (in mg) found in the determined
volume of solution

eg:

written number > 1 : 100 000

> assume it is expressed as > 1 kg : 100 000 liter , hence

it is equal to > 1000 gm : 100 000 000 ml , hence

it is equal to > 1000 000 mg : 100 000 000 ml

so > ...........? : 1.8 ml

so > the mass in each carpule = 0.018 mg

> the most clinically used V.C > epinephrine

-concentration of clinically used vasoconstrictors :

-4-
epinephrine > 1: 1000 ( emergency anaphylaxis )

phenylepunephrine > 1 : 250 000

levonordefrine > 1 : 20 000

norepinephrine > 1 : 30 000

epinephrine > 1 : 400 000 > with popyvacaine > long acting L.A

> used for > post operative pain control , spinal anaesthesia

-BIOTRANSFORMATION O F VASOCONSTRICTORS :

> minute amounts are excreted unchanged by the kidneys

> re-uptake to adrenergic receptors

> escape to blood > inactivated by ( COMT , MAO)

> ( COMT and MAO) > are produced by the liver > hence patients with liver
disease require smaller doses to prevent toxicity

ALTHOUGH NOREPINEPHRINE ACTS MAINLY ON ALPHA RECEPTORS (90%)

and should hence be more potent than epinephrine > it is clinically found to be less
potent > this is due to its rapid uptake > hence it is used in higher concentrations
compared to epinephrine.

If the patient has heart problems >> norepinephrine or levonordephrine

Tricyclic antidepressants >> contraindicated to give LA with VC

,,,, ‫بس لو حبكت يعنى‬

>>levonordephrine
-5-