A Course in Local Anesthesia–Page 2-DoctorSpiller.com

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   Toxicity and dosage==>

<==Anesthetic agents and their history 

Vasoconstrictors

This is the second of seven pages which constitute a course in local anesthetics.  Each page stands on its own, however for a thorough understanding of dental local anesthetics the reader is advised to read the pages in order.

Vasoconstrictors

No matter how quickly an anesthetic agent can enter a nerve, the local blood vessels begin to absorb the unused anesthetic as soon as it is injected.  In order to slow this process down, manufacturers of these solutions add a substance that in low concentrations acts to cause the local blood vessels to constrict, or narrow down.  This restricts the amount of blood and plasma entering and leaving the site of the injection which has the net effect of slowing the vascular absorption of the anesthetic solution.  This keeps the unused anesthetic solution in place longer and prolongs the action of the drug.  The substance used to do this is called a vasoconstrictor (vaso refers to blood vessels and constriction means to close down).  The vasoconstrictor used is the naturally occurring hormone epinephrine or one of its analogs called levonordefrin. Epinephrine is an ideal vasoconstrictor because it is manufactured naturally by the body as adrenaline, sometimes called the “fight or flight hormone”.  In addition to causing a constriction of blood supply, if it enters the general circulation it can cause an increased heart rate and stronger heart beat, along with a feeling of nervousness.  These side effects account for the “rush” that some people feel after receiving an anesthetic shot.

The downside to vasoconstrictors

Most anesthetic solutions are sold with added vasoconstrictor.  Only two, mepivicaine and prilocaine are sold with or without vasoconstrictor (prilocaine is sold under the trade name Citanest®).  Mepivicaine and prilocaine have the advantage of producing only minor vasodilation (the opposite of constriction) and, though both are short acting without their vasoconstrictor added, they still produce adequate anesthesia for short procedures.  The major advantage of using an anesthetic without a vasoconstrictor is that there are virtually no interactions with other drugs the patient may be taking.  Vasoconstrictors may not be used with certain types of blood pressure medications, thyroid meds or tricyclic antidepressants.

The use of vasoconstrictor does carry one additional penalty for the practitioner.  These naturally occurring hormones are not very stable, and must be stabilized by the addition of an acidic preservative.  The presence of the preservative can lower the PH of the anesthetic solution to the range of 3.8 to 5.0, thus reducing the amount of the neutral basic radical (RN) and slowing the onset of action of the anesthetic.  This effect is, thankfully not especially significant, and anesthesia with vasoconstrictor is far and away the most popular choice among practitioners when other clinical considerations permit its use.

Vasoconstrictors are also not used in any body area in which the blood supply must “double back” on itself. This includes such blind ended appendages as the tip of the nose, or the fingers or toes.  In these areas, a vasoconstrictor may block all blood flow to the appendage causing tissue necrosis (death of the tissue).

Allergic reactions

The preservatives necessary to stabilize the vasoconstrictor are paraben derivatives, and these can cause allergic reactions.

Allergic reactions to amine based anesthetics like lidocaine, mepivicaine, prilocaine and articaine are so rare that they are almost non-existent.  The only component of a dental anesthetic that causes allergic reactions is the preservative used to stabilize the vasoconstrictor.

Carpules that do not contain vasoconstrictor do not contain preservatives either.  In almost every case, it is the preservatives, and not the anesthetic itself which plays a roll in allergic reactions.

If you believe that you are allergic to dental anesthesia, ask the dentist to use mepivicaine or prilocaine without vasoconstrictor. Chances are good that you will not suffer an allergic reaction.

Real allergic reactions may cause any or all of the following symptoms:

Watery, runny eyes
Runny nose
Sneezing
Nasal congestion
An itchy rash or hives
Trouble breathing or noisy breathing
Coughing, wheezing
Sneezing
Congestion
Tightness in the lungs
Hoarseness
Chest pain
Low blood pressure
Weak, rapid pulse
Dizziness, fainting
Pale or flushed skin
Hives or welts
Itchy skin
Sweating
Swelling of the throat, face, lips, or tongue
Abdominal pain
Nausea, vomiting
Diarrhea

Other unwanted effects of vasoconstrictors

Very few patients suffer from real allergic reactions to dental anesthetic injections.  However, people often suffer rapid onset of nervousness, rapid heartbeat, sweating, nausea and heart palpitations.  These are the typical “fight or flight” reactions people get when exposed to scary situations.  They are also natural reactions to vasoconstrictors when they enter the bloodstream too quickly.

These symptoms are typical when there is a rapid release of adrenaline during frightening situations.

a·dren·al·ine
noun

A hormone secreted by the adrenal glands, especially in conditions of stress, increasing rates of blood circulation, breathing, and carbohydrate metabolism and preparing muscles for exertion.

The hormone epinephrine extracted from animals or prepared synthetically for medicinal purposes.

The vasoconstrictors used in dental anesthetic preparations are really synthetic forms of adrenaline.

People often mistake these feelings of nervousness, rapid heartbeat, etc. for an allergic reaction.  They are not!  Real allergic reactions are the very serious symptoms listed above.  While these lesser symptoms may seem scary, they are very temporary, and generally harmless.  If you ignore them, they go away quickly.  Real allergic reactions do not subside quickly.

Vasoconstrictor concentrations

The concentration of vasoconstrictor in any given carpule of anesthesia is denoted by a ratio of vasoconstrictor per ml of solution.  For example, a solution may be labeled as 1:100,000.  This concentration represents 1 gm/100,000 ml of solution. This is equivalent to 1000mg/100,000mL or 0.01mg/mL . When you realize that this represents only one gram per 100 liters of solution, you can see that the concentration of vasoconstrictor in any given carpule is miniscule!

A 1:1000 solution translates to 1 mg vaoconstrictor per mL of solution, or 1 gram per Liter.  Here are some others:

dosageequivtable

Most anesthetic solutions contain the minimum amount of vasoconstrictor necessary to constrict local blood vessels and prolong the action of the anesthetic.  Some, however, contain a higher concentration of vasoconstrictor for use in controlling bleeding for specific purposes, such as periodontal surgery.  For example, general purpose lidocaine contains epinephrine in the amount of 1/100,000 for producing profound, prolonged anesthesia.  However, lidocaine also comes with epinephrine at twice the normal concentration (1/50,000) used mostly by periodontists who need to control gingival bleeding during surgery.

Indications and contraindications for vasoconstrictor

Drugs and conditions of concern to the dentist

The use of vasoconstrictor in dentistry has been shown over time to be very safe for almost all patients.  In fact, the use of vasoconstrictor is highly recommended due to the increase in efficacy and longevity of dental anesthesia.

There are no absolute contraindications to the use of vasoconstrictors in dental local anesthetics, since epinephrine is an endogenously produced neurotransmitter.  In 1964, the American Heart Association and the American Dental Association concluded a joint conference by stating that “the typical concentrations of vasoconstrictors contained in local anesthetics are not contraindicated with cardiovascular disease so long as preliminary aspiration is practiced, the agent is injected slowly, and the smallest effective dose is administered.”

Still, there are a few situations in which the use of vasoconstrictor should be reduced.

The California dental association provided some of the following information:

Conditions in which vasoconstrictor should be avoided
or kept to a minimum

  • Uncontrolled hypertension
  • Uncontrolled hyperthyroidism
  • Patients with angina
  • patients who have recently had a myocardial infarction
  • Patients taking NON SELECTIVE Beta Blockers (see table below)
  • Patients taking tricyclic antidepressants (See table below)

Note that patients with hyperthyroidism or hypertension who’s conditions are properly stabilized with medication (except non selective beta blockers) may be anesthetized with reasonable doses of anesthetic solution containing vasoconstrictor.

The following is a list of non selective beta blockers.  If the patient is taking one of these, vasoconstrictor should be avoided

  • carteolol (Cartol)
  • carvedilol (Coreg)
  • labetolol (Normodyne, Trandate)
  • nadolol (Corgard)
  • penbutolol (Levatol)
  • pindolol (Visken)
  • propranolol (Inderal)**
  • sotalol (Betapace)
  • timolol (Blocarden)

The following is a list of tricyclic antidepressants.  If the patient is taking one of these, the amount of vasoconstrictor should berestricted to no more than 3 carpules of 1/100,000

  • amitriptyline (Elavil)
  • amoxapine (Asendin)
  • clomipramine (Norpramin)
  • doxepin (Sinequan)
  • imipramine (Tofranil)
  • nortriptyline (Aventyl, Pamelor)
  • protriptyline (Vivactil)
  • trimipramine (Surmontil)

Cocaine IS ALWAYS DANGEROUS WHEN COMBINED WITH A VASOCONSTRICTOR.  Patients strung out on cocaine are at risk for fatal arrhythmias and must be treated with extreme care.

Vasoconstrictors are NOT contraindicated (i.e.. they are acceptable within accepted guidelines) if the patient is taking drugs within the classifications below:

drugtable

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