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39 Cards in this Set

  • Front
  • Back
What are vasoconstrictors?
an agent that causes narrowing the blood vessels.


prolong and increase the depth of anesthesia
reduce the toxic effect of the drug
render the area of injection with less bleeding
decrease blood flow to the site of injection
Describe the chemical structure of vasoconstrictors
chemically identical or quite similar to the sympathetic nervous system mediators epinephrine and norepinephrine
resemble the response of adrenergic nerves to stimulation and they are classified as sympathomimetic, or adrenergic.
What makes a vascoconstrictors sympathomimetic?
Based on whether or not is has a cathecholamine. if they have amine attached to aliphatic chain, they are called cathecolamines
Name some catecholamines..
Epi, Norepi, levonordefrin, isoproterenol, dopamine
What are some noncatecholamines
amphetamine
ephedrine
phenylephrine
Direct acting drugs vs. indirect
-exert their action directly on adrenergic receptors

indirect: release cathecholamine NE from adrenergic nerve terminals (tachyphylaxis)
Direct acting drug names
Epinephrine
Norepinephrine
Levonordefrin
Isoproterenol
Dopamine
Methoxamine
Phenylephrine
Indirect acting drugs
Tyramine
Anphetamine
Methamphetamine
Hydroxyamphetamine
Mixed action drugs
Metaraminol
Ephredine
What happens if you activate alpha receptor by a sympathomimetric drug?
produces a response that includes the contraction of smooth muscle in vessels (vasoconstriction).
What happens if you active beta receptor? B1 and B2?
Activation of  receptors produces smooth muscle relaxation (vasodilatation and bronchodilatation) and cardiac stimulation.
1 stimulates the heart
2 produces bronchodilatation and vasodilatation
Describe the end effect of stimulating alpha and beta receptors by epinephrine
alpha: increase systolic and diastolic pressure

beta: vasodilation or bronchodilation

with a beta blocker: vasodilation and bronchodilation does not occur
What affect predominates with a low dose epinephrine? high dose?
for low dose, Beta effects predominate so you get vasodilation.

for high dose, alpha effects predominate
Describe teh cardiovascular dynamics of epiephrine
Increased systolic and diastolic pressures
Increased cardiac output (CO = HR X SV)
Increased stroke volume
Increased heart rate
Increased strength of contraction
Increased myocardial oxygen consumption
Describe the respiratory system effects of epinephrine
Is a potent dilator (2 effect) of the smooth muscle of the bronchioles.
Describe the termination of action and elimination of epinephrine
Reuptake by adrenergic nerves ** most commonly done.


Inactivated in the blood by the enzyme catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO), both of which are present in the liver.
What else do we use epinephrine for in the clinic?
acute allergic reactions
bronchospasm
cardiac arrest
vasoconstrictor for hemostasis
vasoconstrictor for local anesthetics
to produce mydriasis
Max amt of epinephrine you can give to someone for a normal healthy patient..?

Patient with clinically sig cardiovascular disease?
0.2 mg per appointment

concentration may be dependent on whether you want hemostasis. ex: 1/50,000 may be better in hemostasis vs. 1/100,000.

Cardiac disease: 0.04 mg per appt.
Side effects and overdose of epinephrine..
CNS stimulation
increases fear, anxiety, tension, restlessness, headache, tremor, weakness
cardiac dysrhythmias
Increased systolic and diastolic pressures
angina
Norepinephrine (Levarterenol)..
Chemical properties
Is relatively stable in acid solution, deteriorating on exposure to light and air.
Acetone-sodium bisulfite is added to retard deterioration (preservative)

Is available in both synthetic and natural forms.
Actions are 90%  receptors and 10%  .

Mostly used in different parts of the world, but not here.
Systemic actions of NE: cardiovasc. dynamics
Decreased heart rate
Increased systolic pressure
Increased diastolic pressure
Unchanged or slightly decrease cardiac output
Increased stroke volume
Increased total peripheral resistance

not as good as epinephrine to activate alpha.
NE: respiratory system actions
Does not relax bronchial smooth muscle as does epinephrine.
It is not clinically effective in the management of bronchospasm.
NE: termination of action and elimination
Reuptake at adrenergic nerve terminals and its oxidation by MAO. Exogenous norepinephrine is inactivated by COMT.
Clinical applications of NE

What are the max doses of NE in a normal healthy patient?
It is used as a vasoconstrictor in local anesthetics and for the management of hypotension

0.34 mg per appt
cardiac pat: 0.14 mg
What are the cardiac alterations after injection of 2% lidocaine with NE 1/50,000
increase in SBP, DBP, and MAP, and decrease in HR.
Levonodefrin - Neo-Cobefrin: chemical properties. Max dose?
Synthetic vasoconstrictor
Direct  receptor stimulation (75%) with some  activity (25%)
Systemic actions similar to epinephrine, but to a lesser degree


Maximum Dosage: 1 mg per appointment
20 ml of a 1:20,000 dilution (11 cartridges)
Obtain with Mepivacaine 2% with Levonodefrin 1: 20,000 dilution
Neo-synephrie (phenylephrine hydrochloride)
Phenylephrine is quite soluble in water.
It is the weakest vasoconstrictor used in dentistry.
Direct  receptor stimulation (95%).
Exerts little or no action on the heart.
Cardiovascular actions of phenylephrine hydrochloride
Cardiovascular dynamics:
Increased systolic and diastolic
Reflex bradycardia
Slightly decreased cardiac output
Rarely associated with provoking cardiac dysrhytmias
1. Pheylephrine hydrochloride. resp system
2. termation
3. side effects and overdose
Respiratory system:
Bronchi are dilated but to a lesser degree.
Is not effective in treating bronchospasm.


Termination of action and elimination:
Undergoes hydroxylation to epinephrine, and then follows a similar pattern as epinephrine.
Side effects and overdose:
CNS effects are minimal
Headache and dysrhythmias have been noted following overdose.
Phenylephrine HCL clinical apps..
max dose?
Vasoconstrictor in local anesthetics
Management of hypotension
Nasal decongestant
Ophthalmic solutions to produce mydriasis

Max dose: 4 mg per appt for healthy pt
ASA III or 4: 1.6 mg
Felypressin (octapressin) chemical characteristics
Is a synthetic analogue of the antidiuratic hormone vasopressin
It acts as a direct stimulant of vascular smooth muscle. Its action appears to be more pronounced on the venous microcirculation.
No direct effects on the myocardium
What factors must be considered in selecting a vasoconstrictor
the length of the dental procedure
the need for hemostasis during and following the procedure.
the requirement for post operative pain control
medical status of the patient
Wht are some relative contraindications for epinephrine?
Patients with more significant disease.
Patients with certain noncardiovascular diseases (such as thyroid dysfunction, diabetes, sulfite sensitivity).
Patients receiving MAO inhibitors, tricyclic antidepresants and phenothiazines.
OraVerse (phentolamine mesylate)
Indicated for the reversal of soft-tissue anesthesia and the functional deficits resulting from an intraoral submucosal injection of a local anesthetic containing a vasoconstrictor
It is not recommended for use in children less than 6 years of age or weighing less than 15 Kg.

can either do infiltration or block injection. 1/2 cartiage is equal to 0.2 mg.

0.4 mg/ 1.7 ml soln per cartridge
What are some warnings and precautions for oraverse
MI, cerebrovascular spasm, and cerebrovasular occlusion have been reported to occur following the parenteral administration of phentolamine. The events occurred in association with marked hypotensive episodes producing shock-like states.

tachycardia, arrythmias may occr
Mechanism of action for OraVerse
Produces an alpha-adrenergic block of relatively short duration resulting in vasodilation when applied to vascular smooth muscle
What may occur with epinephrine towards the latter end of the dental procedure?
The concentration will decrease and the beta affects (vasodilation) will dominate over alpha affects (vasoconstriction). This leads to increase post operative blood loss and may compromise a patient's cardiovascular status.
What is an advantage with phenylephrine over epinephrine in terms of application during the dental procedure?
Phenylephrine does not have any beta effects and is a pure vasoconstrictor. This is longer acting than epinephrine. However, it is a weaker vasoconstrictor than epinephrine so even though it has a longer duration, hemostasis during the procedure isn't as effective. but post operative bleeding passes with less bleeding.

We must note that phenyephrine is not included with any dental cartridge.
What vasoconstrictor constricts venous circulation more than arterial circulation?
Felypressin. It is of minimal value for hemostasis during a procedure and is not in dental cartridges.