carpule constituents

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2. Ester group Amide group Hydroxy group
Composed of an aromatic
group an intermediate chain
containing an ester linkage and
hydrophilic secondary or
tertiary amino group which
forms are water soluble salts
when combined with acids
Composed of aromatic
lipophilic group an intermediate
chain containing aminde
linkage and hydrophilic
secondary or tertiary amide
group which forms also a water
soluble salts when combined
with acids
Are almost insoluble because
they like hydrophilic portion
used as a topical analgesics
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3. I. Benzoic acid esters
A. piperocaine ( Metycaine)
B. Meprylcain ( Oracaine)
c. Isobucain (kinacaine)
II. para-aminobenzoic acid esters
A. procaine (Novacaine)
B.Tetracaine(pontocain)
C.Butethamine(Monocaine)
D.propoxycain (Ravocaine)
E. 2- chloroprocaine (Nesacaine)
F. procaine and Butethamine
(Duocaine)
III.Meta-aminobenzoic acid esters
A.Metabutethamine (Unacaine)
B.primacaine (primacaine)
IV. paraethoxybenzoic acid
esters- paretho-xycaine
(Inracaine)
V.Cyclohexylamino-2-propyl-
benzoate-hexylcaine (Cyclaine)
VI. Anilide (Non ester group)
A. Lidocaine (Xylocaine)
B. Mepivacaine ( Carbocaine)
C. Procaine (Dynacaine)
D. Procaine (Citanest)
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4. comparatively weak and it possessing a low toxicity but enough to provide safe,
sure analgesia and it is rapidly hydrolyzed it is used in dentistry in 2% solutions.
Absorption :
Procaine is readily absorbed following injection into the tissues and hydrolyzed to Para amino benzoic acid and
diethylaminoethanol then catalyzed by an enzyme (plasma cholinesterase) present in the plasma and the liver
The end products, particularly para-aminobenzoic acid, are excreted by the kidney.
Toxicity:
actual toxicity is not known, but 0.5 to 1 Gm. can be tolerated if given slowly over a sufficient period of time. One
gram of a 0.1 % solution ( I Gm. Per 1L.) can be given intravenously within1 ~/2 hours without causing undue toxic
effects. Toxicity can be largely controlled by the a vasoconstrictor
in dentistry it is recommended not to be used in concentrations exceeding 2% because it will
increase vasodilation action , shorten anesthetic time and increases toxicity. in dental practice it is advised not to
use more than 400 mg. (20 ml. of a 2% solution)
Duration of action
2% solution of procaine hydrochloride , without a vasoconstrictor, gives only 12 to 15 minutes of analgesia. The
addition of epinephrine, 1 : 100,000, prolongs the duration to from 30 to 45 minutes. Epinephrine, I . 50,000, added
to the solution produces from 60 to 90 minutes of analgesia.
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5. Procaine capable of both stimulating and depressing the central nervous system Stimulation is
exhibited by excitement, tremors, ataxia, and even convulsions which Procaine produce analgesia,
and even general anesthesia, but safety is narrow in this respect.
Cardiovascular system :
cardiovascular effects of procaine depend on amount of drug used , In small amounts it has no effect
other then vasodilatation of the microcirculation at the injection area. Systemically. procaine
depresses smooth cardiac and skeletal muscles as well as nerves . It depresses excitability.
Diminishes contractility. prolongs conduction time. and increases the refractory period of the heart
large doses of it may produce hypotension
Respiratory system:
procaine have no effect However, large toxic doses may severely depress respiration. In most
instances of the toxic overdose of a local anesthetic, respiratory arrest occurs before cardiac arrest.
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6. Pharmacology : It is white crystalline powder with melting point of 69 C and is used as the
hydrochloride salt . The drug is compatible with all vasoconstrictors and withstand boiling and
Autoclaving . Absorption ; it break down in to the lipid – rich nerve giving a rapid onset of anesthesia
and its in Absorbed in the liver
Nervous system : Lidocaine depresses the NS both centrally & peripherally its depressing
affect on the CNS is observed by lethargic , sleepy patient and even convulsions may appear as a
result of depressing some brain areas . If Lidocaine administered intravenously it can produce some
degree of analgesia and even general anesthesia
Cardiovascular system: the effect varies according to the dosage small doge has no effect
but lidocaine injections result in a rise in blood pressure. It can produce an increase in the excitability
threshold and refractory period of the heart muscle. The conductive system may be affected by a
slowing of the rate of impulse conduction.
Respiratory system: Small doses of Lidocaine have no effect on , however in overdose in
may causes respiratory arrest (apnea) which precedes cardiac arrest in toxic overdose.
Topical Use: used in 4% or 10% topical solutions
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7. similar to lidocaine in its action within the body. It will produce satisfactory anesthesia of moderately long rate.
Working anesthesia has been produced in a fairly short period of time with a duration of from 2 to 4 hours. the drug
is supplied in 1.8 ml carpule. ,cartridges, and the suggested maximum dosage is approximately 300 mg. ( 15 ml. of a
2% solution)
Prilocaine (Citanest):
Pharmacology: similar to lidocaine lesser but it has lesser degree of toxicity to the central nervous
system than lidocaine and undergoes biotransformation more rapidly. Its Metabolites orthotoluidine a
substance that has been found to produce methemoglobin, and it is thus contraindicated in congenital
idiopathic methemoglobinemia rare patient
Dosage: can be used in up to 4% strength, which, without epinephrine, will give from(15 to 20 minutes) of
working anesthesia
when epinephrine in a l :200,000 added to 4% Citanest the product is called Citanest Forte. Although it contains less
epinephrine than lidocaine with epinephrine.
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8. Definition : they are all sympathomimetic amines acting on effector organs to produce same
result as adrenergic postganglionic sympathetic fibers they are un stable in solution so preservative is
added to prevents its oxidization
Mode of actionContraindicationsDisadvantagesAdvantages:
They produce their effects by stimulating alpha
adrenergic constrictor receptors located in the
walls of the arterioles in injection area
Epinephrine may under various conditions
stimulate the beta (adrenergic dilator) to
produce a vasodilation. Most vasoconstrictors
undergo rapid biotransfomation in the blood
stream thus the are short acting. In small
doses no other organs should be greatly
affected. However, the use of large volume,
high concentration or intravascular injection of
even a small amount may result in toxic
manifestations.by stimulation of alpha
1-Diabetes : it may interfere
with insulin metabolism
2- Hypotension : it rises the
blood pressure and accelerate
the heart
3- Cardiac: un balanced dose
may develop ventricular
fibrillation
4-teeth with local sepsis : may
develop post surgical dry
socket
5- pregnancy : may cause
uterine convulsions
Mainly during
practical abuse :
1- To much volume
the needed
2- Repeated
injection increases
toxicity level
3- Intra vascular
injection result in
toxic manifestations
1- Reduce toxicity by
retarding absorption of
the constituents
2-Increase depth and
time of the Anesthesia
3-Decreases the
amount of LA solution
needed
4- Prevents pus or
sepsis absorption during
surgical manipulation .
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9. l . Adrenaline ( epinephrine , supranol ) :
I .Adrenaline is an active principle of the adrenal medulla its obtained from either an extract of mammalian adrenal
glands or prepared synthetically
2. stable in acid solution. 3. It is used in a concentration from I :50.000 to I :30,000
4. light and rubber plasticizers oxidize adrenaline and therefore it should be kept in dark bottles
5. Multi dose bottles with rubber caps cause rapid deterioration of both adrenaline and noradrenaline.
6. The total dosage for dental use should not exceed 0.2 mg.
7 .Adrenaline stimulates both alpha and beta receptors and thus it dilates blood vessels in skeletal muscles and myocardium and
constricts those in the skin.
8.the operator may infiltrate the tissues with a local anesthetic solution containing adrenaline to reduce bleeding
Effects of adrenaline on the heart
has a direct action on the heart----increases the heart rate and the force of myocardium contraction----patient 's
complain of palpitations
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10. 2 . NORADRENALINE (LEVARTERENOL ,
LEVOPHED · NOREPINEPHRINE)
I. It is a neurohormone present in the adrenal _medulla or prepared synthetically
II. less effective than adrenaline therefore used in higher concentration up to I :30,000
III. For dental use dosage should not exceed 0.34 mg or IO ml of a I :30,000.
IV. Vasoconstriction obtained from noradrenaline lasts longer than that obtained from adrenaline
V. actions of noradrenaline are almost entirely on alpha receptor effects (constriction of the
blood vessels in the skeletal muscle and skin)
Effects of Noradrenaline on the heart :
1-rise in systolic and diastolic blood pressure 2-slowing of the heart rate 3-vessels in the skeletal muscles
are constricted 4-enhancement of the coronary blood flow due to coronary vasodilatat1on
5-The total peripheral resistance is increased.
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11. Felypressin is a synthetic posterior lobe pituitary hormone. it is a polypeptide resembling the
naturally occurring posterior pituitary hormone vasopressin . Its action as a vasoconstrictor less than
that of adrenaline but is of longer duration safely used in conjunction with general anaesthetic .
Felypressin has a very low toxicity with unusually high safety margin . It is the
vasoconstrictor of choice if the dental surgeon has any concern regarding patient's of cardiovascular
system.
Healthy adult patients should not be injected witl1 more than 13 ml of a I :2.,000,000 solution at one
visit .This dose should be reduced to not more than 8.8 ml of' a I : 2,000,000 solt1tion in patients
known to have ischemic heart disease.
4.Corbasil (Nordefrin hydrochloride ,Cobefrin)
1. Corbasil is : a sympathornimetic amine like adrenaline ,and noradrenaline its vasoconstrictive
action less then Adrenaline thus it is used in the relatively high concentration of 1: 10,000 solution. it
is less toxic than adrenaline, but in clinical use because of the higher concentration makes its actual
toxicityis similar several deaths reported from its use on thyrotoxic patients
total dosage for dental use should not exceed 1 mg. Corbasil is only one tenth as active a
epinephrine in increasing blood sugar.
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13. Addition of small amount of sodium metabisulphite will take any available oxygen from the solution,
thus preventing oxidation of either adrenaline or nor-adrenaline vasoconstrictor's.
FUNGICIDE: A small quantity of thymoral is added to serve as a fungicide
and prevent the proliferation of minute fungae.
VEHICLE: anaesthetic agent and the additives are dissolved in an isotonic
vehicle, Ringer's fluid is the vehicle of choice. Its formula is Sodium chloride 0.5 gm;
potassium chloride 0.02 gm and Aqua-dist 1 00c.c.
PRESERVATIVE: The sterility of the anaesthetic solution is maintained by a small
amount of preservative such as Capryl hydro-cuprienotoxin or Methyl paraben , but the
latter may cause allergic reaction.
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