Some of local anesthetics used in dentistry

2. Classification
of drugs
Introduction
about
LocalAnethesia
Local
Anethesia
drugs

3. Classification of Local anesthesia
according to :
Onest
Rapid
Lidocaine
Medium
Ropivacaine & Prilocaine
Slow
Bupivacaine & Tetracaine

4. Mechanism of Action
• Alerts depolarization in neurons by blocking the fast voltage gated
sodium (NA+) channels in all cell membrane
• With sufficient blockade , the membrane of the presynaptic
neuron will not depolarize and so fail to transmit the action
potential , leading to its anaethetic effects

5. Action on CNS
1):blocks conduction
around the nerve "
anaesthesia"
2):initially causes
drowsiness &
lethargy
3):higher doses cause
excitation followed
by depression
Action on CVS
1):On Heart: -
Abbreviates effective
refractory period
2):On Blood Vessels :-
Vasodilatation in the
injected area

6. I ):Source & chemistry
Lidocaine, the first amino amid type local anesthetic,
was first synthesized under the name Xylocaine by Swedish
Chemist Nils Lofgren in 1943
Lidocaine

7. • Ph of plain solution : 6.5
• Ph of vasoconstrictor containing solution : 5_5.5
• Onset of action : rapid
• Pregnancy classification : B
• Effective dental concentration : 2 %
• Protein binding : 60_80 %
• Distribution : Lipo-philic , widely distributed into body

8. • Absorption : absorbed rapidly after parental administration & from GIT
& Respiratory Tract
• Metabolism : metabolized in liver
• Excretion : metabolites & unchanged drug are excreted by the kidneys
in the urine
II ):Pharmacokinetics

9. III):Therapeutic Uses
• 1) Local Anesthesia
• 2) Ventricular Tachycardia
• 3) Ventricular Fibrillation
• 4)Cardiac Arrhythmia

10. IV):Adverse reactions
•1)Tremors
•2)Altered taste
•3)Confusion
•4)Drowsiness
•5)Blurred vision
•6)Tinnitus

11. V):Contraindications
• Heart block
• Hypotension
• Bradycardia
• With other drugs as ( Quinidine & Flecainide & Disopyramide &
Procainamide )

12. VI): Precautions
1):If you are using this medicine in the mouth or throat, do not eat or drink
anything for one hour after using it.
2):Do not use cosmetics or other skin care products on the treated skin
areas
3):If you are using the viscous topical solution medicine in the mouth or
throat, be aware of signs of toxicity. If you or your child experience
lethargy, shallow breathing, or seizures after use of this medication,
seek immediate medical attention and do not give any more doses

13. VII): Effect on Pregnancy & lactation
• 1):Effect on pregnancy :
Does not show evidence of harm to the fetus .
• 2):Effect on lactation :
No adverse effect on breastfeeding

14. VIII):Drug interaction
• Lorazepam
• Furosemide
• paracetamol (acetaminophen / hydrocodone)
• Vitamin B12 (cyanocobalamin)
• Vitamin C (ascorbic acid)
• Vitamin D3 (cholecalciferol)
• Esomeprazole

15. IX):Doses
• 1):Usual Adult Dose for Local Anesthesia
• Local Injectable Anesthesia:
-Maximum individual dose: 4 mg/kg (IV regional anesthesia); 4.5
mg/kg (infiltration)
-Maximum total dose: 300 mg .
• 2):Usual Adult Dose for (Ventricular-
Tachycardia/Fibrillation)&Cardiac Arrhythmia
• Initial dose: 50 to 100 mg IV bolus once over 2 to 3 minutes; may
repeat after 5 minutes if necessary not to exceed up to 300 mg in a 1-
hour period
Following bolus administration: 1 to 4 mg/min continuous IV infusion .

16. X):Routes of Administration
1):Intravenous injections ( sometimes combined with "Epinephrine" )
2):Dermal patch ( sometimes combined with
Prilocaine )
3):Topical gel
4):Nasal instillationspray ( combined with
“Phenylephrine” )
5):Epidural
6):Spinal anesthesia

17. XI):Storage
• Solution should be stored at controlled room temperature 15−30°C
(59−86°F).

19. Ropivacaine

20. I):Chemical structure
• A local anaesthetic drug belonging to the amino amide group. The
name ropivacaine refers to both the racemate and the marketed S-
enantiomer .Ropivacaine hydrochloride is commonly marketed by
AstraZeneca under the trade name Naropin.

21. II):Pharmacokinetic properties
• The plasma concentration of ropivacaine depends on the total dose
administered and the route of administration, as well as the
haemodynamic and circulatory condition of the patient and vascularity
of the administration site
• When ropivacaine was administered intravenously in subjects, its
pharmacokinetics were linear and dose proportional up to 80 mg
• The absorption of ropivacaine 150 mg from the epidural space is
complete and biphasic. The mean half-life of the initial phase is
approximately 14 minutes, followed by a slower phase

22. • with a mean absorption t1/2 of approximately 4.2 hours.
• Ropivacaine is bound to plasma proteins to an extent of 94%, mainly to
α1-acid glycoprotein. The total plasma concentration increase during
continuous epidural infusion of ropivacaine is caused by an increase in
the degree of protein binding and subsequent decrease in clearance of
ropivacaine .
• Ropivacaine rapidly crosses the placenta during epidural administration
for caesarean section, resulting in near complete equilibrium of the
free fraction of ropivacaine

23. • ropivacaine in the maternal and foetal circulation However, the total
plasma concentration of ropivacaine was lower in the foetal circulation
than in the maternal circulation, reflecting the binding of ropivacaine to
α1-acid glycoprotein, which is more concentrated in maternal than in
foetal plasma

24. III):Therapeutic uses
Ropivacaine is used as a local (in only one area) anesthesia for a
spinal block, also called an epidural. The medication is used to
provide anesthesia during a surgery or C-section, or to ease
labor pains.
Ropivacaine may also be used for purposes not listed in this
medication guide.

25. IV):Adverse Effects
• Bradycardia, myocardial depression, , cardiac arrhythmias,
edema, hypotension, cardiovascular collapse, cardiac arrest,
palpitation, tachycardia, anginal pain, hypertension (epinephrine-
containing solutions)
• Anxiety, apprehension, chills, headache, restlessness,
nervousness, disorientation, confusion, dizziness, tremors,
twitching, shivering, seizures; CNS depression manifested
restlessness, tremors, drowsiness, unconsciousness, tinnitus
• Nausea, vomiting
• Blurred vision, miosis
• Respiratory arrest, status asthmaticus

26. V):Contraindications / Cautions
 Intra-articular continuous infusion
 Caution if hepatic impairment
 Caution if renal impairment
 Caution if impaired cardiac
 Caution if heart block
 Caution if hypovolemia
•

27. VI):Precautions
• Ropivacaine should only be used by clinicians well versed in the
potential toxicities that may occur with local anesthetics and the
management of those toxicities. Adequate oxygen, resuscitative
equipment and personnel resources should be immediately
available prior to the administration of any local anesthetic.
• The general condition of the patient should be optimized and an
intravenous line inserted prior to receiving major

28. • blocks. All necessary precautions should be taken to prevent
intravascular injection.
• Ropivacaine is contraindicated in any patient with a known
hypersensitivity to ropivacaine or any amide-type local
anesthetic.
• As with all local anesthetics, ropivacaine should be dosed in
increments. Avoid rapid injection in emergency situations where a
fast onset of surgical anesthesia is needed. Aspiration for blood
or cerebrospinal fluid should be performed
• prior to epidural injection of the local anesthetic.

29. VII):Pregnancy & Lactation
• Pregnancy Category: C
• Lactation: not known if excreted in breast milk
• in LIFE-THREATENING emergencies when no safer drug
available. Positive evidence of human fetal risk.
• Do not use in pregnancy. Risks involved outweigh potential
benefits. Safer alternatives exist.

30. VIII ):Interactions
• Ropivacaine can cause numbness over a large portion of your
body. Take care to avoid injury before the feeling has returned
completely.
• Tell your doctor about all your current medicines and any you
start or stop using, especially
 fluvoxamine
 ketoconazole
 an antibiotic--ciprofloxacin, enoxacin, norfloxacin, ofloxacin

31.  a heart rhythm medication--amiodarone (Cordarone, Pacerone),
dronedarone (Multaq), dofetilide (Tikosyn), ibutilide (Corvert), or
sotalol (Betapace).
• This list is not complete. Other drugs may interact with
ropivacaine, including prescription and over-the-counter
medicines, vitamins, and herbal products. Not all possible
interactions are listed in this medication guide.

32. IX):Dosage & Route of Adminsteration
• Ropivacaine is given as an injection through a needle placed into an
area of your middle or lower back near your spine. You will receive this
injection in a hospital or surgical setting.
• Your breathing, blood pressure, oxygen levels, and other vital signs will
be watched closely while you are receiving ropivacaine.
• Some numbing medications can have long-lasting or delayed effects.
Talk to your doctor if you have concerns about this risk. Call your
doctor if you have joint pain or stiffness, or weakness in any part of
your body that occurs after your surgery, even months later.
• Tell your caregivers right away if you think you have received too much
of this medicine.

33. X):Storage
- Store at controlled room temperature (between 68 and 77
degrees F)

35. prilocaine
is a local anesthetic of the amino amide type first prepared by Claes
Tegner and Nils L. In its injectable form (trade name Citanest), it is
often used in dentistry. It is also often combined with lidocaine as a
topical preparation for dermal anesthesia (lidocaine/prilocaine or
EMLA), for treatment of conditions like paresthesia. As it has low
cardiac toxicity, it is commonly used for intravenous regional
anaesthesia

36. I):Source and chemistry
Chemical and physical data
Formula C13H20N2O
Molar mass 220.311 g/mol
Structure

Melting point 37 to 38 °C (99 to 100 °F)
Chemical and physical data
C13H20N2O
220.311 g/mol
37 to 38 °C (99 to 100 °F)

37. II):Pharmacokinetic properties
• Protein binding 55%
• Metabolism Hepatic and renal
• Biological half-life 10-150 minutes, longer with impaired hepatic or
renal function

38. III):Contraindication
• In some patients, ortho-toluidine, a metabolite of prilocaine, may
cause methemoglobinemia, which may be treated with
methylene blue. Prilocaine may also be contraindicated in people
with sickle cell anemia, anemia, or symptomatic hypoxia.
• People with pseudocholinesterase deficiency may have difficulty
metabolizing this anesthetic

39. IV):Therapeutic uses
• Prilocaine is used in the treatment of:
- Pain
• Prilocaine is used in the prevention of:
- Toothache

40. V):Side effect and adverse reaction
• Adverse CNS and cardiovascular effects, swelling and
persistent paresthesia of the lips and oral tissues, persistent
neurologic deficit. (See CNS Effects and also Cardiovascular
Effects, under Cautions.)
• Some side effects of prilocaine may not be reported. Always
consult your doctor or healthcare specialist for medical
advice. You may also report side effects to the FDA.

41. VI):Drug Interactions
• Acecainide
• Amiodarone
• Bretylium
• Dofetilide
• Ibutilide
• Sotalol

42. VII):Precautions
• Keep a list of all your drugs (prescription, natural products, vitamins,
OTC) with you. Give this list to your doctor.
• Check all drugs you are taking with your doctor. This drug may not mix
well with some other drugs.
• Do not eat while your mouth feels numb. You may bite your tongue.
• If you have a weak heart, talk with your doctor.
• Tell your doctor if you are pregnant or plan on getting pregnant.
• Tell your doctor if you are breast-feeding.

43. VIII):Effect on pregnancy and lactation
• Pregnancy
• In a study, the effect of prilocaine on pre- and postnatal development
was examined in rats treated with up to 2.8 times the maximum
recommended human dose of prilocaine in lidocaine-prilocaine gel
from day 6 of gestation to weaning. There was no evidence of altered
postnatal development, viability, or reproductive capacity in any
offspring.
• Lidocaine-prilocaine topical cream has been assigned to pregnancy
category B by the FDA. Animal studies have failed to reveal evidence
of impaired fertility or fetal harm. There are no controlled data in
human pregnancy. prilocaine topical cream is only recommended for
use during pregnancy when benefit outweighs risk

44. • lactation
• probably prilocaine, are excreted into human milk. Following
application of the cream to a nursing mother, the milk:plasma ratio of
lidocaine is 0.4 and is not determined for prilocaine. The manufacturer
recommends that caution be used when administering lidocaine-
prilocaine topical cream to nursing women.

45. IX):Dosages and Routes
• prilocaine periodontal (gingival) gel is used on the gums to cause
numbness or loss of feeling during dental procedures. This medicine
contains a mixture of two topical local anesthetics (numbing
medicines). It deadens the nerve endings in the gum.
• This medicine is available only with your dentist's prescription.

46. X):Storage
• This drug will be given to you in a hospital or doctor's office. You will
not store it at home.
• Store the medicine in a closed container at room temperature, away
from heat, moisture, and direct light. Keep from freezing.
• Keep out of the reach of children.
• Do not keep outdated medicine or medicine no longer needed.
• Ask your healthcare professional how you should dispose of any
medicine you do not use.

47. Bupivacaine
{mercaine}

48. I):Source & chemistry
• Like lidocaine, bupivacaine is an amino-amide anesthetic; the
aromatic head and the hydrocarbon chain are linked by an amide
bond rather than an ester as in earlier local anesthetics
• As a result, the amino-amide anesthetics are more stable and
less likely to cause allergic reactions. Unlike lidocaine, the
terminal amino portion of bupivacaine (as well as mepivacaine,
ropivacaine, and levobupivacaine) is contained within
a piperidine ring; these agents are known as pipecholyl xylidines

49. II):Pharmacokinetic properties
• The rate of systemic absorption of bupivacaine and other local
anesthetics is dependent upon the dose and concentration of
drug administered, the route of administration, the vascularity of
the administration site, and the presence or absence of
epinephrine in the preparation.
• Onset of action (route and dose-dependent): 1-17 min
• Time to peak plasma concentration (for peripheral, epidural, or
caudal block): 30-45 min
• Protein binding: about 95%
• Metabolism: hepatic
• Excretion: renal (6% unchanged)

50. III):Therapeutic uses
• Bupivacaine is indicated for local infiltration, peripheral nerve
block, sympathetic nerve block, and epidural and caudal blocks.
It is sometimes used in combination with epinephrine to prevent
systemic absorption and extend the duration of action. The
0.75% (most concentrated) formulation is used in retrobulbar
block.[7] It is the most commonly used local anesthetic in epidural
anesthesia during labor, as well as in postoperative pain
management.
• NB;
• It can be used in infiltration anaesthesia, conduction anaethesia
&epidural anaesthesia

51. IV):Adverse action
• Hypotension
• Bradycardia
• Ventricular arrhythmia
• Cardiac arrest
• Excitation
• CNS depression
• Convulsion
• Allergic reaction

52. V):Contraindications
• Known or suspected hypersensitivity to bupivacaine.
• Skin infection adjacent to the intended site of injection, concomitant
anticoagulant therapy or an abnormal bleeding tendency.
• Severe anaemia or heart disease.
• Spinal and epidural anaesthetics should never be administered to
dehydrated or hypovolaemic patients.

53. VI):Precautions
• Facilities and equipment for resuscitation should be readily available at
all times.
• Assurance must be obtained that the patient is psychologically
prepared to accept the proposed procedure.
• High blood levels of bupivacaine must be avoided in patients with
hepatic impairment.
• Care must always be taken to avoid inadvertent intravascular injection.

54. VII):Pregnancy and lactation
• Use bupivacaine with caution during pregnancy if benefits outweigh
risks. Animal studies show risk and human studies are not available or
neither animal nor human studies were done.
• Bupivacaine excretion in breast milk is unknown. It is not
recommended if breastfeeding.

55. VIII):Inter action
• Co-administration of oxytocic drugs post-partum may cause severe and
prolonged hypertension. The use of bupivacaine preparations
containing epinephrine during or following the administration of
halothane or trichloroethylene creates a risk of cardiac dysrhythmias

56. IX):Dosage
• The aim is to administer the smallest effective dose. This varies with
the procedure adopted, the degree of anaesthesia required, the rate of
absorption from the injection site and the size and responsive-ness of
the patient. Higher initial blood levels are attained with more
concentrated solutions.
•
• The maximum cumulative safe dose for adults and children of a 0.25%
solution of bupivacaine is 1.5 mg/kg. The table provides a general
guide to dosage in adults. Smaller dosages should be administered to
debilitated, elderly, epileptic and acutely ill patients.

57. • Bupivacaine is generally not recommended for children aged less
than 12 years since there is insufficient information on the
effects of its use in this age group.
•
• Solutions containing preservatives should not be used for spinal,
epidural or caudal anaesthesia.

58. X):Routes
• Parenteral
• topical

59. XI):Storage
• Bupivacaine injection should be kept protected from light and should
not be allowed to freeze. Ampoules should not be used if the solution
is discoloured.

61. Tetracaine

62. I):Source and Chemistry
-Tetracaine was patented in 1930 and come into medical Use
in 1941 . --It's on the world health organization list of essential
medicines in a health system .

63. II):Pharmacokinetic properties
Tetracaine also know as amethocaine is local anesthetic used to numb
the eyes, nose and the foot . It may also be used before starting an
intravenous to decrease pain .

64. III):Therapeutic Uses
It's used to prevent pain and to induce anesthesia.
Topical : used during short surgical procedures and examination of the
eye.
Injectable : it's available in an to be given directly into the spinal cord by
health care professional.

65. IV):Contraindications
In the case of
-Sever burning, sting and swelling
-Redness and warmth
-Nervousness and dizziness
-Breathing problems
-Eye irritation, watering and increase sensitivity to the light

66. V):Precautions
1-Ophthalmic Route
*Protect you eyes from injury while they’re still numb.
*Do not use additional eye drops in the eye until your doctor tells you.
*protect your eyes from anything that may cause irritation like dust or
sand.
2-Topical Application Route
*If you have skin rash, burning, swelling or irritation; stop using the
drug.
*Don’t use cosmetics or other skin care products on the treated skin
areas.

67. VI):Effect On Pregnancy and Lactation
On pregnancy:-
No well controlled studies have been done in pregnant women.
So Tetracaine can be given to pregnant women if clearly needed.
On Lactation:
It’s not known if Tetracaine crossed into human milk. So the doctor and
the mother will decide if the benfits overweigh the risk of using the
drug.

68. VII):Drug Interactions
The drug has over 350 interactions like sulfonamides, sulfasalazine,
sumatriptan, zonisamaide, acetazolamide and celecoxib.

69. VIII):Dosages and Routes
1- Dosage of Tetracaine may be based on the following:
*The condition being treated
*Other medical conditions you have
*Other medications you’re taking
*How you respond to this medication

70. *Area to be anesthetized
*Technique of anesthesia
*Individual Tolerance.
The lowest dosage needed to provide effective anesthesia should be
administrated.
2- Routes
*Topical
*Parenteral

71. IX):Storage
-Store below 40 degree C (104 degree F)
Preferably between 15 and 30 degree C (59 ad 86 degree F)
-Store in a tight, light resistant container
-Protect from Freezing.
*Do not use the solution if it contains crystals or is cloudy or discolored.

72. • www.med.pdn.ac.lk
• www.oregon-crna.org
• www.shabeelpn.files.wordpress.com
• www.apt.med.ubc.com
• www.lvhn.org
• www.drugs.com
• www.mayoclinic.org
• www.wikidoc.org
• www.rxwiki.com
Referances