DRUGS USED IN DENTISTRY

Local Anesthetics
 Action potentials are transient membrane depolarizations that result from a brief increase in the
permeability of the membrane to sodium.
 LA’s work at the receptors on the nerve membrane
 The only site at which the molecules of LA have access to the nerve membrane is at the nodes of Ranvier
where sodium channels are found in abundance.
 It is necessary to deposit enough LA to spread at least 2-3 nodes to ensure effective anesthesia (a length
of approximately 8-10 mm)

How LA’s work:

 Specific Receptor theory:
• Calcium ions exist in bound form with the cell membrane and exert a regulatory effect on the
movement of sodium ions across the nerve membrane.
• Displacement of Calcium ions fro the sodium channel receptor site, which permits
• Binding of the LA molecule to this sodium channel receptor site, which thus produces
• Blockade of the sodium channel and
• Permeability to the Na ion is decreased or eliminated and nerve conduction is interrupted.
o ↓ rate of depolarization
o failure to reach threshold potential
o lack of development of an AP  Conduction blockade
o Cellular depolarization is not sufficient to reduce the membrane potential of a nerve fiber
to its firing level, and a propagated action potential does not develop.
o The nerve membrane remains in a state of polarization b/c the ionic movements
responsible for the AP fail to develop.
 LA molecules
 All LA molecules are amphipathic (both lipophilic and hydrophilic characteristics)
 The pH of the LA solution greatly influences its nerve-blocking action.
 Acidification of tissue decreases LA effectiveness.
 pH of normal tissue is 7.4. pH of an inflamed area is ~ 5
 pH of solutions with epi are 3.3 and pH of solutions w/out epi are 5.5 - 7
 The lower pH is likely to produce a burning sensation and a slightly slower onset of action.
 Increasing the pH of a LA speeds onset of action, increases the clinical effectiveness, and makes
injection more comfortable
 LA’s exist as both the base and the cation. The relative proportion of each varies with the pH of the
solution. Then varies with the pH of the surrounding tissue.
 The two factors involved in the action of a LA are:
• Diffusion of the drug through the nerve sheath (FREE BASE FORM)
• Binding at the receptor site in the ion channel. (CATION FORM)
 It is the pH of the extracellular fluid that determines the ease with which a LA moves from the site of
administration into the axioplasm of the nerve cell
 Adequate blockade of the nerve is more difficult to achieve in infected tissues b/c of the scarcity of
molecules able to cross the nerve sheath
 The greater the initial concentration of the LA, the faster will be the diffusion of its molecules and the
more rapid its onset of action.
 Longer acting LA’s (e.g. bupivacaine) does so b/c of its greater degree of protein binding. Proteins
constitute approximately 10% of the nerve membrane. LA’s with greater protein binding capabilities
attach more securely to the protein receptor site.
Metabolism and Elimination
 Esters:
• Hydrolyzed primarily by pseudocholinesterases.
• Procaine undergoes hydrolysis to para-aminiobenzoic acid (PABA), which is excreted unchanged
into the urine. The allergic rxns associated with ester drugs are usually due to this metabolite.
• Approx 1/2800 persons have an atypical form of pseudocholinesterase, which causes an inability
to hydrolyze ester LA’s. They are at increased risk for toxicity. (Assoc. with Malignant
hyperthermia – relative contraindication)
 Amides:
• Primary site of metabolism of the amide LA’s is the liver.
• Lidocaine, mepivacaine, articaine, etiodocaine, bupivacaine occurs almost entirely in the liver
• Prilocaine undergoes primary metabolism in the liver however there is some lung metabolism as
well. Prilocaine also undergoes more rapid biotransformation

 Significant liver dysfunction or heart failure represents a relative contraindication to the administration
of local anesthetic drugs.
 Problems with metabolites = development of methemoglobinemia in pts receiving large doses of
prilocaine or articaine.
 The kidneys are the primary excretory organ for both LA and its metabolites
 A % of LA will be excreted unchanged in the urine (varies according to the drug)
 Patients with significant renal impairment may be unable to eliminate the parent LA resulting in elevated
blood levels and an increased potential for toxicity.
 Significant renal disease is therefore a relative contraindication to LA administration

Contraindications for LA’s

Medical problem Drugs to avoid Type of Alternative drug
contraindication
LA allergy All LA in same Absolute LA in different class
class
Sulfa allergy Articaine Absolute Non-sulfur
containing LA’s
Bisulfite allergy Vasoconstrictor- Absolute Any LA without
containing LA’s vasoconstrictors
Atypical plasma Esters Relative Amides
pseudocholinesterase
Methemoglobinemia Articaine, Prilocaine Relative Amides
idiopathic or
congenital
Significant liver Amides Relative Esters
dysfunction
Significant renal Amides or esters Relative Amides or esters but
dysfunction use judiciously
Significant CVS High concentrations Relative LA with
disease of epi. (avoid epi concentrations of
retraction cords) 1:200 000 or 1:100
000 or mepivacaine
3% or prilocaine 4%
Clinical High concentrations Relative LA with
hyperthyroidism of vasoconstrictors concentrations of
(avoid epi retraction 1:200 000 or 1:100
cords) 000 or mepivacaine
3% or prilocaine 4%

 Max doses of epi/apt = 0.2mg in a healthy patient

o = 0.04 mg cardiac dose (2 carps of 1:100 000 epi or 4 carps of 1:200 000 epi)
o Levonodefrin 1:20 000 for cardiac pts @ 1mg/apt = 11 carps
 Max dose of LA = 4.4mg/kg or 300mg lidocaine (8.3 carpules)
o 2% means 2g drug in 100mL solution

 In healthy patients, the max dose of LA is reached long before epi considerations
 In patients with underlying CVS disease, epi precautions predominate
 Max calculated doses should always be decreased in medically compromised, debilitated or elderly
patients
 Limit amount of epi to 0.05mg in patients taking TCA’s
 In patients with uncontrolled hyperthyroidism, minimize epi because it could precipitate a thyroid storm

Lidocaine with 1:100 000 epi

Concentration 2% lidocaine Cartridge contains 36mg LA
Max dose = 4.4 mg/kg Max dose = 2.0 mg/lb
Weight (kg) mg Cartridges Weight (lb) mg Cartridges
10 44 1 20 40 1
20 88 2 40 80 2
30 132 3.5 60 120 3
40 176 4.5 80 160 4
50 220 6 100 200 5.5
60 264 7 120 240 6.5
70 300 8 140 280 7.5
80 300 8 160 300 8
90 300 8 180 300 8
100 300 8 200 300 8
Manufacturers recommended dose is as high as 13.5 carpules. 6.6mg/kg or 500mg and 3.0mg/lb of
epinephrine.

Analgesics

Ibuprofen (Motrin®, Advil®, Rufen®, Nuprin®)

 An anti-inflammatory drug. Ibuprofen reduces inflammation and eases mild to moderate pain. It reduces
fever and relieves the symptoms of rheumatoid arthritis (rheumatism), osteoarthritis, menstrual cramps or
premenstrual pain and swelling.
 Ibuprofen is indicated for relief of mild to moderate pain.
 Ineffective for chronic oral pain
 In controlled studies when ibuprofen was compared to aspirin in equally effective doses, the overall
incidence of gastrointestinal complaints was about half that seen in either the aspirin treated patients.
 Do not prescribe in patients taking: Coumadin, furosemide, H2 agonists, methotrexate and lithium
 Contraindicated in individuals with the syndrome of nasal polyps, angioedema, and bronchospastic
reactivity to aspirin or other nonsteroidal anti-inflammatory agents.
 Also contraindicated in patients with coagulopathy because it will worsen the problem
 Contraindicated in renal impairment
 Causes irreversible inhibition of cyclo-oxygenase. The effect on platelets is only the life-span of the
drug. 24-48 hours should be adequate (~3 ½ lives of the drug)
 Generic ibuprofen tablets and caplets are available in 200 mg, 400 mg, 600 mg, and 800 mg tablets for
oral administration and suspension form: 100 mg/5ml
 Pediatric dose = 5-10 mg/kg qid not to exceed 40mg/kg/day
Rx: Ibuprofen 200 mg
Sig: 3 T qid for the first 48 hours then prn pain
Max dose 3200 mg; do not exceed 16 tabs/day

Naprosyn 500mg – NSAID

Mitte: 30 T
Sig: T po q12h x 3d then prn pain
Max dose = 1g/day

Naprosyn Elixir 125mg/5mL– solution if wired shut

Mitte: 300mL
Sig: 20cc po q12h x 3d then prn pain

Acetylsalicylic Acid (Aspirin®)

• Causes a decrease in platelet aggregation but does not have a clinically important effect on post-op
bleeding
• Breakdown in the liver and excreted in the urine (kidneys)
• Depresses the concentration of prothrombin in the plasma and therefore increases bleeding time
• Effect lasts the lifetime of the platelet (7-10 days)
• Inhibits cyclo-oxygenase in an irreversible fashion
• Not a dose dependant phenomenon
• Patients on aspirin daily for CVS effects can discontinue aspirin for 3-days which allows for a sufficient
number of new platelets to arrive into circulation (In consultation with MD)
• Has a hypoglycemic action
• Max dose = 4g/day

Acetaminophen (Tylenol®)
 Acetaminophen is a centrally acting analgesic and is well absorbed orally. Acetaminophen produces
analgesia by elevation of the pain threshold and antipyresis through action on the hypothalamic heat
regulating center. Acetaminophen is equal to aspirin in analgesic and antipyretic effectiveness
 Takes ~90 minutes for analgesic to become effective
 Metabolized in the liver and is contraindicated in patients with liver problems
 Does not have anti-inflammatory effects
 Max dose = 4000 mg; do not exceed 8 500mg tablets/day or 12 regular strength tablets
 Available in : 325 mg, 500 mg tablets; Liquid: 80 mg/5ml, 160 mg/ml; Chewable tablets: 80 mg, 160 mg
 Pediatric dose = 15 mg/kg q4-6 hours not to exceed 5 doses/day.
• See below for manufacturer recommendations and suspensions
Rx: Extra-strength Tylenol (500mg)
Mitte: 30T
Sig: take 2 tablets every 4-6 hours for pain
Do not exceed 8 tablets per day

Children's acetaminophen Chewable Tablets (80mg): 2-3 years: two tablets. 4-5 years: three tablets. 6-8
years: four tablets. 9-10 years: five tablets. 11-12 years: six tablets.

Children's Acetaminophen Elixir and Suspension Liquid (160mg/5ml): (special cup for measuring dosage is
provided) 4-11 months: one-half teaspoon. 12-23 months: three-quarters teaspoon. 2-3 years: one teaspoon. 4-5
years: one and one-half teaspoons. 6-8 years: 2 teaspoons. 9-10 years: two and one-half teaspoons. 11-12 years:
three teaspoons.

Narcotics: -Opiate receptors

• Precise mode of analgesic action of narcotic analgesics is unknown
• Tolerance and dependence with long-term use
• Become less responsive over long-term use
• Overdose can be reversed with naloxone

Codeine – narcotic analgesic

Sig: 30-60mg im/po q4h prn pain
Available in Syrup: 5 mg/mL
Max dose codeine = 2g/day
** Should be taken with another pain med: NSAID, acetaminophen

Tylenol 1 (8 mg codeine, 325mg acetaminophen, 15mg caffeine tabs)

1-2 tabs po q4h prn pain

Tylenol 2 (15mg codeine, 325mg acetaminophen, 15mg caffeine tabs)

1-2 tabs po q4h prn pain

Tylenol 3 (30mg codeine, 325mg acetaminophen, 15mg caffeine tabs)

1-2 tabs po q4h-q6h prn pain; (max dose 4g = 12 T) (Mitte 30 T)

Tylenol 4 (60mg codeine, 325mg acetaminophen, 15mg caffeine tabs)

1 tab po q4-q6h prn pain

Demerol 50mg (Meperidine)

Mitte: 16 T
Sig: Take 1 tab q4h prn pain

Percocet –oxycodone (5mg) and acetaminophen (325mg)

Sig: 1 tablet po q6h prn pain
moderate to moderately severe pain.
Max dose oxycodone = 30mg/day

Morphine – narcotic analgesic

Sig: 10-15mg im q4h prn severe pain
(Can give morphine (5-10mg) for an angina attack or an expected MI)
Dilaudid – narcotic analgesic
Sig: 1-4 mg po q4h prn pain
Comes in 1, 2, 4mg hydromorphone tabs

Antibiotics

Peridex 0.12% (Chlorhexidine –Bisbiguanides)

Mitte: 475mL
Sig: swish 15mL for 1 min then spit bid

Penicillin VK
 3% of population has an allergy
 Bacteriocidal: Inhibits cell wall synthesis by binding to PBP which inhibits PG synthesis
 drug of choice for odontogenic infections (gram + cocci and anaerobes)
 Beter GI absorption than Penicillin G
 Available in tablets of 300mg and oral suspension of 25 mg/mL
 Pediatric doses: 25-50 mg/kg/d; max 3g/d

Rx: Pen VK 300mg

Mitte: 56 Tabs
Sig: 2 T po qid for 7 days
(300-600mg)

Amoxicillin 500mg
 Bacteriocidal: Effective against gram +ve and gram – rods (extended)
 Excellent GI absorption and slow renal elimination (Ab prophy)
 Available in 250 or 500mg tablets or oral suspension: 25 mg/mL, 50mg/mL
 2g ab prophylaxis (4 tabs 1 hour before apt) (child:50mg/kg)
 Maximum dose = 3 g per day
 Pediatric dose for infection: 25-50 mg/kg/day
Rx: Mitte: 21 T
Sig: 1 T po tid x 7d (Good b/c can prescribe with meals)

Flagyl (Metronidazole) 500mg – anaerobes

 Bacteriocidal against anaerobes
 Inhibits DNA synthesis
 Has been shown to be carcinogenic in mice
 Metronidazole has been reported to potentiate the anticoagulant effect of warfarin and other oral
coumarin anticoagulants, resulting in a prolongation of prothrombin time.
 Alcoholic beverages should not be consumed during Metronidazole therapy and for at least one day
afterward because abdominal cramps, nausea, vomiting, headaches, and flushing may occur.
 Tablets available in 250 or 500 mg
 Pediatric dose: 30 mg/kg/day po, divide qid

Rx: Mitte 14 T
 Sig: 500mg bid for 7 days

Clindamycin 300mg
 600mg is antibiotic prophylaxis 2 tabs 1 hour before apt
 Associated with pseudomembranous colitis
 Same coverage as Pen V and flagyl together
 Aerobic gram + cocci and Anaerobes
 Available in tablets of 150 mg or 300 mg or oral suspension of 15 mg/ mL
 Pediatric dose = 20mg/kg; Max dose =2 g/day

Rx: Mitte: 28 T
Sig: Take 300mg of clindamycin po q6h for 7 days (150-450mg)
(do not exceed 4800mg/d)

***if allergy to pen & clindamycin – give Vancomycin

Rx: Vancomycin 300mg

Mitte: 28 T
Sig: 1 T qid until finished
(150-450mg)

Keflex 500mg - cephalosporin (10-15% x-over w/ pen)

 Bactericidal
 Gram + aerobes & Staphalococcus aerues (including penicillinase resistant strains)
 Should be given cautiously to Penicillin sensitive individuals (cross-allergenicity is common)
 Pseudomembranous colitis is a risk following therapy
 Use with caution in renal impairment
 Respiratory infections + infections of the oropharynx (tx of choice for Staphyloccocus)
 Available in tablets 250 mg or 500 mg
Rx: Mitte: 28 Tabs
Sig: T po q6h x 7days

AB Prophylaxis
High risk
• Prosthetic heart valves
• Previous BE
• Complex cyanotic congenital heart disease
• Surgically constructed systemic pulmonary shunts

Moderate risk
• Mitral valve prolapse with valvular regurgitation
• Hypertrophic cardiomyopathy
• Congenital cardiac malformations
• uncorrected patent ductus arteriosus, ventral septal defect coartication of the aorta, bicuspid aortic valve
• Acquired valvular disease (eg. Rheumatic heart disease, calcific aortic stenosis)
IV conscious sedation
Fentanyl narcotic analgesic
interacts w/ CNS (opiod) receptors
reversed w/ Narcan
binds to opiate receptors (µ + K) in CNS causing inhibition of ascending pain pathways
altering the perception of and response to pain  CNS depression

Hexadrol glucocorticoid
blocks phospholipase A in AA cascade

Midazolam (Versed) - benzodiazepiene – conscious sedation

- enhance GABA action
- reversed w/ Flumazenole
------------------------------------------------------------------------------------------------------------
Anaphylaxis
0.3 to 0.5 mL of a 1:1000 epi solution IM, IV, SC
Benadryl (Diphenhydramine HCl) 50mg q6h for the next 24 hours or longer if systems persist
Methylprednisone (comes as Medrol at 4 and 8 mg tablets)

Nausea/Vomitting
Gravol – dimenhydrinate – H1 receptor antagonist
Sig: 50-100mg im/po q6h prn n/v

Dry Socket
throbbing and radiating pain ear and inferior border of mandible
3 -4 days; bad taste and smells bad
20% occurance in mand molars
Irrigation with saline + Alvogyl paste – eugenol + benzocaine

Subperiosteal Infection
7-14 d after surgery
Antibiotics and drainage: amoxicillin + Flagyl or PenV + flagyl or clindamycin

Sinus infections
Amoxicillin or Keflex + Afrin (nasal antihistamine) + Chlor-trimetron (nasal decongestant)
If allergic to Penicillin then azithromycin

Amoxicillin 500mg Afrin Sudafed

Mitte: 21 T Shrinks mucosal membranes (vasoconstriction) Decreases sinus secretions
Sig: 1 T tid 7d Mitte:15 mL Mitte:
Sig: spray 2 puffs each nostril tid x3d Sig: 60 mg tid

If amoxicillin fails to resolve the infection: azithromycin – take 2T stat then 1 tab each day for 5 days

Pericoronitis
Irrigate underneath operculum with hydrogen peroxide 2% or diluted four times per day until definitive
treatment (i.e. extraction)

Fungal infections
Nystatin (1:100 000)
 Disp 60 mL
Sig: Swish 5mL for 30 seconds then swallow

Diflucan 100mg (Fluconazole) * For more serious candidal infections

Disp: 10-15 T
Sig: take 2 tabs the first day then 1 T/d until finished

Angular cheilitis:
 Angular chelitis has to be differentiated from vitamin B complex deficiency
 Nystatin cream: 100 000 USP Nystatin units
 Nystatin and Triamcinolone Acetonide (anti-inflammatory)
 Cream is supplied in 15 g (0.53 oz) tubes, 30 g (1.1 oz) tubes, and 60 g (2.2 oz) tubes.
 Apply twice-daily by gently and thoroughly massaging the preparation into the skin

Erosive Lichen Planus or Erythema multiforme

LIDEX (fluocinonide) cream 0.05% is generally applied to the affected area as a thin film from two to four
times daily (15, 30, 60, 120 g tube) (medium potency steroid)
• Treatment beyond 2 –weeks should be coordinated with the patients physician due to possible
suppression of the hypothalamus-pituiatary-adrenal axis (adrenal insufficiency)

Anti-anxiety – Benxodiazepienes
 The benzodiazepienes are the most effective drugs currently available for the management of anxiety.
They also possess skeletal relaxant properties and are anticonvulsants
 One of the most significant feature of the benzodiazepienes as a group is the very wide margin of safety
between therapeutic and toxic doses
 Bezos produce virtually no changes in CVS function, but are potential respiratory depressants.
 Patients with hepatic dysfunction may receive the benzodiazepienes without the increased risk of side
effects.
 All benzodiazepienes are absorbed relatively rapidly and reliably from the GI tract. Benzos undergo
biotransformation in the liver
 The drugs most ideally suited for pretreatment anxiety control via oral administration in the dental and
surgical setting are oxazepam (serax) and diazepam (valium).
 Allergies, psychoses, and acute narrow-angle glaucoma are contraindications. They may be given to
patients with open-angle glaucoma who are receiving appropriate therapy
 Patients must be advised against driving motor vehicle or operating hazardous machinery.
 Patients must be driven to and from the dental office
 Other CNS depressants such as: alcohol, opiods, and barbiturates should be avoided
 Use of oral bezos in children < 6 months is not recommended.
 Drug doses should be decreased in elderly or debilitated patients

Valium
 Diazepam is rapidly absorbed from the GI tract, schieving peak plasma levels within 2 hours.
The drug may be given 1 hr before treatment because 90% of the maximal clinical effect
develops within this time.
 Highly effective in the preoperative management of apprehension and mild to moderate anxiety.
 Suggested dose is 5-10 mg before bedtime and treatment
 Recommendation for children is 1-2.5mg
 Available in 2, 5, 10 mg tablets

Rx: Valium (Diazepam) 5mg

Disp 2T
 Sig: 1 T before bed and 1 T 1 hour before apt

Serax (Oxazepam) 15-30 mg

 Lack of active metabolites and a short half-life makes oxazepam a preferred benzodiazepiene for
use as an anti-anxiety in dentistry
 Incidence of drowsiness is low
 Peak plasma levels within 1-4 hours

Ativan (lorazepam) 1mg (2-4mg)

• Greater possibility of unwanted sedation
• The use of lorazepam the evening before treatment to ensure that the pt receives a good night sleep
is more reasonable.
• Available 0.5, 1, 2g tablets
Rx: Disp 4 T
Sig 2T before bed and 2 T 1 hour before apt

Properties of Benzodiazepienes
Peak Plasma Level Half-life (hr) Active metabolites
(hr)
Diazepam (Valium) 2 20-70 Yes
Oxazepam (Serax) 1-4 5.7-10.9 No
Lorazepam (Ativan) 2 12 No

Hemostatic agents upon extractions or surgery

• Gelfoam –absorbable gelatin sponge containing collagen
• Liquid prep of topical thrombin – over gelfoam sponge (discontinued at present)
• Oxidized regenerated cellulose – (Surgical)
• Packed under pressure
• Reserved for more persistent bleeding
• Causes delayed healing
• Collagen – promotes platelet aggregation and accelerates blood coagulation
• Bone wax – good to have for vessels bleeding in bone