Local Anesthetics

Local Anesthetics
• Amides vs. Esters
• Pharmacodynamics and Pharmacokinetics
• Calculating LAs
• Injections
 Amides Esters
• Metabolized in the • Metabolized by
liver pseudocholinesterase
in plasma
 Amides Esters
• Lidocaine • Procaine
• Bupivicaine • Cocaine
• Mepivicaine • Tetracaine
• Articaine • Benzocaine
• Prilocaine • More toxic, more
allergic
(methylparaben)
 Amides
• Lidocaine (Xylocaine) safest in children
• Bupivicaine (Marcaine) not safe in children
• Mepivicaine (Carbocaine, Polocaine) causes least vasodilation
• Articaine (Septocaine) has one ester chain
• Prilocaine (Citanest) methemglobinemia
 Esters
• Procaine
• Cocaine vasoconstrictor
• Tetracaine
• Benzocaine
 Pharmacodynamics
• Sodium channel blocker
• Only non-ionized (free base) form can
penetrate neuron membrane
• Critical length
 Pharmacokinetics
• ↑ blood flow shorter duration of action
• ↑ lipid solubility/hydrophobicity more potent
longer duration of action
• ↑ protein binding longer duration of action
• ↓ pKa faster onset of action
– Mepivicaine: 7.6
– Lidocaine, prilocaine, articaine: 7.8
– Bupivicaine: 8.1
 Calculating Local Anesthetic
• 1mL of liquid at sea level weighs 1g
• Carpule/cartridge of anesthetic contains
1.8mL
• So entirety of liquid in carpule weighs how
much?
• 1.8g or 1800mg
• But this isn’t very relevant clinically…
 Calculating Local Anesthetic
• For 100% solution, 1.8g or 1800mg
• For 1% LA, 18mg

• For 2% lidocaine, 36mg per carpule

• For 4% articaine, 72mg per carpule
 Practice Question
• A carpule of 2% lidocaine solution with
1:100,000 epinephrine would contain how
much epinephrine in mg?

• For .001% epinephrine, 0.018mg

 Vasoconstrictor
1. Prolong numbness
2. Reduce toxicity
3. Promote hemostasis
 Toxicity
• Max epinephrine for ASA I patient= 0.2mg
• Max epinephrine for cardiac patient= 0.04mg
• Max lidocaine without vasoconstrictor= 4.4mg/kg
• Max lidocaine with vasoconstrictor= 7mg/kg
Local Anesthetics
 Delivering Local Anesthetic
• “Slow” injection is 1 carpule per minute
 Needle Dimensions
• Length
– Short= 20mm
– Long= 32mm
• Diameter
– 30-gauge= 0.3mm
– 27-gauge= 0.4mm
– 25-gauge= 0.5mm
 3/4 carpule

Inferior Alveolar Nerve Block

• Highest failure rate
• Halstead= classic
• Gow-Gates= open mouth
• Akinosi= closed mouth
 1/4 carpule

Buccal Nerve Block

• Done in tandem with IAN
block
 1/3 carpule

Mental Nerve Block

• Locate rubbery bundle
with finger
• Mental foramen by apices
of premolars
 1/3 carpule

Incisive Nerve Block

• Same as mental nerve block except hold
pressure for 2 minutes after injection to force
anesthetic into mental foramen
 1/2 carpule

Posterior Superior Alveolar Block

• Maxillary molars
• 16mm depth (half the
length of long needle)
• High hematoma risk
 1/2 carpule

Infraorbital Block
• Maxillary anteriors +
premolars
• Also called true ASA block
• Infraorbital foramen
 1/4 carpule

Greater Palatine Nerve Block

• Posterior hard palate
• Greater palatine foramen
 1/4 carpule

Nasopalatine Block
• Hard palate from canine to
canine
• Most painful
 1/2 carpule

Local Infiltration
• Enter in vestibule
• Aim for root apex
• Works well in anterior
because facial cortical
plate is thin
Antibiotics
 Sulfonamides
• Bacteriostatic
• Folate synthesis inhibitor (competes with
PABA)
• Sulfadiazine, Sulfamethoxazole
 Fluoroquinolones
• Bactericidal
• DNA synthesis inhibitor
• Ciprofloxacin, Levofloxacin
 Penicillins
• Bactericidal
• Cell wall synthesis inhibitor, β-lactam
• Cross-allergenic with cephalosporins because they are chemically related

• Penicillin G IV, more sensitive to acid degradation

• Penicillin V oral
• Amoxicillin broad spectrum
• Augmentin amoxicillin + clavulanic acid (β-lactamase-resistant)
• Methicillin β-lactamase-resistant
• Dicloxacillin “
• Ampicillin best/broadest gram-negative spectrum
• Carbenicillin used specifically against pseudomonas
 Cephalosporins
• Bactericidal
• Cell wall synthesis inhibitor, β-lactam
• 1st Gen= Cephalexin (Keflex)
• 2nd Gen= Cefuroxime
• 3rd Gen= Ceftriaxone
• 4th Gen= Cefepime
• 5th Gen= Ceftaroline
 Monobactams
• Bactericidal
• Cell wall synthesis inhibitor, β-lactam
• Aztreonam
 Carbapenems
• Bactericidal
• Cell wall synthesis inhibitor, β-lactam
• Imipenem
 Tetracyclines
• Bacteriostatic
• Protein synthesis inhibitor (30S ribosomal
subunit)
• Tetracycline, Doxycycline, Minocycline
• Broadest antimicrobial spectrum
 Macrolides
• Bacteriostatic
• Protein synthesis inhibitor (50S ribosomal
subunit)
• Erythromycin, Clarithromycin, Azithromycin

Mac likes to throw mice

 Lincosamides
• Bacteriostatic
• Protein synthesis inhibitor (50S ribosomal
subunit)
• Clindamycin, Lincomycin

Link also hides mice

 When is Antibiotic Prophylaxis
Required?
• Cardiovascular conditions
– Prosthetic heart valve
– History of endocarditis
– Heart transplant with valvulopathy/valve dysfunction
– Congenital heart problems
• Compromised immunity
– Organ transplant
– Neutropenia
– Cancer therapy
 Rx for Infective Endocarditis
Prophylaxis
• First choice Amoxicillin 2g 1 hr before tx
• Children, first choice Amoxicillin 50mg/kg 1 hr before tx
• PCN allergy Clindamycin 600mg 1 hr before tx
• Children, PCN allergy Clindamycin 20mg/kg 1 hr before tx
• Non-oral (IV or IM) Ampicillin 2g 30 min before tx
• Children, non-oral Ampicillin 50mg/kg 30 min before tx
 Rx for Prosthetic Joint Prophylaxis
• First choice Keflex 2g 1 hr before tx
 When is Antibiotic Prophylaxis NOT
Required?
• Cardiovascular conditions
– Cardiac pacemaker
– Rheumatic fever without valvular dysfunction
– Mitral valve prolapse without valvular
regurgitation
 Side Effects
• What causes GI upset and pseudomonas colitis? Clindamycin

• What is most likely to cause superinfection? Broad spectrum

antibiotics

• What is associated with aplastic anemia? Chloramphenicol

• What is associated with liver damage? Tetracycline

• What is associated with allergic cholestatic hepatitis?

Erythromycin estolate
 Drug Interactions
• Cidal and static drugs cancel each other out
• Penicillin & probenecid
• Tetracycline & antacids/dairy
• Broad spectrum antibiotics & anticoagulants
• Antibiotics & oral contraceptives
• Macrolides & seldane/digoxin
 Drug Concentration
• Clindamycin à bone
• Tetracycline à gingival crevicular fluid
 Antivirals & Antifungals
• Acyclovir, Valcyclovir à herpes
• Fluconazole, Ketoconazole à candidiasis
– Clotrimazole (Mycelex) is in troche form
Analgesics

• Aspirin (ASA)
• Ibuprofen (Motrin, Advil)
• Naproxen (Aleve)
• Ketorolac (Acular)
• Indomethacin
• Phenylbutazone (“Bute”)
• Diflunisal (Dolobid)
• Celecoxib (Celebrex)
• Meloxicam (Mobic)
NSAIDs
COX 1 and 2 blocker (irreversible) GI
COX 1 and 2 blocker (reversible) kidney
COX 1 and 2 blocker (reversible)
COX 1 and 2 blocker (reversible) IV, IM, or oral
COX 1 and 2 blocker (reversible) blood dyscrasias
COX 1 and 2 blocker (reversible) for animals
COX 1 and 2 blocker (reversible) longer half-life
COX 2 blocker
COX 2 blocker arthritis
 Acetaminophen
• Acetaminophen inhibits pain in CNS liver
• Drug of choice in feverish child, whereas aspirin can cause Reye’s Syndrome
 Maximum Dose
• Ibuprofen 3.2g/day
• Acetaminophen 4g/day
 Therapeutic Effects of Aspirin
• Analgesic à inhibit COX 1 and 2 (PG synthesis)
• Anti-inflammatory à same
• Antipyretic à inhibit PG synthesis in
temperature regulation center of
hypothalamus
• Bleeding time à inhibit TXA2 synthesis
thereby inhibiting platelet aggregation
 Toxic Effects of Aspirin
• Occult bleeding from GI tract
• Tinnitus
• Nausea and vomiting
• Metabolic acidosis
• Decreased tubular resorption of uric acid
• Salicylism
• Delirium
• Hyperventilation
 Corticosteroids
• Prednisone
• Hydrocortisone
• Triamcinolone
• Dexamethasone
 Therapeutic Effects of Steroids
• Analgesic à inhibit phospholipase A2 (AA
synthesis)
• Anti-inflammatory à same
 Side Effects of Steroids
• Gastric ulcers
• Immunosuppression
• Acute adrenal insufficiency
• Osteoporosis
• Hyperglycemia
• Redistribution of body fat
 Narcotics/Opioids
• mu-opioid receptor agonists (in CNS)
• Morphine
• Hydrocodone
• Oxycodone
• Oxycontin controlled release
• Codeine suppresses cough reflex, cough syrup
• Tramadol (Ultram) similar to codeine
• Heroin
• Fentanyl
• Sufentanil
• Carfentanil
• Meperidine (Demerol) lethal if combined with an MAOI
 Combination Narcotics
• Vicodin Hydrocodone + APAP
• Percocet Oxycodone + APAP
• Tylenol 1 300mg APAP + 8mg Codeine
• Tylenol 2 300mg APAP + 15mg Codeine
• Tylenol 3 300mg APAP + 30mg Codeine
• Tylenol 4 300mg APAP + 60mg Codeine
 Therapeutic & Side Effects of
Morphine
• Miosis
• Out of it
• Respiratory depression
• Pneumonia
• Hypotension
• Infrequency
• Nausea and vomiting
• Euphoria and dysphoria
 Overdose and Addiction
• Naloxone inverse agonist, emergency
• Naltrexone antagonist, treat addiction
• Methadone treat addiction
• Pentazocine mixed agonist-antagonist
• Nalbuphine mixed agonist-antagonist
• Buprenorphine mixed agonist-antagonist
 Nitrous Oxide
• Horace Wells was first to use for own
extraction by his assistant
• Sensation before onset à tingling
• Side effect à nausea
• Long term exposure à peripheral neuropathy
• MAC 105%
• Diffusion hypoxia