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compatible with tissue; completely reversible; absence of local and systemic reactions; absence of allergic reactions or hypoallergenic; potent (high solubility); rapid onset (pKa of LA close to tissue pH); effective in doses far below toxic levels; sufficient duration of action for procedure
What are the 8 ideal properties of local anesthetics?
cardiovascular and CNS reactions (similar to those of other LAs)
What is the adverse reaction of dyclonine?
lidocaine; bupivacaine; articaine; benzocaine
What are the 4 commonly used local anesthetics in dentistry?
hydrophilicity
- allows drugs to be dissolved in aqueous solution, prevention drug from precipitating in interstitial fluids
- can access site of action via the aqueous route within Na+ channels
length of dental procedure; requirements for post-op pain control; medical status of the patient
Selection of of vasoconstrictors depend on what 3 things?
vasovagal; hyperventiliation; anaphylactoid reaction
What are the 3 psychogenic reactions of LA (due to insertion of the needle)?
sedation; hypotension; headache; shivering
What are the 4 adverse effects of lidocaine?
dizziness; tremors; blurred vision
What are the 3 adverse effects of mepivacaine?
paresthesia; methemoglobinemia
What are the 2 adverse effects of prilocaine?
increased risk of post-op injury; cardiovascular toxicity
What are the 2 adverse effects of bupivacaine?
paresthesia; methoglobinoemia
What are the 2 adverse effects of articaine?
allergic reaction
What is the adverse effect of procaine?
methemoglobinemia; contraindicated for children under 2
What are the 2 adverse reactions of benzocaine?
contact dermatitis; burning; stinging; angioderma
What are the 4 adverse effects of tetracaine?
local anesthetics
agents used to block pain sensation; absence or loss of sensation in a circumscribed area of the body
- depression of excitation of nerve potentials and inhibition of conduction process in peripheral nerves
- can act on any part of the nervous system and on every type of nerve fiber, reversibly blocking the action potentials responsible for nerve conduction
blocker; Na+
MOA:
- __________ of peripheral nerve conduction
- bind to voltage gated ____ channels and block/prevent the generation and conduction of action potentials
esters
- first group of LA, commonly used topically
- metabolized to para-amino benzoic acid (PABA) --> highest association of allergic reactions
- metabolized in the tissue by pseudocholinesterase - contraindicated in patients with atypical pseudocholinesterase production
amides
- allergic reaction extremely rare
- metabolized in the liver, eliminated through the kidneys
- better lipid solubility, potency, duration of action, and ionization constant
- bind to plasma proteins, RBCs, distributes to all tissue types
lipophilicity
- essential for drug to permeate nerve sheath and nerve membrane
- gain access by crossing hydrophobic route (lipid bilayer or hydrophobic domains of Na+ channels)
acidic; prevent
Inflamed tissue tends to be more _________ which ionize the LA and ____________ absorption into the nerve
bases
LA agents in solution are weak _________
decrease; increase; decrease; cardiovascular
Vasoconstrictors in LA:
- ____________ systemic absorption and risk of toxicity
- ______________ duration of action and depth of anesthesia
- ________________ bleeding
- attention to _____________ effects with patient with uncontrolled cardiac history
lidocaine
What is the safest local anesthetic for pregnant patients?
higher
Distribution of LA:
- highly vascular organs receive ________________ (lower or higher) concentrations of anesthetics (drug redistribution)
esters
What chemical class of local anesthetics are rapidly metabolized?
duration; avoiding side effects
What are the 2 factors involved in the choice of LA?
central nervous system; cardiovascular system
What are the 2 main system affected by LA toxicity?
close
Want pKa of LA to be __________ to pH of tissue
toxicity
What is an adverse effect of local anesthesia?
