Lec 2 Flashcards
(44 cards)
Pharmacokinetics of LA is
Uptake
Distribution
Metabolism(biotransformation)
Excretion
All la possess some degree of
All la possess some degree of
Vasoactivity
Ester local anesthetics are potent ___ drugs
Vasodilating
The most potent vasodilator
Procaine
The only anesthetic that consistently produce vasoconstriction
Cocaine
Vasodilation leads to increase in ?
Increase rate of absorption of la in blood
Decreasing duration and depth of anesthesia
Increase chance of overdose
Routes for administration of la
Oral route
Topical route
Injection
Reason for all la absorbed properly?
High first pass metabolism
When you apply topical route on intact skin it’s produces
When you apply topical route on intact skin it’s produces
No anesthetic action
Emla is
Mixture of local anesthetics lidocaine and prilocaine capable of providing surface anesthetics of intact skin
Commonly used route for administration of LA
Injection
Uptake of la after parenteral administration depends on
Vascularity of injection site
Vasoactivity of drug
Iv time (min)
1
Topical time
5
Intrammandar-me
5-10
Subcutaneous time
30 - 90
Brain head liver lungs kidney and spleen have hugh levels of LA due to their
High level of perfusion
____ has the highest level bcos it has the largest mass of tissue in body
Skeletal muscle
Blood level of LA is influenced by
Rate at which drug is absorbed into CVS
Rate of distribution from the vascular compartment to the tissues
Elimination of drug through metabolic or excretory pathways
Elimination half life is the
Rate at which local anesthetic is removed from the blood the time neceassary for 50% reduction in the blood level
All las can cross the
Blood brain barrier and placenta( cannot give prilocaine)
Metabolism is the mechanism by which
Metabolism is the mechanism by which
The body biologically transforms the active drug into one that is pharmacologically inactive
The overall toxicity of a drug depends on a balance between its
Rate of absorption into the blood stream at site of injection and its
Rate of removal from the blood through the processes of tissue uptake and metabolism
Ester metabolized in
Plasma