Pharmacology 3 Flashcards
(129 cards)
What are some toxic reactions to local anesthetics due to high systemic levels?
Cardiovascular collapse due to myocardial depression, hypotensive shock)
Prilocaine may cause ___ as an adverse effect.
Methemoglobinemia
Local anesthetics act by interfering with the ___ in the neuron.
Sodium transport
In regards to local anesthetics, only the ___ form can penetrate tissue membranes. Inflamed tissue has a lower than normal pH, which decreases the amount of non-ionized form available to penetrate
Non-ionized (or free base form)
True or false… the duration of procaine is longer than that of an equal dose of lidocaine
True
Procaine hydrochloride is metabolized into __ and ___
Diethylaminoethanol
Benzoic acid
Name one short acting anesthetic
Procaine (ester type)
Name three moderate lasting anesthetics
Prilocaine
Mepivicaine (carbocaine)
Lidocaine
Name three long acting local anesthetics
Bupivicaine (marcaine)
Tetracaine
Etidocaine
The duration of action of lidocaine could be increased with the presence of what medication? Why?
Propranolol
Propranolol slows down the heart via beta receptor blockade, thus blood deliver (and lidocaine) to the liver is reduced.
Propranolol and lidocaine also compete for the same enzyme in the liver thus metabolism of lidocaine can be reduced
Methemoglobinemia may result from a toluidine metabolite of the local anesthetic ___, called ___.
Prilocaine
Orthotoluidine
True or false… high plasma levels of local anesthetics may cause depression of inhibitory neurons in the CNS which could result in respiratory depression and death
True
If you inject lidocaine intraoral-arterially, what would likely be the first sign of lidocaine toxicity?
CNS excitation
Initially LAs inhibit central inhibitory neurons, which results in CNS stimulation, which can proceed to convulsions. At higher doses, they inhibit both inhibitory and excitatory neurons, leading to a generalized state of CNS depression which can result in respiratory depression and death
How is a patient with Grave’s disease more sensitive to epinephrine in local anesthetic?
Grave’s disease is an autoimmune disease that causes hyperthyroidism - the resulting high levels of circulating thyroid hormone result in hypermetabolic state with heightened sympathetic activity, which combined with injected epinephrine could result in a hypertensive crisis.
Cardiovascular collapse elicited by a high circulating dose of a local anesthetic may be caused by ____
Myocardial depression
LA’s in toxic doses depress membrane excitability and conduction velocity
What is the most serious consequence of local anesthetic toxicity?
Postconvulsive CNS depression
Local anesthetics block nerve conduction by…
Preventing an increase in membrane permeability to Na+
Only the __ form of LAs can pass through the membrane. Once inside the membrane only the ___ is effective in affecting the __ channel.
Nonionized (free base)
Ionized
Sodium
Most local anesthetics are weak [acids/bases] with a pKa ranging from __-__.
Bases
7.5 - 9.5
True or false… the greater the drug concentration, the faster the onset and the greater the degree of effect
True
True or false… local anesthetics block only myelinated nerve fibers at the nodes of ranvier
True
True or false… the larger the diameter of the nerve fiber, the faster the onset of effect
False… the smaller the diameter the faster the onset
True or false… the faster the penetrance of the drug the faster the onset of effect.
True
1:100,000 epinephrine = ___mg/ml
0.01 mg/ml