Local anesthesia Flashcards
Local anaesthetics block
voltage-gated sodium channels and prevent membrane depolarisation.
pH of Local anaesthetics
LA are weak bases
Voltage-gated sodium channels may be:
Resting (R)
Open or active (O)
Closed or desensitized (I)
LA only affect
open or closed channels.
Therefore local anaesthetics are able to inhibit the development and transmission of electrical currents.
To get inside the cell, LA has to be in what form?
unionized form
It has to be lipid soluble as well.
To bind with the receptor, the molecule has to be in what form?
ionized form
In the cell LA has to be ionized.
This is possible, because LA are weak bases.
In veterinary medicine amide-linked local anaesthetics are used. Give 5 examples of these.
Lidocaine
Bupivacaine
Mepivacaine
Ropivacaine
Prilocaine
Molecular characteristics of LA that influence pharmacodynamics.
pH
dissociation constant (pKa)
lipid solubility
protein binding
The dissociation constant (pKa) partly determines the onset of action of an LA.
pKa – pH at which half the drug is present in the unionised form and half in the ionised form.
Those LA agents with pKa values near body pH offer
a faster onset of action.
Lipid solubility partly determines
potency.
Protein binding partly determines
duration of action.
Tissue penetrance depends on a number of factors (3).
If the tissue is inflamed, it tends to have lower pH and therefore?
pKa, local pH, molecular size etc.
If the tissue is inflamed, it tends to have lower pH and therefore the onset of block is delayed.
Reasons we should we use LA? (5)
Important part of balanced anaesthesia
Reduces the effect of pain to cardorespiratory system.
Reduces the effect of pain to endocrinological system.
Better post-op analgesia
Reduces perioperative complications
Balanced anaesthesia = (3)
Reduced dosages
Reduced side effects
Faster recovery
Side-effects of LA (5)
Allergic reactions
Local tissue injury/neurotoxicity
Systemic toxicity
Vasodilation and hypotension
May also block somatic nerves causing paralysis
Signs of systemic toxicity from LAs
CNS signs: depression, sedation, convulsions, apnea
Cardiovascular: hypoxemia, respiratory arrest, cardiovascular collapse