LA Flashcards
How do LAs work?
They stop never conduction by blocking the voltage-gated Na+ channels
In what order are nerve axons blocked?
A-Delta
C
A-Beta
A-Alpha
What senses are blocked first?
A-delta : sensory (mechano-, thermo-, noci- & chemoreceptors)
What is the mechanism of action for LA?
LA binds to site in NA+ channel
LA blocks channel & prevents Na+ influx
This block action potention generation & propagation
Block persists as long as sufficent # Na+ channels are blocked
What can LA cause?
Bradycardia and hypotension
Wjhat are the 3 components of LA molecules?
Aromatic region
Ester or amide bond
Basic amine side chain
Which part of LA molecules is hydrophilic and which part is hydrophobic?
Aromatic region (Hydrophobic) Basic amine side chain (Hydrophilic)
How is LA presented, and what does this do?
Presented as hydrochloride (B.HCl)
renders the amine base more water soluble
Does LA cross membrane in ionised or un-ionised form?
Only in un-ionised form
What % solutions are used in dental injections?
2-4%
What is the reducing agent used in LA preparations?
sodium metabisulphide
What else, other than reducing agents, are in LA preparations?
Preservatives and fungicide, ± vasoconstrictor
What can cause an allergic reaction between different LA brands?
Different preservatives/fungicides
What are esters used for?
Topical
What are Amides used for?
Injections
Examples of esters
Benzocaine
Cocaine/Procaine but these aren’t used any more
Examples of amides
Lignocaine
Prilocaine
Articaine
Mepivicaine (not used in UK)
What is the first choice amide?
Lignocaine
Are most LAs vasodilators or vasoconstrictors?
Vasodilators
When in LA preparations, what do vasoconstrictors do?
increase duration of action of LA
What are common LA preparation vasoconstrictors?
Adrenaline
Felypressin (synthetic vasopressin)
When can LAs containing felypressin not be used, and why?
Cannot be used on pregnant woment as can induce labour
What effect does adrenaline have on Alpha adrenoreceptors?
Vasoconstriction
What effect does adrenaline have on Beta-2 adrenoreceptors?
Vasodilation
What effect does adrenaline have on Beta-1 adrenoreceptors?
Cardiac muscle:
+ve chronotropic effect = >rate
+ve inotropic effect = >force
What receptors does vasopressin affect?
ADH receptors
What receptors do vasoconstrictors act on?
Vascular smooth muscle
Is adrenaline more effective on alpha or beta receptors?
Equally effective on both
What effect does adrenaline have when given locally?
vasoconstrictor effect - action on Alpha-receptors
What systemic effect does adrenaline have?
it lowers TPR (total peripheral resistance)
What effect does adrenaline have on mean arterial BP?
little to no effect