local anaesthetics Flashcards
Describe the mechanism by which amide-linked local anaesthetics reach their target. (4 marks)
- LA binds to a site in the Na+ channel by going through the myelin sheath
- LA blocks the channel and prevents Na+ influx
- This blocks action potential generation and propagation = PREVENTS DEPOLARISATION
- Block persists so long as a sufficient number of Na+ channels are blocked
How do local anaesthetics block the action potential of cells? (1 mark)
by blocking the voltage gated Na+ channels
Describe which part of the action potential is affected by a local anaesthetic (1 mark)
DEPOLARISATION region as sodium channels are blocked
Explain why the pKa of different types of amide local anaesthetics is relevant to their use.
(1 Mark)
affects the ability to enter lipid membranes of nerve fibres and bind to plasma proteins
the lower pKa = the easier to cross and reach the target
List a pathological event that may influence your choice of local anaesthetic based on the pKa.
(1 Mark)
acidosis
the extracellular pH is lowered, making the local anesthetic molecule more protonated and therefore less able to cross the cell membrane and bind to the ion channels in their charged form. This reduces the effectiveness of the local anesthetic, and it may be necessary to choose an anesthetic with a lower pKa value, such as lidocaine or prilocaine, which are less affected by changes in pH.
What is pterygomandibular raphae?
fibrous band of tissue
connects bony projection on the sphenoid bone to the mandible
Where is ptergomandibular raphae located and how would you identify it in a patient?
in the mandibular trigone, which is a triangular space located between the medial pterygoid muscle, the mandible, and the buccinator muscle.
ask the patient to open their mouth wide and place their finger inside the mouth, just behind the most distal mandibular molar tooth.
ask to close their mouth slowly while maintaining the position of their finger.
then can palpate the fibrous band of tissue running posteriorly from the pterygoid hamulus to the mandible.
Name a topical anaesthetic. (1)
Benzocaine
e.g. xylonor gel
What technique would you use to anaesthetise maxillary teeth? (1)
Infiltration
Which aspect of apex of tooth would you placed needle in maxillary teeth (1)
insert needle in a sulcus in the reflected mucosa just DISTAL TO THE APEX OF THE TOOTH required to be anaesthetised = TOWARD PALATAL ROOT OF THE TOOTH
Innervation of this nerve? (1)
A-delta, C, A-beta, A-alpha
Superior alveolar nerve
What structures pass through the mandibular foramen? (1)
inferior alveolar nerve
mylohyoid nerve
inferior alveolar artery and vein
Infiltration on buccal side of lower tooth also given. Which sensory nerve supplies this region? (1)
buccal nerve, branch of mandibular of trigeminal
Why is no infiltration given on the lingual gingivae? (2)
lingual nerve is a branch of inferior alveolar, IDB ALREADY does that
risk of injury to the lingual artery
rich blood supply so might be ineffective
Name three types of local anaesthetics used for injections. (3)
amides and esters
lidocaine
articaine
prilocaine (e.g. citanest)
bupivacaine
Functions of vasoconstrictor. (2)
- Most local anaesthetics are vasodilators
- Increased blood flow will increase ‘wash-out’ of LA
- To increase duration of action, LA preparations often include a vaso-constrictor:
- Adrenaline
- Felypressin (synthetic vasopressin)
- Vasoconstrictors act on receptors on vascular smooth muscle
Example of vasoconstrictor. (1)
Adrenaline
Felypressin
Mechanism of action of an amide anaesthetic
The anaesthetic binds to SODIUM CHANNELS and prevents sodium influx.
This blocks action potential generation and propagation.
Part of action potential affected in amide anaesthetics
DEPOLARISATION region as sodium channels are blocked
What location is affected to cause anaesthesia (Na channels)
H-gate of voltage gated sodium channels
Anaesthetic used in a healthy individual
Lidocaine 2% with 1:80,000 parts adrenaline
Why do you need to consider pKa
- pKa is related to pH by the Henderson hasselbach equation: pH = pKa + log [base]/[acid]
- The action of anaesthetics is dependent on pH as the active form of the drug B.H+ cannot cross the cell membrane and needs to break down to B and H+. This reaction is dependent upon the hydrogen concentration of the surrounding tissue as an increase in hydrogen ion concentration shifts the reaction towards increasing the active but non-diffusable B.H+.
What pathological condition affects pKa
Inflammation causes DECREASE in pH
what are the 3 components of LA ?
Aromatic (hydrophobic)
Ester/amide
Amine (hydrophilic)
The hydrophilic portion
The lipophilic portion
The intermediate chain
esters - cocaine, benzocaine
amides - lignocaine, articane, prilocaine