ICP L31: LA Pharmacology and equiptment Flashcards
Define anaesthesia
The loss of all sensation to a circumscribed area of the body by depression of excitation in nerve endings/ inhibition of conduction process in peripheral nerves
Define analgesia
The loss of pain sensation ONLY (nociception)
What is LA
Drug which reversibly prevents transmission of the nerve impulses to a region in which it is applied without affecting consciousness like GA
How does LA work
Produces loss of sensation as it prevents pain in a defined area by
- Blocking conduction of APs along nerve fibres
- Blocking entry of Na+ ions needed for membrane depolarisation (and so APs) meaning that the pain sensation from the tooth is not transmitted to the brain
Outline the structure of LA
- Aromatic lipophilic part
- Intermediate amide/ester chain
- Hydrophobic amine portion
What is the metabolism of LA dependant on
The intermediate carbon chain between aromatic lipophilic and amine hydrophobic portions (whether it is an ester or amide)
How do amide intermediate carbon chains affect LA metabolism
These remain stable in the blood and are metabolised in the liver therefore if the patient has reduced hepatic function it will predispose toxicity
Give examples of amide LAs
- Lidocaine
- Bupivacaine
- Articaine
- Mepivacaine
- Prilocaine
All UK LA dental cartridges are amides
How do ester intermediate carbon chains affect LA metabolism
These are rapidly broken down by pseudocholinesterase in the plasma so have a short duration of action and an increased allergy potential
Give examples of ester LAs
- Procaine (Novocaine)
2. Benzocaine (used as a topical anaesthetic gel)
Describe the mechanism of action of LAs in regards to charges
They are weak bases so in solution some molecules are charged and others uncharged -
Uncharged molecules pass through nerve cell membranes which re-equilibriates to charged/uncharged molecules inside the nerve
Inside nerve cells the molecules must be charged to bind to specific receptors and block sodium entry
List the constituents of LA
- LA agent
- Vasoconstrictor (adrenaline/epinephrine/felypressin)
- Reducing agents (stabilise vasoconstrictor by preventing oxidisation)
- Isotonic solution (modified Ringer’s solution)
- Preservatives
Why is adrenaline included in LA (3)
It is a local vasoconstrictor which controls blood flow by reducing the vessel size - thus ensuring less bleeding at the operative site (local infiltration) and less systemic absorption (lowers toxicity which allows higher dosages) and it also prolongs the duration of action
When can the vasoconstrictor part of LA be contraindicated
- Adrenaline in unstable angina and uncontrolled arrhythmias
- Felypressin in late-stage pregnancy because it causes uterine contraction
What are the adverse effects of adrenaline in LA
Adverse effects occur due to B1 adrenergic stimulation
- Increases HR + stroke volume = increased CO
- this can cause cardiac arrhythmias
- take caution with those who have heart disease - Exposure to XS hear/light causes adrenaline breakdown so needs to be stored carefully
- Plain solution LAs don’t contain vasoconstrictor