ICP-31 LA: Pharmacology and Equipment Flashcards
What is the difference between anaesthesia and analgesia
Anaesthesia = loss of all sensation to a circumscribed area of the body by depression of excitation in nerve endings or an inhibition of the condition process in peripheral nerves
Analgesia = Loss of only ‘pain’ sensation (Nociception)
AY BAWS CAN I HABE DE NOTE PLZ
A local anaesthetic injection should not be painful
What is a local anaesthetic
A local anaesthetic can be defined as a drug that reversibly prevent transmission of the nerve impulse in the region to which it is applied, without affecting consciousness
How do local anaesthetics work
By blocking the entry of sodium ions that are required for an action potential to occur
Describe the chemical structure of local anaesthetics
- A lipophilic aromatic portion
- An intermediate chain: amide or ester
- A hydrophilic amine portion
Where are amide LAs metabolised and give examples of amide LAs
Amides are stable in the blood and are metabolised mainly by the liver so patients with reduced hepatic function are predisposed to toxicity:
- Lidocaine
- Bupivacaine
- Articaine
- Mepivacaine
- Prilocaine
AY BAWS CAN I HABE DE NOTE PLZ
All local anaesthetics in dental cartridges in the UK are amides
How are Ester LAs broken down and give examples
Esters are rapidly broken down by pseudocholinesterase in plasma and consequently tend to have a very short duration of action:
- Procaine (Novocain)
- Benzocaine (topical)
How can you tell is an LA is an amide
If it has an “i” in the prefix of the name (before -caine)
Describe the mechanism of action of Local Anaesthetics
- LAs in a cartridge contain charged and uncharged forms
- Uncharged form can cross the nerve cell membrane
- This then re-equilibrates to charged and uncharged forms in the nerve
- Once inside cell, the molecule must be in charged form to bind to specific receptor to block Na+ entry
- This ability to exist in lipid-soluble and charged states is possible as LAs are weak bases
What 2 factors affect the proportion of charged to uncharged molecules following injection
- pH of the tissues
- The dissociation constant (pKa) of the LA molecule
Why are the factors that affect the proportion of charged to uncharged molecules clinically important
- Infection within the tissues can reduce the pH and so reduce the effectiveness of the local anaesthetic
- Agents with a lower pKa will be more effective
What are the constituents of a local anaesthetic cartridge
- Local anaesthetic agent
- +/- vasoconstrictor (adrenaline or felypressin)
- Reducing agents (stabilises the vasoconstrictor by preventing its oxidation)
- Isotonic solution (modified ringer’s solution
- Preservatives (not common anymore)
Why do we add adrenaline to the LA cartridge
- Local vasoconstrictor
- Less bleeding at operative site
- Reduce systemic absorption and consequently lower toxicity
- Prolonged duration of action
What are the potential CVS effects of adrenaline
Increases heart rate and stroke volume and hence cardiac output:
- potential to cause cardiac arrhythmia
- caution needed in those with heart disease
Why should LA cartridges be stored carefully
Exposure to excess heat or light causes the breakdown of adrenaline
In which patients should we be cautious about the use of adrenaline in LAs
In patients with cardiac complications like unstable angina and uncontrolled arrythmias
Why do we need avoid the use of felypressin containing agents in patients in late stage pregnancy
Similar to Oxytocin hormone and Can produce uterine contractions - dose needed for labour is well beyond dose for LA - still avoid its use in pregnancy
What is felypressin
a Synthetic polypeptide
When is the use of felypressin use more acceptable and can be considered instead of adrenaline
When the patient has heart or blood pressure problems or has a tendency of fainting
What is the most widely used LA and in what conc is it used
Lidocaine 2% (20mg/ml)
What are advantageses of using Lidocaine 2% (20mg/ml)
Highly effective with low toxicity and good tissue clearance
Does Lidocaine contain a vasoconstrictor, if so what does it contain
Contains Adrenaline 1:80,000
How long does Lidocaine last for
Pulpal anaesthesia = 45-60 mins
Soft tissues may be numb for 3-5 hours after infiltration/block injections