Local anaesthetic Flashcards
What is analgesia?
Medication that relieves pain only
What is anaesthetic?
Medication that relieves all sensation
What is Local Anaesthetic?
loss of sensation in a circumscribed areas of the body by a depression of excitation in nerve endings or an inhibition of the conduction process in peripheral nerves.
What is local anaesthetic used for?
Controlling operative pain Control post-operative pain Controlling operative haemorrhage Diagnosis of pain Relief of orofacial pain – topical and injection
What are the contents of a local anaesthetic cartridge?
Anaesthetic
Vasoconstrictor
Vehicle (Ringers solution)
Reducing agent – sodium metabisulphite (prevents oxidation of adrenaline)
Fungicide (thymol)
Preservative (most preservative free today)
What general formula do all weak bases have?
Aromatic group – intermediate chain – amino terminal
What are the properties of each part of a weak base?
Aromatic ring - is lipophilic (dissolves in lipid sheath around the nerve)
Intermediate chain - esters (older because gave allergies) or amides
Amino terminal - hydrophilic so is soluble and can transfer through interstitial fluids
What were the disadvantages of the older LA’s having esters for aromatic and intermediate groups?
made them unstable in solution, not autoclavable and antigenic/allergies
What are the advantages of the new LA’s having amides for the aromatic and intermediate groups?
more stable, autoclavable and rarely antigenic
What are Lidocaine, Prilocaine, Mapivacaine, Articaine and Bupivocaine classified as and what is their duration?
All amides
All intermediate duration but Bupivocaine is long acting
What are procaine and benzocaine classified as?
Ester and procaine is short acting
What are local anaesthetics classified as chemically?
Weak organic bases
What are local anaesthetics in solution?
Uncharged free base or positively charged
What can the uncharged molecules of LA do?
Able to penetrate the membrane
more uncharged molecules = faster penetration
What do the charged form of LA bind to?
Specific receptors
What is the drug dispensed as for administration?
As a salt usually hydrochloride - makes them soluble in the water
What is the formula for pH and ionisation?
Log (ionised (water soluble)/ unionised (lipid soluble) = pKa - pH - henderson hasselbach equation
What happens at a lower pH?
Less of the LA solution will be non ionised i.e. infection
Why does LA have to be non charged?
The LA binding site is inside the nerve so molecules need to be able to pass the epineurium, perineurium and endoneurium
What does it re-equilibriate into once the LA is inside the nerve cell?
Mixed charged and non-charged forms.
Which form binds to the specific receptors inside the cell? - blocks sodium channels
The charged form of the LA
What can the non-specific form of LA cause (more about the shape of the molecule)?
The lipophilic portion of the molecule (aromatic ring) may cause swelling of the membrane which blocks the sodium channels (non-specific theory)
What does the LA actually do to the nerve cell?
Blocks its voltage gated sodium channels so initially increases threshold for excitation and then blocks conduction of action potentials
Which type of nerve fibres are affected first and last by LA?
First - small (pain and temp)
Last - large (motor, proprioceptive)
What does LA do to the blood vessel walls?
Blocks sympathetic vasoconstrictors so causes dilation
direct effect on the smooth muscle is variable depending on which LA is used (cocaine constricts, lidocaine dilates)
How do the esters in LA get broken down?
Esterases in blood and liver turn into benzoic acids and alcohol which are excreted in the urine
Why was there a change to amide LA and less ester LA?
1:2800 population lack certain enzymes to break down the esters but okay with the amids
How do amides in LA get broken down?
They are mainly broken down in the liver, oxidised and some conjugated with glucuronic acid and all are excreted via urine so need to take care if severe liver disease
What is the half life of lidocaine?
90 minutes
Why is the breakdown of articaine different even though it is in amide?
It initially undergoes breakdown by esterases in the plasma, and has half life of 20 minutes so rapidly broken down
What are the ideal characteristics of an LA?
Produce complete local analgesia without damaging nerve or other local tissues.
Rapid onset with predictable and appropriate duration.
Isotonic.
Non-toxic systemically.
Readily soluble and stable in solution (adequate shelf-life – usually 2-2½ years).
Sterilizable (esters not autoclavable).
Non-addictive (not cocaine!).
Why is a vasoconstrictor added to the LA?
It delays removal of LA from site (constriction of blood vessels that would take the LA away) but also causes more rapid onset of the anaesthesia so don’t have to wait as long, and also reduces operative bleeding due to the constriction, also prolongs and enhances effects of LA
What is the difference in analgesia time with and without adrenaline added?
Without - 5-20 mins, soft tissues 1 hour
with - 30-60 mins, soft tissues 3 hours
What are the disadvantages of adrenaline in the LA?
Prolonged soft tissue anaesthesia
potential systemic effects with intravascular injection - heart arrythmias (just 2 cartridges can have this effect)
What systemic effects can the adrenaline in the LA have?
Blood pressure - vasodilation of muscles vasoconstriction of skin slight reduction in diastolic BP increase in rate and force of cardiac contractions increase in glucose reduced potassium
Which vasoconstrictor can have effects on the uterus?
Felypressin (octapressin) - beware pregnancy
What can noradrenaline cause?
Increase in BP, can lead to CVA (stroke)
What reducing agent is used in the LA and why?
Sodium metabisulphate to prevent oxidisation of vasoconstrictors (brown discolouration
Why is Ringer’s solution used?
To make the LA isotonic
Which LA is highly affective as a surface anaesthetic, is an ester and long acting but not routinely used?
Amethocaine
Which is the most widely used LA?
Lidocaine 2%
What is the maximum dose of lidocaine in an adult?
4.4mg/kg (approx 7 cartridges)
Which LA is similar to lidocaine?
Mepivacaine
Which LA is approx 2x longer acting than lidocaine?
Bupivacaine - very long acting, used for majory surgery or short term relief for trigeminal neuralgia
Which LA is used if avoiding adrenaline?
Prilocaine - rapid onset, good penetration
Which LA is not yet in routine used and may cause increased incidence of nerve damage? and avoided for nerve blocks
Articaine
Which LA was recently launched in the UK and not in routine use?
Ropivacaine
What is the dose in mg/ml in 2% lidocaine?
20mg/ml
How much LA may a 65kg man have?
- 4mg/kg and there is 20mg/ml
65x4. 4 = 286mg
286/20 = 14.3ml
cartridges have 2.2ml in them
14.3/2.2ml = 6.5 cartridges
easy way = 1/10 cartridge per kg of weight
When is LA contraindicated?
Unmanageable patients
injections into acute infections (regional blocks ok)
possible risk of bleeding with LA block in haemophilia or other bleeding disorders
allergy (rare)