2 - Local Anaesthetics Flashcards
(193 cards)
Local anaesthetics are either:
(1) Injectable
(2) Topical
True
Injectable anaesthetics are:
(1) Amide - Bupivacaine, Lignocaine, Mepivacaine
(2) Ester - Procaine, Cocaine, Tetracaine
(3) Antihistamines - Diphenhydramine
True
Topical anaesthetics are:
(1) Amide - Dibucaine, Lignocaine, Mixture of Lignocaine + Prilocaine (EMLA)
(2) Ester - Benzocaine
(3) Ether - Pramoxine
(4) Ketone - Diclonine
(5) Antihistamines - Diphenhydramine, Doxepine
(6) Substance P depletors - Capsaicin
True
EMLA = eutectic mixture of local anaesthetics
Both amide (lignocaine, Mepivacaine, Bupivacaine) and ester (procaine, benzocaine) local anaesthetic compounds have an aromatic (lipophilic) portion, an amine (hydrophilic) portion, and an intermediate chain (ester or amide)
True
Lipophilicity (from protein binding) appears to correlate with the intrinsic potency of the anaesthetic
True (Bupivacaine is highly lipophilic compared to lignocaine and therefore much more potent, with a longer duration of action)
Absorption of lignocaine (amide) and other injectable local anaesthetics into the systemic circulation in influenced by properties of the agent itself
True
Absorption of lignocaine (amide) and other injectable local anaesthetics into the systemic circulation in influenced by presence of a vasoconstrictor in the injected solution
True (adrenaline reduces absorption)
Absorption of lignocaine (amide) and other injectable local anaesthetics into the systemic circulation in influenced by quantity of the drug injected
True
Absorption of lignocaine (amide) and other injectable local anaesthetics into the systemic circulation in influenced by technique of the injection
True
With the exception of cocaine (has potent vasoconstrictive effects), all other local anaesthetics have varying degrees of vasodilator effects and adrenaline is often added for its haemostatic effect
True
The vasoconstriction caused by adrenaline delays the absorption of the anaesthetic agent, thereby prolonging the anaesthetic effect
True
Without adrenaline, the approximate duration of action of lignocaine is 30-60 mins
True
With adrenaline, the duration of action of lignocaine is extended to 120-360 mins
True (Without adrenaline, the approximate duration of action of lignocaine is 30-60 mins)
Skin and subcutaneous tissues of the face and scalp exhibit higher significant absorption than the trunk or extremities owing to the increase relative density of blood vessels, therefore duration of anaesthesia may be briefer in these highly vascularised areas
True
Injection of the Anaesthetic agents too deeply into subcutaneous fat may give inadequate analgesia particularly on the scalp, resulting in the requiremeant for larger volumes of local anaesthetic injection and increased systemic drug absorption
True
Incorrect local anaesthetic infiltration technique may also lead to direct intravascular injection and risking systemic toxicity
True
Protein binding is the property of local anaesthetics that relates to the relative lipophilicity of the agent
True
Lignocaine = 60-80% protein bound with elimination half-life of 1.5-2 hours
Bupivacaine = 82-96% protein bound with elimination half-life of 5 hours
Amide local anaesthetics (lignocaine, Bupivacaine, Mepivacaine, prilocaine) is metabolised in the liver through hydrolysis by hepatic microsomal enzymes (Cytochrome P450) in the endoplasmic reticulum of hepatocytes
True (metabolism can be dramatically impaired in patients with significant liver dysfunction, therefore putting the patients at risk for systemic toxicity when relatively high volumes are used)
Metabolism of amide local anaesthetics (lignocaine, Bupivacaine, Mepivacaine, prilocaine) can be dramatically impaired in patients with significant liver dysfunction, therefore putting the patients at risk for systemic toxicity when relatively high volumes are used
True (metabolised in the liver by microsomal Cytochrome P450 enzymes)
Lignocaine is specifically metabolised by CYP3A4
True (substrate of CYP3A4)
Ester local anaesthetics (procaine, benzocaine) are metabolised very rapidly in the blood by pseudocholinesterase through hydrolysis to form aromatic acids and amino alcohols
True (in contrast, amides are metabolised in the liver) - approx 4% of the population is deficient in pseudocholinesterase, potentially resulting in slow metabolism
Both amides (lignocaine, Bupivacaine, Mepivacaine, prilocaine) and esters (procaine, benzocaine) are eliminated through renal excretion
True
Lignocaine has a complex excretion process as it is metabolised by CYP3A4 in the liver and then excreted into the bile , but is then reabsorbed from the GI tract and excreted in the urine
True (simplified version = metabolised in the liver, excreted in the kidneys)
Amide and Ester Local anaesthetics prevent nerve depolarisation/block conduction in nerves by minimising or preventing the influx of sodium ions into the nerve axon cell membrane
True (lipophilic portion of the drug allows penetration of the cell membrane, hydrophilic portion of the drug interact with the sodium channels on the inner surface of the cell membrane)