Local anesthetics Flashcards
What are local anesthetics
Substances that cause reversible local anesthesia by touching sensory nerve fibres and endings - inducing absence of sensation
How do local anesthetics work?
They stop the movement of nerve impulses from peripheral nervous system to the brain.W
In which order does sensation disappear?
Pain
Cold
Warm
Touch and pressure
Representatives of local anesthetics
Esters
-Cocaine, Procaine, Tetracaine
Amides
- Lidocaine
- Mepivacaine
- Bupivacaine
- Ropivacaine
Mechanism of action
Inhibit function of various ion channels
- Preventing movement of Na ions, increasing the
depolarisation threshold.
- Reduce permeability of cell membrane to Na ions, closing
Na channels - thereby preventing membrane
depolarisation, leading to anesthesia
Pharmacokinetics
Metabolism in liver and in blood plasma occurs by way of hydrolysis, catalyzed by pseudocholinesterase
-Excreted via kidneys - depending on urine pH
>Slowed down in alkaline urine (metabolites not ionized)
>Enhanced in case of acidic urine
Infiltration anesthesia
Like when you inject lidocaine underneath the skin before cutting into it
Procaine
Weak organic base
Used to perform infiltration, epidural and paravertebral anesthesia
Reduces cardiac excitability - has an antiarrhythmic effect
In large doses, sharp decrease in bp occurs
Lidocaine
2x stronger effect than novocaine
Used for block, infiltration, epidural and topical anesthesia
Quickly penetrates placental barrier
Strong antiarrhythmic effect
Pentobarbitone increases the toxic effect
Symptoms of lidocaine overdose
Muscular tremors, hypotension, nausea, vomiting and cramping
Block anesthesia
Anesthetic is injected around the nerve; it inhibits the impulses that are being transmitted via it
Bupivacaine
Long duration of action
4x more potent and toxic than lidocaine
Used for infiltration, nerve blocks and spinal & intrathecal techniques
Substances with local anesthetic effect
Chrloroethane, liquid nitrogen
Suitable for anesthetics for small areas of skin - if administered to large; frozen site will be painful afterwards
->Not in mouth or nose; may cause deep anesthesia resulting in death
Local anesthesia toxicity; side effects
Primarily related to system toxicity or hypersensitivity
Stimulation of CNS, muscle tremors & cramps - followed by depression
->Cause of death is respiratory arrest