Local anesthetics Flashcards
3 parts of LA
- lipophilic group: usually benzene ring
- hydrophilic group: tertiary amine
- intermediate bond: hydrocarbon chain
intermediate bond
- Ester: -CO-
2. Amide: -HNC-
Ester LA
No ‘i’ prior to -caine
- Procaine
- Cocaine
- Chloroprocaine
- tetracaine
pseudocholinesterase
Amide
(contain an ‘i’ before -caine
- lidocaine
- bupivacaine
- ropivacaine
- mepivacaine
- prilocaine
Uptake: from fastest to slowest
Faster uptake–>higher plasma concentrations–>increasing chance of local anesthetic toxicity
Intravenous > tracheal > intercostal > caudal > paracervical > epidural > brachial plexus > sciatic > subcutaneous
factors influencing absorption and onset of action
- lipid solubility–>penetrate nerve membrane–>potency
2. pKa: lower–>more un-ionized–>speed of action
biotransformation & excretion
Ester: pseudocholinesterase —>water-soluble–>urine
Amide: liver P-450–>kidney
enhance LA effects
- epinephrine: 5mcg/ml (1:200,000) to 20mcg/ml (1:50,000)–>vasoconstricting
- opioids
- alpha-adrenergic agonists: clonidine
- steroids
informed consent: brachial plexus
bleeding, infection, nerve damage, persistent paresthesia or weakness, shortness of breath, and local anesthetic toxicity
paresthesia
a sensation of pricking, tingling, or creeping on the skin that has no objective cause
Intralipid (20% lipid emulsion)
bolus of 1.5 mL/kg over 1 min–> 0.25 mL/kg/min x 30-60 min–>repeated boluses as needed for persistent asystole.
post pain control vs surgical anesthesia
- Bupivacaine & ropivacaine: long duration–>postop pain
2. Lidocaine & mepivacaine: surgical anesthesia (not post op pain d/t short duration)
dyspnea
- phrenic nerve: close to brachial plexus–>anesthetized–>unilateral diaphragm paralysis
- pneumothorax: MC in supraclavicular
- LA toxicity
Increase risk of cardiovascular toxicity of bupivacaine
- pregnancy: progesterone
- hypoxemia
- respiratory acidosis (not alkalosis)
- hyperkalemia (rather than hypo)
What percentage of amide LA are excreted unchanged in urine
<5%