Local anesthetics Flashcards
Local anesthetics - 2 groups
Ester-type local anesthetics
Amide type local anesthetics
Local anesthetics - MOA
Binds to cytoplasmic internal site of the Na channel and prolongs the inactivation state of the channel. This inhibits action potential.
Use-dependent and size-dependent blockade.
Autonomic and sensory nervers are more easily blocked than motor nerves.
Effects of local anesthetics
Anesthesia
Antiarrhythmic activity (most)
Vasodilation (most)
Blockade of autonomic ganglia and neuromuscular transmission
Administration of local anesthetics and ex of clinical uses
Topical: skin, mucous membranes, cornea. Pruritus, minor surgery.
Infiltration: minor surgery, dental procedures.
Ionophoresis.
Nerve block: Ocular surgery
Spinal intrataceal: block somatosensory and motor neurons.
Epidural: labour, delivery.
Local anesthetics - contraindications
Myasthenia gravis
Local anesthetics - adverse effects
Allergic reactions (more common in ester-type).
CNS: Restlessness, tremor, euphoria, sedation, paresthesia, nausea. Seizures, coma, resp failure.
Cardiovascular: Hypotension, cardiac depression, wide QRS-tachyarrh.
Loss of visceral and smoth muscle tone.
From spinal adm: headache, resp depression, meningitis, neurotoxicity.
Local anesthetics - interactions
Potentiate neuromuscular blocking agents.
pH of tissues, acidosis, inflammation decrease efficiency.
Epinephrine: prolong action by vasoconstriction.
Contraindications, complications and cure for using epinephrine to prolong effect of local anesthetics
Contra: end-artery tissue.
Complications: ischemia, necrosis.
Cure: phentolamine (nonselective alpha-blokcer)
Ester-type local anesthetics - 6 drugs
Cocaine Procaine Proparacaine Tetracaine Benzocaine Chloroprocaine
Amide-tyme local anesthetics - 8 drugs
Lidocaine Etidocaine Bupivacaine Levobupivacaine Mepicvacaine Ropivacaine Prilocaine Dibucaine
Cocaine - indications
Nasal, laryngeal and urogenital anesthesia
Benzocaine - indications
Sunburn, pruritus, cough.
Mucous membrane anesthesia.
(nonprescription)
Proparacaine - indications
Ophthmalmic procedures and surgeries
Most common anesthetic used in obstetrics
Bupivacaine
Bupivacaine - adverse effects
More frequently cause cardiac depression.