Showing posts with label Local Anesthetic. Show all posts
Showing posts with label Local Anesthetic. Show all posts

Bupivacaine (Marcaine)

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Name: Bupivacaine (Marcaine)

Class: Local Anesthetic (Amide)

Mechanism: Blocks Na+ & Ca2+ channels ® ¯ rate of rise of action potential, failure to propagate action potential, eventual conduction block. Smaller, unmyelinated fibers are more easily blocked and remain blocked longer.

Absorption: Rapidly absorbed IV & oral. IV absorption can be limited w/a vasoconstrictor. Rapid topical absorption at mucous membranes.

Dist.: Rapidly dist. to highly perfused organs (i.e., brain, liver, kidney, heart). Placental transfer inversely related to level of protein binding. 95% protein bound. \ most preferred obstetric agent.

Metabolism.: Metabolism. by liver microsomal enzymes.

Excretion, : Long duration of action.

Toxicity/S.E.s: Progressive CNS effects—agitation leading to convulsions, generalized CNS and resp. depression, CV depression, death.

Utility: Surface anesthesia, infiltration anesth., field block anesth., nerve block anesth., IV regional anesth., spinal anesth., epidural anesth.

Special Features: 16x as potent as procaine. Sometimes used w/epinephrine to prolong action and decrease system toxicity.

 

Lidocaine (Xylocaine)

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Name: Lidocaine (Xylocaine)

Class: Local Anesthetic (Amide)

Mechanism: Blocks Na+ & Ca2+ channels ® ¯ rate of rise of action potential, failure to propagate action potential, eventual conduction block. Smaller, unmyelinated fibers are more easily blocked and remain blocked longer.

Absorption: Rapidly absorbed IV & oral. IV absorption can be limited w/a vasoconstrictor. Rapid topical absorption at mucous membranes.

Dist.: Rapidly dist. to highly perfused organs (i.e., brain, liver, kidney, heart).

Metabolism.: Metabolism. by liver microsomal enzymes.

Excretion, : Med. duration of action.

Toxicity/S.E.s: Progressive CNS effects—agitation leading to convulsions, generalized CNS and resp. depression, CV depression, death.

Utility: Surface anesthesia, infiltration anesth., field block anesth., nerve block anesth., IV regional anesth., spinal anesth., epidural anesth.

Special Features: 4x as potent as procaine. Sometimes used w/epinephrine to prolong action and decrease system toxicity.

 

Benzocaine

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Name: Benzocaine

Class: Local Anesthetic (Ester)

Mechanism: Blocks Na+ & Ca2+ channels ® ¯ rate of rise of action potential, failure to propagate action potential, eventual conduction block. Smaller, unmyelinated fibers are more easily blocked and remain blocked longer.

Absorption: Topical use only.

Dist.:

Metabolism.: Absorbed benzocaine is rapidly Metabolism. by plasma pseudocholinesterases.

Excretion, :

Toxicity/S.E.s: Too slowly absorbed to produce serious systemic toxicity..

Utility: Sustained anesthetic effect when applied to wounds and ulcerated surfaces.

Special Features:

 

Procaine (Novocain)

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Name: Procaine (Novocain)

Class: Local Anesthetic (Ester)

Mechanism: Blocks Na+ & Ca2+ channels ® ¯ rate of rise of action potential, failure to propagate action potential, eventual conduction block. Smaller, unmyelinated fibers are more easily blocked and remain blocked longer.

Absorption: Rapidly absorbed IV & oral. IV absorption can be limited w/a vasoconstrictor. Rapid topical absorption at mucous membranes.

Dist.: Rapidly dist. to highly perfused organs (i.e., brain, liver, kidney, heart).

Metabolism.: Rapidly Metabolism. by plasma pseudocholinesterases.

Excretion, : Short duration of action.

Toxicity/S.E.s: Progressive CNS effects—agitation leading to convulsions, generalized CNS and resp. depression, CV depression, death. Rare hypersens. rxns assoc. w/histamine release.

Utility: Surface anesthesia, infiltration anesth., field block anesth., nerve block anesth., IV regional anesth., spinal anesth., epidural anesth.

Special Features: Rel. low potency. Sometimes used w/epinephrine to prolong action and decrease system toxicity