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Pharm 10 LA's

LECOM Pharm Ch 10 Local Anesthetics

2 afferent fibers that carry nocioceptor information Aδ-fibers and C-fiber
Pain from Heat about 45*C is carried by what type of fiber C-fiber
Pain from cold below 5*C is carried by what type of fiber? Aδ-fibers
High threshold mechanical nocioceptors transmit pain via what type of fiber? Aδ-fibers and some Aβ-fibers
Polymodal chemical, temperature, and mechanical nocioceptor transmits pain via what fibers? C-fibers
LA’s affect nerves in which order? small non-myelinated>small myelinated>large non-myelinated>large myelinated
Which type of feeling dulls first from LA’s? 2nd? 3rd? 4th? pain>temp>touch>pressure
Do you need more or less anesthetic in infected tissue? more; infected=acidic, LA’s are alkali and become neutralized and unable to bind
Speed and fiber of 1st pain? 5-25 m/s and Aδ-fibers
Speed and fiber of 2nd pain? 1 m/s and C-fibers
Mnemonic for amide-linked LA’s amIdes have 2 I’s in the name; Lidocaine, Prilocaine, Bupivicaine, Articaine
Site of action for LA’s? and conformation affinity? cytoplasmic side of Na+ channel, prefers intermediate, open, and inactive conformations
Higher or lower hydrophobicity increases LA’s partition through membranes? Higher (but not too high or they are stuck in the membrane)
High, moderate, or low hydrophobicity is wanted in a good LA? moderate
What functional group confers the hydrophobicity of an LA? aromatic group
Protonated amine group + , = or – charge? +
Deprotonated amine group: +, =, or – charge? =
Protonated or deprotonated forms of amine cross membranes? deprotonated
Protonated or deprotonated forms of amine binds to target site? protonated
Most difficult nerve bundle layer for LA’s to penetrate? perineurium
Where are ester-linked LA’s metabolized? By what? tissue and plasma; esterases
Where are amide-linked LA’s metabolized? By what? liver; P450 enzymes
Topical anesthetic mixture with concern of “toxicity or addiction” TAC: tetracaine/Adrenaline/Cocaine
Used instead of TAC EMLA
Local anesthetics cause a dose-dependent effect on the heart. What is it? inotropic effect
LA that is also Class I antiarrhythmic lidocaine
Allergic reactions to LA’s usually happen with this class ester-linked
Ester-linked LA that has a know allergenic metabolite. What is the LA? What is the metabolite? Procaine; PABA
4 ester-linked LA’s procaine, 2-chloroprocaine, tetracaine, cocaine
Don’t use this LA if being treated for acute bacterial Infx and Tx with sulfonamides procaine
Short-acting LA, with slow onset, metabolized in the blood stream and excreted by the kidneys procaine
Long acting, high potency, slowly degradation in blood stream. Usually used topically and spinally tetracaine
Most cardiotoxic LA cocaine
Used primarily in ophthalmic and topical anesthesia cocaine
Rapid onset, medium duration, mildly potent, little vasoconstrictive activity, eliminated in the liver lidocaine
For rapid onset of anesthesia do you want an LA with a low or high pKa? low; further below 7.8 the more deprotonated molecules there will be and the faster they diffuse through membranes
Used when a Pt needs medium/long local anesthesia but has a Hx of arrhythmias, and can’t handle Epi; hepatically metabolized prilocaine
Less cardiotoxic enantiomer of bupivacaine and 2 names S-enantiomer; levobupivicaine/ropivicaine
Long duration, highly potent, hepatically metabolized LA; has cardiotoxic SA bupivacaine
Used mainly in dentistry, partially metabolized peripherally and hepatically articaine
Mixture of these 2 LA’s used topically is named this lidocaine and prilocaine; EMLA
Used especially in OB epidurals 2-chloroprocaine
Created by: csheck