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Pharm 10 LA's
LECOM Pharm Ch 10 Local Anesthetics
| Question | Answer |
|---|---|
| 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 |