Lidocaine: Difference between revisions
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{{MedTemplate | {{MedTemplate | ||
| generic | | generic = Lidocaine (hydrochloride) | ||
| brand | | brand = Xylocaine (injectable, oral solution, topical), Lidoderm (patch), ZTLido (patch), Glydo (jelly), EMLA (with prilocaine, topical) | ||
| structure | | structure = | ||
| classes | | classes = [[:Category:Local anesthetics|Local anesthetic (amide class)]], [[:Category:Anesthetics|Anesthetic]], [[:Category:Antiarrhythmics|Antiarrhythmic (Vaughan Williams Class IB)]] | ||
| | | uses = <vote slug="local-anesthesia-use">Local anesthesia for procedures and minor surgery (FDA; infiltration, nerve block, epidural, spinal)</vote>, <vote slug="ventricular-arrhythmias-use">Ventricular arrhythmias (FDA, IV)</vote>, <vote slug="postherpetic-neuralgia-use">Postherpetic neuralgia (FDA, Lidoderm 5% patch)</vote>, <vote slug="topical-pain-use">Topical analgesia for skin and mucosal pain (FDA)</vote>, <vote slug="pediatric-procedure-analgesia-use">Pediatric procedure analgesia (EMLA, LMX-4)</vote> | ||
| uses | | starting_dose = Infiltration: 1-2% solution; '''4.5 mg/kg ceiling without epinephrine, 7 mg/kg with epinephrine'''. IV antiarrhythmic: 1-1.5 mg/kg bolus then infusion 1-4 mg/minute. Lidoderm patch: up to 3 patches per 12 hours | ||
| starting_dose | | preparations = Injection 0.5-4% solutions (with and without epinephrine); topical cream 4-5%; transdermal patch 5% (Lidoderm), 1.8% (ZTLido); oral 2% viscous solution; jelly 2%; ophthalmic | ||
| preparations | | fda_max = '''4.5 mg/kg (without epinephrine), 7 mg/kg (with epinephrine)''' for infiltration; serum level monitoring required for prolonged IV antiarrhythmic use | ||
| fda_max = | | pill_id = | ||
| routes | | routes = Topical, infiltration, intravenous, regional anesthesia (spinal, epidural, nerve block), oral mucosal | ||
| onset | | onset = <1 minute (IV); 1-2 minutes (infiltration); 30+ minutes (patch on adult skin, faster on thinner pediatric skin) | ||
| duration | | duration = 30-90 minutes (infiltration without epinephrine); 90-200 minutes (with epinephrine); 12 hours (patch) | ||
| halflife | | halflife = 1.5-2 hours<ref name="xylocaine-label">FDA Prescribing Information, Xylocaine (lidocaine hydrochloride), Hospira/Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/006488s092lbl.pdf</ref> | ||
| bioavailability = ~35% (oral, extensive first-pass; not used orally for systemic effect); ~100% (IV)<ref name="xylocaine-label" /> | |||
| pregnancy = Extensive use experience in obstetric anesthesia; broadly considered safe<ref name="xylocaine-label" /> | |||
| legal = [[USLegal:Prescription only|Rx-only]] for most formulations; some low-concentration topical formulations are [[USLegal:Over-the-counter|OTC]] (4% cream) | |||
| | | mechanism = <vote slug="lidocaine-mech-claim">Amide-class local anesthetic. Reversible voltage-gated sodium channel blocker, preferentially binding the inactivated and open states, producing '''use-dependent block''' that is more effective on rapidly firing nerves (pain fibers) than slowly firing ones (motor fibers at low concentrations, sensory fibers preferentially). The Vaughan Williams Class IB antiarrhythmic mechanism applies the same sodium channel blockade to ventricular cardiac tissue at therapeutic plasma levels.</vote> Dose-limited by '''systemic toxicity''': CNS toxicity progresses through perioral numbness, tinnitus, seizures, and coma; cardiac toxicity through bradyarrhythmia and asystole at higher concentrations. Hepatic metabolism via CYP1A2 and CYP3A4; accumulates in hepatic impairment and heart failure<ref name="xylocaine-label" />. | ||
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}} | }} | ||
== References == | |||
<references /> | |||
[[Category:Local | [[Category:Local anesthetics]] | ||
[[Category:Anesthetics]] | [[Category:Anesthetics]] | ||
[[Category:Antiarrhythmics]] | |||
Latest revision as of 07:31, 23 May 2026
Lidocaine (hydrochloride)
Xylocaine (injectable, oral solution, topical), Lidoderm (patch), ZTLido (patch), Glydo (jelly), EMLA (with prilocaine, topical)
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Summary
Common uses
Local anesthesia for procedures and minor surgery (FDA; infiltration, nerve block, epidural, spinal)0, Ventricular arrhythmias (FDA, IV)0, Postherpetic neuralgia (FDA, Lidoderm 5% patch)0, Topical analgesia for skin and mucosal pain (FDA)0, Pediatric procedure analgesia (EMLA, LMX-4)0
Pharmacy
Starting dose
Infiltration: 1-2% solution; 4.5 mg/kg ceiling without epinephrine, 7 mg/kg with epinephrine. IV antiarrhythmic: 1-1.5 mg/kg bolus then infusion 1-4 mg/minute. Lidoderm patch: up to 3 patches per 12 hours
Preparations
Injection 0.5-4% solutions (with and without epinephrine); topical cream 4-5%; transdermal patch 5% (Lidoderm), 1.8% (ZTLido); oral 2% viscous solution; jelly 2%; ophthalmic
US FDA Max
4.5 mg/kg (without epinephrine), 7 mg/kg (with epinephrine) for infiltration; serum level monitoring required for prolonged IV antiarrhythmic use
Pharmacology
Routes
Topical, infiltration, intravenous, regional anesthesia (spinal, epidural, nerve block), oral mucosal
Onset
<1 minute (IV); 1-2 minutes (infiltration); 30+ minutes (patch on adult skin, faster on thinner pediatric skin)
Duration
30-90 minutes (infiltration without epinephrine); 90-200 minutes (with epinephrine); 12 hours (patch)
Half-life
1.5-2 hours[1]
Bioavailability
~35% (oral, extensive first-pass; not used orally for systemic effect); ~100% (IV)[1]
Pregnancy
Extensive use experience in obstetric anesthesia; broadly considered safe[1]
Legal status
Purported mechanism
Amide-class local anesthetic. Reversible voltage-gated sodium channel blocker, preferentially binding the inactivated and open states, producing use-dependent block that is more effective on rapidly firing nerves (pain fibers) than slowly firing ones (motor fibers at low concentrations, sensory fibers preferentially). The Vaughan Williams Class IB antiarrhythmic mechanism applies the same sodium channel blockade to ventricular cardiac tissue at therapeutic plasma levels.0 Dose-limited by systemic toxicity: CNS toxicity progresses through perioral numbness, tinnitus, seizures, and coma; cardiac toxicity through bradyarrhythmia and asystole at higher concentrations. Hepatic metabolism via CYP1A2 and CYP3A4; accumulates in hepatic impairment and heart failure[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Xylocaine (lidocaine hydrochloride), Hospira/Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/006488s092lbl.pdf