Pharmacology  ·  Local Anesthetics

Clinical Use, Regional Anesthesia Techniques, and Epinephrine

Epinephrine as additive, six anesthesia techniques, differential block, and dose limits


Mechanism and Benefits
Why Epinephrine Is Added
  • Alpha-1 receptor activation → vasoconstriction at injection site
  • Slows systemic absorption → prolongs duration of anesthesia
  • Reduces peak plasma concentration → lowers toxicity risk
  • Test dose marker: tachycardia (20+ beats/min rise) signals intravascular injection
  • Standard concentration: 1:200,000 (5 micrograms per milliliter)
Contraindications
When NOT to Add Epinephrine
  • End-artery regions: fingers, toes, penis, tip of nose, ear pinnae — ischemia and necrosis risk
  • Intravenous regional anesthesia (Bier block) — systemic release on tourniquet deflation
  • Severe coronary artery disease or uncontrolled hypertension (relative)

Technique Overview
From Topical to Neuraxial
Technique Where drug is deposited High-yield facts
Topical Surface of mucosa or skin EMLA cream for intact skin; cocaine for nasal/pharyngeal; tetracaine for eye
Infiltration Directly into tissue at surgical site Most common technique; minor procedures
Peripheral nerve block Adjacent to named nerve or plexus Anesthetizes entire nerve distribution; ultrasound-guided
Epidural Epidural space (outside dura) Catheter allows repeated dosing; slower onset than spinal; labor analgesia
Spinal Subarachnoid space (cerebrospinal fluid) Rapid dense block; single dose; sympathetic block causes hypotension; post-dural puncture headache risk
Intravenous regional (Bier block) Intravenous into exsanguinated, tourniquet-isolated limb Lidocaine only — never bupivacaine; no epinephrine; tourniquet minimum 20 minutes

Epidural Concentration Effect
Differential Block
  • Low concentration: blocks pain fibers (C and A-delta), preserves motor function — labor analgesia, walking epidural
  • Higher concentration: blocks pain and motor fibers — surgical anesthesia for cesarean section
  • Ropivacaine more motor-sparing than bupivacaine at low concentrations
  • Same drug, different concentration — different clinical outcome
Maximum Dose Limits
Weight-Based Ceiling Doses
  • Lidocaine: ~4–5 mg/kg without epinephrine; ~7 mg/kg with epinephrine
  • Bupivacaine: ~2–3 mg/kg; minimal increase with epinephrine
  • Lower bupivacaine limit reflects severe cardiotoxicity risk
  • Vascular injection sites (intercostal) absorb faster — effectively lower the safe dose
Bier Block Safety Rules
Lidocaine only for intravenous regional anesthesia — never bupivacaine (cardiac arrest risk if tourniquet deflated prematurely). No epinephrine. Tourniquet must remain inflated for minimum 20 minutes. Deflating early releases the full local anesthetic dose into the systemic circulation.

Suggested References

Author / OrganizationTitleSource
Katzung BG, ed.Basic and Clinical Pharmacology. 15th ed.McGraw-Hill; 2021
Brunton LL, Knollmann BC, eds.Goodman & Gilman's The Pharmacological Basis of Therapeutics. 14th ed.McGraw-Hill; 2023
Hadzic A, ed.Hadzic's Peripheral Nerve Blocks and Anatomy for Ultrasound-Guided Regional Anesthesia. 2nd ed.New York: McGraw-Hill; 2011
Taddio A, Ohlsson A, Einarson TR, Stevens B, Koren GA systematic review of lidocaine-prilocaine cream (EMLA) in the treatment of acute pain in neonatesPediatrics. 1998;101(2):E1
Stoelting RK, Hillier SCPharmacology and Physiology in Anesthetic Practice. 4th ed.Philadelphia: Lippincott Williams & Wilkins; 2006:179–207
Becker DE, Reed KLLocal anesthetics: review of pharmacological considerationsAnesth Prog. 2012;59(2):90–102
Neal JM, Brull R, Horn JL, et al.The second ASRA practice advisory on neurologic complications associated with regional anesthesia and pain medicineReg Anesth Pain Med. 2015;40(5):401–430
Urmey WF, Talts KH, Sharrock NEOne hundred percent incidence of hemidiaphragmatic paresis associated with interscalene brachial plexus anesthesia as diagnosed by ultrasonographyAnesth Analg. 1991;72(4):498–503
Jaeger P, Nielsen ZJ, Henningsen MH, Hilsted KL, Mathiesen O, Dahl JBAdductor canal block versus femoral nerve block and quadriceps strength: a randomized, double-blind, placebo-controlled, crossover study in healthy volunteersAnesthesiology. 2013;118(2):409–415
Rosenberg PH, Veering BT, Urmey WFMaximum recommended doses of local anesthetics: a multifactorial conceptReg Anesth Pain Med. 2004;29(6):564–575
Butterworth JF, Mackey DC, Wasnick JD, eds.Morgan and Mikhail's Clinical Anesthesiology. 6th ed.New York: McGraw-Hill; 2018:937–992
Guay J, Nishimori M, Kopp SEpidural local anesthetics versus opioid-based analgesic regimens for postoperative gastrointestinal paralysis, vomiting and pain after abdominal surgeryCochrane Database Syst Rev. 2016;7:CD001893
Haas E, Onel E, Miller H, Ragupathi M, White PFA double-blind, randomized, active-controlled study for post-hemorrhoidectomy pain management with liposome bupivacaine, a novel local anesthetic formulationAm Surg. 2012;78(5):574–581