Drug intelligence / Profile preview

lidocaine + ephedrine

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Subcutaneous, Intramuscular, Intrathecal, Topical, Intranasal
01

Overview

Lidocaine + ephedrine is a combination drug consisting of lidocaine, an amide-type local anesthetic, and ephedrine, a sympathomimetic agent. Lidocaine works by blocking voltage-gated sodium channels in neuronal cell membranes, thereby inhibiting nerve impulse conduction and producing local or regional anesthesia. Ephedrine acts primarily as an agonist at alpha-1, beta-1, and beta-2 adrenergic receptors; it increases blood pressure through vasoconstriction (alpha-1), enhances cardiac output (beta-1), and causes bronchodilation (beta-2). The combination may be used to provide local anesthesia with the added benefit of counteracting hypotension or prolonging anesthetic effect via vasoconstriction. While combinations of lidocaine with other sympathomimetics like epinephrine are common in clinical practice for dental or surgical anesthesia[2][3][4], the specific pairing with ephedrine is less commonly documented but may be considered for its pressor effects during procedures where hypotension is a concern[8].

02

Targets

ADRB1 (β1)NaV (Voltage-gated sodium channels)β-AR (Beta-adrenergic receptor family)ADRA1A (α1A)

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