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cocaine

DAT Inhibitor · Local anesthetic

DAT InhibitorLocal anesthetic
CDSCO approved
EXCRETION
not curated
INTERACTIONS
1 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 3
  • AdrenalineSevereTextbookKDT 7e · p57

Mechanism

Acts as an antagonist to block dopamine (DA) reuptake, thereby potentiating DA signaling and increasing extracellular DA.

Indications

Topical anesthetic in eye and nasal surgeries (limited clinical utility)Topical anesthesia of the upper respiratory tractTopical use as local anesthetic in otolaryngology and tear duct surgeryHorner syndrome (diagnosis)intranasal in combination with topical anesthesia for cannulating the nasolacrimal systemOcular anaesthesia (but use not warranted due to side effects)

Pharmacokinetics

Onset
Fast
Half-life
about 50 min (in plasma)
Metabolism
Degraded by esterases in the liver.

Contraindications

  • Never injected (protoplasmic poison, causes tissue necrosis).

Side effects

Common
addictionstrong reinforcementpsychological dependence (leading to continuous or occasional use)EuphoriaExcitementMental confusionRestlessnessTremor and twitching of musclesConvulsionsUnconsciousnessRespiratory depressionDeath (dose-dependent)Sense of wellbeingDelays fatigueIncreases power of enduranceBradycardia (due to vagal centre stimulation)Rise in BP (due to vasomotor centre stimulation)NauseaVomiting (due to vomiting centre stimulation)Pyrexia (due to temperature regulating centre stimulation and increased muscular activity)Local vasoconstrictionTachycardiaMydriasisConstriction of conjunctival vesselsClouding of corneaSloughing of cornea
Serious
  • Can worsen psychosis
  • High toxicity due to reduced catecholamine uptake in both the central and peripheral nervous systems and resulting prolongation of transmitter dwell time in the synaptic cleft
  • Abuse potential
  • Strokes
  • Heart attacks
  • Cardiac arrhythmias
  • Myocardial ischemia
  • Myocarditis
  • Aortic dissection
  • Cerebral vasoconstriction
  • Seizures
  • Death from traumatic injuries
  • Premature labor
  • Abruptio placentae
  • Psychiatric disorders (anxiety, depression, psychosis)
  • Tissue necrosis (if injected)

Drug interactions

Adrenaline
Severe
Textbook

Potentiation of adrenaline's action.

Source: KDT 7e · p57

Heroin
Moderate
Textbook

Improved euphoria; reduction of negative side effects from each substance.

Not explicitly stated as this is a combination of illicit drugs.

Source: G&G 14e

Norepinephrine
Moderate
Textbook

Potentiating effect on responses to adrenergic impulses and injected catecholamines.

Not explicitly stated.

Source: G&G 14e · p201, 202

Related guidelines

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Sources: KD Tripathi 7e, Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team