Pharmacology · Local anesthetics
Cocaine !
The only local anaesthetic that constricts vessels: a nasal solution for nose surgery. It raises blood pressure, can cause infarction and is often abused.
Updated 2026-11-01
Also called: Cocaine hydrochloride
The figure shows cocaine bound to the human dopamine transporter in its outward-open conformation.
Mechanism of action
Cocaine, an ester of benzoic acid, blocks nerve sodium channels like other local anaesthetics. It also inhibits noradrenaline reuptake at sympathetic nerve endings, which constricts mucosal vessels (less bleeding) and stimulates the heart; in the central nervous system it blocks the dopamine transporter, which explains euphoria and addiction.
- Blocks the sodium channel: mucosal anaesthesia
- Inhibits noradrenaline reuptake: vasoconstriction
- More catecholamines: tachycardia and hypertension
- Blocks the dopamine transporter: euphoria and addiction
Pharmacokinetics
- Absorption
- Topical on the nasal mucosa; part is absorbed into the circulation.
- Metabolism
- Non-enzymatic ester hydrolysis and hepatic carboxylesterases, plasma cholinesterase and CYP3A4.
- Elimination
- Mainly by metabolism; little unchanged in urine.
Indications
- Local anaesthesia of the nasal mucosa for diagnostic procedures and surgery on or through the nasal cavities in adults
Adverse effects
Common
- Hypertension
- Tachycardia
Contraindications
- Hypersensitivity to cocaine or ester-type anaesthetics
- Avoided with recent myocardial infarction, coronary disease, heart failure, arrhythmias or uncontrolled hypertension
Key interactions
- Epinephrine and phenylephrine
- Additive vasoconstriction and cardiac stimulation; combining them in nasal surgery is avoided.
- Reserpine
- Enhances sympathetic stimulation: severe hypertension and arrhythmias.
- Cholinesterase inhibitors
- Raise the risk of cocaine toxicity.
What is monitored
- Blood pressure, heart rate and rhythm after application
- ECG when there are cardiovascular risk factors
- Signs of seizure or agitation
Administration and safety
- Controlled medicine (high abuse potential): secure storage, records and documented destruction of leftovers.
- Topical use on the nasal mucosa only; it is not injected.
- Not combined with other vasoconstrictors in the same procedure.
Nursing care
- Before: ask about heart disease, hypertension, seizures and substance use.
- After: watch blood pressure, pulse, chest pain and neurological signs.
- Account for the units used and the leftovers.
Pregnancy and breastfeeding
There are no data on its medical use in pregnant women; chronic cocaine use in pregnancy is associated with adverse maternal, fetal and neonatal outcomes.
Test yourself
Think of the answer, then tap the question to see it.
Which property sets cocaine apart from other local anaesthetics?
It causes vasoconstriction, because it inhibits noradrenaline reuptake; other local anaesthetics tend to dilate vessels.
Why is epinephrine not combined with cocaine in nasal surgery?
Both increase catecholamines at the receptors: hypertension, arrhythmias and myocardial ischaemia.
Which transporter explains cocaine euphoria and addiction?
The dopamine transporter of the central nervous system, which cocaine blocks.
Related drugs
← Back to the class: Local anesthetics
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - COCAINE HYDROCHLORIDE NASAL solution (DailyMed (U.S. National Library of Medicine), 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 25 (McGraw Hill, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.