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Bupivacaine Hydrochloride And Epinephrine (Bupivacaine Hydrochloride)
Bupivacaine blocks nerve impulse generation and conduction by increasing electrical excitation threshold and slowing action potential rise.
Bupivacaine hydrochloride is an amide local anesthetic indicated for production of local or regional anesthesia in adults for surgical, dental, diagnostic, therapeutic, and obstetrical procedures. It blocks nerve impulses by increasing electrical excitation threshold with a half-life of 2.7 hours and high protein binding of 95%. Significant risks include contraindication in obstetrical paracervical block and intravenous regional anesthesia, with serious drug interactions involving sympathomimetic potentiation and cardiac arrhythmias. Clinical use requires careful patient selection and monitoring for systemic toxicity, particularly with concurrent medications affecting cardiovascular function.
At a glance
| Generic name | Bupivacaine Hydrochloride |
|---|---|
| Sponsor | Pfizer |
| Drug class | Amide local anesthetic |
| Target | Nerve sodium channels |
| Modality | Small molecule |
| Phase | FDA-approved |
| First approval | 1972 |
Mechanism of action
Bupivacaine blocks the generation and conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. The progression of anesthesia follows a specific order of nerve function loss: pain, temperature, touch, proprioception, and skeletal muscle tone, related to the diameter, myelination, and conduction velocity of affected nerve fibers. Epinephrine is added as a vasoconstrictor to slow absorption into the general circulation and prolong maintenance of active tissue concentration.
Approved indications
- Anesthesia for cesarean section
- Itching of skin
- Local Anesthesia for Ophthalmologic Procedure
- Local anesthesia
- Local anesthetic intrathecal block
- Major Nerve Block for Surgery
- Minor Skin Wound Pain
- Regional Anesthesia for Labor Pain
- Regional Anesthesia for Ophthalmologic Surgery
- Regional Anesthesia for Postoperative Pain
- Regional Anesthesia for Surgery
- Skin irritation
Common side effects
- Headache
- Nausea
- Constipation
- Dizziness
- Hypoaesthesia
- Paraesthesia
- Postoperative swelling
- Back pain
- Hypoxia
- Infusion site oedema
- Pain in extremity
- Pruritis
Drug interactions
- Local anesthetics
- Monoamine oxidase inhibitors and tricyclic antidepressants
- Ergot-type oxytocic drugs
- Nonselective beta-adrenergic antagonists
- Drugs associated with methemoglobinemia (nitrates, nitrites, antineoplastic agents, antibiotics, antimalarials, anticonvulsants)
- Potent inhalation anesthetics
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Bupivacaine Hydrochloride And Epinephrine CI brief — competitive landscape report
- Bupivacaine Hydrochloride And Epinephrine updates RSS · CI watch RSS
- Pfizer portfolio CI