Peringatan Keamanan

Most chloroprocaine overdose cases are related to high plasma levels during its therapeutic use or to the unintended administration of a subarachnoid injection. In mice, the intravenous LD50 of chloroprocaine HCl is 97 mg/kg and the subcutaneous LD50 of chloroprocaine HCl is 950 mg/kg. The first consideration in the management of local anesthetic emergencies is prevention, which can be achieved by carefully monitoring patients’ cardiovascular and respiratory vital signs, as well as their state of consciousness. If there are any changes, oxygen should be administered.L43377,L43382

In patients with chloroprocaine overdose with convulsions, underventilation or apnea, the drug label recommends giving immediate attention to maintaining a patent airway, assisted or controlled ventilation with oxygen and a delivery system capable of permitting immediate positive airway pressure by mask. If convulsions persist, provide small increments of an ultra-short acting barbiturate or a benzodiazepine intravenously. Refer to the chloroprocaine drug label for a complete description of the procedures recommended in case of overdose.L43377,L43382

Chloroprocaine

DB01161

small molecule approved investigational

Deskripsi

Chloroprocaine is an ester local anesthetic commonly available in its salt form, chloroprocaine hydrochloride. Similar to other local anesthetics, it increases the threshold for electrical excitation in nerves by slowing the propagation of the nerve impulse and reducing the rate of rise of the action potential.L43402 The pharmacological profile of chloroprocaine is characterized by a short latency and duration, similar to the one observed with lidocaine.A252952 Chloroprocaine can be given as an injection, and is available in formulations with and without methylparaben as a preservative. Both can be given as intrathecal injections for peripheral and central nerve block, but only the preservative-free formulation can be used for lumbar and caudal epidural blocks.A252952,L43382 Topical chloroprocaine for ophthalmic use was approved by the FDA in September 2022 for ocular surface anesthesia.L43387

Struktur Molekul 2D

Berat 270.755
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) In adults, the average _in vitro_ plasma half-life of chloroprocaine is 21 seconds for males and 25 seconds for females. In neonates, the average _in vitro_ plasma half-life is 43 seconds.[L43382] Following intrapartum epidural anesthesia, the apparent _in vivo_ half-life of chloroprocaine detected in maternal plasma was 3.1 minutes (range from 1.5 to 6.4 minutes).[L43377]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Thanks to its low risk for systemic toxicity, chloroprocaine has a rapid onset of action that usually ranges between 6 to 12 minutes.L43377,L43382,L43402 The duration of chloroprocaine-induced anesthesia may be up to 60 minutes. The absorption rate of local anesthetics depends on the total dose and concentration of chloroprocaine, as well as the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic injection. The presence of epinephrine reduces the rate of absorption and plasma concentration of local anesthetics.L43377,L43382 The systemic exposure to chloroprocaine following its topical ocular administration has not been evaluated.L43387

Metabolisme

In plasma, chloroprocaine is quickly metabolized by pseudocholinesterases, a group of enzymes that perform the hydrolysis of the ester linkage. In ocular tissues, chloroprocaine is metabolized by nonspecific esterases.L43387 The hydrolysis of chloroprocaine leads to the production of ß-diethylaminoethanol and 2-chloro-4-aminobenzoic acid, which inhibits the action of the sulfonamides.L43377,L43382,L43387

Rute Eliminasi

Like most local anesthetics and their metabolites, chloroprocaine is mainly excreted by the kidneys. The urinary excretion of chloroprocaine may be affected by urinary perfusion and factors that have an effect on urinary pH.L43377,L43382,L43387

Interaksi Obat

1765 Data
Buprenorphine Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Chloroprocaine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Chloroprocaine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Chloroprocaine.
Hydrocodone Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Chloroprocaine.
Magnesium sulfate The therapeutic efficacy of Chloroprocaine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Chloroprocaine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Chloroprocaine.
Mirtazapine Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Chloroprocaine.
Orphenadrine Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Chloroprocaine.
Pramipexole Chloroprocaine may increase the sedative activities of Pramipexole.
Ropinirole Chloroprocaine may increase the sedative activities of Ropinirole.
Rotigotine Chloroprocaine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Chloroprocaine.
Sodium oxybate The risk or severity of CNS depression can be increased when Chloroprocaine is combined with Sodium oxybate.
Suvorexant Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Chloroprocaine.
Thalidomide Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Chloroprocaine.
Memantine Memantine may increase the neuromuscular blocking activities of Chloroprocaine.
Pegvisomant Pegvisomant may increase the neuromuscular blocking activities of Chloroprocaine.
Mefloquine The risk or severity of methemoglobinemia can be increased when Mefloquine is combined with Chloroprocaine.
Tacrine Tacrine may increase the neuromuscular blocking activities of Chloroprocaine.
Sulpiride Sulpiride may increase the neuromuscular blocking activities of Chloroprocaine.
Profenamine Profenamine may increase the neuromuscular blocking activities of Chloroprocaine.
Chlorpromazine Chlorpromazine may increase the neuromuscular blocking activities of Chloroprocaine.
Gallamine triethiodide Gallamine triethiodide may increase the neuromuscular blocking activities of Chloroprocaine.
Triflupromazine Triflupromazine may increase the neuromuscular blocking activities of Chloroprocaine.
Cisplatin The risk or severity of methemoglobinemia can be increased when Cisplatin is combined with Chloroprocaine.
Cinchocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Chloroprocaine.
Pyridostigmine Pyridostigmine may increase the neuromuscular blocking activities of Chloroprocaine.
Nizatidine Nizatidine may increase the neuromuscular blocking activities of Chloroprocaine.
Galantamine Galantamine may increase the neuromuscular blocking activities of Chloroprocaine.
Isoflurophate Isoflurophate may increase the neuromuscular blocking activities of Chloroprocaine.
Diethylcarbamazine Diethylcarbamazine may increase the neuromuscular blocking activities of Chloroprocaine.
Procaine The risk or severity of adverse effects can be increased when Procaine is combined with Chloroprocaine.
Minaprine Minaprine may increase the neuromuscular blocking activities of Chloroprocaine.
Terbutaline Terbutaline may increase the neuromuscular blocking activities of Chloroprocaine.
Mechlorethamine The risk or severity of methemoglobinemia can be increased when Mechlorethamine is combined with Chloroprocaine.
Hexafluronium Hexafluronium may increase the neuromuscular blocking activities of Chloroprocaine.
Demecarium Demecarium may increase the neuromuscular blocking activities of Chloroprocaine.
Physostigmine Physostigmine may increase the neuromuscular blocking activities of Chloroprocaine.
Rivastigmine Rivastigmine may increase the neuromuscular blocking activities of Chloroprocaine.
Edrophonium Edrophonium may increase the neuromuscular blocking activities of Chloroprocaine.
Procainamide Procainamide may increase the neuromuscular blocking activities of Chloroprocaine.
Ambenonium Ambenonium may increase the neuromuscular blocking activities of Chloroprocaine.
Tubocurarine Tubocurarine may increase the neuromuscular blocking activities of Chloroprocaine.
Ketamine Ketamine may increase the neuromuscular blocking activities of Chloroprocaine.
Decamethonium Decamethonium may increase the neuromuscular blocking activities of Chloroprocaine.
Pancuronium Pancuronium may increase the neuromuscular blocking activities of Chloroprocaine.
Pipecuronium Pipecuronium may increase the neuromuscular blocking activities of Chloroprocaine.
Ginkgo biloba Ginkgo biloba may increase the neuromuscular blocking activities of Chloroprocaine.
Neostigmine Neostigmine may increase the neuromuscular blocking activities of Chloroprocaine.
Bambuterol Bambuterol may increase the neuromuscular blocking activities of Chloroprocaine.
1,10-Phenanthroline 1,10-Phenanthroline may increase the neuromuscular blocking activities of Chloroprocaine.
Thiotepa The risk or severity of methemoglobinemia can be increased when Thiotepa is combined with Chloroprocaine.
Huperzine A Huperzine A may increase the neuromuscular blocking activities of Chloroprocaine.
Phenserine Phenserine may increase the neuromuscular blocking activities of Chloroprocaine.
Regramostim Regramostim may increase the neuromuscular blocking activities of Chloroprocaine.
Aprotinin Aprotinin may increase the neuromuscular blocking activities of Chloroprocaine.
Betaine Betaine may increase the neuromuscular blocking activities of Chloroprocaine.
Capsaicin The risk or severity of adverse effects can be increased when Capsaicin is combined with Chloroprocaine.
Coumaphos Coumaphos may increase the neuromuscular blocking activities of Chloroprocaine.
Dichlorvos Dichlorvos may increase the neuromuscular blocking activities of Chloroprocaine.
Fenthion Fenthion may increase the neuromuscular blocking activities of Chloroprocaine.
Metrifonate Metrifonate may increase the neuromuscular blocking activities of Chloroprocaine.
Acotiamide Acotiamide may increase the neuromuscular blocking activities of Chloroprocaine.
Methanesulfonyl Fluoride Methanesulfonyl Fluoride may increase the neuromuscular blocking activities of Chloroprocaine.
Paraoxon Paraoxon may increase the neuromuscular blocking activities of Chloroprocaine.
Tyrothricin The risk or severity of methemoglobinemia can be increased when Tyrothricin is combined with Chloroprocaine.
Ipidacrine Ipidacrine may increase the neuromuscular blocking activities of Chloroprocaine.
Distigmine Distigmine may increase the neuromuscular blocking activities of Chloroprocaine.
Tretamine The risk or severity of methemoglobinemia can be increased when Tretamine is combined with Chloroprocaine.
Posiphen Posiphen may increase the neuromuscular blocking activities of Chloroprocaine.
Methylphosphinic Acid Methylphosphinic Acid may increase the neuromuscular blocking activities of Chloroprocaine.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Chloroprocaine.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Chloroprocaine.
Ethanol Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Chloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Chloroprocaine.
Paroxetine The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Paroxetine.
Escitalopram The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Escitalopram.
Fluvoxamine The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Trazodone.
Sertraline The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Nefazodone.
Zimelidine The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Seproxetine.

Target Protein

Sodium/potassium-transporting ATPase subunit alpha-1 ATP1A1
Voltage-gated sodium channel alpha subunit SCN1A
Sodium-dependent dopamine transporter SLC6A3

Referensi & Sumber

Synthesis reference: Marks, HC and Rubin, MI (1949). Alkamine esters of 2-chloro-4-amino benzoic acid. US. Patent 2,460,139 Assigned to Wallace & Tiernan Products, Inc. https://patentimages.storage.googleapis.com/6c/19/84/5af4fc6dc359a3/US2460139.pdf
Artikel (PubMed)
  • PMID: 24601887
    Camponovo C, Wulf H, Ghisi D, Fanelli A, Riva T, Cristina D, Vassiliou T, Leschka K, Fanelli G: Intrathecal 1% 2-chloroprocaine vs. 0.5% bupivacaine in ambulatory surgery: a prospective, observer-blinded, randomised, controlled trial. Acta Anaesthesiol Scand. 2014 May;58(5):560-6. doi: 10.1111/aas.12291. Epub 2014 Mar 6.
  • PMID: 26057879
    Wulf H, Hampl K, Steinfeldt T: Speed spinal anesthesia revisited: new drugs and their clinical effects. Curr Opin Anaesthesiol. 2013 Oct;26(5):613-20. doi: 10.1097/ACO.0b013e3283606b71.

Contoh Produk & Brand

Produk: 27 • International brands: 3
Produk
  • (chloroprocaine Hci
    Injection, solution • 10 mg/1mL • Infiltration; Perineural • US • Approved
  • Chloroprocaine Hci
    Injection, solution • 20 mg/1mL • Epidural; Infiltration; Intracaudal; Perineural • US • Approved
  • Chloroprocaine Hci
    Injection, solution • 20 mg/1mL • Infiltration; Perineural • US • Approved
  • Chloroprocaine Hydrochloride
    Injection, solution • 20 mg/1mL • Epidural; Infiltration • US • Generic • Approved
  • Chloroprocaine Hydrochloride
    Injection, solution • 30 mg/1mL • Epidural; Infiltration • US • Generic • Approved
  • Chloroprocaine Hydrochloride
    Injection, solution • 20 mg/1mL • Epidural; Infiltration; Intracaudal; Perineural • US • Generic • Approved
  • Chloroprocaine Hydrochloride
    Injection, solution • 30 mg/1mL • Epidural; Infiltration; Intracaudal; Perineural • US • Generic • Approved
  • Chloroprocaine Hydrochloride
    Injection, solution • 20 mg/1mL • Epidural; Infiltration; Intracaudal • US • Generic • Approved
Menampilkan 8 dari 27 produk.
International Brands
  • Iheezo — Harrow Eye, LLC
  • Nesacaine-CE — AstraZeneca
  • Piocaine

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