Peringatan Keamanan

High systemic doses of ropivacaine can result in central nervous system (CNS) and cardiovascular effects, with the CNS effects usually occurring at lower blood plasma concentrations and additional cardiovascular effects occurring at higher concentrations (although cardiovascular collapse may occur at lower concentrations). CNS effects include CNS excitation involving nervousness, tingling around the mouth, tinnitus, tremor, dizziness, blurred vision, and seizures. CNS depressant effects may follow, associated with drowsiness, loss of consciousness, respiratory depression and apnea. Cardiovascular events may be caused by hypoxemia secondary to respiratory depression and include hypotension, bradycardia, arrhythmias, and/or cardiac arrest.L42140,L42265

Ropivacaine

DB00296

small molecule approved

Deskripsi

Ropivacaine is an aminoamide local anesthetic drug marketed by AstraZeneca under the trade name Naropin. It exists as a racemate of its S- and R-enantiomers, although the marketed form is supplied only as the purified S-enantiomer.L42140

Struktur Molekul 2D

Berat 274.4011
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal half-life of ropivacaine is 1.8 ± 0.7 hours after intravascular administration and 4.2 ± 1 hour after epidural administration.[L42140]
Volume Distribusi Following intravascular infusion, ropivacaine has a steady-state volume of distribution of 41 ± 7 liters.[L42140] Ropivacaine is able to readily cross the placenta.[L42140]
Klirens (Clearance) Following intravenous administration, ropivacaine has a mean plasma clearance of 387 ± 107 mL/min, an unbound plasma clearance of 7.2 ± 1.6 L/min, and a renal clearance of 1 mL/min.[L42140]

Absorpsi

Ropivacaine pharmacokinetics are highly dependent on the dose, route of administration, and patient condition. Following epidural administration ropivacaine undergoes complete and biphasic absorption.L42140

Metabolisme

Ropivacaine undergoes extensive metabolism, primarily via CYP1A2-mediated aromatic hydroxylation to 3-OH-ropivacaine.L42140 The main metabolites excreted in the urine are the N-dealkylated metabolite (PPX) and 3-OH-ropivacaine. Other identified metabolites include 4-OH-ropivacaine, the 3-hydroxy-N-dealkylated (3-OH-PPX) and 4-hydroxy-N-dealkylated (4-OH-PPX) metabolites, and 2-hydroxy-methyl-ropivacaine (which has been identified but not quantified).L42140 Unbound PPX, 3-hydroxy-, and 4-hydroxy-ropivacaine have demonstrated pharmacological activity in animal models less than that of ropivacaine.L42140

Rute Eliminasi

Following intravenous administration, 86% of the administered dose of ropivacaine is excreted in the urine, 1% of which comprises unchanged parent drug.L42140

Interaksi Obat

2327 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Ropivacaine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Ropivacaine is combined with Levodopa.
Risperidone Ropivacaine may increase the hypotensive activities of Risperidone.
Deferasirox The serum concentration of Ropivacaine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Ropivacaine can be increased when it is combined with Peginterferon alfa-2b.
Fluvoxamine The serum concentration of Ropivacaine can be increased when it is combined with Fluvoxamine.
Leflunomide The serum concentration of Ropivacaine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Ropivacaine can be decreased when it is combined with Teriflunomide.
Buprenorphine Ropivacaine 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 Ropivacaine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Ropivacaine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Ropivacaine.
Hydrocodone Ropivacaine 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 Ropivacaine.
Magnesium sulfate The therapeutic efficacy of Ropivacaine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Ropivacaine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Ropivacaine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Ropivacaine.
Mirtazapine Ropivacaine 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 Ropivacaine.
Orphenadrine Ropivacaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Ropivacaine 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 Ropivacaine.
Pramipexole Ropivacaine may increase the sedative activities of Pramipexole.
Ropinirole Ropivacaine may increase the sedative activities of Ropinirole.
Rotigotine Ropivacaine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Ropivacaine.
Sodium oxybate The risk or severity of CNS depression can be increased when Ropivacaine is combined with Sodium oxybate.
Suvorexant Ropivacaine 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 Ropivacaine.
Thalidomide Ropivacaine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Ropivacaine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Prilocaine The risk or severity of methemoglobinemia can be increased when Ropivacaine is combined with Prilocaine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Ropivacaine.
Abiraterone The serum concentration of Ropivacaine can be increased when it is combined with Abiraterone.
Nicorandil Nicorandil may increase the hypotensive activities of Ropivacaine.
Cyproterone acetate The metabolism of Ropivacaine can be increased when combined with Cyproterone acetate.
Ethanol Ropivacaine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Ropivacaine 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 Ropivacaine.
Sibutramine The risk or severity of adverse effects can be increased when Ropivacaine is combined with Sibutramine.
Milnacipran The risk or severity of adverse effects can be increased when Ropivacaine is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Ropivacaine is combined with Desvenlafaxine.
Levomilnacipran Ropivacaine may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Citalopram The risk or severity of adverse effects can be increased when Ropivacaine is combined with Citalopram.
Trazodone The risk or severity of adverse effects can be increased when Ropivacaine is combined with Trazodone.
Sertraline The risk or severity of adverse effects can be increased when Ropivacaine is combined with Sertraline.
Escitalopram The risk or severity of adverse effects can be increased when Ropivacaine is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Ropivacaine is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Ropivacaine is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Ropivacaine is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Ropivacaine is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Ropivacaine is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Ropivacaine is combined with Alaproclate.
Dapsone The risk or severity of methemoglobinemia can be increased when Dapsone is combined with Ropivacaine.
Technetium Tc-99m tilmanocept Ropivacaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Linezolid The risk or severity of methemoglobinemia can be increased when Linezolid is combined with Ropivacaine.
Furazolidone Furazolidone may increase the orthostatic hypotensive activities of Ropivacaine.
Tranylcypromine Tranylcypromine may increase the orthostatic hypotensive activities of Ropivacaine.
Phenelzine Phenelzine may increase the orthostatic hypotensive activities of Ropivacaine.
Minaprine Minaprine may increase the orthostatic hypotensive activities of Ropivacaine.
Selegiline Selegiline may increase the orthostatic hypotensive activities of Ropivacaine.
Procarbazine The risk or severity of methemoglobinemia can be increased when Procarbazine is combined with Ropivacaine.
Moclobemide Moclobemide may increase the orthostatic hypotensive activities of Ropivacaine.
Isocarboxazid Isocarboxazid may increase the orthostatic hypotensive activities of Ropivacaine.
Rasagiline Rasagiline may increase the orthostatic hypotensive activities of Ropivacaine.
Pargyline Pargyline may increase the orthostatic hypotensive activities of Ropivacaine.
Clorgiline Clorgiline may increase the orthostatic hypotensive activities of Ropivacaine.
Iproniazid Iproniazid may increase the orthostatic hypotensive activities of Ropivacaine.
Nialamide Nialamide may increase the orthostatic hypotensive activities of Ropivacaine.
Safinamide Safinamide may increase the orthostatic hypotensive activities of Ropivacaine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Ropivacaine.
Methylene blue Methylene blue may increase the orthostatic hypotensive activities of Ropivacaine.
Hydracarbazine Hydracarbazine may increase the orthostatic hypotensive activities of Ropivacaine.
Pirlindole Pirlindole may increase the orthostatic hypotensive activities of Ropivacaine.
Toloxatone Toloxatone may increase the orthostatic hypotensive activities of Ropivacaine.
Benmoxin Benmoxin may increase the orthostatic hypotensive activities of Ropivacaine.
Mebanazine Mebanazine may increase the orthostatic hypotensive activities of Ropivacaine.
Octamoxin Octamoxin may increase the orthostatic hypotensive activities of Ropivacaine.
Pheniprazine Pheniprazine may increase the orthostatic hypotensive activities of Ropivacaine.
Phenoxypropazine Phenoxypropazine may increase the orthostatic hypotensive activities of Ropivacaine.
Pivhydrazine Pivhydrazine may increase the orthostatic hypotensive activities of Ropivacaine.
Safrazine Safrazine may increase the orthostatic hypotensive activities of Ropivacaine.
Caroxazone Caroxazone may increase the orthostatic hypotensive activities of Ropivacaine.
Harmaline Harmaline may increase the orthostatic hypotensive activities of Ropivacaine.
Brofaromine Brofaromine may increase the orthostatic hypotensive activities of Ropivacaine.
Benzatropine Benzatropine may decrease the excretion rate of Ropivacaine which could result in a higher serum level.
Lamotrigine The risk or severity of methemoglobinemia can be increased when Lamotrigine is combined with Ropivacaine.
Propantheline Ropivacaine may decrease the excretion rate of Propantheline which could result in a higher serum level.
Dicyclomine Ropivacaine may decrease the excretion rate of Dicyclomine which could result in a higher serum level.
Tolterodine Ropivacaine may decrease the excretion rate of Tolterodine which could result in a higher serum level.
Doxacurium The risk or severity of CNS depression can be increased when Ropivacaine is combined with Doxacurium.
Flavoxate Ropivacaine may decrease the excretion rate of Flavoxate which could result in a higher serum level.
Tiotropium Ropivacaine may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Fesoterodine Ropivacaine may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Aclidinium Ropivacaine may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Trimebutine Ropivacaine may decrease the excretion rate of Trimebutine which could result in a higher serum level.
Imidafenacin Ropivacaine may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Ropivacaine may decrease the excretion rate of Propiverine which could result in a higher serum level.
Promethazine The risk or severity of CNS depression can be increased when Ropivacaine is combined with Promethazine.

Target Protein

Sodium channel protein type 10 subunit alpha SCN10A

Referensi & Sumber

Synthesis reference: Peter Jaksch, "Process for the preparation of ropivacaine hydrochloride monohydrate." U.S. Patent US5959112, issued February, 1970.

Contoh Produk & Brand

Produk: 87 • International brands: 0
Produk
  • Dexopin
    Kit • - • Topical • US
  • Naropin
    Injection, solution • 5 mg/1mL • Epidural; Infiltration; Perineural • US • Approved
  • Naropin
    Injection, solution • 7.5 mg/1mL • Epidural; Perineural • US • Approved
  • Naropin
    Injection, solution • 2 mg/1mL • Epidural; Infiltration • US • Approved
  • Naropin
    Injection, solution • 5 mg/1mL • Epidural; Infiltration; Perineural • US • Approved
  • Naropin
    Injection, solution • 10 mg/1mL • Epidural • US • Approved
  • Naropin
    Solution • 2 mg / mL • Epidural; Infiltration • Canada • Approved
  • Naropin
    Solution • 5 mg / mL • Epidural; Infiltration • Canada • Approved
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