Peringatan Keamanan

The oral LD50 in rats was 238 mg/kg.L47951

There is limited clinical experience with levomilnacipran overdose in humans. In clinical studies, cases of ingestions up to 360 mg daily were reported with none being fatal. As there is no known specific antidote, levomilnacipran overdose should be managed with supportive measures, including close medical supervision and monitoring, with the consideration of possible multiple drug involvement. The high volume of distribution of levomilnacipran suggests that dialysis will not be effective in reducing levomilnacipran plasma concentrations.L47946

Levomilnacipran

DB08918

small molecule approved investigational

Deskripsi

Levomilnacipran is a selective serotonin and norepinephrine reuptake inhibitor (SNRI), although it is a more potent inhibitor of norepinephrine reuptake than serotonin reuptake.A261181, A38560 Levomilnacipran is the more active 1S,2R-enantiomer in the racemate milnacipran.A261181, L47956 Once administered, interconversion between levomilnacipran and its stereoisomer does not occur in humans.L47946 First approved by the FDA on July 25, 2013, levomilnacipran is used to treat major depressive disorder in adults.L47956 While levomilnacipran was previously investigated and proposed as a potential treatment for stroke in Europe, the EMA decided against this use.L48011

Struktur Molekul 2D

Berat 246.348
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent terminal elimination half-life of extended-release levomilnacipran is approximately 12 hours.[L47946]
Volume Distribusi Levomilnacipran is widely distributed, with an apparent volume of distribution ranging from 387 to 473 L.[L47946]
Klirens (Clearance) Following oral administration, the mean apparent total clearance of levomilnacipran is 21-29 L/h.[L47946]

Absorpsi

The steady-state concentration of levomilnacipran was dose-proportional when administered at a dose ranging from 25 mg to 300 mg (2.5 times the maximum recommended dosage of levomilnacipran) once daily. After daily dosing of 120 mg levomilnacipran, the mean Cmax value was 341 ng/mL, and the mean steady-state AUC value was 5196 ng x h/mL.L47946 The relative bioavailability of oral levomilnacipran extended-release capsules was 92% when compared to oral solution. The median time to peak concentration (Tmax) of levomilnacipran ranges from six to eight hours after oral administration. Levomilnacipran concentration was not significantly affected when it was administered with food.L47946

Metabolisme

Levomilnacipran undergoes desethylation to form desethyl levomilnacipran (or N-desethyl levomilnacipran) and hydroxylation to form p-hydroxy-levomilnacipran, which are pharmacologically inactive. Both oxidative metabolites can undergo further glucuronidation. Desethylation is primarily catalyzed by CYP3A4 with minor contributions by CYP2C8, 2C19, 2D6, and 2J2.A38560, L47946

Rute Eliminasi

Levomilnacipran and its metabolites are eliminated primarily by renal excretion. Following oral administration of 14C-levomilnacipran solution, approximately 58% of the dose is excreted in urine as unchanged levomilnacipran. N-desethyl levomilnacipran was the major metabolite excreted in the urine, accounting for approximately 18% of the dose. Other identifiable metabolites excreted in the urine were levomilnacipran glucuronide (4%), desethyl levomilnacipran glucuronide (3%), p-hydroxy levomilnacipran glucuronide (1%), and p-hydroxy levomilnacipran (1%).L47946

Interaksi Makanan

5 Data
  • 1. Avoid alcohol. Ingesting alcohol may compromise the extended-release dosage form of levomilnacipran, causing an accelerated release of the drug and increasing its serum concentration.
  • 2. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Taking herbs with antiplatelet or anticoagulant activity may increase the risk of bleeding.
  • 3. Exercise caution with grapefruit products. Grapefruit is a moderate to strong CYP3A4 inhibitor. Do not exceed a maximum levomilnacipran dose of 80mg daily when taking strong CYP3A4 inhibitors.
  • 4. Exercise caution with St. John's Wort. Administering levomilnacipran with St. John's Wort may increase the risk of serotonin syndrome.
  • 5. Take with or without food. Food does not affect drug absorption and exposure to a clinically significant extent.

Interaksi Obat

1554 Data
Cyproheptadine The risk or severity of Tachycardia can be increased when Cyproheptadine is combined with Levomilnacipran.
Desmopressin Desmopressin may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Ioflupane I-123 Levomilnacipran may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.
Linezolid Linezolid may increase the serotonergic activities of Levomilnacipran.
Pimozide The risk or severity of adverse effects can be increased when Levomilnacipran is combined with Pimozide.
Buprenorphine The risk or severity of serotonin syndrome can be increased when Buprenorphine is combined with Levomilnacipran.
Doxylamine The risk or severity of Tachycardia can be increased when Doxylamine is combined with Levomilnacipran.
Dronabinol The risk or severity of adverse effects can be increased when Dronabinol is combined with Levomilnacipran.
Droperidol The risk or severity of adverse effects can be increased when Levomilnacipran is combined with Droperidol.
Hydrocodone The risk or severity of serotonin syndrome can be increased when Hydrocodone is combined with Levomilnacipran.
Methotrimeprazine The risk or severity of serotonin syndrome can be increased when Methotrimeprazine is combined with Levomilnacipran.
Nabilone The risk or severity of adverse effects can be increased when Nabilone is combined with Levomilnacipran.
Orphenadrine The risk or severity of Tachycardia can be increased when Orphenadrine is combined with Levomilnacipran.
Perampanel The metabolism of Levomilnacipran can be increased when combined with Perampanel.
Pramipexole Pramipexole may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Rotigotine The risk or severity of serotonin syndrome can be increased when Rotigotine is combined with Levomilnacipran.
Rufinamide The metabolism of Levomilnacipran can be increased when combined with Rufinamide.
Tapentadol The risk or severity of serotonin syndrome can be increased when Tapentadol is combined with Levomilnacipran.
Thalidomide The metabolism of Levomilnacipran can be increased when combined with Thalidomide.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Levomilnacipran.
Methadone The risk or severity of serotonin syndrome can be increased when Methadone is combined with Levomilnacipran.
Digoxin The risk or severity of hypotension can be increased when Levomilnacipran is combined with Digoxin.
Metildigoxin The risk or severity of hypotension can be increased when Levomilnacipran is combined with Metildigoxin.
Acetyldigoxin The risk or severity of hypotension can be increased when Levomilnacipran is combined with Acetyldigoxin.
Mifepristone The metabolism of Levomilnacipran can be increased when combined with Mifepristone.
Mirabegron Levomilnacipran may increase the tachycardic activities of Mirabegron.
Clomipramine The risk or severity of adverse effects can be increased when Clomipramine is combined with Levomilnacipran.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Levomilnacipran.
Acetylsalicylic acid Levomilnacipran may increase the antiplatelet activities of Acetylsalicylic acid.
Mirtazapine The risk or severity of serotonin syndrome can be increased when Mirtazapine is combined with Levomilnacipran.
Morphine The risk or severity of serotonin syndrome can be increased when Morphine is combined with Levomilnacipran.
Hydromorphone The risk or severity of serotonin syndrome can be increased when Hydromorphone is combined with Levomilnacipran.
Oxycodone The risk or severity of serotonin syndrome can be increased when Oxycodone is combined with Levomilnacipran.
Butorphanol The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Levomilnacipran.
Dextropropoxyphene The risk or severity of serotonin syndrome can be increased when Dextropropoxyphene is combined with Levomilnacipran.
Pentazocine The risk or severity of serotonin syndrome can be increased when Pentazocine is combined with Levomilnacipran.
Sufentanil The risk or severity of serotonin syndrome can be increased when Sufentanil is combined with Levomilnacipran.
Nalbuphine The risk or severity of serotonin syndrome can be increased when Nalbuphine is combined with Levomilnacipran.
Levorphanol The risk or severity of serotonin syndrome can be increased when Levorphanol is combined with Levomilnacipran.
Remifentanil The risk or severity of serotonin syndrome can be increased when Remifentanil is combined with Levomilnacipran.
Diphenoxylate The risk or severity of serotonin syndrome can be increased when Diphenoxylate is combined with Levomilnacipran.
Oxymorphone The risk or severity of serotonin syndrome can be increased when Oxymorphone is combined with Levomilnacipran.
Dezocine The risk or severity of serotonin syndrome can be increased when Dezocine is combined with Levomilnacipran.
Methadyl acetate The risk or severity of serotonin syndrome can be increased when Methadyl acetate is combined with Levomilnacipran.
Dihydroetorphine The risk or severity of serotonin syndrome can be increased when Dihydroetorphine is combined with Levomilnacipran.
Ethylmorphine The risk or severity of serotonin syndrome can be increased when Ethylmorphine is combined with Levomilnacipran.
Etorphine The risk or severity of serotonin syndrome can be increased when Etorphine is combined with Levomilnacipran.
Dextromoramide The risk or severity of serotonin syndrome can be increased when Dextromoramide is combined with Levomilnacipran.
Carfentanil The risk or severity of serotonin syndrome can be increased when Carfentanil is combined with Levomilnacipran.
Dihydrocodeine The risk or severity of serotonin syndrome can be increased when Dihydrocodeine is combined with Levomilnacipran.
Alphacetylmethadol The risk or severity of serotonin syndrome can be increased when Alphacetylmethadol is combined with Levomilnacipran.
Dihydromorphine The risk or severity of serotonin syndrome can be increased when Dihydromorphine is combined with Levomilnacipran.
Ketobemidone The risk or severity of serotonin syndrome can be increased when Ketobemidone is combined with Levomilnacipran.
DPDPE The risk or severity of serotonin syndrome can be increased when DPDPE is combined with Levomilnacipran.
Lofentanil The risk or severity of serotonin syndrome can be increased when Lofentanil is combined with Levomilnacipran.
Opium The risk or severity of serotonin syndrome can be increased when Opium is combined with Levomilnacipran.
Normethadone The risk or severity of serotonin syndrome can be increased when Normethadone is combined with Levomilnacipran.
Piritramide The risk or severity of serotonin syndrome can be increased when Piritramide is combined with Levomilnacipran.
Alphaprodine The risk or severity of serotonin syndrome can be increased when Alphaprodine is combined with Levomilnacipran.
Meptazinol The risk or severity of serotonin syndrome can be increased when Meptazinol is combined with Levomilnacipran.
Phenoperidine The risk or severity of serotonin syndrome can be increased when Phenoperidine is combined with Levomilnacipran.
Phenazocine The risk or severity of serotonin syndrome can be increased when Phenazocine is combined with Levomilnacipran.
Tilidine The risk or severity of serotonin syndrome can be increased when Tilidine is combined with Levomilnacipran.
Bezitramide The risk or severity of serotonin syndrome can be increased when Bezitramide is combined with Levomilnacipran.
Eluxadoline The risk or severity of serotonin syndrome can be increased when Eluxadoline is combined with Levomilnacipran.
Nicomorphine The risk or severity of serotonin syndrome can be increased when Nicomorphine is combined with Levomilnacipran.
Codeine The risk or severity of serotonin syndrome can be increased when Codeine is combined with Levomilnacipran.
Meperidine The risk or severity of serotonin syndrome can be increased when Meperidine is combined with Levomilnacipran.
Alfentanil The risk or severity of serotonin syndrome can be increased when Alfentanil is combined with Levomilnacipran.
Fentanyl The risk or severity of serotonin syndrome can be increased when Fentanyl is combined with Levomilnacipran.
Levacetylmethadol The risk or severity of serotonin syndrome can be increased when Levacetylmethadol is combined with Levomilnacipran.
Iobenguane The therapeutic efficacy of Iobenguane can be decreased when used in combination with Levomilnacipran.
Methyclothiazide Methyclothiazide may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Chlorthalidone Chlorthalidone may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Bendroflumethiazide Bendroflumethiazide may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Metolazone Metolazone may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Benzthiazide Benzthiazide may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Hydroflumethiazide Hydroflumethiazide may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Indapamide Indapamide may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Chlorothiazide Chlorothiazide may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Hydrochlorothiazide Hydrochlorothiazide may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Trichlormethiazide Trichlormethiazide may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Polythiazide Polythiazide may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Quinethazone Quinethazone may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Cyclopenthiazide Cyclopenthiazide may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Epitizide Epitizide may increase the excretion rate of Levomilnacipran which could result in a lower serum level and potentially a reduction in efficacy.
Baclofen Baclofen may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Butabarbital Butabarbital may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Etomidate Levomilnacipran may increase the tachycardic activities of Etomidate.
Tolcapone Tolcapone may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Cetirizine Cetirizine may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Chlorzoxazone Chlorzoxazone may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Thiethylperazine The risk or severity of adverse effects can be increased when Levomilnacipran is combined with Thiethylperazine.
Palonosetron The risk or severity of serotonin syndrome can be increased when Palonosetron is combined with Levomilnacipran.
Gallamine triethiodide The risk or severity of Tachycardia can be increased when Gallamine triethiodide is combined with Levomilnacipran.
Dextromethorphan The risk or severity of serotonin syndrome can be increased when Dextromethorphan is combined with Levomilnacipran.
Mazindol The risk or severity of serotonin syndrome can be increased when Mazindol is combined with Levomilnacipran.
Lisuride The risk or severity of serotonin syndrome can be increased when Lisuride is combined with Levomilnacipran.
Dexmedetomidine Levomilnacipran may increase the tachycardic activities of Dexmedetomidine.
Metaxalone The risk or severity of serotonin syndrome can be increased when Metaxalone is combined with Levomilnacipran.

Target Protein

Sodium-dependent serotonin transporter SLC6A4
Sodium-dependent noradrenaline transporter SLC6A2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25657584
    Asnis GM, Henderson MA: Levomilnacipran for the treatment of major depressive disorder: a review. Neuropsychiatr Dis Treat. 2015 Jan 9;11:125-35. doi: 10.2147/NDT.S54710. eCollection 2015.
  • PMID: 24524592
    Mago R, Mahajan R, Thase ME: Levomilnacipran: a newly approved drug for treatment of major depressive disorder. Expert Rev Clin Pharmacol. 2014 Mar;7(2):137-45. doi: 10.1586/17512433.2014.889563.
  • PMID: 26572745
    Bruno A, Morabito P, Spina E, Muscatello MR: The Role of Levomilnacipran in the Management of Major Depressive Disorder: A Comprehensive Review. Curr Neuropharmacol. 2016;14(2):191-9.

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