About: Milnacipran     Goto   Sponge   NotDistinct   Permalink

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http://linked.open...gbank/description
  • Milnacipran is an antidepressant of the serotonin-norepinephrine reuptake inhibitor class. It more potently inhibits norepinephrine uptake than serotonin. It is provided as a racemic mixture. FDA approved in January 2009. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Leo RJ, Brooks VL: Clinical potential of milnacipran, a serotonin and norepinephrine reuptake inhibitor, in pain. Curr Opin Investig Drugs. 2006 Jul;7(7):637-42. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16869117 # Sato S, Yamakawa Y, Terashima Y, Ohta H, Asada T: Efficacy of milnacipran on cognitive dysfunction with post-stroke depression: preliminary open-label study. Psychiatry Clin Neurosci. 2006 Oct;60(5):584-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16958942 # Simon LS: Is milnacipran effective in treating pain in patients with fibromyalgia? Nat Clin Pract Rheumatol. 2006 Mar;2(3):126-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16932669 # Soya A, Terao T, Nakajima M, Kojima H, Okamoto T, Inoue Y, Iwakawa M, Shinkai K, Yoshimura R, Ueta Y, Nakamura J: Effects of repeated milnacipran administration on brain serotonergic and noradrenergic functions in healthy volunteers. Psychopharmacology (Berl). 2006 Sep;187(4):526-7. Epub 2006 Jul 8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16830129 # King T, Rao S, Vanderah T, Chen Q, Vardanyan A, Porreca F: Differential blockade of nerve injury-induced shift in weight bearing and thermal and tactile hypersensitivity by milnacipran. J Pain. 2006 Jul;7(7):513-20. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16814690 # Moojen VK, Martins MR, Reinke A, Feier G, Agostinho FR, Cechin EM, Quevedo J: Effects of milnacipran in animal models of anxiety and memory. Neurochem Res. 2006 Apr;31(4):571-7. Epub 2006 May 9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16758367 # Moret C, Charveron M, Finberg JP, Couzinier JP, Briley M: Biochemical profile of midalcipran (F 2207), 1-phenyl-1-diethyl-aminocarbonyl-2-aminomethyl-cyclopropane (Z) hydrochloride, a potential fourth generation antidepressant drug. Neuropharmacology. 1985 Dec;24(12):1211-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/3005901 # Briley M, Prost JF, Moret C: Preclinical pharmacology of milnacipran. Int Clin Psychopharmacol. 1996 Sep;11 Suppl 4:9-14. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8923122 # Puozzo C, Panconi E, Deprez D: Pharmacology and pharmacokinetics of milnacipran. Int Clin Psychopharmacol. 2002 Jun;17 Suppl 1:S25-35. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12369608 # Leinonen E, Lepola U, Koponen H, Mehtonen OP, Rimon R: Long-term efficacy and safety of milnacipran compared to clomipramine in patients with major depression. Acta Psychiatr Scand. 1997 Dec;96(6):497-504. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/9421348 # Papakostas GI, Fava M: A meta-analysis of clinical trials comparing milnacipran, a serotonin--norepinephrine reuptake inhibitor, with a selective serotonin reuptake inhibitor for the treatment of major depressive disorder. Eur Neuropsychopharmacol. 2007 Jan;17(1):32-6. Epub 2006 Jun 8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16762534 # Kako Y, Niwa Y, Toyomaki A, Yamanaka H, Kitagawa N, Denda K, Koyama T: A case of adult attention-deficit/hyperactivity disorder alleviated by milnacipran. Prog Neuropsychopharmacol Biol Psychiatry. 2007 Apr 13;31(3):772-5. Epub 2007 Jan 12. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17300859 # Bernstein CD, Albrecht KL, Marcus DA: Milnacipran for fibromyalgia: a useful addition to the treatment armamentarium. Expert Opin Pharmacother. 2013 Mar 19. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23506481 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • The terminal elimination half-life, when given to healthy subjects is 6-8 hours. When given to severe renal impairment patients is 7 - 10 hours. The active enantiomer, d-milnacipran, has a longer elimination half-life (8-10 hours) than the l-enantiomer (4-6 hours). (en)
http://linked.open...ugbank/indication
  • Milnacipran is used to treat moderate to severe clinical depression but this indication is not yet FDA-approved in the USA. Milnacipran is labelled for the treatment of fibromyalgia pain. (en)
sameAs
Title
  • Milnacipran (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Milnacipran inhibits norepinephrine and serotonin reuptake in a 3:1 ratio, in practical use this means a balanced (equal) action upon both transmitters. The serotonin reuptake inhibition is likely to improve depression, while the norepinephrine reuptake inihibition probably improves chronic pain. Milnacipran exerts no significant actions on postynaptic H1, alpha-1, D1, D2, and muscarinic receptors, as well as on benzodiazepine/opiate binding sites. [Wikipedia] (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • It is excreted predominantly unchanged in urine (50%- 60%, 24% as l-milnacipran and 31% as d-milnacipran). The l-milnacipran carbamoyl-O-glucuronide was the major metabolite excreted in urine and accounted for approximately 17% of the dose; approximately 2% of the dose was excreted in urine as d-milnacipran carbamoyl-O-glucuronide. Approximately 8% of the dose was excreted in urine as the N-desethyl milnacipran metabolite. (en)
http://linked.open.../drugbank/synonym
  • Milnacipran (en)
  • (-)-milnacipran (en)
  • Midalcipran (en)
  • Milnacipranum (en)
http://linked.open...drugbank/toxicity
  • LD50, oral, rat: 213 mg/kg. The most frequently occurring adverse reactions (≥ 5% and greater than placebo) were nausea, headache, constipation, dizziness, insomnia, hot flush, hyperhidrosis, vomiting, palpitations, heart rate increased, dry mouth, and hypertension. (en)
http://linked.open...umeOfDistribution
  • 400 L, following a single IV dose to a healthy subject. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...nk/proteinBinding
  • Plasma protein binding is 13%. (en)
http://linked.open...ogy/drugbank/salt
  • (en)
http://linked.open...ynthesisReference
  • Jean Deregnaucourt, "Use of the (1S,2R) enantiomer of milnacipran for the preparation of a drug." U.S. Patent US20040259953, issued December 23, 2004. (en)
http://linked.open...y/mesh/hasConcept
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http://linked.open...ugbank/absorption
  • Milnacipran is well absorbed following oral administration with an absolute bioavailability of 85-90%. Meals have no effect on absorption. Peak concentrations occur 2 -4 hours post-administration and is delayed in elderly patients. Time to steady state = 36 - 48 hours; (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 92623-85-3 (en)
http://linked.open...drugbank/category
  • (en)
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