Milnacipran: Difference between revisions

Milnacipran
Clinical data
Pregnancy; category	X (US);
Routes of; administration	Oral
ATC code	N06AX17 (WHO) ;
Legal status
Legal status	Unscheduled; Rx-only (not approved in the US);
Pharmacokinetic data
Bioavailability	85%
Metabolism	Hepatic
Elimination half-life	8 hours
Excretion	Renal
Identifiers
	IUPAC name (1R,2R)-2-(aminomethyl)-N,N-diethyl-1-phenyl-cyclopropane-1-carboxamide;
CAS Number	92623-85-3;
PubChem CID	65833;
CompTox Dashboard (EPA)	DTXSID601025164 DTXSID3048287, DTXSID601025164 ;
Chemical and physical data
Formula	C15H22N2O
Molar mass	246.348

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Revision as of 10:48, 2 February 2007

Milnacipran is an antidepressant of the serotonin-norepinephrine reuptake inhibitor class.

History

Milnacipran has been approved and sold in Austria since September 1998 under the brand name Ixel®. Cypress Bioscience bought the exclusive rights for approval and marketing of the drug for any purpose in the US and Canada in 2003 from the manufacturer Pierre Fabre; the approval procedure in both countries is ongoing.

Pharmacokinetics

Milnacipran is well absorbed after oral dosing and has a bioavailability of 85%. Meals do not have an influence on the rapidity and extend of absorption. Peak plasma concentrations are reached 2 hours after oral dosing. The elimination half-life of 8 hours is not increased by liver impairment and old age, but by significant renal disease. Milnacipran is conjugated to the inactive glucuronid and excreted in the urine as unchanged drug and conjugate. Only traces of active metabolites are found. Enzymes of the CYP class do not play a role in the metabolism of Milnacipran.

Indications & Dosage

Milnacipran is used to treat:

Moderate to severe clinical depression (Major Depression)
Chronic Pain

The recommended dose for depression is 50mg 2 times daily (after an initial phase of 50mg daily as single dose on days 1 to 4). The dose should be decreased in patients with renal disease. The dosage for the other indications has not been well established so far.

Milnacipran is available in 25mg and 50mg capsules.

After successful treatment of the acute depressive episode, patients should be maintained on Milnacipran for several months (normally 9 months) in order to prevent relapse of depression.

Experimental Uses

In experimental studies Milnacipran showed useful activity as adjunct in the therapy of Fibromyalgia and Lupus, both conditions with potentially devastating effects. In Fibromyalgia the drug improved pain, mood, and fatigue compared to placebo. In Lupus patients pain was alleviated and a sense of well-being was provided.

On January, 5th., 2006, Forest Pharmaceuticals and Cypress Bioscience agreed to commence a phase III multicenter study encompassing 1,200 patients with Fibromyalgia. Early results will be available by mid 2007.

Interactions

MAOIs, Lithium - serotoninergic syndrome, potentially lethal
5-HT1AD-Agonists - coronary vasoconstriction with risk of angina pectoris and myocardial infarction
Epinephrine, Norepinephrine (also in local anesthesia) - hypertensive crisis and possible arrhythmias
Clonidine - antihypertensive action of Clonidine may be antagonized
Digitalis - hemodynemic actions increased
Alcohol - no interactions known

Contraindications

Administration of milnacipran should be avoided in individuals with the following:

Known hypersensitivity to Milnacipran (absolute contraindication)
Patients under 15 years of age (no sufficient clinical data)
Concomitant treatment with irreversibe and reversible (MAO-B) MAO-Inhibitors, Digitalis-Glycosids and 5-HT1D-Agonists (e.g. Sumatriptan) - absolute contraindications -

Administration of milnacipran should be done with caution in individuals with the following:

Concomitant treatment with parenteral Epinephrine, Norepinephrine, with Clonidine and reversible MAO-A-Inhibitors (Moclobemid, Toloxaton).
Advanced renal disease (decreased dosage required)
Hypertrophy of the prostate gland (possibly urination hesitancy induced), with hypertension and heart disease (tachycardia may be a problem) as well as with open angle glaucoma

Milnacipran should not be used during pregnancy because it may cross the placenta barrier and no clinical data exists on harmful effects in humans and animal studies. Milnacipran is contraindicated during lactation because it is excreted in the milk, and it is not known if it is harmful to the newborn.

References/External Links

http://www.ixel.at/fachinfo.html#4.5 Scentific Information on Ixel® (German)
http://www.antiaging-systems.com/a2z/milnacipran.htm
[1]License Agreement Cypress - Pierre Fabre.
http://www.freshnews.com/news/biotech-biomedical/article_29042.html?Cypress+Bioscience Agreement on Study in Fibromyalgia.

@@ Line 24: / Line 24: @@
 Milnacipran has been approved and sold in Austria since September 1998 under the brand name '''Ixel'''&reg;. Cypress Bioscience bought the exclusive rights for approval and marketing of the drug for any purpose in the US and Canada in 2003 from the manufacturer Pierre Fabre; the approval procedure in both countries is ongoing.
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-==Pharmacology==
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-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, Alpha1, D1, D2 and muscarinic receptors as well as on benzodiazepin/opiate binding sites. In a clinical trial with over 1,000 depressed patients Milnacipran showed results comparable to Imipramine and superior to SSRIs, but proved in a different study inferior to Clomipramine. As with other antidepressants 1 to 3 weeks may elapse before significant antidepressive action becomes clinically evident.
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 ==Pharmacokinetics==