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Venlafaxine(brand names: Efexor, Effexorand Trevilor) is an antidepressantof theserotonin-norepinephrine reuptake inhibitor(SNRI) class.[3[!["#his means it increases theconcentrations of the neurotransmittersserotoninandnorepinephrinein the bod$ and the

brain. %irst introduced b$ &$ethin '3, no marketed b$ *fi+er, it is licensedfor thetreatment of maor depressie disorder(//), 0eneralised an1iet$ disorder(2/),panic

disorderandsocial phobia.[4[5

It is usuall$ resered as a second-line treatment for depression due to a combination of itssuperior efficac$ to the first-line treatments like fluo1etine,paro1etineandcitalopramand0reater fre6uenc$ of side effects like nausea, headache,insomnia, drosiness, dr$ mouth,constipation, se1ual d$sfunction, seatin0 and nerousness.[7[#he rate of life-threatenin0 orlethal outcomes for suicidal oerdoses of enlafa1ine is loer than for the #8s, 9Isand

bupropionand comparable to seeral of theSSRIs.['It is metabolised in the bod$ intoanother antidepressant dru0 called desenlafa1ine(O-desmeth$lenlafa1ine) hich is alsosold as an antidepressant, under the brand name *risti6.[''

In ;5, enlafa1ine as the si1th most commonl$ prescribed antidepressant on the

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Gud0ed b$ the same criteria, enlafa1ine as similar in efficac$ to the at$pical antidepressantbupropion(&ellbutrin)H hoeer, the remission rate as si0nificantl$ loer for enlafa1ine.[;;In a double-blind stud$, patients ho did not respond to an SSRI ere sitched toenlafa1ine or citalopram. Similar improement as obsered in both 0roups.[;3

Adverse effects

See alsoDist of aderse effects of enlafa1ine

Suicide

#he

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Discontinuation syndrome

ain article:SSRI discontinuation s$ndrome

*atients stoppin0 enlafa1ine commonl$ e1perienceSSRI discontinuation s$ndrome. #he

hi0h risk of discontinuation s$ndrome s$mptoms ma$ reflect enlafa1ineBs short half-life.[3

/iscontinuation is similar in nature, but not identical to those of SSRIs such asparo1etine(*a1ilorSero1at). Sudden discontinuation of enlafa1ine particularl$ seemed to causediscontinuation s$mptoms durin0 the first 3 da$s in a stud$ of '7 patients. [3's reported in;' b$ Caddad in the ournalDrug Safety, Aanother strate0$ to consider is sitchin0 tofluo1etine, hich ma$ suppress the discontinuation s$mptoms, but hich has little tendenc$to cause such s$mptoms itself,A and then discontinuin0 that. [3

Norepinephrinema$ also hae a si0nificant role in discontinuation s$mptoms. [3;/urin0ithdraal from enlafa1ine, the leels of both serotonin and norepinephrine decrease, rather

than increase, and this ould appear to rule out to1ic (too hi0h) leels of theseneurotransmitters as a likel$ cause of the ithdraal s$mptoms. #he ithdraal s$mptomscan be h$pothesi+ed to result from an oerl$ rapid depriation of neurotransmitter leels.

Serotonin syndrome

#he deelopment of a potentiall$ life-threatenin0 serotonin s$ndrome(also more recentl$classified as Aserotonin to1icit$A)[33ma$ occur ith enlafa1ine treatment, particularl$ ithconcomitant use of serotoner0ic dru0s, includin0 but not limited to SSRIsandSNRIs, man$hallucino0ens such astr$ptaminesandpheneth$lamines(e.0., DS/?DS, /#,/,

mescaline), de1tromethorphan(/L)?de1trorphan(/L9), tramadol, tapentadol,pethidine(meperidine) and triptansand ith dru0s that impair metabolism of serotonin (includin09Is). Serotonin s$ndrome s$mptoms ma$ include mental status chan0es (e.0. a0itation,hallucinations, coma), autonomic instabilit$ (e.0. tach$cardia, labile blood pressure,h$perthermia), neuromuscular aberrations (e.0. h$perrefle1ia, incoordination) and?or0astrointestinal s$mptoms (e.0. nausea, omitin0, diarrhea). =enlafa1ine-induced serotonins$ndrome has also been reported hen enlafa1ine has been taken in isolation in oerdose. [3!n abortie serotonin s$ndrome state, in hich some but not all of the s$mptoms of the fullserotonin s$ndrome are present, has been reported ith enlafa1ine at mid-ran0e dosa0es('" m0 per da$).[3" case of a patient ith serotonin s$ndrome induced b$ lo-doseenlafa1ine (35." m0 per da$) has also been reported. [34

Contraindications

Studies of enlafa1ine in paediatric a0e 0roups hae not established its efficac$.[35=enlafa1ine is not recommended in patients h$persensitieto it, nor should it be taken b$an$one ho is aller0ic to the inactie in0redients, hich include 0elatin,cellulose,eth$lcellulose,iron o1ide,titanium dio1ideand h$promellose.It should not be used inconunction ith a monoamine o1idase inhibitor(9I), as it can cause potentiall$ fatalserotonin s$ndrome.['[;[37

Glaucoma

http://en.wikipedia.org/wiki/SSRI_discontinuation_syndromehttp://en.wikipedia.org/wiki/SSRI_discontinuation_syndromehttp://en.wikipedia.org/wiki/SSRI_discontinuation_syndromehttp://en.wikipedia.org/wiki/SSRI_discontinuation_syndromehttp://en.wikipedia.org/wiki/Biological_half-lifehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid11347722-30http://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid11347722-30http://en.wikipedia.org/wiki/Paroxetinehttp://en.wikipedia.org/wiki/Paxilhttp://en.wikipedia.org/wiki/Seroxathttp://en.wikipedia.org/wiki/Seroxathttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-AmJPsych1997-fava-31http://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid11347722-30http://en.wikipedia.org/wiki/Norepinephrinehttp://en.wikipedia.org/wiki/Norepinephrinehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-PMC1681629-32http://en.wikipedia.org/wiki/Serotonin_syndromehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-Dunkley-33http://en.wikipedia.org/wiki/SSRIhttp://en.wikipedia.org/wiki/SSRIhttp://en.wikipedia.org/wiki/Serotonin-norepinephrine_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Serotonin-norepinephrine_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Tryptaminehttp://en.wikipedia.org/wiki/Tryptaminehttp://en.wikipedia.org/wiki/Phenethylaminehttp://en.wikipedia.org/wiki/Phenethylaminehttp://en.wikipedia.org/wiki/LSDhttp://en.wikipedia.org/wiki/Lysergic_acid_amidehttp://en.wikipedia.org/wiki/Dimethyltryptaminehttp://en.wikipedia.org/wiki/MDMAhttp://en.wikipedia.org/wiki/MDMAhttp://en.wikipedia.org/wiki/MDMAhttp://en.wikipedia.org/wiki/Mescalinehttp://en.wikipedia.org/wiki/Dextromethorphanhttp://en.wikipedia.org/wiki/Dextrorphanhttp://en.wikipedia.org/wiki/Dextrorphanhttp://en.wikipedia.org/wiki/Tramadolhttp://en.wikipedia.org/wiki/Tapentadolhttp://en.wikipedia.org/wiki/Pethidinehttp://en.wikipedia.org/wiki/Triptanhttp://en.wikipedia.org/wiki/Triptanhttp://en.wikipedia.org/wiki/MAOIhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-Kolecki-34http://en.wikipedia.org/wiki/Venlafaxine#cite_note-35http://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid12549949-36http://en.wikipedia.org/wiki/Venlafaxine#cite_note-37http://en.wikipedia.org/wiki/Hypersensitivityhttp://en.wikipedia.org/wiki/Gelatinhttp://en.wikipedia.org/wiki/Cellulosehttp://en.wikipedia.org/wiki/Cellulosehttp://en.wikipedia.org/wiki/Iron_oxidehttp://en.wikipedia.org/wiki/Iron_oxidehttp://en.wikipedia.org/wiki/Titanium_dioxidehttp://en.wikipedia.org/wiki/Titanium_dioxidehttp://en.wikipedia.org/wiki/Hypromellosehttp://en.wikipedia.org/wiki/Hypromellosehttp://en.wikipedia.org/wiki/Monoamine_oxidase_inhibitorhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-TGA-1http://en.wikipedia.org/wiki/Venlafaxine#cite_note-DM-2http://en.wikipedia.org/wiki/Venlafaxine#cite_note-Maudsley-38http://en.wikipedia.org/wiki/SSRI_discontinuation_syndromehttp://en.wikipedia.org/wiki/SSRI_discontinuation_syndromehttp://en.wikipedia.org/wiki/Biological_half-lifehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid11347722-30http://en.wikipedia.org/wiki/Paroxetinehttp://en.wikipedia.org/wiki/Paxilhttp://en.wikipedia.org/wiki/Seroxathttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-AmJPsych1997-fava-31http://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid11347722-30http://en.wikipedia.org/wiki/Norepinephrinehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-PMC1681629-32http://en.wikipedia.org/wiki/Serotonin_syndromehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-Dunkley-33http://en.wikipedia.org/wiki/SSRIhttp://en.wikipedia.org/wiki/Serotonin-norepinephrine_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Tryptaminehttp://en.wikipedia.org/wiki/Phenethylaminehttp://en.wikipedia.org/wiki/LSDhttp://en.wikipedia.org/wiki/Lysergic_acid_amidehttp://en.wikipedia.org/wiki/Dimethyltryptaminehttp://en.wikipedia.org/wiki/MDMAhttp://en.wikipedia.org/wiki/Mescalinehttp://en.wikipedia.org/wiki/Dextromethorphanhttp://en.wikipedia.org/wiki/Dextrorphanhttp://en.wikipedia.org/wiki/Tramadolhttp://en.wikipedia.org/wiki/Tapentadolhttp://en.wikipedia.org/wiki/Pethidinehttp://en.wikipedia.org/wiki/Triptanhttp://en.wikipedia.org/wiki/MAOIhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-Kolecki-34http://en.wikipedia.org/wiki/Venlafaxine#cite_note-35http://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid12549949-36http://en.wikipedia.org/wiki/Venlafaxine#cite_note-37http://en.wikipedia.org/wiki/Hypersensitivityhttp://en.wikipedia.org/wiki/Gelatinhttp://en.wikipedia.org/wiki/Cellulosehttp://en.wikipedia.org/wiki/Iron_oxidehttp://en.wikipedia.org/wiki/Titanium_dioxidehttp://en.wikipedia.org/wiki/Hypromellosehttp://en.wikipedia.org/wiki/Monoamine_oxidase_inhibitorhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-TGA-1http://en.wikipedia.org/wiki/Venlafaxine#cite_note-DM-2http://en.wikipedia.org/wiki/Venlafaxine#cite_note-Maudsley-38

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=enlafa1ine can increase e$e pressure, so those ith 0laucomama$ re6uire more fre6uent e$echecks.[3

Pregnant women

#here are fe ell-controlled studies of enlafa1ine in pre0nant omen. stud$ released ina$ ;' b$ the 8anadian edical ssociation Gournal su00ests use of enlafa1ine doublesthe risk ofmiscarria0e.[![!'8onse6uentl$, enlafa1ine should onl$ be used durin0 pre0nanc$if clearl$ needed.[3*rospectie studies hae not shon an$ statisticall$ si0nificant con0enitalmalformations.[!;#here hae, hoeer, been some reports of self-limitin0 effects on neborninfants.[!3s ith other serotonin reuptake inhibitors(SRIs), these effects are 0enerall$ short-lied, lastin0 onl$ 3 to " da$s,[!!and rarel$ resultin0 in seere complications. [!"

Drug interactions

=enlafa1ine should be taken ith caution hen usin0 St GohnBs ort.[!4=enlafa1ine ma$

loer the sei+ure threshold, and coadministration ith other dru0s that loer the sei+urethreshold such asbupropionand tramadolshould be done ith caution and at lo doses.[!5

Bipolar disorder

=enlafa1ine is not recommended nor approed for the treatment of maor depressie episodesinbipolar disorderas it can induce maniaor mi1ed episodes. =enlafa1ine appears to be morelikel$ than theSSRIsandbupropionto induce mania and mi1ed episodes in bipolar patients.[!7

t!er

#here hae been false positiephenc$clidine(*8*) results caused b$ lar0er doses ofenlafa1ine, ith certain on-site routine urine-based dru0 tests.[!["

verdose

ost patients oerdosin0 ith enlafa1ine deelop onl$ mild s$mptoms. *lasma enlafa1ineconcentrations in oerdose suriors hae ran0ed from 4 to ;! m0?l, hile postmortem bloodleels in fatalities are often in the 'J m0?l ran0e.["'*ublished retrospectie studies report

that enlafa1ine oerdosa0e ma$ be associated ith an increased risk of fatal outcomecompared to that obsered ith SSRI antidepressant products, but loer than that for tric$clicantidepressants. Cealthcare professionals are adised to prescribe Effe1or and Effe1or LR inthe smallest 6uantit$ of capsules consistent ith 0ood patient mana0ement to reduce the riskof oerdose.[";

#here is no specific antidotefor enlafa1ine, and mana0ement is 0enerall$ supportie,proidin0 treatment for the immediate s$mptoms. dministration of actiated charcoalcanpreent absorption of the dru0. onitorin0 of cardiac rh$thm and ital si0ns is indicated.Sei+ures are mana0ed ithben+odia+epinesor other anticonulsants. %orced diuresis,hemodial$sis,e1chan0e transfusion, or hemoperfusionare unlikel$ to be of benefit in

hastenin0 the remoal of enlafa1ine, due to the dru0Bs hi0h olume of distribution.["3

http://en.wikipedia.org/wiki/Glaucomahttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-Medicinedatasheet-Wyeth-39http://en.wikipedia.org/wiki/Venlafaxine#cite_note-Medicinedatasheet-Wyeth-39http://en.wikipedia.org/wiki/Miscarriagehttp://en.wikipedia.org/wiki/Miscarriagehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-40http://en.wikipedia.org/wiki/Venlafaxine#cite_note-40http://en.wikipedia.org/wiki/Venlafaxine#cite_note-41http://en.wikipedia.org/wiki/Venlafaxine#cite_note-Medicinedatasheet-Wyeth-39http://en.wikipedia.org/wiki/Congenital_malformationhttp://en.wikipedia.org/wiki/Congenital_malformationhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-42http://en.wikipedia.org/wiki/Venlafaxine#cite_note-43http://en.wikipedia.org/wiki/Venlafaxine#cite_note-43http://en.wikipedia.org/wiki/Serotonin_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-44http://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid15900008-45http://en.wikipedia.org/wiki/Hypericum_perforatumhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-46http://en.wikipedia.org/wiki/Venlafaxine#cite_note-46http://en.wikipedia.org/wiki/Venlafaxine#cite_note-46http://en.wikipedia.org/wiki/Bupropionhttp://en.wikipedia.org/wiki/Bupropionhttp://en.wikipedia.org/wiki/Tramadolhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid18072153-47http://en.wikipedia.org/wiki/Bipolar_disorderhttp://en.wikipedia.org/wiki/Maniahttp://en.wikipedia.org/wiki/Mixed_episodeshttp://en.wikipedia.org/wiki/Selective_serotonin_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Selective_serotonin_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Bupropionhttp://en.wikipedia.org/wiki/Bupropionhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-48http://en.wikipedia.org/wiki/Phencyclidinehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid17267806-49http://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid11901076-50http://en.wikipedia.org/wiki/Venlafaxine#cite_note-51http://en.wikipedia.org/wiki/Venlafaxine#cite_note-52http://en.wikipedia.org/wiki/Antidotehttp://en.wikipedia.org/wiki/Activated_charcoalhttp://en.wikipedia.org/wiki/Benzodiazepinehttp://en.wikipedia.org/wiki/Forced_diuresishttp://en.wikipedia.org/wiki/Hemodialysishttp://en.wikipedia.org/wiki/Hemodialysishttp://en.wikipedia.org/wiki/Exchange_transfusionhttp://en.wikipedia.org/wiki/Hemoperfusionhttp://en.wikipedia.org/wiki/Volume_of_distributionhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-53http://en.wikipedia.org/wiki/Venlafaxine#cite_note-53http://en.wikipedia.org/wiki/Glaucomahttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-Medicinedatasheet-Wyeth-39http://en.wikipedia.org/wiki/Miscarriagehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-40http://en.wikipedia.org/wiki/Venlafaxine#cite_note-41http://en.wikipedia.org/wiki/Venlafaxine#cite_note-Medicinedatasheet-Wyeth-39http://en.wikipedia.org/wiki/Congenital_malformationhttp://en.wikipedia.org/wiki/Congenital_malformationhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-42http://en.wikipedia.org/wiki/Venlafaxine#cite_note-43http://en.wikipedia.org/wiki/Serotonin_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-44http://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid15900008-45http://en.wikipedia.org/wiki/Hypericum_perforatumhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-46http://en.wikipedia.org/wiki/Bupropionhttp://en.wikipedia.org/wiki/Tramadolhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid18072153-47http://en.wikipedia.org/wiki/Bipolar_disorderhttp://en.wikipedia.org/wiki/Maniahttp://en.wikipedia.org/wiki/Mixed_episodeshttp://en.wikipedia.org/wiki/Selective_serotonin_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Bupropionhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-48http://en.wikipedia.org/wiki/Phencyclidinehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid17267806-49http://en.wikipedia.org/wiki/Venlafaxine#cite_note-pmid11901076-50http://en.wikipedia.org/wiki/Venlafaxine#cite_note-51http://en.wikipedia.org/wiki/Venlafaxine#cite_note-52http://en.wikipedia.org/wiki/Antidotehttp://en.wikipedia.org/wiki/Activated_charcoalhttp://en.wikipedia.org/wiki/Benzodiazepinehttp://en.wikipedia.org/wiki/Forced_diuresishttp://en.wikipedia.org/wiki/Hemodialysishttp://en.wikipedia.org/wiki/Exchange_transfusionhttp://en.wikipedia.org/wiki/Hemoperfusionhttp://en.wikipedia.org/wiki/Volume_of_distributionhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-53

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"ec!anism of action

=enlafa1ine is usuall$ cate0ori+ed as a serotonin-norepinephrine reuptake inhibitor(SNRI),but it has been referred to as a serotonin-norepinephrine-dopamine reuptake inhibitor(SN/RI).["![""It orks b$ blockin0 the transporter AreuptakeA proteinsfor ke$neurotransmittersaffectin0 mood, thereb$ leain0 more actie neurotransmitters in thes$napse. #he neurotransmitters affected are serotoninand norepinephrine. dditionall$, inhi0h doses it eakl$ inhibits the reuptake of dopamine,["4ith recent eidence shoin0 thatthenorepinephrine transporteralso transports some dopamineas ell, since dopamine isinactiated b$ norepinephrine reuptake in thefrontal corte1. #he frontal corte1 lar0el$ lacksdopamine transporters, therefore enlafa1ine can increase dopamine neurotransmission in this

part of the brain.["5["7=enlafa1ine interacts ith opioid receptors (mu-, kappa'- kappa3- anddelta-opioid receptor subt$pes) as ell as the alpha;-adrener0ic receptor, and as shon toincrease pain threshold in mice. &hen mice ere tested ith a hotplate anal0esia meter (tomeasure pain), both enlafa1ine and mirta+apineinduced a dose-dependent, nalo1one-

reersible antinociceptie effect folloin0 intraperitonealinection. #hese findin0s su00estenlafa1ineBs seemin0l$ superior efficac$ in seere depression as narcotics becomeincreasin0l$ used as a measure of last resort for refractor$ cases. ["

P!armaco#inetics

=enlafa1ine is ell absorbed, ith at least ;K of an oral dose bein0 absorbed into s$stemiccirculation. It is e1tensiel$ metaboli+ed in the lier ia the 8M*;/4isoen+$metodesenlafa1ine(O-desmethylvenlafaxine), hich is ust as potent a SNRI as the parentcompound, meanin0 that the differences in metabolism beteen e1tensie andpoormetabolisersare not clinicall$ important in terms of efficac$. Side effects, hoeer, are

reported to be more seere in 8M*;/4poor metabolisers.[4Stead$-state concentrations ofenlafa1ine and itsmetaboliteare attained in thebloodithin 3 da$s. #herapeutic effects areusuall$ achieed ithin 3 to ! eeks. No accumulation of enlafa1ine has been obsereddurin0 chronic administration in health$ subects. #he primar$ route of e1cretion ofenlafa1ine and its metabolites is ia the kidne$s.[3#hehalf-lifeof enlafa1ine is relatiel$short, so patients are directed to adhere to a strict medication routine, aoidin0 missin0 a dose.Een a sin0le missed dose can result in ithdraal s$mptoms.[4'

=enlafa1ine is a substrate of *-0l$coprotein(*-0p), hich pumps it out of the brain. #he 0eneencodin0 *-0p, 8', has the SN*rs;3;"73, ith alleles8 and #. #he maorit$ of people(about 5K of Europeans and K of East sians) hae the ## ariant.[4; ;5 stud$[43

found that carriers of at least one 8 allele (ariant 88 or 8#) are 5.5; times more likel$ thannon-carriers to achiee remissionafter ! eeks of treatment ith amitript$line, citalopram,

paro1etineor enlafa1ine (all *-0p substrates). #he stud$ included patients ith mooddisordersother than maor depression, such asbipolar IIH the ratio is .! if these otherdisorders are e1cluded. t the 4-eek mark, 5"K of 8-carriers had remitted, compared toonl$ 37K of non-carriers.

C!emistry

#hechemical structureof enlafa1ine is desi0nated (R?S)-'-[;-(dimeth$lamino)-'-(!

metho1$phen$l)eth$l c$clohe1anol h$drochloride or (O)-'-[a [a- (dimeth$lamino)meth$l p-metho1$ben+$l c$clohe1anol h$drochloride, and it has the empirical formulaof 8'5C;5N9;.

http://en.wikipedia.org/wiki/Serotonin-norepinephrine_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Serotonin-norepinephrine-dopamine_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-54http://en.wikipedia.org/wiki/Venlafaxine#cite_note-55http://en.wikipedia.org/wiki/Monoamine_transporterhttp://en.wikipedia.org/wiki/Neurotransmitterhttp://en.wikipedia.org/wiki/Synapsehttp://en.wikipedia.org/wiki/Serotoninhttp://en.wikipedia.org/wiki/Norepinephrinehttp://en.wikipedia.org/wiki/Dopaminehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-CNSDrugs2001-Wellington-56http://en.wikipedia.org/wiki/Venlafaxine#cite_note-CNSDrugs2001-Wellington-56http://en.wikipedia.org/wiki/Norepinephrine_transporterhttp://en.wikipedia.org/wiki/Norepinephrine_transporterhttp://en.wikipedia.org/wiki/Dopaminehttp://en.wikipedia.org/wiki/Frontal_cortexhttp://en.wikipedia.org/wiki/Frontal_cortexhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-57http://en.wikipedia.org/wiki/Venlafaxine#cite_note-58http://en.wikipedia.org/wiki/Mirtazapinehttp://en.wikipedia.org/wiki/Intraperitonealhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-59http://en.wikipedia.org/wiki/CYP2D6http://en.wikipedia.org/wiki/Isoenzymehttp://en.wikipedia.org/wiki/Desvenlafaxinehttp://en.wikipedia.org/wiki/Poor_metaboliserhttp://en.wikipedia.org/wiki/Poor_metaboliserhttp://en.wikipedia.org/wiki/Poor_metaboliserhttp://en.wikipedia.org/wiki/CYP2D6http://en.wikipedia.org/wiki/CYP2D6http://en.wikipedia.org/wiki/Venlafaxine#cite_note-JCPT_JClinPharmTher2006-shams-60http://en.wikipedia.org/wiki/Metabolitehttp://en.wikipedia.org/wiki/Metabolitehttp://en.wikipedia.org/wiki/Bloodhttp://en.wikipedia.org/wiki/Kidneyshttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-Medicinedatasheet-Wyeth-39http://en.wikipedia.org/wiki/Venlafaxine#cite_note-Medicinedatasheet-Wyeth-39http://en.wikipedia.org/wiki/Elimination_half-lifehttp://en.wikipedia.org/wiki/Elimination_half-lifehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-ANZ_JPsych1998-parker-61http://en.wikipedia.org/wiki/P-glycoproteinhttp://en.wikipedia.org/wiki/Single-nucleotide_polymorphismhttp://en.wikipedia.org/wiki/Single-nucleotide_polymorphismhttp://en.wikipedia.org/wiki/Allelehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-snpedia_.27583-62http://en.wikipedia.org/wiki/Venlafaxine#cite_note-Neuron:_ABCB1-63http://en.wikipedia.org/wiki/Partial_remissionhttp://en.wikipedia.org/wiki/Amitriptylinehttp://en.wikipedia.org/wiki/Citalopramhttp://en.wikipedia.org/wiki/Paroxetinehttp://en.wikipedia.org/wiki/Mood_disorderhttp://en.wikipedia.org/wiki/Mood_disorderhttp://en.wikipedia.org/wiki/Major_depressive_disorderhttp://en.wikipedia.org/wiki/Bipolar_II_disorderhttp://en.wikipedia.org/wiki/Bipolar_II_disorderhttp://en.wikipedia.org/wiki/Chemical_structurehttp://en.wikipedia.org/wiki/Chemical_structurehttp://en.wikipedia.org/wiki/Empirical_formulahttp://en.wikipedia.org/wiki/Serotonin-norepinephrine_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Serotonin-norepinephrine-dopamine_reuptake_inhibitorhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-54http://en.wikipedia.org/wiki/Venlafaxine#cite_note-55http://en.wikipedia.org/wiki/Monoamine_transporterhttp://en.wikipedia.org/wiki/Neurotransmitterhttp://en.wikipedia.org/wiki/Synapsehttp://en.wikipedia.org/wiki/Serotoninhttp://en.wikipedia.org/wiki/Norepinephrinehttp://en.wikipedia.org/wiki/Dopaminehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-CNSDrugs2001-Wellington-56http://en.wikipedia.org/wiki/Norepinephrine_transporterhttp://en.wikipedia.org/wiki/Dopaminehttp://en.wikipedia.org/wiki/Frontal_cortexhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-57http://en.wikipedia.org/wiki/Venlafaxine#cite_note-58http://en.wikipedia.org/wiki/Mirtazapinehttp://en.wikipedia.org/wiki/Intraperitonealhttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-59http://en.wikipedia.org/wiki/CYP2D6http://en.wikipedia.org/wiki/Isoenzymehttp://en.wikipedia.org/wiki/Desvenlafaxinehttp://en.wikipedia.org/wiki/Poor_metaboliserhttp://en.wikipedia.org/wiki/Poor_metaboliserhttp://en.wikipedia.org/wiki/CYP2D6http://en.wikipedia.org/wiki/Venlafaxine#cite_note-JCPT_JClinPharmTher2006-shams-60http://en.wikipedia.org/wiki/Metabolitehttp://en.wikipedia.org/wiki/Bloodhttp://en.wikipedia.org/wiki/Kidneyshttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-Medicinedatasheet-Wyeth-39http://en.wikipedia.org/wiki/Elimination_half-lifehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-ANZ_JPsych1998-parker-61http://en.wikipedia.org/wiki/P-glycoproteinhttp://en.wikipedia.org/wiki/Single-nucleotide_polymorphismhttp://en.wikipedia.org/wiki/Allelehttp://en.wikipedia.org/wiki/Venlafaxine#cite_note-snpedia_.27583-62http://en.wikipedia.org/wiki/Venlafaxine#cite_note-Neuron:_ABCB1-63http://en.wikipedia.org/wiki/Partial_remissionhttp://en.wikipedia.org/wiki/Amitriptylinehttp://en.wikipedia.org/wiki/Citalopramhttp://en.wikipedia.org/wiki/Paroxetinehttp://en.wikipedia.org/wiki/Mood_disorderhttp://en.wikipedia.org/wiki/Mood_disorderhttp://en.wikipedia.org/wiki/Major_depressive_disorderhttp://en.wikipedia.org/wiki/Bipolar_II_disorderhttp://en.wikipedia.org/wiki/Chemical_structurehttp://en.wikipedia.org/wiki/Empirical_formula

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It is a hite to off-hite cr$stalline solid. =enlafa1ine is structurall$ and pharmacolo0icall$related to the at$pical opioid anal0esictramadol, and more distantl$ to the nel$ releasedopioidtapentadol, but not to an$ of the conentional antidepressant dru0s, includin0 tric$clicantidepressants,SSRIs, 9Is, or RIs.[4!

Availa$le forms

Effe1or LR 5" m0 and '" m0 capsules

2eneric 5"m0 (top) and '"m0 (bottom) enlafa1ine capsules b$ rka

Extended release

=enlafa1ine e1tended release is chemicall$ the same as normal enlafa1ine. #he e1tendedrelease (controlled release) ersion distributes the release of the dru0 into the 0astrointestinaltractoer a lon0er period than normal enlafa1ine. #his results in a loer peak plasmaconcentration. Studies hae shon that the e1tended release formula has a loer incidence of

patients sufferin0 fromnauseaas a side effect, resultin0 in a loer number of patientsstoppin0 their treatment due to nausea.[4"In ustralia, Ne Fealand, #urke$[44andSit+erland, &$ethsells their enlafa1ine LR tablets under the name AEfe1or-LRA (note thespellin0 ith one BfB, rather than AEffe1or-LRA). In ra+il, edle$ sells a enlafa1ine LR

capsule under the brand name lenthus LR. In September ;7, 9smotica *harmaceuticalsbe0an marketin0 enlafa1ine e1tended release tablets in the

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