Efexor XR Tablets

Efexor XR Tablets contains Venlafaxine HCL an oral antidepressant with novel structure. Venlafaxine is designated as (+/-)-1-[a-[(dimethylamino)methyl]-p-methoxybenzyl] cyclohexanol. It is chemically unrelated to other available antidepressant agents. But actions are similar to tricyclic antidepressants like amitriptyline.

More Useful Medicine : Lilac Syrup (Lactulose) Uses

Venlafaxine Tablets Indications

Treatment of depression, including depression with associated anxiety

Treatment of anxiety or generalized anxiety disorder , including long term treatment

For prevention of relapse and prevention of recurrence of depression

Treatment of social anxiety disorder , including long term treatment

Treatment of panic disorder , including long term treatment

Venlafaxine Tablets Psology And Method Of Administration

The following are representative Efexor XR Dosage recommendation.

Meanwhile, It is recommended that Venlafaxine Capsules taken with food at approximately the same time each day. On the other hand, Efexor XR Capsules must swallowed whole with fluid and not divided, crushed, chewed, or dissolved. Or it may administered by carefully opening the Venlafaxine Capsule and sprinkling the entire contents on a spoonful of applesauce. Furthermore, this drugs food mixture should swallowed immediately without chewing and followed with a glass of water to ensure complete swallowing of the pellets.

However, with the exception of patients with social anxiety disorder (SAD) patients not responding to the Efexor XR 75MG /day dose may benefit from dose increase in increments of up to Efexor 75 /day to a maximum of Efexor XR 225 mg/ day. Meanwhile, Extended release Venlafaxine Tablets Dosage increase can made at intervals of 2 weeks or more but not less than 4 days.

On the other hand, Patients treated with Venlafaxine Tablets immediate release tablets may be switched to Venlafxine extended release capsules at the nearest equivalent daily Venlafaxine Dosage. For example, Venlafaxine immediate release tablets 37-5 mg twice daily may switched to Venlafaxine extended release Venlafaxine 75 mg once daily. However, Individual dosage adjustments may be necessary.

Major Depressive Disorder

The recommended stating Venlafaxine Dose extended release capsules is Efexor 75 mg given once daily. Patients not responding to the initial Efexor Xr 75 mg/day doses may benefit from dose increase to a maximum of 225 mg/day.

While the recommended dose of Venlafaxine immediate release tablets in moderately depressed patients is up to 225 mg/ day more severely depressed patient in one study responded to a mean dose of 350 mg/day range of 150 to 375 mg/day.

Generalized Anxiety Disorder

The recommended starting dose of Venlafaxine extended release capsules is Efexor XR 75 mg given once daily. Patients not responding to the Efexor 75 dose may benefit from dose increase to a maximum of 225 mg/day.

Social Anxiety Disorder

The recommended Efexor XR Dose of venlafaxine extended release capsules is Venlafaxine 75 mg given once daily. There is no evidence that higher doses confer any additional benefit .

Panic Disorder

It recommended that a Efexor XR Tablets dose of 37-5 mg/day of Venlafaxine extended release capsule be used for 7 days. The dose should then increased to 75 mg/day. Patients not responding to the Efexor 75 mg/day dose may benefit from dose increase to a maximum of 225 mg.day.

Discontinuing Venlafaxine

Efexor XR Tablets Dose tapering recommended whenever possible when discontinuing Venlafaxine therapy. In clinical trial with venlafaxine extended release capsules, tapering was achieved by reducing the daily dose by 75 mg at 1 weeks intervals. The period required for tapering may depend on the dose,duration of therapy and the individual patient.

Use In Patients With Renal Impairment

The total daily dose of Venlafaxine should be reduced by 25% to 50% for patients with renal impairment with a glomerular filtration rate (GFR) of 10 to 70 ml/min. The total daily dose of Venlafaxine should be reduced by 50% in hemodialysis patients. Because of individual variability in clearance in these patients individualization of dosage may be desirable.

Use in Patients with Hepatic Impairment

The total daily Efexor XR Tablets Dose should be reduced by 50% in patients with mild to moderate hepatic impairment. Reductions of more than 50% may be appropriate for some patients. Because of individual variability in clearance in these patients individualization of dosage may be desirable.

Use in Children and Adolescent

There is insufficient experience with the use of Venlafaxine in patients younger than 18 years of age.

Use in Elderly Patients

No specific dosage adjustments of venlafaxine are recommended based on patient age.

Venlafaxine Tablets Contraindications

Hypersensitivity to Venlafaxine or any excipients in the formulation. Concomitant use of Venlafaxine and any monoamine oxiddase inhibitor (MAOL). Venlafaxine must not initiated for at least 14 after discontinuation of treatment with a MAOL. A should interval may be justified in the case of a reversible MAOL. Venlafaxine must be discontinued for at least 7 days before starting treatment with any MAOl Interaction with other medicine products and other forms of interaction).

Efexor XR Special Warnings And Precautions For Use

Suicide /Suicide Thoughts or Clinical Worsening

All patients treated with Efexor XR Tablets should be monitored appropriately and observed closely for clinical worsening and suicidality. Patients, their families, and their caregivers should be encouraged to be alert to the emergence of anxiety, agitation, panic attacks, insomina, irritability, hostility, aggressiveness, impulsivity, akathisia (psychomotor restlessness) hypomania, mania, other unusual changes in behavior, worsening of depression, and suicidal ideation. Especially when initiating therapy or during any changes in dosage regimen. The risk of suicide attempt must be considered, especially in depressed patients, and the smallest quantity of drug consistent with good patients management, should provided to reduce the risk of overdose Undesirable Effects.

Suicide is a known risk of depression and certain other psychiatric disorder, and these disorder themselves are strong predictors of suicide. Pooled analyses of short term placebo controlled trials of antidepressant medicine (selective serotonin reuptake inhibitors (SSRls) and others showed that these medicines increase the risk of suicidality in children, adolescents, and young adults (ages 18-24 years) with major depression and other psychiatric disorder. Short term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults older than years of age. There was a reduction in the risk of suicidality with antidepressants compared to placebo in adults age 65 years and older.

Bone Fractures

Epidemiological studies show an increase risk of bone fracture in patients receiving to this risk is not fully understood .

Use In Children and Adolescents

Efficacy in patients younger than 18 years of age has not been established.

Regular measurement of weight and blood pressure is recommended if Venlafaxine is used in children and adolescents. Discontinuation of Venlafaxine treatment increase in blood pressure. Measurement of serum cholesterol levels should be considered during long term treatment of serum children and adolescents. Safety in children younger than 6 years of age has not been evaluated.

NMS Like Reactions

As with other serotonergic agents serotonin syndrome, a potentially life threatening condition or NMS like reactions may occur with venlafaxine treatment. Particularty with concomitant use of other serotonergic drugs including SSRls, SNRls and triptans, fentanyl, dextromethorphan, tramadol, tapentadol, meperidine, methadone, pentazocine 211, with drugs that impair metabolism of serotonin including MAOls, e.g. methylene blue, or with antipsychotics or other dopamine antagonists 24,25,26. Symptoms of serotonin syndrome may include mental status changes (e.g.agitation, hallucinations,and coma), autonomic instability (e.g tachycardia, labile blood pressure, and hyperthermia, neuromuscular aberrations(e.g. hyperreflexia, incoordination ), and gastrointestinal symptoms (e.g. nausea, vomiting, and diarrhea) 25 Serotonin syndrome, muscle rigidity, autonomic instability with possible rapid fluctuation of vital signs, and mental sataus changes.If concomitant treatment with Venlafaxin and other agents that may affect the serotonergic and dopaminergic nerrotrans mitter systems is clinically warranted. Careful observation of the patients is advised, particularly during treatment initiation and dose increases.

The concomitant use of Venlafaxine with serotonin such as tryptophan supplements is not recommended.

Angle Closure Glaucoma

Mydriasis may occur in association with Venlafaxine. If is recommended that patients with raised intra-ocular pressure or patients at risk for acute narrow angle glaucoma (angle closure glaucoma ) be closely monitored.

Cardiovascular System

Venlafaxine has not evaluated in patients with a recent history of myocardial interaction or unstable heart disease. Therefore, if should be used with caution in these patients.

However, Dose related increases in blood pressure have reported in some patients treated with venlafaxine. Therefore, Cases of elevated blood pressure requiring immediate treatment have reported in post marketing experience. Most importantly, the measurement of blood pressure recommended for patients receiving venlafaxine. Meanwhile, Pre-existing hypertension should controlled before treatment with venlafaxine. On the other hand, Caution should exercised in patients whose underlying conditions might compromised by increased in blood pressure.

Furthermore, Increases in heart rate can occur, particularly with higher doses. So, Caution should exercised in patients whose underlying conditions might be compromised by increases in heart rate.

Meanwhile, Cases of QTc prolongation, Torsade de Pointes (TdP), ventricular tachycardia and sudden death have reported during the post marketing use of venlafaxine. The majority of reports occurred in association with overdose or in patients with other risk factors for QTc prologation TdP. Therefore venlafaxine should used with caution in patients with risk factors QTc prologation.

Convulsions

However, Covulsions may occur with venlafaxine therapy. But, As with all antidepressants, venlafaxine should be introduced with caution in patients with a antidepressants. So, Venlafaxine should be introduced with caution in patients with a history of convulsions.

Mania / Hypomania

Mania /hypomania may occur in a small proportion of patients with mood disorder who have received antidepressants, including venlafaxine. Meanwhile, as with other anti depressants, venlafaxine should be used cautiously in patients with a history or family history of bipolar disorder.

Aggression

Most importantly, Aggression may occur in a small proportion of patients who have receiving antidepressants. Including venlafaxine treatment, dose reduction or discontinuation. However, As with other antidepressants, venlafaxine should be used cautiously in patients with a history of aggression.

Hyponatremia

On the other hand, Cases of hyponatremia and the syndrome of inapporopriate antidiuretic hormone (SIADH) secretion may occur with venlafaxine. But, Usually in volume depleted or dehydrated patients. On the other hand, Elderly patients, patients taking diuretic and patients who otherwise volume depleted may at greater risk for this event.

Bleeding

Most importantly, Drugs that inhibitor uptake may lead abnormalities of platelet aggregation . Therefore reports of bleeding abnormalities with venlafaxine ranging from skin and mucous membrane bleeding and gastrointestinal hemorrhage 45 to life threatening hemorrhage. 46, 47,48,49,211. However, As with other SRls, venafaxine should used cautiously in patients predisposed to bleeding, including patients on anticoagulants and platelet inhibitors.

Weight Loss

The safety and efficacy of venlafaxine therapy in combination with weight loss agents, including phentermine, have not been established. So, Co administration of venlafaxine hydrochloride and weight loss agents not recommended. On the other hand, Venlafaxine hydrochloride not indicated for weight loss alone or in combination with other products.

Serum Cholesterol

Clinically release increases in serum cholesterol recorded in 5.3 of venlafaxine treated patients and 0.0% of polacebo-treated patients treated for at least 3 months in placebo controlled clinical trials. Meanwhile, Measurement of serum cholesterol levels should considered during long term treatment.

Efexor XR Drug Interactions

Monoamine Oxidase Inhibitors

Furthermore, Severe adverse reactions have reported in patients who have recently discontinued from an MAOl and started on venlafaxine or have recently had venlafaxine therapy discontinued prior to inhitiation of an MAol. However, These reactions have including tremor, myoclous, diaphoresis, nausea, vomiting , flushing, dizziness, and hyperthermia with features resembing NMS, seizures, and death.

CNS Active Drugs

On the other hand, the risk of using venlafaxine in combination with other CNS active drugs has not systematically evaluated. Consequently , caution advised when venlafaxine taken in combination with other CNS active drugs.

Serotonin Syndrome

As with other serotonergic agents , serotonin syndrome, a potentially life threatening condition, may occur with venlafaxine treatment , particular with concomitant use of other agents that may affect the serotonergic neurotransmitter system including triptans , SSRls, other SNRl, lithium sibutramine , fentanyl and its analogues tramadol, dextromethorphan, tapentadol, meperidine , methadone, pentazocine, or SL john,s Wort(Hypericum perforatum), with drugs that impair metabplism of serotonin such as MAOls, including linezolid (an antibiotic which is a reversible non selective MAO) and methylene bule , or with serotonin precursors such as tryptophan supplements .

Meanwhile, If concomitant treatment with venlafaxine and an SSRl , as SNRl or a 5 hydroxytryptamine receptor agonist (triptan) clinically warranted, careful observation of the patients advised , particular during treatment initiation and dose increase. Therefore, the concomitant use of venlafaxine with serotonin precursors (such as tryptophan supplements) not recommended .

Drugs That Prolong the QT Interval

Meanwhile, the risk of QT c prolongation and vertricular arrhythmias (e.g. TdP) increased with concomitant use of other drugs. Which prolong the QTc interval (e.g some antipsychotics and antibiotics ) .

Indinavir

Further, A pharmacokinetic study with indinavir has show a 28 decrease in area under the concentration versus time curve and a 36 decrease in cmax for indinavir did not affect the pharmacokintics of venlafaxine and o desmethylvenlafaxine (ODV). The clinical significance of this interaction is unknown.

Ethanol

Meanwhile, Venlafaxine has shown not to increase the impairment of mental and motor skills caused by ethanol. However ,as with all CNS active drugs ,patients should advised to avoid alcohol consumption while taking venlafaxine .

Haloperidol

Furthermore, in a pharmacokinetic study with haloperidol has shown a 42 decrease in total oral clearance a 70 increase in AUC, an 88 increase in cmax. But no change in half life. 60 The should taken into account in patients treated with haloperidol and venlafaxine concomitantly.

Cimetidine

At steady state , cimetidine has shown to inhibit first pass metabolism of venlafaxine; However , cimetidine had no effect on the pharmacokinetics of ODV. Meanwhile, The overall pharmacological activity of venlafaxine plus ODV expected to increase only slightly in most patients. 61 in the elderly and in patients with hepatic dysfunction ,this interaction may be more pronounced.

Imipramine

Meanwhile, Venlafaxine did not affect the pharmacokinetics of imiprmine and 2 OH imipramine. However , desipramine AUC, Cmax, and Cmin increased by about 35 in the presence of venlafaxine did not affect the pharmacokinetics of venlafaxine and ODV. Therefore, This should taken into account in patients treated with imipramine and venlfaxine concomitantly.

Ketoconazole

A pharmacokinetics study with ketoconazole in extensive metabolizers and poor metabolizers of CYP2D6 resulted in higher plasma concentration of both venlafaxine and ODV in subjects following administration of ketoconazole. Meanwhile, Venlafaxine Cmax increase by 26 in EM subjects and 48 in PM subjects. On the other hand, Cmax values for ODV increased by 14 and 29 in EM and PM subjects, respectivelty . Therefore, Venlafaxine AUC increased by 21 in EM subjects and 70 in PM subjects . AUC values for ODV increased by 23 and 33 in EM and PM subjects, respectiveely.

Metoprolol

Most importantly, concomitant administration of venlafaxine (50 mg every 8 hours for 5 days) and metoprolol (100 mg every 24 hours for 5 days) to healthy volunteers in a pharmacokinetic interaction study for both drugs resulted in increased in plasma concentrations of metoprolol by approximately 30 -40 without altering the plasma concentrations of its active metabolite, hydroxymetoprolol. Venlafaxine appeared to reduce the blood pressure lowering effect of metoprolol in this study of healthy volunteers. Meanwhile, the clinical relevance of this finding in hypertensive patients is unknown. Metoprolol did not alter the pharmacokinetic profile of venlafaxine or its active metabolite, ODV. 65 Caution should exercised with co administration of venlafaxine and metoprolol.

Risperidone

On the other hand, Venlafaxine increased risperidone AUC 32 but did not significantly alter the pharmacokinetic profile of the total active moiety (risperidone plus 9 hydroxyrisperidone ). 66 The clinical significance of this interaction is unknown.

Diazepam

However, Diazepam does not appear to affect the pharmacokinetic of either venlafaxine or ODV. eVenlafaxine has no effects on the pharmacokinetics and pharmacodynamics of diazepam and its active metabolite, desmethydiazepam.

Lithium

Meanwhile, the steady state pharmacokinetics of venlafaxine and ODV not affected when lithium co administered. However, Venlafaxine has no effect on the pharmacokinetics of lithium .

Eletroconvulsive Therapy

Therefore no clinical data establishing the benefit of electroconvulsive therapy combined with Efexor XR Tablets treatment.

Drug Laboratory Test Interactions

False positive urine immunoassay screening tests for PCP and amphetamine have reported in patients taking venlafaxine. Meanwhile, this is due to lack of specificity of the screening tests.

On the other hand, False positive test results may expected for several days following discontinuation of venlafaxine therapy. Meanwhile, Confirmatory tests, such as gas chromatography /mass espectrometry , will distinguish venlafaxine from PCP and amphetamine.

Efexor XR In Pregnncy And Lactation

Most importantly, to know that the safety of Venlafaxine In Pregnancy has not been established. Meanwhile, Venlafaxine During Pregnancy must be administered only if the expected benefits outweigh the possible risks. However, If venlafaxine used until or shortly before birth, discontinuation effects in the newborn should considered. 82 Some neonates exposed to venlafaxine late in the third trimester have developed complication requiring tube feeding , respiratory support, or prolonged hospitaliztion. Such complications can arise immediately upon delivery.

Meanwhile, when Efexor XR Tablets administered orally to pregnant rats throughout gestation and lactation. A decrease in pup weight, an increase in stiliborn pups, and an increase in pup deaths during the first 5 days of lactation. However, when dosing began during pregnancy and continued until weaning. 85 The cause of these deaths not known. Meanwhile, These effects occurred at 10 times the human daily dose (on a mg/kg basis ) or 2.5 times (on a mg/m2 basis ) the human daily dose of 375 mg of venlafaxine. However, the no effect dose for rat pup mortality 1.4 times the human dose, on a mg/kg basis,or 0.25 times the human dose , on a mg/32 basis.

Meanwhile, Venlafaxine and ODV excreted in human milk. Therefore a decision should made whether to breast feed or to discontiune venlafaxine.

Effects On Ability To Drive And Use Machines

Efexor XR Tablets did not affect psychomotor , congnitive , or complex behavior perfomance in healthy volunteers. However , any psychoactive drug may impair judgment, thinking, and motor skilis. Therefore patients should cautioned about their ability to drive or operate hazardous machinery.

Efexor XR Side Effects

Blood And Lymphatic System Side Effects

Agranulocytosis

Aplastic anaemia

Pancytopenia

Neutropenia

Thrombocytopenia

Immune System Disorders

Anaphylactic reaction

Endocrine Disorders

Inappropriate antidiuretic hormone secretion

Blood prolactin increased

Psychiatric Disorders

Delirium

Confusional state

Mania

Hypomania

Depresonalisation

Hallucination

Insomnia

Abnormal dreams

Nervousness

Libido decreased

Agitation

Anorgasmia

Abnormal orgasm

Bruxism

Apathy

Nervous System Disorders

Neuroleptic malignant syndrome

Serotonin syndrome

Akathisia

Syncope

Convulsion

Headache

Dizziness

Sedation

Tremor

Paraesthesia

Dysgeusia

Myoclonus

Balance disorder

Coordination abnormal

Dyskinesia

Dystonia

Tardive dyskinesia

Eye Disorders

Angle closure glaucoma

Visual impairment

Accommodation disorder

Mydriasis

Vascular Disorders

Hypertension

Orthostatic hypotension

Hypotension

Hot flush

Respiratory, Thoracic And Mediastinal Disorders

Dyspnoea, Interstitial lung disease

Pulmonary eosinophillia

Yawing

Gastrointestinal Disorders

Gastrointestinal haemorrhage

Pancreatitis

Diarrhoea

Bomiting

Nausea

Dry mouth

Constipation

Hepatobillary Disorders

Hepatitis

Liver function test abnormal

Skin And Subcutaneous Tissue Disorders

Stevens Johnson Syndrome

Toxic epidermal necrosis

Angioedema

Erythema multiforme

Rash

Hyperhidrosis

Pruritus

Night sweats

Urticaria

Alopecia

Ecchymosis

Photosensitivity reaction

Musculoskeletal And Connective Tissue Disorders

Rhabdomyolysis

Hypertonia

Renal And Urinary Disorders

Urinary hesitation

Pollakiuria

Urinary retention

Urinary incontinence

Reproductive System And Breast Disorders

Ejaculation disorder

Erectile dysfunction

Metrorrhagia

Menorrhagia

General Disorders And Administration Site Conditions

Fatigue

Asthenia

Chills

Mucosal haemorrhage

Investigations

Bleeding time prolonged

Weight Decreased

Weight increased

Blood cholestarol increased

Meanwhile, the following symptoms reported in association with abrupt discontinuation or dose reduction, or tapering of treatment:

Hypomainia

Anxiety

Agitation

Nervousness

Confusion

Insomnia or other sleep disturbances

Fatigue

Somnolence

Paraesthesia

Dizziness

Convulsion

Vertigo

Headache

Flu like symptoms

Tinnitus

Impaired coordination and balance

Tremor

Sweating

Dry mouth

Anorexia

Diarrhoea

Nausea

Vomiting

However, In premarketing studies the majority of discontinuation reactions were mild and resolved without treatment .

Pediatric Patients

In general , the adverse reaction profile of Venlafaxine (in placebo controlled clinical trials) in children and adolescents (aged 6 to 17) was similar to that seen in adults. As with adults, decreased appetite, weight loss, increased blood pressure and increased serum cholesterol observed .

On the other hand, In pediatric clinical trials, the adverse reaction suicidal ideation observed. Also increased reported of hostility and, especially in major depressive disorder, self-harm.

Particular the following adverse reaction observed in pediatric patients.

Abdominal pain

Agitaon

Dyspepsia

Ecchymosis

Epistaxis

Myalgia.

Efexor XR Overdose

In post marketing experience Efexor XR Tablets overdose with venlafaxine reported predominantly in combination with alcohol and other drugs. The most commonly reported events in overdose include tachycardia, changes in levels of consciousness (ranging from somnolence to coma), mydriasis, convulsion, and vomiting . Other events reported include electrocardiographic changes (e.g. prolongation of QT interval , bundle branch block , QRS prolongation), venlafaxine tachycardia, bradycardia, hypotension, vertigo, and death.

Meanwhile, Published retrospective studies report that Venlafaxine Overdose may be associated with an increased risk of fatal outcomes compared to that observed with SSRI antidepressant products. But at lower that that for tricyclic antidepressants . Epidemiological studies have shown that venlafaxine treated patients have a higher burden of suicide risk factors than SSRl treated patients. However, The extent tom which the finding of an increased risk of fatal outcomes can be attributed to the toxicity of venlafaxine in overdose as opposed to some charateristics of venlafaxin treated patients is not clear. Prescriptions for venlafaxine should written for the smallest quantity of drug consistent with good patients management in order to reduce the risk of overdose.

Efexor XR Storage Instructions

Most importantly, protect the drug from sunlight and heat. On the other hand, Store the tablets in well closed container. Most importantly always remember to keep all your medicine out of the reach of the children.

Other Medical Information: Presage Injection 5000 I.U. Uses, Dosage, Side Effects

Efexor Xr (Venlafaxine) 75MG, 150MG Tablets Capsules

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