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PRISTIQ® (desvenlafaxine) Extended-Release Tablets

Please see package insert for additional information and possible updates. The authors make no claims of the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical judgment. Neither GlobalRPh Inc. nor any other party involved in the preparation of this program shall be liable for any special, consequential, or exemplary damages resulting in whole or part from any user's use of or reliance upon this material. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER.    [  Read the disclaimer    |   <<Back    |    ANTIDEPRESSANTS led    ]

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DESCRIPTION CLINICAL PHARMACOLOGY
INDICATIONS AND USAGE CONTRAINDICATIONS
PRECAUTIONS ADVERSE REACTIONS
DOSAGE AND ADMINISTRATION HOW SUPPLIED
WARNINGS

WARNINGS  top of page

WARNING: SUICIDALITY AND ANTIDEPRESSANT DRUGS
Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of Major Depressive Disorder (MDD) and other psychiatric disorders. Anyone considering the use of PRISTIQ® or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. PRISTIQ is not approved for use in pediatric patients [see Warnings and Precautions, Use in Specific Populations, and Patient Counseling Information - PACKAGE INSERT].

(DESCRIPTION) top of page

Initial U.S. Approval: 2008
DESCRIPTION
PRISTIQ is an extended-release tablet for oral administration that contains desvenlafaxine succinate, a structurally novel SNRI for the treatment of MDD. Desvenlafaxine (O-desmethylvenlafaxine) is the major active metabolite of the antidepressant venlafaxine, a medication used to treat major depressive, generalized anxiety, social anxiety and panic disorders.

Desvenlafaxine is designated RS-4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol and has the empirical formula of C16H25NO2 (free base) and C16H25NO2•C4H6O4•H2O (succinate monohydrate). Desvenlafaxine succinate monohydrate has a molecular weight of 399.48.

Desvenlafaxine succinate is a white to off-white powder that is soluble in water. The solubility of desvenlafaxine succinate is pH dependent. Its octanol:aqueous system (at pH 7.0) partition coefficient is 0.21.

PRISTIQ is formulated as an extended-release tablet for once-a-day oral administration.

Each tablet contains 76 or 152 mg of desvenlafaxine succinate equivalent to 50 or 100 mg of desvenlafaxine, respectively.

Inactive ingredients for the 50 mg tablet consist of hypromellose, microcrystalline cellulose, talc, magnesium stearate and film coating, which consists of polyvinyl alcohol, polyethylene glycol, talc, titanium dioxide, and iron oxides.

Inactive ingredients for the 100 mg tablet consist of hypromellose, microcrystalline cellulose, talc, magnesium stearate and film coating, which consists of polyvinyl alcohol, polyethylene glycol, talc, titanium dioxide, iron oxide and FD&C yellow #6.

CLINICAL PHARMACOLOGY: top of page

CLINICAL PHARMACOLOGY

Mechanism of Action
Non-clinical studies have shown that desvenlafaxine succinate is a potent and selective serotonin and norepinephrine reuptake inhibitor (SNRI). The clinical efficacy of desvenlafaxine succinate is thought to be related to the potentiation of these neurotransmitters in the central nervous system.


Pharmacodynamics
Desvenlafaxine lacked significant affinity for numerous receptors, including muscarinic-cholinergic, H1-histaminergic, or alpha1-adrenergic receptors in vitro. PRISTIQ also lacked monoamine oxidase (MAO) inhibitory activity.


Pharmacokinetics
The single-dose pharmacokinetics of desvenlafaxine are linear and dose-proportional in a dose range of 100 to 600 mg/day. The mean terminal half-life, t1/2, is approximately 11 hours. With once-daily dosing, steady-state plasma concentrations are achieved within approximately 4-5 days. At steady-state, multiple-dose accumulation of desvenlafaxine is linear and predictable from the single-dose pharmacokinetic profile.

INDICATIONS AND USAGE  top of page

INDICATIONS AND USAGE
PRISTIQ, a selective serotonin and norepinephrine reuptake inhibitor (SNRI), is indicated for the treatment of major depressive disorder [MDD]

USE IN SPECIFIC POPULATIONS
Dosage adjustment is recommended in patients with severe renal impairment and end-stage renal disease. The dose should not be escalated in moderate to severe impairment or in ESRD.

There is an increased incidence of orthostatic hypotension in PRISTIQ treated patients >/= 65 years.

For elderly patients, the possibility of reduced renal clearance of desvenlafaxine should be considered when determining dose.

Only administer PRISTIQ to pregnant or breastfeeding women if the expected benefits outweigh the possible risks.

CONTRAINDICATIONS top of page

CONTRAINDICATIONS
Hypersensitivity to desvenlafaxine succinate, venlafaxine hydrochloride or any excipients in the PRISTIQ formulation.

Do not use with an MAOI or within 14 days of stopping an MAOI. Allow 7 days after stopping PRISTIQ before starting an MAOI

PRECAUTIONS top of page

WARNINGS AND PRECAUTIONS
  • Clinical Worsening/Suicide Risk: Monitor for clinical worsening and suicide risk
  • Serotonin Syndrome or Neuroleptic Malignant Syndrome (NMS)-like Reactions: Serotonin syndrome or NMS-like reactions have been reported with SSRIs and SNRIs. Discontinue PRISTIQ and initiate supportive treatment
  • Elevated Blood Pressure: Has occurred with PRISTIQ. Hypertension should be controlled before initiating treatment. Monitor blood pressure regularly during treatment
  • Abnormal Bleeding: PRISTIQ may increase the risk of bleeding events. Patients should be cautioned about the risk of bleeding associated with the concomitant use of PRISTIQ and NSAIDs, aspirin, or other drugs that affect coagulation
  • Narrow-angle Glaucoma: Mydriasis has occurred with PRISTIQ. Patients with raised intraocular pressure or those at risk of angle-closure glaucoma should be monitored
  • Activation of Mania/Hypomania: Has occurred. Use cautiously in patients with Bipolar Disorder. Caution patients about the risk of activation of mania/hypomania
  • Cardiovascular/Cerebrovascular Disease: Use cautiously in patients with cardiovascular or cerebrovascular disease
  • Cholesterol and Triglyceride Elevation: Have occurred. Use cautiously in patients with lipid metabolism disorders. Consider monitoring serum cholesterol and triglyceride
  • Discontinuation Symptoms: Have occurred. Taper the dose when possible and monitor for discontinuation symptoms
  • Renal Impairment: Reduces the clearance of PRISTIQ. Dosage adjustment is necessary in severe and ESRD. In moderate renal impairment, the dose should not exceed 50 mg/day
  • Seizure: Can occur. Use cautiously in patients with seizure disorder
  • Hyponatremia: Can occur in association with SIADH
  • Drugs Containing Desvenlafaxine or Venlafaxine: Should not be used concomitantly with PRISTIQ
  • Interstitial Lung Disease and Eosinophilic Pneumonia: Can occur

ADVERSE REACTIONS top of page

ADVERSE REACTIONS
Adverse reactions in patients in short-term fixed-dose studies (incidence >/= 5% and twice the rate of placebo in the 50 or 100 mg dose groups) were: nausea, dizziness, insomnia, hyperhidrosis, constipation, somnolence, decreased appetite, anxiety, and specific male sexual function disorders.

To report SUSPECTED ADVERSE REACTIONS, contact Wyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc., at 1-800-934-5556 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch

DOSAGE AND ADMINISTRATION  top of page

DOSAGE AND ADMINISTRATION
Initial Treatment of Major Depressive Disorder
The recommended dose for PRISTIQ is 50 mg once daily, with or without food.

In clinical studies, doses of 50-400 mg/day were shown to be effective, although no additional benefit was demonstrated at doses greater than 50 mg/day and adverse events and discontinuations were more frequent at higher doses.

When discontinuing therapy, gradual dose reduction is recommended whenever possible to minimize discontinuation symptoms [see Dosage and Administration (2.4) and Warnings and Precautions (5.9)].

PRISTIQ should be taken at approximately the same time each day. Tablets must be swallowed whole with fluid and not divided, crushed, chewed, or dissolved.


2.2 Special Populations

Pregnant women during the third trimester
Neonates exposed to SNRIs or SSRIs late in the third trimester have developed complications requiring prolonged hospitalization, respiratory support, and tube feeding [see Use in Specific Populations (8.1)]. When treating pregnant women with PRISTIQ during the third trimester, the physician should carefully consider the potential risks and benefits of treatment. The physician may consider tapering PRISTIQ in the third trimester.


Patients with renal impairment
No dosage adjustment is necessary in patients with mild renal impairment (24-hr CrCl = 50-80 mL/min).

The recommended dose in patients with moderate renal impairment (24-hr CrCl = 30-50 mL/min) is 50 mg per day. The recommended dose in patients with severe renal impairment (24-hr CrCl < 30 mL/min) or end-stage renal disease (ESRD) is 50 mg every other day. Supplemental doses should not be given to patients after dialysis. The doses should not be escalated in patients with moderate or severe renal impairment, or ESRD [see Warnings and Precautions (5.10), Use in Specific Populations (8.6) and Clinical Pharmacology (12.6)].


Patients with hepatic impairment
The recommended dose in patients with hepatic impairment is 50 mg/day. Dose escalation above 100 mg/day is not recommended [see Clinical Pharmacology (12.6)].


Elderly patients
No dosage adjustment is required solely on the basis of age; however, the possibility of reduced renal clearance of PRISTIQ should be considered when determining the dose [see Use in Specific Populations (8.5) and Clinical Pharmacology (12.6)].


2.3 Maintenance/Continuation/Extended Treatment
It is generally agreed that acute episodes of major depressive disorder require several months or longer of sustained pharmacologic therapy. However, the longer-term efficacy of PRISTIQ at a dose of 50 mg/day that was effective in short-term, controlled studies has not been studied. Patients should be periodically reassessed to determine the need for continued treatment.


2.4 Discontinuing PRISTIQ
Symptoms associated with discontinuation of PRISTIQ, other SNRIs and SSRIs have been reported [see Warnings and Precautions (5.9)]. Patients should be monitored for these symptoms when discontinuing treatment. A gradual reduction in the dose rather than abrupt cessation is recommended whenever possible. If intolerable symptoms occur following a decrease in the dose or upon discontinuation of treatment, then resuming the previously prescribed dose may be considered. Subsequently, the physician may continue decreasing the dose, but at a more gradual rate.


2.5 Switching Patients From Other Antidepressants to PRISTIQ
Discontinuation symptoms have been reported when switching patients from other antidepressants, including venlafaxine, to PRISTIQ. Tapering of the initial antidepressant may be necessary to minimize discontinuation symptoms [see Contraindications (4.2)].


2.6 Switching Patients To or From a Monoamine Oxidase Inhibitor (MAOI)
At least 14 days must elapse between discontinuation of an MAOI and initiation of therapy with PRISTIQ. In addition, at least 7 days must be allowed after stopping PRISTIQ before starting an MAOI [see Contraindications (4.2)].

HOW SUPPLIED top of page

DOSAGE FORMS AND STRENGTHS
PRISTIQ tablets are available as 50 and 100 mg tablets.

Each tablet contains 76 mg or 152 mg of desvenlafaxine succinate equivalent to 50 mg or 100 mg of desvenlafaxine

REFERENCE

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