pharmacopeia

Tartrate

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Mechanism of action

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Although the precise mechanism of action of rivastigmine is unknown, it is thought to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase.

Indications

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  • Rivastigmine tartrate capsules are an acetylcholinesterase inhibitor indicated for treatment of: Mild-to-moderate dementia of the Alzheimer’s type (AD) (1.1) Mild-to-moderate dementia associated with Parkinson’s disease (PD) (1.2) 1.1 Alzheimer’s Disease Rivastigmine tartrate capsules are indicated for the treatment of mild-to-moderate dementia of the Alzheimer's type (AD). 1.2 Parkinson’s Disease Dementia Rivastigmine tartrate capsules are indicated for the treatment of mild-to-moderate dementia associated with Parkinson’s disease (PD).ICD-10: G30.9

Contraindications

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  • Rivastigmine tartrate capsules are contraindicated in patients with: known hypersensitivity to rivastigmine, other carbamate derivatives or other components of the formulation [see Description (11)] a previous history of application site reaction with rivastigmine transdermal patch suggestive of allergic contact dermatitis, in the absence of negative allergy testing [see Warnings and Precautions (5.2)] Isolated cases of generalized skin reactions have been described in postmarketing experience [see Adverse Reactions (6.2)]. Known hypersensitivity to rivastigmine, other carbamate derivatives or other components of the formulation.contraindicated

Dosage & administration

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Alzheimer’s Disease (2.1): Initial Dose: Initiate treatment with 1.5 mg twice a day. Dose Titration: After a minimum of 2 weeks, if tolerated, increase dose to 3 mg twice a day and further to 4.5 mg twice a day and 6 mg twice a day if tolerated with a minimum of 2 weeks at each dose Parkinson’s Disease Dementia (PDD) (2.2): Initial Dose: Initiate treatment with 1.5 mg twice a day. Dose Titration: After a minimum of 4 weeks, if tolerated, increase dose to 3 mg twice a day and further to 4.5 mg twice a day and 6 mg twice a day if tolerated with a minimum of 4 weeks at each dose. Rivastigmine tartrate capsules should be taken with meals in divided doses in the morning and evening (2.1, 2.2). Rivastigmine tartrate oral solution and Rivastigmine tartrate capsules may be interchanged at equal doses (2.5) 2.1 Dosing in Alzheimer's Disease Rivastigmine tartrate capsules should be taken with meals in divided doses in the morning and evening. The recommended dosage of rivastigmine tartrate capsules in Alzheimer’s disease (AD) is 6 mg to 12 mg per day, administered twice a day (daily doses of 3 mg to 6 mg twice a day). There is evidence from the clinical trials that doses at the higher end of this range may be more beneficial. Initial Dose Initiate treatment with the 1.5 mg twice a day with rivastigmine tartrate capsules. Dose Titration After a minimum of 2 weeks and if well tolerated, increase the dose to 3 mg twice a day. Subsequent increases to 4.5 mg twice a day and 6 mg twice a day should be attempted after a minimum of 2 weeks at the previous dose and if well tolerated.

Warnings & precautions

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Gastrointestinal adverse reactions may include significant nausea, vomiting, diarrhea, anorexia/decreased appetite, and weight loss, and may necessitate treatment interruption. Dehydration may result from prolonged vomiting or diarrhea and can be associated with serious outcomes. (5.1) Discontinue rivastigmine in case of disseminated allergic dermatitis, which may occur after oral or transdermal administration (4, 5.2). In patients with suspected allergic contact dermatitis after transdermal rivastigmine use, switch to oral rivastigmine only after negative allergy testing. 5.1 Gastrointestinal Adverse Reactions Rivastigmine tartrate can cause gastrointestinal adverse reactions, including significant nausea, vomiting, diarrhea, anorexia/decreased appetite, and weight loss. Dehydration may result from prolonged vomiting or diarrhea and can be associated with serious outcomes. The incidence and severity of these reactions are dose-related [see Adverse Reactions (6.1)] . For this reason, patients should always be started at a dose of 1.5 mg twice a day and titrated to their maintenance dose. If treatment is interrupted for longer than 3 days, treatment should be reinitiated with the lowest daily dose [see Dosage and Administration (2.3)] to reduce the possibility of severe vomiting and its potentially serious sequelae (e.g., there has been one postmarketing report of severe vomiting with esophageal rupture following inappropriate reinitiation of treatment with a 4.5-mg dose after 8 weeks of treatment interruption).

Adverse reactions

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The following adverse reactions are described below and elsewhere in the labeling: · Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.1)] · Allergic Dermatitis [see Warnings and Precautions (5.2)] · Other Adverse Reactions from Increased Cholinergic Activity [see Warnings and Precautions (5.3)] Most common adverse reactions (greater than 5% and 2 times greater than placebo): nausea, vomiting, anorexia, dyspepsia, and asthenia (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Alembic Pharmaceuticals Limited at 1-866-210-9797 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Rivastigmine tartrate has been administered to over 5,297 individuals during clinical trials worldwide. Of these, 4,326 patients have been treated for at least 3 months, 3,407 patients have been treated for at least 6 months, 2,150 patients have been treated for 1 year, 1,250 patients have been treated for 2 years, and 168 patients have been treated for over 3 years. With regard to exposure to the highest dose, 2,809 patients were exposed to doses of 10 mg to 12 mg, 2,615 patients treated for 3 months, 2,328 patients treated for 6 months, 1,378 patients treated for 1 year, 917 patients treated for 2 years, and 129 patients treated for over 3 years.

Use in specific populations

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8.1 Pregnancy Risk Summary There are no adequate data on the developmental risks associated with the use of rivastigmine tartrate in pregnant women. In animals, no adverse effects on embryo-fetal development were observed at oral doses 2 to 4 times the maximum recommended human dose (MRHD) (see Data) . The background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data Oral administration of rivastigmine to pregnant rats and rabbits throughout organogenesis produced no adverse effects on embryo-fetal development up to the highest dose tested (2.3 mg/kg/day), which is 2 and 4 times, respectively, the MRHD of 12 mg per day on a body surface area (mg/m 2 ) basis. 8.2 Lactation Risk Summary There are no data on the presence of rivastigmine in human milk, the effects on the breastfed infant, or the effects of rivastigmine on milk production. Rivastigmine and its metabolites are excreted in rat milk following oral administration of rivastigmine; levels of rivastigmine plus metabolites in rat milk are approximately 2 times that in maternal plasma.

Pharmacokinetics

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Metabolism
Rivastigmine shows linear pharmacokinetics up to 3 mg twice a day but is nonlinear at higher doses. Doubling the dose from 3 mg to 6 mg twice a day results in a 3-fold increase in area under the curve (AUC).

Overdosage

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Because strategies for the management of overdose are continually evolving, it is advisable to contact a Poison Control Center to determine the latest recommendations for the management of an overdose of any drug. As rivastigmine has a short plasma half-life of about 1 hour and a moderate duration of acetylcholinesterase inhibition of 8 to 10 hours, it is recommended that in cases of asymptomatic overdoses, no further dose of rivastigmine tartrate capsules should be administered for the next 24 hours. As in any case of overdose, general supportive measures should be utilized. Overdosage with cholinesterase inhibitors can result in cholinergic crisis characterized by severe nausea, vomiting, salivation, sweating, bradycardia, hypotension, respiratory depression, collapse and convulsions. Increasing muscle weakness is a possibility and may result in death if respiratory muscles are involved. Atypical responses in blood pressure and heart rate have been reported with other drugs that increase cholinergic activity when coadministered with quaternary anticholinergics such as glycopyrrolate.

Approval history

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  • Aug 7, 1978NDANDA017963Validus Pharms
  • Dec 16, 1992NDANDA019908Cosette
  • Mar 25, 1998NDANDA020771Upjohn
  • Dec 22, 2000NDANDA021228Upjohn
  • Mar 16, 2001NDANDA021262Abbvie
  • Aug 19, 2005NDANDA021770Abbvie
  • Sep 2, 2005NDANDA021774Cosette
  • May 10, 2006NDANDA021928Pf Prism Cv

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
565,641 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Nausea39,4207.0%
  2. 2Drug Ineffective36,9496.5%
  3. 3Fatigue31,3235.5%
  4. 4Death25,1444.4%
  5. 5Dyspnoea24,1394.3%
  6. 6Diarrhoea23,7034.2%
  7. 7Dizziness23,5734.2%
  8. 8Headache21,7073.8%
  9. 9Fall20,7293.7%
  10. 10Pain19,1103.4%
  11. 11Vomiting18,2373.2%
  12. 12Insomnia18,1363.2%
  13. 13Asthenia17,7983.1%
  14. 14Depression17,6063.1%
  15. 15Anxiety17,3603.1%

Literature

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Recent PubMed references pinned to Tartrate as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 635 ClinicalTrials.gov registrations naming Tartrate as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Tartrate work?
Although the precise mechanism of action of rivastigmine is unknown, it is thought to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase.
What is Tartrate used for?
According to FDA labeling, Tartrate carries indications including: Rivastigmine tartrate capsules are an acetylcholinesterase inhibitor indicated for treatment of: Mild-to-moderate dementia of the Alzheimer’s type (AD) (1.1) Mild-to-moderate dementia associated with Parkinson’s disease (PD) (1.2) 1.1 Alzheimer’s Disease Rivastigmine tartrate capsules are indicated for the treatment of mild-to-moderate dementia of the Alzheimer's type (AD). 1.2 Parkinson’s Disease Dementia Rivastigmine tartrate capsules are indicated for the treatment of mild-to-moderate dementia associated with Parkinson’s disease (PD).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What are the contraindications for Tartrate?
Tartrate labeling lists contraindications including: Rivastigmine tartrate capsules are contraindicated in patients with: known hypersensitivity to rivastigmine, other carbamate derivatives or other components of the formulation [see Description (11)] a previous history of application site reaction with rivastigmine transdermal patch suggestive of allergic contact dermatitis, in the absence of negative allergy testing [see Warnings and Precautions (5.2)] Isolated cases of generalized skin reactions have been described in postmarketing experience [see Adverse Reactions (6.2)]. Known hypersensitivity to rivastigmine, other carbamate derivatives or other components of the formulation.. Always consult the full prescribing information and a clinician.
Note. Data for tartrate is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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