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Tolterodine Tartrate 2 mg Tablet, Film Coated, 60-count

by Mylan Pharmaceuticals Inc. · 60 TABLET, FILM COATED in 1 BOTTLE (59762-0800-2)
NDC 59762-0800-02
🏷️ FDA NDC (as labeled) 59762-0800-2 billing pads the package segment with a zero
This package
Contains60-count Cost per ea$0.2483 NADAC Per package$14.90 / 60 tablets Pack sizes2 compare ↓
Also priced by: Medicaid pays $0.4199/unit — full pricing hub ↓
Also comes in: 500 tablets 59762-0800-06
Rx only Brand Discontinued Non-controlled ⚠ Discontinued by firm
🗂️ Data synced Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →
⚠️
Excluded from the active FDA NDC Directory. The labeler reported this product as discontinued, so it is excluded from the active NDC Directory. The listing was last certified through Jul 2026. A label may still appear on DailyMed, but the NDC is no longer in the current FDA NDC Directory. Search the FDA NDC Directory ↗

🆔 Identity & classification

FDA NDC (as labeled) 59762-0800-2
Product NDC 59762-0800
11-digit billing NDC 59762080002
NCPDP billing unit EA — each (per item)
RxCUI 855178, 855194
UNII 5T619TQR3R
UPC 0359762017062, 0359762080028
Application # NDA020771
SPL Set ID 9e432622-2e6f-4cf8-892f-510288dd50f2
Established class (EPC) Cholinergic Muscarinic Antagonist
Mechanism of action Cholinergic Muscarinic Antagonists
DEA schedule Non-controlled
Marketing category NDA AUTHORIZED GENERIC
Marketing status Discontinued
FDA listing status Discontinued by firm (certified through Jul 2026)
Marketing start 2014-01-21
Marketing end 2026-07-31
Route ORAL
Dosage form TABLET, FILM COATED
Substance TOLTERODINE TARTRATE
GPI-14 54100060200330
GPI class Tolterodine Tartrate
GCN Seq No 039139
GCN 37062
HICL code 018047
Ingredient (HICL) Tolterodine Tartrate
HIC1 code R
Therapeutic class — broad (HIC1) Kidney/Urinary Tract
HIC2 code R1
Therapeutic class — intermediate (HIC2) Affect Primarily Kidneys/Urinary Tract
HIC3 code R1A
Therapeutic class — specific (HIC3) Urinary Tract Antispasmodic/Antiincontinence Agent
AHFS code 86:12.04.00
AHFS class Antimuscarinics
FDB label name TOLTERODINE TARTRATE 2 MG TAB
FDB brand name Tolterodine Tartrate
Legend status F — Federal legend — prescription drug or device
TE code (Orange Book) AB · RLD · RS
Why two NDCs? The FDA registers this code as 59762-0800-2 — a 5-4-1 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the package segment → 59762-0800-02. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

🏷️ RxNorm drug class

This medicine belongs to the Cholinergic Muscarinic Antagonist class.

Pharmacologic class Cholinergic Muscarinic Antagonist
Drug family (ATC) Drugs for urinary frequency and incontinence
How it works Cholinergic Muscarinic Antagonists
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

🏭 Manufacturer & labeler

LabelerMylan Pharmaceuticals Inc.
Application holderUPJOHN US 2 LLC
FDA applicationNDA020771 (NDA AUTHORIZED GENERIC)
Labeler code59762
First marketedJan 2014
Product typeHuman Prescription Drug
Portfolio473 products on file
The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

🩺 Clinical

Label name TOLTERODINE TARTRATE 2 MG TAB Ingredient Tolterodine Tartrate
📗 Our plain-language guide HelloPharmacist
  • Tolterodine calms the bladder by blocking the nerve signals that cause it to squeeze too often or too urgently. Most people start noticing fewer urgent trips to the bathroom and le...
  • What exactly does tolterodine do, and how quickly will I notice a difference?
  • Dry mouth is the most common complaint with tolterodine, and it happens because the same receptors that calm your bladder also affect your saliva glands. Sipping water frequently,...
  • The dry mouth is really bothersome — is there anything I can do about it?
📖 Read our full Tolterodine guide →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

🧪 Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

We could not link this NDC to a current FDA Structured Product Label. An inactive-ingredient list is therefore not available from this source.
Where does this data come from?
Source: official FDA Structured Product Labeling (SPL) via DailyMed and the openFDA label index. Structured IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

💲 Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer eaPer package
Retail pharmacies payNADAC · weekly $0.248 $14.90 / 60 tablets
Medicaid paysCMS SDUD · 12 mo $0.4199 $25.19 / 60 tablets
Medicare drug plans payPart D · quarterly No Part D plan price is available for this NDC in our data.
NADAC price history (per ea) — tap or hover for the price & month
Dec 2021 Jul 2022 Dec 2025 Aug 2026 $0.569 $0.206
▼ Down 46% over the last 24 months.
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

🔁 Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Tolterodine Tartrate 2 mg 00093-0018-05 Teva 500 tablets $0.248 AB Availability likely
Tolterodine tartrate 2 mg 33342-0098-09 Macleods 60 tablets $0.248 AB Availability likely
Tolterodine Tartrate 2 mgthis 59762-0800-02 Mylan 60 tablets $0.248 AB Discontinued
Tolterodine Tartrate 2 mg 16571-0127-01 Rising 100 tablets AB FDA listed
Tolterodine Tartrate 2 mg 29300-0240-01 Unichem 100 tablets AB FDA listed
Tolterodine Tartrate 2 mg 31722-0806-01 Camber 10 tablets AB FDA listed
Detrol 2 mg 58151-0099-91 Viatris 60 tablets AB FDA listed
About this product: this is an authorized generic — the brand-name product marketed without its brand name. Other versions are listed above, least expensive first.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2014
On the market since
Jan 2014
📍
2026
Currently FDA-listed
12 years listed
🔓
·
Generic versions listed
see equivalents
Generic appears available

FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.

Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

🗺️ Medicaid utilization & spend

📍 This exact package only: Medicaid data is reported per full 11-digit NDC — labeler, product and pack size — so every number here is for 59762-0800-02, not the drug overall. Other pack sizes report separately.
💊 Pharmacy benefit only: These are Medicaid outpatient pharmacy claims, billed by NDC. They exclude the medical benefit — clinic- or hospital-administered drugs billed under HCPCS J-codes — so drugs used mostly that way (e.g. Avastin, Lucentis, Keytruda) can look low or missing here. That’s expected, not an error.
📅 Q1 2025 – Q4 2025 · 4 quarters of data
ⓘ The newest quarter is usually incomplete when first published; states restate recent quarters in later CMS releases, so the latest figures typically revise upward. State coverage-policy changes can also shift quarter-to-quarter totals.
Prescriptions last 4 qtrs
296
Units reimbursed last 4 qtrs
20.6K
Gross reimbursed last 4 qtrs
$8.6K
Avg / prescription
$29.19
Avg / unit
$0.4199
Latest quarter Q4 2025
15Rx
Medicaid pays / ea
$0.4199
gross reimbursed
vs
NADAC / ea
$0.2483
acquisition cost
=
Spread
+$0.1716
+69% vs cost
What Medicaid paid per ea (before rebates; includes the pharmacy’s dispensing fee) compared with NADAC — the average price pharmacies pay to buy the drug. A positive spread means Medicaid reimbursed more than the purchase price, before manufacturer rebates.
Fee-for-service vs managed care
24% FFS 76% MCO
Fee-for-service · 70 Rx Managed care · 226 Rx
State Medicaid map
Alaska: no data reported AK Maine: no data reported ME Washington: no data reported WA Idaho: no data reported ID Montana: no data reported MT North Dakota: no data reported ND Minnesota: no data reported MN Wisconsin: no data reported WI Michigan: no data reported MI New York: 810 units · 4.1 per 100k residents NY Vermont: no data reported VT New Hampshire: no data reported NH Oregon: no data reported OR Nevada: no data reported NV Wyoming: no data reported WY South Dakota: no data reported SD Iowa: no data reported IA Illinois: no data reported IL Indiana: 1,830 units · 26.7 per 100k residents IN Ohio: no data reported OH Pennsylvania: 2,610 units · 20.1 per 100k residents PA New Jersey: 3,288 units · 35.4 per 100k residents NJ Massachusetts: 5,071 units · 72.4 per 100k residents MA California: 2,508 units · 6.4 per 100k residents CA Utah: no data reported UT Colorado: no data reported CO Nebraska: no data reported NE Missouri: no data reported MO Kentucky: no data reported KY West Virginia: no data reported WV Virginia: 1,164 units · 13.4 per 100k residents VA Maryland: 1,410 units · 22.8 per 100k residents MD Connecticut: no data reported CT Rhode Island: no data reported RI Arizona: no data reported AZ New Mexico: no data reported NM Kansas: no data reported KS Arkansas: no data reported AR Tennessee: no data reported TN North Carolina: 1,092 units · 10.1 per 100k residents NC South Carolina: no data reported SC Delaware: no data reported DE Oklahoma: no data reported OK Louisiana: no data reported LA Mississippi: no data reported MS Alabama: no data reported AL Georgia: 790 units · 7.2 per 100k residents GA D.C.: no data reported DC Hawaii: no data reported HI Texas: no data reported TX Florida: no data reported FL
Units reimbursed · per 100k residents
4.172.4
gray = no data reported
Colors are per 100,000 residents, so big states don’t automatically dominate. Tap or hover a state for its actual totals.
Tap or hover a state
…for its Medicaid breakdown
🏆 Top states by units · per 100k residents
1 Massachusetts 72.4 /100k
2 New Jersey 35.4 /100k
3 Indiana 26.7 /100k
4 Maryland 22.8 /100k
5 Pennsylvania 20.1 /100k
6 Virginia 13.4 /100k
7 North Carolina 10.1 /100k
8 Georgia 7.2 /100k
National units — by quarter
💵 About the dollar figures: “reimbursed” is what Medicaid paid pharmacies before confidential manufacturer rebates, so the program’s real net cost is lower than these numbers. Fee-for-service and managed-care claims are combined unless split above. Source: CMS State Drug Utilization Data; per-100k rates use 2023 Census population estimates.

💊 Medicaid utilization by pack size

Medicaid (SDUD) totals over the four most recent reported quarters for every package size of this drug — handy when a specific package (e.g. a starter/titration pack) carries little or no Medicaid volume on its own.
Drug total (last 4 qtrs): 296 Rx · 20,573 units · $8,639 gross reimbursed
Tap a pack size to open its page. Source: CMS State Drug Utilization Data, last 4 quarters.

📊 Medicare Part D spend CMS · PART D · 2026 (Q1)

Medicare Part D (outpatient prescription) spending for Tolterodine Tartrate — the program that covers self-administered drugs. 6 manufacturers.
⚠️ Drug-level data: CMS publishes Part D spending by drug, not by NDC — these figures combine every manufacturer, strength and package size sold under the name Tolterodine Tartrate. That’s a different level of aggregation than the Medicaid card above, which is specific to this exact 11-digit NDC (pack size included), so the two aren’t directly comparable.
Period
Total Part D spend
$2.42M
Claims incl. refills
43.3K
Beneficiaries
25.8K
Spend / beneficiary
$93.68
Spend / claim
$55.77
Trend by period
💵 About the dollar figures: spending is what Part D plans paid before confidential manufacturer rebates, so the program’s real net cost is lower. A blank patient count means fewer than 11 people — CMS hides counts that small to protect privacy. Source: CMS Medicare Quarterly Part D Spending by Drug (data.cms.gov), updated quarterly.

📦 Packaging — all sizes for this product

Package NDCDescription Per unit Per pack Marketing startStatus
59762-0800-02 You're viewing this 60 TABLET, FILM COATED in 1 BOTTLE (59762-0800-2) $0.2483 / ea $14.90 2014-01-21 Discontinued by firm
59762-0800-06 500 TABLET, FILM COATED in 1 BOTTLE (59762-0800-6) $0.2483 / ea $124.15 2014-01-21 Discontinued by firm

You're viewing the smallest of 2 pack sizes for this product.

This pack has the lowest per-ea cost of the 2 priced pack sizes ($0.2483 NADAC).

In Medicaid, this is the most-dispensed pack of this product — about 100% of fills over the last four reported quarters. See all packs ↓

Pack size FAQ

What quantity is in NDC 59762-0800-02?
NDC 59762-0800-02 is a 60-count package — 60 tablet, film coated in 1 bottle.
What is the difference between NDC 59762-0800-02 and NDC 59762-0800-06?
Both are Tolterodine Tartrate 2 mg Tablet, Film Coated — the drug itself is identical. NDC 59762-0800-02 is the 60-count package, while NDC 59762-0800-06 is the 500 tablets package.
What NDC number is used to bill for this package of Tolterodine Tartrate 2 mg Tablet, Film Coated?
Bill NDC 59762-0800-02 — the 11-digit billing format is 59762080002. Pharmacy and medical claims use the 11-digit form; the FDA label may print a shorter form of the same code.

Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.

🧭 About this NDC listing & data coverage

Finished prescription product No longer marketed (per FDA listing data)
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos — Not published for this NDC No photo available yet for this listing.
Inactive ingredients (structured) — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available.
NADAC pharmacy acquisition price (CMS) ✓ Available
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) ✓ Available
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

What does the discontinued status mean for this NDC?
The labeler reported a marketing end date (or the listing was delisted), so this specific package is no longer actively marketed. Remaining stock may still be dispensed for a time, and the NDC stays valid for historical records and claims — but data feeds (pricing, labeling) typically stop updating for it. Other package sizes or other manufacturers' versions of the same medication may still be marketed — see the equivalents section where available.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The FDA registers it as 59762-0800-2, which is what is printed on the packaging and shown on DailyMed. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero: 59762-0800-02, written without dashes as 59762080002. The Identity section at the top of this page lists every form of this code.
What do the three segments of this NDC mean?
In 59762-0800-02, the first segment (59762) is the labeler code FDA assigned to Mylan Pharmaceuticals Inc.; the middle segment (0800) identifies this specific product — its ingredient, strength, and dosage form; and the last segment (02) identifies this exact package size and type. Together they name one specific package of one specific product.
Does this product come in other package sizes?
Yes — the FDA directory lists 1 other package presentation of this same product, including 500 tablets (59762-0800-06). Each has its own NDC and its own page — see the package list near the top of this page.
Who lists this product with the FDA?
Mylan Pharmaceuticals Inc. is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.

📄 Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage 23 words

INDICATIONS AND USAGE Tolterodine tartrate tablets are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.

⏱️ Dosage and Administration 81 words

DOSAGE AND ADMINISTRATION The initial recommended dose of tolterodine tartrate tablets is 2 mg twice daily. The dose may be lowered to 1 mg twice daily based on individual response and tolerability. For patients with significantly reduced hepatic or renal function or who are currently taking drugs that are potent inhibitors of CYP3A4, the recommended dose of tolterodine tartrate tablets is 1 mg twice daily (see PRECAUTIONS, General , PRECAUTIONS, Reduced Hepatic and Renal Function , and PRECAUTIONS, Drug Interactions ).

Contraindications 51 words

CONTRAINDICATIONS Tolterodine tartrate tablets are contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. Tolterodine tartrate tablets are also contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients, or to fesoterodine fumarate extended-release tablets which, like tolterodine tartrate tablets, are metabolized to 5-hydroxymethyl tolterodine.

⚠️ Warnings 48 words

WARNINGS Anaphylaxis and angioedema requiring hospitalization and emergency medical treatment have occurred with the first or subsequent doses of tolterodine tartrate tablets. In the event of difficulty in breathing, upper airway obstruction, or fall in blood pressure, tolterodine tartrate tablets should be discontinued and appropriate therapy promptly provided.

🤒 Adverse Reactions ~3 min read

ADVERSE REACTIONS The Phase 2 and 3 clinical trial program for tolterodine tartrate tablets included 3071 patients who were treated with tolterodine tartrate tablets (N=2133) or placebo (N=938). The patients were treated with 1, 2, 4, or 8 mg/day for up to 12 months. No differences in the safety profile of tolterodine were identified based on age, gender, race, or metabolism.

The data described below reflect exposure to tolterodine tartrate tablets 2 mg bid in 986 patients and to placebo in 683 patients exposed for 12 weeks in five Phase 3, controlled clinical studies. 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. The adverse reaction information from clinical trials does, however, provide a basis for identifying the adverse events that appear to be related to drug use and approximating rates.

Sixty-six percent of patients receiving tolterodine tartrate tablets 2 mg bid reported adverse events versus 56% of placebo patients. The most common adverse events reported by patients receiving tolterodine tartrate tablets were dry mouth, headache, constipation, vertigo/dizziness, and abdominal pain. Dry mouth, constipation, abnormal vision (accommodation abnormalities), urinary retention, and xerophthalmia are expected side effects of antimuscarinic agents.

Dry mouth was the most frequently reported adverse event for patients treated with tolterodine tartrate tablets 2 mg bid in the Phase 3 clinical studies, occurring in 34.8% of patients treated with tolterodine tartrate tablets and 9.8% of placebo-treated patients. One percent of patients treated with tolterodine tartrate tablets discontinued treatment due to dry mouth. The frequency of discontinuation due to adverse events was highest during the first 4 weeks of treatment.

Seven percent of patients treated with tolterodine tartrate tablets 2 mg bid discontinued treatment due to adverse events versus 6% of placebo patients. The most common adverse events leading to discontinuation of tolterodine tartrate tablets were dizziness and headache. Three percent of patients treated with tolterodine tartrate tablets 2 mg bid reported a serious adverse event versus 4% of placebo patients.

Significant ECG changes in QT and QTc have not been demonstrated in clinical-study patients treated with tolterodine tartrate tablets 2 mg bid. Table 5 lists the adverse events reported in 1% or more of the patients treated with tolterodine tartrate tablets 2 mg bid in the 12-week studies. The adverse events are reported regardless of causality.

Table 5. Incidence in nearest integer. (%) of Adverse Events Exceeding Placebo Rate and Reported in >1% of Patients Treated with Tolterodine TartrateTablets (2 mg bid) in 12-week, Phase 3 Clinical Studies Body System Adverse Event % Tolterodine Tartrate Tablets N=986 % Placebo N=683 Autonomic Nervous accommodation abnormal 2 1 dry mouth 35 10 General chest pain 2 1 fatigue 4 3 headache 7 5 influenza-like symptoms 3 2 Central/Peripheral Nervous vertigo/dizziness 5 3 Gastrointestinal abdominal pain 5 3 constipation 7 4 diarrhea 4 3 dyspepsia 4 1 Urinary dysuria 2 1 Skin/Appendages dry skin 1 0 Musculoskeletal arthralgia 2 1 Vision xerophthalmia 3 2 Psychiatric somnolence 3 2 Metabolic/Nutritional weight gain 1 0 Resistance Mechanism infection 1 0 Post-marketing Surveillance The following events have been reported in association with tolterodine use in worldwide post-marketing experience: General: anaphylaxis and angioedema; Cardiovascular: tachycardia, palpitations, peripheral edema; Central/Peripheral Nervous: confusion, disorientation, memory impairment, hallucinations.

Reports of aggravation of symptoms of dementia (e.g., confusion, disorientation, delusion) have been reported after tolterodine therapy was initiated in patients taking cholinesterase in…

🔄 Drug Interactions 82 words

Drug Interactions CYP3A4 Inhibitors Ketoconazole, an inhibitor of the drug metabolizing enzyme CYP3A4, significantly increased plasma concentrations of tolterodine when coadministered to subjects who were poor metabolizers (see CLINICAL PHARMACOLOGY , Variability in Metabolism and Drug-Drug Interactions ). For patients receiving ketoconazole or other potent CYP3A4 inhibitors such as other azole antifungals (e.g., itraconazole, miconazole) or macrolide antibiotics (e.g., erythromycin, clarithromycin) or cyclosporine or vinblastine, the recommended dose of tolterodine tartrate tablets is 1 mg twice daily (see DOSAGE AND ADMINISTRATION ).

🔄 Drug / Laboratory Test Interactions 12 words

Drug-Laboratory-Test Interactions Interactions between tolterodine and laboratory tests have not been studied.

🤰 Pregnancy 148 words

Pregnancy Tolterodine, administered at oral doses of 20 mg/kg/day (approximately 14 times the human exposure), showed no anomalies or malformations in mice. When given at doses of 30 to 40 mg/kg/day, tolterodine has been shown to be embryolethal, reduce fetal weight, and increase the incidence of fetal abnormalities (cleft palate, digital abnormalities, intra-abdominal hemorrhage, and various skeletal abnormalities, primarily reduced ossification) in mice. At these doses, the AUC values were about 20- to 25-fold higher than in humans.

Rabbits treated subcutaneously at a dose of 0.8 mg/kg/day achieved an AUC of 100 µg·h/L, which is about 3-fold higher than that resulting from the human dose. This dose did not result in any embryotoxicity or teratogenicity. There are no studies of tolterodine in pregnant women.

Therefore, tolterodine tartrate tablets should be used during pregnancy only if the potential benefit for the mother justifies the potential risk to the fetus.

🧒 Pediatric Use 108 words

Pediatric Use Efficacy in the pediatric population has not been demonstrated. Two pediatric phase 3 randomized, placebo-controlled, double-blind, 12-week studies were conducted using tolterodine extended release capsules. A total of 710 pediatric patients (486 on tolterodine tartrate extended-release capsules and 224 on placebo) aged 5–10 years with urinary frequency and urge urinary incontinence were studied.

The percentage of patients with urinary tract infections was higher in patients treated with tolterodine tartrate extended-release capsules (6.6%) compared to patients who received placebo (4.5%). Aggressive, abnormal, and hyperactive behavior and attention disorders occurred in 2.9% of children treated with tolterodine tartrate extended-release capsules compared to 0.9% of children treated with placebo.

🧓 Geriatric Use 51 words

Geriatric Use Of the 1120 patients who were treated in the four Phase 3, 12-week clinical studies of tolterodine tartrate tablets, 474 (42%) were 65 to 91 years of age. No overall differences in safety were observed between the older and younger patients (see CLINICAL PHARMACOLOGY, Pharmacokinetics in Special Populations ).

🆘 Overdosage 140 words

OVERDOSAGE A 27-month-old child who ingested 5 to 7 tolterodine tartrate tablets 2 mg was treated with a suspension of activated charcoal and was hospitalized overnight with symptoms of dry mouth. The child fully recovered. Management of Overdosage Overdosage with tolterodine tartrate tablets can potentially result in severe central anticholinergic effects and should be treated accordingly.

ECG monitoring is recommended in the event of overdosage. In dogs, changes in the QT interval (slight prolongation of 10% to 20%) were observed at a suprapharmacologic dose of 4.5 mg/kg, which is about 68 times higher than the recommended human dose. In clinical trials of normal volunteers and patients, QT interval prolongation was observed with tolterodine immediate release at doses up to 8 mg (4 mg bid) and higher doses were not evaluated (see PRECAUTIONS, Patients with Congenital or Acquired QT Prolongation ).

🧬 Clinical Pharmacology ~3 min read

CLINICAL PHARMACOLOGY Tolterodine is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite.

The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function.

Effects on urodynamic parameters before and 1 and 5 hours after a single 6.4 mg dose of tolterodine immediate release were determined in healthy volunteers. The main effects of tolterodine at 1 and 5 hours were an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure. These findings are consistent with an antimuscarinic action on the lower urinary tract.

Pharmacokinetics Absorption In a study with 14 C-tolterodine solution in healthy volunteers who received a 5 mg oral dose, at least 77% of the radiolabeled dose was absorbed. Tolterodine immediate release is rapidly absorbed, and maximum serum concentrations (C max ) typically occur within 1 to 2 hours after dose administration. C max and area under the concentration-time curve (AUC) determined after dosage of tolterodine immediate release are dose-proportional over the range of 1 to 4 mg.

Effect of Food Food intake increases the bioavailability of tolterodine (average increase 53%), but does not affect the levels of the 5-hydroxymethyl metabolite in extensive metabolizers. This change is not expected to be a safety concern and adjustment of dose is not needed. Distribution Tolterodine is highly bound to plasma proteins, primarily α 1 -acid glycoprotein.

Unbound concentrations of tolterodine average 3.7% ± 0.13% over the concentration range achieved in clinical studies. The 5-hydroxymethyl metabolite is not extensively protein bound, with unbound fraction concentrations averaging 36% ± 4.0%. The blood to serum ratio of tolterodine and the 5-hydroxymethyl metabolite averages 0.6 and 0.8, respectively, indicating that these compounds do not distribute extensively into erythrocytes.

The volume of distribution of tolterodine following administration of a 1.28 mg intravenous dose is 113 ±

26.7L. Metabolism Tolterodine is extensively metabolized by the liver following oral dosing. The primary metabolic route involves the oxidation of the 5-methyl group and is mediated by the cytochrome P450 2D6 (CYP2D6) and leads to the formation of a pharmacologically active 5-hydroxymethyl metabolite.

Further metabolism leads to formation of the 5-carboxylic acid and N-dealkylated 5-carboxylic acid metabolites, which account for 51% ± 14% and 29% ± 6.3% of the metabolites recovered in the urine, respectively. Variability in Metabolism A subset (about 7%) of the population is devoid of CYP2D6, the enzyme responsible for the formation of the 5-hydroxymethyl metabolite of tolterodine. The identified pathway of metabolism for these individuals (“poor metabolizers”) is dealkylation via cytochrome P450 3A4 (CYP3A4) to N -dealkylated tolterodine.

The remainder of the population is referred to as “extensive metabolizers.” Pharmacokinetic studies revealed that tolterodine is metabolized at a slower rate in poor metabolizers than in extensive metabolizers; this results in significantly higher serum concentrations of tolterodine and in negligible concentrations of the 5-hydroxymethyl metabolite. Excretion Following administration of a 5 mg oral dose of 14 C-tolterodine solution to healthy volunteers, 77% of radioactivity was recovered in…

📦 How Supplied / Storage and Handling 108 words

HOW SUPPLIED Tolterodine Tartrate Tablets 1 mg (white, round, biconvex, film-coated tablets engraved with arcs above and below the letters “TO”) and Tolterodine Tartrate Tablets 2 mg (white, round, biconvex, film-coated tablets engraved with arcs above and below the letters “DT”) are supplied as follows: Bottles of 60 1 mg NDC 59762-0170-6 2 mg NDC 59762-0800-2 Bottles of 500 1 mg NDC 59762-0170-1 2 mg NDC 59762-0800-6 Store at 25ºC (77ºF); excursions permitted to 15–30ºC (59–86ºF) [see USP Controlled Room Temperature].

GREENSTONE ® BRAND Distributed by: Greenstone LLC Morgantown, WV 26505 U.S.A. © 2024 Viatris Inc. The brands listed are trademarks of their respective owners. GST:TOLT:R1 Revised: 9/2024

📋 Description 151 words

DESCRIPTION Tolterodine tartrate tablets contain tolterodine tartrate. The active moiety, tolterodine, is a muscarinic receptor antagonist. The chemical name of tolterodine tartrate is (R)-2-[3-[bis(1-methylethyl)-amino]1-phenylpropyl]-4-methylphenol [R-(R*,R*)]-2,3dihydroxybutanedioate (1:1) (salt).

The empirical formula of tolterodine tartrate is C 26 H 37 NO 7 , and its molecular weight is 475.6. The structural formula of tolterodine tartrate is represented below: Tolterodine tartrate is a white, crystalline powder. The pKa value is 9.87 and the solubility in water is 12 mg/mL.

It is soluble in methanol, slightly soluble in ethanol, and practically insoluble in toluene. The partition coefficient (Log D) between n-octanol and water is 1.83 at pH 7.3. Tolterodine tartrate tablets for oral administration contain 1 or 2 mg of tolterodine tartrate.

The inactive ingredients are colloidal anhydrous silica, calcium hydrogen phosphate dihydrate, cellulose microcrystalline, hypromellose, magnesium stearate, sodium starch glycolate (pH 3.0 to 5.0), stearic acid, and titanium dioxide. structural formula of tolterodine tartrate

💬 Information for Patients 47 words

Information for Patients Patients should be informed that antimuscarinic agents such as tolterodine tartrate tablets may produce the following effects: blurred vision, dizziness, or drowsiness. Patients should be advised to exercise caution in decisions to engage in potentially dangerous activities until the drug's effects have been determined.

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.