Trifluridine
Sandoz Inc
Human Prescription Drug
NDC 61314-044Trifluridine is a human prescription drug labeled by 'Sandoz Inc'. National Drug Code (NDC) number for Trifluridine is 61314-044. This drug is available in dosage form of Solution. The names of the active, medicinal ingredients in Trifluridine drug includes Trifluridine - 10 mg/mL . The currest status of Trifluridine drug is Active.
Drug Information:
| Drug NDC: | 61314-044 |
| The labeler code and product code segments of the National Drug Code number, separated by a hyphen. Asterisks are no longer used or included within the product code segment to indicate certain configurations of the NDC. |
| Proprietary Name: | Trifluridine |
| Also known as the trade name. It is the name of the product chosen by the labeler. |
| Product Type: | Human Prescription Drug |
| Indicates the type of product, such as Human Prescription Drug or Human OTC Drug. This data element corresponds to the “Document Type” of the SPL submission for the listing. |
| Non Proprietary Name: | Trifluridine |
| Also known as the generic name, this is usually the active ingredient(s) of the product. |
| Labeler Name: | Sandoz Inc |
| Name of Company corresponding to the labeler code segment of the ProductNDC. |
| Dosage Form: | Solution |
| The translation of the DosageForm Code submitted by the firm. There is no standard, but values may include terms like `tablet` or `solution for injection`.The complete list of codes and translations can be found www.fda.gov/edrls under Structured Product Labeling Resources. |
| Status: | Active |
| FDA does not review and approve unfinished products. Therefore, all products in this file are considered unapproved. |
| Substance Name: | TRIFLURIDINE - 10 mg/mL
|
| This is the active ingredient list. Each ingredient name is the preferred term of the UNII code submitted. |
| Route Details: | OPHTHALMIC
|
| The translation of the Route Code submitted by the firm, indicating route of administration. The complete list of codes and translations can be found at www.fda.gov/edrls under Structured Product Labeling Resources. |
Marketing Information:
An openfda section: An annotation with additional product identifiers, such as NUII and UPC, of the drug product, if available.
| Marketing Category: | ANDA |
| Product types are broken down into several potential Marketing Categories, such as New Drug Application (NDA), Abbreviated New Drug Application (ANDA), BLA, OTC Monograph, or Unapproved Drug. One and only one Marketing Category may be chosen for a product, not all marketing categories are available to all product types. Currently, only final marketed product categories are included. The complete list of codes and translations can be found at www.fda.gov/edrls under Structured Product Labeling Resources. |
| Marketing Start Date: | 14 May, 2001 |
| This is the date that the labeler indicates was the start of its marketing of the drug product. |
| Marketing End Date: | 29 Dec, 2025 |
| This is the date the product will no longer be available on the market. If a product is no longer being manufactured, in most cases, the FDA recommends firms use the expiration date of the last lot produced as the EndMarketingDate, to reflect the potential for drug product to remain available after manufacturing has ceased. Products that are the subject of ongoing manufacturing will not ordinarily have any EndMarketingDate. Products with a value in the EndMarketingDate will be removed from the NDC Directory when the EndMarketingDate is reached. |
| Application Number: | ANDA074311 |
| This corresponds to the NDA, ANDA, or BLA number reported by the labeler for products which have the corresponding Marketing Category designated. If the designated Marketing Category is OTC Monograph Final or OTC Monograph Not Final, then the Application number will be the CFR citation corresponding to the appropriate Monograph (e.g. “part 341”). For unapproved drugs, this field will be null. |
| Listing Expiration Date: | 31 Dec, 2023 |
| This is the date when the listing record will expire if not updated or certified by the firm. |
OpenFDA Information:
An openfda section: An annotation with additional product identifiers, such as NUII and UPC, of the drug product, if available.
| Manufacturer Name: | Sandoz Inc
|
| Name of manufacturer or company that makes this drug product, corresponding to the labeler code segment of the NDC. |
| RxCUI: | 313477
|
| The RxNorm Concept Unique Identifier. RxCUI is a unique number that describes a semantic concept about the drug product, including its ingredients, strength, and dose forms. |
| Original Packager: | Yes
|
| Whether or not the drug has been repackaged for distribution. |
| UPC: | 0361314044754
|
| UPC stands for Universal Product Code. |
| NUI: | N0000175459
N0000175466
N0000175595
N0000000233
|
| Unique identifier applied to a drug concept within the National Drug File Reference Terminology (NDF-RT). |
| UNII: | RMW9V5RW38
|
| Unique Ingredient Identifier, which is a non-proprietary, free, unique, unambiguous, non-semantic, alphanumeric identifier based on a substance’s molecular structure and/or descriptive information. |
| Pharmacologic Class MOA: | Nucleic Acid Synthesis Inhibitors [MoA]
|
| Mechanism of action of the drug—molecular, subcellular, or cellular functional activity—of the drug’s established pharmacologic class. Takes the form of the mechanism of action, followed by `[MoA]` (such as `Calcium Channel Antagonists [MoA]` or `Tumor Necrosis Factor Receptor Blocking Activity [MoA]`. |
| Pharmacologic Class EPC: | Nucleoside Analog Antiviral [EPC]
Nucleoside Metabolic Inhibitor [EPC]
|
| Established pharmacologic class associated with an approved indication of an active moiety (generic drug) that the FDA has determined to be scientifically valid and clinically meaningful. Takes the form of the pharmacologic class, followed by `[EPC]` (such as `Thiazide Diuretic [EPC]` or `Tumor Necrosis Factor Blocker [EPC]`. |
| Pharmacologic Class: | Nucleic Acid Synthesis Inhibitors [MoA]
Nucleoside Analog Antiviral [EPC]
Nucleoside Analog [EXT]
Nucleoside Metabolic Inhibitor [EPC]
|
| These are the reported pharmacological class categories corresponding to the SubstanceNames listed above. |
Packaging Information:
| Package NDC | Description | Marketing Start Date | Marketing End Date | Sample Available |
|---|
| 61314-044-75 | 7.5 mL in 1 BOTTLE, PLASTIC (61314-044-75) | 14 May, 2001 | N/A | No |
| Package NDC number, known as the NDC, identifies the labeler, product, and trade package size. The first segment, the labeler code, is assigned by the FDA. Description tells the size and type of packaging in sentence form. Multilevel packages will have the descriptions concatenated together. |
Product Elements:
Trifluridine trifluridine trifluridine trifluridine acetic acid sodium acetate sodium chloride thimerosal
Indications and Usage:
Indications and usage: trifluridine ophthalmic solution is indicated for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2.
Warnings:
Warnings: the recommended dosage and frequency of administration should not be exceeded (see dosage and administration ).
Dosage and Administration:
Dosage and administration: instill one drop of trifluridine ophthalmic solution onto the cornea of the affected eye every 2 hours while awake for a maximum daily dosage of nine drops until the cornea ulcer has completely re-epithelialized. following re-epithelialization, treatment for an additional 7 days of one drop every 4 hours while awake for a minimum daily dosage of five drops is recommended. if there are no signs of improvement after 7 days of therapy or complete re-epithelialization has not occurred after 14 days of therapy, other forms of therapy should be considered. continuous administration of trifluridine for periods exceeding 21 days should be avoided because of potential ocular toxicity.
Contraindications:
Contraindications: trifluridine ophthalmic solution is contraindicated for patients who develop hypersensitivity reactions or chemical intolerance to trifluridine.
Adverse Reactions:
Adverse reactions: the most frequent adverse reactions reported during controlled clinical trials were mild, transient burning or stinging upon instillation (4.6%) and palpebral edema (2.8%). other adverse reactions in decreasing order of reported frequency were superficial punctate keratopathy, epithelial keratopathy, hypersensitivity reaction, stromal edema, irritation, keratitis sicca, hyperemia, and increased intraocular pressure.
Use in Pregnancy:
Pregnancy: teratogenic effects: pregnancy category c: trifluridine was not teratogenic at doses up to 5 mg/kg/day (23 times the estimated human exposure) when given subcutaneously to rats and rabbits. however, fetal toxicity consisting of delayed ossification of portions of the skeleton occurred at dose levels of 2.5 and 5 mg /kg /day in rats and at 2.5 mg/kg/day in rabbits. in addition, both 2.5 and 5 mg/kg/day produced fetal death and resorption in rabbits. in both rats and rabbits, 1 mg/kg/day (5 times the estimated human exposure) was a no-effect level. there were no teratogenic or fetotoxic effects after topical application of trifluridine (approximately 5 times the estimated human exposure) to the eyes of rabbits on the 6th through the 18th days of pregnancy. in a non-standard test, trifluridine solution has been shown to be teratogenic when injected directly into the yolk sac of chicken eggs. there are no adequate and well-controlled studies in pregnant women. trifluridine ophth
Read more...almic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Pediatric Use:
Pediatric use: safety and effectiveness in pediatric patients below six years of age have not been established.
Geriatric Use:
Geriatric use: no overall differences in safety or effectiveness have been observed between elderly and younger patients.
Overdosage:
Overdosage: overdosage by ocular instillation is unlikely because any excess solution should be quickly expelled from the conjunctival sac. acute overdosage by accidental oral ingestion of trifluridine has not occurred. however, should such ingestion occur, the 75 mg dosage of trifluridine in a 7.5 ml bottle of trifluridine ophthalmic solution is not likely to produce adverse effects. single intravenous doses of 1.5 to 30 mg/kg/day in children and adults with neoplastic disease produce reversible bone marrow depression as the only potentially serious toxic effect and only after three to five courses of therapy. the acute oral ld 50 in the mouse and rat was 4379 mg/kg or higher.
Description:
Description: trifluridine ophthalmic solution (also known as trifluorothymidine, f 3 tdr, f 3 t), an antiviral drug for topical treatment of epithelial keratitis caused by herpes simplex virus. the chemical name of trifluridine is α,α,α-trifluorothymidine. trifluridine has the following structural formula. trifluridine sterile ophthalmic solution contains 1% trifluridine in an aqueous solution with acetic acid and sodium acetate (buffers), sodium chloride, and thimerosal 0.001% (added as a preservative). the ph range is 5.5 to 6.0 and osmolality is approximately 283 mosm. chemical
Clinical Pharmacology:
Clinical pharmacology: trifluridine is a fluorinated pyrimidine nucleoside with in vitro and in vivo activity against herpes simplex virus, types 1 and 2 and vacciniavirus. some strains of adenovirus are also inhibited in vitro . trifluridine is also effective in the treatment of epithelial keratitis that has not responded clinically to the topical administration of idoxuridine or when ocular toxicity or hypersensitivity to idoxuridine has occurred. in a smaller number of patients found to be resistant to topical vidarabine, trifluridine was also effective. trifluridine interferes with dna synthesis in cultured mammalian cells. however, its antiviral mechanism of action is not completely known. in vitro perfusion studies on excised rabbit corneas have shown that trifluridine penetrates the intact cornea as evidenced by recovery of parental drug and its major metabolite, 5-carboxy-2´-deoxyuridine, on the endothelial side of the cornea. absence of the corneal epithelium enhances the p
Read more...enetration of trifluridine approximately two-fold. intraocular penetration of trifluridine occurs after topical instillation of trifluridine into human eyes. decreased corneal integrity or stromal or uveal inflammation may enhance the penetration of trifluridine into the aqueous humor. unlike the results of ocular penetration of trifluridine in vitro , 5-carboxy-2´-deoxyuridine was not found in detectable concentrations within the aqueous humor of the human eye. systemic absorption of trifluridine following therapeutic dosing with trifluridine appears to be negligible. no detectable concentrations of trifluridine or 5-carboxy-2´-deoxyuridine were found in the sera of adult healthy normal subjects who had trifluridine instilled into their eyes seven times daily for 14 consecutive days. clinical studies: during a controlled multicenter clinical trial, 92 of 97 (95%) patients (78 of 81 with dendritic and 14 of 16 with geographic ulcers) responded to therapy with trifluridine as evidenced by complete corneal re-epithelialization within the 14-day therapy period. fifty-six of 75 (75%) patients (49 of 58 with dendritic and 7 of 17 with geographic ulcers) responded to idoxuridine therapy. the mean time to corneal re-epithelialization for dendritic ulcers (6 days) and geographic ulcers (7 days) was similar for both therapies. in other clinical studies, trifluridine was evaluated in the treatment of herpes simplex virus keratitis in patients who were unresponsive or intolerant to the topical administration of idoxuridine or vidarabine. trifluridine was effective in 138 of 150 (92%) patients (109 of 114 with dendritic and 29 of 36 with geographic ulcers) as evidenced by corneal re-epithelialization. the mean time to corneal re-epithelialization was 6 days for patients with dendritic ulcers and 12 days for patients with geographic ulcers. the clinical efficacy of trifluridine in the treatment of stromal keratitis and uveitis due to herpes simplex virus or ophthalmic infections caused by vacciniavirus and adenovirus has not been established by well-controlled clinical trials. trifluridine has not been shown to be effective in the prophylaxis of herpes simplex virus keratoconjunctivitis and epithelial keratitis by well-controlled clinical trials. trifluridine is not effective against bacterial, fungal or chlamydial infections of the cornea or nonviral trophic lesions.
Carcinogenesis and Mutagenesis and Impairment of Fertility:
Carcinogenesis, mutagenesis, impairment of fertility: mutagenic potential: trifluridine has been shown to exert mutagenic, dna-damaging and cell-transforming activities in various standard in vitro test systems, and clastogenic activity in vicia faba cells. it did not induce chromosome aberrations in bone marrow cells of male or female rats following a single subcutaneous dose of 100 mg/kg, but was weakly positive in female, but not in male, rats following daily subcutaneous administration at 700mg/kg/day for 5 days. although the significance of these test results is not clear or fully understood, there exists the possibility that mutagenic agents may cause genetic damage in humans. oncogenic potential: lifetime carcinogenicity bioassays in rats and mice given daily subcutaneous doses of trifluridine have been performed. rats tested at 1.5, 7.5, and 15 mg/kg/day had increased incidences of adenocarcinomas of the intestinal tract and mammary glands, hemangiosarcomas of the spleen and li
Read more...ver, carcinosarcomas of the prostate gland and granulosathecal cell tumors of the ovary. mice were tested at 1, 5 and 10 mg/kg/day; those given 10mg/kg/day trifluridine had significantly increased incidences of adenocarcinomas of the intestinal tract and uterus. those given 10 mg/kg/day also had a significantly increased incidence of testicular atrophy as compared to vehicle control mice.
How Supplied:
How supplied: trifluridine ophthalmic solution, 1% in a 7.5 ml fill packaged in a natural plastic bottle with a natural plastic flat tip and a white plastic closure. 7.5ml- ndc 61314-044-75 store under refrigeration 2-8°c (36-46°f).
Package Label Principal Display Panel:
Principal display panel ndc 61314-044-75 trifluridine ophthalmic solution 1% 7.5 ml sterile sandoz inc. carton