Demser
Metyrosine
Bausch Health Us, Llc
Human Prescription Drug
NDC 25010-305Demser also known as Metyrosine is a human prescription drug labeled by 'Bausch Health Us, Llc'. National Drug Code (NDC) number for Demser is 25010-305. This drug is available in dosage form of Capsule. The names of the active, medicinal ingredients in Demser drug includes Metyrosine - 250 mg/1 . The currest status of Demser drug is Active.
Drug Information:
| Drug NDC: | 25010-305 |
| 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: | Demser |
| 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: | Metyrosine |
| Also known as the generic name, this is usually the active ingredient(s) of the product. |
| Labeler Name: | Bausch Health Us, Llc |
| Name of Company corresponding to the labeler code segment of the ProductNDC. |
| Dosage Form: | Capsule |
| 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: | METYROSINE - 250 mg/1
|
| This is the active ingredient list. Each ingredient name is the preferred term of the UNII code submitted. |
| Route Details: | ORAL
|
| 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: | NDA |
| 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: | 03 Oct, 1979 |
| This is the date that the labeler indicates was the start of its marketing of the drug product. |
| Marketing End Date: | 14 Jan, 2026 |
| 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: | NDA017871 |
| 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: | Bausch Health US, LLC
|
| Name of manufacturer or company that makes this drug product, corresponding to the labeler code segment of the NDC. |
| RxCUI: | 197980
201388
|
| 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. |
| NUI: | N0000175569
N0000175361
|
| Unique identifier applied to a drug concept within the National Drug File Reference Terminology (NDF-RT). |
| UNII: | DOQ0J0TPF7
|
| 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: | Catecholamine 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: | Catecholamine Synthesis 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: | Catecholamine Synthesis Inhibitor [EPC]
Catecholamine Synthesis Inhibitors [MoA]
|
| 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 |
|---|
| 25010-305-15 | 100 CAPSULE in 1 BOTTLE (25010-305-15) | 03 Oct, 1979 | 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:
Demser metyrosine metyrosine metyrosine silicon dioxide fd&c blue no. 2 magnesium stearate titanium dioxide gelatin, unspecified hydroxypropyl cellulose, unspecified two-toned blue aton;305;demser
Indications and Usage:
Indications and usage demser is indicated in the treatment of patients with pheochromocytoma for: 1. preoperative preparation of patients for surgery 2. management of patients when surgery is contraindicated 3. chronic treatment of patients with malignant pheochromocytoma demser is not recommended for the control of essential hypertension.
Warnings:
Warnings maintain fluid volume during and after surgery when demser is used preoperatively, alone or especially in combination with alpha-adrenergic blocking drugs, adequate intravascular volume must be maintained intraoperatively (especially after tumor removal) and postoperatively to avoid hypotension and decreased perfusion of vital organs resulting from vasodilatation and expanded volume capacity. following tumor removal, large volumes of plasma may be needed to maintain blood pressure and central venous pressure within the normal range. in addition, life-threatening arrhythmias may occur during anesthesia and surgery, and may require treatment with a beta-blocker or lidocaine. during surgery, patients should have continuous monitoring of blood pressure and electrocardiogram. intraoperative effects while the preoperative use of demser in patients with pheochromocytoma is thought to decrease intraoperative problems with blood pressure control, demser does not eliminate the danger of
Read more... hypertensive crises or arrhythmias during manipulation of the tumor, and the alpha-adrenergic blocking drug, phentolamine, may be needed. interaction with alcohol demser may add to the sedative effects of alcohol and other cns depressants, e.g., hypnotics, sedatives, and tranquilizers. (see precautions, information for patients and drug interactions . )
Dosage and Administration:
Dosage and administration the recommended initial dosage of demser for adults and children 12 years of age and older is 250 mg orally four times daily. this may be increased by 250 mg to 500 mg every day to a maximum of 4 g/day in divided doses. when used for preoperative preparation, the optimally effective dosage of demser should be given for at least five to seven days. optimally effective dosages of demser usually are between 2 and 3 g/day, and the dose should be titrated by monitoring clinical symptoms and catecholamine excretion. in patients who are hypertensive, dosage should be titrated to achieve normalization of blood pressure and control of clinical symptoms. in patients who are usually normotensive, dosage should be titrated to the amount that will reduce urinary metanephrines and/or vanillylmandelic acid by 50% or more. if patients are not adequately controlled by the use of demser, an alpha-adrenergic blocking agent (phenoxybenzamine) should be added. use of demser in chi
Read more...ldren under 12 years of age has been limited and a dosage schedule for this age group cannot be given.
Contraindications:
Contraindications demser is contraindicated in persons known to be hypersensitive to this compound.
Adverse Reactions:
Adverse reactions central nervous system sedation: the most common adverse reaction to demser is moderate to severe sedation, which has been observed in almost all patients. it occurs at both low and high dosages. sedative effects begin within the first 24 hours of therapy, are maximal after two to three days, and tend to wane during the next few days. sedation usually is not obvious after one week unless the dosage is increased, but at dosages greater than 2000 mg/day some degree of sedation or fatigue may persist. in most patients who experience sedation, temporary changes in sleep pattern occur following withdrawal of the drug. changes consist of insomnia that may last for two or three days and feelings of increased alertness and ambition. even patients who do not experience sedation while on demser may report symptoms of psychic stimulation when the drug is discontinued. extrapyramidal signs: extrapyramidal signs such as drooling, speech difficulty, and tremor have been reported in
Read more... approximately 10% of patients. these occasionally have been accompanied by trismus and frank parkinsonism. anxiety and psychic disturbances: anxiety and psychic disturbances such as depression, hallucinations, disorientation, and confusion may occur. these effects seem to be dose-dependent and may disappear with reduction of dosage. diarrhea diarrhea occurs in about 10% of patients and may be severe. anti-diarrheal agents may be required if continuation of demser is necessary. miscellaneous infrequently, slight swelling of the breast, galactorrhea, nasal stuffiness, decreased salivation, dry mouth, headache, nausea, vomiting, abdominal pain, and impotence or failure of ejaculation may occur. crystalluria (see precautions ) and transient dysuria and hematuria have been observed in a few patients. hematologic disorders (including eosinophilia, anemia, thrombocytopenia, and thrombocytosis), increased sgot levels, peripheral edema, and hypersensitivity reactions such as urticaria and pharyngeal edema have been reported rarely. to report suspected adverse reactions, contact bausch health us, llc at 1-800-321-4576 or fda at 1-800-fda-1088 or www.fda.gov/medwatch.
Overdosage:
Overdosage signs of metyrosine overdosage include those central nervous system effects observed in some patients even at low dosages. at doses exceeding 2000 mg/day, some degree of sedation or feeling of fatigue may persist. doses of 2000-4000 mg/day can result in anxiety or agitated depression, neuromuscular effects (including fine tremor of the hands, gross tremor of the trunk, tightening of the jaw with trismus), diarrhea, and decreased salivation with dry mouth. reduction of drug dose or cessation of treatment results in the disappearance of these symptoms. the acute toxicity of metyrosine was 442 mg/kg and 752 mg/kg in the female mouse and rat, respectively.
Description:
Description demser (metyrosine) is (â)-α-methyl- l -tyrosine or (α-mpt). it has the following structural formula: metyrosine is a white to off-white, crystalline compound of molecular weight 195.22. it is very slightly soluble in water, acetone, and methanol, and insoluble in chloroform and benzene. it is soluble in acidic aqueous solutions. it is also soluble in alkaline aqueous solutions, but is subject to oxidative degradation under these conditions. demser is supplied as capsules for oral administration. each capsule contains 250 mg metyrosine. inactive ingredients are colloidal silicon dioxide, gelatin, hydroxypropyl cellulose, magnesium stearate, titanium dioxide, fd&c blue 2 and edible black ink. image
Clinical Pharmacology:
Clinical pharmacology demser inhibits tyrosine hydroxylase, which catalyzes the first transformation in catecholamine biosynthesis, i.e., the conversion of tyrosine to dihydroxyphenylalanine (dopa). because the first step is also the rate-limiting step, blockade of tyrosine hydroxylase activity results in decreased endogenous levels of catecholamines, usually measured as decreased urinary excretion of catecholamines and their metabolites. in patients with pheochromocytoma, who produce excessive amounts of norepinephrine and epinephrine, administration of 1 to 4 grams of demser per day has reduced catecholamine biosynthesis from about 35% to 80% as measured by the total excretion of catecholamines and their metabolites (metanephrine and vanillylmandelic acid). the maximum biochemical effect usually occurs within two to three days, and the urinary concentration of catecholamines and their metabolites usually returns to pretreatment levels within three to four days after demser is discont
Read more...inued. in some patients the total excretion of catecholamines and catecholamine metabolites may be lowered to normal or near normal levels (less than 10 mg/24 hours). in most patients, the duration of treatment has been two to eight weeks, but several patients have received demser for periods of 1 to 10 years. most patients with pheochromocytoma treated with demser experience decreased frequency and severity of hypertensive attacks with their associated headache, nausea, sweating, and tachycardia. in patients who respond, blood pressure decreases progressively during the first two days of therapy with demser; after withdrawal, blood pressure usually increases gradually to pretreatment values within two to three days. metyrosine is well absorbed from the gastrointestinal tract. from 53% to 88% (mean 69%) was recovered in the urine as unchanged drug following maintenance oral doses of 600 to 4000 mg/24 hours in patients with pheochromocytoma or essential hypertension. less than 1% of the dose was recovered as catechol metabolites. these metabolites are probably not present in sufficient amounts to contribute to the biochemical effects of metyrosine. the quantities excreted, however, are sufficient to interfere with accurate determination of urinary catecholamines determined by routine techniques. plasma half-life of metyrosine determined over an 8-hour period after single oral doses was 3-3.7 hours in three patients. for further information, refer to: sjoerdsma a, engelman k, waldman ta, cooperman lh, hammond wg. pheochromocytoma: current concepts of diagnosis and treatment: combined clinical staff conference at the national institutes of health. ann intern med. 1966;65:1302-1326.
Package Label Principal Display Panel:
Package/label display panel - 250 mg capsules label ndc 25010-305-15 rx only demser ® (metyrosine) capsules 250 mg 100 capsules each capsule contains 250 mg metyrosine bausch health label