metyrosine (Rx)

Brand and Other Names:Demser

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 250mg

Chronic Pheochromocytoma

Indicated for treatment of patients with pheochromocytoma for: 1) preoperative preparation for surgery; 2) management when surgery is contraindicated; and 3) chronic treatment with malignant pheochromocytoma

Initial: 250 mg PO q6hr; may increase by 250-500 mg/day, not to exceed 4 g/day

Maintenance: Typically 2-3 g/day divided q6hr

Dosing Considerations

Not indicated for essential hypertension

When used for preoperative preparation, the optimally effective dose should be given for at least 5-7 days

Psychosis (Orphan)

Treatment of velocardiofacial syndrome associated psychosis

Orphan indication sponsor

  • Aton Pharma, Inc; 3150 Brunswick Place; Lawrenceville, NJ 08648

Dosage Forms & Strengths

capsule

  • 250mg

Chronic Pheochromocytoma

Indicated for treatment of patients with pheochromocytoma for: 1) preoperative preparation for surgery; 2) management when surgery is contraindicated; and 3) chronic treatment with malignant pheochromocytoma

<12 years: Safety and efficacy not established

≥12 years

  • Initial: 250 mg PO q6hr; may increase by 250-500 mg/day, not to exceed 4 g/day
  • Maintenance: Typically 2-3 g/day divided q6hr

Dosing Considerations

Not indicated for essential hypertension

When used for preoperative preparation, the optimally effective dose should be given for at least 5-7 days

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Interactions

Interaction Checker

and metyrosine

No Results

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (4)

              • lofexidine

                lofexidine, metyrosine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • metoclopramide intranasal

                metyrosine, metoclopramide intranasal. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient.

              • olopatadine intranasal

                metyrosine and olopatadine intranasal both increase sedation. Avoid or Use Alternate Drug. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.

              • ropeginterferon alfa 2b

                ropeginterferon alfa 2b and metyrosine both increase Other (see comment). Avoid or Use Alternate Drug. Narcotics, hypnotics or sedatives can produce additive neuropsychiatric side effects. Avoid use and monitor patients receiving the combination for effects of excessive CNS toxicity.

              Monitor Closely (7)

              • carbidopa

                carbidopa increases effects of metyrosine by pharmacodynamic synergism. Use Caution/Monitor. Monitor for hypotension.

              • clonidine

                clonidine, metyrosine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.

              • daridorexant

                metyrosine and daridorexant both increase sedation. Modify Therapy/Monitor Closely. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.

              • difelikefalin

                difelikefalin and metyrosine both increase sedation. Use Caution/Monitor.

              • midazolam intranasal

                midazolam intranasal, metyrosine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Concomitant use of barbiturates, alcohol, or other CNS depressants may increase the risk of hypoventilation, airway obstruction, desaturation, or apnea and may contribute to profound and/or prolonged drug effect.

              • stiripentol

                stiripentol, metyrosine. Either increases effects of the other by sedation. Use Caution/Monitor. Concomitant use stiripentol with other CNS depressants, including alcohol, may increase the risk of sedation and somnolence.

              • xipamide

                xipamide increases effects of metyrosine by pharmacodynamic synergism. Use Caution/Monitor.

              Minor (18)

              • agrimony

                agrimony increases effects of metyrosine by pharmacodynamic synergism. Minor/Significance Unknown.

              • brimonidine

                brimonidine increases effects of metyrosine by pharmacodynamic synergism. Minor/Significance Unknown.

              • chlorpromazine

                metyrosine increases toxicity of chlorpromazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased extrapyramidal symptoms.

              • cornsilk

                cornsilk increases effects of metyrosine by pharmacodynamic synergism. Minor/Significance Unknown.

              • fluphenazine

                metyrosine increases toxicity of fluphenazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased extrapyramidal symptoms.

              • forskolin

                forskolin increases effects of metyrosine by pharmacodynamic synergism. Minor/Significance Unknown.

              • haloperidol

                metyrosine increases effects of haloperidol by pharmacodynamic synergism. Minor/Significance Unknown.

              • maitake

                maitake increases effects of metyrosine by pharmacodynamic synergism. Minor/Significance Unknown.

              • octacosanol

                octacosanol increases effects of metyrosine by pharmacodynamic synergism. Minor/Significance Unknown.

              • perphenazine

                metyrosine increases toxicity of perphenazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased extrapyramidal symptoms.

              • prochlorperazine

                metyrosine increases toxicity of prochlorperazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased extrapyramidal symptoms.

              • promazine

                metyrosine increases toxicity of promazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased extrapyramidal symptoms.

              • promethazine

                metyrosine increases toxicity of promethazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased extrapyramidal symptoms.

              • reishi

                reishi increases effects of metyrosine by pharmacodynamic synergism. Minor/Significance Unknown.

              • shepherd's purse

                shepherd's purse, metyrosine. Other (see comment). Minor/Significance Unknown. Comment: Theoretically, shepherd's purse may interfere with BP control.

              • thioridazine

                metyrosine increases toxicity of thioridazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased extrapyramidal symptoms.

              • tizanidine

                tizanidine increases effects of metyrosine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of hypotension.

              • trifluoperazine

                metyrosine increases toxicity of trifluoperazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased extrapyramidal symptoms.

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              Adverse Effects

              >10%

              Sedation (>20%)

              1-10%

              Diarrhea (10%)

              Exrapyramidal Symptoms (10%)

              Frequency Not Defined

              Fatigue

              Headache

              Psychic Disturbances

              Galactorrhea

              Sexual dysfunction

              Nausea

              Vomiting

              Xerostomia

              Nasal stuffiness

              Dysuria

              Crystalluria

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              Warnings

              Contraindications

              Hypersensitivity to metyrosine

              Cautions

              Additive sedative effects w/ alcohol and other CNS depressants

              Take enough fluid to prevent crystalluria

              Use caution in hepatic or renal impairment

              Not recommended for essential HTN

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              Pregnancy & Lactation

              Pregnancy Category: C

              Lactation: not known if excreted into breast milk, use caution

              Pregnancy Categories

              A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

              B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

              C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

              D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

              X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

              NA: Information not available.

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              Pharmacology

              Mechanism of Action

              Inhibits synthesis of endogenous catecholamines by inhibiting tyrosine hydroxylase

              Pharmacokinetics

              Half-Life: 3-4 hr

              Bioavailability: Well absorbed

              Metabolism: liver

              Metabolite: Catechol metabolites (inactive)

              Excretion: urine 53-88%

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              Demser oral
              -
              250 mg capsule
              Demser oral
              -
              250 mg capsule

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              metyrosine oral

              METYROSINE - ORAL

              (me-TYE-roe-seen)

              COMMON BRAND NAME(S): Demser

              USES: This medication is used to treat high blood pressure in people with a certain adrenal gland tumor (pheochromocytoma). Metyrosine is used to prevent high blood pressure before and immediately after surgery to remove the tumor. It is also used long-term in people who cannot have the surgery. It is not used for other kinds of high blood pressure.Metyrosine prevents the tumor from making certain natural substances (catecholamines) that raise the blood pressure and make the heart beat faster. Lowering the amount of catecholamines lessens the risk of a very serious attack of high blood pressure (hypertensive crisis).

              HOW TO USE: Take this medication by mouth with or without food as directed by your doctor, usually 4 times a day. The dosage is based on your medical condition and response to treatment.Your doctor may direct you to start taking this drug at a low dose and slowly increase your dose until you are taking the best dose for you. Your doctor will check your blood pressure and order lab tests (such as urine tests for catecholamines) to find the best dose.During treatment with this medication, it is important that you get plenty of fluids and pass urine frequently to help avoid kidney and bladder side effects. Ask your doctor how much fluid you should drink and how often you should urinate each day, and follow these instructions carefully.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day. Do not stop taking this medication without consulting your doctor. Keep taking this medication even if you feel well. Most people with high blood pressure do not feel sick. You may have trouble sleeping (insomnia) for 2 to 3 days after you stop taking this medication. Tell your doctor if these symptoms last or get worse or if you have other symptoms of very high blood pressure (such as headache, nausea, sweating, fast heartbeat).This medication is usually taken for at least 5 to 7 days before surgery.Tell your doctor if your condition does not improve or if it worsens (for example, if you have headache, nausea, sweating, fast heartbeat, high blood pressure readings).

              SIDE EFFECTS: Drowsiness, tiredness, dizziness, lightheadedness, dry mouth, and diarrhea may occur as your body adjusts to the medication. If any of these effects last or get worse, tell your doctor or pharmacist promptly.To lower your risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: difficulty speaking, drooling, unwanted/uncontrolled movements, muscle stiffness, shaking (tremor), decrease in sexual ability, tenderness/swelling of the breast, mental/mood changes (such as confusion, depression, severe anxiety), signs of kidney problems (such as change in the amount of urine, painful urination, pink/bloody urine).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Before taking metyrosine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, liver disease, dehydration.Before having surgery, tell your doctor or dentist that you are taking this medication.This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis). Alcohol may also cause you to become dehydrated.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

              DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug are: anti-psychotic medication (such as haloperidol, thiothixene), certain drugs (phenothiazines) used to treat mental/mood conditions or nausea (such as chlorpromazine, prochlorperazine).Tell your doctor or pharmacist if you are taking other products that cause drowsiness such as opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana (cannabis), drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine).Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.Some products have ingredients that could raise your blood pressure. Tell your pharmacist what products you are using, and ask how to use them safely (especially cough-and-cold products, diet aids, or NSAIDs such as ibuprofen/naproxen).

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

              NOTES: Do not share this medication with others.Lab and/or medical tests (such as blood pressure, EKG, urine catecholamine tests) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.Have your blood pressure checked regularly while taking this medication. Learn how to monitor your own blood pressure at home, and share the results with your doctor.

              MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

              STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

              Information last revised December 2022. Copyright(c) 2023 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Formulary

              FormularyPatient Discounts

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              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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              NC NOT COVERED – Drugs that are not covered by the plan.
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              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.