entacapone (Rx)

Brand and Other Names:Comtan
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 200mg

Parkinson Disease

200 mg PO with each dose of levodopa/carbidopa

Not to exceed 1600 mg/day

See also combo with levodopa/carbidopa

Renal Impairment

Dose adjustment not necessary

Hepatic Impairment

Safety and efficacy not established

Not recommended

Parkinson disease

200 mg PO with each dose of levodopa/carbidopa

Not to exceed 1600 mg/day

See also combo with levodopa/carbidopa

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Interactions

Interaction Checker

and entacapone

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      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (4)

            • isocarboxazid

              entacapone, isocarboxazid. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Both nonselective MAO inhibitors and entacapone inhibit catecholamine metabolism, leading to increased levels of catecholamines. Potential for dangerously high HR or BP.

            • lonafarnib

              entacapone will increase the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lonafarnib is a sensitive CYP3A4 substrate. Coadministration with strong or moderate CYP3A4 inhibitors is contraindicated.

            • phenelzine

              entacapone, phenelzine. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Both nonselective MAO inhibitors and entacapone inhibit catecholamine metabolism, leading to increased levels of catecholamines. Potential for dangerously high HR or BP.

            • tranylcypromine

              entacapone, tranylcypromine. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Both nonselective MAO inhibitors and entacapone inhibit catecholamine metabolism, leading to increased levels of catecholamines. Potential for dangerously high HR or BP.

            Serious - Use Alternative (3)

            • infigratinib

              entacapone will increase the level or effect of infigratinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • lurbinectedin

              entacapone will increase the level or effect of lurbinectedin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • metoclopramide intranasal

              entacapone, 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.

            Monitor Closely (13)

            • dobutamine

              entacapone will increase the level or effect of dobutamine by decreasing metabolism. Use Caution/Monitor. Entacapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • dopamine

              entacapone will increase the level or effect of dopamine by decreasing metabolism. Use Caution/Monitor. Entacapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • epinephrine

              entacapone will increase the level or effect of epinephrine by decreasing metabolism. Use Caution/Monitor. Entacapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • epinephrine inhaled

              entacapone will increase the level or effect of epinephrine inhaled by decreasing metabolism. Use Caution/Monitor. Entacapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • epinephrine racemic

              entacapone will increase the level or effect of epinephrine racemic by decreasing metabolism. Use Caution/Monitor. Entacapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • finerenone

              entacapone will increase the level or effect of finerenone by affecting hepatic enzyme CYP2E1 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or moderate CYP3A4 inhibitors. Adjust finererone dosage as needed.

              entacapone will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or weak CYP3A4 inhibitors. Adjust finererone dosage as needed.

            • isavuconazonium sulfate

              entacapone will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • isoproterenol

              entacapone will increase the level or effect of isoproterenol by decreasing metabolism. Use Caution/Monitor. Entacapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • lefamulin

              entacapone will increase the level or effect of lefamulin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor for adverse effects if lefamulin is coadministered with moderate CYP3A inhibitors.

            • methyldopa

              entacapone will increase the level or effect of methyldopa by decreasing metabolism. Use Caution/Monitor. Entacapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • norepinephrine

              entacapone will increase the level or effect of norepinephrine by decreasing metabolism. Use Caution/Monitor. Entacapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • oliceridine

              entacapone will increase the level or effect of oliceridine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If concomitant use is necessary, may require less frequent oliceridine dosing. Closely monitor for respiratory depression and sedation and titrate subsequent doses accordingly. If inhibitor is discontinued, consider increase oliceridine dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal.

            • voclosporin

              entacapone will increase the level or effect of voclosporin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce voclosporin daily dosage to 15.8 mg PO in AM and 7.9 mg PO in PM.

            Minor (0)

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              Adverse Effects

              >10%

              Dyskinesia (25%)

              Nausea (14%)

              Diarrhea (10%)

              Hyperkinesia (10%)

              Urine discoloration (10%)

              1-10%

              Hypokinesia (9%)

              Dizziness (8%)

              Abdominal pain (8%)

              Fatigue (6%)

              Constipation (6%)

              Back pain (4%)

              Vomiting (4%)

              Dry mouth (3%)

              Dyspnea (3%)

              Increased sweating (2%)

              Back pain (2%)

              Anxiety (2%)

              Somnolence (2%)

              Dyspepsia (2%)

              Flatulence (2%)

              Purpura (2%)

              Asthenia (2%)

              Hallucinations (1-4%)

              Taste perversion (1%)

              Agitation (1%)

              Gastritis (1%)

              Bacterial infection (1%)

              Frequency Not Defined

              Insomnia

              Postural hypotension

              Confusion

              Dopaminergic side affects due to increased dopamine levels

              Rare: rhabdomyolysis, retroperitoneal fibrosis

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              Warnings

              Contraindications

              Hypersensitivity

              Cautions

              Use only in combo with levodopa/carbidopa

              Increases plasma levodopa levels, which may result in suddenly falling asleep without prior warning of sleepiness while engaged in activities of daily living; adjust levodopa dose

              Less hepatotoxic than tolcapone

              May be linked to higher melanoma risk in patients with Parkinson Disease

              Diarrhea may occur and be associated with weight loss, dehydration, and hypokalemia; if severe, may be a sign of drug-induced microscopic colitis

              Dyskinesia incidence 25% compared with 15% for placebo

              Dopaminergic therapy in patients with Parkinson disease has been associated with hypotension, orthostatic hypotension, syncope, increased heart rates, possible arrhythmias, and excessive changes in blood pressure

              Hallucinations and psychotic-like behavior reported with dopaminergic therapy

              Rhabdomyolysis, hyperpyrexia, and confusion reported

              Impulse control/compulsive behaviors: Risk of uncontrollable sexual, gambling or other urges

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              Pregnancy & Lactation

              Pregnancy Category: C

              Lactation: excretion in milk unknown; use with 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

              Reversible catechol-O-methyltransferase (COMT) inhibitor that prolongs half life of levodopa in Parkinsonian patients, reducing motor fluctuations

              Pharmacokinetics

              Peak Plasma Time: 1 hr

              Concentration: 1.2 mcg/mL

              Excretion: Feces (90); urine (10%)

              Bioavailability: 35%

              Protein Bound: 98%

              Vd: 20 L

              Half-life elimination: 0.4-0.7 hr (B-phase); 2.4 hr (Y-phase)

              Metabolism: Hepatic glucuronidation

              Total body clearance: 850 mL/min

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              Comtan oral
              -
              200 mg tablet
              entacapone oral
              -
              200 mg tablet
              entacapone oral
              -
              200 mg tablet
              entacapone oral
              -
              200 mg tablet
              entacapone oral
              -
              200 mg tablet
              entacapone oral
              -
              200 mg tablet
              entacapone oral
              -
              200 mg tablet
              entacapone oral
              -
              200 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              entacapone oral

              ENTACAPONE - ORAL

              (en-TACK-up-own)

              COMMON BRAND NAME(S): Comtan

              USES: This medication is used with other medications (levodopa/carbidopa) to treat Parkinson's disease. Entacapone belongs to a class of drugs known as COMT inhibitors. Many people taking levodopa for Parkinson's have problems with the effects of the levodopa wearing off between scheduled doses, causing symptoms to return or worsen. Entacapone blocks a certain natural substance (COMT enzyme) that breaks down the levodopa in the body. This effect allows the levodopa to last longer in the system so that it doesn't wear off before the next dose.

              HOW TO USE: Take this medication by mouth with or without food, usually with each prescribed dose of levodopa/carbidopa (up to 8 times daily) or as directed by your doctor.Dosage is based on your medical condition, liver function, and response to therapy.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 suddenly stop taking this medication unless instructed to do so by your doctor. Doing so may cause your Parkinson's symptoms to become much worse.Tell your doctor if your condition persists or worsens (such as your Parkinson's symptoms are not controlled).

              SIDE EFFECTS: Nausea, vomiting, diarrhea, unwanted/uncontrolled movements, increased sweating, drowsiness, tiredness, dry mouth, gas, and abdominal pain may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Lightheadedness or dizziness upon standing may also occur, especially during the first few weeks of treatment. To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.Many people using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.Some people taking entacapone have fallen asleep suddenly during their usual daily activities (such as talking on the phone, driving). In some cases, sleep occurred without any feelings of drowsiness beforehand. This sleep effect may occur anytime during treatment with entacapone even if you have used this medication for a long time. If you experience increased sleepiness or fall asleep during the day, do not drive or take part in other possibly dangerous activities until you have discussed this effect with your doctor. Your risk of this sleep effect is increased by using alcohol or other medications that can make you drowsy. See also Precautions section.Your urine may turn brownish-orange. This effect is harmless.Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as confusion, hallucinations), unusual strong urges (such as increased gambling, increased sexual urges), fever, muscle stiffness, persistent diarrhea, easy bleeding/bruising, sore/painful muscles, muscle weakness, trouble breathing, pain with breathing.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 entacapone, 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: alcoholism, liver problems, low blood pressure, mental/mood disorders (such as depression, schizophrenia), sleep disorders.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. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis). See also Side Effects section.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this drug, especially drowsiness and confusion.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if 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 of the products that may interact with this drug include: certain MAO inhibitors (isocarboxazid, linezolid, metaxalone, methylene blue, moclobemide, phenelzine, procarbazine, tranylcypromine).Other MAO inhibitors (safinamide, selegiline, rasagiline) may be used cautiously with close monitoring by your doctor. If you are taking rasagiline or selegiline for Parkinson's disease, ask your doctor if you should continue taking it.Entacapone can slow down the removal of other drugs from your body, thereby affecting how they work. These affected drugs include apomorphine, dobutamine, and methyldopa. This is not a complete list.Tell your doctor or pharmacist if you are taking other products that cause drowsiness including alcohol, marijuana (cannabis), antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, and opioid pain relievers (such as codeine).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.

              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. Symptoms of overdose may include severe drowsiness, coma, confusion, agitation.

              NOTES: Do not share this medication with others.Laboratory and/or medical tests (such as liver function tests) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.Keep all medical and lab test appointments.People with Parkinson's disease may have an increased risk for developing skin cancer (melanoma). Tell your doctor promptly if you notice a change in the appearance or size of moles or other unusual skin changes. Ask your doctor if you should have regular skin exams.

              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 medicines 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 September 2021. Copyright(c) 2021 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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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.