entacapone

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: catechol o methyltransferase comt inhibitors

REMS

Parkinson disease when signs and symptoms of end-of-dose wearing-off (so-called fluctuating patients) occur (in combination with levodopa/carbidopa).

Acts as a selective and reversible inhibitor of the enzyme catechol O-methyltransferase (COMT).
Inhibition of COMT prevents the breakdown of levodopa, increasing availability to the CNS.

Therapeutic effects:

Prolongs duration of response to levodopa with end-of-dose motor fluctuations.
Decreased signs and symptoms of Parkinson disease.

Absorption: 35% absorbed following oral administration; absorption is rapid.

Distribution: Widely distributed to tissues.

Protein Binding: 98%.

Metabolism/Excretion: Minimal amounts excreted unchanged; highly metabolized followed by biliary excretion.

Half-Life: Initial phase: 0.4–0.7 hr; second phase: 2.4 hr.

( inhibition of COMT)

ROUTE		ONSET		PEAK		DURATION
PO		unknown		unknown		up to 8 hr

Contraindicated in:

Hypersensitivity;
Psychotic disorder.

Use Cautiously in:

Hepatic impairment;
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children.

CV: hypotension

Derm: MELANOMA

GI: abdominal pain, colitis, diarrhea, nausea (during initiation), retroperitoneal fibrosis

GU: brownish-orange discoloration of urine

MS: dyskinesia, RHABDOMYOLYSIS

Neuro: aggressive behavior, agitation, confusion, delirium, disorientation, dizziness, hallucinations, NEUROLEPTIC MALIGNANT SYNDROME, paranoid ideation, syncope, urges (gambling, sexual)

Resp: pleural effusion, pleural thickening, pulmonary infiltrates

Drug-drug:

Concurrent use with selective MAO inhibitors is not recommended; both agents inhibit the metabolic pathways of catecholamines.
Drugs that are metabolized by COMT, including isoproterenol, epinephrine, norepinephrine, dopamine, and dobutamine, may ↑ risk of tachycardia, ↑ BP, and arrhythmias.
Probenecid, cholestyramine, erythromycin, rifampin, ampicillin, and chloramphenicol may interfere with biliary elimination of entacapone; use concurrently with caution.

PO (Adults ): 200 mg with each dose of levodopa/carbidopa up to a maximum of 8 times daily.

(Generic available)

Tablets: 200 mg
In combination with:
levodopa/carbidopa (Stalevo); see Combination Drugs.

Assess parkinsonian and extrapyramidal symptoms (restlessness or desire to keep moving, rigidity, tremors, pill rolling, mask-like face, shuffling gait, muscle spasms, twisting motions, difficulty speaking or swallowing, loss of balance control) prior to and during therapy. Dyskinesia may ↑ with therapy.
Monitor for development of diarrhea. Usually occurs within 4–12 wk of start of therapy, but may occur as early as the 1st wk and as late as months after initiation of therapy.
Monitor for signs and symptoms of neuroleptic malignant syndrome (↑ temperature, muscular rigidity, altered consciousness, ↑ CK). Symptoms have been associated with rapid dose ↓ or withdrawal of other dopaminergic drugs. Withdrawal should be gradual.

PO: Always administer entacapone with levodopa/carbidopa. Entacapone has no antiparkinsonism effects of its own.

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy. Instruct to take as directed. Take missed doses as soon as possible, up to 2 hr before the next dose. Taper gradually when discontinuing or a withdrawal reaction may occur.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
May cause dizziness or hallucinations. Advise patient to avoid driving or other activities that require alertness until response to the drug is known.
Inform patient that nausea may occur, especially at initiation of therapy, and diarrhea. Advise patient with diarrhea to drink fluids to maintain adequate hydration and monitor for weight loss. If diarrhea is prolonged, may resolve with discontinuation. Therapy may cause change in urine color to brownish orange.
Caution patient to change positions slowly to minimize orthostatic hypotension.
Advise patient to notify health care professional if suspicious or unusual skin changes; agitation; aggression; delirium; hallucinations; or new or ↑ gambling, sexual, or other intense urges occur.
Emphasize the importance of routine follow-up exams.
Rep: Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Prolongs duration of response to levodopa with end-of-dose motor fluctuations.
Decreased signs and symptoms of Parkinson disease.

NDC Code

0527- Lannett Company, Inc.
- 0527-1830- Entacapone
  - 0527-1830-37- 100 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0527-1830-37)

0615- NCS HealthCare of KY, LLC dba Vangard Labs
- 0615-8298- Entacapone
  - 0615-8298-39- 30 TABLET in 1 BLISTER PACK (0615-8298-39)

0781- Sandoz Inc
- 0781-5578- Entacapone
  - 0781-5578-01- 100 TABLET, FILM COATED in 1 BOTTLE (0781-5578-01)

0904- Major Pharmaceuticals
- 0904-6822- Entacapone
  - 0904-6822-07- 30 BLISTER PACK in 1 CARTON (0904-6822-07) / 1 TABLET, FILM COATED in 1 BLISTER PACK

17511- COHANCE LIFESCIENCES LIMITED
- 17511-109-
  - 17511-109-06- 25 kg in 1 DRUM (17511-109-06)

27241- Ajanta Pharma USA Inc.
- 27241-049- Entacapone
  - 27241-049-10- 100 TABLET in 1 BOTTLE (27241-049-10)

33342- Macleods Pharmaceuticals Limited
- 33342-260- Entacapone
  - 33342-260-11- 100 TABLET in 1 BOTTLE (33342-260-11)

33342- Macleods Pharmaceuticals Limited
- 33342-260- Entacapone
  - 33342-260-15- 500 TABLET in 1 BOTTLE (33342-260-15)

46438- Dipharma Francis Srl
- 46438-0005-
  - 46438-0005-0- 30 kg in 1 DRUM (46438-0005-0)

46708- Alembic Pharmaceuticals Limited
- 46708-478- ENTACAPONE
  - 46708-478-31- 100 TABLET, FILM COATED in 1 BOTTLE (46708-478-31)

46708- Alembic Pharmaceuticals Limited
- 46708-478- ENTACAPONE
  - 46708-478-91- 1000 TABLET, FILM COATED in 1 BOTTLE (46708-478-91)

47335- Sun Pharmaceutical Industries, Inc.
- 47335-007- Entacapone
  - 47335-007-88- 100 TABLET, FILM COATED in 1 BOTTLE (47335-007-88)

48087- F.I.S. FABBRICA ITALIANA SINTETICI S.P.A.
- 48087-0080-
  - 48087-0080-0- 50 kg in 1 DRUM (48087-0080-0)

48087- F.I.S. FABBRICA ITALIANA SINTETICI S.P.A.
- 48087-0109-
  48087-0109-0- 50 kg in 1 DRUM (48087-0109-0)

49587- YiChang HEC ChangJiang Pharmaceuical Co.,Ltd.
- 49587-105-
  49587-105-01- 25 kg in 1 DRUM (49587-105-01)

50268- AvPAK
- 50268-295- Entacapone
  50268-295-15- 50 BLISTER PACK in 1 BOX, UNIT-DOSE (50268-295-15) / 1 TABLET, FILM COATED in 1 BLISTER PACK (50268-295-11)

52427- Almatica Pharma LLC
- 52427-800- Comtan
  - 52427-800-01- 1 BOTTLE in 1 CARTON (52427-800-01) / 100 TABLET, FILM COATED in 1 BOTTLE

52483- Orion Corporation, Orion Pharma
- 52483-0014-
  - 52483-0014-0- 1 BAG in 1 DRUM (52483-0014-0) / 62000 TABLET, FILM COATED in 1 BAG

58032- Neuland Laboratories Limited
- 58032-2003-
  58032-2003-0- 1 kg in 1 DRUM (58032-2003-0)

60687- American Health Packaging
- 60687-188- Entacapone
  60687-188-21- 30 BLISTER PACK in 1 BOX, UNIT-DOSE (60687-188-21) / 1 TABLET, FILM COATED in 1 BLISTER PACK (60687-188-11)

62332- Alembic Pharmaceuticals Inc.
- 62332-478- ENTACAPONE
  - 62332-478-31- 100 TABLET, FILM COATED in 1 BOTTLE (62332-478-31)

62332- Alembic Pharmaceuticals Inc.
- 62332-478- ENTACAPONE
  - 62332-478-91- 1000 TABLET, FILM COATED in 1 BOTTLE (62332-478-91)

65085- Piramal Pharma Limited
- 65085-0050-
  - 65085-0050-1- 5 kg in 1 DRUM (65085-0050-1)

65085- Piramal Pharma Limited
- 65085-0050-
  65085-0050-2- 10 kg in 1 DRUM (65085-0050-2)

65085- Piramal Pharma Limited
- 65085-0050-
  65085-0050-3- 15 kg in 1 DRUM (65085-0050-3)

65085- Piramal Pharma Limited
- 65085-0050-
  65085-0050-4- 20 kg in 1 DRUM (65085-0050-4)

65085- Piramal Pharma Limited
- 65085-0050-
  65085-0050-5- 25 kg in 1 DRUM (65085-0050-5)

65372- Jubilant Pharmova Limited
- 65372-1149-
  65372-1149-2- 20 kg in 1 DRUM (65372-1149-2)

65862- Aurobindo Pharma Limited
- 65862-611-
  65862-611-37- 50 kg in 1 DRUM (65862-611-37)

65862- Aurobindo Pharma Limited
- 65862-654- Entacapone
  65862-654-01- 100 TABLET, FILM COATED in 1 BOTTLE (65862-654-01)

65862- Aurobindo Pharma Limited
- 65862-654- Entacapone
  - 65862-654-99- 1000 TABLET, FILM COATED in 1 BOTTLE (65862-654-99)

68022- Suven Pharmaceuticals Limited
- 68022-7015-
  - 68022-7015-2- 25 kg in 1 DRUM (68022-7015-2)

68022- Suven Pharmaceuticals Limited
- 68022-7015-
  68022-7015-3- 10 kg in 1 DRUM (68022-7015-3)

68022- Suven Pharmaceuticals Limited
- 68022-7015-
  68022-7015-8- 1 kg in 1 DRUM (68022-7015-8)

68022- Suven Pharmaceuticals Limited
- 68022-7015-
  68022-7015-9- .001 kg in 1 CONTAINER, FLEXIBLE INTERMEDIATE BULK (68022-7015-9)

68022- Suven Pharmaceuticals Limited
- 68022-7043-
  68022-7043-2- 25 kg in 1 DRUM (68022-7043-2)

68022- Suven Pharmaceuticals Limited
- 68022-7043-
  68022-7043-3- 10 kg in 1 DRUM (68022-7043-3)

68022- Suven Pharmaceuticals Limited
- 68022-7043-
  68022-7043-8- 1 kg in 1 DRUM (68022-7043-8)

68022- Suven Pharmaceuticals Limited
- 68022-7043-
  68022-7043-9- .001 kg in 1 CONTAINER, FLEXIBLE INTERMEDIATE BULK (68022-7043-9)

68554- Hetero Labs Limited
- 68554-0068-
  68554-0068-1- 30 kg in 1 DRUM (68554-0068-1)

71610- Aphena Pharma Solutions - Tennessee, LLC
- 71610-247- Entacapone
  71610-247-83- 3600 TABLET, FILM COATED in 1 BOTTLE (71610-247-83)

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

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US Brand Names ⬆ ⬇

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