Entacapone Tablets (Adcapone) – Product Information
Entacapone tablets (Adcapone) is used in the treatment of Parkinson’s Disease combination with Levodopa and Carbidopa to treat end-of-dose “wearing-off” in patients with Parkinson’s disease. Entacapone tablets effectiveness has not been systematically evaluated in patients with Parkinson’s disease who do not experience end-of-dose "wearing-off".
Adcapone (Entacapone tablets) is available as tablets containing 200 mg Entacapone.
We also stock Syndopa Tablets (Levodopa and Carbidopa Tablets) and Syndopa CR (Levodopa and Carbidopa Tablets Controlled Release)
Name of Drug
Adcapone tablets.
Manufacturer of Adcapone Tablets (Entacapone)
Sun Pharmaceutical Industries Ltd.
Website: www.sunpharma.com
Active Pharmaceutical Ingredient
The active pharmaceutical ingredients contained in Adcapone tablets is Entacapone. Each tablet contains 200 mg of the active ingredient Entacapone .
Mechanism of Action
The mechanism of action of entacapone is believed to be through its ability to inhibit COMT and alter the plasma pharmacokinetics of levodopa. When entacapone is given in conjunction with Levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of Levodopa are greater and more sustained than after administration of Levodopa and an aromatic amino acid decarboxylase inhibitor alone.
It is believed that at a given frequency of Levodopa administration, these more sustained plasma levels of Levodopa result in more constant dopaminergic stimulation in the brain, leading to greater effects on the signs and symptoms of Parkinson’s Disease. The higher Levodopa levels also lead to increased Levodopa adverse effects, sometimes requiring a decrease in the dose of levodopa.
Uses of Adcapone (Generic Entacapone Tablets)
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.
Entacapone Tablets (Adcapone) – Dosage and Administration
Please consult your doctor for exact dosing instructions.
One 200 mg tablet is taken with each Levodopa and Carbidopa dose. The maximum recommended dose is 200 mg ten times daily, i.e. 2,000 mg of Entacapone.
Entacapone enhances the effects of Levodopa. Hence, to reduce Levodopa-related dopaminergic adverse reactions, e.g. dyskinesias, nausea, vomiting and hallucinations, it is often necessary to adjust Levodopa dosage within the first days to first weeks after initiating Entacapone treatment.
The daily dose of Levodopa should be reduced by about 10 to 30% by extending the dosing intervals and/or by reducing the amount of Levodopa per dose, according to the clinical condition of the patient.
Missed Dose Instructions for Entacapone Tablets
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Adcapone Tablets – Contraindications
Adcapone tablets are contraindicated in persons with a hypersensitivity (allergy) to Entacapone or any of the other ingredients of this medicine.
The other contraindications are
- Entacapone is contraindicated in patients with Hepatic impairment.
- Patients with pheochromocytoma due to the increased risk of hypertensive crisis.
- A previous history of neuroleptic malignant syndrome (NMS) and/or non-traumatic rhabdomyolysis.
- Concomitant use of entacapone and non-selective monoamine oxidase (MAO-A and MAO-B) inhibitors (e.g. Phenelzine, Tranylcypromine).
- Concomitant use of a selective MAO-A inhibitor plus a selective MAO-B inhibitor and Entacapone.
- Entacapone should not be given to patients with clinical or laboratory evidence of uncompensated cardiovascular, endocrine, hematologic, pulmonary (including bronchial asthma), or renal disease.
- Entacapone should not be given when administration of a sympathomimetic amine is contraindicated.
- Entacapone is contraindicated in patients with pheochromocytoma due to the increased risk of hypertensive crisis.
- Entacapone should not be given to patients with narrow angle glaucoma.
- Because Levodopa may activate a malignant melanoma, entacapone should not be used in patients with suspicious, undiagnosed skin lesions or a history of melanoma.
Storage Instructions for Entacapone Tablets
Entacapone Tablets (Adcapone) should be stored at 25°C (77°F) excursions permitted to 15°-30°C (59°-86°F). Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing. Keep out of the reach of children and away from pets.
Warnings and Precautions to be taken when using Generic Entacapone Tablets (Adcapone)
Before using tablets please inform your doctor about all the medicines that you take including no prescription medications, over the counter medicines and herbal remedies.
Epidemiological studies have shown that patients with Parkinson’s disease have a higher risk (2- to approximately 6-fold higher) of developing melanoma than the general population. Whether the increased risk observed was due to Parkinson’s disease or other factors, such as drugs used to treat Parkinson’s disease, is unclear. For the reasons stated above, patients and healthcare providers are advised to monitor for melanomas frequently and on a regular basis when using entacapone for any indication.
Prostate cancer has been reported in elderly males during the use of entacapone in combination with levodopa/carbidopa in clinical trials. The clinical relevance of these adverse events is not known. Physicians are advised to adhere to the routine examination schedule for all male patients for symptoms and risk factors of prostate cancer including evaluation prior to initiating treatment with Entacapone.
Medicines known to be metabolized by COMT, such As Isoproterenol, Epinephrine, Norepinephrine, Dopamine, Dobutamine, Alpha-Methyldopa, Apomorphine, Isoetherine and Bitolterol should be administered with caution in patients receiving entacapone regardless of the route of administration (including inhalation), as their interaction may result in increased heart rates, possibly arrhythmias, and excessive changes in blood pressure.
Rhabdomyolysis secondary to severe dyskinesias or neuroleptic malignant syndrome (NMS) has been observed rarely in patients with Parkinson’s disease. Isolated cases of rhabdomyolysis have been reported with Entacapone treatment.
Myocardial infarction and other ischemic heart disease events have been reported with the use of Entacapone in combination with levodopa/DDC inhibitor in clinical trials. Entacapone therapy should be administered with caution to patients with ischaemic heart disease.
Because of its mechanism of action, Entacapone may interfere with the metabolism of medicinal products containing a catechol group and potentiate their action. Entacapone is always given as an adjunct to Levodopa treatment. Hence, the precautions valid for Levodopa treatment should also be taken into account for Entacapone treatment.
Entacapone may aggravate Levodopa-induced orthostatic hypotension. Entacapone should be given cautiously to patients who are taking other medicinal products which may cause orthostatic hypotension.
In clinical studies, adverse dopaminergic effects, e.g. dyskinesia, were more common in patients who received Entacapone and dopamine agonists (such as Bromocriptine), Selegiline or Amantadine compared to those who received placebo with this combination. The doses of other antiparkinsonian medications may need to be adjusted when Entacapone treatment is initiated. For patients experiencing diarrhoea, a follow-up of weight is recommended in order to avoid potential excessive weight decrease. Prolonged or persistent diarrhoea suspected to be related to Entacapone may be a sign of colitis. In the event of prolonged or persistent diarrhoea, Entacapone should be discontinued and appropriate medical therapy and investigations considered.
For patients who experience progressive anorexia, asthenia and weight decrease within a relatively short period of time, a general medical evaluation including liver function should be considered.
Patients should be regularly monitored for the development of impulse control disorders. Patients and caregivers should be made aware that behavioural symptoms of impulse control disorders including pathological gambling, increased libido, hypersexuality, compulsive spending or buying, binge eating and compulsive eating can occur in patients treated with dopamine agonists and/or other dopaminergic treatments such as entacapone in association with levodopa. Review of treatment is recommended if such symptoms develop.
Entapone tablets contain sucrose. Therefore, patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.
Entacapone used in combination with Levodopa has been associated with somnolence and episodes of sudden sleep onset in patients with Parkinson’s disease while engaged in activities of daily living, including the driving of a car, which sometimes resulted in accidents. Therefore caution should therefore be exercised when driving or operating machines
Effects On Ability To Drive And Use Machines
Entacapone in association with Levodopa may have major influence on the ability to drive and use machines. Patients being treated with Entacapone in association with Levodopa and presenting with somnolence and/or sudden sleep onset episodes must be instructed to refrain from driving or engaging in activities where impaired alertness may put themselves or others at risk of serious injury or death (e.g. operating machines) until such recurrent episodes have resolved.
Entacapone may, together with Levodopa, cause dizziness and symptomatic orthostatism. Therefore, caution should be exercised when driving or using machines.
Side Effects of Entacapone Tablets (Adcapone)
Very common Entacapone (Adcapone Tablets) found in double-blind placebo controlled phase III studies are dyskinesia, nausea, and abnormal urine.
Common side effects found in double-blind placebo controlled phase III studies are diarrhoea, Parkinsonism aggravated, dizziness, abdominal pain, insomnia, dry mouth, fatigue, hallucinations, constipation, dystonia, increased sweating, hyperkinesia, headache, leg cramps, confusion, paranoia, fall, postural hypotension, vertigo and tremor.
The following side effects, listed below, have been accumulated both from clinical studies with Entacapone and since the introduction of Entacapone into the market.
Psychiatric disorders
Common: Insomnia, hallucinations, confusion, nightmares
Very rare Agitation
Nervous system disorders
Very common: Dyskinesia
Common: Parkinsonism aggravated, dizziness, dystonia, hyperkinesia
Cardiac disorders
Common: Ischaemic heart disease events other than myocardial infarction(e.g. angina pectoris)
Uncommon: Myocardial infarction
Gastrointestinal disorders
Very common Nausea
Common: Diarrhoea, abdominal pain, dry mouth, constipation, vomiting
Very rare: Anorexia, colitis
Hepato-biliary disorders
Rare Hepatic function tests abnormal
Not known Hepatitis with mainly cholestatic features
Skin and subcutaneous tissue disorders
Rare: Erythematous or maculopapular rash
Very rare: Urticaria
Not known Skin, hair, beard and nail discolourations
Renal and urinary disorders Very common: Urine discolouration General disorders and administration site conditions
Common: Fatigue, sweating increased, fall
Very rare: Weight decrease
Entacapone (Adcapone Tablets) Overdosage
The post-marketing data includes isolated cases of Entacapone (Adcapone Tablets) overdose in which the reported highest daily dose of Entacapone has been 16,000 mg.
The acute symptoms and signs in these cases of overdose included agitation, dsyskinesia, confusional state, coma, bradycardia, ventricular tachycardia, Cheyne-Stokes respiration, mydriasis, decreased activity, somnolence, hypotonia, discolouration of the skin, tongue and conjunctiva, chromaturia, mild renal failure, neuroleptic malignanat syndrome and urticaria.
Management of acute overdosing is symptomatic. Hospitalization is advised and general supportive care is indicated. There is no known antidote to entacapone. The drug is rapidly absorbed and eliminated with a short mean residence time. There is no experience with dialysis or hemoperfusion, and these procedures are unlikely to be of benefit, because Entacapone is highly bound to plasma proteins.
An immediate gastric lavage and repeated doses of charcoal over time may hasten the elimination of entacapone by decreasing the absorption/reabsorption of entacapone from GI tract. The adequacy of the respiratory and circulatory systems should be carefully observed and appropriate supportive measures employed.
In managing overdosage, the possibility of interaction among drugs, especially catechol-structured drugs, should be borne in mind.
Entacapone (Adcapone Tablets) During Pregnancy
Entacapone (Adcapone Tablets) is classified by the US FDA as Pregnancy Category C. In embryofetal development studies, Entacapone was administered to pregnant animals throughout organogenesis at doses of up to 1,000 mg/kg/day in rats and 300 mg/kg/day in rabbits. Increased incidences of fetal variations were evident in litters from rats treated with the highest dose, in the absence of overt signs of maternal toxicity.
There is no experience from clinical studies regarding the use of Comtan in pregnant women.
Therefore, Adcapone tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether is excreted in human milk.
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