Tremonorm - instructions for use, dose, side effects, contraindications

One tablet contains: Active substance: levodopa 250 mg; carbidopa 27 mg (27 mg carbidopa monohydrate is equivalent to 25 mg carbidopa anhydrous) Excipients: pregelatinized starch, FD & C Blue No 2 Lake 12%, starch, microcrystalline cellulose, magnesium stearate.

Pharmacotherapeutic group:An antiparkinsonian remedy.

ATX: & nbsp

N.04.B.A.02 Levodopa and a decarboxylase inhibitor

Pharmacodynamics:

An antiparkinsonian drug is represented by a combination of Carbidopa, an inhibitor of decarboxylase of aromatic amino acids and levodopa, a metabolic precursor of dopamine.

Symptoms of Parkinson's disease are associated with a lack of dopamine in the basal ganglia of the brain.The administration of dopamine to such patients is not effective, since dopamine does not penetrate poorly through the blood-brain barrier. Levodopa, a metabolic precursor of dopamine, penetrates the blood-brain barrier and is converted to dopamine in the basal ganglia.

Ingestion levodopa quickly turns into dopamine in peripheral tissues, and only a small part of the dose taken in unchanged form is transported to the central nervous system. As a result, large doses of levodopa are required to achieve an adequate therapeutic effect.

Carbidopa inhibits the decarboxylation process of levodopa in peripheral tissues and does not penetrate the blood-brain barrier and does not affect the conversion of levodopa to dopamine in the central nervous system. Thus, the combination of carbidopa and levodopa increases the amount of levodopa that enters the brain.

Pharmacokinetics:

Data on the pharmacokinetics of carbidopa are limited. Levodopa when ingested quickly absorbed from the digestive tract. Absorption is 20-30% of the dose, the time of onset of Cmax with oral intake is 2-3 hours.Absorption depends on the rate of evacuation of the contents of the stomach and the pH in it. The presence of food in the stomach slows down absorption. Some food amino acids can compete with levodopa for absorption from the intestine and transport through the blood-brain barrier. In large quantities is contained in the small intestine, liver and kidneys, only 1-3% penetrates the brain. T 1/2 - 3 hours. Excretion: by the kidneys, through the intestine -35% within 7 hours. Metabolized in all tissues, mainly by decarboxylation with the formation of dopamine, which does not penetrate the BBB, metabolites - dopamine, norepinephrine, epinephrine are excreted by the kidneys. About 75% is excreted in the urine in the form of metabolites for 8 hours.

Indications:

- Parkinson's disease;

- Parkinson's syndrome (postencephalic, symptomatic, with intoxication with carbon monoxide and manganese).

Contraindications:

Individual intolerance of the drug, angle-closure glaucoma, mental disorders, hepatic and / or renal failure, heart failure, pulmonary heart, leukopenia, blood diseases, depression, skin diseases of unknown etiology, melanoma and suspicion of it, endocrine system diseases, pregnancy, lactation, children's age (up to 12 years).

Carefully:With cautiousness-expressed general atherosclerosis, arterial hypertension, myocardial infarction with rhythm disturbances (in the anamnesis), bronchial asthma, lung diseases, convulsive syndrome (in the anamnesis), erosive-ulcerative lesions of the gastrointestinal tract.

Dosing and Administration:

General information on dosage: to achieve the optimal therapeutic concentration in the blood and eliminate the side effect of the drug, the dosage is selected individually. This is extremely important for elderly patients and patients taking other drugs.

It is recommended to prescribe inside, 1 tablet (25/250 mg) 3 times a day, then increase the dose by 1 tablet every 2-3 days, until the optimal effect is achieved. Usually, the optimal effect is observed at a dose of 3-6 tablets (25/250 mg daily). The maximum daily dose is 200 mg carbidopa and 2 g levodopa (8 tablets 25 mg / 250 mg). When transferring patients with levodopa medication with an average duration of action to a combination of levodopa with carbidopa, its administration should be discontinued at least 8 hours before the appointment, and in case of transfer from the drug, levodopa long-acting for at least 12 hours.The optimal effect is achieved after 7 days of continuous reception. Dose reduction is necessary with the development of seizures and blepharospasm.

For children: Studies to determine safety and efficacy for children under 12 years of age have not been carried out.

Elderly: to the usual adult dose, elderly patients are more sensitive.

Side effects:At the beginning of treatment: nausea, vomiting, anorexia, epigastric pain, dysphagia, ulcerogenic effect (in predisposed patients); in some cases: heart rhythm disturbances, orthostatic hypotension, In the course of further treatment, self-movement, hemolytic anemia, leukopenia, thrombocytopenia, mental disorders, insomnia, increased excitability, depression, tachycardia, constipation, dyskinesia, hyperkinesia, weight gain.

Overdose:Symptoms: nausea, vomiting, insomnia, increased excitability, hyperkinesia, etc. The first help consists in washing the stomach, taking activated charcoal. If necessary, conduct symptomatic therapy in a hospital. Specific antidote for acute overdose Tremonorm there.The effectiveness of hemodialysis for treatment of overdose of the drug has not been established.

Interaction:

With the simultaneous use of the drug Tremonorm:

- with beta-adrenomimetics, dithiline and agents for inhalation anesthesia, an increased risk of developing cardiac rhythm disturbances is possible;

- with tricyclic antidepressants - reduced bioavailability of levodopa;

- with diazepam, clozepine, phenytoin, clonidine, m-holinoblokatorami, antipsychotic agents (neuroleptics) derivatives of butyrophenone, diphenylbutylpiperidine, thioxanthene, phenothiazine, as well as with pyridoxine; papaverine, reserpine - a decrease in the antiparkinsonian effect is possible;

- with lithium preparations - the risk of developing dyskinesias and hallucinations increases;

- with methyldopa - aggravation of side effects.

With the simultaneous use of Tremonorm with MAO inhibitors (with the exception of MAO-B inhibitors), circulatory disorders are possible. The intake of MAO inhibitors should be discontinued 2 weeks before the start of treatment with the drug. This is due to the accumulation of dopamine and norepinephrine under the influence of levodopa,inactivation of which is inhibited by MAO inhibitors and a high probability of development of excitation, increased blood pressure, tachycardia, facial flushing and dizziness. In patients receiving levodopa, the use of tubocurarine raises the risk of developing arterial hypotension.

Special instructions:It is unacceptable to suddenly stop taking the drug (with a sharp cancellation it is possible to develop a symptom complex resembling a malignant neuroleptic syndrome, including muscle rigidity, fever, mental disturbances, and increased serum creatinophosphinase.) When switching to levodopa with peripheral dopa decarboxylase inhibitors, Levodopa should be discontinued 12 hours before the appointment of the combined preparation.

The drug is not prescribed for elimination of extrapyramidal reactions caused by drugs.

It is necessary to avoid activities that require a high concentration of attention and speed of psychomotor reactions.

In the process of treatment, it is necessary to monitor the patient's mental status, peripheral blood patterns, liver, kidney and cardiovascular functions. Impact on laboratory tests:

Sometimes a positive direct test of Coombs is observed, usually without signs of hemolysis, although in some cases development of autoimmune hemolytic anemia is noted. The drug may discolour the urine.

Form release / dosage:Pills.

Packaging:

For 100 tablets in a vial. 10 tablets in a blister pack.

1 bottle, 5 or 10 blisters in a cardboard pack together with instructions for use.

Storage conditions:Store at a temperature of 15-30 ° C in a place protected from light. Keep out of the reach of children.

Shelf life:In the vial - 4 years. In the blister - 3 years.

Terms of leave from pharmacies:On prescription

Registration number:П N014114 / 01

Date of registration:31.07.2008

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

TEVA Pharmaceutical Industries, Ltd. Israel

Representation: & nbspTeva Teva Israel

Information update date: & nbsp23.08.2015

Illustrated instructions

Instructions

Tremonorm (Tremonorm)