Stimol® [Citrulline Malate]
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PHARMACOTHERAPY GROUP: general tonic.
ATH CODE: А13А
PHARMACOLOGICAL EFFECTS: anti-asthenia effect, and also contributes to liver detoxification.
Citrulline is an amino acid that participates in the ammonia neutralization cycle occurring in the liver, which is formed as a result of the breakdown of nitrogen-containing compounds. Urea is formed in the liver from ammonia. Citrulline is built into the urea cycle, increases the excretion of ammonium ions.
Malate is involved in the Krebs cycle and gluconeogenesis, reduces the concentration of lactate in the blood, helps to normalize the metabolism, activates non-specific protective factors of the body.
PHARMACOKINETICS: the drug is rapidly absorbed from the gastrointestinal tract, the peak plasma concentration is reached on average after 50 minutes. Quickly derived from plasma. After 6 hours, the plasma concentration is close to physiological. Since the active ingredient is involved in the processes of cellular metabolism, only small amounts of it are found in the urine.
used in the symptomatic treatment of functional asthenia: asthenic syndrome, fatigue, increased fatigue, during the period of recovery from illness.
1 sachet contains:
Citrulline malate 1.00 g
Natural orange flavoring sangria 0.10 g
Sodium hydroxide solution 30% 0.1886 g
Purified water to 10.00 ml
DESCRIPTION: colorless or yellowish liquid with an orange smell.
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Dosage and Administration
The drug is taken orally, regardless of the meal, without dividing the tablet into pieces. The optimal daily dose is determined by careful individual selection. As a single dose, only 1 tablet of any dosage should be taken. The maximum daily dose is 1.5 g of levodopa, 2 g of entacapone, 375 mg of carbidopa (corresponds to 10 pills of Stalevo 150 / 37.5 / 200 mg).
If necessary, the introduction of more levodopa reduce the interval between doses of the drug and / or transfer the patient to treatment with Stalevo at a higher dosage (necessarily within the recommended dose). If a smaller amount of levodopa is required, then increase the intervals between taking the drug and / or transfer the patient to Stalevo treatment in a lower dosage. If other drugs containing levodopa are used simultaneously with Stalevo, then the recommendations for the total daily dose of the drug should be carefully followed.
- Severe abnormal liver function.
- angle-closure glaucoma.
- Combined use with non-selective MAO inhibitors of types A and B (for example, phenelzine, tranylcypromine).
- Combined use with selective MAO inhibitors of types A and B.
- Malignant neuroleptic syndrome and / or atraumatic acute rhabdomyolysis (including in history).
- Children's and teenage age up to 18 years.
- Lactation period (breastfeeding).
- Hypersensitivity to the drug.
With caution should use the drug for:
- Severe cardiovascular and pulmonary insufficiency.
- Bronchial asthma.
- Liver disease.
- Kidney disease.
- Diabetes and other decompensated endocrine diseases.
- Erosive and ulcerative lesions of the digestive tract.
- Convulsions (in history).
- With a myocardial infarction in history (with persistent cardiac arrhythmias).
- Psychosis in history and / or during treatment.
- Depression with suicidal tendencies.
- Asocial behavior.
- Open-angle glaucoma.
Caution should be exercised while applying Stalevo with:
- Drugs that can cause orthostatic hypotension.
- With neuroleptics that block dopamine (especially dopamine D2 receptor antagonists).
- With tricyclic antidepressants, desipramine, maprolitine, venlafaxine.
- With warfarin and COMT metabolizable drugs (paroxetine).
The therapeutic effect of Stalevo is reduced, while taking it with dopamine receptor antagonists (some antipsychotics and antiemetic drugs), phenytoin, papaverine. When taken simultaneously with iron preparations, the effectiveness of Stalevo may decrease, since levodopa and entacapone form chelate complexes with iron ions in the gastrointestinal tract. It is necessary to observe the time interval of 2-3 hours between taking Stalevo and iron-containing preparations. The therapeutic effect of Stalevo may be reduced in patients receiving a high-protein diet, due to the competing action of levodopa and some amino acids. Steel is compatible with imizina and moclobemide, pyridoxine hydrochloride, diazepam, ibuprofen.
Pregnancy and Lactation
The drug is contraindicated for use in pregnancy (except in cases where the potential positive effect from taking the drug outweighs the possible risk to the development of the fetus) and during lactation.
It is not designed to eliminate extrapyramidal reactions caused by medication. Before planned general anesthesia, the drug can be taken as long as the patient is allowed oral administration. In the case of long-term therapy, Stalevo requires periodic monitoring of the functions of the liver, the system of hemopoiesis, kidneys, and the cardiovascular system. Monitoring the function of the cardiovascular system is required during the entire period of the initial dose adjustment of the drug.The use of the drug in open-angle glaucoma is possible only with careful control of intraocular pressure. When replacing Stalevo with levodopa + carbidopa therapy (without entacapone), an increase in the dose of levodopa will be required. Cancellation Stalevo spend slowly, if necessary, increasing the dose of levodopa. Therapy with Stalevo does not prevent the use of other anti-parkinsonian drugs. The daily dose of seleginin while taking with the drug Stalevo should not exceed 10 mg.
Influence on ability to drive motor transport and control mechanisms: entacapone in combination with levodopa causes drowsiness and episodic instant sleep. It is necessary to refuse to drive a car and work with machines and mechanisms during the period of taking the drug Stalevo.
Symptoms: increased severity of side effects, with the exception of allergic reactions that are dose-independent.
Treatment: hospitalization, gastric lavage, repeated administration of Activated charcoal. Control of the respiratory, cardiovascular and urinary systems; ECG monitoring, if necessary - antiarrhythmic therapy.
Pyridoxine is ineffective in Stalevo overdose.
- Brand name: Stalevo
- Active ingredient: Levodopa, Entacapone, Carbidopa
- Dosage form: pills, film coated.
- Manufacturer: Orion Corporation
- Country of Origin: Finland
- Use of a microbial model for the determination of drug effects on cell metabolism and energetics: Study of citrulline-malate
- l-Citrulline-malate influence over branched chain amino acid utilization during exercise
- Effects of a first exposure to ethanol on the compositions of neutral and polar lipids in Euglena gracilis Z, taken as a hepatic cell model: Equilibration by citrulline-malate
- Citrulline-malate effect on microsome phospholipids and cytochrome P450 in Euglena grown with ethanol
- Beneficial effects of citrulline malate on skeletal muscle function in endotoxemic rat
- Citrulline malate supplementation increases muscle efficiency in rat skeletal muscle
- Analyse par RMN du P-31 des effets du malate de citrulline sur le métabolisme énergétique musculaire chez l'homme
- Euglena, as a cellular model used in pharmacology for studying the effects of citrulline malate on lactate metabolization
- Oral l-citrulline malate in patients with idiopathic pulmonary arterial hypertension and Eisenmenger Syndrome: A clinical trial
- Effect of citrulline-malate supplementation on plasma amino acids and glycemic and insulinemic responses in horses
- Citrulline malate limits increase in muscle fatigue induced by bacterial endotoxins
- Citrulline/malate promotes aerobic energy production in human exercising muscle
- Effects of Supplemental Citrulline-Malate Ingestion on Blood Lactate, Cardiovascular Dynamics, and Resistance Exercise Performance in Trained Males
- Acute citrulline malate supplementation improves upper- and lower-body submaximal weightlifting exercise performance in resistance-trained females
- Acute citrulline-malate supplementation improves maximal strength and anaerobic power in female, masters athletes tennis players
- Effects of Supplemental Citrulline Malate Ingestion During Repeated Bouts of Lower-Body Exercise in Advanced Weightlifters
- Acute Citrulline-Malate supplementation and high-intensity cycling performance
- Citrulline Malate Enhances Athletic Anaerobic Performance and Relieves Muscle Soreness
- Scientific Opinion on the substantiation of a health claim related to citrulline malate and faster recovery from muscle fatigue after exercise pursuant to Article 13(5) of Regulation (EC) No 1924/2006
- Scientific Opinion on the substantiation of a health claim related to citrulline-malate and faster recovery from muscle fatigue after exercise pursuant to Article 13(5) of Regulation (EC) No 1924/2006
- The Effect of Citrulline/Malate on Blood Lactate Levels in Intensive Exercise
- Effect Of Acute Citrulline-malate Supplementation On Muscular Power
- The Effect of Citrulline Malate on Wingate Anaerobic Power Test Performance
- The Effect of Citrulline Malate Supplementation On Muscle Fatigue Among Healthy Participants