pharmachologic effect
It has a stimulating effect on cardiac activity, slightly dilates the coronary (heart) vessels and bronchi, and increases urination. The diuretic (diuretic) effect is associated primarily with a decrease in tubular reabsorption (reabsorption in the kidneys) of water, sodium and chlorine ions. Theobromine causes mild stimulation of the central nervous system.Indications for use
It is used mainly for mild spasms (sharp narrowing of the lumen) of cerebral vessels, sometimes for edema due to heart and kidney failure.Mode of application
Orally 0.25-0.5 g 1-2 times a day.Side effects
Weak stimulation of the central nervous system.Links
- Official instructions for the drug Theobromine.
- Modern drugs: a complete practical guide. Moscow, 2000. S. A. Kryzhanovsky, M. B. Vititnova.
Description of the drug " Theobromine"on this page is a simplified and expanded version of the official instructions for use. Before purchasing or using the drug, you should consult your doctor and read the instructions approved by the manufacturer.
Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
670. Theobrominum
Theobromine
3,7-Dimethylxanthine
C 7 H 8 N 4 0 2 M. V. 180.17
Description. White crystalline powder, odorless, bitter taste.
Solubility. Very slightly soluble in water, slightly soluble in hot water, very slightly soluble in 95% alcohol, ether, chloroform, easily soluble in dilute alkalis and acids.
Authenticity. 0.1G The drug is placed in a porcelain cup, 10 drops of perhydrol, 10 drops of diluted hydrochloric acid are added and evaporated to dryness in a water bath. The residue is moistened with 1-2 drops of ammonia solution; a purple-red color appears.
K 0.1 G 2 drugs are added ml 0.1 n. caustic soda solution. shake for 2-3 minutes and filter. Add 3 drops of a 2% cobalt chloride solution to the filtrate and mix; A quickly disappearing intense violet color appears and a grayish-blue precipitate is formed almost immediately (different from theophylline and caffeine).
0,05 G the drug is dissolved in mixture 3 ml water and 6 ml sodium hydroxide solution, add 1 ml ammonia solution and 2 ml 5% silver nitrate solution. After shaking, a thick gelatinous mass is formed, which liquefies when heated to 80° and solidifies again when cooled.
Caffeine. About 0.5 G the drug (exactly weighed) is dissolved in 30 ml 0.1 n. caustic soda solution in a separating funnel with a ground-in stopper (you cannot use a rubber stopper), add 10 ml chloroform and shake vigorously. The chloroform extract is dried with anhydrous sodium sulfate and filtered into a weighed cup. Sodium sulfate is washed 3 ml chloroform, collecting it in the same cup. Chloroform is evaporated in a water bath and the residue is dried at 80°C until constant weight. The balance should not exceed 0.5%.
Z-Methylxanthine. 0.5 G the drug is placed in a test tube, 2 are added ml 0.1 n. sodium hydroxide solution, shake for 2 minutes and filter into a test tube through a double filter of small diameter. Add 3 drops of a 2% cobalt chloride solution to the filtrate and mix quickly. The violet color that appears should disappear no later than after 2 minutes.
Chlorides. 2 G The powdered preparation is shaken with 40 ml water for 1 minute and filter through a glass filter, on which a small layer (0.5-1 cm) paper pulp. 10 ml The filtrate must pass the chloride test (not more than 0.004% in the preparation).
Sulfates. 10 ml the same filtrate must pass the test for sulfates (not more than 0.02% in the preparation).
Organic impurities. Solution 0.1 G drug in 2 ml concentrated sulfuric acid should be transparent and colorless.
Weight loss during drying. About 0.5 G The drug (exactly weighed) is dried at 100-105° to constant weight. Weight loss should not exceed 0.5%.
Sulfated ash and heavy metals. Sulfated ash from 0.5 G the drug should not exceed 0.1% and must pass the test for heavy metals (no more than 0.001% in the drug).
Quantitation. About 0.3 G The drug (exactly weighed) is placed in a conical flask with a capacity of 250-300 ml, add 100 ml boiling water (pre-boiled for 5 minutes) and boil on a grid until the drug is completely dissolved. Add 25 to the hot solution ml 0.1 n. silver nitrate solution, stir, cool to room temperature, add 1-1.5 ml phenol red solution and titrated with 0.1 N. with sodium hydroxide solution until a violet-red color appears.
1 ml 0.1 n. caustic soda solution corresponds to 0.01802 G C 7 H 8 N 4 0 2 which in terms of dry matter must be at least 99.0%.
Storage. List B. In a well-closed container.
Highest single oral dose 1.0 G.
Highest daily oral dose 3.0 G.
Instructions for the drug Theobromine, contraindications and methods of use, side effects and reviews about this drug. Doctors' opinions and the opportunity to discuss on the forum.
International nonproprietary names (INN) - active substances or active ingredients of medicinesInstructions for use
Latin name of the substance
Pharmacology
Bronchodilator, dimethixanthin, purine derivative. Inhibits PDE, increases the accumulation of cAMP in tissues, blocks adenosine (purine) receptors; reduces the flow of calcium ions through the channels of cell membranes, reduces the contractile activity of smooth muscles.
Relaxes the muscles of the bronchi, blood vessels (mainly the vessels of the brain, skin and kidneys); has a peripheral vasodilating effect, increases renal blood flow, and has a moderate diuretic effect. Stabilizes the mast cell membrane, inhibits the release of mediators of allergic reactions. Increases mucociliary clearance, stimulates contraction of the diaphragm, improves the function of the respiratory and intercostal muscles, and stimulates the respiratory center. By normalizing respiratory function, it helps saturate the blood with oxygen and reduce the concentration of carbon dioxide; stimulates the respiratory center. Strengthens ventilation of the lungs in conditions of hypokalemia. It has a stimulating effect on the activity of the heart, increases strength and heart rate, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly those of the brain, skin and kidneys). Reduces pulmonary vascular resistance, lowers pressure in the pulmonary circulation.
Expands extrahepatic bile ducts.
Inhibits platelet aggregation (suppresses platelet activating factor and PgE2-alpha), increases the resistance of red blood cells to deformation (improves the rheological properties of blood), reduces thrombus formation and normalizes microcirculation. Has a weak psychostimulating effect.
Contraindications Theobromine
Epilepsy, gastric and duodenal ulcers, gastritis with high acidity, recent history of gastrointestinal bleeding, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, retinal hemorrhage, children under 3 years of age, hypersensitivity to theobromine, as well as xanthine derivatives: caffeine, pentoxifylline, theophylline).
Restrictions on use
Use with caution in severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread vascular atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, chronic heart failure, increased convulsive readiness, liver and/or kidney failure, gastric and duodenal ulcers (in history), with recent bleeding from the gastrointestinal tract, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy, in elderly patients and children.
Side effects decrease with decreasing dosage of theobromine.
During treatment, the patient should be careful when consuming large quantities of caffeine-containing foods or drinks.
Use during pregnancy and lactation
Theobromine should be used with caution during pregnancy and lactation.
Side effects
From the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor.
From the cardiovascular system: palpitations, tachycardia (including in the fetus when taken by a pregnant woman in the third trimester), arrhythmias, decreased blood pressure, cardialgia, increased frequency of angina attacks.
From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with long-term use - loss of appetite.
Allergic reactions: skin rash, itching, fever.
Others: chest pain, tachypnea, flushing, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.
Interaction
With simultaneous use, theobromine increases the likelihood of developing side effects of corticosteroids, mineralocorticoids (hypernatremia), drugs for general anesthesia (the risk of ventricular arrhythmias increases), drugs that excite the central nervous system (increases neurotoxicity).
Antidiarrheal drugs and enterosorbents reduce the absorption of theobromine. Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracizine, being inducers of microsomal oxidation, increase the clearance of theobromine, which may require an increase in its dose.
When used simultaneously with inhibitors of CYP isoenzymes (including macrolide antibiotics, lincomycin, allopurinol, cimetidine, fluoroquinolones), isoprenaline, enoxacin, disulfiram, recombinant interferon alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and with vaccination against influenza, the effect of theobromine is enhanced (its dose may need to be reduced).
Enhances the effect of beta-adrenergic stimulants and diuretics (including by increasing glomerular filtration), reduces the effectiveness of lithium preparations and beta-blockers.
Compatible with antispasmodics, do not use in combination with other xanthine derivatives.
Use with caution simultaneously with anticoagulants.
Directions for use and dosage: Theobromine
Orally, 250 mg 3 times/day after meals.
pills
Pharmachologic effect:
In chemical structure and pharmacological properties it is close to purine alkaloids. Bronchodilator, purine derivative; inhibits phosphodiesterase, increases the accumulation of cAMP in tissues, blocks adenosine (purine) receptors; reduces the flow of calcium ions through the channels of cell membranes, reduces the contractile activity of smooth muscles. Relaxes the muscles of the bronchi, blood vessels (mainly the vessels of the brain, skin and kidneys); has a peripheral vasodilating effect, increases renal blood flow, and has a moderate diuretic effect. Stabilizes the mast cell membrane, inhibits the release of mediators of allergic reactions. Increases mucociliary clearance, stimulates contraction of the diaphragm, improves the function of the respiratory and intercostal muscles, and stimulates the respiratory center. By normalizing respiratory function, it helps saturate the blood with oxygen and reduce the concentration of carbon dioxide; stimulates the breathing centers. Strengthens ventilation of the lungs in conditions of hypokalemia. It has a stimulating effect on the activity of the heart, increases strength and heart rate, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly those of the brain, skin and kidneys). Reduces pulmonary vascular resistance, lowers pressure in the “lesser” circulation. Increases renal blood flow and has a moderate diuretic effect. Expands extrahepatic bile ducts. Inhibits platelet aggregation (suppresses platelet activating factor and PgE2-alpha), increases the resistance of red blood cells to deformation (improves the rheological properties of blood), reduces thrombus formation and normalizes microcirculation. Has a weak psychostimulating effect.
Indications:
Broncho-obstructive syndrome of any origin: bronchial asthma (drug of choice in patients with exercise-induced asthma and as an additional remedy for other forms), COPD (chronic obstructive bronchitis, pulmonary emphysema). Pulmonary hypertension, cor pulmonale, edematous syndrome of renal origin (as part of combination therapy).
Contraindications:
Hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theophylline), epilepsy, peptic ulcer of the stomach and duodenum (in the acute stage - for oral forms, especially non-extended-release tablets), gastritis with high acidity, bleeding from the gastrointestinal tract in a recent history, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, retinal hemorrhage, children under 3 years of age. Caution. Severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread vascular atherosclerosis, HOCM, frequent ventricular extrasystole, CHF, increased convulsive readiness, liver and/or renal failure, peptic ulcer of the stomach and duodenum (history), bleeding from Gastrointestinal tract in a recent history, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy. pregnancy, lactation period, old age, childhood.
Side effects:
From the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor. From the cardiovascular system: palpitations, tachycardia (including in the fetus when taken by a pregnant woman in the third trimester), arrhythmias, decreased blood pressure, cardialgia, increased frequency of angina attacks. From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with long-term use - loss of appetite. Allergic reactions: skin rash, itching, fever. Other: chest pain, tachypnea, flushing, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating. Side effects decrease with decreasing dose of the drug. Overdose. Symptoms: loss of appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, flushing of the facial skin, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremor, convulsions . In severe poisoning, epileptoid seizures may develop (especially in children without any warning signs), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, skeletal muscle necrosis, confusion, renal failure with myoglobinuria. Treatment: drug withdrawal, gastric lavage, administration of activated charcoal, laxatives, intestinal lavage with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasma sorption, hemodialysis (low efficiency, peritoneal dialysis is ineffective), symptomatic therapy (including metoclopramide and ondansetron - when vomiting). If convulsions occur, maintain airway patency and administer oxygen therapy. To stop a seizure - intravenous diazepam, 0.1-0.3 mg/kg (but not more than 10 mg). For severe nausea and vomiting, use metoclopramide or ondansetron (iv).
Directions for use and dosage:
Theobromine is taken orally, 0.25 g 3 times a day after meals.
Special instructions:
Use caution when consuming large amounts of caffeine-containing foods or drinks during treatment.
Interaction:
Increases the likelihood of developing side effects of GCS, MCS (hypernatremia), drugs for general anesthesia (increases the risk of ventricular arrhythmias), drugs that excite the central nervous system (increases neurotoxicity). Antidiarrheal drugs and enterosorbents reduce the absorption of theophylline. Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracizine, being inducers of microsomal oxidation, increase the clearance of theophylline, which may require an increase in its dose. When used simultaneously with P450 inhibitors (including macrolide antibiotics, lincomycin, allopurinol, cimetidine, fluoroquinolones), isoprenaline, enoxacin, disulfiram, recombinant interferon alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and when vaccinated against influenza, the potency of theophylline may increase and require a reduction in its dose. Enhances the effect of beta-adrenergic stimulants and diuretics (including by increasing glomerular filtration), reduces the effectiveness of Li+ drugs and beta-blockers. Compatible with antispasmodics, do not use in combination with other xanthine derivatives. Prescribe with caution simultaneously with anticoagulants.
Before using the drug Theobromine consult your doctor!
Theobromine
Theobromine:: Dosage form
pills
Theobromine:: Pharmacological action
In chemical structure and pharmacological properties it is close to purine alkaloids. Bronchodilator, purine derivative; inhibits phosphodiesterase, increases the accumulation of cAMP in tissues, blocks adenosine (purine) receptors; reduces the flow of calcium ions through the channels of cell membranes, reduces the contractile activity of smooth muscles. Relaxes the muscles of the bronchi, blood vessels (mainly the vessels of the brain, skin and kidneys); has a peripheral vasodilating effect, increases renal blood flow, and has a moderate diuretic effect. Stabilizes the mast cell membrane, inhibits the release of mediators of allergic reactions. Increases mucociliary clearance, stimulates contraction of the diaphragm, improves the function of the respiratory and intercostal muscles, and stimulates the respiratory center. By normalizing respiratory function, it helps saturate the blood with oxygen and reduce the concentration of carbon dioxide; stimulates the breathing centers. Strengthens ventilation of the lungs in conditions of hypokalemia. It has a stimulating effect on the activity of the heart, increases strength and heart rate, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly those of the brain, skin and kidneys). Reduces pulmonary vascular resistance, lowers pressure in the “lesser” circulation. Increases renal blood flow and has a moderate diuretic effect. Expands extrahepatic bile ducts. Inhibits platelet aggregation (suppresses platelet activating factor and PgE2-alpha), increases the resistance of red blood cells to deformation (improves the rheological properties of blood), reduces thrombus formation and normalizes microcirculation. Has a weak psychostimulating effect.
Theobromine:: Indications
Broncho-obstructive syndrome of any origin: bronchial asthma (drug of choice in patients with exercise-induced asthma and as an additional remedy for other forms), COPD (chronic obstructive bronchitis, pulmonary emphysema). Pulmonary hypertension, cor pulmonale, edematous syndrome of renal origin (as part of combination therapy).
Theobromine:: Contraindications
Hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theophylline), epilepsy, peptic ulcer of the stomach and duodenum (in the acute stage - for oral forms, especially non-extended-release tablets), gastritis with high acidity, bleeding from the gastrointestinal tract in a recent history, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, retinal hemorrhage, children under 3 years of age. Caution. Severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread vascular atherosclerosis, HOCM, frequent ventricular extrasystole, CHF, increased convulsive readiness, liver and/or renal failure, peptic ulcer of the stomach and duodenum (history), bleeding from Gastrointestinal tract in a recent history, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy. pregnancy, lactation period, old age, childhood.
Theobromine:: Side effects
From the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor. From the cardiovascular system: palpitations, tachycardia (including in the fetus when taken by a pregnant woman in the third trimester), arrhythmias, decreased blood pressure, cardialgia, increased frequency of angina attacks. From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with long-term use - loss of appetite. Allergic reactions: skin rash, itching, fever. Other: chest pain, tachypnea, flushing, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating. Side effects decrease with decreasing dose of the drug. Overdose. Symptoms: loss of appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, flushing of the facial skin, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremor, convulsions . In severe poisoning, epileptoid seizures may develop (especially in children without any warning signs), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, skeletal muscle necrosis, confusion, renal failure with myoglobinuria. Treatment: drug withdrawal, gastric lavage, administration of activated charcoal, laxatives, intestinal lavage with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasma sorption, hemodialysis (low efficiency, peritoneal dialysis is ineffective), symptomatic therapy (including metoclopramide and ondansetron - when vomiting). If convulsions occur, maintain airway patency and administer oxygen therapy. To stop a seizure - intravenous diazepam, 0.1-0.3 mg/kg (but not more than 10 mg). For severe nausea and vomiting, use metoclopramide or ondansetron (iv).
Theobromine:: Directions for use and dosage
Orally, 0.25 g 3 times a day after meals.
Theobromine:: Special instructions
Use caution when consuming large amounts of caffeine-containing foods or drinks during treatment.
Theobromine:: Interaction
Increases the likelihood of developing side effects of GCS, MCS (hypernatremia), drugs for general anesthesia (increases the risk of ventricular arrhythmias), drugs that excite the central nervous system (increases neurotoxicity). Antidiarrheal drugs and enterosorbents reduce the absorption of theophylline. Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracizine, being inducers of microsomal oxidation, increase the clearance of theophylline, which may require an increase in its dose. When used simultaneously with P450 inhibitors (including macrolide antibiotics, lincomycin, allopurinol, cimetidine, fluoroquinolones), isoprenaline, enoxacin, disulfiram, recombinant interferon alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and when vaccinated against influenza, the potency of theophylline may increase and require a reduction in its dose. Enhances the effect of beta-adrenergic stimulants and diuretics (including by increasing glomerular filtration), reduces the effectiveness of Li+ drugs and beta-blockers. Compatible with antispasmodics, do not use in combination with other xanthine derivatives. Prescribe with caution simultaneously with anticoagulants.
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