$22.75
In stock
Guaranteed refund or reship if you haven't received your order
Secure and encrypted payment processing
We ship to over 40 countries including the USA, UK, Europe, Australia and Japan

Composition:


active ingredients:


1 ml of the solution contains theophylline monohydrate (in terms of theophylline) 2 mg, potassium chloride 0.3 mg, magnesium chloride hexahydrate (in terms of magnesium chloride) 0.2 mg;


excipients: disodium salt of succinic acid, water for injection.


Dosage form. Solution for infusions


Basic physical and chemical properties: transparent colorless liquid.


Pharmacotherapeutic group. Means for systemic use in obstructive airway diseases. Xanthines. Theophylline, a combination without psycholeptics. ATX code R03D A54.


Pharmacological properties


Pharmacodynamics. Theophylline is a bronchodilator, antispasmodic agent.


The mechanism of bronchodilator action is due to the ability of theophylline to block adenosine receptors, non-selectively inhibit the enzyme phosphodiesterase and thereby increase the concentration of cyclic 3',5' - amp (camp) in tissues, inhibit the transport of calcium ions through "slow" channels of cell membranes and reduce its output from intracellular depots. Theophylline inhibits the release of inflammatory mediators from mast cells, increases mucociliary clearance, stimulates diaphragm contraction, and improves the function of respiratory and intercostal muscles.


It shows a distinct bronchodilator effect due to the direct relaxation of the smooth muscles of the bronchi. The manifestation of the bronchospasmolytic effect depends on the concentration of theophylline in the blood.


Normalizes respiratory function, helps to saturate the blood with oxygen and reduce the concentration of carbon dioxide; stimulates the respiratory center. Increases ventilation in conditions of hypokalemia. Inhibits platelet aggregation (inhibits platelet activation factor and prostaglandin F2-alpha), increases the resistance of red blood cells to deformation (improves the rheological properties of blood), reduces thrombosis and normalizes microcirculation.


It stimulates the central nervous system and heart activity, increases the strength and heart rate, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly blood vessels of the brain, skin and kidneys). Reduces perifocal and general brain edema, reduces CSF and, consequently, intracranial pressure. Reduces pulmonary vascular resistance, reduces pressure in the small circle of blood circulation. Increases renal blood flow, shows a moderate diuretic effect. Dilates the extrahepatic biliary tract.


Therapeutic effects develop 5-15 minutes after intravenous administration.


Potassium, the main cation of intracellular fluid, is involved in the utilization of carbohydrates and protein synthesis, and is needed to regulate nerve conduction and muscle contraction, as well as the heart muscle.


Magnesium stabilizes myocardial membranes, suppresses the activity of myosin phosphorylase, due to which a reserve of adenosine triphosphate (ATP) accumulates in cells. The protective effects of magnesium and potassium are additive.


Pharmacokinetics. The bioavailability of the drug is 80-100 %. Binding to plasma proteins is about 60 %. Penetrates through the placental barrier and into breast milk. It is metabolized in the liver (90 %) with the participation of several cytochrome P450 enzymes (the most important CYP1A2). The main metabolites of the drug are: 1,3-dimethylsechoic acid and 3-methylxanthine. Metabolites are excreted by the kidneys. About 7-13% of the administered dose is excreted unchanged (in children – 50%). In infants, a significant part is excreted in the form of caffeine (due to the immaturity of the pathways of its further metabolism). The elimination half – life (T1/2) in non – smokers is 6-12 hours; in smokers, it is significantly shorter – 4-5 hours, in children – 1-5 hours, in newborns and premature infants-10-45 hours. In patients with cirrhosis of the liver, renal failure and alcoholism, T1/2 is prolonged. The total clearance of the drug is reduced in patients with fever, patients with severe respiratory, hepatic and heart failure, with viral infections, in patients over 55 years of age.


Potassium (K+) ions are freely filtered in the glomeruli, but are almost completely reabsorbed in the proximal tubules, and only 10% of the filtered K+ions are excreted. Secretion in the distal tubules and collecting tubules can significantly increase the elimination of K+. The kidneys have a limited ability to maintain K+concentrations.


When administered parenterally, magnesium quickly enters organs and tissues, penetrates the blood-brain barrier, placenta, and penetrates into breast milk in high concentrations. The drug is excreted mainly in the urine.


Clinical characteristics.


Indications.


Bronchial obstructive syndrome in bronchial asthma, bronchitis, emphysema of the lungs, disorders of the respiratory center (nocturnal paroxysmal apnea), "pulmonary heart".


Contraindications.


Hypersensitivity to the components of the drug, as well as to other xanthine derivatives (caffeine, pentoxifylline, theobromine), acute heart failure, angina pectoris, acute myocardial infarction, decompensated chronic heart failure, paroxysmal tachycardia, extrasystole, violation of atrioventricular conduction, severe arterial hyper- hypotension, widespread vascular atherosclerosis, pulmonary edema, hemorrhagic stroke, retinal hemorrhage, glaucoma, a history of bleeding, gastric and duodenal ulcers (acute), gastroesophageal reflux, epilepsy, increased convulsive readiness, uncontrolled hypothyroidism, hyperthyroidism, thyrotoxicosis, severe hepatic and/or renal failure, porphyria, sepsis, acidosis, hyperkalemia hyperchloremia, acute dehydration, significant burns, intestinal obstruction, Addison's disease, patient's age 70 years. Children's age (up to 18 years). Pregnancy and lactation.


Interactions with other drugs and other types of interactions.


During treatment, you should not consume alcoholic beverages, large amounts of food and beverages containing methylxanthine (coffee, tea, cocoa, chocolate, Coca-Cola), drugs related to theophylline (caffeine, theobromine, pentoxifylline), because these substances can increase the stimulating effect of theophylline on the central nervous system.


The effect of theophylline may be enhanced with the simultaneous use of allopurinol, Acyclovir, carbimazole, zafirlukast, cimetidine, nizatidine, disulfiram, phenylbutazone, fluvoxamine, fluconazole, fluoroquinolones, furosemide, imipenem, isoprenaline, interferon alpha, isoniazid, calcium antagonists (verapamil, diltiazem), lincomycin, macrolides, amiodarone, mixelitin, methotrexate, paracetamol, pentoxifylline, oral contraceptives, probenecid, propafenone, propranolol, Ranitidine, tacrin, thiabendazole, ticlopidine, viloxazine, or flu vaccine. In patients who are taking one or more of the above medications in parallel with theophylline, the concentration of theophylline in the blood serum should be monitored and the dose reduced, if necessary.


The combination of theophylline and fluvoxamine should be avoided. If it is impossible to avoid this combination, patients should take half the dose of theophylline and carefully monitor the plasma concentrations of the latter.


When taking ciprofloxacin at the same time, the dose of theophylline should be reduced by at least 60%, and when taking enoxacin at the same time – by 30 %.


The effect of theophylline may decrease with simultaneous administration of antiepileptic drugs (for example, phenytoin, carbamazepine, primidone), barbiturates (especially phenobarbital and pentobarbital), aminoglutemide, magnesium hydroxide, moracizine, rifampicin, ritonavir or sulfinpyrazone. The effect of theophylline may also be less in smokers. In patients who are taking one or more of the above medications simultaneously with theophylline, the concentration of theophylline in the blood serum should be monitored and the dose adjusted.


Concomitant use of theophylline with herbal preparations containing St. John's wort (Hypericum perforatum) should be avoided.


Ephedrine enhances the effect of theophylline.

Theophylline may enhance the effects of beta-receptor agonists, diuretics, and reserpine. Theophylline may reduce the effectiveness of adenosine, lithium carbonate, and beta-receptor antagonists.


Concomitant use of theophylline and beta-receptor antagonists should be avoided, as theophylline may lose its effectiveness.


Combinations of theophylline and benzodiazepine, halothane and lomustine should be used with extreme caution. Halothane anesthesia can cause serious cardiac arrhythmias in patients taking theophylline.


Concomitant use of theophylline with ketamine can lower the seizure threshold, with doxapram – cause stimulation of the central nervous system.


Hypokalemia may occur during treatment with theophylline, especially with combined treatment with beta-receptor agonists, thiazide diuretics, furosemide, corticoids, and hypoxemia; therefore, it is recommended to periodically check the level of potassium in the blood serum.


Application features.


Before Administration, the solution must be heated to body temperature.


Use with caution in diseases of the cardiovascular system, liver, viral infection, prolonged hyperthermia, prostatic hypertrophy, severe hypoxia, diabetes mellitus, glaucoma, the elderly (from 60 to 70 years).


With caution and only in case of urgent need, prescribe the drug in patients with impaired renal function, patients with a history of peptic ulcer of the stomach and duodenum. Patients with a history of seizures should avoid using theophylline and resort to alternative treatment. Increased attention should be paid to the use of the drug in patients suffering from insomnia.


Tobacco smoking and alcohol consumption can lead to an increase in the clearance of theophylline and, consequently, to a decrease in its therapeutic effect and the need for higher doses.


Fever, regardless of its cause, can reduce the rate of elimination of theophylline.


Theophylline can change some laboratory parameters: increase the amount of fatty acids and the level of catecholamines in the urine.


During treatment, it is recommended to regularly monitor the level of potassium in the blood serum and do an ECG, as well as monitor the acid-base balance of the blood, especially in patients with diseases of the cardiovascular system and kidneys.


Animal studies have shown that Derkast with a course of administration can cause a decrease in the levels of hemoglobin, red blood cells and white blood cells to the lower limits of normal. Therefore, it is not recommended to prescribe the drug to patients with reduced levels of these indicators. The data obtained indicate a weak toxic effect of the drug Derkast on the reproductive function of male rats and a moderate mutagenic effect on mammalian somatic cells (mice).


Patients of different races and/or ethnicities are characterized by polymorphism of CYP genes, which causes different activity of liver enzymes that metabolize theophylline. This can lead to the accumulation of theophylline in the patient's blood and contribute to the development of adverse reactions. In this regard, in patients with other races, it is recommended to monitor the level of serum theophylline during treatment with Derkast.


Since theophylline is characterized by a narrow therapeutic range, the likelihood of side effects, with prolonged use, it is advisable to monitor its concentration in blood plasma.


Use during pregnancy or lactation.


The drug is contraindicated during pregnancy. If it is necessary to use the drug, breast-feeding should be discontinued.


Ability to influence the reaction rate when driving vehicles or other mechanisms.


Given that sensitive patients may experience adverse reactions (dizziness, others) when using the drug, during the period of using the drug, you should refrain from driving vehicles and performing other work that requires concentration of attention.


Dosage and administration.


The drug should be administered intravenously, following the rules of administration technique. The dose of the drug should be selected individually, taking into account the possibility of different elimination rates.


If the patient is taking theophylline preparations orally, the dose of theophylline for parenteral administration should be reduced.


When the drug is administered, the patient is in a supine position; the doctor monitors blood pressure, heart rate, respiratory rate and general condition of the patient.


Intravenously administered at a rate of 30-50 drops per minute.


Derkast should be administered at a daily dose of 5 ml/kg of body weight (theophylline 10 mg/1 kg of body weight), on average 300-400 ML (600-800 mg of theophylline), divided into 3 injections. For cachexia and individuals with an initial low body weight, the daily dose should be reduced to 200-250 ML (400-500 mg of theophylline), while no more than 100-125 ML (200-250 mg of theophylline) should be administered during the first administration.


Therapeutic effects develop 5-15 minutes after intravenous administration and last up to 4-6 hours.


If palpitations, dizziness, or nausea occur, the rate of Drug Administration should be reduced.


The duration of treatment depends on the severity and course of the disease, sensitivity to the drug and ranges from several days to two weeks (but not longer than 14 days).


Do not use in patients with severe renal and/or hepatic insufficiency (see Section "contraindications").


Children. The drug should not be used in children (under 18 years of age).


Overdose.


With rapid intravenous administration, convulsions, arrhythmias, severe hypotension, angina pectoris, apathy, weight loss, mental disorders, and ECG changes are possible.


When plasma concentrations of theophylline exceed 20 mg/mL (110 mmol/L), nausea, vomiting (repeated vomiting, sometimes with blood, can lead to dehydration), diarrhea, agitation, tremor, arterial hypertension, hyperventilation, supraventricular and ventricular arrhythmias, hypotension, convulsions, metabolic disorders (hypokalemia, hypercalcemia, hypophosphatemia, hyperuricemia, hyperglycemia, metabolic acidosis, respiratory alkalosis). Other toxic manifestations include dementia, toxic psychosis, symptoms of acute pancreatitis, rhabdomyolysis with renal failure.


Treatment: depends on the severity of symptoms and includes discontinuation of the drug, correction of hemodynamics, stimulation of theophylline excretion from the body (forced diuresis, hemosorption, plasmosorption, hemodialysis, peritoneal dialysis), appointment of symptomatic agents, oxygen therapy, artificial ventilation. To eliminate seizures, diazepam is used intravenously. The use of barbiturates is impractical. In ventricular arrhythmias, the use of antiarrhythmic drugs that have a pro-convulsive effect, such as lidocaine, should be avoided because of the risk of exacerbation of seizures


For efficacy and safety, the serum concentration of theophylline should be maintained in the range of 10-15 mg/kg, if it is not possible to determine the concentration of theophylline in the blood, its daily dose should not exceed 10 mg/kg.


Adverse reactions.


From the central and peripheral nervous system: agitation, restlessness, restlessness, restlessness, sleep disorders, insomnia (especially in children), headache, dizziness, tremor, irritability, convulsions, hallucinations, delusions, epileptiform seizures, confusion/loss of consciousness, presyncopal state.


From the cardiovascular system: palpitations, cardialgia, arrhythmias, tachycardia, extrasystole, decreased blood pressure, heart failure, increased frequency of angina attacks, collapse (with rapid intravenous administration), shock.


From the urinary system: increased diuresis (due to increased glomerular filtration), in elderly patients – difficulty urinating (due to detrusor relaxation).


Immune system disorders: allergic reactions, including rash, urticaria, pruritus, angioedema, exfoliative dermatitis, anaphylactic shock, bronchospasm.


From the gastrointestinal tract: stimulation of gastric acid secretion, stomach pain, decreased appetite, diarrhea, intestinal atony, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer disease, nausea, vomiting.


Metabolic disorders: metabolic acidosis, hypokalemia, hypercalcemia, hyperuricemia, hyperglycemia, violation of the acid-base balance of the blood, rhabdomyolysis.


Local reactions: reactions at the injection site (compaction, hyperemia, soreness).


Others: fever, chills, facial hyperemia, feeling hot, excessive sweating, weakness, shortness of breath.


Expiration date. 2 years.


Storage conditions. Store at a temperature not exceeding 25°C. Do not freeze.  Keep out of reach of children.


Incompatibility. Do not mix with other medicinal products.

Tags: Potassium Chloride, Magnesium Chloride, Theophylline