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Uniphyl Cr (Theophylline)


uniphyl-cr

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Uniphyl Cr (Theophylline) belongs to phosphodiesterase inhibitor, a purine derivative. It increases cAMP accumulation in tissues blocking adenosine receptors. It decreases the entry of calcium ions by means of cell membranes’ channels. It decreases the contractile activity of smooth muscles.

This substance relaxes bronchial muscles and blood vessels. It also provides a peripheral vasodilating effect, enhances renal blood flow. It also contributes to the appearance of a moderate diuretic effect. It balances the mast cell membrane, suppresses the release of triggers of allergic reactions. Uniphyl Cr enhances mucociliary clearance, provokes diaphragm’s contraction, improves the respiratory and intercostal muscles’ function by stimulating the respiratory center.

This drug brings the respiratory function to the norm, helps to saturate the blood with oxygen and reduce the concentration of carbon dioxide. It has a property to stimulates the respiratory centers. It has an effect on the cardiac activity increasing the strength of cardiac contractions and heart rate, coronary blood flow and the oxygen demand of myocardium. It decreases blood vessels’ tone and pulmonary vascular resistance. It lowers blood pressure in the pulmonary circulation. It increases renal blood flow and erythrocyte resistance to deformation. It ensures providing a moderate diuretic effect. It expands the extrahepatic biliary tract. It inhibits platelet aggregation, reduces blood clot formation and normalizes microcirculation.

Indications

Buy Uniphyl Cr if you have one of this broncho-obstructive syndrome of various genesis:

  • bronchial asthma (a drug of choice for exercise-induced asthma and as an additional remedy for other forms of bronchial asthma);
  • COPD (chronic obstructive bronchitis, pulmonary emphysema);
  • pulmonary hypertension;
  • pulmonary heart;
  • edematous syndrome of renal genesis (as part of combination therapy);
  • sleep apnea.

Mode of application

The dosage is selected individually. The initial dose is 400 mg per day. In the case of a good tolerance, the dose can be increased by approximately 25% from the initial every 2-3 days until the optimum therapeutic effect is achieved.

The maximum daily dose that can be used without controlling the concentration of theophylline in the blood plasma:

  • children aged 3-9 years – 24 mg/kg per day;
  • 9-12 years – 20 mg/kg per day;
  • 12-16 years – 18 mg/kg per day;
  • patients aged 16 years and older – 13 mg/kg per day or 900 mg per day.

If, when used in the indicated doses, symptoms of toxic action appear or there is a need to further increase the dose (due to the insufficient therapeutic effect), it is recommended to control theophylline concentration in the blood plasma. The optimal therapeutic concentration of theophylline – 10-20 mg/ml. At lower concentrations, the therapeutic effect is mild, at large concentrations, there is no significant increase in the therapeutic effect, while the risk of side effects increases significantly. The frequency of administration depends on the dosage form.

Overdose

Symptoms of an overdose include anxiety, motor agitation, insomnia, tremor, seizures, photophobia, flushing of face skin, tachypnea, ventricular arrhythmias, tachycardia, decreased appetite, gastralgia, nausea, vomiting (including the rash of blood, reduced vomiting, stomach ache, nausea, vomiting, nausea, diarrhea.

When patients receive very high doses of this drug, patients may experience clouded consciousness, low blood pressure, epileptoid seizures, renal failure accompanied by myoglobinuria, hypoxia, skeletal muscle necrosis, hypokalemia, hyperglycemia, metabolic acidosis. In this case, the drug is excreted through gastric lavage. At the next stage, it is recommended to take activated carbon and laxatives, forced diuresis, intestinal lavage with a mixture of electrolytes and polyethylene glycol, plasma sorption, hemosorption, hemodialysis (its effectiveness is insignificant, and peritoneal dialysis is not fully effective).

Symptomatic therapy is also prescribed: for example, ondansetron or metoclopramide is administered intravenously with severe nausea and vomiting. With the development of a convulsive seizure, it is necessary to monitor the airway and oxygen therapy. To stop an attack, diazepam is administered intravenously at a dose of 0.1–0.3 mg/kg (no more than 10 mg).

Side effects

  • Central nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor.
  • Cardiovascular system: heartbeat, tachycardia (including the fetus when taken in the third trimester), arrhythmias, a decrease in blood pressure, cardialgia, an increase in the frequency of strokes.
  • Digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with prolonged use – loss of appetite.
  • Allergic reactions: skin rash, itching, fever.
  • Other: pain in the chest, tachypnea, the sensation of hot flashes to the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

Side effects decrease with dose reduction.

Contraindications

  • Epilepsy;
  • Increased convulsive readiness;
  • Gastric ulcer and duodenal ulcer in the acute phase;
  • Children’s age up to 3 years;
  • Hypersensitivity to theophylline.

Uniphyl Cr is used with caution in the following cases:

  • gastroesophageal reflux;
  • bleeding from the gastrointestinal tract in recent history;
  • gastric ulcer and 12 duodenal ulcer history; hepatic and/or renal failure;
  • frequent ventricular premature beats;
  • hypertrophic obstructive cardiomyopathy;
  • common vascular atherosclerosis;
  • chronic heart failure;
  • severe coronary insufficiency (angina pectoris, acute phase of myocardial infarction);
  • prostatic hypertrophy;
  • increased convulsive readiness;
  • uncontrolled hypothyroidism or thyrotoxicosis;
  • prolonged hyperthermia;
  • pregnancy;
  • elderly age.

Drug interactions

With simultaneous use of theophylline with sympathomimetics, there is a mutual enhancement of their action; with beta-blockers and lithium preparations – their action mutually decreases. The intensity of theophylline effect may decrease (due to an increase in its clearance) while being used with phenobarbital, rifampicin, isoniazid, carbamazepine, sulfinpyrazone, phenytoin. The intensity of its action may increase (due to a decrease in its clearance) with simultaneous use with macrolide antibiotics, allopurinol, beta-blockers, cimetidine, hormonal contraceptives for oral administration, isoprenaline, lincomycin and during vaccination against influenza. Xanthine derivatives can potentiate hypokalemia caused by the action of beta2-adrenoreceptor stimulants, corticosteroids and diuretics.