Unicontin

Unicontin is a drug that affects the respiratory system, based on theophylline. It is often used in medical practice for respiratory tract obstruction. Drug affiliation: antispasmodics, xanthines.

The drug Unicontin is not freely available and is available only with a prescription from a doctor.

Indications Unicontin

Unicontin is prescribed for obstructive pulmonary pathologies:

• for bronchial asthma;
• for chronic obstructive bronchitis;
• in pulmonary emphysema.

The drug can also be used for the complex treatment of pulmonary hypertension, pulmonary heart disease, and sleep apnea.

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Release form

Unicontin is available in tablet form in a dosage of 400 or 600 mg.

The 400 mg tablet is light, round, flattened, has a dividing notch on one side, as well as engraving MM and U/400.

The 600 mg tablet is white, oblong, convex on both sides, has a dividing line and engravings MM and U/600.

Blister contains 10 tablets. Cardboard packaging consists of 10 blisters.

Unicontin is a prolonged-release drug. Each tablet contains the active ingredient theophylline, as well as additional ingredients: povidone, hydroxyethylcellulose, cetostearyl alcohol, talc, magnesium stearate.

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Pharmacodynamics

The active substance Unicontin is a bronchodilator from the methylxanthine series. It has a stimulating effect on the central nervous system, cardiac muscle and skeletal muscles, helps relieve spasms of smooth muscle fibers, and is also a mild diuretic.

The mechanism of action of the active component is based on its property to suppress the enzyme phosphodiesterase. Theophylline also affects the smooth muscle structures of the coronary arterial vessels, the blood supply of the muscular system and urothelial cells, has a relaxing effect on the uterine muscles, the sphincters of the esophagus and biliary tract.

Unicontin improves blood flow from the right ventricle, which has a positive effect on the degree of cardiac output, on the reduction of resistance in the pulmonary vascular system and the reduction of intrapulmonary pressure. At the same time, the respiratory center is stimulated, the muscles of the diaphragm are activated, urine output increases, and the production of catecholamines by the adrenal glands increases.

Peak efficacy is observed when plasma concentrations reach 5 to 20 mcg/ml.

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Pharmacokinetics

The pharmacokinetic properties of Unicontin may differ depending on the individual characteristics of the patient, since the presence of additional pathologies and the use of certain drugs can significantly affect the kinetic mechanisms. For this reason, experts recommend monitoring the amount of the drug in the blood serum, especially in patients with severe diseases or with prolonged treatment with this drug.

The active ingredient Unicontin is well absorbed in the digestive system. A constant content of the active component is established after 2-3 days from the start of taking the drug. Theophylline soon spreads to almost all tissues and biological environments of the body. Metabolism occurs in the liver, and one of the metabolic products also has a bronchodilator capacity.

Metabolic products and residues of the active ingredient are excreted through the urinary system.

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Dosing and administration

The dosage of Unicontin is prescribed strictly individually, which is associated with some features of the metabolism of patients, their age and weight category. The tablet is taken once a day (in the morning or in the evening), during meals. If the patient took the first dose of the drug on an empty stomach, then in the future he should adhere to this regimen.

The tablet is taken whole, without crushing or chewing. If necessary, the tablet can be divided along the specially applied notch.

Initial dosage of the drug for patients with normal creatinine clearance:

Frequency of dosage changes	Children weighing less than 45 kg	Children weighing over 45 kg and adult patients
Initial dosage	From 12 to 14 mg/kg/day, but not more than 300 mg/day	From 300 to 400 mg/day
After 3 days the dosage is increased	16 mg/kg/day, but not more than 400 mg/day	From 400 to 600 mg/day
After another 3 days, if necessary	20 mg/kg/day, but not more than 600 mg/day	If necessary, more than 600 mg/day is prescribed under strict monitoring of serum concentrations.

In case of impaired creatinine clearance, the dosage of the drug in pediatric patients under 15 years of age should not exceed 16 mg/kg/day (but not more than 400 mg/day).

For patients with changes in creatinine clearance aged 16 years and older, the daily dosage of the drug should not exceed 400 mg.

Selection of dosage depending on the content of the drug in the blood serum:

Maximum serum concentrations of the drug	Dosage selection
Less than 9.9 mcg ml	If the drug is not effective enough, the dosage can be increased by 25%.
From 10 to 14.9 mcg/ml	The current dosage is prescribed with repeated concentration analyses every six months or a year.
From 15 to 19.9 mcg ml	It is necessary to consider reducing the dosage of Unicontin by 10%, even if it is well tolerated.
From 20 to 24.9 mcg ml	It is necessary to reduce the dosage of Unicontin by 25% even with normal tolerability, with a repeat concentration analysis after 3 days.
From 25 to 30 mcg/ml	It is necessary to skip one dose of the drug, and reduce the following dosages by 25%. After 3 days, repeat the concentration analysis.
More than 30 mcg/ml	The dosage should be reduced by at least 50%, followed by a repeat analysis of the content after 3 days.

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Use Unicontin during pregnancy

It has been proven that this Unicontin is able to pass through the placental barrier and be detected in mother’s milk.

During pregnancy, Unicontin can be taken only if the expected benefit to the woman is more important than the possible risk to the future baby. If the drug is prescribed to a pregnant woman, the treatment is carried out under constant monitoring of the level of the active substance in the blood plasma, which will allow careful adjustment of the dosage. It is recommended to refrain from treatment with this drug in the late stages of pregnancy, due to its ability to prevent labor contractions of the uterus.

When breastfeeding, a woman should closely monitor the baby for any allergic reaction to the drug, excessive excitement or insomnia. If such symptoms appear, you should immediately contact a doctor who will decide whether to cancel Unicontin or stop lactation.

Contraindications

• Allergic sensitivity to any of the components of the drug, or to drugs of the xanthine group.
• Acute period of myocardial infarction.
• Tachycardia with irregular heart rhythm.
• Myocardial hypertrophy, obstructive form of cardiomyopathy.
• Hypertension.
• Tendency to epilepsy.
• Increased functionality of the thyroid gland.
• Gastric ulcer and duodenal ulcer.
• Severe liver failure.
• Children under 12 years of age.

Side effects Unicontin

In the initial stages of treatment, transient minor side effects may sometimes be observed:

• the appearance of heartburn, nausea, diarrhea, pain in the abdominal area;
• increased heart rate;
• dizziness, headaches, sleep disorders, feelings of anxiety, agitation, irritability;
• allergic reactions in the form of skin rashes, itching and redness of the skin.

In more severe cases, and in particularly sensitive patients, a sharp drop in blood pressure, heart rhythm disorder, hand tremors, convulsions, and sleep disorders are possible. Sometimes the body temperature may rise, and diuresis may increase.

Hypokalemia, hypercalcemia, hyperglycemia, and elevated uric acid levels are detected in the blood.

Overdose

Symptoms of overdose may occur when the active substance content in the blood serum is more than 110 μmol/liter.

A typical picture might be as follows:

• trembling in the limbs;
• attacks of nausea and vomiting;
• pain in the epigastric region;
• diarrhea;
• rave;
• heart rhythm disorders;
• hypotension;
• convulsions.

Overdose symptoms may appear suddenly, without prior worsening of the condition.

As a help, it is often sufficient to reduce the dosage or temporarily suspend the drug. If the violations are positioned as severe, then the dosage is reduced gradually, under the control of the concentration of the active component in the blood plasma.

In case of intoxication, gastric lavage is prescribed followed by administration of sorbent drugs.

Throughout the recovery period, it is necessary to monitor blood pressure, heart rate and respiratory movements, as well as the content of the active component in the plasma.

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Interactions with other drugs

During the course of therapy with Unicontin, it is prohibited to drink alcoholic beverages. You should also limit foods and liquids containing methylxanthine, which is present in coffee drinks, strong tea, cocoa, cola, and chocolate products.

The effect of Unicontin may be more pronounced when taken simultaneously with allopurinol, cimetidine, phenylbutazone, fluoroquinolone, furosemide, isoniazid, calcium antagonist drugs, lincomycin, macrolide antibiotics, paracetamol, pentoxifylline, oral contraceptives, propranolol, ranitidine, and anti-influenza serum. When combined with any of the listed drugs, it is important to periodically analyze the content of the active component of Unicontin in the blood serum.

When taking Ciprofloxacin at the same time, the dosage of Unicontin should be reduced by approximately 60%, and when taking Enoxacin – by 30%.

The effect of Unicontin is reduced with the simultaneous use of antiepileptic drugs, sleeping pills, magnesium hydroxide, rifampicin, and nicotine.

Unicontin may become ineffective when taken in combination with β-receptor antagonists.

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Storage conditions

The medicine is stored at a temperature of no more than +25°C, in a place protected from sunlight, out of the reach of children.

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Shelf life

The shelf life of the medicine is up to 3 years.

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