Therofun

Terofun is a nasal decongestant drug with systemic effects. It belongs to the group of sympathomimetics.

The component triprolidine suppresses itching and systemic hyperemia that occur with endogenous histamine secretion.

Pseudoephedrine has a powerful anti-edematous effect, and at the same time has an indirect and direct sympathomimetic effect. The substance stimulates cardiac function, has a bronchodilating and vasoconstrictor effect, increases blood pressure, and also stimulates the activity of the central nervous system. [ 1 ]

When compared with ephedrine, it can be noted that pseudoephedrine is much less likely to cause an increase in blood pressure and the development of tachycardia, and also less likely to stimulate the functional activity of the central nervous system. [ 2 ]

Indications Therofun

It is used in the treatment of symptoms of rhinitis (this includes vasomotor rhinitis, which has an allergic origin), and also for flu and colds.

Release form

The drug is released in the form of tablets - 10 pieces in a cell package; in a pack - 2 such packages.

Pharmacodynamics

Triprolidine is a competitive blocker of histamine H1 endings from the alkylamine subclass. It has a minimal cholinolytic effect; it is used as a symptomatic substance – it eliminates manifestations associated with the secretion of histamine.

Pseudoephedrine helps stimulate the action of α-adrenergic receptors of the vessels located inside the mucous membrane of the respiratory tract, leading to their narrowing, which helps to remove swelling in the nasal mucosa, reduce tissue hyperemia and relieve nasal congestion, while increasing the throughput of the respiratory tract.

Pharmacokinetics

The pharmacokinetics of a drug is associated with the pharmacokinetic characteristics of each of its elements.

Pseudoephedrine and triprolidine are well absorbed in the intestine when taken orally.

Triprolidine is involved in synthesis with plasma protein. When taking 1 tablet, the intraplasmic Cmax level of triprolidine reaches approximately 5.5-6.0 ng/ml and is noted after 120 minutes. The half-life of triprolidine is approximately 3.2 hours. Metabolic components are formed during hydroxylation and oxidative dealkylation. Excretion of metabolites occurs with urine. Only approximately 1% of the administered triprolidine remains unchanged during excretion.

The Cmax values of pseudoephedrine are approximately 180 ng/ml and are recorded after 2 hours. The half-life of pseudoephedrine is 5.5 hours.

Some pseudoephedrine participates in intrahepatic metabolic processes with the formation of an inactive metabolic component. Pseudoephedrine together with its metabolites is excreted by the kidneys (approximately 55-75% is unchanged) within 24 hours. The pseudoephedrine secretion index increases as a result of urine acidification and decreases, respectively, with an increase in its pH.

Dosing and administration

It is necessary to take 1 tablet of the medicine 3-4 times a day.

The duration of the therapeutic cycle is selected by the doctor, often it lasts 4-5 days. If you miss a dose, you do not need to double the dose. The medicine is taken with milk or food.

• Application for children

Cannot be used in pediatrics.

Use Therofun during pregnancy

Terofun is prohibited for use in pregnant women.

Triprolidine and pseudoephedrine are secreted in breast milk in small amounts, but there is no information regarding their effect on the infant, so the drug is not used during breastfeeding.

Contraindications

Among the contraindications:

• severe intolerance associated with the elements of the drug;
• increased blood pressure (severe);
• severe form of coronary heart disease;
• coronary atherosclerosis;
• atherosclerosis affecting the cerebral vessels;
• SN;
• thyrotoxicosis;
• severe liver damage;
• use in combination with MAOIs or within 14 days after their withdrawal (this includes the antibacterial drug furazolidone). The combination of pseudoephedrine with the specified category of drugs can provoke an increase in blood pressure.

Side effects Therofun

Main side effects:

• lesions affecting the functioning of the nervous system: insomnia, headaches, tremors, dizziness and agitation. Occasionally, hallucinations, visual disturbances, convulsions, muscle weakness and drowsiness occur;
• problems with the functioning of the cardiovascular system: arrhythmia, tachycardia or collapse;
• allergy symptoms: itching, hyperemia in the chest area and epidermal rashes;
• Others: vomiting, diarrhea, dysuria, urinary problems, dyspnea, anorexia, xerostomia or dryness of the mucous membranes of the nasopharynx and throat.

Overdose

Intoxication causes tachycardia, cardiac arrhythmia, increased or decreased blood pressure, and hallucinations. In addition, mydriasis, weakness, dryness of the epidermis along with mucous membranes, tremor, vomiting, lethargy, and nausea are observed, as well as respiratory depression, hypertensive crisis, and changes in mental state.

Gastric lavage is performed, as well as the use of activated carbon. It is necessary to maintain the function of the cardiovascular system, as well as breathing. The rate of elimination of pseudoephedrine is potentiated by dialysis or forced diuresis.

Interactions with other drugs

The combination of the drug with tricyclics, sympathomimetics (including appetite suppressants with decongestants, as well as amphetamine-type psychostimulants) or MAOIs (furazolidone), which affect the catabolic activity of sympathomimetic amines, causes an increase in blood pressure.

Since Terofun contains the element pseudoephedrine, it is capable of partially neutralizing the antihypertensive effect of drugs that affect sympathetic activity (including betanidine, debrisoquine with bretilium, methyldopa, guanethidine and α- and β-adrenergic blockers).

Although objective data is lacking, people using the medication should avoid drinking alcohol or taking other sedatives that have a central mechanism of action.

Storage conditions

Terofun must be stored in a place protected from sunlight, moisture and access of small children. Temperature indicators – no more than 25°C.

Shelf life

Terofun can be used within 24 months from the date of manufacture of the pharmaceutical product.

Analogues

Analogues of the drug are Actifed, Orinol, Coldar with Terosim, Zestra and Trifed with a Mili spout, as well as Coldflu Plus.