Rhinofluimucil, spray 10 ml

Pharmacotherapeutic group:antagonist.
ATX code: R01AB08.

Pharmacological Properties

Pharmacodynamics

. The mucolytic and vasoconstrictor effect of Rinofluimucil® is a reflection of the pharmacological properties of its active ingredients.

Acetylcysteine has mucolytic activity due to free sulphhydryl group breaking disulphide bonds of mucus glycoproteins and having thinner effect on nasopharyngeal secretion.
Tuaminoheptane sulphate is a sympathomimetic amine having vasoconstrictor effect without systemic action when applied topically.
The two substances act synergistically to reduce intranasal resistance.

Pharmacokinetics

Absorption
After administration of the therapeutic dose (2 pressings of 50 µL) of Rinofluimucil®, the maximum plasma concentration of tuaminohepatan is reached between 0.25 h and 6.0 h.

Distribution
The mean Cmax value of tuaminoheptane after 2 50 µl pressings of Rinofluimucil® was 0.95 ng/ml, the mean Tmax value was 2 h.

Biotransformation
The metabolism of tuaminoheptane sulfate in human hepatocytes has been studied in vitro. No transformation occurred in human hepatocytes under in vitro conditions. The major metabolite of N-acetylcysteine is inorganic sulfate, which is excreted in the urine; other metabolites include taurine, cysteine, and N,N-diacetylcysteine. N-acetylcysteine is rapidly deacetylated to cysteine, which is incorporated into proteins. Excess cysteine enters the liver, where it is either metabolized for excretion or further modified.

Elimation
The average plasma half-life of tuaminoheptane after 2 50 µl pressings of Rinofluimucil® is 9.8 hours. Twelve hours after administration, tuaminoheptane was detected in all subjects (mean 0.42 ng/ml). Twenty-four hours after administration, the mean plasma concentration of tuaminoheptane was 0.30 ng/ml, but in most subjects the concentration was already below the limit of quantification (0.100 ng/ml).

Indications

Acute and subacute rhinitis with thick pus-mucous secretion, chronic rhinitis, vasomotor rhinitis, atrophic rhinitis, sinusitis.

Active ingredient

Acetylcysteine, Tuaminoheptane

Composition

100 ml of the solution contains
active ingredients: acetylcysteine – 1.0 g, tuaminoheptane sulfate – 0.5 g;
excipients: Benzalkonium chloride 0,01 g, 0,75 g hypromellose, 0,02 g dimethate, 0,02 g sodium dihydrophosphate, 0,3 g sodium hydrophosphate dodecahydrate, 0,3 g dithiothreitol 0,1 g, sorbitol 70% 2,0 g, mint flavoring 0,0188 g, ethanol 96% 0,31 g, sodium hydroxide 0,36 g, purified water up to 100 ml.

How to take, the dosage

The drug is injected into the nasal cavity in the form of a spray with a special nebulizer.

Adults: 2 doses of the spray (2 pressings of the valve) into each nasal passage 3 – 4 times a day.

Children over 6 years of age: 1 dose of the spray (1 pressure on the valve) in each nasal passage 3 to 4 times a day.

The duration of treatment should not exceed 7 days.

The recommended doses and course of treatment should not be exceeded without consulting a physician.

Interaction

Despite the low systemic absorption of tuaminoheptane, the following potential interactions should be considered when it is applied topically in the nasal cavity:

– Monoamine oxidase inhibitors (MAOIs), including reversible monoamine oxidase inhibitors (oMOIs): Increase risk of hypertensive crisis;

– Antihypertensive agents (including adrenergic neuron blockers or beta-blockers): may block the hypotensive effects of drugs;

– Cardiac glycosides: may increase the risk of cardiac arrhythmia;

– Ergot alkaloids: may increase the risk of ergotism;

– Parkinson’s disease drugs: May increase risk of cardiovascular toxicity;

– Oxytocin: may increase risk of hypertension;

Special Instructions

In patients with cardiovascular diseases, especially in patients with arterial hypertension, treatment should be carried out under medical supervision.
The drug should be used with caution in patients with asthma. Rhinofluimucil® should be used with caution in children taking into account that the drug is contraindicated in children under 6 years old.
Prolonged use of drugs that constrict blood vessels may impair the normal function of the nasal cavity mucosa and sinuses and cause addiction to the drug. Thus, frequent use for a long time may have adverse effects.
The drug should be used with caution in elderly patients with prostatic hypertrophy because of the risk of urinary retention.
Use, especially prolonged use of topical agents may

cause sensitization: in this case it is necessary to stop using the drug and, if necessary, to resort to appropriate treatment. If there is no complete therapeutic response within a few days, consult a physician; in any case, the duration of treatment should not exceed one week.
At the discretion of the physician, the drug may be combined with appropriate antibiotic therapy.
Tuaminoheptane sulfate may produce a positive doping test.
This drug is not intended for ophthalmic use.

Effects on the ability to drive vehicles, machinery
Has no effect on the ability to drive vehicles and machinery.
No specific studies have been performed, but patients should be informed that in some cases hallucinations have been reported.

Synopsis

Almost colorless transparent liquid with a characteristic minty slightly sulfurous odor.

Contraindications

– Hypersensitivity to the active substance or any of the excipients.

– Cardiovascular disease, including hypertension.

– A history of cerebrovascular disease, including the presence of relevant risk factors (due to alpha-sympathomimetic activity).

– A history of seizures.

– Pheochromocytoma.

– Closed-angle glaucoma.

– Concurrent use of other sympathomimetic nasal agents, including other nasal congestion agents.

Patients who are currently receiving or have received monoamine oxidase inhibitors, including reversible monoamine oxidase inhibitors A (RIMA) for 2 weeks.

Pituitary glandectomy or surgery with dura mater exposure.

– Children under 6 years of age.

With caution:

– Occlusive vascular disease.

– Diabetes mellitus.

– Hyperthyroidism.

– Asthma.

– Prostate hypertrophy because it can make it difficult to urinate.

– Use of beta-blockers.

– Prolonged use may cause recurrence of symptoms of blockage and drug-induced rhinitis.

Side effects

Frequent use in high doses may cause sympathomimetic side effects (such as hyperexcitability, palpitations, tremors, etc.) Sometimes there may be dryness in the nose and throat, as well as acne-like rashes. These reactions, however, disappear completely when you stop taking the drug.
The undesired reactions listed below may be associated with the drug Rinofluimucil® administration; the incidence of the specified undesired reactions is unknown (it is impossible to estimate on the basis of available data):

Overdose

In overdose in adult patients the following symptoms may be observed: arterial hypertension, photophobia, severe headache, tightness in the chest.

In overdose in children, hypothermia with a pronounced sedative effect may occur.

Treatment: symptomatic.

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Pregnancy use

Data from a limited number of patients who have taken this medication during pregnancy do not indicate adverse effects of acetylcysteine on pregnancy or fetal/newborn health. No other relevant epidemiologic data are available to date. Animal studies of acetylcysteine indicate no direct or indirect adverse effects with respect to reproductive toxicity.
There are no data on the use in pregnancy or animal studies of tuaminoheptane or a combination of acetylcysteine and tuaminoheptane.
Use of this medication during pregnancy is not recommended.
Although there is no information on excretion of acetylcysteine or tuaminoheptane into breast milk, the risk to breastfed children cannot be excluded. Use of this medication during breastfeeding is not recommended.