Rinostein^® (Spray) Instructions for Use

Marketing Authorization Holder

Grotex, LLC (Russia)

ATC Code

R01AB08 (Tuaminoheptane in combination with other drugs)

Active Substances

Acetylcysteine (Rec.INN registered by WHO)

Tuaminoheptane (Rec.INN registered by WHO)

Dosage Form

Rinostein®

Nasal spray 10 mg+5 mg/1 ml: 7 ml or 10 ml amp. or vial 1 pc. in a set with a bottle with a spray nozzle

Dosage Form, Packaging, and Composition

Nasal spray as a practically colorless, transparent solution with a characteristic minty and slightly sulfurous odor.

Excipients: sorbitol 70% – 20 mg, sodium dihydrogen phosphate dihydrate – 3.9 mg, ethanol 95% – 3.13 mg, sodium benzoate – 2 mg, disodium hydrogen phosphate dihydrate – 1.5 mg, dithiothreitol – 1 mg, sodium hyaluronate – 1 mg, disodium edetate – 0.2 mg, mint flavor – 0.188 mg, sodium hydroxide – to pH 5.5-7.0, water for injection – to 1 ml.

7 ml – ampoules of colorless glass (1) in a set with a bottle with a screw-on spray nozzle and a tracking label^× – contour cell packaging (1) ^× the tracking label may be affixed to the bottle – cardboard packs.
10 ml – ampoules of colorless glass (1) in a set with a bottle with a screw-on spray nozzle and a tracking label^× – contour cell packaging (1) ^× the tracking label may be affixed to the bottle – cardboard packs.
7 ml – dark glass bottles (1) – cardboard pack in a set with a spray nozzle.
10 ml – dark glass bottles (1) – cardboard pack in a set with a spray nozzle.

Clinical-Pharmacological Group

Drug with mucolytic and vasoconstrictive action for topical use in ENT practice

Pharmacotherapeutic Group

Drugs for the treatment of nasal diseases; decongestants and other drugs for topical use; sympathomimetics, combinations without corticosteroids

Pharmacological Action

Combined medicinal product for intranasal use. It has a mucolytic and vasoconstrictive effect.

Acetylcysteine has mucolytic activity due to the presence of a free sulfhydryl group, which, by breaking the disulfide bonds of mucus glycoproteins, has a thinning effect on the nasopharyngeal secretion.

Tuaminoheptane sulfate is a sympathomimetic amine; when applied topically, it has a vasoconstrictive effect without systemic effects.

These two substances act synergistically to reduce intranasal resistance.

Pharmacokinetics

After administration of a therapeutic dose, the C_max of tuaminoheptane in plasma is reached within the interval of 0.25-6 hours. The mean T_max was 2 hours.

The metabolism of tuaminoheptane sulfate in human hepatocytes was studied in vitro. Under in vitro conditions, no transformation occurred in human hepatocytes. The main 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.

The mean T_1/2 of tuaminoheptane in blood plasma after administration of a therapeutic dose is 9.8 hours. Twelve hours after administration, tuaminoheptane was detected in all subjects (mean value 0.42 ng/ml). Twenty-four hours after administration, the mean concentration of tuaminoheptane in blood plasma 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 purulent-mucous secretion; chronic rhinitis; vasomotor rhinitis; atrophic rhinitis; sinusitis.

ICD codes

Dosage Regimen

Administer intranasally only. Use 3-4 times per day or as directed by a physician.

Prior to first use, prime the spray pump by pressing down several times until a fine mist is produced.

Clear nasal passages before administration. Tilt head slightly forward.

Insert the spray tip into one nostril. Press down firmly and fully on the applicator to release one spray while breathing in gently through the nose.

Repeat the process for the other nostril.

Wipe the spray tip clean after each use. Replace the protective cap securely.

The maximum duration of continuous treatment is 7 days.

Do not exceed the recommended dosage and duration of use to avoid rebound congestion and medication-induced rhinitis.

If symptoms persist beyond one week, discontinue use and consult a physician.

This product is contraindicated in children under 6 years of age.

Avoid contact with eyes. If contact occurs, rinse thoroughly with water.

Adverse Reactions

Immune system disorders: hypersensitivity.

Psychiatric disorders especially with prolonged and/or frequent use – anxiety, hallucinations, delusions.

Nervous system disorders especially with prolonged and/or frequent use – headache, restlessness, agitation, insomnia, tremor.

Cardiovascular system disorders especially with prolonged and/or frequent use: palpitations, tachycardia, arrhythmia, arterial hypertension.

Respiratory system disorders especially with prolonged and/or frequent use: dryness in the nose and throat, sensation of discomfort in the nose, nasal congestion.

Gastrointestinal system disorders: nausea.

Skin and subcutaneous tissue disorders: urticarial rash, rash.

Urinary system disorders: urinary retention.

General disorders: with prolonged and/or frequent use: irritation at the application site, habituation.

Contraindications

Hypersensitivity to the components of the combination; cardiovascular diseases, incl. arterial hypertension; history of cerebrovascular diseases, incl. presence of corresponding risk factors (due to alpha-sympathomimetic activity); history of seizures; pheochromocytoma; angle-closure glaucoma; simultaneous use of other sympathomimetic nasal agents, incl. other decongestants; patients who are currently receiving or have received within 2 weeks MAO inhibitors type A; hypophysectomy or surgery with exposure of the dura mater; children under 6 years of age.

With caution

Occlusive vascular diseases; diabetes mellitus; hyperthyroidism; bronchial asthma; prostatic hypertrophy, as it may make urination difficult; use of beta-blockers; prolonged use may cause recurrence of congestion symptoms and drug-induced rhinitis.

Use in Pregnancy and Lactation

The use of this medicinal product during pregnancy and breastfeeding is not recommended.

Pediatric Use

The use of the drug is contraindicated in children under 6 years of age.

Geriatric Use

The drug should be used with caution in elderly patients with prostatic hypertrophy due to the risk of urinary retention.

Special Precautions

Long-term use of vasoconstrictor drugs may impair the normal function of the nasal mucosa and paranasal sinuses, and also cause habituation. Thus, frequent use over a long period of time may have an adverse effect.

Use with caution in elderly patients with prostatic hyperplasia due to the risk of urinary retention.

If there is no complete therapeutic response within a few days, a doctor should be consulted; in any case, the duration of treatment should not be more than 1 week.

As decided by the doctor, the use of this agent can be combined with appropriate antibacterial therapy.

Effect on ability to drive vehicles and operate machinery

No specific studies have been conducted, but patients should be informed that in some cases hallucinations have been reported.

Drug Interactions

Despite the low systemic absorption of tuaminoheptane, the following potential interactions should be taken into account when applied topically to the nasal cavity: MAO inhibitors, including reversible MAO inhibitors: increased risk of hypertensive crisis; antihypertensive agents (including adrenergic neuron blockers or beta-blockers): may block the hypotensive effect of the drugs; cardiac glycosides: may increase the risk of cardiac arrhythmia; ergot alkaloids: may increase the risk of cardiac arrhythmia; drugs for the treatment of Parkinson’s disease: may increase the risk of toxic effects on the cardiovascular system; oxytocin: may increase the risk of arterial hypertension.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.