Kinedril^® (Tablets) Instructions for Use

Marketing Authorization Holder

FPK PharmVILAR, JSC (Russia)

Manufactured By

Noventis s.r.o. (Czech Republic)

ATC Code

A04AD (Other antiemetic drugs)

Active Substances

Caffeine (Ph.Eur. European Pharmacopoeia)

Moxastine (Rec.INN WHO Registered)

Dosage Form

Kinedril®

Tablets 25 mg+30 mg: 10, 20, or 30 pcs.

Dosage Form, Packaging, and Composition

Tablets are white, round, flat, with a cross-shaped score on one side.

Excipients: lactose monohydrate, corn starch, talc, calcium stearate.

10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
30 pcs. – jars (1) – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker used for motion sickness

Pharmacotherapeutic Group

Antiemetic agent

Pharmacological Action

The pharmacological action of the drug Kinedril^® is due to the properties of its active substances – moxastine theoclate and caffeine.

The drug’s effect begins within 10-15 minutes and lasts up to 2 hours.

Moxastine theoclate is a blocker of H₁-histamine receptors, has antihistamine and sedative properties, exerts an antiemetic and anticholinergic effect, and reduces dizziness.

The action of moxastine is due to a direct reduction in the excitability of the vomiting center and the chemoreceptor trigger zone and a decrease in the body’s sensitivity to impulses that cause acute disturbances of autonomic functions in sensitive individuals, manifested as nausea and vomiting.

Caffeine is a central nervous system stimulant, a phosphodiesterase inhibitor, which in the drug Kinedril^® acts as an auxiliary active substance that reduces the sedative and hypnotic effect of moxastine.

Pharmacokinetics

Moxastine theoclate is well absorbed from the gastrointestinal tract. The relative bioavailability of moxastine theoclate upon oral administration is 55%.

C_max in blood plasma is reached 45-70 minutes after oral administration.

It is rapidly distributed to all organs and tissues of the body, including the central nervous system. T_1/2 is 4-8 hours.

It is metabolized mainly in the liver and excreted as metabolites (excreted faster in children than in adults). Very little is excreted unchanged in the urine.

Caffeine is rapidly absorbed throughout the intestine. C_max is reached 50-75 minutes after oral administration.

Protein binding is 25-36%.

It is rapidly distributed to all organs and tissues of the body, easily penetrates the blood-brain barrier and placenta. The volume of distribution is 0.4-0.6 l/kg; in newborns it is larger – 0.78-0.92 l/kg.

T_1/2 of caffeine is 3-7 hours.

It is metabolized in the liver (about 80%). A number of metabolites are excreted in the urine (about 4% in the form of theophylline).

Indications

• Prevention of nausea and vomiting in motion sickness occurring when using transport (car, train, airplane, ship);
• Treatment and prevention of dizziness of various etiologies (including in Ménière’s disease, vestibular apparatus dysfunction).

ICD codes

Dosage Regimen

The drug is taken orally.

Adults for preventive purposes should take 1 tab. 1 hour before transport departure.

During a long journey, if necessary, 1/2-1 tab. can be taken every 2-3 hours.

The maximum dose is 3 tablets.

Children aged 3 to 6 years are prescribed 1/4 tab.; children aged 6 to 12 years – 1/4-1/2 tab.; children over 12 years – 1/2-1 tab. 2-3 times/day.

Adverse Reactions

Nervous system disorders: low mood, weakness, drowsiness, impaired concentration, vision disorders (impaired accommodation).

Digestive system disorders: diarrhea, constipation, abdominal pain, dry mouth.

Cardiovascular system disorders: tachycardia, decreased blood pressure.

Allergic reactions: rash, itching, skin hyperemia.

Contraindications

• Closed-angle glaucoma;
• Prostatic hyperplasia;
• Pregnancy;
• Lactation period;
• Children under 3 years of age;
• Hypersensitivity to the drug components.

Due to the presence of lactose in the composition, the drug is contraindicated in patients with rare hereditary diseases such as galactose intolerance, lactase deficiency, or glucose-galactose malabsorption.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Pediatric Use

Contraindicated in children under 3 years of age. Used in children over 3 years of age according to indications.

Special Precautions

Effect on the ability to drive vehicles and machinery

Kinedril^® may reduce the ability to concentrate, so the drug should not be taken when performing work requiring increased attention and rapid psychomotor reactions (including by drivers and pilots before a planned trip or flight).

Overdose

Symptoms: dizziness, drowsiness, weakness, loss of consciousness.

Treatment: gastric lavage, administration of activated charcoal, symptomatic therapy.

Drug Interactions

Kinedril^® enhances the effect of hypnotics, antipsychotic drugs (neuroleptics), anxiolytics, ethanol, antispasmodics, and sympatholytics; reduces the effect of indirect anticoagulants, oral hypoglycemic drugs, phenytoin, corticosteroids, and hormonal contraceptives.

MAO inhibitors and acetylcholinesterase inhibitors increase, while barbiturates and pyrazolone derivatives decrease the effectiveness of the drug Kinedril^®.

Storage Conditions

List B. The drug should be stored in a dry, light-protected place, out of the reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 4 years.

Dispensing Status

The drug is dispensed by prescription.

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.