Kinedril

General characteristics. Structure:

Active agent: moksastina теоклат 25,0 mg, caffeine of 30,0 mg. 

Excipient: lactoses monohydrate, starch corn, talc, calcium stearate.

Pharmacological properties:

Pharmacological effect of the drug Kinedril® is caused by properties of the active ingredients which are its part – a moksastina of a teoklat and caffeine. Effect of drug begins in 10-15 min. and remains to 2 h.

Pharmacodynamics.

Moksastina теоклат is a blocker of H1-histamine receptors, has antihistaminic and sedative properties, renders antiemetic and anticholinergic effect, reduces dizziness. Action of a moksastin is caused by direct decrease in excitability of the emetic center and a hemoretseptorny starting zone and decrease in sensitivity of an organism to impulses which cause the acute disorders of vegetative functions which are shown in nausea and vomiting in sensitive people. 

Caffeine is the central psychostimulant, phosphodiesterase inhibitor which in the drug Kinedril® acts as the auxiliary active ingredient reducing sedative and somnolent action of a moksastin.

Firmakokinetika.

Moksastina теоклат is well soaked up from digestive tract. Relative bioavailability of a moksastin of a teoklat at oral administration ~ 55%. The maximum concentration in a blood plasma is reached in 45-70 min. after intake. It is quickly distributed in all bodies and body tissues, including TsNS. An elimination half-life – 4-8 h. It is metabolized, generally in a liver and it is removed in the form of metabolites (at children it is removed quicker, than at adults). With urine in not changed look it is removed very little. 

Caffeine is quickly absorbed throughout intestines. The maximum concentration in 50-75 min. after intake. Communication with proteins – 25-36%. It is quickly distributed in all bodies and body tissues, easily gets through a blood-brain barrier and a placenta. Distribution volume – 0,4-0,6 l/kg, at newborns is it more – 0,78-0,92 l/kg. A caffeine elimination half-life – 3-7 h. It is metabolized in a liver (about 80%). With urine a number of metabolites is removed (about 4% in the form of theophylline).

Indications to use:

Prevention of nausea and vomiting at the disease of the movement arising when using of vehicles (the car, the train, the airplane, the ship). 

Treatment and prevention of dizzinesses of various etiology (including at Menyer's disease, disturbance of activity of a vestibular mechanism).

Route of administration and doses:

Drug is appointed for intake. 

Adult: in the preventive purposes it is necessary to take 1 pill for 1 h before departure of transport. At a long trip it is possible to accept if necessary on 1/2-1 tablet in 2-3 h. The maximum dose – 3 tablets. 

To children: aged from 3 up to 6 years appoint 1/4 tablets; from 6 to 12 years – on 1/4-1/2 tablets; of 12 years is also more senior – on 1/2-1 tablets 2-3 times a day.

Features of use:

Кинедрил® can reduce ability to concentration of attention therefore it is not necessary to take over drug when performing of the work requiring special attention and bystry psychomotor reactions (including to drivers and pilots before the planned trip or flight).

Side effects:

From a nervous system: decrease in mood, weakness, drowsiness, disturbance of concentration of attention, visual disturbance (accommodation disturbance). 

From a GIT: diarrhea, a lock, abdominal pains, dryness in a mouth. 

From cardiovascular system: tachycardia, lowering of arterial pressure. 

Allergic reactions: rash, itch, dermahemia.

Interaction with other medicines:

Кинедрил® strengthens effect of somnolent, antipsychotic medicines (neuroleptics), anxiolytics, ethanol, spasmolysants and sympatholytics; reduces effect of indirect anticoagulants, peroral hypoglycemic medicines, Phenytoinum, glucocorticosteroids and hormonal contraceptives. Monoamine oxidase inhibitors and acetylcholinesterases raise, and barbiturates and derivatives of pyrazyl ketone reduce efficiency of the drug Kinedril®.

Contraindications:

Hypersensitivity to drug components, closed-angle glaucoma, a prostate hyperplasia, pregnancy, the lactation period, children's age (up to 3 years). 

Due to the existence in composition of lactose with rare hereditary diseases, such as intolerance of a galactose, deficit of lactase or glyukozo-galaktozny malabsorption it is contraindicated to patients to accept drug.

Overdose:

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

Treatment: gastric lavage, reception of absorbent carbon, symptomatic therapy.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Tablets of 25 mg + 30 mg. 

On 10 tablets in a blister strip packaging; on 1 or 2 blister strip packagings together with the application instruction in a pack from a cardboard. 

On 30 tablets in banks of light-protective glass, banks from glass melt or banks polymeric; each can together with the application instruction in a pack from a cardboard.