medicalmeds.eu Medicines Antiemetic. Stimulator of motility of digestive tract. Primer

Primer

Producer: Mili Healthcare Ltd (Mili Helskere Ltd) Great Britain

Code of automatic telephone exchange: A03FA

Release form: Firm dosage forms. Tablets.

Indications to use: Not ulcer dyspepsia. Chronic gastritis. Nausea. Vomiting. Esophagitis. Lock. Anorexia.

General characteristics. Structure:

Active ingredient: 50 mg of an itoprid of a hydrochloride.

Excipients: starch corn, lactose, sodium of a kroskarmeloz, povidone-30, isopropyl alcohol, magnesium stearate, sodium of a kroskarmelloz, silicon dioxide colloid, sodium krakhmalglikolit, a gidroksimetilpropiltsellyuloza, the talc purified titanium dioxide, propylene glycol 6000.

The Gastrologichesky drug possessing spasmolytic action, influencing motility of a GIT and promoting acceleration of evacuation of gastric and intestinal contents.

Pharmacological properties:

Pharmacodynamics. Itoprida a hydrochloride – the antagonist of receptors of a dopamine of the D2 type, possesses antikholinesterazny action. Contacting a receptor D2, the dopamine suppresses activity of adenylatecyclase in smooth muscle cells of a GIT that causes its spasmolytic action. Dopamine brakes a peristaltics of a stomach and intestines, renders relaxation of the lower esophageal sphincter, strengthens a gastroesophagal and duodeno-gastric reflux, increases intragastric pressure, reduces blood prolactin level. Blocking receptors of a dopamine of D2, itoprid a hydrochloride increases activity of adenylatecyclase in smooth muscle cells of a GIT thereof the quantity of tsAMF and power providing a cell of smooth muscles increases. Such action creates the bases for activation of a physical activity and a tone of muscles of a GIT. Due to antagonism to D2 dopamine receptor anti-dopamine action can be shown in passing increase in prolactin of blood serum.

Acetylcholine interacts with receptor protein (M3 receptor) in a membrane of a smooth muscle cell. Receptor protein adenylatecyclase activates an internal receptor - a protein kinase that brings to фосфорилюваня proteins. This process causes increase in permeability of a membrane to calcium which stimulates reduction of unstriated muscles of a GIT. Action of acetylcholine is interrupted by hydrolysis, coming under the influence of acetylcholinesterase enzyme. Itoprida a hydrochloride, suppressing activity of acetylcholinesterase, promotes increase in an elimination half-life of endogenous acetylcholine, increase of its action in smooth muscle fabric and stimulates a physical activity and a tone of a GIT.

Itoprida a hydrochloride on the basis of its antagonism to dopamine D2 receptor, has tonic effect on smooth muscles of a GIT. Suppressing activity of acetylcholinesterase, stimulates a physical activity of a stomach at healthy and at pathology in relation to liquid and firm fraction, increases duration of antral and duodenal reductions, accelerates evacuation of gastric contents, improves a gastroduodenalna coordination, stimulates a passage of intestinal contents.

Pharmacokinetics. To 90% of an itoprid of a hydrochloride it is absorbed in intestines. The peak of concentration in a blood plasma comes in 45 minutes after reception of a tablet inside. Meal does not influence absorption of an itoprid of a hydrochloride. Does not get through a gemato-entsefalichesky barrier and into cells of the carrying-out system of a myocardium.

Gives in ацетилюванню and to oxidation in a liver by means of a flavinsoderzhashchy monooksidaza with formation of inactive metabolites which are removed by kidneys. The elimination half-life of an itoprid of a hydrochloride in an organism makes 6 hours. It is removed completely within 12 hours after reception of one dose. Does not kumulirut.

Indications to use:

Symptomatic treatment of the diseases caused by decrease in gastrointestinal motility namely:

• not ulcer dyspepsia,
• chronic gastritis,
• nausea and vomiting of a functional, organic, infectious origin,
• esophagitis of various origin,
• nausea and vomiting,
• lock,
• anorexia.

Route of administration and doses:

To adults and children 12 years are more senior appoint on 1 tablet 3 times a day before meal. To wash down with water, not to chew a tablet.

The average daily dose makes 150 mg, can be reduced taking into account clinical symptomatology, age of the patient and on doctor's orders. The daily dose should not exceed 800 mg.

The recommended course of treatment – 2 - 3 weeks.

Features of use:

Safety of use during pregnancy for the person is not established. Pregnant women should appoint drug in case the expected effect of treatment exceeds risk.

Itoprida a hydrochloride gets to milk of animals who nurse at use of therapeutic doses therefore for treatment feeding by a breast is recommended to be stopped.

Due to an opportunity dizziness to drive the car and to work with mechanical devices it is necessary with care.

Dose adjustment for patients of advanced age is not required, however elderly people with insufficiency have functions of a liver and kidneys, at use of the Primer it is necessary to be careful in connection with a possibility of more frequent emergence of side reactions.

With care to appoint the patient with glaucoma and adenoma of a prostate.

Side effects:

Allergic reactions in the form of skin rashes, an itch, a hyperemia of integuments are possible.

From the alimentary system: diarrhea, a lock, an abdominal cavity pain, increase in activity of liver enzymes are occasionally possible dryness in an oral cavity (ALT, nuclear heating plant, GGTP and ShchF).

From a nervous system: headache, vulnerability, sleeplessness, dizziness.

From endocrine system: increase in level of prolactin of blood is possible.

Treatment by the Primer is necessary prikorotit at emergence of a gynecomastia or galactorrhoea.

From system of blood: the neutropenia can seldom come to light. At identification of a leukopenia it is recommended to stop treatment by the Primer.

From kidneys: there can seldom be an increase in level of creatinine of blood, an urination delay at patients with a prostatauxe.

Others: dorsodynia and increased fatigue.

Interaction with other medicines:

That the system of P450 cytochrome is not involved in metabolism of an itoprid of a hydrochloride interaction with warfarin, diazepam, diclofenac, tiklopidiny, nifedipine, nikardipiny is not noted. Anticholinergics can reduce medical effect of the Primer. Antiulcerous drugs do not reduce pro-kinetic effect of the Primer.

Contraindications:

Hypersensitivity to drug components. Bleedings from a GIT, impassability or perforation of a GIT, the increased blood serum prolactin level. Children's age up to 12 years.