Naulithium

Naumilium is a drug used to eliminate abnormalities in the function of the digestive tract. It is a stimulant of intestinal peristalsis.

Indications of the naumilum

It is used to eliminate vomiting with nausea, which are observed in a period of less than 48 hours.

[1], [2]

Release form

The drug is produced in tablets, 10 pieces inside a blister pack. The pack contains 1 or 3 such packages.

Pharmacodynamics

Domperidone is a dopamine antagonist with antiemetic effects. This element weakly penetrates the BBB, when it is used only rarely are extrapyramidal symptoms (especially in an adult), although it stimulates the secretion of prolactin from the pituitary gland. The antiemetic effect of the drug may be due to a combination of peripheral effects, and antagonism in addition to the dopamine endings within the trigger region of the chemoreceptors located outside the BBB, in the posterior part (area postrema).

Tests performed on animals, and in addition, low values of drugs, noted inside the brain, show that domperidone basically has only a peripheral effect on dopamine ends.

Studies conducted with the participation of people demonstrated that after oral administration, domperidone increases the level of pressure inside the lower part of the esophagus, and besides it improves the processes of anthroduodenal motility and promotes acceleration of gastric emptying.

The element has no effect on the secretory function of the stomach.

[3], [4], [5], [6], [7], [8]

Pharmacokinetics

Domperidone is rapidly absorbed when the tablet is taken orally (on an empty stomach). Peak plasma parameters are noted after the 0.5-1 hour. Low bioavailability values of drugs (about 15%) are due to extensive metabolic processes at the first passage through the liver and intestinal wall. In a healthy person, the bioavailability of a drug increases with use after eating, but those with problems in the work of the digestive tract need to use Naumilium 15-30 minutes before eating.

A reduced level of gastric pH leads to a decrease in the absorption of domperidone. Reduction in the bioavailability after the use of drugs inside occurs if before taking baking soda or cimetidine. If you take the tablet inside after eating, its maximum absorption slows down a little, and the AUC indicator rises slightly.

After oral administration, domperidone does not cumulate and does not induce its own metabolic processes. Peak values within the blood plasma after 1.5 hours (21 ng / ml) after 14 days of use in a dose of 30 mg / day were almost identical to those after the first dose (18 ng / ml). The drug is synthesized with blood plasma proteins by 91-93%.

Studies of drug distribution processes conducted on animals using a substance labeled with a radioactive isotope have demonstrated that it is well distributed within tissues, although it has a low concentration index within the brain. In addition, in animals, small amounts of medicine pass through the placenta.

The hepatic metabolism of domperidone is rapid and extensive. It is carried out by means of hydroxylation processes, and besides N-dealkylation. Tests of metabolic processes in vitro with the use of a diagnostic inhibitor revealed that the element CYP3A4 is the main form of the hemoprotein P450 involved in N-dealkylation, and the components CYP3A4 and CYP1A2 and CYP2E1 are involved in the aromatic hydroxylation of the active drug LS.

Excretion with feces and urine is 66% and 31% of the ingested portion, respectively. Only a small part of the substance is excreted as an unchanged element - about 1% in urine and 10% in feces. The half-life of drugs from the plasma with a single dose - about 7-9 hours (a healthy person). In people with kidney failure of a serious nature, this period is longer.

Dosing and administration

You need to consume the medicine before eating, because when you eat after eating, there is a slight delay in its absorption. The duration of therapy with Naumilium may be a maximum of 7 days.

To relieve the manifestations of vomiting with nausea, adolescents from 16 years and adults should take 1-well tablet (10 mg) three times a day. The maximum size of a daily portion is just 3 tablets - 30 mg.

Without consultation with the doctor, the medicine can be taken only for 48 hours.

Use of the naumilum during pregnancy

There are only limited information on the post-marketing use of Naushilium in pregnant women. Because of this, the drug is allowed to be used only in cases when the doctor believes that the benefits of taking it for the mother will be more likely than the possibility of complications in the fetus.

Tests revealed that the drug is able to pass into the mother's milk. The amount of a substance that can penetrate the baby through the mother's milk is insignificant. The maximum possible relative portion for the baby is approximately 0.1% of the dosage size adopted by the mother, adjusted for weight.

There is no evidence as to whether Domperidone is harmful to the child, which is why it is recommended that breastfeeding be refused for the duration of drug use.

Contraindications

Among the contraindications:

• the presence of intolerance with respect to the drug or its ancillary components;
• prolactinoma;
• presence of disorders of renal or hepatic activity;
• people who have a prolongation of QT-interval values, which is the main factor of heart disorders or diseases;
• presence of liver failure.

Do not use the drug in cases where stimulation of gastric motility may be dangerous - for example, if there is bleeding in the gastrointestinal tract, perforation or mechanical blockage.

[9], [10], [11]

Side effects of the naumilum

Use of the drug may cause the occurrence of such adverse symptoms:

• Immune disorders: single signs of allergy appear, among which anaphylaxis and hypersensitivity;
• disorders in the endocrine system: occasionally increased prolactin levels;
• mental disorders: there is a single feeling of excitement, nervousness, anxiety or irritability, and besides this, the state of depression and weakening or complete disappearance of libido;
• problems with the function of the NS: there is a single feeling of thirst, lethargy or drowsiness, dizziness, migraine, insomnia, acacia, headaches and extrapyramidal symptoms;
• symptoms on the part of the CCC: puffiness, ventricular arrhythmias in severe form, palpitations, prolongation of QT-interval values, changes in the rhythm of cardiac contractions and heart rate develop sporadically, and in addition increase in blood pressure and BCC;
• disorders in the gastrointestinal tract: occasionally there are gastrointestinal disorders, including regurgitation, abdominal pain, burning sensation, nausea, constipation and changes in appetite. Single short-term spasms in the intestine or stomach, diarrhea, dryness of the oral mucosa and eructation occur;
• disturbances of visual function: development of an oculogic crisis is possible;
• lesions of the subcutaneous layers and epidermis: single appear rashes or itching. Perhaps the appearance of edema Quincke or urticaria;
• problems affecting reproductive function and mammary glands: occasionally there is gynecomastia, galactorrhea, increased sensitivity of the mammary glands, pain and swelling in their area or discharge from them, and in addition hot flashes, lactation, amenorrhea and unstable menstrual cycle;
• damage to the function of ODD and connective tissues: occasionally painful sensations occur in the legs;
• disorders of urinary excretion: single-noted painful and frequent urination or delay, and besides dysuria;
• systemic disorders: asthenia develops occasionally;
• others: the development of stomatitis, chills, conjunctivitis, hyperhidrosis, and in addition to this cramps in the calf muscles;
• changes in the indications of laboratory tests: the cholesterol, AST or ALT values increase individually. Occasionally the prolactin index inside the blood increases and there is a deviation from the normal values of functional liver tests.

Since the pituitary gland is located outside the BBB, domperidone is capable of provoking an increase in prolactin levels. Occasionally, such hyperprolactinemia can cause adverse neuroendocrine symptoms (amenorrhea, galactorrhea, or gynecomastia).

At the stage of postmarketing tests, there was no difference between the profiles of drug safety in adolescents and adults (except for extrapyramidal disorders and other signs, excitations and seizures associated with the function of the central nervous system, and observed mainly in adolescents).

Overdose

Among the signs of poisoning - agitation, convulsions, a sense of disorientation or drowsiness, frustration and extrapyramidal disorders.

Do domperidone there is no antidote, so with severe intoxication, you should perform gastric lavage (in the period not more than 60 minutes after consuming drugs) and give the patient activated charcoal. In addition, continuous monitoring of the victim and supportive activities will be required. Holinolitic drugs and drugs that help with Parkinson's disease are effective in controlling extrapyramidal symptoms.

[12], [13], [14],

Interactions with other drugs

It is forbidden to combine erythromycin, ketoconazole and other potent drugs that slow down the activity of the element CYP3A4 with Naushilum, and in addition, drugs prolonging the QT-interval (among them posakonazol, itraconazole with fluconazole, ritonavir, telaprevir, telithromycin, saquinavir with clarithromycin, voriconazole and amiodarone).

Holinolitic medicines can neutralize the anti-diarrheal effect of domperidone.

If combined use with antisecretory agents or antacids is required, it is recommended that they be consumed after meals, and not before (joint taking with domperidone is prohibited, because these medications reduce its bioavailability when administered orally).

Combine domperidone is allowed with such means:

• neuroleptics, since it potentiates their properties;
• dopaminergic agonists (such as bromocriptine and L-dopa), because it inhibits their negative peripheral effects (such as digestive disorders and vomiting with nausea), while not neutralizing their underlying effect.

[15], [16]

Storage conditions

Naumilium should be kept in a place that is closed from access by small children, at temperature values not exceeding 30 ° C.

[17]

Shelf life

Naumilium can be used for 3 years since the release of the drug.

Application for children

The drug is prohibited for use in children under 16 years of age.

Domperidone for children is prescribed only in the minimum acceptable effective portions.

Analogues

Analogues of the drug are such drugs as Metoclopramide, Cerukal and Itomed with Motilium, Motilakom and Passagex.

Reviews

Naumilium is considered a very good antiemetic. In most reviews, it is noted for its high efficacy in stopping nausea with vomiting, which can not be stopped with other medications.