MOTILIUM
Active material: Domperidone
When ATH: A03FA03
CCF: Antiemetic drugs of the central action, blocking dopamine receptors
ICD-10 codes (testimony): K20, K21, K30, R10.1, R11, R12, R14
At KFU: 11.06.02
Manufacturer: JOHNSON & JOHNSON LTD (Russia)
Pharmaceutical form, composition and packaging
◊ Lozenges white or nearly white, round.
| 1 tab. | |
| Domperidone | 10 mg |
Excipients: gelatin, mannitol, Aspartame, Mint essence, poloxamer 188.
10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
Pharmacological action
Antiemetics, Central dopaminovykh receptors Blocker. Domperidone – dopamine antagonist, with, Similarly, metoklopramidu and certain neuroleptic, protivorvotnami properties. However, unlike these drugs domperidone poorly crosses the Geb. Application of domperidone is rarely accompanied by the extrapyramidal side effects, especially in adults, but domperidone stimulates the release of prolactin from the pituitary. Protivorvotnoe effect, perhaps, due to a combination of peripheral (gastrokinetic) action and antagonism of dopamine receptors in the chemoreceptor trigger zone chemoreceptors.
The ingestion of domperidone increases the duration of antralnah and duodenal contractions, accelerates gastric emptying and enhances the lower esophageal sphincter pressure in healthy people.
Domperidone has no effect on gastric secretion.
Pharmacokinetics
Absorption
After intake of prandial domperidone is rapidly absorbed from the digestive tract. Cmax in plasma is approximately 60 m. Low absolute bioavailability of domperidone ingestion (about 15%) due to extensive primary metabolism in the wall of the intestine and the liver.
Domperidone should be 15-30 minutes before eating. Gipoacidnost′ gastric juice reduces removals of domperidone.
In preparation admission after eating to achieve Cmax need more time, and AUC increases slightly.
Distribution
The ingestion of domperidone and induces not koumouliruet not own metabolism. After taking domperidone for 2 week dose 30 mg / Cmax in plasma 90 minutes after the last technique was equal to 21 ng/ml and was almost the same, as after the first dose (18 ng / ml).
Plasma protein binding – 91-93%.
Domperidone concentrations in breast milk of lactating women in 4 times lower, than the respective concentrations in blood plasma.
Metabolism
Domperidone metabolised in the liver by hydroxylation and N-dealkylation.
Deduction
Excretion of urinarily and feces is 31% and 66% from the dose accordingly.
Displays the unaltered with faeces (10%) and urinarily (about 1%).
T1/2 from the blood plasma after administration of a single dose in healthy volunteers is 7-9 no.
Pharmacokinetics in special clinical situations
Patients with severe renal insufficiency (the level of serum creatinine more than 6 mg / dL) T1/2 domperidone increases with 7.4 h to 20.8 no, but the concentration of the drug in plasma below, than in healthy volunteers.
Testimony
is a complex digestive symptoms, often associated with delayed gastric emptying, Gastro-esophageal reflux, esophagitis (feeling overflows in epigastria, bloated feeling, pain in the upper abdomen, belching, flatulence, nausea, vomiting, heartburn);
-nausea and vomiting of functional, organic, infectious origin, caused by radiotherapy, drug therapy or a violation of the diet;
-nausea and vomiting, caused by dopamine agonists in case of their use in Parkinson's disease (such as l-dopa and bromocriptine).
Dosage regimen
At chronic dyspepsia adults and children senior 5 years appoint 10 mg (1 tab.) 3 times / day for 15-30 minutes before meals and, in case of need, before bedtime.
The maximum daily dose children aged 5 to 12 years is 2.4 mg / kg body weight, but not more 80 mg.
If necessary,, in the absence of the effect, to adults and children over the age of 12 years single dose can be doubled. The maximum daily dose – 80 mg.
At nausea and vomiting adults and children over 12 years appoint 20 mg (2 tab.) 3-4 times per day before meals and at bedtime. The maximum daily dose - 80 mg.
Children aged 5 to 12 years appoint 10 mg (1 tab.) 3-4 times per day before meals and at bedtime. The maximum daily dose - 2.4 mg / kg body weight, but not more 80 mg.
Motilium® in the form of tablets for resorption is shown only for adults and children weighing more than 35 kg, in children's practice should mainly use suspension of Motilium®.
At renal failure It is recommended that you increase the interval between administration of medication. Unnecessarily. a very small percentage of the drug is excreted kidneys in an unmodified form, It is unlikely that there is a need for a single dose adjustment in patients with renal insufficiency. However, when reappointing the reception frequency should be reduced to 1-2 times/day depending on the severity of renal failure, You may also need to reduce the dose of.
Rules for the use of pills for resorption
Pills for resorption are available in blister packs. Because the pills are quite fragile, to avoid damage, you should not push through foil.
In order to get hold of the blisters the tablet should take the foil at the edge and completely remove it from the cell, which is a tablet. Then gently push the bottom and remove the Tablet from the package. The tablet should be put on language. Within seconds it disintegrate on the tongue and it can be swallowed with saliva, not drinking water.
Side effect
From the digestive system: seldom-digestive disorders; in a few cases – transient intestinal cramps.
CNS: extrapyramidal symptoms (rarely – children; in a few cases – adult); fully reversible and disappear after the treatment.
On the part of the endocrine system: hyperprolactinemia is possible, rarely leads to galactoree, Gyno, amenorrhea.
Allergic reactions: rarely – rash, hives.
Contraindications
- Gastro-intestinal bleeding;
— mechanical obstruction or perforation, in which stimulation of gastric motor function can be dangerous;
-prolactin-which secretes pituitary tumor (prolactinoma);
-simultaneous oral ketoconazole;
- Children up to age 5 years (for a given dosage form);
- Hypersensitivity to the drug.
FROM caution should designate product in patients with hepatic insufficiency (given the high degree of metabolism in the liver of domperidone).
Pregnancy and lactation
Data on the use of Motiliuma® when pregnancy is not enough.
To date there are no data on the increased risk of malformations in human. Nonetheless, use Motiliuma® Pregnancy is possible only in cases, when the expected benefit of therapy for the mother outweighs the potential risk to the fetus.
Women's concentration in breast milk is domperidone 10-50% from the appropriate concentration in plasma and does not exceed 10 ng / ml. The total number of domperidone, èkskretiruemogo breast milk-less 7 mcg/day when applying the maximum permissible doses. Unknown, whether this level of negative impact on newborns. Therefore, if you must use Motiliuma® lactation breastfeeding should be discontinued.
Cautions
When combined with the application of Motiliuma® antatsidnami or antisekretornymi drugs the past should be taken after meals, ie. they should not be taken concurrently with Motiliumom®.
With long-term therapy patients with kidney disease should be kept under regular observation.
Effects on ability to drive vehicles and management mechanisms
Motilium® does not affect driving ability and working with machinery.
Overdose
Symptoms: drowsiness, disorientation and extrapyramidal reactions, especially in children.
Treatment: application of activated carbon and closely monitored. Anticholinergic agents, preparations, used to treat Parkinson's disease, or antihistamines may be effective when an extrapyramidal reactions.
Drug Interactions
Anticholinergic drugs can neutralize the action of Motiliuma®.
Bioavailability Motiliuma® the ingestion decreases after a previous admission zimetidina or sodium bicarbonate. Do not take antacids and antisecretory drugs simultaneously with Motiliumom®, tk. they reduce its bioavailability.
The main metabolic pathway of domperidone transformation occurs when the participation of izofermenta CYP3A4. Based on in vitro studies we can assume, that, together with the use of domperidone and medicines, significantly inhibiting this CYP, can raise the level of domperidone in plasma. Examples the following are izofermenta CYP3A4 inhibitors medications: antifungals azolovogo series, macrolide antibiotics, HIV protease inhibitors, nefazodon.
Study on healthy volunteers interact with domperidone ketokonazolom revealed, that ketoconazole inhibits CYP3A4-dependent primary metabolism of domperidone, resulting in approximately threefold increase withmax and AUC of domperidone in Plateau phase. The study of interaction between ketoconazole and domperidone shows, that with domperidone in the dose 10 mg 4 times/day and dose ketoconazole 200 mg 2 times/day observed elongation QT interval on 10-20 Ms. In monotherapies domperidonom in similar doses, and when taking a daily dose of 160 mg (what in 2 times higher than the maximum permissible daily dose) There were no clinically significant changes of QT interval.
Theoretically, (tk. the drug has gastrokinetičeskim activity) Motilium® could affect the absorption of simultaneously used drugs, in particular, drugs with a slow release of the active substance or preparations, covered with kishechnorastvorima liner. However, the use of domperidone in patients against the backdrop of the admission of paracetamol or tailored therapy digoxinom will not affect the level of these drugs in the blood.
Motilium® can also be combined with neiroleptikami, which it doesn't increases; dopaminergic agonists of receptors (bromocriptine, levodopa), unwanted peripheral effects which, such as digestive disorders, nausea, vomiting, it suppresses, not neutralizing their basic properties.
Conditions of supply of pharmacies
The drug is resolved to application as an agent Valium holidays.
Conditions and terms
The drug should be stored out of reach of children at temperature from 15 ° to 30 ° C. Shelf life - 2 year.
