Increases the duration of peristaltic contractions of the antrum of the stomach and duodenum, accelerates gastric emptying, when the retardation of the process, increases the tone of the lower esophageal sphincter, eliminates the development of nausea and vomiting.
Domperidone does not penetrate the blood-brain barrier, so the use of domperidone is rarely accompanied by extrapyramidal side effects, especially in adults, but propionate testosterone domperidone stimulates prolactin release from the pituitary. Its antiemetic effect may be due to a combination of peripheral (gastrokinetic) action and antagonism to dopamine receptors in the chemoreceptor trigger zone. Domperidone has no effect on gastric secretion. Pharmacokinetics Absorption after oral administration on an empty stomach – fast (reception after eating, decreased gastric acidity slow down and reduce absorption). Maximum plasma concentration (TC max ) – 1 hour Bioavailability -. 15% (the effect of “first pass” through the liver). Communication with plasma proteins – 90%. Penetrates into various tissues, poorly cross the blood brain barrier (BBB). It is metabolized in the liver and in the intestinal wall (by hydroxylation and N-dealkylation). Displayed through the intestines of 66%, the kidneys – 33%, including unaltered – 1 and 10%, respectively. The half-life (T1 / 2) – 7-9 hours, with severe chronic renal failure (CRF) – lengthened.
Indications
a) Kompeks dyspeptic symptoms, often associated with delayed gastric emptying, gastro – esophageal reflux, esophagitis;
– feeling of fullness in the epigastrium, sense of abdominal distention, pain in the upper abdomen:
– belching, flatulence:
– heartburn with reflux or without casting of gastric contents into the oral cavity.
b) Nausea and vomiting functional, organic, infectious origin caused by radiotherapy, drug therapy or diet disorders, as well as dopamine agonists for the background in the case of their use in Parkinson’s disease (such as L-dopa and bromocriptine)
Pregnancy and lactation
Use of the drug in the I trimester of pregnancy is possible only when the expected benefit of therapy to the mother outweighs the potential risk to the fetus. To date there is no evidence of an increased risk of malformations in humans. Women domperidone concentration in breast milk is 4 times lower than corresponding concentrations in plasma. It is unknown whether propionate testosterone domperidone in this concentration has a negative impact on infants. Therefore, the use Motilak not recommended during lactation (breastfeeding), except in cases when the expected benefit of therapy to the mother outweighs the potential risk to the infant.
Contraindications
Hypersensitivity, bleeding from the gastrointestinal tract, mechanical intestinal obstruction, perforation of the stomach or intestines, prolactinoma, infancy (up to 5 years of age and for children weighing up to 20 kg).
dosage
Tablets: should dissolve in 15-20 minutes before eating. Adults and children over 5 years with chronic dyspeptic phenomena – 10 mg 3-4 times a day and, if necessary, further bedtime. In severe nausea and vomiting -. 20 mg 3-4 times a day and at bedtime
to patients with renal failure dose adjustment is necessary, frequency of intake should not exceed 1-2 times during the day.
Side effect
From the digestive system: transient intestinal cramps. Nervous system: extrapyramidal disorder (in children and patients with increased permeability of the BBB). Allergic reactions: skin rash, urticaria.Other: hyperprolactinemia (galactorrhea, gynecomastia).
Interaction
Cimetidine, sodium bicarbonate reduces the bioavailability of domperidone.
Anticholinergic and antacid drugs (PM) neutralize domperidone.
Increase the concentration of domperidone in the plasma. Antifungal drugs azole, macrolide antibiotics, HIV protease inhibitors, nefazodone (antidepressant)
compatible with the reception antipsychotic drugs (neuroleptics), agonists of dopaminergic receptors (bromocriptine, L-dopa).
Simultaneous treatment with paracetamol and digoxin had no effect on the concentration of these drugs in the blood.
Precautions
Renal / hepatic propionate testosterone insufficiency, during lactation, pregnancy.
Overdose
Symptoms: drowsiness, disorientation, extrapyramidal disorder (especially in children).
Treatment: reception activated carbon, with extrapyramidal disorders – anticholinergic drugs, antihistamines or antiparkinsonian drugs with anticholinergic properties. anabolic steroids online pharmacy
