| Preclinical data have shown that loperamide is a substrate of P-glycoprotein. Concomitant administration of loperamide (at a dose of 16 mg) with P-glycoprotein inhibitors (quinidine, ritonavir) led to an increase in loperamide plasma levels 2-3. Clinical significance of that pharmacokinetic interaction when using loperamide in recommended doses is unknown.
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Concomitant use of loperamide (4 mg single dose) and itraconazole, an inhibitor of CYP3A4 and P-glycoprotein resulted in a 3-4-fold increase in loperamide concentrations in plasma. In the same study, an inhibitor of CYP2C8 gemfibrozil content loperamide increased approximately 2-fold. The combined use of gemfibrozil and itraconazole resulted in a 4-fold increase in loperamide maximum concentration in plasma and 13-fold increase in total plasma exposure. This increase was not associated with effects on the central nervous system (CNS) that determined using psychomotor tests (ie, subjective drowsiness and test replacement numeric characters).
Concomitant use of loperamide (16 mg single dose) and ketoconazole, an inhibitor of CYP3A4 and P-glycoprotein, resulted in a 5-fold increase in loperamide concentrations in plasma. This increase was not associated with increased pharmacodynamic effects determined using pupilometriyi.
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Desmopressin Concomitant treatment for oral administration resulted in a 3-fold increase in the concentration of desmopressin in plasma, probably due to the slower motility of the gastrointestinal tract.
It is expected that drugs with similar pharmacological properties may enhance the effect of loperamide and medicinal products that accelerate the passage of food in the gastrointestinal tract, can reduce its effect.
The application features
Treatment is symptomatic diarrhea. If you can identify the etiology of diseases (or indicate that you need to do), then if possible should be specific treatment.
In patients with diarrhea, especially in children, debilitated patients elderly may be dehydration and electrolyte imbalance. In such cases, the most important measure is the use of replacement therapy to replenish fluids and electrolytes.
Use of the drug does not replace appropriate amount of fluid entering and restore electrolytes.
Because resistant diarrhea may indicate a potentially more serious condition, the drug should not be used for a long time, until the cause of diarrhea will be investigated.
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In acute diarrhea, if clinical improvement is not observed within 48 hours, the use of loperamide hydrochloride should stop and consult a doctor.
Patients with acquired immunodeficiency syndrome taking Imodium® diarrhea, should immediately stop treatment at the first signs of bloating. There are some reports of intestinal obstruction with increased risk of toxic megacolon in patients AIDS patients with infectious colitis both viral and bacterial origin, the treatment of loperamide hydrochloride.
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