The concomitant administration of loperamide 4 mg single dose and itraconazole, an inhibitor of CYP3A4 and P-glycoprotein, resulted in a 3 to 4-fold increase in loperamide plasma concentrations. In the same study a CYP2C8 inhibitor, gemfibrozil, increased loperamide by approximately 2-fold.
The combination of itraconazole and gemfibrozil resulted in a 4-fold increase in peak plasma levels of loperamide and a fold increase in total plasma exposure.
These increases were not associated with central nervous system CNS effects as measured by psychomotor tests i. The concomitant administration of loperamide 16 mg single dose and ketoconazole, an inhibitor of CYP3A4 and P-glycoprotein, resulted in a 5-fold increase in loperamide plasma concentrations. This increase was not associated with increased pharmacodynamic effects as measured by pupillometry. It is expected that drugs with similar pharmacological properties may potentiate loperamide's effect and that drugs that accelerate gastrointestinal transit may decrease its effect.
As with other drugs, it is not advisable to administer this medicine in pregnancy, especially during the first trimester. Breast-Feeding Small amounts of loperamide may appear in human breast milk. Therefore, this medicine is not recommended during breast-feeding. Women who are pregnant or breast feeding infants should therefore be advised to consult their doctor for appropriate treatment. Fertility The effect on human fertility has not been evaluated.
Therefore, it is advisable to use caution when driving a car or operating machinery. The study reported that the use of loperamide should be contraindicated in children under 3 years old, systemically ill, malnourished, moderately dehydrated, or have bloody diarrhea.
Studies in rat models have shown no teratogenicity , but there have not been sufficient studies in humans. This, however, was only one study with a small sample size. As an example, when saquinavir concentrations can decrease by half when given with loperamide.
As such, when combined with other antimotility drugs, there is an increased risk of constipation. These drugs include other opioids , antihistamines , antipsychotics , and anticholinergics. Loperamide works like morphine , decreasing the activity of the myenteric plexus, which decreases the tone of the longitudinal and circular smooth muscles of the intestinal wall.
Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex. Imodium comes in various forms: All forms of Imodium can be taken either with or without food. Imodium capsules should be swallowed whole with a drink of water. Imodium instants should be placed on the tongue and allowed to dissolve in the saliva.
You can then swallow this without needing a drink. To treat acute diarrhoea: Adults and adolescents aged 12 years and over should take two 2mg tablets or capsules 4mg total dose straight away, and then one more 2mg tablet or capsule after each loose stool. Do not take more than a total of eight tablets or capsules in 24 hours. Stop taking loperamide as soon as your symptoms settle down.
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