Imodium

Imodium is a drug that has a depressant effect on peristaltic function.

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Indications Imodium

It is indicated for the elimination of such disorders:

• treatment of symptoms of acute diarrhea (for children aged 12 years and over, as well as adults);
• treatment of symptoms of acute types of diarrhea that occur due to IBS (for adults over 18 years of age), provided that a doctor has made a primary diagnosis.

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Release form

Available in capsules, 6 or 20 pieces in a blister plate. The package contains 1 blister.

Imodium lingual is a tablet that dissolves in the mouth.

Imodium Plus is an antidiarrheal medication available as chewable tablets.

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Pharmacodynamics

Loperamide hydrochloride is synthesized with opiate endings on the intestinal walls. With this action, the process of releasing PG and acetylcholine is inhibited, as a result of which progressive peristalsis decreases and the period of passage of food products through the digestive tract is extended, and at the same time the ability of the intestinal walls to absorb liquids is increased.

The active component of the drug increases the tone of the anal sphincter, which helps reduce fecal incontinence along with the urge to empty the bowels.

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Pharmacokinetics

Large amounts of orally administered loperamide are absorbed into the intestine, but intensive first-pass metabolism processes provide only 0.3% of the systemic bioavailability of the substance.

Data from rat distribution studies have shown that it has a strong affinity for the intestinal wall, mainly with subsequent synthesis with the ends within the longitudinal muscle layer. The synthesis of the component with protein is 95%, it is mainly bound to albumins. Preclinical data show that loperamide is a substrate of P-glycoprotein.

Almost all loperamide extraction occurs in the liver. Here it is mainly conjugated and then excreted in the bile. The oxidative process of N-demethylation is the main route of metabolism of the substance, which is carried out mainly by the elements CYP3A4, as well as CYP2C8. Since the first liver pass is very intense, the plasma level of unchanged drug remains quite low.

The half-life of the substance in humans is about 11 hours (range 9-14 hours). The unchanged component with its decay products is mainly excreted in the feces.

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Dosing and administration

The drug is not used at the initial stage of therapy for severe diarrhea, which is accompanied by a decrease in water and electrolyte levels. In such cases, it is recommended to compensate for fluid loss by using replacement therapy (oral or parenteral methods).

The capsules are taken with water.

To eliminate symptoms of acute diarrhea in children aged 12 years and over, as well as adults, the initial dosage is 2 capsules (4 mg), and then 1 capsule (2 mg) should be taken with each subsequent loose stool. The standard daily dosage is 6-8 mg (or 3-4 capsules). No more than 12 mg of the medicine (i.e. 6 capsules) is allowed per day when treating acute diarrhea.

When eliminating the symptoms of acute diarrhea that arose due to the development of IBS, for adults (when the doctor makes a primary diagnosis), the initial dose is 4 mg (2 capsules), after which it is necessary to drink 1 capsule each time loose stools appear or as prescribed by the attending doctor. It is allowed to drink no more than 6 capsules per day (dosage 12 mg).

If there is no improvement within 48 hours (acute diarrhea) after using the drug, it is recommended to stop taking the medication.

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Use Imodium during pregnancy

It is prohibited to use the medicine during pregnancy.

If there are any disorders, pregnant and lactating women should consult a doctor to get appropriate treatment.

Contraindications

Among the contraindications of the drug:

• severe intolerance to loperamide hydrochloride, as well as any of the other components of the drug;
• children under 12 years of age;
• in the presence of an acute form of dysentery, which is characterized by high temperature, as well as blood in the stool;
• in the acute stage of ulcerative colitis or in the pseudomembranous form of colitis, which are associated with the use of antibiotics with a broad spectrum of action;
• in the bacterial form of enterocolitis caused by microbes of the genus Salmonella, Shigella or Campylobacter.

It is not recommended to use Imodium when there is a risk that the suppression of peristalsis will cause serious complications in the patient, including intestinal obstruction, as well as megacolon (along with the toxic form of this pathology).

If flatulence, constipation or intestinal obstruction occurs, you must immediately stop using the drug.

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Side effects Imodium

When eliminating acute diarrhea, the following side effects may develop, which were identified during clinical trials:

• nervous system organs: development of sharp headaches; more rarely – the appearance of dizziness;
• digestive system organs: flatulence, nausea, constipation; less commonly – discomfort in the abdomen, abdominal pain, dry mouth mucous membranes, dyspeptic symptoms, and also pain in the upper abdomen;
• subcutaneous tissue and skin: appearance of rashes.

The following adverse reactions have been identified during post-marketing studies:

• organs of the immune system: hypersensitivity reactions are observed sporadically, including anaphylactic reactions (including anaphylaxis), as well as anaphylactoid manifestations;
• nervous system organs: problems with coordination, suppression or loss of consciousness, a feeling of drowsiness or stupor arise occasionally, hypertonicity develops;
• visual organs: in isolated situations, miosis develops;
• digestive system organs: occasionally intestinal obstruction begins (in some cases even in paralytic form), and also megacolon (sometimes in toxic form);
• subcutaneous tissues and skin: rarely, bullous rashes, urticaria, Quincke's edema, itching, and in addition, erythema multiforme, Lyell's syndrome or Stevens-Johnson syndrome appear;
• urinary system and kidneys: urinary retention develops occasionally;
• General disorders: severe fatigue occurs at isolated moments.

Overdose

In case of overdose (this also includes conditional overdose due to liver dysfunction), symptoms of CNS depression may develop, such as coordination disorder, stupor, miosis, respiratory depression, and increased muscle tone. In addition, urinary retention or symptoms similar to intestinal obstruction may develop.

Children may have increased sensitivity to CNS effects.

If an overdose develops, immediate consultation with a doctor is required. If signs of a disorder appear, naloxone may be used as an antidote. Since the duration of Imodium's effect exceeds the period of action of naloxone (1-3 hours), the latter may be prescribed again. To detect possible suppression of the central nervous system, the patient's condition must be closely monitored for at least 48 hours.

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Interactions with other drugs

There is data on interaction with drugs that have similar pharmacological characteristics. Children should not be prescribed drugs that have a suppressive effect on the central nervous system function together with Imodium.

Preclinical studies demonstrate that loperamide is a P-glycoprotein substrate. When loperamide (16 mg) was co-administered with P-glycoprotein inhibitors (such as ritonavir or quinidine), plasma loperamide levels doubled/tripled. The clinical significance of this interaction at recommended loperamide doses remains unknown.

The combination of loperamide (single dose of 4 mg) with itraconazole, as well as an inhibitor of the CYP3A4 element, as well as P-glycoprotein, increases the plasma level of loperamide by 3-4 times. During the same testing, an inhibitor of the CYP2C8 element (gemfibrozil) increased the level of the active substance of the drug by approximately two times.

Concomitant use with itraconazole and gemfibrozil increased peak plasma loperamide levels fourfold and AUC by 13-fold. This increase was not associated with CNS effects as measured by psychomotor testing.

A single dose (16 mg) of loperamide in combination with ketoconazole, an inhibitor of the CYP3A4 element, and P-glycoprotein allows for a 5-fold increase in the level of loperamide in the blood plasma. This indicator is not associated with an increase in pharmacodynamic properties; the determination was made using pupillometry.

Taking the drug in combination with oral desmopressin leads to an increase in the latter's levels in plasma (by 3 times). Most likely, this is due to a slowdown in gastrointestinal motility.

There is an opinion that drugs with similar medicinal effects can enhance the properties of loperamide, but drugs that speed up the passage of food products through the gastrointestinal tract, on the contrary, can weaken its effectiveness.

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Storage conditions

The medicine must be kept in conditions suitable for medicines, inaccessible to children. Temperature values - maximum 25°C.

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Shelf life

Imodium can be used for 5 years from the date of release of the drug.

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