Loperamide, 2 mg capsules 10 pcs

Pharmacotherapeutic group: Antidiarrheal.

TAC code: A07DA03.

Pharmacological properties.

Binding to opioid receptors of the intestinal wall (stimulation of cholinergic and adrenergic neurons through guanine nucleotides), reduces tone and motility of intestinal smooth muscle, slows the passage of intestinal contents, reduces excretion of fluid and electrolytes with feces. Increases the tone of the anal sphincter, helps to retain feces and reduce urges to defecation. The action comes on quickly and lasts 4-6 hours.

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Indications

Active ingredient

Composition

1 capsule contains:

active ingredient: loperamide hydrochloride – 2 mg;

excipients:

lactose monohydrate -104.5 mg,

cup starch -30.0 mg,

talk – 1, 4mg,

magnesium stearate – 1.4 mg,

/p>

colloidal silicon dioxide (aerosil) – 0.7 mg;

solid gelatin capsules

(composition of capsule shell): titanium dioxide – 2.0000%, gelatin – up to 100%,

capsule cap composition: petent blue dye

How to take, the dosage

Ingestion. In adults in acute and chronic diarrhea 2 capsules (4 mg) are prescribed orally, then 1 capsule (2 mg) after each act of defecation in case of liquid stool. In chronic diarrhea, the dose is further adjusted so that the frequency of stools is 1-2 times per day, which is usually achieved with a maintenance dose of 2-4 capsules (4-8 mg) per day.

The maximum daily dose is 8 capsules (16 mg). If there is no effect after taking 16 mg daily for 10 days, it is not advisable to continue taking it.

Children over 6 years of age take 1 capsule (2 mg) after each act of defecation in case of loose stools. The maximum daily dose is 3 capsules (6 mg).

The treatment with loperamide should be discontinued after normalization of stools or if there are no stools within 12 hours.

Patients with renal insufficiency and elderly patients do not require dosage adjustment.

Interaction

According to preclinical studies, loperamide is a substrate of P-glycoprotein. When concomitant use of loperamide (single dose of 16 mg) and quinidine or ritonavir, which are P-glycoprotein inhibitors, plasma concentrations of loperamide increased by 2-3 times. The clinical significance of the described pharmacokinetic interaction with P-glycoprotein inhibitors when using loperamide at the recommended doses is unknown.

The simultaneous use of loperamide (single dose of 4 mg) and itraconazole, an inhibitor of CYP3A4 isoenzyme and P-glycoprotein, resulted in an increase of loperamide concentration in blood plasma by 3-4 times. In the same study, use of the CYP2C8 isoenzyme inhibitor, gemfibrozil, resulted in an increase in plasma concentrations of loperamide by approximately 2-fold. When using a combination of itraconazole and gemfibrozil, the peak plasma concentration of loperamide increased 4-fold and the total concentration increased 13-fold. This increase was not related to the effect on the CNS, as assessed by psychomotor tests (i.e., subjective assessment of drowsiness and the numeric symbol replacement test). Concomitant use of loperamide (single dose of 16 mg) and ketoconazole, an inhibitor of CYP3A4 isoenzyme and P-glycoprotein, resulted in a fivefold increase in plasma loperamide concentration. This increase was not associated with an increase in pharmacodynamic action as assessed by pupil size.

Concomitant oral administration of desmopressin resulted in a 3-fold increase in plasma desmopressin concentration, probably due to a slowing of gastrointestinal motility.

It is expected that drugs with similar pharmacological properties may enhance the effects of loperamide, and drugs that increase the rate of gastrointestinal passage may decrease the effects of loperamide.

Special Instructions

If there is no effect after 2 days of using loperamide, a doctor should be consulted. If constipation or bloating develop during treatment, loperamide should be discontinued.

In patients with impaired liver function, close monitoring of signs of toxic CNS damage (stupor, impaired coordination of movements, somnolence, miosis, muscle hypertonicity, respiratory depression increased fatigue, drowsiness, dizziness) is necessary.

The treatment with loperamide does not replace correction of the water-electrolyte balance that develops during diarrhea. During treatment of diarrhea (especially in children) it is necessary to compensate for fluid and electrolyte loss. Dehydration may contribute to changes in response to loperamide.

In individual cases of AIDS patients with infectious colitis of both viral and bacterial nature, toxic dilatation of the colon may develop when treated with loperamide.

Impact on driving and operating machinery

When treating, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration and quick psychomotor reactions.

Contraindications

Side effects

Allergic reactions: skin rash, itching, angioneurotic edema, in some cases – erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis.

Digestive system disorders: dryness of the oral mucosa, pain or discomfort in the stomach, nausea, vomiting, constipation, abdominal distension, colic, and in some cases – intestinal obstruction.

CNS and peripheral nervous system disorders: fatigue, drowsiness, dizziness.

Others: urinary retention.

Overdose

Symptoms: central nervous system depression (stupor, poor coordination, drowsiness, miosis, muscle hypertonus, respiratory depression), urinary retention, intestinal obstruction. Children may be more sensitive to the effects of loperamide on the CNS than adults.

In patients with loperamide hydrochloride overdose, cardiac complications such as prolongation of the QT interval, development of torsade de pointes ventricular tachycardia, other serious ventricular arrhythmias, cardiac arrest, and syncope have been observed. Fatal cases have also been reported.

Treatment: the antidote is naloxone; given that loperamide has a longer duration of action than naloxone, repeated administration of naloxone is possible. Medical observation for at least 48 hours is necessary.

Pregnancy use

In preclinical studies of favipiravir at doses similar to or lower than clinical doses, early embryo death and teratogenicity were observed.

The drug AREPLIVIR is contraindicated in pregnant women and in men and women during pregnancy planning. If AREPLIVIR is prescribed to women capable of childbearing (including postmenopausal women less than 2 years old), it is necessary to confirm a negative result of a pregnancy test before starting treatment. A repeat pregnancy test should be performed after the end of the drug.

It is necessary to use effective methods of contraception (condom with spermicide) during and after taking the drug: for 1 month for women and 3 months for men.

If AREPLIVIR is prescribed to breastfeeding women it is necessary to stop breastfeeding while taking the drug and for 7 days after it ends because the main metabolite of favipiravir passes into the breast milk.

Similarities