Loperamide Hexal 2 mg Diarrhea 15 Capsules

Capsules based on Loperamide hydrochloride .

Therapeutic indications

Loperamide Hexal is used in the treatment of acute and chronic diarrhea. After ileostomy it allows to decrease the number and volume of discharges and to increase their consistency.

Dosage and Posology

The drug should be taken according to the following doses and methods in adults and children aged between 6 and 17 years. The capsules should be taken with a little liquid. The effervescent tablets are dissolved in a glass of water.

• Acute diarrhea Adults: The starting dose is 2 capsules or 2 effervescent tablets or 60 drops (4 mg) for adults and 1 capsule or 1 effervescent tablet or 30 drops (2 mg) for children; thereafter 1 capsule or 1 effervescent tablet or 30 drops (2 mg) after each subsequent evacuation of unformed (soft) faeces.
• Chronic diarrhea Normal defecation can almost always be achieved with a dose adapted to each patient. Adults: The starting dose is 2 capsules or 2 effervescent tablets or 60 drops (4 mg) per day for adults and 1 capsule or 1 effervescent tablet or 30 drops (2 mg) for children. This starting dose is adjusted until 1 or 2 stools are formed per day, which is generally possible with a maintenance dose of 1 - 6 capsules or effervescent tablets (2 mg - 12 mg) per day.

Warning: for adults the maximum daily dose in case of acute and chronic diarrhea is 8 capsules or effervescent tablets (16 mg). For children, the dose must be related to body weight (3 capsules or effervescent tablets / 20 kg) but must not exceed a maximum of 8 tablets per day. Decrease the dose as soon as the stool has normalized; stop treatment in case of constipation.

• Children aged between 2 and 5 years Oral solution 15 drops of oral solution = 1 mg of loperamide per 10 kg of body weight, 2 or 3 times a day. Treatment with loperamide hydrochloride should be stopped as soon as there is a normalization of the stool or if there has been no more stool formation for more than 12 hours. Warning: the maximum daily dose is 3 mg of loperamide per 10 kg of body weight.
• Children under 2 years of age Loperamide hydrochloride should not be used in children under 2 years of age. Elderly No dose adjustment is required in the elderly.
• No dose adjustment is required in patients with renal impairment.
• Although no pharmacokinetic data are available in patients with hepatic impairment, loperamide hydrochloride should be used with caution in these patients due to impaired first pass metabolism.

Warning: do not use for more than 2 days.

Overdose

In case of overdose (including relative overdose, due to liver dysfunction) CNS depression (stupor, coordination abnormalities, somnolence, miosis, muscle hypertonia and respiratory depression), urinary retention and ileus may occur. Children may be more sensitive to central nervous system effects than adults. Therefore it is recommended to keep the product out of their reach because in cases of erroneous administration in children under 4 years of age, for absolute overdose (accidental intake of excessive doses) or relative (for accumulation in the blood of drug not metabolized, even if administered at the correct doses), constipation may occur and, as with many other drugs (e.g. sulfonamides), in the case of immaturity of the blood-brain barrier, undesirable effects such as central nervous system depression, accompanied by drowsiness and bradypnea . In this case, the patient should be kept under careful observation for 48 hours in order to highlight a possible depression of the central nervous system.

Measures in case of overdose: gastric lavage, inducement of vomiting, enema or administration of laxatives. If symptoms of overdose develop, naloxone can be given as an antidote. Since the duration of action of loperamide is longer than that of naloxone (1 to 3 hours), repeated treatment with naloxone may be indicated. Therefore the patient should be monitored closely for at least 48 hours in order to detect any CNS depression.

Contraindications

• Hypersensitivity to the active substance or to any of the excipients
• In patients with acute dysentery characterized by blood in stool and high fever or in patients with acute ulcerative colitis or in patients with bacterial enterocolitis caused by invasive organisms, including Salmonella, Shigella and Campilobacter or in patients with pseudomembranous colitis associated with antibiotic use broad spectrum
• Loperamide hydrochloride should not be used when inhibition of peristalsis is to be avoided due to the possible risk of significant sequelae, including ileus, megacolon and toxic megacolon.
• Loperamide hydrochloride should be discontinued immediately if constipation, abdominal distension or ileus develop.

Side effects

• Adults and children aged ≥12 years

The safety of loperamide hydrochloride was evaluated in 3076 adults and children aged ≥12 years who participated in 31 controlled and uncontrolled clinical trials with loperamide hydrochloride used for the treatment of diarrhea. Of these, 26 studies were on acute diarrhea (N = 2755) and 5 on chronic diarrhea (N = 321). The most commonly reported adverse drug reactions (ADRs) (i.e. with an incidence ≥1%) in clinical trials with loperamide hydrochloride for the treatment of acute diarrhea were: constipation (2.7%), flatulence ( 1.7%), headache (1.2%) and nausea (1.1%). In clinical trials for the treatment of chronic diarrhea the most commonly reported ADRs (i.e. with an incidence ≥1%) were: flatulence (2.8%), constipation (2.2%), nausea (1.2 %) and dizziness (1.2%). The data in Table 1 represent the results from 3076 adults and children aged ≥12 years who participated in 31 controlled and uncontrolled clinical trials with loperamide hydrochloride used for the treatment of diarrhea. Of these, 26 studies were on acute diarrhea (N = 2755) and 5 on chronic diarrhea (N = 321). The frequency categories in Table 1 are defined according to the following convention: very common (≥ 1/10), common (≥ 1/100 to <1/10), uncommon (≥ 1 / 1,000 to <1/100 ), rare (≥ 1 / 10,000, <1 / 1,000) and very rare (<1 / 10,000)

Frequency of adverse drug reactions reported with the use of loperamide hydrochloride during clinical trials in adults and children aged ≥12 years

- Nervous system disorders

• Acute diarrhea: Headache (Common), Dizziness (Uncommon)
• Chronic Diarrhea: Headache (Uncommon), Dizziness (Common)

- Gastrointestinal disorders

• Acute Diarrhea: Constipation, nausea, flatulence (Common), Abdominal pain, abdominal discomfort, dry mouth (Uncommon), Abdominal pain upper, vomiting (Uncommon), Abdominal distension (Rare)
• Chronic diarrhea: Constipation, nausea, flatulence (Common), Abdominal pain, abdominal discomfort, dry mouth (Uncommon), Dyspepsia (Uncommon)

- Skin and subcutaneous tissue disorders

• Acute Diarrhea: Rash (Uncommon)

The post-marketing adverse reaction reporting process for loperamide did not differentiate between indications for the treatment of chronic versus acute diarrhea or between adults and children; consequently, the post-marketing adverse reactions for loperamide listed below are cumulative for the two indications and patient populations. Adverse reactions identified post-marketing for loperamide hydrochloride are listed below by MedDRA Dictionary System Organ Class and Preferred Terms (PT).

• Immune system disorders: Hypersensitivity reaction, Anaphylactic reaction (including anaphylactic shock), Anaphylactoid reaction
• Nervous system disorders: Somnolence, loss of consciousness, stupor, depressed level of consciousness, hypertonia, coordination disturbances
• Eye disorders: Miosis
• Gastrointestinal disorders: Ileus (including paralytic ileus), megacolon (including toxic megacolon) and glossodynia
• Skin and subcutaneous tissue disorders: Bullous rash (including Stevens-Johnson syndrome, toxic epidermal necrolysis and erythema multiforme), angioedema, urticaria, pruritus
• Renal and urinary disorders: Urinary retention
• General Disorders and Administration Site Conditions: Fatigue

The safety of loperamide hydrochloride was evaluated in 607 patients aged 10 days to 13 years who participated in 13 controlled and uncontrolled clinical trials with loperamide hydrochloride used for the treatment of acute diarrhea. In general, the profile of ADRs in this patient population was similar to that observed in clinical trials with loperamide hydrochloride in adults and children aged 12 years and older.

Pregnancy and breastfeeding

Although there are no indications that loperamide hydrochloride possesses teratogenic or embryotoxic properties, the anticipated therapeutic benefits must be weighed against the potential risks before administering loperamide hydrochloride during pregnancy, especially during the first trimester. Small amounts of loperamide can appear in human breast milk. Therefore loperamide hydrochloride is not recommended during breastfeeding.

Special warnings

Treatment of diarrhea with loperamide hydrochloride is symptomatic only. Whenever an underlying etiology can be determined, specific treatment should be given when appropriate. Fluid and electrolyte depletion may occur in patients with diarrhea, especially children. In these cases, the most important countermeasure is the administration of adequate fluid and electrolyte replacement therapy. Loperamide hydrochloride should not be given to children 2 to 6 years of age without prescription and medical supervision.

In acute diarrhea, if no improvement in clinical symptoms is observed within 48 hours, administration of loperamide hydrochloride should be discontinued and patients should be advised to consult their physician. AIDS patients treated with loperamide hydrochloride for diarrhea should discontinue therapy at the first signs of abdominal distension. Isolated cases of constipation with an increased risk of toxic megacolon have been reported in AIDS patients with infectious colitis caused by viral and bacterial pathogens treated with loperamide hydrochloride.

Although no pharmacokinetic data are available in patients with hepatic impairment, loperamide hydrochloride should be used with caution in such patients due to decreased first pass metabolism. Patients with hepatic dysfunction should be carefully monitored for signs of central nervous system (CNS) toxicity.

Loperamide Hexal 2 mg hard capsules contain lactose, therefore patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption syndrome should not take this medicine.

Expiry and retention

Check the expiration date indicated on the package. The expiry date indicated on the package refers to the product in intact packaging, correctly stored. This medicine does not require any special storage conditions.

Warning : do not use the medicine after the expiry date indicated on the package.

Composition

One capsule of Loperamide Hexal contains:

Active principle

loperamide hydrochloride 2 mg equal to loperamide 1.8 mg

Excipients

Lactose, corn starch, magnesium stearate, talc Capsule body: gelatin, black iron oxide (E172), titanium dioxide (E171) Lid: gelatin, black iron oxide (E172), yellow iron oxide (E172), patent blue (E131) ), titanium dioxide (E171)