LOPERAMIDE AUR 15CPS 2MG

LOPERAMI AUROBINDO 2 MG CAPSUDE

active ingredients

Each rigid capsule contains 2 mg of loperamide hydrochloride. Excipient with known effects: Each rigid capsule contains 144,6 mg of lactose monohydrate. For the full list of excipients, see paragraph 6.1.

Excellent

Content of the capsule: Lactose monohydrate Corn starch Magnesium stearate Capsule envelope: Titanium oxide (E171) Gelatin Printing Ink: Rubber Black Iron oxide (E172)

Therapeutic indications

For the symptomatic treatment of acute diarrhea in adults and children aged 12 and over.

Contraindications

Hypersensitivity to the active ingredient or any other excipient listed in paragraph 6.1. When it is necessary to avoid the inhibition of peristalsis due to a possible risk of significant sequel included ileo, megacolon, toxic megacolon and some poisoning in particular: • Children under the age of 12 • When there is ileum or constipation and when abdominal distension develops • In patients with acute ulcerative colitis • In patients with enterocolitis caused by invasive organisms including Salmonella, Shigella and Campylobacter • In patients with pseudomembranous colitis associated with the use of broad spectrum antibiotics. Loperamide Aurobindo should not be used alone in acute dysentery, which is characterized by blood in the feces and high body temperature.

Population

Population Adults and children over 12 years of age: Two capsules to be taken immediately, followed by a capsule after each diarrhoic discharge, up to a maximum of six capsules in 24 hours. Children under 12 years of age: Not recommended. Use in the elderly No dose change is required. Kidney damage No dose change is required for patients with kidney damage. Epathetic Comprogation Although there is no pharmacokinetic data available in patients with hepatic impairment Loperamide Aurobindo must be used with caution in these patients due to reduced first-pass metabolism (see paragraph 4.4 Special warnings and precautions of use). Method of administration Oral use.

Conservation

Store at a temperature below 30°C.

Warnings

The treatment of diarrhea with loperamide is only symptomatic. If appropriate, a specific treatment should be given whenever a basic etiology can be determined. In acute diarrhea the priority is the prevention or reversal of hydroelectrolysis. This is particularly important in small children and in fragile and elderly patients with acute diarrhea. The use of loperamide hydrochloride does not preclude the administration of an electrolyte replacement therapy. Since persistent diarrhea can be a potentially more severe condition indicator, loperamide hydrochloride should not be used for prolonged periods until the basic cause of diarrhea was sought. Loperamide Hydrochloride should be used with caution when the liver function necessary for the metabolism of the drug is imperfect (e.g. in cases of severe liver disorders), since this could cause a relative overdose that leads to a toxicity charged to the SNC. Patients with AIDS treated with loperamide hydrochloride for diarrhea must stop therapy at the first signs of abdominal distension. Isolated cases of toxic megacolons were reported in patients with AIDS with infectious colitis from both bacterial and viral pathogens treated with loperamide hydrochloride. When clinical changes are not observed in acute diarrhea within 48 hours, the administration of loperamide must be interrupted and patients should be advised to consult the doctor. Treatment with loperamide must be stopped immediately in case of development of constipation, abdominal or subile distension. Heart events have been reported including the extension of the QT and that of the QRS complex, point twists in association with overdose. Some cases were fatal (see paragraph 4.9). Overdose can make the presence of Brugada syndrome manifest. Patients should not exceed the recommended dose and/or recommended duration of therapy. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency, or glucose-galactose mal absorption, should not take this medicine.

Interactions

Non-clinical data showed that loperamide hydrochloride is a substrate of glycoprotein P. Moreover, loperamde is metabolized mainly by CYP3A4 and CYP2C8. Concurrent administration of loperamide (16 mg in single dose) with chinidine or ritonavir, both glycoprotein inhibitors P, caused a 2-3-fold increase in plasma levels of loperamide. The results of a published pharmacokinetics study suggested that the concomitant administration of loperamide with oral desmopressin may lead to an increase of 3 times of plasma concentrations of desmopressin although no clinical effects have been reported. Possible interactions with medicines that delay intestinal peristalsis (e.g. anti-colinergic drugs) may occur as the effects of loperamide may be enhanced. The administration of itraconazole with loperamide (4 mg in single dose) increased plasma levels of loperamide 3-4 times. In addition, gemfibrozil, a CYP2C8 inhibitor, increased loperamide AUC by 2 times. Concurrent use of itraconazole and gemfibrozil with loperamide increased C_max and average loperamide AUC of about 2 and 13 times respectively. This increase did not lead to measurable effects on SNC. Concurrent administration of loperamide (16 mg per single dose) and chetoconazole, a CYP3A4 inhibitor and glycoprotein P has resulted in a 5-fold increase in plasma concentrations of loperamide. This increase was not associated with increased pharmacodynamic effects as measured by pupillometry. The clinical relevance of these pharmacokinetic interactions is not known, when loperamide is administered at recommended doses (2 mg, up to the maximum daily dose of 12 mg).

Effects

Adults and children aged ≥ 12 years The safety of loperamide hydrochloride was assessed in 2755 adults and children aged ≥12 years who participated in 26 controlled and uncontrolled clinical trials of loperamide hydrochloride used for treating acute diarrhea. The most commonly reported adverse reactions to the drug (ADRs) (≥1% incidence) in clinical studies with loperamide hydrochloride in acute diarrhea were: constipation (2.7%), flatulence (1.7%), headache (1.2%) and nausea (1.1%). Table 1 shows the ADRs reported using loperamide hydrochloride in clinical trials (acute diarrhea) and post-marketing experience. Frequency categories use the following convention: very common (≥1/10), common (≥1/100, Table 1 adverse reactions to the drug

Classification for systems and organs	Indication
	Town	Uncommon	Rare
Immune system disorders			Reactions of hypersensitivitya, Anaphylactic reaction (including anaphylactic shock)a, Anaphylactoid reactiona
Diseases of the nervous system	Kefalea, Chief	Sleepa	Loss of consciousnessa, Amazementa, Depressed Level of Consciencea, Hypertoniaa, Abnormal coordinationa
Pathologies of the eye			Othera
Gastrointestinal diseases	Stipsi, Nausea, Flatulenza	Abdominal Pain, Abdominal Fastidium, Dry Mouth, Upper Abdominal Pain, Vomito, Dispepsiaa	Ileoa (including paralytical ileo), Megacolona (including toxic megacolonb), Glossa, Abdominal Distension
Pathologies of skin and subcutaneous tissue		Skin rash	Bullous skin rasha (including Stevens-Johnson syndrome, toxic epidermal necrolysis and erythema multiforme), Angioedemaa, Orticariaa, Itchinga
Kidney and urinary pathologies			Urinary retentiona
Systemic pathologies and conditions for administration			Fatiguea

^a The inclusion of this term is based on post-marketing cases for loperamide hydrochloride. As the process for determining post-marketing ADRs does not differentiate between chronic and acute indications or adults and children, the frequency is evaluated on the basis of all clinical studies with loperamide hydrochloride (acute and chronic), including studies in children ≤ 12 years (N=3683). ^b See paragraph 4.4 Special warnings and precautions for use. Reporting of suspicious adverse reactions The reporting of suspicious adverse reactions that occur after the authorization of the medicinal product is important, as it allows continuous monitoring of the benefit/risk ratio of the medicinal product. Healthcare workers are required to report any suspected adverse reaction via the national reporting system at the address http://www.agenziafarmaco.gov.it/content/come-segnalare-una-sospetta-reazione-avversa.

Overdosing

Synonyms In cases of overdose (including relative overdose due to hepatic dysfunction) depression of the SNC may occur (stupor, abnormal coordination, drowsiness, myosis, muscle hypertonia and respiratory depression), urinary retention and ileum. Children can be even more sensitive to the effects on SNC than adults. In patients who ingested excessive doses of loperamide, cardiac events were observed such as extension of the QT range and the QRS complex, point torsion, other severe ventricular arrhythmias, cardiac arrest and syncope (see paragraph 4.4). Fatal cases have also been reported. Overdose can make the presence of Brugada syndrome manifest. Treatment If you experience overdose symptoms, it can be given naxolone as an antidote. Since the duration of loperamide action is longer than that of naxolone (1-3 hours), repeated treatment with naxolone can be indicated. Therefore the patient must be closely monitored for at least 48 hours to detect any possible SNC depression sign.

Pregnancy

Limited data on the use of loperamide in pregnant women are available. In one of two epidemiological studies the use of loperamide during the first phase of pregnancy suggested a possible moderate increase in the risk of hypopadia, however it was not possible to identify an increase in the risk of major malformations. Animal studies do not indicate direct or indirect harmful effects on reproductive toxicity (see paragraph 5.3). In man, safety in pregnancy has not been established, although according to animal studies there are no indications that loperamide hydrochloride possess teratogenic or embryotoxic properties. If possible, the use of loperamide should be avoided during the first trimester of pregnancy, however it can be used during the second and third trimester of pregnancy.

Food

Small amounts of loperamide can be found in breast milk. Therefore, this medicine is not recommended during lactation. Pregnant or breastfeeding women should therefore be advised to consult their physician for proper treatment.

Fertility

Only high doses of loperamide hydrochloride influenced female fertility in non-clinical studies (see paragraph 5.3).

Source: Farmadati