COMPOSITION:

Active substance:

1 tablet contains Loperamide Hydrochloride 2 mg, Simethicone 125 mg.

Additional ingredients: Magnesium aluminium silicate, Lactose monohydrate, Microcrystalline cellulose, Calcium hydrogen phosphate, Stearic acid, Colloidal anhydrous silica, Croscarmellose sodium, Povidone K-30, Opadry II Yellow 85G52482: polyvinyl alcohol, talk, titanium dioxide (E171), polyethylene glycol, lecithin, iron oxide yellow (E172).

INDICATIONS:

Symptomatic treatment of acute diarrhoea accompanied with abdominal discomfort, including bloating, spasmodic pain and meteorism.

DOSAGE:

Adults:

The initial dose is 2 tablets singly, then it is used 1 tablet after each act of defecation, but not more than 4 tablets per day. The duration of usage is not more than 2 days.

Children above 12 years old:

The initial dose is 1 tablet singly, then it is used 1 tablet after each act of defecation, but not more than 4 tablets per day. The duration of usage is not more than 2 days.

Elderly patients:

The dose adjustment is not necessary for the treatment of elderly patients.

Kidney dysfunction:

The dose adjustment is not necessary for patients with kidney dysfunction.

Despite the fact that pharmacokinetic data on the effects of the preparation in patients with liver dysfunction is not available, Loflatil® should be used with caution in such patients because of slowing of metabolism of the first passage. (see “Appropriate safety measures in administration”).

ADVERSE REACTIONS:

Below side effects are classified as follows:

Very common (≥ 1 / 10), common (≥ 1 / 100, <1 / 10); uncommon (≥ 1 / 1, 000, <1 / 100), rare (≥ 1 / 10 000, <1 / 1000); very rare (<1 / 10, 000) including isolated reports.

Uncommon – skin rash; very rare – urticaria, itch, isolated reports – angioedema, bullous eruptions (including Stevens-Johnson syndrome), erythema multiforme, toxic epidermal necrolysis, anaphylactic shock, anaphylactoid reaction.

Digestive tract:

Common – taste change, dry mouth, nausea, uncommon – constipation; very rare – megacolon (including toxic megacolon), intestinal obstruction, abdominal pain, vomiting, bloating, dyspepsia, meteorism.

Nervous system:

Uncommon – drowsiness, very rare – dizziness, depression of consciousness, depression, headache, tremor, fatigue.

Urinary system:

Isolated reports – urinary retention.

Drug interactions:

There is no information about clinical significant drug interaction of Loperamide Hydrochloride or Simeticone with other medicines.

There were reports on interactions with medicines, which have similar pharmacological properties. Agents that have inhibitory effects on central nervous system are not simultaneously used with Loflatil® in children.

Co-administration of Loperamide (at a dose of 16 mg) with inhibitors of P-glycoprotein (quinidine, ritonavir) caused an increasing of plasma level of Loperamide by 2 – 3 times.

Clinical significance of such pharmacokinetic interaction during administration of Loperamide at recommended doses (2 mg to 8 mg of maximum daily dose) is unknown.

Pregnancy and lactation:

Experience of Loperamide and Simethicone use during pregnancy is limited, so the preparation can be administered only if the expected benefit to the mother overweights the potential risk to the fetus.

A small amount of Loperamide have been detected in breast milk, so Loflatil® administration during lactation is not recommended.

Children:

It is administered to children above 12 years old.

Patients with diarrhea, especially children, may have dehydration and electrolyte imbalance. In such cases the most important measure is the use of replacement therapy to replenish fluids and electrolytes.

In case of clinical effect absence within 48 hours the use of Loflatil® preparation should be discontinued and a patient should consult a doctor to clarify the diagnosis.

Patients with secondary immunodeficiency syndrome, who use Loflatil® in case of diarrhea, should immediately discontinue the treatment in case of first signs of abdominal distention. There are isolated reports of cases of toxic megacolon in AIDS patients with infectious colitis, both of viral and bacterial origin, during the treatment with Loperamide Hydrochloride.

Despite the fact that pharmacokinetic data for patients with liver dysfunction is not available, Loflatil® should be used with caution in such patients because of slowing of metabolism of the first passage. Patients with liver dysfunction should be under close supervision of a physician in order to timely detect signs of toxic central nervous system.

Agents that prolong the transit time may cause the development of toxic megacolon in patients of this group.

Loflatil® should not be used when it is necessary to avoid the inhibition of peristalsis. It is necessary to discontinue immediately the preparation use, if it is developed constipation, bloating or partial intestinal obstruction.

Overdose:

:

In case of overdose (including overdose caused by liver dysfunction) it is possible a central nervous system depression (stupor, disorders of moving coordination, drowsiness, miosis, increasing of muscles tonus, respiratory depression) and paralytic ileus, urinary retention. In children the depression of CNS may occur more frequently.

Treatment:

In case of overdose symptoms the patient should be introduced Naloxone as antidote. Since half-life of Loperamide is more than half-life of Naloxone (1 to 3 hours) it may be necessary an additional introduction of Naloxone. It is required a round-the-clock monitoring of respiratory function. It is necessary a close monitoring of patient’s condition for not less than 48 hours to identify possible CNS depression.

Ability to influence reaction velocity while driving or operating any other mechanisms.

During the preparation treatment it is necessary to avoid driving a motor transport and operating potentially dangerous mechanisms.

CONTRAINDICATIONS:

Individual hypersensibility to components of the preparation.

Constipation, ileus. Patients with rare congenital forms of fructose intolerance, lactase deficiency, malabsorption of glucose-galactose or sucrase-isomaltase deficiency.

Loflatil® is not used for primary therapy of patients with:

– acute dysentery, which is characterized by presence of blood in stool and fever;

– acute ulcerative colitis;

– pseudomembranous colitis associated with broad spectrum of antibiotics;

– bacterial enterocolitis caused by invasive microorganisms, including Salmonella, Shigella and Campylobacter;

– liver dysfunction necessary for metabolism of the preparation, as far as it may cause a relative overdose.

Loflatil® must not be used at all if necessary to avoid the inhibition of peristalsis due to possible risk of significant complications, including ileus, megacolon and toxic megacolon.

PHARMACOLOGICAL PROPERTIES:

Loperamide Hydrochloride binds to opioid receptors of intestine wall that leads to inhibition of propulsive motility, slowing movement of intestinal content and enhancement of water resorption and electrolytes. Loperamide does not change physiological intestinal flora and improves the tone of anal sphincter that prevents fecal incontinence and reduces the amount of defecation urge to defecate.

Simethicone is an inert surface-active compound, which has defoaming properties and therefore relieves the symptoms associated with diarrhea, including bloating, abdominal discomfort, bloating and cramping.

Average half-life period of Loflatil® in human is 10.8 hours and varies 9 to 14 hours.

Loperamide Hydrochloride is readily absorbed from the intestine, but is almost completely extracted and metabolised by liver, where it is conjugated and excreted with the bile as conjugated metabolites. As a result of intense metabolism of the first passage plasma concentrations of unchanged Loperamide are very low. Loperamide metabolites are primarily excreted with faeces. Simethicone is not absorbed from the digestive tract at all.

PHARMACEUTICAL CHARACTERISTICS:

General physico-chemical properties:

Yellow, capsule shaped, film-coated tablets with a break line on one side.

Shelf-life:

3 years.

Storage:

Store in a dry, protected from light place at the temperature not more 25° C.

Keep it out of reach of children Package:

There are 10 tablets in a strip or blister, each strip or blister is in a carton pack, and there are 10 packs in a carton box.

Conditions of supply:

Without prescription:

There are 10 tablets in a blister, each blister is in a carton pack.

There are 10 tablets in a strip, each strip is in a carton pack.

With prescription:

There are 10 tablets in a blister, each blister is in a carton pack, and there are 10 packs in a carton box.

There are 10 tablets in a strip, each strip is in a carton pack, and there are 10 packs in a carton box.