Diaflush Loperamide Hydrochloride Capsules

DIAFLUSH
Loperamide Hydrochloride Capsules USP 2mg

 

For medical/pharmacy professionals only

 

DOSAGE FORM AND STRENGTH

Dosage Form: Capsule

Strength: 2mg

 

HISTORY OF ACTIVE INGREDIENTS

Loperamide Hydrochloride is a piperidine derivative, an opioid antimotility drug used against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.

 

NET CONTENT

Composition
Each Hard Gelatin Capsule contains:
Loperamide Hydrochloride USP 2mg
Excipients q.s.
Approved colours used in empty capsule shells.

 

CLINICAL PHARMACOLOGY

ATC CODE: A07DA03

 

PHARMACODYNAMICS

Loperamide hydrochloride is a synthetic opioid which inhibits gut motility by binding to opiate receptors in the gut wall and may also reduce gastrointestinal secretions, resulting in improvement in diarrhoea symptoms. Loperamide aIso increases the tone of the anal sphincter.

 

PHARMACOIGNETICS

More than 65% of a dose of loperamide is reported to be absorbed from the gastrointestinal tract. The drug undergoes considerable first pass metabolism in the liver and excretion via the bile in the faeces as the inactive conjugate. As a result of the drugs high affinity for the gut wall and its high first pass metabolism very little loperamide reaches the systemic circulation and therefore there is only a small amount of urinary excretion. The elimination half life is reported to be about 10 hours.

 

INDICATION USAGE

For the symptomatic treatment of acute diarrhoea, in adults and children 6 years and over.

For the symptomatic treatment of acute episodes of diarrhoea associated with acute bowel syndrome in adults and aged above 18 years over following initial diagnosis by a doctor.

 

CONTRAINDICATION

Loperamide Hydrochloride is contraindicated in patients with known hypersensitivity to loperamide HCI or to any of the excipients.

 

INTERACTIONS

Non-clinical data have shown that loperamide is a P-glycoprotein substrate. Concomitant administration of loperamide (16mg single dose) with quinidine, or ritonavir, resulted in a 2 to 3-fold increase in loperamide plasma levels. The clinical relevance of this pharmacokinetic interaction with P-glycoprotein inhibitors, when loperamide is given at recommended doses, is unknown. The concomitant administration of loperamide (4 mg single dose) and itraconazole, resulted in a 3 to 4-fold increase in loperamide plasma concentrations. The concomitant administration of loperamide (16 mg single dose) and ketoconazole, an inhibitor of CYP3A4 and P-glycoprotein, resulted in a 5-fold increase in loperamide plasma concentrations. The increase was not associated with increased pharmacodynamic effects as measured by pupillometry. Concomitant treatment with oral desmopressin resulted in a 2-fold increase of desmopressin plasma concentrations, presumably due to slower gastrointestinal motility.

 

WARNINGS

Only take Ioperamide HCI to treat acute episodes of diarrhoea associated with irritable bowel syndrome (IBS) if your doctor has previously diagnosed IBS.

If any of the following now apply, do not use the product without first consulting your doctor even if you know you have IBS:

If you are 40 years or over and it is some time since your last attack of IBS or the symptoms are different this time.

If you have recently passed blood from the bowel.

If you suffer from severe constipation.

If you are feeling sick or vomiting.

If you have lost your appetite or lost weight.

If you have difficulty or pain passing urine.

If you have a fever.

If you have recently travelled abroad.

Consult your doctor if you develop new symptoms, or if your symptoms worsen, or if your symptoms have not improved over two weeks.

 

PREGNANCY AND LACTATION

It is not advisable to administer this medicine in pregnancy. Women who are pregnant or breast feeding should therefore be advised to consult their doctor for appropriate treatment.

Although there is no indication that loperamide HCI possesses teratogenic or embryotoxic properties it should not be administered in pregnancy.

Small amounts of loperamide HCI may appear in human breast-milk. Therefore loperamide HCI is not recommended during breast-feeding.

 

ADVERSE REACTIONS

Headache, hypersensitivity reactions, dizziness, vomiting, constipation, nausea, urinary retention, fatigue, dyspepsia, Abdominal distention, flatulence, megacolon, abdominal pain, abdominal discomfort.

 

OVERDOSE

In case of overdose (including relative overdose due to hepatic dysfunction), CNS depression (stupor, coordination abnormality, somnolence, miosis, muscular hypertonia, and respiratory depression), urinary retention, constipation and ileus may occur. Children may be more sensitive to CNS effects than adults.

 

Treatment

If symptoms of overdose occur, neloxone can be given as an antidote. Since the duration of action of loperamide is longer than that of naloxone (Ito 3 hours), repeated treatment with naloxone might be indicated. Therefore, the patient should be monitored closely for at least 48 hours in order to detect possible CNS depression.

 

DOSAGE AND ADMINISTRATION

As directed by the physician.

 

PACK SIZE

10 x 1 x 10 Capsules in a carton along with leaflet.

 

STORAGE

Store in a dry place at temperature below 25oC. Protect from light.

Keep all medicines out of the reach of children.

 

NAFDAC Reg. No.: 044639

 

Manufactured in India by

LABORATE PHARMACEUTICAL (INDIA)

E-11, Ind. Area, Panipat-132 103

 

Sole Agent

EMBASSY PHARMACEUTICAL & CHEMICALS LTD.

Lagos, Nigeria.