Drug Interaction:
Bioavailability increased by co-tromoxazole, ritonavir, saquuinnavir.
Respiratory depressin reported when administered with quinidine
Loperamide increases GI absorption of desmopression and decrease exposure to saquinavir
Indication:
Diarrhoea.
FIXED DOSE COMBINATIONS APPROVED BY DCG(I)
FROM JANUARY 1961 TILL NOVEMBER 2014
Name of Drug Indication Date of Approval
Loperamide Hcl 2mg + 16-10-2001
Simethicone 125mg tablet
For control of diarrhoea in adults only
Adverse Reaction:
Abdominal pain, distention, discomfort, constipation, dry mouth, nausea, vomiting, drowsiness, fatigue, rash, toxic megacolon in colitis.
Contra-Indications:
Condition when inhibition of persitalsis is undesirable ( e.g. ileus or megacolon ) antibiotic induced cloitis, active inflammatory bowel disease, if abdominal distention develops during use , abdominal pain in absence of diarrheoa
Special precautions:
Concomittant specific therapy must given in those with infectious diarrhoeas, hepatic dysfunction.Inflammatory bowel disease. Pregnancy and lactation
Dosages/ Overdosage Etc:
Inications:
Diarrhoea.
Dosage: Adults- 4mg after loose bowel movement followed by 2mg. Do not exceed 8mg/day for no more than 2 days.
Patient Information:
LOPERAMIDE-
1.Do not exceed the prescribed dose.
2.May cause drowsiness or dizziness.Use caution while driving or performing tasks which require alertness, coordination or physical dextrity.
3.May cause dryness of mouth.
4.Inform your doctor if diarrhoea persists or if fever,palpitations or abnormal distention occur.
5. Allergies- Tell your doctor if you have had any allergic reactions to loperamide or any food substances, preservative, or dyes
6. Pregnancy- studies not done on humans. However studies in animals have not shown that loperamide causes cancerr or birth defects or lessens the chances of becoming pregnant even when given in doses many times the human dose.
7. Breast feeding- not known whether loperamide passes into breast milk. Mothers who are taking this medicine wish to breast feed shold discuss this with their doctor.
8. Children- medicine should not be used in children under 6 years of age unless directed by the doctor. Very young children are very sensitive to the effects of lopramide and may incr the chances of side effects during treatment. Also fluid loss caused by darrhea may result in a serious health problems. Do not give medicine to children without first checking with the doctor.
9. Older adults- fluid loss caused by diarrhea may causeserioushealth problems ( dehydration ) . Loperamide may hide the symptoms of dehydration. For this reason elderly persons with diarrhea in addtion to using this medicine for diarrhea must receive a sufficient amount of liquids to replace fluid lost by the body.
10. Other medicines- tell your doctor if you are taking any other medicines- Antibiotics such as Cephalosporins Cindamycin Erythromycin Achromycin- these antibiotics cause diarrhea ,loperamide make the diarrhea caused by antibiotics or make it last longer or worse Narcotic pain medicine- greater chance that severe constipation may occur if loperamide is used together with narcotic medicine.
11. Other medical problems- Tellyourdoctor if have other medical problems- suc as- Colitis- a more serious problem ofvthe colon may develop of youuseloperamide Dysentry-condition may get worse , a different kind of treatment may be needed Liver disease- chance of severe central nervous system side effects may be greater in patients with liver diseases
12. Dosing- follow your doctors orders. doseofloperamidedosemay bedifferntfor different persons- Do not change unless your doctor tells you to do so.
12. Missed dose- If you miss a dose take it as sooas yurember. If it isalmosttime for the followingdose. skip the dose and go back to yurnormal schedule Do not double doses.
13. Storage- Keep out of reach of children Store away from heat and direct sunlight Do not store medicines in the bathroom, near the kitchen sink or in damp places. Heat and moisture may cause the medicine to break down.
Keep the liquid form of medicines from freezing Do not keep outdated medicines or medicine no longer needed. Be sure that the disacarded medicines is keptout of the reach of children.
Pharmacology/ Pharmacokinetics:
Pharmacology:
Loperamide slows intestinal mobility and affects water and electrolyte movement through the bowel. It inhibits peristaltis by a direct effect on the circular and longitudinal muscles of the intestinal wall.It reduces daily fecal volume,increases viscocity and bulk density and diminishes loss o fluid and electrolytes.
Pharmacokinetis:
Loperamide is 40% absorbed after oral administration and does not penetrate well into the brain. Peak plasma levels appear approximately 5 hours after capsule administration,2.5 hours after liquid administration and are similar for both the formulations. Metabolism: The apparent elimination half-life is 10.8 hours(range 9.5 to 14.4 hous). Of a 4mg oral dose,25% is excreted unchanged in the faces,and 1.3% is excreted in the urine as free drug and glucuronic and congugate within 3 days.
Interaction with Food:
None reported
Pregnancy and lactation:
Pregnancy:
Safety for use during pregnancy has not been established.
Use with caution.
Lactation:
Safety for use in the nursing mother has not been established.