Loperamide
Mechanism :
It is an opioid antimotility agent that suppresses gut movement and reduces gastrointestinal secretions. Loperamide acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide binds to the opiate receptor in the gut wall. Consequently, it inhibits the release of acetylcholine and prostaglandins, thereby reducing peristalsis, and increasing intestinal transit time. Loperamide increases the tone of the anal sphincter, thereby reducing incontinence and urgency.
Indication :
- Chronic diarrhea
- Short bowel syndrome
Contraindications :
Contraindicated in patients with a known hypersensitivity to loperamide; in patients with abdominal pain in the absence of diarrhea; in infants below 24 months of age; as the primary therapy- in patients with acute dysentery, which is characterized by blood in stools and high fever, in patients with acute ulcerative colitis, in patients with bacterial enterocolitis caused by invasive organisms including Salmonella, Shigella, and Campylobacter and in patients with pseudomembranous colitis associated with the use of broad-spectrum antibiotics.
Dosing :
Chronic diarrhea, Short bowel syndrome:
80-240 microgram/kg/day orally in two divided doses.
Adverse Effect :
Paralytic ileus, abdominal cramps and bloating of GIT, urticaria, skin reactions, dizziness, dry mouth, vomiting, nausea, tiredness, drowsiness, constipation.
Interaction :
Contraindicated:
Potassium acid phosphate, Potassium chloride, Potassium citrate, Potassium phosphate.
Avoid/Use Alternative:
Potassium iodide, Pramlintide.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
20-50 | Dose as in normal renal function |
10-20 | Dose as in normal renal function |
<10 | Dose as in normal renal function. Maximum dose usually 12 mg daily depending on tolerability |
Dose in Patients undergoing Renal Replacement Therapies
CAPD | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
HD | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
HDF/High flux | Unknown dialysability. Dose as in GFR<10 mL/min |
CAV/VVHD | Unlikely to be dialysed. Dose as in normal renal function |
Hepatic Dose :
No dose adjustments are recommended. Loperamide undergoes significant first-pass hepatic metabolism.