loperamide and furazolidone

Action and Spectrum

Actions and spectrum: 

loperamide: 

• Action: loperamide is an antidiarrheal medication. It acts by binding to receptors in intestines, slowing down the movement of the gut muscles. This results in increased absorption of water and electrolytes, leading to firmer stools and reduced diarrhea. 
• Spectrum: loperamide is primarily used to treat acute and chronic diarrhea. It is effective in managing diarrhea associated with various causes, including viral infections, food poisoning, traveler’s diarrhea, and irritable bowel syndrome with diarrhea. 

furazolidone: 

• Action: furazolidone is an antibiotic with antimicrobial properties. It acts by inhibiting growth and replication of certain bacteria and other microorganisms. It can also have some activity against protozoa. 
• Spectrum: furazolidone is used to treat bacterial and protozoal infections, particularly those affecting the gastrointestinal tract. It is effective against certain bacteria, including those that can cause foodborne illnesses and some types of diarrhea. It may also have activity against certain parasitic infections. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Dizziness 

Nausea 

Decreased B.P 

Urticaria 

Arthralgia 

Headache

Vomiting 

Deafness 

Fever 

Dry mouth 

Gastric discomfort 

Constipation 

Abdominal pain 

Drowsiness 

Tiredness 

Allergic reaction 

Black Box Warning

Black Box Warning: 

There is no specific black box warning associated with the combination of loperamide and furazolidone. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Known Allergy: Individuals with a known allergy or hypersensitivity to loperamide or any of its components should not use this medication. 
• Acute Dysentery: loperamide is not recommended for the treatment of acute dysentery (bloody diarrhea), as it may prolong the infection. 
• Bacterial Enterocolitis: loperamide is contraindicated in cases of bacterial enterocolitis (infection of the intestines caused by certain bacteria) because it may inhibit the body’s ability to clear the infection. 
• Monoamine Oxidase Inhibitors (MAOIs): furazolidone interacts with MAOIs, a class of antidepressant medications. It can lead to a potentially life-threatening hypertensive crisis. Therefore, individuals taking MAOIs or who have taken them within the past two weeks should not use furazolidone.

Caution: 

• Cardiac Effects: High doses of loperamide can affect the heart’s electrical activity and may lead to serious cardiac events, including arrhythmias. Combining it with other medications, especially those that affect the heart, should be done with caution. 
• Liver Function: loperamide should be used with caution in individuals with liver disease, as it may accumulate to higher levels in the body and cause adverse effects. 
• Neuropathy: Long-term use of furazolidone has been associated with peripheral neuropathy (nerve damage) in some cases. Be cautious if you have a history of neuropathy or nerve disorders. 
• Children: furazolidone is typically not recommended for use in children under the age of 1 or as otherwise specified by a healthcare provider.

Comorbidities: 

• Cardiac Conditions: Individuals with pre-existing cardiac conditions, such as arrhythmias or heart rhythm disorders, should use loperamide with caution, especially if considering higher doses than recommended. 
• Gastrointestinal Conditions: Individuals with certain gastrointestinal conditions, such as inflammatory bowel disease (IBD), should consult a healthcare provider before using loperamide. 
• Pregnancy and Breastfeeding: furazolidone should be used with caution during pregnancy and lactation, and its use should be determined by a healthcare provider. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

loperamide is an antidiarrheal medication that works by binding to specific receptors in the intestines. This action slows down the movement of gut muscles, allowing for increased absorption of water and electrolytes. As a result, loperamide helps to firm up stools and reduce diarrhea. It primarily acts locally within the gastrointestinal tract. 

furazolidone, on the other hand, is an antibiotic with antimicrobial properties. It functions by inhibiting the growth and replication of certain bacteria and protozoa, particularly those affecting the gastrointestinal tract. The combination of these two medications would theoretically aim to address both the antimicrobial and antidiarrheal aspects of certain gastrointestinal infections.  

Pharmacodynamics: 

• Action on Gut Motility: loperamide primarily acts within the gastrointestinal tract. It binds to opioid receptors in the intestinal wall, specifically the mu-opioid receptors. This binding reduces the activity of the intestinal muscles, leading to decreased motility and transit time. Slowing down gut motility allows for increased absorption of water and electrolytes, resulting in firmer stools and a reduction in the frequency and urgency of diarrhea. 
• Local Effect: loperamide’s effects are local and limited to the gastrointestinal system. It does not cross blood-brain barrier, which helps minimize central nervous system side effects commonly associated with opioids. 
• Inhibition of Microbial Growth: furazolidone inhibits the growth and replication of certain bacteria and protozoa by interfering with their metabolic processes. It acts on microbial enzymes, disrupting their ability to function properly. This antimicrobial effect targets infections within the gastrointestinal tract.

Pharmacokinetics: 

loperamide: 

• Absorption: loperamide is absorbed from gastrointestinal tract after oral administration. It undergoes first-pass metabolism in the liver, resulting in limited systemic exposure. The absorption is rapid, with peak plasma concentrations occurring within 2 to 5 hours. 
• Distribution: loperamide is distributed primarily to the gastrointestinal tissues, where it exerts its local effects. It has a limited distribution to other body tissues and does not readily cross the blood-brain barrier, which helps prevent central nervous system side effects. 
• Metabolism: loperamide undergoes extensive metabolism in the liver, primarily via cytochrome P450 enzymes, including CYP2C8 and CYP3A4. The major metabolite, desmethylloperamide, is pharmacologically active and contributes to the antidiarrheal effects. 
• Excretion: Both loperamide and its metabolites are excreted in the urine and feces, with a half-life of 9 to 14 hours.  

furazolidone: 

• Absorption: furazolidone is absorbed from the gastrointestinal tract after oral administration. Its absorption may be affected by food, with better absorption observed on an empty stomach.  
• Distribution: furazolidone is distributed widely throughout the body, including various tissues and body fluids. It can reach therapeutic concentrations in the gastrointestinal tract, where it exerts its antimicrobial effects. 
• Metabolism: furazolidone undergoes metabolic transformations in the liver. It is metabolized into various metabolites, some of which have antimicrobial activity. The exact metabolic pathways and active metabolites may vary between individuals. 
• Excretion: furazolidone and its metabolites are primarily excreted in the urine. The elimination half-life is short, ranging from 2 to 4 hours. 

Adminstartion

Administration: 

• Dosage: The dosage of each medication and the dosing schedule would be determined by the healthcare provider based on the specific clinical condition being treated. It is crucial to follow the prescribed dosages carefully. 
• Timing: The timing of administration may be specified by the healthcare provider. For instance, they may recommend taking one medication before the other, or they may stagger the dosages to optimize their effects. 
• Duration: The duration of treatment with this combination will depend on nature and severity of the condition. Patients should complete the full course of treatment as prescribed, even if symptoms improve before the medication is finished. 
• Food Interactions: Some medications are best taken on an empty stomach, while others may be taken with food. Patients should follow any food-related instructions provided by their healthcare provider or on the medication labels. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: loperamide and furazolidone 

Pronounced: (loh-PER-uh-mide-and- fyoor-a-ZOHL-i-dohn)  

Why do we use loperamide and furazolidone? 

It is widely used to relieve acute diarrhea, including diarrhea and diarrhea associated with gastrointestinal infections. It works by slowing down gut motility and reducing the frequency of bowel movements. It may be prescribed to treat bacterial and protozoal infections in gastrointestinal tract, such as those caused by certain strains of bacteria or protozoa responsible for foodborne illnesses and diarrhea. It has been used as part of combination therapy to eradicate Helicobacter pylori, a bacterium associated with peptic ulcers and gastritis.