Linaclotide (Linzess) is an orally available, non-absorbable medicine that acts on the intestinal lumen relieving the symptoms of constipation and visceral pain.
Linaclotide (Linzess) Indications:
It is indicated in adult patients for the treatment of:
- chronic idiopathic constipation in adults.
- Irritable bowel syndrome with constipation (IBS-C):
Linaclotide (Linzess) dose in Adults:
Linaclotide (Linzess) Dose in the treatment of chronic idiopathic constipation (CIC):
- 145 mcg orally once a day.
- A lower dose of 72 mcg once a day may be used in some patients based on the presentation and tolerability.
Linaclotide (Linzess) Dose in the treatment of Irritable bowel syndrome with constipation (IBS-C):
- 290 mcg orally once a day.
Linaclotide (Linzess) use in Children:
The safety and efficacy of the drug in children have not been established.
Pregnancy Risk Category: N (not assigned)
- Infant drug exposure is much less likely because the drug has low systemic absorption.
Linaclotide can be used during breastfeeding
- When administered in the recommended doses, the drug and its activemetabolites are not absorbed.
- It is unknown whether the drug will be excreted into breastmilk.
- Manufacturers recommend weighing the risks to the infant and the benefits to the mother when considering treatment.
Linaclotide (Linzess) dose in kidney disease:
- Adjustment in the dose in not necessary.
Linaclotide (Linzess) dose in liver disease:
- Adjustment in the dose in not necessary.
Common Side Effects of Linaclotide (Linzess):
Less Common Side Effects of Linaclotide (Linzess):
Central Nervous System:
Endocrine & Metabolic:
- Abdominal Pain
- Abdominal Distension
- Viral Gastroenteritis
- Severe Diarrhea
- Fecal Incontinence
- Gastroesophageal Reflux Disease
- Upper Respiratory Tract Infection
Contraindications to Linaclotide (Linzess):
- Allergic reactions to the drug or any component of the formulation
- Pediatric patients less than 6 years of age
- patients with a known or suspected mechanical gastrointestinal obstruction.
Warnings and Precautions
- Linaclotide may cause diarrhea that may be associated with volume loss if severe.
- Diarrhea may be more severe if the drug is taken with a high-fat meal.
- Patients may develop syncope, dizziness, hypotension, and electrolyte abnormalities (hyponatremia and hypokalemia) that may require hospitalization.
- In severe cases, treatment should be discontinued and the patient should be resuscitated with intravenous fluids.
IBS-C (IBS with predominant constipation):
- Monitor for abdominal pain,
- Bowel movements
- Quality and frequency of bowel movements
CIC (chronic idiopathic constipation):
- Frequency of spontaneous bowel movements
- Quality of bowel movements
- Frequency of straining during bowel movements.
How to administer Linaclotide (Linzess)?
- You should swallow the capsule whole. You should take the capsule on an empty stomach.
- It is best to do this at least 30 minutes before eating. High-fat meals can cause severe diarrhea or dehydration.
- Individuals who are unable to swallow the capsule whole can open it and mix the contents in water or applesauce.
- They can then administer the medication orally or through a nasogastric tube.
Administration of the drug in applesauce
- Take 1 teaspoon (5 mL) of the contents from the capsule.
- All contents must be taken in one go. The beads should not ever be chewed or stored for future uses.
Water is used for the administration of the drug
- Place the contents of 1 capsule in a cup of 30ml water. Boil and cool to room temperature.
- Mix the mixture for 20 seconds. Then, drink it immediately. Mix 30 ml more water and swirl the mixture.
- It is not recommended to store the mixture for future use.
The drug is embedded on the beads' surface. The drug is not required to be dissolved in its entirety.
Linaclotide can be administered via a nasogastric tube or gastric feeding tube.
- Mix the contents of the capsule in 30ml water. Boil the water and let it cool to room temperature.
- Mixture is gently stirred for 20 seconds, and then aspirated using the feeding syringe. Use a steady pressure to force the beads-water mixture into a tube.
- You can repeat the procedure by adding 30 ml more water to any beads that are still in tact.
- After the administration of the drug, the nasogastric/gastric tube should be flushed in warm water with at least 10ml.
You don't have to dissolve all beads and flush them through a tube in order to get the entire dose.
Mechanism of action of Linaclotide (Linzess):
- Linaclotide, along with its active metabolites, bind to and activate Guanylate Cyclose-C at the luminal surface the intestinal epithelium.
- This causes an increase in intracellular and extracellular levels of cyclic Guanosine monophosphate (cGMP), which results in chloride and bicarbonate efflux to the intestinal lumen.
- The result is an increase in GI transit.
- The increase in extracellular cGMP can also reduce visceral pain through reducing pain-sensing neuro activity.
- It is very low. Plasma concentrations cannot be measured at the recommended doses.
- The active metabolites are formed within the GI tract. By proteolytic degrading, the metabolites and parent drug are converted to smaller peptides or amino acids in the intestinal lumen.
- Primarily feces (3% to 5%; as the active metabolite)
International Brands of Linaclotide:
Linaclotide Brand Names in Pakistan:
No Brands Available in Pakistan.