Linaclotide (Linzess) is an orally available, non-absorbable medicine that acts on the intestinal lumen relieving the symptoms of constipation and visceral pain.

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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):

• Gastrointestinal:

  • Diarrhea

Less Common Side Effects of Linaclotide (Linzess):

• Central Nervous System:

  • Headache
  • Fatigue

• Endocrine & Metabolic:

  • Dehydration

• Gastrointestinal:

  • Abdominal Pain
  • Flatulence
  • Abdominal Distension
  • Viral Gastroenteritis
  • Severe Diarrhea
  • Dyspepsia
  • Fecal Incontinence
  • Gastroesophageal Reflux Disease
  • Vomiting

• Respiratory:

  • Upper Respiratory Tract Infection
  • Sinusitis

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

• Diarrhea:
  • 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.

Monitor:

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.

Notice:

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.

Notice:

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.

Systemic Absorption

• It is very low. Plasma concentrations cannot be measured at the recommended doses.

Metabolism:

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• 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.

Excretion:

• Primarily feces (3% to 5%; as the active metabolite)

International Brands of Linaclotide:

• Linzess
• Constella

Linaclotide Brand Names in Pakistan:

No Brands Available in Pakistan.