Linzess

Linzess is an oral medication for the treatment of constipation. It is the first in a new class of drugs called guanylate cyclase-C agonists. It is used for relieving symptoms of irritable bowel syndrome with constipation (IBS-C) and for treating chronic constipation of unknown cause (idiopathic constipation) in adults.

Linzess is also used to treat functional constipation in children and adolescents 6 to 17 years of age. It is not known if Linzess is safe and effective in children with functional constipation less than 6 years of age or in children with IBS-C less than 18 years of age.

Linzess works locally in the intestine (it is not absorbed into the body) to increase bowel movements and reduce pain. Linaclotide's effects are due to an increase in the production of a chemical called cyclic guanosine monophosphate which increases fluid secretion into the intestine and reduces the sensitivity of pain-sensing nerves. The FDA approved linaclotide in August 2012.

Risk of serious dehydration in pediatric patients less than 2 years of age

Linzess is contraindicated in patients less than 2 years of age; in nonclinical studies in neonatal mice, administration of a single, clinically relevant adult oral dose of linaclotide caused deaths due to dehydration

The most common side effects of linaclotide are:

• diarrhea,
• stomach pain,
• gas, and
• stomach distention.

Linaclotide should be stopped if patients develop severe diarrhea. Other important side effects include:

• headache,
• fatigue,
• respiratory infections,
• sinusitis, and
• stomach or intestinal viral infections.

Rarely, patients may experience passage of blood from the rectum.

Linaclotide should be taken on an empty stomach at least 30 minutes before the first meal of the day at approximately the same time. 

For patients who are unable to swallow the capsule whole, Linzess capsules can be opened and administered orally in either applesauce or with bottled water or administered with water via a nasogastric or gastrostomy tube.

Irritable Bowel Syndrome with Constipation (IBS-C) In Adults

The recommended dosage of Linzess is 290 mcg orally once daily.

Chronic Idiopathic Constipation (CIC) in Adults

The recommended dosage of Linzess is 145 mcg orally once daily. A dosage of 72 mcg once daily may be used based on individual presentation or tolerability.

Functional Constipation (FC) in Pediatric Patients 6 To 17 Years of Age

The recommended dosage of Linzess is 72 mcg orally once daily.

Preparation and Administration Instructions

• Take Linzess on an empty stomach, at least 30 minutes prior to a meal, at approximately the same time each day.
• If a dose is missed, skip the missed dose and take the next dose at the regular time. Do not take 2 doses at the same time.
• Do not crush or chew Linzess capsule or capsule contents.
• Swallow Linzess capsule whole.
• For patients who are unable to swallow the capsule whole, LINZESS capsules can be opened and administered orally in either applesauce or with water or administered with water via a nasogastric or gastrostomy tube. Sprinkling of LINZESS beads on other soft foods or in other liquids has not been tested.

Oral Administration in Applesauce

1. Place one teaspoonful of room-temperature applesauce into a clean container.
2. Open the capsule.
3. Sprinkle the entire contents (beads) on applesauce.
4. Consume the entire contents immediately. Do not chew the beads. Do not store the bead-applesauce mixture for later use.

Oral Administration in Water

1. Pour approximately 30 mL of room-temperature bottled water into a clean cup.
2. Open the capsule.
3. Sprinkle the entire contents (beads) into the water.
4. Gently swirl beads and water for at least 20 seconds.
5. Swallow the entire mixture of beads and water immediately.
6. Add another 30 mL of water to any beads remaining in cup, swirl for 20 seconds, and swallow immediately.
7. Do not store the bead-water mixture for later use.

Note

The drug is coated on the surface of the beads and will dissolve off the beads into the water. The beads will remain visible and will not dissolve. Therefore, it is not necessary to consume all the beads to deliver the complete dose.

Administration with Water via A Nasogastric or Gastrostomy Tube

1. Open the capsule and empty the beads into a clean container with 30 mL of room temperature bottled water.
2. Mix by gently swirling beads for at least 20 seconds.
3. Draw-up the beads and water mixture into an appropriately sized catheter-tipped syringe and apply rapid and steady pressure (10 mL/10 seconds) to dispense the syringe contents into the tube.
4. Add another 30 mL of water to any beads remaining in the container and repeat the process.
5. After administering the bead-water mixture, flush nasogastric/ gastrostomy tube with a minimum of 10 mL of water.

Note

It is not necessary to flush all the beads through to deliver the complete dose.

Drug interaction studies have not been conducted.

Linaclotide has not been adequately evaluated in pregnant women.

It is not known whether linaclotide is excreted in human milk. It is unlikely that linaclotide is excreted in breast milk because it is poorly absorbed and therefore undetectable in blood at recommended doses.

What preparations of linaclotide (Linzess) are available?

Capsules: 145 and 290 mcg

How should I keep linaclotide (Linzess) stored?

Linaclotide should be stored at room temperature, 15 C to 30 C (59 F to 86 F). It should be kept in the original container and protected from moisture. The dessicant (drying agent) should not be removed from the container.