Dosage & Administration
The recommended dosage in adults is:
The recommended dosage in pediatric patients:
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.
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.
Note: It is not necessary to flush all the beads through to deliver the complete dose.
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Linzess Prescribing Information
LINZESS is contraindicated in:
- Patients less than 2 years of age due to the risk of serious dehydration[see Warnings and Precautions (5.1), Use in Specific Populations (8.4)].
- Patients with known or suspected mechanical gastrointestinal obstruction.
- Patients less than 2 years of age.
- Patients with known or suspected mechanical gastrointestinal obstruction.
LINZESS is contraindicated in patients less than 2 years of age. In neonatal mice (human age equivalent of approximately 0 to 28 days), linaclotide increased fluid secretion as a consequence of age-dependent elevated GC-C agonism which was associated with increased mortality within the first 24 hours due to dehydration. There was no age-dependent trend in GC-C intestinal expression in a clinical study of children 2 to less than 18 years of age; however, there are insufficient data available on GC-C intestinal expression in children less than 2 years of age to assess the risk of developing diarrhea and its potentially serious consequences in these patients
LINZESS is contraindicated in patients less than 2 years of age due to the risk of serious dehydration. In nonclinical studies, deaths occurred within 24 hours in neonatal mice (human age equivalent of approximately 0 to 28 days) following oral administration of linaclotide which increased fluid secretion as a consequence of age-dependent elevated GC-C agonism resulting in rapid and severe dehydration
In a clinical GC-C ontogeny study in children 6 months to less than 18 years of age (N=99) to measure GC-C mRNA expression levels in duodenal and colonic samples to evaluate the risk of diarrhea and severe dehydration due to GC-C agonism, there was insufficient data on GC-C intestinal expression to assess the risk of developing diarrhea and its potentially serious consequences in children less than 2 years of age
The safety and effectiveness of LINZESS for the treatment of FC have been established in pediatric patients 6 years of age and older. Use of LINZESS for this indication is supported by evidence from adequate and well-controlled studies in adults and pediatric patients 6 to 17 years of age. The safety of LINZESS in adult and pediatric patients in these clinical studies was similar
The safety and effectiveness of LINZESS for the treatment of FC have not been established in pediatric patients less than 6 years of age.
The safety and effectiveness of LINZESS for the treatment of IBS-C have been established in pediatric patients 7 years of age and older. Use of LINZESS for this indication is supported by evidence from adequate and well-controlled studies in adults and pediatric patients 7 to 17 years of age. The safety of LINZESS in adult and pediatric patients in these clinical studies was similar
The safety and effectiveness of LINZESS for the treatment of IBS-C have not been established in pediatric patients less than 7 years of age.
In toxicology studies in neonatal mice, oral administration of linaclotide at 10 mcg/kg/day caused deaths on post-natal day 7 (human age equivalent of approximately 0 to 28 days). These deaths were due to rapid and severe dehydration produced by significant fluid shifts into the intestinal lumen resulting from GC-C agonism in neonatal mice
Tolerability to linaclotide increases with age in juvenile mice. In 2-week-old mice, linaclotide was well tolerated at a dose of 50 mcg/kg/day, but deaths occurred after a single oral dose of 100 mcg/kg. In 3-week-old mice, linaclotide was well tolerated at 100 mcg/kg/day, but deaths occurred after a single oral dose of 600 mcg/kg.
Indications and Usage (1 INDICATIONS AND USAGE LINZESS is indicated for the treatment of: • irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older • chronic idiopathic constipation (CIC) in adults • functional constipation (FC) in pediatric patients 6 years of age and older LINZESS is a guanylate cyclase-C agonist indicated for treatment of:
| 11/2025 |
Dosage and Administration, Recommended Dosage (2.1 Recommended Dosage Irritable Bowel Syndrome with Constipation (IBS-C) : The recommended dosage of LINZESS is: • Adults : 290 mcg orally once daily• Pediatric patients 7 years of age and older : 145 mcg orally once dailyChronic Idiopathic Constipation (CIC) in Adults The recommended dosage of LINZESS in adults 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 Years of Age and Older The recommended dosage of LINZESS in pediatric patients 6 years of age and older is 72 mcg orally once daily. | 11/2025 |
Warnings and Precautions, Diarrhea (5.000000000000000e+00 2 Diarrhea In adults, diarrhea was the most common adverse reaction of LINZESS-treated patients in the pooled IBS-C and CIC double-blind placebo-controlled trials. The incidence of diarrhea was similar between the IBS-C and CIC populations. Severe diarrhea was reported in 2% of adult patients with IBS-C or CIC treated with LINZESS 145 mcg or 290 mcg once daily, and in <1% of adult patients with CIC treated with LINZESS 72 mcg once daily [see Adverse Reactions ( 6.1 )] .In pediatric patients, diarrhea was also the most common adverse reaction of LINZESS-treated patients in IBS-C and FC clinical trials. In two double-blind trials, diarrhea was reported in 4% of pediatric patients 6 to 17 years of age with FC treated with LINZESS 72 mcg once daily, and 7% and 8% of pediatric patients 7 to 17 years of age with IBS-C treated with LINZESS 145 mcg and 290 mcg once daily, respectively. In clinical trials, severe diarrhea was reported in one pediatric patient with FC treated with LINZESS 72 mcg once daily [see Adverse Reactions ( 6.1 )] and in one pediatric patient with IBS-C treated with LINZESS at a dosage higher than the recommended 145 mcg once daily dosage for IBS-C.In post-marketing experience, severe diarrhea associated with dizziness, syncope, hypotension and electrolyte abnormalities (hypokalemia and hyponatremia) requiring hospitalization or intravenous fluid administration have been reported in patients treated with LINZESS. If severe diarrhea occurs, suspend dosing and rehydrate the patient. | 11/2025 |
LINZESS is indicated for the treatment of:
• chronic idiopathic constipation (CIC) in adults
• functional constipation (FC) in pediatric patients 6 years of age and older
The recommended dosage in adults is:
- IBS-C: 290 mcg orally once daily. ()2.1Recommended DosageIrritable Bowel Syndrome with Constipation (IBS-C):
The recommended dosage of LINZESS is:
•
Adults: 290 mcg orally once daily•Pediatric patients 7 years of age and older: 145 mcg orally once dailyChronic Idiopathic Constipation (CIC)inAdultsThe recommended dosage of LINZESS in adults 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) inPediatric Patients6YearsofAge and OlderThe recommended dosage of LINZESS in pediatric patients 6 years of age and older is 72 mcg orally once daily.
- CIC: 145 mcg orally once daily or 72 mcg orally once daily based on individual presentation or tolerability. ()2.1Recommended DosageIrritable Bowel Syndrome with Constipation (IBS-C):
The recommended dosage of LINZESS is:
•
Adults: 290 mcg orally once daily•Pediatric patients 7 years of age and older: 145 mcg orally once dailyChronic Idiopathic Constipation (CIC)inAdultsThe recommended dosage of LINZESS in adults 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) inPediatric Patients6YearsofAge and OlderThe recommended dosage of LINZESS in pediatric patients 6 years of age and older is 72 mcg orally once daily.
The recommended dosage in pediatric patients:
- 7 years of age and older with IBS-C: 145 mcg orally once daily. ()2.1Recommended DosageIrritable Bowel Syndrome with Constipation (IBS-C):
The recommended dosage of LINZESS is:
•
Adults: 290 mcg orally once daily•Pediatric patients 7 years of age and older: 145 mcg orally once dailyChronic Idiopathic Constipation (CIC)inAdultsThe recommended dosage of LINZESS in adults 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) inPediatric Patients6YearsofAge and OlderThe recommended dosage of LINZESS in pediatric patients 6 years of age and older is 72 mcg orally once daily.
- 6 years of ageand olderwithFC: 72 mcg orally once daily. ()2.1Recommended DosageIrritable Bowel Syndrome with Constipation (IBS-C):
The recommended dosage of LINZESS is:
•
Adults: 290 mcg orally once daily•Pediatric patients 7 years of age and older: 145 mcg orally once dailyChronic Idiopathic Constipation (CIC)inAdultsThe recommended dosage of LINZESS in adults 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) inPediatric Patients6YearsofAge and OlderThe recommended dosage of LINZESS in pediatric patients 6 years of age and older is 72 mcg orally once daily.
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.
- Place one teaspoonful of room-temperature applesauce into a clean container.
- Open the capsule.
- Sprinkle the entire contents (beads) on applesauce.
- Consume the entire contents immediately. Do not chew the beads. Do not store the bead-applesauce mixture for later use.
- Pour approximately 30 mL of room-temperature bottled water into a clean cup.
- Open the capsule.
- Sprinkle the entire contents (beads) into the water.
- Gently swirl beads and water for at least 20 seconds.
- Swallow the entire mixture of beads and water immediately.
- Add another 30 mL of water to any beads remaining in cup, swirl for 20 seconds, and swallow immediately.
- 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.
- Open the capsule and empty the beads into a clean container with 30 mL of room-temperature bottled water.
- Mix by gently swirling beads for at least 20 seconds.
- 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.
- Add another 30 mL of water to any beads remaining in the container and repeat the process.
- 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.
- Take on empty stomach at least 30 minutes prior to a meal at approximately the same time each day.
- Do not crush or chew LINZESS capsule or capsule contents.
- For patients who have difficulty swallowing capsules whole or those with a nasogastric or gastrostomy tube, see full prescribing information for instructions for opening the capsule and administering with applesauce or water.
LINZESS capsules are white to off-white opaque:
- 72 mcg; gray imprint “FL 72”
- 145 mcg; gray imprint “FL 145”
- 290 mcg; gray imprint “FL 290”
Linaclotide and its active metabolite are negligibly absorbed systemically following oral administration
LINZESS is minimally absorbed with negligible systemic availability following oral administration. Concentrations of linaclotide and its active metabolite in plasma are below the limit of quantitation after oral doses of 72 mcg, 145 mcg, or 290 mcg were administered. Therefore, standard pharmacokinetic parameters such as area under the curve (AUC), maximum concentration (Cmax), and half-life (t½) cannot be calculated.
Neither linaclotide nor its active metabolite were detected in the plasma following administration of LINZESS 290 mcg once daily for 7 days both in the non-fed and fed state in healthy subjects.
Given that linaclotide plasma concentrations following recommended oral doses are not measurable, linaclotide is not expected to be distributed to tissues to any clinically relevant extent.
Linaclotide is metabolized within the gastrointestinal tract to its principal, active metabolite by loss of the terminal tyrosine moiety. Both linaclotide and the metabolite are proteolytically degraded within the intestinal lumen to smaller peptides and naturally occurring amino acids.
Active peptide recovery in the stool samples of fed and fasted healthy subjects following administration of LINZESS 290 mcg once daily for seven days averaged about 5% (fasted) and about 3% (fed) and all of it as the active metabolite.
Renal or hepatic impairment is not expected to affect the clearance of linaclotide or the active metabolite because linaclotide metabolism occurs within the gastrointestinal tract and plasma concentrations are not measurable in plasma following administration of the recommended dosage.
No drug-drug interaction studies have been conducted with LINZESS. Systemic exposures of drug and active metabolite are negligible following oral administration.
Linaclotide does not interact with the cytochrome P450 enzyme system based on the results of in vitro studies. In addition, linaclotide does not interact with common efflux and uptake transporters (including the efflux transporter P-glycoprotein (P-gp)). Based on these
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the United States general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
The potential for linaclotide to cause harm to embryo-fetal development was studied in rats, rabbits and mice. In pregnant mice, oral dose levels of at least 40,000 mcg/kg/day given during organogenesis produced severe maternal toxicity including death, reduction of gravid uterine and fetal weights, and effects on fetal morphology. Oral doses of 5,000 mcg/kg/day did not produce maternal toxicity or any adverse effects on embryo-fetal development in mice. Oral administration of up to 100,000 mcg/kg/day in rats and 40,000 mcg/kg/day in rabbits during organogenesis produced no maternal toxicity and no effects on embryo-fetal development. Additionally, oral administration of up to 100,000 mcg/kg/day in rats during organogenesis through lactation produced no developmental abnormalities or effects on growth, learning and memory, or fertility in the offspring through maturation.
The maximum recommended human dose is approximately 5 mcg/kg/day, based on a 60-kg body weight. Limited systemic exposure to linaclotide was achieved in animals during organogenesis (AUC = 40, 640, and 25 ng•hr/mL in rats, rabbits, and mice, respectively, at the highest dose levels). Linaclotide and its active metabolite are not measurable in human plasma following administration of the recommended clinical dosages. Therefore, animal and human doses should not be compared directly for evaluating relative exposure.