Known Uses and side effects of Linzess (Laxative)

By Tamon

What is Linzess?

Linzess (linaclotide) is a laxative, a medication that softens the content of the intestine and eases the passing out of feces.  It works by increasing the secretion of chloride and water in the intestines, which can help soften stools and stimulate bowel movements. Linzess uses Guanylate Cyclase-C (GC-C) agonist, which is a substance that stimulates the secretion of bicarbonate and chloride into the intestinal lumen, which then increases intestinal fluid and accelerates intestinal transit.

Linzess is a prescription medicine that is used to treat cases of chronic constipation, or a chronic irritable bowel syndrome (IBS) in adults who have actually had constipation as the main symptom. However, the safety and effectiveness of Linzess has not yet been established in patients who are under 18 years of age. As one of the uses of Linzess, we have seen that it helps to initiate bowel movement. That notwithstanding the dosage of Linzess should strictly be followed as advised by your pharmacist or health care provider. In a nut shell if one does not seek advice from a medical expert before consumption, the patient may experience some negative side effects of Linzess. Looking at Linzess uses, some points will be repeated below for emphasis.

Linzess Uses (Uses of Linzess)

Linzess increases the secretion of chloride and water in the intestines is used to control the following;

Irritable bowel syndrome coupled with constipation

Chronic idiopathic constipation

Important information

Linzess is not recommended for use by people who have a blockage in your intestines.

Linzess should also not be given to children who are younger than 6 years old. The active component, Linaclotide has been associated with severe dehydration in children younger than 6 years. Thus, this medication should never be given to children or teenagers unless it’s been prescribed by a medical professional whom must have evaluated the benefits and risk to potential side effects.

It is advisable that you take Linzess very early in the morning before taking any meal (on an empty stomach) and waiting about least 30 minutes before taking your first meal. Do not chew, crush, break, or open the Linzess capsule. Swallow it in its whole form.

Some side effects of Linzess can be serious thus, we recommend immediately stopping the use of this medication and call your health care provider if you notice any symptom of Linzzess side effects such as bloody, black, or tarry stools, severe or ongoing diarrhea, or severe stomach pain.

People with allergic to lincaclotide and other stomach complications should not use Linzess for whatever reason unless it’s being administered and monitor by a medical professional.


Beside the fact that Linaclotide can cause severe dehydration in a child, it is not yet known whether Linzess will harm an unborn baby. It is however important to inform your doctor if you are pregnant or plan to become pregnant while using this drug.

Similarly, it is not known whether linaclotide passes into breast milk or if it could cause harm to a nursing baby. Inform your doctor if you are breast-feeding a baby.

How should I take Linzess?

Take Linzess exactly as prescribed by your health expert. Follow the directions on your prescription label or leaflet. It is not healthy for you to take this medicine in larger or smaller amounts or for longer than recommended.

Take your dose of Linzess very early in the morning before the consumption of any meal, and wait about 30 minutes having your first meal for the day.

You should not grind, chew, or break a Linzess capsule. Swallow the capsule in its entirety.

However, if you cannot swallow the capsule whole or if you have swallowing difficulties, you may just open the capsule and sprinkle the contents (medicine) into a spoonful of applesauce or bottled water. Do not chew, grind or break this medicine before swallowing. Once you have taken out a drug do not save it for future use.

However, you may want to take this drug, it is very important that you take it on an empty stomach, early in the morning and give an interval of at least 30 minutes before taking your first meal.

Depending on the patient’s needs, medicine from the Linzess capsule may be administered through a gastronomy tube or a nasogastric (NG).

Doctors and pharmacists should always advise the patient to read through the medication guide or instruction leaflet (sheets) that comes with the drug. Carefully go through the information on how to mix the medicine from the capsule with either an applesauce or water, or how to administer the medicine through a feeding tube. Remember to pose all doubts or question to your doctor or pharmacist and do not go on to take this medicine if you have any doubt.

Symptoms may not disappears or improve not until it is about 14 days (2 weeks), thus, you have to keep on using the medication as directed. Call your doctor if the symptoms do not improve, or if they get worse as you use Linzess.


Store at standard room temperature away from moisture and/or heat

Keep Linzess and all other medications away from high temperatures and away from the direct rays from the sun.

Always keep the capsules in their original container, along with the packet of the moisture-absorbing preservative that comes with this medicine. Keep all bottles containing medication tightly closed.

Keep Linzess and any other medicine or chemicals out of the reach of children and pets. Linzess has been side to cause severe dehydration and diarrhea in children who accidentally swallows this medicine. This is a case for emergency and should be treated with urgency when it occurs. Preparation and Instructions for Administration

For some adult patients who have problem with their swallowing abilities, Linzess capsules can be opened, mixed with either applesauce or with water and then administered orally. You can also administer this medication with some water via a nasogastric or gastrostomy tube.

Note: The drug has been coated on the surface of the beads and will dissolve off the beads into the water. The beads will still be visible and will not dissolve. It is therefore not necessary to consume all the beads in order to deliver the complete dose. Remember to take this medication as prescribe by your health care provider or pharmacist and in case of any doubt, talk to your doctor about it before commencing treatment.

Storage requirements:

  • It is good to keep the drug in its original container to protect it from moisture.

  • Do not remove desiccant (drying agent) from the container.

  • Once the Linzess container is opened, the drug must be used within 18 weeks.

Linzess dosing information (Dosage of Linzess)

In order for you to appreciate some of the uses of Linzess it is very important for you to follow the dosage. The dosage of Linzess is seen as given below

 The Usual Adult Dose for Irritable Bowel Syndrome:

  • 290 mcg orally one time a day

This is for emphasis

  • Take Linzess very early in the morning on an empty stomach, and wait at least 30 minutes before going for your first meal of the day
  • Do not break it apart, grind or chew medicine but swallow it whole
  • Use: Linzess is use as a laxative in subjects suffering (constipation) with an irritable bowel syndrome, to soften their intestinal content.


The Usual Adult Dose for Constipation:

  • 145 mcg orally one time a day

This is for emphasis

  • You should swallow capsules whole; do not break it apart or chew
  • Use: For any chronic idiopathic constipation

Other Recommended Dosage of Linzess

​For people with an Irritable Bowel Syndrome who also have Constipation (IBS-C)

​The recommended or prescribed dosage of LINZESS to be given is an oral 290 mcg one time a day.

​Chronic Idiopathic Constipation (CIC)

​The recommended or prescribed dosage of LINZESS to be given is an oral 145 mcg once a day. Lower dosage strength of an oral 72 mcg once a day may also be used based on subject’s clinical record or tolerability

What happens if I miss a dose?

You should be advice to take the missed dose as soon as you remember. However, if it is closer to the time for the next scheduled dose, skip the missed dose. You should never take extra dose or double dose the medicine in a bit to make up the missed dose.

What happens if I overdose?

If you or your patient overdoses, seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What other things should I avoid while taking Linzess?

You are advised to strictly follow your doctor's instructions about any restrictions on your type of food, beverages, or other activities.

What other drugs will affect Linzess?

Some other drugs when taken together may interact with linaclotide. This may include prescribed drug, over-the-counter, vitamin, and/herbal medicines. Therefore, you should inform your doctor about all medications that you use, and those you start or stop using during your treatment.

Linzess side effects (side effects of Linzess)

If you do not understand Linzess uses, seek advice from your doctor in order to avoid negative side effects of this drug. However, side effects of Linzess may or may not occur in some patients at the prescribed dosage. Some of these adverse reactions or side effects of Linzess may be severe requiring an emergency medical help while others may just mild which usually disappears following discontinuation of treatment. If you notice any Linzess side effects or if you have any signs of an allergic reaction to Linzess such as hives; difficult breathing; swelling of your lips, throat, tongue, or face then you should get emergency medical help

Stop using Linzess immediately and call your doctor at once if you have:

  • A severe or ongoing diarrhea;
  • some signs of an electrolyte imbalance - increased thirst or rate of urination, leg cramps, confusion, mood changes, fluttering in your chest, feeling unsteady, irregular heartbeats, muscle weakness or limp feeling;
  • some severe stomach pains; or
  • diarrhea with dizziness or occasional light-headed feeling (as if you might pass out);
  • dark colored, bloody, or tarry stools.

Some common Linzess side effects may include:

  • diarrhea;
  • stomach pain;
  • gas; or
  • bloating or a full feeling in your stomach.
  • For the Consumer

Applies to linaclotide: oral capsule

In addition to the desirable effects, some other undesirable or unwanted effects (also known as adverse reactions or Linzess side effects) may be caused by linaclotide (the active ingredient contained inside Linzess). Some of these reactions may be serious, requiring an emergency medical help while others may be mild or less severe and usually disappear following the discontinuation of the medicine hence requiring no medical attention.

Major Side Effects

You should to do your best check with your doctor immediately if any of these side effects occur when you are taking linaclotide:

Less common:

  • Heartburn
  • loss of appetite
  • nausea
  • vomiting
  • weakness


  • Bleeding from the rectum (noticed in feces)
  • confusion
  • cough
  • decreased urination
  • difficulty in swallowing
  • dizziness
  • dry mouth
  • fainting
  • fast heartbeat
  • hives or welts, itching of the body, or skin rash or redness
  • increase in the heart rate
  • lightheadedness
  • loss of bowel control
  • rapid breathing
  • shortness of breath
  • sunken eyes
  • thirst
  • tightness in the chest
  • unusual tiredness or weakness
  • wrinkled skin

Minor Side Effects

Some of the side effects of Linzess, refer to as minor side effects may not need any medical attention. These effects usually disappear as your body tries to adapt or adjust to the medicine during treatment. They usually just go away on their own. Your health care provider may also be able to tell you about some other ways to reduce or prevent some of these Linzess side effects. However, some of these side effect may persist and therefor requiring the help of a pharmacist or medical doctor. If at all any of the following side effects continue, are bothersome or if you have any concerns about them, check with your health care professional (doctor):

More common:

  • Body aches or pain
  • chills
  • ear congestion
  • excess air or gas inside the stomach or intestines
  • fever
  • full or bloated feeling
  • headache
  • loss of voice
  • passing gas
  • sneezing
  • sore throat
  • stuffy or runny (watery) nose

Less common:

  • Acid or sour stomach
  • belching
  • indigestion
  • pain or tenderness around your eyes and cheekbones
  • pressure inside the stomach
  • stomach discomforts or upset
  • swelling of the abdomen or the stomach area
  • For Healthcare Professionals


Very common: Diarrhea

Common: Abdominal pain, viral gastroenteritis, flatulence, abdominal distension, gastroesophageal reflux disease, fecal incontinence, vomiting, dyspepsia

Uncommon: Defecation urgency


Uncommon: Orthostatic hypotension


Uncommon: Urticaria 

Frequency not reported: Rash


Some of the most popularly reported reasons for treatment discontinuation were diarrhea and abdominal pain.


Uncommon: Hematochezia, melena, some rectal hemorrhages


Uncommon: Allergic reactions


Uncommon: Dehydration, decreased appetite, hypokalemia

Rare: Decreased blood bicarbonate

Nervous system

Common: Headache, dizziness


Common: Fatigue


Common: infection in the upper respiratory tract, sinusitis

This is however, not a complete list of the possible side effects of Linzess. You should talk with your doctor for information on the possible side effects associated with Linzess intake and don’t forget to tell him if you develop ant reaction when taking this drug. You may also report all your side effects to FDA at 1-800-FDA-1088.

Renal Dose Adjustments

  • No adjustment has been recommended

Liver Dose Adjustments

  • No adjustment has been recommended

Special Populations

Hepatic Impairment

  • No dosage adjustments are needed.

Renal Impairment

  • No dosage adjustments are needed.

Geriatric Patients

  • There are no specific dosage recommendations as at now.

Pediatric Warning: Linaclotide has contradictions in pediatric patients up to 6 years of age; in some nonclinical studies, administration of just a single, clinically relevant adult oral dose of linaclotide caused some deaths due to dehydration in young juvenile mice so please avoid use of linaclotide in pediatric patients 6 through 17 years of age.

Standards of safety and efficacy have not yet been established in patients who are younger than 18 years.
Consult the WARNINGS section for additional precautions.


  • Data not available

Other Warnings and Precautions


Diarrhea may occur, generally within the first 2 weeks of therapy.

Severe diarrhea has reported in 2% of patients receiving linaclotide 145 or 290 mcg daily and in <1% of those receiving 72 mcg daily.Also, severe diarrhea that was associated with dizziness, hypotension, syncope, and hypokalemia (low potassium level) and hyponatremia (low sodium level) and may need hospitalization or IV fluids has also been reported.

It is advisable to interrupt linaclotide and rehydrate patient if severe diarrhea develops.

Use of Linzess in Specific Populations


Not expected to result in fetal exposure if it is administered to pregnant women; however, available data on use in pregnant women are insufficient to inform a fetal risk.

There is no evidence of adverse embryofetal developmental effects in studies in rats and rabbits, but also severe maternal toxicity and associated effects on fetal morphology observed in studies in mice at dosages that were much higher than recommended human dosages. No other developmental abnormalities and no effects on growth, the learning and memory, or fertility observed in the offspring of the exposed rats.

A limited systemic exposure to linaclotide was recorded in these animal species. Please do not directly compare animal and human doses for evaluating relative exposure.


It is not known whether linaclotide distributes into human milk, or affects human milk production, or affects the breast-fed infant.

It is not known or certain whether the negligible systemic absorption observed in adults will result in any clinically significant or important exposure in breastfed infants. There may be high risk for severe adverse effects following exposure. Consider the benefits of breastfeeding and the importance this medicine to the woman; also consider any potential adverse reaction (side effects) on the breastfed infant from the drug or underlying maternal condition. 

Pediatric Use

Contraindicated in all infants and children <6 years of age; avoid use in children and adolescents who are 6 to <18 years of age. The safety and/or efficacy in pediatric patients (children) <18 years of age is not yet established, and deaths reported within just 24 hours of administration in neonatal mice (age approximately equivalent to human age which was 0–28 days).

In the neonatal mice, a daily dose of 10 mcg/kg linaclotide resulted in deaths. These deaths were associated with severe dehydration caused by an increase in fluid secreted into the intestine. This is a direct consequence of GC-C stimulation. The ability to the system to tolerate linaclotide increased with age in the juvenile mice, however, a good number of deaths were also recorded following a single dose of 100 mcg/kg to 2 weeks old mice or 600 mcg/kg in mice that where 3 weeks of age.

Because of the rise in the GC-C present in the intestine, infants and/or children younger than 6 years of age may be at a high risks of developing diarrhea and other potentially serious side effects compared with individuals who are older than 6 years of age. Although no deaths were observed in the older juvenile mice, avoid the use of linaclotide in little children and adolescents 6 to 18 years of age because of the deaths reported in neonatal mice and lack of safety and efficacy data in the pediatric patients.

Geriatric Use

There is no sufficient data in geriatric patients (patients who are at least 65 years of age) to be able to conclude whether geriatric patients have different respond than younger subjects. However, doses should be chosen with much caution due to age-related decreases in cardiac hepatic, and/or kidney functions and also the risk for concomitant disease and/or drug therapies.

Interactions for Linaclotide

It does not however interact with CYP isoenzymes secreated in the system.

Linzess does not interact with uptake transporters and common efflux, such as P-glycoprotein (P-gp), in vitro.

No formal drug interaction studies have been conducted at the moment of writing this article. However, systemic exposure to Linzess and its active metabolite is not significant following an oral administration. The reactions facilitated by common transporters or CYP enzymes not expected. 

  • Absorption
  • Pharmacokinetics
  • Bioavailability

It is minimally absorbed; negligible systemic bioavailability following an oral administration.


Administration immediately after a relatively high-fat breakfast resulted in some looser stools and higher stool frequency.

Plasma Concentrations

At the recommended dosages, plasma concentrations are below actual measurable levels.



It is not expected to be distributed to tissues to any clinically relevant extent.



Metabolized by carboxypeptidase A in the GI tract; parent drug and active metabolite are proteolytically degraded (broken down) in intestinal lumen to smaller peptides and amino acids.

Elimination Route

3–5% of the orally administered dose excreted in feces as active peptide, mainly as an active metabolite.


Binds to GC-C receptor on luminal surface of the intestinal epithelium. Stimulation of the  GC-C causes increased concentrations of the cyclic guanosine monophosphate (cGMP), which then activates the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel leading to a secretion of chloride and bicarbonate into intestinal lumen; results in increased intestinal fluid and accelerated (increased speed) intestinal transit.

Noticeable changes stool consistency and increases stool frequency.

In animals, it causes decreased visceral hyperalgesia and abdominal pain; effect thought to be mediated by the activation of GC-C. Mechanism(s) of abdominal pain relief in patients with IBS with constipation are not fully elucidated.


Having looked at Linzess uses, its dosage, side effects and a host of others, I call on you to take general caution when taking any type of medication.

A disclaimer: this write-up is meant to guide patients and student health personnel who have doubts and should never be used in place of a doctor’s expertise.