LINZESS/CONSTELLA (Linaclotide)

What is this medication?

LINZESS/CONSTELLA (Linaclotide)
Anticholinergic Agent

Brand Name US: Linzess
Canadian Equivalent: Constella

Linaclotide is indicated for treatment of chronic idiopathic constipation (CIC), Irritable bowel syndrome with constipation (IBS-C).

ALERT: WARNING
Linaclotide is contraindicated in pediatric patients less than 6 years; in nonclinical studies in neonatal mice, administration of a single, clinically relevant adult oral dose of linaclotide caused deaths due to dehydration. Avoid use of linaclotide in patients 6 years to less than 18 years. The safety and effectiveness of linaclotide has not been established in patients less than 18 years.

How does this medication work? 

Linaclotide and its active metabolite bind and agonize guanylate cyclase-C on the luminal surface of intestinal epithelium. Intracellular and extracellular cyclic guanosine monophosphate (cGMP) concentrations are raised resulting in the secretion of chloride and bicarbonate into the intestinal lumen. Intestinal fluid increases and GI transit is accelerated. Increased extracellular cGMP may decrease visceral pain by reducing pain-sensing nerve activity.

How should I take this medication? 

CIC: 
Oral: Take 145 mcg once daily; 72 mcg once daily may be used based on patient presentation or tolerability.

IBS-C: 
Oral: Take 290 mcg once daily.

How to Take: Administer at least 30 minutes before the first meal of the day on an empty stomach; loose stools and greater stool frequency may occur after administration with a high-fat breakfast. Swallow capsule whole; do not break, crush, or chew capsules or capsule contents.

What should I watch for while using this medication? 

Before starting LINZESS/CONSTELLA (Linaclotide) make sure your physician is aware of any allergies or medications you currently take.  May cause severe diarrhea associated with dizziness, syncope, hypotension, and electrolyte abnormalities (hypokalemia and hyponatremia) requiring hospitalization or IV fluids.  Consider discontinuation of therapy and rehydration if severe diarrhea occurs. Administration with a high-fat meal may worsen diarrhea.

What if I miss a dose?

If you miss a dose of medication, try to take it as soon as possible. However, if it is almost time for your next dose, take only that scheduled dose. Do not take double or extra doses.

How should I store this medication?

Keep out of the reach of children at all times. Store at room temperature, 59 to 86° F (15 to 30° C). Protect from light. Keep the container tightly closed. Properly dispose of any unused medication after the expiration date.

What are the possible side effects of using this medication?

Diarrhea, abdominal pain, flatulence, 

Note this is not a complete list of side effects for LINZESS/CONSTELLA (Linaclotide), only common ones.