Generic
Linaclotide
2 brands available in the market
At a glance
Linaclotide is a guanylate cyclase-C agonist indicated in adults for the treatment of irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC).
Description
Linaclotide is an orally administered, peptide agonist of guanylate cyclase 2C. Chemically, it is a heterodetic cyclic peptide consisting of fourteen amino acids. Linaclotide is minimally absorbed with negligible systemic availability following oral administration. It is metabolized within the gastrointestinal tract to its principal active metabolite by loss of the terminal tyrosine moiety.
Indications
- Irritable bowel syndrome with constipation (IBS-C) - adults
- Chronic idiopathic constipation (CIC) - adults
Therapeutic class
Other Laxative Preparations
Pharmacological class
Guanylate Cyclase-C Agonist
Pharmacology
Linaclotide activates guanylate cyclase-C receptors, increasing intestinal fluid secretion and reducing intestinal transit time, relieving constipation.
Mechanism of action
Relieves constipation by increasing intestinal fluid secretion and reducing intestinal transit time.
Dosage
IBS-C (Adults): 290 mcg PO once daily
CIC (Adults): 145 mcg PO once daily; 72 mcg once daily (based on individual presentation or tolerability)
Administration
- Swallow capsules whole; do not chew, crush or break
- Take on an empty stomach, at least 30 minutes before breakfast
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember. If it's almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.
Side effects
Common Side Effects:
- Diarrhea (most common)
- Abdominal pain/discomfort
- Flatulence
- Abdominal distension
- Headache
- Upper respiratory tract infection
- Sinusitis
- Nausea
- Vomiting
- Heartburn
- Fecal incontinence
Precautions & warnings
- Contraindicated in patients less than 6 years of age (risk of serious dehydration)
- Avoid use in pediatric patients 6 to less than 18 years of age (safety data not established)
- If severe diarrhea occurs, suspend dosing and rehydrate the patient
- Do not use in patients with known or suspected mechanical gastrointestinal obstruction
Contraindications
- Patients less than 6 years of age
- Known or suspected mechanical gastrointestinal obstruction
Drug interactions
No significant drug interactions known (systemic exposure is negligible).
Food interactions
Food intake (especially high-fat breakfast) may affect stool consistency and frequency; taking on an empty stomach is preferred.
Use in pregnancy
Use in Pregnancy: Linaclotide use in pregnancy has limited data (Category C); use only if potential benefit justifies potential risk to the fetus.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if excreted in human milk; not measurable in plasma at recommended clinical doses.
Pediatric use
Contraindicated in children less than 6 years of age; avoid use in children 6 to less than 18 years (safety and efficacy not established).
Geriatric use
No dose adjustment needed in elderly.
Renal / hepatic impairment
No dose adjustment needed for renal or hepatic impairment (negligible systemic absorption).
Overdose effects
Overdose: diarrhea is the most common adverse reaction.
Storage conditions
Store between 2-8°C in a frost-free place; keep away from light; keep out of reach of children.
Chemical structure
Linaclotide