Linaclotide (Linzess) Dosage Calculator
Linaclotide (brand name Linzess/Constella) is a synthetic 14-amino-acid peptide and first-in-class guanylate cyclase-C (GC-C) agonist approved by the FDA in 2012 for the treatment of irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC).
72mcg · Daily
Summary: Add 0mL BAC water to your 0.072mg vial. Draw to < 0.1 units on a U-100 syringe for a 72mcg dose. This vial will last 0 doses.
Cycle Planner
Linaclotide (Linzess) Pharmacokinetics
Linaclotide (Linzess) Dosing Protocol
| Level | Dose / Injection | Frequency |
|---|---|---|
| Beginner | 72mcg | Daily |
| Moderate | 145mcg | Daily |
| Aggressive | 290mcg | Daily |
Note: Linaclotide is an oral peptide capsule — no injection or reconstitution required. It is one of the few FDA-approved peptide drugs taken by mouth. It acts entirely within the gut lumen with negligible systemic absorption (<0.1% bioavailability). Take on an empty stomach at least 30 minutes before the first meal of the day. The 72 mcg dose is approved for chronic idiopathic constipation (CIC) and pediatric functional constipation (ages 6-17). The 145 mcg dose is for CIC in adults. The 290 mcg dose is specifically for IBS-C in adults. Do NOT use in children under 6 years — contraindicated due to risk of severe dehydration.
About Linaclotide (Linzess)
Linaclotide (brand name Linzess/Constella) is a synthetic 14-amino-acid peptide and first-in-class guanylate cyclase-C (GC-C) agonist approved by the FDA in 2012 for the treatment of irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC). Structurally related to the endogenous hormones guanylin and uroguanylin, linaclotide contains three intramolecular disulfide bonds (Cys1-Cys6, Cys2-Cys10, Cys5-Cys13) that lock it into a compact, protease-resistant conformation. It is one of the rare peptide therapeutics designed for oral administration — the capsule survives gastric acid, and the peptide acts locally on the luminal surface of intestinal epithelial cells without entering the bloodstream. Upon binding GC-C receptors, linaclotide triggers intracellular cGMP production, which activates CFTR chloride channels and drives fluid secretion into the intestinal lumen, accelerating transit. Extracellular cGMP also modulates visceral afferent nerve signaling, reducing abdominal pain — a dual mechanism that addresses both constipation and visceral hypersensitivity. Two pivotal Phase 3 trials demonstrated that 290 mcg daily significantly improved IBS-C symptoms, with approximately 34% of patients meeting the FDA composite responder endpoint versus 14-21% on placebo (NNT of 5-8). For CIC, Phase 3 trials of 145 mcg and 290 mcg met primary efficacy endpoints with NNT of 6-10. The drug has an excellent safety profile with diarrhea (14-20%) as the most common side effect — a pharmacological extension of its mechanism rather than an off-target toxicity.