Linaclotide
LINZESS
What it isGuanylate cyclase-C agonist that increases intestinal fluid secretion; IBS-C and chronic idiopathic constipation.
Why this oneUnlike plecanatide, food amplifies its gastrointestinal effects, so it is taken on an empty stomach.
What limits itDiarrhea is dose-limiting; it is contraindicated under age 2, and severe cases require stopping and rehydration.
FDA-approved for
- IBS-C/chronic constipation (2012)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Irritable bowel syndrome with constipation (IBS-C) | Adults | 290 mcg QD | 290 mcg QD | 290 mcg QD |
| Chronic idiopathic constipation (CIC) | Adults | 145 mcg QD (72 mcg QD by presentation/tolerability) | 145 mcg QD | 145 mcg QD |
| IBS-C | Pediatric >=7 yr | 145 mcg QD | 145 mcg QD | 145 mcg QD |
| Functional constipation (FC) | Pediatric >=2 yr | 72 mcg QD | 72 mcg QD | 72 mcg QD |
Renal Undefined
Hepatic Undefined
Instructions
- Take on an empty stomach at least 30 minutes before the first meal of the day, at approximately the same time daily.
- Swallow capsule whole; do not crush or chew.
- If unable to swallow: open and sprinkle beads on a teaspoon of applesauce or in ~30 mL water (swirl >=20 s) and consume immediately; may give via NG/G-tube in water.
- If a dose is missed, skip it and take the next at the regular time; do not double.
Contraindications
- Patients less than 2 years of age (risk of serious dehydration)
- Known or suspected mechanical gastrointestinal obstruction
Cautions
- Diarrhea, sometimes severe — may cause dehydration, hypokalemia/hyponatremia, hypotension, syncope; suspend dosing and rehydrate if severe
Adverse reactions
- Diarrhea
- Abdominal pain
- Flatulence
- Abdominal distension
- Hypersensitivity (rare): anaphylaxis, angioedema, urticaria
Pregnancy Negligible systemic absorption; maternal use not expected to result in fetal exposure; human data insufficient.
Lactation Not detected in human milk; not expected to expose the breastfed infant.
NO BOXED WARNINGS
Principal riskDiarrhea; contraindicated under age 2
Cost, est. cash$10–$500/bag or supply
Generic entry2021
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityLocal irritation, sensitization or administration-site injury; negligible systemic toxicity at usual use.
Mechanism of action: Linaclotide ballicule
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