linaCLOtide
General
Pronunciation:
lin-a-kloe-tide
Trade Name(s)
- Constella
- Linzess
Ther. Class.
anti irritable bowel syndrome agents
Pharm. Class.
guanylate cyclase-C agonists
Indications
- Irritable bowel syndrome with constipation (IBS-C).
- Chronic idiopathic constipation (CIC).
- Functional constipation.
Action
Locally increases levels of cyclic guanosine monophosphate (cGMP); accelerates transit time, increases intestinal fluid and decreases pain sensation.
Therapeutic Effect(s):
Increased frequency of bowel movements with decreased pain associated with IBS-C, CIC, or functional constipation.
Pharmacokinetics
Absorption: Minimally absorbed, action is primarily local.
Distribution: Stays within the GI tract with minimal distribution.
Metabolism and Excretion: Converted to its principal active metabolite within the GI tract; subsequently locally degraded to smaller peptides and amino acids; 3–5% found in stool, mostly as the active metabolite.
Half-life: Unknown.
TIME/ACTION PROFILE (improvement in GI symptoms)
| ROUTE | ONSET | PEAK | DURATION |
|---|---|---|---|
| PO | unknown | 6–9 wk | 1 wk† |
Contraindication/Precautions
Contraindicated in:
- Known/suspected mechanical GI obstruction
- Pedi: Children <2 yr (↑ risk of severe dehydration).
Use Cautiously in:
- OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
- Pedi: Children ≥2 yr (safety and effectiveness not established).
Adverse Reactions/Side Effects
CNS: fatigue
GI: diarrhea, abdominal distention, abdominal pain, flatulence, gastrointestinal reflux, vomiting
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
Interactions
Drug-Drug
None reported.
Route/Dosage
Irritable Bowel Syndrome with Constipation
PO (Adults): 290 mcg once daily.
Chronic Idiopathic Constipation
PO (Adults): 145 mcg once daily; 72 mcg once daily may be used based on patient presentation or tolerability.
Functional Constipation
PO (Children ≥6 yr): 72 mcg once daily.
Availability (generic available)
Capsules: 72 mcg, 145 mcg, 290 mcg
Assessment
- Assess patient for symptoms of IBS (abdominal pain or discomfort, bloating, constipation). If severe diarrhea occurs, hold therapy and rehydrate patient. May require IV fluids.
Implementation
Do not confuse linaclotide with linagliptin.
- PO Administer once daily on an empty stomach, 30 minutes before eating first meal of the day. DNC: Swallow capsules whole; do not open, break, dissolve, or chew.
- For patients with difficulty swallowing, open capsule and sprinkle entire capsule contents in 1 teaspoon applesauce or 30 mL water. For applesauce, consume immediately; do not chew beads or store for later. For water, swirl water and beads gently for at least 20 seconds. Swallow entire mixture immediately. Add another 30 mL of water to any beads remaining in cup, swirl for 20 seconds, and swallow immediately. Do not store mixture for later use. Water method may also be used for NG or G-tube administration.
Patient/Family Teaching
- Instruct patient to take as directed. Keep capsules in original bottle with desiccant packet to help keep medication dry; keep bottle tightly closed. If a dose is missed, omit and take next dose at regular time; do not double doses.
- Inform patient that diarrhea often begins within first 2 wks of therapy. Stop taking and notify health care professional if severe diarrhea occurs. Contact health care professional and go to nearest hospital emergency room immediately if bright red, bloody stools or black stools that look like tar occur.
- Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
- Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.
Evaluation/Desired Outcomes
- Increased frequency of bowel movements with decreased pain associated with IBS-C or CIC.
- Increased frequency of bowel movements in pediatric patients 6 to 17 years of age with functional constipation.