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)

Contraindication/Precautions

Contraindicated in:

• Known/suspected mechanical GI obstruction;
• Pedi:  Black Box:   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

GI: diarrhea, abdominal distention, abdominal pain, flatulence, gastrointestinal reflux, vomiting

Neuro: fatigue

* 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 min 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 one 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 ≥20 sec. Swallow entire mixture immediately. Add another 30 mL of water to any beads remaining in cup, swirl for 20 sec, 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

• Explain the purpose and side effects of linaclotide. 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. Advise patient to read  Patient Information  before starting and with each Rx refill in case of changes.
• Inform patient that diarrhea often begins within first 2 wk of therapy. Stop taking and notify health care provider if severe diarrhea occurs. Contact health care provider 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 provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
• OB:  Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected.

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 6–17 yr of age with functional constipation.