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linaclotide

General

Pronunciation:
lin-a-kloe-tide


Trade Name(s)

  • Constella Canadian Tradename
  • 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).

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 or CIC.

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 IBS-C or ICI symptoms)

ROUTEONSETPEAKDURATION
POunknown6–9 wk1 wk†
†Following discontinuation.

Contraindication/Precautions

Contraindicated in:

  • Known/suspected mechanical GI obstruction
  • Pedi: Children <18 yr (safety and effectiveness not established).

Use Cautiously in:

  • Lactation: Use cautiously in nursing women
  • OB: Use during pregnancy only if potential maternal benefit justifies potential risk to the fetus.

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 noted.

Route/Dosage

IBS-C

PO: (Adults) 290 mcg once daily.

CIC

PO: (Adults) 145 mcg once daily; 72 mcg once daily may be used based on patient presentation or tolerability.

Availability

Capsules: 72 mcg, 145 mcg, 290 mcg

Assessment

  • Assess patient for symptoms of IBS (abdominal pain or discomfort, bloating, constipation). If severe diarrhea occurs, withhold therapy and rehydrate patient. May require IV fluids.

Potential Diagnoses

Implementation

  • PO: Administer once daily on an empty stomach 30 minutes before eating first meal of the day. 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 patient 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.

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Citation

Quiring, Courtney, et al. "Linaclotide." Davis's Drug Guide, 16th ed., F.A. Davis Company, 2019. Medicine Central, im.unboundmedicine.com/medicine/view/Davis-Drug-Guide/109844/all/linaclotide.
Quiring C, Sanoski CA, Vallerand AH. Linaclotide. Davis's Drug Guide. 16th ed. F.A. Davis Company; 2019. https://im.unboundmedicine.com/medicine/view/Davis-Drug-Guide/109844/all/linaclotide. Accessed June 16, 2019.
Quiring, C., Sanoski, C. A., & Vallerand, A. H. (2019). Linaclotide. In Davis's Drug Guide. Available from https://im.unboundmedicine.com/medicine/view/Davis-Drug-Guide/109844/all/linaclotide
Quiring C, Sanoski CA, Vallerand AH. Linaclotide [Internet]. In: Davis's Drug Guide. F.A. Davis Company; 2019. [cited 2019 June 16]. Available from: https://im.unboundmedicine.com/medicine/view/Davis-Drug-Guide/109844/all/linaclotide.
* Article titles in AMA citation format should be in sentence-case
TY - ELEC T1 - linaclotide ID - 109844 A1 - Quiring,Courtney, AU - Sanoski,Cynthia A, AU - Vallerand,April Hazard, BT - Davis's Drug Guide UR - https://im.unboundmedicine.com/medicine/view/Davis-Drug-Guide/109844/all/linaclotide PB - F.A. Davis Company ET - 16 DB - Medicine Central DP - Unbound Medicine ER -