linaclotide

linaclotide

(lin-a-kloe-tide) ,

Linzess

(trade name)

Classification

Therapeutic: anti irritable bowel syndrome agents
Pharmacologic: guanylate cyclase c agonists
Pregnancy Category: C

Indications

Treatment of irritable bowel syndrome with constipation (IBS-C) or chronic idiopathic constipation (CIC).

Action

Locally increases levels of cyclic guanosine monophosphate (cGMP); accelerates transit time, increases intestinal fluid and decreases pain sensation.

Therapeutic effects

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.

Contraindications/Precautions

Contraindicated in: Known/suspected mechanical GI obstruction; Pediatric: Children <17 yr.
Use Cautiously in: Lactation: Use cautiously in nursing women; Obstetric: Use during pregnancy only if potential maternal benefit justifies potential risk to the fetus.

Adverse Reactions/Side Effects

Central nervous system

  • fatigue

Gastrointestinal

  • diarrhea (most frequent)
  • abdominal distention
  • abdominal pain
  • flatulence
  • gastrointestinal reflux
  • vomiting

Interactions

Drug-Drug interaction

None noted.

Route/Dosage

Oral (Adults) IBS-C—290 mcg once daily; CIC—145 mcg once daily.

Availability

Capsules: 145 mcg, 290 mcg

Nursing implications

Nursing assessment

  • Assess patient for symptoms of IBS (abdominal pain or discomfort, bloating, constipation).

Potential Nursing Diagnoses

Constipation (Indications)
Diarrhea (Adverse Reactions)

Implementation

  • Oral: 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.

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.
  • 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.
References in periodicals archive ?
Summary: [170 Pages Report] Peptide Based Gastrointestinal Disorders Therapeutics Market research report categorizes the global market By Drug (Teduglutide, Linaclotide), By Distribution Channel (Hospital Pharmacies, Retail Pharmacies, Online Pharmacies), & By Region (North America, Latin America, Europe, Japan, APEJ, MEA).
The company discovered, developed and are commercialising linaclotide, the US branded prescription market leader for adults with irritable bowel syndrome with constipation (IBS-C) or chronic idiopathic constipation.
Under the terms of the agreement, Ironwood will provide AHP disease education to gastroenterologists and other healthcare practitioners that Ironwood currently calls on for LINZESS(linaclotide).
Linaclotide is a first-in-class drug developed for the treatment of IBS-C or CC, based on the guanylin, uroguanylin, and STa peptide structure.
This edition has new drugs, including aclidinium bromide, felbamate, icosapent ethyl, linaclotide, peginesatide acetate, perampanel, rotigotine, and teriflunomide, and updated group monographs for antipsychotic agents, benzodiazepenes, calcium channel blocking agents, estrogens, macrolides, opioid analgesics, proton pump inhibitors, selective serotonin reuptake inhibitors, and serotonin 5-HT1 receptor agonists.
There are four gastrointestinal agents: crofelemer (Fulyzaq; antidiarrheal), linaclotide (Linzess; laxative), teduglutide (Gattex; short bowel syndrome), and the combination of sodium picosulfate, magnesium oxide, and citric acid (Prepopik; osmotic laxative).
Drugs that won FDA approval in 2012 include lorcaserin hydrochloride (Belviq) to treat overweight and obsesity, mirabegron (Myrbetriq) for overactive bladder, and linaclotide (Linzess) to treat idiopathic constipation and irritable bowel syndrome with constipation in adults.
Drugs that won FDA approval in 2012 include lorcaserin hydrochloride (Belvig) to treat overweight and obesity, mirabegron (Myrbetrig) for overactive bladder, and linaclotide (Linzess) to treat idiopathic constipation and irritable bowel syndrome with constipation in adults.
The Food and Drug Administration approved linaclotide on Aug.
(NASDAQ: IRWD) will be presenting linaclotide results from Phase 3 clinical trials in patients with irritable bowel syndrome with constipation (IBSa[euro]C) during the 2011 Digestive Disease Week (DDW) annual meeting that will be held in Chicago from May 7 through May 10, 2011.
In addition, we plan to submit new drug applications for aclidinium and linaclotide in the second half of this year and for two additional products in calendar 2012."
The company said it will use the money to develop and commercialise linaclotide in the US with its partner Forest Laboratories, to back its overall research and development efforts and for general corporate purposes.