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 ?
linaclotide contribution from our partner Astellas in Japan increased significantly, DUZALLO was approved and launched, and we advanced six exciting mid- and late-stage clinical trials.
Ironwood Pharmaceuticals is commercializing two innovative primary care products: linaclotide for adults with irritable bowel syndrome with constipation (IBS-C) or chronic idiopathic constipation (CIC), and lesinurad, which is approved to be taken with a xanthine oxidase inhibitor (XOI) for the treatment of hyperuricemia associated with uncontrolled gout.
Eleven pharmaceutical agents or classes of drugs are used to treat IBS: linaclotide (Linzess), lubipro-stone (Amitiza), eluxadoline (Viberzi), polyethylene glycol laxatives (Miralax, Glycolax), rifaximin (Xifaxan), alosetron (Lotronex), loperamide (Imodium), tricyclic antidepressants (Elavil), selective serotonin reuptake inhibitors (Prozac, Zoloft) and antispasmodics (Atropine, Bentyl), and plecanatide (Trulance), approved in January 2017.
FIGURE 3 harmacologic therapies for irritable bowel syndrome by symptom (13,14) Abdominal pain/-discomfort ** Antidepressants * (TCAs/SSRIs) ** Alosetron (5-THE antagonist) ** Dicyclomine ** Hyoscyamine * Constipation ** Fiber * ** MOM/PEG solution * ** Linaclotide (guanylate Cyclase-C agonist Bloating ** Rifaximin ** Probiotics * Diarrhea ** Loperamide * ** Diphenoxylate-astropine * ** Cholestyramine * ** Alosetron ** Rifaximin ** Eluxadoline * Not currently approved by the US Food and Drug Administration for the treatment of irritable bowel syndrome.
Frissora points to linaclotide (Linzess) to treat constipation, a serum-derived bovine protein medical food (EnteraGam) for diarrhea, and a gut-only antibiotic called rifaximin (Xifaxan) to help relieve symptoms of gas, bloat, flatulence, rumbling in the abdomen, and diarrhea.
Abdominal cramping, discomfort, and diarrhea are the adverse events commonly reported by patients for linaclotide (about 4%) [52, 129, 130].
Some newly developed drugs, such as lubiprostone and linaclotide specifically target intestinal secretion in order to improve in particular constipation (Andresen et al.
IBS medications include anti-diarrheals, drugs like hyoscyamine (Levsin[R]) and dicyclomine (Bentyl[R]) to control colon spasms, and fiber supplements, laxatives, or drugs like linaclotide (Linzess[R]) or lubiprostone (Amitiza[R]) to ease constipation.
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.