linaclotide

REMS

Irritable bowel syndrome with constipation (IBS-C).
Chronic idiopathic constipation (CIC).
Functional constipation.

Contraind./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).

Adv. Reactions/Side Effects ⬆ ⬇

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

Neuro: fatigue

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

(Generic available)

Capsules: 72 mcg; 145 mcg; 290 mcg

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.

US Brand Names ⬆ ⬇

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, CIC, or functional constipation.

Classifications ⬆ ⬇

Therapeutic Classification: anti irritable bowel syndrome agents

Pharmacologic Classification: guanylate cyclase-C agonists

Pharmacokinetics ⬆ ⬇

Absorption: Minimally absorbed, action is primarily local.

Distribution: Stays within the GI tract with minimal distribution.

Metabolism/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.

Canadian Brand Names ⬆ ⬇

Time/Action Profile ⬆ ⬇

(improvement in GI symptoms)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	6–9 wk	1 wk‡

‡Following discontinuation.

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.

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Indications ⬇