lubiprostone

Therapeutic Classification: laxatives

Pharmacologic Classification: chloride channel activators

Indications ⬆ ⬇

REMS

Chronic idiopathic constipation.
Irritable bowel syndrome with constipation in women ≥18 yr.
Opioid-induced constipation in adults with chronic, non-cancer pain, including those with chronic pain related to prior cancer or its treatment who do not need frequent (e.g. weekly) opioid dose escalation.

Action ⬆ ⬇

Increases intestinal fluid secretion by activating chloride channels in intestinal epithelium.

Therapeutic effects:

Decreased symptoms of chronic constipation.

Pharmacokinetics ⬆ ⬇

Absorption: Minimal absorption, action is primarily in GI tract.

Distribution: Minimal systemic distribution.

Metabolism/Excretion: Metabolized by enzymes in the GI tract. Primary metabolite (M3) is excreted in urine (60%) and feces (30%).

Half-Life: Unknown.

Time/Action Profile ⬆ ⬇

(reduction in symptoms)

ROUTE	ONSET	PEAK	DURATION
PO	within 1 wk	1 wk	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Mechanical GI obstruction;
Lactation: Lactation.

Use Cautiously in:

Severe diarrhea;
Moderate or severe hepatic impairment (dose ↓ recommended);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension, peripheral edema, syncope

GI: diarrhea, nausea, abdominal distention, abdominal pain, dry mouth, dyspepsia, reflux, vomiting

MS: arthralgia

Neuro: dizziness, headache

Resp: dyspnea

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of antihypertensives may ↑ risk of hypotension and/or syncope.

Route/Dosage ⬆ ⬇

Chronic Idiopathic Constipation and Opioid-Induced Constipation

PO (Adults ): 24 mcg twice daily.

Hepatic Impairment

PO (Adults ): Moderate hepatic impairment (Child-Pugh Class B)-16 mcg twice daily; if patient tolerates, can titrate to 24 mcg twice daily, if needed; Severe hepatic impairment (Child-Pugh Class C)-8 mcg twice daily; if patient tolerates, can titrate to 24 mcg twice daily, if needed.

Irritable Bowel Syndrome with Constipation

PO (Adults ): 8 mcg twice daily.

Hepatic Impairment

PO (Adults ): Severe hepatic impairment (Child-Pugh Class C)-8 mcg once daily; if patient tolerates, can titrate to 8 mcg twice daily, if needed.

Availability ⬆ ⬇

(Generic available)

Capsules: 8 mcg; 24 mcg

Assessment ⬆ ⬇

Assess for abdominal distention, presence of bowel sounds, and usual bowel patterns prior to and periodically during therapy.
Assess color, consistency, and amount of stool produced.

Implementation ⬆ ⬇

Patients with symptoms suggestive of mechanical GI obstruction should be evaluated prior to initiating therapy.
PO: Administer with food and water to decrease nausea. DNC: Swallow capsules whole; do not crush, break or chew.
- Do not administer to patients with severe diarrhea.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take lubiprostone as directed.
Inform patient that dyspnea or chest tightness may occur within 1 hr of first dose; usually resolves within 3 hrs, but may return with repeat doses.
Advise patients that lubiprostone may cause diarrhea. Advise patient to notify health care professional if diarrhea becomes severe.
Inform patient that syncope and hypotension may occur, usually with the 24 mcg twice daily dose. May recur with next dose. Usually resolves with discontinuation of therapy.
May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. If used during breastfeeding, monitor infant for diarrhea.

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Pronunciation ⬇

Classifications ⬆ ⬇