Dosing & Uses
Dosage Forms & Strengths
capsule
- 8mcg
- 24mcg
Chronic Idiopathic Constipation
Indicated for treatment of chronic idiopathic constipation (CIC) in adults
24 mcg PO BID
Irritable Bowel Syndrome With Constipation
Indicated for treatment of irritable bowel syndrome with constipation (IBS-C) in women aged ≥18 years
8 mcg PO BID
Opioid-Induced Constipation
Indicated for treatment of opioid-induced constipation (OIC) in adults with chronic noncancer pain, including patients with chronic pain related to prior cancer or its treatment who do not require frequent (eg, weekly) opioid dosage escalation
24 mcg PO BID
Limitations of use: Effectiveness in patients taking diphenylheptane opioids (eg, methadone) has not been established
Dosage Modifications
Hepatic impairment
- Mild: No dosage adjustment required
Moderate (Child-Pugh B)
- CIC or OIC: 16 mcg PO BID; if modified dose is tolerated and adequate response has not been obtained after appropriate interval, dose can be escalated to full standard dose with appropriate monitoring of patient response
- IBS-C: No dosage adjustment required
Severe (Child-Pugh C)
- CIC or OIC: 8 mcg PO BID
- IBS-C: 8 mcg PO qDay
- If modified dose is tolerated and adequate response has not been obtained after appropriate interval, dose can be escalated to full standard dose with appropriate monitoring of patient response
Safety and efficacy not established
Adverse Effects
>10%
Nausea (8-29%)
Diarrhea (7-12%)
Headache (2-11%)
1-10%
Abdominal pain (4-8%)
Abdominal distension (3-6%)
Flatulence (4-6%)
Vomiting (3%)
Loose stools (3%)
Edema (1-3%)
Abdominal discomfort (1-3%)
Dizziness (3%)
Chest discomfort/pain (2%)
Dyspnea (2%)
Dyspepsia (2%)
Fatigue (2%)
Dry mouth (1%)
Postmarketing Reports
Cardiovascular: Syncope and/or hypotension, tachycardia
Gastrointestinal: Ischemic colitis
General: Asthenia
Immune system: Hypersensitivity reactions including rash, swelling, throat tightness, malaise
Musculoskeletal: Muscle cramps or muscle spasms
Warnings
Contraindications
Hypersensitivity
Mechanical GI obstruction
Cautions
In patients with symptoms suggestive of mechanical GI obstruction, perform a thorough evaluation to confirm the absence of an obstruction prior to initiating therapy (see Contraindications)
Potential for acute dyspnea described as sensation of chest tightness and difficulty breathing within 30-60 minutes after the first dose; instruct patients to contact healthcare provider if dyspnea occurs
Avoid use in patients with severe diarrhea; instruct patients of potential for diarrhea to occur during treatment
May cause nausea and diarrhea (taking with food reduces chance of nausea); dose adjustment recommended
Syncope and hypotension reported, some of which required hospitalization; most cases occurred in patients taking 24 mcg twice daily and some occurred within hour after taking first dose or subsequent doses; patients should be aware of risk of syncope and hypotension during treatment and other adverse reactions, such as diarrhea or vomiting may increase this risk
Drug interaction overview
- Diphenylheptane opioids (eg, methadone) have been shown in nonclinical studies to dose dependently reduce the activation of ClC-2 by lubiprostone in GI tract
Pregnancy & Lactation
Pregnancy
Following oral administration, concentrations of lubiprostone in plasma are below the level of quantitation; however, one of the metabolites, M3, has measurable systemic concentrations
Data are not available to inform a drug associated risk of adverse developmental outcomes
Animal studies
- Animal studies did not show an increase in structural malformations; however, a doses dependent increase in fetal loss was observed in pregnant guinea pigs at 0.2-6 times the MRHD
Lactation
No data are available on the presence in human milk of the refect on milk production
Animal studies
- Neither lubiprostone nor its active metabolite (M3) were present in milk of lactating rats
- When a drug is not present in animal milk, it is likely that the drug will not be present in human milk
- If present, lubiprostone may cause diarrhea in the breastfed infant lubiprostone may cause diarrhea on effect of breastfed infants
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Locally acting chloride channel activator; increases intestinal fluid secretion and intestinal motility; acts locally at apical portion of intestine
Absorption
Low systemic absorption
Peak plasma time: 1 hr
Distribution
Protein binding: 94% in vitro (may be irrelevant because of low systemic absorption)
Metabolism
Probably metabolized in stomach and jejunum by carbonyl anhydrase
Elimination
Half-life: 0.9-1.4 hr
Excretion: Urine (60%), feces (trace amounts)
Administration
Oral Administration
Administer with food and water
Swallow capsules whole and do not break apart or chew
Assess periodically the need for continuous therapy
Storage
25°C (77°F); excursions permitted to 15-30°C (59-86°F)
Protect from light and extreme temperatures
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| lubiprostone oral - | 24 mcg capsule |  | |
| lubiprostone oral - | 8 mcg capsule |  | |
| lubiprostone oral - | 8 mcg capsule |  | |
| lubiprostone oral - | 24 mcg capsule |  | |
| lubiprostone oral - | 24 mcg capsule |  | |
| lubiprostone oral - | 8 mcg capsule |  | |
| Amitiza oral - | 8 mcg capsule | | |
| Amitiza oral - | 24 mcg capsule | |
Copyright © 2010 First DataBank, Inc.
Patient Handout
lubiprostone oral
LUBIPROSTONE - ORAL
(loo-bi-PROST-own)
COMMON BRAND NAME(S): Amitiza
USES: This medication is used to treat certain types of constipation (chronic idiopathic constipation, irritable bowel syndrome with constipation). Chronic idiopathic constipation has an unknown cause and is not due to diet, other diseases, or drugs.Lubiprostone is also used to treat constipation caused by opioid medications in people with ongoing pain due to medical conditions other than cancer.This medication may improve symptoms such as bloating and abdominal discomfort, improve stool texture, lessen the need to strain, and decrease the feeling of not completely relieving oneself. Lubiprostone belongs to a class of drugs known as chloride channel activators. It works by increasing the amount of fluid within your intestines, making the passage of stool easier.
HOW TO USE: Take this medication by mouth with food and water as directed by your doctor, usually twice daily. Swallow the medication whole. Do not break or chew the medication.The dosage is based on your medical condition and response to treatment.Use this medication regularly in order to get the most benefit from it. Remember to take it at the same times each day.You should talk to your doctor regularly about whether you still need this treatment.Inform your doctor if your condition lasts or gets worse.
SIDE EFFECTS: Nausea, diarrhea, gas, vomiting, dry mouth, runny nose, cough, fever, headache, joint/back pain, or trouble sleeping may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: swelling of arms/legs, mental/mood changes.This medication may cause low blood pressure and possibly fainting. Diarrhea and vomiting may increase the risk of these side effects. Stop taking this medication and tell your doctor right away if any of these serious side effects occur: fainting, dizziness, severe diarrhea/vomiting.Lubiprostone may rarely cause trouble breathing and chest tightness within 30 to 60 minutes after the first dose. This reaction is usually not serious and generally goes away within 3 hours. It may happen again with other doses. However, you may not be able to tell this reaction apart from a rare, severe reaction that also causes trouble breathing and/or chest pain. Get medical help right away if you develop any trouble breathing or chest tightness/discomfort/pain.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking lubiprostone, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: certain stomach/intestinal problems (blockage, severe diarrhea), liver disease.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this drug passes into breast milk, but it may have undesirable effects (such as causing diarrhea) on a nursing infant. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: fainting, flushing, paleness, loss of appetite, sweating.
NOTES: Do not share this medication with others.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised January 2022. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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