Lubiprostone


Full Generic Medicine Info
Dosage/Direction for Use

Oral
Chronic idiopathic constipation
Adult: 24 mcg bid.
Hepatic impairment: Moderate (Child-Pugh class B): Initially, 16 mcg bid; may adjust to 24 mcg bid if tolerated and acceptable clinical response has not been achieved after an appropriate interval at a lower dose. Severe (Child-Pugh class C): Initially, 8 mcg bid; may increase to 16-24 mcg bid if tolerated and acceptable clinical response has not been achieved after an appropriate interval at a lower dose.

Oral
Opioid-induced constipation
Adult: In patients with chronic non-cancer pain (including patients with chronic pain related to prior cancer or its treatment who do not require frequent opioid dosage escalation): 24 mcg bid.
Hepatic impairment: Moderate (Child-Pugh class B): Initially, 16 mcg bid; may adjust to 24 mcg bid if tolerated and acceptable clinical response has not been achieved after an appropriate interval at a lower dose. Severe (Child-Pugh class C): Initially, 8 mcg bid; may increase to 16-24 mcg bid if tolerated and acceptable clinical response has not been achieved after an appropriate interval at a lower dose.

Oral
Constipation-predominant irritable bowel syndrome
Adult: In women ≥18 years: 8 mcg bid.
Hepatic impairment: Severe (Child-Pugh class C): Initially, 8 mcg once daily; may adjust to 8 mcg bid if tolerated and acceptable clinical response has not been achieved after an appropriate interval at a lower dose.
Administration
Should be taken with food.
Contraindications
Known or suspected mechanical gastrointestinal obstruction, severe diarrhoea.
Special Precautions
Moderate to severe hepatic impairment (Child-Pugh class B or C). Pregnancy and lactation. Not established for use in the treatment of opioid-induced constipation in patients taking diphenylheptane opioids (e.g. methadone). Monitoring Parameters Obtain LFT and evaluate for symptoms of mechanical gastrointestinal obstruction prior to initiation of therapy. Monitor blood pressure regularly. Assess for symptoms of hypotension.
Adverse Reactions
Significant: Nausea, syncope or hypotension, dyspnoea. Cardiac disorders: Chest discomfort or pain, palpitations, tachycardia. Gastrointestinal disorders: Abdominal pain or distention, diarrhoea, dry mouth, flatulence, dyspepsia, vomiting, constipation, dysgeusia, eructation, faecal incontinence, bowel urgency, gastritis, GERD, rectal haemorrhage. General disorders and administration site conditions: Oedema, peripheral oedema, fatigue, lethargy, malaise. Immune system disorders: Hypersensitivity (e.g. rash, swelling and throat tightness). Investigations: Decreased serum K, increased ALT/AST, weight gain. Metabolism and nutrition disorders: Anorexia. Musculoskeletal and connective tissue disorders: Fibromyalgia, joint swelling, muscle cramps or spasms, myalgia. Nervous system disorders: Dizziness, headache, tremors. Psychiatric disorders: Anxiety, depression. Renal and urinary disorders: Pollakiuria, UTI. Respiratory, thoracic and mediastinal disorders: Cough, pharyngolaryngeal pain, influenza. Skin and subcutaneous tissue disorders: Erythema, hyperhidrosis. Vascular disorders: Ischaemic colitis.
Drug Interactions
Decreased effect when concomitantly administered with diphenylheptane opioids (e.g methadone, levomethadone).
Action
Lubiprostone is a selective, locally-acting chloride-channel activator acting on the apical (luminal) part of gastrointestinal epithelium that increases the secretion of chloride-containing intestinal fluid without changing the serum concentration of Na and K. This increases intestinal motility, thus aiding the passage of stool and bypassing the opiate's antisecretory action which is the product of secretomotor neuron excitability suppression.
Absorption: Absorption of the parent drug is below the quantitation level (10 pg/mL); M3 (active metabolite): Low. Bioavailability: Low. Time to peak plasma concentration: Approx 1.1 hours (M3).
Distribution: Minimal distribution beyond the gastrointestinal tissue. Plasma protein binding: Approx 94%.
Metabolism: Rapidly and extensively metabolised, possibly within the stomach and jejunum, via reduction and oxidation by carbonyl reductase into active M3 metabolite and other metabolites.
Excretion: Mainly via urine (approx 60%); faeces (approx 30%). Elimination half-life: Approx 0.9-1.4 hours (M3).
Storage
Oral: Store at 25°C. Protect from light and extreme temperatures.
ATC Classification
A06AX03 - lubiprostone ; Belongs to the class of other laxatives.
Disclaimer: This information is independently developed by CIMS based on lubiprostone from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 CIMS. All rights reserved. Powered by CIMSAsia.com
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