Chronic idiopathic constipation; Opioid-induced constipation:
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.
Constipation-predominant irritable bowel syndrome:
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.
Should be taken with food.
Known or suspected mechanical gastrointestinal obstruction, severe diarrhoea.
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).
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.
Obtain LFT and evaluate for symptoms of mechanical gastrointestinal obstruction prior to initiation of therapy. Monitor blood pressure regularly. Assess for symptoms of hypotension.
Decreased effect when concomitantly administered with diphenylheptane opioids (e.g methadone, levomethadone).
Description: Mechanism of 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. Pharmacokinetics: 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).
Store at 25°C. Protect from light and extreme temperatures.
A06AX03 - lubiprostone ; Belongs to the class of other laxatives.
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