Lubiprostone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Chronic idiopathic constipation
Adult: 24 mcg bid.

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.

Oral
Constipation-predominant irritable bowel syndrome
Adult: In women ≥18 years: 8 mcg bid.
Hepatic Impairment
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.
Cách dùng
Should be taken with food.
Chống chỉ định
Known or suspected mechanical gastrointestinal obstruction, severe diarrhoea.
Thận trọng
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).
Phản ứng phụ
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.
MonitoringParameters
Obtain LFT and evaluate for symptoms of mechanical gastrointestinal obstruction prior to initiation of therapy. Monitor blood pressure regularly. Assess for symptoms of hypotension.
Tương tác
Decreased effect when concomitantly administered with diphenylheptane opioids (e.g methadone, levomethadone).
Tác dụng
Description: 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).
Đặc tính

Chemical Structure Image
Lubiprostone

Source: National Center for Biotechnology Information (2020). PubChem Compound Summary for CID 157920, Lubiprostone. Retrieved September 24, 2020 from https://pubchem.ncbi.nlm.nih.gov/compound/Lubiprostone.

Bảo quản
Store at 25°C. Protect from light and extreme temperatures.
Phân loại MIMS
Phân loại ATC
A06AX03 - lubiprostone ; Belongs to the class of other laxatives.
References
Amitiza Capsule, Gelatin Coated (Takeda Pharmaceuticals America, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 07/09/2020.

Amitiza Capsules (Sucampo Pharmaceuticals, Inc.). U.S. FDA. https://www.fda.gov/. Accessed 07/09/2920.

Anon. Lubiprostone. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 07/09/2020.

Anon. Lubiprostone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/09/2020.

Buckingham R (ed). Lubiprostone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/09/2020.

Lubiprostone. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com/. Accessed 07/09/2020.

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