Lubiprostone (Amitiza) - Uses, Dose, Side effects

Lubiprostone (Amitiza) acts in the gastrointestinal lumen and increase the GI transit and intestinal fluid secretion.

Lubiprostone (Amitiza) Indications:

  • It is indicated in the treatment of the following conditions:

    • Chronic idiopathic constipation (CIC) in adults
    • Irritable bowel syndrome (IBS) with constipation
    • Opioid-induced constipation (OIC) in adult patients with chronic pain related to prior cancer or its treatment who do not require frequent opioid dose escalation.

Lubiprostone (Amitiza) Dose in Adults:

Lubiprostone (Amitiza) Dose in the treatment of chronic idiopathic constipation:

  • 24 mcg orally two times a day.

Dose in the treatment of Irritable bowel syndrome with constipation in females 18 years of age or more:

  • 8 mcg orally two times a day

Lubiprostone (Amitiza) Dose in the treatment of opioid-induced constipation:

  • 24 mcg orally two times a day.

Lubiprostone (Amitiza) dose in children:

The safety and efficacy of the drug in children have not been established.


Pregnancy Risk Category: C

  • Negative fetal outcomes have been documented in animal reproduction studies.

Use of lubiprostone while breastfeeding

  • It is unknown whether the active metabolite or drug are excreted into breastmilk.
  • Manufacturer recommends that you monitor your infant for signs of diarrhea.
  • Manufacturers recommend weighing the risks to the infant from drug exposure and the benefits for the mother.

Dose in Kidney disease:

Adjustment in the dose is not necessary.

Lubiprostone (Amitiza) Dose in Liver disease:

  • Mild hepatic impairment (Child-Pugh class A):

    • No dosage adjustment is necessary.
  • Moderate hepatic impairment (Child-Pugh class B):

    • Chronic idiopathic constipation or opioid-induced constipation:

      • 16 mcg two times a day initially.
      • The dose may be increased to 24 mcg two times a day if an adequate response has not been obtained and the drug is tolerated.
    • Irritable bowel syndrome with constipation:

      • Adjustment in the dose is not necessary.
  • Severe hepatic impairment (Child-Pugh class C):

    • Chronic idiopathic constipation or opioid-induced constipation:

      • 8 mcg two times a day initially.
      • The dose may be increased to 16 to 24 mcg two times a day if an adequate response has not been obtained and the drug is tolerated.
    • Irritable bowel syndrome with constipation:

      • 8 mcg once a day initially.
      • The dose may be increased to 8 mcg two times a day if an adequate response has not been obtaine and the drug is well tolerated.

Common Side Effects of Lubiprostone (Amitiza):

  • Central nervous system:

    • Headache
  • Gastrointestinal:

    • Nausea
    • Diarrhea

Less Common Side Effects of Lubiprostone (Amitiza):

  • Cardiovascular:

    • Edema
    • Chest discomfort
    • Chest pain
    • Peripheral edema
  • Central nervous system:

    • Dizziness
    • Fatigue
  • Gastrointestinal:

    • Abdominal pain
    • Flatulence
    • Abdominal distention
    • Abdominal distress
    • Loose stools
    • Vomiting
    • Dyspepsia
    • Xerostomia
  • Respiratory:

    • Dyspnea

Contraindications to Lubiprostone (Amitiza):

Patients with a suspected or known mechanical GI (gastrointestinal obstruction) are not advised to use it.

Warnings and precautions

  • Dyspnea
    • Dyspnea can occur after the first dose. It may manifest as tightness in the chest and difficulty taking deep breaths.
    • Dyspnea can occur immediately (within 30-60 minutes) following the first dose. However, it has been reported to also occur with subsequent dosing.
  • Nausea:
    • To reduce nausea and improve GI tolerability, the drug should be taken with food
  • Hypotension and syncope:
    • Syncope and hypotension may occur when the drug is combined with antihypertensive medications or higher doses.
    • Hypotension can occur after the first dose. It will usually resolve before the next scheduled dose or after discontinuation.
    • Patients may require hospitalization in severe cases.
  • Diarrhea:
    • Patients with severe diarrhea should avoid it.
  • Gastrointestinal obstruction:
    • Patients with mechanical gastrointestinal obstruction should avoid it.
    • Before prescribing any drug, all patients must be examined for mechanical GI obstruction.
  • Hepatic impairment
    • Patients with severe or moderate hepatic impairment may be at greater risk of drug exposure. Adjustments in doses may be necessary.

Lubiprostone: Drug Interaction

Risk Factor C (Monitor therapy)

Levomethadone

May diminish the therapeutic effect of Lubiprostone.

Methadone

May diminish the therapeutic effect of Lubiprostone.

 

Monitor:

  • Bowel frequency and consistency
  • Liver function tests at baseline and periodically as indicated.

How to administer Lubiprostone (Amitiza)?

Oral: Administer with food and water. Swallow whole; do not break or chew.


Mechanism of action of Lubiprostone (Amitiza):

  • It acts locally on the apical membrane in the gastrointestinal tract and is a chloride channel activater.
  • This bypasses the antisecretory effects opiates have on secretomotor neuron excitability.

Absorption:

  • The systemic absorption of the parent drug is poor while that of the active metabolite is low.

Distribution

  • beyond the gastrointestinal tract is minimal.

Plasma proteins binding:

  • 94%

Metabolism:

  • Extensively within the stomach and jejunum by carbonyl reductase to active (M3) and inactive metabolites rapidly.

Bioavailability:

  • The bioavailability of the drug is minimal

Half-life elimination

  • The half-life elimination of the active metabolite (M3) is 0.9 to 1.4 hours

The time to reach peak plasma concentration:

  • about 1.1 hours for the active metabolite (M3).

Excretion:

  • Parent drug and M3: Feces (trace amounts)

International Brands of Lubiprostone:

  • Amitiza
  • Amiprostone
  • Lubilax
  • Lubistone
  • Lubowel
  • Lupicont
  • Luprostam
  • Modulex

Lubiprostone Brand Names in Pakistan:

No Brands Available in Pakistan.

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