Prucalopride (Motegrity) is a highly selective 5 HT-4 receptor agonist. It is used to treat chronic idiopathic constipation in adults.

Constipation, as per the latest Rome III criteria is defined as: "a symptom complex which must include at least two of the following:

• Straining,
• Lumpy or hard stools,
• A sensation of incomplete evacuation,
• A sensation of anorectal obstruction or blockage,
• Manual manoeuvres to facilitate defecation
• Less than three defecations per week"

It is also utilised as an off-label therapy for people with persistent pain who have been exposed to opioids but do not have cancer.

Prucalopride dose in Adults

Prucalopride dose (Motegrity dosing) in the treatment of chronic idiopathic constipation:

• 2 mg orally once a day.
• Treatment with additional laxatives may be considered if bowel movements do not occur within 3 consecutive days (of prucalopride use)

Prucalopride dose in Children

Not studied in children.

Pregnancy Risk Category: C

• Its use in pregnancy is not well-documented.
• In trials, pregnant women experienced spontaneous abortions.
• It is important to advise women of child bearing age about the use of contraception.

Prucalopride use during breastfeeding:

• It is excreted from breast milk.
• Manufacturers recommend that you weigh the benefits and risks of breastfeeding and drug exposure for your infant.

Prulacopride (Motegrity dosing) dose in Kidney disease:

• CrCl ≥30 mL/minute:

  • Adjustmen in the dose is not required.

• CrCl <30 mL/minute:

  • 1 mg once a day

• ESRD requiring hemodialysis:

  • Avoid using it.

Prucalopride dose in liver disease:

The manufacturer has not provided any dose adjustment in patients with liver disease.

Common Side Effects of Prucalopride (Motegrity side effects) Include:

• Central nervous system:

  • Headache

• Gastrointestinal:

  • Abdominal Pain
  • Nausea
  • Diarrhea

Less Common Side Effects of Prucalopride (Motegrity side effects):

• Central Nervous System:

  • Dizziness
  • Fatigue
  • Migraine

• Genitourinary:

  • Pollakiuria

• Gastrointestinal:

  • Abdominal Distension
  • Flatulence
  • Vomiting
  • Severe Diarrhea
  • Abnormal Bowel Sounds
  • Decreased Appetite

Contraindication to Prucalopride (Motegrity) Include:

• Severe allergic reactions to prucalopride or any other component of the formulation.
• Patients on dialysis and severe kidney impairment
• IBD (Crohn's, ulcerative colitis and toxic megacolon)
• Structural disorders in the gastrointestinal tract, such as intestinal perforation or obstruction.
• Paralytic ileus and functional disorders of the stomach are examples.

Warnings and precautions

• CNS effects

  • It can cause dizziness or fatigue.
  • Patients who are required to be alert for mental tasks should be advised of the dangers.

• Diarrhea:

  • Diarrhea can sometimes become quite severe.
  • Diarrhea is most common during the first week of treatment. It usually resolves in a few days.
  • If severe diarrhea persists, it is important to contact a healthcare professional immediately and stop taking any medication.

• Suicidal thoughts and behaviors:

  • Patients suffering from depression should be cautious when taking the drug. It may worsen their symptoms or cause suicidal thoughts.
  • In such cases, treatment must be stopped immediately

• Renal impairment

  • Prucalopride is excreted mainly via the kidneys. Patients with advanced kidney disease or patients on dialysis should avoid Prucalopride.
  • The dose should be decreased in moderately severe cases of kidney disease.

Prucalopride: Drug Interaction

Monitor:

• Bowel movements frequency
• Worsening of depression
• Suicidal thoughts and behavior

How to administer Prucalopride (Motegrity)?

It is taken orally without regard to meals.

Mechanism of action of Prucalopride (Motegrity):

• Prucalopride, a 5-HT-4 receptor agonist, is highly selective. 
• Prucalopride promotes nonadrenergic, cholinergic and noncholinergic neurotransmission through enteric neurons.
• It causes excessive intestinal secretion and stimulates the peristaltic reflex. This increases the gastrointestinal motility.

Absorption is Rapid Distribution: 567 L after intravenous administration. About 30% of the drug is protein-bound. It has a bioavailability of more than 90% Half-life elimination is about 24 hours.The half-life elimination lengthens to 34, 43, and 47 hours in patients with mild, moderate, and severe kidney disease. Time to reach the peak serum concentration is 2 to 3 hours. Excretion: It is primarily excreted as unchanged drug in urine (84.2%). 13.3% is excreted in the feces.

International Brands of Prucalopride:

• Motegrity

• Resotran

• Constinon

• Prucasoft

• Resolor

Prucalopride brands in Pakistan:

1. Tab. P-pride 2 mg ( Wilshire pharmaceuticals)

2. Tab. Pru-CIC 1 mg and 2 mg (Searle Pharma)

3. Tab. Pru-vix 1 mg and 2 mg (Highnoon Pharma)

The estimated price of Tab Prucalopride 1 mg in Pakistan is PKR 300 per 10 tablets.

The price of 2 mg Prucalopride in Pakistan is PKR 400 per ten tablets.