Prucalopride

What is prucalopride?

Prucalopride is a prescription medicine that is used to treat constipation.

Description

MOTEGRITY (prucalopride) tablets for oral use contain prucalopride succinate, a dihydrobenzofurancarboxamide that is a serotonin type 4 (5-HT4) receptor agonist. The IUPAC name is: 4-amino-5-chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydrobenzofuran-7-carboxamide succinate.

The molecular formula is C18H26ClN3O3.C4H6O4 and the molecular weight is 485.96. The structural formula is:

Prucalopride succinate is a white to almost white powder. It is highly soluble in acidic aqueous media and alkaline aqueous media up to a pH of approximately 9.

Each 1-mg film-coated tablet of MOTEGRITY contains 1 mg of prucalopride (equivalent to 1.32 mg prucalopride succinate), and the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, and microcrystalline cellulose. The coating for the 1-mg tablet contains hypromellose, lactose monohydrate, polyethylene glycol 3000, titanium dioxide, and triacetin.

Each 2-mg film-coated tablet of MOTEGRITY contains 2 mg of prucalopride (equivalent to 2.64 mg prucalopride succinate), and the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, and microcrystalline cellulose. The coating for the 2-mg tablet contains hypromellose, lactose monohydrate, polyethylene glycol 3000, titanium dioxide, triacetin, red iron oxide, yellow iron oxide, and FD&C Blue #2.

Mechanism of Action

Prucalopride, a selective serotonin type 4 (5-HT4) receptor agonist, is a gastrointestinal (GI) prokinetic agent that stimulates colonic peristalsis (high-amplitude propagating contractions [HAPCs]), which increases bowel motility.

Prucalopride was devoid of effects mediated via 5-HT2A, 5-HT2B, 5-HT3, motilin or CCK-A receptors in vitro at concentrations exceeding 5-HT4 receptor affinity by 150-fold or greater. In isolated GI tissues from various animal species, prucalopride facilitated acetylcholine release to enhance the amplitude of contractions and stimulate peristalsis. In rats and dogs, prucalopride stimulated gastrointestinal motility with contractions starting from the proximal colon to the anal sphincter.

Before taking prucalopride, tell your doctor:

• If you are allergic to prucalopride; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
• If you have any of these health problems: Bowel problems like bowel block, Crohn’s disease, hole in the GI (gastrointestinal) tract, or ulcerative colitis.
• If you have kidney disease or are on dialysis.
• If you have a rare hereditary problem of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption.

This is not a list of all drugs or health problems that interact with prucalopride.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take prucalopride with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take prucalopride?

• Tell all of your health care providers that you take prucalopride. This includes your doctors, nurses, pharmacists, and dentists.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using prucalopride while you are pregnant.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

How is prucalopride best taken?

Use prucalopride as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take with or without food.
• Keep taking prucalopride as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

• Take a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

What are the side effects of prucalopride that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• New or worse behavior or mood changes like depression or thoughts of killing yourself.

What are some other side effects of prucalopride?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Headache.
• Upset stomach or throwing up.
• Diarrhea.
• Belly pain.
• Bloating.
• Gas.
• Dizziness.
• Feeling tired or weak.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out prucalopride?

• Store in the original container at room temperature.
• Store in a dry place. Do not store in a bathroom.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.

Labe

PRINCIPAL DISPLAY PANEL – 1 MG TABLET BOTTLE LABEL

• Rx Only
  NDC 54092-546-01
• motegrity®
  (prucalopride) tablets
• 1 mg
• Usual Dose: One tablet once daily.
  30 Tablets

 

PRINCIPAL DISPLAY PANEL – 2 MG TABLET BOTTLE CARTON

• NDC 54092-547-03
• motegrity®
  (prucalopride) tablets
• 2 mg
• Usual Dose: One tablet once daily.
  Patient Sample – Not for Sale
• 30 Tablets
• Rx Only
• Takeda

SRC: NLM .