Pracalog 1/Pracalog 2

Prucalopride.

Each film coated tablet of Pracalog 1 contains Prucalopride succinate 1.321 mg eq. to Prucalopride 1 mg.
Each film coated tablet of Pracalog 2 contains Prucalopride succinate 2.642 mg eq. to Prucalopride 2 mg.

Pharmacology: Pharmacodynamics: Prucalopride is a selective agonist of serotonin type 4 (5-HT4) receptors resulting in gastrointestinal prokinetic stimulation that increases colonic motility as measured by the number of high-amplitude propagating contractions (HAPCs).
Pharmacokinetics: Absorption: Rapid.
Distribution: Vd: 567 L.
Protein binding: ~30%.
Metabolism: Substrate of CYP3A4 (in vitro), not extensively metabolized.
Bioavailability: > 90%, Concomitant intake of food does not influence the oral bioavailability.
Half-life elimination: ~24 hours.
Time to peak: 2-3 hours.
Excretion: Primarily as unchanged drug: Urine (55.1%-73.8%), feces (3.7%-8.1%).

Prucalopride is indicated for symptomatic treatment of chronic constipation in adults in whom laxative fall to provide adequate relief.

Prucalopride is film coated tablet for oral administration without regard to meals.
Adult: 2 mg once daily.
Geriatric (age >65 years): Initial dose 1 mg once daily may increase to 2 mg once daily if necessary.
Children & adolescent: Prucalopride should not be used in children and adolescents younger than 18 years.
Dose adjustment: Renal impairment: The dose for patients with severe renal impairment (GFR <30 mL/min/1.73 m²) is 1 mg once daily and no dose adjustment for patients with mild to moderate renal impairment.
Hepatic impairment: No dose adjustment for patients with mild to moderate hepatic impairment (Child Pugh class A or B) and patients with severe hepatic impairment (Child Pugh class C) is 1 mg once daily may increase to 2 mg once daily if needed and well tolerated.
If the intake of once daily prucalopride in not effective after 4 weeks of treatment the patient should be re-examined and the benefit of continue treatment reconsidered.
Reassess for therapeutic benefit at regular intervals if prolong therapy (>3 months) is needed.

Overdose has not been reported. Overdose effects are similar to adverse effects reported at therapeutic doses. Headache, nausea, and diarrhea may occur. A specific toxic dose has not been established.
Treatment is symptomatic and supportive. Correct any significant fluid and/or electrolyte abnormalities in patients with severe diarrhea.

Hypersensitivity to prucalopride or any component of the formulation.
Renal impairment requiring dialysis.
Intestinal perforation or obstructive due to structural or functional disorder of the gut wall, obstructive ileus, severe inflammatory condition of the GI tract (e.g. Crohn disease, ulcerative colitis, toxic megacolon/mega rectum.

Use with caution in patients with a history of arrhythmia, ischemic cardiovascular disease, pre-excitation syndromes (e.g. Wolff- Parkinson-White syndrome) or AV nodal rhythm disorders.
Use with caution in severe hepatic impairment (Child-Pugh class C) initial dose reduction is recommended.
Use with caution in renal impairment dose reduction is recommended in severe impairment and contraindicated in patients requiring dialysis.
Use with caution in patients with severe and unstable concomitant disease (e.g. Cancer, AIDs, psychiatric, hepatic, pulmonary, insulin dependent diabetes mellitus) has not been studied.
Patients with severe or persistent diarrhea should discontinue therapy and consult health care provider.
Discontinue therapy if severe and/or worsening abdominal symptoms, bloody diarrhea, or rectal bleeding and advise patient to discontinue treatment and consult health care provider.
May cause CNS depression (particularly during the first day of treatment), which may impair physical or mental abilities, patients must be cautioned about performing tasks that require mental alertness (e.g. operating machine or driving).
Pracalog 1 and Pracalog 2 contain lactose, do not use in patients with galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption syndromes
Effects on ability to drive and use machines: No studies on the effects of prucalopride on the ability to drive and use machines have been performed. Prucalopride has been associated with dizziness and fatigue particularly during the first day of treatment which may have an effect on driving and using machines.

Pregnancy: Adverse events have not been observed in animal reproduction studies. Spontaneous abortion has been observed in pregnant women during clinical trials, although a causal association with prucalopride has not been established. Use during pregnancy is not recommended. Women of childbearing potential should employ effective contraception during therapy.
Lactation: Prucalopride is excreted in breast milk. In the absence of human data in women who actively breast-feeding, breast-feeding is not recommended.

Central nervous system: Dizziness, fatigue, headache, malaise.
Genitourinary: Pollakiuria.
Gastrointestinal: Abdominal pain, abnormal bowel sounds, anorexia diarrhea, dyspepsia, flatulence, gastroenteritis, nausea, upper abdominal pain, vomiting.
Neuromuscular & Skeletal: Muscle spasm.
Miscellaneous: Fever.
Rare but important or life threatening: Angina pectoris, anxiety, atrial arrhythmia, cardiac arrhythmia, bronchitis, chest pain, cholecystitis, cholelithiasis, confusion, constipation, depression, dyspnea, hyperhidrosis, migraine, myocardial infarction, ovarian cyst, pancreatitis, pneumonia, sinusitis, stomach discomfort, supraventricular tachycardia, syncope, tremor, urinary incontinence, urinary tract infection, vaginal hemorrhage.

Metabolism/transport effects substrate of P-glycoprotein.
There are no known interaction where it is recommended to avoid concomitant use.
May interact with potent inhibitors of P-glycoprotein.

Store at below 30°C.

Laxatives, Purgatives

A06AX05 - prucalopride ; Belongs to the class of other laxatives.

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