Plecanatide
Plecanatide Uses, Dosage, Side Effects, Food Interaction and all others data.
Plecanatide is a drug approved in January 2017 by the FDA for the treatment of chronic idiopathic constipation (CIC). It should not be used in children less than six years of age, and should be avoided in patients six years to 18 years of age
Food Effect Subjects who received either a low-fat, low calorie (LF-LC) meal or a high fat, high calorie (HF-HC) meal reported looser stools than fasted subjects up to 24 hours after a single dose of 9 mg (3 times the recommended dose). In clinical studies, Plecanatide was administered with or without food.
| Trade Name | Plecanatide |
| Availability | Prescription only |
| Generic | Plecanatide |
| Plecanatide Other Names | Guanilib, Plecanatide |
| Related Drugs | dicyclomine, Bentyl, hyoscyamine, Amitiza, Metamucil, Trulance, Motegrity, prucalopride, Lotronex, lactitol |
| Weight | 3mg |
| Type | Oral tablet |
| Formula | C65H104N18O26S4 |
| Weight | Average: 1681.89 Monoisotopic: 1680.625200237 |
| Protein binding | Plecanatide exhibits little to no binding to human serum albumin or human α-1-acid glycoprotein. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Plecanatide is a laxative used to treat chronic idiopathic constipation and IBS with constipation.
Plecanatide stimulates intestinal fluid secretions in the gastrointestinal tract to support regular bowel function. Plecanatide, taken orally once daily, works locally in the upper GI tract to stimulate secretion of intestinal fluid and support regular bowel function.
Plecanatide is also used to associated treatment for these conditions: Chronic idiopathic constipation (CIC)
How Plecanatide works
Guanylate cyclase C (GC-C) agonist Plecanatide and its active metabolite bind to GC-C and act locally on the luminal surface of intestinal epithelial cells; GC-C activation leads to increased cyclic guanosine monophosphate (cGMP), which, in turn, stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly by activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit. In animal models, plecanatide has been shown to increase fluid secretion into the gastrointestinal (GI) tract, accelerate intestinal transit, and cause changes in stool consistency. In an animal model of visceral pain, plecanatide reduced abdominal muscle contractions, a measure of intestinal pain. The mechanism has not been studied.
Toxicity
Single oral doses of plecanatide at 0.5 mg/kg and 10 mg/kg caused mortality in young juvenile mice on postnatal days 7 and 14, respectively (human age equivalent of approximately 1 month to less than 2 years).
Food Interaction
- Take with or without food.
Plecanatide Disease Interaction
Volume of Distribution
Concentrations of plecanatide and its active metabolite in plasma are below the limit of quantitation after an oral dose of 3 mg. Therefore, the volume of distribution can not be calculated.
Elimination Route
Plecanatide is minimally absorbed with negligible systemic availability following oral administration. Concentrations of plecanatide and its active metabolite in plasma are below the limit of quantitation after an oral dose of 3 mg. Therefore, standard pharmacokinetic parameters such as AUC, maximum concentration (Cmax), and half-life (t½) cannot be calculated.
Half Life
half-life (t½) cannot be calculated due to negligible systemic absorbance
Clearance
No excretion studies have been conducted in humans.
Elimination Route
No excretion studies have been conducted in humans. Plecanatide and its active metabolite are not measurable in plasma following administration of the recommended clinical doses.
Innovators Monograph
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