plecanatide is indicated for the treatment of which of the following conditions?

Descriptions Plecanatide is used to treat chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C). It works by increasing the fluid secretion of the bowels, which helps ease the passage of stools and relieve the symptoms of constipation.

Full Answer

What are the uses of Plecanatide?

Plecanatide is used to treat chronic idiopathic constipation, or irritable bowel syndrome with constipation. Plecanatide may also be used for purposes not listed in this medication guide.

Is Plecanatide an effective treatment for chronic constipation?

As of January 2017, plecanatide is approved in the United States for the treatment of chronic idiopathic constipation in adults.

Does Plecanatide work better with or without food?

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.

What is the one letter sequence for Plecanatide?

(one-letter sequence: NDECELCVNVACTGCL). Plecanatide is nearly structurally identical to human uroguanylin, apart from the substitution of Asp 3 with Glu 3. Disulfide bonds exist between Cys 4 and Cys 12, as well as Cys 7 and Cys 15.

How does plecanatide work?

Plecanatide works as a laxative by drawing water in to the gastrointestinal tract thereby softening stool and encouraging its natural passage. Similar to its endogenous counterpart, plecanatide activates guanylate cyclase-C on endothelial cells within the gastrointestinal tract.

How many amino acids are in a plecanatide?

Plecanatide is a 16 amino acid peptide with the amino acid sequence:

What is the name of the drug that is used to treat constipation?

Plecanatide (brand name Trulance ), is a drug approved by the FDA for the treatment of chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation. Plecanatide is an agonist of guanylate cyclase-C. Plecanatide increases intestinal transit and fluid through a buildup of cGMP.

Is plecanatide safe?

Plecanatide has been shown to be safe and effective. It has shown to be at least equally as effective as its main competitor, linaclotide (brand name Linzess), but has been shown to have a lower rate of diarrhea as an adverse drug reaction.

Is plecanatide approved for constipation?

As of January 2017, plecanatide is approved in the United States for the treatment of chronic idiopathic constipation in adults. The presence of this condition is determined using the Rome III diagnostic criteria for chronic constipation which requires that the patient meet stool frequency, stool consistency, incomplete evacuation, and straining requirements in addition to not being a likely candidate for irritable bowel syndrome. The symptoms should also have been present for at least three of the last six months to establish the chronic nature of the condition before treatment with plecanatide is indicated.

Does plecanatide have an antinociceptive effect?

Plecanatide is also known to have an anti-nociceptive effect in animal models, however the exact mechanism of action is not yet fully elucidated.

Can plecanatide cause death?

Use of plecanatide by persons under the age of 6 poses a serious dehydration risk and studies have demonstrated plecanatide can cause death in juvenile mice due to this dehydrating effect. Use of plecanatide is also contraindicated in persons who are suspected of having a mechanical gastrointestinal obstruction.

Overview of Plecanatide

Plecanatide is a guanylate cyclase C agonist which was approved in Jan 2017 by US FDA for the treatment of chronic idiopathic constipation (CIC) in adults.

When should Plecanatide not to be taken? (Contraindications)

Plecanatide should not be taken in patients • Allergic to plecanatide tablets. • Obstruction of the gastrointestinal tract either known or mechanical. • Children under 6 years of age because of the increased risk of severe dehydration. • Safety is not established for the 6 to 18 age group.

What is plecanatide used for?

Plecanatide is a laxative used to treat chronic idiopathic constipation and IBS with constipation.

How does plecanatide work?

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.

What is GC-C agonist?

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.

How much plecanatide is absorbed?

Concentrations of plecanatide and its active metabolite in plasma are below the limit of quantitation after an oral dose of 3 mg.

Where is plecanatide metabolized?

Plecanatide is metabolized in the GI tract to an active metabolite by loss of the terminal leucine moiety. Both plecanatide and the metabolite are proteolytically degraded within the intestinal lumen to smaller peptides and naturally occurring amino acids. Route of elimination.

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Is plecanatide excreted in humans?

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.

Before Using

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Proper Use

Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects.

Precautions

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly and to check for unwanted effects.

Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

How much plecanatide is absorbed?

Concentrations of plecanatide and its active metabolite in plasma are below the limit of quantitation after an oral plecanatide dose of 3 mg. Therefore, standard pharmacokinetic parameters such as AUC, Cmax, and half-life cannot be calculated.

What is plecanatide GC-C?

Plecanatide is structurally related to uroguanylin, and similar to uroguanylin, plecanatide functions as a guanylate cyclase-C (GC-C) agonist. Both plecanatide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation in intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel. This action results in increased intestinal fluid and accelerated gastrointestinal (GI) transit. In animal models, plecanatide has been shown to increase fluid secretion into the GI tract, accelerate GI transit, and cause changes in stool consistency. In addition, in an animal model of visceral pain, plecanatide reduced abdominal muscle contractions, a measure of intestinal pain; the mechanism has not been studied.

How long does plecanatide stay in breast milk?

After administration of multiple doses of plecanatide 3 mg once daily for 2 weeks to nursing mothers, plecanatide and its active metabolite were not measurable in breast milk collected at 2 hours, 6 hours, and 12 hours post-dosing.

Is plecanatide safe for children?

Plecanatide is contraindicated in neonates, infants, and children up to 6 years of age. In nonclinical studies, deaths due to dehydration occurred within 24 hours in young juvenile mice (1 to 3 week-old mice; approximately equivalent to human pediatric patients less than 2 years of age) after administration of single oral doses of plecanatide; deaths did not occur in older juvenile mice (approximately equivalent to humans ages 12 to 17 years). Nevertheless, due to the deaths in young juvenile mice and the lack of clinical safety and efficacy data in pediatric patients, use should be avoided in pediatric patients 6 to 17 years of age.

Can plecanatide cause diarrhea?

Plecanatide should not be administered to patients with severe diarrhea. Diarrhea is the most common adverse effect of plecanatide. Inform patients to notify their health care provider if they develop diarrhea. For severe cases of diarrhea, the healthcare provider should suspend plecanatide treatment and rehydrate the patient.

Is plecanatide contraindicated?

Plecanatide is contraindicated in patients with known or suspected mechanical GI obstruction. Patients with current symptoms (e.g., abdominal pain) that may be suggestive of mechanical GI obstruction should be medically evaluated before using plecanatide.

How to administer a saline tablet?

Administration in water for oral ingestion: Place the tablet in a clean cup. Pour approximately 30 mL of room temperature water into the cup. Mix by gently swirling the tablet and water mixture for at least 10 seconds. The tablet will fall apart into the water. Swallow the entire mixture immediately. If any portion of the tablet remains in the cup, add another 30 mL of water, swirl for 10 seconds, and swallow immediately. Do not store the mixture for later use.

What is plecanatide agonist?

Plecanatide is a structural analog of human uroguanylin, and similarly to uroguanylin, plecanatide functions as a guanylate cyclase-C (GC-C) ago nist. Both plecanatide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation of extracellular cGMP has been associated with a decrease in the activity of pain-sensing nerves in animal models of visceral pain. Elevation of intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through 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.

How long does plecanatide last in mice?

In young juvenile mice (human age equivalent of approximately 1 month to less than 2 years), plecanatide increased fluid-secretion into the intestines as a consequence of stimulation of guanylate cyclase-C (GC-C), resulting in mortality in some mice within the first 24 hours, apparently due to dehydration.

What is TRULANCE used for?

TRULANCE is a prescription medicine used in adults to treat: a type of constipation called chronic idiopathic constipation (CIC). Idiopathic means the cause of the constipation is unknown. irritable bowel syndrome with constipation (IBS-C).

What is the name of the condition that causes constipation?

a type of constipation called chronic idiopathic constipation ( CIC ). Idiopathic means the cause of the constipation is unknown. irritable bowel syndrome with constipation ( IBS -C). It is not known if TRULANCE is safe and effective in children less than 18 years of age.

What are the adverse reactions of tricare?

Adverse reactions reported in less than 2% of TRULANCE-treated patients and at an incidence greater than placebo were: sinusitis, upper respiratory tract infection, abdominal distension, flatulence, abdominal tenderness, and increased liver biochemical tests (2 patients with alanine aminotransferase (ALT) greater than 5 to 15 times the upper limit of normal and 3 patients with aspartate aminotransferase (AST) greater than 5 times the upper limit of normal).

Does plecanatide affect fetal development?

In animal developmental studies, no effects on embryo-fetal development were observed with oral administration of plecanatide in mice and rabbits during organogenesis at doses much higher than the recommended human dosage.

How to report side effects of prescription drugs?

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.

Where is plecanatide metabolized?

Plecanatide exhibits little to no binding to human serum albumin-1-acid glycoprotein.or human αElimination Metabolism Plecanatide is metabolized in the GI tract to an active metabolite by loss of the terminal leucine moiety. Both plecanatide and the metabolite are proteolytically degraded within the intestinal lumen to smaller peptides and naturally occurring amino acids.

What is plecanatide GC-C?

Plecanatide is structurally related to human uroguanylin, and similar to uroguanylin, plecanatide functions as a guanylate cyclase-C (GC-C) agonist. Both plecanatide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation of intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through 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.

Is plecanatide absorbed in milk?

There is no information regarding the presence of plecanatide in human milk, or its effects on milk production or the breastfed infant. No lactation studies in animals have been conducted. Plecanatide and its active metabolite are negligibly absorbed systemically following oral administration [see Clinical Pharmacology

Can adverse reaction rates be directly compared with rates in the clinical trials of another drug?

Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Is plecanatide carcinogenic?

The carcinogenic potential of plecanatide was assessed in 2-year carcinogenicity studies in mice and rats. Plecanatide was not tumorigenic in mice at oral doses up to 90 mg/kg/day or in rats at oral doses up to 100 mg/kg/day. Limited systemic exposure to plecanatide was achieved at the tested dose levels in animals, whereas no detectable exposure occurred in humans. Therefore, animal and human doses should not be compared directly for evaluating relative exposure.

Identification

Pharmacology

• Indication
  1. Plecanatide is indicated for the treatment of chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C) in adult patients.5Reduce drug development failure ratesBuild, train, & validate machine-learning models with evidence-based and structured datase…

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