Trulance (plecanatide)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Plecanatide, a guanylate cyclase-C (GC-C) agonist, stimulates secretion of chloride and bicarbonate into the intestinal lumen, which increases intestinal fluid and accelerates intestinal transit.
Plecanatide, a guanylate cyclase-C (GC-C) agonist, is a 16-amino acid peptide structurally related to endogenous uroguanylin peptide hormone. The parent drug and its active metabolite bind to GC-C receptors on the luminal surface of the intestinal epithelium, which increases intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). In turn, increased intracellular concentrations of cGMP trigger a signal-transduction cascade activating the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel.
This results in secretion of chloride and bicarbonate into the intestinal lumen causing increased intestinal fluid and accelerated intestinal transit.
In animal models, plecanatide has been shown to reduce abdominal muscle contractions (a measure of intestinal pain), increase fluid secretion into the GI tract, accelerate intestinal transit, and change stool consistency. Further research is needed to determine the precise mechanism(s) by which plecanatide relieves intestinal pain.
After oral administration, plecanatide is minimally absorbed with negligible systemic bioavailability. Administration of a single 9-mg dose of plecanatide with either a low-fat, low-calorie or a high-fat, high-calorie meal resulted in looser stools compared with administration in the fasting state. Plecanatide is metabolized in the GI tract to an active metabolite via lysis of the terminal leucine moiety.
Plecanatide and its metabolite are proteolytically degraded within the intestinal lumen to smaller peptides and naturally occurring amino acids.
USES: See also Warning section. Plecanatide is used to treat certain types of bowel problems (chronic idiopathic constipation, irritable bowel syndrome with constipation). It works by increasing fluid in your intestines and helping speed up movement of food through the gut.
Plecanatide may improve stool texture and lessen symptoms such as straining and feelings of incomplete bowel movements.
Generic name: plecanatide
Pronunciation: (ple-KAN-a-tide)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Trulance
Indications
The following indications are listed for Trulance:
- Chronic Idiopathic Constipation
- Constipation Predominant Irritable Bowel Syndrome
Also known as: Constipation Predominant Ibs.
Dosing
The recommended adult dosage of plecanatide for the symptomatic treatment of chronic idiopathic constipation is 3 mg once daily. A dosage of 6 mg daily is not recommended; in clinical trials, the 6-mg daily dosage did not provide additional clinical benefit beyond that provided by the 3-mg daily dosage and was associated with an increased incidence of adverse effects.
Plecanatide is administered orally without regard to food. Although administration with a meal resulted in looser stools when compared with administration in the fasted state, plecanatide was administered with or without food in clinical trials.
Plecanatide tablets should be swallowed whole. Alternatively, for patients who are unable to swallow whole tablets, plecanatide tablets may be crushed and administered orally mixed in applesauce or dispersed in water and administered orally or via a nasogastric or gastric feeding tube. The manufacturer states that mixing crushed plecanatide tablets in soft foods other than applesauce or dispersing the tablets in liquids other than water has not been studied.
If a dose of plecanatide is missed, a double dose should not be administered to make up for the missed dose. The next dose should be taken at the regularly scheduled time.
For administration in applesauce, a plecanatide 3-mg tablet should be crushed to a powder and mixed with one teaspoonful of room-temperature applesauce in a clean container. The entire mixture should be consumed immediately and should not be stored for later use.
For oral administration as an aqueous dispersion, a plecanatide 3-mg tablet should be placed in a clean cup, approximately 30 mL of room-temperature water should then be added to the cup, and the mixture should be gently swirled for at least 10 seconds to disperse the disintegrating tablet. The entire mixture should be consumed immediately. Any residue remaining in the cup should be dispersed in an additional 30 mL of water, gently swirled again for at least 10 seconds, and then consumed immediately. The mixture should not be stored for later use.
For administration via nasogastric or gastric feeding tube, a plecanatide 3-mg tablet should be placed in a clean cup, approximately 30 mL of room-temperature water should be added to the cup, and the mixture should be gently swirled for at least 15 seconds to disperse the disintegrating tablet. The nasogastric or gastric feeding tube should be flushed with 30 mL of water and then the entire contents of the mixture should be drawn up into a syringe and administered immediately. Any residue remaining in the cup should be dispersed in an additional 30 mL of water, gently swirled again for at least 15 seconds, and then administered via the nasogastric or gastric feeding tube using the same syringe. Following administration of the dose, the nasogastric or gastric feeding tube should be flushed with at least 10 mL of water using either the same syringe or a new syringe. The mixture should not be stored for later use.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Because plasma concentrations of plecanatide and its active metabolite are not measurable in adults following oral administration at the recommended dosage, only enzyme and transporter systems that are expressed in the GI tract have been evaluated for interaction potential. In vitro studies indicate that plecanatide and its active metabolite do not inhibit cytochrome P-450 (CYP) isoenzyme 2C9 or 3A4, do not induce CYP3A4, and are not substrates or inhibitors of P-glycoprotein (P-gp) or breast cancer resistance protein (BCRP).
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Plecanatide is contraindicated in infants and children younger than 6 years of age. (See Pediatric Use under Warnings/Precautions: Specific Populations, in Cautions.) The drug also is contraindicated in any patient with known or suspected mechanical GI obstruction.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Diarrhea was reported in 5% of patients with chronic idiopathic constipation receiving plecanatide 3 mg daily and more frequently with the drug than with placebo.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Plecanatide is contraindicated in infants and children younger than 6 years of age and should be avoided in children and adolescents 6 years to younger than 18 years of age.
Safety and efficacy of plecanatide in pediatric patients younger than 18 years of age have not been established, and the drug has caused deaths within 24 hours of administration in toxicology studies in juvenile mice (age approximately equivalent to a human age of 1 month to younger than 2 years). The deaths in young juvenile mice occurred following single oral doses of plecanatide 0.5 and 10 mg/kg administered on postnatal days 7 and 14, respectively. The deaths apparently were due to dehydration resulting from increased fluid secretion into the intestine as a consequence of guanylate cyclase-C (GC-C) stimulation. Because of increased intestinal expression of GC-C, infants and children younger than 6 years of age may be at greater risk of developing diarrhea and its potentially serious consequences compared with individuals 6 years of age and older. Although no deaths were observed in older juvenile mice, use of plecanatide should be avoided in children and adolescents 6 years to younger than 18 years of age because of the deaths reported in younger mice and the lack of safety and efficacy data in pediatric patients. Although administration of the recommended plecanatide dosage (approximately 0.05 mg/kg daily in a 60-kg individual) in adults does not result in measurable plasma concentrations of the drug, systemic absorption was observed in juvenile animal toxicology studies; animal and human doses should not be compared directly for evaluating relative exposure.
Since systemic absorption of plecanatide and its active metabolite is negligible following oral administration, the drug is not expected to result in fetal exposure if administered to pregnant women. However, available data on use of plecanatide in pregnant women are insufficient to inform fetal risk.
No adverse effects on embryofetal development were observed in mice or rabbits when plecanatide was administered orally during organogenesis at dosages up to 800 or 250 mg/kg daily, respectively. In addition, no developmental abnormalities and no effects on growth, learning and memory, or fertility were observed in the offspring of mice that received plecanatide orally at dosages up to 600 mg/kg daily during the period of organogenesis through lactation. Limited systemic exposure to plecanatide was achieved in rabbits during the period of organogenesis. Animal and human doses should not be compared directly for evaluating relative exposure.
It is not known whether plecanatide is distributed into human milk, affects milk production, or affects the breast-fed infant.
Systemic absorption of plecanatide and its active metabolite is negligible following oral administration. It is not known whether the negligible systemic absorption observed in adults will result in clinically important exposure in breast-fed infants. The benefits of breast-feeding and the importance of plecanatide to the woman should be considered along with potential adverse effects on the breast-fed infant from the drug or from the underlying maternal condition. Exposure of infants to plecanatide could result in serious adverse effects. (See Pediatric Use under Warnings/Precautions: Specific Populations, in Cautions.)
Clinical trials of plecanatide did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger adults. In clinical trials in patients with chronic idiopathic constipation, 10% of patients were 65 years of age and older, while 2% were 75 years of age and older. Because of the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly, dosage selection for geriatric patients should be cautious.
ICD codes
No ICD codes are available for this drug.
Formulary status
Search health-plan coverage for this drug by ZIP code.
Choose the first character of a health plan name.
Last reviewed · Source: First Databank (FDB) drug data
On this page
Actions
Sign in to save favorites
Saving this drug requires a free Physicians Office Resource account.