Tenapanor is contraindicated in patients <6 years of age; in nonclinical studies in young juvenile rats, administration of tenapanor caused deaths presumed to be due to dehydration. Avoid use of tenapanor in patients 6 to <12 years of age. The safety and effectiveness of tenapanor have not been established in patients <18 years of age.
Irritable bowel syndrome with constipation:
Note: Reserve for patients in whom other therapies for constipation have failed (Wald 2022).
Oral: 50 mg twice daily (Chey 2021; Chey 2017). Some experts consider alternative therapy in patients without improvement by 4 weeks (Wald 2022).
There are no dosage adjustments provided in the manufacturer's labeling; however, dosage adjustment is unlikely due to low systemic absorption and minimal renal excretion of tenapanor.
There are no dosage adjustments provided in the manufacturer's labeling; however, dosage adjustment is unlikely due to low systemic absorption.
Refer to adult dosing.
Severe diarrhea: Discontinue treatment.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Ibsrela: 50 mg
No
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Ibsrela: 50 mg
An FDA-approved patient medication guide, which is available with the product information and at https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/211801s004lbl.pdf#page=14, must be dispensed with this medication.
Oral: Administer immediately prior to breakfast or the first meal of the day and immediately prior to dinner.
Irritable bowel syndrome with constipation: Treatment of irritable bowel syndrome with constipation in adults.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults.
>10%: Gastrointestinal: Diarrhea (15% to 16%; severe diarrhea: 3%)
1% to 10%:
Gastrointestinal: Abdominal distension (2% to 3%), abnormal bowel sounds (<2%), flatulence (3%)
Hematologic & oncologic: Rectal hemorrhage (<2%)
Nervous system: Dizziness (2%)
Patients <6 years of age; known or suspected mechanical GI obstruction.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to tenapanor or any component of the formulation.
Concerns related to adverse effects:
• Diarrhea: May cause diarrhea (including severe cases).
Disease-related concerns:
• Renal impairment: May increase the risk for adverse reactions, including diarrhea and hyperkalemia (requiring hospitalization).
Substrate of CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Enalapril: Tenapanor may decrease serum concentrations of the active metabolite(s) of Enalapril. Tenapanor may decrease the serum concentration of Enalapril. Risk C: Monitor therapy
Administration 5 to 10 minutes before a meal increased the 24-hour stool sodium excretion compared to administration in the fasting state.
Patients who could become pregnant were not included in the initial clinical trials (Chey 2020). Tenapanor has limited systemic absorption following oral administration. Use during pregnancy is not expected to result in significant exposure to the fetus.
It is not known if tenapanor is present in breast milk.
Tenapanor has limited systemic absorption following oral administration; clinically relevant exposure via breast milk is not expected. According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.
Frequency of bowel movements; signs and symptoms of dehydration in patients with diarrhea; serum potassium in patients with renal impairment.
Tenapanor is a sodium/hydrogen exchanger 3 inhibitor, which acts locally to reduce sodium absorption from the small intestine and colon. Reduced sodium absorption results in increased intestinal lumen water secretion, accelerating intestinal transit time, and softening stool consistency. Tenapanor also decreases intestinal permeability and visceral hypersensitivity in animal models, which may reduce abdominal pain.
Absorption: Minimal.
Protein binding: ~99%.
Metabolism: Hepatic via CYP3A4/5 primarily to inactive metabolite M1.
Excretion: Feces (~79% as unchanged drug); urine (~9% as metabolites).
Tablets (Ibsrela Oral)
50 mg (per each): $32.40
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
