Ibsrela (tenapanor HCl)
Irritable Bowel Syndrome Agents Oral Tablet
Last reviewed · Source: First Databank (FDB) drug data
Overview
Tenapanor is a locally acting inhibitor of sodium/hydrogen exchanger isoform 3 (NHE3), a protein that facilitates absorption of intestinal sodium through proton exchange.
Tenapanor is a locally acting inhibitor of sodium/hydrogen exchanger isoform 3 (NHE3), which is expressed on the apical surface of the small intestine and colon and transports sodium in exchange for intracellular protons across cell membranes. NHE3 is primarily responsible for absorption of dietary sodium from the intestinal lumen through proton exchange. Intestinal inhibition of NHE3 by tenapanor reduces absorption of sodium from the small intestine and colon, resulting in increased water secretion into the intestinal lumen, which accelerates intestinal transit and results in a softer stool consistency.
In animal models, tenapanor reduced abdominal pain by decreasing visceral hypersensitivity and intestinal permeability. In a rat model of colonic hypersensitivity, tenapanor reduced visceral hyperalgesia and normalized colonic sensory neuronal excitability.
Tenapanor is minimally absorbed following oral administration. Plasma concentrations of tenapanor were below the limit of quantitation in most samples obtained from healthy individuals following oral administration of single or repeated (50 mg twice daily) doses of the drug. Therefore, pharmacokinetic parameters such as area under the plasma concentration-time curve (AUC), peak plasma concentration, and half-life could not be determined.
Tenapanor is metabolized principally by cytochrome P-450 (CYP) isoenzyme 3A4/5, and its major metabolite, M1, is detected at low concentrations in plasma. In vitro and animal studies indicate that M1 is not active against NHE3. In vitro, tenapanor and M1 are approximately 99 and 97% bound, respectively, to plasma proteins.
Following oral administration of a single 15-mg radiolabeled dose of tenapanor in healthy individuals, approximately 70 or 79% of the radioactivity was excreted in feces within 120 or 240 hours, respectively, mostly as unchanged drug (65% of the administered dose within 144 hours). Approximately 9% of the administered dose was recovered in urine, mainly as metabolites. Recovery of M1 in urine accounted for 1.5% of the administered dose within 144 hours.
USES: See also Warning section. Tenapanor is used to treat a certain bowel problem (irritable bowel syndrome with constipation). It works by increasing fluid in your intestines and helping speed up movement of food through the gut.
Tenapanor may improve stool texture and lessen abdominal pain/discomfort.
Generic name: tenapanor HCl
Pronunciation: (ten-A-pa-nor)
Drug class: Irritable Bowel Syndrome Agents
Therapeutic class: Gastrointestinal Therapy Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Ibsrela
Indications
The following indications are listed for Ibsrela:
- Constipation Predominant Irritable Bowel Syndrome
Also known as: Constipation Predominant Ibs.
Dosing
Dosage of tenapanor hydrochloride is expressed in terms of tenapanor.
The recommended adult dosage of tenapanor for the symptomatic treatment of irritable bowel syndrome (IBS) with constipation is 50 mg twice daily.
Tenapanor hydrochloride is administered orally twice daily, immediately prior to breakfast or the first meal of the day and immediately prior to dinner. Administration of tenapanor 5-10 minutes before a meal increases 24-hour stool sodium excretion compared with administration under fed or fasting conditions.
If a dose is missed, the missed dose should be omitted and the next dose taken at the regularly scheduled time. Two doses should not be taken at the same time to make up for a missed dose. Tenapanor should be stored at 20-25degreesC in the original container in a dry place; protect from moisture.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Ibsrela 50 Mg Tablet | Maintenance | Take 1 tablet (50 mg) by oral route 2 times per day. |
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
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
*Pediatric patients younger than 6 years of age due to the risk of serious dehydration.
*Known or suspected mechanical GI obstruction.
- Gastrointestinal obstruction
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in 2% or more of patients receiving tenapanor include diarrhea, abdominal distension, flatulence, and dizziness.
Rare or Very Rare
- Dehydration
- Rectal bleeding
More Frequent
- Abdominal distension
- Diarrhea
- Dizziness
- Flatulence
Rare or Very Rare
- Bowel sounds hyperactive
- Pruritus of skin
- Skin rash
- Urticaria
Precautions
No enhanced messaging available.
Tenapanor is contraindicated in pediatric patients younger than 6 years of age and should be avoided in children 6 years to younger than 12 years of age. Safety and efficacy of the drug have not been established in patients younger than 18 years of age. Tenapanor has caused deaths in toxicology studies in young juvenile rats (age approximately equivalent to a human age of younger than 2 years). Data are lacking in older juvenile rats (age approximately equivalent to a human age of 2 years to younger than 12 years).
One toxicology study in neonatal rats was terminated early because of deaths and decreases in body weight (reductions of 24-33% compared with placebo) at tenapanor dosages of 5-10 mg/kg daily. In a second study, neonatal rats received tenapanor at dosages of 0.1-5 mg/kg daily on postnatal days 5-24. Treatment-related deaths were observed at dosages of 0.5-5 mg/kg daily and occurred as early as postnatal day 8, with most of the deaths occurring between postnatal days 15 and 25. At a dosage of 5 mg/kg daily, mean body weight was reduced by 35-47% compared with control animals. Slight (5-11%) reductions in mean tibial length were observed in animals receiving tenapanor 0.5-5 mg/kg daily and correlated with the decrements in body weight observed at these dosages. Decreased spleen, thymus, and/or ovary weight; GI distension; and microscopic findings of increased osteoclasts, eroded bone, and/or decreased bone in the sternum and/or femorotibial joint also were observed at dosages of 0.5-5 mg/kg daily.
Since tenapanor is minimally absorbed following oral administration (i.e., plasma concentrations are below the limit of quantification), the drug is not expected to result in fetal exposure if administered to pregnant women. Limited data regarding tenapanor exposure during pregnancy have not identified any drug-associated risk for major birth defects, spontaneous abortion, or adverse maternal or fetal outcomes.
In reproduction studies in pregnant rats and rabbits, no adverse fetal effects were observed at dosages of 0.1 and up to 8.8 times, respectively, the maximum recommended human dosage. In a prenatal and postnatal developmental study in mice, no adverse developmental effects were observed at tenapanor dosages up to approximately 9.7 times the maximum recommended human dosage.
It is not known whether tenapanor is distributed into milk, affects milk production, or affects the breast-fed infant. Tenapanor is minimally absorbed following oral administration (i.e., plasma concentrations are below the limit of quantification), and the manufacturer states that the minimal systemic absorption will not result in clinically important exposure in breast-fed infants. The benefits of breast-feeding should be considered along with the woman's clinical need for tenapanor and any potential adverse effects on the breast-fed infant from the drug or from the underlying maternal condition.
The manufacturer makes no specific dosage recommendations for geriatric patients.
In placebo-controlled clinical trials of tenapanor for symptomatic treatment of IBS with constipation, 8% of patients were 65 years of age or older. Although no overall differences in efficacy or safety were observed between geriatric patients and younger adults, the possibility that some older patients may exhibit increased sensitivity to the drug cannot be ruled out.
ICD codes
| Code | Type | Description |
|---|---|---|
| Constipation predominant irritable bowel syndrome | ||
| K58.1 | ICD10CM | Irritable bowel syndrome with constipation |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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