Ibsrela
Ibsrela Uses, Dosage, Side Effects, Food Interaction and all others data.
Ibsrela is a novel, small molecule medication approved in September 2019 for the treatment of constipation-predominant irritable bowel-syndrome (IBS-C). It was first designed and synthesized in 2012. As an inhibitor of the sodium/hydrogen exchanger isoform 3 (NHE3) transporter, it is the first and currently only medication within its class and therefore exists as a novel alternative in the treatment of IBS-C.
Through the inhibition of dietary sodium absorption tenapanor causes an increase in water secretion into the intestines, thereby decreasing transit time and softening stool consistency.
| Trade Name | Ibsrela |
| Availability | Prescription only |
| Generic | Tenapanor |
| Tenapanor Other Names | Tenapanor |
| Related Drugs | dicyclomine, Bentyl, hyoscyamine, Amitiza, Metamucil, Lotronex |
| Weight | ibs + c, |
| Type | Tablets date of approval: september 12, 2019 company: ardelyx, inc. treatment for: irritable bowel syndrome with constipation |
| Formula | C50H66Cl4N8O10S2 |
| Weight | Average: 1145.04 Monoisotopic: 1142.3097435 |
| Protein binding | Both tenapanor and its principle metabolite, M1, are highly plasma protein bound at approximately 99% and 97%, respectively. The specific proteins to which tenapanor and its metabolite binds have yet to be elucidated. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States, |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Ibsrela is an NHE3 inhibitor indicated for the treatment of constipation-predominant irritable bowel syndrome (IBS-C).
Ibsrela is indicated for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) in adults. It is also currently being investigated as a treatment for hyperphosphatemia in chronic kidney disease patients undergoing dialysis (NCT02081534 and NCT02675998).
Ibsrela is also used to associated treatment for these conditions: Constipation-predominant Irritable Bowel Syndrome (IBS-C)
How Ibsrela works
Ibsrela is a locally-acting small molecule inhibitor of the sodium/hydrogen exchanger isoform 3 (NHE3), an antiporter expressed on the apical surface of enterocytes in the small intestine and colon which is involved in sodium-fluid homeostasis. By inhibiting this antiporter tenapanor causes retention of sodium within the lumen of the intestine - this results in an osmotic gradient that draws water into the lumen and softens stool consistency.
There is some evidence that tenapanor can inhibit the uptake of dietary phosphorus in the gastrointestinal tract, though the exact mechanism of this activity has yet to be elucidated.
Toxicity
Symptoms of overdose are likely to be consistent with tenapanor's adverse effect profile, and may therefore include gastrointestinal effects such as diarrhea. Dehydration may occur depending on duration and severity of diarrhea. No specific management strategies have been proposed in cases of overdose.
Food Interaction
- Take before a meal. Ibsrela should be administered immediately prior to the first meal of the day and immediately prior to dinner.
[Moderate] ADJUST DOSING INTERVAL: Administration of tenapanor immediately before a meal may enhance its effectiveness.
In clinical trials, administration of tenapanor 5 to 10 minutes before a meal increased the 24-hour stool sodium excretion compared to taking tenapanor in the fed or fasting state.
The resulting higher levels of sodium in the intestine and colon cause an increase in water secretion into the intestinal lumen, which accelerates intestinal transit time and results in a softer stool consistency.
MANAGEMENT: The manufacturer recommends administering tenapanor immediately prior to breakfast or the first meal of the day and immediately prior to dinner.
Elimination Route
Ibsrela undergoes very minimal systemic absorption following oral administration. During clinical trials, plasma concentrations were below the limit of quantitation (i.e. less than 0.5 ng/mL) in the majority of samples from healthy subjects - for this reason, typical pharmacokinetic values related to absorption such as AUC and Cmax were unable to be ascertained.
The effects of tenapanor are greatest when administered 5 to 10 minutes before meals.
Half Life
Ibsrela's FDA label states that its half-life could not be determined during clinical trials due to its minimal systemic absorption resulting in plasma concentrations below the limit of quantitation (i.e. less than 0.5 ng/mL).
Elimination Route
Following administration of a radio labeled dose of tenapanor, 70% of the radioactivity was excreted in the feces within 120 hours of administration and 79% within 240 hours. Approximately 65% of the total dose is excreted as unchanged parent drug within 144 hours of administration. Only 9% of the administered dose was found in the urine, existing primarily as metabolites. Ibsrela's M1 metabolite is excreted unchanged in the urine and accounts for approximately 1.5% of the total dose within 144 hours of administration.
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