Ibsrela

Name: Ibsrela

Dosing & Uses

Dosage Forms & Strengths

tablet

  • 50mg

Irritable Bowel Syndrome with Constipation

Indicated for irritable bowel syndrome with constipation (IBS-C) in adults

50 mg PO BID immediately before breakfast and dinner

Dosage Modifications

Renal or hepatic impairment: No dose adjustments required

Adverse Effects

>10%

Diarrhea (15-16%)

1-10%

Abdominal distension (2-3%)

Flatulence (3%)

Severe diarrhea (2.5%)

Dizziness (2%)

Rectal bleeding (

Warnings

Black Box Warnings

Contraindicated in patients aged

Pregnancy & Lactation

Pregnancy

Tenapanor is minimally absorbed systemically, with plasma concentrations below the limit of quantification

Maternal use is not expected to result in fetal drug exposure

Lactation

Data are not available regarding the presence in either human or animal milk, its effects on milk production, or its effects on the breastfed infant

The minimal systemic absorption of tenapanor will not result in a clinically relevant exposure to breastfed infants

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Pharmacology

Mechanism of Action

Tenapanor is a locally acting inhibitor of the sodium/hydrogen exchanger 3 (NHE3), an antiporter, also known as a countertransporter, on the apical surface of the small intestine and colon primarily responsible for absorption of dietary sodium

In vitro and animal studies indicate its major metabolite, M1, is not active against NHE3

NHE3 inhibition reduces sodium absorption from the small intestine and colon, resulting in an increase in water secretion into the intestinal lumen, which accelerates intestinal transit time and results in a softer stool consistency

May decrease abdominal pain by decreasing visceral hypersensitivity; shown to reduce visceral hyperalgesia and to normalize colonic neural excitability in animal models

Absorption

Minimally absorbed following repeated BID PO administration; plasma concentrations were below the limit of quantitation (

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