tenapanor (Rx)

Brand and Other Names:Ibsrela
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Dosing & Uses

AdultPediatric

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

<18 years: Safety and efficacy not established

Also see Black Box Warning and Contraindications

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Adverse Effects

>10%

Diarrhea (15-16%)

1-10%

Abdominal distension (2-3%)

Flatulence (3%)

Severe diarrhea (2.5%)

Dizziness (2%)

Rectal bleeding (<2%)

Abnormal GI sounds (<2%)

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Warnings

Black Box Warnings

Contraindicated in patients aged <6 yr

In nonclinical studies in young juvenile rats, tenapanor administration caused deaths presumed to be due to dehydration

Avoid use in patients aged 6 to <12 yr

Safety and effectiveness have not been established in patients aged <18 yr

Contraindications

Children aged <6 years owing to risk of serious dehydration

Known or suspected mechanical GI obstruction

Cautions

Diarrhea may occur; if severe, suspend dosing and rehydrate patient

Contraindicated in children aged <6 yr; avoid use in children aged 6-12 yr owing to risk of dehydration in young children

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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.

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Pharmacology

Mechanism of Action

Tenapanor is a locally acting inhibitor of the sodium/hydrogen exchanger 3 (NHE3), an antiporter expressed 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 (<0.5 ng/mL)

Peak plasma concentration (M1 metabolite): ~13 ng/mL after single 50-mg dose; 15 ng/mL (steady-state)

Effect of food

  • Administration of tenapanor 5-10 minutes before a meal increased 24-hr stool sodium excretion compared with taking tenapanor in the fed or fasting condition

Distribution

Protein bound: 99%; 97% (M1 metabolite)

Metabolism

Metabolized primarily by CYP3A4/5, and low levels of its major metabolite, M1, are detected in plasma

Elimination

Excretion: 70% (feces); 9% (urine)

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Administration

Oral Administration

Take immediately before breakfast or the first meal of the day and immediately before dinner

Missed dose

  • Skip missed dose and take the next dose at the regular time
  • Do not take 2 doses at the same time

Storage

Store at 68-77ºF (20-25ºC)

Keep in tightly closed original container and protect from moisture

Do not remove desiccant from the bottle

Do not subdivide or repackage

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Images

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Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
  • Manage and view all your plans together – even plans in different states.
  • Compare formulary status to other drugs in the same class.
  • Access your plan list on any device – mobile or desktop.

The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.