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Telotristat Ethyl: Side Effects, Uses, Dosage, Interactions, Warnings

Telotristat Ethyl

What Is Telotristat Ethyl Used For and How Does it Work?

Telotristat ethyl is used for carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy in adults inadequately controlled by SSA therapy.

Telotristat ethyl is available under the following different brand names: Xermelo.

What Are the Dosages of Telotristat Ethyl?

Dosage Forms and Strengths

Tablets

  • 250 mg

Dosage Considerations – Should be Given as Follows:

Carcinoid Syndrome Diarrhea

  • Indicated for carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy in adults inadequately controlled by SSA therapy
  • 50 mg orally three times daily
  • Safety and efficacy not established in pediatric patients

Safety and efficacy not established in pediatric patients.

What Are Side Effects Associated with Using Telotristat Ethyl?

Common side effects of telotristat_ethyl include:

  • Nausea
  • Headache
  • Increased GGT
  • Depression
  • Swelling of extremities
  • Gas (flatulence)
  • Decreased appetite
  • Fever
  • Abdominal pain
  • Constipation
  • Increased alkaline phosphatase
  • Increased ALT and AST

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

What Other Drugs Interact with Telotristat Ethyl?

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

Severe interactions of telotristat ethyl include:

  • doravirine

Serious interactions of telotristat ethyl include:

  • avapritinib
  • entrectinib
  • fedratinib
  • lemborexant
  • lorlatinib
  • pretomanid
  • siponimod
  • tazemetostat
  • voxelotor
  • zanubrutinib

Telotristat ethyl has moderate interactions with at least 32 different drugs.

Telotristat ethyl has no listed mild interactions with other drugs.

What Are Warnings and Precautions for Telotristat Ethyl?

Warnings

This medication contains telotristat ethyl. Do not take Xermelo if you are allergic to telotristat ethyl or any ingredients contained in this drug.

Contraindications

  • None

Effects of Drug Abuse

  • No information is available.

Short-Term Effects

  • See "What Are Side Effects Associated with Using Telotristat Ethyl?"

Long-Term Effects

  • See "What Are Side Effects Associated with Using Telotristat Ethyl?"

Cautions

Reduces bowel movement frequency; monitor for development of constipation and/or severe, persistent, or worsening abdominal pain; discontinue if severe constipation or severe persistent or worsening abdominal pain develops

Drug interaction overview

  • Telotristat ethyl induces CYP3A4 and may reduce systemic exposure of sensitive CYP3A4 substrates
  • Short-acting octreotide decreases telotristat Cmax and AUC by 79% and 68%, respectively; administer octreotide at least 30 minutes after telotristat ethyl (also see Administration)

Pregnancy and Lactation

There are no human data regarding the use of telotristat ethyl in pregnant women to inform a drug-associated risk. Consult your doctor.

It is unknown if telotristat ethyl is distributed in human breast milk. Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for telotristat ethyl, and any potential adverse effects on the breastfed infant from the drug or the underlying maternal condition. If telotristat ethyl is administered to a breastfeeding woman, monitor the infant for constipation.

References
https://reference.medscape.com/drug/xermelo-telotristat-ethyl-1000118