tel-OH-tri-state ETH-il

Therapeutic Classification: antidiarrheals

Pharmacologic Classification: tryptophan hydroxylase inhibitors

• Carcinoid syndrome diarrhea uncontrolled by treatment with somatostatin analog (with somatostatin analog).

• Inhibits tryptophan hydroxylase which reduces production of serotonin and subsequent motility and inflammation in gastrointestinal tract.

• Reduced frequency of carcinoid syndrome diarrhea.

Absorption: Absorption increased with food (especially high-fat meal).

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Telotristat ethyl is metabolized via hydrolysis to active metabolite (telostriat); telotristat is further metabolized in the liver; primarily excreted in feces.

Half-life: Telotristat ethyl — 0.6 hr; telotristat — 5 hr.

(plasma levels)

Contraindicated in:

• None.

Use Cautiously in:

• OB: Safety not established
• Lactation: Use only if potential benefit of breast feeding justifies potential risk to the infant; closely monitor infant for constipation
• Pedi: Safety and effectiveness not established.

CNS: headache, depression.

CV: peripheral edema.

GI: nausea, abdominal pain, constipation, ↓ appetite, flatulence, ↑ liver enzymes.

Misc: fever.

Drug-Drug:

• May ↓ levels of CYP3A4 substrates, including midazolam; may need to ↑ dose of CYP3A4 substrate.
• Octreotide (short-acting) may ↓ levels of telostriat; administer short-acting octreotide 30 min before telostriat.

• PO (Adults): 250 mg 3 times daily.

• Tablets: 250 mg;

• Assess bowel status prior to and periodically during therapy. Monitor for development of constipation and/or severe, persistent, or worsening abdominal pain. Discontinue telotristat ethyl if severe constipation or severe persistent or worsening abdominal pain occur.

• PO: Administer 3 times daily with food. If used in conjunction with octreotide, administer octreotide at least 30 min after telotristat ethyl.

• Instruct patient to take telotristat ethyl as directed. If a dose is missed, omit and take next regularly scheduled dose; do not take 2 doses at same time.
• Advise patient to discontinue telotristat ethyl if severe constipation occurs.
• Advise female patient to notify health care professional if pregnancy is planned or suspected or if breast feeding. If breast feeding during therapy, monitor infant for constipation.

• Resolution of diarrhea.

Xermelo

• Diarrhea (Indications).
• Risk for constipation (Adverse Reactions).

NDC Code^*

• 70183- Lexicon Pharmaceuticals, Inc.
  • 70183-125- Xermelo
    • 70183-125-84- 4 BOX in 1 CASE (70183-125-84) > 7 BLISTER PACK in 1 BOX (70183-125-21) > 3 TABLET in 1 BLISTER PACK (70183-125-03)