telotristat ethyl

Therapeutic Classification: antidiarrheals

Pharmacologic Classification: tryptophan hydroxylase inhibitors

Indications ⬆ ⬇

REMS

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

Action ⬆ ⬇

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

Therapeutic effects:

Reduced frequency of carcinoid syndrome diarrhea.

Pharmacokinetics ⬆ ⬇

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.

Time/Action Profile ⬆ ⬇

(plasma levels)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	0.5–2 hr (telotstriat ethyl); 1–3 hr (telotstriat)	8 hr

Contraind./Precautions ⬆ ⬇

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.

Adv. Reactions/Side Effects ⬆ ⬇

CNS: headache, depression

CV: peripheral edema

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

Misc: fever

Interactions ⬆ ⬇

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.

Route/Dosage ⬆ ⬇

PO (Adults ): 250 mg 3 times daily.

Availability ⬆ ⬇

Assessment ⬆ ⬇

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.

Implementation ⬆ ⬇

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

Patient/Family Teaching ⬆ ⬇

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.

Evaluation/Desired Outcomes ⬆ ⬇

Resolution of diarrhea.

US Brand Names ⬆ ⬇

Pot. Nursing Diagnoses ⬆ ⬇

Diarrhea(Indications)
Risk for constipation
(Adverse Reactions)

Code ⬆

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)

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Pronunciation ⬇

Classifications ⬆ ⬇