Important Safety Information for Oral Tirzepatide

What is Oral Tirzepatide?

Oral Tirzepatide is a prescription sublingual (under-the-tongue) formulation of tirzepatide, a dual GLP-1/GIP receptor agonist used for weight management in adults. When combined with a healthy diet and increased physical activity, it helps regulate appetite and support sustainable weight loss. This needle-free formulation is absorbed through the tissues under your tongue, providing an alternative to injectable tirzepatide.

Boxed Warning: Thyroid C-Cell Tumor Risk

Animal studies have demonstrated that tirzepatide causes thyroid C-cell tumors. Whether tirzepatide causes thyroid tumors, including medullary thyroid carcinoma (MTC), in humans is unknown. Tirzepatide is contraindicated in patients with a personal or family history of MTC or in patients with MEN 2 syndrome.

Watch for and report symptoms that may indicate thyroid tumors:

• A mass or lump in your neck
• Difficulty swallowing or a sensation of something stuck in your throat
• Hoarseness or changes in your voice
• Trouble breathing

Who Should Not Use Oral Tirzepatide?

Do not use this medication if you:

• Have or have had medullary thyroid carcinoma (MTC) or have family members with this condition
• Have Multiple Endocrine Neoplasia syndrome type 2 (MEN 2)
• Have had a serious allergic reaction to tirzepatide
• Have severe gastroparesis or other severe gastrointestinal motility disorders
• Are pregnant or may become pregnant
• Are nursing a baby

Warnings and Precautions

1. Acute PancreatitisPancreatitis has been reported in patients using tirzepatide. Symptoms include severe upper abdominal pain (often radiating to the back), nausea, and vomiting. Discontinue oral tirzepatide immediately if pancreatitis is suspected and seek medical care. Do not resume if pancreatitis is confirmed.

2. Risk of Low Blood SugarIf you take oral tirzepatide with insulin or medications that cause insulin release, you may experience hypoglycemia. Learn to recognize low blood sugar symptoms and always have a fast-acting sugar source available.

3. Kidney Function ChangesDehydration caused by gastrointestinal side effects (vomiting, diarrhea) can worsen kidney function. Patients with existing kidney problems are at higher risk. Stay hydrated and report severe or prolonged GI symptoms to your provider.

4. Gallbladder ComplicationsTirzepatide may increase gallbladder disease risk. Contact your healthcare provider if you develop sudden severe abdominal pain, particularly in the upper right area, with nausea or vomiting.

5. Allergic ReactionsSevere hypersensitivity reactions including anaphylaxis have occurred. Stop taking oral tirzepatide and get emergency help if you experience swelling of face/throat, severe rash, difficulty breathing, or signs of shock.

6. Gastrointestinal Adverse EffectsNausea, vomiting, diarrhea, and constipation are common, especially during initial treatment. These effects may be more pronounced with oral formulations. Take as directed and report persistent symptoms to your provider.

7. Pre-Surgical ConsiderationsTirzepatide delays stomach emptying. Inform all healthcare providers about your use of this medication before any surgical or endoscopic procedure, as it may affect preoperative fasting protocols.

Common Side Effects

The most common side effects include:

• Nausea
• Diarrhea
• Constipation
• Vomiting
• Decreased appetite
• Indigestion
• Stomach discomfort
• Acid reflux
• Fatigue
• Headache

Most gastrointestinal side effects occur early in treatment or when doses are increased and tend to improve over time.

Pregnancy and Breastfeeding

Pregnancy: Do not use oral tirzepatide if you are pregnant. There is no benefit to weight loss during pregnancy, and animal studies suggest potential harm to a developing baby. Stop this medication at least 4 weeks before trying to conceive.

Breastfeeding: Whether tirzepatide passes into breast milk is unknown. Because of potential risks to infants, you should either stop breastfeeding or stop using this medication—discuss with your healthcare provider.

Drug Interactions

Inform your healthcare provider about all medications you take:

• Insulin and sulfonylureas – increased risk of low blood sugar
• Birth control pills – may have reduced effectiveness; use backup contraception
• Medications that require precise absorption timing
• Other GLP-1 or GIP-based medications – do not use together

How to Take Oral Tirzepatide

• Place the prescribed dose under your tongue using the provided dropper
• Hold under your tongue for at least 90 seconds before swallowing
• Do not eat or drink anything (except water) for 30 minutes before and after taking your dose
• Take at the same time each day for consistent absorption
• Follow your provider's dosing instructions exactly

Storage

• Store at room temperature, away from direct sunlight and excessive heat
• Keep the bottle tightly closed when not in use
• Do not freeze
• Keep out of reach of children

When to Seek Emergency Medical Care

Seek immediate medical attention for:

• Severe abdominal pain that doesn't resolve
• Signs of allergic reaction (swelling, difficulty breathing, severe rash)
• Severe dehydration (extreme thirst, very dark urine, dizziness, confusion)
• Signs of low blood sugar that don't respond to treatment
• Any symptoms that concern you

Reporting Side Effects

You may report side effects to the FDA at www.fda.gov/medwatch or by calling 1-800-FDA-1088.

Consult your healthcare provider with any questions about oral tirzepatide and whether it is appropriate for you.

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