Oral vs Injectable Tirzepatide: Which is More Effective

When it comes to managing weight and metabolic health, tirzepatide has quickly risen through the ranks to take its place alongside semaglutide. As a dual-agonist with an impressive bioavailability of approximately 80%, it has shown to be highly effective in weight management.

It is so effective, it was fast-tracked for FDA-approval and was approved for weight loss in November 2023.

Currently, tirzepatide is only approved as prefilled injectable pens under the brand names Mounjaro and Zepbound. Despite patient preference for oral medications over injectables, oral tirzepatide is not widely available.

While there are rumors of some companies developing oral tirzepatide formulations, none have advanced beyond preliminary stages to clinical testing yet. There are, however, compounded oral tirzepatide tablets available.

What is oral tirzepatide?

Oral tirzepatide is a tablet form of the popular weight loss drug. While it is typically sold as an injectable, there are compounded oral tirzepatide options available through many pharmacies.

Medications are compounded when a drug is in shortage, according to the FDA. The FDA’s drug shortage list lists tirzepatide as “currently in shortage.” So, it is no surprise that there are compounded versions available.

Since there is a demand for oral tirzepatide options, many compounding pharmacies have formulated the medication as oral tirzepatide tablets as opposed to the typical injections.

Is compounded oral tirzepatide safe?

This can be a tricky question to answer, because it relies on several factors. Namely if the compounding pharmacy is reputable and contains the correct amounts of the medication.

Though these medications do contain the same active ingredient (tirzepatide), they will not be the same formulation as the name brand medications. There are currently no FDA-approved tirzepatide generics, so compounded medications are the only other option.

Unfortunately, the FDA does not approve or regulate compounded medications. You want to make sure that your compounded oral tirzepatide supplier is getting their tirzepatide from a registered source and is compounding in a proper sterile environment.

Eli Lilly, the manufacturer of Mounjaro and Zepbound, is the only FDA-approved tirzepatide medication supplier and they do not provide tirzepatide to compounding pharmacies

But, the FDA has a list of registered suppliers you can check.

It is vital that you do your due diligence when looking for compounded oral tirzepatide tablets. There are many unauthorized and counterfeit tirzepatide medications being sold.

Here are the basic guidelines you should follow:

Verify the source. Check the FDA’s list of registered suppliers and the FDA database to see if the facility is registered.
Watch for red flags. Mounjaro® or Zepbound® are registered trademarks. If compounded pharmacies or suppliers are advertising using the brand names, this is illegal.
Check for reviews. Research the compounding pharmacy or seller’s reputation through online reviews and references from other patients or healthcare providers. But, be sure to verify from multiple sources. It is possible to fake reviews, though they are usually obvious.

Is oral tirzepatide effective?

Since compounded medications are unique to the compounding pharmacy, it is difficult to test for efficacy. The active ingredient (tirzepatide) is the same in oral tirzepatide, but the inactive ingredients and other additives may change the efficacy of the medication.

When it comes to the overall efficacy of oral medications vs injectables, it can vary. It is possible that oral tirzepatide may require a higher dose when compared to the standard medication.

This is true in semaglutide (Ozempic). Semaglutide’s injectable medication shows an average 15-20% weight loss at standard doses compared to the 5 pound weight loss of oral doses (3 mg, 7 mg, and 14 mg). At higher doses, such as 50 mg there is an average 15% loss.

Oral tirzepatide side effects

Again, the inactive ingredients may change things. But, the active ingredient (tirzepatide) has a list of potential side effects that can range from mild and temporary to more severe.

Oral tirzepatide side effects can include:

Gastrointestinal (GI) issues such as nausea, vomiting, diarrhea, and constipation occur in as many as 10% of patients.
Fatigue is common as you take in fewer calories
Headaches can occur
With extreme weight loss, there is the possibility of developing Telogen effluvium (TE) (non-scarring hair loss)

More severe side effects include:

Pancreatitis
Liver and kidney issues
Gallbladder injury
A potential increase in risk of thyroid C-cell tumors—though , a recent study suggests that there is no substantial increase in thyroid cancer risk.

Oral tirzepatide cost

Since oral tirzepatide is unique to the compounding pharmacy, the cost will vary based on the seller. It will cost significantly less than the name brand medications, though.

Zepbound, the tirzepatide name brand FDA-approved for weight loss, typically costs about $1000 for a month’s supply.

With compounded tirzepatide medications, the cost is usually below $500 per month. Heally offers a monthly subscription ($399/month) as a way to save.

Oral vs injectable tirzepatide

It is difficult to truly compare the two, since the FDA-approved medications are more clinically researched. The inactive ingredients and additives may also impact the efficacy of compounded oral tirzepatide.

But, generally speaking, the main difference between the two is the method of administration and the frequency of doses.

Injectable tirzepatide is a once-weekly injection. Oral tirzepatide would need to be taken daily.

If you do not want to take an injectable medication and trust the compounding pharmacy/seller or oral tirzepatide tablets, then the oral tirzepatide may be the right choice for you.

When it comes to efficacy, we know that injectable tirzepatide shows clinically significant results. At 15 mg weekly (the maximum dose), the average weight loss is 20.9%. When combined with low-calorie diets and regular exercise, that number can jump to 26%.

Ultimately, the decision is yours to make.