Rybelsus: No Needles? No Problem!

The World’s First Oral GLP-1 RA, Rybelsus, Just Made Gaining Control of Diabetes Even Easier!

Are you concerned about using needles but need to control your diabetes and lose weight? Not to worry! In addition to its once-weekly injectable formulation (Ozempic, injectable semaglutide), semaglutide now also comes in an oral tablet.  Just approved in September 2019 by the U.S. Food and Drug Administration (FDA) for the treatment of adults with type 2 diabetes (T2D), Rybelsus (oral semaglutide tablets) is the world’s first and only oral Glucagon like peptide-1 receptor agonist (GLP-1 RA) medication.

How Does Rybelsus Work In Our Body?

Rybelsus is a GLP-1 RA, an incretin based therapy for T2D. GLP-1 is a hormone that occurs naturally in our body, and Rybelsus is a synthetic compound that is designed to work similarly. When glucose concentrations rise, Rybelsus signals the pancreas to release insulin to lower glucose values, only when they are high. It also slows the liver’s own glucose production. In addition, it makes people feel fuller faster, so they are satisfied with less food. The overall result is a great control of blood glucose, both after meals as well as throughout the day.

Unlike all other injectable GLP1 RA’s, Rybelsus has been specially formulated to protect it from breaking down in the acidic nature of the stomach. It has a special addition called salcaprozate sodium (SNAC), which facilitates the absorption of the drug after it is taken orally.

How Do You Take Rybelsus?

Rybelsus comes in tablets of 3mg, 7mg, and 14mg and should be taken once daily. In order to allow the medication to work best, several important instructions need to be followed:

(1) Take Rybelsus upon waking, on an empty stomach; (2) Take with not more than 4 oz of plain water; and (3) Wait 30 minutes before eating or taking any other medications; waiting less will lessen the effect, and waiting longer may increase the exposure to the drug.

Initially, a low dose of 3mg is given for 30 days. This is the starting dose which allows the body to get used to the drug. Once this dose is tolerated, the dose increases to 7mg for 30 more days. If additional glucose control is needed, then the dose can be increased to the maximum of 14 mg once per day.

What Can You Expect?

Rybelsus use has demonstrated improvements in both blood glucose concentrations and A1c, as well as reductions in weight. In clinical studies, Rybelsus reduced A1c by an average of 0.9-1.4%, and weight loss of up to 4.4kg (~10 lbs). Additionally, the studies suggest that Rybelsus can also reduce the risk of cardiovascular problems such as stroke and heart attack. An application for this additional indication for use is pending with the FDA, and a decision is expected early next year.

Similar to all GLP-1 RA medications and due to the mechanism of the drug, Rybelsus reduces gut motility (this is usually what make people feel fuller faster), and mild to moderate stomach upset and/or nausea may occur. Usually these symptoms go away within a few weeks of starting Rybelsus, and eating smaller food portions throughout the day may help alleviate the indigestion symptoms. In clinical trials, some people experienced worsening of their diabetic retinopathy, mostly because Rybelsus works so quickly. This is part of the reason treatment is started with a low dose, and increased gradually over a few months.

Is Rybelsus Right for You?

Before starting Rybelsus, you and your provider will want to discuss your medical and family history. Specifically, discuss if you have problems with your pancreas or kidney, have a history of diabetic retinopathy, are pregnant or planning to become pregnant, have any history of severe gastrointestinal (GI) disease, thyroid cancer, or family history of thyroid cancer. Getting an annual dilated eye exam is also recommended. Also, be sure to inform your healthcare provider of all prescription, over-the-counter, and herbal medications that you are taking in order to avoid any drug interactions.

Bottom Line:

Like other GLP-1 RAs, Rybelsus is a strong A1c reducer with the added benefits of weight loss and potential cardiovascular protection. But, unlike other available GLP-1 RAs, Rybelsus is a once-daily oral tablet and will appeal to patients who may be opposed to injectable T2D therapies. Talk to your healthcare provider to determine if Rybelsus is a good option to help control blood glucose and weight, as well as reach your A1c goals.

 

 

Authors:

James Park, 3rd Year Student Pharmacist at UCSD Skaggs School of Pharmacy and Pharmaceutical Sciences.

Candis M. Morello, Pharm D, CDE, FCSHP, FASHP, Associate Dean for Student Affairs and Professor of Clinical Pharmacy at UCSD Skaggs School of Pharmacy and Pharmaceutical Sciences, Clinical Pharmacist Specialist at VASDHS.

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