Graves’ Disease: What Medications Are Available?

Graves’ disease is a chronic autoimmune disorder that affects the thyroid, a small gland located at the base of your neck. The condition causes an overproduction of the two thyroid hormones, triiodothyronine (T3) and thyroxine (T4), which is known as hyperthyroidism.

Medications form an important part of the treatment of Graves’ disease. They work by preventing the excessive production of thyroid hormones, reducing symptoms associated with hyperthyroidism, and treating the secondary complications of the disease. 

There are four types of medications that can treat Graves’ disease: 

1. Anti-thyroid medications 

2. Beta-blockers

3. Potassium iodide

4. Steroids 

Not all of these medications might be suitable for you, and it is essential to consult with your doctor before taking something new. 

Antithyroid medications (thioamides)

There are a few types of antithyroid medications, including the following:

• Methimazole (Tapazole) 

• Propylthiouracil (Propacil)

• Carbimazole (Camazol), which is currently not approved for use in the United States 

How are antithyroid medications used?

Antithyroid medications are typically taken for 12 to 18 months,¹ even if your hyperthyroidism symptoms subside during this time. 

This length of treatment has been shown to offer the best chance of remission. Over time, your dosage can be reduced if you continue to show improvements. 

The starting dosage of methimazole is usually between 10mg to 40mg,² and it is taken once per day. With propylthiouracil, the starting dosage is between 50mg to 150mg,² taken three times per day.

For carbimazole, the starting dose is 20mg to 60mg,³ taken once per day.

How do thioamides help with Graves’ disease?

Antithyroid medications stop the thyroid from producing hormones (T3 and T4). This is achieved by preventing the uptake of iodine, which helps the thyroid produce its hormones. 

This action, in turn, reduces the symptoms of hyperthyroidism and restores normal thyroid function. 

Thioamides can also be used as supplementary treatments in the following circumstances:

• Before or after radioiodine therapy

• Before thyroid surgery to restore normal thyroid function (euthyroidism) and minimize the risk of complications during surgery

• Alongside other treatments such as beta-blockers

• Propylthiouracil can inhibit the conversion of T4 to T3 (T3 is stronger and more biologically active than T4) 

What are the benefits of antithyroid medications? 

Studies show that after 12 to 18 months of using antithyroid medications, patients’ remission rates for Graves’ disease range from 30% to 70%.⁴ 

What are the risks and side effects?

Antithyroid medications are not a quick fix. It can take three to six weeks, and even up to three months⁵ in some cases before you notice a significant improvement in symptoms. 

This is because antithyroid medications only block the formation of new thyroid hormones; they do not remove hormones that are stored or circulating through the bloodstream. 

In addition, antithyroid medications are not a definitive cure for Graves’ disease. There is a chance that your hyperthyroidism associated with Graves’ disease will return. 

Some of the side effects of thioamides include: 

• Allergic reactions, such as a rash 

• Gastrointestinal problems  

• A low white blood cell count (agranulocytosis)

• Joint pain

• Liver failure

A low white blood cell count increases your risk of infections. If you experience a sudden onset of sore throat, fever, or mouth ulcers, these could be signs of agranulocytosis, and you should seek urgent medical attention. 

Women in their first trimester of pregnancy are also advised to use propylthiouracil, as methimazole has a high risk of congenital disabilities. 

Propylthiouracil is the treatment of choice in pregnancy, as long as doses less than 300mg per day are used. 

However, propylthiouracil does come with a risk of liver disease, so except for pregnant women, methimazole is usually the recommended medication for people with Graves’ disease. 

While taking antithyroid medications, there is also a chance that you could develop hypothyroidism, a condition where the thyroid doesn’t produce enough thyroid hormones. 

Not taking the medication correctly or stopping it altogether can cause thyroid storm (severe thyrotoxicosis), a sudden worsening of severe hyperthyroidism symptoms that can be fatal. Always consult your doctor before discontinuing your medications.

Beta-blockers

Beta-blockers are most commonly used to treat cardiovascular diseases such as high blood pressure. However, they can also be used for managing hyperthyroidism. 

Examples of beta-blockers include atenolol (Tenormin), propranolol (Inderal), and metoprolol (Lopressor). Propranolol is the preferred option for managing hyperthyroidism. 

How are beta-blockers used?  

In Graves’ disease, beta-blockers are often used in the following conditions: 

• Control symptoms before radioiodine is administered

• If antithyroid medications are unsuitable

• Relieve symptoms while waiting for test results or for longer-term medications to begin working

With propranolol, you will start with a low dose of 20mg to 40mg,⁶ four times per day. This can go up to 240mg-480mg⁷ per day if there is no concern about your ability to clear it from your body safely. 

The use of beta-blockers can be continued until your thyroid functions normally, that is, until your thyroid hormones are within a normal range. 

How do beta-blockers help with Graves’ disease?

Beta-blockers reduce some of the symptoms associated with hyperthyroidism, such as rapid heart rate, heat intolerance, palpitations, muscle tremors, and anxiety. This is achieved by blocking the effects of a chemical messenger called adrenaline. 

Beta-blockers can also inhibit the enzyme⁸ that converts T4 to T3. 

Furthermore, these medications can help to prevent excess blood loss during surgery. 

What are the benefits? 

Beta-blockers work quickly, allowing for prompt control of symptoms. 

Non-selective beta-blockers such as propranolol directly affect hypermetabolism, a defining feature of hyperthyroidism. 

What are the risks and side effects?

Beta-blockers only treat symptoms, and they do not stop the thyroid from over-producing thyroid hormones or remove your thyroid antibodies. This means they don’t directly treat Graves’ disease. 

Because of this, it is important to use beta-blockers in conjunction with other treatments such as antithyroid medications, surgery, or radioiodine therapy. 

The side effects of beta-blockers include nausea, low heart rate, insomnia, anxiety, and low blood sugar levels. Additionally, beta-blockers can be dangerous in people with

• Decompensated heart failure

• A low heart rate

• Spontaneous low blood sugar levels 

• Asthma⁷

Potassium iodide

Potassium iodide is a salt made of a stable form of iodine. It protects the thyroid gland from radioactive iodine and subsequent radiation damage. 

How is potassium iodide used?

Potassium iodide comes in the form of tablets or oral solutions. 

For oral solutions, you will need to add a few drops of potassium iodide into water or juice; this helps prevent gastrointestinal issues. These solutions can be taken three times daily, starting ten days before surgery, if used for this purpose. 

The typical dosage is about 250mg per day. It should be noted that a safe and effective dosage has not yet been determined for children. 

Benefits occur two to seven days after commencing treatment. Potassium iodide is usually only used for two weeks due to the risk of adverse effects if used long-term. 

How does potassium iodide help with Graves’ disease?

After potassium iodide is rapidly absorbed, it can block radioactive iodine uptake into the thyroid gland (via the Wolff-Chaikoff effect).⁹ 

Studies have shown it to be effective for hyperthyroidism, and a potassium iodide preparation is recommended by the American Thyroid Association guidelines.

Potassium iodide has a few important uses in Graves’ disease. In the short term, it can be used in combination with antithyroid medications. It leads to a faster normalization⁸ of thyroid hormone levels, particularly in the first two weeks of treatment. 

It is often used for a short period before surgery (thyroidectomy) to reduce the production and release of thyroid hormones. It will prevent blood loss in surgery by reducing the vascularity of the thyroid gland. 

Potassium iodide is also used after radioiodine therapy. It may be used if beta-blockers fail to control hyperthyroidism.

What are the benefits?

In a study of people with Graves’ disease¹⁰ who experienced side effects from antithyroid medications, potassium iodide therapy was beneficial in two-thirds of cases, and 40% of users reached remission. 

The usage of potassium iodide is also reversible,⁹ which helps limit severe side effects. 

What are the risks and side effects?

Potential side effects of potassium iodide usage include swelling in the salivary glands, a metallic taste in the mouth, sore teeth and gums, diarrhea, and stomach pain. 

Toxicity can cause iodide-induced hypothyroidism with prolonged use, but this is reversible with discontinuation. 

Potassium iodide is not recommended for:

• Pregnant or breastfeeding women, due to the risks to the fetus

• Immunocompromised people

• People with an allergy to iodine

• People with chronic kidney failure

Steroids for Graves’ dermopathy and Graves’ ophthalmopathy

Steroids containing hydrocortisone are beneficial when Graves’ disease affects the skin via a rare condition known as Graves’ dermopathy. Although mild cases can improve without treatment, moderate to severe cases can benefit from certain steroids.  

Corticosteroids such as prednisone are the most common medication used for Graves’ ophthalmopathy, another condition associated with one-third of people who have Graves’ disease. 

With Graves’ ophthalmopathy, the muscles and tissues behind the eyes are affected by the body’s autoimmune response and become inflamed, causing them to bulge outward. 

How are they used?

For Graves’ dermopathy, steroids can take the form of a cream that is directly applied onto the skin or may be given as an intravenous (IV) injection. Their role is to reduce the inflammation that is causing negative skin effects. 

For Graves’ ophthalmopathy, steroids can be taken orally. However, studies show that taking a higher dosage of steroids through an IV can be more effective and cause fewer side effects. 

How do they help with Graves’ disease?

Steroids reduce the inflammation that is the underlying cause of the skin effects associated with Graves’ dermopathy. They also help reduce the immune response and the swelling behind the eyeballs in Graves’ ophthalmopathy. 

What are the benefits?

A study showed that prednisone led to reduced retraction¹¹ of the upper eyelid and less prominent bulging after just one week. 

After four weeks, there were no signs of inflammation in the anterior segment of the eye. After twelve weeks, there were further improvements. 

What are the risks and side effects? 

Possible side effects of steroids include fluid retention, weight gain, and high blood pressure. 

Steroids are generally not a long-term option for treating Graves’ ophthalmopathy or Graves’ dermopathy. Extensive use can lead to weak and brittle bones (osteoporosis) and muscle weakness. 

Teprotumumab

Teprotumumab (Tepezza) is a drug recently approved by the US Food and Drug Administration (FDA).¹¹

How does teprotumumab help with Graves’ disease?

Studies of teprotumumab have shown promising results, with 71% and 83%¹¹ of patients in two different studies experiencing at least a 2mm reduction in the bulging eyes (proptosis). 

How is teprotumumab used?

Teprotumumab is usually given through an intravenous injection once every three weeks, for up to a total of eight times. The recommended dose¹² is an initial 10mg/kg, with subsequent treatments using 20mg/kg. 

What are the benefits?

According to the FDA, teprotumumab provides an alternative, non-surgical option¹¹ that can alter the course of the disease and prevent patients from needing multiple invasive surgeries. 

What are the risks and side effects?

Some of the possible side effects of teprotumumab include nausea, muscle spasms, diarrhea, high blood sugar, dry skin, an altered sense of taste, and hearing loss. 

These symptoms are usually temporary¹³ and are believed to be less severe than the side effects of steroids or radiotherapy.

Pregnant women should not use teprotumumab due to risks to the fetus. If you are planning a pregnancy, it is advised to discontinue teprotumumab at least six months beforehand. 

Teprotumumab may also worsen pre-existing inflammatory bowel disease. 

The lowdown

Medications are an effective way to treat Graves’ disease, hyperthyroidism, and its associated symptoms. 

However, there is no guarantee that any of these medications will cure hyperthyroidism, as even with anti-thyroid drugs, there is a risk of recurrence. In this case, other forms of treatment should be considered, such as surgery or radioiodine therapy.