Rozerem: Side Effects and Effectiveness

Rozerem (ramelteon) was originally approved by the Food and Drug Administration (FDA) in 2005 for the treatment of insomnia—specifically, trouble falling asleep. According to the FDA, Rozerem falls under the sedative-hypnotic drug class that contains other drugs including, but not limited to, Ambien (zolpidem), Lunesta (eszopiclone), and Restoril (temazepam).

While many medications fall under the sedative-hypnotic class, there are subclasses based on the way the drugs work on the body. According to a 2015 literature review published in the journal Expert Opinion on Drug Metabolism & Toxicology, Rozerem was the first member of a novel class of hypnotics called selective melatonin receptor agonists.

In other words, Rozerem was the first of its kind in this class to mimic melatonin, a hormone that your body makes to help regulate your body's natural sleep-wake cycle. At the time of Rozerem's approval, none of the other sedative-hypnotics worked in this way.

Side Effects of Rozerem

As with any medication, Rozerem will have side effects for some people. According to the National Library of Medicine's resource MedlinePlus, common side effects include:

• Drowsiness or tiredness
• Dizziness

MedlinePlus also describes potential serious adverse reactions of Rozerem that warrant an immediate call to your healthcare provider, or in some cases, emergency care. They include:

• Swelling of the tongue or throat
• Difficulty swallowing or breathing
• Feeling that the throat is closing
• Nausea
• Vomiting
• Irregular or missed menstrual periods
• Milky discharge from the nipples
• Decreased sexual desire
• Fertility problems

The Rozerem prescription insert also lists exacerbated insomnia as a possible side effect. So taking Rozerem could potentially do the opposite of what you're trying to accomplish by taking it.

MedlinePlus warns users taking Rozerem to only take it at bedtime and to be ready to sleep at least 7–8 hours. This is because of its sleep-inducing effects, which can occur within 30 minutes of taking it. Rozerem should not be taken with or shortly after meals.

Talk with your healthcare provider or pharmacist if you're prescribed Rozerem and are taking other medications, as several potential drug interactions can take place. MedlinePlus recommends caution if you're taking antifungal medications; certain antacids; certain antibiotics; certain HIV medications; medications for anxiety, pain, or seizures; and sedatives or other sleeping pills.

Does Rozerem Work?

Despite its FDA approval, studies remain mixed on the efficacy of Rozerem. In other words, it's not clear how well Rozerem works.

Rozerem, like its over-the-counter (OTC) relative melatonin, works as a chronobiotic, explained Matthew Ebben, PhD, a sleep specialist at the Weill Cornell Medical College. A chronobiotic is a substance that can shift your body's internal clock.

"[Rozerem] may work for someone who needs to have their circadian rhythms shifted—if someone's internal clock got messed up because of jet lag, and they want to sleep at all the wrong times, for example," said Ebben. "But for people who just aren't sleepy at all—traditional insomniacs—it's unclear whether Rozerem really makes much of a difference."

The efficacy was seemingly so minimal, that the European Medicines Agency rejected the Takeda Pharmaceutical Company's application for approval of Rozerem, according to a 2018 review in the journal Pharmacological Reviews. But study authors of this same review feel that there is sufficient clinical evidence for use of Rozerem in some people with trouble falling asleep.

So if Rozerem works similarly to a melatonin supplement, why not just take OTC melatonin? One word: quality. As a prescription medication, Rozerem is held to high standards in terms of ingredients and strength of the product; supplements, on the other hand, are not regulated by the FDA and there's no way to verify their contents.

To take this topic a little deeper, your body has three receptors for melatonin. When you take a melatonin supplement, melatonin binds to all three receptors, making no distinction between them. Rozerem works differently. According to a 2006 American Family Physician review published shortly after the drug was first approved, Rozerem is highly selective and binds only to two of the three receptors.

Also, many of the other sedative-hypnotics have the potential for abuse or dependence. Because of their highly addictive qualities, these drugs are controlled substances. However, Rozerem is different. It does not have the same potential for abuse, so the FDA said it is not a controlled substance.

Even 12 years after it was first approved by the FDA, Rozerem is still not likely to be abused. A 2017 review of sleep-inducing drugs in the journal US Pharmacist concluded that Rozerem did not have the same addictive qualities as the other drugs in its class.

A Quick Review

If you have trouble falling asleep, and you've tried OTC melatonin but haven't gotten the results you'd like, Rozerem might be worth trying. While it's similar to melatonin supplements, it's designed to work more efficiently with the body's melatonin receptors. Rozerem also has an advantage over other sedative-hypnotic medication: it has not been shown to be addictive, so it is less likely to be abused.