Ramelteon (Oral)

Ramelteon is an insomnia treatment which induces drowsiness to help patients get to sleep and sleep for longer.

Overview

Ramelteon is a sleep medicine used to treat insomnia. It is a central nervous system (CNS) depressant, which means that it slows down the nervous system in order to induce drowsiness and sleepiness. It works in much the same way as melatonin, a substance which occurs naturally in the body to help us sleep. Ramelteon is taken at bed time to help patients get to sleep faster and sleep for longer throughout the night.

When sleeping medicines like ramelteon are used for extended periods of time, the body builds up a tolerance to them and they become less effective. For this reason, ramelteon is only designed for short term periods of one to two days, and never for longer than two weeks at a time. People with insomnia often have disordered sleeping patterns, and short periods of treatment with ramelteon can help them to establish a healthier sleep routine so that they are more likely to get to sleep once they stop taking the medicine.

Ramelteon is only available with a doctor's prescription. It is administered orally in the form of tablets, and is known in the US under brand name Rozerem.

Conditions treated

  • Insomnia

Type of medicine

  • Central nervous system (CNS) depressant

Side Effects

Ramelteon can cause a variety of side effects as well as its intended effects. The most common side effects are dizziness and sleepiness. Neither of these effects usually require medical treatment unless they become prolonged or persistent during the day. If so, discuss them with your doctor.

Some side effects associated with ramelteon are serious and require urgent medical attention. Contact your doctor immediately or visit the ER if you notice any of the following side effects:

  • Difficulty breathing
  • Joint or muscle pain
  • Cough
  • Confusion
  • Behavior changes
  • Nightmares
  • Hallucinations
  • Memory loss or problems
  • Upset stomach
  • Vomiting
  • Stop in menstruation
  • Nipple discharge
  • Difficulty getting pregnant
  • Reduced sex drive
  • Signs of allergic reaction, such as:
  • Rash
  • Hives
  • Itching
  • Blistered or peeling skin
  • Wheezing
  • Swollen face, lips, tongue or throat
  • Unusual hoarseness
  • Breathing problems

Signs of depression, such as:

  • Suicidal thoughts
  • Unusual anxiety
  • Nervousness
  • Mood swings
  • Abnormal thinking
  • Lack of interest in life

Sign of angioedema, such as:

  • Swollen hands, face, eyes, lips, tongue or throat
  • Breathing problems
  • Difficulty swallowing
  • Unusual hoarseness

If you notice other side effects not listed here, talk to your doctor as soon as possible.

Dosage

For the treatment of insomnia, the recommended dose of ramelteon is 8 mg taken once each day at bedtime. This may vary depending on your medical history; always follow your doctor's instructions.

The safety and efficacy of ramelteon has not been established in pediatric patients. Doctors may still prescribe it if they deem it safe and helpful, and they will determine an appropriate dose.

How to take ramelteon

You should swallow ramelteon tablets whole, without crushing, breaking or chewing them, no sooner than 30 minutes before you go to bed. The tablets will make you drowsy, so only take them if you know you will be able to sleep for 7 to 8 hours. It is recommended that you complete your bedtime preparations immediately after taking ramelteon and then get into bed.

Do not take ramelteon with food or shortly after food as this could make it less effective. Don't plan to perform other activities after taking the medicine.

If you find that the medicine doesn't help you sleep or makes your insomnia worse, call your doctor. If insomnia persists after 7 to 10 days after treatment with ramelteon, there could be other health conditions to blame and you may be required to undergo further tests.

Missed doses

If you miss a dose of ramelteon, only take it if you will be able to sleep for the next 7 to 8 hours. Otherwise, simply skip the dose and take the next dose the following night as usual. For example, if you realize you have missed a dose half an hour or an hour after going to bed, it may be safe to take it. However, if you wake in the middle of the night and realize you forgot to take the medicine and there are only a few hours left before you need to get up, do not take the missed dose. If you do miss and skip a dose, do not double the dose on the following night; take a single dose as usual. Doubling doses could cause severe and dangerous side effects.

Interactions

Ramelteon should never be taken with the following medicines:

  • Fluvoxamine (Luvox)
  • Sodium Oxybate (Xyrem)

If you take either of these medicines, your doctor will either avoid prescribing ramelteon or they may change the other medicines you take.

The following medicines are not recommended for use at the same time as ramelteon, but if both medicines are absolutely necessary, they may still be prescribed with dosage adjustments:

  • Alfentanil
  • Bromazepam
  • Bromopride
  • Buprenorphine (Probuphine)
  • Butorphanol (Stadol NS)
  • Carbinoxamine (Arbinoxa, Karbinal ER, Ryvent, Histex, Carbinoxamine PD, Pediox, Pediatex, Palgic, Carboxine, Cordron NR, Mintex PD)
  • Codeine
  • Dihydrocodeine
  • Doxylamine (Unisom, Nytol Maximum Strength, Aldex AN)
  • Fentanyl Sublimaze ()
  • Flibanserin (Abstral, Actiq, Duragesic, Fentora, Lonsys, Lazanda, Subsys)
  • Fospropofol (Lusedra)
  • Hydrocodone (Hysingla, Zohydro)
  • Hydromorphone (Hysingla ER, Zohydro ER)
  • Meclizine (Bonine, Antivert, D-Vert, Driminate II, Dramamine Less Drowsy, Meclicot, Ru-Vert-M, Medivert, Meni-D)
  • Meperidine (Demerol HCl)
  • Methadone (Dolophine, Methadose, Diskets)
  • Morphine (Arymo ER, Kadian, MorphaBond ER, MS Contin)
  • Oxycodone (Oxaydo, OxyCONTIN, Oxyfast, Roxicodone, Xtampza ER)
  • Oxymorphone (Opana, Numorphan HCl)
  • Pentazocine (Talwin)
  • Periciazine
  • Propofol (Diprivan, Propoven)
  • Remifentanil (Ultiva)
  • Sufentanil
  • Tapentadol (Nucynta)
  • Tramadol (ConZip, Ultram)
  • Zolpidem (Ambien, Edluar, Intermezzo, Zolpimist)

The following medicines can increase the risk of side effects when taken at the same time as ramelteon. However, if both drugs are necessary, your doctor may continue to prescribe them. They may adjust dosages or adjust the times at which you take some medicines.

  • Donepezil (Aricept)
  • Doxepin
  • Fluconazole (Diflucan)
  • Ketoconazole (Nizoral)

Warnings

Risk of respiratory depression

Ramelteon is a CNS depressant and therefore poses a risk of life-threatening respiratory depression, in which breathing can slow to such an extent that it causes unconsciousness or death.

The risk of respiratory depression is heightened in patients with the following conditions:

  • Sleep apnea
  • Asthma
  • Chronic obstructive pulmonary disease (COPD)
  • Emphysema
  • Asthma
  • Bronchitis

Make sure your doctor knows if you suffer from any of these conditions or other conditions related to breathing, the lungs or airways. You may not be able to take ramelteon, depending on the severity of your condition.

The risk of respiratory depression is also heightened if patients take other CNS depressants at the same time as ramelteon. Make sure your doctor knows about all the medicines you take, particularly any of the following:

  • Antidepressants
  • Anti-anxiety medicines
  • Anti-seizure medicines or medicines for epilepsy
  • Muscle relaxants
  • Sedatives
  • Cold and flu medicines
  • Allergic rhinitis medicines and antihistamines
  • Opioid painkillers

Some medicines available over the counter (OTC), particularly cold, flu and anti-allergy medicines, contain ingredients which depress the central nervous system. Always check with your doctor or a pharmacist before taking OTC medicines at the same time as ramelteon.

Avoid alcohol

Alcohol is a CNS depressant and can increase the risk of respiratory and other serious side effects when taking ramelteon. Avoid alcohol completely when taking this medicine. If you think you might have trouble avoiding alcohol while taking this drug, let your doctor know.

Risk of mental depression

Ramelteon can cause extreme low moods (depression) and suicidal thoughts or actions. This risk is heightened in individuals who have a history of depression or suicidal ideation. Tell your doctor immediately if you notice changes in your mood or you have thoughts of harming yourself. You should also tell them if you experience any of the following symptoms:

  • Agitated mood
  • Anxiety
  • Unusual excitement or hyperactivity
  • Hallucinations
  • Nightmares
  • Memory problems

Risk of sleepwalking

There have been rare instances of individuals getting out of bed and doing various activities (such as driving, preparing and eating food, making phone calls) while still partially asleep while taking ramelteon. These individuals usually had no recollection of doing these activities when they woke up. If you find that you have been sleep walking or doing other activities while asleep, let your doctor know immediately.

Daytime drowsiness

You may find that ramelteon makes you feel drowsy during the day. Do not drive, operate machinery or perform any other activities which require you to be alert if you feel drowsy. It is usually safest to avoid driving or operating machinery when you first begin taking the medicine until you know how it affects you during the day.

Pregnancy and childbirth

Ramelteon is a pregnancy category C drug, which means it should only be used during pregnancy if the potential benefits of the drug far outweigh the risks. Animal studies have demonstrated a risk to the fetus, and there are no adequate studies in human pregnancies to determine what effects it may have on human fetuses.

It is not known whether ramelteon is excreted in human breast milk, but it is known that it's excreted in animal milk. The drug is associated with increased prolactin levels and could therefore pose a risk to nursing infants if it is excreted into human milk. For this reason, caution is recommended when considering prescribing the drug to nursing mothers. It may be safer to discontinue breastfeeding while taking this medicine.

Liver disease

Patients with liver disease may not be able to take ramelteon, since decreased liver function can result in the drug remaining in the body for much longer than normal. This increases the risk or severity of side effects. In patients with moderate liver disease, the drug may be used with caution and dosages may be reduced. The drug is not recommended for patients with severe liver disease.

Allergy

Let your doctor know about all allergic reactions you have suffered from in the past, particularly if you have had a reaction to drugs like ramelteon or any of the ingredients in ramelteon.

If you notice signs of allergic reaction, tell your doctor immediately or visit the ER. Symptoms of allergies include:

  • Rash
  • Hives
  • Itching
  • Wheezing
  • Shortness of breath
  • Cough
  • Swollen face, lips, tongue or throat

Storage

You should store ramelteon at room temperature in the container it came in, with the cap tightly closed at all times. It should be kept from freezing and away from heat, moisture and direct light. Do not store it in the bathroom.

CNS depressants like ramelteon can be incredibly dangerous if taken in high quantities or by individuals to which it has not been prescribed. Never let anyone else take your medicine, and keep it well away from children and pets. If you live with children, store it up and away from the ground and avoid using pill containers or minders which do not have childproof safety caps.

If you have unused or leftover ramelteon, do not hold onto it. Instead, ask your healthcare provider how to safely dispose of it. They, or your local garbage or recycling department, may have a medicine take-back program you could use. Do not flush it down the toilet or pour it down the drain.

Summary

Ramelteon is an oral medicine which treats insomnia. Designed for short term use, it induces sleepiness and drowsiness to help patients get to sleep faster and stay asleep for 7 to 8 hours. It should be taken at night, without food, around 30 minutes before bed.

This drug is a central nervous system (CNS) depressant and could cause very serious side effects if taken with other CNS depressants. You should avoid alcohol completely while taking this medicine, and let your doctor know if you take drugs such as antidepressants, sedatives, anti-anxiety medicines and opioid painkillers.

In some instances, ramelteon can cause severe mental depression. Tell your doctor right away if you find your mood becomes very low or you have thoughts of suicide.

 

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Last Reviewed:
January 30, 2018
Last Updated:
April 05, 2018
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