ramelteon

Action and Spectrum

Actions and Spectrum:

Actions:

• Helps promote relaxation and drowsiness
• Improves the ability to fall asleep
• Increases the duration of sleep
• May improve the quality of sleep

Spectrum:

• ramelteon is specifically used to treat insomnia, specifically difficulty falling asleep.
• It is not indicated for other sleep disorders such as sleep apnea or restless leg syndrome.
• It should not be used as a sedative or hypnotic for other conditions such as anxiety or depression.
• It should not be used in combination with other sleep medications or alcohol.
• It should be used with caution in patients with liver or kidney problems, as it may be metabolized differently in these individuals.

Drug Interaction

Adverse Reaction

Frequency defined

1-10%

Fatigue

Somnolence

Headache

Dizziness

Nausea

Dysgeusia

Frequency Not Defined

Hallucinations

Worsening of insomnia

Depression

Black Box Warning

Black Box Warning

ramelteon used to treat insomnia, carries a black box warning regarding the potential for increased risk of depression and suicidal thoughts.

Contraindication / Caution

Contraindication/Caution:

Contraindication:

• Individuals who are allergic to ramelteon or any of its ingredients should not take the medication.

Caution:

• ramelteon should be used with caution in individuals with a history of depression or other mental health conditions, as it may increase the risk of suicidal thoughts or behavior.
• Individuals with a history of drug or alcohol abuse should also use caution when taking ramelteon, as it may increase the risk of addiction or abuse.
• ramelteon may cause drowsiness or dizziness, and it is recommended to avoid driving or operating heavy machinery while taking the medication.
• The medication should be used with caution in individuals with liver or kidney disease, as it may be metabolized differently in these individuals and may increase the risk of side effects.

ramelteon should be used with caution in individuals taking medications that may interact with it, such as fluvoxamine, ketoconazole, or rifampin. Consult with a healthcare professional before taking any new medications while taking ramelteon.

Pregnancy / Lactation

Pregnancy warnings:   

US FDA pregnancy category: C

Lactation:

Excreted into human milk is unknown

Pregnancy Categories:     

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.  

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.  

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.  

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:

ramelteon is a medication used for the treatment of insomnia. It is a melatonin receptor agonist, which means it works by mimicking the effects of the hormone melatonin in the body. Melatonin is a hormone that regulates the sleep-wake cycle, and its levels naturally increase in the evening to promote sleep.

Pharmacodynamics:

ramelteon binds to the melatonin receptors in the brain, specifically the MT1 and MT2 receptors. By binding to these receptors, it helps to regulate the sleep-wake cycle and promote sleep. It also has a lower binding affinity for other receptors in the brain, such as the serotonin and GABA receptors, which helps to minimize the potential for side effects.

Pharmacokinetics:

Absorption

ramelteon is well absorbed after oral administration, with an absorption rate of 84%. However, due to extensive first-pass metabolism, its bioavailability is relatively low at 1.8%

Distribution

Once absorbed, ramelteon is highly protein-bound, with 82% of the medication being bound to proteins in the blood. This can affect its overall activity and distribution within the body

Metabolism

ramelteon is primarily metabolized by the liver enzyme CYP1A2. This enzyme is responsible for breaking down the medication and reducing its active levels in the body

Elimination and excretion

Most of the medication is excreted via the urine, with 84% of the dose being eliminated in this way. A small amount (4%) is eliminated in the feces. The elimination half-life is approximately 1 hour, which means it is rapidly metabolized and eliminated from the body

Adminstartion

Administration:

Oral Administration

It should be taken orally, usually 30 minutes before bedtime. The recommended starting dose is 8 mg per day, which can be increased to a maximum of 16 mg per day if needed.

It is important to take ramelteon exactly as prescribed by your healthcare provider. Do not take more or less than the recommended dose, and do not take it for longer than prescribed.

Do not drink alcohol while taking Ramelteon, as it can increase the risk of side effects. Also, do not take other sedatives or sleep medications while taking Ramelteon, as it can cause excessive drowsiness and other serious side effects.

If you miss a dose of Ramelteon, do not take a double dose to make up for it. Just take your next scheduled dose at the usual time.

If you experience any side effects while taking Ramelteon, such as drowsiness, dizziness, or nausea, contact your healthcare provider immediately.

It is important to talk to your healthcare provider about any medical conditions you have or any other medications or supplements you are taking before starting treatment with ramelteon.

Patient Information Leaflet

Patient information leaflet

Generic Name: ramelteon

Why do we use ramelteon?

ramelteon is used to treat insomnia, which is a sleep disorder characterized by difficulty falling asleep or staying asleep. It works by binding to a specific receptor in the brain called the melatonin receptor, which helps regulate the body’s sleep-wake cycle. By binding to this receptor, ramelteon helps promote feelings of sleepiness and relaxation, making it easier for people with insomnia to fall asleep and stay asleep. ramelteon is typically used for short-term treatment of insomnia and is not recommended for long-term use.