Ramelteon

Ramelteon is the first in a new class of sleep agents that selectively binds to the melatonin receptors in the suprachiasmatic nucleus (SCN). It is used for insomnia, particularly delayed sleep onset. Ramelteon has not been shown to produce dependence and has shown no potential for abuse. Ramelteon has been approved by the U.S. Food and Drug Administration for the treatment of insomnia.

Although ramelteon is a prescription drug, unlike the majority of other sedative-hypnotic drugs, it is not categorized as a prohibited substance. Ramelteon’s long-term usage has not been examined. The drug has no potential for addiction, and neither the withdrawal symptoms nor rebound insomnia (a condition where sleeplessness gets worse after the drug is stopped) pose any real risks.

What is the mechanism of action of Ramelteon? 

Ramelteon mimics the natural hormone melatonin, which is secreted in the brain by the pineal gland. Ramelteon acts on melatonin receptors, much like the natural hormone that plays a role in regulating sleep and our circadian cycle.

Specifically, Ramelteon is the first selective melatonin agonist. It works by mimicking melatonin (MT), a naturally occurring hormone that is produced during the sleep period and thought to be responsible for the regulation of the circadian rhythm underlying the normal sleep-wake cycle. Ramelteon has a high affinity for the MT1 and MT2 receptors. The MT1 and MT2 receptors are located in the brain’s suprachiasmatic nuclei (SCN), which is known as the body’s “master clock” because it regulates the 24-hour sleep-wake cycle. Ramelteon has an active metabolite that is less potent but circulates in higher concentrations than the parent compound. The metabolite also has weak affinity for the 5HT2b receptor.

What is the recommended dose of Ramelteon?

Only one 8- mg pill is available for Ramelteon. for Ramelteon It is advised to take the 8 mg dosage 30 minutes before going to bed. Ramelteon shouldn’t be taken with food or right away after eating, particularly if it was a high-fat meal. This might hinder the medication’s efficacy by delaying its absorption.

What happens when you take an overdose of Ramelteon?

Clinical experience with ramelteon overdoses is limited. The overall amount of sleep drug consumed and if the medication was used in conjunction with other medications—particularly other CNS depressants—determine how severe the overdose was.

• Symptoms include swelling of the tongue or throat, trouble breathing, nausea, and vomiting.

Every potential overdose of ramelteon should be considered an emergency at the ER. The prescription bottle of the drug along with any extra drugs linked to the overdose should also be brought, as the data on the prescription label can help the treating physician estimate the quantity of pills consumed.

What are the side effects associated with Ramelteon administration?

The most often reported adverse effects associated with ramelteon are fatigue, headaches, nausea, and dizziness. Ramelteon’s short half-life makes it unlikely that it will produce noticeable sedation or sleepiness during the day. However, some patients, particularly the elderly, may feel a little sleepy during the day.

Symptoms may include body aches or pain, changes in taste, chills, coughing, difficulty breathing, difficulty in moving, Discouragement, ear congestion, feeling sad or empty, Fever, a general feeling of discomfort or illness, Irritability, joint pain, loss of appetite, loss of interest or pleasure, loss of taste, loss of voice, muscle aching or cramping, muscle pain or stiffness, nasal congestion, pain in joints, runny nose, Shivering, Sleeplessness, Sneezing, sore throat, Sweating, swollen joints, trouble concentrating, trouble sleeping, being unable to sleep, unusual tiredness or weakness, and vomiting.

What are the precautions taken when Ramelteon is used?

After taking a single nighttime dosage of ramelteon, people should be informed that it may impair their coordination and alertness.

•  As a result, they shouldn’t drive or engage in other activities requiring alertness. Senior citizens who may have impaired reflexes and coordination are more likely to fall and hurt themselves. 

When using ramelteon with other drugs that depress the central nervous system (CNS), such as alcohol, drugs, antihistamines, and barbiturates, the effects on the CNS may become more pronounced. Regular (particularly frequent) usage of Ramelteon may result in dependence, much like other sleep aids. The possibility of dependence When ramelteon is provided under a doctor’s supervision and used at the recommended dosage, the risk of dependency is very minimal. There haven’t been any reports of rebound sleeplessness or withdrawal symptoms while stopping Ramelteon.

• Ramelteon shouldn’t be taken with food or right away after eating, particularly if it is a high-fat meal.
• Ramelteon should only be taken when needed for sleep, about 30 minutes before going to sleep. Do not take more than the prescribed dose.
• Keep the medication in the original labeled, light-resistant container, away from heat and moisture to avoid drug degradation by them.
•  Keep Ramelteon away from your children.
• Ramelteon may cause daytime drowsiness and impair alertness. Use caution when driving or performing tasks that require alertness. Avoid alcohol when taking ramelteon; the combination may increase sedation and drowsiness and impair coordination.

What is the effect of Ramelteon on pregnancy and lactation?

• Ramelteon is classified as pregnancy category C.

Ramelteon has not been clinically studied in pregnant women, and nothing is known about the risks associated with using it during pregnancy.

•  Ramelteon usage is not advised while a woman is pregnant.

The excretion of ramelteon in breast milk is unknown. When taking a sleep aid, it is not advised for a woman to breastfeed her infant.

This drug has been associated with an effect on reproductive hormones, such as decreased testosterone levels and increased prolactin levels.
It is not known what effect chronic or intermittent use of this drug may have on the reproductive axis in developing humans.

What are the possible drug interactions with Ramelteon?

When used with other drugs, Ramelteon may cause disruptions to the enzymes responsible for breaking it down, which will delay its excretion. This can raise the dosage of ramelteon and intensify its pharmacological effects and negative effects. Therefore, when using the prescription drugs listed in the table below, together with ramelteon, patients should be aware of possible drug interactions.

• Alcohol has an additive effect on the sedative effects of ramelteon and may make the side effects of incoordination, drowsiness, and dizziness worse.
• The antifungal agents Nizoral (ketoconazole) and Diflucan (fluconazole) may inhibit the metabolism of ramelteon, elevating drug levels and the potential for side effects.
• The antidepressant Luvox (fluvoxamine) inhibits the metabolism of ramelteon, significantly increasing plasma levels and having the potential for side effects.
• Rifampin, an antibiotic for the treatment of tuberculosis, may affect the levels of ramelteon, decreasing plasma levels and the effectiveness of the sleep medication.

What are Ramelteon’s disease interactions?

There are five disease interactions with Ramelteon, which include:

• Depression.
• severe renal impairment.
• sleep apnea.
• Glaucoma.
• liver disease.