雷美替胺(Ramelteon)的功效与作用都有哪些

Ramelteon is a prescription sleeping pill developed by Takeda Pharmaceuticals of Japan. It was approved by the US FDA in July 2005 and is marketed under the trade name Rozerem.

Efficacy and effects of Ramelteon

It is a highly selective melatonin receptor agonist that does not act on the common GABA receptors in the brain (the target of traditional sleeping pills). Instead, it specifically targets and activates the melatonin MT₁ and MT₂ receptors located in the suprachiasmatic nucleus of the brain, improving the symptoms of difficulty falling asleep in patients with insomnia.

Indications of Ramelteon

Ramelteon is used to treat insomnia characterized by difficulty falling asleep.

The pictures are from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Ramelteon usage and dosage

1. Standard dose

The recommended dose is 8 mg, once a day.

2. Medication time

It must be taken within 30 minutes before you plan to go to sleep. After taking the medication, you should prepare for bed immediately and should not engage in other activities, especially things that require concentration or alertness (such as driving, operating machinery).

3. How to take it

Do not take it with a high-fat meal or immediately after a meal. It is recommended to take the medicine on a non-full stomach. Tablets should be swallowed whole and not broken, crushed or chewed.

4. Medication adjustment for special groups

(1) Patients with hepatic insufficiency: Those with mild liver impairment should use it with caution; those with moderate impairment should be more cautious and consult their doctor whether the dose needs to be adjusted; patients with severe liver impairment are prohibited from using it.

(2) Elderly patients and patients with renal insufficiency: Usually no dose adjustment is required.

Important precautions for Ramelteon

1. Severe allergic reactions

In rare cases, angioedema (such as swelling of the tongue and throat) and allergic reactions may occur. Once symptoms such as difficulty breathing and larynx closing occur, you need to seek medical attention immediately and do not use the drug again.

2. Complex sleep behaviors

Patients may perform activities while not fully awake and have no memory afterwards, such as "sleepwalking", preparing and eating food, making phone calls, having sex, etc. If this happens, you must stop taking the medicine immediately and contact your doctor.

3. Endocrine effects

Long-term use may affect reproductive hormone levels, leading to a decrease in testosterone and an increase in prolactin, which may manifest as female menstrual disorders, non-lactation lactation, loss of sexual desire in both men and women, or fertility problems.

4. Interaction between alcohol and drugs

It is absolutely forbidden to use it together with alcohol. The combined use of the two will superimpose the central depressant effect and increase the risk of drowsiness and complex sleep behaviors.

Do not use it in combination with strong CYP1A2 inhibitors (such as fluvoxamine), otherwise it will cause a sharp increase in the blood concentration of ramelteon, which is extremely dangerous.