Top 9 Uses and Precautions when using Keikai

1. What is Keikai?

Information about Keikai:

• Keikai serves to assist and promote quality sleep in individuals dealing with insomnia through the effectiveness of the Melatonin compound.
• Melatonin, a hormone produced from the pineal gland with the amino acid tryptophan, increases the concentrations of gamma-aminobutyric acid and serotonin in the central and subdorsal regions of the brain. It also enhances the activity of pyridoxine kinase, an enzyme related to the synthesis of aminobutyric acid, dopamine, and serotonin. Physiologically, melatonin secretion peaks post-dusk, reaching its zenith between 2 - 4 AM, diminishing with the onset of daylight. The product is linked to circadian rhythm control, light-dark cycles, sleep-inducing effects, and increased sleep tendencies. The product is non-addictive and functions to regulate natural sleep, biological rhythms, and enhance sleep quality.
• Upon entering the body, Keikai is fully absorbed from the gastrointestinal mucosa in adults, potentially reduced by 50% in the elderly. Its biological availability is approximately 15%. First-pass metabolism is significant (around 85%). Peak concentration appears after 3 hours. Food slows absorption and reduces peak concentration (Cmax). Serum protein binding rate is about 60%, primarily binding to albumin, alpha1-glycoprotein, and high-density lipoproteins. Melatonin undergoes hepatic metabolism. The primary metabolite, 6-sulphatoxy-melatonin (6-S-MT), is inactive. Complete excretion occurs within approximately 12 hours after product ingestion.

Thông tin về sản phẩm Keikai:

• Keikai công dụng trong việc hỗ trợ, giúp ngủ ngon ở người mắc chứng mất ngủ nhờ hiệu quả từ dược chất Melatonin.
• Melatonin là một hormon được sản xuất từ tuyến tùng nhờ các acid amin tryptophan. Các kết quả nghiên cứu chỉ ra rằng dược chất melatonin làm tăng nồng độ chất acid aminobutyric và serotonin ở trung não và ở vùng dưới đồi, đồng thời cũng gây tăng hoạt tính của pyridoxin-kinaz, enzym liên quan đến quá trình tổng hợp aminobutyric acid, chất dopamin và serotonin. Về sinh lý, có sự tăng tiết chất melatonin ngay sau hoàng hôn, đạt đỉnh vào khoảng 2 - 4 giờ sáng, giảm đi khi về sáng. Sản phẩm có liên quan đến kiểm soát nhịp ngày đêm, cũng có liên quan đến chu kỳ sáng - tối, tác dụng gây ngủ, tăng khuynh hướng ngủ. Sản phẩm không gây nghiện, có tác dụng điều hòa giấc ngủ tự nhiên, điều hòa nhịp sinh học, cải thiện chất lượng giấc ngủ.
• Sau khi vào cơ thể, sản phẩm Keikai được hấp thu hoàn toàn từ niêm mạc đường tiêu hóa ở người lớn, có thể giảm 50% ở người già. Khả dụng sinh học của sản phẩm khoảng 15%. Chuyển hóa sản phẩm lần đầu lớn (khoảng 85%). Nồng độ sản phẩm đạt đỉnh xuất hiện sau 3 giờ. Thức ăn làm chậm sự hấp thu và giảm nồng độ đỉnh Cmax của sản phẩm. Tỉ lệ gắn protein huyết tương khoảng 60%, chủ yếu sản phẩm gắn với albumin, các acid alpha 1-glycoprotein, các lipoprotein tỷ trọng cao. Melatonin chuyển hóa qua gan. Chất chuyển hóa chính 6-sulphat oxy-melatonin( viết tắt là 6-S-MT) không còn hoạt tính. Sản phẩm được bài tiết hoàn toàn trong khoảng 12 giờ sau khi uống sản phẩm.

2. Pharmacodynamic Characteristics

Pharmacokinetic Properties

• Absorption: The product is fully absorbed from the gastrointestinal tract in adults and may be reduced by approximately 50% in the elderly. Melatonin kinetics are linear within the dose range of 2 - 8 mg.
  Bioavailability is about 15%. First-pass metabolism is substantial (85%). Tmax occurs after 3 hours. Absorption rate and Cmax are influenced by food. Food slows absorption and decreases peak concentration (Cmax).
• Distribution: Serum protein binding is approximately 60% in vitro. Melatonin primarily binds to albumin, alpha1-glycoprotein, and high-density lipoprotein.
• Metabolism: Experimental data suggest that melatonin undergoes metabolism through the CYP1A1, CYP1A2, and CYP2C19 isoenzymes of hepatic cytochrome P450. The major metabolite is 6-sulphatoxy-melatonin (6-S-MT) with no activity. Metabolites are completely excreted within 12 hours after product ingestion.
• Elimination: The half-life of the product is 3.5 - 4 hours. Excretion occurs through urine as metabolites, with 89% as 6-hydroxymelatonin sulfate and glucuronide conjugates, and 2% as unchanged melatonin

• Melatonin is a hormone produced by the pineal gland from the amino acid tryptophan. Research findings indicate that melatonin increases the concentration of amino-butylic acid and serotonin in the midbrain and sub-dorsal region, while enhancing the activity of pyridoxine kinase, an enzyme associated with the synthesis of amino-butylic acid, dopamine, and serotonin. Physiologically, melatonin secretion rises after sunset, peaks between 2 - 4 am, and decreases towards morning. Melatonin is linked to circadian rhythm control and the light-dark cycle. It is also associated with sleep-inducing effects and promotes sleep tendencies.
• Melatonin regulates natural sleep patterns. Non-addictive, melatonin helps the body regulate its biological rhythm.
• The activity of melatonin on MT1, MT2, and MT3 receptors contributes to its sleep-inducing properties, as these receptors (mainly MT1 and MT2) regulate circadian rhythm and sleep cycles.
• Due to melatonin's role in sleep regulation, circadian rhythm, and age-related decline in endogenous melatonin production, it may be effective in improving sleep quality, especially in patients aged 55 and older with primary insomnia.

Administration:

Keikai product is taken orally, ideally, patients should consume the product after dinner, approximately 1 - 2 hours before bedtime.

Dosage:

The usual dose is one tablet per day.

Indications:

Keikai product is prescribed for short-term treatment of symptoms of primary insomnia in patients aged 55 and above.

Contraindications:

Avoid using Keikai product in patients with allergies or hypersensitivity to melatonin or any excipient.

Similar to other products, Keikai may interact with a variety of products, specifically as follows:

• Products inducing CYP3A at concentrations higher than therapeutic levels. The clinical relevance of this finding is currently unclear. The product does not induce CYP1A enzymes.
• The product primarily undergoes metabolism through intermediary CYP1A enzymes. Therefore, potential interactions may occur with other products that also affect CYP1A enzymes.
• Avoid combining the product with fluvoxamine, as fluvoxamine may increase the concentration of Keikai product by inhibiting the metabolism of melatonin by liver enzymes such as P450, CYP1A2.
• Exercise caution when combining the product with 5- or 8-methoxypsoralen, estrogen, cimetidine, as they may increase melatonin levels.
• Cigarette smoke may reduce the concentration of the product due to CYP1A2 induction.
• CYP1A2 inhibitors such as quinolone antibiotics may increase melatonin levels.
• CYP1A2 inducers such as carbamazepine and rifampicin antibiotics may decrease melatonin levels.
• Avoid simultaneous use of alcohol with melatonin, as it may reduce the efficacy of the treatment product.
• The product may enhance the sedative effects of both benzodiazepines and non-benzodiazepines such as zaleplon, zopiclone, zolpidem.

Unintended effects during the use of Keikai product include:

• Nervousness, headaches, insomnia, sore throat, dizziness, drowsiness, abdominal pain, dry mouth, constipation, back pain, muscle weakness, weight gain...
• If patients experience discomfort or any of the above unintended effects while using the product, they should inform their doctor.

Overdose:

• Symptoms: Overdose symptoms are often intensified manifestations of unintended effects. However, occasionally, more unusual and dangerous symptoms may also occur.
• Treatment: Do not be complacent; closely monitor the patient, anticipating rapid deterioration. Seek emergency medical attention upon observing any unusual signs to ensure patient safety.

Missed Dose:

Supplement the missed dose if within 1 – 2 hours of the scheduled product use. If the dose has been missed for an extended period, do not double the dose; take the correct dose afterward. Do not take more than two consecutive missed doses.

Caution When Using the Product:

• Exercise caution for patients using antidepressants or sedatives.
• Be cautious for patients with kidney disease, galactose intolerance, or LAPP lactase deficiency.
• For pregnant or breastfeeding women: Use the product with caution if considering it for pregnant or breastfeeding women. For an accurate decision, patients should consult with a doctor before deciding to use the product.
• For drivers, machine operators, heavy labor: Keikai product should not be used by drivers and machine operators as it affects mental function and concentration.
• During treatment, patients need to adhere to the instructions, not self-adjust the dosage for quick effectiveness.
• During treatment, patients should minimize the consumption of alcohol-containing foods or beverages and stimulants.

Keikai Product Interactions:

• Avoid combining this product with fluvoxamine, cimetidine, 5- or 8-methoxypsoralen, estrogen, quinolones, carbamazepine, rifampicin, zaleplon, zopiclone.
• While using this product, patients should refrain from alcohol, beer, and stimulant use.
• Therefore, during product use, limit the intake of alcoholic and carbonated beverages. Also, patients should list the products or dietary supplements they are using at this time so that the doctor can be aware and advise to avoid unwanted product interactions.

Note:

Do not use expired or visibly altered products, such as mold or color changes in the product. Keep the product out of the reach of children to prevent accidental ingestion during play.