Is It Safe to Take an Antihistamine During Pregnancy?

The main ingredient of this product is zaleplon, and its chemical name is 3- [3-cyanopyrazole (1,5-a) pyrimidin-7] -N-ethylacetoaniline.
Molecular formula: C ₁₂ H ₁₅ N ₅ O
Molecular weight: 305.34

Baijiemin (Zaleplon Tablets), the indication is a short-term treatment for insomnia with difficulty falling asleep. Clinical research results show that Zaleplon can shorten the time to fall asleep, but it has not yet been shown to increase sleep time and reduce the number of arousal .

Drug Name: Bai Jiemin
Drug type: Prescription drugs, medicines for medical workers' injuries

Special medicine: Psychotropic drugs
Use classification: Other sedative hypnotics

Baijiemin ingredients

Baijiemin Traits

This product is a white tablet.

Baijiemin indication

It is suitable for short-term treatment of insomnia with difficulty falling asleep. The clinical research results show that zaleplon can shorten the time to fall asleep, but it has not been shown to increase the sleep time and reduce the number of arousal.

Baijiemin specifications

5mg

Baijiemin usage and dosage

Adults take 5 mg to 10 mg (1 to 2 tablets) orally once a day and take it before bedtime or when they have difficulty falling asleep. For lighter patients, the recommended dose is 5 mg (1 tablet) at a time. For elderly patients, diabetic patients and patients with mild to moderate liver dysfunction, the recommended dose is 5 mg (1 tablet) at a time. Take only once a night. The duration of continuous medication is limited to 7-10 days. If insomnia does not decrease after taking 7-10 days, the doctor should re-evaluate the cause of insomnia.

Baijiemin adverse reactions

After taking Zaleplon, you may experience mild headaches, drowsiness, dizziness, dry mouth, sweating and anorexia, abdominal pain, nausea and vomiting, fatigue, memory difficulties, dreaminess, depression, tremor, unstable standing, and recovery. Depending on other visual problems, insanity and other adverse reactions. Other adverse reactions include:
After taking zaleplon (10 or 20 mg), short-term memory loss will occur in about 1 hour, and the loss effect is stronger at the 20 mg dose, but there is no loss effect after 2 hours;
After taking zaleplon (10 or 20 mg), the sedative and mental disorders are expected for about 1 hour, but there is no such effect after 2 hours;
Rebound insomnia is dose-dependent. Clinical trials have shown that there is no or few rebound insomnia in the 5mg and 10mg groups on the first night after discontinuation, and some in the 20mg group, but it disappears the next night;
Occasional transient leukocyte elevation;
Occasionally, transient transaminase elevation.

Bai Jie Min Taboo

1. Those who are allergic to this product are prohibited.
2, severe liver and kidney dysfunction are disabled.
3. Patients with sleep apnea syndrome are disabled.
4, disabled patients with myasthenia gravis.
5, severe dyspnea or chest disease disabled.

Attention to Baijiemin

In order to ensure the safe and effective use of Zaleplon, it is necessary to pay attention to the following matters: 1. This product is a second class of psychotropic drugs specially managed by the state. It must strictly abide by the national regulations on psychotropic drugs and be used strictly under the guidance of a doctor.
2. Do not exceed the period of use specified by your doctor. Long-term use may cause dependence. Use with caution in patients with a history of drug abuse.
3. After taking Zaleplon, please contact your doctor if you notice any behavioral or mental disorders.
4. Tell your doctor about all the medicines you may take, including over-the-counter medications. If you drink alcohol, tell your doctor. It is forbidden to drink alcohol while taking zaleplon or other sleeping pills.
5. Do not take this product unless you can guarantee more than 4 hours of sleep time.
6. Do not increase the amount of Zaleplon without your doctor's instructions.
7. When taking Zaleplon or other sleeping pills for the first time, you should know that some of these drugs will still be used the next day. When you need to be conscious, such as driving a car, driving a machine, etc., you should use it with caution.
8. It may be difficult to fall asleep in the first or two nights after stopping taking the medicine.
9. If you are pregnant or about to become pregnant or breastfeeding, tell your doctor.
10. Do not share zaleplon with others. Keep medicines out of the reach of children.
11. If you have depression, tell your doctor that the doctor should give as little medicine as possible to the person with depression to prevent overdose.
12. Zaleplon has rapid onset of action and should be taken immediately before going to bed, or when it is difficult to fall asleep after going to bed.
13. In order for Zaleplon to work better, please do not apply this product immediately after using up a high-fat diet.
14. Because adverse reactions to zaleplon are dose-related, the lowest possible dose should be used, especially in the elderly.
15. When used in combination with drugs that act on the brain, the sequelae may be exacerbated by the synergistic effect, causing you to sleep in the morning. These drugs include: drugs used to treat mental illness (such as antipsychotics, hypnotics, anxiolytics, sedatives, antidepressants). Anesthetics and drugs used to treat allergies (such as sedative antihistamines).

Medicine for pregnant women and lactating women

The safety of taking this product during pregnancy has not been confirmed by data, and this product is metabolized into milk. Therefore, lactating mothers and women who are or will be pregnant should not use this product.

Baijiemin children medication

There is no data to confirm the safety of children taking this product, so children (less than 18 years old) are prohibited from using this product.

Baijiemin elderly medicine

This product can be used in the elderly, including those older than 75 years. The pharmacokinetics of this product is not significantly different in elderly and elderly women, including those older than 75 years, compared with healthy young volunteers. Because elderly patients are more sensitive to the effects of sleeping pills, the recommended dose is 5 mg.

Baijiemin Drug Interaction

And central nervous system drug ethanol: This product can enhance the damage to the central nervous system by ethanol, but does not affect the pharmacokinetics of ethanol.
Imipramine: After combining this product with imipramine, the level of awakening is reduced, and the ability of motor and mental action is impaired. The interaction is pharmacodynamics without pharmacokinetic changes.
Parrot: This product has no interaction with Parrot.
Thiolidazine: After this product and thiolidazine, the level of awakening is reduced, and the ability of motor and mental activity is impaired. The interaction is pharmacodynamics without pharmacokinetic changes.
With enzyme induction / inhibition drugs: combined with enzyme inducers such as rifampicin, will reduce the C _max and AUC of this product by 4 times.
The combination of diphenhydramine and diphenhydramine has no pharmacokinetic interaction, but due to the sedative effect of both, special attention should be paid to the combination.
Combination with drugs that affect renal elimination: No significant pharmacokinetic changes when combined with ibuprofen.

Baijiemin overdose

Studies of overdose of zaleplon have been few. In preclinical studies, it was noted that excessive medication has central nervous system inhibitory effects and mild symptoms include: lethargy, lethargy, and confusion. Severe symptoms include ataxia, hypotonia, hypotension, and sometimes coma until death.
Suggested treatment: Animal studies have shown that flumazenil antagonizes zaleplon, but has not yet been used clinically. Treat in accordance with the general principles of overdose management, and ensure support and symptomatic treatment.

Baijiemin Pharmacology and Toxicology

Pharmacological effects Zaleplon, as a hypnotic, has a chemical structure different from that of benzodiazepines, barbiturates, and other known hypnotic drugs, and may act by acting on -aminobutyric acid-benzodiazepine (GABA-BZ ) Receptor complex and exert its pharmacological effect.
Non-clinical studies have shown that zaleplon can selectively bind to the brain GABA _A receptor complex alpha subunit ₁ receptor. Zaleplon binding to purified GABA _A receptors (() 112 [-1]) and (() 212 [-1]) The experimental results show that it has low affinity to the above receptors and can preferentially bind to Omega-1 receptor.
Toxicology Reproductive toxicity In the reproductive toxicity test, rats were given zaleplon 100mg / kg / day (based on body surface area, approximately 49 times the recommended maximum human dose) before mating, which can cause animal death and Fertility decline. Later research continued to show that zaleplon mainly caused impaired fertility in female animals. The teratogenic sensitivities of pregnant rats and rabbits were orally given Zaleplon 100 and 50 mg / kg / day (based on body surface area, approximately 49 times and 48 times the maximum recommended human dose). Teratogenic effects. However, after oral administration of zaleplon to rats at 100 mg / kg / day, the fetuses were stunted before and after birth; this dose can also cause maternal toxicity, which can cause signs of toxicity and slow weight gain during administration. The dose that has no effect on the cyanosis of rat offspring is 10 mg / kg / day (based on body surface area, approximately 5 times the maximum recommended human dose). The cyanosis of rabbit embryos and fetuses was not affected at all doses. In the perinatal test, female rats were given zaleplon at 7 mg / kg / day during late pregnancy and lactation. The offspring gave birth and postnatal mortality increased, and growth and cyanosis slowed. No maternal toxicity was observed in animals at this dose. The non-influenced dose for cyanosis of the offspring is 1 mg / kg / day (based on body surface area, about 0.5 times the maximum recommended human dose). Studies have shown that exposure of the offspring to the drug in the womb and during lactation may cause adverse reactions in viability and cyanosis.
Genotoxicity Tests of chromosomal aberrations in Chinese hamster ovary cells in vitro show that zaleplon has a mutagenic effect regardless of the presence or absence of metabolic activators, which can cause aberrations in chromosome structure and number (polyploid and intranuclear re-replication). In the in vitro human lymphocyte test, chromosome number aberration was caused only under the conditions of its highest test concentration and metabolic activator. Zaleplon did not show mutagenicity in the in vitro Ames cell test and the Chinese hamster ovary HGPRT gene mutation test. In the mouse bone marrow micronucleus test and rat bone marrow chromosome aberration test, there is no dehiscence effect, and it does not cause DNA damage in rat liver extracellular DNA synthesis test.
Teratogenicity Carry on life-long carcinogenicity tests in rats and mice. Mice were orally given zaleplon 25, 50, 100, and 200 mg / kg / day for two consecutive years (based on body surface area, approximately 6-49 times the maximum recommended human dose). The liver of female rats in the high-dose group The incidence of cellular adenomas increased significantly. Rats were orally given zaleplon for 1, 2 or 10 mg / kg / day (converted by body surface area, approximately 0.5-10 times the maximum recommended human dose) for two consecutive years. No significant carcinogenicity was observed.

Baijiemin Pharmacokinetics

According to foreign literature reports, more than 500 healthy people (including young and old), breastfeeding women, and patients with liver or kidney disease were investigated for pharmacokinetics of zaleplon. In healthy subjects, a single pharmacokinetic study of 60 mg and 15 mg and 30 mg once a day was performed for 10 days. Zaleplon was quickly absorbed, reaching a peak concentration of about 1 hour, and cleared. The half-life (t _1/2 ) is about 1 hour. Zaleplon is administered once a day without drug accumulation, and its pharmacokinetics are proportional to the dose within the therapeutic range.
1. Absorption: After oral administration of zaleplon, the absorption is rapid and complete, reaching the peak plasma concentration in about 1 hour. Its absolute bioavailability is approximately 30%, with significant first-pass effects.
2. Distribution: Zaleplon is a lipophilic compound. After intravenous administration, the volume of distribution is about 1.4L / kg. The in vitro plasma protein binding rate is about 60% ± 15%, and it is not limited by the concentration range of 10 to 1000 ng / ml of Zaleplon, which indicates that Zaleplon is insensitive to changes in protein binding rate. Zaleplon The ratio between blood and plasma is about 1, which means that zaleplon is distributed uniformly throughout the blood and not widely in red blood cells.
3. Metabolism: After oral administration, zaleplon is extensively metabolized. In urine, only 1% of the dose is the original drug. Zaleplon is mainly converted to 5-oxydeoxy by aldehyde oxidase. Ethyl zaleplon, which is rarely metabolized by CYP3A4 to deethyl zaleplon, and is quickly converted by aldehyde oxidase to 5-oxodeethyl zaleplon. These metabolites are then converted by Converted to glucuronic acid compounds and eliminated in urine, all zalepromone metabolites have no pharmacological activity.
4. Excretion: Zaleplon is cleared quickly after oral or intravenous administration. The average t _{1/2 is} about 1 hour. Zaleplon oral plasma clearance is about 3L / h / kg. Intravenous plasma. The clearance rate is about 1 L / h / kg. If the liver blood is normal and nephron clearance is neglected, the liver extraction rate of zaleplon is estimated to be 0.7, indicating that the first-pass effect of zaleplon is very obvious.
After taking radiolabeled zaleplon, 70% can be recovered in urine within 48 hours (71% in 6 days), including all zaleplon metabolites and their glucuronic acid, and 17% can be recovered in feces, mainly 5-oxo-zaleprom.
5. Food effect: In healthy adults, high-fat and indigestible foods can prolong the absorption of zaleplon, the delay time is about 2 hours, and the C _{max is} reduced by about 35%. Zaleplon AUC and elimination There is no significant effect on half-life, which suggests that taking zaleplon immediately after consuming high-fat and indigestible foods will have an effect on the onset time.
The results of three studies of pharmacokinetics of zaleplon in the elderly showed that the pharmacokinetics of zaleplon did not differ significantly from those of young people.
Gender: There is no significant difference in the pharmacokinetics of zaleplon in men and women.
Ethnicity: The pharmacokinetics of zaleplon were studied with Japanese as the representative of Asians. For this group, C _max and AUC were increased by 37% and 64%, respectively. This may be related to different body weights, or it may be due to diet , Environmental or other factors cause different enzyme activities.
Liver injury: Zaleplon is metabolized by the liver first, followed by systemic metabolism. Its oral clearance is reduced by 70% and 87% in patients with compensatory and compensatory dysfunction. Compared with healthy people, the average C _max and AUC has been significantly reduced. Therefore, when taking zaleplon in patients with moderate or mild liver damage, the dose should be appropriately reduced. Zaleplon is not recommended for patients with severe liver damage.
Kidney injury: Because less than 1% of the original drug Zaleplon excreted by the kidney, there is no significant change in the pharmacokinetics of patients with renal insufficiency, so there is no need to adjust the dose for patients with moderate to mild kidney injury. But further research is needed for patients with severe kidney damage.

Baijiemin Storage

Sealed, protected from light, cool and dry place

Baijiemin Packaging

5mg / tablet × 14 tablets / box

Baijiemin validity period

Tentative two years

Baijiemin approval number

National Medicine Standard H20031297

Baijiemin Production Enterprise

Dalian Meiluo Pharmaceutical Factory