He Yue Desmopressin Tablets For central diabetes insipidus.

去氨加压素片

Generic name: desmopressin acetate tablets
Chinese Pinyin: Cusuan Quanjiayasu Pian
English name: Desmopressin Acetate Tablets
Product name: Heyue
Ingredients: The main ingredient of this product is desmopressin acetate.
Properties: This product is a white piece.
Indications: 1. This product is used to treat central diabetes insipidus. After taking this product, it can reduce urine excretion, increase urine osmotic pressure, reduce plasma osmotic pressure, thereby reducing frequent urination and nocturia.
2. This product is used to treat nocturnal enuresis in patients aged 6 years or older.
Specification: 0.1mg×30 tablets/box
Usage and dosage: The dosage varies from person to person and should be adjusted separately.
Treatment of Central Diabetes Insipidus: The appropriate initial dose for adults and children is 0.1 mg each time, three times a day. Then adjust the dose according to the patient's efficacy. According to clinical experience, the total daily amount is between 0.2-1.2 mg. The appropriate dose for most patients is 0.1-0.2 mg three times a day.
Treatment of nocturnal enuresis: The initial appropriate dose is 0.2 mg before going to bed, if the effect is not significant, it can be increased to 0.4 mg. After three months of continuous use, the drug should be discontinued for at least one week in order to assess the need for continued treatment. Drinking water should be restricted during treatment, see "Precautions" for details.
Adverse reactions: Unrestricted drinking water when using desmopressin acetate may cause water retention/hyponatremia, with/without the following signs and symptoms (headache, nausea/vomiting, decreased serum sodium, weight gain, more serious) Those can cause convulsions).
In the treatment of nocturnal enuresis and diabetes insipidus, common adverse reactions include headache, abdominal pain and nausea; rare skin allergic reactions, hyponatremia and mood disorders; only a few reports of systemic allergic reactions.
Contraindications: Desmopressin acetate should not be used in the following situations:
—Patients with habitual or mental polydipsia (urine volume exceeding 40 ml/kg/24 hours);
—Patients with cardiac insufficiency or other diseases who need to take diuretics;
—Patients with moderate to severe renal insufficiency (creatinine clearance rate is less than 50 ml/min);
-Patients with syndrome of abnormal secretion of antidiuretic hormone (SIADH);
-Patients with hyponatremia;
-Those who are allergic to desmopressin acetate or other ingredients of the drug.
Note: Urgent urinary incontinence patients: patients with frequent urination or polyuria caused by organ diseases (such as benign prostatic hyperplasia, urinary tract infection, bladder stones/bladder cancer); patients with polydipsia and diabetes are not suitable for treatment with this product.
When desmopressin acetate tablets are used to treat nocturnal enuresis, drinking water should be restricted 1 hour before and 8 hours after taking the drug. If drinking water is not strictly controlled during treatment, water retention and/or hyponatremia and its complications (headache, nausea/vomiting, weight gain, and more severe cases can cause convulsions) will occur. At this time, treatment should be terminated until the patient has fully recovered.
The elderly, patients with low blood sodium levels and high 24-hour urine output (more than 2.8 to 3.0 liters) are at higher risk of hyponatremia.
In the following cases, drinking water should be strictly controlled and the patient's blood sodium level should be monitored:
-When combined with drugs known to cause abnormal antidiuretic hormone secretion syndrome (SIADH) (such as tricyclic antidepressants, selective serotonin reuptake inhibitors, chlorpromazine, carbamazepine),
-When combined with non-steroidal anti-inflammatory drugs (NSAIDs).
During treatment, when acute complications of fluid and/or electrolyte imbalance (such as systemic infection, fever, and gastroenteritis) occur, treatment should be stopped immediately.
Drug interactions: In order to avoid hyponatremia, in the following cases, drinking water should be strictly controlled and the patient's blood sodium level should be monitored:
-When combined with drugs known to cause abnormal antidiuretic hormone secretion syndrome (SIADH) (such as tricyclic antidepressants, selective serotonin reuptake inhibitors, chlorpromazine, carbamazepine), this type of Drugs can enhance the antidiuretic effect and increase the risk of fluid retention;
-When combined with non-steroidal anti-inflammatory drugs (NSAIDs), these drugs may cause water retention/hyponatremia.
Co-administration of loperamide will cause the plasma concentration of desmopressin acetate to increase three-fold, which will increase the risk of water retention/hyponatremia. Although it has not been proven, it may also have this effect when combined with other drugs that slow down bowel movement.
Combination of simethicone may reduce the absorption of desmopressin acetate.
In vitro studies of human microsomes have confirmed that desmopressin acetate is not metabolized in the liver. Therefore, the possibility of interaction between desmopressin acetate and drugs that affect liver metabolism is unlikely. However, no formal in vivo drug interaction studies have been conducted.
The bioavailability of desmopressin acetate varies moderately to highly within and between individuals. Eating a standard meal with a fat intake of 27% at the same time or 1.5 hours earlier than the medication will reduce the absorption rate of desmopressin acetate by 40%. No effect of food on the pharmacodynamics (urine volume or osmotic pressure) of desmopressin acetate was observed. However, it is not ruled out that some patients may affect the effect of the drug when eating at the same time.
Pharmacology and Toxicology: This medicine contains desmopressin acetate, which is similar in structure to the natural hormone arginine vasopressin. The main difference between it and arginine vasopressin is the deamination of 1-cysteine ​​and the substitution of 8-D-arginine for 8-L-arginine. After these structural changes, the clinical dose of desmopressin acetate has a longer action time without the side effects of compression.
toxicity
If you drink a lot of water, even normal doses can cause water poisoning. The dose ranges from 0.3 μg/kg (intravenous administration) to 2.4 μg/kg (intranasal administration), which has caused hyponatremia and convulsions in adults and children; on the other hand, nasal administration in infants of 5 months 40 micrograms or 80 micrograms administered to a 5-year-old child through the nasal cavity had no effect. The newborn infant was given 4 micrograms parenterally, and symptoms of oliguria and weight gain appeared.
Preclinical safety data
No abnormal findings were found in the safety monitoring process and safety summary of desmopressin acetate.
Pharmacokinetics: The bioavailability of oral desmopressin acetate is between 0.08 and 0.16%. The peak plasma concentration appears about 1 to 1.5 hours later; the peak plasma concentration (Cmax) and the area under the plasma concentration-time curve (AUC value) do not increase in proportion to the dose. The volume of distribution is 0.2 to 0.3 liters/kg. Desmopressin acetate cannot penetrate the blood-brain barrier. The average elimination half-life is 2 to 3 hours.
In vitro studies on human liver microsomes show that desmopressin acetate is almost not metabolized in the liver. Therefore, desmopressin acetate may not be metabolized in the human liver.
Within 24 hours after intravenous injection, desmopressin acetate detected in urine was 45% of the dose.
Medication for pregnant women and lactating women: pregnant women
Limited data (a study of 53 pregnant women with diabetes insipidus) confirms that desmopressin acetate has no effect on the health of pregnant women and fetuses/newborns. There are still no other relevant epidemiological data. Research on laboratory animals cannot prove that the drug has direct or indirect effects on pregnant women, embryo/fetal formation, childbirth and postpartum stages. Therefore, pregnant women should use it with caution.
Breastfeeding women
After nasal administration of high-dose desmopressin acetate (300 micrograms), the breast milk test showed that desmopressin acetate can be secreted into the milk, but the baby absorbs very little from the milk and is lower than the amount needed to affect the diuretic effect the amount. It is not clear whether desmopressin acetate accumulates in breast milk after repeated administration.
Child medication: Desmopressin acetate tablets should be used with caution in young patients.
Medication for elderly patients: Clinical trial studies have shown that elderly patients over 65 years of age are more likely to develop hyponatremia. Therefore, it is not recommended to use this product for elderly people over 65 years of age at the beginning of treatment, especially in situations that may cause fluid or electrolyte imbalance. Patients who need to check their serum sodium levels before starting treatment, 3 days after starting the medication or increasing the dose, and when the treating physician considers it necessary to take the medication, may consider using this product.
Overdose: Excessive use increases the risk of water retention and hyponatremia.
Treatment: The treatment of hyponatremia should depend on the situation. The following suggestions can be used:
For asymptomatic patients with hyponatremia, in addition to discontinuing desmopressin acetate, drinking water should be restricted; for symptomatic patients, infusion of isotonic or hypertonic sodium chloride solution should be added; when the symptoms of body fluid retention In severe cases (convulsions or unconsciousness), furosemide is added.
Symptoms: headache, nausea, water retention, hyponatremia, oliguria, convulsions and pulmonary edema.
Storage: sealed, protected from light, and stored in a dry place below 25℃.
Packaging: Aluminum foil packaging. 10 pieces/board, 3 boards per box.
Validity period: 24 months
Executive standard: Standard YBH04082010 of the State Food and Drug Administration
Approval number: National Medicine Zhunzi H20103402
Company Name: Hainan Zhonghe Pharmaceutical Co., Ltd.
Company Address: Bonded Zone, No. 168, Nanhai Avenue, Haikou City, Hainan Province