Moxonidine Hydrochloride Tablets

Moxonidine is a new type of central antihypertensive drug. It is a selective agonist with high affinity for imidazoline I1 receptors. Depending on the species, tissue and ligand used, the selectivity of this product for imidazoline I1 receptors can be as high as 600 times that for alpha;2 adrenergic receptors. In vivo binding to central imidazoline I1 receptors is significantly related to the degree of blood pressure reduction. In animal experiments, pretreatment with an alpha;2 adrenergic receptor antagonist with affinity for imidazoline receptor sites can offset the blood pressure drop caused by this product. In vitro, this product is a selective agonist of alpha;2 adrenergic receptors, which is 288 times stronger than binding to alpha;1 adrenergic receptors. The antihypertensive effect of this product has no obvious relationship with alpha;2 adrenergic receptor binding. Mouse pharmacology experiments show that this product can reduce the number of spontaneous activities, cooperate with pentobarbital to promote sleep in mice, and inhibit central nervous system activity; it slows down the heart rate while lowering blood pressure, but has no obvious effect on ECG and respiratory rate and depth. Toxicity experiments on rats showed that as the dosage increased, general drug reactions such as loose hair, less activity and slow weight gain appeared; abnormal urine test; elevated liver enzymes; and pathological histological abnormalities were mainly seen in the kidneys and heart. Most abnormal indicators recovered after four weeks of drug withdrawal. Toxicity experiments on mice showed that the LD50 (median lethal dose) for a single oral gavage was 190 mg/kg; the LD50 for a single intravenous injection was 37 mg/kg; histological examination of dead mice revealed that all of the organs except the left heart were damaged.

The main ingredient of this product is moxonidine hydrochloride. 4-Chloro-N-(4,5-dihydro-1-hydro-imidazolyl-2)-6-methoxy-2-methyl-5-aminopyrimidine hydrochloride monohydrate

This product is a film-coated tablet, which appears white after removing the film coating.

Mild to moderate essential hypertension.

This product should be used on an individualized basis. Generally, start with the lowest dose, which is 0.2 mg, once a day, in the morning. If the desired effect cannot be achieved, the dose can be adjusted to 0.4 mg per day within three weeks, taken in the morning or 0.2 mg each in the morning and evening. The single dose should not exceed 0.4 mg or the daily dose should not exceed 0.6 mg. For patients with mild or moderate renal insufficiency, the single dose should not exceed 0.2 mg or the daily dose should not exceed 0.4 mg.

At the beginning of treatment, symptoms such as dry mouth, fatigue and headache may occur; dizziness, insomnia and lower limb weakness may occur occasionally. Gastrointestinal discomfort is rare, and some may have skin allergic reactions.

1. Sick sinus syndrome. 2. II and III degree sinoatrial or atrioventricular block. 3. Bradycardia, pulse rate below 50 beats per minute at rest. 4. Severe arrhythmia. 5. Severe heart failure. 6. Unstable angina. 7. Severe liver disease. 8. Patients with moderate or severe renal failure (glomerular filtration rate below 30 ml/min). 9. Angioedema. 10. Intermittent claudication, Raynaud's syndrome, Parkinson's syndrome, epilepsy, glaucoma, etc.

Precautions for children: Children under 16 years old are prohibited. Precautions for pregnancy and lactation: Precautions for pregnant and lactating women are prohibited. Precautions for the elderly: Elderly patients should use it with caution and the initial dose should be small because their sensitivity to the drug is sometimes difficult to estimate.

1. When used in combination with beta-blockers, blood pressure is lowered at the beginning, and then a strong rebound phenomenon occurs. 2. When used in combination with other antihypertensive drugs, the antihypertensive effect of this product can be enhanced. 3. When used in combination with benzyl oxadiazine, the antihypertensive effect of this product can be weakened. 4. When used in combination with alcohol, sedatives or anesthetics, its antihypertensive effect can be enhanced.

Keep in a light-proof and airtight container.

0.2mg

24 months

Changchun Haiwang Biological Pharmaceutical Co., Ltd.

• Founded in:

  1995-01-25

• Address:

  No. 833, Huoju Road, Qianjin Street, High-tech Development Zone, Changchun City, Jilin Province;

• Tax NO.:

  91220101243880532N

• Registered Funds:

  20 million yuan

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