Levobunolol hydrochloride eye drops
Function and Efficacy
1. This product should be used with caution in patients with known contraindications to systemic beta-adrenergic blockers, including abnormal bradycardia and atrioventricular block of degree I or above. Congenital heart failure 1 Levobunolol is a non-selective beta-adrenergic receptor blocker that blocks both beta-1 and beta-2 receptors. Levobunolol's receptor blocking effect is 60 times stronger than its dextrorotatory isomer, but the direct myocardial depressant effect is the same, so the levorotatory isomer-levobunolol is used. Levobunolol has no obvious local anesthetic effect and intrinsic sympathomimetic effect. 2 This product is levobunolol hydrochloride eye drops, which has an intraocular pressure-lowering effect on patients with high and normal intraocular pressure. The intraocular pressure-lowering effect is the same as timolol, and the maximum intraocular pressure-lowering amplitude is 7mmHg. 3 The drug effect of this product can be detected within one hour after taking drops, and the effect reaches a peak in 2 to 6 hours. The drug effect can be maintained for 24 hours after a single dose. The long duration of pharmacological action is the biggest advantage of this product. Its mechanism is that the plasma half-life of the main drug levobunolol is relatively long, which is 6 hours, while its main metabolite dihydrobutyralone has the same intraocular pressure-lowering effect as the main drug, and its half-life is longer, reaching 7 hours. 4 The intraocular pressure-lowering mechanism of this product is mainly to reduce the production of aqueous humor. This product has no effect on the outflow of aqueous humor through the uveal sclera, the ease of aqueous humor outflow, and the venous pressure on the sclera. Non-clinical toxicology study: Carcinogenicity: Animal experiments show that long-term and large-scale oral administration of levobunolol hydrochloride can significantly increase the incidence of benign leiomyoma in female mice and benign liver tumors in male rats. Mutagenicity: In vivo and in vitro animal experiments did not show that levobunolol hydrochloride has mutagenic activity. Reproductive toxicity: Animal experiments show that large doses of oral levobunolol hydrochloride have no effect on the reproductive function of male and female mice.
Ingredients
Levobunolol Hydrochloride
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| Levobunolol hydrochlorideIngredients |
A non-selective beta-adrenal receptor blocker that blocks both beta-1 and beta-2 receptors. It has no obvious local anesthetic effect and intrinsic sympathomimetic effect. It reduces intraocular pressure by reducing the production of aqueous humor. It has an intraocular pressure-lowering effect on patients with high and normal intraocular pressure, with a maximum intraocular pressure-lowering amplitude of 7 mmHg. The pharmacological effect lasts for a long time and can last for 24 hours after a single dose. More |
27912-14-7 | 6 |
Appearance
This product is a colorless clear solution.
Indication
It has a good effect of reducing intraocular pressure in primary open-angle glaucoma. For some secondary glaucoma, ocular hypertension, closed-angle glaucoma that is not completely controlled after surgery, and other glaucoma that is ineffective with other drugs and surgery, the addition of this product to the eye drops can further enhance the effect of reducing intraocular pressure.
Usage and Dosage
Eye drops, 1 drop at a time, 1-2 times a day. Drop into the conjunctival sac, and press the inner corner of the lacrimal sac with your fingers for 3-5 minutes after dropping.
Adverse Reactions
One-third of patients experienced temporary eye burning and eye stinging. 5% of patients experienced conjunctivitis. Some patients experienced slow heart rate and decreased blood pressure. 1Other rare eye adverse reactions include: changes in heart rhythm, dyspnea, iridocyclitis, headache, dizziness, transient ataxia, drowsiness, itching and urticaria. 2The following very rare adverse reactions may also occur with this product: (1) Systemic symptoms: weakness, chest pain. (2) Cardiovascular system: bradycardia, arrhythmia, hypotension, syncope, heart block, cerebrovascular accident, cerebral ischemia, heart failure, angina pectoris, palpitations, cardiac arrest. (3) Digestive system: nausea, diarrhea. (4) Nervous system: depression, mental confusion, aggravation of myasthenia gravis symptoms, paresthesia. (5) Skin: allergic reactions, including local and systemic rashes, alopecia, Steven-Johnson syndrome. (6) Respiratory system: bronchospasm, respiratory failure, dyspnea, nasal congestion. (7) Endocrine system: masking hypoglycemia symptoms in diabetic patients after taking insulin or hypoglycemic drugs. (8) Urogenital system: impotence.
Precautions
1. Patients with bronchial asthma or a history of bronchial asthma, severe chronic obstructive pulmonary disease. 2. Sinus bradycardia, Ⅱ or Ⅲ degree atrioventricular block, obvious heart failure, cardiogenic shock. 3. Patients who are allergic to this product.
Special Population Medication
Precautions for children: The safety and effectiveness of pediatric use have not been established. Precautions for pregnancy and lactation: It is not clear whether it is secreted through breast milk. It is known that systemic β-blockers and topical timolol can be secreted through breast milk, so lactating women should be careful when using this product. There are no adaptations and good controlled studies for pregnant women. Levobunolol should only be considered when its possible beneficial effects outweigh its possible side effects on the fetus. Precautions for the elderly: It is not clear yet.
Drug Interactions
1. When used in combination with adrenaline, it can cause pupil dilation. 2. Patients who are taking catecholamine-depleting drugs (such as reserpine) should be closely observed when using this product, because it can cause hypotension and significant bradycardia, the latter of which can cause dizziness, syncope or orthostatic hypotension. 3. It is not recommended to use two local beta-receptor blockers at the same time. 4. This product should be used with caution in combination with calcium channel antagonists, because it can cause atrioventricular conduction block, left ventricular failure and hypotension. For patients with impaired cardiac function, the two drugs should be avoided in combination. 5. This product can further prolong atrioventricular conduction time when used in combination with digitalis and calcium channel antagonists. 6. Phenothiazines can increase the antihypertensive effect of beta-receptor blockers because they can inhibit each other's metabolic pathways.
Storage
Store at 15-25°C away from light.
Packaging Specification
5ml:25mg
Validity Period
24 months