What Are the Different Types of Eye Drops for Children?
Latanoprost eye drops are indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma and ocular hypertension.
- Drug Name
- Latanoprost eye drops
- Drug type
- Prescription drugs, topical drugs, medical insurance workers' injuries
- Use classification
- Other ophthalmic drugs
- Latanoprost eye drops are indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma and ocular hypertension.
Latanoprost eye drops ingredients
- Main ingredients and chemical names: Latanoprost, (Z) -7-[(1R, 2R, 3R, 5S) 3,5-dihydroxy-2-[(3R) -3-hydroxy-5-phenyl I-pentyl] cyclopentyl] -5-heptenoic acid isopropyl.
Its structural formula:
Molecular formula: C 26 H 40 O 5
Molecular weight; 432.58
Latanoprost eye drops properties
- This product is a colorless clear liquid.
Latanoprost Eye Drops Indications
- Reduces elevated intraocular pressure in patients with open-angle glaucoma and ocular hypertension.
Latanoprost eye drops specifications
- 1ml: 50g
2.5ml: 125g
Latanoprost eye drops usage dosage
- Recommended dosage for adults (including elderly):
One drop at a time, once a day, onto the affected eye. Use it best at night.
This product should not be used more than once a day, because the increase in the number of medications will weaken the effect of reducing intraocular pressure.
If you forget to take the medicine, you should still use it as usual in the next medicine.
As with other eye drops, the lacrimal sac at the inner corner of the eye should be pressed for 1 minute immediately after each eye drop to reduce systemic absorption (occlusion of the punctum).
The use of two or more prostaglandins and prostaglandin analogs (including latanoprost) is not recommended. It has been reported that the use of such drugs more than once a day may reduce the ocular lowering effect of latanoprost, causing abnormal intraocular pressure.
Contact lenses (contact lenses) should be removed before using this product, and it can be re- worn after 15 minutes of use.
If other ophthalmic drugs are needed, they should be taken at least 5 minutes apart.
As with other eye drops, the lacrimal sac at the corner of the eye should be pressed for 1 minute after each eye drop to reduce systemic absorption (occlusion of the punctum).
Children: See [Children's Medication].
Latanoprost eye drops adverse reactions
- Most of the adverse events observed were in the eye. In a 5-year open-label latanoprost safety study, 33% of patients developed iris pigmentation (see [Precautions]). Other ocular adverse events are generally transient and occur only with medication.
According to the frequency of occurrence, adverse events can be divided into: very common (1 / 10), common (1 / 100 and <1/10), rare (1 / 1000 and <1/100), and rare (1 / 10,000 and <1/1000), very rare (<1 / 10,000). Unknown (cannot be estimated from existing data).
Infections and Infestations <br Unknown: Herpes keratitis<br /> Eye eyes [u] are common [/ u]: iris pigmentation, mild to moderate conjunctival congestion, eye irritation (burning, gritty , Pruritus, tingling, and foreign body sensation), changes in eyelashes and hairs (longer, thicker, pigmented, increased number of eyelashes) (mostly Japanese patients).
[u] Common [/ u]: temporary spotted epithelial erosion (mostly asymptomatic), blepharitis, eye pain, photophobia.
[u] Uncommon [/ u]: Eyelid edema, dry eyes, keratitis, blurred vision, conjunctivitis.
[u] rare [/ u]: iritis / uveitis (many patients have concomitant incentives), macular edema, symptomatic corneal edema and erosion, periorbital edema, inverted eyelashes sometimes cause eye irritation, Double-row eyelashes (double-row eyelashes) at the gland opening.
[u] Unknown [/ u]: Changes in the iris cysts, periorbital, and eyelids cause the eyelid grooves to deepen.
Nervous system < br Unknown: headache, dizziness.
Heart < br Very rare: aggravates angina in patients with heart disease.
Unknown: palpitations.
Breathing, chest and mediastinum < br Rare: asthma, exacerbation of asthma, and difficulty breathing.
Skin and subcutaneous tissues < br Rare: skin rash.
Rare: local skin reaction to the eyelid, darkening of the eyelid skin.
Unknown: toxic epidermal necrolysis.
Skeletal muscle and connective tissue < br brUnknown: myalgia, joint pain.
Whole body and site of administration <br /> is very rare: chest pain.
Children < br Two short-term clinical trials in pediatric patients (12 weeks, a total of 93 patients, 25 and 68 subjects, respectively) showed that children are similar to adults in safety and there are no new adverse effects event. Safety was similar across subgroups of children of different ages. Compared with adults, the more frequent adverse events in children are nasopharyngitis and fever.
Latanoprost Eye Drops Contraindications
- People who are allergic to any of the ingredients in this eye drop.
Latanoprost eye drops precautions
- This product may increase the amount of brown pigment in the iris and gradually cause eye color changes. Patients should be informed of the possibility of eye color changes before deciding on treatment. Unilateral treatment can lead to permanent eye asymmetry.
Eye color changes are mainly observed in patients with mixed iris colors, such as blue-brown, gray-brown, green-brown, and yellow-brown mixed colors. Color changes usually begin within the first 8 months of treatment, but a few patients can also occur later. Based on evidence obtained from continuous photography, this effect can occur in 30% of patients in clinical studies with a treatment period of more than 4 years.
Most patients have slight changes in iris color that are usually not clinically observed. The incidence of color change in patients with mixed iris colors ranges from 7% to 85%, with the highest incidence of yellow-brown mixed colors.
No color change was observed in pure blue eyes, and very few patient color changes were observed in pure gray, green, or brown eyes.
The color change is due to an increase in melanin content in melanocytes at the base of the iris, but an increase in the number of non-melanocytes themselves. The typical feature is that the brown pigmentation around the pupil is distributed concentrically and peripherally, but the entire iris or part of the iris is darker brown. Once discontinued, the iris brown pigment will not deepen any further. So far in clinical studies, this change has not been accompanied by any symptoms or pathological changes.
The treatment does not affect the moles or spots of the iris. Pigment accumulation in the trabecular meshwork or other parts of the anterior chamber has not been observed in clinical studies. The acquired long-term medication experience of more than 5 years shows that iris pigmentation has no adverse clinical effects or effects, and patients with iris pigmentation can continue to use this product. However, patients should be checked regularly, depending on the clinical situation, if necessary, treatment with this product can be discontinued.
This product has limited experience in chronic angle-closure glaucoma, open-angle glaucoma with implanted intraocular lens, and pigmented glaucoma. This product has no experience in inflammatory and neovascular glaucoma and inflammatory eye diseases. This product has no effect or little effect on the pupil, but this product has no experience in acute attack of angle-closure glaucoma. Therefore, before gaining more experience, it is recommended to use this product with caution in the above situations.
The perioperative study data of this product for cataract surgery is limited, and it should be used with caution in such patients.
Patients with a history of herpetic keratitis should use this product with caution. For patients with herpes simplex keratitis during active inflammation and patients with a history of recurrent herpetic keratitis, this product should be avoided, especially in combination with other prostaglandin analogs.
Existing cases of macular edema in patients who have no lens, intraocular lens with posterior capsular bag tear or implanted anterior chamber intraocular lens, or patients with known risk factors for macular cystic edema (such as diabetic retinopathy and retinal vein occlusion) Report (see [Adverse Reactions]).
Therefore, this product should be used with caution in patients without lens, intraocular lens with posterior capsule tear or implantable anterior chamber intraocular lens, or patients with known risk factors for macular cystic edema.
This product can be used in patients with known risk factors for iritis / uveitis, but caution should be used.
Asthma patients have limited experience with this product. There are currently some reports of exacerbation of asthma and / or dyspnea after using this product. Therefore, these patients should be used with caution until sufficient experience is obtained (see [Adverse Reactions]).
Periorbital skin color changes were observed, most of which were reported by the Japanese population. Current experience shows that the changes in the color of the periorbital skin are not permanent, and some patients continue to use this product to disappear after the treatment.
Latanoprost may gradually change the eyelids and hairs of the treated eye and the surrounding area. These changes include lengthening, thickening, deepening, increased number of eyelashes or body hair, and inverted eyelashes. Changes in eyelashes are reversible after discontinuation.
This product contains benzalkonium chloride, which is used as a preservative in eye drops. It has been reported that benzalkonium chloride can cause punctate keratopathy and / or toxic ulcerative keratopathy, which may cause eye irritation and discolor contact lenses. Dry eye patients or patients with low corneal immune function need to pay close attention when long-term or frequent use of this product. Contact lenses may absorb benzalkonium chloride, so it should be removed before using this product, and it can be worn after 15 minutes of use (see [Dosage and Administration]).
Impact on the ability to drive and operate machines <br /> This product has a slight or moderate impact on the ability to drive and operate machines.
Similar to other ophthalmic medications, infusions may cause transient blurred vision. Patients are advised to drive and operate the machine after the symptoms have disappeared.
Latanoprost eye drops for pregnant and lactating women
- Fertility:
Latanoprost has not been found to affect fertility in male and female animals in animal studies. (See [Pharmacology and Toxicology])
Pregnant women:
The effect of this product on human pregnancy safety has not yet been established, but it may have potential pharmacological effects on the pregnancy, fetus and newborn, so pregnant women should not use this product.
Lactation:
Latanoprost and its metabolites may enter breast milk, so lactating women should not use this product or stop breastfeeding.
Latanoprost eye drops for children
- The safety and effectiveness of pediatric medications have not been established. This product is not recommended for children.
Latanoprost eye drops for elderly
- See [Dosage and Administration].
Latanoprost eye drops drug interactions
- still uncertain.
Elevated intraocular pressure has been reported with the simultaneous use of two prostaglandin analog eye drops. Therefore, it is not recommended to use two or more prostaglandins, prostaglandin analogs, or prostaglandin derivatives at the same time.
Latanoprost eye drops overdose
- Excessive eye drops of this product, in addition to eye irritation and conjunctival congestion, no other eye side effects have been found.
If you accidentally ingest this product, please pay attention to the following information: Each bottle of eye drops contains 125 micrograms of latanoprost, and more than 90% of latanoprost is metabolized when it first passes through the liver. Healthy volunteers injected latanoprost 3 g / kg intravenously without any symptoms, but 5.5-10 g / kg can cause nausea, abdominal pain, dizziness, fatigue, hot flushes and sweating. Intravenous infusion of latanoprost in monkeys up to 500 g / kg also had no significant cardiovascular system effect.
Intravenous administration of latanoprost in monkeys can cause transient bronchoconstriction. However, patients with moderate bronchial asthma did not have bronchoconstriction caused by latanoprost when the dose of this product was 7 times the clinical dose.
If an overdose occurs, treat it symptomatically.
Latanoprost eye drops pharmacology and toxicology
- Pharmacological effects:
The active ingredient latanoprost is an analog of prostaglandin F 2 , which is a selective prostaglandin FP receptor agonist, which can reduce intraocular pressure by increasing aqueous humor outflow. In humans, the reduction of intraocular pressure begins approximately 3-4 hours after administration and reaches its maximum effect 8-12 hours. The effect of lowering intraocular pressure can be maintained for at least 24 hours. Studies in animals and humans have shown that the main mechanism of action of the drug is to increase the uveal scleral outflow of aqueous humor, although it has also been reported in humans to increase the convenience of aqueous humor (reduce drainage resistance).
Main clinical studies have proven that this product is effective as a single drug. Although no clear clinical studies of the combination have been conducted, a 3-month study showed that latanoprost was effective in combination with a -adrenergic blocker (timolol). Short-term studies (1 or 2 weeks) have shown that the combination of latanoprost with a dipivalyl epinephrine and an oral carbonic anhydrase inhibitor (acetazole 2 amine) has a combined effect of at least the effect Partial overlay.
Clinical studies have also shown that latanoprost has no significant effect on the production of aqueous humor and has no effect on the blood-water humor barrier.
At clinical doses and in studies in monkeys, latanoprost has no or negligible effect on blood circulation in the eye. However, mild to moderate conjunctival or scleral congestion may occur with topical application.
Monkeys undergoing extracapsular lens extraction have been using latanoprost for a long time and have been determined by fluorescent angiography to have no effect on retinal blood vessels.
Short-term treatment with latanoprost did not cause leakage of intraocular lens fluorescein.
The clinical therapeutic dose of latanoprost has not been found to have a significant pharmacological effect on the cardiovascular or respiratory system.
Toxicology research:
Eye and systemic toxicity studies of latanoprost were performed in several animals. In general, latanoprost is well tolerated and has a large safety margin. The clinical ophthalmic dose and systemic toxicity dose are at least 1000 times different. Unanesthetized monkeys received high-dose latanoprost intravenously (approximately 100 times the clinical dose / kg body weight) and observed an increase in respiratory rate, which may reflect transient bronchoconstriction. Latanoprost has no sensitizing properties in animal tests.
In rabbits and monkeys, no ocular toxicity was observed at a dose of 100 meg / eye / day of latanoprost (clinical dose of 1.5 meg / eye / day). But latanoprost causes increased iris pigmentation in monkeys.
The mechanism of pigment increase seems to stimulate melanin production in iris melanocytes, but no proliferative changes were observed. Iris pigmentation changes can be permanent.
In the long-term ocular toxicity study, the administration of latanoprost 6mcg / eye / day also caused enlarged palpebral fissure, which was reversible and occurred only at doses higher than the clinical dose. This effect has not been observed in humans.
Latanoprost was negative in bacterial mutation reversal tests, mouse lymphoma gene mutation tests, and mouse micronucleus tests. Chromosomal abnormalities were observed in an in vitro human lymphocyte test. Prostaglandin F 2 , a normally present prostaglandin, has also observed a similar effect, indicating that this effect is common to this class of substances.
Regarding the mutagenicity test, irregular DNA synthesis studies in vivo and in vitro were performed in rats, and the results were negative, indicating that latanoprost has no mutagenic effect. Carcinogenicity tests in mice and rats were also negative.
Animal tests have not found any effect of latanoprost on male and female fertility. In rat embryo toxicity studies, latanoprost was administered intravenously at doses of 5, 50, and 250 g / kg / day without any embryo toxicity. However, in rabbits, latanoprost doses of 5 g / kg / day or more can cause embryo death.
A dose of 5 g / kg / day (approximately 100 times the clinical dose) can cause significant embryonic fetal toxicity, manifested by increased incidence of late absorption and miscarriage and reduced fetal weight.
No teratogenic effects were found.
Pharmacokinetics of latanoprost eye drops
- Latanoprost (molecular weight 432.58) is an isopropylated prodrug and is inactive. It is biologically active when converted to latanoprost acid after hydrolysis. Prodrugs are well absorbed through the cornea, and all drugs that enter the aqueous humor have been hydrolyzed when they pass through the cornea.
Human studies have shown that the peak drug concentration in aqueous humor is reached approximately 2 hours after topical application. After topical application in monkeys, latanoprost was distributed in the anterior chamber, conjunctiva, and eyelids, and only a small amount of the drug reached the posterior chamber of the eye.
Latanoprost is hardly metabolized in the eye. Metabolism occurs mainly in the liver. The half-life in human plasma is 17 minutes. The main metabolites 1,2-dinorde and 1,2,3,4-tetrademetrol have no or only weak biological activity in animal tests and are mainly excreted from urine.
Latanoprost eye drops storage
- Refrigerate at 2-8 ° C before opening and save from light.
After opening, it can be stored at room temperature below 25 and used up within 4 weeks.
Latanoprost Eye Drops Packaging
- The eye drops are packed in polyethylene plastic bottles, plus a carton package, 2.5ml / bottle / box.
Validation of Latanoprost Eye Drops
- 36 months
Latanoprost Eye Drops
- Import drug registration standard JX19990382 [1]