Lipasudil Hydrochloride Eye Drops 0.4% 5mL×5 GLANATEC ophthalmic solution 0.4% GLANATEC ophthalmic solution

Granatech Eye Drops 0.4% is a sterile aqueous eye drop for glaucoma and ocular hypertension, suitable for patients who have insufficient response to other treatments or cannot use them. It promotes aqueous humor outflow by inhibiting Rho kinase to reduce intraocular pressure.

Basic information of medicine

1. Generic name : Ripasudil Hydrochloride Hydrate
2. English name : GLANATEC ophthalmic solution 0.4%
3. Product name : グラナテック eye drops 0.4%
4. Dosage form : eye drops (sterile water-based eye drops)
5. Indications :
   It is used for glaucoma and high eye pressure when other glaucoma treatments are ineffective or cannot be used.
6. Element :
   • Active ingredients: 1 mL contains 4.896 mg of ritrasulfonic acid hydride (equivalent to 4.0 mg of ritrasulfuric acid).
   • Additives: Anhydrous リン acid dihydrate Na, グリセリン, water acidified Na, concentrated ベンザルコニウム chloride solution 50.
7. Properties :
   • pH: 5.0-7.0;
   • Osmotic pressure ratio: about 1 (relative to physiological saline);
   • Appearance: Colorless to light yellow clear liquid.

Dosage

Taboo

Precautions

1. Special Populations

• Pregnant women : Use only if benefits clearly outweigh risks.
• Breastfeeding mothers : Weigh the benefits of treatment against the nutritional value of breast milk and consider whether to continue or stop breastfeeding (animal experiments have shown that drugs can enter breast milk).
• Children, etc .: No clinical trials using efficacy and safety as indicators have been conducted.
• Elderly people : No special mention, need to use the medicine with caution according to physical condition.

2. Medication Instructions

• When applying eye drops, avoid contact between the tip of the container and the eye to prevent contamination of the drug solution.
• After applying the drops to the eye, compress the tear sac for 1 to 5 minutes and close the eye.
• When using with other eye drops, wait at least 5 minutes between use.
• Those who wear soft contact lenses need to remove the lenses first and wait at least 5 minutes after eye drops before putting them back on.

3. Drug storage

• Storage method: Store at room temperature;
• Validity period: 3 years.

Adverse Reactions

1. Allergic reaction

• Unknown frequency: contact dermatitis, eyelid swelling, foggy vision.

2. Digestive system reactions

• Not mentioned (mainly eye reactions).

Other eye reactions

• More than 5% : conjunctival congestion (69.0%, mostly transient when applied to the eye), conjunctivitis (including allergic), blepharitis (including allergic), and eye irritation.
• 0.1-5% or less : corneal epithelial disorders (corneal abrasions, punctate keratitis, etc.), itching, eye abnormalities, eye fat, eye pain, conjunctival filter cells, and increased intraocular pressure.

Drug interactions

1. Contraindications for concurrent use

2. Precautions for concurrent use

Pharmacological Action

1. Rho kinase inhibitory effect : selectively inhibits human ROCK-1 and ROCK-2, promoting aqueous humor outflow.
2. Improve aqueous humor outflow : Increase the aqueous humor outflow rate through the vascular column-Shulem tube pathway without affecting the amount of aqueous humor produced.
3. Intraocular pressure lowering effect : Animal experiments show a concentration-dependent intraocular pressure lowering effect.

Pharmacokinetics

1. absorb :
   • After repeated eye drops in healthy adults, the plasma concentration of the drug quickly reaches a peak (tmax is about 0.083 to 0.5 hours) and migrates rapidly through the systemic circulation.
   • After a single eye drop in rabbits, the drug concentration in the cornea and aqueous humor reached its peak at 0.25 hours, and in the lens at 0.5 hours.
2. excretion :
   • After a single eye drop, the excretion rate in urine is: 1.34% of the drug and about 48.68% of the metabolite M1, mainly excreted within 12 hours.

Clinical Research

1. Validity :
   • When used alone or in combination with latanoprost or timolol, it significantly reduces intraocular pressure, and the effect is stable with long-term (52 weeks) use.
2. Security :
   • The main side effect is conjunctival congestion (up to 73.6% when used alone), followed by eye irritation, corneal epithelial disorders, etc., most of which are mild and reversible.

Packing Specifications

Production information

Manufacturer : Kowa Co., Ltd.