Cosopt Combination Eye Drops 5mg 10pcs

Cosopt Dorzolamide/Timolol Combined Eye Drops is a compound ophthalmic drug used for intraocular pressure control. Its main ingredients are Dorzolamide (carbonic anhydrase inhibitor) and Timolol (non-selective beta-receptor blocker). It synergistically reduces intraocular pressure through a dual mechanism: Dorzolamide reduces aqueous humor production, and Timolol further inhibits aqueous humor secretion. It is suitable for patients with open-angle glaucoma and ocular hypertension, especially for those who need combined treatment because single drug control is not good.

1. Basic information of the drug

1. Common name: ドルゾラミド顩桩桩・チモロールマレイン acid chloride eye drops
2. English name: COSOPT ophthalmic solution; COSOPT Mini ophthalmic solution
3. Product Name: Kostudio Eye Drops with Combination; Kostudio with Eye Drops
4. Dosage form: Sterile aqueous eye drops
5. Indications: Used for glaucoma and ocular hypertension that are not sufficiently effective with other glaucoma treatment drugs
6. Element
   • コソプト Mixed Eye Drops: 1mL Contains 11.13 mg of dimethyl chloride (based on 10 mg of ドルゾラミド), 6.83 mg of チモロールマレイン acid chloride (based on 5 mg of チモロール) mg); the additives are tetrahydrofuran acid hydrate and tatonic acid dihydrochloride. Water and substances, ヒドロキシエチルセルロース, ポリソルベート80, pH Conditioner.
   • コソプトミニ Mixed Eye Drops: 1mL Contains ドルゾラミドララララ 11.13mg (calculated as ドルゾラミド 10mg), チモロールマレイン acid chloride 6.8 3 mg (5 mg based on チモロール); additives are クエン acid ナトリウム hydrate, ヒドロキシエチルセルロース, D - Manitoba, pH adjuster.
7. Characteristics
   • Cosop eye drops: pH 5.5-5.8, osmotic pressure ratio 0.4-0.5, colorless, clear, slightly viscous sterile aqueous eye drops.
   • Cosoptomin eye drops: pH 5.5-5.8, osmotic pressure ratio 0.95-1.25, colorless, clear, slightly viscous, sterile aqueous eye drops.

2. Usage and Dosage

3. Taboo

1. Patients with a history of allergy to the ingredients of this drug.
2. Patients with bronchial asthma or a history of it, patients with bronchospasm or severe chronic obstructive pulmonary disease (may precipitate or aggravate asthma attacks).
3. Patients with uncontrolled heart failure, sinus bradycardia, atrioventricular block (II or III degree), or cardiogenic shock (may aggravate these symptoms).
4. Patients with severe renal impairment.

IV. Precautions

1. Special Populations
   • Comorbidities/Past medical history: patients with right heart failure caused by pulmonary hypertension (may aggravate symptoms); patients with congestive heart failure (may aggravate symptoms); patients with diabetic ketoacidosis and metabolic acidosis (may enhance the inhibition of myocardial contractility by acidosis); patients with poorly controlled diabetes (need to pay attention to blood sugar, which may mask the symptoms of hypoglycemia); patients with a history of intraocular surgery (may increase the risk of corneal edema due to a decrease in the number of corneal endothelial cells); patients with acute angle-closure glaucoma (surgical treatment should be considered when using this product).
   • Patients with renal impairment: Contraindicated in patients with severe renal impairment (components may accumulate).
   • Patients with hepatic dysfunction: No clinical studies have been conducted in patients with hepatic dysfunction.
   • People of reproductive potential: be aware of the associated risks.
   • Pregnant women: Only give if the therapeutic benefits outweigh the risks (animal studies have shown possible effects).
   • Lactating women: The therapeutic benefits and nutritional benefits of breast milk should be considered comprehensively to decide whether to continue breastfeeding (trimerulone salt may enter human breast milk).
   • Children: No clinical studies have been conducted in children.
   • Elderly people: Physiological functions generally decline, so please pay attention.
2. Medication Instructions
   • When applying eye drops, be careful not to let the tip of the container touch the eyes directly to prevent contamination of the drug solution.
   • After opening the affected eye, apply the solution into the conjunctival sac, close the eye for 1-5 minutes and press the lacrimal sac before opening the eye.
   • There should be at least 5 minutes between use and other eye drops.
   • Cosoptomin eye drops: When using, the first 1-2 drops must be discarded (remove the container fragments when opening); because it does not contain preservatives, it can only be used once after opening, and the remaining liquid must be discarded.
   • If eye irritation occurs, accompanied by severe tearing, the drug may be washed away and the desired effect may not be achieved.
3. Drug storage
   • Cosupplement eye drops: After opening the outer box, keep it away from light and store at room temperature.
   • Cosoptomin eye drops: After opening the aluminum foil package, place the eye drops in the included light-proof medicine bag and store at room temperature. Use within 1 year. Store at room temperature.
   • Both preparations need to be stored away from light.

5. Adverse Reactions

1. Allergic reactions: Ocular pemphigoid (conjunctival congestion, corneal epithelial disorders, etc.), systemic lupus erythematosus, mucocutaneous ocular syndrome (Stevens-Johnson syndrome), toxic epidermal necrolysis (TEN), etc. may occur (frequency unknown).
2. Digestive system reactions: diarrhea, indigestion, nausea, dry mouth, abdominal pain, etc. may occur (frequency unknown).
3. Other serious side effects: bronchospasm, dyspnea, respiratory failure (frequency unknown, due to bronchial smooth muscle contraction caused by beta-receptor blockade); heart block, congestive heart failure, cardiac arrest (frequency unknown, due to the negative chronotropic and inotropic effects of beta-receptor blockade); cerebral ischemia, cerebrovascular disorders (frequency unknown).
4. Other side effects
   • Eyes: Eye irritation symptoms (shimmer, burning sensation, etc., more than 5%); keratitis, conjunctival congestion, etc. (1-5%); corneal disorders, etc. (less than 1%); corneal hypoesthesia, visual impairment, etc. (frequency unknown).
   • Circulator: Absence, edema, retinopathy, etc. (frequency unknown).
   • Psychoneural system: headache (1-5%); depression, aggravation of myasthenia gravis, etc. (frequency unknown).

6. Drug Interactions

1. Drosalamide is mainly metabolized by CYP2C9, 2C19 and 3A4, while chmolal is mainly metabolized by CYP2D6.
2. Use Note
   • OmidiPagiso Propil: The frequency of ocular inflammatory side effects such as conjunctival hyperemia increased (mechanism unknown).
   • Adrenaline and dipivoxil hydrochloride: There have been reports of enhanced mydriasis (mechanism unknown).
   • Catalytic amine depressants (such as Lecelpin, etc.): May excessively inhibit the sympathetic nerves, leading to hypotension, bradycardia, etc. (may additively enhance the β-blocking effect).
   • β-blockers (systemic administration, such as Atenolol, etc.): May enhance the intraocular pressure-lowering effect or the systemic effect of β-blockers (the effects may be additive).
   • Calciomer antagonists (such as berapamil hydrochloride, etc.): May cause atrioventricular conduction disorders, left ventricular failure, and hypotension (enhanced interaction).
   • Digitarics (such as Digikin, etc.): Cardiac conduction disorders (such as bradycardia, etc., which additively enhance the inhibitory effect on cardiac stimulation conduction) may occur.
   • Drugs with CYP2D6 inhibitory effects (such as cinizin sulfate salts and substances, etc.): May enhance β-blocking effects (such as reduced heart rate, etc., may inhibit metabolic enzymes and increase the blood concentration of this agent).
   • Carbohydrate dehydratase inhibitors (systemic administration, such as Asetasolamide, etc.): May enhance the systemic effects of carbohydrate dehydratase inhibitors (the effects may be additive).
   • Aspirin (large amounts): May enhance the side effects of either or both drugs (aspirin may inhibit plasma protein binding and renal excretion of carbonic anhydrase inhibitors, and carbonic anhydrase inhibitors may lower blood pH and increase the transfer of salicylic acid from plasma to tissues).

7. Pharmacological Action

1. Regulation of biofilm function: No relevant clear content.
2. Improve metabolic abnormalities: No relevant clear content.
3. Regulating blood lipids: No relevant clear content.
4. Protect blood vessels
   • Vasodilator effect: In pig experiments, intravenous administration of 500 mg of drosolamidor hydrochloride showed retinal vasodilation.
   • Effect on ocular blood flow: After using 1% Dolusolamide eye drops in patients with normal intraocular pressure glaucoma, the minimum blood flow velocity of the central retinal artery increased.
5. Others: Drosolamide salt reduces aqueous humor production by inhibiting carbonic acid dehydratase isoenzyme II; trimoxetine salt inhibits aqueous humor production by blocking β-receptors. The two work together to lower intraocular pressure.

8. Pharmacokinetics

1. Absorption: After single-point eyedrop in both eyes of 8 healthy adults, the Cmax of dolusolamide in whole blood was 39.4±10.7ng/mL, and the Cmax of timolol in plasma was 1.32±0.583ng/mL (mean±SD).
2. Excretion: After repeated instillation of 2.5% Dolusol eye drops in healthy adult males, the amount excreted in urine by the 8th day was 0.6% of the total dose; after repeated instillation of 2% Dolusol eye drops in patients with ocular hypertension, the amount excreted in urine was 140µg after 28 days, mainly in the form of unchanged form; after a single oral dose of 14C-Chimolol in humans, 6-23% of the excretion in urine was unchanged form.

IX. Clinical Research

10. Packaging specifications

1. Cosupplement eye drops: plastic eye drop container, 5mL x 10 pieces.
2. Cosoprotin eye drops: Plastic eye drop container, 0.4mL x 60 pieces (1 aluminum foil bag, 20 pieces x 3 bags).

11. Production Information

Manufacturer: Santen Pharmaceutical Co., Ltd.