Glaucostat
Glaucostat Uses, Dosage, Side Effects, Food Interaction and all others data.
Glaucostat is an analogue of prostaglandin F2α. Glaucostat is a prostanoid selective FP receptor agonist that is believed to reduce the intraocular pressure (IOP) by increasing the outflow of aqueous humor. Studies in animals and man suggest that the main mechanism of action is increased uveoscleral outflow. Elevated IOP represents a major risk factor for glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss.
Glaucostat effectively decreases intraocular pressure by increasing uveoscleral outflow. A decrease in intraocular pressure has been measured within 3–4 hours post-administration, reaches a maximum decrease at 8–12 hours, and can be maintained for a period of 24 hours.
A note on eye and periorbital changes
Between 3 to 10% of patients taking latanoprost have experienced iris pigmentation after about 3-4 months of latanoprost use. Patients should be notified of this risk before initiating treatment. It may occur in both patients with light-colored irides (green-brown or blue/grey-brown) or dark-colored (brown) irides, but is less pronounced in the latter group. This drug may also cause other ocular effects including infrequent conjunctival hyperemia, pigmentation of periocular tissues, eyelash changes, hypertrichosis, and ocular irritation.
| Trade Name | Glaucostat |
| Generic | Latanoprost |
| Latanoprost Other Names | Latanoprost, Latanoprostum |
| Type | |
| Formula | C26H40O5 |
| Weight | Average: 432.5928 Monoisotopic: 432.28757439 |
| Protein binding | Latanoprost is about 90% plasma protein-bound. |
| Groups | Approved, Investigational |
| Therapeutic Class | Drugs for miotics and glaucoma |
| Manufacturer | |
| Available Country | Argentina |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Glaucostat Sterile Ophthalmic Solution is used for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Glaucostat is also used to associated treatment for these conditions: Increased Intra Ocular Pressure (IOP), Ocular Hypertension, Open Angle Glaucoma (OAG)
How Glaucostat works
Elevated intraocular pressure leads to an increased risk of glaucomatous visual field loss. The higher the intraocular pressure, the higher the risk of damage to the optic nerve and loss of visual field. Glaucostat selectively stimulates the prostaglandin F2 alpha receptor and this results in a decreased intraocular pressure (IOP) via the increased outflow of aqueous humor, which is often implicated in cases of elevated intraocular pressure. Possible specific mechanisms of the abovementioned increased aqueous outflow are the remodeling of the extracellular matrix and regulation of matrix metalloproteinases. These actions result in higher tissue permeability related to humor outflow pathways, which likely change outflow resistance and/or outflow rates.
Dosage
Glaucostat dosage
The recommended dosage is 1 drop (1.5 mcg) in the affected eye(s) once daily in the evening. This is for topical ophthalmic use only. Not for injection or oral use.
Side Effects
Eyelash changes (increased length, thickness, pigmentation, and number of lashes); eyelid skin darkening; intraocular inflammation (iritis/uveitis); iris pigmentation changes; and macular edema, including cystoid macular edema. The ocular adverse events and ocular signs and symptoms reported in 5- 15% of the patients on latanoprost in the 6 month, multicenter, double-masked, active-controlled trials were blurred vision, burning and stinging, conjunctival hyperemia, foreign body sensation, itching, increased pigmentation of the iris, and punctate epithelial keratopathy. Local conjunctiva hyperemia was observed; however, less than 1% of the latanoprost treated patients required discontinuation of therapy because of intolerance to conjunctival hyperemia.
Toxicity
The oral LD50 in the rat is > 50 mg/kg.
An overdose of latanoprost is not expected to result in dangerous patient outcomes, however, conjunctival or episcleral hyperemia may occur.An intravenous infusion of 3 μg/kg of latanoprost in healthy volunteers led to mean plasma concentrations of 200 times higher than a normally administered therapeutic dose and no adverse effects were noted. One study suggested that an overdose of latanoprost lead to cystoid macular edema after a large, unintended overdose. This resolved within 4 weeks after 4 weeks following treatment with nepafenac 0.3% eye drops in addition to oral acetazolamide. Contact the local poison control center for updated guidance on the management of a latanoprost overdose.
Precaution
Ophthalmic Solution may gradually increase the pigmentation of the iris. The eye color change is due to increased melanin content in the stromal melanocytes of the iris rather than to an increase in the number of melanocytes. During clinical trials, the increase in brown iris pigment has not been shown to progress further upon discontinuation of treatment, but the resultant color change may be permanent. Eyelid skin darkening, which may be reversible. There may be increased length, thickness, pigmentation, the number of lashes or hairs, and misdirected growth of eyelashes. Eyelash changes are usually reversible upon discontinuation of treatment. It should be used with caution in patients with a history of intraocular inflammation (iritis/uveitis) and should generally not be used in patients with active intraocular inflammation. This drug should be used with caution in patients who do not have an intact posterior capsule or who have known risk factors for macular edema.
Interaction
In vitro studies have shown that precipitation occurs when eye drops containing thimerosal are mixed with latanoprost. If such drugs are used they should be administered with an interval of at least 5 minutes between applications.
Food Interaction
No interactions found.Volume of Distribution
The volume of distribution of latanoprost is 0.16 ± 0.02 L/kg. The activated acid form of latanoprost can be measured in aqueous humor in the initial 4 hours post-administration, and it is measured in the plasma only for 1 hour following ophthalmic administration. This drug is more lipophilic than its parent prostaglandin and easily penetrates the cornea. It has been shown to cross the placenta in rats.
Elimination Route
This drug is rapidly absorbed in the cornea as an isopropyl ester prodrug and is then activated by the process of hydrolysis. A small amount of this drug is systemically absorbed. The Cmax of latanoprost in the systemic circulation is reached after 5 minutes and is measured to be 53 pg/mL. The Cmax in the aqueous humor is attained within 2 hours after administration. and has been estimated to be 15-30 ng/mL.
Half Life
The elimination half-life of latanoprost from the plasma is about 17 minutes. The elimination half-life of latanoprost from the eye is estimated at 2–3 hours.
Clearance
The systemic clearance of latanoprost is 7 mL/min/kg.
Elimination Route
After hepatic beta-oxidation, the metabolites of latanoprost are primarily found to be excreted by the kidneys. About 88% of the latanoprost dose is recovered in the urine after topical administration. About 15% of a dose is reported to be excreted in the feces.
Pregnancy & Breastfeeding use
Pregnancy Category C. There are no adequate and well controlled studies in pregnant women. The drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Contraindication
Known hypersensitivity to latanoprost, benzalkonium chloride or any other ingredients in this product.
Special Warning
Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Use: No overall differences in safety or effectiveness have been observed between elderly and younger patients.
Storage Condition
Before opening the cap, keep the bottle in its box in a refrigerator (2°-8° C) protected from light. After opening, keep the bottle in its box in a cool place below 25° C. The contents should be used within one month after the dropper is opened. Keep out of reach of children
Innovators Monograph
You find simplified version here Glaucostat
Glaucostat contains Latanoprost see full prescribing information from innovator Glaucostat Monograph, Glaucostat MSDS, Glaucostat FDA label
FAQ
What is Glaucostat used for?
Glaucostat is a medication used to treat increased pressure inside the eye. This includes ocular hypertension and open angle glaucoma. It is applied as eye drops to the eyes. Onset of effects is usually within four hours, and they last for up to a day. Increased pressure can damage your optic nerve and cause vision loss or blindness. Your doctor may give it to you if you have glaucoma or high pressure in the eye (ocular hypertension).
Is Glaucostat safe to use?
The results of this open-label, multicenter, multinational, uncontrolled study demonstrate that 0.005 percent Glaucostat administered once daily as adjunctive therapy for up to five years is safe and effective in reducing IOP in patients with primary open-angle and exfoliative glaucoma. Many people using this medication do not have serious side effects.
How does Glaucostat work?
Glaucostat works by increasing the natural flow of liquid from inside your eye into your bloodstream. This lowers the pressure within your eye and stops your sight getting worse.
What are the common side effects of Glaucostat?
Common side effects of Glaucostat are include:
- change in eye colour – usually seen within 8 months of using the eyedrops
- redness of the eye, inflamed eyelid (blepharitis) or eye infection (conjunctivitis)
- irritated eye and eye pain (burning, itching, stinging or a feeling as if something's in your eye)
- changes to your eyelashes (growing longer and thicker)
-
sensitivity to light (photophobia)
Is Glaucostat safe during pregnancy?
Exposure to Glaucostat at any stage in pregnancy would not usually be regarded as medical grounds for termination of pregnancy or any additional fetal monitoring.
Is Glaucostat safe during breastfeeding?
No information is available on the use of Glaucostat during breastfeeding. Because of its short half-life it is not likely to reach the bloodstream of the infant or cause any adverse effects in breastfed infants.
Can I drink alcohol with Glaucostat?
Yes, you can drink alcohol with Glaucostat.
Can I drive after taking Glaucostat?
This Glaucostat may cause blurred vision or other vision problems. If these occur, do not drive, use machines, or do anything else that could be dangerous if you are not able to see well. If these eye changes are bothersome, check with your doctor.
What time should I take Glaucostat?
The usual dose for adults and children is 1 drop into the affected eye(s) once a day. It's best to do this is in the evening as Glaucostat works better then. It comes as a bottle with an eye dropper or a box of single-use droppers.
How many time can I take Glaucostat daily?
Usually you use Glaucostat eyedrops once a day.
How long does Glaucostat take to work?
The pressure in your eye will start to reduce 3 to 4 hours after using the eyedrops. Glaucostat reaches full effect after 8 to 12 hours, the reduced pressure will last for at least 24 hours.
How long does Glaucostat stay in my system?
Elimination half-life from these tissues is 3 to 4 hours, although trace amounts can still be detected 24 hours after subministration. Analysis shows that latanoprost does not reach the posterior segment of the eye, being detectable only in more anterior tissues.
How long can I take Glaucostat for a long time?
Glaucostat stably reduced IOP over a long term and maintained visual field in approximately 70% of eyes with glaucoma after treatment for 5 years.
What happen If I forget dose of Glaucostat?
If you forget a dose by more than a couple of hours, skip the missed dose and use your eyedrops as usual the next day. Never use 2 doses at the same time. Never use an extra dose to make up for a forgotten one. If you often forget doses, it may help to set an alarm to remind you. You could ask your pharmacist for advice on other ways to remember your medicines.
What happen if I use too much Glaucostat?
Using too many drops can irritate your eye and make it water and turn red. This should get better, but if you are worried about it ask your doctor or pharmacist for advice.
Will Glaucostat affect my contraception?
Glaucostat does not stop contraceptive pills working, including the combined pill or emergency contraception.
Will Glaucostat affect my fertility?
There's no clear evidence to suggest that taking latanoprost will reduce fertility in either men or women. However, speak to a pharmacist or your doctor before taking it if you're trying to get pregnant.
Can Glaucostat affects my heart ?
Glaucostat is well known that topical ophthalmic medications are capable ofpro- ducing serious cardiovascular effects, including congestive heart failure, arrhythmias, and death.
Is Glaucostat bad for the kidneys?
Glaucostat should be used cautiously in patients with renal disease (e.g., renal failure, renal impairment) or hepatic disease. There have been no studies on safe use in these patients.
Can Glaucostat affect blood pressure?
There were no significant differences in changes in mean values of spirometry, pulse rate, or blood pressure.
Should I stop using Glaucostat?
You may also have darkening of the eyelid skin color or longer, thicker, and darker eyelashes. These changes to the iris, eyelid, and lashes may be permanent even if you stop using Glaucostat.
