Vyzulta (latanoprostene bunod)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Latanoprostene bunod, a synthetic analog of naturally occurring prostaglandin F2alpha (PGF2alpha), is an ocular hypotensive agent.
Latanoprostene bunod, a synthetic analog of naturally occurring prostaglandin F2alpha (PGF2alpha), is an ocular hypotensive agent.
Latanoprostene bunod is a prodrug that is rapidly metabolized by cellular esterases to 2 active moieties (i.e., latanoprost acid (prostaglandin agonist) and butanediol mononitrate (nitric oxide donor)) following topical ophthalmic administration and these active metabolites reduce intraocular pressure (IOP) by a dual mechanism of action. Latanoprostene bunod treatment increases aqueous humor outflow within both the trabecular meshwork (conventional route) and the uveoscleral pathway (nonconventional route). Latanoprost acid increases aqueous humor outflow via the uveoscleral pathway; butanediol mononitrate releases nitric oxide, inducing relaxation and increasing aqueous humor outflow through the trabecular meshwork and Schlemm's canal.
The release of nitric oxide causes human trabecular meshwork relaxation through activation of the cyclic guanosine monophosphate (cGMP) signaling pathway and reduction in myosin light chain-2 (MLC- 2) phosphorylation. A synergistic effect on aqueous humor outflow resulting from the drug's dual mechanism of action may contribute to the additional IOP-lowering effects of latanoprostene bunod compared with latanoprost. Following topical application of latanoprostene bunod ophthalmic solution to the eye, reduction in IOP occurs within 1-3 hours and peaks within 11-13 hours.
Although quantifiable plasma concentrations of latanoprostene bunod and its active metabolite, butanediol mononitrate, have not been detected following topical administration of the drug to the eye, the other active metabolite, latanoprost acid, has been detected in plasma. In one study following topical application of latanoprostene bunod 0.024% solution once daily to each eye for 28 days in healthy individuals, plasma concentrations of latanoprostene bunod were undetectable (lower limit of quantitation 10 pg/mL) after the dose on days 1 and 28. Plasma concentrations of butanediol mononitrate also were undetectable (lower limit of quantitation 200 pg/mL).
Latanoprost acid was detected in plasma (lower limit of quantitation 30 pg/mL) and mean maximal plasma concentrations of this metabolite were 59.1 and 51.1 pg/mL on days 1 and 28, respectively. The mean time to maximal plasma concentrations of latanoprost acid was approximately 5 minutes following administration of latanoprostene bunod on both days 1 and 28. However, elimination of latanoprost acid from human plasma is rapid and plasma concentrations dropped below the lower limit of quantitation (30 pg/mL) in most individuals by 15 minutes following the dose.
After latanoprost acid reaches the systemic circulation, it is mainly metabolized by the liver to the 1,2-dinor and 1,2,3,4-tetranor metabolites via fatty acid beta-oxidation. Butanediol mononitrate is metabolized to 1,4-butanediol and nitric oxide; the metabolite 1,4-butanediol is further oxidized to succinic acid and enters the tricarboxylic acid cycle.
USES: Latanoprostene bunod is used to treat high pressure inside the eye due to glaucoma (open-angle type) or other eye diseases (such as ocular hypertension). Lowering high pressure inside the eye can help prevent blindness. This medication works by controlling the flow of fluid within the eye to maintain a normal pressure.
Generic name: latanoprostene bunod
Pronunciation: (la-TAN-oh-PROS-teen BUE-nod)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Vyzulta
Indications
The following indications are listed for Vyzulta:
- Ocular Hypertension
- Open Angle Glaucoma
Also known as: Chronic Glaucoma, Compensated Glaucoma, Glaucoma Simplex, Increased Intraocular Pressure, Increased Iop, Open-Angle Glaucoma, Raised Intraocular Pressure, Simple Glaucoma.
Dosing
For the treatment of open-angle glaucoma or ocular hypertension, 1 drop of latanoprostene bunod 0.024% solution should be instilled into the conjunctival sac of the affected eye(s) once daily in the evening. Latanoprostene bunod should not be administered more frequently than once daily since more frequent dosing may diminish the intraocular pressure (IOP)-lowering effect of the drug.
If the target IOP is not achieved, alternative or additional ocular hypotensive agents may be required. (See Uses: Ocular Hypertension and Glaucoma.)
Latanoprostene bunod is applied topically to the eye(s) as a 0.024% ophthalmic solution.
Care should be taken to avoid contaminating the solution container. (See Bacterial Keratitis under Cautions: Warnings/Precautions.)
Contact lenses should be removed prior to administration of latanoprostene bunod; contact lenses may be reinserted 15 minutes following administration of the dose. (See Use with Contact Lenses under Cautions: Warnings/Precautions.)
If the patient is receiving more than one topical ophthalmic drug, the drugs should be administered at least 5 minutes apart.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies using latanoprostene bunod have been performed to date. However, interactions are not expected because of limited systemic exposure following topical application to the eye.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
The manufacturer states there are no known contraindications to the use of latanoprostene bunod.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in 2% or more of patients receiving latanoprostene bunod ophthalmic solution include conjunctival hyperemia, eye irritation, eye pain, and instillation site pain.
Approximately 0.6% of patients receiving latanoprostene bunod ophthalmic solution in clinical trials discontinued therapy because of adverse ocular reactions, including ocular hyperemia, conjunctival irritation, conjunctival edema, eye irritation, blurred vision, punctate keratitis, and foreign body sensation.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Use of latanoprostene bunod ophthalmic solution in pediatric patients 16 years of age or younger is not recommended because of potential safety concerns related to increased pigmentation following long-term use. (See Pigmentation under Cautions: Warnings/Precautions.)
There are no available data regarding use of latanoprostene bunod ophthalmic solution in pregnant women to inform any drug-associated risk.
Latanoprostene bunod has caused miscarriages, abortions, and fetal harm in rabbits. The drug was shown to be abortifacient and teratogenic when administered IV to pregnant rabbits at exposures 0.28 times or greater than the clinical dose. Dosages of 20 mcg/kg daily or greater (23 times or greater the clinical dose) produced 100% embryofetal lethality in rabbits. In rats, no treatment-related teratogenic effects were observed when the drug was administered IV at a dosage of 150 mcg/kg daily (87 times the clinical dose).
It is not known whether latanoprostene bunod and/or its metabolites are distributed into human milk following topical application to the eye. Data also are not available on the effects of the drug on the breast-fed child or on milk production.
The benefits of breast-feeding should be considered along with the importance of the drug to the woman and any potential adverse effects on the breast-fed child from the drug or underlying maternal condition.
No overall differences in safety or efficacy of latanoprostene bunod ophthalmic solution have been observed between geriatric patients and younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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