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General Description:

Ripasudil, identified by CAS number 223645-67-8, is a notable compound with significant therapeutic applications. Ripasudil, as hydrochloride hydrate (K-115), is a specifc Rho-associated coiled-coil containing protein kinase (ROCK) inhibitor used for the treatment of glaucoma and ocular hypertension. It was first approved for treatment in Japan in September 2014. This medication is available in the form of a 0.4% eye drop solution under the brand name Glanatec. Ripasudil is a well tolerated medication that is used when other drugs have been proven to be non-effective or cannot be administered.

Indications:

This drug is primarily indicated for: Ripasudil has been proven to be effective in the twice daily treatment of glaucoma and ocular hypertension. It is currently in studies to be approved for both diabetic retinopathy and diabetic macular oedema. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Half-life:

The half-life of Ripasudil is an important consideration for its dosing schedule: The half life of Ripasudil is 0.455 hrs. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Ripasudil exhibits a strong affinity for binding with plasma proteins: The plasma protein binding rate of Ripasudil is 55.4-59.8%. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Ripasudil from the body primarily occurs through: Riapsudil is cleared by the kidneys at a rate of 7.112L/h. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Clearance:

The clearance rate of Ripasudil is a critical factor in determining its safe and effective dosage: Ripasudil has a renal clearance of 7.112 L/h. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Ripasudil exerts its therapeutic effects through: Ripasudil has high intraocular permeability and works by decreasing intraocular pressure (IOP) in a dose-dependent manner and increasing flow facility. The maximum reduction of IOP occurs after 1 to 2 hours. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Ripasudil functions by: Ripasudil is a highly selective and potent Rho-associated coiled/coil-containing kinase protein (ROCK) inhibitor. Rho-kinase (ROCK) is an effector protein of Rho which binds with Rho to form a Rho/Rho-kinase complex. This complex then regulates many physiological functions including smooth muscle contractions, chemotaxis, neural growth and gene expression. ROCK comes in 2 isoforms: ROCK-1 and ROCK-2 and these two isoforms are distributed widely in our tissues including ocular tissues such as the iris, retina, trabecular meshwork and ciliary muscles. Atypical regulation of ROCK levels is involved in the pathogenesis of diseases such as glaucoma, ocular hypertension, cataracts and other retinal disorders. Ripasudil acts as very highly selective and potent inhibitor with an IC50 of Ripasudil with ROCK-1 of 0.051 umol/L and with ROCK-2 of 0.019 umol/L. ROCK inhibitors have efficacy in reducing IOP by acting on the trabecular meshwork in the eye directly to increase conventional outflow through the Schlemm’s canal. Ripasudil will inhibit ROCK and induce cytoskeletal changes including the retraction and rounding of cell bodies and cause disruption of actin bundles in this trabecular meshwork. This can reduce the compaction of trabecular meshwork tissue and eventually result in increased aqueous outflow in the eye and reduced resistance to fluid flow. Thus, Ripasudil is effective by inducing cytoskeletal changes which are depending on ROCK inhibition. Ripasudil decreases IOP by increasing outflow facility along with modulating the behavior of trabecular meshwork cells and Schlemm’s canal endothelial (SCE) cell permeability along with a disruption of the tight junction. When Ripasudil is used in combination with prostaglandin analogues it results in increased uveoscleral outflow and when used in combination with beta blockers it results in reduced aqueous production. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Ripasudil belongs to the class of organic compounds known as isoquinolines and derivatives. These are aromatic polycyclic compounds containing an isoquinoline moiety, which consists of a benzene ring fused to a pyridine ring and forming benzo[c]pyridine, classified under the direct parent group Isoquinolines and derivatives. This compound is a part of the Organic compounds, falling under the Organoheterocyclic compounds superclass, and categorized within the Isoquinolines and derivatives class, specifically within the None subclass.

Categories:

Ripasudil is categorized under the following therapeutic classes: Amides, Antiglaucoma Preparations and Miotics, Heterocyclic Compounds, Fused-Ring, Ophthalmologicals, rho-Associated Kinases, antagonists & inhibitors, Sensory Organs, Sulfones, Sulfur Compounds. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.