Netarsudil Latanoprost
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Netarsudil Latanoprost
Netarsudil, sold under the brand name Rhopressa among others, is a medication for the treatment of glaucoma. In the United States, in December 2017, the Food and Drug Administration (FDA) approved a 0.02% ophthalmic solution for the lowering of elevated intraocular pressure in people with open-angle glaucoma or ocular hypertension. The European Medicines Agency approved it in 2019 for the same uses under the brand name Rhokiinsa. The FDA considers it to be a first-in-class medication. Contraindications Netarsudil has no contraindications apart from known hypersensitivity to the drug. Adverse effects The most common side effects are hyperaemia (increased blood flow associated with redness, in 51% of patients) in the conjunctiva, cornea verticillata (drug deposits in the cornea, in 17%), and eye pain (in 17%). All other side effects occur in fewer than 10% of people. Hypersensitivity reactions occur in fewer than 1%. Overdose Overdosing netarsudil is unlikely because concent ...
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Ophthalmic Drug Administration
Ophthalmic drug administration is the administration of a drug to the eyes, most typically as an eye drop formulation. Topical formulations are used to combat a multitude of diseased states of the eye. These states may include bacterial infections, eye injury, glaucoma, and dry eye. However, there are many challenges associated with topical delivery of drugs to the cornea of the eye. Eye drop formulations Two of the largest challenges faced when using topicals to treat pathological states of the eye include patient compliance and ineffective absorbance of drugs into the cornea. In fact, researchers in this field of drug delivery agree that less than 7% of drugs delivered to the eye reach and penetrate the corneal barrier, therefore, increasing the frequency of dosing used for topicals. This is one of the fundamental problem associated with using topicals to deliver drugs to the cornea and therefore leads to the increased demand for patient compliance. Together, these two factors ...
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Aqueous Humor
The aqueous humour is a transparent water-like fluid similar to plasma, but containing low protein concentrations. It is secreted from the ciliary body, a structure supporting the lens of the eyeball. It fills both the anterior and the posterior chambers of the eye, and is not to be confused with the vitreous humour, which is located in the space between the lens and the retina, also known as the posterior cavity or vitreous chamber. Blood cannot normally enter the eyeball. Structure Composition *Amino acids: transported by ciliary muscles *98% water *Electrolytes ( pH = 7.4 -one source gives 7.1) **Sodium = 142.09 **Potassium = 2.2 - 4.0 **Calcium = 1.8 **Magnesium = 1.1 **Chloride = 131.6 **HCO3- = 20.15 **Phosphate = 0.62 ** Osm = 304 *Ascorbic acid *Glutathione *Immunoglobulins Function *Maintains the intraocular pressure and inflates the globe of the eye. It is this hydrostatic pressure that keeps the eyeball in a roughly spherical shape and keeps the walls of the eyeball ...
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Ophthalmology Drugs
Ophthalmology ( ) is a surgical subspecialty within medicine that deals with the diagnosis and treatment of eye disorders. An ophthalmologist is a physician who undergoes subspecialty training in medical and surgical eye care. Following a medical degree, a doctor specialising in ophthalmology must pursue additional postgraduate residency training specific to that field. This may include a one-year integrated internship that involves more general medical training in other fields such as internal medicine or general surgery. Following residency, additional specialty training (or fellowship) may be sought in a particular aspect of eye pathology. Ophthalmologists prescribe medications to treat eye diseases, implement laser therapy, and perform surgery when needed. Ophthalmologists provide both primary and specialty eye care - medical and surgical. Most ophthalmologists participate in academic research on eye diseases at some point in their training and many include research as part ...
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Netarsudil/latanoprost
Netarsudil/latanoprost, sold under the brand name Rocklatan among others, is a fixed-dose combination medication use to treat elevated intraocular pressure (IOP) in people with open-angle glaucoma or ocular hypertension. It contains netarsudil mesylate and latanoprost. It is applied as eye drops to the eyes. The most common side effects include conjunctival hyperaemia (red eye), pain at the site where the medicine was applied, cornea verticillata (deposits in the cornea, the transparent layer in front of the eye that covers the pupil and iris), pruritus (itching of the eye), erythema (reddening) and discomfort in the eye, increased lacrimation (watery eyes), and conjunctival haemorrhage (bleeding in the surface layer of the eye). Netarsudil/latanoprost was approved for medical use in the United States in March 2019, and in the European Union in January 2021. Medical uses Netarsudil/latanoprost is indicated In medicine, an indication is a valid reason to use a certain ...
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Methanol
Methanol (also called methyl alcohol and wood spirit, amongst other names) is an organic chemical and the simplest aliphatic alcohol, with the formula C H3 O H (a methyl group linked to a hydroxyl group, often abbreviated as MeOH). It is a light, volatile, colourless, flammable liquid with a distinctive alcoholic odour similar to that of ethanol (potable alcohol). A polar solvent, methanol acquired the name wood alcohol because it was once produced chiefly by the destructive distillation of wood. Today, methanol is mainly produced industrially by hydrogenation of carbon monoxide. Methanol consists of a methyl group linked to a polar hydroxyl group. With more than 20 million tons produced annually, it is used as a precursor to other commodity chemicals, including formaldehyde, acetic acid, methyl tert-butyl ether, methyl benzoate, anisole, peroxyacids, as well as a host of more specialised chemicals. Occurrence Small amounts of methanol are present in normal, healthy hu ...
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Solubility
In chemistry, solubility is the ability of a substance, the solute, to form a solution with another substance, the solvent. Insolubility is the opposite property, the inability of the solute to form such a solution. The extent of the solubility of a substance in a specific solvent is generally measured as the concentration of the solute in a saturated solution, one in which no more solute can be dissolved. At this point, the two substances are said to be at the solubility equilibrium. For some solutes and solvents, there may be no such limit, in which case the two substances are said to be " miscible in all proportions" (or just "miscible"). The solute can be a solid, a liquid, or a gas, while the solvent is usually solid or liquid. Both may be pure substances, or may themselves be solutions. Gases are always miscible in all proportions, except in very extreme situations,J. de Swaan Arons and G. A. M. Diepen (1966): "Gas—Gas Equilibria". ''Journal of Chemical Physics'', ...
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Hygroscopic
Hygroscopy is the phenomenon of attracting and holding water molecules via either absorption or adsorption from the surrounding environment, which is usually at normal or room temperature. If water molecules become suspended among the substance's molecules, adsorbing substances can become physically changed, e.g., changing in volume, boiling point, viscosity or some other physical characteristic or property of the substance. For example, a finely dispersed hygroscopic powder, such as a salt, may become clumpy over time due to collection of moisture from the surrounding environment. ''Deliquescent'' materials are sufficiently hygroscopic that they absorb so much water that they become liquid and form an aqueous solution. Etymology and pronunciation The word ''hygroscopy'' () uses combining forms of '' hygro-'' and '' -scopy''. Unlike any other ''-scopy'' word, it no longer refers to a viewing or imaging mode. It did begin that way, with the word ''hygroscope'' referring in th ...
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Mesilate
In organosulfur chemistry, a mesylate is any salt or ester of methanesulfonic acid (). In salts, the mesylate is present as the anion. When modifying the international nonproprietary name of a pharmaceutical substance containing the group or anion, the spelling used is sometimes mesilate (as in ''imatinib mesilate'', the mesylate salt of imatinib). Mesylate esters are a group of organic compounds that share a common functional group with the general structure , abbreviated , where R is an organic substituent. Mesylate is considered a leaving group in nucleophilic substitution reactions. Preparation Mesylates are generally prepared by treating an alcohol and methanesulfonyl chloride in the presence of a base, such as triethylamine. Mesyl Related to mesylate is the mesyl (Ms) or methanesulfonyl (CH3SO2) functional group. Methanesulfonyl chloride is often referred to as mesyl chloride. Whereas mesylates are often hydrolytically labile, mesyl groups, when attached to nitro ...
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Elimination Half-life
Biological half-life (also known as elimination half-life, pharmacologic half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration ( Cmax) to half of Cmax in the blood plasma, and is denoted by the abbreviation t_. This is used to measure the removal of things such as metabolites, drugs, and signalling molecules from the body. Typically, the biological half-life refers to the body's natural cleansing through the function of the liver and through the excretion of the measured substance through the kidneys and intestines. This concept is used when the rate of removal is roughly exponential. In a medical context, half-life explicitly describes the time it takes for the blood plasma concentration of a substance to halve (''plasma half-life'') its steady-state when circulating in the full blood of an organism. This measurement is useful in medicine, pharmacology and pharmacokinetics because it helps det ...
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Blood Plasma
Blood plasma is a light amber-colored liquid component of blood in which blood cells are absent, but contains proteins and other constituents of whole blood in suspension. It makes up about 55% of the body's total blood volume. It is the intravascular part of extracellular fluid (all body fluid outside cells). It is mostly water (up to 95% by volume), and contains important dissolved proteins (6–8%; e.g., serum albumins, globulins, and fibrinogen), glucose, clotting factors, electrolytes (, , , , , etc.), hormones, carbon dioxide (plasma being the main medium for excretory product transportation), and oxygen. It plays a vital role in an intravascular osmotic effect that keeps electrolyte concentration balanced and protects the body from infection and other blood-related disorders. Blood plasma is separated from the blood by spinning a vessel of fresh blood containing an anticoagulant in a centrifuge until the blood cells fall to the bottom of the tube. The blood plasma is t ...
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Esterase
An esterase is a hydrolase enzyme that splits esters into an acid and an alcohol in a chemical reaction with water called hydrolysis. A wide range of different esterases exist that differ in their substrate specificity, their protein structure, and their biological function. EC classification/list of enzymes * ''EC 3.1.1'': Carboxylic ester hydrolases ** Acetylesterase (EC 3.1.1.6), splits off acetyl groups *** Cholinesterase **** Acetylcholinesterase, inactivates the neurotransmitter acetylcholine **** Pseudocholinesterase, broad substrate specificity, found in the blood plasma and in the liver ** Pectinesterase (EC 3.1.1.11), clarifies fruit juices * ''EC 3.1.2'': Thiolester hydrolases ** Thioesterase *** Ubiquitin carboxy-terminal hydrolase L1 * ''EC 3.1.3'': Phosphoric monoester hydrolases ** Phosphatase (EC 3.1.3.x), hydrolyses phosphoric acid monoesters into a phosphate ion and an alcohol *** Alkaline phosphatase, removes phosphate groups from many types of molecules, ...
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