Prostaglandin Analogs
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Prostaglandin Analogs
Prostaglandin analogues are a class of drugs that bind to a prostaglandin receptor. Wider use of prostaglandin analogues is limited by unwanted side effects and their abortive potential. Uses Prostaglandin analogues such as misoprostol are used in treatment of duodenal and gastric ulcers. Misoprostol and other prostaglandin analogues protect the lining of the gastrointestinal tract from harmful stomach acid and are especially indicated for the elderly on continuous doses of NSAIDs. In the field of ophthalmology, drugs of this class are used to lower intraocular pressure (IOP) in people with glaucoma. Up until the late 1970s prostaglandins were thought to raise IOP, but a paper published in 1977 showed that prostaglandin F2α lowered it, and subsequent studies found that this was due to increasing the outflow of aqueous humor, mainly by relaxing the ciliary muscle, and possibly also due to changes in extracellular matrix and to widening of spaces within the trabecular meshwork. ...
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Class Of Drugs
A drug class is a set of medications and other compounds that have a similar chemical structures, the same mechanism of action (i.e. binding to the same biological target), a related mode of action, and/or are used to treat the same disease. In several dominant drug classification systems, these four types of classifications form a hierarchy. For example, the fibrates are a chemical class of drugs (amphipathic carboxylic acids) that share the same mechanism of action (PPAR agonist) and mode of action (reducing blood triglycerides), and that are used to prevent and treat the same disease (atherosclerosis). Conversely, not all PPAR agonists are fibrates, not all triglyceride lowering agents are PPAR agonists, and not all drugs used to treat atherosclerosis are triglyceride-lowering agents. A drug class is typically defined by a prototype drug, the most important, and typically the first developed drug within the class, used as a reference for comparison. Comprehensive Systems ...
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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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Tafluprost
Tafluprost (trade names Taflotan by Santen Pharmaceutical, Zioptan by Merck in the US and Saflutan by Mundipharma in Australia) is a prostaglandin analogue. It is used topically (as eye drops) to control the progression of open-angle glaucoma and in the management of ocular hypertension, alone or in combination with other medication. It reduces intraocular pressure by increasing the outflow of aqueous fluid from the eyes. Adverse effects The most common side effect is conjunctival hyperemia, which occurs in 4 to 20% of patients. Less common side effects include stinging of the eyes, headache, and respiratory infections. Rare side effects are dyspnoea (breathing difficulties), worsening of asthma, and macular oedema. Interactions Nonsteroidal anti-inflammatory drugs (NSAIDs) can either reduce or increase the effect of tafluprost. Timolol eye drops, a common kind of glaucoma medication, does not negatively interact with this drug. No interactions with systemic (for example, o ...
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Travoprost
Travoprost, sold under the brand name Travatan among others, is a medication used to treat high pressure inside the eye including glaucoma. Specifically it is used for open angle glaucoma when other agents are not sufficient. It is used as an eye drop. Effects generally occur within two hours. Common side effects include red eyes, blurry vision, eye pain, dry eyes, and change in color of the eyes. Other significant side effects may include cataracts. Use during pregnancy or breastfeeding is generally not recommended. It is a prostaglandin analog and works by increasing the outflow of aqueous fluid from the eyes. Travoprost was approved for medical use in the United States and in the European Union in 2001. It is available as a generic medication in the United Kingdom. In 2020, it was the 304th most commonly prescribed medication in the United States, with more than 1million prescriptions. Medical uses Travoprost is used to treat high pressure inside the eye including glaucom ...
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Bimatoprost
Bimatoprost, sold under the brand name Lumigan among others, is a medication used to treat high pressure inside the eye including glaucoma. Specifically it is used for open angle glaucoma when other agents are not sufficient. It may also be used to increase the size of the eyelashes. It is used as an eye drop and effects generally occur within four hours. Common side effects include red eyes, dry eyes, change in color of the eyes, blurry vision, and cataracts. Use during pregnancy or breastfeeding is generally not recommended. It is a prostaglandin analog and works by increasing the outflow of aqueous fluid from the eyes. Bimatoprost was approved for medical use in the United States in 2001. It is available as a generic medication. In 2020, it was the 166th most commonly prescribed medication in the United States, with more than 3million prescriptions. Uses Medical Bimatoprost is used for the treatment of open-angle glaucoma and ocular hypertension in adults, either alone or ...
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Latanoprost
Latanoprost, sold under the brand name Xalatan among others, 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. Common side effects include blurry vision, redness of the eye, itchiness, and darkening of the iris. Latanoprost is in the prostaglandin analogue family of medications. It works by increasing the outflow of aqueous fluid from the eyes through the uveoscleral tract. Latanoprost was approved for medical use in the United States in 1996. It is on the World Health Organization's List of Essential Medicines. Latanoprost is available as a generic medication. In 2020, it was the 77th most commonly prescribed medication in the United States with more than 9million prescriptions. It is available as a combination with netarsudil and with timolol. Medical uses Open-angle glaucoma ...
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Prodrugs
A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects. History Many herbal extracts historically used in medicine contain glycosides (sugar derivatives) of the active agent, which are hydrolyzed in the intestines to release the active and more bioavailable aglycone. For example, salicin is a β-D-glucopyranosid ...
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Trabecular Meshwork
The trabecular meshwork is an area of tissue in the eye located around the base of the cornea, near the ciliary body, and is responsible for draining the aqueous humor from the eye via the anterior chamber (the chamber on the front of the eye covered by the cornea). The tissue is spongy and lined by trabeculocytes; it allows fluid to drain into a set of tubes called Schlemm's canal which is lined by endothelium with blood and lymphatic properties that allow aqueous humor to flow into the blood system. Structure The meshwork is divided up into three parts, with characteristically different ultrastructures: #''Inner uveal meshwork'' - Closest to the anterior chamber angle, contains thin cord-like trabeculae, orientated predominantly in a radial fashion, enclosing trabeculae spaces larger than the corneoscleral meshwork. #''Corneoscleral meshwork'' - Contains a large amount of elastin, arranged as a series of thin, flat, perforated sheets arranged in a laminar pattern; cons ...
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Extracellular Matrix
In biology, the extracellular matrix (ECM), also called intercellular matrix, is a three-dimensional network consisting of extracellular macromolecules and minerals, such as collagen, enzymes, glycoproteins and hydroxyapatite that provide structural and biochemical support to surrounding cells. Because multicellularity evolved independently in different multicellular lineages, the composition of ECM varies between multicellular structures; however, cell adhesion, cell-to-cell communication and differentiation are common functions of the ECM. The animal extracellular matrix includes the interstitial matrix and the basement membrane. Interstitial matrix is present between various animal cells (i.e., in the intercellular spaces). Gels of polysaccharides and fibrous proteins fill the Interstitial fluid, interstitial space and act as a compression buffer against the stress placed on the ECM. Basement membranes are sheet-like depositions of ECM on which various epithelial cells rest ...
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Ciliary Muscle
The ciliary muscle is an intrinsic muscle of the eye formed as a ring of smooth muscleSchachar, Ronald A. (2012). "Anatomy and Physiology." (Chapter 4) . in the eye's middle layer, uvea ( vascular layer). It controls accommodation for viewing objects at varying distances and regulates the flow of aqueous humor into Schlemm's canal. It also changes the shape of the lens within the eye but not the size of the pupil which is carried out by the sphincter pupillae muscle and dilator pupillae. Structure Development The ciliary muscle develops from mesenchyme within the choroid and is considered a cranial neural crest derivative.Dudek RW, Fix JD (2004). "Eye" (chapter 9). ''Embryology - Board Review Series'' (3rd edition, illustrated). Lippincott Williams & Wilkins. p. 92. , . Books.Google.com. Retrieved on 2010-01-17 from https://books.google.com/books?id=MmoJQWsJteoC. Nerve supply The ciliary muscle receives parasympathetic fibers from the short ciliary nerves that arise fro ...
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Prostaglandin F2α
Prostaglandin F2α (PGF2α in prostanoid nomenclature), pharmaceutically termed carboprost is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient. Prostaglandins are lipids throughout the entire body that have a hormone-like function. In pregnancy, PGF2 is medically used to sustain contracture and provoke myometrial ischemia to accelerate labor and prevent significant blood loss in labor. Additionally, PGF2 has been linked to being naturally involved in the process of labor. It has been seen that there are higher levels of PGF2 in maternal fluid during labor when compared to at term. This signifies that there is likely a biological use and significance to the production and secretion of PGF2 in labor. Prostaglandin is also used to treat uterine infections in domestic animals. In domestic mammals, it is produced by the uterus when stimulated by oxytocin, in the event that there has been no implantation during the luteal phase. It acts on t ...
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Prostaglandin Receptor
Prostaglandin receptors or prostanoid receptors represent a sub-class of cell surface membrane Receptor (biochemistry), receptors that are regarded as the primary receptors for one or more of the classical, naturally occurring prostanoids viz., prostaglandin D2, (i.e. PGD2), PGE2, PGF2alpha, prostacyclin (PGI2), thromboxane A2 (TXA2), and PGH2. They are named based on the prostanoid to which they preferentially bind and respond, e.g. the receptor responsive to PGI2 at lower concentrations than any other prostanoid is named the Prostacyclin receptor (IP). One exception to this rule is the receptor for thromboxane A2 (TP) which binds and responds to PGH2 and TXA2 equally well. All of the prostanoid receptors are G protein-coupled receptors belonging to the Rhodopsin-like receptors, Subfamily A14 of the rhodopsin-like receptor family except for the Prostaglandin DP2 receptor which is more closely related in amino acid sequence and functionality to chemotactic factor receptors such as th ...
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