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Encyclopedia > Sublingual

Sublingual, literally 'under the tongue', from Latin, refers to a pharmacological route of administration in which certain drugs are entered directly into the bloodstream via absorption under the tongue. Many pharmaceuticals are prepared for sublingual administration. These commonly include cardiovascular drugs, steroids, barbituates, some enzymes and increasingly frequently, certain vitamins and minerals. Latin is an ancient Indo-European language originally spoken in the region around Rome called Latium. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... Oral medication A medication is a licenced drug taken to cure or reduce symptoms of an illness or medical condition. ...


The principle behind sublingual administration is fairly simple. When a chemical comes in contact with the mucous membrane, or buccal mucosa, it diffuses into the epithelium beneath the tongue. This region contains a high density of blood vessels, and as a result, via osmosis, the substance quickly enters the blood stream at the sublingual artery. Quickly thereafter, the substance is carried by blood flow to the connected lingual artery, which takes up the chemical and translates it to its source: the carotid artery. This artery is connected directly to the brain. The mucous membranes (or mucosae; singular: mucosa) are linings of ectodermic origin, covered in epithelium, and are involved in absorption and secretion. ... Buccal mucosa is mucous membrane of the inside of the cheek. ... In zootomy, epithelium is a tissue composed of a layer of cells. ... Osmosis is the diffusion of a liquid (most often assumed to be water, but it can be any liquid solvent) through a partially-permeable membrane from a region of low solvent potential to a region of high solvent potential. ... The lingual artery arises from the external carotid between the superior thyroid and external maxillary; it first runs obliquely upward and medialward to the greater cornu of the hyoid bone; it then curves downward and forward, forming a loop which is crossed by the hypoglossal nerve, and passing beneath the... The carotid artery is a major artery of the head and neck that supplies blood to the head and neck. ...


In theory, sublingual routes of administration have certain advantages over simple oral administration. This route is often faster, and entering a drug into one's body sublingually ensures that the substance will only come in contact with the enzymes in saliva prior to entry into the bloodstream. Drugs otherwise orally administered must instead survive the incredibly hostile environment of the gastrointestinal tract. This may mean a much greater percentage of the original substance is degraded either by the myriad of enzymes in the GI tract, such as monoamine oxidase, or the strong acids it contains. Additionally, after GI absorption, the drug is sent to the liver where the drug may be extensively metabolized; this is known as the first pass effect of drug metabolism. Due to the degradative qualities of the stomach and intestine, or the solubility of the GI tract, certain substances, such as salvinorin A may only be administered orally via the sublingual route. The gastrointestinal tract or digestive tract, also referred to as the GI tract or the alimentary canal or the gut, is the system of organs within multicellular animals which takes in food, digests it to extract energy and nutrients, and expels the remaining waste. ... Ribbon diagram of the enzyme TIM. TIM is catalytically perfect, meaning its conversion rate is limited, or nearly limited to its substrate diffusion rate. ... Monoamine oxidase Monoamine oxidases (singular abbreviation MAO) (EC 1. ... The liver is the largest internal organ of the human body. ... The first pass effect (or first pass metabolism) is a phenomenon of drug metabolism. ... Salvinorin A is the main active psychotropic constituent of the plant Salvia divinorum (diviners sage, Mexican mint). ...


Almost any form of substance is appropriate for sublingual administration, so long as in that form the substance can readily enter into solution with the saliva in the mouth. Chemicals prepared as powders, solutions, or even aerosol sprays may all make use of this method. However, a number of factors, such as pH, molecular weight, and lipid solubility (to name just a few) of a substance may determine whether the route is practical or not. Based on these properties, it is entirely possible that a drug, which will readily become a solution with saliva, simply diffuses too slowly (or not at all) in the buccal mucosa to be effective.


Psychoactives, too, may be applied sublingually. LSD, MDMA, morphine, and many other drugs including the psychedelic tryptamines and phenethylamines are all viable candidates for administration via this route. Most often, the drug in question is powdered and placed in the mouth (often directly under the tongue). If held there long enough, the drug will diffuse into the blood stream, bypassing the GI tract. This is definitely a preferred method to simple oral administration, because MAO is known to oxidize many drugs (especially the tryptamines such as DMT) and because this route translates the chemical directly to the brain, where most psychoactives act. However, this method is severely limited because only a small amount of the substance can be entered in this way, and often a large amount remains to be swallowed. For other uses, see LSD (disambiguation). ... ecstasy and religious ecstasy MDMA, most commonly known today by the street name ecstasy, is a synthetic entactogen of the phenethylamine family whose primary effect is to stimulate the brain to rapidly secrete large amounts of serotonin, causing a general sense of openness, empathy, energy, euphoria, and well-being. ... Morphine (INN) (IPA: ) is a powerful opioid analgesic drug and is the principal active agent in opium. ... Tryptamine (3-(2-aminoethyl)indole) is a monoamine compound that is widespread in nature. ... Phenethylamine (β-Phenylethylamine) is an alkaloid and monoamine. ... DMT is a three-letter acronym (TLA) which may stand for Desoxymethyltestosterone Digital Monetary Trust Dimethyltryptamine Discrete multitone modulation Discrete monitor timing (a VESA standard for computer displays) This is a disambiguation page — a navigational aid which lists other pages that might otherwise share the same title. ...


  Results from FactBites:
 
Effect of pH on Sublingual Absorption of Oxycodone Hydrochloride (2692 words)
The purpose of this study was to develop a sublingual spray drug delivery formulation of oxycodone for acute pain management, using rabbit as the animal model, and to evaluate the effect of formulation pH on the sublingual absorption of oxycodone.
Following sublingual spray administration, the bioavailability of formulation 1 and formulation 2 were obtained by comparing the mean AUC after intravenous and sublingual administration and were found to be 45.4% ± 20.1%, and 70.1% ± 17.9%, respectively (Figure 2).
Also, a sublingual formulation of oxycodone permits the use of lower doses of oxycodone for pain management, since a greater portion of the medication is absorbed directly into the bloodstream, thereby allowing a direct route to the afflicted target area.
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