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Pivmecillinam
Pivmecillinam (INN) or amdinocillin pivoxil (USAN, trade names Selexid, Penomax and Coactabs) is an orally active prodrug of mecillinam, an extended-spectrum penicillin antibiotic. Pivmecillinam is the pivaloyloxymethyl ester of mecillinam. Pivmecillinam is only considered to be active against Gram-negative bacteria, and is used primarily in the treatment of lower urinary tract infections. In the Nordic countries, it has been widely used in that indication since the 1970s. It has been proposed as the first-line drug of choice for empirical treatment of acute cystitis. It has also been used to treat paratyphoid fever and shigellosis. Activity Adverse effects The adverse effect profile of pivmecillinam is similar to that of other penicillins. The most common side effects of mecillinam use are rash and gastrointestinal upset, including nausea and vomiting. Retrieved on August 31, 2008. Prodrugs that release pivalic acid when broken down by the body — such as pivmecillinam, pi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pivampicillin
Pivampicillin is a pivaloyloxymethyl ester of ampicillin. It is a prodrug, which is thought to enhance the oral bioavailability of ampicillin because of its greater lipophilicity compared to that of ampicillin. Adverse effects Prodrugs that release pivalic acid when broken down by the body—such as pivampicillin, pivmecillinam, and cefditoren pivoxil—have long been known to deplete levels of carnitine. This effect is not due to the drug itself but to pivalate, which is mostly removed from the body by forming a conjugate with carnitine. Although short-term use of these drugs can cause a marked decrease in blood levels of carnitine, it is unlikely to be of clinical significance; long-term use, however, is not recommended. Availability Worldwide, pivampicillin is only available in Denmark, where it is sold as Pondocillin® by PharmaCoDane, or Miraxid® by LEO Pharma LEO Pharma A/S is a multinational Danish pharmaceutical company, founded in 1908, with a presence in about 100 co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mecillinam
Mecillinam (INN) or amdinocillin (USAN) is an extended-spectrum penicillin antibiotic of the amidinopenicillin class that binds specifically to penicillin binding protein 2 (PBP2), and is only considered to be active against Gram-negative bacteria. It is used primarily in the treatment of urinary tract infections, and has also been used to treat typhoid and paratyphoid fever. Because mecillinam has very low oral bioavailability, an orally active prodrug was developed: pivmecillinam. Medical uses Mecillinam is used in the treatment of infections due to susceptible gram-negative bacteria, especially urinary tract infections which are most commonly caused by ''Escherichia coli''. Mecillinam is active against most pathogenic Gram-negative bacteria, except ''Pseudomonas aeruginosa'' and some species of ''Proteus''. Retrieved on August 31, 2008. Freely available with registration. Several studies have also found it to be as effective as other antibiotics for treating ''Staphylococcus sa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mecillinam
Mecillinam (INN) or amdinocillin (USAN) is an extended-spectrum penicillin antibiotic of the amidinopenicillin class that binds specifically to penicillin binding protein 2 (PBP2), and is only considered to be active against Gram-negative bacteria. It is used primarily in the treatment of urinary tract infections, and has also been used to treat typhoid and paratyphoid fever. Because mecillinam has very low oral bioavailability, an orally active prodrug was developed: pivmecillinam. Medical uses Mecillinam is used in the treatment of infections due to susceptible gram-negative bacteria, especially urinary tract infections which are most commonly caused by ''Escherichia coli''. Mecillinam is active against most pathogenic Gram-negative bacteria, except ''Pseudomonas aeruginosa'' and some species of ''Proteus''. Retrieved on August 31, 2008. Freely available with registration. Several studies have also found it to be as effective as other antibiotics for treating ''Staphylococcus sa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pivaloyloxymethyl
Pivaloyloxymethyl (POM, pivoxil, pivoxyl) is a protecting group used in organic synthesis.''Protective Groups in Organic Synthesis'', 3rd Edition, Theodora M. Greene and Peter G. M. Wuts, The POM radical has the formula (CH3)3C-CO-O-CH2. The POM group is also sometimes used to produce prodrugs. For example, the POM group can be attached to a negatively charged organophosphate group(s) of a drug causing a neutralization of the negative charge, which can allow the drug to become more lipid-soluble and thus more able to diffuse passively across cell membranes into cells. Upon entry into cells, the POM portion of the molecule can be removed by cellular processes resulting in release of active drug. Clinically used prodrugs containing pivaloyloxymethyl groups include adefovir dipivoxil, pivampicillin, cefditoren pivoxil, pivmecillinam, and valproate pivoxil. Tenofovir disoproxil contains a very similar prodrug group. See also * Pivalic acid Pivalic acid is a carboxylic acid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydrolysis
Hydrolysis (; ) is any chemical reaction in which a molecule of water breaks one or more chemical bonds. The term is used broadly for substitution reaction, substitution, elimination reaction, elimination, and solvation reactions in which water is the nucleophile. Biological hydrolysis is the cleavage of biomolecules where a water molecule is consumed to effect the separation of a larger molecule into component parts. When a carbohydrate is broken into its component sugar molecules by hydrolysis (e.g., sucrose being broken down into glucose and fructose), this is recognized as saccharification. Hydrolysis reactions can be the reverse of a condensation reaction in which two molecules join into a larger one and eject a water molecule. Thus hydrolysis adds water to break down, whereas condensation builds up by removing water. Types Usually hydrolysis is a chemical process in which a molecule of water is added to a substance. Sometimes this addition causes both the substance and w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Paratyphoid Fever
Paratyphoid fever, also known simply as paratyphoid, is a bacterial infection caused by one of the three types of ''Salmonella enterica''. Symptoms usually begin 6–30 days after exposure and are the same as those of typhoid fever. Often, a gradual onset of a high fever occurs over several days. Weakness, loss of appetite, and headaches also commonly occur. Some people develop a skin rash with rose-colored spots. Without treatment, symptoms may last weeks or months. Other people may carry the bacteria without being affected; however, they are still able to spread the disease to others. Typhoid and paratyphoid are of similar severity. Paratyphoid and typhoid fever are types of enteric fever. Paratyphoid is caused by the bacterium ''Salmonella enterica'' of the serotypes Paratyphi A, Paratyphi B, or Paratyphi C growing in the intestines and blood. They are usually spread by eating or drinking food or water contaminated with the feces of an infected person. They may occur when a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Penicillins
Penicillins (P, PCN or PEN) are a group of β-lactam antibiotics originally obtained from ''Penicillium'' moulds, principally '' P. chrysogenum'' and '' P. rubens''. Most penicillins in clinical use are synthesised by P. chrysogenum using deep tank fermentation and then purified. A number of natural penicillins have been discovered, but only two purified compounds are in clinical use: penicillin G (intramuscular or intravenous use) and penicillin V (given by mouth). Penicillins were among the first medications to be effective against many bacterial infections caused by staphylococci and streptococci. They are still widely used today for different bacterial infections, though many types of bacteria have developed resistance following extensive use. 10% of the population claims penicillin allergies but because the frequency of positive skin test results decreases by 10% with each year of avoidance, 90% of these patients can tolerate penicillin. Additionally, those with ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carnitine
Carnitine is a quaternary ammonium compound involved in metabolism in most mammals, plants, and some bacteria. In support of energy metabolism, carnitine transports long-chain fatty acids into mitochondria to be oxidized for energy production, and also participates in removing products of metabolism from cells. Given its key metabolic roles, carnitine is concentrated in tissues like skeletal and cardiac muscle that metabolize fatty acids as an energy source. Generally individuals, including strict vegetarians, synthesize enough L-carnitine in vivo. Carnitine exists as one of two stereoisomers (the two enantiomers -carnitine (''S''-(+)-) and -carnitine (''R''-(−)-)). Both are biologically active, but only -carnitine naturally occurs in animals, and -carnitine is toxic as it inhibits the activity of the -form. At room temperature, pure carnitine is a whiteish powder, and a water-soluble zwitterion with relatively low toxicity. Derived from amino acids, carnitine was first extracte ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cefditoren Pivoxil
Cefditoren, also known as cefditoren pivoxil is an antibiotic used to treat infections caused by Gram-positive and Gram-negative bacteria that are resistant to other antibiotics. It is mainly used for treatment of community acquired pneumonia. It is taken by mouth and is in the cephalosporin family of antibiotics, which is part of the broader beta-lactam group of antibiotics. Structure Like other cephalosporins, cefditoren has a β-lactam ring at the 7 position of cephalosporin ring that is responsible for its inhibitory action on bacterial cell wall synthesis. In addition to the cephem nucleus common to all cephalosporins, cefditoren has an aminothiazole group that enhances its activity against Gram-negative organisms, a methylthiazole group that enhances its activity against Gram-positive organisms, a methoxyimino group that gives it stability against β-lactamases, and a pivoxil ester group that enhances oral bioavailability. Antimicrobial activity The spectrum of cefdi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pivalic Acid
Pivalic acid is a carboxylic acid with a molecular formula of (CH3)3CCO2H. This colourless, odiferous organic compound is solid at room temperature. A common abbreviation for the pivalyl or pivaloyl group (''t''-BuC(O)) is Piv and for pivalic acid (''t''-BuC(O)OH) is PivOH. Preparation Industrial route Pivalic acid is prepared by hydrocarboxylation of isobutene via the Koch reaction: :(CH3)2C=CH2 + CO + H2O → (CH3)3CCO2H Such reactions require an acid catalyst such as hydrogen fluoride. ''tert''-Butyl alcohol and isobutyl alcohol can also be used in place of isobutene. Globally, several million kilograms are produced annually. Pivalic acid is also economically recovered as a byproduct from the production of semisynthetic penicillins like ampicillin and amoxycillin. Laboratory methods It was originally prepared by the oxidation of pinacolone with chromic acid and by the hydrolysis of ''tert''-butyl cyanide. Convenient laboratory routes proceed via ''tert''-butyl chloride via ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vomiting
Vomiting (also known as emesis and throwing up) is the involuntary, forceful expulsion of the contents of one's stomach through the mouth and sometimes the Human nose, nose. Vomiting can be the result of ailments like Food-poisoning, food poisoning, gastroenteritis, pregnancy, motion sickness, or hangover; or it can be an after effect of diseases such as brain tumors, elevated intracranial pressure, or overexposure to ionizing radiation. The feeling that one is about to vomit is called nausea; it often precedes, but does not always lead to vomiting. Impairment due to Alcoholic drink, alcohol or anesthesia can cause inhalation of vomit, leading to suffocation. In severe cases, where dehydration develops, intravenous fluid may be required. Antiemetics are sometimes necessary to suppress nausea and vomiting. Self-induced vomiting can be a component of an eating disorder such as bulimia nervosa, bulimia, and is itself now classified as an eating disorder on its own, purging di ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
