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Analgesics Analgesics Analgesics are common pain relievers. Some analgesics also have antipyretic properties as well. They can be used to reduce fever. Some analgesics are also antiinflammatory drugs. They reduce inflamation as well 2 Classification of Analgesics Analgesics Strong Analgesics Mild Analgesics Aspirin Ibuprofen Acetaminophen Opium Heroin Codeine 3 Mild Analgesics Mild Analgesics include many over-the-counter pain relievers and fever depressants. Examples of mild analgesics include aspirin, acetaminophen, and ibuprofen. 4 Mechanism of Mild Analgesics The mechanism by which mild analgesics act is still controversial. It is believed that they inhibit the formation of prostaglandins at the site of the injury. Prostaglandins are involved in the transmission of pain signals to the brain 5 Aspirin Aspirin is a derivative of salicyclic acid Salicyclic acid was found in the bark of the willow tree and was used as a pain reliever and as a way to relieve fever symptoms of malaria. Aspirin Salicyclic Acid 6 Aspirin In 1899, Felix Hoffman, a chemist from the Bayer Company, developed a lowcost process to synthesize an ethanoate ester of salicyclic acid, called aspirin In the synthesis of aspirin, the ethanoic acid forms an ester with the alcohol group on the second carbon 7 Aspirin As a mild analgesic, aspirin is believed to inhibit the enzyme, Prostaglandin Synthase which is formed at the site of an injury. This inhibits the production of prostaglandins which produce fever and swelling as well as transmitting pain signals to the brain. 8 Aspirin -- Uses and Benefits Aspirin is able to reduce pain and fevers and dilate blood vessels Aspirin enlarges blood vessels which helps prevent blood clots. This vasodilation of the surface blood vessels also allows an increase of heat released which lowers the temperature of a fever Aspirin is also taken to prevent recurring heart attacks It may also be effective in preventing prostate cancer 9 Side Effects of Aspirin Aspirin can irritate the stomach lining which may lead to ulcers If aspirin is used over long periods of time, it may lead to problems with blood clotting An overdose on aspirin, such as the case with some arthritis sufferers, may lead to dizziness, ringing in the ears, gastrointestinal problems, mental confusion, and bleeding. Some people are allergic to aspirin leading to bronchial asthma In children under 12 Aspirin has been linked10 Antibacterial and Antiviral Drugs 11 Antibacterials Bacteria Definition Replication Shapes Diseases Antibacterials 1. 2. 3. 4. 1. 2. Penicillin Discovery of Synthesis Structure Ways it functions General Antibacterials Problems Possible solutions 12 Characteristics of Bacteria Single celled or non- cellular Spherical,spiral or rod–shaped organisms Lack chlorophyll Reproduce by fission Important as pathogens and for biochemical properties. 13 Infectious Bacteria Cocci – Sphericial Often cause sore throats and pneumonia Bacilli – Rod shaped Mycolbacterium cause tuberculosis Spirochete – Spiral shaped Syphilis, gum infections 14 Structure of a Bacterium Capsule – Protective layer of bacteria. made of proteins, sugars, and lipids Cell wall – Provides the bacteria with its shape and structure. Cell membrane – permeable membrane that transfers nutrients and chemicals in and out of the cell. Cytoplasm – Liquid within the cell which serves to protect cell parts as well as move materials throughout the cell. Contains glycogen, lipids and other nutrients Ribosomes – synthesizes proteins. DNA – Single chromosome controls the functions of the cell. Flagella – A tail-like appendage used for movement. Pilus – Small hairs whose purpose is to stick to surfaces. Can also be used in reproduction. 15 Structure a Bacterium Bacteria can be either aerobic or anaerobic Aerobic:-- require oxygen for metabolism. They are more likely to infect surface areas such as the skin and the respiratory tract. Anaerobic – multiply in oxygen free and in low oxygen surroundings such as the intestines. 16 Replication by Binary Fission One cell is split into two separate cells. 17 Bacterial Caused Diseases Anthrax Cholera Plague Q-Fever Strep Throat Staph Infections Tuberculosis 18 The Discovery of Penicillin Penicillin was discovered in 1929 by scientist Alexander Fleming. He left for vacation with an agar plate covered with the bacteria Staphylococcus aureus. When he returned he noticed that the fungus, Penicillium, had grown on the plate The bacteria colony surrounding the fungus had become transparent because the bacterial cells had undergone lysis. 19 Development of Penicillin Several years later Howard Florey and E.B. Chain stumbled across Fleming’s research papers and were intrigued by his findings. They were convinced that Flemming’s discovery could save a lot of lives, prevent pain, and make it much easier to fight infectious diseases and prevent other infections. They developed a way to mass produce penicillin making it available to soldiers wounded in world war II. Florey and Chain were awarded the Nobel Prize in 1945 for their work on penicillin. 20 Penicillin Structure Penicillins have a special structure that allows them to interfere with the formation of the cell wall when bacteria reproduce The general structure of penicillin 21 How Does it Function? Penicillin prevents the cross linking of small peptide chains in peptidoglycan, which is the main polymer in bacterial cell walls. They do not affect bacteria which already exist, rather Penicillin’s affect the synthesis of new bacteria. The new bacteria grow without the ability to maintain cell rigidity, making them susceptible to osmotic lysis. 22 The Action of Penicillins The amide group in the beta lactam is more reactive due to the strained ring. The structure of the beta lactam is similar to the structures of cysteine and valine. The beta lactam binds to the enzyme that synthesizes the cell wall in bacteria, blocking its action. As a result the bacteria rupture and break and cannot reproduce. Note the similarities in structure to the beta lactam. 23 Bacterial Immunity to Penicillin Antibiotic Resistance – Mutated bacteria which are immune to antibiotics are more likely to survive when excessive antibacterials are used. Bacteria develop enzymes known as penicillinases that destroy or render penicillin ineffective. New antibiotics are developed by changing the R group side chain. 24 Structure of Penicillin Penicillin is a group of compounds which all contain the same basic ring structure, known as beta-lactam. It is comprised of two amino-acids (valine and cyteine) through a tripeptide intermediate. The third amino acid (the R group) is replaced by another group, which gives different characteristics to differing penicillins. 25 Narrow Range and Broad Range Antibiotics Narrow range antibiotics target specific kinds of bacteria. They are usually more potent. Broad range antibiotics are effective against a wide range of bacteria. When doctors diagnose patients suspected of having bacterial infections, they must first take samples of body fluids, and try to determine the precise type of infection. A broad range antibiotic might be prescribed initially. Once a bacterial infection is properly diagnosed it may be appropriate to switch to a narrow range antibiotic. 26 Overuse of Penicillin Leads to greater immunity of bacteria to penicillin, since the strongest and most resistant strains survive. Greater doses of penicillin are required to be effective Danger of developing super bacteria Kill beneficial bacteria as well as harmful bacteria 27 Penicillin Synthesis A sterilized growth medium and an inoculum of strongly growing hyphae is added to stainless steel fermenters. The fermenters stirred continuously and glucose, nitrate and sterile air are periodically added. 28