BIOPHARMACEUTICAL AND BIOPRODUCTS BY PUAN AZDUWIN BINTI KHASRI 6 DECEMBER 2012 INTRODUCTION • A drug is any absorbed substance that changes or enhances a physical or psychological function in the body. • A drug can be a gas, a liquid, or a solid. • Drugs have been used by humans for thousands of years to alleviate pain and illness. NAMING DRUGS • The most accurate names of drugs are the chemical names that define their structures. • A proprietary name (trade name or brand name) identifies a commercial product and distinguishes it from other products. • Each drug is also given a generic name that any pharmaceutical company can use to identify the product. EXAMPLE OF DRUGS Trade name: Benzocaine Generic name: Benzocaine Chemical name: Ethyl paraaminobenzoate Trade name: Novocain Generic name: Procaine Chemical name: 2(diethylamino)ethyl 4aminobenzoate LEAD COMPOUNDS • The goal of the medicinal chemist is to find compounds that have potent effects on given diseases, with minimum side effects. • A naturally occurring drug can serve as a prototype (lead compound). • Analogs of the lead compound are synthesized in order to find one that might have improved therapeutic properties or fewer side effects. • Changing the structure of the lead compound is called molecular modification. MOLECULAR MODIFICATION-COCAINE • Lead compound: Cocaine is a highly effective local anesthetic, but it produces disturbing effects on the central nervous system(CNS). • Improved: Retains the local anesthetic property without CNS effects. Molecular Modification Anesthetics Analgesics RANDOM SCREENING • A random screen, also known as a blind screen,is a search for a pharmacologically active compound without having any information about which chemical structures might show activity. • An important part of random screening is recognizing an effective compound Serendipity in Drug DevelopmentThe Tranquilizer Librium • The Tranquilizer Librium -another drug that was discovered accidentally. Structural modification of Librium led to the generation of other tranquilizers: Drugs as Enzyme Inhibitors Penicillin destroys bacteria by inhibiting the enzyme that synthesizes bacterial cell walls: Bacteria develop resistance to penicillin by secreting penicillinase, which destroys penicillin: 12 One penicillinase inhibitor is a sulfone, which is easily prepared from penicillin by oxidizing the sulfur atom with a peroxyacid Mechanism of Penicillinase Inhibition by Sulfone 14 Antiviral Drugs Antiviral drugs (antivirotics) are a class of medication used specifically for treating viral infection Viruses are smaller than bacteria. A virus consists of nucleic acid—either DNA or RNA— surrounded by a coat of protein. Most antiviral drugs are analogs of nucleosides, interfering with DNA or RNA synthesis. ANTIVIRAL DRUGS Type of antiviral drugs • Acyclovir : can fool the virus into incorporating it instead of guanine into the virus’s DNA. • Cytarabine: used for acute myelocytic leukemia, competes with cytosine for incorporation into viral DNA. • Ribarvirin :is a broad-spectrum antiviral agent that inhibits viral mRNA synthesis • Idoxuridine: for the topical treatment of ocular infections (U.S only), it is used for herpes infections in other countries. THE END