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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: BenzocaineGeneric name: BenzocaineChemical name: Ethyl para-aminobenzoate
Trade name: NovocainGeneric name: ProcaineChemical name: 2-(diethylamino)ethyl 4-aminobenzoate
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.
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 Development- The Tranquilizer Librium
• The Tranquilizer Librium -another drug that was discovered accidentally.
Drugs as Enzyme Inhibitors
Penicillin destroys bacteria by inhibiting the enzyme thatsynthesizes bacterial cell walls:
One penicillinase inhibitor is a sulfone, which is easily prepared from penicillin by oxidizing the sulfur atom with a peroxyacid
Antiviral DrugsAntiviral drugs (antivirotics) are a class of medication used specifically for treating viral infectionViruses 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.
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.