BIOPHARMACEUTICAL AND BIOPRODUCTS BY PUAN AZDUWIN BINTI KHASRI 6 DECEMBER 2012 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. 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. 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 para- aminobenzoate Trade name: Novocain Generic name: Procaine Chemical 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. 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. 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 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.

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: Penicillin destroys bacteria by inhibiting the enzyme that synthesizes bacterial cell walls:

12 Bacteria develop resistance to penicillin by secreting penicillinase, which destroys penicillin: Bacteria develop resistance to penicillin by secreting penicillinase, which destroys penicillin:

One penicillinase inhibitor is a sulfone, which is easily prepared from penicillin by oxidizing the sulfur atom with a peroxyacid

14 Mechanism of Penicillinase Inhibition by Sulfone

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 (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. 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.

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