Dr. Steven I. Dworkin
How are Drugs Named?• Chemical Name
– Specifies chemical structure• Pre patent or release name
– Typically drug company letters and numbers• Generic Name
– Nonproprietary name (each drug has only one generic name)
• Brand or Trade Name– Market name for a particular company
• Common or Street Name– Users name
Dr. Steven I. Dworkin
What’s in a Name
Chemical Name Generic Name Trade Name
N-(4-hydroxyphenyl) acetamide Acetaminophen Tylenol
7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one
Diazepam Valium
4-[4-(p-chlorophenyl)-4-hydroxypiperidino]-4'-fluorobutyrophenone
Haloperidol Haldol
5-thia-1-azabicyclo [4.2.0]-oct-2-ene-2 carboxylic acid, 7-[(aminophenylacetyl)amino]-3-methyl-8-oxo-, monohydrate
Cephalexin Keflex, Keforal, Keftabs
DL-threo-2-(methylamino)-1-phenylpropan-1-ol
Pseudoephedrine Sudafed
N''-cyano-N-methyl-N'-[2-[[(5-methyl-1H-imidazol-4-yl) methyl]thio]ethyl]guanidine
Cimetidine Tagamet
Dr. Steven I. Dworkin
Rose
Chemical Name isobutylphenyl propionic acid
In-house name
Generic Name ibuprofen
Brand Names Advil, Children's Advil/Motrin, Medipren, Motrin, Nuprin, Pediacare Fever etc
Street Non-asprin headache reliever
ibuprofen (ī'byūprō'fən) , nonsteroidal anti-inflammatory drug (NSAID) that reduces pain, fever, and inflammation. Along with naproxen and ketoprofen, ibuprofen belongs to the propionic acid class of NSAIDs. It was first made available in 1967. Like other NSAIDs, it acts by inhibiting the body's production of prostaglandins. Available over the counter in a variety of preparations (e.g., Advil, Motrin, Nuprin), it is commonly used to treat rheumatoid arthritis, gout, and painful menstruation. Side effects include rash, alteration of platelet function and bleeding, and intestinal upset, which can lead to gastritis. Like other NSAIDS, it appears to have no potential for abuse or physical dependence. It should not be used by those who are allergic to aspirin.
Dr. Steven I. Dworkin
Classification of Drugs
• Grouping by chemical structure.
Specific Examples
Core Structure Generic Name Trade Name
Tetracyclines Doxycycline Vibramycine
Corticosteroids Prednisone Meticorten
Benzodiazepines Diazepam Valium
Dr. Steven I. Dworkin
Classification of Drugs
• Mechanism of action
– Serotonin uptake inhibitors
• antidepressants
– beta blockers
• Anti-hypertensives
– H2 blockers
• Anti-histamines
Dr. Steven I. Dworkin
Drug Classification
• Therapeutic Categories and Subcategories
Therapeutic Category Examples of Subcategories
Analygesics NSAIDs
Opioids
Antibiotics Tetracyclines
Penicillins
Cephalosporins
Antihypertensive –Blockers
Diuretics
ACE Inhibitors
Anti-inflammatory drugs NSAIDs
Corticosteroids
Asthma Drugs –Blockers
Corticosteroids
Leukotriene modifiers
Dr. Steven I. Dworkin
Drug Classification
Classification Characteristics
OTC drugs Drugs that do not require a prescription. May contain a lower dose of a prescribed compound,
Prescription drugs Greater potential for adverse effects. Untoward drug interactions may occur. Use is monitored by a physician.
Controlled Substances Schedules drugs evaluated for abuse liability. More restrictive requirements regarding distribution, storage, and record keeping
Dr. Steven I. Dworkin
The Feds
Year Act Purpose Comment
1906 Federal Pure food act
Prohibit adulteration and misbranding of medications
USP standards established for ingredients. Drug did not have to be safe or effective
1938 Drug and Cosmetic Act
Required safety of new drug approval by FDA
Start of NDA process
1952 Durham-Humphrey Amendment
Differentiated prescription and nonprescription
Drugs unsafe without medical supervision required prescription, refill restriction
1962 Kefauver-Harris Amendment
Required effectiveness of prescription and nonprescription approval by FDA
Drugs developed between 1938-1962 included
1970 Comprehensive Drug Abuse Act
Established Categories for drugs with abuse potential.
DEA to enforce the act
Dr. Steven I. Dworkin
Pre Clinical Trials• In vitro studies• In vivo studies
– Use of standard animal models• Efficacy• Potency• Safety• LD determination• ED determinations
– Therapeutic Ratio• Abuse Potential or Liability
– Drug self-administration
Dr. Steven I. Dworkin
Clinical Trials
• Introduction– Before a pharmaceutical company can initiate testing in humans, it must
conduct extensive preclinical or laboratory research. • Preclinical research typically involves years of experiments in animal
and human cells. The compounds are also extensively tested in animals.
• 100-300k compounds screens 100-300 compounds 1 or 2 lead compounds
• Pharmaceutical company provides selected data to the Food and Drug Administration (FDA) with a requesting approval to begin testing the drug in humans.
• This is called an Investigational New Drug application (IND).• Typically this is when the clock starts clicking and the PC has the
next 11 years of exclusive patent rights.
Dr. Steven I. Dworkin
Phase Purpose Subjects Duration Outcome
Phase I how drug absorbed, metabolized, and excreted and side effects over range of doses
healthy volunteers (20 to 100), who are usually paid for participating in the study.
several months 70 percent of experimental drugs pass this initial phase of testing
Phase II determine relative safety of the new drug, and its effectiveness.
.
several hundred patients randomized trials, drug vs control often blinded.
several months to two years 33 percent of experimental drugs successfully complete both phase I and phase II studies
Phase III provide drug company and the FDA with a more thorough understanding of the drug's effectiveness, benefits, and the range of possible adverse reactions.
several hundred to several thousand patients., most phase III studies are randomized and blinded trials.
several years Seventy to 90 percent of drugs that enter phase III studies successfully complete this phase of testing FDA approval for market
ing the drug.
Phase IV objectives: (1) studies often compare a drug with other drugs already in the market; (2) studies are often designed to monitor a drug's long-term effectiveness and impact on a patient's quality of life; and (3) many studies are designed to determine the cost-effectiveness of a drug therapy relative to other traditional and new therapies.
Dr. Steven I. Dworkin
Issues
• The New Drug War (non-US markets)• Involvement of Pharmaceutical Companies• Involvement of Interest Groups• Role of advisory panel• Role of FDA officials• Publication and disclosure of negative findings• When things go wrong?
– Cox-2 inhibitors• Media
– Steroids– Alternative Medications
Dr. Steven I. Dworkin
Questions
• Why are drugs categorized?• What are the major differences between name brand and generics
drugs?• Approximately how many drugs are tested for every drug that is
approved ?• What federal agency is responsible for determining the safety and
efficacy of new pharmaceuticals?• What federal agency is responsible for enforcing the regulations for
scheduled compounds• What are the basic differences between OTC and prescription drugs?• Under what conditions can a schedule I drug be prescribed for a
patient.• Name 2 Schedule II and 3 Schedule III compounds, what is one major
difference between these compounds (difference of Schedule II compared to Schedule III) ?
• Who is responsible for the appropriate use of a compound?