Evolution of Medicinal Drugs

Medicinal Origins

Legislation & Regulation

Drug Testing & Approval

Introduction *Historical Trends

Major Areas of Pharmacology

Pharmacology is a science that studies the effects of drugs within a living system.

Toxicology concerned with the harmful effects of drugs

Pharmacy the study of preparing and dispensing medications and a place.

Pharmacotherapeutics how drugs are used in the treatment of disease.

Pharmacodynamics Pharmacokinetics

Basic Terminology

Adverse Effect Agonist Antagonist Chemical Name Contraindications Dose Drug Drug indication

Generic name Mechanism of action OTC Pharmacology Receptor Side effect Site of action Trade name

Substance Misuse & Abuse Terms

Drug Misuse Substance Abuse Drug Abuse Physical Dependence Psychological

Dependence Addiction Illicit Drugs

Diagnostic Statistical Manual –IVfor Substance Dependence

At least three symptoms in 12 months: Tolerance Withdrawal Use beyond intention Inability to reduce usage Time-consuming Valued activities abandoned or reduced Use continues despite problems

DSM-IV Criteria for Substance Abuse

One or more of the following in 12 months: Substance use repeatedly leads to failure to

fulfull home, work, or school responsibilities Repeated substance use in physically

hazardous situations Repeated legal problems for substance use Continued use despite resulting, repeated

social or interpersonal problems.

Medicines that Changed the World

Medicines that Changed the World

Opium– Sedative/painkiller

Smallpox vaccine 19thC– 1798 vax prevent illness

Salvarsan (arsphenamine) – 1910 20th cent-cure illness– Syphillis spirochete

Insulin– 1920– Few other drugs have

helped so many so fast!

Psychopharmacology ’50s– Drugs can treat mental illness

Enovid ’60s – 1960 The’PILL’– Alter normal physio process

Thalidomide– 1950’s birth defects– Prompted radical changes in

regulation of medicines– 1990 reemerged (MS, leprosy)

Reasons for Medication Use

Prevention Vaccines Antimalaria agents Antibiotic prophylaxis

Curative Antibacterial Oncology drugs Antifungal

Control of Disease Process

Antihypertensives Antidiabetics Thyroid agents

Palliation Analgesics Oncology drugs

Reasons for Different Routes of Administration

Convenience Preferred route is unavailable Rapid onset of action is desired Target delivery of drug to specific site of action Prolong duration of action

DosageRoutes Forms

Oral (by mouth)– Swallowed, SL, Buccal

Parenteral (injection)– IV,IM,SQ, ICranial,

epidural, Intraperitoneal Topical

– Applied to surface of skin or mucous membranes- Transdermal

– Respiratory: inhaled, intra-nasal, smoke, volatile gases

Tabs, caps, sol, elix, susp, lozenges, ’take a powder!’

Solutions & suspensions Ung, crm, ltn, otic, opth,

inhalants, suppos Rectal/vaginal Nasogastral

Plants Cinchona Bark

Purple Foxglove

Poppy (Opium)

Quinidine

Digitalis

Morphine Codeine

Anti Arrthymic

Cardiotonic

Analges/Antitussive

Minerals Magnesium

Zinc

Gold/Silver

MOM

ZnOxide

Auranofin/SilverNitr

Antacid/Laxative

Skin Protectant

RA/Anti-infective

Animals Pancreas Cow/Hog

Stomach Cow/Hog

Thyroid glands

Insulin

PepsinThyroid,USP

Antidiabetic

Digestive enzyme

Hormone

Synthetic Meperidine

Diphenoxylate

Co-Trimoxazole

Omeprazole

Demerol

Lomotil

Bactrim/Septra

Prilosec

Analgesic

Anti-diarrhea

Anti-Infective

Gastric acid inhibitor

Bioengineer Erythropoietin Epogen RBC Stimulant

Legend Drugs Over-the-Counter

Prescription ONLY Legend Statement

– ‘Federal law prohibits dispensing of this drug without a prescription’

Transfer Warning– ‘State or federal law

prohibits the transfer of this drug to any person other than the person to whom it was prescribed’

Prescription is not required

– Safe,effective– Taken w/o medical

supervision– Dose low (Why?)

– Negligible abuse potential Maybe????

Atomic(molecular) composition

Chemical Name Structural Formula Nonproprietary Name

(generic)– Stems & classes

Therapeutic class …pril

Proprietary Name (brand)

NDC #

Drug Names & Classifications

Drug Legislation & Regulation

FDAFDA Food & Drug Administration

FTCFTC Federal Trade Commission

DEADEA Drug Enforcement Agency

Controlled Substances Act

Schedule I– Heroin,THC

Schedule II– Methadone

Schedule III– Valium, Vicodin

Schedule IV– Alprazolam, Darvocet

Schedule V– Lomotil

Phases of Clinical Trials

Drug Testing & ApprovalClinical Trials

10-15 years from lab to US patients Only 1 in 5000 cmpds make it to human testing Only 1 in 5 tested in humans is approved Testing Phases (double blind, placebo controlled)

Phase I-lab animals, safety, 6 yr/5000 cmpds Phase II-hlthy,(50-100), dose, safe, PK, 2 yr/5cmpd Phase III-treat ill(100-500),SE, PD, dose curve, 2yr Phase IV-treat ill(1000-5000), LT use, special grps

FDA Phase IV

File NDA at FDA Review process &

approval (or not)

Year 1 or more

Post Marketing Surveillance

Additional testing as required by the FDA

Continuous monitoring of drug in public use

Generic Medications

Patent for 17 years on parent compound

Expires! Law suits? Open season for

manufacturers to capture the generic market on that particular drug

FDA Pregnancy Safety Categories

Category A adequate studies indicate no risk to the fetus in the 1st trimester & no evidence of risk in later trimesters.

Category B animal reproduction studies have not demonstrated a risk to fetus, but no well controlled human studies.

Category C animal studies report adverse effect on fetus, no human studies, benefit/risk.

FDA Pregnancy Safety cont.

Category D there is evidence of human fetal risk, but the potential benefits from the use of the drug may be acceptable if safer drugs are not available or ineffective.

Category X studies in animal or humans demonstrate fetal abnormalities or adverse reaction reports indicating fetal risk. Risk outweighs any benefit. These drugs should not be used in pregnant women.

Summary Slide