PHM 338 Quiz 1

full agonist

full agonist

Ability of a drug to produce 100% of the maximum response regardless of the potency

agonism

production of a molecular/cellular response to an interaction between a molecule and a receptor that activates the receptor; can be a drug or endogenous ligand

body systems

groups of organs that perform specific functions in the human body; can see measurable actions; ex. beta-blockers --> reduces pulse rate

component tissues

beta-blockers --> negative chronotrope

cellular level

beta-blockers --> prevents elevation of cAMP

molecular level

beta-blockers --> competitive antagonism of norepinephrine to cardiac beta1 receptors

levels of drug activity

-body systems

-component tissues

-cellular level

-molecular level

replace

iron in anemia is an example of how drugs ________

interrupt

ipratropium slowing down mucus production is an example of how drugs __________

potentiate

to make more active; to strengthen; cathartics before sigmoidoscopy is an example of how drugs ___________

existing

drugs modify ______________ functions

multiple

drugs exert _______________ effects

ex. Minoxidil lowers blood pressure AND prevents hair loss

interact

drugs typically ____________ with something to exert an effect

pharmaceutics

The science of preparing and dispensing drugs, including dosage form design

dosage form

form in which drugs are manufactured; includes elixirs, tablets, capsules, suppositories, parenteral drugs, and transdermal systems

pharmacokinetics

The study of the absorption, metabolism, distribution, and elimination of drugs; "what the body does to the drug"

pharmacodynamics

the study of the action or effects of drugs on living systems; "what the drug does to the body"

schedule I drugs

• High Potential for abuse

• no medical use

• research protocol only

• may lead to severe dependence

• ex. heroin, marijuana, LSD, mescaline, peyote, ecstasy

schedule II drugs

• high abuse potential

• accepted medical use (ONLY DIFFERENCE FROM SCHEDULE I)

• may lead to severe dependence

• must be written on an official prescription form

• no refills

• ex. oxycodone, morphine, meperidine, cocaine, pentobarbital, amphetamine

schedule III drugs

• less abuse potential than I & II

• accepted medical use

• low/moderate physical dependence, high psychological dependence

• written/oral prescription

• 6 months of refills

• acetaminophen w/ codeine, buprenorphine (Suboxone), anabolic steroids, ketamine

schedule IV drugs

• less abuse potential than III

• accepted medical use

• limited dependence

• written/oral prescription

• 6 months of refills

• phenobarbital, diazepam (Valium), carisoprodol (Soma)

schedule V drugs

• less abuse potential than IV

• accepted medical use

• limited dependence

• may or may not require prescription

• codeine in limited quantities (cough syrup)

pharmaceutical equivalence & bioequivalence

generic drug approval criteria

pharmaceutical equivalence

medications that have the same active ingredients, dosage form, strength, route; may differ in shape, scoring, excipients (inactive ingredients)

bioequivalence

The rate and extent of absorption of drug are not significantly different from pioneer drug

80-125%

The bioequivalence of a generic drug must be at least _____________%

Pure Food and Drug Act of 1906

• protects public from adulterated/mislabeled drugs and food

• Requires drug companies to list if 1 of 11 dangerous/addicting drugs present

• Prohibits false/misleading claims about curative properties of drug on package

• Only drugs sold via interstate/international commerce were covered

• Designated The United States Pharmacopeia and National Formulary as official standards for strength and purity

Food, Drug, and Cosmetic Act of 1938

• Drug manufacturers must:

  • Test for harmful effects

  • Drug labels must be accurate and complete

Durham-Humphrey Amendment of 1952

Specified how prescription drugs can be ordered and dispensed

Kefauver-Harris Amendment of 1962

• Required proof of both safety and efficacy prior to approval

• Permitted generic versions of drugs initially marked from 1938-1962

Drug Price Competition and Patent Term Restoration Act of 1984

• Generics submit Abbreviated New Drug application

• Provides 5 years of market exclusivity for pioneer drugs

  • For development of new indications, dosage forms, dosage regimens

• Generics could be approved for drugs introduced after 1962

Controlled Substances Act of 1970

• Classifies controlled substances according to their abuse potentials

• Prescriptions are electronically transmitted to the DPS

  • Identify shady prescribers, potential abusers, diversion (pharmacies that order much more than what is distributed)

NDA

• Phase I

  • Initial pharmacologic evaluation

  • Small number of normal volunteers

• Phase II

  • Limited controlled evaluation

  • Increasing doses, pts with disease

  • Effectiveness and side effects

• Phase III

  • Extended clinical evaluation

  • Determines clinical effectiveness, drug safety, establishment of safe/effective dose

• Preclinical (6.5 years), Phase I (1.5 years), Phase II (2 years), Phase III (3.5 years), FDA review (1.5 years)

  • 5 enter trials → 1 approved

Phase I

• Initial pharmacologic evaluation

• Small number of normal volunteers

• 1.5 years

  • 5 enter trials

Phase II

• Limited controlled evaluation

• Increasing doses, pts with disease

• Effectiveness and side effects

• 2 years

Phase III

• Extended clinical evaluation

• Determines clinical effectiveness, drug safety, establishment of safe/effective dose

• 3.5 years

Phase IV

• FDA Review

• 1.5 years

• only 1 drug approved

ANDA

• 2 requirements:

• Pharmaceutical equivalence

  • Same active ingredients, dosage form, strength, route

  • May differ in shape, scoring, expedients

• Bioequivalence

  • Rate & extent of absorption are not significantly different from pioneer drug

  • AUC (total drug exposure in body), Cmax (concentration max), T max (time to reach Cmax)

plants, animals, microbes, minerals, synthetics, semi-synthetics, biosynthetics

sources of drugs

plants

• drug source

• aspirin - willow tree

• laudanum - opium poppy

animals

• drug source

• Insulin - cows/pigs

• Conjugated estrogens - horses

• Pepsin - cow stomach

• Fish oil - anchovies, sardines

• Antitoxin sera - diphtheria, tetanus

microbes

• drug source

• Penicillin - penicillium molds

• Dextran - lactobacillus family

minerals

drug source

• Ferrous sulfate - pts with iron deficiency anemia

• Magnesium sulfate - constipation

• Selenium - dandruff

synthetics

drug source

• Aspirin

• Antihistamines

• Anesthetics

• Fentanyl

semi-synthetics

drug source

• Ampicillin - from penicillin

biosynthetics

drug source

• Hepatitis B vaccine (yeast), recombinant insulin (bacteria)

primary reference

• Clinical research studies

• Provides most recent information

• Requires longer time commitment and skilled expertise in literature evaluation to assess application to patient care

• Ex. New England Journal of Medicine, Clinical Nursing Research

secondary reference

• Databases used to search for primary literature

  • Ex. Medline database

tertiary reference

• Summarizes, evaluates, or interprets primary sources

• Ex. textbooks, journal review articles, clinical guidelines, databases (Daily Med, Orange Book), Compendia (Davis’s Nursing Drug Guide)

plants

most common drug source