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PDA Exam 2, Part 1
Drugs as Therapeutic Agents
41
Pharmacology
Professional
02/13/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
What stimulated passage of the Pure Food and Drug Act of 1906?
Definition
Journalists publishing unhygenic conditions in the food industry
Term
What was the effect of the Pure Food and Drug Act of 1906?
Definition
Prevention of adulteration and mislabling

(No effect on safety/efficacy)
Term
What was the effect of the Harrison Narcotic Act of 1914?
Definition
Registration of people handling narcotics and the purchase of a tax stamp

Required prescription, so even doctors couldn't treat "addiction"
Term
What government entity regulated marijuana sales first?
Definition
States regulated before the Feds

(Tax act passed in 1937, considered a narcotic)
Term
What was the effect of the Controlled Substances Act of 1970?
Definition
Created schedules to rank drugs by the potential to cause abuse or dependency

("War on Drugs" has waxed and waned)
Term
What stimulated passage of the Food, Drug, and Cosmetics Act of 1938?
Definition
Sulfanilamide tragedy

(Massengill made an elixer using poisonous ethylene glycol as a solvent, 100 people died)
Term
What was the effect of the Food, Drug, and Cosmetics Act of 1938?
Definition
Mandated testing for drug safety (not efficacy)
Term
What stimulated passage of the Harris-Kefauver amendment of 1962?
Definition
Thalidomide disaster

(Medicine for morning sickness caused horrible birth defects)
Term
What was the effect of the Harris-Kefauver amendment of 1962?
Definition
Mandated that toxicological studies should be done and efficacy should be proven

Mandated standards for clinical trials
Term
What four ways are the actions of drugs described?
Definition
1. Symptomatic
2. Physiological
3. Cellular
4. Molecular or biophysical
Term
What is the difference between specific and non-specific drugs?
Definition
Specific drugs aim directly at the source of the disease

Non-specific treat a symptom of disease (most drugs)
Term
What was the first drug that proved drug development/crystallization is effective?
Definition
Penicillin
Term
Define chemotherapeutic agents
Definition
Agents used to eradicate bacteria, fungi, parasites, viruses and cancer cells
Term
What is the hallmark of chemotherapeutic agents?
Definition
Selective toxicity between invader and host; work best if lethal but may be suppressive
Term
What is a disadvantage of a chemotherapeutic agent that is not lethal, and is only suppresive?
Definition
They must depend on the host immune system to destroy invading cells
Term
What drugs inhibit bacteria cell wall synthesis?
Definition
Penicillin and friends
Term
What drugs inhibit bacteria ribosomes?
Definition
Aminoglycosides and macrolides (erythromycin)
Term
What drugs inhibit bacteria DNA synthesis and integrity?
Definition

sulfonamides inhibit folic acid

 

trimethoprim inhibits dihydrofolate reductase

 

quinolones inhibit topoisomerase

Term
What drugs inhibit fungi cell membrane ergosterol?
Definition

Function inhbited by amphotericin B

 

Synthesis by ketoconazole and friends

Term
What drugs inhibit fungi DNA synthesis?
Definition
5-fluorocytosine
Term
Give some examples of parasites that can be treated by complex drugs
Definition
Malaria, ameba, helminths
Term
List four classes of drugs that inhibit viruses
Definition

1. Attachment and entry inhibitors

2. Uncoating inhibitors

3. Polymerase/protease inhibitors (HIV drugs)

4. Neuarminidase inhbitors

Term
List two classes of drugs that inhibit cancer
Definition
1. Inhibitors of DNA synthesis or integrity (more toxic)

2. Inhibitors of cellular signal transduction (affect TK, growth factors, etc)
Term
Describe the general characteristics of pharmacotherapeutic agents
Definition
-Usually by binding receptors
-Can increase or decrease organ function
-Generally graded responses
-Often toxic
-Generally reversible
Term
Define pharmacotherapeutic agent
Definition
Drugs which are used to either:

a) replace naturally occurring endogenous substances
b) regulate body functions
c) alter mood and behavior
Term
What determines selectivity of drug action?
Definition
-Distribution to or exclusion from an organ (ex. blood brain barrier)

-The enzymes they work on

-Receptors
Term
Define receptors
Definition
Cellular proteins which bind with endogenous compounds including hormones, neurotransmitters and mediators of inflammation and mediate their cellular effects.
Term
Who discovered cell receptors? How were they confirmed?
Definition

Langley, Ehrlich and Loewi

 

Existence of receptors strengthened by calculations of how much of the surface area of the cell is covered by a drug when producing an effect

Term
Are receptor-drug interactions always very structured?
Definition
Not always.

eg. antihistamines don't even resemble histamines, they "blob" onto the receptors
Term
What allows drugs to bind to receptors
Definition
-Structural complementation
-Steroselectivity (chirality)
-Geometic/ cis-trans isomers
Term
What are the three types of chemical interactions that can allow a drug to bind to a receptor?
Definition

1. Weak, reversible (intermolecular forces)

2. Strong- irreversible (covalent) ex. carcinogenesis

3. Induced fit binding

Term
Define orthosteric site
Definition
The "active site" where the drugs or endogenous mediator binds
Term
Define allosteric site
Definition
Site where binding changes the functioning of the ligand binding at the orthosteric site

Can increase or decrease ligand binding at the active site
Term
Which are more effective, drugs binding at orthosteric or allosteric sites?
Definition
Drugs binding at alloesteric sites are actually considered to produce more finely-tuned responses than drugs acting at orthosteric sites
Term
What does ABCs stand for?
Definition

The alphabet, of course! jk

 

ATP-binding cassettes, a membrane transporter

Term
Define ATP-binding cassettes.

Where are they found?
Definition
Membrane transporters that actively transport agents across membranes by efflux

Only in liver, kidney, intestine and blood-brain barrier
Term
Define P-glycoprotein
Definition
An ATP-binding cassette important for efflux of drugs from intestinal cells to gut lumen, from hepatic cells to bile and from cerebrospinal fluid to blood.
Term
What are the most important ATP binding cassettes?
Definition
-ABCB1, better known as MDR1 or p-glycoprotein
-MRPs

-BESP
-BCRP
-Chloride ion transporters in lungs
Term
Define SLC transporters
Definition
The solute carrier family (SLC) of transporters; transport ions and nonionic compounds by facilitated diffusion or secondary active trasport
Term
Give some examples of SLC transporters
Definition
-Neurotransmitter reuptake transporters
-Organic anion/cation transporters (OATs/OCTs)
-Liver transporters (ex. statin drugs)
-Renal ion transporters
-Some in blood brain barrier
Term
List drugs that do not act on receptors
Definition
Those that act physically or chemically:
-Chelating agents
-Osmotic cathartics
-General anesthetic agents


Those that work through enzymatic mechanisms:
-Cholineasterase inhibitors
-MAO inhibitors
-Some chemotherapeutic agents
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