Term
| What stimulated passage of the Pure Food and Drug Act of 1906? |
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Definition
| Journalists publishing unhygenic conditions in the food industry |
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Term
| What was the effect of the Pure Food and Drug Act of 1906? |
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Definition
Prevention of adulteration and mislabling
(No effect on safety/efficacy) |
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Term
| What was the effect of the Harrison Narcotic Act of 1914? |
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Definition
Registration of people handling narcotics and the purchase of a tax stamp
Required prescription, so even doctors couldn't treat "addiction" |
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Term
| What government entity regulated marijuana sales first? |
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Definition
States regulated before the Feds
(Tax act passed in 1937, considered a narcotic) |
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Term
| What was the effect of the Controlled Substances Act of 1970? |
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Definition
Created schedules to rank drugs by the potential to cause abuse or dependency
("War on Drugs" has waxed and waned) |
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Term
| What stimulated passage of the Food, Drug, and Cosmetics Act of 1938? |
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Definition
Sulfanilamide tragedy
(Massengill made an elixer using poisonous ethylene glycol as a solvent, 100 people died) |
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Term
| What was the effect of the Food, Drug, and Cosmetics Act of 1938? |
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Definition
| Mandated testing for drug safety (not efficacy) |
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Term
| What stimulated passage of the Harris-Kefauver amendment of 1962? |
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Definition
Thalidomide disaster
(Medicine for morning sickness caused horrible birth defects) |
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Term
| What was the effect of the Harris-Kefauver amendment of 1962? |
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Definition
Mandated that toxicological studies should be done and efficacy should be proven
Mandated standards for clinical trials |
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Term
| What four ways are the actions of drugs described? |
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Definition
1. Symptomatic
2. Physiological
3. Cellular
4. Molecular or biophysical |
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Term
| What is the difference between specific and non-specific drugs? |
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Definition
Specific drugs aim directly at the source of the disease
Non-specific treat a symptom of disease (most drugs) |
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Term
| What was the first drug that proved drug development/crystallization is effective? |
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Definition
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Term
| Define chemotherapeutic agents |
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Definition
| Agents used to eradicate bacteria, fungi, parasites, viruses and cancer cells |
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Term
| What is the hallmark of chemotherapeutic agents? |
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Definition
| Selective toxicity between invader and host; work best if lethal but may be suppressive |
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Term
| What is a disadvantage of a chemotherapeutic agent that is not lethal, and is only suppresive? |
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Definition
| They must depend on the host immune system to destroy invading cells |
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Term
| What drugs inhibit bacteria cell wall synthesis? |
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Definition
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Term
| What drugs inhibit bacteria ribosomes? |
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Definition
| Aminoglycosides and macrolides (erythromycin) |
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Term
| What drugs inhibit bacteria DNA synthesis and integrity? |
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Definition
sulfonamides inhibit folic acid
trimethoprim inhibits dihydrofolate reductase
quinolones inhibit topoisomerase |
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Term
| What drugs inhibit fungi cell membrane ergosterol? |
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Definition
Function inhbited by amphotericin B
Synthesis by ketoconazole and friends |
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Term
| What drugs inhibit fungi DNA synthesis? |
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Definition
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Term
| Give some examples of parasites that can be treated by complex drugs |
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Definition
| Malaria, ameba, helminths |
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Term
| List four classes of drugs that inhibit viruses |
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Definition
1. Attachment and entry inhibitors
2. Uncoating inhibitors
3. Polymerase/protease inhibitors (HIV drugs)
4. Neuarminidase inhbitors |
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Term
| List two classes of drugs that inhibit cancer |
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Definition
1. Inhibitors of DNA synthesis or integrity (more toxic)
2. Inhibitors of cellular signal transduction (affect TK, growth factors, etc) |
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Term
| Describe the general characteristics of pharmacotherapeutic agents |
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Definition
-Usually by binding receptors
-Can increase or decrease organ function
-Generally graded responses
-Often toxic
-Generally reversible |
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Term
| Define pharmacotherapeutic agent |
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Definition
Drugs which are used to either:
a) replace naturally occurring endogenous substances
b) regulate body functions
c) alter mood and behavior |
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Term
| What determines selectivity of drug action? |
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Definition
-Distribution to or exclusion from an organ (ex. blood brain barrier)
-The enzymes they work on
-Receptors |
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Term
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Definition
| Cellular proteins which bind with endogenous compounds including hormones, neurotransmitters and mediators of inflammation and mediate their cellular effects. |
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Term
| Who discovered cell receptors? How were they confirmed? |
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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 |
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Term
| Are receptor-drug interactions always very structured? |
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Definition
Not always.
eg. antihistamines don't even resemble histamines, they "blob" onto the receptors |
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Term
| What allows drugs to bind to receptors |
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Definition
-Structural complementation
-Steroselectivity (chirality)
-Geometic/ cis-trans isomers |
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Term
| What are the three types of chemical interactions that can allow a drug to bind to a receptor? |
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Definition
1. Weak, reversible (intermolecular forces)
2. Strong- irreversible (covalent) ex. carcinogenesis
3. Induced fit binding |
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Term
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Definition
| The "active site" where the drugs or endogenous mediator binds |
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Term
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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 |
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Term
| Which are more effective, drugs binding at orthosteric or allosteric sites? |
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Definition
| Drugs binding at alloesteric sites are actually considered to produce more finely-tuned responses than drugs acting at orthosteric sites |
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Term
| What does ABCs stand for? |
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Definition
The alphabet, of course! jk
ATP-binding cassettes, a membrane transporter |
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Term
Define ATP-binding cassettes.
Where are they found? |
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Definition
Membrane transporters that actively transport agents across membranes by efflux
Only in liver, kidney, intestine and blood-brain barrier |
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Term
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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. |
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Term
| What are the most important ATP binding cassettes? |
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Definition
-ABCB1, better known as MDR1 or p-glycoprotein
-MRPs
-BESP
-BCRP
-Chloride ion transporters in lungs |
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Term
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Definition
| The solute carrier family (SLC) of transporters; transport ions and nonionic compounds by facilitated diffusion or secondary active trasport |
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Term
| Give some examples of SLC transporters |
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Definition
-Neurotransmitter reuptake transporters
-Organic anion/cation transporters (OATs/OCTs)
-Liver transporters (ex. statin drugs)
-Renal ion transporters
-Some in blood brain barrier |
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Term
| List drugs that do not act on receptors |
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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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