Principles of Pharmacology

Question 1

Curare

Answer 1

arrows dipped in it and used as a poison causing paralysis and death, used to relax muscles during surgery

Question 2

Ergot

Answer 2

grows on heads of rye and used as a poison, ergotamine used as a migraine medication causing vasoconstriction, ergonovine used to hasten uterine contractions and stop uterine bleeding after childbirth

Question 3

Reserpine and Chlorpromazine

Answer 3

isolated from rauwolfia plants to reduce tension, anxiety and lower bp; chlorpromazine used preferentially to treat mentally ill

Question 4

LSD

Answer 4

synthesized by Albert Hoffman; similar in structure to ergotamine and ergonovine causing psychedelic effects and supported the idea that mental illness might be due to chemical imbalance

Question 5

Anaesthetics

Answer 5

NO used in extraction of teeth and ether used as anesthesia during surgery

Question 6

Organoarsenicals

Answer 6

Paul Ehrlich is the father of chemotherapy; lead to the cure of syphilis bc these compounds selectively bind to parasites

Question 7

Sulfa Drugs

Answer 7

introduced by Gerard Domagk for the treatment of bacterial diseases

Question 8

Penicillin

Answer 8

Alexander Flemming discovered penicllin as the first antibiotic against gram positive bacteria

Question 9

Streptomycin

Answer 9

Selman Waksman discovered streptomycin as an antibiotic effective in treating tuberculosis and gram-negative bacterial infections

Question 10

Drug discovery

Answer 10

drug target is determined and pharmacological effects observed; if promise is shown safety and efficacy studies are done

Question 11

Pre-clinical studies

Answer 11

toxicology study to determine the effects on organ systems that are not the target organ, and pharmacology study to determine the detailed MOA

Question 12

Clinical Trial Initial steps

Answer 12

proof of safety and efficacy and methodology of proposed clinical trial is submitted and reviewed

Question 13

Clinical Trial Phase 1

Answer 13

conducted in a limited number of healthy individuals to carefully examine MOA and adverse effects; efficacy not tested

Question 14

Clinical Trial Phase 2

Answer 14

conducted in patients with the disease the drug is designed to treat to test the efficacy

Question 15

Clinical Trial Phase 3

Answer 15

controlled randomized clinical trial to license and market drug and tested in a large group of people for more extensive periods of time (where the target pop, inclusion/ exclusion, placebo, etc. come into play)

Question 16

Clinical Trial Phase 4

Answer 16

post-marketing surveillance; risks that are delayed or less frequent might not appear in phase 3

Question 17

Drug Targets

Answer 17

drugs bind to receptors of certain tissues and can be agonists (stimulate receptor) or antagonist (block response at receptor), chemical reactions (antacids) and physical chemical factors (like cholestyramine binding to bile acids)

Question 18

Drug Efficacy

Answer 18

max pharmacological effect that can be produced independent of the potency

Question 19

Drug Potency

Answer 19

the dose of the drug required to produce a response of a certain magnitude; normally 50% of the maximal response for that drug

Question 20

Therapeutic Index and Therapeutic Range

Answer 20

the relationship between concentrations causing adverse effects (TD) and those causing desired effects (ED) (the larger the greater); range refers to the dose that keeps the blood conc. of the drug above minimum conc. that produces a desirable effect but below the conc. that produces a toxic response

Question 21

Dose Response curve

Answer 21

once threshold is reached and a certain number of receptors have been activated, a small increase in dose will have a large change in response (linear portion) and also where ED50 occurs (dose that will result in 50% of maximal effect, or dose that is effective in 50% of pop)

Question 22

On the skin (topical administration)

Answer 22

drugs applied to skin to treat mild to moderate skin conditions

Question 23

Through the skin (topical administration)

Answer 23

application of drug to the skin for absorption into general circulation; convenient and delivers steady drug supply while bypassing internal enzymes, but can be expensive and a local irritant

Question 24

Inhalation (topical administration)

Answer 24

gaseous anesthetics, as well as steroids and other drugs for lung disease inhaled, the doses are small and toxicities associated with oral medications are avoided, but it requires proper use by the patient

Question 25

Mouth (enteral administration)

Answer 25

most common, convenient, inexpensive and non-invasive means that can be self administered; first pass through the liver which reduces the amount of active drug left to enter circulation and there is variable absorption between patients; slow onset of 0.5-1h

Question 26

Rectum (enteral administration)

Answer 26

systemic or local effect for patients who are vomiting and a less invasive approach for comatose patients; digestive enzymes are bypassed, but not all drugs are available as suppositories and absorption is slow, incomplete and variable

Question 27

Sublingual and Buccal (enteral administration)

Answer 27

under the tongue and under the cheek and bypasses enzymes in the stomach, intestine and livers but are not always adequately absorbed and will then act as an oral drug; rapid 1-4 min onset

Question 28

Intravenous (parenteral administration)

Answer 28

injected into blood to produce an immediate response (15-30 sec) for drugs that are poorly absorbed but can have intense response, is costly and prep must be sterile

Question 29

Intramuscular (parenteral administration)

Answer 29

drug injected deep into muscle; 10-20 min onset

Question 30

Subcutaneous (parenteral administration)

Answer 30

drug injected into deepest layer of skin; 15-30 min onset

Question 31

Bioavailability

Answer 31

fraction of the administered drug that reaches the systemic circulation in an active form

Question 32

Absorption

Answer 32

crosses biological membranes via diffusion, or active/ mediated transport

Question 33

Distribution

Answer 33

movement of drug from blood to the site of action and other tissues; the greater the blood flow the more rapidly the drug reaches that organ

Question 34

Metabolism

Answer 34

conversion of drug to its metabolites that are usually devoid of pharmacological actions and mostly occurs in the liver but also in most other organs; first P450 unmasks or add functional group, then a large water moiety is added to make it water soluble for excretion

Question 35

Excretion

Answer 35

majority through kidneys (needs to be water soluble), GI tract, lungs, saliva and sweat, breast milk

Question 36

Drug Interactions

Answer 36

increased or decreased absorption of a second drug, can block the inactivation of a second drug and increase its effect, can facilitate the excretion of a second drug and decrease its effect