module 1 Flashcards
pharmacology can be defined as
the science of drugs, there uses effects and mechanisms
historical influences on modern pharmacology
discoveries of ancient civilization , the roles of poison and the influence of religion
380 BCE
Pupil of Aristotle wrote book that included opium
1803 in germany,
Serturner, a pharmacist isolated crystals of morphine from opium and discovered its pain relief capability
opium contains
10% morphine and 0.5% codeine and was given the name from from morpheus god of dreams
earliest recorded drug experiments
China in 2700 BCE in which ma Huang was used to treat flus and cough. –> today ephedrine has been isolated from the ma Huang plant to treat asthma
ancient Egypt and drugs
ebers papyrus in 1550 BCE was used as a medical textbook
Curare is
plant derived drug in South America that was used as a poison to hunt animals. Causes paralysis of muscles and eventual death my respiratory paralysis
in modern medicine curare was used as
anesthetists in surgery
what is ergot ?
a poisonous fungus found on the head of rye and is found in abundance during wet seasons
ergot effect on nervous system
mental frenzy , hallucination and convulsions
ergot effect on cardiovascular system
can cause constriction of blood vessels , limiting blood supply to fingers and toes and limbs which will eventually become black and die off
ergot and reproductive system
can cause violent contractions of the uterus , was sometimes used for labour
ergotamine
a compound derived from ergot and is useful in treating migraines through contstriction of blood vessels
ergonovine
compound of ergot that is used to hasten birth as to force uterine contractions. can also be used to stop bleeding after birth
religion and drugs
ancient societies healers were doctors and priests , plants were used to alter state of conciusness to be able to talk to the gods
ex) Peyote in Mexico, has LSDA properties
A drug can be defined as
substance received by a biological system that is not received for nutritive purposes and will influence the biological functions on an organism - chemicals , biological agents and herbal products are all considered drugs
drugs that act on the brain
alter the normal signalling ex) LSD
How was LSD discovered
Albert hofman who worked for Swiss pharmaceutical firm , synthesized LSD and chemical structure was similar to ergotamine and ergonovine
LSD contribution to pharmacology
certain mental illness might be due to production of potent substances in the brain and produce psychiatric disturbances
1900’s what drug came out ?
organoarsenicals designed by Paul ehrlich which would bind to parasites and cured syphilis
1930s drug discovery
sulpha drugs which were the first synthetic drugs to treat bacterial infections
antibiotic refers to
specifically to chemical substances produced by microorganism and not synthetic compounds
drug discovery in 1940s
Fleming discovered the first antibiotic known as penicillin and was used for gram positive disease
drug discovery in the 1950s’
Waksman discovered discovered streptomycin antibiotic which was a turning point of tuberculosis and gram negative bacterial disease
what are the 5 key steps of drug discovery ?
basic research/ drug discovery, preclinical trials , clinical trials, health Canada review , post market surveillance and phase IV clinical trial
what is the first stage in basic research
identification of the target, where a receptor is identified
step 2 in basic research
studying the target, in which a lead compound is identified and enters into more testing to look at safety and efficacy
pharmacological studies of new drugs are used to
determine the detailed mechanism of action of the new drug
toxicology studies of new drug entail,
the possible risk or harm of new drug , acute toxicity and chronic toxicity are looked at
if company wants to test new drug on people what 3 things need to fist take place
1) investigation - submission to highly qualified scientists who will approve admission
2) methodology, of the proposed clinical trial in humans
3) proof of safety- must be shown to be safe with several animal models and be submitted to the health products and food branch
what are phase 1 clinical trials
carefully evaluate absorption, distribution and elimination and adverse effects of new drug - efficacy is not assessed however tolerability is looked at with 20- 80 volunteers
phase 2 clinical trial
trying to determine if the drug is effective in a limited number of people ( 100- 500). drug safety is carefully looked at
phase 3 clinical trial
also known as randomized control trials and are the main studies used for marketing of drug
number of participants and phase 3 trial and duration
test drug in larger number of people( 1000+) and range from months to years
goals of phase 3 trial
to determine how safe and effective the drug is compared to no treatment ( placebo)
location and cost of phase 3 trials
are considered multicenter and take place in many cities and can cost from 1 million to 50 million
what are the 3 larger stages of phase 3 clinical trials
1- determining enrolment prior to the study
2-allocating participants to treatment groups
3-monitoring and analyzing results
the target population includes
group of patients for who the drug is intended ex) drug to treat hypertension , adults who have been clinically diagnosed with it would be target population
study population is
subset of the target population , 2 factors that influence this is inclusion/ expulsion criteria and consent
why are comorbities often included ?
to be representative of target population
obtaining consent means that
document which outlines purpose of study , the procedures that will be used and possible risks and benefits
what is meant by double blind design
neither investigator or participant is aware of treatment assignment group
- bias can occur otherwise
what is randomization ?
when patients are assigned to either treatment group or to control group in a random fashion
why is randomization used
ensures that confounding variables ( known and unknown ) are distributed equally between the 2 groups - and also removes possible bias in assigning patients to groups
placebo is
identical to experimental drug but does not contain the active ingredient , there is often placebo effect when taking drugs in which symptoms get better
Gold standard drug is known as
accepted by the medical community as the best available treatment for the given condition
when analyzing results what3 things need to be considered ?
compliance, quality of life and statistics
patient compliance refers to ?
how often the participant took the drug
what is meant by bioequivelant ?
both generic and brand name drugs will contain the same active ingredient and give similar blood levels
what is a receptor ?
molecule or complex of molecules located outside or inside the cell that has regulatory or functional role in the organism
receptors are bound to and activated by
endogenous ligands which are substances found in the body like hormones and neurotransmitters
location of receptors will determine
where the drug will act and whether the response that results from the drug - receptor interaction is beneficial or detrimental
how does opioid receptors location result in different effects ?
when they bind to receptors in the brain , causes pain relief , when they bind to receptors in stomach, causes constipation
other drug targets include
chemical reactions and physical chemical forces
chemical reactions include ?
when antacid neutralizes the stomach through aid base neutralization
how does cholestyramine work ?( physical chemical force )
binds to bile acids in GI tract preventing their reabsorption and increasing the elimination of bile salts that are used to make cholesterol