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PHAR 100 > PHAR 100 Module 1 > Flashcards

PHAR 100 Module 1 Flashcards

1
Q

drugs

A

any substance received by a biological system that is not received for nutritive purposes, and which influences the biological function of the organism

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2
Q

pharmacology

A

the science of drugs, including their uses, effects and modes of action

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3
Q

ancient China

A

classified drugs according to taste

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4
Q

ancient Greece

A

opium, morphine

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5
Q

influence of religion

A

medicine men were physicians and priests

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6
Q

curare

A
  • acts on animals voluntary muscles, causing paralysis and death
  • used by anesthetists during surgery, helps relax muscles
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7
Q

ergot

A
  • incorporated in bread in Middle ages, killing many
  • symptoms: mental frenzy, convulsions, constriction of blood vessels that led to limbs causing them to die, violent contractions of uterus
  • in modern era, 2 active principles have been isolated from ergot
  • ergotamine → treatment of migraines, constricts blood vessels to head
  • ergotovine - arrest uterine bleeding after birth
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8
Q

drugs acting on brain → reserpine and chlorpromazine

A
  • reduce tension, anxiety, lower BP
  • chlorpromazine is preferred to reserpine for management of the mentally ill
  • makes people placid
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9
Q

drugs acting on brain → lysergic acid diethylaminde (LSD)

A

psychedelic effects

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10
Q

drugs acting on brain → anaesthetics

A
  • nitrous oxide → useful for extracting teeth

- ether → used in surgery

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11
Q

drugs acting against infectious diseases → organoarsenicals

A
  • Paul Ehrlich (father of chemotherapy)

- bound to parasites

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12
Q

drugs acting against infectious diseases → sulfa drugs

A

1st successful synthetic drugs for treatment of bacterial disease → termed antibacterial compounds

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13
Q

drugs acting against infectious diseases → penicillin

A
  • 1st antibiotic

- use in therapy of gram-positive bacterial diseases

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14
Q

drugs acting against infectious diseases → streptomycin

A

treatment of tuberculosis and gram-negative bacterial diseases

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15
Q

drug development process

A
  • identify a biological target
  • determine pharmacological effects
  • if compound shows promise, it will be identified as a lead compound
  • enters more studies for safety and efficacy
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16
Q

stages in drug development → drug discovery

A
  • 3-6 years
  • research and discovery of target (25,000 compounds)
  • preclinical testing → safety & efficacy (30 compounds)
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17
Q

stages in drug development → clinical trials

A
  • 6-7 years
  • phase 1 → safety & tolerability (5-30 compounds)
  • phase 2 → effectiveness, safety & pharmacokinetics (2-3 compounds)
  • phase 3 → effectiveness & safety (1 compound)
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18
Q

stages in drug development → health Canada/FDA approved drug

A
  • health Canada review and manufacturing → drug approval and production
  • phase 4 → long-term safety
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19
Q

toxicology studies

A

determine the effect of the new drug on organ systems other than the targeted organ

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20
Q

pharmacology studies

A

determine the detailed mechanism of action of the new drug

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21
Q

phase 1 clinical trials

A
  • 20-100 healthy volunteers

- absorption, distribution, elimination and adverse effects are studied

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22
Q

phase 2 clinical trials

A
  • conducted in patients who have the disease/condition (100-500 ppl)
  • looks at safety
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23
Q

phase 3 clinical trials

A
  • controlled randomized clinical trials
  • test 1000+ ppl
  • conducted at city centres for diversity
  • goal is to determine whether drug is safe/effective
24
Q

target population

A

group of patients for whom the drug is intended

25
Q

inclusion/exclusion criteria

A

define characteristics of patients to be used in the study; try to eliminate all other variables

26
Q

ethical considerations and consent

A

informed consent

27
Q

study population randomized allocation

A
  • randomization ensures that patients with different characteristics are equally distributed between the treatment and control group, maximizing the comparability of the groups and removes bias
28
Q

treatment and control groups

A
  • treatment groups receives drug

- control group → placebo or gold-standard drug

29
Q

blinded assessment

A

double-blind

30
Q

outcome

A

results of treatment measured in an objective, reliable manner

31
Q

compliance

A

how often the patient takes the drug

32
Q

quality of life

A

important when considering usefulness of drug

33
Q

analysis of results

A

experimental drug compared to control drug using stats

34
Q

generic vs. brand name

A
  • if a drug undergoing development shows promise and a manufacturer wants to put it on the market, then a generic name for the drug is selected (and apply for a patent for 20yrs)
  • after patent expires, other manufacturers can make copies of the original brand name drug and sell it under their own brand name
  • brand name and generic drug will contain the identical active ingredient as the original brand name drug, in the same amount and dosage form
35
Q

bioavailability studies

A
  • compares blood levels after administration of both the brand name drug and the new brand name/generic drug to healthy volunteers
  • ensures the 2 drugs are bioequivelent
36
Q

drug advertising techniques

A
  • catch audience attention
  • use celebrities or authorities to endorse product
  • fear
  • offering easy solution for problems
  • before-after technique
  • discredit drugs produced by other manufacturers and praise yours
37
Q

receptors

A
  • normally bound to and activated by endogenous ligands (hormones and neurotransmitters)
  • most drugs can mimic the action of, or block the effect of, the endogenous ligand at the receptor
  • drugs that bind to and stimulate a receptor are called agonists, and drugs that bind to but block the response at a receptor are called antagonists
  • lock and key analogy
38
Q

dose-response relationship

A
  • intensity of the pharmacological effects produced by a drug increases in proportion to dose
  • for a drug to achieve it’s desired response, many receptors need to be activated at once
  • as dose/concentration of drug increases, more and more receptors are activated
  • a threshold exists, where a certain number of receptors need to be activated before an effect will be seen
39
Q

dose-response curve

A

how much drug you need in your body to see a specific effect

40
Q

efficacy

A
  • the maximum pharmacological response that can be produced by a specific drug in that biological system
  • amount of drug needed doesn’t matter, the maximum effect the drug can produce matters
  • efficacy is more important than potency
41
Q

potency

A
  • the dose of a drug that is required to produce a response of a certain magnitude, usually 50% of the maximal response for that drug
  • drug A is more potent than drug be (need to take less of drug A to achieve the same effect from drug B)
42
Q

therapeutic range

A

the aim of therapy is to give a dose that keeps blood concentration above the minimum concentration, but below the concentration that produces a toxic response

43
Q

pharmacokinetics

A
  • movement of drug into, through and out of the body

- 4 major processes are involved: absorption, distribution, metabolism, excretion

44
Q

topical administration

A
  • on the skin → drugs applied to skin for local effect can be absorbed and produce a systemic effect
  • through the skin → transdermal drug delivery is the application of a drug to the skin for absorption into general circulation for a systemic effect; steady supply for several days; bypasses enzymes in body
  • inhalation → drugs are rapidly absorbed from the lungs; local and systemic effects
45
Q

enteral administration (enter blood through mouth of GI tract)

A
  • mouth → enzymes in liver can decrease amount of active drug left to enter circulation
  • rectum → digestive enzymes of stomach and intestine are bypassed
  • sublingual and buccal → enzymes of stomach, intestine and liver are bypassed
46
Q

parenteral administration

A
  • intravenous (IV) → can be used for drugs that are poorly absorbed; needs to be made into a solution in water for injection
  • intramuscular → drug is injected deep into a muscle
  • subcutaneous → drug is injected into deepest layer of skin
47
Q

absorption

A
  • movement of a drug from the site of administration into the blood
  • occurs by 3 ways: diffusion through aqueous pores, diffusion through lipids; active or carrier-mediated transport
48
Q

distribution

A
  • the movement of a drug from the blood to the site of action and other tissues
  • can result in termination of the therapeutic effects of some drugs
49
Q

metabolism

A
  • the conversion of a drug to a different chemical compound

- drug must be water-soluble to be eliminated by the kidneys

50
Q

biotransformation

A
  • occurs in the liver
  • phase 1 → add/unmask a functional group on the drug so phase 2 can add a large water soluble molecule; P450 - enzymes capable of biotransforming drugs are found in most tissues, but are present in [high] in the liver
  • phase 2 → add a large water soluble moiety to the product resulting from phase 1, making the metabolite water soluble for excretion
51
Q

excretion

A
  • moving the drug and its metabolites out of the body

- kidneys, GI tract (feces), lungs, saliva/sweat, breast milk

52
Q

half-life

A
  • the time needed for the liver and kidney to remove half the drug from the body
53
Q

variations in drug response

A
  • genetic factors
  • environmental factors
  • other disease states
  • altered physiological states (ex: pregnant)
  • other drugs present
54
Q

adverse effects

A
  • extension of therapeutic effect
  • unrelated to main drug action
  • allergic reaction
  • drug dependence or addiction
  • teratogenesis (birth defects)
  • adverse biotransformation reactions
55
Q

drug toxicity

A
  • assessed using a measure called the therapeutic index, which is calculated by the formula: TI = TD50/ED50
  • TD50 = toxic dose in 50% of the population
  • ED50 = effective dose in 50% of the population
  • therapeutic index tells you how safe the drug is
  • the higher the therapeutic index, the safer the drug
56
Q

drug-drug interactions

A

occurs when one drug changes the pharmacological effect of a second drug; occur during absorption or metabolism

57
Q

drug-food interactions

A

involve the interference of food with drugs taken con-currently

PHAR 100 (6 decks)

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