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G) Pharmacology - Therapeutics > Introduction to Pharmacology > Flashcards

Introduction to Pharmacology Flashcards

1
Q

what is clinical pharmacology?

A

Clinical Pharmacology is the scientific discipline that involves all
aspects of the relationship between drugs and humans.

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2
Q

define pharmacology. [drug-study]

A

It the study of substances that interact with living systems through chemical processes,especially by binding to regulatory molecules and activating or inhibiting normal body processes.

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3
Q

what concept do drug and receptors follow?

A

lock and key

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4
Q

what are receptors?

A 
-they are molecular substances or macromolecules present in tissues that combine chemically with a drug.
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5
Q

what do receptors interact with?

A 
receptors will interact with only a limited number of structurally related or   
complementary compounds.
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6
Q

what is the function of receptors?

A 
receptors exist to function as receptors for neurotransmitters, hormones or other physiological substances.
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7
Q

what was the publication of William Witherings about?

A 
publication on the use of  foxglove in the treatment of heart failure.
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8
Q

in the early 20th century what was discovered in pharmacology?

A 
sulphonamides and penicillins
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9
Q

what medicine did they discontinue in 1953?

A 
Thalidomide
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10
Q

when did this drug (thalidomide) get taken up again? what is it used for? what did it fail to be used for?

A

taken up again in 1954. used as a sedative. it was ineffective as an anti-histamine and as an anti-convulsant. also used for morning sickness,cold & flu preparations and antidiarrhoeals.

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11
Q

what are the side effects of the drug Thalidomide? when did they notice them?

A 
noticed in late 1950s. they were -severe limb abnormalities -deafness -blindness -cleft palate -internal abnormalities
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12
Q

who convinced manufacturers and the world of the link between the thalidomide drug and horrific birth defects?

A 
Frances Kelsey
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13
Q

because of thalidomide what changed in the pharmacology field?

A 
it led to changes in regulatory practices. now extensive safety and eficacy testing of the drugs is required before release onto the market. [research done in FDA, MCC and now SAHPRA]
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14
Q

in new research areas what is the use thalidomide? [3]

A 
1. It inhibits angiogenesis (the development of new blood vessels) in cancer.
2. as an anti-inflammatory.
3. stimulates the immune system - TB in AIDS patients.
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15
Q

what is drug development?

A 
making drugs for the purpose of treatment or recreational use. While developing a drug you look at different stages and how they affect the body. until you get to your desired clinical effect.
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16
Q

List 6 steps we go by when developing a drug.

A 
-Molecucular pharmacology
-Cell pharmacology
-Cell physiology
-Tissue physiology
-Organ physiology
-Clinical effect
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17
Q

what is the drug discovery or development process? discuss

A
  • First there will a discovery of the drug or the making of it. The drug will undergo refinement chemically and biologically. refining its characterisation.
  • After the refining process the drug goes through safety and toxicity checks: here they check for and develop the formular of the drug that is most safe and effective for the purpose of the drug creation. tests at this stage are done on animals.
  • Next volunteers are taken for testing of the drug and patient studies are done.
  • in being used in humans it allowd for regulatory processes to be done. regulate the frequency of the drug taking and other stuff.
  • After regulation it is Marketing. drug is sold to companies and pharmacies.
  • It gets monitored after its been registered. [post registeration monitoreing]
  • Next it is lessons and developments. what happens after marketing the drug and what have they learned what can they fix. if any thing perculiar transpired the drug goes in for refinement and more testing.
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18
Q

define discovery and development.

A 
[development = converting that structure to a useful drug]
discovery = finding new active structure]
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19
Q

what are the 3 kinds of studies?

A 
1. Pre-clinical 
2. Clinical
3. Post marketing surveillance aka Pharmacovigilance.
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20
Q

what is pharmacovigilance?

A 
also known as drug safety:it is the practice of monitoring the effects of medical drugs after they have been licensed for use, especially in order to identify and evaluate previously unreported adverse reactions. e.g "the partnership hopes to develop diagnostic tools to improve pharmacovigilance"
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21
Q

define eficacy.

A 
Efficacy is the capacity to produce an effect (eg, lower BP). Efficacy can be  
assessed accurately only in ideal conditions (ie, when patients are selected  
by proper criteria and strictly adhere to the dosing schedule). Thus, efficacy  
is measured under expert supervision in a group of patients most likely to  
have a response to a drug, such as in a controlled clinical trial.
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22
Q

define effectiveness.

A 
Effectiveness differs from efficacy in that it takes into account how well a  
drug works in real-world use; often, a drug that is efficacious in clinical trials  
is not very effective in actual use. For example, a drug may have high  
efficacy in lowering BP but may have low effectiveness because it causes  
so many adverse effects that patients stop taking it.
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23
Q

what is adverse reaction?

A 
Adverse reaction - A response to a drug which is noxious and unintended,  
and which occurs at doses normally used in man for the prophylaxis,  
diagnosis, or therapy of disease, or for the modification of physiological  
function.
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24
Q

what is pharmacokinetics?

A 
 1.Pharmacokinetics (what the body does to a drug as it moves through the body)
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25
Q

what are the 6 key domains?

```

A

i) Pharmacological principles
ii) Optimal choice and use of medicines
iii)Hazards of medicines use.
iv)Investigating drug effects
v)Investigating medicines use
vi)Managing medicines use
~~~

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26
Q

what do we mean by (i) pharmacological principles?

```

A

=Pharmacodynamics and pharmacokinetics

```

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27
Q

what do we mean by (ii) optimal choice and use of medicines?

A 
-rational medicines selection and use, evidence-based practice, cost-effectiveness, measuring response, dose adjustment, adherence/concordance.
28
Q

what are (iii) hazards of medicines use?

A 
pharmacogenetics, adverse reactions,  poisoning, drug interactions, medication errors
29
Q

how do we (iv) investigate drug effects?

A 
(design, conduct, and interpretation of  clinical pharmacological research, research ethics, Good Clinical  Practice, statistical analysis
30
Q

how do we (v) investigate medicines use?

A 
observational research,  pharmacovigilance, pharmaco-epidemiology, pharmaco-economics
31
Q

how do we (vi) manage medicines use?

A 
Pharmacy & Therapeutics Committees, prescribing policies, formularies, standard treatment guidelines.
32
Q

what is pharmacotherapy?

A 
 medical treatment by means of drugs.
33
Q

in pharmacotherapy what do we consider when dealing with a medicine? [3]

A 
1. Indications – the registered reason to use a medicine 
2. Contraindications – conditions in which the use of the medicine is not recommended (or should be used with caution) 
3. Precautions – warnings about specific patient populations like:
>Very young (neonates, infants, children) 
> Very old (elderly, geriatrics) 
> Those with problems (renal disease, liver disease) 
> Pharmacogenetic diversity (slow or fast metabolisers)
34
Q

what is ADME?

A 
Absorption, Distribution, Metabolism, Excretion
35
Q

larger molecules [drugs] pass through?

A 
lipid membrane
36
Q

small and water-soluble molecules [drugs] pass though?

A 
pores
37
Q

what does the drugs ability to pass through the cell membrane depend on?

A 
depends on its ability to dissolve in lipid and water.
38
Q

the route of administration of the drug depends on? [3]

A 
1. Drug properties e.g insulin cannot be given orally
2. Ease of administration e.g oral more convenient than injection 
3. How soon the action [effect of drug] is required.
39
Q

when is oral administration of drugs not suitable?

A 
Oral administration is not suitable if medicine cannot get from gut  into blood in sufficient quantities.
40
Q

what happens when we administer a drug orally when it shouldn’t, give examples. [3]

A 
1. It gets destroyed in gut e.g. by enzymes in the case of insulin 
e.g. by acid in the case of penicillin G 
2. If drug is highly charged (polar) and therefore unable to cross lipid membranes e.g. streptomycin 
3. Drug gets metabolised so quickly in the liver that little reaches the system i.e. First Pass Effect e.g. glyceryl trinitrate
41
Q

what are the factors that affect the absorption of orally administered drugs? discuss

A 
1. Food 
•it could bind to drug in gut preventing absorption e.g. milk and tetracycline 
• food delays gastric emptying and so can delay absorption of the drug.
2. Formulation 
• drugs in aqueous solution are more rapidly absorbed than those in solid form. #Solids must first disintegrate and then dissolve 
• slow release preparations
42
Q

what is meant by parenteral? =

A 
 Parenteral means administered or occurring elsewhere in the body than the mouth and alimentary canal.
43
Q

what are the disadvantages or ‘hiccups’ of parenteral administration of drugs?

A 
- more expensive 
- less safe 
- requires skill 
- must be sterile 
- must be pyrogen free
44
Q

when is it useful to administer drugs parenterally? [3]

A 
1. If properties of drug make it unsuitable for oral administration. e.g insulin
2. If the patient is unconscious/ vomiting
3. If faster action is required.
45
Q

define subcutaneous(s.c) and intramuscular (i.m). how can the rate of absorption be altered?

A 
s.c = under the skin
i.m into the muscle
#Rate of absorption can  be altered by changing  formulation
46
Q

why should we be slow when administering drugs via the intravenous(i.v) administration route?

A 
 must be slow as danger that temporarily high  concentration of the drug will effect a vital organ e.g.  heart / brain
47
Q

why cant some drugs be administered intravenously?

A 
 e.g Oily vehicles, these are drugs that cause hemolysis or precipitation and should not be given through this route.
48
Q

drug administration through mucous membranes, list them.

A 
- Sublingual (under tongue)
- Rectal (suppositories)
- Pulmonary epithelium
49
Q

what is avoided when administering a drug sublingually?

A 
When you administer a drug under the tongue you avoid hepatic metabolism e.g glyceryl trinitrate.
50
Q

when is it useful to administer a drug rectally?

A 
when a patient is vomiting.
51
Q

why administer drug in pulmonary epithelium?

A 
-large surface area for absorption- gaseous , volatile drug. e.g Anaesthetic
- also solutions can be atomised to act on receptors  in the airway e.g. β2 receptors in asthma.
52
Q

discuss drug administration through the skin.

A 
abraded / broken skin more readily penetrated  than normal skin 
• some substances can enter through normal  
skin – must be very lipid soluble e.g. - organophosphate insecticide poisoning 
#some drugs in patches placed on  the skin
53
Q

give examples of how drugs are administered to skin.

A 
drugs in patches, organophosphate insecticide poisoning.
54
Q

what do we base how we choose medicine on? [4]

A 
— Efficacy 
— Safety 
— Suitability 
— Cost
55
Q

how to use medicine safely?

A 
(Must have) Foundation 
(Have gone through) Themes (LGRS, cases) 
(Must have) Clinical years and experience 
(Must be ) a Safe and effective prescriber, and life-long learner
56
Q
  • A prescriber does a) to find numerical information that will help them choose b)
A 
a) They navigate literature.
b) the right treatment and the right dose.
57
Q
  • differentiate between dilute to’ vs ‘dilute with.
A 
If  you have 7mL of solution and you dilute it with 10mL of saline, how much of the diluted solution do you have?
with 7mL’ means you add 7mL of liquid to whatever you have in the beaker i.e. you start with 10mL and you add 7mL to get 17mL
.............................
If you have 2mL of solution and you add saline to 10mL to dilute it, how much of the diluted solution do you have?
‘to 10mL’ means to the 10mL mark on the beaker 
   so you start with 2mL and add (10mL-2mL) to get to the 10mL mark  
   i.e. you add 8mL saline
58
Q

Discuss concentration

A

e.g. Think of a cup of tea with one spoonful of sugar and another cup with two spoonful of sugar. The second is sweeter because the concentration of the sugar is greater.

First cup = 5g of sugar is dissolved in 250 mL of how water. so, the concentration is is 5g in 250mL or 5g/250mL = 5000mg/250mL = 20 mg/mL (5000mg/500mL)

59
Q

Pharmacodynamics.

A

What the drug does to the body.

60
Q

Pharmacokinetics

A

What the body does to the drug, how they [drugs] move through out the body and move out of/ excreted from the body.

61
Q

Absorption of the drug

A

after administration most drugs need to reach the bloodstream. because that is how they are transported to their sites of action. But if a drug is administered by I.V.route, which is intravenous, already in blood and no absorption is required. other routes need absorption as they have to pass through a series of membranes to reach the blood.[via diffusion= pore between cells] Passive diffusion, moves down the concentration gradient. if small go through pore, lithium. if larger have to pass across the lipid membrane. if polar or ionised= water-soluble = pore. if apolar or un-ionised=lipid soluble = passes lipid membrane. most drugs are weak acids or weak bases and can occur in two forms (one water-soluble and one lipid-soluble) how much it is water or lipid-soluble depends on pH. diffusion may use membrane components[proteins] like carrier facilitated diffusion. active transport goes up a concentration gradient and needs energy.

62
Q

Distribution of the drug

A

the drug now needs to be distributed between plasma and other tissues, unless the drug is protein bound, it can cross ordinary capillaries into the interstitial fluid [fluid between cells]. drug passage into cells depends on the ability to pass the membrane. once the drug is in the blood, can be carried in plasma[dissolved], on plasma protein e.g albumin. D + P = DP [unbound drug + plasma protein =bound drug]. only unbound drug [D] is free to attach to site of action, or to move out of capillaries and to act. an example is PHENYTOIN, which is an anticonvulsant drug. useful for epilepsy. free drug concentration will increase if: -amount of plasma protein decreases because of malnutrition. -or if the free drug is displaced from being bound, by another drug. this other drug binds more readily to plasma protein. passage of drugs [particularly water-soluble drugs] into some areas is more limited. example passage into the brain is limited by the blood-brain barrier.

63
Q

Metabolism of the drug

A
  • The drug is also distributed to the site of action. After action, the drug must be eliminated via liver and kidney, hepatic and renal respectively.
    Liver [hepatic] metabolism- biotransformation, the metabolism is carried by enzymes. The main aims of metabolism are: To inactivate drugs and make more water-soluble [polar] for excretion. sometimes these happen. [drug goes from being active to more active, e.g. Codeine to morphine] [active to toxic e.g. paracetamol] [Inactive to active e.g. cortisone to cortisol (hydrocortisone)]
    I.E - metabolism sometimes occurs before action. [first need to be metabolized??]
    Biotransformation reactions: Type I- Non-synthetic reactions (Groups changed or removed) e.g. Hydrolysis(water is added) and Type II- Synthetic reactions [Groups are added i.e. something new synthesized] something else is made or added to your molecule. e.g. Glucuronide conjugation [Glucuronic acid made in the body from glucose is added onto the drug.] Results of Glucuronide conjugation -1. addition of large molecule means the drug cannot fit in the receptor, so its inactivation. -2.Increased polarity and water solubility, for excretion in urine or if large excretion in bile. if passed to gut bile, bacteria remove glucuronic acid (because it is like glucose and they can use it) and drug D (lipid-soluble) is reabsorbed. Enterohepatic circulation.
64
Q

Excretion of the drug

A

via urine or feces

65
Q

What is Pharmacodynamics?

A

2.Pharmacodynamics (what a drug does to

the body as the drug is being absorbed,metabolized, and excreted)

G) Pharmacology - Therapeutics (1 decks)

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