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Flashcards in Phamacodynamics Deck (33):
1

what is pharmacodynamics

study of the biochemical and physiological effects of drugs and their mechanisms of action, including the relationship between the dose (or concentration) of a drug and the effect it produces

2

the effects of most drugs results from what

their reversible association with a functional macromolecular component of the cell

3

what is a receptor or "drug target"

a functional macromolecular component

4

the receptor is a component of what

a cell or organisms that interacts with a drug and initiates the chain of biochemical or physiological events lead to the effects of the drug

5

what are the general types of drug receptors for endogenous physiological regulatory molecules

-neurotransmitters
-hormones & growth factors
-autocoids (substances which are formed and act locally)

6

other cellular proteins or constituents of drug receptors

-enzymes
-transport proteins; carrier molecules
-ion channnels
-structural proteins
-nucleic acids; nuclear transcription factors/elements

7

define agonists

drugs that mimic the effects of endogenous ligands by interaction with the same receptor

8

define antagoinists

compounds that inhibit the response of a specific agonist by competition for binding sites

9

how are drug receptors identified or classified

on the basis of the relative potencies of structurally related agonists and the effect or lack thereof, of selective antagonists or agonists

10

what are the major signalling mechanisms

1. intracellular response elements; transcription factors; DNA-coupled receptors
2. transmembrane enzymes, including tyrosine protein kinases
3. ligand gated ion channels (iontropic)
4. G protein coupled receptors (metabotropic)

11

see diagrams: slide 6-9

see diagrams: slide 6-9

12

name a few drug actions not mediated by receptors

1. chelating agents
2. antacids
3. chemical neutralization
4. osmotic diuretics

13

what are chelating agents

drugs used to treat pts whose body is heavily burdened or has high levels of toxic metals; chelating agents bind heavy metals, take them to the kidney and excrete them; only interacting with heavy metal, not other body tissue

14

what are antacids

neutralize stomach acid, don’t interact with receptor

15

what are chemical neutralization

treat certain toxicities. Ex. Heprain a coagulant is a heavily charged polysaccharide. If too much heparin is in the body the pt will start to bleed. The anecdote for heparin is to squirt in protame which is heavily positively charged

16

what are osmotic diuretics

manatal, works as an osmotic particle exerting coagulative propeties, gets filtered in the glomerulus, doesn’t get reabsorbed and then draws water in with it bc of its osmotic properties and increases urine formation; not interacting with receptors

17

see diagrams: slide 12-13

see diagrams: slide 12-13

18

what is the spare-receptor concept

-a maximal effect can be produced by a drug when only a small proportion of receptor is occupied; the response is not linearly proportional

19

see diagrams: slide 15+16

see diagrams: slide 15+16

20

efficacy

- the maximum effect of a drug is termed efficacy
-this term does not refer to the therapeutic efficacy of the drug, but to the stimulus properties of the drug receptor complex

21

potency

- is a comparative measure that refers to the different doses of two drugs that are needed to produce the same effect

22

(Full) Agonist

-is a drug capable of generating a maximal response

23

Partial Agoinst

- is a drug that will generate a response, but that response is less than the maximum

24

antagonist

- is a drug that reduces the effect of an agonist (an agonist must be present?)

25

inverse agonist

- is a drug that stabilizes an “active receptor” in the inactive conformation

26

see diagrams: slide 18-21

see diagrams: slide 18-21

27

what are they types of drug antagonism

1. competitive
2. noncompetitive
3. physiologic (functional)
4. Chemical (neutralization)

28

see diagrams: pic 23-26

see diagrams: pic 23-26

29

what pharmacodynamic changes occur with aging

-CNS more "sensitive"
-Beta adrenoceptors "less sensitive"
-orthostatic hypotension is more common
-potassium, electrolyte imbalance is more common
-the incidence of occult blood loss with aspirin or NSAIDs is higher

30

what is heterogeneity in the elderly

aging associated with physiologic decline and an increase in the prevalence of disease

31

how is heterogeneity in the elderly slowed

by maintaing physical fitness

32

what clinically impacts heterogeneity in the elderly

-increased biologic variation is characteristic of this age group
-physiologic functions that affect drug disposition
-each pt must be evaluated individually

33

geriatric prescribing

-Adequate review of patient medication regimens; obtain a detailed drug history
-Critically address whether drug therapy is indicated at all; reevaluate drug use at frequent intervals
-Consider physiologic or pathologic changes that may affect drug response
-Pick endpoints to follow carefully
Start low and go slow
-Communicate effectively; enhance patient compliance; emphasize the alliance with the patient