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pharmacology > pharmacodynamics > Flashcards

pharmacodynamics Flashcards

1
Q

define pharmacodynamics

A
  • drugs acting on body
  • interaction with receptor
  • to reduce symptoms and disease
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2
Q

example of drugs non-receptor mechanism

A
  • metal chelators = reduce metal ions overload
  • antacids = neutralize gastric acid
  • osmotic diuretics eg: mannitol
  • bile acid binding resins eg: colestipol
  • general anaesthetics
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3
Q

characteristics of drugs

A
  • size range 100-1000
  • shape and charge that complement binding site of receptor
  • many are weak acids/weak bases
  • unionized form that being absorb
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4
Q

types of receptors

A
  • proteins

- nucleic acids (DNA/ RNA)

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5
Q

drug-receptor interaction

A
  • lock and key fit 3D structure
  • non-covalent chemical interactions
  • usually reversible
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6
Q

what is Ka?

A
  • equilibrium dissociation constant

- drugs that binds 50% of available receptors at equilibrium

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7
Q

name of drugs for using in industries

A

code name eg: D365

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8
Q

name of drugs for using in worlwide

A

generic (non-proprietary) name eg: verapamil

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9
Q

what happen when 2 ligands bind at the same receptor?

A

cause competition thus reduce the time spent receptor-bound for each ligand

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10
Q

what is side effects?

A
  • unwanted reactions eg: nausea
  • when drugs act on non-target receptors
  • increase when doses increase
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11
Q

4 types of receptor proteins

A
  • ion channels
  • G protein-coupled receptors
  • kinase-linked receptors
  • intracellular receptors
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12
Q

what is ion channels?

A
  • 4-5 subunits
  • ligand-gated
  • conduct Na, K, Cl, Ca
  • fast communication
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13
Q

examples of ion channels

A
  • nAChR
  • GABA(a) receptor
  • Glycine receptor
  • Glutamate receptor
  • Purine receptor
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14
Q

what is G protein-coupled receptors?

A
  • receptors that linked to effectors via G protein
  • single polypeptide chain
  • spanning membrane 7 times
  • third intra loop couples to G protein
  • small ligands bind to helix cluster
  • larger ligands bind to extracellular surface
  • process seconds to minutes
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15
Q

examples of GPCR

A
  • mAChR
  • adrenoceptors
  • Serotonin receptor
  • GABA(b) receptor
  • dopamine receptor
  • histamine receptor
  • opiod receptor
  • eicosanoid receptor
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16
Q

function of 2nd messengers

A

activate protein kinases that phosphorylate target proteins

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17
Q

types of 2nd messengers

A
  • cAMP
  • cGMP
  • Diacylgylcerol (DAG)
  • IP3
  • Ca2+
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18
Q

cAMP?

A
  • formed from ATP by adenylate cyclase
  • activates PKA
  • hydrolysis by phosphodiesterase
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19
Q

cGMP?

A
  • formed from GTP by guanylate cyclase
  • activates PKG
  • hydrolysis by phosphodiesterase
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20
Q

DAG and IP3?

A
  • formed from phosphoinositides by phospholipase C
  • IP3 triggers Ca release from ER
  • DAG co-activates PKC
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21
Q

Ca2+ activates?

A
  • PKC
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22
Q

what is kinase-linked receptors?

A
  • intracellular part of receptor has catalytic activity

- especially for hormones

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23
Q

types of kinase-linked receptor

A
  • tyrosine kinase receptor
  • serine/threonine kinase receptor
  • guanylate cyclase
24
Q

tyrosine kinase receptor

A
  • regulate growth, differentiation, development

- receptors for insulin, epidermal growth factor (EGF), platelet-derived growth factor (PDGF) etc

25
Q

serine/threonine kinase receptor

A

eg: tumour growth factor (TGF) Beta receptor

26
Q

what is intracellular receptors?

A
  • in cytosol/nucleus
  • activated receptor bind to DNA and alter genes transcription
  • process minutes to hours
  • for therapeutic consequences
27
Q

intracellular receptors response to

A
  • steroids and vitamin D
  • thyroid hormone
  • inducers of drug metabolism eg: barbiturates
28
Q

functions of peroxisome proliferator-activated receptor

A

regulate genes for lipid, carbohydrate metabolism and transport

29
Q

define desensitization

A

decrease in response to drug with repeated doses

30
Q

examples of desensitization

A
  • accelerated drug clearance
  • reduced receptor response due to modification
  • reduced no. of receptors due to lower expression
  • depletion of mediators eg: NA
  • physiological adaptation
  • drug resistance
31
Q

characteristic of linear plot graph drug-receptor

A
  • hyperbolic curve

- potency

32
Q

characteristic of semi-log graph drug-receptor

A
  • sigmoidal curve

- efficacy

33
Q

define full agonist

A
  • drug that restore maximal response
  • shifting resting state to activated state of receptor
  • efficacy =1
34
Q

define partial agonist

A
  • agonist if work alone
  • act as antagonist when act with other agonist drugs
  • efficacy = less than 1
35
Q

define inverse agonist

A
  • shifting activated receptor to resting state

- cause inactivation of receptor and no response

36
Q

define antagonist

A
  • give equal affinity to both resting and activated receptor
  • inhibit action of agonist but not on itself
  • response not affected and on graph 0
37
Q

2 types of antagonists

A
  • competitive

- non-competitive

38
Q

effect of competitive antagonist

A
  • can be overcome by increasing [agonist]
  • maximal response not affected
  • shifts curve to the right
39
Q

effect of non-competitive antagonist

A
  • cannot be overcome
  • reduces maximal response
  • decrease efficacy
40
Q

candidates for new drugs derive from:

A
  • chemical modification of known molecules
  • screening of natural products
  • rational drug design
  • biotechnology
41
Q

steps of drug development and testing

A
  1. in vitro studies
  2. animal testing
  3. clinical testing/trials (human)
  4. marketing
42
Q

phases in clinical trials

A
  1. is it safe?
  2. does it work?
  3. does it work double-blind?
43
Q

types of tests in preclinical

A
  • molecular screening
  • cellular and tissue screening
  • whole animal studies
44
Q

types of toxicity testing

A
  • acute toxicity
  • subacute and chronic toxicity
  • reproductive toxicity
  • carcinogenicity
  • mutagenicity
45
Q

acute toxicity?

A

effect of large dose up to lethal level

46
Q

subacute and chronic toxicity?

A

effects of multiple doses

47
Q

reproductive toxicity?

A

affect fertility, teratology, lactation, postnatal development

48
Q

mutagenicity?

A

genetic stability of bacteria and mammalian cells in culture

49
Q

limitations of preclinical testing?

A
  1. time and cost for toxic test
  2. need large no. of animals
  3. limits on extrapolation of animal data to humans
  4. rare adverse effect not detected
50
Q

what to do when variable disease happen?

A

use cross-over

51
Q

what happen when other disease influence the test result?

A
  • use cross-over

- proper selection of patients based on medical histories

52
Q

what happen when subject and observer bias?

A
  • use placebo response

- use single and double blind design

53
Q

elaborate phase 1 clinical trials

A
  • is it safe?
  • dose versus effect
  • pharmacokinetics
  • ~ 1 year
54
Q

elaborate phase 2 clinical trials

A
  • does it work?
  • safety and efficacy
  • include single blind crossover design
  • ~ 2- 5 years
55
Q

explain phase 3 clinical trials

A
  • does it work double blind?
  • to verify effectiveness and monitor safety for long term use
  • include double blind crossover design
  • ~ 2- 4 years
56
Q

explain phase 4 post-marketing surveillance

A
  • monitor drug safety under actual use

- to detect any rare adverse effects

pharmacology (2 decks)

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