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Flashcards in Pharmacodynamics Deck (23):
1

how do most drugs produce their effect

by binding to protein molecules

2

what is the only important exception to protein being the receptor for drugs

DNA (sometimes drugs bind to it)

3

two types of ion channels

voltage gated channels and ligand gated ion channel

4

describe voltage gated ion channel

conductance is regulated by changes in the membrane potential

5

describe ligand gated ion channel

conductance is regulated by ligands such as GABA, Ca2+, and etc binding to the channel

6

example of voltage gated ion channel drug and how it works

local anesthetics which block voltage gated sodium channels from transmitting pain information from the periphery to the CNS

7

example of ligand gated ion channel drug

benzos which bind to GABA receptors thereby enhancing the ability of GABA to open chloride channels

8

what does cAMP hormone mediate

-mobilization of stored energy
-increases rate and contraction force of the heart muscle
-relaxation of smooth muscle

9

what degrades cAMP and what is cAMP degraded to

cAMP is degrades to 5'AMP by phosphodiesterases (PDE)

10

big difference between IP3 and DAG

IP3 releases Ca from ER while DAG alongside Ca activates protein kinase C (PKC)

11

examples of ligand regulated transmembrane enzyme

tyrosine kinase, serine/threonine kinase, guanylyl cyclase

12

examples of tyrosine kinases

insulin receptor, epidermal growth factor receptor (EGFR), platelet derived growth factor (PDGFR), nerve growth factor receptor (NGFR)

13

what do cytokine receptors respond to

growth hormone, prolactin, erythropoietin, and interferons
PIGE

14

what does the cytokine receptor bind to

intracellular tyrosine kinase, from the Janus-kinase (JAK) family

15

JAK then phosphorylates another set of proteins referred to as

STAT (signal transducers and activators of transcription) --> pathway is referred to as JAK/STAT pathway

16

what are statins

competitive inhibitors of HMG-CoA reductase, the enzyme that catalyzes the first step of cholesterol biosynthesis

17

what is the result/effect of using statin

it decreases intracellular cholesterol hence causing an up-regulation of LDL receptors in hepatocytes (in order to increase the intracellular cholesterol) and this leads to increased clearance of LDL from the blood

18

what are structural proteins

structures such as tubulin that are important targets for anti neoplastic drugs

19

what type of drugs cause irreversible competitive antagonism

those that have reactive groups hence can form covalent bonds with the receptors

20

examples of drugs that are irreversible competitive antagonist

-phenoxybenzamine (alpha adrenoreceptor blocker)
-aspirin, omeprazole, MAO inhibitors which are irreversible enzyme inhibitors

21

effect of a drug gradually diminishing when giving continuously or repeatedly and occurs within course of few minutes is described as

desensitization or tachyphylaxis

22

gradual decrease in responsiveness to a drug and taking days to weeks to develop is described as

tolerance

23

loss of therapeutic efficacy

refractoriness

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