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Pharmacology > Mechansims Of Drug Action > Flashcards

Mechansims Of Drug Action Flashcards

(52 cards)

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1
Q

Drug effects vs drug action

A

Drug effects on human body
Drug action at cellular or molecular level

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2
Q

Which molecule is needed for drugs to work

A

Protein molecules = receptors, regulatory proteins, enzymes, transport proteins, structural proteins, tumor antigens
But drugs do not necessarily affect the proteins always

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3
Q

What is responsible for the selectivity of drug action

A

Receptors

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4
Q

Types of bonds between drugs and the sites

A

Weak hydrogen bonds
Ionic bonds
Covalent bonds
Van der Walz bonds

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5
Q

Important receptors for drugs

A

Tumor necrosis factor receptors
Toll-like receptors
Notch receptors
Hedgehog receptors

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6
Q

Which receptor activated by IL-1

A

Sphingomyelinase-linked receptor

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7
Q

How do the receptors function

A

Receptors should be activated by signals
Signal should be transduced
Transduced signal should be amplified

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8
Q

Ionotropic receptors

A

Effects are observed very fast
Receptor itself a channel for the ion
Nicotonic receptors : Na channel
GABAa receptors: Cl channel

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9
Q

Metabotropic receptors ( G-protein coupled receptors)

A

Linked to G-protein
Slow
Muscarinic
5-HT
Opioid
Dopaminergic
Peptide transmitters
Adrenoceptors
Olfactory sensory receptors
GPCRs

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10
Q

Features of G-protein coupled receptors

A

G proteins are associated with GTP,GDP
G proteins have 3 subunits: alpha,beta,gamma

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11
Q

Receptors has two states

A

Resting state
Activated state —> Ga leaves and activates Adenylyl cyclase which produces cAMP

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12
Q

Targets of G-proteins

A

Adenylate cyclase system
Phospholipase C/ Inositol phosphate system
Regulation of ion channels

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13
Q

Functions of G-proteins

A

3 types of Galpha: Gs, Gi, Gq
Gs and Gi show affinity to Adenylate cyclase
Gi inhibts Adenylate cyclase
Gs activates Adenylate cyclase
Gq controls Phospholipase C

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14
Q

Phospholipase C/ İnostiol phosphate system

A

Activation of this system is the second important messenger system
PLC— PIP2— IP3+DAG
IP3—> release of Ca
DAG—> activates Protein Kinase C

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15
Q

Muscarnic receptors

A

In myocardium
Conductance of K channels and produce hyperpolarication, inhibition of the cell

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16
Q

Opioids receptors

A

Open K channels and produce hyperpolarization

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17
Q

Gs
Effector ?
Effects?

A

Effector= Adenylate cyclase —> Stimulation
= Ca channels—> Stimulation
= Na channels—> Inhibition

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18
Q

Gi
Effector?
Effects?

A

Effector= Adenylate cyclase—> Inhibiton
= Ca,Na,K channels—> Inhibiton

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19
Q

Gq
Effector?
Effects?

A

Effector= PLC,PLA2—> Stimulation
* specific for eye

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20
Q

Features of Tyrosine kinases linked receptors

A

Growth factors, cytokines and insulin receptors
Extracellular ligand binding site
Intracellular polypeptide chain
Stimulation of these causes dimerization of receptors and activation of thyrosine kinase

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21
Q

Growth factors that activate Thyrosine Kinases

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A

Epidermal Growth Factor= stimulates proliferation and differentiation of epi cells
Platelet-derived growth factor= stimulates growth of smooth muscle cells,glial cells and fibroblasts

22
Q

Thyrosine kinase receptor diseases

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A

Mutatation in these receptors causes cancer
Congenital malformations

23
Q

Cytokine receptors

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A

Activated by bringing together two JAK kinases
JAKs activate STATs
STATs are the transcriptional factors that regulate gene expression

24
Q

Serine/Threonine Kinases Receptor

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A

Growth factor receptors
Activated by the formation of dimeric structure
Activate Smads—> controls cellular proliferation and differentiation

25
Guanylate-cyclase linked receptors
Act on 2 types of guanylate cyclase
26
Tumor necrosis factor receptor family
Lymphocytes produce 3 forms of TNF Shock and inflammation Killing tumor cells Protection from bacterial infections Development of the immune system Regulate Cell proliferation Regulate Death Alter gene expression by activating NF-kB
27
Toll like receptors
Sense and responses to infection Required for resistance to fungal infections Dimeric TLRs on the plasma membrane of DCs —> sense foreign molecules and respond by secreting TNF,IL-1,IL-6 TLR3 located in endosomes which binds to dsRNA
28
Notch receptors
Ligands= Delta Regulate cellular fates during embryonic development Force the neighboring cells to chose a different fate than their own
29
Hedgehog receptors
Two membrane proteins= Patched, Smoothened Required for signal transduction during development Regulate cellular differentiation Formation of neural tube Mutation of this causes developmental defects Patched mutation causes basal cell carcinoma Smoothened is a proto-oncogene
30
Which molecules produce gene transcription through intracellular receptors
Thyroid hormones Vitamin D Steroids
31
Receptors that produce gene transcription have 3 domains
DNA-binding domain Ligand binding domain Domain that binds transcription factors
32
When receptors that produce gene transcription are inactive they bind to which molecules
HSP
33
Endogenous or Synthetic agonists
Bind to receptors and activate them
34
Antagonists
Bind to receptors but do not activate them Inhibit the binding of the agonists Do not produce any effect
35
Partial agonists **
In the presence of antagonist—> act as agonists In the presence of agonists—> act as antagonists LOWER EFFECT
36
Inverse agonists
Opposite effects of agonists Reduce the activity below the basal levels Occupies the receptor so that agonists can not bind
37
Biased agonists
Agonist that activates only one portion of a receptors signaling pathway while inhibiting the other portion
38
Types of Antagonism
Competitive Irreversible Chemical Physiological
39
Competitive antagonism
Compete for the receptor against the agonists Higher concentrations are required for full inhibition E max does not change Reversible if agonist concentration is increased
40
Irreversible antagonism
Bind to receptors at very high affinity Bind irreversibly Produce ab uncompetitive antagonism Spare receptors can stop them to produce irreversible effects E max can not be reached
41
Pharmacological antagonism
Competitive antagonism Irreversible antagonism
42
Chemical antagonists
Do not require a receptor One drug inhibits or inactivates other drug
43
Physiological antagonism
Drug that counters the effects of another by binding to a different receptor and causing opposing effects
44
Potency
Refers to the EC50 or ED50 of the drug Affinity and coupling efficiency for the drug determines it
45
Efficacy
Meausre of the ability of the drug to treat condition it is indicated for Ability can depend on the ROA, absorption, distribution
46
Therapeutic index
TD50/ED50 Median toxic dose/ median effective dose
47
DNEL,NOAEL,LOAEL
DNEL: Derived no effect level NOAEL: No observed adverse effect level LOAEL: Lowest observed adverse effect level
48
Idıosynchrasy
Drug reaction that is not normal, not seen in other patients Depends on genetics or biological differences Hypersensitivity
49
Tachyphlaxis
Type of tolerance Tolerance develops so fast
50
Continuous administration of an agonist may produce
Tolerance Overshoot —> the number of receptors decrease the effector systems become more hypersensitive
51
Up-regulation Down-regulation
Up-regulation: increase in the number of receptors Down-regulation: decrease in the number of receptors
52
Desensitization
Effect of drug is decreased due to function of receptors affected 2 types: Homologus,Heterologous

Pharmacology (6 decks)

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