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Pharmacology > Mechansims Of Drug Action > Flashcards

Mechansims Of Drug Action Flashcards

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

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

A

Mutatation in these receptors causes cancer
Congenital malformations

23
Q

Cytokine receptors

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

A

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

25
Q

Guanylate-cyclase linked receptors

A

Act on 2 types of guanylate cyclase

26
Q

Tumor necrosis factor receptor family

A

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
Q

Toll like receptors

A

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
Q

Notch receptors

A

Ligands= Delta
Regulate cellular fates during embryonic development
Force the neighboring cells to chose a different fate than their own

29
Q

Hedgehog receptors

A

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
Q

Which molecules produce gene transcription through intracellular receptors

A

Thyroid hormones
Vitamin D
Steroids

31
Q

Receptors that produce gene transcription have 3 domains

A

DNA-binding domain
Ligand binding domain
Domain that binds transcription factors

32
Q

When receptors that produce gene transcription are inactive they bind to which molecules

A

HSP

33
Q

Endogenous or Synthetic agonists

A

Bind to receptors and activate them

34
Q

Antagonists

A

Bind to receptors but do not activate them
Inhibit the binding of the agonists
Do not produce any effect

35
Q

Partial agonists **

A

In the presence of antagonist—> act as agonists
In the presence of agonists—> act as antagonists
LOWER EFFECT

36
Q

Inverse agonists

A

Opposite effects of agonists
Reduce the activity below the basal levels
Occupies the receptor so that agonists can not bind

37
Q

Biased agonists

A

Agonist that activates only one portion of a receptors signaling pathway while inhibiting the other portion

38
Q

Types of Antagonism

A

Competitive
Irreversible
Chemical
Physiological

39
Q

Competitive antagonism

A

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
Q

Irreversible antagonism

A

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
Q

Pharmacological antagonism

A

Competitive antagonism
Irreversible antagonism

42
Q

Chemical antagonists

A

Do not require a receptor
One drug inhibits or inactivates other drug

43
Q

Physiological antagonism

A

Drug that counters the effects of another by binding to a different receptor and causing opposing effects

44
Q

Potency

A

Refers to the EC50 or ED50 of the drug
Affinity and coupling efficiency for the drug determines it

45
Q

Efficacy

A

Meausre of the ability of the drug to treat condition it is indicated for
Ability can depend on the ROA, absorption, distribution

46
Q

Therapeutic index

A

TD50/ED50
Median toxic dose/ median effective dose

47
Q

DNEL,NOAEL,LOAEL

A

DNEL: Derived no effect level
NOAEL: No observed adverse effect level
LOAEL: Lowest observed adverse effect level

48
Q

Idıosynchrasy

A

Drug reaction that is not normal, not seen in other patients
Depends on genetics or biological differences
Hypersensitivity

49
Q

Tachyphlaxis

A

Type of tolerance
Tolerance develops so fast

50
Q

Continuous administration of an agonist may produce

A

Tolerance
Overshoot —> the number of receptors decrease the effector systems become more hypersensitive

51
Q

Up-regulation
Down-regulation

A

Up-regulation: increase in the number of receptors
Down-regulation: decrease in the number of receptors

52
Q

Desensitization

A

Effect of drug is decreased due to function of receptors affected
2 types: Homologus,Heterologous

Pharmacology (6 decks)

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