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BIOM 3090 > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

Drugs are categorized (scheduled) based on…..

A

-Safety concerns
-Abuse potential
-Ability of patients to understand and execute directions for their use

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2
Q

Scheduling of drugs/products dictates………

A

-How drug is obtained by the patient
-How drug is prescribed by physician for dispensing from a pharmacy

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3
Q

NAPRA I

A

Prescription needed for sale by Pharmacist; includes prescription drugs (Pr) ie found on the PDL, also narcotics (N), Controlled substances (C1, C2, C3) and targeted substances (TS) eg. Fentanyl patch

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4
Q

NAPRA II

A

Prescription not required; must be
dispensed by pharmacist ie. behind
the counter eg. insulin

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5
Q

NAPRA III

A

Client may obtain at pharmacy
without need of pharmacist eg.
ranitidine (ZantacⓇ )

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6
Q

Unscheduled

A

Client may obtain at retail stores
as well as pharmacy eg. naproxen
(Aleve Ⓡ )

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7
Q

The actions of drugs on the body are termed

A

Pharmacodynamics

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8
Q

The actions of the body on drugs is termed

A

Pharmacokinetics

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9
Q

At room temperature, most drugs are

A

Solid (e.g. aspirin)

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10
Q

Useful drugs must

A

-Have properties enabling transport from the site of administration to the target site (aka biophase)
-Be inactivated and excreted from the body at a reasonable rate to avoid duration of action concerns

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11
Q

Macromolecular components of the organism are called

A

Receptors

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12
Q

Most drugs are

A

Small organic molecules that produce effects by reacting with receptor

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13
Q

Proteins represent the most important type of receptor for drugs (4 examples)

A
  • some hormones eg. insulin, growth factors, neurotransmitters
  • enzymes for metabolic pathways
  • transporters eg. Na+ , K+ -ATPase
  • structural proteins eg. tubulin and nucleic acids
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14
Q

Physiological receptors

A

Regulatory proteins in the plasma
membrane of cells

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15
Q

Signal transduction pathway

A

The receptor, its cellular target and any intermediary molecules

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16
Q

Drugs that do not act on receptors

A

-Antacids directly neutralize HCl in the stomach
-Osmotic diuretics eg. mannitol promote increased urine formation by osmotic forces in the lumen of renal tubules

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17
Q

Proteins consist of a sequence of aa’s determined by DNA code called

A

Primary structure

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18
Q

Protein aa’s interact with other nearby aa’s on the same protein (is called..)

A

Secondary structure

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19
Q

Tertiary structure results from

A

Interaction of more distant aa’s along the protein molecule (
Hydrogen, ionic and covalent (disulfide) bonds)

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20
Q

Multiple polypeptides can interact to form more complex structures called

A

Quaternary structure

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21
Q

Favorability of a drug-receptor binding interaction is called

A

Affinity

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22
Q

In order for drugs to interact selectively with receptor binding
sites, they need to possess adequate

A

-size
-shape
-charge and atomic composition

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23
Q

Size (Lower limit)

A

minimum size needed to impart specificity of action and allow binding to select receptors

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24
Q

Size (Upper limit)

A

size limit allowing reasonable movement in the body to sites of action

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25
Q

Size (Lower limit)

A

size limit allowing reasonable movement in the body to sites of action

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26
Q

Where must very large drugs (eg. Protein therapeutics) often be administered?

A

directly into compartments where they have effects

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27
Q

Drugs and receptors interact by means of

A

Chemical forces or bonds

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28
Q

Drugs that bind thru multiple weak bonds to their receptors require

A

More precise fit (are more selective)

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29
Q

Bond strength order

A

Covalent > ionic > hydrogen >
van der waals

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30
Q

Covalent bonds are usually

A

Irreversible (few drugs rely on these receptors, must synthesize new receptors)

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31
Q

Intermolecular Interactions

A

Sum total of forces imparts high
affinity of the drug for receptor

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32
Q

Enantiomers

A

S (left-handed) and R (right-handed;) nomenclature based on organization of the atoms attached to the chiral center

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33
Q

Ranitidine (what is it and what does it do)

A

H2 (histamine receptor) antagonist or blocker
-Used to treat gastroduodenal ulcers by reducing HCl production

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34
Q

Lidocaine

A

Na+ channel blocker
-Highly expressed in several tissues
-Widespread adverse effects possible in CNS and heart if drug reaches the systemic circulation

35
Q

2 major functions of physiological receptors

A
  • ligand binding via ligand-binding domain
  • message propagation via effector domain
36
Q

Drugs modify cellular function after binding to receptors

A

-initiate
-enhance
-diminish
-terminate (block)

37
Q

4 major types of drug receptors

A

-Transmembrane
Ion Channels
-Transmembrane
G-protein Coupled
-Transmembrane
Enzymatic Cytosolic Domain Coupled
-Intracellular

38
Q

Polar (charged) anions and cations have key roles in

A

-Neurotransmission
-Cardiac conduction
-Smooth and Skeletal Muscle contraction
-Secretion

39
Q

Ion channels can be classified based on: (3)

A
  • Architecture ie. subunits
  • Ions conducted thru the channel
  • Mechanism of activation
  • Ligand and Voltage activated channels
    are major drug targets
40
Q

Major ligand gated channels are found in the _______ and list 2 examples

A

CNS,

41
Q

2 excitatory NTs

A

ACh or glutamate

42
Q

2 Inhibitor NTs

A

glycine or GABA

43
Q

One ligand gated channel

A

nicotinic acetylcholine receptor

44
Q

nicotinic acetylcholine receptor in the closed state

A

Channel pore is occluded by bulky amino acid side chains

45
Q

Full opening (activation) of the nicotinic acetylcholine receptor channel occurs with

A

Binding of 2 molecules of ACh to the α subunits and
a conformational change = pore opening

46
Q

Electrolytes passed in nicotinic acetylcholine receptor channel

A

Na+ is the major electrolyte passed; K+ can also pass

47
Q

How can refractory period be prolonged

A

Local anesthetics eg. lidocaine
bind to the channel

48
Q

Sulfonylurea receptor (SUR1)

A
  • Regulates the ATP-dependent K+ channel in pancreatic β-cells
  • Sulfonylurea class oral hypoglycemics eg. Glipizide facilitate closure of the channel and secretion of insulin by binding to the
    SUR1 receptor
49
Q

Most abundant
class of receptors in the body

A

G-protein coupled receptors (GPCRs)

50
Q

How many GPCRs do humans express and what are majority dedicated to

A

Humans express over 800 GPCRs
* Over half dedicated to sensory perception (sight, taste, smell)
(Remainder dedicated to regulating nerve activity, tension in smooth
muscle, metabolism, force and rate of cardiac contraction, and
secretion of most glands)

51
Q

G proteins

A

intracellular heterotrimeric GTP-binding regulatory proteins termed G proteins

52
Q

Signals from G proteins are usually terminated by

A

hydrolysis of GTP to GDP by inherent GTP-ase activity of the α subunit

53
Q

One major role for G proteins is to activate ________ _______ that produce _______ _______

A

Effector molecules, second messengers

54
Q

Well characterized effector molecules

A

adenylyl cyclase, guanylyl cyclase, phospholipase C, various ion channels

55
Q

One important receptor class in the G protein receptor family is
the

A

β-adrenergic receptor group

56
Q

Catecholamines (epinephrine and norepinephrine) are ____________ and what do they do

A

endogenous ligands
-Stimulate the production of second messenger cAMP and cellular effects based on tissue localization

57
Q

Key G protein mediated second messengers (4)

A

-cGMP
-IP3
-cAMP
-DAG

58
Q

Transmembrane
Receptors with Enzymatic Cytosolic Domains role

A

play important roles in cell metabolism, growth
and differentiation……tonic activation can cause tumors

59
Q

A difference between Transmembrane
Receptors with Enzymatic Cytosolic Domains and G proteins

A

Consist of single membrane spanning proteins compared to the
seven membrane spanning G protein receptors

60
Q

Many transmembrane
Receptors with Enzymatic Cytosolic Domains form ______ or ________ _______ to transmit their signals

A

dimers, multisubunit complexes

61
Q

Transmembrane
Receptors with Enzymatic Cytosolic Domains activity inclues

A

adding/removing phosphate
groups from specific aa’s

62
Q

2 examples of Transmembrane Receptors with Enzymatic Cytosolic Domains

A

-Receptor tyrosine kinases
-Tyrosine kinase-associated receptors

63
Q

Receptor tyrosine kinases RTKs) include

A

SH2 domains on other signaling molecules (such as Grb2)

64
Q

Receptor tyrosine kinases include endogenous ligands such as

A

Insulin, PDGF, VEGF

65
Q

Tyrosine Kinase-Associated Receptors include ______ receptors

A

cytokine

66
Q

Tyrosine Kinase-Associated Receptors hormones

A

growth hormone and prolactin

67
Q

Do Tyrosine Kinase-Associated Receptors have enzymatic activity

A

No

68
Q

JAK/STAT pathway simplified

A
  • Dimerization allows for binding of an intracellular
    tyrosine kinase ie. Janus Kinase (JAK)
  • JAKs phosphorylate other proteins (STAT) which translocate to the nucleus
69
Q

Two types of intracellular receptors

A

-nuclear hormone receptors
-NO synthase and soluble guanylyl cyclase

70
Q

Nuclear hormone receptors

A

Circulating steroid hormones are lipophilic diffusing thru the plasma
membrane to bind transcription factors = modify nuclear events

71
Q

Nuclear hormone receptors possess

A

a ligand binding domain and a DNA binding domain

72
Q

(Nuclear hormone receptors) nuclear events depend on

A

which co-activators or co-repressors of gene transcription are recruited

73
Q

Nuclear hormone receptors gene transcription duration

A
  • Gene transcription is slow (min to hrs) but usually long-lasting
  • Lag on (slow onset of cellular effects)
  • Lag off (slow offset of cellular effects)
  • eg. Glucocorticoids (dexamethasone)
74
Q

Isoforms of NO and where is it produced

A

-Endothelial (eNOS)
-Inducible (iNOS)
-Neuronal (nNOS)

75
Q

What does NO bind to and what does it do

A

NO binds to the N-terminal domain of soluble GC (guanylyl cyclase) and enhances (200-
400X) its activation of cGMP

76
Q

Vascular smooth muscle effects of cGMP and what are they due to

A
  • Mainly due to cGMP acting on PKG
  • Vasodilation from reduced
    intracellular calcium levels
    eg. nitrovasodilators and
    angina pectoris
77
Q

Drug receptors outside of PM for communication

A
  • Vasoconstriction: ACE inhibitors eg.enalapril for hypertension
  • Neurotransmitters: Acetylcholinesterase inhibitors eg. tacrine
    for treatment of Alzheimer’s disease
78
Q

Drug receptors that provide a cell surface adhesion function

A
  • Allows cell-cell interaction for various functions eg. inflammation,
    coagulation (eptifibatide an antagonist of the platelet GPIIb-IIIa receptor)
79
Q

Drug receptor providing structural role for cell

A

Antineoplastics: Microtubule inhibitors eg. paclitaxel for cancer therapy

80
Q

How do cells integrate multiple signals to produce a coherent cellular response?

A

Signaling convergence by second messengers can generate coordinated net cellular effects

81
Q

The magnitude of a cellular response to a ligand is generally ________ than the initiating stimulus

A

greater

82
Q

Small influx of Ca2+ thru
voltage gated Ca2+ channels triggers the release of _________
amounts from intracellular stores

A

large

83
Q
A

BIOM 3090 (12 decks)

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