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Pharmacology > Intro to Pharm > Flashcards

Intro to Pharm Flashcards

1
Q

• The study of the effects of drugs on the function of

living systems

A

Pharmacology

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2
Q

A chemical substance of known structure, other
than a nutrient or an essential dietary ingredient,
which, when administered to a living organism,
produces a biological effect

A

Drug

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3
Q

inverse proportionality between pressure and volume of gas

A

Boyle’s Law:

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4
Q 
• Father of Modern Chemotherapy
— German physician-scientist
— How to differentiate healthy 
tissue from invading pathogen?
— Staining techniques led 
eventually to Gram staining
— arsphenamine (Salvasan)
* Treatment of syphilis
— 1908 Nobel Prize 
* contributions to immunology
A

Paul Ehrlich (1854-1915)

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5
Q
  • Absorption
  • Distribution
  • Metabolism
  • Excretion of drugs
A

Pharmacokinetics

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6
Q
  • Drug-receptor interactions
  • Signal transduction
  • Drug effects
A

Pharmacodynamics

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7
Q
  • the metabolic fate of a drug based on individual genetic differences
  • study of genetic influences on the responses to drugs
A

Pharmacogenetics

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8
Q

• the genetic basis of a drug’s absorption, distribution, metabolism, excretion, and receptor-target affinity
— the genetic basis of a drug’s pharmacokinetics and pharmacodynamics
— an extension of pharmacogenetics
• use of genetic information to guide the choice of drug therapy on an individual basis

A

Pharmacogenomics

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9
Q

• The study of drug effects at the population
level
• Concerned with variability of drug effects
between individuals in a population and
between populations
• Made possible with “Big Data” sets

A

Pharmacoepidemiology

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10
Q

• The study of cost and benefits/detriments
of drugs used clinically
• Made possible with “Big Data” sets

A

Pharmacoeconomics

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11
Q

— administrative body that oversees drug

evaluation process

A

U.S. Food & Drug Administration (FDA)

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12
Q

____ grants approval for marketing new
drug products
— evidence of safety and efficacy
— “safe” does not mean complete absence of risk

A

FDA

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13
Q

— prohibited full FDA review of supplements and botanicals as drugs
— established labeling requirements for dietary supplements
- burden of proof of safety/effectiveness is on manufacturer not on FDA

A

Dietary Supplement Health and Education Act (1994)

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14
Q

________ as defined by FDA
• A substance recognized by an official pharmacopoeia or
formulary
• A substance intended for use in the diagnosis, cure,
mitigation, treatment, or prevention of disease
• A substance (other than food) intended to affect the
structure or any function of the body
• A substance intended for use as a component of a
medicine but not a device or a component, part or
accessory of a device
• Biological products are included within this definition
and are generally covered by the same laws and
regulations, but differences exist regarding their
manufacturing processes (chemical process versus
biological process.)

A

Drug

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15
Q

________ as defined by FDA
• It is the same as a brand name drug in dosage,
safety, strength, how it is taken, quality, performance, and
intended use
• Before approving a generic drug product, FDA requires many
rigorous tests and procedures to assure that the generic drug
can be substituted for the brand name drug
• The FDA bases evaluations of substitutability, or therapeutic
equivalence of generic drugs on scientific evaluations
• By law, a generic drug product must contain the identical
amounts of the same active ingredient(s) as the brand name
product
• Drug products evaluated as “therapeutically equivalent” can
be expected to have equal effect and no difference when
substituted for the brand name product

A

Generic drug

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16
Q

What are the 5 protein targets for drug binding?

A
  • Receptors
  • Enzymes
  • Carrier Molecules (Transporters)
  • Ion Channels
  • Specific Circulating Plasma Proteins
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17
Q 
• Protein molecule which function to 
recognize and respond to 
endogenous chemical signals
— protein molecules which function to 
recognize specific endogenous ligands
— may also recognize/bind xenobiotics
• Classified based on ligands
— increasing focus on developing new 
classification system based on 
genomics
A

Drug receptor

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18
Q

• For a drug to be useful:
— must act selectively on particular cells and
tissues
— must show a high degree of binding site
specificity

A

Drug Specificity

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19
Q

For a _____ to function as a receptor:
— generally shows a high degree of ligand
specificity
— bind only molecules of certain physico-
chemical properties
* size, shape, charge, lipophilicity, etc

A

protein

20
Q

(Drug-receptor interactions)
(most common)
— weaker: hydrogen bonding and van der Waals forces (dipoles)
— stronger: ionic bonding

A

Electrostatic

21
Q

(Drug-receptor interactions)
(less common)
— weak associations of hydrophobic compounds with hydrophobic domains of receptors

A

Hydrophobic

22
Q 
(Drug-receptor interactions)
 (relatively rare)
— permanent, lasting bonding
— aspirin and cyclooxygenase
— omeprazole and proton pump
A

Covalent

23
Q 
— more soluble in oil than water
* i.e. more soluble in fat than blood
— steroids
— readily diffuse across membranes
— more likely to by metabolized by gut and liver
A

Lipophilicity

24
Q

— more soluble in water than oil
* i.e. more soluble in blood than fat
— small molecules, weak acids/bases
* ionized at physiologic pH (7.4)
— not as easy to diffuse across plasma membranes
— more likely to be excreted unchanged by kidney

A

Hydrophilic

25
Q

____ is the pH at which the concentrations of

ionized and unionized species are equal

A

pKa

26
Q

— tendency of a drug to bind to the receptor
— dissociation constant (Kd) = concentration required for 50% saturation of available receptors
— inversely proportional to affinity
* higher the Kd (nM), lower the affinity

A

Affinity

27
Q

— tendency of a drug to activate the receptor once bound

— generally expressed as dose-response curves or concentration-effect curves

A

Efficacy

28
Q

— posses significant efficacy

A

Agonist

29
Q

= elicits maximal response

A

full agonist

30
Q

= elicits partial response, even when 100% of receptors are occupied

A

partial agonist

31
Q

— possess zero efficacy

A

Antagonist

32
Q

— bind to the same receptor, but do not prevent binding of the agonist
— can may enhance or inhibit the action of agonists

A

Allosteric Agonists and Antagonists

33
Q

If you add an antagonist to an agonist, how will the dose response curve shift?

A

Shifts to right

34
Q

If you add an allosteric inhibitor to an agonist, how will the dose response curve shift?

A

Flattens curve

35
Q

— high affinity for Ra and stabilize Ra on binding
— shift nearly entire pool of receptors from Ri to Ra-D (Ra bound to drug)
— maximal effect is produced

A

• Full Agonist

36
Q

— do not stabilize Ra as effectively
— significant fraction stays in Ri-D pool
— only partially effective no matter how high concentration
— some can act as agonist (if no full agonist is present) or antagonist (if if full agonist is present)
* e.g. pindolol, b-adrenergic receptor antagonist when epinephrine is present; agonist when absent (“intrinsic sympathomimetic activity”)

A

• Partial Agonist

37
Q

— Ra-D and Ri-D stay in same relative amounts as in the absence of any drug
— no change in effect measured
— block effects of agonist (neutral antagonist)

A

• Antagonist

38
Q

— higher affinity for Ri than for Ra
— stabilize Ri on binding
— reduces any constitutive activity of receptor thus producing opposite effects as a conventional agonist
* e.g. g-aminobutyric acid (GABA) receptors; diazepam agonist, flumazenil antagonist, experimental compounds act as inverse agonist

A

Inverse Agonist

39
Q

= equilibrium dissociation constant or concentration

of drug where 50% of receptors are bound

A

Kd

40
Q

= concentration of drug that produces 50% of

maximal effect/response

A

EC50

41
Q

— bind to same site on receptor as agonist
— compete with agonist for binding
— with fixed agonist concentration, progressive increases in antagonist will progressively decrease effect up to completely abolishing it
— increasing agonist concentration can overcome competitive antagonist

A

• Competitive Antagonist

42
Q

— often bind covalently and irreversibly
— often allosteric inhibition but can be same binding site as agonist
— increasing agonist concentration may not overcome noncompetitive antagonist

A

Noncompetitive Antagonist

43
Q

— for example: ionic interaction between positively charged protamine and negatively charged heparin
* protamine antagonizes heparin

A

Chemical Antagonist

44
Q

— for example: different regulatory pathways mediated by different receptors resulting in opposing actions
* anticholinergic atropine can physiologically antagonize effects of b-blockers on heart rate

A

Physiologic Antagonist

45
Q

— one drug increases the metabolism of the other

* rifampin increases metabolism of many drugs

A

Pharmacokinetic Antagonist

46
Q 
— change in receptors
* phosphorylation of receptor
— translocation of receptors
* b-adrenergic receptor internalization
— exhaustion of mediators
* neurotransmitter depletion
— increased drug metabolism
— physiologic adaptation
* blood pressure lowering from a diuretic
— active extrusion of drug from cell
* multi-drug resistance (P-glycoprotein)
-down regulation
A

• Desensitization (a.k.a. Tachyphylaxis)

Pharmacology (12 decks)

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