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Pharmacology-1 > General Principles > Flashcards

General Principles Flashcards

1
Q

Pharmacokinetics

A

What the patient does to the drug

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2
Q

Pharmacodynamics

A

What the drug does to the patient

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3
Q

Drug

A

any substance that changes biologic fnx through chemical aciton

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4
Q

agonist

A

activating drug

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5
Q

inhibition

A

antagonist drug

-can be overcome by increasing dose

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6
Q

Hormones/Xenobiotics/Poisons

A

endogenous/exogenous/usually harmful effects

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7
Q

side effect

A

harm at therapeutic doses

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8
Q

toxicity

A

may refer to sideeffects or commonly to adverse effects related to supratherapeutic dosing

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9
Q

What are 3 drug principles?

A
  1. MW ~100-1000 g/mol
  2. receptor interaction through bonding (electrostatic, ionic or covalent)
  3. drug shape confers specificity (stereoisomers impt)
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10
Q

steroisomerism

A
  • whenever C binds 4 diff groups there are two ways this can occus
    1. handedness
    2. chirality
  • drugs are manufactured and given as racemic mixtures–>one is more active than the other.
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11
Q

Which isomer is more active?

A

the one with the flat, hydrophobic reguins,

-less reactive isomer is the one with polar region

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12
Q

Allosteric interactions

A
  • substances that bind to receptors, but not at the same site as drug agonist
  • may inhibit or activate receptor
  • cannot be overcome by increasing drug dose
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13
Q

Draw the dose response curve

A
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14
Q

Partial Agonist

A

Binds receptor and activates it to less degree of a full agonist

  • less intrinsic efficacy–>increase dose does not overcome limitation
  • seen clinically
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15
Q

What would happen if you have an partial agonist opiod to a patient already on a full agonist opioid medicine?

A
  • partial agonist will act as an antagonist
  • competes w/ full agonist for the receptor
  • prevents full efficacy (bc doesn stabilize the activated form of the receptor)
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16
Q

Inverse agonist

A

-binds to receptor and decreases effect

(stabilized the inactive form of the receptor reducing activity below baseline)

  • like an antagonist, but not
  • ex. Antihistamines
17
Q

Neutral Antagonist

A

“fixes” the ratio of active and inactive forms of receptor

prevents any effect of agonist drugs if present in sufficient quantity

-not used clinically

18
Q

Dose response curve for Full, partial, and inverse agonist

A
19
Q

Drug duration

A

generally as long as a drug occupies receptor,

covalent binding to R may require generation of new R to terminate action

20
Q

Binding selectivity

A

many drugs selective for receptor, inert binding sites affect drug distribution

21
Q

Action of drugs

A
  1. absorbed from site of administration
  2. Distributed through body tissues
  3. Metabolized
  4. Eliminated
22
Q

What are the different types of drug permeation?

A
  1. aqueous diffusion
  2. lipid diffusion
  3. special carriers (esp. large molecules)
  4. Endo/exocytosis
23
Q

Are drugs weak acids and bases?

A

yes,

carbaxylic acids, amine bases

-both protonated and unprotonated forms found at physiologic pH

24
Q

What is the equation for the ratio of conjugate acid to conjugate base

A

log (protonated/unprotonated)= pka-pH

lower pH=more protonated

high pH=less protonated

-pka=pH where molecules is 1/2 dissociated

25
Q

Explain Ion trapping

A
  • generally only uncharged molecules diffuse passively across cell membranes
  • can manipulate pH of body fluids by giving NH4Cl or NaHCO3 to trap drugs by keeping them ionized
26
Q

Zero-Order

A

rate of drug elimination is constant regardless of drug concentration

27
Q

When would you see zero-order elimination?

A

when metabolism/elimination pathways are saturated

ex. seen clinically w/ EtoH and aspirin

28
Q

First Order Elimination

A
  • rate of drug elimination is proportional to the drug concentraion
  • Hyperbolic curve
  • most drugs have 1st order elimination
29
Q

1st order semi-log plot

A
  • slope of line is related to half-life
  • steeper=shorter 1/2 life
  • half life concept only works for 1st order elimination kinetics
30
Q

Half-Life

A

Time to eliminate 1/2 of the drug

Pharmacology-1 (15 decks)

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