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PSYC475 psychopharm > pharmacokinetics / pharmacodynamics > Flashcards

pharmacokinetics / pharmacodynamics Flashcards

(81 cards)

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1
Q

ADME

A

Absorption
Distribution
Metabolism
Elimination

ADME = bioavailability

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2
Q

pharmacokinetics studies…

A

how does a drug get to its target?

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3
Q

pharmacodynamics studies…

A

when a drug binds to its target, what is the effect?

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4
Q

absorption includes…

A

how does a drug get into the bloodstream?

ROA

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5
Q

enteral ROA

A

(through the GI tract)
oral
rectal

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6
Q

parenteral ROA

A

(non GI)
injection
inhalation
topical (skin)
mucousal / sublingual

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7
Q

requirements for oral ROA

A

water soluable

stable / resistant to stomach acids & enzymes and liver enzymes

partially lipid soluable

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8
Q

first pass metabolism

A
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9
Q

prodrug

A
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10
Q

advantages / disadvantages of oral ROA

A

+: easy / non invasive
-: stomach upset / nausea ; actual concentration in blood stream less accurate compared to parenteral; many drugs cannot withstand GI tract

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11
Q

common drug abbreviations

A

ac – before meals
pc – after meals
hs – at bedtime
NTE – not to exceed
prn – as needed (also qs)
qXh – every X hours
qd – once daily
bid – twice a day
tid – 3 times a day
qid – 4 times a day
XR – extended release

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12
Q

rectal ROA advantages / disadvantages

A
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13
Q

parenteral ROA advantages / disadvantages

A
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14
Q

IV ROA advantages / disadvantages

A
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15
Q

IM ROA advantages / disadvantages

A
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16
Q

subcutaneous ROA advantages / disadvantages

A

Advantages:
-fairly rapid

Disadvantages:
-Large volumes not recommended
-Skin irritation

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17
Q

inhalation ROA advantages / disadvantages

A

Advantages:
Extremely rapid – can be even faster than i.v.!
Rapid accumulation in brain

Disadvantages:
Extremely rapid
lung irritation, possible
lung disease with
repeated administration

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18
Q

mucosal ROA advantages / disadvantages

A
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19
Q

sublingual / buccal ROA advantages / disadvantages

A

Advantages: non-invasive, relatively easy, does not go through GI system (more drug gets into system)

Disadvantages: may be unpleasant, have to be able to hold substance in mouth and not swallow

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20
Q

topical ROA advantages / disadvantages

A
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21
Q

Cmax

A

highest level of concentration in blood

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22
Q

bioavailability

A

% of drug in system (compared to IV administration)

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23
Q
A
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24
Q

volume of distribution (define)

a higher Vd is associated with________

A

The volume necessary to contain the total amount of administered drug at the same concentration observed in plasma.

In general, higher Vd is associated with:
longer excretion time
more drug needed to get into brain
longer time to get into brain

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25
26
BBB
27
28
29
metabolism is...
how are drugs broken down
30
31
most common route of elimination
kidney
32
drug half life
33
34
**drug accumulation
If a second dose of drug is given before the first dose is eliminated, the overall concentration in the blood will be greater than that of the first dose alone. With repeated administrations, concentrations are additive. If 100 mg of a drug with a half-life of 4 hrs is given at noon, at 4:00pm there will be 50 mg in the blood. If another 100 mg of drug is given at 4:00pm, how much drug will be in the blood at 8:00pm? 75 mg = 25mg (1st dose; 2nd half-life) + 50mg (2nd dose; 1st half-life)
35
**steady state concentration
Consistent level of drug in body achieved by repeated, regular-interval dosing ~4-6 half-lives 1st = 50% 2nd = 75% 3rd = 87.5% 4th = 93.75% 5th = 96.875% 6th = 98.44% At steady state the amount of drug eliminated per unit time is equal to the amount of drug absorbed per unit time
36
theraputic drug monitoring
37
drug tolerance
A progressive decline in response with repeated usage of a drug.
38
types of drug tolerance
1: Metabolic tolerance Usually due to upregulation of enzymes 2: Pharmacodynamic tolerance Down-regulation of receptors or sensitivity 3: Behavioral conditioning (learning) Homeostatic theory Physiological processes can be conditioned to specific stimuli or environments
39
dependence
Administration of drug is required to avoid withdrawal symptoms
40
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special populations? considerations?
1: pregnant people 2: children 3: elderly
42
3 reasons drugs may differ in their effectiveness
1: different mechanisms 2: lipid soluability 3: affinity for site of action
43
bonds formed between drug and receptor are typically ______
ionic (weak, reversible)
44
3 types of drug names
1: chemical 2: generic 3: trade
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47
how do ionotropic receptors work?
Ionotropic receptors have recognition sites located on the ion channel. Activation of receptor change shape of channel fast / brief / rapid open and close / affect membrane voltage
48
metabotrophic receptors
A recognition site extends into the extracellular fluid, and a special protein called a G protein is located on the receptor’s intracellular side. G proteins can open nearby ion channels or activate second messengers. slower / longer / varied effects actions can be direct or indirect
49
competitive vs noncompetitive binding
Competitive Binding: Drug occupies the same binding site on the receptor that the NT occupies -drug with higher affinity / concentration wins Noncompetitive Binding: Drug occupies a different binding site on the receptor than the NT
50
isomers
Molecules that have the same molecular formula, but a different shape: Same “ingredients” - put together in diff ways Isomers bx diff
51
optical isomers
Isomers that are mirror images of each other Enantiomers The distinction is important, as often only one form will be biologically active, or the different forms will produce different effects
52
53
racemic mixture / racemate
Most substances contain both isomers in equal proportions (50% L and 50% D) Only ½ the molecules are biologically active
54
why purify a racemate?
By purifying a racemic mixture so that the drug only contains the biologically active isomer, a drug’s potency can be increased.
55
why do side effects happen
Same receptors responsible for multiple bx , or sometimes other receptors / systems activated other than target
56
what do dose response curves tell us?
Potency: Amount of drug required to elicit response Efficacy: Maximum effect obtainable Slope: The difference in concentration required between a minimal and maximal effect Variability: individual differences in response
57
ED50 is....
the dose at which a 50% response is achieved
58
LD50 is....
the dose at which 50% of subjects die
59
the larger the TI ....
the safer the drug
60
TI formula
TI = LD50/ED50
61
drug interactions
62
placebo effects
63
Which route of administration is characterized as "enteral"?
oral and rectal
64
Drugs administered "sublingually" (under the tongue) and drugs administered orally are absorbed mostly in the ____________ and ____________, respectively.
mouth; small intestine
65
What are the two main differences between capillaries in the periphery and capillaries in the brain?
Capillaries in the brain have tighter junctions and are surrounded by membranes of astrocyte cells
66
which is the most dangerous mode of drug administration?
IV
67
The degradation of drugs by enzymes present in the gastrointestinal tract and liver is known as:
first pass metabolism
68
most drugs are excreted via ...
the kidneys
69
The time for the plasma level of a drug to fall by 50% is called the
elimination half life
70
The "steady-state" concentration of a drug (the stable level achieved in blood with repeated, regular dosing) is
achieved when the amount of drug administered per until time equals the amount eliminated per unit time
71
The ability of liver enzymes to degrade a drug more efficiently in the continued presence of the drug is termed
Metabolic tolerance
72
"Pharmacodynamic" tolerance occurs in the _______________; "metabolic" tolerance occurs in the ____________________.
Synapse/neuron; liver
73
The study of the effects a drug has when it binds to it's target/receptor is termed
pharmacodynamics
74
A drug that is more efficacious than another drug has
a larger maximum effect
75
most side effects are...
predictable and mild
76
The observation that caffeine cannot exert as much central nervous system stimulation as amphetamine indicates that caffeine
is less efficacious than amphetamine
77
during pregnancy, intestinal motility.....
intestinal motility decreases
78
a drug that is more potent than another drug has ....
a smaller ED50
79
According to the DEA the most dangerous drugs are typically scheduled as
schedule 1
80
affinity refers to...
the strength of attraction between a molecule (ligand) and it's target (receptor)
81
A drug that blocks the effect of the naturally occurring (endogenous) compound is called:
antagonist

PSYC475 psychopharm (14 decks)

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