Pharmacodynamics Flashcards

(71 cards)

1
Q

any chemical substance that
affects living processes

A

Drug

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2
Q

normal component of cell or
tissue where drug can bind

A

Receptor

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3
Q

establish and maintain for a certain time, an effective concentration of the drug in the immediate vicinity of its site of action

A

Biophase

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4
Q

Factors responsible for maintaining biophase (6)

A

Drug Dose/ Amount of Drug
Route of Administration
Degree of Ionization
Lipid Solubility
Plasma Protein binding
Rate Biotransformation and Excretion

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5
Q

Type of Dose-Response Relationship where if the dose drug is increased, the magnitude or intensity of response also increases

A

Graded Dose-response Relationship

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6
Q

Type of Dose-Relationship where if the dose of the drug increases, the number of proportion of animals exhibiting a response also increases

A

Quantal Dose-Response Relationship

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7
Q

Dose-reponse relationship with a all-or-nothing response

A

Quantal Dose-response Relationship- either the dose produces a response at a certain amount or it doesnt elicit any response

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8
Q

dose that will produce a response in 50% of the animal population

A

median effective dose or ED50

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9
Q

dose that will produce death in 50% of the animal population

A

median lethal dose or LD50

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10
Q

a drug that possesses affinity for a particular kind of receptor, and the ability to cause a change in this receptor that give rise to an observable effect

A

Agonist

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11
Q

type of agonist wherein the drug binds to the same site as an endogenouse ligand

A

Primary agonist

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12
Q

type of agonist that produces maximal effect under given set of conditions

A

Full agonist

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13
Q

type of agonist that produces only a submaximal effect regardless of the amount of the drug applied

A

Partial agonist

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14
Q

any drug that counteracts the effect of an agonist

A

Antagonist

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15
Q

Type of antagonism were it interacts with the receptor or any component of the receptor or any component of the effector

A

Pharmacologic Antagonism

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16
Q

antagonists that compete for the same receptor with the agonist, which both have affinity

A

Competitive antagonists

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17
Q

Prevents the agonist from producing its effect at a given receptor site, also inhibits any component of stimulus

A

Non-competitive antagonist

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18
Q

type of antagonist where the it does not cause its effect by interaction with tissue receptor sites by interact with the agonist itself

A

chemical antagonist

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19
Q

a type of antagonism where a drug counters the effect of another by simple chemical reaction/neutralization

A

chemical antagonism

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20
Q

the ability of the drug to bind or combine with receptor, thereby initiating an action

A

Affinity

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21
Q

characterized by the maximal effect the drug can produce

A

efficacy (intrinsic activity)

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22
Q

capacity to preferentially produce a particular effect

A

selectivity

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23
Q

characteristic effect of a drug that is produced at a lower dose than those required to elicit other response

A

Selectivity
Example: Xylazine
= sedative (efficacy) in right amount
= emetic (selectivity) less dose”

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24
Q

when all the effects produced by a drug are due to a single mechanism of action

A

SPECIFICITY
Example: AtSO4 (Atropine sulfate)
- Mydriasis (pupil) = anti-muscarinic
- Antiperistalsis (G.I Tract) = anti-muscarinic
- Decrease salivation = anti-muscarinic”

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25
refers to the dose that must be administered to produce a particular effect of given intensity
POTENCY
26
margin of safety wherein it is obtained from the ratio of the mediam lethal dose to the median effective dose LD50/ED50
Therapeutic Index
27
Margin of safety wherein it is derived from the ratio of the extremes LD1/ED99
Certain Safety factor
28
Drugs that do not directly need a receptor (7)
1. Inhalant Anesthetics 2. Osmotic Diuretics 3. Saline Cathartics (feces will become watery) 4. Antacids 5. Urinary Acidifiers 6. Urinary Alkalinizers 7. Antiseptics (e.g. Iodine)"
29
the rate-limiting step that determines release of drug from the dosage form
Dissolution
30
technique used when dissolution is enhanced by decreasing the particle size of the drug
micronization
31
Dissolution is enhanced by administering the drug in the what form?
salt form
32
what state should the drug be following dissolution?
1. must be stable2. must be sufficiently lipid-soluble to diffuse into the cell membrane, penetrate barrier and enter blood circulation
33
principle site of drug absorption in the GIT
small intestine - because of the extensive area that has rich blood supply
34
Intact skin allows passage of _______, but retards _________.
small lipophilic substances; diffusion of water soluble molecule
35
Absorption from topical site is enhanced from a/an ________ solution.
oil-in-water base
36
T/F: Drugs in oily vehicle or suspensions should not be given I.V
T - This is because the suspended drug particles physically block blood capillaries and the oil phase of a water-in-oil injection could cause a fat metabolism, again blocking blood vessels.
37
Absorption of drug from I.M or S.C is rapid, if it is given in ______ solution.
aqueous
38
In I.M. or S.C., rate of absorption is determined by _______.
vascularity of the area
39
extent to which a drug administered as a particular dosage form reach/enters the systemic circulation intact"
Bioavailability
40
rated by the time at which it reached the peak plasma concentrated.
Rate of absorption
41
organ for biotransformation
liver
42
no. 1 enzyme for the drug to undergo oxidation which will result to metabolites which has polar characteristics"
cytochromes
43
Smooth-surfaces Endoplasmic Reticlum (SER) is broken down into small vesicle known as ______
microsome
44
Microsomal enzyme + oxygen ; have been classified as ______
Mixed-function oxidases (MFO)
45
_______ will combine with oxygen that will result to mixed function oxidases for oxidation and hydrolysis. (PHASE I)
NADPH (Nicotinamide Adenine Phosphate)
46
Outer layer of mitochondria has ______ enzyme with can cause ___,____, or ____ of biogenic amine.
monoamine oxidase (MAO); oxidation,reduction or deamination
47
______is important metabolic pathway for ester-linkage and amide-bond
Hydrolysis
48
Non-polar metabolites will bind/conjugate that is why the reaction is called _________"
Conjugation Reaction
49
______ is the most important metabolic pathway for endogenous compound"
Glucuronide
50
Cats lack what enzyme for synthetic reaction
Glucoronyl transferase
51
dogs lack what enzyme for synthetic reactions
arylamine acetylerase
52
pigs lack what enzyme for synthetic reaction
phenol sulfurase
53
Metabolite of Pentobarbital (anesthetic)
Active-Inactive = Pentobarbital alcohol
54
Metabolite of Phenobarbital
Active-Inactive = p-hyrdoxyphenobarbital
55
Metabolite of Phenytoin
Active-Inactive = p-hydroxyphenyl derivative
56
Metabolite of Amphetamine
Active-Inactive = phenylacetone
57
Metabolite of Phenothiazine
Active-Inactive = phenothiazine sulfoxide
58
Metabolite of Procaine
Active-Inactive = (PABA) para-aminobenzoic acid
59
Metabolite of Phenylbutazone
Active-Active = Oxyphenbritazone
60
Metabolite of Aspirin
Active-active = salicylic acid
61
Metabolite of pro-panol
Active-active = 4-hydroxypropranolol
62
Metabolite of Diazepam
Active-active = N-desmethyldiazepam
63
Metabolite of Primadone
Active-active = Phenobarbital
64
Metabolite of spironolactone
Active-active = Canrenone
65
Metabolite of Prontozil
Inactive-active = sulfanilamide
66
has a wide variety of oxidative reactions, the most prominent is for metabolism of lipid-soluble and steroid drugs.
Microsomal enzymes
67
Metabolite of Hetacillin
Inactive-active = Ampicillin
68
Metabolite of Parathion
Inactive-active = paraoxon
69
Routes of Drug Excretion (4)
RenalBilliary ExcretionPulmonary Excretion Less Important - Milk, saliva, sweat, eggs
70
defined as time required for the body to eliminate one-half of remaining drug
Half-life
71
Volume of plasma cleared of the drug by various elimination processes per unit of time.
Body clearance