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Pharmacology > Intro to Pharm > Flashcards

Intro to Pharm Flashcards

1
Q

Agonist

A

binds to same site as ligand and makes same signal

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2
Q

Allosteric Agonist

A

binds to diff site than ligand
no signal
greater response than agonist

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3
Q

Partial Agonist

A

binds to same site
same signal
weaker response

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4
Q

Antagonist

A

same site
no signal
weaker response- inhibits agonist

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5
Q

Competitive Antagonist

A

reversibly bind
same site
receptor can reach max effect with enough agonist concentration

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6
Q

Non-competitive Antagonist

A

irreversibly bind
diff site
receptor cannot reach max effect

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7
Q

Therapeutic Index

TI

A

TD/ED

higher numbers = safer drug

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8
Q

Potency

A

concentration to produce 50% of max effect (EC50)

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9
Q

Efficacy

A

Emax

peak of dose-response relationship

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10
Q

Pharmacologic Antagonism

A

one receptor

responds to one drug while is inhibited by another

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11
Q

Chemical Antagonism

A

no receptor

2 drugs bind to each other and antagonize each other

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12
Q

Physiologic Antagonism

A

D1 affects R1, D2 affects R2

receptors oppose each other

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13
Q

Absorption

A

movement of drug from administration site to blood

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14
Q

Distribution

A

drug mvmt through blood throughout the body

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15
Q

Biotransformation

A

metabolism

drug converted to form where it is more easily eliminated

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16
Q

Elimination

A

excretion of drug from body

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17
Q

Oral Route

A

convenient but slow

subject to first pass effect

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18
Q

First Pass Effect

A

most of drug metabolized in liver before it reaches blood stream

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19
Q

Sublingual and Buccal

A

direct absorption into bloodstream

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20
Q

Intramuscular

A

fast absorption

can be given higher dose

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21
Q

Subcutaneous

A

slower absorption

can be given higher doses

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22
Q

Intravenous

A

NO ABSORPTION

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23
Q

Inhalation

A

Fastest absorption

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24
Q

Topical

A

for local effect

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25
Transdermal
for systemic effect
26
Passive Diffusion
driven by concentration gradient- no E | no carrier- not saturable
27
Facilitated Diffusion
driven by concentration gradient- no E | carrier- saturable
28
Active Transport
against gradient- E needed | carrier- saturable
29
Charged or uncharged pass best through membranes?
uncharged
30
- pKa
acidic
31
+ pKa
basic
32
pKa
pH where 50% is ionized and 50% is nonionized
33
Lipid Soluble
nonionized
34
Water Soluble
ionized
35
Basic pH will do what to weak acids?
get rid of it
36
Basic pH will do what to weak bases?
keep it
37
Acidic pH will do what to weak bases?
get rid of it
38
Acidic pH will do what to weak acids?
keep it
39
pH of the Stomach
1
40
pH of the SI
6
41
pH of Blood
7.4
42
pH of Urine
5-8
43
pKa > pH
mainly HA and BH+
44
pKa < pH
mainly A- and B
45
pKa = pH
``` HA = A- BH+ = B ```
46
Acidic Drugs
HA
47
Basic Drugs
BH+
48
Treatment for Hepatic Encephalopathy
Lactulose | fixes hyperammonemia
49
Lactulose
``` converts ammonia (NH3) to ammonium (NH4+) turns GI basic ```
50
Weak acid overdose treated with....
bicarbonate | urine pH = 8
51
Weak base overdose treated with....
``` Ammonium chloride (NH4Cl) urine pH = 5 ```
52
Physical factors affecting absorption
blood flow to absorption site surface area contact time
53
Bioavailability
fraction of dose that reaches bloodstream | = Route/ Injected X 100
54
Factors affecting bioavailability
First pass hepatic metabolism (decreases) solubility of drug (hyrophilic decreases) chemical instability
55
Lag Time
time from administration to entrance into bloodstream | 0 in IV
56
Onset of Activity
how long it takes for the drug to start working
57
Duration of Action
How long the drug works
58
Volume of Distribution | Vd
hypothetical volume of fluid in which a drug is disseminated | = amount of drug in body/ concentration in blood
59
High Vd
high volume of distribution | does not stay in blood
60
Low Vd
Low volume of distribution | drug stays in blood
61
Increasing Vd has what affect on half life?
increases it
62
Placenta and Drug Transfer
drugs cross by simple diffusion lipid sol/ nonionized enter easily NOT a barrier to drugs
63
Drug Metabolism
converting drug to an inactive form
64
Metabolism- Prodrugs
convert drugs to an active from
65
Benzodiazepine Metabolism
administered in an active for and its metabolites are active as well
66
Phase 1 Metabolism
uses cytochrome P450 in smooth ER oxidation, reduction, hydrolysis
67
Phase 2 Metabolism
conjugation reactions in cytoplasm needs transferase enzymes young kids can't do- drug accumulates
68
Conjugation Reaction
uses a transferase enzyme to attach a molecule from the body to the drug makes the drug bigger and more likely to be eliminated (except in kids)
69
Liver
most important organ for drug metabolism
70
Cytochrome P450s that metabolize most drugs
CYP2C CYP2D CYP3A- 50% of all drugs
71
CYP Inducers
increase expression of p450s speeds up metabolic process reduce plasma lvls and effectiveness of drugs
72
Drugs that are CYP Inducers
benzopyrenes (cig smoke), chronic ethanol, carbamazepine, rifampin, phenytoin
73
CYP Inhibitors
decrease expression of P450s slows metabolic process increases plasma lvl and toxicity risk bad when mixed with drugs w/ low TI
74
Drugs that are CYP Inhibitors
cimetidine, erythromycin, grapefruit juice
75
Glucuronidation
most common Phase 2 | uses glucuronosyl transferase
76
Sulfation
Phase 2 | uses sulfotransferase
77
Acetylation
Phase 2 | uses acetyltransferase
78
Glomerular Filtration
only free, unbound drug filtered (too big) | lipid solubility and pH do not affect
79
Proximal Tubular Secretion
requires an OAT and OBT for drug secretion | undeveloped in young kids
80
Distal Tubular Reabsorption
drugs diffuse out into systemic circulation if they are uncharged pH changes will increase ionized form/ decrease reabsorption/ increase elimination
81
First Order Kinetics
constant fraction is eliminated per unit time half life constant nonsaturating kinetics
82
Zero Order Kinetics
constant amount of drug is eliminated per unit time half life not constant saturating kinetics
83
Drugs that have zero order kinetics
aspirin ethanol phenytoin
84
Half Life Formula
0.693 x Vd / CL
85
Maintenance Dose
maintain plasma concentration of long period of time | chronic
86
Loading Dose
quickly increase blood plasma concentration | acute
87
Maintenance Dose Formula
= Css x CL / F | conc at steady state x clearance / bioavailabilty
88
Loading Dose Formula
= Css x Vd / F
89
When do you give a loading dose?
when a long time period is needed to reach steady state via continuous IV
90
Steady State
maintenance dose needed to reach and stay at
91
Clinical Steady State
4-5 half lives
92
Dosage Adjustment for Renal Failure
Correct Dose = ave dose x creatinine clearance / 100 mL/min

Pharmacology (12 decks)

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