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PHARMACOLOGY > CHAPTER 1- INTRO TO DRUGS > Flashcards

CHAPTER 1- INTRO TO DRUGS Flashcards

1
Q

pharmacology is…

A

the study of biological effects of chemicals.

drugs are therapeutic/helpful/or potentially dangerous

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2
Q

pharmacokinetics

A

what the body does to the drug (absorption, etc…)

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3
Q

pharmacodynamics

A

what the drug does to the body

think Dynamics-Drugs (D-D)

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4
Q

what is a drug? how long to discover?

A

any substance that is used/intended to modify physiological systems or pathological states for the benefit of the recipient

15 to 20 yrs to develop

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5
Q

Drug evaluation: How many phases

A

preclinical trials, phase I studies, phase II, phase III, phase IV

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6
Q

Preclinical trials

A

chemicals are tested on lab animals

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7
Q

Phase I studies

A

chemicals tested on human volunteers, NOT those with the disease
testing safety of chemicals

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8
Q

Phase II studies

A

drug tried on informed patients WITH the disease

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9
Q

Phase III studies

A

drug used in vast clinical market

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10
Q

Phase IV studies

A

continual evaluation of the drug

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11
Q

generic drugs

A

-chemicals produced by companies involved only in manufacturing of drugs
-patent made on original drug eventually expires and leads to…

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12
Q

brand name drugs

A

other companies can make a bioequivalent drug that usually costs more
ex) acetaminophen v. tylenol

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13
Q

over the counter drugs (OTC)

A

available without prescription for self treatment
- many of these were “grandfathered”

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14
Q

drug names (4)

A

chemical, generic, official, brand

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15
Q

pharmacokinetics: ADME what is it?

A

ADME determines the onset, intensity, and duration of drug action

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16
Q

what does ADME stand for?

A

Absorption
Distribution
Metabolism
Excretion

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17
Q

ADME- Absorption

A

The movement of drug from the site of administration into the systemic circulation

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18
Q

ADME- Distribution

A

movement of the drug from the bloodstream into various body tissues/organs.
this depends on blood flow through the tissue
- can trap in tissue or be moving in and out

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19
Q

ADME- Metabolism

A

biotransformation of a drug into more polar substances

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20
Q

ADME- Excretion

A

removal of a drug from the body (urine, bile, tears, breast milk, saliva, sweat, or feces)

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21
Q

Chemical Instability

A

some drugs cannot be taken by a certain route/moa (method of administration), therefore it is considered chem instability
- ex) insulin is destroyed by the stomach if taken orally

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22
Q

Excipients

A

ingredients/substances other than the active drug used in the drug product for binding/long term stabilization

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23
Q

Binders

A

used to hold together products in a drug (ex. in Tylenol tablets)

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24
Q

Pharmacokinetic curve:
MEC- minimum effective concentration

A

the amount of a drug needed to cause a therapeutic EFFECT

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25
Q

Cmax

A

MAX amount of drug that reaches the plasma after dose is given (concentration)

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26
Q

what is duration of drug action?

A

how long the patient will experience the drug’s effects

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27
Q

onset

A

how long it takes to see the beginning of therapeutic effect

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28
Q

bioavailability

A

fraction of administered dose of drug that reaches the systemic circulation
- think about how it changes between different routes (orally v. IV)

29
Q

Factors that influence bioavailability

A

-route of administration
-first pass hepatic metabolism
-solubility of the drug
-chemical instability
-nature of the drug formulation

30
Q

First-pass hepatic metabolism

A

the drug gets metabolized at a specific location, the liver, resulting in decrease concentration of the ACTIVE drug at the site of action.
- drug becomes less active as it passes through the liver

31
Q

routes of drug administration: 3 main

A

enteral (mouth), parenteral (injection), and other

32
Q

Enteral administration

A

by mouth
- oral, sublingual, buccal (lozenge)

33
Q

Parenteral administration

A

Intravenous (IV), Intramuscular (IM), Subcutaneous (SC), Intradermal (ID)

34
Q

OTHER administration

A

oral inhalation (inhaler), nasal (decongestants), topical, transdermal (patches), rectal (suppositories)

35
Q

which route provides the highest plasma concentration and shortest onset?

A

IV. takes least time to reach concentration of the drug in the blood

36
Q

IV- Intravenous
- absorption?
- onset?

A
  • rapid absorption
  • 100% bioavailability
  • rapid onset (time till seeing effect)
  • IRREVERSIBLE, causing tissue damage, fear, pain
  • IV curve

PROS
- useful when unconscious, intubated, or need rapid onset
CONS
- poor compliance of patient

37
Q

SC- Subcutaneous

A
  • constant/slow absorption
  • sustained effect
  • not useful for skin/tissue irritating drugs
    may cause pain/necrosis
  • short needle under the skin, pouch may form at site of injx.
38
Q

IM- Intramuscular

A
  • rapid absorption with AQ drug solution
  • slow/sustained absorption with NON AQ drug solution
  • dependent on BLOOD FLOW and the water solubility of the drug
39
Q

intramuscular absorption depends on…

A

BLOOD FLOW!
INC flow rate = INC absorption

40
Q

PO- Oral
absorption

A
  • absorption is VARIABLE
    -convenient, economical, safe
    CON: reduced conc. of drug in systemic circ (bloodstream)
41
Q

OTHER routes: Rectal

A
  • irregular and incomplete absorption
  • 50% of drug absorbed bypasses liver
    can cause irritation to mucous membranes
42
Q

OTHER routes: oral inhalation

A
  • rapid circulation in lungs bc of SURFACE AREA
  • avoid of first pass loss
  • local application= drug at desired site of action
43
Q

OTHER routes: nasal inhalation

A

decongestants and corticosteroids

44
Q

OTHER routes: topical
- 2 effects

A
  • applied to skin of mucous membranes
  • can have local OR systemic effect
    (ex skin mycosis vs. nicotine patch)
45
Q

OTHER routes: transdermal

A

type of topical
- sustained delivery of drugs
- absorption depends on nature of skin/ lipophilicity of drug into our membranes

46
Q

ABSORPTION: how is it affected?

A

by route of administrtion, environment of where drug is absorbed, chemical characteristics of drug

47
Q

GI tract absorption: 4 types

A

passive diffusion: move with the conc gradient, NO ATP

facilitated diffusion: transmembrane carrier proteins pass large molecules, NO ATP

active transport: carrier proteins, against conc gradient, YES ATP

endo/exocytosis: engulfing drug and transporting with vesicle (drugs with high MW), YES ATP

48
Q

pH effect on drug absorption

A

drug passes through membrane easily if its UNCHARGED/NEUTRAL

Acids: weak acids in neutral form A- pass easily in ACIDIC enviro

Bases: weak bases in neutral form B pass easily in BASIC enviro

49
Q

why is pH important when determining whether to use an ACIDIC or BASIC drug?

A

You want the drug to be in its neutral form, dissociated. If the drug is placed in its opposite environment, an acid-base reaction will occur resulting in protonated molecules and difficulties passing through membranes.
- weak acid thrives in stomach which has acidic pH
- weak base would not thrive in this enviro

50
Q

acidic drugs stay neutral when the pH is..

A

less than the pKa (more acidic)

51
Q

basic drugs stay neutral when the pH is…

A

larger than the pKa (more basic)

52
Q

How does blood flow influence absorption?

A

inc blood flow, inc absorp
- ex) intestines receive from blood flow than the stomach

53
Q

How does surface area influence absorption?

A

inc SA, inc absorp
- intestinal wall have microvilli

54
Q

How does contact time influence absorption?

A

inc contact time, inc absorp
if drug passes too fast through the GI, it will NOT absorb well

ex of decreased contact time: vomiting, diarrhea

55
Q

How does P-GP expression influence absorption?

A

P-GP is a transporter that pumps drugs out of the cell (efflux)
- if the drug is a substrate of P-GP, conc of drug that reaches blood DECREASES
- drug will be pumped OUT instead of going INTO bloodstream

56
Q

DISTRIBUTION: depends on?

A

_the drug reversibly leaves the blood stream and enters the ECF and tissues (performs its effect)

  • Cardiac output and local blood flow
  • capillary permeability
  • tissue volume (ICF)
  • degree of binding the drug to plasma and tissue proteins
  • relative lipophilicity of the drug
57
Q

Distribution: capillary permeability

A

depends on capillary structure and chemical nature of the drug

58
Q

Distribution: degree of binding of the drug depends on which protein?

A

albumin is major drug binding protein
- tissue reservoirs prolong drug actions

59
Q

Volume of Distribution (Vd)

A

fluid volume required to contain the entire drug in the body at the same conc measured in plasma
- highly distributed in adipose=large Vd
- primarily retained in vascular compartment=low Vd

60
Q

Drug Clearance (CL)
-Unit of volume

A

estimates volume of blood from which the drug is cleared per unit of time
- clearance through hepatic metabolism and kidney

61
Q

Half life

A

time is takes to reduce the plasma drug conc by HALF
- tells us how long it takes for drug to be eliminated

62
Q

Drug Metabolism occurs where

A

the liver.
- transformed into polar molecules to be easily eliminated by kidney

63
Q

drug metabolism phase I and II

A

Phase I: P450 CYP enzyme, biotransformation and chemically changing structure
Phase II: conjugated drug with molecules (polar compounds) in our body for excretion

64
Q

Drug metabolism: ISOFORMS

A

CYP Isoforms: drug can be specifically metabolism by one or more CYP enzymes

65
Q

CYP inducer and inhibitor

A

inducer: induce CYP activity
inhibitor: inhibit CYP activity and slow down metabolism/production of metabolites

66
Q

DRUG-DRUG Interaction

A

2 drugs, 1 is an inhibitor, resulting in slower metabolism

67
Q

DRUG METABOLISM QUESTION:
Drug A is a CYP3A4 inducer while Drug B relies on CYP for its metabolism. If A and B are coadministered, what happens to the half-life of drug B?

A

The half-life of drug B is SHORTER
, the time to metabolize is REDUCED/faster metabolism bc of the inducer

68
Q

Urinary Excretion

A

removal of drugs from the body through the kidneys

69
Q

path of Urinary excretion

A

A) glomerular filtration (free drug through capillary slits)
B) active secretion through transporters (anions and cations/ acids and bases have their own system)
C) passive reabsorption: keeps drug in urine
- drug conc inc, uncharged drug diffuses out
- urine pH can alter excretion

PHARMACOLOGY (29 decks)

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