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Pharm 313 > p'kinetics and p'dynamics > Flashcards

p'kinetics and p'dynamics Flashcards

1
Q

What is pharmacokinetics?

A

study of drug movement thru the body

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2
Q

4 process of pharmacokinetics?

A
  1. absorption
  2. distribution
  3. metabolism
  4. excretion
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3
Q

3 ways for drugs to cross cell membrane? Which is most common?

A
  1. channels/pores (small)
  2. transport system (requires energy)
  3. direct penetration (move thru cell membrane itself)
    - most common
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4
Q

What makes a drug or molecule most likely to pass thru cell membrane?

A

a drug needs to LIPID SOLUBE to pass thru lipid bilayer

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5
Q

What are 2 other factors that effect a molecules ability to enter a cell? (think basic chemistry)

A
  • polarity (like dissolves like) – polar molecules cant pass tru bilayer
  • ions cannot pass thru
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6
Q

Movement of a drug from site of administration into the blood….

A

Absorption

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7
Q

What are factors that can effect absorption?

A
  • rate of dissolution (pill vs liquid)
  • increase rate of absorption: if increase surface area, blood flow, lipid solubility
  • ph partitioning (acidic accumulate on alkaline side and vice versa)
  • route of administration
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8
Q

What is the difference b/w parental and enteral administration?

A 
PARENTAL = absorbed direct into bld stream (IV,IM,SubCu,Intra-arterial)
ENTERAL= absorbed/taken in by GI tract
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9
Q

What are 2 types of coatings/formats for enteral medication?

A
  • Enteric = won’t dissolve in stomach = dissolves in intestine
  • Sustained release= released steadily thru out the day
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10
Q

Which administration is fastest and which is slowest?

A 
fast = IV (30-60 sec) 
slow= ingestion (30-90 minutes)
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11
Q

Drug movement from the blood to the interstitial space and cells…

A

Distribution

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12
Q

Factors that affect distribution

A
  • blood flow to tissues
  • ability of drug to exit the vascular system (Blood brain barrier, placenta, protein binding)
  • ability of drugs to enter cells
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13
Q

Enzymatic alteration of a drug….

A

Metabolism

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14
Q

Where does drug metabolism primarily occur?

A

LIVER

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15
Q

What is the hepatic enzyme system that changes drugs and is 12 closely related enzyme families?

A

Cytochrome P450 system

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16
Q

What changes does metabolism cause to a drug?

A
  • accelerate excretion
  • in/activation
  • toxicity
  • increase metabolism (inducers)
  • decrease metabolism (inhibitors)
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17
Q

What is the First Pass Effect?

A

=rapid hepatic inactivation of certain ORAL drugs

oral drug > GI absorption > hepatic portal vein takes to live > liver metabolizes drug >blood stream circulation

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18
Q

Where do all oral medications (except sublingual) go before systemic circulation?

A

LIVER

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19
Q

What are some results of the First pass effect?

A
  • inactivates portion fo drug
  • decrease therapeutic effect > give higher dose
  • delayed time to take effect
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20
Q

Removal of drugs from the body…

A

Excretion

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21
Q

What organ usually takes care of drug excretion? what are some other methods for excretion?

A

KIDNEY

other: bile, lungs, milk, sweat, saliva, skin, hair, tears, liver

22
Q

3 ways kidney effects excretion

A
  1. GFR (if attached to albumin = cant fit in glomerulus for filtration)
  2. Passive Tubular Reabsorption (lipid soluble drugs passively move into blood from tubule)
  3. Active Tubular Secretion (pump drugs from blood into tubular urine)
23
Q

What do we look at to see if a drug worked?

A

Plasma Drug Levels

24
Q

What is a single dose time course?

A

what happens with one dose of drug

25
Q

When are drug levels highest?

A

during absorption and distribution

26
Q

When are drug levels lowest?

A

metabolism and excretion

27
Q

What is a drug 1/2 life?

A

time it takes for amount of drug in body to decrease by 50%

28
Q

Why do I care about Drug 1/2 life (3 reasons)

A
  1. duration of action after single dose
  2. time required to reach steady state
  3. dosing frequency
29
Q

How many half lives does it take to reach plateau?

A

4 (as long as dosage remains constant)

30
Q

What is a loading dose?

A

increase initial dose of drug to achieve plateau more quickly

31
Q

How many half lives does it take for most of drug to be eliminated from body?

A

4

32
Q

What is the difference between Peak and Trough?

A

PEAK= greatest concentration of drug in BLOOD
-30 min AFTER infusion

TROUGH= greatest concentration of drug in TISSUE
-30 min PRIOR to next infusion

33
Q

What is pharmacodynamics?

A

study of DRUGS effect on BODY

-aka what drugs due to the body and how they do it

34
Q

3 Dose response relationships?

A
  1. increase dose > response progressively increase
  2. EFFICACY
  3. POTENCY
35
Q

What is the difference between Efficacy and Potency?

A

EFFICACY= largest effect a drug can produce (limits of tylenol to treat pain)

POTENCY= dosage needed to produce effect (#of MG)

36
Q

Morphine (2 mg) vs Dilaudid (.3MG) have same EFFICACY but

A

Dilaudid is more potent because it needs less mg to produce same effect

37
Q

What makes the specificity of a drug possible?

A

Receptors

38
Q

What happens in you increase a drugs selectivity?

A

decrease side effects

** selectivity does NOT equal safety

39
Q

What do drugs that bind to receptors do?

A

Mimic or block body’s natural function

40
Q

Receptors work as a ___ and ____ mechanism

A

lock and key

41
Q

A drugs strength of attraction to a receptor is …..

A

affinity

42
Q

A drugs ability to activate a receptor upon binding is….

A

intrinsic activity

43
Q

This kind of drug activates receptors and MIMICS the body’s response

A

Agonist

44
Q

This kind of drug blocks action by binding to receptors

A

Antagonist

45
Q

Do Agonists have affinity or intrinsic activity?

A

BOTH

46
Q

Do Antagonists have affinity or intrinsic activity?

A

Affinity but no intrinsic activity

47
Q

How do agonist and antagonists effect processes?

A 
Agonist = slower or faster process
Antagonist = no observable effect unless agonist present
48
Q

What is a partial agonist?

A
  • acts like agonist and antagonist

- cannot produce full effect of agonist (detox drug for heroin makes feel sick but also help with detox)

49
Q

What is the difference between competitive and noncompetitive antagonists?

A

Competitive = binds REVERSIBLY (surmountable)
Non competitive = binds IRREVERSIBLY (insurmountable)
-reduces # of binding spots for agonist

50
Q

What is Average Effective Dose?

A

ED50

-dose required to produce a therapeutic effect in 50% of ppl

51
Q

What is a Lethal Dose?

A

LD50

-dose that is lethal to 50% of animals treated

52
Q

What is the relationship between therapeutic index, and drug safety as it pertains to lethal dose?

A

^ therapeutic index = ^ safety of drug

—> more space b/w safe and lethal dose

Pharm 313 (26 decks)

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