Kinetics And Dynamics Flashcards

(47 cards)

1
Q

Pharmacokinetics

A

The study of the basic processes that determine the duration and intensity of the drug’s affect

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2
Q

To have the desired effect, a drug must

A

Reach its target

Be of sufficient concentration

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3
Q

Active transport

A

Requires energy to move a substance from an area of low concentration to an area of high concentration

  • mitochondria produce ATP
  • ATP -> ADP for biochemical energy
  • energy facilitates movement of ions up the concentration gradient
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4
Q

Passive transport

A

Movement of a substance without the use of energy from an area of high concentration to an area of low concentration

  • diffusion
  • osmosis
  • filtration
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5
Q

Diffusion

A

Substances move until equilibrium is achieved
Passive diffusion - move from high to low concentration
Facilitated diffusion - move via carrier proteins from high concentration to low concentration

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6
Q

Osmosis

A

Movement of water from an area of low solute concentration to an area of high solute concentration (e.g., water follows salt)

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7
Q

Filtration (in osmosis)

A

Hydrostatic pressure that forces water or dissolved particles through a semipermeable membrane

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8
Q

Processes included in pharmacokinetics

A

Absorption, distribution, biotransformation (metabolism), elimination

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9
Q

Drug absorption

A

Process of movement of a drug from the site of application into the body and specific target

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10
Q

Factors effecting rate of drug absorption

A
  • drug solubility
  • drug concentration
  • drug pH (acid/base)
  • site of absorption
  • circulatory status (force and volume of blood flow)
  • bioavailability (amount of medication in systemic circulation)
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11
Q

Drug solubility

A

The tendency of a drug to dissolve
“like dissolves like” (e.g., fat soluble penetrate fat containing cells)
- human body is 60% water
- Drugs given in water solutions are dissolved more quickly that’s those in oil-based, suspensions, or solid forms
- May be beneficial to have slower/faster absorption based on desired effect

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12
Q

Drug concentration

A

Drugs given in high concentrations are more quickly absorbed that those in low concentrations
- Drugs with various routes may have various concentrations (e.g., epi)

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13
Q

Drug pH

A

Acidic versus basic (alkaline)

  • Acidic drugs absorbed more readily in acidic environments (e.g. stomach)
  • Basic drugs more rapidly absorbed in alkaline environments (e.g. kidneys)
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14
Q

Site of absorption

A

Absorption depends on whether the drugs have to pass through various membranes prior to entering general circulation

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15
Q

Blood supply to site of absorption

A

Different body tissues and organs have varied degrees of blood supply
- Pulmonary epithelium, sublingual, muscles = rapid absorption
- Fatty tissue (SC) = poor blood supply, slower
System blood flow will affect absorption (eg., hypothermia, shock, dehydration)

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16
Q

Bioavailability

A

The amount of drug that is still active after it reaches its target tissue
- Must be sufficient amount to produce desired effect

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17
Q

Distribution

A

Process whereby a drug is transported from the site of absorption to the site of action. Factors:

  • cardiovascular function
  • regional blood flow
  • drug storage reservoirs
  • physiological barriers
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18
Q

Cardiovascular function

A

When normal, drugs are distributed initially to highly perfused areas like the brain, heart, lungs, liver
- Then delivered to GI system, skin, muscles, fat

Impaired cardiovascular system:

  • slows drug distribution
  • has unpredictable drug distribution
  • decreased drug delivery with poor perfusion
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19
Q

Regional blood flow

A

Many drugs travel through the body by binding to circulating proteins (eg., hemoglobin)
- depending on ability to bind, some portion of the drug will not be free to exert its pharmacological effect
Affected by:
- cardiogenic shock
- compromised cerebral circulation, etc.

20
Q

Bound drug (distribution)

A

When the drug binds with the receptor protein or becomes stored in the body’s fatty tissues

21
Q

Unbound drug (distribution)

A

When the drug is available to target tissues

22
Q

What are the most common circulating proteins that drugs bind to?

A

Albumin, followed by hemoglobin and globulin

23
Q

Blood-brain barrier or blood-cerebrospinal barrier

A

Tightly packed cell membranes restrict damaging drugs and toxins
- Prevents most drugs from passing directly into brain

24
Q

What does the blood-brain barrier consist of?

A

-Network of capillary endothelial cells that have no pores
- Surrounded by glial connective tissue
- Impermeable to water soluble drugs
Act as an effective barrier between the CNS and PNS

25
Placental barrier
Protects from some substances passing from the mother into fetal circulation To cross, the drug must be: - lipid soluble - non-protein bound
26
Biotransformation
Metabolization of a drug into different chemicals called metabolites - makes drug into a more/less active metabolite that is water soluble for elimination
27
What is biotransformation dependent upon?
- Chemical composition - Protein binding capacity - Metabolizing system function (eg., liver)
28
What happens with decreased biotransformation
Metabolization is slowed, cumulative drug effects may occur
29
What happens with increased biotransformation
Metabolism of drugs happening quickly. Dosing rates may need to be increased to maintain concentration - Tolerance. Same reason addicts increase “dose” as body more effectively metabolizes the drug
30
Biotransformation inhibition
Drugs inhibiting the metabolism of other drugs (eg., alcohol and acetaminophen)
31
Elimination
Movement of a drug or its metabolites from: - Tissues back into circulation - Circulation to the organs of excretion Changes in normal rates of elimination may result in accumulation of drug in the body
32
Drug half-life
Time required for the total amount of a drug in the body to dismiss by half - Tells us how long a drug will stay in the body - Most drugs eliminated after 5 half-lives
33
Pharmacodynamics
What a drug will do to the body - How a drug will work is based on it reaching its target cells - Receptors on target cells is where drug enter the cells to cause a reaction Drug and receptors bind to initiate a response Receptors are “locks” and drugs are “key”
34
Predictable responses
Anticipation of a response beyond the desired effect - side effects (adverse reactions) - risk-benefit ratio
35
Factors effecting drug responses
- Age - Weight - Gender - Environment - Time of administration - Condition of the patient - Genetic factors
36
Four phases of drug action
1. Administration phase- drug enters body 2. Pharmaceutical phase- drug is broken down 3. Pharmacokinetics phase- body alters the drug 4. Pharmacodynamics phase- drug affects the body
37
Therapeutic index
The minimum drug amount necessary for an ideal or desired response in the body - excess could be toxic/fatal - dosage determined by reaching ideal effects from drug - guidelines established for minimum concentrations to reach desire effects
38
Iatrogenic responses
An adverse condition inadvertently induced in a patient by the treatment given (eg. Allergy, infection)
39
Minimum concentration
The concentration of a drug needed to become effective
40
Receptor theory (mechanism of action)
Majority of drugs act by binding to the protein molecules on the surfaces of cells - stimulate or inhibit Affected by: - Affinity - Efficacy
41
Affinity
Force of attraction between a drug and receptor | - different meds may bind to same receptor site but bonds may vary
42
Efficacy
A drug’s ability to cause the expected response Mediated by: - number of receptors - ability of the drug molecule to activate the receptor
43
Therapeutic threshold
The minimum concentration necessary for a drug to produce its desired effect. - some drugs have very narrow therapeutic indices - below therapeutic threshold = no desired response/undesired response - above therapeutic threshold = harmful/toxic effects
44
Drug storage resevoirs
Tend to delay the medications onset of action and prolongs its duration of effect - depends on if drug is bound or unbound Tissue reservoirs include fat, bone, muscle
45
Physiological barriers
A protective mechanism for drug distribution. Includes: - blood-brain barrier - placenta barrier
46
What is the blood-brain barrier ineffective against?
- oxygen - carbon dioxide - fat soluble molecules (anaesthetics, nicotine, entenox, ALCOHOL)
47
What can cross the placenta barrier?
Materials that are: - lipid soluble - non-protein bound