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Pharm 1 > 02. Introduction to Pharmacokinetics > Flashcards

02. Introduction to Pharmacokinetics Flashcards

1
Q

Define Pharmacodynamics

A

The effects of drugs and their mechanisms of action. “The effect of the drug on the body.”

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2
Q

Define Pharmacokinetics

A

The movement of the drugs through the body. “The effect of the body on the drug.”

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3
Q

Define Pharmacotherapeutics

A

The clinical (therapeutic) use of drugs. “Using drugs to treat disease.

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4
Q

Define Therapeutic index

A

Ratio: “Effective dose vs. harmful dose.”

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5
Q

How do drugs cross membranes? (3)

A
  • Via channels and pores
  • Via transport systems
  • Via direct penetration of the membrane (lipid soluble drugs do this)
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6
Q

ADME

  • Acronym to communicate the basic tenets of _______________.
  • What does it stand for?
A

Acronym to communicate the basic tenets of pharmacokinetics.

  • Drug ABSORPTION
  • Drug DISTRIBUTION
  • Drug METABOLISM
  • Drug EXCRETION
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7
Q

Define drug absorption.

A

The movement of a drug from the site of administration into the blood.

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8
Q

Define drug distribution.

A

Once in the blood, the movement of drugs throughout the body.

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9
Q

DRUG METABOLISM

  • also known as…
  • define, give primary organ
A
  • AKA Biotransformation.
  • The enzymatic alteration of drug structure. Done by and large by the liver. For most drugs this is the first step in their excretion.
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10
Q

3 routes of drug administration

A

1) Enteral (orally or g-tube)
2) Parenteral (skin, inhaler, etc)
3) IV (absorption process is skipped with this one– straight to the blood.)

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11
Q

Liver excretes to _______

Kidney excretes to _______

A

Bile, urine.

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12
Q

3 drug characteristics that affect pharmacokinetic movement

A
  • Lipid solubility
  • Ionization
  • Protein binding
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13
Q

LIPID SOLUBILITY

  • Define
  • Pharmacokinetic parameters affected (2)
A
  • A measure of the ability of a drug to dissolve in water verses lipid.
  • Effects…
    1) Membrane diffusion
    2) ADME (Absorption, distribution, metabolism, excretion)
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14
Q

IONIZATION (Pka)

  • Define
  • Pharmacokinetic parameter affected
A
  • When drugs are charged. Acidic drugs are ionized in basic solutions and basic drugs are ionized in acidic solutions.
  • Effects RATE and LOCATION of drug absorption.
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15
Q

PROTEIN BINDING

  • Define
  • Pharmacokinetic parameter affected (3)
A
  • The extent to which a drug binds to plasma proteins

- Effects distribution, metabolism and excretion.

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16
Q

Define Bioavailability

A

The fractional extent to which a dose of drug reaches the blood stream and its site of action. (Eg if you take 100mg of teh drug and it has a bioavailability of 50%, that means that only 50 mg is going to hit the bloodstream.)

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17
Q

Bioavailability is usually talking about what route of administration?

A

Oral

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18
Q

Bioavailability depends on (3) factors

A

1) Physiochemical properties of the drug
2) Route of administration
3) Metabolic or excretory capacity by the liver or intestines for the drug.

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19
Q

What are 3 types of patients whose bioavailability you really want to pay attention to?

A
  • Infants
  • Elderly
  • Liver compromised
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20
Q

Characteristics of ORAL administration

  • Drug absorption
  • Advantages
  • Disadvantages
A
  • Absorption is variable and can depend on many factors
  • Pro: Most convenient and economical, often also the most safe.
  • Con: Requires patient compliance. Bioavailability can be erratic and incomplete.
21
Q

Characteristics of INTRAVENOUS administration

  • Drug absorption
  • Advantages
  • Disadvantages
A
  • Bypasses absorption. Potential immediate effects – suitable for large volumes and irritating substances.
  • Valuable for emergency use, permits titration.
  • Increased risk of adverse side effects.
22
Q

Titration

A

Method of drug administration where you are giving someone an individual dose based on the particular therapeutic target you want. You can really only do this with an IV drug.

23
Q

Characteristics of SUBCUTANEOUS administration

  • Drug absorption
  • Advantages
  • Disadvantages
A
  • Absorption can be prompt or slow depending on drug preparation, can be affected by changes in blood flow to tissue.
  • Suitable for self-administration
  • Not suitable for large volumes, possible pain or necrosis as site.
24
Q

Characteristics of INTRAMUSCULAR administration

  • Drug absorption
  • Advantages
  • Disadvantages
A
  • Absorption can be prompt or slow depending on drug preparation, can be affected by changes in blood flow to tissue.
  • Suitable for self-administration
  • Contraindicated with anticoagulants (because there is a potential for more bleeding)
25
Q

2 characteristics of SUBLINGUAL administration

A
  • Absorbed via oral mucosa

- Bypasses the liver

26
Q

3 characteristics of TRANSDERMAL administration

A
  • Absorbed through intact skin
  • Drugs are usually highly lipid soluble
  • Compromised skin integrity can greatly affect absorption
27
Q

3 characteristics of RECTAL administration

A
  • 50% of drugs absorbed via the rectum will bypass the liver
  • Absorption can be irregular and incomplete.
  • Some drugs may irritate the rectal mucosa
28
Q

3 characteristics of INTRA-ARTERIAL administration

A
  • Administration requires great care
  • Can help localize drug effects (very dilute by the time drug passes to the rest of the body)
  • Bypasses liver
29
Q

2 characteristics of INTRATHECAL administration

A
  • Drugs administered into CSF (in spinal subarachnoid space or brain intravenous space)
  • Bypasses BBB
30
Q

5 characteristics of INHALED (pulmonary absorption) administration:

  • Absorbed through what?
  • Used mostly for ______ and _________
  • Speed of absorption
  • Bypasses _______
  • Provides local application for what organ?
A
  • Absorbed through pulmonary epithelium and mucous membranes of the respiratory tract
  • Used mostly for gases and aerosolized droplets
  • Almost instantaneous absorption
  • Bypasses liver
  • Provides local application when lungs = target
31
Q

3 characteristics of TOPICAL application

A
  • To mucous membranes
  • Usually for local effects
  • Only occasionally systemically absorbed
32
Q

Drug distribution is dependent on 4 physiological factors:

A
  • Cardiac output
  • Regional blood flow
  • Capillary permeability
  • Tissue volume
33
Q

Drug distribution is dependent on 3 physiochemical properties:

A
  • Lipid solubility
  • pH partitioning
  • Drug binding to plasma proteins and / or tissue macromolecules
34
Q

What is pH partitioning?

A

Sometimes a drug will cross the membrane in an un-iodized form, then becomes iodized in that place and cannot leave that space.

35
Q

What is sequestration, in talking about drug distribution? +example

A

When a drug enters into a certain tissue type and sort of lingers. That tissue becomes a reservoir for that drug, thus changing the distribution aspects.

Example: PROSAC is relatively fat-soluble, so it has a high level of sequestration, meaning that it takes a few weeks for a patient’s blood levels to climb to therapeutic levels.

36
Q

Usually, the metabolism of drugs causes inactivation. If the metabolism of a drug causes ACTIVATION, the drug is called a ______.

A

Prodrug

37
Q

For most drugs, metabolism involves ___________ reactions that generate more polar inactive metabolites that are more readily excreted from the body.

A

Biotransformation

38
Q

Enzyme systems for drug metabolism are found primarily in the (1). Other sites of metabolism include (2), (3), (4)

A

1) Liver
2) GI Tract
3) Kidneys
4) Lungs

39
Q

Superfamily of liver enzymes responsible for biotransformation of the vast majority of drugs.

A

The Cytochrome P-450 Superfamily

40
Q

Drug tolerance happens at one of two places.

A

1) The site of action

2) The site of metabolism (ie the liver ups its game)

41
Q

Basis for drug-drug interactions (5):

A
  • Drug inducers vs. drug inhibitors
  • Common inducers and inhibitors
  • Drug tolerance and cross-tolerance
  • Inter-individual variation in metabolic capacity for certain drugs
  • Metabolic activation of chemicals to toxic and carcinogenic derivatives
42
Q

What is cross-tolerance?

A

Pt builds tolerance for one drug and subsequently has tolerance for similar drugs

43
Q

Usually, _________ are eliminated in their unchanged form, and ________ are eliminated in an inactive form (after biotransformation

A

Water soluble drugs

Lipid soluble drugs

44
Q
  • 3 most common drug excretion routes

- 5 other drug excretion routes

A
  • Renal, biliary, fecal

- Seat, saliva, tears, breastmilk, lungs

45
Q

Considerations of the renal excretions of drugs (4):

A
  • Lipid solubility
  • Organic anions and cations
  • Renal blood flow
  • GFR (Glomular Filtration Rate) and urinary output
46
Q

What is the fundamental tenet of clinical pharmacokinetics?

A

A relationship exists between the pharmacological effect of a drug and the accessible blood or plasma concentration of that drug.

47
Q

Four important parameters of pharmacokinetics:

A
  • Bioavailability
  • Volume of distribution
  • Clearance
  • Elimination half-life
48
Q

With a long half life, it takes a ______ time to get a steady dose.

A

LONGER

49
Q

What is a loading dose?

A

You jack up the dose to get effects sooner, then lower it to a maintenance dose.

Pharm 1 (6 decks)

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