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Pharmacology > Basic Pharmacology Principles > Flashcards

Basic Pharmacology Principles Flashcards

1
Q

Pharmacology

A

Study of drugs

How new drugs are developed

  • Phase I, II and III; clinical trials
  • Post-marketing surveillance
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2
Q

Drug-Dose Relationship

A

Dose-response curve; depicts the relationship between drug dose and magnitude of effect

Doses below the curve do not produce a pharmacological response.

Doses above the curve do not produce much additional pharmacological response
-May have unwanted effects-> toxicity

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3
Q

Types of Drug Reponses

A

Quantal
-May or may not occur

Graded
-Biological effects can be measured continually up to the maximum responding capacity

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4
Q

Drug Selectivity

A

Ratio of the dose producing undesired effects to the dose producing the desired effects
Minimum effective concentration (MEC); level below which therapeutic effects will not occur
Minimum toxic concentration (MTC): level above which toxic effects begin
Therapeutic index or range: MTC to MEC

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5
Q

Drug Response in the Real World

A

Placebo effect

Dose-effect relationship in real world

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6
Q

Brand vs. Generic Drugs

A

Both brand and generic drugs contain same active ingredient
Differences in inactive ingredients
U.S. Food and Drug Administration (FDA) Orange book rates generic substitutions for brand-name products

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7
Q

Receptors

A 
Ion channel receptors
Receptors coupled to G Proteins
Transmembrane receptors
Intracellular receptors regulating gene expression
Enzymes
Drug action of receptors
Disease states and receptors
Non-receptor mechanisms
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8
Q

Drug-Receptor Interactions

A

Most drugs work by binding to receptors
Receptors are located on the cell surface
The drug molecule must “fit” into the receptor

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9
Q

Drug-Receptor Binding

A

Drug-receptor binding is reversible
Drug-receptor binding is selective
Drug-receptor biinding is graded
-The more reception filled, the greater the pharmacological response
Drugs that bind to receptors may be agonists, partial agonists, or antagonists

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10
Q

Pharmacokinetics

A

Absorption
Distribution
Metabolism
Excretion

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11
Q

Absorbtion

A 
Parental administration
Oral administration
Site of administration
Bioavailibility
Peak blood levels
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12
Q

Distribution

A

Definition: movement of absorbed drug in bodily fluids throughout body to target tissues
Distribution requires adequate blood supply
-Drug distribution to areas of high blood flow first
-Areas of low blood flow next
Properties that affect distribution
-Water or lipid solubility
-Size of molecule
-Acid vs basic environment
-Henderson-Hasselbalch relationship (pH of solution)
-Protein binding
-Transporters
-Volume of distribution

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13
Q

Protein Binding

A

Drugs exist in bound and unbound states
-Travel when bound; cross membranes when unbound
“Highly” protein bound
Ratio of bound drug usually remains stable
Low plasma proteins (low albumen) will result in more free drug circulation

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14
Q

Competition for Protein-Binding Sites

A

Finite number of plasma proteins
Compete and displace each other-> more free drug
Higher risk for toxicity
More drug may be eliminated

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15
Q

Tissue Distribution

A 
Fat
-Lipid-soluble fats have a high affinity for adipose tissue
-Adipose tissue has low blood flow 
Bone
-Some drugs have affinity for bone
Blood brain barrier
-Relatively impenetrable
-Usually protective
-Only lipid-soluble drugs cross barrier
Placental barrier
-Many drugs pass barrier
-Low-molecular-weight drugs pass easier
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16
Q

Metabolism

A 
Phase I and Phase II metaboism
-Phase I: nonsynthetic reactions
-Phase II: synthetic or conjugation reactions
Cytochrome P450 (CYP450)
-Organized into numbered families
-CYP1, CYP2, CYP3
Metabolism and half-life
17
Q

Factors that Influence Metabolism

A 
Age
Genetically determined differences
Pregnancy
Liver disease
Time of day
Enviornment
Diet
Alcohol
Drug interactions 
Drugs undergo one of both of two types of chemical reactions in the liver
-Phase I: oxidation, hydrolysis, or reducation to increase water solubility of drug molecules
-Phase II: conjugation or union of drug molecule with water-soluble substance
18
Q

Phase I Enzyme: CYP450 Isoenzymes

A

The majority of drugs are metabolized in the liver by the hepatic isoenzymes
CYP450 isoenzymes
Most common: 1A2, 2C9, 2C19, 2D6, 3A4, (3A3/4)

19
Q

Prodrug Metabolism

A

A prodrug is a drug that is administered in an inactive (or significantly less active) form
Once administered the prodrug is metabolized in the body into the active compound

ASA

20
Q

CYP450 and Drug Interactions

A

The enzymes may be slowed (inhibited) or increased (induced)

Concurrent therapy with ace inhibitor or inducer may alter the metabolism of medication

21
Q

Excretion

A 
Definition: removal of the drug from the body by the organs of elimination
Most drugs are eliminated by the kidneys
Drugs are also eliminated by:
-Lungs
-GI tract
-Sweat and saliva
Mammary glands (via breast milk)
22
Q

Renal Elimination

A

Passive glomerular filtration
Active tubular secretion
Tubular reabsorption

23
Q

Glomerular Filtration

A

The availability of the drug for glomerular filtration
Drug must be unbound from protein
Free, unbound and water-soluble metabolites are filtered by the glomeruli

24
Q

Factors that Affect Renal Excretion

A

Kidney Function
Age
Hydration
Cardiac Output

25
Q

GI Tract Excretion

A

Biliaryn excretion
-After being metabolized in the liver, the metabolite is excreted into the bile
-Some drugs may then be reabsorbed in the intestine
-Enterohepatic cycle
Fecal excretion

26
Q

Lung Excretion

A

Gases
General anesthestics and volatile liquids
Rate of excretion based on respiratory rate and pulmonary blood flow

27
Q

Sweat/Salivary Excretion

A

Not very many drugs
Excretion in sweat may be a cause of advnerse effects, such as a rash or dermatitis
Salivary excretion
May be the reason patients complain of “taste” in their mouth with certain drugs

28
Q

Mammary Excretion

A

Many drugs are excreted in breast milk

Breast milk is acidic

Pharmacology (14 decks)

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