Lecture 1 Pharmacology Flashcards

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1
Q

4 stages of Pharmacokinetics

A
  1. Absorption
  2. Distribution
  3. Metabolism
  4. Elimination
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2
Q

Absorption

A
  • Drugs are made available to the body fluids that distribute the drugs to organ systems
  • Passive: high to low
  • Active: low to hight
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3
Q

What are the 2 key factors in absorption

A
  • route of a administration
  • dosage formulation
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4
Q

Bioavailability

A
  • Measurement of completeness of absorption
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5
Q

Enteral Administration of Absorption

A
  • Oral: first pass effect, taken by mouth, subject to liver and GI system
  • Buccal: between gum and the inner lining of the mouth cheeks
  • Sublingual: not subject to first pass by liver, taken under tongue
  • Rectal: Good blood and lymph supply, fast-acting, easy distribution
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6
Q

Parenteral Administration of Absorption

A
  • Transdermal: through skin administration, Iontophoresis and phonophoresis
  • Topical: Applied directly to skin, Steroid Cream, numbing creams
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7
Q

First pass effect

A
  • only applies to ORAL MEDS
  • Absorbed in the alimentary canal
  • Transported to the liver through the portal vein
  • Dosage must be large enough to survive first pass effect
  • Liver metabolizes drugs
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8
Q

Controlled Release Preparations

A
  • Can be Timed, extended, sustained release
  • Slow, uniform dissolution of the drug so that more drug can reach the systemic circulation

-Less doses per day, more sustained levels

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9
Q

Enteric-coated or delayed release formulations

A
  • resist stomach acid
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10
Q

Distribution

A
  • movement or transport of a drug to the site of action
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11
Q

Distribution depends on which 4 factors

A
  • Tissue Permeability
  • Blood flow
  • Binding to plasma proteins
  • Binding to subcellular components
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12
Q

Distribution: Tissue Permeability

A
  • highly lipid soluble drug can pass through easier
  • Blood-Brain Barrier: filters selectively to protect CNS (limiting the substances that enter the brain and spinal cord)
  • Morphine: across the BBB to act on CNS itself
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13
Q

Distribution: Blood Flow

A
  • Better Blood flow = Better distribution
  • Drugs circulating in the bloodstream will gain greater access to perfused tissues
  • Disease can reduce blood flow, leading to less drug being delivered to tissues
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14
Q

Distribution: Binding to plasma proteins

A
  • Drugs form reversible bonds to circulating proteins
  • only the unbound or “free” drug can reach target tissue and have effects
  • Bound drug not available for therapeutic effect
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15
Q

Distribution: Binding to subcellular components

A
  • Drugs bound to specific intracellular components can not take effects or be distributed
  • Subcellular organelles can trap the drug within the cell
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16
Q

Other factors affecting distribution

A

Competition between medications for the same receptors

17
Q

Metabolism: Biotransformation

A
  • Biotransformation: chemical changes that take place after taking a drug
  • Metabolite: altered version of the original compound, usually inactive or reduced level of activity
18
Q

What is the primary function of biotransformation

A
  • drug termination
19
Q

Primary Biotransformation location

A
  • Liver
    others include: lungs, kidneys, skin, GI epithelium
20
Q

Metabolism: Enzyme Induction

A
  • prolonged use of medication leads to reduced effects and higher tolerance, because body is adjusting to it
21
Q

Tolerance

A
  • Repeated same dose produce a lower response, so needs to increase amounts of a drug
  • often seen with Narcotic/ Analgesics
22
Q

Primary sites for drug excretion

A

Kidneys

23
Q

Gomerular filtration

A

drugs are filtered through the glomerulus and then carried through the tubule into the urine

24
Q

Polar vs. nonpolar compound

A
  • Polar: cannot be diffuse back into circulation
  • nonpolar: can be reabsorbed back into system
  • drugs that bind to plasma proteins will remain to circulation; not bound will be excreted
25
Q

The rate of drug elimination is important for?

A

Determining the amount/frequency of its dosage

26
Q

Drug administration greater than elimination

A

drug will accumulate, may reach toxic levels

27
Q

Drug administration less than elimination

A

drug may not reach therapeutic levels

28
Q

Elimination: Clearance

A

Organ or tissues’ ability to eliminate the drug

29
Q

Which two factors are involved in Clearance

A
  1. Blood Flow to the organ
  2. Fraction of the drug removed from the plasma
30
Q

Elimination Half-Life

A
  • rate of disappearance
  • the time it takes for the concentration of the drug in the plasma to fall to 1/2 of its original amount
31
Q

Biological Half-Life

A
  • Drug response
  • the time in which the duration of action falls to 1/2 of its orignical duration
32
Q

Drug responses vary according to?

A
  • Genetics
  • Disease
  • Age
  • Drug Interactions
  • Diet
  • Gender