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BMR 605 > TEST 1 General Principles of Pharmacology 1 & 2 > Flashcards

TEST 1 General Principles of Pharmacology 1 & 2 Flashcards

1
Q

What are the 3 physiochemical properties?

A
  • Molecular Size
  • Degree of Solubility (Fat or Water)
  • Ionic Character (Charge)
    • Acidic, Basic, and Neutral.
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2
Q

What determines molecular size?

A

Determined by the number and type of atoms present in the drug molecule and how these atoms are arranged in space.

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3
Q

What is the Partition Coefficient? (Definition)

A

A measure of overal polarity

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4
Q

What is the partition coeffiecient? (Formula)

A

P.C. = Concentration of drug in fat or lipid
Concentration of drug in water

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5
Q

Acids are? and acid form 2 letter symbol.

A

Proton Donors, HA

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6
Q

Bases are? and 2 character symbol?

A

Proton acceptors, B:

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7
Q

Acid form to conjugate base equation?

A

HA + H2O ⇔ H3O+ + A-

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8
Q

Base form to conjugate acid form equation?

A

B: +

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9
Q

What are 7 Acidic Functional groups found in drug molecules?

A

CSS-IUPE

  1. Carboxylic Acids
  2. Sulfonamides
  3. Sulfonylureas
  4. Imides
  5. Ureides
  6. Phenols
  7. Enols
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10
Q

What are 2 basic Functional Groups that are found in drug molecules?

A

AG

  1. Amines
  2. Guanidines
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11
Q

What is the Henderson-Hasselbalch Equation?

A

pH = pK + log (Base)

(Acid)

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12
Q

Three ways in which drugs cross biological membranes?

A
  • Filtration through pores
  • Passive Diffusion across lipid-like membranes (Un-charged drugs)
    • Simple passive
    • Carrier facilitated
  • Active Transport across lipid-like membranes (Charged drugs)
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13
Q

Difference between Filtration through pores and passive diffusion?

A
  • Filtration through pores:
    • Rate dependent on pressure gradient and on the size of the particle in relation to the size of the pore.
  • Passive Diffusion:
    • Molecules must possess the ability to:
      • dissolve in the aqueous phases bathing the membrane
      • dissolve in the lipid-like network of the membrane itself
    • Occurs in the direction of the concentration gradient and in proportion to the physical force of that gradient.
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14
Q

3 Routes of Enteral Administration?

A
  • Oral (p.o.)
  • Sublingual
  • Rectal
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15
Q

6 Routes of Parenteral (non-intestinal)?

A
  1. Subcutaneous (s.c.)
  2. Intramuscular (i.m.)
  3. Intravenous (i.v.)
  4. Intraarterial (i.a.)
  5. Inhalation
  6. Intrathecal
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16
Q

3 Routes of Topical Drug administration?

A
  1. Patches
  2. Dermatological and Opthalomological applications
  3. Intravaginal
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17
Q

What are the details of oral drug administration?

A
  1. Absorption occurs from stomach and small intestine (primary site for all drugs)
    1. Primarily by passive diffusion
    2. Rate:
      1. Depends on rate of dissolution of tablet/capsule
      2. P.C. of the drug
      3. Chemical Nature of the drug (Acidic, Basic, Neutral)
    3. Small intestine has larger surface area, and drugs stay there longer than the stomach.
  2. Drugs move from GI tract to Liver by portal system.
  3. First Pass Elimination
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18
Q

What are the details of sublingual drug administration?

A
  • Absorption via passive diffusion
  • Drugs enter general circulation before passing through the liver
  • Commonly used for nitroglycerin.
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19
Q

What are the details of the Rectal route of drug administration?

A
  • Absorption via passive diffusion
  • Drugs enter general circulation before passing through the liver
  • Good for unconscious or vomiting patients
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20
Q

What are the details of the subcutaneous route of drug administration?

A
  • Absorption occurs by passive diffusion through capillary membranes
    • Lipid soluble drugs.
  • Small molecules enter through pores
  • Large water soluble molecules enter blood via pores (but slowly)
  • Rate of absorption depends on blood flow to injection site.
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21
Q

What are the details of the intramuscular route of drug administration?

A
  • Generally the same as subcutaneous route
  • Can use larger volumes than s.c. route; more irritating drugs
  • Good for orally labile drugs ( e.g. Insulin)
  • Depot preparations
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22
Q

What are the details of the intravenous route of drug administration?

A
  • No absorption involved, drugs placed into the blood
  • Advantage - rapid onset of action; known amount of drug delivered
  • Drug cannot be withdrawn or absorption retarded
  • Good for emergency situations or hospitalized patients
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23
Q

What are the details of the Intraarterial route of drug administration?

A
  • Achieve high concentration of drug into one body site (e.g. liver)
    • Cancer treatment
24
Q

What are the details of the inhalation route of drug administration?

A
  • Primarily used for anesthetic/analgesic gases
  • Absorption occurs via passive diffusion
25
Q

What are the details of the Intrathecal route of drug administration?

A
  • Injection into spinal subarachroid space
  • Used in spinal anethesia and in CNS chemotherapy.
26
Q

What are the common types of drugs delivered by patches?

A

Nitroglycerin, nicotine, and clonidine

27
Q

What type of drugs are given intravaginally?

A

Antimicrobials

28
Q

What are the 5 factors that influence drug distribution?

A

PBPBD

  1. Physiochemical properties
  2. Nature of biological membranes encountered
  3. Protein binding and storage
  4. Blood perfusing a given tissue
  5. Disease states
29
Q

Details of drug distribution of capillary endothelial membrane?

A
  • First barrier to distribution
  • Same processes for drugs leaving
  • Special Capillaries
    • Kidney
    • Liver
30
Q

Membrane details of the Blood-Brain and Blood-CSF barriers?

A
  • Drugs cross blood-brain barrier mainly via passive diffusion
  • BBB - tight junctions between brain capillary endothelial cells
  • Drugs enter CSF via passive diffusion at ventricles or via active bidirectional transport systems in the choroid plexus.
  • Active transport primarily out of CSF and into the blood.
31
Q

Details of the Fetal Barrier

A
  • The placenta
    • Similar characteristics as capillary beds
    • Most drugs enter the fetus
32
Q

Details of “other” membrane barriers

A
  1. Prostate - Prostatic fluid pH = 6.4
    1. Ion trapping of basic drugs
    2. Blood supply
33
Q

kcal/mole of Covalent bond?

A

40-140 kcal/mole

34
Q

Storage and redistribution

What were the two examples of protein binding?

A

Albumin and a-glycoprotein

35
Q

Storage and Redistribution

Storage in fat details

A
  • Lipid soluble drugs (e.g. thiopental)
  • Environmental chemicals (PCBs, dioxins)
  • Poor blood supply
36
Q

Storage and Redistribution?

Details of storage in bone?

A
  • Drugs - tetracyclines (Calcium complexes)
  • Metals - lead (replace calcium in bone)
37
Q

Storage and Redistribution

Storage in non-target tissue?

A
  • Aminoglycosides; cephalosporins - Kidney
  • Anesthetics - fat
38
Q

Storage and Redistribution

Details of redistribution?

A
  • Can terminate pharmacological action of drugs
  • Initial distribution depends on blood flow to a body region.
39
Q

Where does Biotransformation of drugs occur primarily and ancillarily?

A
  • Primarily: Liver
  • Ancillarily: Kidney, Lung, nerve tissue, plasma, or GI tract.
40
Q

What are the 5 results of Biotransformation?

A
  1. Activate an inactive drug
  2. Inactivate an active drug
  3. Convert active drug to active metabolite
  4. Convert active drug or metabolite to toxic metabolite
  5. Metabolites are generally polar, more water soluble and excreted faster than the parent drug.
41
Q

What are the classes of biotransformation reactions?

A
  • Phase 1
    • Oxidation
    • Reduction
    • Hydrolysis
  • Phase 2
    • Conjugation or Synthesis
42
Q

Details of Microsomal enzymes

A
  • Located in smooth ER
  • Oxidative enzymes are known as mixed function oxidases (MFO)
    • Cytochrome P-450, terminal oxidase MFO
    • Require substrates be lipid soluble
    • Inducible (drugs: e.g. barbiturates; environmental chemicals)
43
Q

Details of non-microsomal enzymes?

A
  • Located in cytosol and mitochondria
  • Non-inducible
44
Q

7 Factors that influence the rate of biotransformation?

A
  1. Enzyme inducers (e.g. smoking, environmental agents, drugs)
  2. Enzyme inhibitors (e.g. competing drugs)
  3. Age
  4. Liver function/disease
  5. Nutritional State
  6. Genetics (e.g. acetylation)
  7. Gender
45
Q

Two forms of drug excretion?

A

Hepatic and Renal

46
Q

Details of Hepatic excretion?

A
  • Biliary excretion of drugs
    • Excretion of a drug from bile into the GI tract
  • Enterohepatic cycling
    • Liver to Small Intestine to portal system to liver.
47
Q

What are the three processes of Renal excretion of drugs?

A
  1. Filtration of drugs through pores in the glomerular capillary membrane
  2. Active transport of anionic and cationic forms of drugs in the proximal protion of the nephron.
  3. Non-ionic back diffusion of uncharged drugs occurs in the distal portion of the nephron.
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BMR 605 (10 decks)

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