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Advanced Pharmacology > Chapter 1: Basic Principles > Flashcards

Chapter 1: Basic Principles Flashcards

1
Q

What is Pharmacology?

A

Study of chemical interactions with living systems
-Medical Pharmacology: Substances used to prevent, diagnose, and treat disease

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2
Q

What is Toxicology?

A

Study of undesirable effects of chemicals on livings systems
-Toxins: Organic from living things
- Poisons: Inorganic from nonliving

Paracelsus: Father of toxicology
-Any compound can become poisonous if excessive amounts were taken in

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3
Q

History of Pharmacology

A

-First Recorded physician- Imhotep
-Still use traditional Chinese Medicine: Use of plants and animals (ex. Rhino horn used for fertility, Bear bile- Covid)
-People confused Rod of Asclepius and Caduceus
-Material Medica: First textbook of pharmacology
-Want Controlled Drug trials
>Avoid anecdotal evidence (Imermectin for COVID)

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4
Q

Pharmacodynamics

A

Effect of drug on the body (Why are we taking it?)

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5
Q

Pharmacokinetics

A

Effect of body on drug (ADME)

A: Absorption- Move across a barrier
D: Distribution- Where is the drug going to end up
M: Metabolism- Activate vs. Inactivate
E: Elimination- How do we get rid of it?

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6
Q

What is an agonist?

A

Molecule that binds to a receptor site that elicits a response similar to endogenous ligand
-Degree of response may differ from endogenous ligand

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7
Q

What is an antagonist?

A

Block endogenous ligand from binding to the receptor site
-Does not elicit a response

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8
Q

Allosteric Site

A

Molecule binds at a site away from orthosteric site, but still on same protein
Causes a conformational change change of the orthosteric site
-Activator vs Inhibitor

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9
Q

Orthosteric Site

A

Drug binds to the same site as the endogenous ligand

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10
Q

Bond Strength

A
  1. Covalent Bond Strongest (50-150 kcal/mol)
  2. Ionic (5-10)
  3. Hydrogen Bond (2-5)
    -Van der Waals Forces
  4. Hydrophobic: Not really bonds- just trying to stay away from water (0.5-1)
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11
Q

Bond Strength Relationship with Specificity

A

Inverse Relationship
-Strong bond=Less Specific

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12
Q

What is a racemic mixture?

A

Combination of R:S Isomers
-R:S isomers interact differently with receptor site so can cause different responses/side effects

-Sterioisomeres

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13
Q

Partial Agonist

A

Effect is much weaker than full agonist
- Absence of Full Agonist- Agonist
- Presence of Full Agonist- Antagonist
>Why? Competing for same receptor sites

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14
Q

Inverse Agonist

A

Agonist that favors (greater affinity) the INACTIVE form of receptor; suppresses response
- Acts as an antagonist b/c binds to inactive receptor so less active receptors available
-To have this; need to have constituent activity at the site with endogenous ligands still acting on site
>If site doesn’t have activity, then inverse agonist can’t occur

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15
Q

Competitive Antagonist/Inhibitor

A

Bind to same site so inhibits response by competition

Surmountable: Increase Agonist concentration and will achieve same Emax/response
-Increase EC50 or ED50 (move EC50 to the right on log dose vs response curve)

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16
Q

Non-Competitive Antagonist/ Allosteric Inhibitor

A

Binds to a different site causing a change to orthosteric site
-Receptor was a square, but now a circle so agonist
unable to bind

Insurmountable: No increase in agonist concentration will elicit same response
- Emax: Decreases
- EC50: Stays the same (i.e changing the scale)

17
Q

Irreversible Inhibitor

A

Binds to the same site, but unable to break connection
ex) covalent bond forms so inhibitor it does’t leave

Can be competitive or noncompetitive

Insurmountable: No increase in agonist
concentration will elicit same response because it is decreasing the amount of available sites
- Emax: Decreases
- EC50: Stays the same (i.e changing the scale)

18
Q

Beta 1 Receptor

A

Think Heart
-Agonist: increases heart rate
>Direct: Epi, Norepinephrine
>Indirect (mimic): Cocaine, Amphetamine (Blocks reuptake in synapse so epi stay longer)
-Partial: consider them anatagonist
>Pindolol, Acebutolol
-Antagonist: Keep same/constituent activity ~70 BPM
>Propanolol, Atenolol
-Inverse: further decrease constituent activity (decrease HR)
>Carvedilol, Nadolol

19
Q

Duration of Drug Action Scenarios

A
  1. Only act as long as drug binds receptor
    - tightly bound=longer duration; vice versa
  2. Long term downstream effects last until downstream effectors go away
    -Elicits a downstream effect: Cascade
    -Covalent bonds- receptor degraded (lysosome)
  3. Desensitization- Constantly being signaled; response will shut down (GPCRs)
20
Q

Good vs. Bad Receptor

A

Good:
- Selective: Only bind 1 ligand so not competing with other ligands
- Alteration: Changes shape/conformation that elicits cascade
Bad:
- Non-regulatory molecules that bind drugs with no detectable change in function
> Drug Carriers: Good for carrying stuff around body

21
Q

Drug Carriers

A

Plasma Proteins (Albumin):
- Free drugs cross borders; bound drugs don’t
- Decreased levels based on nutrition, liver funct.
- Other drugs may displace (kick) one another off
Types:
- Albumin: Binds mostly to acidic (release H+)
- alpha-acid glycoprotein: Binds mostly basic (release OH-)
- Lipoprotein: neutral drugs (cholesterol)

22
Q

What is potency?

A

Concentration of drug (EC50/ED50)required to produce 50% of maximal effect
- Sedation vs. very drowsy
- More potent: reaches EC50/ED50 with less drug dose

23
Q

Maximal Efficacy

A

-Greatest possible responses drug can deliver
- Emax higher
- Ex) Cardiac output increase comparing diff ionotropes
-Must also take into account drug toxicity

24
Q

Median Effective Dose (ED50)

A

Drug dose when 50% of population elicits the response we want

25
Q

Median Toxic Dose (TD50)

A

Dose of drug when 50% of population begin to elicit negative side effects

26
Q

Median Lethal Dose (LD50)

A

Dose of Drug when 50% of population dies

27
Q

Therapeutic Index

A

Establishes margin of safety of drug

Calculation: TD50/ED50
-Larger number/Wider margin means drug is safer
-Smaller number/Narrow margin: Probably should closely monitor patient (Digoxin)

28
Q

Bmax & Kd

A

Bmax: 100% of target receptors bounds
Kd: Drug concentration that binds 50% of target receptors

29
Q

Emax vs. EC50

A

Emax: Maximal drug response/effect
EC50: Concentration of drug that results in 50% response/effect

Ex) Pain scale

30
Q

Variations in Drug Response

A
  1. Drug-Drug Interactions
    -Ex) Phenytoin & Carbamazepine
  2. Individual patient responses vary
    -Idiosyncratic
    -Unusual: genetics (pharmacogenomics); hyporeact vs. hyperreact
  3. Tolerance: response changes over course
    Ex) Morphine
    -Tachyphylaxis: Quick tolerance (nitric oxide)
    4.Chemical Antagonist: interacts directly with the drug being antagonized to remove or prevent it from binding with its receptor site
  4. Physiology Antagonism
31
Q

Causes of Variation

A
  1. Alteration in conc of drug that actually reaches the receptor (Pharmacokinetics- ADME)
    -Age, weight, sex, disease state
  2. Variation in conc of endogenous receptor ligand
    Ex) Differing amount of epi circulating in body in diff people so B-blocker dose needed may be diff
    3.Alteration in # or function of receptors
    -Less receptors to begin w/ or receptor # decreasing
  3. Changes in components of response downstream to receptor
    - Post receptor process: use up messenger more quickly
    - Largest & most important cause of variation
    -Body has natural ability to compensate
32
Q

Physiologic Antagonism

A

Two different receptors causing a squelching of the intended response
Ex)
-Beta: Sympathetic response
-Muscarinic: Parasympathetic response

33
Q

Henderson Hasselbach Equation

A

PH= PKA + LOG (A-)/(HA)
-log function so 1x, 10x, 100x, 1000x

PH > PKA: Favors Unprotonated

PH < PKA: Favors Protonated

34
Q

Acidic Drugs

A

Release H+ into solution

Protonated form is uncharged
Unprotonated form is charged

“Trapping” in urine
OD with weak acid give NaHCO3 (Bicarb)
-Want to alkalinize urine

35
Q

Basic Drugs

A

Absorbs H+ from solution

Protonated: Charged
Unprotonated: Uncharged

“Trapping” Drug in Urine
OD with weak base give Ascorbic acid (Vit. C)
-Want to acidify urine

36
Q

Agonist mimic (indirect agonist)

A

Effects downstream inhibitors
Ex) usually blocks enzyme down the cascade
-Cocaine, amphetamine act like beta agonist but aren’t really effecting same receptor

37
Q

Understand Log dose vs. Response Curve

A

A: agonist alone
A+B: Competitive inhibitor
A+C: Allosteric/Noncompetitive Activator
A+D: Noncompetitive Inhibitor

Advanced Pharmacology (7 decks)

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