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PHAR 300 > Lec. 2 - Pharmacodynamics 1 > Flashcards

Lec. 2 - Pharmacodynamics 1 Flashcards

1
Q

What are the 3 ways drugs can be named?

A
  • Chemical name: useful for chemical formula + structure
  • Generic name: universal name adopted by USAN and WHO
  • Trade name: Registered trademark
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2
Q

What’s the difference between pharmacodynamics and pharmacokinetics?

A

Pharmacodynamics: what the drug does to the body

Pharmacokinetics: what the body does to the drugs

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3
Q

What are indications?

And contraindications?

A

Indications: when/how to use drug

Contraindications: when/how NOT to use drug

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4
Q

What are the 4 principles of pharmacokinetics?

A
  1. Absorption
  2. Distribution
  3. Metabolism
  4. Excretion

ADME!

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5
Q

What are the 4 mechanisms through which a drug can affect a system?

A

Through…

  1. Receptors
  2. Ion channels
  3. Enzymes
  4. Immune system
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6
Q

What are 6 principle methods of drug administration?

A 
Sublingual
Parenteral
Inhalation
Topical
Oral
Rectal

(SPIT, OR [else])

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7
Q

What are 4 features of oral administration of drugs?

A
  • easy/cheap/convenient
  • generally uses modified-release tablets
  • Most absorption in small intestine (some in stomach)
  • Significant amount of drug is inactivated by the liver during first pass
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8
Q

Describe how the liver affects drug absorption upon administration.

A

First pass effect:

Upon absorption into the blood stream, the drug passes into the liver, which inactivates a significant portion of the drug.

Proportion of what’s left (compared to administration) is called bioavailability.

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9
Q

Describe 3 features of parenteral drug administration

A
  • Injection
  • Fast, accurate, bypasses liver
  • 3 injection sites (from superficial to deepest):
    1. Subcutaneous
    2. Intravenously
    3. Intramuscularly
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10
Q

Describe inhalation as drug administration.

A

-lungs have large surface area, so there is a greater amount of distribution

  • Systemic effects occur in seconds
    (ex. Cigarette in 7 seconds reached brain)

-Nasal mucosa effects in minutes
(Ex. Cocaine)

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11
Q

Describe 2 features of topical drug administration.

A
  • skin is made to prevent absorption, so more difficult

- still some methods of workaround (ex. The patch)

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12
Q

Describe 3 features of sublingual drug administration

A
  • under the tongue
  • straight into vasculature, avoids first pass of liver
  • very rapid effects
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13
Q

How do drugs effect an organism (micro to macro)

A

Targets…

Subcellular structure (ex. Receptors)
->
Cell
->
Tissues
->
Organs/organ systems
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14
Q

What is drug selectivity?

A

What is the drug target? How localized will the effect be?

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15
Q

What are some drugs that have little to no specificity (name 4)

A
  • Osmotic agents
  • Acidifying drugs
  • Alkylinizing drugs
  • metal chelators

Basically, simple chemical agents that diffuse around

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16
Q

What is a drug receptor?

How do they mediate drug activity?

A

A macro molecular protein (generally membrane bound) to which endogenous ligand or exogenous agonist/antagonist will bind.

Link to cellular response machinery allows for downstream effect

17
Q

Name methods of transmembrane signalling mechanisms

A

I. Intracellular receptor

II. R-activated enzyme

III. R-activated tyrosine kinase

IV. R-Activated ion channel

V. G protein coupled receptor

18
Q

Describe ion channels (4)

A
  • Transmembrane protein
  • Very specific in which ion it allows passage (selectivity pire)

-3 states:
I. Open
II. Closed
III. Inactivated

-Voltage/binding/pressure controlled

19
Q

What are carrier molecules? What is there function in cells?

A

Transport proteins that help regulate and maintain electrochemical gradient.

20
Q

What are GPCRs (3)

A

-7 transmembrane domains

-g-protein activation will activate or inhibit an enzyme, which produces a second messenger that either
•Opens/closes ion channel
•Has other cellular downstream effects

-frequent target of hormones

21
Q

What is receptor turnover?

A

After use, a receptor can be recycled, degraded or more

22
Q

How does receptor Tyrosine kinase work?

A

Dimerization!

  1. Ligand binds first receptor
  2. Second receptor diner is es
  3. Activates TKR proteins (through phosphorylation)
  4. Causes downstream effects, such as transcription
23
Q

Describe cytokines receptor activity

A

Similar to TKRs, dimerize to activate, intracellular proteins are phosphorylation, then relocate to nucleus and activate transcription

24
Q

What are naturetic peptide receptors?

A

Receptors that respond to peptides (less common)

25
Q

Describe 4 features of intracellular receptors

A
  • Found within cells (not on membrane)
  • Hormones must diffuse to activate (ie ligands must be lipophilic)
  • Function - alter gene transcription/protein synthesis

-3 main types
I. Estrogen
II. Progesterone
III. Glucocorticoid

26
Q

What is the timescale of response for

  1. Ion channels
  2. GPCRs
  3. Enzymes
  4. DNA-linked receptors
A
  1. Msec
  2. Sec
  3. Min
  4. Hours
27
Q

Are there drugs that bypass receptor activity? Ex.?

A

Yes, some interrupt/stabilize actual cell processes,

ex. Drugs that interrupt microtubule formation (disrupting mitosis)

PHAR 300 (9 decks)

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