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Pharm > Lecture 3 > Flashcards

Lecture 3 Flashcards

1
Q

Ligand

A

Molecules that bind to receptors

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2
Q

What is a protein that participates in intracellular communication via chemical signals?

A

Receptor

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3
Q

What are the 4 major classes of receptors?

A

Ligand-gated Ion channels
Protein Receptors
G-Protein Coupled receptors
Ligand-activated transcription factors

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4
Q

Nictonic Ach, glutamate, Glycine and GABA(a) all use what type of receptor?

A

Ligand-gated ion channels

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5
Q

Growth factors, insulin, and peptide hormones use which kind of receptor?

A

Protein receptor

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6
Q

Muscarinic receptor, alpha and beta adrenergic receptor proteins, and eicosamoids use what type of receptor?

A

G-Protein coupled receptors

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7
Q

steroid hormones, thyroid hormone, vit D use what kind of receptor?

A

Ligand-activated transcription factors

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8
Q

activating the alpha1-adrenergic receptor lead to what?

A

Activation of phospholipase

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9
Q

activating the alpha2- adrenergic receptor leads to what?

A

Inhibition of adenylyl cyclase

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10
Q

activating the B-adrenergic receptor leads to what?

A

Stimulation of adenylyl cyclase

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11
Q

Activation of muscarinic receptor leads to what?

A

Activation of phospholipase

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12
Q

What are the two general classes of ion channels?

A

Voltage-gated

Ligand-gated

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13
Q

What type of ion channel is activated by alterations in membrane voltage? (Na+ channel)

A

Voltage-gated ion channel

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14
Q

Some ion channels are able to become _________ and in this state the channels permeability can’t be altered for a certain period of time.

A

Refractory or inactivated

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15
Q

What type ion channel if activated after binding specific ligands or drugs?

A

Ligand-gated

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16
Q

What two drug classes act by altering the conductance of ion channels?

A 
Local anesthetics (voltage)
Benzodiazepines  (ligand)
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17
Q

How is cAMP produced?

A

Activation of adenyly cyclase by alpha-GTP subunits

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18
Q

What are two benefits of a signal-transduction pathway (second messenger)?

A

Signal amplification

Signal specificity

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19
Q

What is an example of a protein-linked kinase receptor?

A

Tyrosine kinase (has insulin receptors)

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20
Q

What receptor requires a signal to pass through the plasma membrane?

A

Intracellular receptors

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21
Q

What are important drug receptors located outside the plasma membrane?

A

Extracellular receptors

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22
Q

What are 2 drugs that have strong chemical bonds (covalent) that are irreversible?

A

Chemo

Aspirin (for the life of the platelet ~7 days)

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23
Q

Spare receptors are common for those that bind what?

A

Hormones and neurotransmitters

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24
Q

All these terms refer to what: Desensitization, tachyphylaxis, refractoriness, resistance, tolerance
?

A

Effect of a drug often diminishes when given continuously or repeatedly

25
Q

Loss of receptor function leads to what?

A

Rapid desensitization due to change in receptor conformation

26
Q

Reduction of receptor number leads to what?

A

Long-term desensitization due to change in receptor number

27
Q

What are 2 ways drug desensitization can happen that aren’t receptor mediated?

A
  1. Reduction of receptor coupled signaling components

2. Increased metabolic degradation

27
Q

what are some advantages of sublingual route of administration?

A

Rapid response
No 1st pass effect
bypass GI acids

27
Q

What is the reduction or ameiloration of drug effects due to opposing homeostatic response?

A

Physiological adaptation

27
Q

What is the probability of a drug occupying a receptor at any given instance?

A

Affinity

27
Q

What is the way the body handles the drug through absorption, distribution, biotransformation, and elimination?

A

Pharmacokinetics

27
Q

What is the process by which a drug leaves its site of administration and reaches the blood stream.

A

absorption

27
Q

What is the process by which the drug leaves the blood stream and enters the interstitial and/or cellular fluids

A

Distribution

27
Q

The alteration of the chemical structure of a drug by an enzyme

A

metabolism

27
Q

Most drugs move _____ across a membrane.

A

Passively

27
Q

Most diffusion occurs _____ cells, not between them.

A

through

27
Q

The greater the fraction of the drug that is ________, the greater the rate of diffusion.

A

Nonionized (uncharged)

27
Q

Non-ionized drugs diffuse easily at a ____ pH

A

High

27
Q

An intrathecal injection goes where?

A

Spinal fluid

27
Q

IP injection goes where?

A

Intraperitineal (into intestines)

27
Q

What is the max volume for an IM injection?

A

3 mL (in buttocks)

27
Q

WHat is the max for a subQ injection?

A

1 mL

27
Q

What type of administration should be used on an unconscious patient?

A

Rectal

27
Q

What is first pass metabolism?

A

Where the drug goes through portal circulation. Can inactivate a drug

29
Q

Which has a faster absorption- IM or SubQ?

A

IM

46
Q

What type of parenteral administration has the greatest risk of infection?

A

IV

47
Q

ligands include:

A

drugs, signaling molecules, hormones, neurotransmitters

48
Q

If a drug binds to a receptor but doesn’t produce a response it is referred to as what?

A

antagonist

49
Q

Time for ligand-gated ion channels?

A

hours to occur

50
Q

Time for protein receptors?

A

seconds to minutes

51
Q

Time for G-protein Coupled Receptors?

A

seconds to minutes

52
Q

Time for ligand-activated transcription factors?

A

milliseconds! (fastest)

53
Q

Examples of intracellular receptors (4)

A

nitric oxide, steroid, thyroid hormone, vitamin D

54
Q

most drug-receptor interactions are?

A

reversible and weak chemical bonds

55
Q

What binds reversibly to active site and blocks agonist?

A

Competitive Antagonist

56
Q

What binds irreversibly and prevents conformational change required for the activation of receptors?

A

Noncompetitive Antagonist

57
Q

What is an example that increases metabolic degradation?

A

Barbiturates - induce P450 enzymes that degrade drug

58
Q

Efficacy

A

magnitude of effect that can be produced by a drug

Pharm (29 decks)

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