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3.23 > Lecture 2: Drug/ Target Interactions > Flashcards

Lecture 2: Drug/ Target Interactions Flashcards

1
Q

What are the drug characteristics that affect absorption? (4)

A

Molecular weight, ionisation, solubility and formulation

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2
Q

What patient factors affect absorption?

A
  • Route of administration
  • Contents of GI tract
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3
Q

Do drugs bound to plasma proteins cross the membrane?

A

No

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4
Q

How does malnutrition lead to an increase in free drug?

A

Malnutrition means a decrease in albumin so an increase in free drug.

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5
Q

Where do lipophilic drugs accumulate?

A

Adipose tissue

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6
Q

How much of digoxin is absorbed?

A

70-80%

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7
Q

What is the half life of digoxin?

A

26-45 hours

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8
Q

What is the primary route of metabolism?

A

Liver

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9
Q

What can statins interact with? (4)

A
  • Grapefruit
  • Warfarin
  • Courmarins
  • Certain antimycotics
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10
Q

How do you calculate the therapeutic index?

A

minimum toxic dose/ minimum effective dose

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11
Q

What drugs are renally cleared? (8)

A
  • Aminoglycosides
  • Glycopeptides
  • Amikacin
  • Gentaminic
  • Vancomycin
  • Digoxin
  • Lithium
  • morphine 6-glucuronide
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12
Q

What is steady state?

A

Drug administered is equal to the amount of drug eliminated within one dosing interval resulting in a plateau or contant serum drug level

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13
Q

How many half lifes does it take to reach 100% steady state?

A

5

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14
Q

What is efficacy?

A

The degree to which a drug is able to produce the desires response

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15
Q

What is the effective concentration 50% ?

A

Concentration of the drug which induces a specified clinical effect in 50% of subjects

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16
Q

What is the lethal dose 50%

A

Concentration of the drug which induces death in 50% of subjects

17
Q

What is the theraputic index?

A

Measure of the safety of the drug

18
Q

What is the margin of safety?

A

Margin between the theraputic and lethal doses

19
Q

What is an agonist?

A

A ligand that binds and actiavtes a receptor

20
Q

Give examples of endogenous ligands?

A
  • Neaurotransmitters
  • Hormones
21
Q

How long do ion channel linked receptors take to exert an effect?

A

Milliseconds

22
Q

How long do G-protien linked receptors take to exert an effect?

A

Seconds

23
Q

How long do tyrosine kinase linked linked receptors take to exert an effect?

A

Minutes

24
Q

How long do DNA linked receptors take to exert an effect?

A

Hours to days

25
Q

Give an example of an ion channel linked receptor?

A

Nicotinic acetylecholine receptor

26
Q

Give an example of a G-protien linked receptor?

A

B-adrenergic receptor

27
Q

Give an example of a tyrosine kinase linked receptor?

A

Insulin receptor

28
Q

Give an example of an DNA linked linked receptor?

A

Steroid receptor

29
Q

Where are cell surface receptors found?

A
  • Cell surface
  • On an organelle within the cell
  • In the cytoplasm
30
Q

What can cell surface receptors be?

A

Proteins or glucoprotiens

31
Q

What actions can occur when a drug binds to its receptor?

A
  • Ions channel opens and closes
  • Second messenger is activated: cAMP, Calcium, inositol phosphates etc. This initiates a series of chemical reactions
  • Cellular function can be turned on/ off
32
Q

What is the treatment for cardiovascular disease?

A

Manipulation of cardiac output, peripheral vascular resistance and blood volume

33
Q

What is the prevention for cardiovascular disease?

A
  • Reduce platelet adhesion
  • Reduce cholesterol
34
Q

How do you reduce atherogenesis?

A

Reduce platelet adhesion

35
Q

What is used to reduce platelet adhesion?

A
  • Irreversible cyclooxygenase inhibitors: aspirin
  • Adenosine diphosphate receptor inhibitor: clopidogrel
36
Q

What drugs cause contraction?

A
  • calcium channel blocker
  • Agonst
  • Noradraline
  • Histamine
  • angiotensin
37
Q

What drugs cause relaxation?

A
  • Potassium channel activators
  • Adenosine
  • B agonist
  • Prostaglandins
38
Q

What causes cell relaxation?

A
  • Noradrenaline
  • Histamine
  • Angiotensin
39
Q

What agonists cause cell relaxation and hyperpolarisation?

A
  • Adenosine
  • B agonists
  • Prostaglandins
  • PDE Inhibitor

3.23 (26 decks)

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