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[Ther 201] 1st Exam Transes > Quantitative Analysis of Drug-Receptor Interactions (C.I. Valencia, MD) > Flashcards

Quantitative Analysis of Drug-Receptor Interactions (C.I. Valencia, MD) Flashcards

1
Q

T/F: Pharmacokinetics deals with “dose”, while pharmacodynamics deals with “concentration”.

A

True

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2
Q

What is the cardinal rule in Pharmacology?

A

You cannot create a new drug effect. You can only alter cellular function. Drugs are simply modulators.

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3
Q

What does drug molecule-receptor binding lead to?

A

Enhancement, inhibition or blockade of molecular signals

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4
Q

T/F: Clinical effects are only those we can observe with our five senses.

A

True

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5
Q

How do you know how much of a drug you need to achieve a certain effect?

A

Look at the dose-response relationship.

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6
Q

Enumerate the three most important properties of a drug

A

Efficacy
Safety/Lack of Toxicity
Quality

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7
Q

T/F: More is always better in terms of bioavailability

A

False

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8
Q

Differentiate generics and innovators

A

Generics usually have a dirty synthetic pathway but are cheaper than innovators.

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9
Q

How many % of drug actions are not mediated through receptors?

A

10%

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10
Q

T/F: Mannitol and acetylcystein are example of receptor-mediated drugs.

A

False

They are not.

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11
Q

What drugs do not bind to receptors?

A

Antacids
Osmotic diuretics
Acid-base reactions

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12
Q

T/F: A dose does not necessarily translate to an effective drug concentration.

A

True

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13
Q

How does the ligand interact with its receptor?

A

Lock-and-key fashion

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14
Q

What is the property that pertains to the orientation of the receptor in three-dimensional space?

A

Stereospecificity

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15
Q

What are the four types of protein receptors?

A
  1. Receptors for endogenous regulatory ligands
  2. Enzymes of metabolic pathways
  3. Enzymes in transport processes
  4. Structural proteins
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16
Q

What determines differences in drug effects in different tissues?

A
  1. Drug properties
  2. Receptor properties
  3. Tissue properties
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17
Q

Define: enantiomers

A

These are non superimposable mirror images of the same substance.

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18
Q

Describe: Erasomate

A
  1. Sold as an anti-parasitic

2. Made up of levamisol (-) and teramisol (+)

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19
Q

Describe: Stirizine

A

Antihistamine

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20
Q

Describe the up regulatory effect of propanolol

A

It is a beta adrenergic antagonist that lowers blood pressure. Next dosage has a greater effect.

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21
Q

Describe the down regulatory effect of sulfonylurea

A

Overstimulation of agonists in the pancreas leads to decreased efficacy of the drug.

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22
Q

What is the effect of opium analgesics on the brain?

A

Stimulates mu, delta and kappa receptors leading to analgesia

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23
Q

Give an example of a covalent interaction between drug and receptor.

A

Acetyl group of ASA and cyclooxygenase

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24
Q

What are the chemical forces involved in drug-receptor interaction?

A

Covalent bonds
Electrostatic
Hydrophobic bonds

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25
Q

What is the inactive form of ampicillin?

A

Pivampicillin

26
Q

What are the types of dose response curves?

A

Graded Response Curve

Quantal Response Curve

27
Q

What is the shape of the non-logarithmic graded response curve?

A

Hyperbolic

28
Q

T/F: The central portion of the sigmoid graded response curve is nearly linear.

A

True

29
Q

What do you call the highest intensity of effect a drug can achieve?

A

Efficacy

30
Q

Why is there variability in the dose response curve?

A

It depends on the person, age, weight, clearance effect, dose, etc.

31
Q

Describe steep and gradual dose response curves.

A

Steep: cobra ready to bite
Gradual: resting Buddha

32
Q

Give the formula for therapeutic index

A

Therapeutic Index = LD50/ED50

33
Q

In the presence of a competitive antagonist, the response curve is shifted to the?

A

Right

34
Q

Describe: Maximal effect

A

Point at which a drug’s effect plateaus even with continued increase in dose

35
Q

Differentiate efficacy and potency

A

Efficacy - effect of drug irrespective of dose

Potency - effect of drug with respect to dose

36
Q

Potency is determined by what variable?

A

EC50 or ED50

37
Q

If a drug expires, what happens to its potency?

A

It will degrade.

38
Q

T/F: Dose is dependent on the smallest concentration available.

A

False

It is dependent on what is feasible to be taken in by humans.

39
Q

T/F: Potency is not an important factor.

A

True

40
Q

T/F: You should always choose a drug that is more potent than efficient.

A

False

It should be more efficient. We don’t care about potency.

41
Q

Describe: Quantal Response Curve

A

All or none event

Concentration vs. number responding

42
Q

What do you call patients who respond to a small dose of a drug?

A

Sensitive

43
Q

What do you call patients who only respond to high concentrations of a drug?

A

Tolerant

44
Q

T/F: Not all persons will manifest with a positive quantal response at the same drug concentration due to variation.

A

True

45
Q

How many % of respondents will respond to a median dose of the drug?

A

68%

46
Q

What are quantal dose curves used for?

A

Generating the margin of safety for a particular drug

47
Q

Enumerate the different examples of non-receptor drug action

A
  1. Acid-base neutralisation
  2. Colligative effects in the bronchi (acetylcysteine-initiated breakage of disulphide bonds)
  3. Counterfeit incorporation mechanism (purine and pyrimidine analogs in cancer treatment)
  4. Osmolality effects in the brain (mannitol and brain)
48
Q

T/F: Therapeutic index = margin of safety

A

True

49
Q

What is the desirable margin of safety?

A

100 - 1000

50
Q

What harmful effects can phenobarbital cause?

A

Apnea and coma

51
Q

Is diazepam a safe sedative?

A

Yes

52
Q

T/F: TIs of 5 and below indicate drugs with relatively greater potential for toxicity.

A

False

Statement is true for TIs of 4 and below.

53
Q

Describe the mechanism of action of azoles

A

They possess a heterocyclic ring with sulfur and nitrogen inside, which is used against amoeba and fungi.

54
Q

Describe: citrizine

A
  1. Drug used to treat colorectal cancer

2. Possesses a combination of L-citirizine and D-citirizine

55
Q

What is the phenomenon that occurs when the diagnostic, preventive and therapeutic action of a drug is modified or altered by another drug when administered concomitantly?

A

Drug interaction

56
Q

What are the quantitative aspects of pharmacodynamic drug interactions?

A
  1. Synergism/potentiation
  2. Addition
  3. Inhibition
57
Q

What causes pharmacokinetic drug interactions?

A

Alterations to ADME

58
Q

What are the clinical classifications of drug interactions?

A
  1. Beneficial

2. Adverse

59
Q

What are the requirements of rational therapy?

A
  1. Diagnostic certainty
  2. Pathophysiological understanding
  3. Pharmacological understanding
  4. Optimal drug & dose administration
  5. Picking efficacy/toxicity end points and monitoring
  6. Open communication and willingness to alter regimen
60
Q

Enumerate the factors that affect therapeutic outcomes

A
  1. Age
  2. Drug-drug interactions
  3. Fixed-dose combination
  4. Placebo effects
  5. Tolerance
  6. Genetic factors
61
Q

Enumerate the factors that contribute to lack of efficacy

A
  1. Misdiagnosis
  2. Poor compliance
  3. Poor choice of dosage
  4. Development of separate illness
  5. Use of other drugs
  6. Undetected genetic/environmental variables
  7. Unknown therapy by another physician

[Ther 201] 1st Exam Transes (11 decks)

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