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BPM DLA1 > Lecture 29 > Flashcards

Lecture 29 Flashcards

1
Q

With what bond does drug mostly bind to drug receptor? (3)

A

hydrogen, ionic, or hydrophobic bonds with receptor

*Rarely, drugs form covalent bonds with their receptor

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2
Q

Which characteristics of drug determine whether it will bind to a particular receptor or not? (3)

A

size, shape, and charge of a drug

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3
Q

3 examples of drug that target ion channel

A

local anesthetics (block voltage-gated sodium channel)
Sedative-hypnotics
Anti-epileptics

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4
Q

How does drug targeting ion channel work?

A

drugs act by altering the conductance of ion channels

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5
Q

How does local anasthetic work?

A

the drug permeate through cell membrane and bind to cytosolic side of voltage-gated sodium channel blocking the channel.

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6
Q

2 examples of drugs that target g-protein linked receptor

A
  1. albuterol (beta2-agonist)

2. Propranolol (beta-antagonist)

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7
Q

2 examples of enzyme-linked receptor

A
  1. insulin receptor

2. epidermal growth factor receptor

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8
Q

What happens if gain-of-function mutation occur in tyrosine kinase receptor?

A

Tyrosine kinase receptors play a role in cellular growth and differentiation, so it is proto-oncogene. If the mutation occur, it can lead to cancer. So inhibitor of receptor is anticancer agents.

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9
Q

What is the drug imatinib?

A

tyrosine kinase inhibitor effective for leukemia

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10
Q

3 examples of nuclear receptor

A
  1. steroid hormone
  2. thyroid hormone
  3. vitaminD
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11
Q

Mechanism of nuclear receptor

A

hormone permeates through cell membrane and binds to intracellular receptor in cytosol. Then, hormone-receptor complex enters nucleus to bind to DNA, which leads to transcription.

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12
Q

3 examples of drugs that target enzyme

A

aspirin, ibuprofen, omeprazole

Most of these drugs work by inhibiting enzyme

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13
Q

examples of drugs that target transporter

A

prozac block serotonin re uptake by bind to transporter at synamptic cleft (used for treating psychiatric disorder)

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14
Q

examples of drugs that target structural proteins

A

some anticancer drugs bind to tubulin and prevent polymerization of spindle fiber, arresting cell division at metaphase.

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15
Q

1 examples of drugs that does not bind to receptor

A

antacids does not interact with receptor, but neutralize gastric acid chemically.

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16
Q

2 types of dose-response curves

A

graded & quantal

17
Q

Equation and shape of graded dose-response curve

A

E= (Emax *C) / (C+EC50)

Hyperbolic curve

18
Q

B= (Bmax*C) / (C + KD)

What does equation mean?

A

it is a relation between drug bound (B) to receptors and the concentration (C) of free drug

19
Q

B= (Bmax*C) / (C + KD)

In this equation, what does KD mean?

A

KD characterize the receptor’s affinity for the drug. Lower the KD, binding affinity is high.

20
Q

Compare binding curve and dose-response curve

A

shape looks the same (hyperbolic)
but binding curve is the relationship between drug bound to receptors and concentration of free drug while drug-response curve is relationship between concentration of drug and maximal effect of drug.

21
Q

How does logarithm of concentration change the shape of graded-dose-response curve and binding curve?

A

change from hyperbolic to sigmoidal curve

22
Q

What does it mean if EC50 is lower than KD?

A

It means an agonist does not have to occupy all receptor to evoke a full response. because certain number of receptors are spare and signal amplification occur. Due to signal amplification, not all receptor has to be bound to induce full effect of drug.

23
Q

Efficacy

A

magnitude of the response a drug produces.

maximal efficacy = E max

24
Q

Potency

A

a measure of concentration or amount of drug necessary to produce an effect of a given magnitude, determined by EC50

25
Q

Difference between agonist and antagonist and their effect on efficacy and affinity.

A

Agonist binds to receptor and brings about an effect, thus have receptor affinity and efficacy.
Antagonist inhibits the action of an agonist but has no effect in the absence of agonist. Thus it has receptor affinity but no efficacy.

26
Q

Competitive antagonism can be reversible and irreversible. Compare and contrast in terms of Emax and EC50.

A

For reversible, Emax is the same, EC50 moves to left.
The antagonist is surmountable by adding more agonist
For irreversible, Emax is reduced, EC50 same.
The antagonist is insurmountable, since receptor can respond to agonist.

27
Q

What is noncompetitive antagonism? (in terms of Emax, EC50)

A

it is allosteric antagonism, where antagonist binding at different site of agonist reduces action of agonist.
* Insurmountable, thus Emax decreased, EC50 decreased

28
Q

The curve shape of irreversible competitive antagonism and noncompetitive antagonism, are the same?

A

YES

29
Q

Two types of nonreceptor antagonism

A

physiological and chemical antagonism

30
Q

What is physiological antagonism? & example

A

One drug opposes another drug but through different receptors
ex) epinephrine (increase BP and bronchodilation) & histamine (decrease BP and bronchoconstriction)

31
Q

What is chemical antagonism? & example

A

a chemical antagonist reacts chemically with an agonist to form an inactive product.
ex) protamine, a protein which is positively charged, counteracts the effect of heparin (negatively charged)

32
Q

Difference between full and partial agonist. Their effect on Emax and efficacy

A

Partial agonist produce submaximal response at full receptor occupancy than agonist&raquo_space; lower E max&raquo_space; less efficacy
* Partial agonist can act as competitive antagonist in the presence of full agonist, by competing with full agonist for receptor occupancy.

33
Q

What is constitutive activity of receptor?

A

many receptor system shows some activity in the absence of agonist, that fraction of the receptors is always in the active state

34
Q

What is inverse agonist

A

it reverse the constitutive activity of the receptor

35
Q

What is quantal dose-effect curves?

A

it plots the fraction of population that responds to a given dose of drug as a function of drug dose, unlike graded, it defines response as either present or not present.

36
Q

Difference between ED50, TD50, LD50

A

ED50 : Dose at which 50% individuals exhibit specified quantal effect
TD50: Dose at which a particular toxic effect in 50% of animals produced
LD50 : Dose required to cause death in 50% of animals

37
Q

Therapeutic index (2)

A

TD50/ED50 or LD50/ED50

38
Q

Describe safe drug in terms of TD50 and ED50

A

Safe drug will have large toxic dose and a small effective dose

39
Q

What is therapeutic window?

A

the dosage range between the minimum effective therapeutic concentration and the minimum toxic concentration

BPM DLA1 (47 decks)

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