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Pharmacology Exam 1 (Lauren) > L2 and 3 Pharmacodynamics II and III > Flashcards

L2 and 3 Pharmacodynamics II and III Flashcards

1
Q

Are Kd and EC50 usually the same?

A

Yes, unless there are spare receptors

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2
Q

What does the curve of an antagonist drug look like?

A

a FLAT LINE

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3
Q

What does a competitive antagonist do to ED50 and Emax?

A

ED50 increases

Emax unchanged

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4
Q

What does a non-competitive antagonist do to ED50 and Emax?

A

ED50 might change

Emax decreases

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5
Q

Can you overcome the effects of competitive antagonists?

A

YES, by increasing the dose of the agonist

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6
Q

As antagonist concentration increases the potency of the agonist _______

A

Decreases (increases EC50)

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7
Q

What are the 2 mechanisms of non-competitive antagonists?

A
  1. Bing to a secondary site and inhibit receptor binding (allosteric)
  2. Covalently (irreversibly) bind to the same site as the agonist
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8
Q

Can you overcome the effect of non competitive antagonism by increaseing the dose of the agonist?

A

NO

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9
Q

What is an example of physical/functional antagonism/.

A

Reversing a fall in blood pressure due to histamine by giving epinephrine

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10
Q

What is an example of chemical antagonism?

A

Neutralizing stomach acid with antacids

Also inactiviating heparin with protamine sulfate

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11
Q

THe dose response curve for a partial agonist will have _______ Bmax and Emax compared to the full agonist

A

Lower

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12
Q

In the presence of full agonists, partial agonists act like ________

A

Competitive antagonists

So you could overcome the effects of the partial agonist by giving increasing dose of the full agonist

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13
Q

How do intracellular receptors and their ligands have an effect?

A

Modify gene transcription in the nucleus (slow effect but long lasting)

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14
Q

What is an example of lipid soluble ligands and their intracellular receptors?

A

Binding of glucocorticoids to remove heat shock protein

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15
Q

How do tyrosine kinase receptors effect biochemical processes

A

PHOSPHORYLATION of things

Often growth factors and insuliN

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16
Q

What pathway is activated by cytokine receptors?

A

JAK/STAT

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17
Q

What are examples of ligand gated ion channels?

A

Acetylcholine binging to Nicotnic receptors and opening Na+ channels

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18
Q

What is an example of voltage gated ion channels?

A

Local anesthetics and anticonvulsants

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19
Q

What kind of an effect does GABA have?

A

Sedative effect

Opens Cl- channels

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20
Q

What effect do G protein coupled receptors have on signal magnitude?

A

The signal is amplified

One ligand results in multiple effector signals

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21
Q

What does desensitization mean?

A

The response to a G-protein coupled receptor will decrease over time and the number of receptors will be lowered

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22
Q

What pathway os activated by tyrosine kinases (TPK)?

A

Ras/RAF

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23
Q

What pathway is activated by cytokines?

A

JAK/STAT

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24
Q

What increases when Gq receptors are activated ?

A

Intracellular calcium

Phospholipase C, DAG, IP3 etc etc

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25
Q

What is an example of Polyphospoinositide signaling?

IP3

A

M1 and M3 muscarinic receptors (ACh)

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26
Q

What type of receptors are Gs

A

Beta

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27
Q

What type of receptors are Gi

A

Alpha 2

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28
Q

What type of receptors are Gq?

A

Alpha 1

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29
Q

Which way does the dose response curve shift if a system has spare receptors?

A

Left

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30
Q

Does an agonists have both efficacy and affinity?

A

Yes

31
Q

Does affinity have anything to do with drug efficacy?

A

NO

32
Q

Which kind of DR curve provides information regarding potency and Emax?

Graded or quantal?

A

Graded

33
Q

Which tupe of DR curve indicates the variability among individuals:
Graded or Quantal?

A

Quantal

34
Q

Which type of DR curve is used to determine the therapeutic index and margin of safety:
Graded or Quantal?

A

quantal

35
Q

What number shows the amount either in percentage or as a multiplication factor, by which ED99 may have to be increased to produce death in 1% of the population?

A

Therapeutic index and margin of safety

36
Q

What is tolerance?

A

Response to a drug diminishes with repeated or chronic administration

37
Q

What is pharmacokinetic tolerance?

A

Response to a drug decreases because the enzymes that metabolize the drug are induced, and DRUG LEVELS CHANGE

38
Q

What is an example of pharmacokinetic tolerance?

A

Phenytoin increasing metabolism of leothyroxine

39
Q

Do drug levels change in pharmacokinetic tolerance?

A

YES

40
Q

What is pharmacodynamic tolerance

A

Response decreases due to changes in receptor number or function. DRUG LEVELS DO NOT CHANGE

41
Q

Do drug levels change in pharmacodynamic tolerance?

A

NO

42
Q

What explains decreased efficacy of opioids even though dosage is the same?

A

Pharmacodynamic tolerance

43
Q

What is physiologic tolerance?

A

Occurs when two agents with opposite effects are administered together
Ex: histamine + norepinephrine

44
Q

What is competitive tolerance?

A

Occurs when a receptor antagonist is administered with an agonist
Ex: yohimbine may block the hypotensive effect of clonidine

45
Q

What is Tachyphylaxis

A

VERY RAPID development of tolerance following repeated dose over short period of time
Ex: Meth addict smoking every 15 minutes

46
Q

What usually causes tachyphylaxis?

A

Stimulants

47
Q

How does an ion channel respond to being desensitized?

A

Converts it to an altered state that remains closed

Ex: succinylcholine on nicotinic ACh receptor

48
Q

How does G-protein receptor respond to being desensitized?

A

The receptor coupling effector gets phosphorylation to an inactive form (GRK, B-arrestin)

Ex: B-receptor

49
Q

What is “a process of ligand-induced endocarditis and degradation of receptors”

A

Down-regulation

50
Q

In general, agonists cause a ______-regulation of receptors if chronically administered

A

down

51
Q

What is the difference between summation and synergism?

A

Summation: 1+1=2

Synergism: 1+1=5

52
Q

Summation or synergism: two drugs acting by the same mechanism

A

Summation

53
Q

What is an example of synergism

A

Depression of CNS produced by diazepam plus ethanol. Act on GABA receptor but on different sites

54
Q

How does administration of an antagonist result in supersensitivity to a drug?

A

Up-regulation of receptors due to prolonged presence of antagonist

55
Q

What is denervation supersensitivuty?

A

Develops when presynaptic nerve has been destroyed, resulting in a decrease of endogenous ligand, but a HUGE increase in receptors.
If you ever get that drug again, it’s a huge response.

56
Q

What happens if a drug is displaced from plasma binding sites?

A

The response to that drug is intensified

Ex: 99% of warfarin is bound to albumin, and 1% is free and active. If only 98% is bound due to getting kicked off by phenytoin, you now have twice as much active warfarin.

57
Q

Do you increase or decrease a patients warfarin dose if they start taking phenytoin?

A

DECREASE

58
Q

What is another term for “overdose”

A

Overextension of the therapeutic effect

59
Q

What is the treatment for overextension-type toxicities (overdose)

A

Find approprotate dose that is effective but not toxic. If that cant be done (chemotherapy), give sub-therapeutic levels of two drugs that will act synergistically

60
Q

What usually causes an abnormal response to a drug that is NOT immunologically mediated/

A

PharmacoGENETIC disorders

61
Q

What happens when you give succinylcholine to patients with abnormal serum cholinesterase?

A

Apnea; prolonged paralyzation

62
Q

What could explain a patient not getting any pain relief from codeine?

A

Patient may have deficiency in CYP 2D6

codeine must be metabolized for full analgesic effect

63
Q 
These are symptoms of what type of drug allergy:
Gi allergy
Hives
Asthmma
Anaphylactic shock
A

Type I-anaphylactic reaction

64
Q

What is the treatment for type I anaphylactic reactions?

A

Injection of epinephrine

Corticosteroids

65
Q

Penicillin induced hemolytic anemia is what type of drug reaction?

A

Type II

66
Q

What mediates Type IV delayed hypersensitivity reactions?

A

CELL - MEDIATED

Sensitized T-cells

67
Q

Contact dermatitis is an example of which type of hypersensitive reaction/

A

Type IV- Delayed hypersensitivity reaction

68
Q

What type of hypersensitivity reaction causes serum sickness?

A

Type III Arthrus reactions

69
Q

What are the symptoms of serum sickness?

A

Urticaria
Arthritis
Lymphadenopathy
Fever

70
Q

Erythema multoforme and SJS are forms of what?

A

Serum sickness- Type III Arthrus reaction

71
Q

What kind of drugs frequently cause Type III Arthrus reactions/serum sickness?

A

Anticonvulsants

Sulfonamides

Penicillins

72
Q

Smoking and charbroiled foods can increase the metabolism of many drugs including warfarin. What is this type of tolerance called?

A

Pharmacokinetic

73
Q

Why do you have to take a patient off propranolol if you give them epinephrine for bronchodilation?

A

Propranolol is a non-selective B-adrenoceptor antagonist that has anti bronchodilation effects.
Verapamil is a better blood pressure drug since it is a calcium channel blocker with no effects on bronchodilation

Pharmacology Exam 1 (Lauren) (7 decks)

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