Introduction to Pharmacology (Maria Concepcion Sison, MD) Flashcards

1
Q

Body of knowledge concerned with the action of chemicals on biologic systems

A

Pharmacology

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2
Q

A substance that brings about a change in biologic function through chemical actions

A

Drug

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3
Q

A substance intended for use in the modification or exploration of the physiological system or pathological states for the benefit of the recipient

A

Drug (WHO definition)

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4
Q

T/F: Drugs can cause anaphylactic shock

A

True

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5
Q

Medical pharmacology is concerned with the use of chemicals in the (1), (2), and (3) of disease especially in humans.

A

(1) Prevention
(2) Diagnosis
(3) Treatment

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6
Q

What substances are used in pharmacologic prevention?

A
  1. Vitamins
  2. Vaccines
  3. Antibiotics
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7
Q

Concerned with the undesirable effects of chemicals on the living system

A

Toxicology

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8
Q

According to Paracelsus, what makes the poison?

A

The dose

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9
Q

The field concerned with the mechanisms of action and therapeutic and toxic effects of drugs. It describes the relationship between the concentration and pharmacological response.

A

Pharmacodynamics

REMEMBER: “D” for drug on body

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10
Q

Deals with the absorption, distribution, and elimination of drugs

A

Pharmacokinetics

REMEMBER: “K” for katawan on drug

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11
Q

A discipline that involves all aspects of the relationship between drugs and humans. Its ultimate goal is safe and effective prescribing.

A

Clinical Pharmacology

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12
Q

Reasons why drug therapy has changed over the last 4 decades

A
  1. Potency and diversity of drugs available
  2. Number of diseases that can be treated
  3. Impact of molecular biology on the development of drugs
  4. Pharmacological principles that underpin the rational use of medicines
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13
Q

What diseases have been eradicated in wealthier nations due to drug therapy?

A
  1. Pertussis
  2. Poliomyelitis
  3. Diphtheria
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14
Q

What common chronic diseases have benefited from the evolution of drug therapy?

A
  1. Asthma
  2. Hypertension
  3. Hypercholesterolemia
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15
Q

When did pharmacology start?

A

When the process of purification was introduced in the field of chemistry

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16
Q

What is the primitive form of the pharmacy?

A

Apothecary system

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17
Q

The person who discovered digoxin

A

Dr. William Wuthering of Scotland

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18
Q

What plant is digoxin derived from?

A

Purple foxglove (Digitalis purpurea)

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19
Q

What were the practical uses of digoxin prior to Wuthering’s discovery?

A
  1. Poison
  2. Healing of wounds (topical)
  3. Treatment of edema
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20
Q

When was digoxin officially introduced by Wuthering?

A

1785

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21
Q

What other diseases was digoxin used for for which it was unsuccessful in treating?

A

Adenitis, bronchitis, tuberculosis, typhoid, asthma, epilepsy, hydrocephalus, insanity and others

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22
Q

Describe the therapeutic index of digoxin

A

Narrow

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23
Q

The Father of Pharmacology

A

Oswald Schmiedeberg of France

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24
Q

What did Schmiedeberg isolate from the foxglove?

A

Digitoxin, the first pure glycoside

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25
Q

Who is the French pharmacist who isolated “digitalin” from foxglove 6 years before Schmiedeberg?

A

Nativelle, a French pharmacist

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26
Q

Who else discovered glycosides?

A

Mannheim and Kraft

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27
Q

What was digoxin marketed as in 1957?

A

Lanicor

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28
Q

Who said “Facts and facts alone are the basis of science.”?

A

Francois Magendie of France

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29
Q

What did Claude Bernard of France do?

A

Studied curare and CO gas on animals

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30
Q

What did Rudolph Buchheim of Germany do?

A

He established the first laboratory for experimental pharmacology in his basement.

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31
Q

Who coined the term “chemotherapy” and launched the antimicrobial era?

A

Paul Ehrlich of Germany

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32
Q

Who were the two notable individuals that contributed to the development of pharmacology in England?

A

John Newport Langley and Sir Henry Hallett Dale

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33
Q

Who introduced histamine as a receptor substance?

A

John Newport Langley of England

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34
Q

Who identified acetylcholine as a possible neurotransmitter?

A

Sir Henry Hallett Dale of England

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35
Q

The Father of American Pharmacology

A

John Jacob Abel

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36
Q

The Father of Philippine Pharmacology

A

Dr. Daniel De La Paz

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37
Q

Progress in physiology, biochemistry and molecular biology led to a more (1) approach to drug designs.

A

(1) Targeted

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38
Q

What were the first anti-hypertensive drugs to be developed?

A

Angiotensin Converting Enzyme (ACE) inhibitors

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39
Q

What are the different kinds of anti-hypertensive drugs?

A
  1. ACE inhibitors
  2. Angiotensin Receptor Blockers (ARBs)
  3. Renin inhibitors
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40
Q

What is the mechanism of action of an ACE inhibitor?

A

Prevents the conversion of AI to AII and bradykinin to inactive metabolites

41
Q

Properties of Angiotensin II

A
  1. Potent vasoconstrictor

2. Promotes release of aldosterone

42
Q

What is the equation for blood pressure?

A

BP = Cardiac Output x Peripheral Vascular Resistance

43
Q

ACE inhibitors are also known as?

A

Kininases

44
Q

What is the most common side effect of taking ACE inhibitors?

A

Cough due to decreased breakdown of bradykinins

45
Q

What is the mechanism of action of renin inhibitors?

A

They prevent the conversion of angiotensinogen to angiotensin I.

46
Q

What is the mechanism of action of angiotensin receptor blockers?

A

They prevent the conversion of angiotensin II to AT1 and AT2.

47
Q

What converts kininogen to bradykinin?

A

Kallikrein

48
Q

What is an example of a direct renin inhibitor?

A

Aliskiren

49
Q

Define: Chemotherapy

A

Use of chemotherapeutic agents to destroy microbes, parasites or cancer cells with minimal effect on healthy living tissues

50
Q

Define: Pharmacogenetics

A

It deals with genetically mediated variations in drug responses.

51
Q

Define: Pharmacogenomics

A

Use of genetic information to guide choice of drug therapy and/or dosage given to patient

52
Q

Define: Biopharmaceutics

A

It deals with the development of new drug delivery systems and dosage forms.

53
Q

What is the study of drug effects at the population level?

A

Pharmacoepidemiology

54
Q

Described in quantitative terms (i.e. sigmoid dose-response curves)

A

Pharmacodynamics

55
Q

What is the basis of development of most drugs?

A

Drug-receptor binding

56
Q

Example of a non-receptor mediated drug

A

Maalox or AlMgOH

57
Q

Explain: “Specificity is reciprocal.”

A

Certain classes of drugs bind only to certain targets. Conversely, certain targets only recognise certain classes of drugs.

58
Q

T/F: There are drugs that are completely specific in their actions.

A

False

59
Q

What side effects can penicillin cause?

A

Hypersensitivity and renal failure

60
Q

What are the different receptor conformations?

A
  1. Active

2. Inactive

61
Q

Define: Agonist

A

It favours the active receptor conformation.

62
Q

Define: Antagonist

A

It favours the inactive receptor conformation.

63
Q

What is an exception to the drug-receptor interaction?

A

Blood vessels

They maintain their tone despite absence of a ligand.

64
Q

Describe the mechanism of action of digoxin

A

Inhibits Na+/K+ ATPase -> lowers Na+ ingress -> increases Ca2+ -> increases contractility

65
Q

What enzyme inhibition effects does digoxin have on non cardiac tissue?

A
  1. Decreased sympathetic outflow from CNS
  2. Sensitization of the cardiac baroreceptors
  3. Reduction of renal tubular reabsorption of Na+
  4. Suppression of renin release from kidney
66
Q

What conditions can digoxin be used for?

A
  1. Congestive heart failure
  2. Atrial fibrillation
  3. Flutter
67
Q

Digitalis affects which parts of the body?

A

All excitable tissues including smooth muscle and CNS

68
Q

What does digitalis do to the heart?

A

Causes arrythmia

69
Q

What does digitalis do to the GI tract?

A

Causes anorexia, nausea, vomiting and diarrhea

70
Q

What effects can digitalis have on the nervous system?

A

Disorientation, hallucination and visual disturbances

71
Q

What is the therapeutic range of digitalis?

A

0.5 - 2.0 ng/mL (narrow)

72
Q

What is elimination?

A

Metabolism and excretion

73
Q

Deals with mathematical description of drug movement into, within and exit from the body

A

Pharmacokinetics

74
Q

Describe drug in the blood

A

Either free or protein-bound

75
Q

Which compartment model does digoxin follow?

A

Two-compartment model

76
Q

What is a very important assumption in pharmacokinetics regarding drug intake?

A

Once it is taken it, it is distributed uniformly.

77
Q

What is the formula for initial concentration?

A

Initial Concentration = Loading Dose/Volume of Distribution

78
Q

What is the formula for volume of distribution?

A

Volume of Distribution = Loading Dose/Initial Concentration

79
Q

Define: Steady-state condition

A

Rate of drug elimination equals rate of administration

80
Q

What is the formula for steady-state concentration?

A

Cpss = (fraction absorbed x maintenance dose)/(dosing interval x clearance)

81
Q

Define: Clearance

A

Ratio of the rate of elimination of drug to the concentration of drug in the plasma

82
Q

What is the relationship between of half-life, volume of distribution and clearance?

A

Half-life is directly proportional to volume of distribution and inversely proportional to clearance.

83
Q

What is the formula for half-life?

A

Half-life = (0.693)(Volume of Distribution)/Clearance

84
Q

What is the relationship between half-life and rate of action of the drug?

A

A shorter half-life means faster action, while a longer half-life means slower action.

85
Q

What are the values for F, Vd, half-life, percent metabolized and plasma protein binding of digoxin?

A
F = 0.75
Vd = 6.3 L/kg
Half-life = 40 hrs
Plasma protein binding = 20 - 40%
Percent metabolized = <40%
86
Q

What circulation contributes to the long half-life of digoxin?

A

Enterohepatic circulation

87
Q

What substance binds toxic drugs in the intestines?

A

Activated charcoal

88
Q

What proportion of digoxin is excreted unchanged in the kidney?

A

2/3

89
Q

What are the recommendations for digoxin use?

A
  1. Not a first-line drug
  2. Used only for symptom control
  3. To be used in patients with heart failure and atrial fibrillation
90
Q

What is rational drug use?

A
  1. Therapeutic efficacy
  2. Avoidance of toxicity
  3. Socially-responsible prescribing behaviour
91
Q

How many percent of doctor visits end in prescription writing?

A

70 - 90%

92
Q

How much does drug development cost on average?

A

$1.7 B

93
Q

What is the danger in patients taking multiple drugs?

A

Drug interactions may occur.

94
Q

What is the danger in elderly taking drugs?

A

There is more potential for adverse drug reactions.

95
Q

What aspect of pharmaceutical companies remain a threat to cost-effective prescribing decisions?

A

Direct-to-consumer advertising

96
Q

Enumerate the Rule of Rights

A
  1. Right indication
  2. Right drug
  3. Right route, dosage and duration
  4. Right patient
  5. Right patient information
  6. Right evaluation
  7. Right price

I Do Right for Patients. Patients Enable Practice.

97
Q

Define: Efficacy

A

How it can bring about what you want for the patient

98
Q

Define: Safety

A

Weighing benefits vs. risks and checking for contraindications and adverse effects