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Principles Of Pharmacology > Week 2 > Flashcards

Week 2 Flashcards

1
Q

Outline the processes that occur between administration of a drug and its effects.

A 
Dose administration. 
Disintegration / dissolution. 
Absorption
Distribution
Metabolism
Excretion
Drug-receptor Action
Effect
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2
Q

What is used to aid the disintegration/ dissolution of drugs?

A

Excipients

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3
Q

What is drug disposition?

A

The movement of the drug though the body aiming to form a pool of active drugs in the body.

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4
Q

What happens to drugs one they have formed active pools in the body?

A

Move reversibly to the site of action.

Move reversibly to tissues to be stored.

Cause metabolic activation (reversibly).

Cause metabolic inactivation

May be directly excreted

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5
Q

What causes the Cmax of a curve showing drug concentration against time?

A

Rate of absorption and rate of elimination.

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6
Q

How is the dose administered shown on a graph of drug concentration against time?

A

It is where the initial point on the y axis is plotted. Should be at time 0 on the x axis.

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7
Q

How is therapeutic range calculated?

A

(Maximum safe concentration)/ (Minimum effective concentration)

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8
Q

Define toxic dose of a drug.

A

The minimum dose required to produce adverse effects.

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9
Q

Define maximum safe concentration of a drug.

A

Maximum safe concentration of drug in the plasma above which adverse effects are precipitated.

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10
Q

Define therapeutic window of a drug.

A

The range of dosage of a drug of its concentration in a bodily system that provides safe and effective therapy.

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11
Q

Define minimum effective concentration of a drug.

A

The minimum concentration of a drug in serum required to produce a desired pharmacological effect in most patients.

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12
Q

Define ineffective range of a drug.

A

Insufficient drug concentration present to produce the desired pharmacological effect.

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13
Q

What is Phenytoin used to treat?

A

Used to reduce the number of seizure episodes in people with epilepsy or people who have had brain or neural surgery.

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14
Q

What are the negatives of using Phenytoin as a seizure treatment.

A

Has many adverse effects when the dosage reaches the toxic range.

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15
Q

Name drugs which have a narrow therapeutic range.

A

Phenytoin

Warfarin

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16
Q

What Warfarin used for?

A

It is an anticoagulant used to reduce blood clots.

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17
Q

What happens if too much warfarin is taken?

A

Can lead to haemorrhages if the dosage reaches the toxic range.

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18
Q

Why does treatment with warfarin often require many dosage adjustments?

A

Warfarin has a very narrow therapeutic range which can affect the patients response.

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19
Q

What issues can arise if warfarin treatment doesn’t work?

A

Thrombotic effects

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20
Q

What are thrombotic effects?

A

Blood clots blocking blood vessels

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21
Q

Why is warfarin often used over more recently formed coagulants?

A

It is cheaper.

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22
Q

How man routes of administrate have U.S food and drug administration listed?

A

Over 100

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23
Q

What are the 2 main categories of drug administration.

A

Enteral

Parenteral

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24
Q

What is meant by enteral drug administration?

A

Via the digestive tract

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25
Q

What is meant by parenteral drug administration?

A

Not via the digestive tract

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26
Q

What is sublingual drug administration ?

A

Placing a drug under your tongue to be dissolved and absorbed into the blood stream.

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27
Q

What is transdermal drug administration?

A

Active ingredients delivered across the skin for systemic distribution.

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28
Q

What is topical drug administration?

A

Medication applied to a particular body surface.

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29
Q

Give the positives of oral drug administration.

A 
Convenient
Economical
Not painful
Portable
No specialised training or person required. 
Safe 
Can be removed from the body via vomiting. 
Variety of dosage forms  
No sterilisation needed
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30
Q

What are the negatives of oral drug administration.

A

Hard to take if lack of compliance.

Patient concordance needed.

variable absorption

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31
Q

What is patient concordance?

A

Consultation between a health care professional and a patient.

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32
Q

Define bioavailability.

A

The proportion of the drug in a dosage form that reaches the systemic circulation.

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33
Q

Why is the drug administered often reduced in dosage by the time it reaches the systemic circulation?

A

Degradation by the stomach and intestines.
May not be absorbed effectively.
Destroyed by the gut wall.
Destroyed by the liver.

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34
Q

What causes degradation of drugs by the stomach and intestines?

A

Bile, stomach acid, enzymes

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35
Q

What causes degradation of drugs by the gut wall and liver?

A

Enzymes

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36
Q

What vein carries drugs to the systemic circulation?

A

Hepatic vein

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37
Q

What artery carries blood away from the systemic circulation?

A

Hepatic artery

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38
Q

What circulation system do drugs travel in?

A

Systemic

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39
Q

Where is the majority of an administered drug absorbed?

A

Small intestine

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40
Q

What is first pass metabolism?

A

The liver and the gut wall sometimes extract and metabolise some drugs so efficiently that the amount reaching the systemic circulation is considerably less than the amount initially absorbed.

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41
Q

What is another name for First-pass metabolism?

A

Pre-systemic metabolism

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42
Q

Who created the first-pass metabolism method?

A

Rang and Dale

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43
Q

Name some drugs that do First-pass metabolism.

A 
Glyceryl Trinitrate
Levodopa
Morphine
Proporanolol
Salbutamol
Lidocaine
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44
Q

What is Glyceryl Trinitrate used to treat?

A

Angina

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45
Q

What is angina?

A

Chest pain due to insufficient blood (and therefore oxygen) supply to the heart muscles.

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46
Q

How is Glyceryl Trinitrate administered?

A

Sublingually

47
Q

What is the benefit of sublingual administration over oral administration?

A

Sublingual drugs are absorbed directly into the blood vessels so bypass the gut wall and liver. They therefore avoid first-pass metabolism and are less likely to be degraded by enzymes.

48
Q

What is levodopa used to treat?

A

Parkisons disease

49
Q

What is Parkisons disease?

A

Loss of functioning nerve cells in part of the brain leading to a reduction in dopamine release. Effects bodily movements.

50
Q

What is the main use of morphine?

A

To reduce pain

51
Q

What is the main use of Propranolol?

A

BEta blocker used to treat high blood pressure.

52
Q

What are beta blockers used to treat?

A

High blood pressure

53
Q

How do beta blockers work?

A

They reduce the effects of adrenaline and epinephrine, causing the heart to beat more slowly and with less force. Lowers blood pressure.

54
Q

What is Salbutamol used to treat?

A

Astha

55
Q

What is Lidocaine used to treat?

A

Used to numb tissues

56
Q

When is rectal administration helpful?

A

When nausea and vomiting is occurring - couldn’t keep oral medication in the body.

57
Q

What type of administrative drug method is used to treat haemorrhoids?

A

Rectal topical administration

58
Q

What is an intradermal injection?

A

Superficial injection into the skin.

59
Q

Wat is an intramuscular injection?

A

Injection into the muscles

60
Q

What are intramuscular injections often used for?

A

Depot injections

61
Q

What is a depot injection?

A

A slow release form of medication.

62
Q

What are the risks of intramuscular injections?

A

Hitting a vein

63
Q

What are the benefits of intramuscular injections?

A

Can inject alot of drug

64
Q

What are subcutaneous injections?

A

Between the skin and muscle

65
Q

What are the negatives of subcutaneous injections to administer drugs?

A

Can only administer a small amount

66
Q

What are intravenous injections?

A

Directly injecting into veins

67
Q

What are the benefits of intravenous drug administration?

A

No absorption needed so less drug is lost via metabolism.

Fast results

68
Q

What are intra-arterial drug injections often used for?

A

Targets drugs to specific organs by administering into the arteries that supply these organs.

69
Q

What are intraperitoneal injections?

A

Administered through the peritoneum which is a thin membrane that lines that abdominal cavity.

70
Q

When are intrapeitoneal injections often used?

A

When injecting animals.

For dialysis.

71
Q

What are intra-articular injections?

A

Injecting into a joint

72
Q

What is the primary aim of intra-articular injections to administer drugs?

A

To relive pain

73
Q

What are intra-articular injections often used to treat ?

A

Arthritis

74
Q

What are Intrathecal injections?

A

Injection into the spina cord

75
Q

What is an epidural injection?

A

Injection around the spinal cord.

76
Q

What are epidurals mainly used for ?

A

As anaesthetics to stop the feeling of pain.

77
Q

What are the 2 possible effects of inhaled administration?

A

Systemic

Topical

78
Q

Give examples of transdermal drug treatments.

A

Glyceryl Trinitrate - Transdermal patch for treating angina.

Selegille - transdermal antidepressant patch.

79
Q

What is Selegille used to treat?

A

Depression

80
Q

What are the benefits of drugs being administered topically?

A

Avoids systemic exposure

81
Q

What must happen for a drug to be absorbed?

A

It must be solubilized

82
Q

What are the main differences in drug absorption caused by?

A

First pass metabolism

83
Q

What are the 4 methods of dugs crossing through barriers/ membranes?

A
  1. Direct diffusion through the lipid bi-layer.
  2. Carrier- mediated transport.
  3. Diffusion through aqueous pores.
  4. Pinocytosis
84
Q

What type of drugs can diffuse through aqueous pores?

A

Extremely small

85
Q

What type of drugs cross membrane barriers by pinocytosis?

A

Large

86
Q

What are the main factors affecting rate of diffusion of drugs?

A

Surface area
Concentration gradient
Molecular Size
Lipid solubility

87
Q

What is pinocytosis?

A

A type of endocytosis.
The cell engulfs external substances and gathers them into a membrane-bound vesicle. The vesicle then invaginates (forms a pocked) and pinches off to form a vesicle in the cytoplasm.

88
Q

How does molecular size affect rate of diffusion?

A

The greater the molecular size, the lower the rate of diffusion

89
Q

How does lipid solubility affect rate of diffusion?

A

The greater the lipid solubility, the greater the rate of diffusion

90
Q

What is used to measure lipid solubility?

A

The partition coefficient

91
Q

What is the partition coefficient?

A

The ratio of the concentration of a drug in one phase solvent compared to another.

92
Q

How is partition coefficient calculated?

A

(Concentration of a drug in oil)/ (concentration of a drug in water)

93
Q

What does a high partition coefficient of a drug mean?

A

It has a high lipid solubility

94
Q

What does it mean if a drug has a low partition coefficient?

A

It has a low lipid solubility

95
Q

What type of molecules are able to diffuse simply through a lipid bi-layer?

A

Gases
Non-polar molecules
Some small polar molecules

96
Q

What type of molecules are unable to move through the phospholipid bilayer by simple diffusion?

A

Large polar molecules

Ions

97
Q

Define weak acids and bases.

A

They can only be partly ionised in aqueous solution.

98
Q

Define strong acids and bases.

A

They can be fully ionised in aqueous solutions.

99
Q

What affects the ionisation potential of weak acids and weak bases?

A

The pH of the surroundings.

100
Q

What form of a drug can be absorbed in terms of ionisation ?

A

Unionized can be absorbed

101
Q

How do ionised drugs react with water?

A

They attract water.

102
Q

What do weak acids dissociate into?

A

An anion and H

+

103
Q

What is a negatively charged ion called?

A

An anion

104
Q

What is a positively charged ion called?

A

A cation

105
Q

What affects the degree of dissociation of weak acids and bases?

A

pH of the surrounding solution.

106
Q

Is drug dissociation favoured in alkaline or acidic environments?

A

Greater dissociation occurs in basic alkaline environments.

107
Q

In what type of environment is dissociation of a drug less likely to occur?

A

In acidic conditions

108
Q

Is absorption of a drug more likely in basic or acidic conditions and why?

A

In acidic conditions. Because less dissociation occurs in acidic environments and therefore the drug will be absorbed in its unionised form.

109
Q

Is a drug likely to be ionised or unionised in the stomach ?

A

Ionised

110
Q

Is a drug likely to be ionised or unionised in the small intestine?

A

Unionised

111
Q

What type of chemical is morphine?

A

Weak base

112
Q

What type of chemical is aspirin?

A

Weak acidic

113
Q

When are weak acids less ionised and therefore more likely to be absorbed ?

A

Low pH

114
Q

When are weak bases less ionised and therefore more likely to be absorbed?

A

High pH

Principles Of Pharmacology (11 decks)

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