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Principles Of Pharmacology > Week 2 > Flashcards

Week 2 Flashcards

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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
What is meant by parenteral drug administration?
Not via the digestive tract
26
What is sublingual drug administration ?
Placing a drug under your tongue to be dissolved and absorbed into the blood stream.
27
What is transdermal drug administration?
Active ingredients delivered across the skin for systemic distribution.
28
What is topical drug administration?
Medication applied to a particular body surface.
29
Give the positives of oral drug administration.
``` 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 ```
30
What are the negatives of oral drug administration.
Hard to take if lack of compliance. Patient concordance needed. variable absorption
31
What is patient concordance?
Consultation between a health care professional and a patient.
32
Define bioavailability.
The proportion of the drug in a dosage form that reaches the systemic circulation.
33
Why is the drug administered often reduced in dosage by the time it reaches the systemic circulation?
Degradation by the stomach and intestines. May not be absorbed effectively. Destroyed by the gut wall. Destroyed by the liver.
34
What causes degradation of drugs by the stomach and intestines?
Bile, stomach acid, enzymes
35
What causes degradation of drugs by the gut wall and liver?
Enzymes
36
What vein carries drugs to the systemic circulation?
Hepatic vein
37
What artery carries blood away from the systemic circulation?
Hepatic artery
38
What circulation system do drugs travel in?
Systemic
39
Where is the majority of an administered drug absorbed?
Small intestine
40
What is first pass metabolism?
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.
41
What is another name for First-pass metabolism?
Pre-systemic metabolism
42
Who created the first-pass metabolism method?
Rang and Dale
43
Name some drugs that do First-pass metabolism.
``` Glyceryl Trinitrate Levodopa Morphine Proporanolol Salbutamol Lidocaine ```
44
What is Glyceryl Trinitrate used to treat?
Angina
45
What is angina?
Chest pain due to insufficient blood (and therefore oxygen) supply to the heart muscles.
46
How is Glyceryl Trinitrate administered?
Sublingually
47
What is the benefit of sublingual administration over oral administration?
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
What is levodopa used to treat?
Parkisons disease
49
What is Parkisons disease?
Loss of functioning nerve cells in part of the brain leading to a reduction in dopamine release. Effects bodily movements.
50
What is the main use of morphine?
To reduce pain
51
What is the main use of Propranolol?
BEta blocker used to treat high blood pressure.
52
What are beta blockers used to treat?
High blood pressure
53
How do beta blockers work?
They reduce the effects of adrenaline and epinephrine, causing the heart to beat more slowly and with less force. Lowers blood pressure.
54
What is Salbutamol used to treat?
Astha
55
What is Lidocaine used to treat?
Used to numb tissues
56
When is rectal administration helpful?
When nausea and vomiting is occurring - couldn't keep oral medication in the body.
57
What type of administrative drug method is used to treat haemorrhoids?
Rectal topical administration
58
What is an intradermal injection?
Superficial injection into the skin.
59
Wat is an intramuscular injection?
Injection into the muscles
60
What are intramuscular injections often used for?
Depot injections
61
What is a depot injection?
A slow release form of medication.
62
What are the risks of intramuscular injections?
Hitting a vein
63
What are the benefits of intramuscular injections?
Can inject alot of drug
64
What are subcutaneous injections?
Between the skin and muscle
65
What are the negatives of subcutaneous injections to administer drugs?
Can only administer a small amount
66
What are intravenous injections?
Directly injecting into veins
67
What are the benefits of intravenous drug administration?
No absorption needed so less drug is lost via metabolism. | Fast results
68
What are intra-arterial drug injections often used for?
Targets drugs to specific organs by administering into the arteries that supply these organs.
69
What are intraperitoneal injections?
Administered through the peritoneum which is a thin membrane that lines that abdominal cavity.
70
When are intrapeitoneal injections often used?
When injecting animals. | For dialysis.
71
What are intra-articular injections?
Injecting into a joint
72
What is the primary aim of intra-articular injections to administer drugs?
To relive pain
73
What are intra-articular injections often used to treat ?
Arthritis
74
What are Intrathecal injections?
Injection into the spina cord
75
What is an epidural injection?
Injection around the spinal cord.
76
What are epidurals mainly used for ?
As anaesthetics to stop the feeling of pain.
77
What are the 2 possible effects of inhaled administration?
Systemic | Topical
78
Give examples of transdermal drug treatments.
Glyceryl Trinitrate - Transdermal patch for treating angina. Selegille - transdermal antidepressant patch.
79
What is Selegille used to treat?
Depression
80
What are the benefits of drugs being administered topically?
Avoids systemic exposure
81
What must happen for a drug to be absorbed?
It must be solubilized
82
What are the main differences in drug absorption caused by?
First pass metabolism
83
What are the 4 methods of dugs crossing through barriers/ membranes?
1. Direct diffusion through the lipid bi-layer. 2. Carrier- mediated transport. 3. Diffusion through aqueous pores. 4. Pinocytosis
84
What type of drugs can diffuse through aqueous pores?
Extremely small
85
What type of drugs cross membrane barriers by pinocytosis?
Large
86
What are the main factors affecting rate of diffusion of drugs?
Surface area Concentration gradient Molecular Size Lipid solubility
87
What is pinocytosis?
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
How does molecular size affect rate of diffusion?
The greater the molecular size, the lower the rate of diffusion
89
How does lipid solubility affect rate of diffusion?
The greater the lipid solubility, the greater the rate of diffusion
90
What is used to measure lipid solubility?
The partition coefficient
91
What is the partition coefficient?
The ratio of the concentration of a drug in one phase solvent compared to another.
92
How is partition coefficient calculated?
(Concentration of a drug in oil)/ (concentration of a drug in water)
93
What does a high partition coefficient of a drug mean?
It has a high lipid solubility
94
What does it mean if a drug has a low partition coefficient?
It has a low lipid solubility
95
What type of molecules are able to diffuse simply through a lipid bi-layer?
Gases Non-polar molecules Some small polar molecules
96
What type of molecules are unable to move through the phospholipid bilayer by simple diffusion?
Large polar molecules | Ions
97
Define weak acids and bases.
They can only be partly ionised in aqueous solution.
98
Define strong acids and bases.
They can be fully ionised in aqueous solutions.
99
What affects the ionisation potential of weak acids and weak bases?
The pH of the surroundings.
100
What form of a drug can be absorbed in terms of ionisation ?
Unionized can be absorbed
101
How do ionised drugs react with water?
They attract water.
102
What do weak acids dissociate into?
An anion and H | +
103
What is a negatively charged ion called?
An anion
104
What is a positively charged ion called?
A cation
105
What affects the degree of dissociation of weak acids and bases?
pH of the surrounding solution.
106
Is drug dissociation favoured in alkaline or acidic environments?
Greater dissociation occurs in basic alkaline environments.
107
In what type of environment is dissociation of a drug less likely to occur?
In acidic conditions
108
Is absorption of a drug more likely in basic or acidic conditions and why?
In acidic conditions. Because less dissociation occurs in acidic environments and therefore the drug will be absorbed in its unionised form.
109
Is a drug likely to be ionised or unionised in the stomach ?
Ionised
110
Is a drug likely to be ionised or unionised in the small intestine?
Unionised
111
What type of chemical is morphine?
Weak base
112
What type of chemical is aspirin?
Weak acidic
113
When are weak acids less ionised and therefore more likely to be absorbed ?
Low pH
114
When are weak bases less ionised and therefore more likely to be absorbed?
High pH

Principles Of Pharmacology (11 decks)

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