pharmacology Flashcards

1
Q

what is a drug

A

this is a chemical that is used to prevent , diagnose, treat or cure pathological issues.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

drug action

A

drug binding onto a molecule.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

drug affinity

A

ability of a drug to bind onto a receptor and elicit a response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

efficacy

A

ability of a drug to cause a response after binding onto a receptor.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

factors that pharmacological effect depend on

A

affinity
efficacy
residence time

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what is meant by residence time

A

total time spent by the drug on the receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

factors that can influence receptor response

A

1.polymorphic variation - different people have different genes that code for the receptor proteins .
2.age -older people less receptors that are expressed.
3.disease
4.drug treatment for example clonidine is a drug for hypertension and addition of this molecule is seen as not balancing in homeostasis.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

agonist receptors

A

they bind to the receptor and they cause a response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

antagonists ligand

A

bind to the receptor and causes no activation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

competitive ligand

A

competes with the other ligands for site for binding while the non - competitive changes the shape of the binding site.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

pharmacodynamics

A

effects of the drug on a specific site

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

what is meant by pharmacokinetics

A

what the body does to the drug that is ADME

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Biophase

A

the effect site of the drug (the physical region in which the
drug target is located)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

bioavailability

A

this is the extent and rate at which the drug reaches its site of action

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

how is bioavailability measured

A

measured by injecting the drug in the systemic circulation through IV administration.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

best routes of administration

A

IV
SC/IM
PR/PO

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

what is meant by half life of a drug

A

that is the time it takes to reach half it concentration in the blood.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

methods of drug lost

A

through barriers that is why IV route is usually the best option .

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

bioavailability and the mode of administration

A

IV has the highest bioavailability because there is no loss of the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

what is the benefit of a half life

A

adjustment of a dose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

concentration max interpretation

A

too low means there is no therapeutic effect while too high means toxicity.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

what is meant by therapeutic index

A

this is the ratio of the the dose that causes therapeutic effect to the dose that causes toxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

narrow therapeutic index

A

prescription with care

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

very large therapeutic effect

A

not so many problems

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

movement of the drug from the plasma

A

-plasma to interstitial fluid
then to intracellular fluid which has to cross the cell membrane .
-sometimes has to cross other fluids such as CSF, peritoneal , humours etc.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

movement of plasma to interstitial fluid

A

filtration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

paracellular movement

A

filtration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

transcellular movement

A

from the interstitial fluid to the intracellular

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

types of barriers to be crossed during drug penetration

A

passage through the basement membrane to the epithelial cell

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

types of movement that occur

A

movement by diffusion
facilitated diffusion
active transport

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

factors that affect movement of drugs into the cell

A

1.lipophilicity
2.ionisation
3.blood supply and perfusion.
4.size of a drug
5.existence of some transport mechanism.
6.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

elimination of a drug

A

this refers to metabolism and excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

body`s mechanism of preventing the exposure to alien molecules.

A

1.blood brain barrier
2.physical removal of a drug through urine, blood , sweat and breath.
3.characteristics that promote entry limit exit such as size , lipophilic or not etc.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

metabolism are easily excreted than parent

A

metabolites render the drug more polar

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

phases of metabolism of drug

A

Phase I (functionalisation); Phase II (synthetic)

36
Q

organ for drug metabolism

A

liver

37
Q

what is metabolism of a drug

A

breaking the drug to a form that can easily be eliminated by the body .

38
Q

examples for enzymes that are used to metabolise the drugs

A

cytochrome 450

39
Q

what are the main routes of administration of a drug

A

Intravenous: not absorbed
* Oral (most common)
* Subcutaneous
* Intramuscular
* Other GI (rectal, sublingual)
* Nasal
* Inhalation
* Transdermal

40
Q

what is absorption of a drug

A

this is the process of mass transfer from site of administration to bloodstream

41
Q

factors that affect the process of absorption of a drug

A

1.physio-chemical properties ( eg polarity , size, charge etc)
2.bioavailability
3.physiological factors.
4.anatomical factors.

42
Q

topical administration of a drug

A

-Topical “of a place”
-Skin, mucous membranes, ears, eyes.

43
Q

reason for topical administration of a drug

A

1.Adverse events: Excess effect at site of action… but can be “off-target”
2. Aim: to reduce exposure beyond site of action

44
Q

rationale of local anaesthetics

A

they cause the blockage of potassium ion channels.

45
Q

factors to consider before administering local anaesthetics

A

1.dosing which depends on :
patient factors eg children , elderly and pregnant women.
2.inject only in superficial not deep.
3.co administer with adrenaline
4.avoid highly vascularised tissue

46
Q

routes for absorption

A

1.Enteral (oral; sublingual; rectal).
2. Parenteral (SC; IM; pulmonary? Nasal?)… IV.
3. Oral: Most common, most desirable.

47
Q

why oral administration

A

1.cheapest
2.easiest and doesn`t require equipment.
3.higher compliance that is it is non invasive.

48
Q

factors affecting oral absorption

A

1.solubilty ; some drugs are affected by gut contents( tetracycline)
2.gastric emptying time this will affect the time required for the drug to reach the SI for metabolism.
3.pH change in the gut leading to ionisation and less ability to move into the cell.
4.gut flora
5.lung phase 1 and liver phase 2
illness

49
Q

which drugs can be affected by gut contents

A

tetracyclines

50
Q

crossing barriers for for drugs

A

paracellular
transcellular

51
Q

fick`s first law application

A

1.Diffusion coefficient
2* (Size etc)
3* Partition coefficient
4* Thickness of membrane
5* Total membrane area
6* Driving force is the drug
concentration
7* ‘Sink’ condition

52
Q

first order kinetics

A

-for diffusion of drugs into the cell membrane.
the rate of absorption is directly proportional to the rate of concentration of the drug.

53
Q

door theory

A

facilitated diffusion for bigger sized molecules

54
Q

molecules used for facilitated transport

A

-Channel proteins: molecules of
appropriate size and charge.
-Carrier proteins.

55
Q

curve for the facilitated diffusion

A

there is saturation whereby even the increase in the concentration will not lead to an increase in the rate of absorption.

56
Q

tissues where there are barriers for distribution

A

brain
testes
ovary
placenta

57
Q

how are the drugs distributed in the body

A

1.they bind onto the plasma protein and are transported through that .
2.they also bind on lipoproteins .
3.also bind on glycoproteins.

58
Q

what is the volume of distribution

A

this is a proportionality constant between a total amount of drug in the body and the amount in the plasma at any one time.

59
Q

importance of volume of distribution

A

1.drugs with a low volume of distribution remain in the plasma
drugs
2. high volume of distribution tend to leave plasma ie there is more distribution.

60
Q

how does volume of distribution influence plasma

A

1.the drug is cleared form the plasma and redistributed from other tissues.
2.because of this the plasma volume declines slowly .
drugs with high volume of distribution have a longer elimination half life.

61
Q

what is a steady state of a drug

A

the rate of drug administration is equal to the rate of drug elimination.

62
Q

what happens if a half life is long

A

there is a maintenance dose that is added.

63
Q

factors affecting the choice administration

A
  • Oral route – much is about cost, convenience, acceptability etc
  • Drawbacks: first pass metabolism; factors that affect absorption
  • IV – speed; criticality of Cp
  • Drawbacks: 100% bioavailability means rapidly perfused
    compartments get rapid exposure; needs to be aqueous solution;
    acceptability
  • IM – usually safer than IV; rapid absorption of aqueous drugs
  • Drawbacks: Painful; clots, abscesses etc; dependence on blood flow
  • SC – Similar to IM, but less painful etc
  • Drawbacks: Irritation; impact on local tissue
64
Q

inhaled medications

A

metabolism or absorption in the lung
oral bioavailability

65
Q

manipulation of the dosage form

A

LADME ; liberation and absorption

66
Q

reason why there is no absorption of drugs in the oral cavity

A

because there is limited contact in the mouth so although the mouth is highly vascularised there is less absorption.

67
Q

absorption of drugs

A

absorption of drugs mainly takes place in the small intestines.

68
Q

how does gastric emptying affect the absorption of a drug

A

time taken for the drug to reach the main absorption site that is the small intestine.

69
Q

factors that affect the rate of gastric emptying

A

food for example fatty food slows down gastric emptying.

70
Q

how does food affect the extent of absorption

A

Food may enhance the extent of absorption for poorly soluble drugs (eg, griseofulvin), reduce it for drugs degraded in the stomach (eg, penicillin G), or have little or no effect.

71
Q

reason why most absorption is in the small intestine

A

In the GI tract, the small intestine has the largest surface area for drug absorption, and its membranes are more permeable than those in the stomach

72
Q

pH affects absorption

A

Certain pH promote ionisation of drug and this leads to changes in the solubility of the drug.

73
Q

blood flow and absorption

A

Decreased blood flow (eg, in shock) may lower the concentration gradient across the intestinal mucosa and reduce absorption by passive diffusion.

74
Q

Gut bacteria and absorption of drugs

A

GI microflora may reduce absorption.

75
Q

absorption of drugs that have been administered through the lymphatic system

A

If protein drugs with a molecular mass > 20,000 g/mol are injected IM or sc, movement across capillary membranes is so slow that most absorption occurs via the lymphatic system. In such cases, drug delivery to systemic circulation is slow and often incomplete because of first-pass metabolism (metabolism of a drug before it reaches systemic circulation) by proteolytic enzymes in the lymphatics.

76
Q

a drug that is bound to a protein is inactivee

A

yes

77
Q

a drug with a high volume of distribution

A

there is a high concentration of drugs that is in circulation and that means there is less drug concentration in the plasma .

78
Q

half life for volume of distribution

A
  • Half-life = 0.693 x (Vd
    /Clearance)
79
Q

what is the significance of volume of distribution

A

dosing that is to understand how fast or slow a drug is retained in the blood system.

80
Q

what is meant by loading dose

A

this is the dose that is initially put into the system .

81
Q

calculation of loading dose

A

volume of distribution by concentration of the drug in the plasma

82
Q

when is steady state achieved

A

after approximately 4 half lives

83
Q

what is drug metabolism

A

process of converting medication into a less or more active form

84
Q

reason for metabolism

A

create metabolites that can be excreted.

85
Q
A