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Pharmacology > Principles > Flashcards

Principles Flashcards

0
Q

Define pharmacokinetics

A

What the body does to the drug (absorption, distribution, metabolism, and excretion)

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1
Q

Define pharmacodynamics

A

What a drug does to the body and how it does it (biological effects and mechanism of action)

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2
Q

Define the term agonist

A

A drug that binds to a receptor to produce a cellular response

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3
Q

Define the term antagonist

A

A drug that blocks the actions of an agonist and normal body chemical

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4
Q

Define affinity

A

The strength of association between ligand and receptor

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5
Q

Define efficacy

A

The ability of an agonist to evoke a cellular response

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6
Q

Define EC50

A

The concentration of agonist that elicits a half maximal response

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7
Q

Define potency

A

The most potent is the drug that produces a response at the lowest concentration

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8
Q

Define orthosteric

A

The primary binding site of a ligand

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9
Q

Define allosteric

A

When an antagonist binds to the receptor not at the active site preventing activation

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10
Q

Define pKa

A

The pH at which 50% of the drug is ionised and 50% is unionised.

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11
Q

What are the 5 factors affecting GI absorption.

A 
GI motility 
pH at the absorption site
Blood flow to stomach and intestines
The way in which the table is manufactured 
Physicochemical interactions
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12
Q

Define GI motility

A

The rate of stomach emptying and movement through the intestines

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13
Q

Why does the way the tablet/capsule is manufactured affect absorption?

A

They can be customised to release drugs at different rates and sites

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14
Q

Define systemic availability

A

The % of drug absorbed into systemic circulation -
IV = 100%
Oral has to go through first-pass metabolism

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15
Q

Define the term efferent signals

A

Signals going away from the CNS

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16
Q

Define the term afferent signals

A

Signals moving towards the CNS

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17
Q

What is the ANS responsible for?

A

Carrying output from the CNS to the whole body apart from skeletal muscles

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18
Q

What does the sympathetic ANS do?

A

Responsible for body’s response to stress. Fight or flight?

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19
Q

What does parasympathetic ANS do?

A

Coordinates the body’s basic homeostatic functions

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20
Q

What is the transmitter in the preganglionic neurones?

A

Acetylcholine

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21
Q

What is the usual transmitter in postganglionic neurones in the sympathetic division?

A

Noradrenaline

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22
Q

What is the transmitter in postganglionic neurones of the parasympathetic system?

A

Acetylcholine

23
Q

What are cholinergic neurones?

A

Neurones that use acetylcholine as the transmitter

24
Q

Are postganglionic neurones longer in sympathetic or parasympathetic system?

A

Sympathetic

25
Q

Which ganglionic synapse used noradrenaline opposed to acetylcholine?

A

Sympathetic Postganglionic neuron

26
Q

What are the postganglionic receptors of the sympathetic nervous system?

A

Adrenoceptors

27
Q

What are the postganglionic receptors of parasympathetic nervous system?

A

G-protein Muscarinic acetylcholine

28
Q

Where do M1 muscarinic ACh receptors act and what G protein couples with it?

A

M1 couples with Gq in the stomach to stimulate phospholipase C which causes increased acid secretion.

29
Q

What G protein couples with M2 muscarinic receptors (parasympathetic) and what effect does this have?

A

Gi couples with M2 muscarinic ACh receptors in the heart resulting in inhibition of andeylyl Cyclase, opening K+ channels causing decreased heart rate (vagus nerve)

30
Q

What G protein couples with M3 muscarinic receptors (parasympathetic) and what effect does this have?

A

Gq couples with M3 muscarinic ACh receptors resulting in stimulation of phospholipase C causing increased secretion of saliva in the mouth

31
Q

Which muscarinic ACh receptor (parasympathetic) doesn’t couple with Gq

A

M2 - it couples with Gi in the heart

32
Q

Which G protein couples with beta 1 and 2 sympathetic adrenoceptors at the neuroeffector junction?

A

Gs

33
Q

Which G protein does sympathetic adrenoceptor beta 1 couple with at the neuroeffector junction and what does this cause?

A

Gs causing stimulation of adenylyl Cyclase resulting in increased rate and force of the heart

34
Q

Which G protein does sympathetic adrenoceptor beta 2 couple with at the neuroeffector junction and what does this cause?

A

Gs causing stimulation of adenylyl Cyclase resulting in relaxation of the bronchial and vascular smooth muscle

35
Q

Which G protein does sympathetic adrenoceptor alpha 1 couple with at the neuroeffector junction and what does this cause?

A

Gq causing stimulation of phospholipase C resulting in contraction of vascular smooth muscle

36
Q

Which G protein does sympathetic adrenoceptor alpha 2 couple with at the neuroeffector junction and what does this cause?

A

Gi causing inhibition of adenylyl Cyclase resulting in inhibition of NA release

37
Q

Does the sympathetic or parasympathetic nervous system cause contraction and relaxation of the vascular smooth muscle?

A

Sympathetic - beta 2 receptor caused relaxation

Alpha 1 causes contraction

38
Q

What do Gs, Gq and Gi proteins do?

A

Gs stimulates adenylyl Cyclase
Gq stimulates phospholipase C
Gi inhibits adenylyl Cyclase

39
Q

What action does cocaine have on the sympathetic post-ganglionic neurone

A

Blocks U1 preventing re-uptake of NA into post-ganglionic neurone resulting in large amounts of NA in the synapse increasing adrenoceptor stimulation :(i.e. Increased vasoconstriction and increased heart rate)

40
Q

What effect do amphetamines have on the sympathetic post-ganglionic neurone?

A

Enters post-ganglionic neurone via U1 and blocks the NA degradation MAO enzyme preventing NA breakdown. It then causes U1 to run backwards and NA goes in a loop, leaving the cell at U1 as well as entering it resulting in a build up of NA in the synapse and increased adrenoceptor stimulation
(i.e. Increased vasoconstriction and heart rate)

41
Q

What do prazosin, atenolol and salbutamol act on and do?

A

Prazosin - alpha 1 antagonist
Atenolol - beta 1 antagonsit
Salbutamol - beta 2 agonist

42
Q

What effect does atropine have on the parasympathetic post-ganglionic neurone?

A

It blocks muscarinic ACh receptors preventing release of adenylyl Cyclase from M2 therefore causing an increase in heart rate. Therefore used to reverse bradycardia.

43
Q

What is the therapeutic ratio and how is it calculated?

A

The window between minimum and maximum concentrations of drugs in which they are effective
Calculated by maximum tolerated dose divided by minimum effective concentration

44
Q

What are first order kinetics?

A

Rate of elimination is directly proportional to the drug concentration (half life)

45
Q

What are zero order kinetics?

A

When a drug is eliminated at a constant rate rather than a half life.
I.e. Ethanol - lose a set volume per hour regardless of concentration

46
Q

Define membrane difference

A

The difference in potential (charge) between the inside and the outside of the cell

47
Q

Define depolarization

A

When the membrane potential becomes less negative (or more positive)

48
Q

Define hyperpolarization

A

When the membrane potential becomes more negative

49
Q

What charge is the inside of a cell usually?

A

Negative

50
Q

What is the normal membrane potential for neurones?

A

-80mV

51
Q

What happens to K+ and Na+ to cause a change in membrane potential?

A

K+ leaves the cell

Na+ enters the cell

52
Q

Define ENa and what is it’s value?

A

The membrane potential at which Na enters and leaves the cell at the same rate (equilibrium). This is +60mV

53
Q

Define EK and what is it’s value?

A

The membrane potential at which K enters and leaves the cell at the same rate (equilibrium). This is -100mV

54
Q

What type of channels are responsible for Na+ and K+ movement?

A

Voltage-activated Na+/K+ channels

55
Q

What are action potentials?

A

Brief electrical signals in which the polarity of the nerve cell membrane is reversed (goes from negative to positive)

56
Q

What is the refractory period?

A

A period in which no stimulus can elicit a second action potential as the voltage-activated Na+ channels are inactivated

Pharmacology (10 decks)

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