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3MB Transition Block > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Pharmacodynamics is…

A

What a drug does to the body

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2
Q

Pharmacokinetics is….

A

What the body does to a drug

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3
Q

Affinity is…

A

Strength of association between ligand and receptor

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4
Q

Efficacy is….

A

Ability of an agonist to evoke a cellular response

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5
Q

Antagonist is…

A

Drug that blocks the actions of an agonist

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6
Q

Agonist is…

A

Drug that binds to a receptor to produce a cellular response

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7
Q

Agonist possess ___________ while antagonist possess ________________ but lack _________

A

Affinity and efficacy
Affinity but lack efficacy

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8
Q

Competitive antagonism

A

Binding of agonist and antagonist occur at same (orthosteric) site

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9
Q

Competitive antagonism curve changes

A

Parallel rightward shift of agonist concentration response curve with no depression in maximal response

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10
Q

Non-competitive antagonism

A

Agonist binds to normal site and antagonist binds to separate (allosteric) site

Both may occupy sites simultaneously, but activation cannot occur when antagonist is bound

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11
Q

Non-competitive antagonism curve changes

A

Depress the slop and maximum response curve, but do not cause a rightward shift

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12
Q

Absorption is

A

Process by which a drug enters the body from its site of administration

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13
Q

Distribution is……

A

Process by which drug leaves circulation and enters the tissues perfused by blood

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14
Q

Metabolism is…..

A

Process by which tissue enzymes catalyse chemical conversion of a drug to a more polar form that is more readily excreted from the body

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15
Q

Excretion is…

A

Processes that remove the drug from the body

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16
Q

Factors Controlling Drug Absorption

A

Solubility
Chemical stability
Lipid to water partition coefficient
Degree of ionisation

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17
Q

T or F: Only ionised forms readily diffuse across the lipid bilayer

A

False → only unionised forms readily diffuse across the lipid bilayer

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18
Q

Volume of distribution (Vd) is….

A

Volume into which a drug appears to be distributed with a concentration equal to that of plasma

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19
Q

How is Vd calculated for IV preparation of drug

A

Vd = dose/plasma concentration

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20
Q

T or F: The higher the therapeutic ratio the safer the drug

A

True

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21
Q

How is Therapeutic Ratio calculated

A

Therapeutic Ratio = MTC/MEC

22
Q

Therapeutic Ratio is…..

A

Any concentration of drug between the minimum effective concentration (MEC) and maximum tolerated concentration (MTC)

23
Q

First order kinetics

A

Rate of elimination directly proportional to drug concentration → most drugs have this

24
Q

Clearance is….

A

The volume of plasma cleared of drug in unit time

25
Q

In first order kinetics, half-life is inversely proportional to _______________

A

Elimination rate constant

26
Q

How is Rate of elimination calculated

A

Rate of elimination = Clearance x Plasma concentration

27
Q

Half-life is

A

Time for the concentration of drug in plasma to halve

28
Q

Loading dose is…

A

Initial higher dose of drug before stepping down to lower maintenance dose

It accelerates the time at which a steady state can be reached and when plasma concentration becomes adequate

29
Q

Depolarisation

A

The membrane potential becomes less negative (or even positive)

30
Q

Hyperpolarisation

A

The membrane potential becomes more negative

31
Q

Sympathetic preganglionic neurones always _____ while post ganglionic neurone usually _______

A

ACh
Noradrenaline

32
Q

Sympathetic system has ____________ outflow

A

Thoraco-Lumbar (T1-L2)

33
Q

Effects of sympathetic system on the body

A

Increases HR and force of contraction

Relaxes bronchi, decreases mucus production

Reduces GI motility and constricts sphincters

Vasoconstriction but relaxation in skeletal muscle

Release of adrenaline from adrenal gland

Ejaculation

34
Q

Parasympathetic preganglionic neurones always _____ while post ganglionic neurone usually _____

A

ACh

35
Q

Parasympathetic system outflow from…

A

Cranial nerves III, VII, IX and X
Cranio-sacral outflow
Thoraco-lumbar outflow
Sacral spinal nerves

36
Q

Effects of parasympathetic system on the body

A

Decreases HR

Bronchoconstriction, stimulates mucus production

Increases GI motility and relaxes sphincters

No effect on blood vessels or adrenal glands

Erection

37
Q

Selective, competitive antagonist of a1
Vasodilator used as anti-hypertensive

Which drug?

A

Prazosin

38
Q

Selective, competitive antagonist of B1
Used as an anti-anginal and anti-hypertensive agent

Which drug?

A

Atenolol

39
Q

Selective agonist at B2
Used as bronchodilator in asthma

Which drug?

A

Salbutamol

40
Q

Competitive antagonist of Muscarinic ACh receptors, does not block nicotinic ACh receptors
Blocks parasympathetic division of ANS
Used to reverse bradycardia post MI and in AChE poisoning

Which drug?

A

Atropine

41
Q

What are the different G-protein coupled adrenoceptor subtypes and their functions at sympathetic neuroeffector junctions?

A

B1 – stimulates through Gs stimulating adenylyl cyclase increasing heart rate and force

B2 – stimulates through Gs stimulating adenylyl cyclase causing relaxation bronchial and vascular

a1 – stimulates through Gq stimulating phospholipase C causing contraction of vascular smooth muscle

a2 – stimulates through Gi stimulating inhibition of adenylyl cyclase causing inhibition of NA

42
Q

What are the individual roles of muscarinic receptors M1, M2 and M3?

A

M1 – signals to specific G-protein (Gq) which stimulates phospholipase C which causes increased acid secretion in the stomach.

M2 – signal to specific G-protein (Gi) which stimulates inhibition of adenylyl cyclase which opens K+ channel causing decreased heart rate.

M3 – signals to specific G-protein (Gq) which stimulates phospholipase C production which causes increased secretion of saliva or contraction of visceral smooth muscle.

42
Q

Which two receptors can ACh activate?

A

Nicotinic (ligand gated receptors)

Muscarinic (G-protein coupled receptors)

43
Q

Describe how G-proteins function

A

Signal Agonist binds to and activates receptor

G protein couples with receptor

Guanine nucleotide exchange (GDP dissociates and GTP binds to alpha subunit)

Subunit dissociation (G protein dissociates into alpha subunit and beta-gamma subunit)

G protein alpha subunit combines with and modifies activity of effector to bring about the desired signal

Agonist may dissociate from receptor at any time, but signaling will still occur

44
Q

Which is faster, ligand gated ion channels or G-protein coupled?

A

Ligand gated channels

45
Q

Zero order kinetics

A

Drugs that are eliminated at a constant rate, regardless of their concentration

An increase in drug concentration will have no effect on the rate of elimination

46
Q

How many half lives does it take to reach a steady state?

A

5

47
Q

How is steady state calculated

A

Maintenance dose rate/clearance

48
Q

Phase 1 metabolism of drugs causes change in drug via…..

A

Oxidation, reduction or hydrolysis

49
Q

Phase 2 metabolism of drugs causes change in drug via…..

A

Conjugation of drug with a polar molecule to form a water-soluble metabolite

49
Q

Conjugated product is readily excreted via the __________ in phase 2 metabolism

A

Kidneys

3MB Transition Block (10 decks)

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