Pharmacology Flashcards

1
Q

Pharmacology

A

What a drug does to the body

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2
Q

Pharmacokinetics

A

What the body does to a drug

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3
Q

Ligand

A

A substance that is bound to a protein

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4
Q

Drug

A

Any single synthetic or natural substance of known structure used in the treatment, prevention or diagnosis of disease

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5
Q

Medicine

A

Chemical preparation containing one or more drugs

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6
Q

Selectivity

A

The ability of a drug to distinguish between different molecular targets within the body

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7
Q

Agonist

A

Drug that binds to a receptor to produce a cellular response

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8
Q

Affinity

A

Strength of association between ligand and receptor

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9
Q

Efficacy

A

Ability of an agonist to evoke a cellular response

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10
Q

Partial agonist

A

An agonist that in a given tissue, under specified conditions, cannot elicit as large an effect as can another agonist acting through the same receptors in the same tissue

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11
Q

Antagonist

A

drug that reduces, or blocks, the actions of an agonist by binding to the same receptor - do not activate them (possess affinity but lack efficiacy)

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12
Q

Potency

A

Amount of drug required to produce a desired effect

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13
Q

EC50

A

Concentration of agonist that elicits half maximal effect

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14
Q

Competitive Antagonism

A

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

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15
Q

Non competitive antagonism

A

Agonist binds to normal site and antagonist binds to seperate (allosteric) site. Both may occupy sites simultaneously

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16
Q

Drug metabolism

A

Enzyme conversion of the drug to another chemical entity

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17
Q

Where do phase I and II of metabolic metabolism take place

A

The Liver

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18
Q

What does metabolism in the liver reduce

A

Bioavailability of drugs when administered orally

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19
Q

What is bioavailability (F)

A

The amount of drug that eventually reaches systematic circulation of an administered dose of the drug

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20
Q

Where are hepatic drug metabolizing enzymes embedded

A

SER of the hepatocytes

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21
Q

Phase I metabolism

A

Change in the drug by oxidation, reduction or hydrolysis

22
Q

What is oxidation

A

Drug molecule incorporates an atom of oxygen to form a hydroxyl group

23
Q

WHat enzyme is oxidation accomplished by

A

Cytochrome P450 enzymes

24
Q

What can cytoplasmic enzymes do

A

Metabolise drugs

25
Phase II metabolism
Involve the combination of the drug with one of several polar molecules to form a water-soluble metabolite conjugation
26
True/False : some drugs (e.g. codeine) can go directly to phase II metabolism
True
27
Absorption
Drug is absorbed from site of administration, entry into the plasma
28
Distribution
Drug leaves bloodstream and is distributed into interstitial and intracellular fluid
29
Metabolism
Drug transformation by metabolism-liver and other tissues
30
Excretion
Drug excreted in urine, faeces or bile
31
Different ways for movement of drugs across cell barriers
Passive diffusion, facilitated diffusion, active transport, endocytosis, pH and ionisation, pH trapping
32
Passive diffusion
Directly through the lipid (drugs with high lipid solubility)
33
Facilitated diffusion
*does not require energy *movement is down a concentration gradient *water-soluble drugs
34
Active transport
*requires energy *can move molecules against concentration gradient *water-soluble drugs
35
Endocytosis
*invagination of part of the membrane *drug is encased in a small vesicle, then released inside the cell *transport of large drugs across cell membrane
36
what form of drugs readily diffuse across the lipid bilayer (ionised or unionised)
unionised
37
What is clearance
An expression of the elimination of a drug from the body (the volume of blood removed of a drug per unit time)
38
What can clearance be broken down into
Renal (CLR) Hepatic (CLH) Other (CHO)
39
Does drug elimination initially increase or decrease as drug plasma concentration increases
increases
40
when does steady state (SS) exist
when rate of drug administration (R0) = rate of elimination (RE)
41
calculation for dosage rate required to maintain steady state
=drug plasma X CL
42
Elimination half life (t1/2) =
(0.693 x Vd)/CL
43
What does elimination half life determine
The time required to reach SS and also time required for drug to be removed from the body
44
What are reflexes
negative feedback loops within the PNS and CNS
45
What is the Autonomic nervous system (in the PNS) divided into
Eteric (ENS) sympathetic and parasympathetic
46
Tell me about sympathetic ANS
Flight or Flight Preganglionic neurons originate in the thoracolumbar region
47
Tell me about parasympathetic ANS
Rest and Digest Preganglionic neurons originate in the craniosacral region
48
What is the transmitter for sympathetic preganglionic neurons
acetylcholine
49
What is the transmitter for sympathetic postganglionic neurons
noradrenaline
50
What is the transmitter for parasympathetic preganglionic neurons
acetylcholine
51
What is the transmitter for parasympathetic postganglionic neurons
acetylcholine
52
Are acetylcholine and noradrenaline the only transmitters released from the sympathetic and parasympathetic
no