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
Q

Phase II metabolism

A

Involve the combination of the drug with one of several polar molecules to form a water-soluble metabolite conjugation

26
Q

True/False : some drugs (e.g. codeine) can go directly to phase II metabolism

A

True

27
Q

Absorption

A

Drug is absorbed from site of administration, entry into the plasma

28
Q

Distribution

A

Drug leaves bloodstream and is distributed into interstitial and intracellular fluid

29
Q

Metabolism

A

Drug transformation by metabolism-liver and other tissues

30
Q

Excretion

A

Drug excreted in urine, faeces or bile

31
Q

Different ways for movement of drugs across cell barriers

A

Passive diffusion, facilitated diffusion, active transport, endocytosis, pH and ionisation, pH trapping

32
Q

Passive diffusion

A

Directly through the lipid (drugs with high lipid solubility)

33
Q

Facilitated diffusion

A

*does not require energy
*movement is down a concentration gradient
*water-soluble drugs

34
Q

Active transport

A

*requires energy
*can move molecules against concentration gradient
*water-soluble drugs

35
Q

Endocytosis

A

*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
Q

what form of drugs readily diffuse across the lipid bilayer (ionised or unionised)

A

unionised

37
Q

What is clearance

A

An expression of the elimination of a drug from the body (the volume of blood removed of a drug per unit time)

38
Q

What can clearance be broken down into

A

Renal (CLR)
Hepatic (CLH)
Other (CHO)

39
Q

Does drug elimination initially increase or decrease as drug plasma concentration increases

A

increases

40
Q

when does steady state (SS) exist

A

when rate of drug administration (R0) = rate of elimination (RE)

41
Q

calculation for dosage rate required to maintain steady state

A

=drug plasma X CL

42
Q

Elimination half life (t1/2) =

A

(0.693 x Vd)/CL

43
Q

What does elimination half life determine

A

The time required to reach SS and also time required for drug to be removed from the body

44
Q

What are reflexes

A

negative feedback loops within the PNS and CNS

45
Q

What is the Autonomic nervous system (in the PNS) divided into

A

Eteric (ENS) sympathetic and parasympathetic

46
Q

Tell me about sympathetic ANS

A

Flight or Flight

Preganglionic neurons originate in the thoracolumbar region

47
Q

Tell me about parasympathetic ANS

A

Rest and Digest

Preganglionic neurons originate in the craniosacral region

48
Q

What is the transmitter for sympathetic preganglionic neurons

A

acetylcholine

49
Q

What is the transmitter for sympathetic postganglionic neurons

A

noradrenaline

50
Q

What is the transmitter for parasympathetic preganglionic neurons

A

acetylcholine

51
Q

What is the transmitter for parasympathetic postganglionic neurons

A

acetylcholine

52
Q

Are acetylcholine and noradrenaline the only transmitters released from the sympathetic and parasympathetic

A

no