B7 Flashcards

1
Q

metabolism

A

how drugs are transformed in body

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2
Q

excretion

A

elimination of substances

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3
Q

how is a drug metabolised

A

parent drug is converted to their inactive, polar metabolites which decrease their effect on the body

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4
Q

prodrugs

A

metabolites are more active than parent compounds

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5
Q

metabolism can lead to production of

A
inactive metabolites
active metabolites
metabolites with increased potency
metabolites with decreased potency
toxic metabolites
metabolites with different pharma actions
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6
Q

factors influencing metabolism

A
diet
disease
hormonal status
age
genetics
liver function
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7
Q

phase I reaction

A

non synthetic

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8
Q

phase II reaction

A

synthetic

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9
Q

principles of phase I

A
enzyme catalysed
no conjugation
oxidations
reductions
hydrolysis
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10
Q

principles of phase II

A

enzyme catalysed conjugation

reaction of a drug with an endogenous substance

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11
Q

what does phase II reaction require

A

energy and a functional group from phase I as the site of conjugation

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12
Q

glucuronyl tranferase

A

phase II enzymes that catalyse conjugation of glucuronic acid

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13
Q

what happens in metabolites arent removed

A

they accumulate and can have toxic effects

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14
Q

routes of elimination

A
urine
sweat
faeces
milk
lungs
saliva
tears
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15
Q

net renal excretion

A

glomerular filtration at the glomerulus + tubular secretion at the prox tubule - tubular resorption throughout the tubule

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16
Q

filtration is affected by

A

plasma protein binding

17
Q

reabsorption is affected by

A

lipid solubility
conc gradient
urinary ph

18
Q

renal clearance

A

CL = conc of drug per ml of urine x (volume or urine excreted per minute / conc of drug per ml plasma)

19
Q

total body clearance

A

renal clearance + metabolism

20
Q

factors influencing renal clearance

A
age
other drugs
diseases
renal failure
Ti
21
Q

hepatic extraction ratio

A

amount of drugs removed in liver/ amount of drug entering organ

22
Q

first pass effect

A

decreases concentration

a drug with a hepatic extraction ratio of 1 will have 0% bioavailability