elementary drug metabolism Flashcards

1
Q

drug metabolism

A

enzymatic conversion of the drug to another chemical entity

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2
Q

what is the msot important drug metabolising organ

A

liver

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3
Q

what other organs also ocntribute

A

kidney gut mucosa and lungs and skin

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4
Q

when is bioavailabilty reduced

A

when administered orally

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5
Q

bioavailability

A

amount of drug that eventually reaches systemic circulation of an administered dose of the drug
quantity reaching systemic circulation /quantity adminsitered

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6
Q

where doe the phases of metabolism occur

A

in the liver

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7
Q

where are hepatic drug metabolizing enzymes

A

embedded in smooth endoplasmic reticulum of the liver hepatocytes

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8
Q

which cross plasma membrane to be metabolised more readily

A

non polar as can cross membrane more readily

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9
Q

phase 1 metaboism

A

change in the drug by oxidation reduction or hydrolysis to form a chemically reactive metabolite that can be active/ toxic

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10
Q

what is the oxidation phase accomplished by

A

cytphcrome p450 enzymes

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11
Q

what occurs during the oxidation phase

A

drug molecule incorporates one atom of 02 to the drug to form a hydroxyl group

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12
Q

role of cytoplasmic enzymes

A

can metabolise the durg

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13
Q

what are susceptible to hyrolysis

A

ester and amide bonds

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14
Q

what can phase 1 produce

A

harmful metabolites during oxidation

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15
Q

what are cytochrome p450 enzymes

A

membrane bound haem proteins

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16
Q

genetics of p450

A

some poeple lack such acitity leading to higher drug plasma levels
some have higher leading to lower plasma levels.. reduced drug action

17
Q

phase 2 reaction

A

involve the combination of the dryg with one of the several polar molecules to form a water soluble metabolite; conjugation

18
Q

what terminates all biological acitvty

A

phase 2 reactions

19
Q

conjugated produces

A

can be readily excreted via kidney

20
Q

can some drugs go directly to phase 2

A

yes

21
Q
A