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17 Cards in this Set
- Front
- Back
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Metabolism has 2 phases. ___A___ consists of conjugating with ___B___ to become more ___C__.
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Phase 2
glucuronic acid water soluble |
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Metabolism has 2 phases. __A__ consists of adding or removing a __B__ to go from being ___C___ to ___D___.
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Phase 1
functional group lipid soluble water soluble |
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Drug metabolism by hydrolysis occurs only in ___A___. This is via the enzyme ___B___ which exists in ___C(2 places)___.
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Esters
esterase liver/plasma |
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Requirements of the electron transport metabolization system for drugs
3 things 2 enzymes |
molecular O2
NADPH p450 p450 reductase p450 b5 reductase |
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Electron transport metabolization.
p450 is bound to ___A___, which binds to the drug. Then, this complex receives an electron from ___B___ via the enzyme___C___. The reduced compound reacts w/ ___D___, and then gets a second electron from ___E___ via the enzyme ___F___ or via ___G___ via the enzyme ___H____. THen, the drug releases in the form of __I___, leaving behind____J____ |
a - Fe 3+
b - NADPH c - p450 reductase d- O2 e - NADPH f - p450 reductase g - NADH h - p450 b5 reductase i - drug-OH j - p450 Fe3+ |
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Types of drugs
Amine Ether Aromatic alkane (rch2ch3) tertiary amine secondary amine sulfur terminal amine Which undergo N/O dealkylation in phase 1? |
Amine, Ether
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Types of drugs
Amine Ether Aromatic alkane (rch2ch3) tertiary amine secondary amine sulfur terminal amine Which undergo side chain/aromatic hydroxylation in phase 1 metabolism? |
Aromatic
Alkane |
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Types of drugs
Amine Ether Aromatic alkane (rch2ch3) tertiary amine secondary amine sulfur terminal amine Which undergo N-oxidation/N-hydroxylation in phase 1 metabolism? |
Secondary/tertiary amines
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Types of drugs
Amine Ether Aromatic alkane (rch2ch3) tertiary amine secondary amine sulfur terminal amine Which undergo sulfoxide formation in phase 1 metabolism? |
sulfur compounds
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Types of drugs
Amine Ether Aromatic alkane (rch2ch3) tertiary amine secondary amine sulfur terminal amine Which undergo deamination in phase 1 metabolism? |
Terminal amines
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For glucuronide conjugation (aka ___A___) the enzyme is ___B___.
The substrates are ___C___, and it occurs in the ___D(3)___. The product is ___E___ which becomes ___F___ as ___G__ is released. |
phase 2 metabolism
microsomal glucuronyl transferase drug products from phase 1 liver, intestinal epitheleum, kidney Drug-gluc acid complex glucuronide UDP |
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In naming CYP isoforms, the figure represents __A__ the second ___B___ and the 3rd ___.
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family
subfamily single member |
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What is the most common isoform of CYP?
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CYP3A4/5
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A prodrug is a ___A____, and they are significant when___B___ via ___C___ or ___D___
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biologically inactive chemical molecule
the body converts them to active usually via p450 or plasma enzymes |
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An example of a prodrug is ___A___ which is an anti-platelet drug. Converted by CYP __B__ which also does the popular drug __C__.
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Clopidogrel (PLAVIX)
2C19 Diazepam |
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An example of a prodrug is ___A___ which is converted by ___B___ in the plasma to become ____C____ which is a potent anesthetic.
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fospropofol (LUSEDRA)
alkaline phosphatase Propofol |
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CYP 1A2----
CYP2C9 ---- CYP2C19 ----- CYP2E1 ---- CYP2D6---- CYP3A4/5---- |
CYP 1A2----Theophylline
CYP2C9 ---- warfarin CYP2C19 -----diazepam CYP2E1 ---- acetaminophen CYP2D6----codein CYP3A4/5----carbamazepine, diazepam, triazolam |
