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20 Cards in this Set
- Front
- Back
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weak acid in acid medium is?
can it pass? |
non-ionized
yes |
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weak base in acid medium is?
can it pass? |
ionized
no |
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pharmaceutical phase
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swallow, disintegration, dissolution
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whats special about sublingual
what the drug has to be |
without metabolism via liver
lipophilic and uncharged to be absorbed in oral mucosa |
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albumin binds
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lipophilic and anionic (weak acid)
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Alpha 1 acid glycoprotein binds
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cationic, and very hydrophilic drugs
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result of malnutrtion in
1. albumin 2. alpha 1 ACID GLYCORPROTEIN |
1. less albumin, higher free conc. of drug
2. more alpha 1, lower free drug conc. |
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Volume of Distribution formula
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Vd=D/C
Total amount of drug in body=D plasma conc. of drug=C |
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Vd of small VD?
intermediate VD? |
0.057 L/kg
0.2L/KG |
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phase 1 metabolism modification
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increase polarity by -OH -NH2
Redox and hydrolysis more/less active or equal active P450 |
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phase 2 metabolism modification
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increase polarity by conjugation
glucuronic, sulfate, acetate, aa. less active |
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UGTs
UDP-glucuronosynltransferase transfer? modification? |
glucuronic acid
more polar |
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Sulfotransferases (SULTs)
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sulfate to hydroxyl
more polar |
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Glutathione S Transferases (GSTs)
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glutathion, anti-oxidant,
less toxic |
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N-acetyltransferases (NATs)
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acetyle group,
genetic polymorphism |
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Thiopurine Methyltransferase (TPMT)
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methyl, from S-adenosylmethionine
genetic polymorphism, protective |
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CYP2C9 SNPs
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metabolize anticoagulant drug warfarin
require lower dose of warfarin, can cause bleeding |
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CYP2D6
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metabolize codeine to morphine (morphine>codeine)
4 genotypes ultra rapid:increase, with multiple copy of gene extensive: normal intermediate: reduced poor:none |
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UGT1A1 SNPs
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decrease activity
an anticancer compound -increase risk of diarrhea and bone marrow suppression |
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NAT2 SNPs
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acetylate drug "isoniazid used to treat Tb" and caffeine and cancer causing chemicals
patieient slow/rapid acetylator slow acetylator: more isonizid toxicisty and more cancer |
