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35 Cards in this Set
- Front
- Back
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what are the two pathways needed to produce NADPH for P450 reactions?
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1. Embden-Meyerhof Pathway
2. PPP |
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What are the 5 mechanisms for drug metabolism?
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1. Oxidative reactions
2. Glucuronidation 3. Esterases 4. MAO 5. Alcohol and aldehyde dehydrogenase |
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what amine is present in chese and wine?
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tyramine
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what is used in treatment of parkinsons?
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MAOI
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metabolism of thiopental
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IV anesthetic --> pentobarbital (barbiturate)
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metabolism of parathion
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insecticide --> paraoxon (cholinesterase inhibitor)
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metabolism of CCl4
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dry cleaning --> free radical scavenger
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metabolism of terfenadine
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toxic antihitamine precursor --> histamine
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metabolism of Norepi
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Epi
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metabolism of morphine
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morphine-6-glucoronide
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metabolism of sulfasalazine
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5-ASA
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metabolism of EtOH
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acetaldehyde
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metabolism of procainamide
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NAPA
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inducers of P450 enzymes
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- cigarettes
- phenobarbital (barbituate) - rifampin (inhibits mRNA polymerase) - phenytoin (anti-epileptic) - carbamazepine (anti-epileptic, induces own metabolism) |
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inhibitors of P450 enzymes
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- cimetidine and ketoconazole
- disulfiram (aldehyde dehydrogenase) - metronidazole -like disulfiram - cimetidien antifungals (ketoconazole, itraconazole) - antibiotics (erythromycins, trolenadomycin, clarithromycin) - HIV protease inhibhitors - some SSRI, PPI, grapefruit juice |
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what prototypical drug displaces plasma binding of coadministered drugs?
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warfarin
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what are the genetics of G6PD deficiency?
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sex linked
protective against malaria |
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what is the mechanism of G6PD toxicity?
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Red cells don't make NADPH (part of the PPP)--> you can't make glutathione peroxidase --> cell is susceptible to oxidative damage --> hemolysis by H2O2 buildup
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what drugs/compounds should be avoided in people with G6PD?
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- primaquine (antimalarial)
- nitrofuratoin (antibiotic for UTIs) - napththalene (moth balls) - fava beans |
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what is the mechanism behind pseudocholinesterase deficiency toxicity?
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pseudocholinesterase breaks down succinylcholine. Post-surgical paralysis is prolonged.
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Tell me more about succinyl choline
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has a high affinity for nicotinic receptors, but is resistant to AChE
- can induce a depolarizing blockade |
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what is prophyria?
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problems with heme synthesis
- barbiturates induce d-ALA synthetase which leads to accumulation of heme precursors (d-ALA), which are neurotoxic |
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are fast acetylators autosomal dominant?
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yes
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what do you have to watch out for if you're a slow acetylator?
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sulfonamide toxicity
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what is the mechanism of sulfa drugs?
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In bacteria, antibacterial sulfonamides act as competitive inhibitors of the enzyme dihydropteroate synthetase, DHPS. DHPS catalyses the conversion of PABA (para-aminobenzoate) to dihydropteroate, a key step in folate synthesis. Folate is necessary for the cell to synthesize nucleic acids
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what is the mechanism of sulfonamide toxicity?
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metabolite sulfapyridine gives toxitiy
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what other drugs can cause toxicity in slow acetylators?
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isoniazid
hydralazine |
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how do isoniazid and hydralazine cause toxity?
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induces autoimmune reactions by inducing autoanitibodies aginast myeloperoxidase --> lupus like
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which drugs are given as prodrugs?
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- cyclophosphamide
- sulfasalazine - enalapril - terfenedine |
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what is cyclophosphamide used for?
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chemotherapy for lymphomas
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what is sulfasalazine used for?
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anti-inflammatory agent in the treatment of IBD as well as for RA.
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what is enalapril used for?
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ACE inhibitor used for hypertension and CHF
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what is terfenedine used for?
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active ingredient in the antihistamines
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which drugs/substances are made more toxic by drug metabolism?
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- ethylene glycol
- CCl4 |
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which drugs/substances show a carcinogenic effect after metabolism?
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- aflatoxin
- polycyclic aromatic hydrocarbons (cigarettes) |
