Term
| What drug is associated with "pfcrt"? (plasmodium falciparum c________ resistance transporter gene) |
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Definition
| chloroquine. This transporter effluxes out the chloroquinine, so it is not effective in the plasmodium :( |
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Term
| What drug(s) are associated with deficiency of G6PD? |
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Definition
| Primaquine, sulfonamides (?). If person is already deficient in G6PD and cant make enough glutathione to combat oxidative stress as it is, having primaquine on top of it won't help. primaquine forms toxic metabolites that methylate hemoglobin and decreases Hgb ability to carry oxygen, so leads to hemolysis of RBC :( |
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Term
| What disease is associated with mutated CCR5 (chemokine receptor 5)? What drug has been created to mimic the blockage of CCR5? |
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Definition
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Term
| What drug(s) are associated with HER receptors? |
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Definition
| breast cancer drug, Trastuzmab. It interferes with the HER receptors. Not all breast cancer patients have HER receptors, so must know if she has them before prescribing this med. |
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Term
| What drug(s) are associated with CYP2D6? |
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Definition
| Codeine (a prodrug). Will turn into morphine when 3-OH is hydrolyzed by CYP 2D6. Therefore, decreased 2D6 means there is decreased effectiveness (such as in PM). Created synthetic opioids to combat this issue. |
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Term
| What drug(s) are associated with CYP2J2? How do we bypass the issue with variants of 2J2? |
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Definition
| Terfenadine. Variants in 2J2 can cause increased risk of arrhythimas by prolonging QT interval. Was replaced by fexofenadine to bypass this issue. Fexofenadine has no cardiotoxic effects because does not use CYP 2J2 :) |
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Term
| What drug(s) are associated with CYP2C9? How do we bypass the issue with variants of 2C9? |
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Definition
| Warfarin. CYP2C9 enzymes metabolize warfarin, so variability in 2C9 means it's difficult to predict optimal dose per patient. Can bypass this issue with newer drugs such as dabigatran and rivaroxaban. Dabigatran is hydrolyzed by carbamate hydrolase, NOT 2C9 :) |
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Term
| Warfarin is metabolized by 2C9. Dabigatran is not. What metabolized dabigatran instead? |
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Definition
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Term
| What drug(s) are associated with CYP 2C19? What can we use to bypass issues with variants of 2C19? |
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Definition
Clopidogrel (a prodrug). If there is a variant with 2C19 that causes it to be absent or reduced, clopidogrel will not get metabolized to active form and will not be effective. Thus we will see CV issues. *2 & *3 often result in nonfunctional 2C19 enzymes. *2 is common in asians (30%), blacks (17%), and whites (15%). *4,5,6,7, & *8 results in absent or reduced function enzymes. Not as common as *2 & *3. These patients as PM of clopidogrel and should use alternative drug.
We can use prasugrel or ticagrelor.
Prasugrel (a prodrug) does not involve CYP2C19 but it is still a thienopyridine. Prasugrel also has an addition oxygen which helps it to become active.
Ticagrelor (NOT a prodrug) does not involve CYP 2C19 nor is it a thienopyridine or prodrug :) |
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