Term
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Definition
| Group of heme containing enzymes responsible for phase I metabolism |
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Term
| a drug with a high affinity for an enzyme will do what to the metabolism of a low affinity drug? |
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Definition
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Term
| What is the most abundant pathway of the CYP-450 where many of our most common drugs are metabolized? |
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Definition
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Term
| What drugs are metabolized by the CYP450 3A4 pathway? |
|
Definition
Macrolides (antibiotics)
Fluoxetine (prozac)
Grape fruit juice - interacts with antifungals & antihypertensives
indanivir - used in HIV
itraconazole - anti fungal drugs
ketoconazole
ritonavir |
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Term
| What are the sub families of the CYP 450 inhibitors? |
|
Definition
inhibitors slow down the metabolism of the other drug and keep it around longer (increases)
1A2
2C19
2C9
2D6
34A |
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Term
|
Definition
| Cimetidine - (tagament) Quinolone (levoflocicin, ciprofloxicin) |
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Term
|
Definition
| Fluoxetine (Prozac) Ketocanazole (antifungal) Nizarole ( antifungal) Lansoprazole (antifungal) |
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Term
|
Definition
| amiodarone ( antiarthymic drug) fluconazole ( antifungal) Isonaiazid ( anti TB drug) |
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Term
|
Definition
| Amiodarone Cimetidine Clomipramine ( ocd tricyclic antidepressant) Paroxetine (Paxil) Ritonavir - boosting dose for HIV |
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Term
|
Definition
Protease Inhibitors
amiodarone
clarithromycin
erythromycin
grapefruit juice
ketoconazole
fluoxetine
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|
|
Term
| What sites does Cimetidine work as an inhibitor? |
|
Definition
|
|
Term
| What sites does Fluoxetine (prozac) work as an inhibitor? |
|
Definition
|
|
Term
| What sites does ketocanazole work as an inhibitor? |
|
Definition
|
|
Term
| What site does Ritonavir work as an inhibitor? |
|
Definition
|
|
Term
| What sites does Amiodarone work as an inhibitor? |
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Definition
|
|
Term
| Name the CYP 450 inducers |
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Definition
| 1A2 tobacco 2C9 rifampin (powerful inducer) 2E1 ethanol, isoniazid 34A - Carbamarazpine - and inhibitor and an inducer |
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Term
|
Definition
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|
Term
| Name a powerful inducer that is used as an agent to eliminate antibiotics |
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Definition
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|
Term
| Name a powerful inducer and inhibitor |
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Definition
|
|
Term
| Where is Cytochrome P-450 primarily located? |
|
Definition
| membranes of the smooth endoplastic reticulum. |
|
|
Term
| Where is the most common site for Cytochrome P-450 in the body? |
|
Definition
|
|
Term
| Which phase is the most common phase of the Cytochrome P-450 where interactions occur most? |
|
Definition
|
|
Term
| What factors play a role in drug metabolism at phase 1? |
|
Definition
| oxidation, reduction, hydrolysis Ethnicity whether you are a slow or fast metabolizer esp if over age 80 |
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Term
|
Definition
| synthesis and oxidation as well - |
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Term
|
Definition
| a substance stimulates the synthesis of the enzyme and metabolic capacity is increased. It eliminates the drug faster. |
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Term
|
Definition
| a drug with a high affinity for an enzyme will SLOW metabolism of a low affinity drug. Competitive binding at an enzymes binding site is receptor inhibition |
|
|
Term
| What is the most abundant pathway of the Cytochrome P-450, where many common drugs are given and metabolized by Cytochrome P-450? |
|
Definition
|
|
Term
| List the most common drugs that are metabolized by Cytochrome P-450 3A4 pathway |
|
Definition
Macrolides ( antibiotics) Fluoxetine (prozac) grapefruit juice -( interacts with antifungals and antihypertensives)
indanivir - (used in HIV )
itraconazole - antifungal drugs
Ketoconazole
ritonavir |
|
|
Term
| What can happen when an inhibitor is added to a substrate? |
|
Definition
| Fluoxetine is added to nortriptyilline - bc Fluoxetine is an inhibitor it will increase the levels of nortriptylline which is a substrate ( neither an inhibitor or inducer) |
|
|
Term
| What happens with a substrate is added to an inhibitor? |
|
Definition
| ex nortiprtylline is added to fluoxetine - it will lead to an increased level of nortriptylline. |
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Term
| What happens when an inducer is added to a substrate? |
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Definition
| Carbamezepine is added to haldol - Carbamezepine is an inducer so it will lead to a decrease in the levels of haldol in systematic circulation. |
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|
Term
| What happens when a substrate is added to an inducer? |
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Definition
| Haldol is added to Carbamezepine this will lead to a lower than expected level of haldol in the blood |
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|
Term
| What is reversal of inhibition? |
|
Definition
| Cimetidine is discountinued in the presence of nortriptyline, leading to a decrase in the nortriptyline blood level. This is IMPORTANT |
|
|
Term
| What is reversal of induction? |
|
Definition
| a pt on amitriptyline abruptly stops smoking - leading to an increase in amitriptyline blood levels bc nicotine is an inducer and inducers will increase your amount. |
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Term
|
Definition
219
Fluoxetine
ketocanazole
lansoprazole |
|
|
Term
|
Definition
2C9
amiodarone,
fluconazole
isoniazid |
|
|
Term
|
Definition
2DC
paroxetine,
Amiodarone
cimetidine,
clomipramine,
ritonavir |
|
|
Term
| What is the decatron dance? |
|
Definition
Dexamethasone can cause itching in the genital area and motor movements if given too quickly.
if over 15mg you need to give IV slowly |
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