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57 Cards in this Set

  • Front
  • Back
List 5 fluid compartments that are sites of exclsuion to drugs
Cerebral fluid
Ocular fluid
Lymph fluid
Fetal Fluid
Pleural fluid

2 major drug binding plasma proteins
1. Albumin

2. Orosomucoid = alpha1 acid glycoprotein
What is the "negative acute phase plasma protein"?
Name 2 drugs that decrease in the body if albumin is at a lower concentration

What is the "Positive acute phase plasma protein"?
When does Orosomucoid increase its concentration?
with Inflammation
Name two drugs that increase in concentration in the body when Orosomucoid increases

What 3 things can alter the concentration of free drug in plasma?
1. Dose
2. Disease (albuminemia, uremia)
3. Co-administration of other drugs
During which semester is the fetus most vulnerable to the teratogenic effects of drugs?
1st semester
How do drugs enter mammary milk?
passive diffusion
List 3 general drugs that accumulate in milk and why they do so
1. Weak organic bases = milk is more acidic than plasma = "ion trap"

2. Tetracyclines = chelate with calcium

3. Lipid-soluble drugs = milk has high fat content
Explain Thiopental Redistribution
-Thiopental is IV administered
-initally distributed to areas of highest blood flow: brain, liver, kidneys
-drug is then redistributed to and stored in muscle and adipose tissue = terminated by redistribution
The action of what group of drugs are terminated by redistribution?
Lipid soluble CNS active drugs

**The duration of action of an initial dose may depend more on the redistribution rate rather than on the half-life
**With repeated doses, fat and other tissue depots become saturated, resulting in longer durations of action than the first dose
List 5 things that contribute to the blood brain barrier
1. tight jxns
2. glia wrappings
3. low CSF protein = lower than plasma causes drugs to want to stay in plasma
4. Enzymes
5. Transporters
List the 5 factors affecting distribution
1. blood flow to the organ
2. the solubility of the drug
3. level of binding to substances in the blood versus binding to substances in tissues
4. transporters
5. ion-trapping
What do Phase 1 reactions do to drugs?
change the functionality of the drug
-metabolite with modified activity
-inactive metabolite
What do Phase 2 reactions do to drugs?
Synthesis = add something on to the molecule = make drug more hydrophilic
What are sometimes referred to as Phase 3 clearance?
3 important Phase 1 reactions
1. Oxidation = loss of electron
2. Reduction = gain of electron
3. Hydrolysis

6 important Phase 2 reactions
1. Glucuronidation
2. Sulfate conjugation
3. Acetylation
4. Glutathione conjugation
5. Methylation
6. Glycine conjugation

*1 and 2 are most important
Where are Phase 1 drug-metabolizing enzymes (mixed function oxidases or monooxygenases) located?
in lipophilic membranes of SER
Phase 1 biotransformation oxidation usually occurs by what?
Cytochrome P450 isozyme
What are the 4 Oxidation requirements for Phase 1 biotransformation?
1. Cytochrome P450
2. Cytochrome P450 reductase
4. Molecular Oxygen
CYP's that encode enzymes for most drug biotransfomations
CYP 1, 2, and 3
CYP that is extensively express in GI responsible for poor oral bioavailability (first-pass)
Drugs that induce CYP2C9 (3)

**To See 9 Fen-Fen Rif's**
Drugs that induce CYP2C19 (4)

To See 19 "Barbs, Carbs, Fins, and Rifs"
What CYP do the following drugs induce?

Polycyclic aromatic compounds
Drugs that induce CYP3A4 (2)
1. Glucocorticoids

2. Anticonvulsants
Drugs that induce CYP2E1 (3)
1. Chronic Alcohol
2. Isoniazid
3. Activates carcinogenic nitrosamines

**2 Erick's = Chronic Alcoholic -> Must "ISO"late them
**Erick should not take Acetaminophen
CYP that when induced converts Acetominophen to a toxic metabolite

*induced by Isoniazid and Chronic Alcohol
What CYP metabolizes Terfenadine and Astemizole?
List 2 drugs that markedly increase the toxicity of Terfenadine, why, and the physiologic effect
-Erythromycin and Ketoconazole

-They inhibit CYP3A4 which causes Terfenadine to accumulate

-QT prolongation -> -> -> Torsade de points

*Terfenadine must be metabolized to be activated (active product is Fexofenadine)
List 8 inducers of phase 1 biotransformation (cause other drugs to be metabolized more quickly)
1. Phenobarbital
2. Phenytoin
3. Carbamazepine
4. Polycyclic aromatics
5. Glucocorticoids
6. Chronic Alcohol
7. Rifampin
8. St. John's Wort

*1-3 are Anticonvulsants

**St. John, the Chronic Alcoholic, Smokes, eats Carbs, takes Phen-Phen, and gets shots of Cortisol, all while playing Rifs on the guitar
List 6 inhibitors of phase 1 biotransformation (decrease the metabolism of drugs)
1. Cimetidine
2. Ketoconazole
3. Chloramphenicol
4. Erythromycin
5. Acute Alcohol
6. Grapefruit juice

2 possible ways a Phase 2 drug conjugate can be formed
1. via high energy intermediate and the parent compound

2. Phase 1 metabolite by a transfer enzyme
Phase 2 major route of metabolism for both drugs and endogenous compounds
Glucuronide conjugation
Glucuronide transferase activity is localized to this organelle and organ

By what process are glucuronides secreted in the kidney and liver
ACTIVE transport = against their concentration gradient with use of ATP
2 Phase-2 reactions that especially make compounds more water-soluble and excretable
1. Sulfation
2. Glucuronidation
2 Phase 2 rxns that often make drugs less water-soluble
1. Methylation

2. Acetylation
Crystalluria results when __1__(rxn) products of __2__(compound) precipitate in __3__(pH) tubular urine
1. acetylated
2. sulfonamides
3. acidic
Which Phase reactions are more likely to be preserved in the elderly, Phase 1 or 2?
Phase 2 reactions
6 liver diseases that can cause decreased drug metabolism
1. Fatty liver
2. Hepatitis
3. Cirrhosis
4. Hemochromatosis
5. Liver tumors
6. Drug-induced liver damage
2 CYP polymorphisms that can affect biotransformation in different races

Do not give this drug if a person has 2 non-functional alleles of Thiopurine S-methytransferase
6-mercaptopurine b/c will cause toxicity
20% of asians and blacks have a polymorphism of this CYP that has POOR METABOLISM (PM)
CYP 2C19
If prescribing for Warfarin, you should genetically test for these genes (2)

What would be the ADR?
1. CYP 2C9
2. Vitamin K Epoxide Reductase

ADR = bleeding
If giving Isoniazid (anti-TB) what gene should be tested for?

What would be the ADR?
N-acetyltransferase (Phase II Conjugation)

If prescribing 6-Mercaptopurine what gene should be tested for?


Therapeutical use of Mercaptopurine?
Thiopurine S-methytransferase

Hematological toxicity

Acute Lymphoblastic Leukemia
If prescribing Irinotecan, what metabolic gene should be tested for?


Irinotecan therapeutical use?
1. UDP-Glucuronosyltransferase (UGT1A1)

2. Diarrhea or neutropenia

3. colon cancer
If giving Codeine, what gene should be tested for?


Codeine therapeutical use?

lack of analgesic effect

The reactive metabolite of Acetaminophen may induce this adverse response
Reactive metabolites of Aflatoxin may induce this adverse response
Reactive metabolites of Cyclophosphamide may induce this adverse response
What are 2 Weak Organic Base drugs that can accumulate in Milk and cause harm to babies who are breast-feeding?

CYP that when induced activates Carcinogenic Nitrosamines

What induces it? (2)

Isoniazid & Chronic Alcohol