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General Principles
Pharmacology: General
| Question | Answer |
|---|---|
| 1. Drugs that remain in the plasma compartment of the body have a volume of distribution (Vd) of: 2. In which ionization state are drugs better able to permeate lipid membranes? | 1. low Vd (3-4L) 2. only the nonionized (uncharged) form crosses membranes |
| 1. In which ionization state are drugs better cleared from the body? 2. What is the ionization of a drug when the pH of the surrounding environment is at the pKa of the drug? | 1. ionized (charged) 2. 50% ionized and 50% nonionized |
| At what pH would the following drugs be ionized? 1. acidic drugs 2. basic drugs | 1. high pH (drug donates a proton to environment) 2. low pH (drug accepts a proton from environment) |
| 1. Where in the body will the following drugs be best absorbed? 1. acidic drugs 2. basic drugs | 1. stomach (low pH so drug is nonionized) 2. small intestine (high pH so drug is nonionized) |
| 1. What is the fastest route of drug absorption? 2. How do you calculate total body water? | 1. inhalation 2. patient's weight x 60% |
| What are the compartments for total body water? | 1. extracellular (14L) which is composed of plasma (3L) and interstitial (11L) 2. Intracellular |
| What is the difference between phase I and phase II types of biotransformation? | 1. phase I: cytochrome P450 2. phase II: conjugation via transferases |
| What is gray baby syndrome? Why is it seen? | 1. chloramphenicol toxicity 2. the drug is metabolized by glucuronidation which has reduced activity in neonates |
| 1. Where is the cell are cytochrome P450 enzymes found? 2. Which cytochrome P450 enzyme metabolizes a majority of the drugs on the market? 3. Which drugs induce SLE-like symptoms? | 1. smooth ER 2. 3A4 3. hydralazine > procainamide > isoniazide |
| Inducers of cytochrome P450: | Queen Barb Steals Phen-phen and Refuses Greasy Carbs Chronically 1. Quinidine 2. Barbiturates 3. St. John's Wort 4. Phenytoin 5. Rifampin 6. Griseofulvin 7. Carbamazepine 8. Chronical alcohol use |
| Inhibitors of cytochrome P450: | Inhibit drinking from a KEG or you'll be Acutely SICk 1. Ketoconazole 2. Erythromycin 3. Grapefruit juice 4. Acute alcohol 5. Sulfonamides 6. Isoniazide 7. Cimetidine |
| 1. What role do beer, red wine and cheese play in drug metabolism? 2. zero-order elimination 3. first order elimination | 1. contain tyramine that is metabolized by phase I monoamine oxidase reaction 2. constant amount eliminated 3. constant fraction eliminated |
| 1. How many half lives does it take to get to steady state? 2. What percentage of steady state is reached after one half-life? | 1. 4-5 half lives 2. 50% |
| What is the effect of mixing a partial agonist and a full agonist? | the partial agonist displaces the full agonist from the receptor and the response is reduced - the partial agonist is acting as an antagonist |
| Which kind of antagonism: 1. competitive antagonism for the same receptor 2. two agonist with opposing action (i.e. vasoconstrictor vs vasodilator) 3. interacts directly with drug to remove it or prevent it from binding target | 1. Pharmacologic antagonist 2. Physiologic antagonism 3. Chemical antagonism |
| How is therapeutic index calculated? | TI = LD50/ED50 (TILE) dose that is lethal to 50% of the population divided by dose that is effected to 50% of the population |
| 1. How do irreversible inhibitors effect Km and Vmax? 2. How do reversible inhibitors effect Km and Vmax? | 1. decrease Vmax; no effect on Km 2. no effect on Vmax; ↑ Km (less affinity) |
| What is similar of all drugs with "phen" in the name? | 1. lipid soluble 2. cross the blood-brain-barrier 3. liver metabolism |
| 1. Efficacy 2. Potency | 1. Maximal effect a drug can produce 2. Amount of drug needed for a given effect (related to effective dose, ED50) |
| Toxicity Antidotes: 1. Acetaminophen 2. Salicylates 3. Amphetamines 4. Antimuscarinic agent | 1. N-acetylcysteine 2. NaHCO3 (alkalinize urine) 3. NH4Cl (acidify urine) 4. Physostigmine salicylate |
| Toxicity Antidotes: 1. β-blockers 2. Iron 3. Lead 4. Cyanide | 1. glucagon 2. Deferoamine 3. dimercaprol, CaEDTA 4. Nitrite, thiosulfate |
| Toxicity Antidotes: 1. Methemoglobin 2. Methanol 3. Opioids 4. Benzodiazepines | 1. Methylene blue 2. Ethanol 3. Naloxone/naltrexone 4. Flumazenil |
| Toxicity Antidotes: 1. TCAs 2. Warfarin 3. tPA 4. theophylline | 1. NaHCO3 (Alkalinize urine) 2. Vitamin K, fresh frozen plasma 3. aminocaproic acid 4. β-blocker |
| What effect do the following have on efficacy and potency: 1. competitive inhibitors 2. noncompetitive inhibitors | 1. ↓ potency (↑ dose required for effect - same as ↑ Km) 2. ↓ efficacy (less max effect - Vmax) |
Created by:
amichael87
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