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General Principles

Pharmacology: General

QuestionAnswer
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