Pharmacology: General
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| 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
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| 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
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| 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)
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| 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)
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| 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%
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| What are the compartments for total body water? | 1. extracellular (14L) which is composed of plasma (3L) and interstitial (11L)
2. Intracellular
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| What is the difference between phase I and phase II types of biotransformation? | 1. phase I: cytochrome P450
2. phase II: conjugation via transferases
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| 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
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| 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
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| 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
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| 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
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| 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
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| 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%
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| 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
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| 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
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| 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
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| 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)
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| What is similar of all drugs with "phen" in the name? | 1. lipid soluble
2. cross the blood-brain-barrier
3. liver metabolism
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| 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)
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| 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
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| Toxicity Antidotes: 1. β-blockers 2. Iron 3. Lead 4. Cyanide | 1. glucagon
2. Deferoamine
3. dimercaprol, CaEDTA
4. Nitrite, thiosulfate
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| Toxicity Antidotes: 1. Methemoglobin 2. Methanol 3. Opioids 4. Benzodiazepines | 1. Methylene blue
2. Ethanol
3. Naloxone/naltrexone
4. Flumazenil
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| 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
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| 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)
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