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Anesthesia Pharm1
Basics
| Question | Answer |
|---|---|
| Pharmacological antagonists: | 1) prevent binding of other molecules to the receptor by their binding to the receptor 2) atropine (blocks ACh action on the heart |
| Most important factor influencing drug absorption rate following intramuscular injection: | injection site blood flow |
| Weak organic acid, pKa 6.5. Percent ionization at pH 7.5? | 90%- For a one order of magnitude change (6.5 to 7.5-one power of 10), the choice is 10% or 90%; in the case of an acid, a pH higher than the pKa promotes increased ionization. |
| Term having to do with drug actions on the body: | harmacodynamics |
| Drug with this ionization property most likely to diffuse from intestine (pH 8.4) to blood (pH 7.4)? a. weak acid (pKa 7.4) b. weak base (pKa 8.4) c. weak acid (pKa 8.4) d. weak base (pKa 6.4) e. weak acid (pKa 6.4) | c. weak acid (pKa 8.4) |
| General term having to do with actions of the body on the drug: | pharmacokinetics |
| Most drug have molecular weights between: | 100 and 1000 |
| Bond type that is seen in some drug-receptor interactions and tends to very strong, often nearly irreversible: | Covalent |
| when pH=pk, 50% of the molecules are ionized. For the weak acid to lose more protons (charged), the pH needs to be above the pKa. So, Increasing ionization at pH ABOVE pKa? weak acid or weak base? | weak acid |
| # Example(s) of covalent drug-receptor interactions: 1. activated phenoxybenzamine-receptor 2. anti-cancer DNA alkylating drugs, like cyclophosphamide (Cytoxan) 3. ? norepinephrine 4. A & B 5. A, B & C | 4. = 1. activated phenoxybenzamine-receptor 2. anti-cancer DNA alkylating drugs, like cyclophosphamide (Cytoxan) |
| Drug-transport system described as "energy requiring": 1. glomerular filtration 2. facilitated diffusion 3. active transport | 3. active transport |
| Dramatic decrease in systemic availability of a drug following oral administration is most likely due to? # extreme drug instability at stomach pH # hepatic "first-pass" effect # drug metabolized by gut flora # tablet does not dissolve | # hepatic "first-pass" effect |
| Drug delivery method LEAST suitable for long term (days to weeks) slow release? 1. pellet implant under the skin (subcutaneous) 2. time release capsule 3. i.m. injection of a drug-oil suspension? 4. transdermal patch 5. X none of the above | time release capsule |
| # Faster drug absorption: 1.lung or 2. stomach | Lung |
| Most common mechanism of drug permeation: 1. endocytosis 2. carrier-mediated transport 3. active-transport 4. passive diffusion | passive diffusion |
| Characteristics those aqueous diffusion: 1. occurs within large intracellular and extracellular components 2. occurs across epithelial membrane tight junctions 3.occurs across endothelial blood vessel lining -- often through pores | All of the above |
| Description of enantiomers: 1. may be readily superimposed 2. enantiomers, when presence in equal proportions, are referred to as racemates 3.may be characterized by absolute configuration or by direction in which enantiomers rotate polarized light | 2 & 3 |
| Major types of chemical forces/bonds: 1. hydrophobic interactions 2. electrostatic 3. covalent | all of the above |
| Examples of enantiomeric differences: 1.cardiotoxicity with both enantiomers of bupivacaine. 2. Ropivacaine less cardiotoxic than bupivacaine because it is metabolized faster 3.cisatracurium = atracurium isomer that doesn't = histamine release. | 3.cisatracurium = atracurium isomer that doesn't = histamine release. |
| # The binding of the activated form of phenoxybenzamine (alpha-receptor antagonist) with the alpha receptor is an example of this type of chemical force/bond: 1. electrostatic 2. covalent 3. hydrophobic interactions | covalent |
| # Percentage of all drugs that exist as enantiomeric pairs: 1. less than 1% 2. 5%-15% 3. 30% 4. > 50% 5. > 90% | > 50% |
| # Characteristic(s) of enantiomers: 1. chemically identical 2. mirror images of each other 3. both 4. neither | both |
| Factors that influence the rate of passive movement to molecules down the concentration gradient (Fick's Law)? 1.concentration difference 2. area across which diffusion occurs 3.drug mobility in the diffusion panel 4.thicknesslength of the diffusion pass | all |
| Saturable transport system(s): 1. X facilitated diffusion 2. X passive diffusion 3. X active transport | 1. X facilitated diffusion, 3. X active transport |
| Stereoselectivity and metabolism: 1. ? enzymes typically exhibit stereoselectivity -- a preference for one or the other enantiomeric form 2. ? duration of action of one enantiomer may be different from the other | both |