Erstellt von Katie Scanlon
vor fast 8 Jahre
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Frage | Antworten |
Volume of Distribution Vd | Vd= Amt of drug/ desired plasma concen |
Vd Lipo/hydro PHILIC | Vd TBW > 0.6 L/kg or > 42 L = LIPOPHILIC Vd TBW < 0.6 L/kg or < 42 L = HYDROPHILIC |
Loading dose calc | Loading dose= Vd x Desired Plasma Conce Bioavailability (1) |
Clearance: Directly vs Inversely | Directly: Blood flow to organ Extraction ratio Drug dose Inversely: Half-life Drug concen in central compartment |
Elimination Half-Life | Half life Drug Elim% Drug Remaining% 0 - 0 - 100 1 - 50 - 50 2 - 75 - 25 3 - 87.5 - 12.5 4 - 93.75 - 6.25 5 - 96.875 - 3.125 |
Half life vs Half time | Half life: time it takes for 50% of the drug to be removed from the BODY Half time: time it takes for 50% of the drug to be removed from the PLASMA |
Like Dissolves Like | Drug: Solution Acid: Basic sol = Highly ionized Acid: Acidic sol = Unionized Base: Acidic = Highly ionized Base: Basic = Unionized |
Ion Trapping | Maternal Alkalosis & fetal acidosis ^Union fraction of locals crosses placenta Fetal acidosis - protonates the LA+ "trapping" the LA in the fetus |
Plasma Protein Binding | Drug storage in the blood Albumin: negative charge; acidic >basic Alpha-1 acid glycoprotein: basic drugs Beta-globulin: binds basic drugs |
Plasma Concen: Albumin & Alpha-1 acid glycoprotein | Decreased Albumin: Liver/renal dz, Age, malnutrition, prego a-1 acid glycoprotein: Neonates, prego Increased a-1 acid glycoprotein: Sx stress, MI, pain, RA, Age |
Plasma Protein Binding & Vd | Vd is INVERSELY r/t plasma protein binding Highly protein bound drugs slower metabolism and elimination |
Metabolism Phases (3) | 1- Oxidation: + O2 - reduction: + e- - hydrolysis: + H2O 2 - Conjugation (H2O soluble, inactive) 3 - Elimination (kidney, liver, GI) |
Perfusion dependent vs Capacity dependent | Perfusion dependent: Fenta, lido, Prop Capacity dependent: Diazepam & Roc |
Extraction Ratio formula | Extraction Ratio = Arterial - Venous concen Arterial concen |
ER > 0.7 ER < 0.3 | Flow limited elimination ER > 0.7 blood flow Capacity limited elimination ER < 0.3 enzyme induction |
LOW ER Drugs | Roc Benzo's (most) Methadone Thiopental Theophylline Phenytoin |
P450 Enzymes: Inducers vs Inhibitors | Induce: Tobacco, Barbs, Phenytoin, ethanol, Rifampin, carbamazepine Inhibitor: grapefruit, SSRIs, cimetidine, omperazole, isoniazid, erythromyocin, -azole |
Other enzymes | CYP 3A4: Opioids Benzos LA's CYP 2D6: Codeine, oxy-hydrocodone CYP 1A2: Theophylline |
Polarity & Elimination | Hydrophilic drugs - excreted unchanged Lipophilic drugs - biotransformation to ^H2O solubility |
Transport drugs to urine: | 1- Glomerular filtration: non-protein bound drugs & free fraction are filtered 2 - Organic Anion/Cation transporters: OAT-anion: furosemide, thiazide, PCN OCT-cation: morphine, meperidine, dopa |
Urine pH Reabsorption & Excretion | Acidic Urine: AAA Reabsorption of acidic Excretion of basic Basic Urine: BBB Reabsorption of acidic Excretion of basic |
Metabolism in the Plasma | |
Difference between: Kinetics Biophasics Dynamics | |
Dose Response Curve: Efficacy & Potency | |
Dose Response Curve: Affinity for receptor | |
Agonists Partial Agonists Antagonists Inverse Agonists (graph) | |
Drugs administered together | Addition: 1+ 1 = 2 Synergism: 1 + 1 = 3 Potentiation: 1 + 0 = 3 Antagonism = 1 + 1 = 0 |
Therapeutic Index | Measure of drug safety TI = Lethal dose50/Effective dose50 |
ED 50 | Effective dose 50 = dose that produces expected clinical response in 50% of pop. POTENCY |
LD 50 | Lethal dose 50 = dose that produces death in 50% of pop. |
Chirality | Molecule with 3D asymmetry 1chiral carbon = 2 enantiomers |
Enantiomerism | Molecules that are Mirror images & can't be superimposed Dextrorotary clockwise: R (rectus) d or + Levorotary counterclock: S (sinister) l or - |
Enantiomerism in Anesthesia | Ketamine & Thiopental Methohexital Iso & Des Mepivacaine, Prilo, Bupi, CisAtra Morphine & Methadone Ibuprofen & Toradol (* Bupi & Cardiac toxicity: R > S) |
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