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9 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Physiochemical properties of lignocaine |
- Amide LA - pKa 7.9 - 25% unionised at pH 7.4 - Rel. lipid solubility 150 (heptane-buffer coefficient 2.9) |
- Structure - pKa - % unionised at 7.4 - Lipid solubility |
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Pharmacokinetic properties of lignocaine |
- PPB 70% (A1AG) - Metabolised in liver by dealkylation (HER 0.63) - Metabolites excreted in urine - Elimination half-life 100 min - Clearance reduced in presence of hepatic / cardiac failure |
- Protein binding - metabolism, HER - excretion - elimination half life |
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Pharmacodynamic properties of lignocaine |
- relative potency 2 - fast onset - moderate duration of action - toxic plasma conc >5 mcg/ml - max dose 3mg/kg or 7mg/kg with adrenaline |
- potency - onset - duration - toxic plasma conc - safe dose |
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Physiochemical properties of prilocaine |
- amide LA - pKa 7.7 - 33% unionised at pH 7.4 - Rel lipid solubility 50 (heptane-buffer coefficient 0.9) |
- Structure - pKa - % unionised at 7.4 - Lipid solubility |
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Pharmacokinetic properties of prilocaine |
- PPB 55% - Most rapidly metabolised amide LA (liver, kidney, lung) - O-toluidine may precipitate methaemoglobinaemia - Elimination half life 100 min |
- Protein binding - metabolism - elimination half life |
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Pharmacodynamic properties of prilocaine |
- Relative potency 2 - Onset fast - Duration moderate - Toxic plasma conc >5 mcg/ml - Safe dose 6 mg/kg or 9 mg/kg with adrenaline |
- potency - onset - duration - toxic plasma conc - safe dose |
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Physiochemical properties of cocaine |
- Ester LA - pKa 8.6 - 5% unionised at pH 7.4 |
- Structure - pKa - % unionised at 7.4 |
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Pharmacokinetic properties of cocaine |
- 95% PPB - significant hepatic hydrolysis to inactive products which are excreted in the urine - elimination half life 100 min |
- protein binding - metabolism - elimination half life |
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Pharmacodynamic properties of cocaine |
- MOA: blocks uptake 1 and MAO while also stimulating the CNS, so increased risk of hypertension and arrhythmias - moderate onset - short duration - toxic plasma conc 0.5 mcg/ml - vasoconstrictor at all doses |
- MOA - Onset - Duration - Toxic plasma conc |
