Lidocaine:
Introduction:
Thesis: Lidocaine is a widely used local anesthetic that can be used in many types of conditions, however the focus will be on the local anesthetic administration in dental procedures.
1. Structural information and chemical properties: (National Center)
a. Chemical name and trade name: 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide, Lidocaine
b. Chemical structure: (Figure 1: Lidocaine Structure)
c. Molecular formula: C14H22N2O
d. Molecular weight: 234.343 g/mol
e. Log P (or Log D) value: 2.4
f. Water solubility: 4.1 g/L
Potentially useful information: HBD-1, HBA-2, Rotatable bonds-5
2. Uses/Conditions it is used to treat: (Mayo Clinic)
Local anesthetic and antiarrhythmic. Available only with prescription. …show more content…
Administration route
i. Link to chemical properties: Main focus will be on intravenous injection.
b. Distribution i. Volume of distribution
(Figure 4) (Yuko Ikeda, M.D.) ii. Passage through cell membranes, blood-brain barrier, or placental barrier? Highly soluble in fatty adipose tissues. (National Center)
c. Metabolism
i. Primary metabolites (show structures): (Sigma Aldrich) (Figure 5) ii. Type of modification (oxidation, reduction, hydrolysis, hydration, conjugation): Modification was done to the tertiary amine by reduction. (Sigma Aldrich) iii. Enzymes and organs involved in the metabolism iv. Prodrug? Liver is main route of metabolism. (National Center)
d. Excretion/Elimination i. Route- Is excreted/eliminated through the hepatic route i.e the kidneys. (National Center) ii. Clearance Rate- Clearance-0.64 +/- 0.18 L/min (National Center)
5. Dosage issues
a. Bioavailability: It should be noted that injection is favored for administration because only roughly 35% of the concentration of the drug remains after metabolism through oral ingestion. (National Center)
b. Therapeutic window (efficacy vs. toxicity) - Toxicity can be common if dosing and pharmacokinetic are not monitored carefully. Can cause toxicity in the Central Nervous System. (Yuko Ikeda,
Introduction:
Thesis: Lidocaine is a widely used local anesthetic that can be used in many types of conditions, however the focus will be on the local anesthetic administration in dental procedures.
1. Structural information and chemical properties: (National Center)
a. Chemical name and trade name: 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide, Lidocaine
b. Chemical structure: (Figure 1: Lidocaine Structure)
c. Molecular formula: C14H22N2O
d. Molecular weight: 234.343 g/mol
e. Log P (or Log D) value: 2.4
f. Water solubility: 4.1 g/L
Potentially useful information: HBD-1, HBA-2, Rotatable bonds-5
2. Uses/Conditions it is used to treat: (Mayo Clinic)
Local anesthetic and antiarrhythmic. Available only with prescription. …show more content…
Administration route
i. Link to chemical properties: Main focus will be on intravenous injection.
b. Distribution i. Volume of distribution
(Figure 4) (Yuko Ikeda, M.D.) ii. Passage through cell membranes, blood-brain barrier, or placental barrier? Highly soluble in fatty adipose tissues. (National Center)
c. Metabolism
i. Primary metabolites (show structures): (Sigma Aldrich) (Figure 5) ii. Type of modification (oxidation, reduction, hydrolysis, hydration, conjugation): Modification was done to the tertiary amine by reduction. (Sigma Aldrich) iii. Enzymes and organs involved in the metabolism iv. Prodrug? Liver is main route of metabolism. (National Center)
d. Excretion/Elimination i. Route- Is excreted/eliminated through the hepatic route i.e the kidneys. (National Center) ii. Clearance Rate- Clearance-0.64 +/- 0.18 L/min (National Center)
5. Dosage issues
a. Bioavailability: It should be noted that injection is favored for administration because only roughly 35% of the concentration of the drug remains after metabolism through oral ingestion. (National Center)
b. Therapeutic window (efficacy vs. toxicity) - Toxicity can be common if dosing and pharmacokinetic are not monitored carefully. Can cause toxicity in the Central Nervous System. (Yuko Ikeda,