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Pharmacokinetic Considerations for Moderate and Deep Sedation
Daniel E. Becker DDS
Article Category: Research Article
Volume/Issue: Volume 58: Issue 4
Online Publication Date: Jan 01, 2011
DOI: 10.2344/0003-3006-58.4.166
Page Range: 166 – 173

individuals and clinical situations. Most sedative agents can calm and sedate patients adequately, provided a sufficient concentration is achieved within the targeted neural tissues. An understanding of the challenge of achieving an effective but safe drug concentration in the brain rests on an appreciation of fundamental principles of pharmacokinetics. Pharmacodynamic issues, drug actions and effects, will be the topic of a subsequent continuing education article. Pharmacokinetic processes include drug absorption, biotransformation (metabolism), distribution, and

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Pharmacokinetics of Lidocaine With Epinephrine Following Local Anesthesia Reversal With Phentolamine Mesylate
Paul A. Moore DMD, PhD, MPH,
 Elliot V. Hersh DMD, MS, PhD,
 Athena S. Papas DMD, PhD,
 J. Max Goodson DDS, PhD,
 John A. Yagiela DDS, PhD,
 Bruce Rutherford DDS, PhD,
 Seigried Rogy PhD, and
 Laura Navalta MS
Article Category: Research Article
Volume/Issue: Volume 55: Issue 2
Online Publication Date: Jan 01, 2008
DOI: 10.2344/0003-3006(2008)55[40:POLWEF]2.0.CO;2
Page Range: 40 – 48

of the pharmacokinetics of lidocaine and phentolamine was performed. This article describes the pharmacokinetics of phentolamine following administration of intraoral and intravenous injections. Additionally, the effects of phentolamine mesylate reversal on the pharmacokinetics of lidocaine with epinephrine when administered for maxillary and mandibular local anesthesia were evaluated. Methods This was a single-center, open-label, 4-treatment, phase 1 crossover study designed and statistically powered to evaluate the pharmacokinetics of

Figure 1.; Pharmacokinetic considerations. The concentration of drug at the target tissue is determined by combined influences of absorption, metabolism, distribution, and elimination (excretion). Notice obstacles to bioavailability (serum concentration) following oral and intramuscular administration compared to those following intravenous administration.
Daniel E. Becker
Figure 1.
Figure 1.

Pharmacokinetic considerations. The concentration of drug at the target tissue is determined by combined influences of absorption, metabolism, distribution, and elimination (excretion). Notice obstacles to bioavailability (serum concentration) following oral and intramuscular administration compared to those following intravenous administration.

Figure 5.; Pharmacokinetic compartments. Following an intravenous bolus, drug introduced into the bloodstream (central compartment) distributes into peripheral tissues (peripheral compartment). In the three-compartment model these tissues are divided into those highly perfused (shallow) and less perfused (deep). As the serum concentration declines due to distribution or elimination, drug in the peripheral compartments will equilibrate by redistribution into the central compartment. The time-concentration curve illustrates the decline in serum concentration attributable to rapid distribution into highly perfused tissues, intermediate distribution to less perfused tissues, and a slow decline due to drug elimination.
Daniel E. Becker
Figure 5.
Figure 5.

Pharmacokinetic compartments. Following an intravenous bolus, drug introduced into the bloodstream (central compartment) distributes into peripheral tissues (peripheral compartment). In the three-compartment model these tissues are divided into those highly perfused (shallow) and less perfused (deep). As the serum concentration declines due to distribution or elimination, drug in the peripheral compartments will equilibrate by redistribution into the central compartment. The time-concentration curve illustrates the decline in serum concentration attributable to rapid distribution into highly perfused tissues, intermediate distribution to less perfused tissues, and a slow decline due to drug elimination.

Drug Therapy in Dental Practice: General Principles
Daniel E. Becker DDS
Article Category: Research Article
Volume/Issue: Volume 53: Issue 4
Online Publication Date: Jan 01, 2006
DOI: 10.2344/0003-3006(2006)53[140:DTIDPG]2.0.CO;2
Page Range: 140 – 146

Pharmacokinetic processes are major determinants of the intensity and duration of a drug's effect. The clinician's primary consideration when administering a drug is bioavailability. This refers to the fraction of an administered dose that reaches the systemic circulation or targeted tissue in active form. A drug administered topically on a mucosal lesion or one injected intravenously (IV) will be 100% bioavailable, but a number of variables may reduce the bioavailability of a drug administered by other routes. ABSORPTION

Epinephrine Affects Pharmacokinetics of Ropivacaine Infiltrated Into Palate
Mikiko Yamashiro DDS, PhD,
 Shuichi Hashimoto PhD,
 Asako Yasuda DDS, PhD, and
 Katsuhisa Sunada DDS, PhD
Article Category: Research Article
Volume/Issue: Volume 63: Issue 2
Online Publication Date: Jan 01, 2016
DOI: 10.2344/0003-3006-63.2.71
Page Range: 71 – 79

palatal mucosa, including the injection site. It is reported that the addition of 5 μg/mL epinephrine to ropivacaine improves the anesthetic efficacy and duration of maxillary infiltration anesthesia. 6 However, there is no report demonstrating how epinephrine influences the efficacy of oral infiltration anesthesia with ropivacaine. We hypothesized that epinephrine affects the pharmacokinetics of ropivacaine by retaining ropivacaine in the mucosa of the injected area. The authors investigated the hypothesis using the time-dependent distribution of ropivacaine in the

Optimal Timing of Intravenous Acetaminophen Administration for Postoperative Analgesia
Maho Shinoda DDS,
 Akiko Nishimura DDS, PhD,
 Erika Sugiyama PhD,
 Hitoshi Sato PhD, and
 Takehiko Iijima DDS, PhD
Article Category: Research Article
Volume/Issue: Volume 69: Issue 2
Online Publication Date: Jul 18, 2022
DOI: 10.2344/anpr-69-02-05
Page Range: 3 – 10

plasma concentration is not considered to be an effect site. This hypothesis is supported by the measurement of APAP concentrations in cerebrospinal fluid after intravenous (IV) administration in children and adults. 10 , 11 Based on these findings, the administration of APAP 1 to 2 hours before anticipated pain and fever has been recommended in children. 12 Although the early administration of APAP is recommended for the purpose of postoperative analgesia, pharmacokinetic and pharmacodynamic studies of APAP and its exerted effect on postoperative pain are rare. The

The Local Pharmacokinetics of 3H-Ropivacaine and 14C-Lidocaine After Maxillary Infiltration Anesthesia in Rats
Hiromi Kimi DDS, PhD,
 Mikiko Yamashiro DDS, PhD, and
 Shuichi Hashimoto PhD
Article Category: Research Article
Volume/Issue: Volume 59: Issue 2
Online Publication Date: Jan 01, 2012
DOI: 10.2344/11-14.1
Page Range: 75 – 81

Figure 1.; Drug absorption. Following oral (PO) or topical administration, a drug requires lipid solubility in order to diffuse through the epithelium to reach the capillaries. When administered by intramuscular (IM) or subcutaneous (SC) injection, lipid solubility is not required to reach the capillaries. Once absorbed following PO administration, a drug must travel through the portal system to liver before reaching systemic circulation (venae cavae). See text for further explanation.
Daniel E. Becker
Figure 1.
Figure 1.

Drug absorption. Following oral (PO) or topical administration, a drug requires lipid solubility in order to diffuse through the epithelium to reach the capillaries. When administered by intramuscular (IM) or subcutaneous (SC) injection, lipid solubility is not required to reach the capillaries. Once absorbed following PO administration, a drug must travel through the portal system to liver before reaching systemic circulation (venae cavae). See text for further explanation.

Figure 2.; Drug distribution. Drug molecules (D) circulate in blood stream unbound and bound to plasma proteins. Only unbound drug is free to distribute into tissues. Systemically, distribution is a simple matter of diffusion through the loosely-joined endothelium of the capillaries. Distribution to the brain requires lipid solubility because the capillary endothelium is tightly bound and wrapped with astrocytes.
Daniel E. Becker
Figure 2.
Figure 2.

Drug distribution. Drug molecules (D) circulate in blood stream unbound and bound to plasma proteins. Only unbound drug is free to distribute into tissues. Systemically, distribution is a simple matter of diffusion through the loosely-joined endothelium of the capillaries. Distribution to the brain requires lipid solubility because the capillary endothelium is tightly bound and wrapped with astrocytes.