Propofol in a modified cyclodextrin formulation: first human study of dose-response with emphasis on injection pain

Crystal B Wallentine1, Noriko Shimode, Talmage D Egan

  • 1Department of Anesthesiology, University of Utah, Salt Lake City, UT, USA.

Anesthesia and Analgesia
|September 6, 2011
PubMed
Abstract

Related Concept Videos

Parenteral Anesthetics: Overview01:24

Parenteral Anesthetics: Overview

Intravenous anesthetics are drugs administered parenterally to induce anesthesia or sedation. Propofol is a widely used agent formulated as a 1% emulsion in soybean oil, glycerol, and egg phosphatide. It induces rapid anesthesia primarily due to its rapid distribution from the bloodstream to target tissues and is metabolized in the liver. However, it can cause significant pain on injection and hypertriglyceridemia. Fospropofol, a water-based prodrug of propofol, lacks these adverse effects.
One-Compartment Open Model for IV Bolus Administration: General Considerations01:19

One-Compartment Open Model for IV Bolus Administration: General Considerations

The one-compartment model is a pharmacokinetic tool that models the body as a single, uniform compartment, facilitating the understanding of drug distribution and elimination. This model is particularly beneficial for intravenous (IV) bolus administration, where the drug rapidly circulates throughout the body.
The drug's presence in the body is defined by an equation representing the difference between the rates of drug entry and exit. Key parameters—elimination rate constant, half-life,...
IV Infusion to Oral Dosing: Conversion Methods01:28

IV Infusion to Oral Dosing: Conversion Methods

The development of extended-release formulations has facilitated the transition from intravenous to oral medication, offering a more convenient and patient-friendly approach to drug administration. This transition, however, requires careful management to ensure that therapeutic drug levels are maintained, preserving efficacy and avoiding adverse effects. Understanding pharmacokinetic principles and dosage calculations is critical during this process.Pharmacokinetics of the...
Drug Delivery: Parenteral Route01:29

Drug Delivery: Parenteral Route

The parenteral route is a critical method of drug administration. It delivers compounds directly into the systemic circulation and bypasses the gastrointestinal tract. This approach is particularly advantageous for drugs that exhibit poor absorption or instability when administered orally.
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
Drug Delivery: Miscellaneous Routes01:22

Drug Delivery: Miscellaneous Routes

Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection,  and rectal administration provide localized effects with reduced toxicity.
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs through the...
Opioid Analgesics: Synthetic and Semisynthetic Opioids01:15

Opioid Analgesics: Synthetic and Semisynthetic Opioids

Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...