First-Pass Metabolism

The effect of the first liver passage For a perorally administered pharmaceutical agent to exert its effects at the site of action, it usually must enter the systemic circulation. To do so, it must pass through the intestinal wall, the liver, and part of the circulatory system. Despite complete absorption in the intestine, the bioavailability … First-Pass Metabolism

Ondansetron

Products Ondansetron is commercially available in the form of film-coated tablets, meltable tablets (lingual tablets), as a syrup, and as an infusion/injection preparation. In addition to the original Zofran, generic versions are also available. Ondansetron was introduced in 1991 as the first active ingredient from the group of 5-HT3 receptor antagonists was approved. Structure and … Ondansetron

Antitussives

Products Antitussives are commercially available in the form of tablets, capsules, as cough syrups, and drops, among others. Structure and properties Antitussives do not have a uniform chemical structure. However, many are derived from natural opium alkaloids (opioids). Effects Antitussives have cough-irritating (antitussive) properties. They reduce the frequency and intensity of coughing attacks. Their effects … Antitussives

Metabolism (Biotransformation)

Introduction Biotransformation is an endogenous pharmacokinetic process that leads to a change in the chemical structure of active pharmaceutical ingredients. The organism’s general goal in doing so is to make the foreign substances more hydrophilic and to direct them to excretion via the urine or stool. Otherwise, they could be deposited in the body and … Metabolism (Biotransformation)

Methamphetamine

Products Methamphetamine is no longer registered as a drug in many countries. Pervitin has been out of commerce for some time. Methamphetamine is one of the narcotics and is subject to more stringent prescription requirements, but it is not a banned substance. In principle, medicines could be prepared in pharmacies as a magisterial prescription. In … Methamphetamine

Sorbitol

Products Sorbitol is found alone or in combination with other active ingredients in various laxatives (e.g., Pursana). It is also marketed as an open product and as a solution. Structure and properties Sorbitol (C6H14O6, Mr = 182.2 g/mol) exists as D-sorbitol, a white crystalline powder with a sweet taste that is very soluble in water. … Sorbitol

Cannabidiol

Products In many countries, there are currently no medicines approved that contain only cannabidiol. However, the active ingredient is a component of the cannabis oral spray Sativex, which is registered as a drug for MS treatment in many countries and also contains THC. The oral solution Epidiolex or Epidyolex was approved as a drug in … Cannabidiol

Low-Molecular-Weight Heparins

Products Low-molecular-weight heparins are commercially available as injectable solutions, in the form of prefilled syringes, ampoules, and lancing ampoules. The active ingredients now commonly used in many countries were first approved in the late 1980s. Biosimilars are available in some countries. The active ingredients are abbreviated in English with the acronym LMWH (low molecular weight … Low-Molecular-Weight Heparins

Niflumic Acid

Products There are currently no registered medicines containing niflumic acid in many countries. It is administered in the form of capsules and gel, among others. Structure and properties Niflumic acid (C13H9F3N2O2, Mr = 282.2 g/mol) exists as a pale yellow crystalline powder that is practically insoluble in water. It is an anthranilic acid derivative such … Niflumic Acid

MDEA (Methylenedioxyethylamphetamine)

Products MDEA is one of the narcotics and banned substances in many countries. It is not commercially available. MDEA was first mentioned in the 1970s in the books of Alexander Shulgin. Structure and properties Methylenedioxyethylamphetamine (C12H17NO2, Mr = 207.3 g/mol) is a 3,4-methylenedioxy derivative of an -ethylated amphetamine. It is structurally closely related to ecstasy … MDEA (Methylenedioxyethylamphetamine)

MDPV

Products 3,4-Methylenedioxypyrovalerone (MDPV) is not licensed in many countries. It is one of the prohibited narcotics (d) and is therefore not commercially available. MDPV was developed as a designer drug and was therefore initially available legally in many countries. It was marketed as “bath salts” to give it a legal appearance. Structure and properties MDPV … MDPV