Products Azithromycin is commercially available in the form of film-coated tablets, powder for preparation of a suspension, and granules (Zithromax, generic). Furthermore, a granule for the preparation of a sustained-release oral suspension is available (Zithromax Uno). Eye drops have also been released in some countries. Azithromycin has been approved in many countries since 1992. Structure … Azithromycin
Products Risedronate is available as weekly 35 mg tablets and as 30 mg tablets (Actonel, generic). Actonel 5 mg and 75 mg tablets are off-label in many countries. Risedronate has been approved since 2000. Generic versions went on sale in 2012. Structure and properties Risedronate (C7H10NO7P2Na – 2.5 H2O, Mr = 350.1 g/mol) is a … Risedronate
Products Acamprosate is commercially available in the form of enteric-coated film-coated tablets (Campral). The active ingredient has been approved in many countries since 1995. Structure and properties Acamprosate (C5H11NO4S, Mr =181.2 g/mol) is present in drugs as acamprosate calcium, a white powder that is readily soluble in water. It has structural similarities to the neurotransmitter … Acamprosate
Products Entecavir is commercially available as film-coated tablets and as an oral solution (Baraclude). It has been approved in many countries since 2006. Generic versions have been available since 2017. Structure and properties Entecavir (C12H15N5O3, Mr = 277.3 g/mol) is a 2′-deoxyguanosine nucleoside analog. It exists as a white powder that is sparingly soluble in … Entecavir
Products Benzodiazepines are commercially available in the form of tablets, melting tablets, capsules, drops, and injectables, among others (selection). Chlordiazepoxide (Librium), the first benzodiazepine, was synthesized in the 1950s by Leo Sternbach at Hoffmann-La Roche and was launched in 1960. The second active ingredient, the well-known diazepam (Valium), was launched in 1962. Numerous other drugs … Benzodiazepines Effects and Side Effects
Products Caspofungin must be administered as an infusion solution because of its low oral bioavailability (Cancidas, generics). It has been approved in many countries since 2002 and was the first member of the echinocandins. Structure and properties Caspofungin is present in drugs as caspofungin diacetate (C52H88N10O15 – 2C2H4O2, Mr = 1213.42 g/mol), a hygroscopic white … Caspofungin
Products Retigabine was approved in many countries as film-coated tablets since 2011 (Trobalt). In the United States, it is referred to as ezogabine. It was discontinued in 2017. Structure Retigabine (C16H18FN3O2, Mr = 303.3 g/mol) is a carbamate that was developed starting from the analgesic flupirtine. The free primary amino group is -glucuronidated (see below). … Retigabine (Ezogabine)
Products Pasireotide is commercially available as an injectable (Signifor, Signifor LAR). It was approved in the EU and many countries in 2012. Structure and properties Pasireotide (C59H67N9O9, Mr = 1046.2 g/mol) is present in the drug as pasireotide diaspartate or as pasireotide pamoate. It is a cyclohexapeptide and an analog of the hormone somatostatin. Somatostatin … Pasireotide
Products Melatonin receptor agonists are commercially available in tablet and capsule form. Structure and properties Melatonin receptor agonists are structurally derived from and related to the natural hormone melatonin. Effects Melatonin, a sleep hormone produced by the pineal (pineal) gland of the brain from tryptophan, has a central role in the body in regulating the … Melatonin Receptor Agonists
Products Abacavir is commercially available as film-coated tablets and as an oral solution (Ziagen, combination products). It has been approved in many countries since 1999. Generic versions are approved. Structure and properties Abacavir (C14H18N6O, Mr = 286.3 g/mol) is present in drugs, among other forms, as abacavir sulfate, a white crystalline powder that is soluble … Abacavir
Definition and mechanisms A pharmacokinetic booster is an agent that improves the pharmacokinetic properties of another agent. It is a desirable drug interaction It can exert its effects at different levels (ADME): Absorption (uptake into the body). Distribution (distribution) Metabolism and first-pass metabolism (metabolization). Elimination (excretion) Pharmacokinetic enhancers can increase absorption, increase distribution to an … Pharmacokinetic Booster
Products Ambrisentan is commercially available in the form of film-coated tablets (Volibris). It has been approved in many countries since 2008. Generic versions were registered in 2020. Structure and properties Ambrisentan (C22H22N2O4, Mr = 378.4 g/mol) is a dimethylpyrimidine, diphenyl and propionic acid derivative and exists as a white crystalline powder that is practically insoluble … Ambrisentan
