Zileuton

Products Zileuton is commercially available in the United States in tablet and powder form (Zyflo). It is not currently approved in many countries. Structure and properties Zileuton (C11H12N2O2S, Mr = 236.3 g/mol) is an almost odorless, white, crystalline powder that is practically insoluble in water. It exists as a racemate. Both enantiomers are pharmacologically active. … Zileuton

Prolongation of the QT Interval

Symptoms Drug-induced prolongation of the QT interval can rarely lead to severe arrhythmias. This is polymorphic ventricular tachycardia, known as torsade de pointes arrhythmia. It can be seen on the ECG as a wave-like structure. Due to the dysfunction, the heart cannot maintain blood pressure and can only pump insufficient blood and oxygen to the … Prolongation of the QT Interval

Terfenadine: Effects, Uses & Risks

Terfenadine is an anti-allergic drug and is used to treat allergic reactions. Because it competes for the receptor site for histamine in the human body, the body’s own hormone histamine can no longer dock. Histamine is responsible for allergic symptoms such as itching and redness. Terfenadine is administered in tablet form. It has been withdrawn … Terfenadine: Effects, Uses & Risks

Antihistamines for Allergies

Products Antihistamines are often taken in the form of tablets. In addition, drops, solutions, lozenges, capsules, gels, creams, eye drops, nasal sprays, and injectable solutions are also available, among others. The first active ingredient from this group was phenbenzamine (Antergan), developed in France in the 1940s. It is no longer commercially available today. Structure and … Antihistamines for Allergies

Dronedarone

Products Dronedarone is commercially available in the form of film-coated tablets (Multaq). It was approved in 2009, first in the United States, then in Canada, in many countries, and in November throughout the European Union. Structure and properties Dronedarone (C31H44N2O5S, Mr = 556.76 g/mol) is a benzofuran derivative and an analog of the antiarrhythmic drug … Dronedarone

Fexofenadine

Products Fexofenadine is commercially available in tablet form (Telfast, Telfastin Allergo, generic). It was approved in many countries in 1997 and has been available without a doctor’s prescription since 2010. Telfastin Allergo 120 for self-medication went on sale in February 2011. Fexofenadine is the successor product to terfenadine (Teldane), which had to be withdrawn from … Fexofenadine

Interactions with Grapefruit Juice

Background That grapefruit juice can cause drug-drug interactions was discovered by chance in a clinical trial in 1989 and confirmed in an experiment by the same research group in 1991 (Bailey et al, 1989, 1991). This showed that simultaneous ingestion of grapefruit juice with the calcium channel blocker felodipine significantly increases the bioavailability of felodipine. … Interactions with Grapefruit Juice

Erythromycin

Products Erythromycin is commercially available for peroral administration in tablet and granular form (Erythrocin / Erythrocin ES). This article refers to the drugs intended for ingestion. Erythromycin was first approved in the 1950s. Structure and properties Erythromycin is a natural substance produced by the bacterium (formerly: ). In oral medications, it is present as erythromycin … Erythromycin

Aprepitant

Products Aprepitant is commercially available in the form of capsules (Emend). It has been approved in many countries since 2003. Structure and properties Aprepitant (C23H21F7N4O3, Mr = 534.4 g/mol) is a morpholine and triazol-3-one derivative. It exists as a white crystalline powder that is practically insoluble in water. For intravenous use, the more water-soluble prodrug … Aprepitant

Loratadine

Products Loratadine is commercially available in tablet form (Claritine, Claritine Pollen, generics). It has been approved in many countries since 1991. The active metabolite desloratadine is also available (Aerius, generics). Structure and properties Loratadine (C22H23ClN2O2, Mr = 382.9 g/mol) exists as a white crystalline powder that is practically insoluble in water. It is a prodrug … Loratadine

Terfenadine

Products Terfenadine (Teldane tablets/suspension) is no longer on the market in many countries. Possible alternatives are the successor product fexofenadine (Telfast) or other 2nd generation antihistamines. Structure and properties Terfenadine (C32H41NO2, Mr = 471.7 g/mol) is a racemate. It exists as a white crystalline powder that is very sparingly soluble in water. Terfenadine is a … Terfenadine

Mibefradil

Products Mibefradil (Posicor tablets) was launched in many countries in 1996 and withdrawn from the market in 1998 because of potential interactions. It is no longer commercially available. Structure and properties Mibefradil (C29H38FN3O3, Mr = 495.6 g/mol) is a benzimidazole and a tetralol derivative. It is present in drugs as mibefradildihydrochloride. Effects Mibefradil (ATC C08CX01) … Mibefradil