Products Zolmitriptan is commercially available as film-coated tablets, meltable tablets, and as a nasal spray (Zomig, generics). It has been approved in many countries since 1997. Generic versions entered the market in 2012. Structure and properties Zolmitriptan (C16H21N3O2, Mr = 287.4 g/mol) is an indole and oxazolidinone derivative structurally related to serotonin. It exists as … Zolmitriptan
Products Zopiclone is commercially available in tablet form (Imovane, auto-generics). It has been approved in many countries since 1993. In the United States, the pure -enantiomer eszopiclone is also available (Lunesta). Structure and properties Zopiclone (C17H17ClN6O3, Mr = 388.8 g/mol) is a racemate and belongs to the cyclopyrrolones. It exists as a white to slightly … Zopiclone
Products Dihydropyridines are commercially available in many countries in the form of film-coated tablets, sustained-release tablets, capsules, and injectables. Nifedipine from Bayer (Adalat) was the first active ingredient from this group to enter the market in the mid-1970s. Today, amlodipine (Norvasc, generics) is most commonly prescribed. Structure and properties The name 1,4-dihydropyridines is derived from … Dihydropyridine
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
Definition Accumulation refers to the accumulation of an active pharmaceutical ingredient in the organism during regular drug administration. The term comes from the Latin (to accumulate). It occurs when there is an imbalance between the intake and elimination of the active ingredient. If the dosing interval is too short, too much drug is administered. If … Cumulation
Products Many drugs are available in the form of suppositories. The most commonly administered in the office are acetaminophen suppositories for the treatment of fever and pain in infants and children (photo, click to enlarge). Definition Suppositories are single-dose medicinal preparations with a solid consistency. They usually have an elongated, torpedo-like shape and a smooth … Suppositories (Suppositories)
Definition So-called “creeping in” is a gradual increase in the dose of a drug over days or a few weeks. This is used to slowly accustom the patient to the drug and to test individual tolerability. Creeping in helps to avoid undesirable effects. The target dose may be predefined or determined individually. In the second … Gradual Increase of the Dose of a Drug
Products Transdermal patches are approved as medicinal products. They offer themselves as an alternative to other modes of application such as peroral and parenteral administration. The first products were launched in the 1970s. Structure and properties Transdermal patches are flexible pharmaceutical preparations of varying sizes and thinness that contain one or more active ingredients. They … Transdermal Patches
Products Valaciclovir is commercially available in the form of film-coated tablets (Valtrex, generic). It has been approved in many countries since 1995. Structure and properties Valaciclovir (C13H20N6O4, Mr = 324.3 g/mol) is the ester of the natural amino acid valine and the antiviral drug aciclovir. It is present in drugs as valaciclovir hydrochloride, a white … Valaciclovir
Introduction Elimination is a pharmacokinetic process that describes the irreversible removal of active pharmaceutical ingredients from the body. It is composed of biotransformation (metabolism) and excretion (elimination). The most important organs for excretion are the kidney and the liver. However, drugs can also be excreted through the respiratory tract, hair, saliva, milk, tears, and sweat. … Elimination
Controlled release from the drug The special design of a drug can be used to achieve delayed, prolonged, continuous, and controlled release of the active ingredient over an extended period of time. This allows the timing, location, and rate of release to be influenced. Galenics Sustained-release drugs include sustained-release tablets, sustained-release capsules, sustained-release granules, and … Retardation
Elimination at the kidney The kidneys, along with the liver, play a central role in the elimination of pharmaceutical agents. They can be filtered at the glomerulus of the nephron, actively secreted at the proximal tubule, and reabsorbed at various tubular segments. In renal insufficiency, these processes are impaired. This may result in a renally … Dose Adjustment in Renal Insufficiency
