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Lipinski's rule of five, also known as Pfizer's rule of five or simply the rule of five (RO5), is a rule of thumb to evaluate druglikeness or determine if a chemical compound with a certain pharmacological or biological activity has chemical properties and physical properties that would likely make it an orally active drug in humans.
In rough terms, drugs with a high lipid solubility (non-polar drugs), low rates of ionization, or low plasma protein binding capabilities have higher volumes of distribution than drugs which are more polar, more highly ionized or exhibit high plasma protein binding in the body's environment.
The polar surface area (PSA) or topological polar surface area (TPSA) of a molecule is defined as the surface sum over all polar atoms or molecules, primarily oxygen and nitrogen, also including their attached hydrogen atoms. PSA is a commonly used medicinal chemistry metric for the
As the evidence and consensus for use of the drug increases and strengthens, its class of indication is improved. [6] Preferred drugs (and other treatments) are also referred to a "first line" or "primary" while others are called "second line", "third line" etc. [7] [8] A drug may be indicated as an "adjunct" or "adjuvant", added to a first ...
The effect of non-depolarizing neuromuscular-blocking drugs may be reversed with acetylcholinesterase inhibitors, neostigmine, and edrophonium, as commonly used examples. Of these, edrophonium has a faster onset of action than neostigmine, but it is unreliable when used to antagonize deep neuromuscular block. [ 29 ]
When used appropriately, formularies can help manage drug costs imposed on the insurance policy. [7] However, for drugs that are not on formulary, patients must pay a larger percentage of the cost of the drug, sometimes 100%. Formularies vary between drug plans and differ in the breadth of drugs covered and costs of co-pay and premiums.
The features need to match different chemical groups with similar properties, in order to identify novel ligands. Ligand-receptor interactions are typically "polar positive", "polar negative" or "hydrophobic". A well-defined pharmacophore model includes both hydrophobic volumes and hydrogen bond vectors.
Non-depolarizing drug Atracurium: Atracurium is commonly associated with histamine-related symptoms, most notably flushing and erythema . [ 25 ] Less commonly seen adverse effects include urticaria , hypotension , wheezing, tachycardia , bronchospasm , dyspnea , bradycardia, and laryngospasm. [ 4 ]