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Thrombin demonstrates a high level of allosteric regulation. [2] Allosterism in thrombin is regulated by the exosites 1 and 2 and the sodium binding site. A recent patent review has shown that the general consensus among researchers is that allosteric inhibitors may provide a more regulatable anticoagulant. [3]
Even less safe are drugs such as digoxin, a cardiac glycoside; its therapeutic index is approximately 2:1. [12] Other examples of drugs with a narrow therapeutic range, which may require drug monitoring both to achieve therapeutic levels and to minimize toxicity, include dimercaprol, theophylline, warfarin and lithium carbonate.
Osteoporosis, including drug- and cancer-related osteoporosis, giant cell tumour of bone and hypercalcaemia of malignancies: Hypercholesterolaemia, cataract, urinary retention, hypocalcaemia, osteonecrosis of the jaw and anaphylaxis. Gemtuzumab ozogamicin: IV: CD33 antibody that induces apoptosis of the tagged cell. Acute myeloid leukaemia
Dabigatran etexilate is rapidly absorbed, it lacks interaction with cytochrome P450 enzymes and with other food and drugs, there is no need for routine monitoring and it has a broad therapeutic index and a fixed-dose administration, which is excellent safety compared with warfarin. [4]
Version 3.0 also included drug transporter data, drug pathway data, drug pricing, patent and manufacturing data as well as data on >5000 experimental drugs. Version 4.0 was released in 2014. [ 4 ] This version included 1558 FDA-approved small molecule drugs, 155 biotech drugs and 4200 unique drug targets.
Theophylline, also known as 1,3-dimethylxanthine, is a drug that inhibits phosphodiesterase and blocks adenosine receptors. [1] It is used to treat chronic obstructive pulmonary disease (COPD) and asthma. [2] Its pharmacology is similar to other methylxanthine drugs (e.g., theobromine and caffeine). [1]
Phenytoin has a narrow therapeutic index. Its therapeutic range for both anticonvulsant and antiarrhythmic effect is 10–20 μg/mL. Avoid giving intramuscular formulation unless necessary due to skin cell death and local tissue destruction. Elderly patients may show earlier signs of toxicity.
Afatinib, sold under the brand name Gilotrif among others, is a medication which is used to treat non-small cell lung carcinoma (NSCLC). [2] [3] [4] It belongs to the tyrosine kinase inhibitor family of medications. [5] It is taken by mouth. [5] [1]