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Baricitinib is a Janus kinase (JAK) inhibitor that reversibly inhibits Janus kinase 1 with a half maximal inhibitory concentration (IC 50) of 5.9 nM and Janus kinase 2 with an IC 50 of 5.7 nM. Tyrosine kinase 2 , which belongs to the same enzyme family, is affected less (IC 50 = 53 nM), and Janus kinase 3 far less (IC 50 > 400 nM).
Half maximal inhibitory concentration (IC 50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC 50 is a quantitative measure that indicates how much of a particular inhibitory substance (e.g. drug) is needed to inhibit, in vitro, a given biological process or biological component by 50%. [1]
Common side effects include joint pain, diarrhea, nausea, headaches, and muscle pains. [5] Serious side effects may include rhabdomyolysis, liver problems, and diabetes. [5] Use during pregnancy may harm the fetus. [5] Like all statins, pravastatin works by inhibiting HMG-CoA reductase, an enzyme found in liver that plays a role in producing ...
Cholesterol absorption inhibitors are known to have a synergistic effect when combined a class of antihyperlipidemics called statins, to achieve an overall serum cholesterol target. For statin-resistant or statin-sensitive populations that are characterized by low one-year compliance rates, such a combination therapy is proving to be especially ...
The ED50 is commonly used as a measure of the reasonable expectancy of a drug effect, but does not necessarily represent the dose that a clinician might use. This depends on the need for the effect, and also the toxicity. The toxicity and even the lethality of a drug can be quantified by the TD 50 and LD 50 respectively. Ideally, the effective ...
Hypercholesterolemia is not a risk factor for mortality in persons older than 70 years and risks from statin drugs are more increased after age 85. [2] Fibrates are indicated for hypertriglyceridemia. Fibrates typically lower triglycerides by 20% to 50%. Level of the good cholesterol HDL is also increased.
However, due to its relatively severe adverse effects in comparison to other statins, its market use was discontinued. [citation needed] The strengths of the available cerivastatin medicine ranged from 0.2 - 0.8 mg, resulting in an actual dose of 1.9 - 13.1 μg/kg body weight for which rhabdomyolysis has been reported. [14]
Ezetimibe/atorvastatin (trade names Liptruzet, Atozet) is a cholesterol lowering combination drug.In the United States, it was approved in May 2013, by the Food and Drug Administration for the treatment of elevated low-density lipoprotein (LDL) in patients with primary or mixed hyperlipidemia as adjunctive therapy to diet. [1]