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The monitoring of warfarin and keeping the international normalized ratio (INR) between 2.0 and 3.0, along with avoiding over and under treatment, has driven a search for an alternative. [ 3 ] [ 14 ] A naturally occurring inhibitor of factor Xa was reported in 1971 by Spellman et al. from the dog hookworm. [ 15 ]
Ximelagatran showed good efficacy compared with warfarin in several trials in prevention and treatment of deep vein thrombosis and as thromboprophylaxis in atrial fibrillation. [1] Development was stopped by manufacturer AstraZeneca , however, because of reports of liver enzyme derangements and liver failure .
Vitamin K1-warfarin interaction effect: When warfarin levels are high, people have more risk of bleeding. Conversely, lower levels of warfarin lead to increased risk of blood clots. A narrow range exists where the benefits of warfarin are greater than the risks, its therapeutic window. Certain drugs, herbal medicines, and foods can interact ...
Cardiovascular agents are drugs that affect the rate and intensity of cardiac contraction, blood vessel diameters, blood volume, blood clotting and blood cholesterol levels. [1] They are indicated to treat diseases related to the heart or the vascular system (blood vessels), such as hypertension , hyperlipidemia , coagulation disorders , heart ...
Phenytoin, a CYP2C9 inducer, would increase its activity and the rate of warfarin breakdown, thereby reducing its efficacy. [25] Patients should avoid the co-administration of warfarin and phenytoin. In cases where both drugs must be used together, warfarin dosing may be titrated up to cope with the reduced efficacy. [26]
There can be interactions between the drugs that rely on CYP4F2 on their metabolism or bioactivation (e.g., fingolimod, furamidine, warfarin) [87] [97] and the substances that inhibit or induce CYP4F2 expression, such as statins and peroxisomal proliferators (drugs to lower low-density lipoproteins and reduce risk of risk of cardiovascular ...
The drugs are structurally similar to vitamin K and act as competitive inhibitors of the enzyme. The term "vitamin K antagonist" is a misnomer , as the drugs do not directly antagonise the action of vitamin K in the pharmacological sense, but rather the recycling of vitamin K.
The potency of ticagrelor was brought back to the same level as cangrelor by changing the purine with triazolopyrimidine. The sugar ribose unit was also replaced with a cyclopentyl group to avoid possible instability of the glycosidic bond. The group at the left hand side of the structure was replaced with the sidecain R1.