Chapter 6 deck 2 Flashcards
Among the many reasons for genetic variations, an interesting one that specifically apply for CYP to D6 is
Gene duplication. The name suggests, some necessities, duplication of the illegal coding for 2D six result in increased protein expression or for ultra-rapid metabolism and markedly reduced activity some drugs. The percentage of populations that shows June duplication the CYP to D6 across different countries shown below
CYP2D6 and Tamoxifen
Recently, the normative effects in variable is a forms of CYP 226 have on metabolism and therapeutic efficacy of tamoxifin in some patients have received much attention. With referenct to tamoxifen, the rol of CYP2D6 is not so much the metabolism of this durg as it is to activate it by conversion to endoxifen inside the cell. Parmacogentic vation of CYP2D6 has been shown in clincal trials conduced in the UK an dgermany to lead to veraiabl hearputic otcums in strogen sensitive cnacers
CYP2D6 and opiod analgesics
Opioid analgesics such as coding rely on sips like this one to convert them to their active form, morphine. Genetic polymorphisms of CYP to the six enzyme can greatly alter the effect that coding has on patients who are for metabolize visual Ultram tranquilizers. Ultra metabolize or types we not experience analgesic effect of the drug and normal doses or metabolizes may not be able to convert coatings with active metabolite morphine, thus experience and little or no clinical benefit. Other narcotics that are active when administered to patients they produce effects of asset access road and even lower end of therapeutic dosing
In August 2012 the Food and Drug Administration acknowledged that it was considering the legal codes of coding and some pediatric patients and estimated that
Number of ultra-rapid metabolizes is generally 1 to 7 per 100 people, may be as high as 2100 and some ethnic groups. Consequently in April 2017, the FDA at the black box warning to the drug levels of coding containing cough syrup and pain medications Tina Conine should not be used in children younger than 12 years including a warning for codices and children aged 12 to 18 years obese, have obstructive sleep apnea, severe lung diseases
CYP 2C9 is the primary route of metabolism for
About 100 different drugs in humans. All sums CIP to see nine substances are the most common drugs, such as glipizide, losartan, and celecoxib. Other drug substrates include those of have a narrow therapeutic index, such as phenotoin in the entity regular divisions
Warfarin acts by inhibiting the enzyme
Vitamin K epoxide reductase, which prevents the formation of functional vitamin K. This action in turn inhibits the activation of clotting factors in the letter, causing the anticoagulant effect.
Warfarin is available as a racemic mixture, of which the S-enantiomer, which is the more bioactive form, metabolized by
CYP to C9.
The presence of CYP to see nine mutations associated with a reduction in the metabolism of
S-warfarin
Work remains dosing requirements are lower in patients with
CYP2c9*2
CYP2c9*3
CYP2c9* 2 variant evinces a ___ and a the cyp2c9*3 varriant a ___ reduction in warfarna cleaance resulting in adjusted dose requirements in these patients compared to noncarriers
30%
90%
CYP3A4
Group of Iceland and is responsible for 50% of the metabolism. As I stand in his response (Williams 1:5 the family is in primary care samples of the classes included -azole antifunglas, calcium channel blockers, antihistamines, anticonvulsants, microbials, words.
P glycoprotein
The membrane-bound, ATP dependent transport system responsible for the reflux of a variety of venal bionics from cells the extracellular fluid. This included the ejection of drugs from cells, usually cancer concentration gradients. PGP, also known as multidrug resistance protein is a product of ABCB1 and ABCB4 genes and is a member of the adenosine triphosphate fighting Family Court.
Differential expression of PGP explain
Tissue specific and temporal variations in East looks efficacy in different cells. In fact, chemoresistance than cancer therapeutics is strongly linked with PGP expression, more PGP protein expressed by the so the greater the floats potential of Zeno bionics such as anticancer drugs.
PGP at the site of the GI tract
effluxes hydrophilic drugs out of the cells and inhibts drug absorption throug ht GI tract. As drugs passively diffuse through the GI tract, Pgp pumpms move drugs from the cytoplasmic areas to extracellualr fluid.
PGP affects
the level of digoxin available for absorption and elmination.