Chapter 6 deck 2 Flashcards

1
Q

Among the many reasons for genetic variations, an interesting one that specifically apply for CYP to D6 is

A

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

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2
Q

CYP2D6 and Tamoxifen

A

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

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3
Q

CYP2D6 and opiod analgesics

A

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

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4
Q

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

A

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

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5
Q

CYP 2C9 is the primary route of metabolism for

A

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

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6
Q

Warfarin acts by inhibiting the enzyme

A

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.

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7
Q

Warfarin is available as a racemic mixture, of which the S-enantiomer, which is the more bioactive form, metabolized by

A

CYP to C9.

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8
Q

The presence of CYP to see nine mutations associated with a reduction in the metabolism of

A

S-warfarin

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9
Q

Work remains dosing requirements are lower in patients with

A

CYP2c9*2

CYP2c9*3

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10
Q

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

A

30%

90%

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11
Q

CYP3A4

A

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.

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12
Q

P glycoprotein

A

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.

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13
Q

Differential expression of PGP explain

A

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.

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14
Q

PGP at the site of the GI tract

A

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.

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15
Q

PGP affects

A

the level of digoxin available for absorption and elmination.

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16
Q

If a pgp is administered then blood levels of substrates will

A

rise as seen when quinidine is administered with digoxin

17
Q

Drugs can be categorized as

A

Reversible suicidal inhibitors were PGP. For example calcium channel blockers and high dose steroids are considered as reversible inhibitors of both PGP’s and CYP 450.

18
Q

Grapefruit and ritonavir are

A

Suicidal agents for both PGP and CYP 450, meaning the effect of grapefruit juice will be prolonged, perhaps of the 24 hours

19
Q

The CYP 450 enzyme and families 1 to 3 mediate

A

78% to 80% of all phase I dependent metabolism of clinical use drugs

20
Q

The polymorphic forms of CYP 450s are responsible for

A

The development of a video syncretic ADRs.

21
Q

56% of all drug cited in AR studies are metabolized by

A

Polymorphic phase I enzymes which 86% are P 450s

22
Q

VKORC1

A

An encoding subunit of the vitamin K at the Zide reductase complex, was found to cause a rare syndrome of warfarin resistance. Subsequently the variance have been found to account for much greater fraction variability in warfarin response up to 21%

23
Q

2007 the FDA in the black box warning to carbamazepine recommending testing

A

HLA-B*1502 allele in patients with Asian ancestry for initiating therapy because these patients are at high risk for developing Stevens-Johnson syndrome or toxic epidermal necrolysis.