Pharm Unit 1

Front 1

What is used to treat acetaminophen poisoning?

Back 1

n-acetylcysteine cause restores GSH stores

Front 2

What are some common inhibitors for CYP450s?

Back 2

diltiazam
emycin
fluconazole
grapefruit
ritonavir

Front 3

Drugs that upregulate CYP3A4 may also upregulate the expression of which transport protein?

Back 3

P-gylcoprotein, because P-gp and CYP3A4 have similar tissue distributions and many drugs are substrates of both systems and together they work to prevent accumulation of toxic substances

Front 4

Drugs that affect P-gp can be either substrates or inhibitors, what are some examples?

Back 4

substrates (get transported out): anti-cancer drugs, steroids, protease inhibitors, rifampin, erythromycin, cyclosporin A

inhibitors (allow accumulation in cell): cyclosporin A, tamoxifen, quinidine

Front 5

CYP5?

Back 5

thromboxane A2 synthase, is in the arachidonic acid cascade cyclic pathway, works after COX 1 and 2 which are inhibited by NSAIDS

Front 6

CYP7A?

Back 6

first and rate limiting step of bile acid synthesis

Front 7

CYP8A?

Back 7

prostacyclin synthase (prostaglandin I2), part of regulatory component of hemostasis that opposes CYP5 that makes thromboxane A2

Front 8

CYP11A1?

Back 8

converts cholesterol to pregnenolone, FIRST step in steroid synthesis

defects lead to lack of glucocorticoids, feminization, and hypertension

Front 9

CYP11B1?

Back 9

can make cortisol or corticosterone from their precursors

defects lead to congenital adrenal hyperplase

Front 10

CYP11B2?

Back 10

aldosterone synthase

defects lead to congenital hypoaldosteronism

Front 11

CYP17?

Back 11

two enzymes in one, required for testosterone and estrogen

defects affect pubertal development`

Front 12

CYP19?

Back 12

aromatase that makes estrogen

defect causes lack of estrogen and failure of women to develop at puberty

Front 13

CYP21?

Back 13

steroid hydroxylase

defects cause congenital adrenal hyperplasia due to lack of cotisol synthesis, so its precursor builds up causing excessive androgen synthesis, resulting in virilization

Front 14

CYP51?

Back 14

makes cholesterol from lanosterol

target of triazole and antifungal drugs like ketoconazole

found in M.tuberculosis

Front 15

CYP1A2 induced by what?

Back 15

smoking. and high levels of CYP1A2 linked to colon cancer

Front 16

CYP3A4 substrates induced by?

Back 16

barbiturates
carbamazeine
macrolides
phyenytoin

Front 17

CYP3A4 substrates?

Back 17

-antiarrhythmics, anxiolytics
-oral contraceptives, chemotherapy, HIV Tx, immunosuppression, antihistamines, THC

Front 18

Clinical significance of CYP3A4 substrate induction?

Back 18

LESS EFFECT

Front 19

Acetaminophen poisoning caused by?

Back 19

NAPQI intermediate that normally reacts with glutathione

Front 20

What are common CYP inhibitors?

Back 20

diltiazam
emycin
fluconazole
grapefruit
ritonavir

competitive for enzyme, leave the CYPs inactive, associated with toxicity

Front 21

Pharmacological antagonism?

Back 21

agonist and antagonist compete for same receptor (1 receptor involved)

Front 22

Physiological antagonism?

Back 22

2 agonist bind to 2 different receptors, each agonist elicits physiological response but these responses oppose each other

Front 23

Chemical antagonism?

Back 23

antagonist directly interacts with the agonist (no receptors involved)

ie antacids, or chelating agents

Front 24

Mechanism of action of cholera toxin???

Back 24

modifies Gas subunit by transferring ADP-ribose from NAD to Arginine thus causing inhibition

Front 25

Pertussis toxin mechanism of action?

Back 25

ADP-ribosylates the cysteine residues of Gai/o subunits which then results in blocking of the interaction of the subunit with receptor