Other Definitions
atorvastatin (dict)
Atorvastatin
bgcolor="#ffffff" align="center" colspan="2" |
align="center" colspan="2" |
R*)
-2-(4-fluorophenyl)-beta, delta-dihydroxy-5- (1-methylethyl)-3-phenyl-4-
(phenylamino)carbonyl
-1H- pyrrole-1-heptanoic acid
IUPAC
name
CAS number
134523-00-5
ATC code
C10AA05
bgcolor="#eeeeee" |
Chemical formula
bgcolor="#ddeeff" | (C
33
H
34
FN
2
O
5
)
2
Ca3H
2
O
bgcolor="#eeeeee" |
Molecular weight
bgcolor="#ddeeff" | 1209.42
bgcolor="#eeeeee" |
Bioavailability
bgcolor="#ddeeff" | 12%
bgcolor="#eeeeee" | Metabolism
bgcolor="#ddeeff" |
Liver
bgcolor="#eeeeee" |
Elimination half life
bgcolor="#ddeeff" | 14 hours
bgcolor="#eeeeee" |
Excretion
bgcolor="#ddeeff" |
Bile
bgcolor="#eeeeee" |
Pregnancy category
bgcolor="#ddeeff" | X (
USA
)
D (
Aust
)
bgcolor="#eeeeee" |
Legal status
bgcolor="#ddeeff" | Schedule 4 (
Aust
)
bgcolor="#eeeeee" | Routes of administration
bgcolor="#ddeeff" | oral
In
medicine
and
pharmacology
,
atorvastatin
(
Lipitor®
or atorvastatin
calcium
) is a member of the drug class of
statins
, used for lowering
cholesterol
and thereby preventing
cardiovascular disease
. Atorvastatin inhibits a rate-determining
enzyme
located in hepatic tissue used in cholesterol synthesis, which lowers the amount of cholesterol produced. This also has the effect of lowering the total amount of
LDL cholesterol
. Unlike
simvastatin
and
pravastatin
, atorvastatin is a completely
synthetic
compound. It is currently being marketed by the
pharmaceutical company
Pfizer
as Lipitor.
Available forms
Atorvastatin is available as
Lipitor
in tablet form (10, 20, 40 or 80 mg) for oral administration. Tablets are white, elliptical, and film coated.
Mechanism of Action
Atorvastatin is a competitive
inhibitor
of
HMG-CoA reductase
. This enzyme catalyzes the reduction of
3-hydroxy-3-methylglutaryl-coenzyme A
to
mevalonate
, which is the rate limiting step in hepatic
cholesterol
synthesis. Because cholesterol synthesis decreases, hepatic cells increase the number of LDL receptors on the surface of the cells, which increase the amount of LDL uptake by the hepatic cells, and decreases the amount of LDL in the blood.
References
Lipitor: Prescribing Information.
(2004) Pfizer Ireland Pharmaceuticals.
External links
Manufacturer's site
(lipitor.com)
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