Atorvastatin drug data and news

Atorvastatin drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Atorvastatin
Brand Names/Synonyms Atorvastatin; Atorvastatin Calcium; Atorvastatin Calcium Salt; Atorvastatin, Calcium Salt; CCRIS 7159; CI 981; Cardyl; HSDB 7039; Lipitor; Sotis; Torvast; Tozalip; Xavator
Indication For management as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels in patients with primary hypercholesterolemia and mixed dyslipidemia.
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Description Not Available
Pharmacology Atorvastatin, a selective, competitive HMG-CoA reductase inhibitor, is used to lower cholesterol and triglycerides in patients with hypercholesterolemia and mixed dyslipidemia and in the treatment of homozygous familial hypercholesterolemia. Atorvastatin has a unique structure, long half-life, and hepatic selectivity, explaining its greater LDL-lowering potency compared to other HMG-CoA reductase inhibitors.
Mechanism Of Action Atorvastatin selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. As HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate, this results in a decrease in mevalonate, a precursor of cholesterol, and a subsequent decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol.
Atorvastatin News
(When available)

King Shares Look Unattractive Based On Generic Threats  06 Mar 2006
The analyst noted that King's Sonata sales are being clipped following the launch of Lunesta from Sepracor (nasdaq: SEPR - news - people ) and Ambien CR from ... - Forbes

First-timers face the long red carpet  06 Mar 2006
But on Saturday night, he had trouble sleeping, so he took a few pills and learned something: "Oscar trumps Ambien. I got three hours of sleep.''. ... - Inland Valley Daily Bulletin,

Critics Worry About Sleeping Pills' 'Unknown Risk'  Mar 5, 2006
It's exhausting.". She got a prescription for Ambien, the popular sleeping pill, and immediately began sleeping through the night. ... - ABC News

Sleep aids a booming business  Mar 3, 2006
France's Sanofi-Aventis introduced its Ambien sleeping pill to the United States in 1993 and now dominates the more than $2 billion market for prescription ... - San Francisco Chronicle,

Assessment of Current and Future Opportunities and Threats in the ...  Mar 2, 2006
Until recently, the insomnia market has been dominated by Ambien, Sonata, and Imovane, and the older hypnotics such as benzodiazepines. ... - Genetic Engineering News,

Investors Overly Bullish On Pfizer's Insomnia Drug  Feb 28, 2006
..."Based on the strong market growth driven by Lunesta and Ambien CR, and the Pfizer partnership, we believe the market is overestimating Indiplon's market ... - Forbes

Sleeping pill war will keep you awake  Mar 2, 2006
Ambien, (zolpidem tartrate) the market leader, holds the high ground, selling like hotcakes under the premise that it is "safer" and not dangerously addictive ... - Common Ground.ca,

The Sleep Racket  Feb 28, 2006
Sleeping pills, led by Ambien, rack up more than $2 billion a year in the US Then there is the revenue from overnight stays at sleep clinics, over-the-counter ... - Forbes

Lifestyle changes may be surest path to sleep  Mar 5, 2006
Relatively new prescription drugs like Ambien and Lunesta are generally effective and pose a lower risk of dependency than earlier sleeping pills, researchers ... - San Francisco Chronicle,

Finding solace in second place  Mar 4, 2006
...currently coaching, with six. He must wait another year, but that's not what will keep Drury reaching for Ambien. "It's not about ... - Daily Herald,

Losing Sleep over Money or Money over Sleep? Sleep over It!  Feb 28, 2006
Solutions, Inc. Z pills—like Ambien and Lunesta, are ruling the sleepless , and rendering the drug market alive and kicking. Sleep ... - MedIndia,

Sanofi Aventis "overweight"  Mar 1, 2006
The analyst expects the increased sales of the Ambien franchise to offset any impact of the delay in Acomplia market launch on the 2010 sales. - New Ratings

RECORD SALES OF SLEEPING PILLS ARE CAUSING WORRIES  Feb 7, 2006
...night. And more and more are turning to a new generation of sleep aids like Ambien, the best seller, and its competitor, Lunesta. ... - Amherst Times.com,

Sleep treatments rise to the occasion  Feb 26, 2006
Nardone saw a doctor, who prescribed Ambien for her insomnia. ... Ambien, Lunesta and Sonata are called benzodiazepine-receptor agonists. ... - USA Today

Living Well: Pills are not a sound strategy for insomnia woes  Feb 19, 2006
...airing these days on television. Chances are you have viewed the ads for Ambien or Lunesta or both. They promise a good night's ... - Seattle Post Intelligencer

HealthFirst-Sleeping aids  Feb 20, 2006
...people, Colette tried to fight her sleep trouble by eliminating caffeine, warm tea and a bath before bed., but nothing worked as well as a little pill - Ambien ... - ABC12.com,

Valley of the Dollars  Feb 14, 2006
...to the soothing yet meaningless name.) Currently, about $2.5 billion of sleeping pills are sold in the US each year; almost all of that is Ambien (the numbers ... - CNN/Money

OF HUMAN INTEREST Sleep-starved Americans scramble of solutions  Mar 1, 2006
Ads for prescription sleeping pills such as Ambien and Lunesta have become a familiar presence, particularly in media aimed at women, who studies indicate ... - Indianapolis Star,

Take Home Lunesta Take Home Peaceful Sleep  Feb 9, 2006
Guaranteed Peaceful Sleep with Ambien and Lunesta The new generation sleeping aids like Ambien (the best seller in US) and Lunesta (tough competitor to Ambien ... - LiveArticles.org,

In Life Story of a Gambino Turncoat, Keys to the Gotti Case  Feb 23, 2006
...unable to sleep. A doctor prescribed Zoloft, used to treat depression and panic attacks, and Ambien, for insomnia. After waking ... - New York Times,

Losing money over sleep  Feb 26, 2006
Solutions, Inc. And new prescription sleeping pills—known as Z pills—like Ambien and Lunesta, continue to hit the market. Even ... - Financial Express,

Experts Concerned By Rise In Prescription Sleep Aid Usage  Feb 22, 2006
...night's sleep. We've seen the ads for drugs such as Lunesta and Ambien -- a huge marketing campaign for a variety of sleep drugs. They ... - NewsNet5.com,

Surge in ads drives sales of the latest sleep pills  Feb 7, 2006
And more and more are turning to a new generation of sleep aids like Ambien, the bestseller, and its newest competitor, Lunesta. ... - International Herald Tribune,

Insomnia treatments: a market refusing to lie down  Feb 23, 2006
...period, an increase that will be driven primarily by the launch and continued up-take of Sepracor's Lunesta, Takeda's Rozerem and Sanofi-Aventis' Ambien CR, as ... - Pharmaceutical Business Review

Can a chill really cause a cold?  Feb 21, 2006
The reader who asked the question reported that the Ambien he took helped him get to sleep, though it was a few months beyond its "use by" date. ... - Asbury Park Press,

Concerns Arise Over Sleeping Pills  Feb 7, 2006
...long-term use. More people are also turning to a new generation of sleep aids such as Ambien and Lunestra. Some researchers said ... - Boston Channel.com,

Sleep: Can't get enough of it  Mar 1, 2006
...percent increase from 2004. Ambien, made by Sanofi-Aventis, remains the pill of choice for most Americans. But it's facing stiff ... - San Francisco Chronicle,

Sanofi-Aventis' Battered Charm  Mar 1, 2006
...drug market from Sepracor's (SEPR) 2005 launch of Lunestra and Pfizer's (PFE) planned release of Indiplon will likely affect sales of Sanofi's Ambien sleep aid ... - BusinessWeek

HOME PAGE FOR THE WORLD'S BUSINESS LEADERS  Mar 2, 2006
...immediate problem. This year household names like Zocor, Pravachol, Zoloft and Ambien face generic competition for the first time. Next ... - Forbes

Use of sleep aids becomes prominent  Feb 9, 2006
...company IMS Health. Ambien is the most popular prescribed sleeping pill, but Lunesta is quickly catching up. Drug manufactures spent ... - The Graphic,

Sleep: People Can't Get Enough  Feb 27, 2006
Solutions, Inc. And new prescription sleeping pills -- known as Z pills -- like Ambien and Lunesta, continue to hit the market. Even ... - WTOP,

Microsoft Brings EU Fight to Web  Mar 1, 2006
Instead of Ambien, read this document to get to sleep. The South Korean government wants to chop apart Windows like a brick in a tae kwon do tournament. ... - Redmond,

Acomplia?s Approval Delayed  Feb 27, 2006
...“It may not be as negative as some people are thinking,� he said, noting the example of Ambien CR, which had a delayed approval, but debuted with a ... - PharmExec.com,

Sanofi-Aventis Reports Strong Growth of 25.7% in 2005 Adjusted EPS ...  Feb 24, 2006
...fourth quarter was affected by the introduction of generics of 4 products(2) in the United States -- Significant commercial spend on the launch of Ambien CR(TM ... - International News Service,

Sleep disorders on rise locally, nationally  Feb 18, 2006
Treatment for sleep disorders varies. Some physicians prescribe medications, including Ambien and Lunesta to help patients get a decent night's sleep. ... - Press & Sun-Bulletin,

DATAMONITOR: Insomnia: Costing Sufferers Sleep & Economies Money  Feb 22, 2006
The current market leader is Sanofi-Aventis's Ambien, generating revenues of over $2 billion in 2004**, but it will face competition from generics from 2006 ... - PharmaLive.com (press release),

Parsons sentenced for violating probation  Feb 27, 2006
Friday, Parsons admitted violating the terms of her probation and pleaded guilty to the charge of stealing Ambien and hydrocodone from an elderly lady whom ... - The Capital Journal,

Editorial: Generic approval backlog costing Americans money  Feb 28, 2006
2005. And a number of the most popular drugs, including Zocor, Zoloft and Ambien, will have expired patents in the next four years. ... - Appleton Post Crescent,

The Ten-Point Escape Plan: Taipei  Feb 27, 2006
Plan on a five-day stay, after which it’s an easy jump to other Asian hot spots. 1. Bring some Ambien for the eighteen-hour flight to Taipei. ... - New York Magazine,

Questions about sleeping pill use  Feb 12, 2006
He believes, while most Americans don't get enough sleep, sleeping pills such as Ambien or Lunesta aren't intended for everyone. ... - KVUE (subscription),

New Rochelle nurse sentenced for forging prescriptions  Feb 9, 2006
...and October 1, 2004, Floriano worked as a nurse at a private doctors’ office and forged prescriptions for controlled substances, including Ambien and Codeine ... - Mid-Hudson News,

Health Alert: Sleep aids  Feb 8, 2006
...percent in the past five years. Two drugs in particular, Ambien and Lunesta, have been heavily marketed. Experts like Dr. Charles Bae ... - WIS,

Americans Getting Hooked on Sleeping Pills  Feb 8, 2006
...alone. Experts say ads for drugs like Ambien and Lunesta may be driving people to ask their doctors for the prescriptions. Wilmington ... - WECT,

Here's an image for 2008: Romney vs. Kerry  Feb 14, 2006
Try to cover that on the nightly news. Hold the Ambien. For this race, reality television would have to be recruited to plumb the candidates' souls. ... - The Republican,

More And More People Are Using Sleeping Pills  Feb 7, 2006
Although the newer drugs, like Ambien, are not believed to carry the same risk of dependence as older sleeping pills which contain barbiturates, they still can ... - CBS4Boston,

Sleeping Pill Use on the Rise in the Tennessee Valley  Feb 8, 2006
...center. He says patients having trouble sleeping see him, and automatically ask for brand name pills like Lunesta or Ambien. But ... - WDEF,

Some Doctors Say Americans Take Drugs Too Often  Feb 9, 2006
...like caffeine. Others seem to have just burst on the scene. Lauren Nackman heard about the sleep aid Ambien from friends. She was ... - CBS 13,

Dosage Forms Tablets contain 10, 20, or 40mg atorvastatin
Drug_Category Anticholesteremic Agents; HMG-CoA Reductase Inhibitors; ATC:C10AA05
Absorption Atorvastatin is rapidly absorbed after oral administration. The absolute bioavailability of atorvastatin (parent drug) is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%.
Interactions -->Interactions for Atorvastatin:

The risk of myopathy during treatment with drugs of this class is increased with concurrent administration of cyclosporine, fibric acid derivatives, niacin (nicotinic acid), erythromycin, azole antifungals.

Antacid: When atorvastatin and MaaloxÒ TC suspension were coadministered, plasma concentrations of atorvastatin decreased approximately 35%. However, LDL-C reduction was not altered.

Antipyrine: Because atorvastatin does not affect the pharmacokinetics of antipyrine, interactions with other drugs metabolized via the same cytochrome isozymes are not expected.

Colestipol: Plasma concentrations of atorvastatin decreased approximately 25% when colestipol and atorvastatin were coadministered. However, LDL-C reduction was greater when atorvastatin and colestipol were coadministered than when either drug was given alone.

Cimetidine: Atorvastatin plasma concentrations and LDL-C reduction were not altered by coadministration of cimetidine.

Digoxin: When multiple doses of atorvastatin and digoxin were coadministered, steady-state plasma digoxin concentrations increased by approximately 20%. Patients taking digoxin should be monitored appropriately.

Erythromycin: In healthy individuals, plasma concentrations of atorvastatin increased approximately 40% with coadministration of atorvastatin and erythromycin, a known inhibitor of cytochrome P450 3A4.

Oral Contraceptives: Coadministration of atorvastatin and an oral contraceptive increased AUC values for norethindrone and ethinyl estradiol by approximately 30% and 20%. These increases should be considered when selecting an oral contraceptive for a woman taking atorvastatin.

Warfarin: Atorvastatin had no clinically significant effect on prothrombin time when administered to patients receiving chronic warfarin treatment.

Endocrine Function

HMG-CoA reductase inhibitors interfere with cholesterol synthesis and theoretically might blunt adrenal and/or gonadal steroid production. Clinical studies have shown that atorvastatin does not reduce basal plasma cortisol concentration or impair adrenal reserve. The effects of HMG-CoA reductase inhibitors on male fertility have not been studied in adequate numbers of patients. The effects, if any, on the pituitary-gonadal axis in premenopausal women are unknown. Caution should be exercised if an HMG-CoA reductase inhibitor is administered concomitantly with drugs that may decrease the levels or activity of endogenous steroid hormones, such as ketoconazole, spironolactone, and cimetidine.

CNS Toxicity

Brain hemorrhage was seen in a female dog treated for 3 months at 120 mg/kg/day. Brain hemorrhage and optic nerve vacuolation were seen in another female dog that was sacrificed in moribund condition after 11 weeks of escalating doses up to 280 mg/kg/day. The 120 mg/kg dose resulted in a systemic exposure approximately 16 times the human plasma area-under-the-curve (AUC, 0-24 hours) based on the maximum human dose of 80 mg/day. A single tonic convulsion was seen in each of 2 male dogs (one treated at 10 mg/kg/day and one at 120 mg/kg/day) in a 2-year study. No CNS lesions have been observed in mice after chronic treatment for up to 2 years at doses up to 400 mg/kg/day or in rats at doses up to 100 mg/kg/day. These doses were 6 to 11 times (mouse) and 8 to 16 times (rat) the human AUC (0-24) based on the maximum recommended human dose of 80 mg/day.

CNS vascular lesions, characterized by perivascular hemorrhages, edema, and mononuclear cell infiltration of perivascular spaces, have been observed in dogs treated with other members of this class. A chemically similar drug in this class produced optic nerve degeneration (Wallerian degeneration of retinogeniculate fibers) in clinically normal dogs in a dose-dependent fashion at a dose that produced plasma drug levels about 30 times higher than the mean drug level in humans taking the highest recommended dose.

 

 

Toxicity Rhabdomyolysis, eye hemorrhages, and liver problems.
Organisms Affected Humans and other mammals
Chemical IUPAC Name 7-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl]-3,5-dihydroxy-heptanoicacid
Chemical Formula C33H35FN2O5
Molecular Weight 558.64 g/mol
Smiles String CC(C)C1=C(C(=C(N1CCC(CC(CC(=O)O)O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4
Melting Point 159.2-160.7oC
Water Solubility Sodium salt soluble in water, 20.4ug/ml (pH2.1), 1.23 mg/ml (pH6.0)
State White to off-white crystalline powder.
LogP/Hphobicity 6.259
Isoelectric Point Not Available
Biotransformation Atorvastatin is extensively metabolized to ortho- and parahydroxylated derivatives and various beta-oxidation products. In vitro inhibition of HMG-CoA reductase by ortho- and parahydroxylated metabolites is equivalent to that of atorvastatin. Approximately 70% of circulating inhibitory activity for HMG-CoA reductase is attributed to active metabolites.
Half Life 14 hours
Protein Binding [%] 98%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Atorvastatin.html
http://www.rxlist.com/cgi/generic/atorvastatin.htm
Drug Type Approved Drug
Accession No APRD00055
CAS Registry Number 134523-00-5
KEGG Compound ID C06834
PubChem ID SID:205162
PharmGKB ID PA448500
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2243097

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