Pharmacology: Nisoldipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nisoldipine is similar to other peripheral vasodilators. Nisoldipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Mechanism Of Action: By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nisoldipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Drug Category: Vasodilator Agents; Antihypertensive Agents; ATC:C08CA07
Interactions:
DrugBank: Interactions for Nisoldipine
Interactions for Nisoldipine:
A 30 to 45% increase in AUC and Cmax of nisoldipine was observed with concomitant administration of
cimetidine 400 mg twice daily. Ranitidine 150 mg twice daily did not interact significantly with nisoldipine (AUC was
decreased by 15-20 %). No pharmacodynamic effects of either histamine H2 receptor antagonist were
observed.
Coadministration of phenytoin with 40 mg SULAR tablets in epileptic patients lowered the nisoldipine plasma
concentrations to undetectable levels. Coadministration of SULAR with phenytoin or any known CYP3A4 inducer should be
avoided and alternative antihypertensive therapy should be considered. Pharmacokinetic interactions between
nisoldipine and beta-blockers (atenolol, propranolol) were variable and not significant. Propranolol attenuated the
heart rate increase following administration of immediate release nisoldipine. The blood pressure effect of SULAR
tended to be greater in patients on atenolol than in patients on no other antihypertensive therapy. Quinidine at 648
mg bid decreased the bioavailability (AUC) of nisoldipine by 26%, but not the peak concentration. The immediate
release, but not the coat-core formulation of nisoldipine increased plasma quinidine concentrations by about 20%.
This interaction was not accompanied by ECG changes and its clinical significance is not known. No significant
interactions were found between nisoldipine and warfarin or digoxin.
Chemical IUPAC Name: methyl2-methylpropyl2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Chemical Formula: C20H24N2O6
Half Life: 7-12 hours
Drug Type: Approved Drug
# Accession No: APRD00635
CAS Registry Number: 63675-72-9
Nisoldipine News (When available)
Pfizer’s Norvasc minimizes risk of heart attack, stroke ...Dec 19, 2005 Vanguard, ...amongst patients with high blood pressure and additional cardiovascular risk factors who received a treatment regimen based on Norvasc (amlodipine besylate ...
DemiDose(TM) Pill Splitter Allays Concern Over Dose Accuracy in ...Jan 11, 2006 PR Newswire (press release), ...splits many of the highest priced brand name prescription pharmaceutical tablets, eg, Cialis(R), Fosamax(R), Levitra(R), Lipitor(R), Norvasc(R), Viagra(R ...
Generics bolster drugstore profitsJan 15, 2006 Fort Wayne Journal Gazette, Lehman says the pharmaceutical industry will lose an additional $14.9 billion to generics next year, lead by Pfizer Inc.’s blood pressure drug Norvasc. ...
Seniors aided in Medicare drug plan changesJan 7, 2006 Detroit Free Press, And he ran out of his blood-pressure medicine, Norvasc, earlier this week. ... The cash price for 30 Norvasc tablets is about $50. He can't afford that, either. ...
Pfizer to pay $1.3bn for control of diabetes drugJan 13, 2006 MSN Money The company faces about $14bn worth of lost sales over several years because of patent expiries on other key drugs, including Zoloft, Zithromax and Norvasc. ...
Dr Reddy’s to 'lick' US patentsJan 4, 2006 Financial Express, One is a variation of Pfizer Inc.'s $3.6 billion-a-year hypertension drug Norvasc, in which it changed a salt in the composition. ...
Pfizer gets in another blockbusterDec 22, 2005 Business Standard, Caduet, a new generation cardiovascular drug, is a combination of Lipitor (atorvastatin calcium) and Norvasc (amlodipine besylate) — the two leading ...
Coroner calls for better drug paper trailJan 9, 2006 Toronto Star, Grey market would mean the Norvasc, used to treat high blood pressure and angina, was real, Pfizer-made medication but meant for another market. ...
Chief Coroner makes recommendations resulting from investigation ...Jan 9, 2006 Canada NewsWire (press release), The Office of the Chief Coroner has issued six recommendations after reviewing the deaths of 11 Hamilton patients for whom the drug Norvasc (amlodipine) had ...
Advair may get a stronger warning labelJan 11, 2006 Daily Press, ...our medicines. I take Lipitor for cholesterol, Norvasc, Altace and Toprol-XL for high blood pressure and Actos for diabetes. My ...
Lipitor Patent Win Boosts Pfizer SharesDec 22, 2005 Leading The Charge, Pfizer is losing patent protection on several important products including antidepressant Zoloft, antibiotic Zithromax and blood pressure medicine Norvasc. ...
Coroner wants action to stop fake drugsJan 9, 2006 Hamilton Spectator (subscription), ...grey-market pills. Grey market would mean the Norvasc was real, Pfizer-made medication but meant for another market. Detective Joe ...
Drug Prices in Medicare Plans are 48% Higher Than Veterans' PricesDec 22, 2005 Common Dreams (press release), Norvasc (5 mg., calcium channel blocker): lowest VA price is $301.68; lowest Medicare plan price is $458.88 - a difference of $157.20, or 52.1 percent. ...
In fine healthJan 8, 2006 Business Standard, ...challenge strategy was in March 2004, when the US FDA barred it from launching the generic version of Pfizer’s anti-hypertension drug Norvasc before the ...
Net druggists await impact of new US drug planJan 1, 2006 CTV.ca, RCMP raided King West Pharmacy last fall and charged a former part-owner with 11 offences related to the alleged sale of counterfeit heart medication, Norvasc. ...
Ages change for assistanceJan 6, 2006 Scottsboro Daily Sentinel, Senior Rx often helps facilitate savings for the purchase of drugs like Celebrex, Mobic, Toprol, Norvasc, Nexium, and Prevacaid. ...
Pfizer struggles as generics pummel its drugsJan 6, 2006 Pittsburgh Post Gazette, ...protection on its huge-selling antibiotic Zithromax in November, and will lose its antidepressant Zoloft this year and blood-pressure pill Norvasc in 2007. ...
The 14 Worst Corporate EvildoersJan 3, 2006 Axis of Logic, In addition to Viagra, Zoloft, Zithromax and Norvasc, Pfizer produces the HIV/AIDS-related drugs Rescriptor, Viracept and Diflucan (fluconazole). ...
The People's PharmacyJan 1, 2006 Seattle Times, Q: My job was outsourced last year, and I lost my health coverage. I take Lipitor, Norvasc, Altace, Toprol-XL and Actos. My wife takes Fosamax and Aciphex. ...
Medicare drug plans much costlier than VA drugsJan 4, 2006 Rock River Times, ...higher. Norvasc, 5 mg., calcium channel blocker, VA: $301.68; Medicare: $458.88, a difference of $157.20 or 52.1 percent higher. ...
Generic drugs help bolster chain profitsJan 8, 2006 MLive.com, Lehman says the pharmaceutical industry will lose another $14.9 billion to generics next year, lead by Pfizer Inc.'s blood pressure drug Norvasc.
Drug's patent win heartens PfizerDec 18, 2005 Australian, ...faces about $US14 billion worth of lost sales over the period of a few years due to patent expiries on other key drugs, including Zoloft, Zithromax and Norvasc ...
Courtroom lotteryDec 19, 2005 Business Standard, ...in 2002 and when the US federal drug administration ruled against the company launching the generic version of the anti-hypertension drug, Norvasc, in 2004. ...
Viagra debuts in India at Rs 463Dec 20, 2005 Financial Express, Caduet was launched in the global market in January 2004, and is a dual combination of Norvasc and Lipitor, and treats both high blood pressure and high ...
Matthew Herper On The Drug IndustryDec 27, 2005 Forbes With big-selling drugs such as Pfizer’s Norvasc for high blood pressure and Merck's (nyse: MRK - news - people ) Zocor for elevated cholesterol going generic ...
Ranbaxy: Courting troubleDec 19, 2005 Business Standard, ...in March quarter 2004, too, the USFDA had also barred Dr Reddy’s from launching the generic version of Pfizer’s anti-hypertension drug Norvasc, before the ...
Medicare Part D available starting Jan. 1Dec 26, 2005 Saipan Tribune, Part D that a patient may expect to pay-in addition to the $30 per month premium-are $26 per prescription for common drugs such as Lipitor and Norvasc and up ...
VA prescription drugs a bargain vs. MedicareDec 23, 2005 Mohave Valley News, Norvasc, a calcium channel blocker, costs $301 under the VA plan, while it costs $458 under Medicare, a difference of 52 percent. ...
End to patents means major headache for drug makersDec 23, 2005 The Journal News.com, ...a third of its total revenue over the next three years from the expiration of patents on Zoloft and other drugs, including its heart drug Norvasc, according to ...
New drug launches flood CVD marketDec 26, 2005 Financial Express, DCGI). The drug is a combination of two of Pfizer’s blockbusters, Lipitor (atorvastatin calcium) and Norvasc (amlodipine besylate). ...
First Horizon, Bayer Expand ContractJan 9, 2006 MSN Money ...said Monday that the company and Bayer AG Bayer AG agreed to expand their agreement for the Sular high blood pressure medication. ...
First Horizon Continues to Grow Its Partnership with Bayer ...Jan 9, 2006 PharmaLive.com (press release), ...for Federal programs to increase sales; foreign currency exchange rate protection; and the opportunity for expanded international distribution rights for Sular ...
Business news briefs: 1/11/06Jan 10, 2006 Pittsburgh Post Gazette, ...of Alpharetta, Ga., amended their agreement through which Bayer manufactures First Horizon's Sular prescription high blood pressure medication. ...
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