Felodipine drug data and news

Felodipine 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 Felodipine
Brand Names/Synonyms AGON SR; Agon; CHEMBANK1781; Dl-Felodipine; FEXOFENADINE HCL; Faropenem; Feloday; Felodipina [Inn-Spanish]; Felodipine; Felodipine [Usan:Ban:Inn]; Felodipinum [Inn-Latin]; Felodur Er; Felogard; Fexofenadine Hydrochloride; Fexofinadine Hcl; Flodil; H 154/82; H-154/82; Hydac; Lexxel; Modip; Munobal; Munobal Retard; Penedil; Perfudal; Plandil; Plendil; Plendil Depottab; Plendil Er; Plendil Retard; Preslow; Prevex; Renedil; Splendil
Indication For the treatment of hypertension
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Description Not Available
Pharmacology Felodipine, 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. Felodipine is similar to other peripheral vasodilators. Felodipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes blocking the calcium channels. 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 Felodipine is Ca++ channel blocker. It reversibly competes with nitrendipine and/or other calcium channel blockers for dihydropyridine binding sites, blocks voltage-dependent Ca++ currents in vascular smooth muscle and cultured rabbit atrial cells, and blocks potassium- induced contracture of the rat portal vein. By blocker the Ca++ channels, Felodipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes and results in a decrease of peripheral vascular resistance.
Felodipine News
(When available)

Reduce platelet aggregation, blood clotting, inflammation, nervous ...  Jan 12, 2006
There might be interactions of coumarins with the calcium channel blocker felodipine (Plendil), a drug used to treat high blood pressure. ... - Health24.com,

Heart medicines cheaper  Nov 30, 2005
...about 4000 patients already took amlodipine – an alternative blood pressure medication for those who did not respond well to the main treatment felodipine. ... - Stuff.co.nz,

Full funding for cardiac treatments  Nov 29, 2005
..."Felodipine is already fully funded and it is likely that most people will continue to be prescribed felodipine if their blood pressure is controlled using it ... - Scoop.co.nz (press release),

AstraZeneca Provides Additional Support to Hurricane Victims  Nov 17, 2005
2.5% and prilocaine 2.5%), FASLODEX® (fulvestrant), NEXIUM® (esomeprazole magnesium), NOLVADEX® (tamoxifen citrate), PLENDIL® (felodipine ER), PULMICORT ... - Yahoo! News (press release)

AstraZeneca Provides Additional Support to Hurricane Victims  Nov 17, 2005
...and prilocaine 2.5%), FASLODEX(R) (fulvestrant), NEXIUM(R) (esomeprazole magnesium), NOLVADEX(R) (tamoxifen citrate), PLENDIL(R) (felodipine ER), PULMICORT ... - PR Newswire (press release),

URL/Mutual Tracking to Achieve Another Record Year in Sales ...  Sep 12, 2005
Contributing to URL/Mutual's successes has been the continued success of Felodipine 2.5mg, 5mg and 10mg ER Tablets (AB-rated to Astra-Zeneca's Plendil ER ... - PR Newswire (press release),

AstraZeneca Pledges More Than $1 Million in Contributions and ...  Sep 1, 2005
2.5% and prilocaine 2.5%), FASLODEX® (fulvestrant), NEXIUM® (esomeprazole magnesium), NOLVADEX® (tamoxifen citrate), PLENDIL® (felodipine ER), PULMICORT ... - Yahoo! News (press release)

AstraZeneca Pledges More Than $1 Million in Contributions and ...  Sep 1, 2005
...and prilocaine 2.5%), FASLODEX(R) (fulvestrant), NEXIUM(R) (esomeprazole magnesium), NOLVADEX(R) (tamoxifen citrate), PLENDIL(R) (felodipine ER), PULMICORT ... - PR Newswire (press release),

Many Filipinos diabetic and hypertensive  Aug 12, 2005
...just approved for the Philippine market is Triapin (manufactured by Sanofi-Adventis), which is a combination of two active ingredients: ramipril and felodipine ... - INQ7 Interactive, Inc.,

Common germ uncommonly causes death  Jun 2, 2005
Overdoing their use can bring on diarrhea. DEAR DR. DONOHUE: The doctor at the Veteran's Administration has prescribed felodipine for my high blood pressure. ... - Yuma Sun,

Grapefruit and Prescription Drugs: Mix Carefully  Mar 29, 2005
...of Western Ontario in London, Ontario, to see whether people needed to stop drinking alcohol while they were taking a drug called felodipine (Plandil), one of ... - Forbes

Dunne maintains PHARMAC attack  Apr 5, 2005
2. Patients prescribed the blood pressure medication felodipine have suffered massive disruptions and uncertainty over the last several years. ... - Scoop.co.nz

Drugs to combat hypertension  Apr 12, 2005
Calcium antagonists are drugs that usually end with the syllable "-pine" like felodipine, nicardipine and nisoldipine. But they are very expensive. ... - Sun Star,

Non-diabetic proteinuric nephropathies, add-on therapy provides no ...  Mar 11, 2005
The patients in intensified blood-pressure control group received add-on therapy with the Felodipine (5-10 mg/day), a calcium-channel blocker. ... - Xagena.it,

Neophyte solon bares drug cartel  Mar 2, 2005
...“Just to give you an idea how successful India is in its national drug policy, an anti-hypertensive drug -- Plendil [Felodipine] tablet 10 milligrams -- the ... - ABS CBN News,

Management of Hypertension in Older Persons  Feb 21, 2005
...making them beneficial in atrial fibrillation and supraventricular tachyarrythmias.22 Dihydropyridines (ie, amlodipine [Norvasc], felodipine [Plendil]) are ... - RedNova.com,

Dosage Forms Oral tablets
Drug_Category Vasodilator Agents; Antihypertensive Agents; Antiarrhythmic Agents; Dihydropyridines; ATC:C08CA02
Absorption 15%
Interactions -->Interactions for Felodipine:

CYP3A4 Inhibitors—Felodipine is metabolized by CYP3A4. Co-administration of CYP3A4 inhibitors (eg, ketoconazole, itraconazole, erythromycin, grapefruit juice, cimetidine) with felodipine may lead to several- fold increases in the plasma levels of felodipine, either due to an increase in bioavailability or due to a decrease in metabolism. These increases in concentration may lead to increased effects, (lower blood pressure and increased heart rate). These effects have been observed with co-administration of itraconazole (a potent CYP3A4 inhibitor). Caution should be used when CYP3A4 inhibitors are co-administered with felodipine. A conservative approach to dosing felodipine should be taken. The following specific interactions have been reported:

Itraconazole—Co-administration of another extended release formulation of felodipine with itraconazole resulted in approximately 8-fold increase in the AUC, more than 6- fold increase in the Cmax, and 2-fold prolongation in the half- life of felodipine.

Erythromycin—Co-administration of felodipine (PLENDIL) with erythromycin resulted in approximately 2.5- fold increase in the AUC and Cmax, and about 2- fold prolongation in the half- life of felodipine.

Grapefruit juice—Co-administration of felodipine with grapefruit juice resulted in more than 2-fold increase in the AUC and Cmax, but no prolongation in the half- life of felodipine.

Cimetidine—Co-administration of felodipine with cimetidine (a non-specific CYP-450 inhibitor) resulted in an increase of approximately 50% in the AUC and the Cmax, of felodipine.

Beta-Blocking Agents— A pharmacokinetic study of felodipine in conjunction with metoprolol demonstrated no significant effects on the pharmacokinetics of felodipine. The AUC and Cmax of metoprolol, however, were increased approximately 31 and 38%, respectively. In controlled clinical trials, however, beta blockers including metoprolol were concurrently administered with felodipine and were well tolerated.

Digoxin— When given concomitantly with PLENDIL the pharmacokinetics of digoxin in patients with heart failure were not significantly altered.

Anticonvulsants— In a pharmacokinetic study, maximum plasma concentrations of felodipine were considerably lower in epileptic patients on long-term anticonvulsant therapy (eg, phenytoin, carbamazepine, or phenobarbital) than in healthy volunteers. In such patients, the mean area under the felodipine plasma concentration-time curve was also reduced to approximately 6% of that observed in healthy volunteers. Since a clinically significant interaction may be anticipated, alternative antihypertensive therapy should be considered in these patients.

Tacrolimus— Felodipine may increase the blood concentration of tacrolimus. When given concomitantly with felodipine, the tacrolimus blood concentration should be followed and the tacrolimus dose may need to be adjusted.

Other Concomitant Therapy— In healthy subjects there were no clinically significant interactions when felodipine was given concomitantly with indomethacin or spironolactone.

Interaction with Food— See CLINICAL PHARMACOLOGY, Pharmacokinetics and Metabolism.

Toxicity excessive peripheral vasodilation with marked hypotension and possibly bradycardia
Organisms Affected Humans and other mammals
Chemical IUPAC Name methylethyl4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
Chemical Formula C18H19Cl2NO4
Molecular Weight 384.253 g/mol
Smiles String CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C
Melting Point 145°C
Water Solubility 19.7 mg/L
State slightly yellowish, crystalline powder
LogP/Hphobicity 4.121
Isoelectric Point Not Available
Biotransformation Hepatic
Half Life 14.1 hours
Protein Binding [%] 99%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Felodipine.html
http://www.rxlist.com/cgi/generic2/felo.htm
Drug Type Approved Drug
Accession No APRD00374
CAS Registry Number 72509-76-3
KEGG Compound ID C06995
PubChem ID SID:189780
PharmGKB ID Not Available
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2222000

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