Felodipine

trade names: Plendil, Renedil; drug class: calcium channel blocker; action: inhibits calcium ion influx across cell membrane during cardiac depolarization; produces relaxation of coronary vascular smooth muscle; dilates coronary arteries; decreases SA/AV node conduction; uses: essential hypertension, alone or with other antihypertensives, chronic angina pectoris.

Brand names: Plendil®

Chemical formula:

Español:
• Felodipino, Tableta oral de liberación prolongada

Felodipine Oral tablet, extended-release

What is this medicine?

FELODIPINE (fe LOE di peen) is a calcium-channel blocker. It affects the amount of calcium found in your heart and muscle cells. This relaxes your blood vessels, which can reduce the amount of work the heart has to do. This medicine is used to lower high blood pressure.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•heart problems, low blood pressure, slow or irregular heartbeat
•liver disease
•previous heart attack
•an unusual or allergic reaction to felodipine, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Do not crush or chew. Take this medicine either on an empty stomach or with a light meal. Take your doses at regular intervals. Do not take your medicine more often then directed. Do not suddenly stop taking this medicine. Ask your doctor or health care professional how you can gradually reduce the dose.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•grapefruit juice

This medicine may also interact with the following medications:
•cimetidine
•medicines for fungal infections like fluconazole, itraconazole, ketoconazole, voriconazole
•medicines for high blood pressure
•medicines for seizures like carbamazepine, phenobarbital, and phenytoin
•certain antibiotics like clarithromycin and erythromycin
•some medicines for heart-rhythm problems
•tacrolimus

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular check ups. Check your blood pressure and pulse rate regularly. Ask your health care professional what your blood pressure and pulse rate should be, and when you should contact him or her.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this drug affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can make you more drowsy and dizzy. Avoid alcoholic drinks.

This medicine can cause dental problems for some patients. Clean and floss your teeth carefully and regularly. Check with your dentist if your gums get swollen or inflamed and have the dentist clean your teeth regularly.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•fainting spells, lightheadedness
•irregular heartbeat, chest pain, palpitations
•swelling of the legs and ankles

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•constipation
•decreased sexual function or desire
•facial flushing
•headache
•nausea
•weakness or tiredness

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature below 30 degrees C (86 degrees F). Keep container tightly closed. Protect from light. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Felodipine
Systematic (IUPAC) name
3-ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
Identifiers
CAS number	72509-76-3
ATC code	C08CA02
PubChem	3333
DrugBank	APRD00374
Chemical data
Formula	C18H19Cl2NO4
Mol. mass	383.069 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	>95% [1]
Metabolism	Hepatic
Half life	??
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C(US)
Legal status	℞ Prescription only
Routes	Oral
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Felodipine is a calcium channel blocker (calcium antagonist), a drug used to control hypertension (high blood pressure). It is marketed with the brand name Plendil by AstraZeneca. The formulation patent for the substance expired in 2007.

AstraZeneca dropped Plendil from its support and AZ&Me free Rx access program in October 2008.

Interactions

Recent findings have suggested that felodipine in combination with grapefruit juice can cause toxic effects. Oral administration of felodipine is first metabolized in the gastrointestinal tract and liver by the enzyme CYP3A4. Grapefruit juice contains bergamottin which is found to have an inhibiting effect over this enzyme and as a result the bioavailability of the drug increases, raising the risk for abnormal side effects. ^[2]

References

1. ^ Blychert E. (1992). "Felodipine pharmacokinetics and plasma concentration vs effect relationships". Blood Press Suppl. 2: 1–30. 
2. ^ Jawad Kiani, Sardar Z Imam (October 30 2007). "Medicinal importance of grapefruit juice and its interaction with various drugs". Nutr J. 6 (33): 33. doi:10.1186/1475-2891-6-33. PMID 17971226. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2147024. Retrieved 2008-04-09. 

v • d • e Channel blocker: calcium channel blockers (C08) Selective Dihydropyridines ("-dipine") Amlodipine# • Aranidipine • Azelnidipine • Barnidipine • Benidipine • Cilnidipine • Clevidipine • Efonidipine • Felodipine • Isradipine • Lacidipine • Manidipine • Lercanidipine • Nicardipine • Nifedipine# • Nilvadipine • Nimodipine • Nisoldipine • Nitrendipine • Pranidipine Phenylalkylamines ("-pamil") Gallopamil • Verapamil 1-4 Benzothiazepines ("-tiazem") Diltiazem • Clentiazem Non-selective Fendiline • Bepridil • Lidoflazine • Perhexiline Other/ungrouped Amrinone  • Anandamide  • Anipamil  • Azimilide  • Bencyclane  • Bepridil  • Berbamine  • Bevantolol  • Canadine  • Carboxyamido-Triazole  • Caroverine  • Cinnarizine  • Conotoxins  • Darodipine  • Dauricine  • Devapamil  • Dimeditiapramine  • Dotarizine  • Emopamil  • Enpiperate  • Eperisone  • Falipamil  • Fantofarone  • Fasudil  • Fenamic acid  • Fendiline  • Flunarizine  • Fosfedil  • Gabapentin  • Lamotrigine  • Lidoflazine  • Magnesium sulfate  • Manoalide  • Mepirodipine  • Mibefradil  • Monatepil  • Naftopidil  • Niguldipine  • Niludipin  • Norverapamil  • Ochratoxin A  • Octylonium  • Osthol  • Oxodipine  • Perhexiline  • Pinaverium  • Piperidine  • Pregabalin  • Prenylamine  • Risedronic acid  • Ryodipine  • Sesamodil  • Stepholidine  • Terodiline  • Tetrahydropalmatine  • Tetrandrine  • Tolfenamic acid  • Tranilast #WHO-EM. ‡Withdrawn from market. CLINICAL TRIALS: †Phase III. §Never to phase III

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