felodipine (Cabren, Cardioplen XL, Felendil XL, Felogen XL, Felotens XL, Keloc SR, Neofel XL, Plendil, Renedil, Vascalpha)

Dosing and uses of Cabren, Cardioplen XL (felodipine)

• Adult
• Pediatric
• Geriatric

 

Adult dosage forms and strengths

tablets, extended release

• 2.5mg
• 5mg
• 10mg

 

Hypertension

Initial 2.5-5 mg PO qd

Maint: 2.5-10 mg PO qD; some recommend up to 20 mg/day

 

Hepatic Impairment

Initial: 2.5 mg PO qd

 

Other Indications & Uses

Off-label: congestive heart failure, angina

Good choice in hyperlipidemia patients

 

Pediatric dosage forms and strengths

tablets, extended release

• 2.5mg
• 5mg
• 10mg

 

Hypertension (Off-label)

Initial 2.5 mg PO qD; no more than 10 mg PO qd

 

Other Indications & Uses

Safety & efficacy not established

 

Geriatric dosage forms and strengths

Initial dose: 2.5 mg PO qD; dosage should be adjusted according to patient response, and any increase made at intervals of at least 2 weeks.

Maximum dosage is 10 mg PO once daily.

 

Cabren, Cardioplen XL (felodipine) adverse (side) effects

>10%

Headache (11-15%)

 

1-10%

Peripheral edema (2-17%)

Flushing (4-7%)

Dizziness (1.1-3.4%)

Tachycardia (0.4-2.5%)

 

Frequency not defined

Gingival hyperplasia

Rash

Upper respiratory infection

 

Warnings

Contraindications

Hypersensitivity

 

Cautions

CHF, aortic stenosis, hypotension (initially or after dose increases), persistent progressive dermatologic rxns, exacerbation of angina (during initiation of tx, after dose incr, or withdrawal of beta blocker), liver impairment

Pts w/ heart failure or compromised ventricular function (especially with beta blocker)

Avoid taking with grapefruit juice

Sustained release product

 

Pregnancy and lactation

Pregnancy category: C

Lactation: excretion in milk unknown/not recommended

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Cabren, Cardioplen XL (felodipine)

Half-Life: 10-16 hr

Onset: 2-5 hr

Duration: 24 hr

 

Peak Plasma Time: 2-5 hr

Tx range: 4-6 nmol/L

Toxic range: >30 nmol/L

 

Excretion

Urine: 37%

Feces: 10%

 

Other Information

Bioavailability: 20%

Protein Bound: 99%

Vd: 10 L/kg

Metabolism: hepatic P450 enzyme CYP3A4

Metabolites: pyridine analog (inactive)

Clearance: 823 mL/min

Dialyzable: HD: no

 

Mechanism of action

Ca channel blocker: inhibits transmembrane influx of extracellular Ca ions across myocardial & vascular smooth muscle cell membranes, without changing serum calcium concentrations, resulting in inhibition of cardiac & vascular smooth muscle contraction, thereby dilating main coronary & systemic arteries

Produces vasodilation and decreases peripheral resistance