Lercanidipine Hydrochloride

Registered South African indications:

• Hypertension

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Breastfeeding
• Severe renal impairment
• Severe hepatic impairment
• Left ventricular outflow tract obstruction
• Untreated congestive cardiac failure
• Unstable angina pectoris
• Myocardial infarction <1month
• Women of child-bearing potential unless effective contraception used
• Coadministration with strong CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, ritonavir, erythromycin and fluoxetine)
• Coadministration with ciclosporin
• Coadministration with grapefruit juice
• Since there is no clinical experience in patients under the age of 18 years, use in children is not recommended

Cautions

• Mild to moderate hepatic impairment
• Mild to moderate renal impairment
• Elderly
• Sick sinus syndrome
• Left ventricular dysfunction
• Ischaemic heart disease
• Angina pectoris
• Lapp lactase insufficiency
• Galactosaemia
• Glucose/galactose malabsorption

Forms avail. in SA and covered in this monograph: tab

Essential hypertension - mild and moderate

• Oral (tab): 10-20mg, dly

Wait at least 2 weeks before up-titrating dose

Tablets should be taken at least 15min before meal

Not established for use in children below 18 years (see Contraindications)

Pregnancy

• Contraindicated
• There are no adequate data from the use of lercanidipine in pregnant women. Non-clinical data provide no evidence of a teratogenic effect in the rat and the rabbit and reproductive performance in the rat was unimpaired. Since other dihydropyridine compounds have been found teratogenic in animals, lercanidipine should not be administered during pregnancy or to women with childbearing potential unless effective contraception is used

Breastfeeding

• Contraindicated
• Because of high lipophilicity of lercanidipine, distribution in milk may be expected. Therefore, it should not be administered to breastfeeding mothers

Renal Impairment

• Mild to moderate: Caution; no dose adjustment recommended 
• Severe: Contraindicated

Hepatic Impairment

• Mild-moderate: Caution; no dose adjustment recommended
• Severe: Contraindicated

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Headache
• Dizziness
• Somnolence

Cardiovascular Disorders

• Tachycardia
• Palpitations
• Peripheral oedema
• Angina pectoris
• Chest pain
• Myocardial infarction
• Hypotension
• Flushing

Gastrointestinal Disorders

• Dyspepsia
• Diarrhoea
• Abdominal pain
• Vomiting
• Gingival hypertrophy

Hepatobiliary Disorders

• Raised hepatic transaminases

Genitourinary Disorders

• Polyuria
• Urinary frequency

Musculoskeletal Disorders

• Myalgia

Skin and Subcutaneous Tissue Disorders

• Rash

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity

• CYP3A4 inhibitors
• Ketoconazole
• Itraconazole
• Ritonavir
• Erythromycin
• Fluoxetine
• CYP3A4 inducers
• CYP3A4 substrates
• Ciclosporin
• Grapefruit juice
• Alcohol
• Beta blockers

None routine

Lercanidipine is a calcium antagonist of the dihydropyridine group that inhibits the transmembrane influx of calcium into cardiac and smooth muscle. This has a direct relaxant effect on vascular smooth muscle thus lowering total peripheral resistance. It is devoid of negative inotropic effects due to its high vascular selectivity.

Tablet 10mg

• Lercanidipine Teva 10 (Teva)
• Lertens 10 (Ranbaxy Pharmaceuticals)
• Lerzan 10 (Forrester Pharma)
• Zanidip (Litha Pharma) originator

Tablet 20mg

• Lercanidipine Teva 20 (Teva)
• Lertens 20 (Ranbaxy Pharmaceuticals)
• Lerzan 20 (Forrester Pharma)
• Zanidip (Litha Pharma) originator

COMBINATION PREPARATIONS

Lercanidipine/ Enalapril

Tablet 10mg/10mg

• Zaneril (Litha) originator

Tablet 10mg/20mg

• Zaneril (Litha) originator