Nicardipine hydrochloride
- Drugs List
- Dosage
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Capsules containing 20mg nicardipine hydrochloride
Capsules containing 30mg nicardipine hydrochloride
Drugs List
Dosage
An interval of at least 3 days must be given in between dose increases to allow steady state plasma levels to be achieved.
Adults
Starting dose - 20mg three times a day. Dose can be titrated upwards as needed.
Maintenance dose - 30mg three times a day is usually adequate but doses in the range of 20mg to 40mg three times a day have been used.
Elderly
Titration should be done with care as nicardipine may lower systolic pressure more than diastolic pressure in elderly patients.
Children
Adolescents
Patients with Renal Impairment
Use with caution. Nicardipine blood levels may be elevated in some renally impaired patients. Therefore, start with a low dose and titrate to blood pressure and response. The dose interval may also need to be extended.
The Renal Drug Handbook suggests the following:
Glomerular filtration rate 20 - 50ml/minute: dose as in normal renal function.
Glomerular filtration rate less that 20ml/minute: dose as in normal renal function. Start with low dose.
Patients with Hepatic Impairment
An increased nicardipine half-life has been seen in patients with severe hepatic impairment, therefore using the lowest starting dose or extending the dosing interval should be considered.
Additional Dosage Information
Careful titration is required, especially when given in combination with diuretics or beta-blockers.
When changing therapy from beta-blockers to nicardipine, gradually reduce the beta-blocker over 8 -10 days as calcium antagonists provide no protection against abrupt beta-blocker withdrawal.
Nicardipine may be used in combination with other antihypertensive agents but the additive effects should be considered due to the risk of postural hypotension.
Contraindications
Pregnancy (see Pregnancy section)
Advanced or clinically significant aortic stenosis
Cardiogenic shock
Acute angina attacks
Unstable angina
Within 1 month of myocardial infarction
Porphyria
Children under 18 years
Precautions and Warnings
Careful titration is required, especially when given in combination with diuretics or beta-blockers.
When changing therapy from beta-blockers to nicardipine, gradually reduce the beta-blocker over 8 -10 days as calcium antagonists provide no protection against abrupt beta-blocker withdrawal.
Discontinue in patients who experience ischaemic pain within 30 minutes of starting therapy or increasing the dose. Discontinue if exists ischaemic pain worsens.
There is some evidence that sudden withdrawal of calcium channel blockers may be associated with exacerbation of angina.
Patients with severe left ventricular dysfunction or cardiac failure may experience a worsening of cardiac failure.
Caution should be observed in patients with hypotension or poor cardiac reserve.
The dose should be carefully titrated to avoid the occurrence of systemic hypotension. An exaggerated fall in blood pressure and reflex tachycardia can cause further cardiovascular complications such as myocardial infarction and cerebrovascular ischaemia.
Not suitable for treatment of acute angina attacks in chronically stable angina.
Not suitable for secondary prevention of myocardial infarction. Calcium channel blockers do not reduce the risk of myocardial infarction in unstable angina.
Hepatic impairment - (see Dosage: Patients with Hepatic Impairment).
Renal impairment - (see Dosage: Patients with Renal Impairment).
Elderly - (see Dosage: Elderly).
Breastfeeding - (see Lactation section)
Nicardipine may inhibit labour.
Advise patients not to drive or operate machinery if affected by side effects such as dizziness, lethargy and transient blindness.
Grapefruit products increase the bioavailability of dihydropyridine calcium channel blockers. Patients should be advised to avoid grapefruit products.
Use in Porphyria
ContraindicatedPregnancy and Lactation
Pregnancy
Contraindicated during pregnancy.
Some dihydropyridine compounds have been found to be teratogenic in animals. Dose-related embryotoxicity, but not teratogenicity was observed in reproduction studies using intravenous nicardipine in rats and rabbits. Embryotoxic intravenous doses were about 2.5 and 0.5 times, respectively, the maximum recommended human dose (MRHD). At 50 times the MRHD in rats, dystocia, reduced birth weigh, reduced neonatal survival, and reduced neonatal weight gain were noted. Nicardipine administered intravenously in pregnant rhesus monkeys has been associated with foetal hypoxaemia and acidosis.
There is little experience with the use of nicardipine in human pregnancy. Embryogenesis is a highly calcium-dependent process and experimental findings indicate that early embryonic differentiation can be disturbed by this class of drug. Nicardipine may inhibit labour.
Nicardipine has been used for the treatment of hypertension during pregnancy and as a tocolytic in premature labour. However, the manufacturer states that nicardipine should not be administered during pregnancy. Schaefer comments that tocolysis with calcium antagonist is acceptable when clearly indicated and following a normal course of pregnancy (although caution is required regarding its use simultaneously with magnesium sulfate). Schaefer suggests that if exposure to nicardipine has occurred during the first trimester, a detailed ultrasound diagnosis is advisable. Overall exposure to a calcium antagonist during pregnancy is not an indication for either invasive diagnostic procedures or termination of pregnancy. An alternative drug may be preferred.
The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Recommended for use in pregnancy in manufacturer? - No
Animal data - Nicardipine has been shown to produce embryotoxicity.
Pregnancy-specific adverse effects on the mother - may inhibit labour.
Lactation
Use with extreme caution during breastfeeding.
Levels in human milk are very low. It has been estimated that the relative infant dose is 0.07% of the weight-adjusted maternal dose. No paediatric concerns have been reported from one study.
The manufacturer state that nicardipine should not be administered to nursing mothers. However, other organisations considers nicardipine usually compatible with breastfeeding. Information on LactMed states the because of the low levels of nicardipine in breast milk, amounts ingested by the infant are small and would not be expected to cause any adverse effects in breastfed infants. No special precaution are required. Information from UK Drugs in Lactation Advisory Service states that for nicardipine there is insufficient information relating to breastfeeding to allow classification as a safe drug, however it can be administrated to breastfeeding mothers only where the mother and infant can be monitored. An alternative drug may be preferred.
Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1
Considered suitable by manufacturer? - No
UK Drugs in Lactation Advisory Service Classification - Insufficient information relating to breastfeeding to allow classification as a safe drug.
Drug substance licensed in infants? - No.
Counselling
Advise patient to avoid consuming grapefruit products as they increase the bioavailability of dihydropyridine Ca channel blockers.
Advise patients not to drive or operate machinery if affected by side effects such as dizziness, lethargy and transient blindness.
Side Effects
Headache
Heat sensation
Flushing
Palpitations
Nausea
Aggravation of angina
Drowsiness
Insomnia
Tinnitus
Paraesthesia
Functional disorders
Itching
Rash
Hepatic impairment
Renal impairment
Increased frequency of micturition
Dyspnoea
Gastro-intestinal symptoms
Depression
Impotence
Thrombocytopenia
Peripheral oedema
Hypotension
Tachycardia
Increase in alkaline phosphatase
Serum bilirubin increased
Increase in serum ALT/AST
Increase in serum glucose
Increase in blood urea nitrogen
Increase in creatinine
Dizziness
Myocardial infarction
Lethargy
Eye pain
Visual disturbances
Syncope
Vertigo
Mood changes
Myocardial ischaemia
Cerebral ischaemia
Blindness (temporary)
Fever
Cholestasis
Hypersensitivity reactions
Gingival hyperplasia
Pruritus
Myalgia
Tremor
Gynaecomastia
Migraine
Overdosage
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Shelf Life and Storage
Do not store above 25 degrees C
Reference Sources
British National Formulary, 61st Edition (2011) Pharmaceutical Press, London.
Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 2nd edition (2007) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.
Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 8th edition (2008) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.
Martindale: The Complete Drug Reference, 37th edition (2011) ed. Sweetman, S. Pharmaceutical Press, London.
Medications and Mothers' Milk, 14th Edition (2010) Hale, T. Hale Publishing, Amarillo, Texas.
Summary of Product Characteristics: Cardene 20 and 30mg: Astellas Pharma Ltd. Revised December 2010.
The Renal Drug Handbook. 3rd edition. (2009) ed. Ashley, C and Currie, Radcliffe Publishing Ltd, Abingdon.
National Institute for Health and Clinical excellence (NICE) clinical guidance 107: Hypertension in pregnancy. Issue date August 2010
Available at: https://guidance.nice.org.uk/CG107
Last accessed: August 9, 2011.
UK Drugs in Lactation Advisory Service.
Available at: https://www.ukmicentral.nhs.uk/drugpreg/qrg_p1.asp
Last accessed: August 9, 2011.
US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
Available at: https://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT
Nicardipine. Last revised: December 7, 2010.
Last accessed: August 9, 2011.
Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
FDB Disclaimer : FDB Multilex is intended for the use of healthcare professionals and is provided on the basis that the healthcare professionals will retain FULL and SOLE responsibility for deciding what treatment to prescribe or dispense for any particular patient or circumstance.