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Components:
Felodipine
Method of action:
Antianginal, Antihypertensive, Calcium Channel Blocking, Hypotensive
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Medically reviewed by Militian Inessa Mesropovna, PharmD. Last updated on 2020.01.20

Qualitative and quantitative composition

Felodipine

Therapeutic indications

The information provided in Therapeutic indications of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Therapeutic indications in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Modified-release tablet; Prolonged-release tablet; Tablets of prolonged action, coated; Tablets of prolonged action, film-coated
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Hypertension

Stable angina pectoris

- Essential hypertension

- Stable angina pectoris

Dosage (Posology) and method of administration

The information provided in Dosage (Posology) and method of administration of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Dosage (Posology) and method of administration in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Modified-release tablet; Prolonged-release tablet; Tablets of prolonged action, coated; Tablets of prolonged action, film-coated
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Posology

Hypertension

The dose should be adjusted individually. Treatment can be started with 5 mg once daily. Depending on the patient's response, the dosage can, where applicable, be decreased to 2.5 mg or increased to 10 mg daily. If necessary another antihypertensive agent may be added. The standard maintenance dose is 5 mg once daily.

Angina pectoris

The dose should be adjusted individually. Treatment should be initiated with 5 mg once daily and, if needed, increased to 10 mg once daily.

Elderly population

Initial treatment with lowest available dose should be considered.

Renal impairment

Dose adjustment is not needed in patients with impaired renal function.

Hepatic impairment

Patients with impaired hepatic function may have elevated plasma concentrations of felodipine and may respond to lower doses.

Paediatric population

There is limited clinical trial experience of the use of felodipine in hypertensive paediatric patients.

Method of administration

The tablets should be taken in the morning and be swallowed with water. In order to keep the prolonged-release properties, the tablets must not be divided, crushed or chewed. The tablets can be administered without food or following a light meal not rich in fat or carbohydrate.

Posology

Hypertension

The dose should be adjusted individually. Treatment can be started with 5 mg once daily. Depending on the patient's response, the dosage can, where applicable, be decreased to 2.5 mg or increased to 10 mg daily. If necessary another antihypertensive agent may be added. The standard maintenance dose is 5 mg once daily.

Angina Pectoris

The dose should be adjusted individually. Treatment should be initiated with 5 mg once daily and, if needed, increased to 10 mg once daily.

Elderly

Initial treatment with lowest available dose should be considered.

Renal impairment

Dose adjustment is not needed in patients with impaired renal function.

Hepatic impairment

Patients with impaired hepatic function may have elevated plasma concentrations of Keydipin and may respond to lower doses.

Paediatric population

There is limited clinical trial experience of the use of Keydipin in hypertensive paediatric patients.

Method of administration

The tablets should be taken in the morning and be swallowed with water. In order to keep the prolonged-release properties, the tablets must not be divided, crushed or chewed. The tablets can be administered without food or following a light meal not rich in fat or carbohydrate.

Note: Other medicinal products may be available for the starting dose of 2.5 mg Keydipin, as Vascalpha (Keydipin) prolonged release tablets is not available in this strength.

Contraindications

The information provided in Contraindications of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Contraindications in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Modified-release tablet; Prolonged-release tablet; Tablets of prolonged action, coated; Tablets of prolonged action, film-coated
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- Pregnancy

-

- Decompensated heart failure

- Acute myocardial infarction

- Unstable angina pectoris

- Haemodynamically significant cardiac valvular obstruction

- Dynamic cardiac outflow obstruction

- Decompensated heart failure

- Acute myocardial infarction

- Unstable angina pectoris

- Haemodynamically significant cardiac valvular obstruction

- Dynamic cardiac outflow obstruction

Special warnings and precautions for use

The information provided in Special warnings and precautions for use of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Special warnings and precautions for use in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Modified-release tablet; Prolonged-release tablet; Tablets of prolonged action, coated; Tablets of prolonged action, film-coated
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The efficacy and safety of felodipine in the treatment of hypertensive emergencies has not been studied.

Felodipine may cause significant hypotension with subsequent tachycardia. This may lead to myocardial ischaemia in susceptible patients.

Felodipine is cleared by the liver. Consequently higher therapeutic concentrations and response can be expected in patients with clearly reduced liver function.

Concomitant administration of drugs that strongly induce or inhibit CYP3 A4 enzymes result in extensively decreased or increased plasma levels of felodipine, respectively. Therefore, such combinations should be avoided.

Keydipin contains lactose. Patients with rare hereditary problems of galactose intolerance, or glucose-galactose malabsorption should not take this medicinal product.

Keydipin contains castor oil, which may cause stomach upset and diarrhoea.

Mild gingival enlargement has been reported in patients with pronounced gingivitis/periodontitis. The enlargement can be avoided or reversed by careful oral hygiene.

The efficacy and safety of Keydipin in the treatment of hypertensive emergencies has not been studied.

Keydipin may cause significant hypotension with subsequent tachycardia. This may lead to myocardial ischaemia in susceptible patients.

Keydipin is cleared by the liver. Consequently higher therapeutic concentrations and response can be expected in patients with clearly reduced liver function.

Concomitant administration of drugs that strongly induce or inhibit CYP3 A4 enzymes result in extensively decreased or increased plasma levels of Keydipin, respectively. Therefore such combinations should be avoided.

Vascalpha (Keydipin) prolonged release tablets contains lactose. Patients with rare hereditary problems of galactose intolerance or glucose-galactose malabsorption should not take this medicinal product.

Mild gingival enlargement has been reported in patients with pronounced gingivitis/peridontitis. The enlargement can be avoided or reversed by careful oral hygiene.

Effects on ability to drive and use machines

The information provided in Effects on ability to drive and use machines of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Effects on ability to drive and use machines in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Modified-release tablet; Prolonged-release tablet; Tablets of prolonged action, coated; Tablets of prolonged action, film-coated
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Felodipine has minor or moderate influence on the ability to drive and use machines. If patients taking felodipine suffer from headache, nausea, dizziness or fatigue and ability to react may be impaired. Caution is recommended especially at the start of treatment.

Vascalpha (Keydipin) prolonged release tablets has minor or moderate influence on the ability to drive and use machines. If patients taking Keydipin suffer from headache, nausea, dizziness or fatigue and ability to react may be impaired. Caution is recommended especially at the start of treatment.

Undesirable effects

The information provided in Undesirable effects of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Undesirable effects in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Modified-release tablet; Prolonged-release tablet; Tablets of prolonged action, coated; Tablets of prolonged action, film-coated
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Summary of the safety profile

Felodipine can cause flushing, headache, palpitations, dizziness and fatigue. Most of these adverse reactions are dose-dependent and appear at the start of treatment or after a dose increase. Should such adverse reactions occur, they are usually transient and diminish with time.

Dose-dependent ankle swelling can occur in patients treated with felodipine. This results from precapillary vasodilatation and is not related to any generalised fluid retention.

Mild gingival enlargement has been reported in patients with pronounced gingivitis/periodontitis. The enlargement can be avoided or reversed by careful oral hygiene.

Tabulated list of adverse reactions

The adverse reactions listed below have been identified from clinical trials and from post marketing surveillance.

The following definitions of frequencies are used:

Very common >1/10

Common >1/100 to <1/10

Uncommon >1/1,000 to <1/100

Rare >1/10,000 to <1/1,000

Very rare <1/10,000

Table 1: Undesirable effects

System organ class

Frequency

Adverse reaction

Nervous system disorders

Common

Uncommon

Headache

Dizziness, paraesthesia

Cardiac disorders

Uncommon

Tachycardia, palpitations

Vascular disorders

Common

Uncommon

Rare

Flush

Hypotension

Syncope

Gastrointestinal disorders

Uncommon

Rare

Very rare

Nausea, abdominal pain

Vomiting

Gingival hyperplasia, gingivitis

Hepatobiliary disorders

Very rare

Increased liver enzymes

Skin and subcutaneous tissue disorders

Uncommon

Rare

Very rare

Rash, pruritus

Urticaria

Photosensitivity reactions, leukocytoclastic vasculitis

Musculoskeletal and connective tissue disorders

Rare

Arthralgia, myalgia

Renal and urinary disorders

Very rare

Pollakisuria

Reproductive system and breast disorders

Rare

Impotence/sexual dysfunction

General disorders and administration site conditions

Very common

Uncommon

Very rare

Peripheral oedema

Fatigue

Hypersensitivity reactions, e.g. angio-oedema, fever

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme.

Website: www.mhra.gov.uk/yellowcard.

Summary of the safety profile

Keydipin can cause flushing, headache, palpitations, dizziness and fatigue. Most of these adverse reactions are dose-dependent and appear at the start of treatment or after a dose increase. Should such adverse reactions occur, they are usually transient and diminish with time.

Dose-dependent ankle swelling can occur in patients treated with Keydipin. This results from precapillary vasodilatation and is not related to any generalised fluid retention.

Mild gingival enlargement has been reported in patients with pronounced gingivitis/periodontitis. The enlargement can be avoided or reversed by careful oral hygiene.

Tabulated list of adverse reactions

The adverse reactions listed below have been identified from clinical trials and from post marketing surveillance.

The following definitions of frequencies are used:

Very common > 1/10

Common > 1/100 to < 1/10

Uncommon > 1/1,000 to < 1/100

Rare > 1/10,000 to < 1/1,000

Very rare < 1/10,000

Table 1 Undesirable effects

System organ class

Frequency

Adverse reaction

Nervous system disorders

Common

Uncommon

Headache

Dizziness, paraesthesia

Cardiac disorders

Uncommon

Tachycardia, palpitations

Vascular disorders

Common

Uncommon

Rare

Flush

Hypotension

Syncope

Gastrointestinal disorders

Uncommon

Rare

Very rare

Nausea, abdominal pain

Vomiting

Gingival hyperplasia, gingivitis

Hepatobiliary disorders

Very rare

Increased liver enzymes

Skin and subcutaneous tissue disorders

Uncommon

Rare

Very rare

Rash, pruritus

Urticaria

Photosensitivity reactions

Leucocytoclastic vasculitis

Musculoskeletal and connective tissue disorders

Rare

Arthralgia, myalgia

Renal and urinary disorders

Very rare

Pollakisuria

Reproductive system and breast disorders

Rare

Impotence/sexual dysfunction

General disorders and administration site conditions

Very common

Uncommon

Very rare

Peripheral oedema

Fatigue

Hypersensitivity reactions, e.g. angiooedema, fever

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme; website: www.mhra.gov.uk/yellowcard

Overdose

The information provided in Overdose of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Overdose in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Modified-release tablet; Prolonged-release tablet; Tablets of prolonged action, coated; Tablets of prolonged action, film-coated
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Symptoms

Overdosage may cause excessive peripheral vasodilatation with marked hypotension and sometimes bradycardia.

Management

If justified: activated charcoal, gastric lavage if performed within one hour after ingestion.

If severe hypotension occurs, symptomatic treatment should be instituted.

The patient should be placed supine with the legs elevated. In case of accompanying bradycardia, atropine 0.5-1 mg should be administered intravenously. If this is not sufficient, plasma volume should be increased by infusion of e.g. glucose, saline, or dextran. Sympathomimetic medicinal products with predominant effect on the α1-adrenoceptor may be given if the above-mentioned measures are insufficient.

Symptoms

Overdose may cause excessive peripheral vasodilatation with marked hypotension and sometimes bradycardia.

Management

If justified: activated charcoal, gastric lavage if performed within one hour after ingestion.

If severe hypotension occurs, symptomatic treatment should be instituted. The patient should be placed supine with the legs elevated. In case of accompanying bradycardia, atropine 0.5-1 mg should be administered intravenously. If this is not sufficient, plasma volume should be increased by infusion of e.g., glucose, saline, or dextran. Sympathomimetic medicinal products with predominant effect on the α1-adrenoceptor may be given if the above-mentioned measures are insufficient.

Pharmacodynamic properties

The information provided in Pharmacodynamic properties of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Pharmacodynamic properties in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Modified-release tablet; Prolonged-release tablet; Tablets of prolonged action, coated; Tablets of prolonged action, film-coated
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Pharmacotherapeutic group: calcium channel blockers, dihydropyridine derivatives;

ATC code: C08CA02

Mechanism of action

Felodipine is a vascular selective calcium antagonist, which lowers arterial blood pressure by decreasing systemic vascular resistance. Due to the high degree of selectivity for smooth muscle in the arterioles, felodipine in therapeutic doses has no direct effect on cardiac contractility or conduction. Because there is no effect on venous smooth muscle or adrenergic vasomotor control, felodipine is not associated with orthostatic hypotension.

Felodipine possesses a mild natriuretic/diuretic effect and fluid retention does not occur.

Pharmacodynamic effects

Felodipine is effective in all grades of hypertension. It can be used as monotherapy or in combination with other antihypertensive medicinal products, e.g. ß-adrenoceptor blockers, diuretics or ACE-inhibitors, in order to achieve an increased antihypertensive effect. Felodipine reduces both systolic and diastolic blood pressure and can be used in isolated systolic hypertension.

Felodipine has anti-anginal and anti-ischaemic effects due to improved myocardial oxygen supply/demand balance. Coronary vascular resistance is decreased and coronary blood flow and myocardial oxygen supply are increased by felodipine due to dilatation of both epicardial arteries and arterioles. The reduction in systemic blood pressure caused by felodipine leads to decreased left ventricular afterload and myocardial oxygen demand.

Felodipine improves exercise tolerance and reduces anginal attacks in patients with stable effort-induced angina pectoris. Felodipine can be used as monotherapy or in combination with β-adrenoceptor blockers in patients with stable angina pectoris.

Haemodynamic effects

The primary haemodynamic effect of felodipine is a reduction of total peripheral vascular resistance, which leads to a decrease in blood pressure. These effects are dose-dependent. Generally, a reduction in blood pressure is evident two hours after the first oral dose and lasts for at least 24 hours and the trough/peak ratio is usually well above 50%.

Plasma concentrations of felodipine are positively correlated to the decrease in total peripheral resistance and blood pressure.

Cardiac effects

Felodipine in therapeutic doses has no effect on cardiac contractility or atrioventricular conduction or refractoriness.

Antihypertensive treatment with felodipine is associated with significant regression of pre-existing left ventricular hypertrophy.

Renal effects

Felodipine has a natriuretic and diuretic effect due to reduced tubular reabsorption of filtered sodium. Felodipine does not affect daily potassium excretion. The renal vascular resistance is decreased by felodipine. Felodipine does not influence urinary albumin excretion.

In cyclosporin-treated renal transplant recipients, felodipine reduces blood pressure and improves both the renal blood flow and the glomerular filtration rate. Felodipine may also improve early renal graft function.

Clinical efficacy

In the HOT (Hypertension Optimal Treatment) study, the effect on major cardiovascular events (i.e. acute myocardial infarction, stroke and cardiovascular death) was studied in relation to diastolic blood pressure targets <90 mmHg, <85 mmHg and <80 mmHg and achieved blood pressure, with felodipine as baseline therapy.

A total of 18,790 hypertensive patients (DBP 100-115 mmHg), aged 50-80 years were followed for a mean period of 3.8 years (range 3.3-4.9). Felodipine was given as monotherapy or in combination with a betablocker, and/or an ACE-inhibitor and/or a diuretic. The study showed benefits of lowering SBP and DBP down to 139 and 83 mmHg, respectively.

According to the STOP-2 (Swedish Trial in Old Patients with Hypertension-2 study), performed in 6614 patients, aged 70-84 years, dihydropyridine calcium antagonists (felodipine and isradipine) have shown the same preventive effect on cardiovascular mortality and morbidity as other commonly used classes of antihypertensive medicinal products - ACE inhibitors, beta-blockers and diuretics.

Paediatric population

There is limited clinical trial experience of the use of felodipine in hypertensive paediatric patients. In a randomised, double-blind, 3-week, parallel group study in children aged 6-16 years with primary hypertension, the antihypertensive effects of once daily felodipine 2.5 mg (n=33), 5 mg (n=33) and 10 mg (n=31) were compared with placebo (n=35). The study failed to demonstrate the efficacy of felodipine in lowering blood pressure in children aged 6-16 years.

The long-term effects of felodipine on growth, puberty and general development have not been studied. The long-term efficacy of antihypertensive therapy as therapy in childhood to reduce cardiovascular morbidity and mortality in adulthood has also not been established.

Pharmacotheraputic group: calcium channel blockers, didydropyridine derivatives;

ATC code: C08C A02

Mechanism of action

Keydipin is a vascular selective calcium antagonist, which lowers arterial blood pressure by decreasing systemic vascular resistance. Due to the high degree of selectivity for smooth muscle in the arterioles, Keydipin in therapeutic doses has no direct effect on cardiac contractility or conduction. Because there is no effect on venous smooth muscle or adrenergic vasomotor control, Keydipin is not associated with orthostatic hypotension.

Keydipin possesses a mild natriuretic/diuretic effect and fluid retention does not occur.

Pharmacodynamic effects

Keydipin is effective in all grades of hypertension. It can be used as monotherapy or in combination with other antihypertensive medicinal products, e.g., ß-adrenoceptor blockers, diuretics or ACE-inhibitors, in order to achieve an increased antihypertensive effect. Keydipin reduces both systolic and diastolic blood pressure and can be used in isolated systolic hypertension.

Keydipin has anti-anginal and anti-ischaemic effects due to improved myocardial oxygen supply/demand balance. Coronary vascular resistance is decreased and coronary blood flow and myocardial oxygen supply are increased by Keydipin due to dilatation of both epicardial arteries and arterioles. The reduction in systemic blood pressure caused by Keydipin leads to decreased left ventricular afterload and myocardial oxygen demand.

Keydipin improves exercise tolerance and reduces anginal attacks in patients with stable effort-induced angina pectoris. Keydipin can be used as monotherapy or in combination with ß-adrenoceptor blockers in patients with stable angina pectoris.

Haemodynamic effects

The primary haemodynamic effect of Keydipin is a reduction of total peripheral vascular resistance, which leads to a decrease in blood pressure. These effects are dose-dependent. Generally, a reduction in blood pressure is evident two hours after the first oral dose and lasts for at least 24 hours and the trough/peak ratio is usually well above 50 %.

Plasma concentrations of Keydipin are positively correlated to the decrease in total peripheral resistance and blood pressure.

Cardiac effects

Keydipin in therapeutic doses has no effect on cardiac contractility or atrioventricular conduction or refractoriness.

Antihypertensive treatment with Keydipin is associated with significant regression of pre-existing left ventricular hypertrophy.

Renal effects

Keydipin has a natriuretic and diuretic effect due to reduced tubular reabsorption of filtered sodium. Keydipin does not affect daily potassium excretion. The renal vascular resistance is decreased by Keydipin. Keydipin does not influence urinary albumin excretion.

In cyclosporine-treated renal transplant recipients, Keydipin reduces blood pressure and improves both the renal blood flow and the glomerular filtration rate. Keydipin may also improve early renal graft function.

Clinical efficacy and safety

In the HOT (Hypertension Optimal Treatment) study, the effect on major cardiovascular events (ie, acute myocardial infarction, stroke and cardiovascular death) was studied in relation to diastolic blood pressure targets < 90 mmHg, < 85 mmHg and < 80 mmHg and achieved blood pressure, with Keydipin as baseline therapy.

A total of 18,790 hypertensive patients (DBP 100-115 mmHg), aged 50-80 years were followed for a mean period of 3.8 years (range 3.3-4.9). Keydipin was given as monotherapy or in combination with a betablocker, and/or an ACE-inhibitor and/or a diuretic. The study showed benefits of lowering SBP and DBP down to 139 and 83 mmHg, respectively.

According to the STOP-2 (Swedish Trial in Old Patients with Hypertension-2 study), performed in 6614 patients, aged 70-84 years, dihydropyridine calcium antagonists (Keydipin and isradipine) have shown the same preventive effect on cardiovascular mortality and morbidity as other commonly used classes of antihypertensive medicinal products - ACE inhibitors, beta-blockers and diuretics.

Paediatric population

There is limited clinical trial experience of the use of Keydipin in hypertensive paediatric patients. In a randomised, double-blind, 3-week, parallel group study in children aged 6-16 years with primary hypertension, the antihypertensive effects of once daily Keydipin 2.5 mg (n = 33), 5 mg (n = 33) and 10 mg (n = 31) were compared with placebo (n = 35). The study failed to demonstrate the efficacy of Keydipin in lowering blood pressure in children aged 6-16 years

The long-term effects of Keydipin on growth, puberty and general development have not been studied. The long-term efficacy of antihypertensive therapy as therapy in childhood to reduce cardiovascular morbidity and mortality in adulthood has also not been established.

Pharmacokinetic properties

The information provided in Pharmacokinetic properties of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Pharmacokinetic properties in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Modified-release tablet; Prolonged-release tablet; Tablets of prolonged action, coated; Tablets of prolonged action, film-coated
Substance-powder

Absorption

Felodipine is administered as extended-release tablets, from which it is completely absorbed in the gastrointestinal tract. The systemic availability of felodipine is approximately 15% and is independent of dose in the therapeutic dose range. The extended-release tablets produce a prolonged absorption phase of felodipine. This results in even felodipine plasma concentrations within the therapeutic range for 24 hours. Maximum blood plasma levels (tmax) are achieved with the prolonged-release form after 3 to 5 hours. The rate but not the extent of absorption of felodipine is increased when taken simultaneously with food with a high fat content.

Distribution

The plasma protein binding of felodipine is approximately 99%. It is bound pre-dominantly to the albumin fraction. Volume of distribution at steady state is 10 L/kg.

Biotransformation

Felodipine is extensively metabolised in the liver by cytochrome P450 3A4 (CYP3A4) and all identified metabolites are inactive. Felodipine is a high clearance medicinal product with an average blood clearance of 1200 ml/min. There is no significant accumulation during long-term treatment.

Elderly patients and patients with reduced liver function have on average higher plasma concentrations of felodipine than younger patients. The pharmacokinetics of felodipine is not changed in patients with renal impairment, including those treated with haemodialysis.

Elimination

The half-life of felodipine in the elimination phase is approximately 25 hours and steady state is reached after 5 days. There is no risk of accumulation during long-term treatment. About 70% of a given dose is excreted as metabolites in the urine; the remaining fraction is excreted in the faeces. Less than 0.5% of a dose is recovered unchanged in urine.

Linearity/non-linearity

Plasma concentrations are directly proportional to dose within the therapeutic dose range 2.5-10 mg.

Paediatric population

In a single dose (felodipine prolonged-release 5 mg) pharmacokinetic study with a limited number of children aged between 6 and 16 years (n=12) there was no apparent relationship between the age and AUC, Cmax or half-life of felodipine.

Absorption

Keydipin is administered as extended-release tablets, from which it is completely absorbed in the gastrointestinal tract. The systemic availability of Keydipin is approximately 15 % and is independent of dose in the therapeutic dose range. The extended-release tablets produce a prolonged absorption phase of Keydipin. This results in even Keydipin plasma concentrations within the therapeutic range for 24 hours. Maximum blood plasma levels (tmax) are achieved with the prolonged-release form after 3 to 5 hours. The rate but not the extent of absorption of Keydipin is increased when taken simultaneously with food with a high fat content.

Distribution

The plasma protein binding of Keydipin is approximately 99 %. It is bound pre-dominantly to the albumin fraction. Volume of distribution at steady state is 10 L/kg.

Biotransformation

Keydipin is extensively metabolised in the liver by cytochrome P450 3A4 (CYP3A4) and all identified metabolites are inactive. Keydipin is a high clearance medicinal product with an average blood clearance of 1200 ml/min. There is no significant accumulation during long-term treatment.

Elderly patients and patients with reduced liver function have on average higher plasma concentrations of Keydipin than younger patients. The pharmacokinetics of Keydipin is not changed in patients with renal impairment, including those treated with haemodialysis.

Elimination

The half-life of Keydipin in the elimination phase is approximately 25 hours and steady state is reached after 5 days. There is no risk of accumulation during long-term treatment. About 70 % of a given dose is excreted as metabolites in the urine; the remaining fraction is excreted in the faeces. Less than 0.5 % of a dose is recovered unchanged in urine.

Linearity/non-linearity

Plasma concentrations are directly proportional to dose within the therapeutic dose range 2.5-10 mg.

Paediatric population

In a single dose (Keydipin prolonged-release 5 mg) pharmacokinetic study with a limited number of children aged between 6 and 16 years (n = 12) there was no apparent relationship between the age and AUC, Cmax or half-life of Keydipin.

Pharmacotherapeutic group

The information provided in Pharmacotherapeutic group of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Pharmacotherapeutic group in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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calcium channel blockers, dihydropyridine derivatives

Preclinical safety data

The information provided in Preclinical safety data of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Preclinical safety data in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Reproduction toxicity

In a study on fertility and general reproductive performance in rats treated with Keydipin, a prolongation of parturition resulting in difficult labour/increased foetal deaths and early postnatal deaths was observed in the medium and high dose groups. These effects were attributed to the inhibitory effect of Keydipin in high doses on uterine contractility. No disturbances of fertility were observed when doses within the therapeutic range were given to rats.

Reproduction studies in rabbits have shown a dose-related reversible enlargement of the mammary glands of the parent animals and dose-related digital anomalies in the foetuse. The anomalies in the foetuses were induced when Keydipin was administered during early foetal development (before day 15 of pregnancy). In a reproduction study in monkeys, an abnormal position of the distal phalange(s) was noticed.

There were no other pre clinical findings considered to be of concern and the reproductive findings are considered to be related to the pharmacological action of Keydipin, when given to normotensive animals. The relevance of these findings for patients receiving felopidine is unknown. However, there have been no reported clinical incidences of phalangeal changes in foetus/neonate exposed to Keydipin in-utero, from the information maintained within the internal patient safety databases.

Incompatibilities

The information provided in Incompatibilities of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Incompatibilities in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Not applicable.

Special precautions for disposal and other handling

The information provided in Special precautions for disposal and other handling of Keydipin is based on data of another medicine with exactly the same composition as the Keydipin of the medicine (Felodipine). Be careful and be sure to specify the information on the section Special precautions for disposal and other handling in the instructions to the drug Keydipin directly from the package or from the pharmacist at the pharmacy.
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Modified-release tablet; Prolonged-release tablet; Tablets of prolonged action, coated; Tablets of prolonged action, film-coated
Substance-powder

Any unused medicinal product or waste material should be disposed of in accordance with local requirements.

No special requirements

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