benidipine

Action and Spectrum

Actions and Spectrum: 

Action 

benidipine is a calcium channel blocker (CCB) that exerts its pharmacological action by selectively inhibiting L-type calcium channels, primarily in vascular smooth muscle cells. This inhibition of calcium influx into the smooth muscle cells leads to relaxation of the blood vessel walls, resulting in vasodilation. By reducing the contractility of these cells and dilating blood vessels, benidipine effectively lowers blood pressure. This action helps to reduce peripheral vascular resistance, making it particularly suitable for the treatment of hypertension (high blood pressure). Its mechanism of action contributes to a decrease in the heart’s workload and an improvement in blood flow through the coronary arteries. 

Spectrum: 

The spectrum of benidipine’s use is primarily centered around managing hypertension. It is indicated for individuals with essential hypertension, which is high blood pressure without an identifiable underlying cause. benidipine is often prescribed as a monotherapy for hypertension. Still, it can also be used with other antihypertensive medications, such as diuretics or ACE inhibitors, to achieve optimal blood pressure control.

Its long-lasting antihypertensive effects and the potential for additional cardiovascular benefits, such as coronary artery dilation, make it a valuable option in managing high blood pressure and related conditions. As with any medication, it should be supervised by a healthcare provider who can tailor the treatment plan to the individual’s needs and monitor its effectiveness and safety. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Elevated liver enzymes 

Headache 

Vomiting 

Light-headedness 

Palpitation 

Dizziness 

Malaise 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: benidipine should not be used in individuals with a known hypersensitivity or allergy to the drug or its components. Allergic reactions to medications can be severe and even life-threatening. 
• Severe Hypotension (Low Blood Pressure): benidipine can cause a drop in BP as part of its mechanism of action. It should not be used in individuals with severe hypotension, as it may worsen their condition. 
• Severe Liver Impairment: benidipine is metabolized by the liver, and its clearance from the body may be affected in individuals with severe liver impairment. It is contraindicated in individuals with severe hepatic dysfunction. Your healthcare provider will assess your liver function before prescribing benidipine. 
• Pregnancy and Lactation: The safety of benidipine during pregnancy and breastfeeding is not well-established. It is generally not recommended for use in pregnant condition or breastfeeding women unless the potential benefits outweigh the potential risks. Alternative antihypertensive medications with a better safety profile during pregnancy and breastfeeding may be considered. 
• Certain Drug Interactions: benidipine may interact with other medications, potentially leading to adverse effects or reduced effectiveness.  
• Previous Hypersensitivity Reactions to Other Calcium Channel Blockers: Individuals with hypersensitivity reactions to other calcium channel blockers should exercise caution when considering benidipine, as there may be an increased risk of cross-reactivity. 

Caution 

• Hypotension (Low Blood Pressure): benidipine’s primary mechanism of action is to relax blood vessels, which can lead to a decrease in blood pressure. Individuals taking benidipine should be cautioned about the potential for low blood pressure, especially when getting up from a sitting or lying position.  
• Dizziness and Lightheadedness: benidipine may cause dizziness, lightheadedness, or fainting in some individuals, especially when starting the medication or when the dosage is adjusted.  
• Fluid and Electrolyte Imbalance: Like other antihypertensive medications, benidipine may lead to fluid retention and electrolyte imbalances in some individuals.  
• Renal Function: benidipine is primarily excreted by the kidneys. Caution should be exercised in individuals with impaired renal function, and the dosage may need to be adjusted based on the individual’s renal function. 
• Liver Function: As mentioned earlier, benidipine is metabolized by the liver. Individuals with mild to moderate liver impairment may need dosage adjustments, while those with severe liver impairment should avoid benidipine altogether. 
• Elderly Population: Elderly individuals may be more sensitive to the effects of benidipine, including its blood pressure-lowering effects and the risk of dizziness. Lower starting doses may be considered in this population. 
• Grapefruit Juice: Grapefruit juice can interact with certain medications, including some calcium channel blockers. It may increase the blood levels of benidipine, potentially leading to an enhanced risk of side effects. Patients should be cautious about consuming grapefruit or grapefruit juice while taking benidipine. 
• Interactions with Other Medications: benidipine may interact with other medications, including other antihypertensive drugs, leading to additive effects or potential adverse reactions. Healthcare providers should carefully review the patient’s medication list to avoid harmful drug interactions. 
• Pregnancy and Lactation: As mentioned previously, the use of benidipine during pregnancy and breastfeeding should be approached with caution. The potential benefits and also risks should be carefully weighed, and alternative medications with established safety profiles may be considered. 
• Allergic Reactions: While rare, allergic reactions to benidipine can occur. Patients should be informed about the signs of an allergic reaction (e.g., rash, itching, swelling, severe dizziness, difficulty breathing). 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

benidipine (Caritec) is a dihydropyridine-type calcium channel blocker (CCB) used primarily in the treatment of hypertension (high blood pressure). Its pharmacological action involves the selective inhibition of L-type calcium channels in a smooth muscle cells of blood vessels. By blocking calcium influx into these cells, benidipine reduces their contractility, leading to vasodilation (relaxation of blood vessels).

This vasodilatory effect results in decreased peripheral vascular resistance and a subsequent reduction in BP. benidipine exhibits slow-onset, long-lasting antihypertensive effects, making it suitable for once-daily dosing. Additionally, it may have antianginal properties by dilating coronary arteries, potentially increasing blood flow to the heart muscle. benidipine’s pharmacological profile contributes to its effectiveness in lowering blood pressure and managing hypertension. 

Pharmacodynamics: 

Mechanism of action: benidipine is a calcium channel blocker (CCB) with a mechanism of action primarily centered on its ability to block calcium channels in specific cells. Specifically, it belongs to the dihydropyridine class of CCBs.  

• Calcium Channels: There are specialized proteins called calcium channels within various cells, including smooth muscle cells in blood vessels and cardiac muscle cells in the heart. When activated, these channels allow the controlled entry of calcium ions (Ca2+) into the cells. 
• Vasodilation: benidipine targets L-type calcium channels predominantly found in vascular smooth muscle cells. Calcium ions flow into the smooth muscle cells when various stimuli, such as nerve signals or hormones activate these channels. This influx of calcium ions triggers muscle contraction, leading to blood vessels’ narrowing (constriction). 
• Blocking Calcium Influx: benidipine acts as a calcium channel blocker by binding to and inhibiting L-type calcium channels in vascular smooth muscle cells. By doing so, benidipine prevents the entry of calcium ions into the cells. 
• Smooth Muscle Relaxation: When calcium ions are blocked from entering the smooth muscle cells, the cells are less able to contract. As a result, the muscle fibers in the walls of blood vessels relax, leading to vasodilation or the widening of the blood vessels.  
• Blood Pressure Reduction: Reducing vascular resistance due to smooth muscle relaxation leads to a drop in blood pressure. The heart does not have to work as hard to pump blood through dilated blood vessels, so cardiac workload is also reduced. This makes benidipine effective in lowering blood pressure. 
• Other Effects: benidipine may also affect the heart and blood vessels. For example, it can dilate coronary arteries, potentially improving blood flow to the heart muscle. This action may benefit individuals with coronary artery disease or angina (chest pain). 

Pharmacokinetics: 

Absorption 

benidipine is administered orally as tablets or capsules and is absorbed from the gastrointestinal tract after oral administration. Food does not significantly affect its absorption, so it can be taken with or without meals. After oral ingestion, benidipine enters the bloodstream and becomes available for its pharmacological action. 

Distribution 

benidipine is distributed throughout the body, primarily in the vascular smooth muscle cells, where it exerts its calcium channel-blocking effects. It also has a high affinity for binding to the plasma proteins, which can affect its distribution within the bloodstream. The drug’s distribution may vary among individuals based on age, body composition, and any underlying medical conditions. 

Metabolism 

benidipine undergoes extensive hepatic (liver) metabolism, primarily through the cytochrome P450 enzyme system, specifically the CYP3A4 enzyme. benidipine is transformed into various metabolites during metabolism, some of which may also possess pharmacological activity. The exact details of its metabolic pathways and metabolite profiles may vary among individuals and can be influenced by genetic variability and drug interactions. 

Elimination and Excretion 

The primary route of excretion for benidipine and its metabolites is through the urine. The kidneys generally plays a key role in eliminating the drug and its byproducts from the body. The exact elimination half-life of benidipine can vary from person to person but is typically in the range of several hours.

Adminstartion

Administration: 

benidipine is typically administered as an oral medication in tablets or capsules. benidipine’s specific dosage and administration instructions may vary depending on the individual’s medical condition and the prescribing healthcare provider’s recommendations.  

• Dosage: The recommended dosage of benidipine will vary from person to person depend on their medical condition, age, and other factors. Typically, the initial dose is relatively low and may be increased gradually as needed to achieve the desired blood pressure control. Do not change your dose without consulting your healthcare provider. 
• Frequency: benidipine is usually taken once daily, preferably in the morning with or without food. Taking it simultaneously daily can help you remember to take your medication consistently. 
• Swallow Whole: Swallow the benidipine tablet or capsule whole with a glass of water.  
• Avoid Grapefruit: Avoid consuming grapefruit or grapefruit juice while taking benidipine, as it can interact with the drug and increase the risk of side effects. 
• Compliance: It’s essential to take benidipine regularly as your healthcare provider prescribes, even if you start feeling better or your blood pressure improves. Hypertension often requires ongoing treatment, and discontinuing the medication without medical guidance can lead to a rise in blood pressure. 
• Monitoring: Your healthcare provider will regularly monitor your blood pressure and overall health while taking benidipine. Be sure to attend all scheduled check-up appointments and follow any additional recommendations your healthcare team provides. 
• Adverse Effects: If you experience any unusual or severe side effects while taking benidipine, contact your healthcare provider immediately. Common side effects might include dizziness, headache, flushing, or swelling of the ankles. However, not everyone will experience these side effects. 
• Missed Dose: If a dose is missed, taking it as soon as possible is generally recommended. However, if the next scheduled dose is missed, it should be skipped and the following dose should be taken at the appropriate time. It is key to avoid taking a double dose of the drug in order to compensate for the missed dose. 
• Storage: Store benidipine at room temperature, away from light and moisture. Follow any specific storage instructions provided on the medication packaging. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: benidipine 

Why do we use benidipine? 

benidipine (Caritec) is a calcium channel blocker (CCB) medication primarily used for the therapy of hypertension (high blood pressure).  

• Hypertension (High Blood Pressure): benidipine is primarily indicated for the management of hypertension. It typically works by relaxing the smooth muscle in blood vessel walls, which leads to vasodilation and a reduction in blood pressure. Lowering blood pressure helps diminish the risk of complications associated with hypertension, like heart disease, stroke, and kidney problems. 

In some cases, benidipine may be used as monotherapy (a single medication) for hypertension. Still, it is often prescribed with other antihypertensive drugs to achieve optimal blood pressure control.