nitrendipine

Action and Spectrum

Actions and Spectrum: 

• Calcium Channels Blockade: nitrendipine blocks explicitly L-type calcium channels. These channels are present in the membranes of vascular smooth muscle cells and cardiac muscle cells. When these channels open, they allow calcium ions to enter the cells, which leads to muscle contraction. By blocking these calcium channels, nitrendipine reduces the influx of calcium ions, resulting in the relaxation of vascular smooth muscles and a reduction in peripheral vascular resistance. This vasodilation helps in lowering blood pressure. 
• Arterial selectivity: nitrendipine is considered an arterioselective calcium channel blocker. It has a more substantial effect on arteries’ smooth muscle cells than veins. This arterial selectivity is significant in managing hypertension, as it decreases systemic vascular resistance without significantly affecting venous capacitance. 

nitrendipine primarily affects arterial smooth muscles and significantly impacts arterioles more than veins. This leads to the following effects: 

• Antihypertensive Effect: By relaxing arterial smooth muscles, nitrendipine reduces peripheral vascular resistance, lowering blood pressure. It’s used to manage essential hypertension and secondary hypertension. 
• Angina Treatment: nitrendipine’s vasodilatory effect on coronary arteries increases blood flow to the heart muscle, which can help alleviate angina symptoms. Angina is chest pain or discomfort when the heart muscle doesn’t receive enough oxygen-rich blood.

Drug Interaction

Adverse Reaction

Frequency not defined 

None 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: nitrendipine should not be used in individuals with a known hypersensitivity or allergy to the drug or its components. 
• Acute Myocardial Infarction (Heart Attack): nitrendipine is generally not recommended for use during the acute phase of a myocardial infarction (heart attack), as it may further compromise cardiac function. 
• Cardiogenic Shock: nitrendipine should be avoided in patients with cardiogenic shock, where the heart cannot pump enough blood to meet the body’s needs. 
• Unstable Angina: nitrendipine is typically not used in patients with unstable angina, a severe form of angina where symptoms become more frequent and severe or occur at rest. 
• Aortic Stenosis: nitrendipine may be contraindicated in patients with severe aortic stenosis, where the aortic valve narrows, impeding blood flow from the heart. 
• Severe Hypotension: Use of nitrendipine is cautioned in patients with severe hypotension (low blood pressure), as it can further lower blood pressure. 
• Severe Hepatic Impairment: nitrendipine should be used cautiously in patients with severe hepatic impairment (liver dysfunction) due to potential effects on drug metabolism and elimination. 

Caution: 

• Hypotension: nitrendipine can cause a decrease in blood pressure, which might lead to symptoms like dizziness, lightheadedness, or fainting, especially when standing up quickly.  
• Elderly Patients: Elderly individuals may be more susceptible to the hypotensive effects of nitrendipine. Dosage adjustments might be necessary to avoid excessive blood pressure lowering. 
• Liver Function: Patients with impaired liver function should use nitrendipine cautiously, as the drug is metabolized in the liver.  
• Renal Function: While nitrendipine is not primarily eliminated through the kidneys, caution is still advised in patients with severe renal impairment (kidney dysfunction). 
• Heart Failure: In patients with heart failure, nitrendipine should be used cautiously. The medication’s effects on cardiac function must be carefully monitored, and therapy adjustments might be necessary. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: N/A 

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: 

nitrendipine works by selectively blocking L-type calcium channels in the smooth muscle cells of blood vessels and the heart’s cardiac muscle cells. These channels allow calcium ions to enter the cells, a crucial step in muscle contraction. By blocking these calcium channels, nitrendipine reduces the influx of calcium ions into the cells, leading to the relaxation of smooth muscles in blood vessel walls and a decrease in cardiac contractility. This results in vasodilation (widening of blood vessels) and decreased cardiac workload, contributing to its antihypertensive and anti-anginal effects. 

Pharmacokinetics: 

Absorption 

nitrendipine is administered orally in the form of tablets or capsules. After oral intake, it is absorbed from the gastrointestinal tract into the bloodstream. The absorption process can be influenced by factors such as the drug’s formulation, food in the stomach, and the individual’s physiological characteristics. 

Distribution 

Once absorbed into the bloodstream, nitrendipine is distributed throughout the body. It binds to plasma proteins, mainly albumin, to varying degrees. The drug’s distribution is primarily influenced by its lipophilic nature, meaning it has an affinity for lipid-rich tissues. 

Metabolism 

nitrendipine undergoes extensive metabolism in the liver. The primary enzyme responsible for its metabolism is cytochrome P450 3A4 (CYP3A4). This metabolism results in the formation of both active and inactive metabolites. The active metabolites also contribute to the drug’s pharmacological effects. 

Elimination and Excretion  

The metabolites of nitrendipine, along with a smaller portion of unchanged drug, are excreted from the body primarily through the urine and, to a lesser extent, in feces. Renal excretion plays a significant role in eliminating the drug and its metabolites from the body. 

The elimination half-life of nitrendipine, which is the time it takes for half of the drug to be eliminated from the body, is around 12 to 24 hours. This relatively long half-life allows for once-daily dosing in many cases. 

Adminstartion

Administration: 

Oral administration 

It is typically administered orally in the form of tablets or capsules 

Patient Information Leaflet

Patient information leaflet 

Generic Name: nitrendipine 

Why do we use nitrendipine? 

nitrendipine is a medication primarily used to treat hypertension (high blood pressure) and angina pectoris (chest pain). Here are the main uses of nitrendipine: 

• Hypertension (High Blood Pressure): nitrendipine is commonly prescribed to lower blood pressure in individuals with hypertension. It belongs to the class of drugs known as calcium channel blockers, specifically dihydropyridines. By blocking calcium channels in the smooth muscle cells of blood vessels, nitrendipine causes vasodilation (widening of blood vessels) and reduces the resistance to blood flow. This results in a decrease in blood pressure, helping to manage hypertension and reduce the risk of associated cardiovascular complications. 
• Angina Pectoris: nitrendipine is also used to treat angina pectoris, a condition characterized by chest pain or discomfort due to inadequate blood flow to the heart muscle. The drug’s vasodilatory effects on coronary and peripheral arteries lead to decreased cardiac workload and reduced myocardial oxygen demand. This helps alleviate anginal symptoms and improve exercise tolerance in individuals with stable angina.