bicisate dihydrochloride

Action and Spectrum

Actions and Spectrum: 

bicisate dihydrochloride, known as Neurolite, is a radiopharmaceutical agent used in nuclear medicine imaging procedures. It is primarily used for single photon emission computed tomography (SPECT) brain imaging to assess regional cerebral blood flow. The compound contains technetium-99m (99mTc), which emits gamma rays that imaging devices can detect. 

Action:  

The action of bicisate dihydrochloride is based on its ability to be taken up by brain tissue in proportion to local cerebral blood flow. It is injected into the bloodstream and quickly reaches the brain, distributed in regions with active blood flow. Emitting gamma rays allows for the visualization of blood flow patterns in the brain and assists in diagnosing various neurological conditions. 

Spectrum:  

bicisate dihydrochloride is not used for protection against ultraviolet (UV) radiation like sunscreen ingredients. Instead, it is used for medical imaging purposes. Its “spectrum” refers to the emission of gamma rays during its radioactive decay, a type of electromagnetic radiation. This emitted radiation is detected by imaging equipment to create detailed images of blood flow and brain function. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Chest pain (angina) 

Feeling unwell (malaise) 

Agitation 

Seizure 

Lightheadedness/fainting 

Cardiac failure 

Anxiety 

Problems with smell 

Rash 

Headache 

Hallucinations 

High blood pressure (hypertension) 

Apnea 

Nausea 

Dizziness 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Allergies or Sensitivities: Individuals with a known allergy or sensitivity to bicisate dihydrochloride or its components should avoid its use. 
• Pregnancy and Breastfeeding: bicisate dihydrochloride involves radioactive material, and its safety during pregnancy and breastfeeding is not well established. The potential risks and benefits have to be evaluated, and alternative imaging methods may be considered. 
• Age and Pediatric Use: bicisate dihydrochloride in children and infants may require special considerations, and a healthcare professional should evaluate its safety and efficacy in this population. 
• Serious Medical Conditions: Patients with serious medical conditions, such as severe cardiovascular or cerebrovascular disease, may need special monitoring or caution when undergoing bicisate dihydrochloride procedures. 
• Recent Radiopharmaceutical Use: Certain other radiopharmaceutical agents or nuclear medicine procedures close to bicisate dihydrochloride imaging may require careful timing and coordination. 
• Acute Medical Conditions: Acute medical conditions that may affect blood flow to the brain or interfere with the imaging procedure may warrant delaying the use of bicisate dihydrochloride. 

Caution 

• Radiation Exposure: bicisate dihydrochloride contains radioactive technetium-99m (99mTc), which emits gamma radiation. While the amount of radiation exposure during a typical imaging procedure is generally considered safe, caution is advised, especially for pregnant women, breastfeeding mothers, and individuals who may undergo multiple imaging procedures over a short period. 
• Pregnancy and Breastfeeding: bicisate dihydrochloride involves radiation exposure, and its use during pregnancy and breastfeeding should be carefully considered. The potential risks and benefits have to be discussed with a healthcare provider, and alternative imaging methods may be explored. 
• Radiation Safety Precautions: Healthcare professionals administering bicisate dihydrochloride and performing nuclear medicine procedures should adhere to established radiation safety protocols to minimize radiation exposure to themselves and patients. 
• Pre-existing Medical Conditions: Patients with certain types of medical conditions, like severe kidney or liver disease, may require special precautions or adjustments in administering bicisate dihydrochloride. These conditions can affect the distribution and elimination of the radiopharmaceutical. 
• Medication Interactions: Some medications may interfere with the imaging results or the behavior of bicisate dihydrochloride in the body. It’s essential to provide your healthcare provider with a complete list of medications, supplements, and medical history before the procedure. 
• Patient Comfort: Nuclear medicine procedures involving bicisate dihydrochloride may require the patient to lie still for a prolonged period. Patients with difficulty lying still or who experience claustrophobia should discuss these concerns with their healthcare provider. 
• Pediatric Use: Pediatric patients may require special considerations, including appropriate imaging protocols and dose adjustments when using bicisate dihydrochloride. 

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. 
• 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: 

bicisate dihydrochloride, a radiopharmaceutical used in nuclear medicine, contains technetium-99m (99mTc), emitting gamma radiation. Administered intravenously, it distributes to brain tissue in proportion to regional cerebral blood flow. Gamma emissions during radioactive decay are detected by imaging equipment, enabling single photon emission computed tomography (SPECT) imaging of brain blood perfusion.

bicisate dihydrochloride’s distribution in brain tissue reflects local blood flow, aiding in diagnosing neurological conditions such as stroke, tumors, and dementia. Its pharmacology involves emitting gamma rays for imaging rather than conventional drug effects, contributing to functional brain assessment. 

Pharmacodynamics: 

Mechanism of action: The action of bicisate dihydrochloride (Neurolite) is rooted in its use as a radiopharmaceutical agent for brain imaging, specifically single photon emission computed tomography (SPECT). Unlike traditional drugs that exert pharmacological effects, the primary purpose of bicisate dihydrochloride is to provide visual information about cerebral blood flow and brain perfusion patterns.  

• Labeling with Technetium-99m (99mTc): bicisate dihydrochloride is a compound that contains technetium-99m (99mTc), a radioactive isotope. The radiopharmaceutical is prepared by labeling bicisate dihydrochloride with technetium-99m. This radiolabeling process creates a compound that emits gamma radiation. 
• Intravenous Administration: bicisate dihydrochloride, labeled with technetium-99m, is administered intravenously to the patient. It quickly enters the bloodstream. 
• Distribution in the Brain: After entering the bloodstream, bicisate dihydrochloride distributes throughout the body, including the brain. Significantly, its distribution within the brain is directly related to regional cerebral blood flow. 
• Gamma Emissions and Imaging: As the technetium-99m undergoes radioactive decay, it emits gamma radiation. A gamma camera detects the emitted gamma rays during SPECT imaging. The intensity of the detected gamma rays corresponds to the amount of radiopharmaceutical present in different brain regions. 
• Image Reconstruction: The detected gamma emissions create images of the brain’s perfusion patterns. These images provide valuable information about blood flow to different brain areas. Changes in blood flow can indicate various neurological conditions, such as stroke, tumors, and other brain disorders. 

Pharmacokinetics: 

Absorption 

bicisate dihydrochloride is administered intravenously, allowing it to enter the bloodstream quickly. It then rapidly distributes throughout the body, including the brain. 

Distribution 

bicisate dihydrochloride’s distribution within the brain is directly related to regional cerebral blood flow, which provides valuable information about brain perfusion patterns. 

Metabolism 

Unlike traditional pharmaceuticals, radiopharmaceuticals like bicisate dihydrochloride do not undergo typical metabolic processes. They decay over time through radioactive decay. 

Elimination and Excretion 

After imaging, the radioactive material naturally decays and is gradually eliminated from the body through normal bodily processes, primarily urine. 

Adminstartion

Administration: 

bicisate dihydrochloride (trade name: Neurolite) is a radiopharmaceutical agent used in nuclear medicine imaging procedures, specifically for single photon emission computed tomography imaging procedure of the brain to assess regional cerebral blood flow.  

• Preparation: The radiopharmaceutical bicisate dihydrochloride is prepared by a qualified nuclear medicine technologist or pharmacist. The technetium-99m (99mTc) labeled compound is prepared as a solution for injection. 
• Injection: bicisate dihydrochloride is administered as an intravenous injection. A healthcare professional, typically a nurse or a radiology technologist, inserts an intravenous (IV) catheter into a vein, usually in the arm. 
• Injection Site: The IV catheter delivers the prepared bicisate dihydrochloride solution into the bloodstream. The injection is generally performed slowly over a brief period, often a few seconds to a minute. 
• Patient Rest and Imaging: After the injection, the patient may need to rest quietly to allow the radiopharmaceutical to distribute within the brain tissue. 
• Imaging Procedure: The patient is positioned under a SPECT imaging machine. The SPECT camera detects the gamma radiation emitted by the radiopharmaceutical and creates images of blood flow in the brain from different angles. 
• Duration: The procedure can vary but is typically completed within a few hours. Patients might be required to stay still during imaging. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: bicisate dihydrochloride 

Why do we use bicisate dihydrochloride? 

bicisate dihydrochloride is a radiopharmaceutical agent used in nuclear medicine imaging procedures to assess regional cerebral blood flow. It is primarily used for single photon emission computed tomography (SPECT) brain imaging.  

• Cerebral Blood Flow Assessment: bicisate dihydrochloride is used to evaluate the brain’s regional cerebral blood flow (rCBF). It provides information about the blood perfusion patterns in different brain regions, which can aid in diagnosing and assessing various neurological conditions. 
• Brain Imaging: bicisate dihydrochloride, when used in SPECT imaging, helps visualize blood flow distribution in the brain. This imaging technique is valuable in diagnosing and monitoring conditions such as stroke, brain tumors, epilepsy, Alzheimer’s disease, dementia, and other neurological disorders. 
• Detection of Blood Flow Abnormalities: bicisate dihydrochloride SPECT imaging can detect brain areas with abnormal blood flow, such as regions with reduced or increased perfusion. These abnormalities can provide insights into the underlying causes of neurological symptoms and guide treatment decisions. 
• Assessment of Brain Function: By visualizing blood flow patterns, bicisate dihydrochloride imaging can indirectly provide information about brain function. Changes in blood flow can indicate neuronal activity and help clinicians understand the functional status of different brain regions.