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|Adenoscan |
Drugs search, click the first letter of a drug name: | A | B | C | D | E | F | G | H | I | J | K | L | M | N | O | P | Q | R | S | T | U | V | W | X | Y | Z | 1 | 2 | 3 | 4 | 5 | 6 | 8 | 9 Home AdenoscanGeneric Name: adenosine Dosage Form: Injection DescriptionAdenosine is an endogenous nucleoside occurring in all cells of the body. It is chemically 6-amino-9-beta-D-ribofuranosyl-9-H-purine and has the following structural formula: C10H13N5O4 267.24 Adenosine is a white crystalline powder. It is soluble in water and practically insoluble in alcohol. Solubility increases by warming and lowering the pH of the solution. Each Adenoscan vial contains a sterile, non-pyrogenic solution of adenosine 3 mg/mL and sodium chloride 9 mg/mL in Water for Injection, q.s. The pH of the solution is between 4.5 and 7.5. Clinical PharmacologyMechanism of Action Adenosine is a potent vasodilator in most vascular beds, except in renal afferent arterioles and hepatic veins where it produces vasoconstriction. Adenosine is thought to exert its pharmacological effects through activation of purine receptors (cell-surface A1 and A2 adenosine receptors). Although the exact mechanism by which adenosine receptor activation relaxes vascular smooth muscle is not known, there is evidence to support both inhibition of the slow inward calcium current reducing calcium uptake, and activation of adenylate cyclase through A2 receptors in smooth muscle cells. Adenosine may also lessen vascular tone by modulating sympathetic neurotransmission. The intracellular uptake of adenosine is mediated by a specific transmembrane nucleoside transport system. Once inside the cell, adenosine is rapidly phosphorylated by adenosine kinase to adenosine monophosphate, or deaminated by adenosine deaminase to inosine. These intracellular metabolites of adenosine are not vasoactive. Myocardial uptake of thallium-201 is directly proportional to coronary blood flow. Since Adenoscan significantly increases blood flow in normal coronary arteries with little or no increase in stenotic arteries, Adenoscan causes relatively less thallium-201 uptake in vascular territories supplied by stenotic coronary arteries i.e., a greater difference is seen after Adenoscan between areas served by normal and areas served by stenotic vessels than is seen prior to Adenoscan. Hemodynamics Pharmacokinetics Clinical Trials Intracoronary Doppler flow catheter studies have demonstrated that a dose of intravenous Adenoscan of 140 mcg/kg/min produces maximum coronary hyperemia (relative to intracoronary papaverine) in approximately 95% of cases within two to three minutes of the onset of the infusion. Coronary blood flow velocity returns to basal levels within one to two minutes of discontinuing the Adenoscan infusion. Indications and UsageIntravenous Adenoscan is indicated as an adjunct to thallium-201 myocardial perfusion scintigraphy in patients unable to exercise adequately (See WARNINGS). ContraindicationsIntravenous Adenoscan (adenosine injection) should not be administered to individuals with:
WarningsFatal Cardiac Arrest, Life Threatening Ventricular Arrhythmias, and Myocardial Infarction Sinoatrial and Atrioventricular Nodal Block Hypotension Hypertension Bronchoconstriction Adenosine administered by inhalation has been reported to cause bronchoconstriction in asthmatic patients, presumably due to mast cell degranulation and histamine release. These effects have not been observed in normal subjects. Adenoscan has been administered to a limited number of patients with asthma and mild to moderate exacerbation of their symptoms has been reported. Respiratory compromise has occurred during adenosine infusion in patients with obstructive pulmonary disease. Adenoscan should be used with caution in patients with obstructive lung disease not associated with bronchoconstriction (e.g., emphysema, bronchitis, etc.) and should be avoided in patients with bronchoconstriction or bronchospasm (e.g., asthma). Adenoscan should be discontinued in any patient who develops severe respiratory difficulties. PrecautionsDrug interactionsIntravenous Adenoscan (adenosine injection) has been given with other cardioactive drugs (such as beta adrenergic blocking agents, cardiac glycosides, and calcium channel blockers) without apparent adverse interactions, but its effectiveness with these agents has not been systematically evaluated. Because of the potential for additive or synergistic depressant effects on the SA and AV nodes, however, Adenoscan should be used with caution in the presence of these agents. The vasoactive effects of Adenoscan are inhibited by adenosine receptor antagonists, such as methylxanthines (e.g., caffeine and theophylline). The safety and efficacy of Adenoscan in the presence of these agents has not been systematically evaluated. The vasoactive effects of Adenoscan are potentiated by nucleoside transport inhibitors, such as dipyridamole. The safety and efficacy of Adenoscan in the presence of dipyridamole has not been systematically evaluated. Whenever possible, drugs that might inhibit or augment the effects of adenosine should be withheld for at least five half-lives prior to the use of Adenoscan. Carcinogenesis, mutagenesis, impairment of fertilityStudies in animals have not been performed to evaluate the carcinogenic potential of Adenoscan (adenosine injection). Adenosine was negative for genotoxic potential in the Salmonella (Ames Test) and Mammalian Microsome Assay. Adenosine, however, like other nucleosides at millimolar concentrations present for several doubling times of cells in culture, is known to produce a variety of chromosomal alterations. Fertility studies in animals have not been conducted with adenosine. Pregnancy Category CAnimal reproduction studies have not been conducted with adenosine; nor have studies been performed in pregnant women. Because it is not known whether Adenoscan can cause fetal harm when administered to pregnant women, Adenoscan should be used during pregnancy only if clearly needed. Pediatric useThe safety and effectiveness of Adenoscan in patients less than 18 years of age have not been established. Geriatric useClinical studies of Adenoscan did not include sufficient numbers of subjects aged younger than 65 years to determine whether they respond differently. Other reported experience has not revealed clinically relevant differences of the response of elderly in comparison to younger patients. Greater sensitivity of some older individuals, however, cannot be ruled out. Adverse ReactionsThe following reactions with an incidence of at least 1% were reported with intravenous Adenoscan among 1421 patients enrolled in controlled and uncontrolled U.S. clinical trials. Despite the short half-life of adenosine, 10.6% of the side effects occurred not with the infusion of Adenoscan but several hours after the infusion terminated. Also, 8.4% of the side effects that began coincident with the infusion persisted for up to 24 hours after the infusion was complete. In many cases, it is not possible to know whether these late adverse events are the result of Adenoscan infusion.
Adverse experiences of any severity reported in less than 1% of patients include: Body as a Whole Back discomfort; lower extremity discomfort; weakness Cardiovascular System Nonfatal myocardial infarction; life-threatening ventricular arrhythmia; third-degree AV block; bradycardia; palpitation; sinus exit block; sinus pause; sweating; T-wave changes; hypertension (systolic blood pressure > 200 mm Hg) Central Nervous System Drowsiness; emotional instability; tremors Genital/Urinary System Vaginal pressure; urgency Respiratory System Cough Special Senses Blurred vision; dry mouth; ear discomfort; metallic taste; nasal congestion; scotomas; tongue discomfort Post Marketing Experience (see WARNINGS) The following adverse events have been reported from marketing experience with Adenoscan. Because these events are reported voluntarily from a population of uncertain size, are associated with concomitant diseases and multiple drug therapies and surgical procedures, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Decisions to include these events in labeling are typically based on one or more of the following factors: (1) seriousness of the event, (2) frequency of the reporting, (3) strength of causal connection to the drug, or a combination of these factors. Body as a Whole Injection site reaction Central Nervous System Seizure activity, including tonic clonic (grand mal) seizures, and loss of consciousness Digestive Nausea and vomiting Respiratory Respiratory arrest OVERDOSAGEThe half-life of adenosine is less than 10 seconds and side effects of Adenoscan (when they occur) usually resolve quickly when the infusion is discontinued, although delayed or persistent effects have been observed. Methylxanthines, such as caffeine and theophylline, are competitive adenosine receptor antagonists and theophylline has been used to effectively terminate persistent side effects. In controlled U.S. clinical trials, theophylline (50-125 mg slow intravenous injection) was needed to abort Adenoscan side effects in less than 2% of patients. Dosage and AdministrationFor intravenous infusion only. Adenoscan should be given as a continuous peripheral intravenous infusion. The recommended intravenous dose for adults is 140 mcg/kg/min infused for six minutes (total dose of 0.84 mg/kg). The required dose of thallium-201 should be injected at the midpoint of the Adenoscan infusion (i.e., after the first three minutes of Adenoscan). Thallium-201 is physically compatible with Adenoscan and may be injected directly into the Adenoscan infusion set. The injection should be as close to the venous access as possible to prevent an inadvertent increase in the dose of Adenoscan (the contents of the IV tubing) being administered. There are no data on the safety or efficacy of alternative Adenoscan infusion protocols. The safety and efficacy of Adenoscan administered by the intracoronary route have not been established. The following Adenoscan infusion nomogram may be used to determine the appropriate infusion rate corrected for total body weight:
This nomogram was derived from the following general formula: Note: Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration. How SuppliedAdenoscan (adenosine injection) is supplied as 20 mL and 30 mL vials of sterile, nonpyrogenic solution in normal saline.
Store at controlled room temperature 15°-30°C (59°-86°F) Do not refrigerate as crystallization may occur. If crystallization has occurred, dissolve crystals by warming to room temperature. The solution must be clear at the time of use. Contains no preservative. Discard unused portion. Rx only Marketed by: Astellas Pharma US, Inc. Manufactured by: Hospira, Inc. Lake Forest, IL 60045 USA July 2005
Revised: 08/2006 Where can I get more information about Adenoscan ? We recommend to use www.Drugs.com Typical mistypes for Adenoscan zdenoscan, sdenoscan, wdenoscan, qdenoscan, asenoscan, axenoscan, acenoscan, afenoscan, arenoscan, aeenoscan, adwnoscan, adsnoscan, addnoscan, adrnoscan, ad4noscan, ad3noscan, adeboscan, ademoscan, adejoscan, adehoscan, adeniscan, adenkscan, adenlscan, adenpscan, aden0scan, aden9scan, adenoacan, adenozcan, adenoxcan, adenodcan, adenoecan, adenowcan, adenosxan, adenosvan, adenosfan, adenosdan, adenosczn, adenoscsn, adenoscwn, adenoscqn, adenoscab, adenoscam, adenoscaj, adenoscah, denoscan, aenoscan, adnoscan, adeoscan, adenscan, adenocan, adenosan, adenoscn, adenosca, daenoscan, aednoscan, adneoscan, adeonscan, adensocan, adenocsan, adenosacn, adenoscna, aadenoscan, addenoscan, adeenoscan, adennoscan, adenooscan, adenosscan, adenosccan, adenoscaan, adenoscann, etc.
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