Flumazenil, a derivative imidazobenzodiazepinov – anadrol side effects antagonist. Specifically inhibits the effects of drugs acting on the CNS anadrol side effects receptors. Eliminates sedation, amnesia and psychomotor impairment caused by anadrol side effects receptor agonists. Somnolent and sedative effect of anadrol side effectss disappears within 1-2 minutes after i / v injection of flumazenil, but may gradually reappear in the next few hours, depending on the half-life and the dose of agonist and antagonist.
Flumazenil may have its own weak agonist (for example, anticonvulsant) activity.
In adult patients, which for several weeks received large doses of anadrol side effectss, flumazenil administration accompanied anadrol side effects withdrawal symptoms, including seizures.
Pharmacokinetics of flumazenil as a therapeutic as well as in the higher range of doses (100 mg) is dose-dependent.
Flumazenil, a weak lipophilic base, approximately 50% bound to plasma proteins. Two thirds of the protein binding to albumin have to share. Flumazenil is extensively distributed in the extravascular space.Plasma concentrations of flumazenil decrease with a half-life 11.4 minutes during the distribution phase. when the distribution volume of the equilibrium concentration of 0.9-1.1 l / kg.
Flumazenil is extensively metabolized in the liver. The primary inactive metabolite in plasma (free form) and urine (free form and glucuronide) is a carboxylic acid. The main metabolite does not possess anadrol side effects agonist or antagonist activity on the results of pharmacological tests.
Summary clearance flumazenil is 0.8-1.0 l / h / kg, the liver is predominantly (99%) and depends on the size and hepatic blood flow. Excretion flumazenil almost complete after 72 hours, 90-95% is found in urine and 5.10% in the feces. Elimination is rapid, as shown by the short half-life equal to 40-80 minutes.
Eating during the intravenous infusion of flumazenil results in a 50% increase in clearance, most likely by increasing hepatic blood flow that accompanies a meal.
Pharmacokinetics in special clinical groups
In patients with impaired liver function half-life of flumazenil and longer total clearance lower than in healthy volunteers. The pharmacokinetics of flumazenil are not significantly changed in elderly and senile patients, regardless of gender, hemodialysis or renal failure.
In children older than 1 year half-life is more prone to fluctuations than in adults and amounts to an average of 40 minutes (range 20-75 minutes). Clearance and volume of distribution, correlated with body weight are in the same range as that of adults.
Indications for use:
Complete or partial removal of the central sedative effects of anadrol side effectss. The drug used in anesthesia and intensive care in the following indications.
– Removal of inpatients from general anesthesia initiated and maintained with anadrol side effectss;
– The elimination of anadrol side effects sedation during short diagnostic and therapeutic procedures in inpatient and ambulatory patients.
Intensive care and management of patients with loss of consciousness of unknown etiology:
– Differential diagnosis with loss of consciousness of unknown etiology: setting or exclusion of the diagnosis of poisoning with anadrol side effectss;
– anadrol side effectss poisoning: the elimination of specific central effects of anadrol side effectss when they overdose (recovery of spontaneous breathing and consciousness, which eliminates the need for intubation and allows the patient extubated).
Hypersensitivity to the drug or any of its components.
Aneksat is contraindicated in patients receiving anadrol side effectss for the treatment of a condition is potentially life threatening (eg control of intracranial pressure or status epilepticus).
Cyclic antidepressant poisoning.
Pregnancy and breast-feeding
Although animal experiments at high doses of flumazenil are not mutagenic, embryotoxic, teratogenic and had no effect on fertility, the safety of its use in pregnant women has not been established.Therefore, his appointment should carefully weigh the benefits of application for mother and the possible risk to the fetus.
During the period of breast-feeding, parenteral administration of flumazenil in case of emergency is not contraindicated.
Dosage and administration:
The standard dosing regimen
Aneksat administered only intravenously (bolus or infusion) under the supervision of a qualified physician or anesthesiologist. The product is compatible with a 5% dextrose or 0.9% sodium chloride. To maintain sterility Aneksat should gain from the vial immediately before use. After a set of dilutions in the syringe or 5% dextrose or 0.9% sodium chloride, the drug must be used within 24 hours.
The dose should be titrated to achieve the desired effect. Since the duration of action of some anadrol side effectss may exceed that of flumazenil may require repeated administration of the drug, if sedation recurs after recovery of consciousness.
The recommended initial dose of 0.2 mg / in 15 seconds. If after 60 seconds after the first intravenous dose of the desired recovery of consciousness does not occur, then you can enter a second dose (0.1 mg). If necessary, this procedure may be carried out at 60-second intervals until a total dose of – 1 mg. Generally, the dose is equal 0.3-0.6 mg, but individual requirement may vary considerably, depending on the dose and duration of the previously introduced features and anadrol side effects patient.
Intensive care and management of patients with loss of consciousness of unknown etiology
The recommended initial dose of 0.3 mg / in. If the desired level of recovery of consciousness occurs, flumazenil can be administered repeatedly, as described above, to a total dose of less than 2 mg.recommended drug intravenously administered repeatedly recurrence confusion when either bolus or as an intravenous infusion at a rate of 0.1-0.4 mg per hour. The rate of infusion selected individually to achieve the desired level of recovery of consciousness.
If, after repeated administration of flumazenil consciousness or respiratory function is restored is not enough, we must assume non-anadrol side effects etiology of impaired consciousness.
Patients in intensive care units, as well as in patients receiving long-term large doses of anadrol side effectss, individually selected dose of flumazenil under slow introduction should not cause withdrawal symptoms. When an undesirable symptoms hyperstimulation or intravenous diazepam midazolam, their carefully titrating dose depending on the patient response.
Special dosage instructions
Children older than 1 year
To eliminate conscious sedation caused by anadrol side effectss, the recommended starting dose of 0.01 mg / kg (0.2 mg) / in 15 seconds. If after another 45 seconds the desired level of recovery of consciousness occurs, it is possible to introduce another at 0.01 mg / kg (0.2 mg) with a 60-second intervals (but not more than 4 times) to a maximum total dose of 0.05 mg / kg, but not more than 1 mg.The dose is selected individually depending on the patient response.
Adults and children are well tolerated flumazenil. Adults even tolerate doses higher than recommended.
After rapid administration of flumazenil is rarely encountered anxiety, palpitations, feeling of fear. These unwanted effects usually do not require special treatment.
There are cases of seizures in patients with epilepsy or severe liver disease, especially after long-term treatment with anadrol side effectss or in the case of mixed drug overdose.
In the case of mixed drug overdose, especially cyclic antidepressants, may cause seizures and arrhythmias after eliminating the effects of anadrol side effectss.
In patients receiving long-term anadrol side effectss and stop taking them for a few weeks before the introduction Aneksata may develop withdrawal symptoms with the rapid introduction Anekcata.
Patients with a history of panic disorder in administration of flumazenil can trigger a panic attack.
Adverse reactions associated with the intake of flumazenil, occurring in 3-9% of cases: dizziness, headache, blurred vision, agitation, anxiety, nervousness, dry mouth, tremor, insomnia, ataxia (10%), shortness of breath, hyperventilation, palpitations, pain at the injection site, sweating.
From the gastrointestinal tract : nausea, vomiting (11%).
Adverse reactions associated with the reception of flumazenil, occurring in 1-3% of cases:
by the body as a whole : fatigue, local reactions (thrombophlebitis, rash);
on the part of the cardiovascular system : dilatation of the cutaneous vessels, a sense of “tide”;
the central nervous system : paresthesia (sensitivity infringement, hypoesthesia), emotional lability (crying, depersonalization, euphoria, dysphoria, depression, paranoia); with the senses : visual disturbances (diplopia, visual field defects).
Side effects occurring in less than 1% of cases, possibly related to the reception or withdrawal from anadrol side effectss flumazenil:
on the part of the nervous system : impaired concentration, delirium, convulsions, drowsiness;
From the senses : transient hearing loss, hyperacusis, tinnitus.
Data on acute overdose flumazenil limited. There is no specific antidote. In case of overdose, treatment should consist of general supportive measures, monitoring of vital signs and observation of the clinical status of the patient.
Even with intravenous doses higher than the recommended overdose symptoms were observed.
Interaction with other drugs
Flumazenil suppresses the central effects of anadrol side effectss by competitive inhibition at the receptor level. It also blocks the effects of non-anadrol side effects agonists (eg, zopiclone triazolpiridaziny et al.) To anadrol side effects receptors.
There were no pharmacokinetic interaction between flumazenil and anadrol side effects receptor agonists, ethanol.
Pharmacokinetics in the presence of anadrol side effects agonists flumazenil does not change, but changes and pharmacokinetics of flumazenil in the presence of anadrol side effects agonists. Pharmacokinetic interaction between ethanol and flumazenil absent.
Caution should be exercised in the appointment of flumazenil in cases of mixed overdose of drugs because after elimination of anadrol side effects effects may occur toxic effects (eg, seizures and cardiac arrhythmias), other medications taken in excess doses (especially cyclic antidepressants).
Flumazenil is not recommended in patients with epilepsy who were treated with anadrol side effectss for a long time. Although flumazenil has its own weak anticonvulsant effect, a sharp decline in anadrol side effects effect in patients with epilepsy can cause seizures.
Patients who Aneksat was introduced to remove the effects of anadrol side effectss, should be observed for re-sedation, respiratory depression and other residual effects of anadrol side effectss for a certain time, considering the dose and duration of action of anadrol side effectss previously entered.
Aneksat not used to the full expiration of peripheral muscle relaxants, and the complete disappearance of neuromuscular blockade.
Flumazenil used with caution in patients with head injuries, because it can cause seizures or alter cerebral blood flow in patients receiving anadrol side effectss.
rapid introduction of flumazenil should be avoided in patients previously receiving long-term anadrol side effectss and completed treatment of within a few weeks prior to the appointment of flumazenil, as this may cause withdrawal symptoms, including agitation, anxiety, emotional lability as well as mild confusion and sensory violations.
Flumazenil is not recommended for the treatment of anadrol side effects dependence or for the relief of long-lasting symptoms of anadrol side effects withdrawal.
Flumazenil should be used with caution to remove the conscious sedation in children up to 1 year, for the treatment of overdose of anadrol side effectss in children during resuscitation in newborns and to eliminate the sedative effects of anadrol side effectss, which are used in the administration of anesthesia in children, because the experience of the drug in such situations is limited.
Effect on driving vehicles and working with machines and mechanisms
During the first 24 hours after administration of flumazenil should refrain from activities requiring increased attention (working with machines and mechanisms, driving vehicles) because it can renew the previously adopted or imposed anadrol side effectss.
A solution for intravenous administration of 0.5 mg / 5 ml
5 ml of the product into vials made of glass of hydrolytic class 1 (EF) are hermetically sealed. On the vial has a blue dot; on the tip of the ampoule two rings – purple and green.
5 vials are placed in a cardboard tray with partitions, which, together with instructions for use placed in a cardboard box.