Buy Phenazepam pills 2.5 mg 50 pcs
  • Buy Phenazepam pills 2.5 mg 50 pcs

Phenazepam®

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2019-06-23
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Clinical Pharmacology

Pharmacotherapeutic group:
anxiolytic agent (tranquilizer).
ATH code:
[N05ВХ]
Pharmacological properties
Anxiolytic agent (tranquilizer) benzodiazepine series. It has anxiolytic, sedative-hypnotic, anticonvulsant and central muscle relaxant effect.
Pharmacodynamics
Strengthens the inhibitory effect of gamma-aminobutyric acid (GABA) on the transmission of nerve impulses. Stimulates benzodiazepine receptors located in the allosteric center of the postsynaptic GABA receptors of the ascending activating reticular formation of the brain stem and the intercalary neurons of the lateral horns of the spinal cord; reduces the excitability of the subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes.
Anxiolytic effect is due to the effect on the almond-shaped complex of the limbic system and is manifested in the reduction of emotional stress, easing anxiety, fear, anxiety.
Sedation is due to the effect on the reticular formation of the brain stem and the nonspecific nuclei of the thalamus and is manifested by a decrease in the symptoms of neurotic origin (anxiety, fear).
The productive symptoms of psychotic genesis (acute delusional, hallucinatory, affective disorders) practically do not affect, a decrease in affective tension, delusional disorders is rarely observed.
The hypnotic effect is associated with inhibition of the cells of the reticular formation of the brain stem. Reduces the impact of emotional, vegetative and motor stimuli that violate the mechanism of sleep.
Anticonvulsant action is implemented by enhancing presynaptic inhibition, suppresses the spread of convulsive impulse, but does not remove the excited state of the focus. The central muscle relaxant effect is due to the inhibition of polysynaptic spinal afferent inhibitory pathways (to a lesser extent and monosynaptic). Direct inhibition of motor nerves and muscle function is also possible.
Pharmacokinetics
After ingestion is well absorbed from the gastrointestinal tract (GIT), the time to reach the maximum concentration (TCmax) in the blood plasma is 1-2 hours. Metabolized in the liver. The elimination half-life (T1 / 2) is 6-10-18 hours. It is mainly excreted by the kidneys as metabolites.

Indications

The drug is used in various neurotic, neurosis-like psychopathic, psychopathic and other conditions, accompanied by anxiety, fear, increased irritability, tension, emotional lability. With reactive psychosis, hypochondria-senesthopathic syndrome (including those resistant to other tranquilizers), autonomic dysfunction and sleep disorders, for the prevention of states of fear and emotional stress.
As an anticonvulsant - temporal and myoclonic epilepsy.
In neurological practice, Phenazepam® is used to treat hyperkinesis and tics, muscle stiffness, vegetative lability.

Composition

1 tablet contains:
active ingredient: Bromdihydrochlorophenylbenzodiazepine (Phenazepam) - 0.5 mg or 1 mg or 2.5 mg;
excipients: lactose monohydrate - 81.5 mg or 122.0 mg or 161.5 mg, potato starch -15.0 mg or 22.5 mg or 30.0 mg, croscarmellose sodium (primelloza) - 2.0 mg or 3.0 mg or 4.0 mg, calcium stearate — 1.0 mg or 1.5 mg or 2.0 mg.

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Phenazepam®

Dosage and Administration

Inside: for sleep disorders - 0.5 MHz 20-30 minutes before sleep. For the treatment of neurotic, psychopathic, neurosis-like and psychopathic states, the initial dose is 0.5-1 mg 2-3 times a day. After 2-4 days, taking into account the effectiveness and tolerability of the dose can be increased to 4-6 mg / day.
With severe agitation, fear, anxiety, treatment begins with a dose of 3 mg / day, quickly increasing the dose to obtain a therapeutic effect.
In the treatment of epilepsy -2-10 mg / day.
For the treatment of alcohol withdrawal - inside, at 2-5 mg / day.
The average daily dose is 1.5-5 mg, it is divided into 2-3 doses, usually 0.5-1 mg in the morning and afternoon, and up to 2.5 mg per night. In neurological practice, for diseases with muscular hypertonus, 2-3 mg 1-2 times / day are prescribed.
The maximum daily dose is 10 mg.
In order to avoid the development of drug dependence during course treatment, the duration of phenazepam is 2 weeks (in some cases, the duration of treatment can be extended to 2 months). With the abolition of phenazepam reduce the dose gradually.

Adverse reactions

From the side of the central nervous system and peripheral nervous system: at the beginning of treatment (especially in elderly patients) drowsiness, feeling tired, dizzy, decreased ability to concentrate, ataxia, disorientation, instability of gait, slowing down of mental and motor reactions, confusion; rarely - headache, euphoria, depression, tremor, memory loss, impaired motor coordination (especially at high doses), depressed mood, dystonic extrapyramidal reactions (uncontrolled movements, including the pelvis), asthenia, muscle weakness, dysarthria, epileptic seizures (in ballroom epilepsy); extremely rarely - paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal tendency, muscle spasm, hallucinations, agitation, irritability, anxiety, insomnia).
On the part of the blood-forming organs: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia.
On the part of the digestive system: dry mouth or drooling, heartburn, nausea, vomiting, loss of appetite, constipation or diarrhea; abnormal liver function, increased activity of hepatic transaminases and alkaline phosphatase, jaundice.
On the part of the urogenital system: urinary incontinence, urinary retention, impaired renal function, decreased or increased libido, dysmenorrhea.
Allergic reactions: skin rash, itching.
Other: addiction, drug addiction; lowering blood pressure (BP); rarely impaired vision (diplopia), weight loss, tachycardia.
With a sharp decrease in dose or discontinuation of treatment, withdrawal syndrome (irritability, nervousness, sleep disturbances, dysphoria, smooth muscle spasm of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, including hyperacusia, paresthesia, photophobia, tachycardia, convulsions, rarely acute psychosis).

Coma, shock, myasthenia, angle-closure glaucoma (acute attack or predisposition), acute alcohol poisoning (with a weakening of vital functions), narcotic analgesics and hypnotics, severe chronic obstructive pulmonary disease (increased respiratory failure), acute respiratory failure, severe depression (suicidal tendencies may occur); pregnancy (especially the first trimester), lactation, children and adolescents under 18 years of age (safety and efficacy not determined), hypersensitivity (including to other benzodiazepines).
Carefully
Use with caution in hepatic and / or renal failure, cerebral and spinal ataxia, drug dependence in history, susceptibility to psychoactive drug abuse, hyperkinesia, organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, sleep apnea (established or presumptive ), elderly patients.

Drug interactions

With simultaneous use of phenazepam reduces the effectiveness of levodopa in patients with parkinsonism.
Phenazepam may increase zidovudine toxicity.
Mutual enhancement of the effect is noted with simultaneous use of antipsychotic, antiepileptic or hypnotic drugs, as well as central muscle relaxants, narcotic analgesics, ethanol.
Inhibitors of microsomal oxidation increase the risk of toxic effects. Inductors of liver microsomal enzymes reduce efficacy.
Increases the concentration of imipramine in the serum.
With simultaneous use with antihypertensive agents may increase antihypertensive action. Against the background of the simultaneous appointment of clozapine may increase respiratory depression.

Special instructions

In case of renal and / or hepatic insufficiency and long-term treatment, it is necessary to monitor the pattern of peripheral blood and the activity of liver enzymes.
In patients who have not previously taken psychoactive drugs, there is a therapeutic response to the use of phenazepam at lower doses, compared with patients taking antidepressants, anxiolytics, or those suffering from alcoholism.
Like other benzodiazepines, it has the ability to cause drug dependence with prolonged administration in large doses (more than 4 mg / suc). With a sudden cessation of treatment, withdrawal syndrome (including depression, irritability, insomnia, and increased sweating) may occur, especially with prolonged use (more than 8-12 weeks). If patients experience such unusual reactions as increased aggressiveness, acute states of arousal, fear, suicidal thoughts, hallucinations, increased muscle cramps, difficulty falling asleep, shallow sleep, treatment should be stopped.
In the process of treatment, it is strictly forbidden for patients to use ethanol.
The efficacy and safety of the drug in patients younger than 18 years has not been established.
Influence on ability to drive motor transport and control mechanisms
During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.

Overdosage

Symptoms: pronounced depression of consciousness, cardiac and respiratory activity, marked drowsiness, prolonged confusion, reduced reflexes, prolonged dysarthria, nystagmus, tremor, bradycardia, shortness of breath or difficulty breathing, decreased blood pressure, coma.
Treatment: gastric lavage, reception of Activated charcoal, hemodialysis is ineffective, control of vital body functions, maintenance of respiratory and cardiovascular activities, symptomatic therapy. Specific antagonist fpumazenil (in a hospital) (in / in 0.2 mg, if necessary, up to 1 mg in 5% glucose solution or 0.9% sodium chloride solution).

  • Brand name: Phenazepam
  • Active ingredient: Bromohydrochlorophenylbenzodiazepine
  • Dosage form: Pills
  • Manufacturer: Abbott

Studies and clinical trials of Phenazepam (Click to expand)

  1. The relation between the status of adaptive system and the number of postoperative complications in patients with gastrointestinal cancer: The effect of phenazepam
  2. Changes in postsynaptic excitation processes in the presence of the Soviet benzodiazepine derivative phenazepam
  3. Effect of phenazepam on ethanol intake in rats
  4. A model of the kinetics of blood levels of phenazepam and its metabolite 3-hydroxyphenazepam in cats
  5. Genetic differences in the antiseizure effect and metabolic rate of phenazepam
  6. Effect of diazepam and phenazepam on nervous regulation of the cerebral circulation
  7. Appraisal of the tranquilizing action of phenazepam and mebicar by the averaged cortical evoked potentials method during perception of emotionally meaningful words
  8. Phenazepam-induced dissociated state of reversible amnesia
  9. Role of GABA-ergic and dopaminergic mechanisms in the development of the “rebound” syndrome after cessation of long-term administration of phenazepam
  10. Protective action of phenazepam and sodium hydroxybutyrate on somatic manifestations of immobilization stress
  11. Effect of the specific benzodiazepine antagonist R015-1788 on inhibition of hippocampal unit activity evoked by phenazepam
  12. Character of correlation between the anticonvulsant action of phenazepam and its level in the mouse brain
  13. Effect of subchronic administration of phenazepam and synthetic antioxidants on cerebral cortical synaptic membrane function of rats exposed to long-term stress
  14. Intrahepatic circulation of14C-phenazepam and its metabolites in albino rats
  15. The use of mini pigs — A new kind of experimental animal — To study the embryotropic action of phenazepam
  16. Effect of pantogam, nicotinamide, and phenazepam on seizure activity
  17. Changes in antioxidative activity and composition of blood erythrocyte phospholipids induced in neurotic patients by phenazepam
  18. Distribution of14C-hydrogenated analog of phenazepam in some mouse organs and tissues
  19. Inherited differences in plasma cyclic nucleotide levels of mice exposed to stress and treated with phenazepam
  20. Hydroxylation of the aromatic and heterocyclic rings of the phenazepam molecule in the endoplasmic reticulum of albino rats and mice
  21. GABA-ergic mechanisms of cerebrovascular effects of phenazepam and diazepam
  22. Effect of the antioxidant dibunol, alone and combined with phenazepam, on conflict behavior in rats
  23. Role of the hippocampal theta rhythm in the mechanism of the anxiolytic action of phenazepam
  24. Effect of trifluoperazine and haloperidol on activity of phenazepam

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