Relium

Relium – психолептик, renders somnolent, anticonvulsant, sedative, anxiolytic, myorelaxation action.

Form of release and structure

Dosage forms:

• Solution for intravenous (in/in) and intramuscular introduction (in oil): transparent or slightly opalescent liquid, from colourless before chartreuse coloring (on 2 ml in glass colourless ampoules, on 5 ampoules in the pallet, in a cardboard pack of 1, 2 or 10 pallets);
• Tablets, coated (on 20 pieces in the blister, in a cardboard pack 1 blister).

For in/in and introductions in oil contains in 1 ml of solution:

• Active ingredient: diazepam – 5 mg;
• Auxiliary components: sodium benzoate, benzyl alcohol, the benzoic acid, alcohol (ethanol of 96%), propylene glycol, water for injections.

In 1 tablet, coated, contains:

• Active ingredient: diazepam – 5 mg;
• Auxiliary components: twin 80, potato starch, quinolinic yellow (E104), magnesium stearate, lactose, gelatin, talc;
• Structure of a cover: polyethyleneglycol 6000, cellulose acetate phthalate.

Indications to use

• Sleep disorders;
• Conditions of alarm, neurosises, including against the background of oncological pathologies, an arterial hypertension, heart failure, a peptic ulcer of a stomach and a duodenum;
• Epilepsy, epileptic status;
• Spasms of muscles of the central origin;
• Tension of skeletal muscles at posttraumatic states and motive rehabilitation (for the purpose of undervoltage);
• Abstinence at alcoholism;
• Eclampsia;
• Tetanus;
• Pernicious vomiting;
• Premedication in surgical practice and at diagnostic procedures.

Contraindications

• The expressed respiratory insufficiency of various etiology, disorder of breath of the central origin;
• Consciousness disturbance;
• Glaucoma;
• Myasthenia;
• Period of pregnancy and feeding by a breast;
• Depressions with suicide attempts;
• Shock, coma, head injuries;
• Acute intoxication alcohol, narcotic, somnolent, psychotropic drugs;
• Individual intolerance of components of drug.

Besides, it is contraindicated in/in administration of solution at an absentia epileptica or Lennox-Gasto's syndrome, in/in and introduction in oil aged up to 5 weeks of life.

It is impossible to apply tablets at children under 2 years.

With care patients should appoint Relium at a liver and/or renal failure, a cerebral and spinal ataxy, a hyperkinesia, organic diseases of a brain, the psychosis (risk of paradoxical reactions), a hypoproteinemia established or an estimated apnoea during sleep, at advanced age, at the instruction in the anamnesis to epilepsy, epileptic seizures, the dependence phenomena.

Route of administration and dosage

Solution for in/in and introductions in oil
Solution is intended for in oil and in/in jet or drop introduction.

Solution in oil is entered deeply into large muscles.

For in/in jet introductions of 2 ml of drug mix from 8 ml 5% of solution of glucose or normal saline solution, rate of administering – no more than 4 ml 1 minute.

For in/in drop introductions of 20 ml (10 ampoules) of Relium dissolve in 500 ml 5% of solution of glucose or normal saline solution, rate of administering – 40 ml within 60 minutes.

The recommended dosing for in/in or introductions in oil by the adult patient:

• Acute cases of alarm and concern: on 2-5 mg of 1 times a day, for achievement of clinical effect – in the same dose repeatedly in 180-240 minutes;
• Phobic frustration in a severe form: 5-10 mg, if necessary in 180-240 minutes are shown repeated introduction in the same dose;
• Alcoholic abstinence syndrome: 10 mg once, for achievement of clinical effect in 180-240 minutes it is possible to enter 5-10 mg in addition;
• Tetanus, athetosis, muscular spasms: 5-10 mg, are in case of need possible increase in a dose;
• Hard cases of recurrent convulsive attacks, epileptic status: the initial dose – 5-10 mg once, then in 10-15 minutes and 120-240 minutes is allowed repeated introduction, but no more than 30 mg totally;
• Premedication: in/in slowly – 10 mg, in the absence of simultaneous use of narcotic analgetics – to 20 mg, or in oil – 5-10 mg in 30 minutes prior to the procedure.

When using drug in a countershock to the patient in/in enter in 5-10 minutes prior to the procedure 5-10 mg.

Patients from the liver broken functions and/or kidneys need to lower a dose.

At advanced age or at the weakened condition of the patient it is recommended to appoint 1/2 usual doses.

The recommended dosing in pediatrics:

• Tetanus: aged from 5 weeks of life up to 5 years – 1-2 mg, of 5 years are also more senior – 5-10 mg; the drug is administered in oil or slowly in/in, for achievement of desirable effect perhaps repeated introduction in 180-240 minutes;
• Epileptic status, heavy recurrent convulsive attacks: under control of respiratory function in/in slowly – to babies from 5 weeks of life to 5 years (with a speed of 0,2-0,5 mg within 2-5 minutes) – no more than 5 mg, of 5 years are also more senior (with rate of administering of 1 mg within 2-5 minutes) – no more than 10 mg. For achievement of clinical effect the procedure is repeated in 120-240 minutes.

Tablets, coated
Pill is taken inside.

The dose and the period of use are appointed by the doctor on the basis of clinical indications.

The recommended dosing for adults:

• Sleeplessness: quickly on 5-10 mg in 30 minutes prior to a dream;
• Alcoholic abstinence syndrome: on 10 mg 3 times a day, the maximum daily dose – 60 mg;
• Spastic conditions of muscles: on 5 mg 1-3 times a day, if necessary it is possible to increase a daily dose to 60 mg.

The recommended daily dosing for children:

• 2-3 years: 2-5 mg;
• 4-7 years: 4-6 mg;
• 8-18 years: 5-8 mg.

The daily dose for children in proportion is divided into 2-3 receptions.

Side effects

• Nervous system: at the beginning of use (especially at patients at advanced age) – slackness, increased fatigue, obtusion of emotions, disturbance of concentration of attention, delay of motor and mental reactions, antegrade amnesia; headache, drowsiness, dizziness, confusion of consciousness, reaction delay, ataxy, disorientation; seldom – depression of mood, euphoria, catalepsy, the uncontrollable movements of a body and an eye, a dysarthtia, a hyporeflexia; paradoxical reactions – aggression flashes, fear, psychomotor excitement, a muscular spasm, suicide bent, hallucinations, confusion of consciousness, acute excitement, uneasiness, sleeplessness, irritability, a depression;
• Cardiovascular system: lowering of arterial pressure, heartbeat, tachycardia;
• Bodies of a hemopoiesis: anemia, neutropenia, leukopenia, thrombocytopenia, agranulocytosis (weakness, hyperthermia, fever, pharyngalgia, feeling of fatigue);
• Alimentary system: heartburn, dryness in a mouth, vomiting, a hiccups, a gastralgia, anorexia, increase in activity of liver enzymes, abnormal liver functions, jaundice;
• Allergic reactions: very seldom – a skin itch, rash, a small tortoiseshell, anaphylactic reactions;
• Urinogenital system: disturbances libido, dysmenorrhea, renal failure;
• Influence on a fruit: oppression of the central nervous system, teratogenecity (especially in the I trimester of pregnancy), breath disturbance, disturbance of a sucking reflex;
• At use in obstetrics: hypothermia, muscular hypotension, диспноэ;
• Others: medicinal dependence, accustoming; seldom – dysfunction of external respiration, oppression of a respiratory center, weight reduction of a body, disturbance of clearness of sight, a diplopia, bulimia; against the background of a sharp dose decline or drug withdrawal – a withdrawal; at bystry in introduction – respiratory depression and blood circulations;
• Local reactions: (at introduction in oil) sometimes – phlebitis; often – pain, an erythema in the place of an injection.

Special instructions

At organic changes of a brain (it is recommended to avoid parenteral administration), respiratory and heart failure, a myasthenia, closed-angle glaucoma or predisposition to it should apply diazepam with extra care.

Under observation of the doctor, especially at the beginning of therapy, it is necessary to appoint drug against the background of prolonged use of beta adrenoblockers, anti-hypertensive central acting agents, anticoagulants, cardiac glycosides.

The gradual dose decline at Relium cancellation as the sudden termination can cause excitement, concern, spasms, a tremor is required.

Alcohol intake during treatment is categorically contraindicated.

At emergence of paradoxical reactions diazepam should be cancelled.

At administration of drug in oil increase in activity of a kreatinfosfokinaza in a blood plasma is possible.

Intra arterial introduction is not allowed.

For treatment it is necessary to refuse control of vehicles and mechanisms.

Medicinal interaction

At simultaneous use of Relium:

• Neuroleptics, opioid analgetics, sedative and hypnagogues, drugs for an anesthesia and other drugs oppressing the central nervous system (CNS) – strengthen the oppressing influence on a respiratory center and TsNS, promote emergence of the expressed arterial hypotension;
• Muscle relaxants – strengthen the action, increasing risk of developing of an apnoea;
• Tricyclic antidepressants (including amitriptyline) – increase cholinergic effect, the oppressing influence on TsNS, level of concentration of antidepressants;
• Oral contraceptives – activity of diazepam increases, the risk of development of breakthrough bleedings increases;
• Caffeine – reduces sedative, anxiolytic effect of diazepam;
• Antiepileptic means (Phenytoinum, carbamazepine) and other drugs causing induction of enzymes of a liver – accelerate diazepam removal;
• Clozapine – promotes development the expressed arterial hypotension, a loss of consciousness, respiratory depression;
• Metoprolol – risk of deterioration in psychomotor reactions, decrease in visual acuity;
• The levodopa – can lose protivoparkinsonichesky action;
• Lity a carbonate – coma development is possible;
• Risperidon – risk of development of a malignant antipsychotic syndrome;
• Paracetamol – reduces excretion of diazepam and its metabolite;
• Rifampicin – strengthens metabolism of diazepam and accelerates its removal;
• Theophylline – breaks drug sedation;
• Cimetidinum, Disulfiramum, омепразол – can increase intensity and duration of effect of diazepam;
• Fluvoksamin – promotes increase in level of concentration of diazepam in a blood plasma and to development of the undesirable phenomena;
• Phenytoinum, phenobarbital – can cause diazepam metabolism acceleration;
• Bupivacaine – increases the contents in a blood plasma;
• Diclofenac – causes strengthening of dizziness;
• The isoniazid – slows down removal of diazepam from an organism;
• Ethanol, etanolsoderzhashchy drugs – strengthen the oppressing action on a respiratory center and TsNS in general, increase risk of emergence of a syndrome of pathological intoxication.

Drug oppresses metabolism of Phenytoinum and strengthens its action.

The mechanism and extent of medicinal interaction at reception of Relium against the background of long preliminary therapy by beta adrenoblockers, anti-hypertensive central acting agents, anticoagulants, cardiac glycosides are unpredictable.

Terms and storage conditions

To store in the unavailable to children, protected from light place at a temperature up to 25 °C, to protect tablets from moisture.

Period of validity – 3 years.