Diazepam: instructions for using the medicine, structure, Contraindications

When ATH: N05BA01

Diazepam: characteristic

Anxiolytic, benzodiazepine derivative.

White or white with a faint yellowish tinge crystalline powder with a molecular weight 284,74. Practically insoluble in water, it is soluble in alcohol, soluble in chloroform.

Diazepam: pharmachologic effect

Anxiolytic, anticonvulsant, miorelaksiruyuschee, central, sedation, snotvornoe.

Diazepam: application

As sedation, anxiolytic and hypnotic.

Neurology and Psychiatry. All types of anxiety disorders, incl. neuroses, psihopatii, and psihopatopodobnyh state, accompanied by anxiety, fear, increased irritability, emotional stress; anxious syndrome in endogenous mental diseases, incl. schizophrenia (aid in the complex therapy), with organic brain lesions, incl. cerebrovascular diseases (in combination therapy as an adjunct); senesto-hypochondriacal, obsessive and phobic disorders, paranoid-hallucinatory state; somatovegetativnye violation, motor stimulation of different etiologies in neurology and psychiatry; tension headache; sleep disorders; vertebral syndrome; abstinence symptom (alcohol, drugs), incl. delirium tremens (in the complex therapy). In pediatric practice: neurotic and neurosis-like states, accompanied by emotional stress, anxiously, fear, increased irritability, headache, sleep disorders, enuresis, disorders of mood and behavior, etc.. Cardiology. Angina, myocardial infarction, hypertension, etc.. Anesthesiology and Surgery. Premedication before and immediately before surgery and endoscopic procedures, induction of anesthesia, as a component of a combined anesthetic (at ataralgezii in combination with analgesics). Obstetrics and gynecology. Eclampsia, facilitating labor (for parenteral administration), miscarriage, premature detachment of the placenta (for parenteral administration); menopausal and menstrual psychosomatic disorders. Dermatological practice. Eczema and other diseases, accompanied by itching, irritability (Combination Therapy).

As anticonvulsants.

Epilepsy (adjuvant, in a combination therapy), status epilepticus and severe recurrent seizures (for parenteral administration, adjuvant); stolbnyak.

As a means of miorelaksiruyuschego.

Spasms of central origin, associated with damage to the brain or spinal cord (cerebral paralysis, athetosis); spasm of skeletal muscle at a local trauma (adjuvant); spasticskie of other diseases of the musculoskeletal system-Myositis, ʙursit, arthritis, revmaticheskiy spondylitis, progressive chronic polyarthritis; arthrosis, accompanied by skeletal muscle strain.

Diazepam: Contraindications

Hypersensitivity, acute liver disease and kidney failure, severe hepatic insufficiency, myasthenia gravis, suicidal, drug or alcohol dependence (except for the treatment of acute withdrawal syndrome), severe respiratory failure, expressed hypercapnia, tserebralynaya and spinalynaya ataxia, acute attack of glaucoma, zakrыtougolynaya glaucoma, pregnancy (I trimester), lactation, Age to 30 days.

Diazepam: restrictions on use

Chronic respiratory failure, syndrome, sleep apnea, expressed by the human kidney, otkrыtougolynaya glaucoma (against the background of adequate therapy), Age to 6 Months (Only for health reasons in the hospital), pregnancy (II and III trimester).

Diazepam: use during pregnancy and lactation

It contraindicated in I trimester of pregnancy (It increases the risk of congenital malformations). In II and III trimester of pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Diazepam: side effects

From the nervous system and sensory organs: slackness, drowsiness, fatigue; ataxia, blunting of emotions, blurred vision, diplopia, nistagmo, tremor, reaction speed and concentration, deterioration in short-term memory, dysarthria, slurred speech; confusion, depression, fainting, headache, dizziness; paradoxical reactions (severe agitation, alarm, hallucinations, nightmares, fits of rage, misbehavior); anterogradnaya amnesia.

Cardio-vascular system and blood (hematopoiesis, hemostasis): bradycardia, neutropenia.

From the digestive tract: violation of salivation (dry mouth or hypersalivation), nausea, constipation.

Other: allergic reactions (hives, rash), urinary incontinence, urinary retention, changes in libido, increase in liver transaminases and alkaline phosphatase, jaundice.

For parenteral administration: injection site reactions (thrombosis, phlebitis, the formation of infiltrates); with the rapid on/in the introduction-gipotenzia, cardiovascular collapse, violation of the respiratory function, Ikotech.

Perhaps the development of addiction, Drug Dependence, withdrawal, aftereffect syndrome (muscular weakness, decreased performance), rebound-синдрома (cm. Precautions).

Diazepam: interaction

Potentiates the effects of alcohol, anticonvulsants and antihypertensives, neuroleptics, tricyclic antidepressants, analgesics (incl. narcotic analgesics), hypnotic drugs, general anesthetics, muscle relaxants, antihistamine drugs with sedative effect. Analeptiki, psychostimulants-reduce activity. Antacids may decrease the speed, but not the extent of absorption of diazepam.

Isoniazid slows excretion of diazepam (and increases its concentration in blood). Inhibitors of microsomal oxidation (incl. cimetidine, ketoconazole, fluvoxamine, fluoxetine, omeprazole) alter the pharmacokinetics and increase the duration of the effect of diazepam. Rifampicin reduces the concentration of diazepam in the blood. Erythromycin slows the metabolism of diazepam in the liver. Diazepam may alter plasma concentrations of phenytoin.

Diazepam: overdose

Symptoms: CNS depression of varying severity (from drowsiness to coma): severe drowsiness, slackness, weakness, decreased muscle tone, ataxia, prolonged confusion, oppression reflexes, coma; also possible hypotension, respiratory depression.

Treatment: induction of vomiting and the appointment of activated carbon (If the patient is conscious), Gastric lavage through a tube (If the patient is unconscious), simptomaticheskaya therapy, monitoring vital functions, in / in a liquid (to enhance diuresis), if necessary, ventilation. In the development field should not be used barbiturates. As a specific antidote used benzodiazepine receptor antagonist flumazenil (in hospital). Hemodialysis maloeffyektivyen.

Diazepam: Dosing and Administration

Inside, I /, / m, rectally. The mode set is strictly individual, depending on the evidence, the disease, portability, etc.. Treatment should start with the lowest effective dose, corresponding specific form of pathology.

Usual adult dosage when administered: Elementary-5-10 mg, daily — 5-20 mg, the maximum single- 20 mg, the maximum daily 60 mg.

The on/in and/m introduction the average single dose for adults is 10 mg, average daily — 30 mg, the maximum single- 30 mg, the maximum daily 70 mg. The duration of treatment with parenteral administration should not exceed 3-5 days (then, if necessary, moving to a reception inside), the total duration of treatment should be as short as possible and should not exceed 2-3 months (including the period of gradual reduction of the dose). Increasing the duration of treatment in excess of 2-3 months is possible only after repeated careful assessment of the patient. Before re-rate the break must be at least 3 Sun.

The dose and duration of treatment for children picked individually, depending on the nature of the disease, age, body weight of the child.

Patients in elderly, as well as in patients with impaired liver function should begin treatment with lower doses.

Diazepam: precautions

Not recommended for monotherapy of benzodiazepines in combination with depression anxiety (possible suicide attempts). Due to the possibility of paradoxical reactions, incl. aggressive behavior, used with caution in patients with personality and behavioral disorders. Paradoxical reactions occur more often in children and elderly patients. In the event of paradoxical reactions diazepam should be discontinued.

During treatment with diazepam is unacceptable consumption of alcoholic beverages.

Should not be used during the drivers of vehicles and people, whose work requires quick mental and physical reactions, and is associated with high concentration of attention.

Diazepam in children under 14 years is allowed only in well justified cases, the duration of treatment should be minimal.

When receiving diazepam (Even at therapeutic doses) may develop addiction, formation of physical and psychological dependence. The risk of dependence increases when using large doses and with increasing duration of administration, as well as in patients with drug and alcohol addiction in history. Abolition of diazepam should be gradual, by reducing the dose, to reduce the risk of withdrawal and rebound-syndrome. When abrupt cancellation after long-term use or high doses occurs withdrawal (headache and muscle pain, anxiety, alarm, confusion, tremor, convulsions), in severe cases, depersonalization, hallucinations, seizures (abrupt withdrawal of epilepsy). Transient syndrome, whereby symptoms, served as the reason for the appointment of diazepam, resumed in a more pronounced form (rebound-синдром), It may also be accompanied by changes in mood, anxiety, etc..

Prolonged use should be periodically monitored picture peripheral blood and liver function.

Use at doses above 30 mg (especially the / m or /) during 15 hours before giving birth can cause neonatal apnea, gipotenziю, gipotermiю, rejection of the breast, etc..

There are cases of benzodiazepine addiction.

Diazepam: Special instructions

It should be taken into account, that anxiety or stress, associated with daily stress, usually does not require treatment with anxiolytics.

Not be mixed in the same syringe with other drugs diazepam (possible deposition of the drug on the walls). The on / in the introduction should be administered in a large vein and slowly, Monitoring respiratory function. Avoid getting the solution in the artery and extravasal space.

Diazepam: interaction

Active substanceDescription of interaction
AzelastinFMR: synergism. Strengthens (mutually) effect on the CNS (It degrades the performance of the central nervous system and reduces the speed of psychomotor reactions).
AlprazolamFMR: synergism. Strengthens (mutually) CNS depression; in the background I / O administration of diazepam increases the risk of apnea.
BuprenorphineFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the diazepam dose should be reduced, at least, on 1/3 — deprimacija and deepens the risk of apnea.
BuspironeFMR: synergism. Strengthens (mutually) effect; in the background I / O administration of diazepam increases CNS depression and increased risk of sleep apnea.
Sodium valproateFMR. Against the background of the effect of diazepam attenuated; with a joint appointment is not possible increase in the frequency and / or severity of seizures grand mal, which may require increased doses.
Valproic AcidFMR. Against the background of the effect of diazepam attenuated; with a joint appointment is not possible increase in the frequency and / or severity of seizures grand mal, which may require increased doses.
VenlafaxineFMR: synergism.

Do effect.

HaloperidolFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea.
GidroksizinFMR: synergism. Strengthens (mutually) effect; in the background I / O administration of diazepam increases CNS depression and increased risk of sleep apnea.
GlipizideFKV. FMR: synergism. Against the background of diazepam, has a greater ability to bind to plasma proteins, may increase the effect (gipoglikemiâ).
DisulьfiramInhibits microsomal enzymes, inhibits the biotransformation, increases plasma concentration.
DifengidraminFMR: synergism. Against the backdrop of intensified hypnotic effect of diazepam.
DroperidolFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea.
ZolpidemFMR: synergism. Increases (mutually) effects. Against the background of / in the introduction of diazepam is enhanced CNS depression and increased risk of sleep apnea.
IsoniazidFKV. Slowing down the excretion, increases the concentration in the tissues.
IzofluranFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea.
ItraconazoleFKV. FMR: synergism. Biotransformation slows and increases the plasma concentration (It strengthens and extends the hypnotic and sedative effects)
CarbamazepineFKV. FMR. Stimulates biotransformation, reduces the concentration in the blood, and T1/2. Against the background of diazepam antiepileptic effect is reduced: it is possible more frequent attacks grand mal, which may necessitate increasing the dose.
QuetiapineFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea.
KetamineFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea.
KetoconazoleFKV. FMR: synergism. Biotransformation slows and increases the plasma concentration (It strengthens and extends the hypnotic and sedative effects).
KlozapynFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea.
ClonazepamFMR: synergism. Strengthens (mutually) CNS depression; with a joint appointment in the convulsive disorders may increase the frequency and / or severity of seizures grand mal, which may lead to the need to increase the dose of clonazepam.
CodeineFMR: synergism.

Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea, therefore, the dose should be reduced, at least, on 1/3.

LamotrigineFMR. Against the background of the effect of diazepam attenuated, and it may increase the frequency and / or severity of attacks grand mal, which may require increased doses.
LevetiracetamFMR. Against the background of the effect of diazepam attenuated, and does not exclude more frequent attacks grand mal, which may necessitate increasing the dose.
Levothyroxine sodiumFKV. Against the background of diazepam changed distribution and biotransformation.
LorazepamFMR: synergism. Do effect. Against the background of / in the introduction of diazepam increases CNS depression and increased risk of sleep apnea.
MaprotilinFMR: synergism.

Do effect.

MidazolamFMR: synergism. Increases (mutually) effects. Against the background of / in the introduction of diazepam is enhanced CNS depression and increased risk of sleep apnea.
MirtazapineFMR: synergism. Strengthens (mutually) CNS depression; the combined appointment worsen cognitive function and motor coordination.
MoclobemideFMR: synergism.

Strengthens (mutually) effect.

Morphine sulfateFMR: synergism.

Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea, therefore, the dose should be reduced, at least, on 1/3.

OxazepamFMR: synergism. Do effect. Against the background of / in the introduction of diazepam increases CNS depression and increased risk of sleep apnea.
OlanzapineFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea.
OmeprazoleFKV. FMR. As an inhibitor of microsomal oxidation slows down and prolongs the effects of the elimination of.
OrnithineFV. The solutions are not compatible (should not be mixed "in the same syringe").
ParoxetineFMR: synergism. Enhances CNS depression.
PerfenazynFMR: synergism. Strengthens (mutually) CNS depression.
PramipexoleFMR: synergism. Sedative effect; In sharing caution.
PrymydonFMR. Against the background of the effect of diazepam attenuated, and it is possible more frequent attacks grand mal, which may necessitate increasing the dose.
ProcarbazineFMR: synergism.

Do effect.

PromethazineFMR: synergism. Strengthens (mutually) CNS depression.
PropofolFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea.
RisperidoneFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea; In sharing caution.
RifampicinFKV. Inducing system of microsomal enzymes, accelerates biotransformation, reduces the concentration in the blood, and T1/2 .
SelegilineFMR: synergism. Do effect.
SertralineFMR: synergism. Enhances CNS depression.
TioridazinFMR: synergism. Strengthens (mutually) CNS depression.
TopiramateFMR: synergism. Strengthens (mutually) CNS depression. Against the background of the effect of diazepam attenuated, and it is possible more frequent attacks grand mal, which may necessitate increasing the dose.
TrifluoperazineFMR: synergism. Strengthens (mutually) CNS depression.
PhenytoinFMR.

Against the background of the effect of diazepam attenuated, and it is possible more frequent attacks grand mal, which may necessitate increasing the dose.

PhenobarbitalFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea. Co-administration with epilepsy weakens the effect of phenobarbital, and does not exclude more frequent attacks grand mal, which may necessitate increasing the dose.
FentanylFMR: synergism.

Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea, therefore, the dose should be reduced, at least, on 1/3.

FluvoxamineFKV. As an inhibitor of microsomal oxidation slows down and prolongs the effect of elimination; concomitant use is not recommended.
FlufenazinFMR: synergism.

Strengthens (mutually) CNS depression.

XlordiazepoksidFMR: synergism. Strengthens (mutually) effect. Against the background of / in the introduction of diazepam increases the risk of apnea.
ChlorpromazineFMR: synergism.

Strengthens (mutually) CNS depression.

ChlorprothixeneFMR: synergism. Strengthens (mutually) CNS depression. Against the background of / in the introduction of diazepam increases the risk of apnea.
CetirizineFMR: synergism. Strengthens (mutually) effect on the CNS (It degrades the performance of the central nervous system and reduces the speed of psychomotor reactions).
EʙastinFMR. Strengthens (mutually) CNS depression.
ErythromycinFKV. Slows biotransformation, increases the concentration in plasma.
EthanolFMR: synergism. Strengthens (mutually) CNS depression.
EthosuximideFMR. Against the background of the effect of diazepam attenuated, and it may increase in frequency and / or severity of seizures grand mal, which may require increased doses.

Back to top button