Product Name: Diazepam
Common Brand Names: Valium
Pharmaceutical Category: Antidepressants / Anti Anxiety
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There is an additional general information about this medication active ingredient diazepam:
Diazepam is a benzodiazepine derivative tranquilizer. It provides anxiolytic, sedative, anticonvulsant, central muscle relaxant effect. The mechanism of action is associated with increased inhibitory effect of GABA in the CNS. Muscle relaxant effect is also due to the inhibition of spinal reflexes. This medication may cause anticholinergic effects.
Diazepam has rapid absorption. Cmax in plasma observed after 90 min. Plasma protein binding is 98%. Diazepam crosses the placental barrier into the cerebrospinal fluid; excreted in breast milk; metabolized in the liver; excreted by the kidneys - 70%.
Why is Diazepam prescribed?
neuroses, borderline states with symptoms of stress, restlessness, anxiety, fear
sleep disturbance, motor stimulation of various etiologies in neurology and psychiatry, withdrawal syndrome in chronic alcoholism
spastic conditions associated with lesions of the brain or spinal cord, and myositis, bursitis, arthritis, accompanied by a voltage of skeletal muscle
premedication before anesthesia as a component of combined anesthesia
relief labor, premature birth, abruptio placenta, tetanus
Dosage and administration
Diazepam prescribed for oral, IV, IM, rectal use. The daily dose of Diazepam ranges from 0.5 mg to 60 mg. Single dose, frequency and duration of use are set individually.
Diazepam side effects
CNS: drowsiness, dizziness, muscle weakness; rare - confusion, depression, blurred vision, diplopia, dysarthria, headache, tremor, ataxia; in single cases - a paradoxical response: excitement, anxiety, sleep disturbances, hallucinations. After IV injection is sometimes seen a hiccup. With prolonged use may develop drug dependence, memory impairment.
Digestive system: rarely - constipation, nausea, dry mouth, excessive salivation; in single cases - raising the level of transaminases and alkaline phosphatase in blood plasma, jaundice.
Endocrine system: rarely - increased or decreased libido.
Urinary system: rare - incontinence.
Cardiovascular system: when administered parenteral may be some fall in blood pressure.
Respiratory system: when administered parenteral in single cases - respiratory disorders.
Allergic reactions: rarely - a skin rash.
Myasthenia gravis, severe chronic hypercapnia. Specifying a history of alcohol or drug dependence (except for acute withdrawal). Hypersensitivity to diazepam and other benzodiazepines.
Diazepam using during pregnancy and breastfeeding
Diazepam should not be used in the I trimester of pregnancy, except in cases of extreme necessity. Diazepam taking during pregnancy may significantly change fetal heart rate.
When used in obstetrics doses recommended to facilitate childbirth, newborns (most preterm) it is possible temporary muscular hypotonia, hypothermia, respiratory failure.
When taken regularly during lactation breastfeeding should be discontinued.
Should avoid the use of diazepam in newborn infants, since they have not yet fully formed enzyme system involved in the metabolism of diazepam.
Diazepam with caution used in patients with cardiac and respiratory failure, organic changes in the brain (in such cases are advised to avoid parenteral administration of diazepam), with angle-closure glaucoma and predisposition to it, in myasthenia.
There are needed special care when using Diazepam (especially at the beginning of treatment) for patients receiving long-term antihypertensive medications of central action, beta-blockers, anticoagulants, cardiac glycosides.
If you cancel the therapy dose should be reduced gradually. With the sudden cancellation of diazepam after prolonged use may concern, excitement, tremors, convulsions. This medicine should be abolished in the development of paradoxical reactions (acute agitation, anxiety, sleep disturbances and hallucinations).
After I.M. injection of diazepam may increase the activity of CK in the blood plasma (which should be considered in the differential diagnosis of myocardial infarction).
Avoid IA injection.
Avoid alcohol during the period of treatment.
Diazepam can cause slowing of psychomotor responses that should be considered for patients involved in potentially danger activities.
Diazepam drug interactions
When used Diazepam with drugs providing a depressing effect on the CNS (including with antipsychotics, sedatives, hypnotics, opioid analgesics, drugs for anesthesia), enhanced inhibitory effect on the central nervous system, the respiratory center, pronounced arterial hypotension.
When used Diazepam with the tricyclic antidepressants (including amitriptyline) may be increasing of the CNS depressant effect, increasing concentrations of antidepressants and increased cholinergic action.
Patients receiving long-term antihypertensive medications central action, beta-blockers, anticoagulants, cardiac glycosides, the extent and mechanisms of drug interactions are unpredictable.
Simultaneous administration with muscle relaxants the action of muscle relaxants increases, also increases the risk of apnea.
Co-administration with oral contraceptives may increase the effects of diazepam. The risk of breakthrough bleeding increases.
Simultaneous administration with bupivacaine may increase the concentration of bupivacaine in blood plasma; with diclofenac - may increase dizziness; with isoniazid - a decrease of diazepam elimination from the body.
Drugs that cause induction of liver enzymes, including antiepileptic drugs (carbamazepine, phenytoin) may accelerate the elimination of diazepam.
When this medicine used with caffeine decreases sedative and possibly anxiolytic action of diazepam.
Simultaneous administration with with clozapine may be expressed as hypotension, respiratory depression, loss of consciousness; with levodopa - may suppress antiparkinsonian action; with lithium carbonate - described a case of coma, with metoprolol - possible decreased visual acuity, impairment of psychomotor reactions.
Simultaneous administration with paracetamol may decrease excretion of diazepam and its metabolite desmethyldiazepam; with risperidone - described the cases of NMS.
Co-administration with rifampicin increased excretion of diazepam is due to a significant increase in its metabolism under the influence of rifampicin.
Theophylline at low doses changes a sedative effect of diazepam.
In rare cases diazepam inhibits the metabolism and increases the effect of phenytoin. Phenobarbital and phenytoin may accelerate the metabolism of diazepam.
Fluvoxamine increases plasma concentrations and side effects of Diazepam.
Cimetidine, omeprazole, disulfiram may increase the intensity and duration of action of diazepam.
Alcohol and alcohol containing drugs enhanced inhibitory effect on the central nervous system (mainly on the respiratory center) but can also occur syndrome of pathological intoxication.
Diazepam in case of emergency / overdose
Symptoms: CNS depression of varying severity (from lethargy to coma): severe drowsiness, lethargy, weakness, decreased muscle tone, ataxia, prolonged confusion, depression of reflexes, coma; perhaps hypotension, respiratory depression.
Treatment: induction of vomiting and the appointment of activated charcoal (if the patient is conscious), gastric lavage through a tube (if patient is unconscious), symptomatic therapy, monitor vital functions, liquids' intravenous injection (to increase urine output), if necessary - artificial ventilation. With the development of excitation barbiturates should not be used. In hospital conditions used a benzodiazepine receptor antagonist flumazenil as specific antidote. Hemodialysis is ineffective.