Product Name: Ativan
Generic Name: Lorazepam
Common Brands: Temesta, Tavor
Pharmaceutical Categories: Antidepressants, Anti Anxiety
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Here is an additional general information about this medication active ingredient lorazepam:
Ativan is an anxiolytic drug (tranquilizer), a derivative of benzodiazepine. This medication has anxiolytic, sedative, hypnotic, anticonvulsant, muscle relaxant central, antiemetic effect. The mechanism of the anxiolytic, sedative and hypnotic action is associated with increased inhibitory effect of GABA in the CNS. Anticonvulsant action, apparently in part due to increased presynaptic inhibition; inhibited the spread of epileptogenic activity arising in the epileptogenic foci in the cortex, thalamus and limbic structures, but not removed the excited state of the hearth. Muscle relaxant effect is primarily associated with the suppression of spinal polysynaptic afferent pathways and, presumably, an inhibition of monosynaptic afferent pathways; possibly also a direct inhibitory effect on motor nerves and muscle function.
After oral administration the bioavailability of Ativan is 95-99%. The plasma proteins binding is about 80%. Vd is 1.3 L / kg. Lorazepam is metabolized in the liver by conjugation to form inactive metabolites. T1/2 is 8-15 h. This medicine is derived primarily by the kidneys.
Why is Ativan prescribed?
Anxiety (including related to depression), sleep disturbances due to anxiety or transient stressful situation, neuroses and neurosis-like states, panic disorder, endogenous psychoses: mania, catatonic state, anxiety and excitement in schizophrenia; acute alcoholic delirium; premedication in anesthesia, epilepsy (in combination therapy), status epilepticus; symptomatic convulsive status; psychosomatic disorders and headaches.
Dosage and administration
For oral administration for adults and adolescents the dose is 0.5-4 mg 1-3 times / day. In IV or IM introduction a single dose is 50 mg / kg, the dose frequency is set depending on the evidence and the clinical situation.
The maximum daily dose when Ativan administered orally is 10 mg, for IV and IM injections a single dose is 4 mg.
Ativan side effects, adverse reactions
CNS: rarely - dizziness, ataxia, fatigue, muscle weakness; in some cases - the episodes of amnesia.
Digestive system: rarely - dry mouth, dysphagia, nausea, diarrhea, constipation, appetite disorders; in some cases - liver function abnormalities.
Allergic reactions: rarely - skin rash, itching.
Laboratory parameters: changes in peripheral blood.
Local reactions: for IV injections can be phlebitis or venous thrombosis.
Myasthenia gravis, angle-closure glaucoma, acute intoxication with psychotropic drugs, acute alcohol intoxication, increased sensitivity to lorazepam.
Using during pregnancy and breastfeeding
During pregnancy, especially in the I trimester, apply Ativan only under strict indications. Lorazepam and / or its metabolites are excreted in breast milk. provision. It should be borne in mind that newborns benzodiazepines metabolized more slowly than adults, therefore it is possible accumulation of the active substance and / or its metabolites in the body of the child.
With extreme caution Ativan is used in closed-angle glaucoma is suspected, severe chronic obstructive pulmonary disease, in a coma, shock, epilepsy, renal dysfunction, hyperkinesis, hypoproteinemia, severe depression, organic brain disease, porphyria, psychosis with suspected sleep apnea.
The development of adverse reactions are more likely at the beginning of treatment and in cases of exceeding the recommended doses.
With prolonged use of lorazepam may develop addiction and drug dependence.
In the case of using this medication for sedation it may be required reducing the dose of fentanyl derivative used for induction of anesthesia, and it is possible a reduction of time before the mind with induction doses.
Patients receiving Ativan should refrain from activities in potentially hazardous activities that require attention and psychomotor speed of reaction.
Ativan drug interactions
When this drug applied simultaneously with:
- drugs which have a depressing effect on the CNS, with alcohol, alcohol containing drugs increased inhibitory effect on the CNS.
- Ativan and alcohol may develop agitation, aggression, pathological intoxication (the development of this condition does not depend on the amount received ethanol).
- diminishes the effectiveness of oral contraceptives.
- enhanced effect of depolarizing relaxants.
- nicotine increases the metabolism of lorazepam, and decreases its activity.
- probenecid may interfere with the binding of lorazepam with glucuronic acid, resulting in higher concentrations in blood plasma, and by enhancing the therapeutic effect may develop excessive sedation.
Ativan in case of emergency / overdose
Symptoms: drowsiness, hypotension, confusion, depression of reflexes, coma.
Treatment: induction of vomiting, gastric lavage, IV introduction of norepinephrine to increase blood pressure, symptomatic therapy, monitoring of vital functions. The introduction of a specific antidote - an antagonist of benzodiazepine receptors flumazenil (in hospital).