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The active ingredient Valproic acid is used to treat epilepsy and seizures as well as for mood stabilization in bipolar disorder. In addition, it is because of its large effective range for the treatment of other diseases such as hereditary diseases examined, HIV and cancer. Here you can read everything you need to action and use of Valproic acid, side effects and interactions.
How Valproic acid acts
In the human brain, the nerve cells (neurons) communicate with one another by distributing chemical messengers (neurotransmitters) that of adjacent nerve cells of certain docking sites (receptors) are perceived. These signal transduction via neurotransmitters can either subsequent nerve cell excite or inhibit – depending on the kind of neurotransmitter and the kind of the receptor. Here, for example, a glutamic acid-causing (“excitatory”) neurotransmitter, GABA (gamma-aminobutyric acid) is an inhibitory (“inhibitory”) neurotransmitter in the brain.
People with seizures and nerve cells throughout the brain, or only in certain areas of the brain are overly excitable. They arise massive excitation signal waves – either spontaneously or as a result of certain triggers. This can cause the classic symptoms of epilepsy: convulsions with tense or fast moving (twitching) muscles and / or loss of consciousness
drugs such as Valproic acid inhibit one hand the excitatory neurotransmitter effects and reinforce simultaneously the effect of inhibitory neurotransmitter GABA. This damping mode of action of Valproic acid also explains why it may alleviate manic phases in patients with bipolar disorder.
Up, degradation and excretion of Valproic acid
After taking Valproic acid is absorbed in the intestine and passes via the bloodstream to the brain, where it crosses the blood-brain barrier without any problems. The concentration of Valproic acid in the brain reaches about ten percent of the concentration in the blood.
The drug is metabolized in the liver to many metabolic products, of which some are also potentially effective against seizures. These are mainly excreted in the urine. Approximately twelve to 16 hours after ingestion, the concentration of the drug has been halved again in the blood.
When will Valproic acid used?
The active substance Valproic acid is used to treat many forms of epilepsy. These include, for example:
- generalized seizures in the form of absence seizures (petit mal seizure with short awareness Pause)
- generalized seizures in the form of myoclonic seizures (with twitching of muscle groups)
- generalized seizures in the form of tonic-clonic seizures (grand mal seizure with loss of consciousness, fall, cramping and twitching of muscle groups)
- partial seizures (focal seizures) simple style with retaining consciousness
- focal seizures complex type with disturbed consciousness
- partial seizures with secondary generalization (becoming a generalized seizure)
Similarly, Valproic acid can be used together with other active ingredients in other forms of epilepsy.
Valproic acid is also approved for bipolar disorder when the drug lithium is not tolerated or for other reasons can not be used to treat the manic episodes. Also for the prevention of manic episodes of drug can be taken.
Valproic acid is usually employed in the longer term, but can also be used only for short-term treatment of manic episodes.
How Valproic acid is used
Valproic acid and its more water-soluble sodium or calcium salt (often just called “valproate”) are used as tablets, extended release (prolonged-release tablets), gastro-resistant tablets as well as offered as an oral solution and for injection.
The long-term treatment with Valproic acid is usually with oral dosage forms, the solution is reserved for oral children under six years and patients with dysphagia. Treatment is started with a low dose that is then within several weeks increases slowly. Usual doses in adults be 1000-1800 mg Valproic acid (corresponding to about 1200 to 2100 milligrams of sodium valproate). The total daily dose should be divided depending on the individual tolerability in consultation with the doctor two to four divided doses. The drug should be taken about an hour before meals fasting with a glass of water.
What are the side effects of Valproic acid?
The most common side effect is the increase in the concentration of ammonia in the blood. Taken alone, this increase is not critical, however, high ammonia levels trigger symptoms such as vomiting, ataxia, impaired consciousness, low blood pressure and increased seizure tendency. When such complaints occur, the treatment should be discontinued with Valproic acid or the dose reduced (in consultation with the doctor). In one to ten percent of patients also show Valproic acid side effects such as a decrease in platelets (through a reduced formation in the bone marrow), an irregular menstrual cycle, hand tremors, paresthesia, or loss.
What should be considered when taking Valproic acid?
medicine called Valproic acid can contribute to the treatment of children from three years (in exceptional cases also below), be used in adolescents, adults and elderly patients.
The combination with other medicines, the Valproic acid concentration decrease or increase in the body. Thus, agents such as mefloquine (for malaria) and carbapenems (antibiotics) reduce Valproic acid levels in the body. Other agents increase it, with features such as anti-epileptic agents (phenobarbital, Phenytoin, primidone, Carbamazepine, felbamate), gastric acid inhibitors (cimetidine), certain antibiotics (Erythromycin, rifampin) and the antidepressant Fluoxetine.
Conversely, the Valproic acid alter the way other drugs. For example, you increase the effect of other antiepileptics partly why the combined treatment should be done by an experienced doctor. Likewise Valproic acid can increase the effect of anticoagulants and thus the bleeding tendency.
Valproic acid can potentially damage the liver. Before and during treatment should therefore Liver function should be monitored in order to respond quickly when necessary. In hepatic impairment, the doctor will decide carefully on an application.
Because Valproic acid is teratogenic, pregnant and nursing mothers should not be treated with Valproic acid. In addition, should during treatment with Valproic acid always adequate prevention measures are taken.
How to obtain drugs with Valproic acid
Valproic acid is available on prescription in each strength and dosage form, ie only available by a prescription at the pharmacy.
Since when Valproic acid is known?
The Valproic acid was first synthesized by chemist Beverly Burton in 1881st As the acid is very well suited for dissolving water-insoluble substances, it was often used in chemistry. Only in 1962, the French scientist Pierre Eymard noticed in the study of plant constituents that the anticonvulsant effect of the studied plant extracts does not go back to the ingredients but the solvent Valproic acid. As early as 1967 Valproic acid has been approved in France as a remedy for epilepsy. Because the drug is no longer protected by patents, are now offering many pharmaceutical manufacturers preparations containing the active substance Valproic acid .