Views: 0 Author: Site Editor Publish Time: 2022-04-27 Origin: Site
Pregabalin is an antiepileptic drug, which is mainly used clinically for the single or combined treatment of tonic-clonic seizures (grand mal), simple partial seizures and complex partial seizures. It is also used in the treatment of essential tremor and senile tremor.
l What is the pharmacology and toxicology of Pregabalin?
l What are the interactions between Pregabalin and other drugs?
l What is the pharmacokinetic information for Pregabalin?
This product is an anti-epileptic drug. The main metabolite in the body is phenobarbital. In vitro electrophysiological experiments have shown that it can open the chloride ion channel of nerve cells and hyperpolarize the cells, mimicking the effect of γ-aminobutyric acid (GABA).
At the therapeutic concentration, it can reduce the excitatory effect of glutamate, strengthen the inhibitory effect of γ-aminobutyric acid, inhibit the single-synaptic and polysynaptic transmission of the central nervous system, reduce the excitability of the entire nerve cell, and improve the electrical stimulation threshold of the motor cortex. Raising the seizure threshold can also inhibit the spread of focal discharge.
1. Alcohol consumption, general anesthesia, drugs with central nervous system inhibitory effect, and magnesium sulfate for injection can increase central nervous system activity or respiratory inhibition when combined with this product, and the dosage needs to be adjusted.
2. When Pregabalin is combined with anticoagulants, corticosteroids, digitalis, digoxin, doxycycline hydrochloride or tricyclic antidepressants, the metabolism of these drugs is accelerated due to the induction of phenobarbital on liver enzymes. and reduced efficacy.
3. When Pregabalin is used in combination with monoamine oxidase inhibitors, the metabolism of this product may be inhibited and poisoning may occur.
4. This product can reduce the intestinal absorption of vitamin B12 and increase the excretion of vitamin C by the kidney. Due to the positive induction of liver enzymes, the metabolism of vitamin D can be accelerated.
5. Combination with vasopressin may increase the risk of arrhythmia or coronary insufficiency.
6. When Pregabalin is used in combination with carbamazepine, the curative effect is reduced due to the positive induction of liver enzymes between the two. The blood concentration should be measured.
7. When Pregabalin is used in combination with other antiepileptic drugs, due to changes in metabolism, the form of epileptic seizures will change, and the dosage should be adjusted in time.
8. When Pregabalin is used in combination with sodium valproate, the blood concentration of this product will increase, and the half-life of valproic acid will be shortened. The dosage should be adjusted to avoid poisoning.
9. It should not be used in combination with phenobarbital.
10. The metabolism of this product is accelerated when used in combination with phenytoin sodium. Contraceptive failure can occur when combined with contraceptives.
Pregabalin is rapidly absorbed from the gastrointestinal tract by oral administration, but is slower than that of phenobarbital. The bioavailability in children is about 92%. After oral administration, the blood drug concentration reaches its peak value (0.5 to 9 hours) within 3 to 4 hours. The plasma protein binding rate is low, about 20%. It is widely distributed and has a wide range of parts in the body. /2 about 10 to 15 hours. Metabolized by the liver into active products phenethyl diamide (PEMA) and phenobarbital, the former T1/2 is 24 to 48 hours, the latter adult T1/2 is 50 to 144 hours, and children are 40 to 70 hours. 15-25% of the absorbed primidone in adults is converted into phenobarbital, and the plasma concentration reaches a steady state within a week of taking the drug, and the effective plasma concentration is 10-20 μg/ml. After administration, approximately 20-40% is excreted by the kidneys in the form of primidone, 30% as PEMA, and 25% as phenobarbital. It can pass through the placenta and be secreted into breast milk.
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