From time to time, muscle cramps bother many people. However, few people wonder why such conditions generally arise.
According to experts, convulsions can be different: generalized (tonic, clonic, tonic-clonic and myoclonic), as well as partial (simple and complex). To treat the last seizures, a drug such as Gabapentin is used. Instructions for use, reviews and contraindications for this medication will be presented below.
It should immediately be noted that partial convulsive seizures are characterized by the absence of loss of consciousness. Such states are single. They are manifested by seizures of a clonic nature, involving the muscles of the hands, feet and face.
Release form, description, packaging of the drug and its composition
In what form is the drug "Gabapentin" sold? Patient reviews report that this medicine can be purchased at the pharmacy in the form of hard white gelatin capsules. Their contents are white or yellowish medicinal powder.
The active ingredient of this tool is gabapentin. Also, its composition includes additional substances in the form of sodium carboxymethyl starch, calcium stearate and microcrystalline cellulose. As for the capsules, they contain gelatin and titanium dioxide.
In what packaging is the drug Gabapentin sold? Customer reviews say that on the shelves of pharmacies this medication can be found in cardboard packs, which contain either polymer cans with capsules or contour cells.
The principle of action of the drug
How does the drug "Gabapentin"? The instruction (reviews about the drug is presented at the end of the article) reports that this drug is very similar in structure to the neurotransmitter gamma-aminobutyric acid (abbreviated GABA). However, it should be noted that its principle of action is fundamentally different from other medicines that interact with GABA receptors (for example, valproic acid, barbiturates, benzodiazepine, GABA transaminase inhibitors, GABA uptake inhibitors, GABA agonists and prodrug forms of GABA).
The drug in question does not have GABA-like properties and does not affect the capture and metabolism of GABA in any way. Studies by specialists have shown that the active substance of this agent, binding to the α2-δ subunit of voltage-dependent calcium channels, significantly reduces the flow of calcium ions, which play a crucial role in the occurrence of neuropathic pain.
Features of the anticonvulsant drug
What other properties does the drug “Gabapentin” have? Reviews of doctors say that it is very effective in neuropathic pain. Taking this medication reduces the glutamate-dependent death of neurons, increases the synthesis of GABA, as well as the process of suppression and release of neurotransmitters of the monoamine group.
It cannot be said that in clinically significant concentrations the drug “Gabapentin” does not bind to other drug receptors (or neurotransmitters), including GABAA and GABAA receptors, as well as glutamate, benzodiazepine receptors, glycine and N-methyl-D- aspartate.
Unlike Carbamazepine and Phenytoin, the medication in question does not interact with sodium channels. The drug "Gabapentin" partially attenuates the effects of such a glutamate receptor agonist as N-methyl-D-aspartate. Moreover, it slightly reduces the release of monoamine neurotransmitters.
Kinetic properties of the drug
What kinetic parameters are inherent in Gabapentin capsules? Patient reviews will not be able to answer this question. To find it, you will have to consult experienced specialists or the attached instructions.
According to the latter, the bioavailability of said drug is not proportional to the dosage taken. With an increase in the amount of the drug, it decreases.
After taking the medication inside, its highest concentration in plasma is noted after 3 hours. The absolute bioavailability of the drug in capsules is approximately 60%. Food, including very fatty foods, has no effect on the kinetics of the drug.
The elimination of "Gabapentin" from the patient’s blood is carried out according to a linear model. The half-life of the drug does not depend on the dose taken and is about 5-7 hours.
The kinetic properties of the drug do not change even with its repeated use. The concentration of the drug in the blood can be predicted based on the results of a single dose.
The drug "Gabapentin" practically does not bind to plasma proteins (less than 3%). It is excreted unchanged by the kidneys.
The drug is not exposed to metabolism. Moreover, it does not induce oxidative liver enzymes that are involved in the metabolism of other drugs.
The clearance of this drug from the blood decreases in elderly patients and people with impaired renal function.
The drug "Gabapentin" is removed from the body through hemodialysis.
Indications for taking the medicine
What diseases are the drugs considered by us especially effective? What do the reviews say about this?
"Gabapentin" works well with:
- neuropathic pain in adult patients (18 years of age and older);
- monotherapy or as an additional drug for the treatment of partial seizures, accompanied by secondary generalization in adults and adolescents from 12 years.
Contraindications to taking the medication
What contraindications does the drug “Gabapentin” have? Reviews on the application report that it negatively affects the body if the medication was taken with:
- hypersensitivity to any of the substances;
- partial seizures under the age of 12 years.
With extreme caution, this remedy is prescribed for renal failure.
How should I take gabapentin?
Reviews (with neuralgia this tool helps very well) say that this drug should be prescribed only by an experienced doctor, after making the correct diagnosis.
Gelatin capsules are taken orally, swallowing them in their entirety. Use the drug regardless of food, drinking plenty of liquid. If you want to reduce the dosage, cancel the medication or replace it with an analog, then this should be done gradually, over one week.
Treatment of neuropathic pain in adults
How does the medication in question work in this condition? What do the medical reviews say about this? "Gabapentin" is very effective in neuropathic pain. In the treatment of this condition, the initial daily dose of the drug should be 900 mg. The specified number is divided into three doses. If required, the dose is gradually increased to the maximum (that is, up to 3600 mg per day).
Partial cramps
How should the gabapentin medication be taken with this disease? Reviews report that this tool can be prescribed not only for adults, but also for adolescents from 12 years old.
The effective dose for partial seizures is considered to be 900-2400 mg per day. Therapy of this disease can be started with 300 mg of the drug three times a day. In the future, the daily dose must be increased to 900 mg, and then to 2400 mg per day (divided into three equal doses).
The time interval between doses of the drug when it is taken three times should not be higher than 12 hours (in order to avoid the resumption of seizures).
Side effects
What adverse reactions may occur while taking an anticonvulsant? What do consumer reviews say about this? "Gabapentin" in the treatment of neuropathic pain can cause:
- asthenia, accidental injuries, pain of various localization, back pain, infection, flu-like syndrome, headache, weight gain, peripheral edema;
- impaired gait, ataxia, amnesia, hypesthesia, confusion, dizziness, impaired thinking, drowsiness, tremor;
- constipation, flatulence, diarrhea, vomiting, dry mouth, dyspepsia, nausea, abdominal pain;
- skin rash;
- shortness of breath, pharyngitis;
- amblyopia.
In the treatment of partial seizures, this medication contributes to the appearance of:
- back pain, fatigue, fever, headache, viral infection, peripheral edema, weight gain, asthenia, malaise, facial swelling;
- constipation, dental diseases, diarrhea, dyspepsia, increased appetite, dry mouth or throat, nausea or vomiting, abdominal pain, flatulence, anorexia, gingivitis;
- symptoms of vasodilation or hypertension;
- leukopenia, purpura;
- fractures, myalgia and arthralgia;
- amnesia, ataxia, confusion, impaired coordination, depression, dysarthria, emotional lability, insomnia, nervousness, nystagmus, drowsiness, impaired thinking, tremors, muscle twitches, dizziness, hyperkinesia; amplification, weakening or absence of reflexes, anxiety, paresthesia, hostility;
- abrasions, acne, itching of the skin, skin rash;
- cough, pharyngitis, rhinitis, pneumonia;
- amblyopia, diplopia, visual impairment;
- urinary tract infections, impotence.
Overdose cases
What symptoms of an overdose can the medication mentioned cause? What do the reviews say about this? “Gabapentin” in case of an overdose causes double vision, dizziness, drowsiness, speech impairment, lethargy and diarrhea.
To eliminate such conditions, symptomatic therapy is carried out, as well as the stomach of the victim is washed and activated carbon is given to him.
Patients with severe renal failure are shown hemodialysis.
The drug "Gabapentin" and alcohol
Reviews of experts report that the effectiveness of the drug in question is very high. But this is only if, during the period of its use, the patient completely refused to drink alcohol.
If this drug is combined with alcohol, then the patient may noticeably increase adverse reactions from the central nervous system (stupidity, ataxia, and others).
Drug interaction
The drug "Gabapentin" in neurology, reviews of which are more positive in nature, can not be combined with all medicines.
According to the instructions, antacids reduce the bioavailability of this drug.
Myelotoxic drugs increase the hematotoxicity of Gabapentin capsules.
When combined with morphine, its pharmacokinetics does not change. However, with this combination, probable adverse reactions from the nervous system should be monitored.
The medication in question can be taken simultaneously with antiepileptic drugs (for example, “Phenobarbital”, “Carbamazepine”, “Phenytoin” and valproic acid) and oral contraceptives. At the same time, its kinetics does not change.
Special recommendations
Despite the fact that withdrawal syndrome with the occurrence of seizures during therapy with "Gabapentin" was not noted, a sharp cessation of treatment with antiepileptic drugs in people with partial seizures can still provoke the occurrence of severe seizures.
The medication in question is not an effective tool aimed at combating abscess-epilepsy.
People who need complex therapy with morphine may need an increased dose of Gabapentin. In this case, it is necessary to ensure constant monitoring of the patient's condition for the development of drowsiness. When it is detected, the dose of drugs should be adequately reduced.
When Gabapentin was combined with other anticonvulsants , false-positive results were recorded during urine protein determination using Ames N-Multistix SG test strips. In this regard, for such studies, it is recommended to use a more specific precipitation method using sulfosalicylic acid.
Reviews of specialists and consumers
Most reviews by doctors and patients about the drug "Gabapentin" are positive. Their messages say that this medication effectively copes with the task. However, when combined with alcohol, serious adverse reactions from the nervous system often develop.
It should be noted that the abrupt cancellation of this drug can cause patients dull consciousness, lethargy and bad mood.
Many people say that while taking this drug they have depression and suicidal thoughts. Also, the medication very often causes the development of acute pancreatitis.
Experts recommend conducting treatment with the drug "Gabapentin" only under the supervision of a doctor who, if necessary, can quickly adjust the treatment regimen.