Tegretol

Tegretol is an anti-epileptic drug.

Indications Tegretola

Tegretol is used in the treatment of many pathologies:
1. Epilepsy;
2. Alcohol withdrawal;
3. Inflammation of the trigeminal (primary or in multiple sclerosis) and glossopharyngeal nerve (primary);
4. Manic states (prevention of complications and reduction of clinical manifestations);
5. Degenerative-dystrophic lesion of nerve fibers of diabetic etiology with pain symptom;
6. Diabetes insipidus;
7. Possible use:

• mental disorders;
• aggressive behavior in patients with depression;
• anxiety;
• pain of neurogenic origin;
• migraine prevention.

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Release form

The medicine is available in three forms - syrup, tablets and capsules. The syrup is packaged in 100 ml bottles, each pack contains one piece and a measuring spoon. The capsules and tablets are packaged in blisters of ten units, each pack may contain three to five tablets.

Pharmacodynamics

The active substance of Tegretol is Carbamazepine, but there is insufficient information about its mechanism. The main effect is blocking sodium channels, as a result of which sodium-dependent potentials are prevented in weakened neurons. In addition, Tegretol regulates the membranes of excited nerve fibers, suppresses the formation of secondary neuronal discharges and thereby reduces the synaptic conduction of excitatory impulses.
Regulation of neuronal membranes, a decrease in glutamate causes the anticonvulsant effect of the drug. But the suppression of dopamine and norepinephrine causes the antimanic effect.
In the treatment of most neurological pathologies, Tegretol exhibits neutropic activity. It also relieves pain attacks in inflammation of the trigeminal nerve of primary or secondary etiology. The drug increases the threshold of spastic readiness, reduced in alcohol withdrawal, and due to this, tremor decreases, nervousness decreases, and gait improves.
In central diabetes mellitus, the drug reduces the feeling of thirst in patients and decreases the volume of urination.

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Pharmacokinetics

Tegretol is absorbed completely, but at different rates in patients. Maximum bioavailability can reach one hundred percent. The concentration reaches its maximum value after twelve hours. And stable positions - after one to two weeks. But it is worth noting that these indicators depend on many factors (for example, the patient's status before treatment, duration and scheme of therapy).
Carbamazepine reacts with serum proteins by seventy to eighty percent. The remaining twenty to thirty percent relate to the concentration of the unchanged substance in the cerebrospinal fluid and saliva. In breast milk, the concentration of the drug is about 25 - 60% and corresponds to the level in the serum. In addition, Tegretol passes through the placental barrier.
Metabolism occurs in the liver. The half-life is about 36 hours, but with prolonged use it will decrease to 16-24 hours. At a dosage of 400 mg, 72% will be excreted in the urine, 28 - in the feces.
Because of the high rate of drug elimination, children may require higher doses than adults (based on the child's weight per kg).
There is no information on whether dosage adjustments are needed for geriatric patients or those with pathological changes in liver or kidney function.

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Dosing and administration

The medicine should be taken orally only with a small amount of water. For uniform distribution of the active substance in the syrup, it should be shaken before use (after tightly closing the bottle). The medicine can be used as a mototherapy.
The syrup is used for patients who have difficulty swallowing, or those who need an accurate dosage in the treatment regimen. Treatment should be started with small dosages, since the density of Carbamazepine in the syrup increases more strongly (in relation to tablets). For this, the daily dose can be divided into three uses. If this is not done, undesirable effects may occur.
It will be necessary to increase the dosage if there is a need to switch from Tegretol to Tegretol CR, and it is also advisable to switch to mototherapy. This is explained by the fact that in this form, with minor or myoclonic seizures, the medicine does not have the desired effect.
Treatment, under the control of the concentration level of the medicine, should be started with minimal doses, gradually increasing them. If combined therapy is used, it is also necessary to start with minimal doses.

Thus, the initial daily dose should be no more than 0.2 g of the drug, divided into two doses. Then it can be gradually increased, with an average of 0.8-1.2 grams consumed in two or three doses. If necessary, the dose can be increased to two grams.
In pediatrics (children under four years old), treatment starts with a maximum of 0.06 mg per day, with a gradual increase of 0.02-0.06 mg no more than once every two days. At an older age, treatment starts with 0.1 grams per day, with an increase of 0.1 grams per week.
For children under three years old, only syrup can be used.

The maximum daily dose for inflammation of the trigeminal nerve at the beginning of treatment is 0.4 grams. Then it increases until the pain disappears (on average to 0.8 grams). Then it decreases to the one that can relieve the pain. For elderly patients, the initial daily dose is no more than 0.2 grams.
For the treatment of withdrawal, an average dose of 0.6 grams is used (divided into three doses). In severe cases, the dose can be increased to 0.4 grams per day. Most often, in this case, Tegretol is used together with sedatives and sleeping pills. Then, when the acute period of the pathological process passes, the medication can be used as mototherapy.
In cerebral diabetes insipidus (if it is associated with an increase in the amount of urine and constant thirst), the dose starts with 0.4-0.6 grams per day. In this case, the dose for children is selected individually.
The dose, divided into two to four uses per day and amounting to 0.4-0.8 grams, is used to relieve pain due to diabetic neuropathy.
For the treatment of manic states, a daily dose of up to 1.6 grams is used, quickly increasing it. To maintain the patient's condition, the dose is increased gradually, for normal tolerance of therapy.

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Use Tegretola during pregnancy

Before using Tegretol, it is necessary to carefully evaluate the possible benefit for the mother with the risk to the development of the child. This is especially important in the first trimester of gestation. When taking Tegretol, it is necessary to take additional folic acid before and during the gestation period. Since antiepileptic drugs cause a significant decrease in the level of this vitamin, as a result, the fetus may develop intrauterine pathology. There is also information that due to the use of antiepileptic drugs, bleeding may develop in newborns. Therefore, in the last weeks of pregnancy, the expectant mother must be prescribed vitamin K1 for prevention.
In addition, children may experience seizures or respiratory depression if Tegretol is taken in combination with other antiepileptic drugs during the gestation period. The newborn may also experience vomiting, diarrhea, or decreased appetite if the mother took Carbamazepine during pregnancy. Most likely, this will be an expression of withdrawal syndrome.
Since the medication gets into breast milk, breastfeeding should be stopped while using it.

Contraindications

The medication should not be used for treatment in the presence of the following pathological processes:
1. Fructose intolerance;
2. Atrioventricular block.
It can be used with caution in the case of:
1. Heart pathology;
2. Hypothyroidism;
3. Increased intraocular pressure;
4. Gestational period;
5. Breastfeeding period;
6. Old age

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Side effects Tegretola

When prescribing Tegretol, the patient should be warned about the possible occurrence of the following adverse reactions:

• a visual disorder characterized by double vision;
• taste disturbance;
• paralysis, paresthesia;
• allergy, anaphylaxis;
• arrhythmia, low or high blood pressure;
• depression, aggression;
• disorientation in space;
• asthenia;
• erythroderma;
• pain in the epigastric region;
• bowel movements;
• hallucinations (auditory or visual);
• peripheral neuropathy;
• thrombophlebitis, thromboembolism;
• hyperhidrosis;
• increased drowsiness, asthenia;
• agranulocytosis;
• ataxia, muscle spasm;
• swelling;
• stomatitis, dry oral mucosa, glossitis;
• tremor;
• decreased spermatogenesis, impotence;
• renal dysfunction, anuria, hematuria;
• liver failure;
• inflammation of the pancreas;
• vasculitis;
• arthralgia;
• glaucoma, nystagmus;
• lymphadenopathy, leukemia, anemia;
• dermatitis of various origins;
• pneumonia;
• photosensitivity.

As the dosage increases, the side effects will increase.

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Overdose

When using doses exceeding those recommended for administration, the patient will most likely experience the following pathological conditions:
Convulsions, CNS depression, disorientation, agitation, hyperreflexia, speech impairment, coma;

• Hyperglycemia;
• Hypothermia;
• Tachycardia, hypertension or hypotension, cardiac arrest;
• Pulmonary edema, respiratory depression,
• Vomiting, dyskinesia, food retention in the stomach, decreased gastrointestinal motility, acidosis;
• Nystagmus, blurred vision, mydriasis;
• Anuria, oliguria;
• Increased creatine phosphokinase levels;
• Dysarthria, ataxia

Therapy is symptomatic. To assess the degree of overdose, medical personnel must measure the concentration of the drug in the plasma. The patient must be under medical supervision in a hospital, where he will definitely have his stomach washed and be given sorbents. In case of low blood pressure, Dopamine will be administered intravenously, and in case of hyponatremia, fluid will be administered to reduce the risk of brain tissue edema. Hemodialysis is not used due to its low efficiency. But it is worth keeping in mind that the symptoms may reappear. This is explained by the slow absorption of Tegretol.

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Interactions with other drugs

When Tegretol is used in combination with certain medications, various types of interactions are possible:

• Clobase, Haloperidol, Warfarin, corticosteroids and other drugs that are metabolized in the liver – Tegretol increases their metabolism and reduces their effect.
• Phenytoin – Tegretol reduces or, conversely, increases the concentration of Phenytoin.
• Phenobarbital - the concentration of Tegretol in the blood serum will decrease;
• Macrolides, calcium antagonists – increase the concentration of Tegretol.
• Metoclopramide - increases side effects.
• Hydrochlorothiazide, furosemide - an adverse reaction in the form of hyponatremia may occur.
• Oral contraceptives - when taken simultaneously, their effectiveness may decrease, and bleeding in the middle of the menstrual cycle may occur.
• Alcoholic drinks - side effects will increase.

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Storage conditions

Both the syrup and the tablets should be kept in a place that is inaccessible to children, observing the temperature regime (not higher than 30°C).

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Special instructions

Reviews
Tegretol has been on the pharmaceutical market for quite a long time, it has established itself as an effective remedy. It is especially often prescribed for epilepsy. If the patient has been prescribed this medication to treat withdrawal symptoms, it is advisable to use it in a hospital under the supervision of medical personnel.

Shelf life

The medication must not be used for treatment after five years from the date of manufacture.