Tegretol
Tegretol
Tegretol (Carbamazepine)Pharmacological action
Antiepileptic preparation. Along with antiepileptic, the preparation possesses also neurotropic and psychotropic action.
As an antiepileptic agent, Tegretol it is effective at focal (partial) convulsive attacks (simple and complex), accompanied or not accompanied by secondary generalisation, at generalised toniko-clonic convulsive attacks, and also at a combination of the specified types of attacks.
In clinical researches at use of Tegretol as monotherapy at patients with an epilepsy (in particular at children and teenagers), psychotropic action of a preparation which, in particular, was shown in positive influence on uneasiness and depression symptoms, and also in irritability and aggression depression has been noted. In other researches positive influence of a preparation on the indicators characterising attention, ability to training and storing has been noted.
As a neurotropic agent, Tegretol it is effective at a number of neurologic diseases so, for example, it prevents painful attacks at an idiopathic and secondary epileptiform neuralgia. Besides, Tegretol is applied to simplification of a neurogenic pain at various conditions, including a tabes, posttraumatic paresthesias. At a syndrome of an alcoholic abstinence Tegretol raises a threshold of convulsive readiness (which at the given condition it is lowered) and reduces expression of clinical implications of a syndrome, such as excitability, a tremor, gait disturbances.
As a psychotropic drug, Tegretol it is effective at affective disturbances, namely, for treatment of acute maniacal conditions, for supporting treatment of bipolar affective (maniacally-depressive) disorders (both as monotherapy, and in a combination to neuroleptics, antidepressants or lithium preparations), at schizoaffective psychoses, maniacal psychoses where it is applied in a combination with neuroleptics, and also at acute polymorphic schizophrenia (rapid cycling episodes).
The mechanism of action of carbamazepine - active substance of Tegretol - is found out only partially. Carbamazepine stabilises membranes of excessively raised nervous fibers. Anticonvulsant action of a preparation basically is caused by depression of liberation of a glutamate and stabilisation of membranes of neurones whereas the antimaniacal effect can be caused oppression of a metabolism of Dopaminum and Noradrenalinum.
Indications
- An epilepsy: difficult or simple partial convulsive attacks (with loss or without a loss of consciousness) with secondary generalisation or without it; generalised toniko-clonic convulsive attacks; the admixed forms of convulsive attacks.
(Tegretol can be applied as monotherapy, and as a part of the combined therapy.
Tegretol is usually noneffective at small attacks (petit mal, an absentia epileptica) and myoclonic attacks.);
- Acute maniacal conditions and a maintenance therapy of bipolar affective disorders for the purpose of preventive maintenance of exacerbations or weakening of clinical implications of an exacerbation;
- A syndrome of an alcoholic abstinence;
- An idiopathic epileptiform neuralgia and an epileptiform neuralgia at a multiple sclerosis (typical and atypical); an idiopathic neuralgia of a glossopharyngeal nerve;
- A diabetic neuropathy with a painful syndrome;
Dosage regimen
The preparation can be accepted during time, after meal or in intervals between food intakes together with a liquid small amount.
Tablets (the whole tablet or half if so it is prescribed by the doctor) should be swallowed entirely, not chewing, washing down with a liquid small amount. As the active substance is liberated from tablets slowly and gradually, they are prescribed by 2 times/days
At an epilepsy when it is possible, Tegretol should be prescribed in the form of monotherapy.
Treatment begin with application of a small daily dose which in the subsequent slowly raise before achievement of optimum effect.
For selection of an optimum dose of a preparation there can be useful a definition of level of active substance in a blood plasma.
For adults the initial dose of Tegretol makes on 100-200 mg 1 or 2 times/days Then a dose slowly raise, before achievement of optimum medical effect; usually it is reached at the dose of 400 mg/sut prescribed in 2-3 receptions. By some patient Tegretol dose, a component 1.6 g or even 2 g a day can be demanded.
At children aged is more senior 4 years treatment can it is begun with preparation application in a dose of 100 mg/24h; a dose raise gradually - every week on 100 mg.
Maintenance doses: 10-20 mg/kg/24h (in stages).
Age of the child the Daily dose
4-5 years of 200-400 mg (in 1-2 receptions)
6-10 years of 400-600 mg (in 2-3 receptions)
11-15 years of 600-1000 mg (in 2-3 receptions)
At an epileptiform neuralgia the initial dose of Tegretol makes 200-400 mg/days It slowly raise before disappearance of painful sensations (usually to a dose on 200 mg 3-4 times/sut), and then gradually lower to the minimum supporting. The recommended initial dose for patients of advanced age makes on 100 mg 2 times/days
At a syndrome of an alcoholic abstinence the average dose makes on 200 mg 3 times/days In serious cases within first several days a dose can be raised (for example, to a dose on 400 mg 3 times/sut). At serious implications of an alcoholic abstinence treatment begin a combination of Tegretol with sedatively-soporific preparations (for example, Chlordiasepoxidum). After the permission of an acute phase treatment by Tegretol can be continued in the form of monotherapy.
At a diabetic neuropathy with a painful syndrome the average dose of Tegretol makes on 200 mg 2-4 times/days
At acute maniacal conditions and supporting treatment of affective (bipolar) disorders daily doses make 400-1600 mg. An average daily dose - 400-600 mg (in 2-3 receptions). At an acute maniacal condition Tegretol dose should be raised quickly enough. In a case of a maintenance therapy of bipolar disorders, with a view of maintenance of optimum shipping, the gradual augmentation of a dose at small size is recommended.
Clinical experience shows, that some patients at use of tablets can have a necessity for rising of a dose of a preparation.
Considering medicinal interactions and various pharmacokinetics of antiepileptic preparations, elderly patients of a dose of Tegretol should select with care.
Side effect
Certain types of by-effects, for example from party TSNS (giddiness, a headache, drowsiness, the general delicacy, a diplopia), GASTROINTESTINAL TRACT (a nausea, vomiting) or allergic dermal reactions, meet more or less often, especially in the beginning of treatment by Tegretol, at use of too big initial dose of a preparation or at treatment of patients of advanced age.
From party TSNS and peripheric nervous system: very often - giddiness, drowsiness, the general delicacy; often - a headache, a diplopia, disturbances of accommodation of sight (for example, sight misting); sometimes - abnormal consensual movements (for example, a tremor, a "flitting" tremor/asterixis/, a dystonia, habit spasms); a nystagmus; oculomotor disturbances, speech disturbances (for example, a dysarthtia or muffled speech), choreoathetoid disorders, a peripheric neuritis, paresthesias, muscular delicacy and symptoms of a paresis, hallucination (visual or acoustical), depression, appetite loss, anxiety, aggressive behaviour, excitation, a disorientation; very seldom - psychosis activation. Carbamazepine role as the preparation causing or promoting development of a malignant antipsychotic syndrome, especially when it is prescribed together with neuroleptics, remains obscure.
Allergic reactions: very often - allergic dermal reactions, an urticaria which can be appreciable the expressed; sometimes - an exfoliative dermatitis, an erythrosis; an itch; very seldom - Stevens-Johnson's syndrome, a toxic epidermal necrolysis.
Dermatological reactions: very seldom - photosensitivity, a nodulose erythema, disturbances of a xanthopathy, purple, diaphoresis intensifying, abaissement of hair. It was informed on rare cases of a hirsutism, however the causal interrelation of this complication with Tegretol reception remains obscure.
From hemopoiesis system: very often - a leukopenia; often - a thrombocytopenia, an eosinophilia; seldom - a leukocytosis, deficiency of Acidum folicum; very seldom - an agranulocytosis, an aplastic anaemia, a true erythrocyte aplasia, an acute alternating porphyria, a reticulocytosis, and, probably, hemolitic anaemia.
From a liver: very often - rising of level the scale-glutamiltransferazy (owing to an induction of this enzyme in a liver), that usually has no clinical value; sometimes - rising of level of transaminases; seldom - a hepatitis of the cholestatic, parenchymatous (hepatocellular) or admixed type, an icterus.
From the party GASTROINTESTINAL TRACT: very often - a nausea, vomiting; often - dryness in a mouth; sometimes - a diarrhoeia or a constipation, abdominal pains; very seldom - a glossitis, a stomatitis, a pancreatitis.
From cardiovascular system: seldom - disturbances of endocardiac conductivity; an arterial hypertensia or a hypotension; very seldom - a bradycardia, arrhythmias, AV blockade with syncopes, a collapse, a congestive heart failure, an exacerbation of ischemic illness, a thrombophlebitis.
From endocrine system and a metabolism: often - edemas, a liquid delay, augmentation of mass of a body, a hyponatremia and depression of an osmolarity of plasma owing to the effect similar to action of an antidiuretic hormone, that in rare instances leads to the hyponatremia of delution accompanied by a lethargy, vomiting, a headache, a disorientation and neurologic disturbances; very seldom - rising of level of Prolactinum, accompanied or not accompanied by such implications as a galactorrhea, a gynecomastia; changes of indicators of function of a thyroid gland - depression of level of a L-thyroxine (FT4, T4, T3) that usually is not accompanied by clinical implications; disturbances of a metabolism of an osteal tissue (depression of level of calcium and 25-Oh-holekaltsiferola in a blood plasma), that leads to an osteomalacia; on occasion - rising of concentration of cholesterol, including cholesterol of lipoproteins of high density, and triglycerides.
From genitourinary system: very seldom - an intersticial nephritis, renal insufficiency, disturbance of function of kidneys (for example, an albuminuria, a hematuria, an oliguria, urea/azotemia rising), the speeded up emiction, an ischuria, disorders of sexual function/impotency.
From sense organs: very seldom - disturbances of gustatory sensations, cataract, a conjunctivitis; hearing disorders, including a sonitus, a hyperacusia, changes of perception of height of a sound.
From osteomuscular system: very seldom - arthralgias, muscular pains or cramps.
From respiratory system: very seldom - reactions of hypersensitivity from the lungs, characterised by a fever, a dyspnea, a pneumonitis or a pneumonia.
Contraindications
- AV blockade;
- Presence in the anamnesis of episodes of suppression of a medullar hemopoiesis or data on an acute alternating porphyria;
- A hypersensibility to carbamazepine or similar medicinal preparations in the chemical relation.
Pregnancy and lactemia
Treatment by epilepsy Tegretol at pregnancy should be carried out with extra care.
At women of genital age Tegretol should be applied, whenever possible, as monotherapy as at application for the person of combinations of antiepileptic agents frequency of congenital anomalies of a foetus exceeded that at those who received each of these agents in the form of monotherapy.
It is necessary to prescribe the minimum effective dose of Tegretol. The regular control of level of carbamazepine in a blood plasma Is recommended.
At offensive of pregnancy at the woman receiving Tegretol or in the event that there is a question on Tegretol appointment at pregnancy, it is necessary to compare carefully expected advantages of therapy and its possible complications, especially in I trimester of pregnancy.
It is known, that children who are born at mothers, sick of an epilepsy, more often others are predisposed to disturbances of pre-natal development, including developmental anomalies. It was informed that carbamazepine, as well as all basic antiepileptic agents, is capable to raise risk of occurrence of these disturbances though the final confirmation of it which would be received as a result of controllable researches with application of Tegretol as monotherapy, is not available till now.
It is known, that at pregnancy deficiency of Acidum folicum develops. It was informed that antiepileptic agents strengthen this deficiency. It can promote augmentation of frequency of congenital defects at children who are born at women, accepting antiepileptic agents. Therefore to and during pregnancy additional reception of Acidum folicum is recommended.
For the purpose of preventive maintenance of the raised staxis at newborns to women last weeks pregnancy, and also the newborn recommends to prescribe vitamin K1.
Carbamazepine is allocated with thoracal milk, concentration in it make 25-60 % from level in a blood plasma. Therefore it is necessary to compare advantages and possible undesirable consequences of thoracal feeding in the conditions of proceeding therapy by Tegretol. Mothers accepting Tegretol, can continue thoracal feeding but provided that for the child observation concerning development of possible side-effects (for example, the expressed drowsiness, allergic dermal reactions) will be established.
Special indicatings
During Tegretol reception the agranulocytosis and an aplastic anaemia can develop. However, because these conditions arise very seldom, difficultly to calculate concrete value of their risk. It is known, that total risk of development of an agranulocytosis in the general population which were not receiving treatments, makes 4.7 cases on 1 million population a year, and an aplastic anaemia - 2.0 cases on 1 million population a year.
During application of Tegretol with various frequency transient or proof depression of number of thrombocytes or leucocytes becomes perceptible. Nevertheless, before the treatment beginning, and also periodically in the course of treatment it is necessary to carry out clinical analyses of blood, including calculation of number of thrombocytes and, probably, reticulocytes and also to define iron level in blood serum.
When during treatment low level of number of leucocytes or thrombocytes is noted (or the tendency to their depression), it is necessary to observe of a condition of the patient and indicators of the developed clinical analysis of blood attentively. If signs of appreciable oppression of an osteal brain are taped, Tegretol should be cancelled.
Tegretol should be cancelled immediately in the event that signs and the symptoms presumably testifying to development of serious dermatological reactions - for example, Stevens-Johnson's syndrome or a Lyell's disease become perceptible.
Tegretol should be applied only under condition of maintenance of medical observation.
It is necessary to be careful at application of Tegretol for patients with the admixed forms of convulsive attacks, including absentias epileptica (typical and atypical). In all these cases Tegretol can cause intensifying of attacks. If it occurs, Tegretol should be cancelled.
Before appointment of Tegretol and in the course of treatment research of function of a liver, especially at patients in which anamnesis there are data on liver diseases, and also at patients of advanced age is necessary. In case of intensifying of already available disturbances of function of a liver or at occurrence of active disease of a liver Tegretol should be cancelled immediately.
It is necessary to inform of patients the information on the precursory symptoms of toxicity inherent to probable hematological disturbances, and also on symptoms from integuments and a liver. The patient inform on necessity immediately to address to the doctor in case of occurrence of such undesirable reactions, as a fever, pharyngalgias, an eruption, ulcers in oral cavities, causeless occurrence of ecchymoses, hemorrhages in the form of petechias or purples.
To patients who in the anamnesis have data on diseases of heart, a liver, kidneys, collateral hematological reactions to other medical products or about cancellation before spent treatment by Tegretol, the preparation should be prescribed only after the careful analysis of a parity between expected effect of treatment and possible risk of therapy, and at maintenance of the attentive and regular control.
Before the beginning of treatment by Tegretol and periodically in the course of therapy research of the general analysis of urine and urea level in blood is recommended.
Weakly expressed dermal reactions, for example, the isolated macular or makulo-papular exanthema, in most cases are transitional and not serious, usually pass within several days or weeks even at continuation of treatment or after a preparation dose decline. Nevertheless, the patient should be at this time under steadfast observation of the doctor.
Tegretol possesses weak anticholinergic activity. Therefore in case of application of a preparation for patients with the raised ophthalmotonus the constant control of this indicator is necessary.
By present time separate reports on disturbances of a man's fecundity and-or spermatogenesis disturbances are registered. However the causal interrelation of these disturbances with Tegretol reception is not established yet.
Reports on occurrence at women of bleedings during the period between a menses in cases when peroral contraceptives were simultaneously applied are known. Tegretol can negatively affect reliability of peroral contraceptive preparations, therefore women of genital age in treatment by Tegretol should apply alternative methods of preservation from pregnancy.
Though the interrelation between size of a dose of a preparation and carbamazepine level in a blood plasma, and also between carbamazepine level in a blood plasma and its clinical efficiency or shipping is rather insignificant, nevertheless, regular definition of level of carbamazepine can to appear useful in following situations: at sharp rising of frequency of attacks; to check up, whether the patient accepts a preparation properly; at pregnancy; at treatment of children or teenagers; at suspicion on disturbances of an absorption of a preparation; at suspicion on development of toxic reactions in case the patient accepts some medical products.
The sudden termination of reception of Tegretol can provoke convulsive attacks. If it is necessary to interrupt sharply treatment by Tegretol sick of an epilepsy, in this case it is necessary to carry out transition to other antiepileptic agent under cover of the preparation shown in such cases (for example, Diazepamum entered i.v. or it is rectal, or Phenytoinum entered i.v.).
Tegretol as well as other psychotropic drugs, shipping of alcohol can reduce. In this connection, the patient is recommended to refuse the alcohol use.
Use in pediatrics
Some cases of convulsive attacks and-or respiratory depressions at the newborns which mothers accepted Tegretol simultaneously with other anticonvulsant preparations are described. Besides, in connection with reception of Tegretol by mothers it was informed also on several cases of vomiting, a diarrhoeia and-or a subnutrition at newborns. Probably, these reactions represent implications at newborns of a withdrawal.
Influence on ability to driving of motor transport and to management of mechanisms
Ability of the patient accepting Tegretol, to fast reaction, especially in the beginning of therapy or in dose selection, can be broken owing to occurrence of giddinesses and drowsiness. Therefore at driving of the car or management of mechanisms the patient should show care.
Overdosage
The symptoms arising at an overdosage, cardiovascular and respiratory systems.
The central nervous system: a disorientation, drowsiness, excitation, hallucinations, a coma; sight misting, muffled speech, a dysarthtia, a nystagmus, dyskinesia, a hyperreflexia (in the beginning), a hyporeflexia (later); cramps, psychomotor disorders, a myoclonus, a hypothermia, a mydriasis.
Respiratory system: a respiratory depression, a fluid lungs.
Cardiovascular system: a tachycardia, an arterial hypotension, sometimes - a hypertensia, disturbances of conductivity with expansion of complex QRS; a cardiac standstill accompanied by a loss of consciousness.
GASTROINTESTINAL TRACT: vomiting, a delay of a passage of nutrition from a stomach, depression of a motility of a colon.
Treatment. In the beginning treatment should be based on a clinical condition of the patient; hospitalisation is shown. Definition of concentration of carbamazepine in plasma for poisoning acknowledgement by this agent and an estimation of degree of an overdosage is spent.
Evacuation of a contained stomach, gastric lavage, application of the activated coal is carried out. Late evacuation of gastric contents can lead to the delayed absorption and repeated occurrence of symptoms of an intoxication in recover. The symptomatic maintenance therapy in intensive care unit, monitoring of functions of heart, careful correction of electrolytic disorders is applied. The specific antidote is absent.
Special references
At development of an arterial hypotension Dopaminum or Dobutaminum introduction is shown i.v.; at development of disturbances of a rhythm of heart treatment select individually; at development of cramps - introduction of anticonvulsants, at hyponatremia development (a water intoxication) - restriction of introduction of a liquid that can promote prevention of an edematization of a brain.
Hemosorption carrying out on coal sorbents is recommended. It was informed on an inefficiency of an artificial diuresis, a hemodialysis and a peritoneal dialysis.
It is necessary to expect possibility of repeated intensifying of symptoms of an overdosage for the second and third day after its beginning that is caused by the slowed down absorption of a preparation.
Conditions and periods of storage
Tablets should be protected from moisture influence. Tablets should be stored at temperature not above 25 C; to protect from moisture influence. The preparation should be stored in a place inaccessible to children. The preparation should not be used after the term noted on packing.
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