Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Anticonvulsant with analgesic and anxiolytic action. Pregabalin is an analog of GABA.
It is assumed that the analgesic and anticonvulsant action is due to the binding of pregabalin to the additional subunit (? 2- delta-protein) of the potential-dependent calcium channels in the CNS, which leads to the irreversible replacement of [3H] -gabapentin.
Pregabalin reduces clinical manifestations of generalized anxiety disorder.
PHARMACOKINETICS
After oral administration, pregabalin is rapidly absorbed from the digestive tract. C max in plasma is achieved in 1 h as in single or repeated administration. Bioavailability of pregabalinum at intake makes? 90% and does not depend on the dose. With repeated application, the equilibrium state is reached after 24-48 hours. After application, Cmax decreases by about 25-30%, and the time to reach Cmax increases to about 2.5 hours. However, the intake of food does not have a clinically significant effect on the total absorption of pregabalin .
The pharmacokinetics of pregabalin in the range of recommended daily doses is linear, interindividual variability is low (<20%).
The apparent V d of pregabalin after oral administration is approximately 0.56 l / kg. Pregabalin does not bind to plasma proteins.
Pregabalinum is practically not exposed to a metabolism. After taking labeled pregabalin, approximately 98% of the radioactive label was detected in the urine unchanged. The proportion of the N-methylated pregabalin derivative, which is the main metabolite found in the urine, was 0.9% of the dose. There were no signs of racemization of the S-enantiomer of pregabalin into the R-enantiomer.
Pregabalin is excreted mainly by the kidneys in unchanged form. The mean T 1/2 is 6.3 h. The clearance of pregabalin from the plasma and the kidney clearance are directly proportional to the CK.
Parameters of pharmacokinetics of pregabalin in equilibrium in healthy volunteers, in patients with epilepsy receiving antiepileptic therapy, and in patients receiving it for chronic pain syndromes were similar.
If the kidney function is disturbed, it should be borne in mind that pregabalin clearance is directly proportional to QC. Pregabalin is effectively removed from the plasma during hemodialysis (after a 4-hour hemodialysis session, pregabalin concentrations in the plasma are reduced by approximately 50%).
The pharmacokinetics of pregabalin in patients with impaired liver function has not been specifically studied. Pregabalinum is practically not exposed to a metabolism and deduced basically in the unchanged kind with urine, therefore infringement of function of a liver should not essentially change concentration of a preparation in a plasma.
When prescribing the drug, patients older than 65 years should take into account that the clearance of pregabalin with age tends to decrease, which reflects the age-related decrease in QC. Elderly people with impaired renal function may need to reduce the dose of the drug.
INDICATIONS
Treatment of neuropathic pain in adults.
Treatment of fibromyalgia in adults.
Epilepsy: as an additional therapy in adults with partial seizures, accompanied or not accompanied by secondary generalization.
Treatment of generalized anxiety disorder in adults.
DOSING MODE
Is taken orally regardless of meals in a daily dose of 150 to 600 mg in 2 or 3 divided doses.
If treatment should be stopped, then it is recommended to do this gradually for at least 1 week.
For patients with impaired renal function, the dose is selected individually, taking into account QC.
In patients with impaired liver function, dose adjustment is not required.
Patients older than 65 years may need to reduce the dose of pregabalin due to a decrease in kidney function.
In the case of missing a dose of pregabalin, the next dose should be taken as soon as possible, but the missed dose should not be taken if the next admission time is appropriate.
SIDE EFFECT
From the side of the psyche: often - euphoria, confusion, decreased libido, irritability, insomnia, disorientation; infrequently - depersonalization, anorgasmia, anxiety, depression, agitation, lability of mood, depressed mood, difficulty in choosing words, hallucinations, unusual dreams, increased libido, panic attacks, apathy, increased insomnia; rarely - disinhibition, high spirits.
From the nervous system: very often - dizziness, drowsiness; often - ataxia, impaired attention, impaired coordination, memory impairment, tremor, dysarthria, paresthesia, imbalance, amnesia, sedation, lethargy; infrequently - cognitive disorders, hypoesthesia, nystagmus, speech disorders, myoclonic cramps, weakening of reflexes, dyskinesia, psychomotor agitation, postural dizziness, hyperesthesia, loss of taste sensations, burning sensation on the mucous membranes and skin, intentional tremor, stupor, fainting; rarely - hypokinesia, parosmia, dysgraphy; frequency unknown - headache.
From the senses: often - dizziness, blurred vision, diplopia; infrequent - hyperacusis, narrowing of visual fields, reduced visual acuity, eye pain, asthenopia, dry eyes, puffiness of eyes, increased lacrimation; rarely - flashes of sparks in front of the eyes, eye irritation, mydriasis, oscilloscopy (subjective sensation of fluctuations in the subjects under consideration), impaired perception of the depth of vision, loss of peripheral vision, strabismus, increased brightness of visual perception; frequency is unknown - keratitis.
From the side of metabolism: often - increased appetite, weight gain; infrequently - anorexia, hypoglycemia; rarely - a decrease in body weight.
From the cardiovascular system: infrequently - tachycardia, AV-blockade of the I degree, hot flashes, lower blood pressure, cold extremities, increased blood pressure; rarely - sinus tachycardia, sinus arrhythmia, sinus bradycardia; frequency unknown - chronic heart failure, prolongation of QT interval.
On the part of the respiratory system: infrequently - shortness of breath, cough, dryness of the nasal mucosa, nasopharyngitis; rarely - nasal congestion, nosebleed, rhinitis, snoring, a feeling of tightness in the throat; infrequently - pulmonary edema.
On the part of the digestive system: often - dry mouth, constipation, vomiting, flatulence, bloating; infrequently - increased salivation, gastroesophageal reflux, hypoesthesia of the oral mucosa; rarely - ascites, dysphagia, pancreatitis; frequency unknown - swelling of the tongue, nausea, diarrhea.
From the musculoskeletal system: infrequent - muscle twitching, swelling of the joints, muscle spasms, myalgia, arthralgia, back pain, pain in the limbs, stiffness in the muscles; rarely - spasm of the neck muscles, neck pain, rhabdomyolysis.
From the urinary system: infrequently - dysuria, urinary incontinence; rarely - oliguria, renal insufficiency.
From the side of the reproductive system: often - erectile dysfunction; infrequently - delay of ejaculation, sexual dysfunction; rarely - amenorrhea, pain in the mammary glands, discharge from the mammary glands, dysmenorrhea, enlargement of mammary glands in the volume.
From the hemopoietic system: rarely - neutropenia.
Dermatological reactions: infrequent - skin hyperemia, sweating, papular rash; rarely - cold sweat; frequency is unknown - itching, Stevens-Johnson syndrome.
Allergic reactions: rarely - hives; frequency is unknown - angioedema), hypersensitivity.
On the part of laboratory indicators: infrequently - increased activity of ALT, AST, KFK, decrease in the number of platelets; rarely - an increase in the content of glucose and creatinine in the blood, a decrease in the level of potassium in the blood, a decrease in the number of leukocytes in the blood.
Other: often - fatigue, peripheral edema, a feeling of intoxication, a violation of gait; infrequently - asthenia, falls, thirst, a feeling of restraint in the chest, generalized edema, chills, pain; rarely - hyperthermia.
CONTRAINDICATIONS
Children and adolescents up to 17 years of age, hypersensitivity to pregabalin.
PREGNANCY AND LACTATION
Adequate strictly controlled studies of the safety of the use of pregabalin in pregnancy have not been conducted. When using pregabalin, women of reproductive age should use adequate methods of contraception.
It is not known whether pregabalin is excreted in human breast milk. If it is necessary to use pregabalin during lactation, the question of stopping breastfeeding should be solved.
In experimental animal studies, pregabalin exerted a toxic effect on reproductive function. It has been established that pregabalin is excreted in breast milk in rats.
SPECIAL INSTRUCTIONS
With caution should be used for kidney failure, with heart failure. In connection with the registered single cases of uncontrolled use of pregabalin, it must be used with caution in patients with drug dependence in the anamnesis (during the treatment in such cases strict medical control is required).
In patients with diabetes mellitus, in case of weight gain in the background of pregabalin treatment, dosage adjustment of hypoglycemic drugs may be required.
Pregabalinum should be canceled in case of development of symptoms of angioneurotic edema (such as, facial edema, perioral edema or swelling of the tissues of the upper respiratory tract).
Pregabalin, like other anticonvulsants, can increase the risk of suicidal thoughts or behavior. Therefore, during the period of treatment, patients need careful medical supervision for the appearance or deterioration of depression, the appearance of suicidal thoughts or behavior.
Treatment with pregabalin was accompanied by dizziness and drowsiness, which increases the risk of accidental injuries (falls) in the elderly. In the course of postmarketing use, there were also cases of loss of consciousness, confusion and violation of cognitive functions. Therefore, until patients will not appreciate the possible effects of pregabalin, they should be careful.
Data on the possibility of canceling other anticonvulsants in suppression of seizures with pregabalin and the feasibility of monotherapy with pregabalin are insufficient. There are reports of the development of seizures, including. epileptic status and minor seizures, with the use of pregabalin or immediately after the end of therapy.
There were also cases of development of renal failure, in some cases after the abolition of pregabalin kidney function was restored.
As a result of cancellation of pregabalin after prolonged or short-term therapy, the following undesirable phenomena were observed: insomnia, headache, nausea, diarrhea, flu-like syndrome, depression, sweating, dizziness, convulsions and anxiety. Information on the incidence and severity of manifestations of the syndrome of cancellation of pregabalin, depending on the duration of therapy, and its dose is not available.
In the post-marketing application of pregabalin, chronic heart failure was reported against pregabalin therapy primarily in elderly patients who had cardiac dysfunction and who received the drug for neuropathy. Therefore, pregabalin should be used with caution in this category of patients. After the abolition of pregabalin, the disappearance of manifestations of such reactions is possible.
The frequency of CNS side reactions, especially such as drowsiness, is increased in the treatment of central neuropathic pain caused by spinal cord injury, which, however, may result from the summation of the effects of pregabalin and other concomitant drugs (for example, antispastic). This circumstance should be taken into account when presgabalin is prescribed for this indication.
There are reports of cases of development of dependence when using pregabalin. Patients with drug dependence in a history need careful medical observation for symptoms of dependence on pregabalin.
There have been cases of encephalopathy, especially in patients with concomitant diseases, which can lead to the development of encephalopathy.
Impact on the ability to drive vehicles and manage mechanisms
Pregabalin may cause dizziness and drowsiness and accordingly affect the ability to drive vehicles and use complex techniques. Patients should not drive vehicles, use complex equipment or engage in other potentially hazardous activities until an individual response to pregabalin is established.
DRUG INTERACTION
There were reported cases of respiratory failure and coma development with the simultaneous use of pregabalin with other drugs that depress the central nervous system.
It was also reported about the negative effect of pregabalin on gastrointestinal tract activity (including the development of intestinal obstruction, paralytic ileus, constipation) with concomitant use with drugs that cause constipation (such as non-narcotic analgesics).
Repeated oral administration of pregabalin with oxycodone, lorazepam or ethanol did not have a clinically significant effect on respiration. Pregabalin, apparently, enhances cognitive and motor function disorders caused by oxycodone. Pregabalin can enhance the effects of ethanol and lorazepam.
