Product Name: Pregabalin
Generic Name: Pregabalin
Common Brands: Lyrica
Pharmaceutical Categories: Epilepsy, Anti-Convulsants
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Here is an additional general information about this medication active ingredient pregabalin:
Pregabalin is an antiepileptic drugs which active ingredient is an analogue of gamma-aminobutirovoy acid (GABA).
Although the exact mechanism of action of pregabalin still uncertain, it was found that pregabalin binds with an additional subunit (alpha-2-delta protein) of voltage-dependent calcium channels in the CNS, it is assumed that such binding may contribute to the manifestation of its analgesic and anticonvulsant effects.
Pharmacokinetics of pregabalin in the range of recommended doses is linear, the intra-individual variability is low (< 20%). The pharmacokinetics of Pregabalin with repeated use can be predicted on the basis of data reception unit dose. Consequently, there is no need for regular monitoring of the concentration of pregabalin. Pregabalin is rapidly absorbed after oral administration on an empty stomach. Cmax in plasma is reached after 1 h both at single and repeated application. Bioavailability of pregabalin for oral admistration is or more than 90% and not dose-dependent. For doubled application an equilibrium is reached in 24-48 hours. Absorption of pregabalin is deteriorating under the influence of food. Than Cmax decreased by about 25-30%, and time to Cmax increased to approximately 2.5 hours. However, eating has no clinically significant effect on the overall absorption of pregabalin.
Why is Pregabalin prescribed?
- a treatment of neuropathic pain in adults.
- as an subsidiary aid in adults with partial seizures accompanied or not by secondary generalization.
Dosage and administration
Pregabalin is taken orally, regardless of eating in a daily dose of 150 to 600 mg 2 or 3 times.
Treatment of neuropathic pain started with a dose of 150 mg / day. Depending on the achieved effect and tolerability in 3-7 days the dose can be increased to 300 mg / day, and if necessary even after 7 days - up to a maximum dose of 600 mg / day.
Epilepsy treatment begins with a dose of 150 mg / day. Due to the effect and tolerability in 1 week the dose may be increased to 300 mg / day, and a week later - to a maximum dose of 600 mg / day.
Pregabalin side effects
Hematopoietic system: rarely - neutropenia.
Metabolism: often - increased appetite, weight gain, less often - anorexia, rarely - hypoglycemia, weight loss.
Psyche: often - euphoria, confusion, decreased libido, irritability, less often - depersonalization, anorgasmia, anxiety, depression, agitation, mood lability, increased insomnia, depressed mood, difficulty in finding words, hallucinations, unusual dreams, increased libido, panic attacks, apathy, rarely - disinhibition, elation.
CNS and peripheral nervous system: very often - dizziness, drowsiness; often - ataxia, impaired attention, impaired coordination, memory impairment, tremor, dysarthria, paresthesias; less frequently - cognitive dysfunction, hypesthesia, visual field defects, nystagmus, speech disorder, myoclonic seizures, the weakening of reflexes, dyskinesia, psychomotor hyperactivity and dizziness in the upright position, hypersthesia, loss of taste, burning sensation on the mucous membranes and skin, the intention tremor, stupor, faint; rarely - hypokinesia, parosmiya, chirospasm.
Vision: often - fog before the eyes, double vision; less often - reduced visual acuity, eye pain, asthenopia, as well as dry eyes, swollen eyes, excessive tearing; rarely - flickering sparks before the eyes, eye irritation, mydriasis, ostsillopsiya (subjective feeling vibrations considered subjects), impaired depth perception vision, loss of peripheral vision, strabismus, increasing the brightness of visual perception.
Hearing and vestibular: often - dizziness, rarely - giperakuziya.
Cardio-vascular system: less often - tachycardia, flushing, rarely - decreased blood pressure, cold extremities, increased blood pressure, AV-block I degree, sinus tachycardia, sinus arrhythmia, sinus bradycardia.
Respiratory system: less often - shortness of breath, dryness of the nasal mucosa, rarely - nasopharyngitis, cough, nasal congestion, nosebleeds, rhinitis, snoring, feeling of tightness in the throat.
Digestive system: often - dry mouth, constipation, vomiting, flatulence, less often - increased salivation, gastroesophageal reflux, reduce the sensation of feeling in the mouth, rarely - ascites, dysphagia, pancreatitis.
Dermatological reactions: less often - sweating, papulleznaya rash, rarely - a cold sweat, urticaria.
Musculoskeletal system: less often - twitching of muscles, swelling of joints, muscle cramps, myalgia, arthralgia, back pain, pain in the limbs, stiffness in muscles, rarely - a spasm of neck muscles, neck pain, rhabdomyolysis.
With the urinary system: less often - dysuria, urinary incontinence, rarely - oliguria, renal failure.
Reproductive system: often - erectile dysfunction, less often - delayed ejaculation, sexual dysfunction, rarely - amenorrhea, breast pain, discharge from the breast, dysmenorrhea, hypertrophy of the mammary glands.
From the body as a whole: often - fatigue, peripheral edema and generalized edema, feeling drunk, disturbance of gait, less often - asthenia, fall, thirst, chest tightness, rarely - increased pain with anasarca, fever, chills.
childhood and adolescence to 17 years (currently there is no data of using Lyrica for this type of patients)
hypersensitivity to active substance or to any other component of the drug.
Lyrica should be prescribed with precautions in renal failure in the presence of rare inherited diseases.
Using during pregnancy and breastfeeding
There is no adequate data on the use of pregabalin in pregnancy.
In experimental animal studies Lyrica has toxic effects on reproductive function.
Due to this the drug Lyrica can be prescribed during pregnancy only if the intended benefits to the mother clearly outweighs the potential risk to the fetus.
Using the drug Lyrica women of childbearing age should use adequate contraceptive methods.
There is no information about pregabalin excretion in breast milk of women.
However, experimental studies have found that it is excreted in breast milk of rats.
Regarding this during treatment by Pregabalin is recommended to stop breastfeeding.
The drug should not be prescribed for patients with hereditary intolerance to galactose, deficiency of lactase lapp (lactase deficiency in some peoples of the North), malabsorption of glucose / galactose.
For some patients with diabetes in the case of weight gain during treatment with the drug Pregabalin may require adjustment of doses of hypoglycemic drugs.
Treatment with Lyrica accompanied by dizziness and drowsiness, which increase the risk of accidental injury (falls) in older people.
As long as patients do not appreciate the possible effects of the drug, they should proceed with caution.
Information about the possibility of removing other anticonvulsants in the suppression of seizures and whether pregabalin monotherapy with this drug are not enough.
Safety and efficacy of the drug in children under the age of 12 years and adolescents aged 12-17 years have not been established.
The drug Lyrica may cause dizziness and drowsiness and consequently affect your ability to drive and use sophisticated technology. Patients should not drive, use sophisticated technology, or perform other potentially dangerous activities until it is determined by the individual patient's response to the drug.
Pregabalin drug interactions
Pregabalin is excreted in the urine mostly unchanged, undergoes minimal metabolism in humans (in the form of metabolites with urine output of less than 2% of dose), did not inhibit the metabolism of other drugs in vitro and is not bound to plasma proteins, so it is unlikely to engage in a pharmacokinetic interaction.
Not found evidence of clinically significant pharmacokinetic interaction pregabalin with phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone or ethanol. It was established that oral hypoglycemic agents, diuretics, insulin, phenobarbital, topiramate and tiagabine has no clinically significant effect on pregabalin clearance.
With use of oral contraceptives containing norethisterone and / or ethinyl estradiol, in conjunction with the equilibrium pregabalin pharmacokinetics of both drugs was unchanged.
Repeated oral application of pregabalin with oxycodone, lorazepam or ethanol has no clinically significant effect on respiration. Apparently pregabalin enhances cognitive disorders and motor function caused by oxycodone. Pregabalin can increase the effects of ethanol and lorazepam.
Pregabalin in case of emergency / overdose
With an overdose of Pregabalin (up to 15 grams) any of adverse reactions were not been reported.
Treatment: gastric lavage, supportive therapy, if necessary - hemodialysis.