Lyrica® – (Pregabalin)
ATX analogues N03AX16 Pregabalin
Antiepileptic drug (Antiepileptic drugs)
Nosological classification (ICD-10):
List of ICD-10 codes
Capsules 1 capsule.
Pregabalin | 25 mg | 75 mg | 150 mg | 300 mg |
Excipients: lactose monohydrate – 35 / 8.25 / 16.5 / 33 mg; corn starch – 20/8.375/16.75/33.5 mg; talc – 20 / 8.375 / 16.75 / 33.5 mg.
body: titanium dioxide (2.4423/2.4423/2.4423/2.4423%), gelatin (for all dosages – up to 100%)
cap: iron dye red oxide (for a dosage of 75 mg – 1.7361%, for a dosage of 300 mg – 0.7361%); titanium dioxide (2.4423/0.409/2.4423/0.409%); gelatin (for all dosages – up to 100%).
ink: shellac (24–27%); ethanol (23–26%); isopropanol (0.5-3%); butanol (0.5–3%); propylene glycol (3-7%); concentrated ammonia solution (1–2%); potassium hydroxide (0.05–0.1%); purified water (15–18%); iron dye black oxide (24–28%)
Description of the dosage form:
Capsules, 25 mg: hard, gelatin, size No. 4, with a cap and a white body. Black ink on the capsule body indicates the dosage and product code (“PGN 25”), on the cap – “Pfizer”.
Capsules, 75 mg: hard, gelatin, size #4, with a red-brown to dark red-brown* cap and a white body. Black ink on the capsule body indicates the dosage and product code (“PGN 75”), on the cap – “Pfizer”.
Capsules, 150 mg: hard, gelatin, size No. 2, with a white cap and a white body. Black ink on the capsule body indicates the dosage and product code (“PGN 150”), on the cap – “Pfizer”.
Capsules, 300 mg: hard, gelatin, size #0, with red-brown to dark red-brown cap* and white body. Black ink on the capsule body indicates the dosage and product code (“PGN 300”), on the cap – “Pfizer”.
The contents of the capsule are white powder.
In the original manufacturer’s certificates, these colors are described as: “orange”; “from light red-brown to red-brown” – “light orange”, which corresponds to the color of the comparison pantones used in the European Union for this type of analysis.
Pharmacological action – antiepileptic.
The active substance is pregabalin – an analogue of GABA – (S) -3- (aminomethyl) -5-methylhexanoic acid.
Mechanism of action:
It was found that pregabalin binds to an additional subunit (α-2-delta protein) of voltage-gated calcium channels in the CNS, irreversibly replacing (3H)-gabapentin. It is assumed that such binding may contribute to the manifestation of its analgesic and anticonvulsant effects.
Pregabalin has been shown to be effective in patients with diabetic neuropathy and postherpetic neuralgia.
It was found that when taking pregabalin courses up to 13 weeks 2 times a day and up to 8 weeks 3 times a day, in general, the risk of side effects and the effectiveness of the drug when taken 2 or 3 times a day are the same.
When taken in a course lasting up to 13 weeks, the pain decreased during the 1st week, and the effect persisted until the end of treatment.
There was a 50% reduction in pain index in 35% of patients treated with Lyrica and 18% of patients treated with placebo. Among patients who did not experience drowsiness, the effect of such a reduction in pain was observed in 33% of patients in the pregabalin group and 18% of patients in the placebo group. Somnolence occurred in 48% of patients treated with pregabalin and 16% of patients treated with placebo.
A marked reduction in the pain symptoms associated with fibromyalgia has been observed with the use of pregabalin at doses of 300 to 600 mg/day. The effectiveness of doses of 450 and 600 mg / day is comparable, but tolerability of 600 mg / day is usually worse.
Also, the use of pregabalin is associated with a marked improvement in the functional activity of patients and a decrease in the severity of sleep disorders. The use of pregabalin at a dose of 600 mg/day led to a more pronounced improvement in sleep compared with a dose of 300–450 mg/day.
When taking the drug for 12 weeks, 2 or 3 times a day, the marked risk of side effects and the effectiveness of the drug are the same. The decrease in the frequency of seizures began within the 1st week.
Generalized Anxiety Disorder:
A decrease in the symptoms of generalized anxiety disorder is noted on the 1st week of treatment. When using the drug for 8 weeks, 52% of patients treated with pregabalin and 38% of patients treated with placebo had a 50% reduction in symptoms according to the Hamilton anxiety scale (HAM-A).
The pharmacokinetic parameters of pregabalin at steady state in healthy volunteers with epilepsy who received antiepileptic therapy and patients who received it for chronic pain syndromes were similar.
Pregabalin is rapidly absorbed on an empty stomach. Tmax of the drug in plasma is 1 hour both for single and repeated use. The oral bioavailability of pregabalin is ≥90% and is dose independent. With repeated use, Css is reached after 24-48 hours. When using the drug after a meal, Cmax decreases by about 25-30%, and Tmax increases by about 2.5 hours. However, food intake does not have a clinically significant effect on the total absorption of pregabalin.
Vd pregabalin after oral administration is approximately 0.56 l / kg. The drug does not bind to plasma proteins.
Pregabalin is practically not metabolized. After administration of labeled pregabalin, approximately 98% of the radioactive label is determined in the urine in unchanged form. The proportion of the N-methylated derivative of Lyric®, which is the main metabolite found in urine, is 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 unchanged.
The average T1 / 2 is 6.3 hours. Plasma clearance of pregabalin and renal clearance are directly proportional to creatinine clearance. In patients with impaired renal function and patients on hemodialysis, dose adjustment is necessary.
Linearity/Nonlinearity. The pharmacokinetics of pregabalin in the range of recommended daily doses is linear, inter-individual variability is low (<20%). Repeated dose pharmacokinetics can be predicted from single dose data. Therefore, there is no need for regular monitoring of pregabalin concentrations.
Does not have a clinically significant effect on plasma concentrations of Lyric.
Impaired kidney function. Pregabalin clearance is directly proportional to creatinine clearance. Given that the drug is mainly excreted by the kidneys, it is recommended to reduce the dose of pregabalin in patients with impaired renal function. In addition, pregabalin is effectively removed from plasma during hemodialysis (after a 4-hour hemodialysis session, plasma concentrations of pregabalin are reduced by about 50%), after hemodialysis, an additional dose of the drug must be prescribed.
Impaired liver function. The pharmacokinetics of pregabalin in patients with hepatic impairment has not been specifically studied. Pregabalin is practically not metabolized and is excreted mainly unchanged in the urine, so impaired liver function should not significantly alter plasma concentrations of the drug.
Elderly patients (over 65 years old). Pregabalin clearance tends to decrease with age, reflecting an age-related decline in creatinine clearance. Elderly people with impaired renal function may need to reduce the dose of the drug.
Buy Lyrica® – Pregabalin
Neuropathic pain in adults;
With caution: renal failure; heart failure; possible presence of rare hereditary diseases. In connection with the reported isolated cases of uncontrolled use of pregabalin, it should be prescribed with caution in patients with a history of drug dependence. Such patients need close medical supervision during drug treatment.
Use during pregnancy and lactation
There are no adequate data on the use of pregabalin during pregnancy.
In experimental studies on animals, the drug had a toxic effect on reproductive function. Therefore, pregabalin should only be used during pregnancy if the potential benefit to the mother clearly outweighs the potential risk to the fetus.
Women of reproductive age should use adequate methods of contraception while receiving pregabalin.
There is no information on the excretion of pregabalin in breast milk in women, but it has been observed that in rats it is excreted in breast milk. Therefore, breastfeeding is not recommended during treatment with pregabalin.
Based on clinical experience with pregabalin in more than 12,000 patients, the most common adverse events were dizziness and drowsiness. The phenomena observed were usually mild or moderate. The rate of discontinuation of pregabalin and placebo due to adverse reactions was 14% and 7%, respectively. The main adverse events that required discontinuation of treatment were dizziness (4%) and drowsiness (3%), depending on their subjective tolerance.
Other side effects that also lead to drug withdrawal are ataxia, confusion, asthenia, impaired attention, blurred vision, impaired coordination, peripheral edema.
Listed below are all adverse events that occurred more than in the placebo group (affecting more than 1 person). They are distributed according to system-organ classes and frequency: very often – ≥1/10; often – ≥1/100, <1/10; infrequently – ≥1/1000, <1/100; rarely – <1/1000.
The listed adverse events could be associated with the underlying disease and / or concomitant therapy.
Infections and invasions: infrequently – nasopharyngitis.
From the blood and lymphatic system: rarely – neutropenia.
Metabolism and nutrition disorders: often – increased appetite; infrequently – anorexia, hypoglycemia.
Mental disorders: often – euphoria, confusion, decreased / increased libido, irritability, increased insomnia / insomnia, disorientation; infrequently – depersonalization, anorgasmia, anxiety, depression, agitation, mood lability, depressed mood, difficulty in finding words, hallucinations, unusual dreams, panic attacks, apathy; rarely – disinhibition, high spirits.
Neurological disorders: very often – dizziness, drowsiness; often – ataxia, impaired attention, impaired coordination, memory impairment, tremor, dysarthria, paresthesia, imbalance, amnesia, sedation, lethargy; infrequently – cognitive disorders, hypesthesia, nystagmus, speech disturbance, myoclonic convulsions, 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, dysgraphia.
On the part of the organ of vision: often – blurred vision, diplopia; infrequently – narrowing of the visual fields, decreased visual acuity, eye pain, asthenopia, as well as dry eyes, swelling of the eyes, increased lacrimation; rarely – flashing sparks before the eyes, eye irritation, mydriasis, oscillopsia (subjective sensation of fluctuation of the objects in question), impaired perception of visual depth, loss of peripheral vision, strabismus, increased brightness of visual perception.
From the side of the organ of hearing and the vestibular apparatus: often – vertigo; infrequently – hyperacusis.
From the side of the CCC: infrequently – tachycardia, AV blockade of the 1st degree, flushing of the face, lowering blood pressure, cold extremities, increased blood pressure, skin flushing; rarely – sinus tachycardia, sinus arrhythmia, sinus bradycardia.
From the respiratory system: infrequently – shortness of breath, cough, dryness of the nasal mucosa; rarely – nasal congestion, nosebleeds, rhinitis, snoring, tightness in the throat.
From the digestive system: often – dry mouth, constipation, vomiting, flatulence, bloating; infrequently – increased salivation, gastroesophageal reflux, hypesthesia of the oral mucosa; rarely – ascites, dysphagia, pancreatitis.
On the part of the skin: infrequently – sweating, papular rash; rarely – cold sweat, urticaria.
From the musculoskeletal system: infrequently – muscle twitching, joint swelling, muscle spasms, myalgia, arthralgia, back pain, pain in the extremities, muscle stiffness; rarely – spasm of the cervical muscles, neck pain, rhabdomyolysis.
From the urinary system: infrequently – dysuria, urinary incontinence; rarely – oliguria, renal failure.
From the reproductive system: often – erectile dysfunction; infrequently – delayed ejaculation, sexual dysfunction; rarely – amenorrhea, pain in the mammary glands, discharge from the mammary glands, dysmenorrhea, enlargement of the mammary glands in volume.
Other: often – fatigue, swelling, incl. peripheral, feeling of intoxication, gait disturbance; infrequently – asthenia, falls, thirst, chest tightness, generalized edema, chills, pain, pathological sensations; rarely – hyperthermia.
Laboratory indicators and instrumental data: often – an increase in body weight; infrequently – an increase in the activity of ALT, CPK, AST, a decrease in the number of platelets; rarely – an increase in the concentration of glucose and blood creatinine, a decrease in the concentration of blood potassium, a decrease in body weight, a decrease in the number of leukocytes in the blood.
Other increased fatigue:
Pregabalin is excreted in the urine, mostly unchanged, undergoes minimal metabolism in humans (less than 2% of the dose is excreted in the urine as metabolites), does not inhibit the metabolism of other drugs in vitro and does not bind to plasma proteins, so it is unlikely to be able to enter into a pharmacokinetic interaction.
There was no evidence of a clinically significant pharmacokinetic interaction of pregabalin with phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone, or ethanol. Oral hypoglycemic agents, diuretics, insulin, phenobarbital, tiagabine, and topiramate have not been shown to have a clinically significant effect on pregabalin clearance.
When using oral contraceptives containing norethisterone and / or ethinylestradiol, along with pregabalin, the equilibrium pharmacokinetics of the drugs did not change, the price of the drug.
Respiratory failure and coma have been reported with concomitant use of pregabalin with other drugs that depress the central nervous system. It was also reported about the negative impact of pregabalin on the activity of the gastrointestinal tract (including the development of intestinal obstruction, paralytic ileus, constipation) when used simultaneously with drugs that cause constipation (such as non-narcotic analgesics).
Repeated oral pregabalin with oxycodone, lorazepam, or ethanol had no clinically significant effect on respiration. Pregabalin appears to enhance the cognitive and motor impairments induced by oxycodone. Pregabalin may enhance the effects of ethanol and lorazepam.
How dangerous is Lyrica®!!!
Ephedrine and methadone addictions are almost one hundred percent similar in their symptoms to lyric addiction. Constantly using Lyrica®, the patient becomes completely dependent on the drug.
The psyche is broken. The patient constantly experiences a feeling of anxiety, he develops tachycardia. It is very easy to get hooked on medicine. Many drug addicts start using lyrics just to get rid of drug addiction. They numb withdrawal symptoms by using Lyrica® in small doses and quantities. However, drug addicts quickly break down. They use Lyrica® several times more than necessary. The result is very deplorable – the patient becomes dependent on the lyrics, with all the ensuing negative consequences.
Memory problems, headaches and dizziness are the main symptoms experienced by a person hooked on this drug. Lyrica harms libido, erection problems appear, sexual weakness
From the use of lyrics is almost impossible to wean yourself. And if you take Lyrica® for a long time without resorting to the help of doctors, it is likely that the patient will die soon. The body cannot withstand such a load.
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