Lyrica tablets - a drug, consequences of use, how to get off?

Pharmacological properties

Lyrica is a drug with antiepileptic and anticonvulsant activity. The active component of the drug is pregabalin - an alkylated analogue of gamma-aminobutyric acid, however, despite the structural similarity of the molecules, pregabalin does not have the activity characteristic of gamma-aminobutyric acid. Pregabalin has neither direct nor indirect GABAergic effects. The mechanism of action of the drug is based on its ability to bind to the alpha-2-delta subunits of neuronal calcium channels (N- and P/O-type calcium channels), resulting in a decrease in calcium transport into neuronal cells in response to the action potential. The drug is characterized by a high degree of affinity for alpha-2-delta protein located in the tissues of the central nervous system. The use of the drug leads to a decrease in the release of pain neurotransmitters (including glutamate, norepinephrine and substance P) into the synaptic cleft when neurons are excited. Due to such changes, under the influence of the drug, impulse conduction is selectively suppressed; it should be noted that the drug Lyrica suppresses the excitability of the neuron network only under pathological conditions.

The drug has an analgesic effect for pain of neuropathic etiology and postoperative pain syndrome, including conditions such as hyperalgesia and alodynia. The drug in a therapeutic dose is well tolerated by patients; during studies, the absence of a teratogenic effect was noted when the drug was used in doses 2 times higher than the therapeutic one. As a result of a number of studies, the absence of carcinogenic and genotoxic effects of pregabalin was noted. After oral administration, the drug is well absorbed from the gastrointestinal tract, the peak concentration of the active substance in the blood plasma is observed 1 hour after oral administration of the drug. With repeated use of Lyrica, the time to reach the maximum plasma concentration of the active substance does not change. The bioavailability of the drug does not depend on the dose taken and is about 90%. With repeated use of the drug, equilibrium concentrations of pregabalin are achieved within 24-48 hours. Eating reduces the rate and degree of absorption of pregabalin, so when taking the drug simultaneously with food, the time to reach the peak of the active substance in plasma increases by 2.5 hours, and the maximum plasma concentrations of the drug are reduced by 25-30% (compared to the data obtained after administration drug on an empty stomach). It should be noted that food intake does not have a clinically significant effect on the amount of absorption. The drug does not bind to plasma proteins. Pregabalin penetrates well through the blood-brain and hematoplacental barriers and is also excreted in breast milk. A small part of the drug (less than 1%) is metabolized to form an N-methylated compound. The drug is excreted unchanged in the urine. About 1% of the drug is excreted in the urine as a metabolite. The half-life of the drug is 6.3 hours. It should be noted that pregabalin clearance is directly proportional to creatinine clearance. In patients taking antiepileptic drugs and patients suffering from chronic pain syndrome, pharmacokinetics are similar to those in healthy volunteers. In patients suffering from impaired renal function, dose adjustment is necessary. The decrease in pregabalin clearance in patients with renal failure is directly proportional to the decrease in creatinine clearance. Patients with reduced creatinine clearance need to reduce the dose of Lyrica, and patients on hemodialysis need to increase the dose of pregabalin after a hemodialysis session (after 4 hours of hemodialysis, about 50% of the dose of the drug is removed from the blood plasma). In patients suffering from liver failure, dosage adjustment of the drug is usually not required, since pregabalin is metabolized in small quantities, and impaired liver function does not have a significant effect on the pharmacokinetics of the drug. In elderly patients, there is a decrease in the clearance of creatinine and pregabalin; it is recommended to adjust the dose of Lyrica in patients with age-related renal impairment.

Side effects from Lyrica

Like any other drug, Lyrica has an impressive list of side effects: tremors of the limbs, nausea, vomiting, insomnia, increased sweating, hallucinations, dry mucous membranes, bloating, lack of sexual desire and erection. Due to frequent diarrhea, it is possible to wash out all useful substances from the body, in particular calcium, which threatens osteoporosis.

Memory lapses, so common to many drug addicts, are also relevant when taking Lyrica. A person may not remember what happened an hour or a day ago.

How does it affect potency?

As mentioned above, the drug almost completely eliminates libido. At the same time, problems with potency may not be solved even after stopping taking Lyrica. There are known cases of infertility.

How addiction is formed

The addiction to the drug forms unnoticed by the user - the first doses only bring a feeling of high. Next, the body begins to adapt to the active substance and requires increasingly larger dosages to return to the original sensations. Often, an increase in the amount of Lyrica can cause a sharp change in mood and causeless aggression even towards close people. There are known cases of suicide under the influence of the drug.

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Directions for use and dosage

Lyrica is taken orally; it is recommended to swallow the capsule whole, without chewing or crushing, with a sufficient amount of water. The drug is taken regardless of meals. The duration of the course of treatment and the dose of the drug are determined by the attending physician individually for each patient, depending on the nature of the disease and the patient’s personal characteristics. Adult patients suffering from neuropathic pain are usually prescribed the drug at an initial dose of 75 mg 2 times a day. If necessary, the dose is gradually increased to 150 mg 2 times a day (this dose is optimal for most patients with pain of neuropathic etiology). Some patients, depending on individual sensitivity to pregabalin and the severity of the disease, require higher doses of the drug. In this case, the dose is first gradually increased to 150 mg 2 times a day, then the dose can be increased to 300 mg of the drug 2 times a day (an interval of at least 7 days must be maintained between each dose increase). The maximum daily dose of the drug is 600 mg. The therapeutic effect develops within a week after starting to use the drug. The duration of the course of treatment is determined by the attending physician. After completing the course of treatment, the drug is discontinued by gradually reducing the dose over at least 7 days. Adults and adolescents over the age of 12 years with epilepsy are usually prescribed the drug at an initial dose of 75 mg 2 times a day. A week after the start of therapy, if necessary, the dose of the drug can be increased to 150 mg 2 times a day. Further dose increases, if necessary, are carried out 7 days after the previous dose increase. The maximum daily dose of the drug is 600 mg. The duration of the course of treatment with the drug is determined by the attending physician. For patients taking other anticonvulsants, no dose adjustment of pregabalin is required since the drug does not affect the concentrations and pharmacological effects of other anticonvulsants. Discontinuation of Lyrica should be gradual over a period of at least 7 days. For patients with impaired renal function, the dose of the drug is determined depending on the creatinine clearance: Patients with a creatinine clearance of more than 60 ml/min are usually prescribed the drug at an initial daily dose of 150 mg. The maximum daily dose of the drug is 600 mg. It is recommended to divide the daily dose of the drug into 2 doses. Patients with creatinine clearance from 30 to 60 ml/min are usually prescribed the drug at an initial daily dose of 75 mg. The maximum daily dose of the drug is 300 mg. It is recommended to take the daily dose of the drug at one time or divide it into 2 doses. Patients with a creatinine clearance of 15 to 30 ml/min are usually prescribed the drug at an initial daily dose of 25-50 mg. The maximum daily dose of the drug is 150 mg. It is recommended to take the daily dose of the drug at one time or divide it into 2 doses. Patients with creatinine clearance less than 15 ml/min are usually prescribed the drug at an initial daily dose of 25 mg. The maximum daily dose of the drug is 75 mg. It is recommended to take the daily dose of the drug at one time. For patients suffering from impaired renal function who are on hemodialysis, it is recommended to prescribe an additional dose of Lyrica after a hemodialysis session (since about 50% of the taken dose of pregabalin is removed from the blood plasma during a 4-hour hemodialysis session). Typically, at the beginning of treatment, the additional dose of pregabalin after hemodialysis is 25 mg, but depending on the individual sensitivity of the patient to the drug, the dose can be gradually increased to 100 mg. Patients suffering from impaired liver function do not need dose adjustment of Lyrica. If it is necessary to use the drug in elderly patients, it is recommended to check renal function before starting the use of pregabalin. Elderly patients with normal renal function do not require pregabalin dose adjustment.

Lyrica Test

It was already mentioned above that this drug is not detected by standard urine and blood tests. These tests are designed to detect marijuana, heroin, cocaine and other drugs. It is possible to conduct a chemical and toxicological examination. However, the medicine does not belong to the list of narcotic substances.

Side effects

The use of the drug Lyrica is usually well tolerated by patients, however, in isolated cases, side effects may develop (it is possible that the development of side effects is associated with the course of the underlying disease): From the gastrointestinal tract: appetite disturbances (both increased appetite and anorexia), dry mouth, nausea, vomiting, stool disorders, flatulence. In addition, the development of hypersalivation, oral hypoesthesia and gastroesophageal reflux is possible. In isolated cases, patients experienced the development of pancreatitis, hypoglycemia, ascites and dysphagia. From the cardiovascular system and hematopoietic system: tachycardia, neutropenia, hyperemia and flushing, first degree atrioventricular block, changes in blood pressure. In isolated cases, the development of sinus arrhythmia is possible (the development of both tachycardia and bradycardia was noted). From the central and peripheral nervous system: dizziness, headache, drowsiness, ataxia, decreased attention, impaired coordination, euphoria, increased irritability, confusion. In addition, it is possible to develop a violation of mnestic function, memory loss, tremor, dysarthria, paresthesia, speech impairment, difficulty finding words, anxiety, and depersonalization. Some patients experienced the development of sleep disorders, including insomnia and unusual dreams. When using the drug, patients experienced sudden mood swings, depression, causeless anxiety, hallucinations, apathy, high spirits, psychomotor hyperactivity, hyperesthesia, decreased reflexes, dyskinesia, and the development of an acute anxiety state with a panic reaction. In isolated cases, hypokinesia, diplopia and parsomia may develop. From the senses: impaired taste sensitivity, hyperacusis, visual impairment, including diplopia, dry eyes, decreased visual acuity, lacrimation, asthenopia, eye pain. In isolated cases, the development of photopsia, eye irritation, mydriasis, peripheral vision impairment, oscillopsia and strabismus was noted. From the respiratory system: respiratory failure, dry mucous membranes, cough, rhinitis, nasopharyngitis, snoring. In addition, nosebleeds and a feeling of constriction in the throat may develop. From the musculoskeletal system: muscle fasciculation, cramps, muscle and joint pain, joint swelling, muscle stiffness, pain in the back and limbs. In isolated cases, the development of neck muscle spasm and rhabdomyolysis was noted. From the genitourinary system: decreased amount of urine, development of renal failure, urinary incontinence, erectile dysfunction, ejaculation disorders, amenorrhea, dysmenorrhea, decreased or increased libido, anorgasmia. Allergic reactions: skin rash, itching, urticaria, papular rash. Others: increased sweating, soreness and hypertrophy of the mammary glands, discharge from the mammary glands. When using the drug, there is a change in some laboratory test parameters, including an increase in the activity of hepatic transferases, an increase in the concentrations of creatinine and glucose in the blood, a decrease in the number of platelets and leukocytes in the blood, and hypokalemia.

Clinical picture of overdose

The manifestation of intoxication from capsules directly depends on how many “magic” pills the patient consumed. Also important is the fact in what form the drug was taken and what it was mixed with.

At the initial stage of an overdose, dizziness, cloudiness of consciousness, incoherent speech, fatigue, apathy and drowsiness are observed. Then, as the tablets dissolve and are absorbed into the body, vomiting, nausea, and diarrhea are added to all of the above.

Mental effects Physical consequences
1. Suicidal thoughts Chills, trembling
2. Panic Pathological drowsiness or insomnia
3. Depression Joint pain
4. Manic syndrome Frequent fainting
5. Intellectual and memory disorders Loss of taste bud sensitivity

Patients may notice trembling of the eyeballs, weakness, and loss of reflexes. Also noticeable is the twitching of the limbs, and then a complete loss of stability. During an overdose, patients lose taste and feel a burning sensation in the larynx. Addicts who deliberately exceed the dosage recommended by their doctor can develop diseases of the entire digestive system.

Long-term intoxication is characterized by such signs as excess fluid in the abdominal cavity, decreased tone, cholecystitis, and impaired peristalsis. Due to the large amount of acid in the stomach, the mucous membrane of the esophagus becomes inflamed. In addition, there is pain in the lower back and chills. Drug addicts who have low body resistance to drugs may experience an allergic reaction. You may notice swelling, red spots, and various rashes on the skin. Lyrica has a strong effect on the liver, poisoning it. Thus, the possibility of overdose increases. Not even just once, but several times.

Additional symptoms of increasing the dose include: rapid heartbeat, hypertension, pressure surges, red spots on the face and neck, fever, cold hands and feet. Some drug addicts add ethyl alcohol to Lyrica. After this, when diagnosed by doctors, problems in the functioning of the respiratory system are identified. At first, patients may notice a cough without paying attention to it. But then a feeling of coma and dry throat may appear. If medical assistance is not provided in time, the patient may experience pulmonary edema, convulsions, fainting and, as a result, a coma.

Pregnancy

Due to the lack of reliable data on the safety of the use of pregabalin during pregnancy, Lyrica can only be used under the strict supervision of the attending physician, who, before prescribing the drug, must carefully weigh the expected benefits for the mother and the potential risks for the fetus. Before starting the use of Lyrica, it is recommended to exclude pregnancy; during pregabalin therapy, women are advised to use reliable contraception. Experiments revealed the excretion of pregabalin in rats through breast milk. There is no data on the excretion of the drug in breast milk in humans. If it is necessary to prescribe the drug during lactation, it is recommended to resolve the issue of stopping breastfeeding.

Main signs of using Lyrica

When a person starts taking Lyrica, family and friends may not notice at first. As usually happens, loved ones are the last to know everything and at the last moment. If you notice any changes in behavior, you need to closely monitor the patient. His gait will give him away. It will stagger in different directions, and there will be no smell of alcohol. The addict will sweat profusely and have dilated pupils. Changes can also be observed in a person’s mood; it will fluctuate throughout the day. You can also notice causeless aggression.

Addiction to drugs occurs most quickly in adolescents. Their immunity is quite weak, not fully formed, so vascular permeability is higher than in adults. At this age, an overdose from Lyrica is highly likely. Due to the fact that the drug costs a lot of money, schoolchildren deceive their parents for the next dose. Specialists are even familiar with cases when relatives themselves run to the pharmacy to buy pills. Relatives, trying to alleviate the condition of their child, without knowing it, make it even worse. Many begin to invent various illnesses, forcing their friends to buy another pack of pills.

Lyrica tablets have a fairly narrow therapeutic range. Adults should be aware that in all cases except epilepsy and neurological disorders, the drug will cause an overdose.

Interaction with other drugs

Pregabalin is slightly metabolized in the body and practically does not bind to plasma proteins, so the pharmacokinetic interaction of Lyrica with other drugs is unlikely. When used simultaneously, the drug enhances the effect of ethanol and lorazepam. With the simultaneous use of pregabalin and oxycodone, there is an increase in disturbances in mnestic function and basic motor functions, which are caused by taking oxycodone. The drug does not affect the pharmacological effects of other anticonvulsants, as well as the effectiveness of oral contraceptives, diuretics, oral antidiabetic agents and insulin.

Is it possible to die from Lyrica?

This medicine, at an adequate dosage prescribed by a doctor for the treatment of certain diseases, is not capable of causing death. But drug addicts most often combine Lyrica with other drugs or alcohol, and also do not control the number of pills. In this case, an overdose occurs and the corresponding phenomena are vomiting, diarrhea, confusion and coma.

If a drug addict has heart or kidney problems (and almost 80 percent of drug users have them), then death from an overdose is also possible. It is worth noting that such cases occur when taking Lyrica for a sufficiently long time. The lethal dose of a drug is individual for everyone, it all depends on the duration of use and the condition of the body as a whole.

DOTOXIFICATION

First aid for overdose

Only highly qualified specialists know how to remove the narcotic substance “Lyrica” from the patient’s body. First of all, if you experience symptoms of an overdose, you should call an ambulance. If the patient took the drug with other narcotic substances, then death can be prevented by administering an antidote.

In order to alleviate the drug addict’s condition, it is necessary to put the person on his side, cover him and try to calm him down. Then you need to cleanse the stomach with a potassium solution. The patient should be given strong sweet tea, adsorbents, and enterosorbents.

If necessary, clinic doctors can hospitalize a drug addict. In a specialized institution he will undergo detoxification therapy, vitamins, diuretics, and saline solutions will be used. In case of severe complications of overdose, longer treatment with blood purification procedures will be required.

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