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  • Pregabalin | apollo +9191 46 950 950

    Pregabalin | apollo +9191 46 950 950

    Pregabalin

    CAS Number : 148553-50-8

    Molecular Formula : C8H17NO2 Molecular Weight : 159.226 g/mol

    Systematic (IUPAC) : (3S)-3-(aminomethyl)-5- methylhexanoic acid

    Type : small molecule

    Description

    Pregabalin is an anticonvulsant drug used for neuropathic pain, as an adjunct therapy for partial seizures, and in generalized anxiety disorder. It was

  • designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade name Lyrica. It is considered to have a dependence liability if misused, and is classified as a Schedule V drug in the

    U.S.

    Categories Anticonvulsants

    Analgesics

    Taxonomy

    Kingdom : Organic

    Classes

    Amino Acids Carboxylic Acids and Derivatives

    Substructures Amino Acids

    Hydroxy Compounds Acetates

    Aliphatic and Aryl Amines Carboxylic Acids and Derivatives

    Pharmacology

    Indication : For management of neuropathic pain associated with diabetic peripheral neuropathy and

    postherpetic neuralgia.

  • Pharmacodynamics : Pregabalin is a new anticonvulsant drug indicated as an add on therapy for

    partial onset seizures and for certain types of neuropathic pain. It was designed as a more potent successor to a related drug, gabapentin. Pregabalin

    binds to the alpha2-delta subunit of the voltage-gated calcium channel in the central nervous system. While pregabalin is a structural derivative of the inhibitory

    neurotransmitter gamma- aminobutyric acid (GABA), it does not bind directly to GABAA, GABAB, or

    benzodiazepine receptors, does not augment GABAA responses in cultured neurons, does not alter rat brain GABA concentration or have acute effects on GABA uptake or degradation. However, in cultured neurons prolonged application of pregabalin increases the

    density of GABA transporter protein and increases the rate of functional GABA transport. Pregabalin does not block sodium channels, is not active at opiate receptors, and does not alter cyclooxygenase enzyme activity. It is inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline

    reuptake.

    Mechanism of action : Pregabalin binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. Although the mechanism of action of

    pregabalin is unknown, results with genetically modified mice and with compounds structurally related to

    pregabalin (such as gabapentin) suggest that binding to the alpha2-delta subunit may be involved in pregabalins antinociceptive and antiseizure effects in animal models.

    In vitro, pregabalin reduces the calcium-dependent

  • release of several neurotransmitters, possibly by modulation of calcium channel function.

    Absorption : Well absorbed after oral administration.

    Volume of distribution : 0.5 L/kg

    Metabolism : Negligible

    Route of elimination : Pregabalin is eliminated from the systemic circulation primarily by renal excretion as

    unchanged drug.

    Half life : ~6 hours

    Clearance : Renal cl=67.0 80.9 mL/min

    Affected organisms : Humans and other mammals

    Drug Class And Mechanisms

    Pregabalin is an oral medication that is chemically related to gabapentin (Neurontin, Gabarone). It is used for treating pain caused by neurologic diseases such as postherpetic neuralgia as well as seizures. It also is used for treating fibromyalgia. The mechanism of action of pregabalin is unknown. Pregabalin binds to calcium channels on nerves and may modify the release of neurotransmitters (chemicals that nerves use to

    communicate with each other). Reducing communication between nerves may contribute to

  • pregabalin's effect on pain and seizures. The FDA approved pregabalin in December 2004.

    Dosing

    Pregabalin may be taken with or without food. The initial dose for neuropathic pain is 50 mg three times a day (150 mg/day). The dose may be increased to a

    maximum dose of 100 mg 3 times daily (300 mg/day) after one week.

    The recommended dose for postherpetic neuralgia is 75-150 mg twice daily or 50-100 mg three times daily. Begin dosing at 75 mg two times a day or 50 mg three times a day (150 mg/day). The dose may be increased to 100 mg 3 times daily (300 mg/day) after one week. If pain relief

    is inadequate after 2-4 weeks of treatment at 300 mg/day, the dose may be increased to 300 mg twice daily or 200 mg three times daily. Doses greater than

    300 mg cause more side effects. The recommended dose for treating seizures is 150-600 mg/day divided into 2 or 3 doses, starting at at 150 mg daily and increasing based on response and tolerability. Fibromyalgia is treated with 300-450 mg/day in 2 or 3

    divided doses.

    Drug interactions

    Alcohol and drugs that cause sedation may increase the sedative effects of pregabalin. Pioglitazone (Actos) and

    rosiglitazone (Avandia) cause weight gain, fluid retention and possibly heart failure. Therefore,

    combining pregabalin with these drugs may increase the occurrence of weight gain and fluid retention.

  • Why is this medication prescribed? Pregabalin is used to relieve neuropathic pain (pain from damaged nerves) that can occur in your arms,

    hands, fingers, legs, feet, or toes if you have diabetes or in the area of your rash if you have had shingles (a painful rash that occurs after infection with herpes zoster). It is also used to treat fibromyalgia (a long-

    lasting condition that may cause pain, muscle stiffness and tenderness, tiredness, and difficulty falling asleep or

    staying asleep). Pregabalin is used with other medications to treat certain types of seizures in people with epilepsy. Pregabalin is in a class of medications called anticonvulsants. It works by decreasing the

    number of pain signals that are sent out by damaged nerves in the body.

    How should this medicine be used?

    Pregabalin comes as a capsule to take by mouth. It is usually taken with or without food two or three times a day. Take pregabalin at around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain

    any part you do not understand. Your doctor will probably start you on a low dose of

    pregabalin and may gradually increase your dose during the first week of treatment.

    Take pregabalin exactly as directed. Pregabalin may be habit forming. Do not take a larger dose, take it more

    often, or take it for a longer period of time than prescribed by your doctor.

    Pregabalin may help control your symptoms but will not cure your condition. It may take several weeks or longer before you feel the full benefit of pregabalin. Continue to

  • take pregabalin even if you feel well. Do not stop taking pregabalin without talking to your doctor, even if you experience side effects such as unusual changes in behavior or mood. If you suddenly stop taking

    pregabalin, you may experience withdrawal symptoms, including trouble falling asleep or staying asleep,

    nausea, diarrhea, headaches, or seizures. Your doctor will probably decrease your dose gradually over at least

    one week. Your doctor or pharmacist will give you the

    manufacturer's patient information sheet (Medication Guide) when you begin treatment with pregabalin and

    each time you refill your prescription. Read the information carefully and ask your doctor or pharmacist if you have any questions. You can also visit the Food

    and Drug Administration (FDA) website

    Other uses for this medicine

    This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

    What special precautions should I follow?

    Before taking pregabalin, tell your doctor and pharmacist if you are allergic to pregabalin, any other medications, or any of the

    ingredients in pregabalin capsules. Ask your pharmacist for a list of the ingredients.

    tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan

    to take. Be sure to mention any of the following: angiotensin converting enzyme (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), captopril (Capoten, in

  • Capozide), enalapril (Vasotec, in Vaseretic, Lexxel), fosinopril (Monopril), lisinopril (Prinivil, Zestril, in

    Prinzide, Zestoretic), moexipril (Univasc, in Uniretic), perindopril (Aceon), quinapril (Accupril, in Accuretic, Quinaretic), ramipril (Altace), and trandolapril (Mavik, in Tarka); antidepressants; antihistamines; medications for anxiety, including lorazepam (Ativan); medications for mental illness or seizures; certain medications for diabetes such as pioglitazone (Actos, in Duetact) and rosiglitazone (Avandia, in Avandaryl, Avandamet); narcotic pain medications, including oxycodone

    (OxyContin, in Percocet, others); sedatives; sleeping pills; and tranquilizers. Your doctor may need to change the doses of your medications or monitor you carefully

    for side effects. tell your doctor if you drink or have ever drunk large amounts of alcohol, use or have ever used street drugs, or have overused prescription medications. Also tell

    your doctor if you have or have ever had swelling of the eyes, face, lips, tongue, or throat; problems with your vision, bleeding problems or a low number of platelets (type of blood cell needed for blood clotting) in your

    blood, or heart or kidney disease. tell

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