pregabalin | apollo +9191 46 950 950 pregab .pregabalin | apollo +9191 46 950 950 pregabalin |...
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Pregabalin | apollo +9191 46 950 950
Pregabalin | apollo +9191 46 950 950
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
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
Kingdom : Organic
Amino Acids Carboxylic Acids and Derivatives
Substructures Amino Acids
Hydroxy Compounds Acetates
Aliphatic and Aryl Amines Carboxylic Acids and Derivatives
Indication : For management of neuropathic pain associated with diabetic peripheral neuropathy and
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
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
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.
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
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