What is Pregabalin

Pregabalin is a medication that is used for the treatment of epilepsy (brain disorder characterized by recurring seizures), neuropathic pain (pain arising due to damaged nerves), fibromyalgia (condition characterized by muscular or musculoskeletal pain with stiffness and localized tenderness at specific points on the body), and generalized anxiety disorder.

Pregabalin: Structure and chemical information.
                                    Pregabalin: Structure and chemical information.

Pregabalin generic and brand name

  • The drug is mainly available under generic name Pregabalin and commonly marketed by Pfizer under the brand name Lyrica.
  • Pregabalin was originally marketed as Lyrica and is marketed under a number of brand names worldwide (Gabafit, Gabamax, Galinerve, Gabasafe, Maxgalin, Nuramed, Pevesca, pregab, PEGANEX, Pregaba, Progab, Proage etc).
  • No generic version of the drug is available in the United States until recently and the drug is classified as a Schedule V drug.

What is the source of the drug (natural or synthetic)

  • Pregabalin is a synthetic, gamma-aminobutyric acid (GABA) derivative that blocks calcium channels and function as anti-convulsant, anti-epileptic, anxiolytic, and analgesic agent.

Why is Pregabalin prescribed

  • Pregabalin is a anticonvulsants class of drug that works by decreasing the number of pain signals that are sent out by damaged nerves in the body.
  • Pregabalin plays a key role in the management of neuropathic pain caused due to diabetes or shingles (herpes zoster) infection.
  • The drug is also prescribed for treatment of nerve pain arising due to spinal cord injury.
  • It is also recommended for the treatment of fibromyalgia.
  • The drug is indicated in the treatment of Generalised Anxiety Disorder (GAD) in adults.
  • The drug is also indicated as adjunctive therapy for the treatment of partial onset seizures in adults with epilepsy who also take other drugs for seizures.

Pharmacophore structure: Information about the chemical structure of the drug

Pregabalin chemically belongs to the class of organic compounds which are known as  Gamma amino acids and derivatives. These are amino acids containing a (-NH2) group attached to the gamma carbon atom. The detailed chemical classification of Pregabalin is described below:

Kingdom Organic compounds
Super Class Organic acids and derivatives
Class Carboxylic acids and derivatives
Sub Class Amino acids, peptides and analogues
Direct Parent Gamma amino acids and derivatives

 Chemical information of the drug

  • Pregabalin is a derivatives of Gamma-aminobutyric acid derivative (GABA).
  • It is a synthetic Aliphatic acyclic compounds with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activit
  • The molecular weight of the compound is 159.23 g/mol.
  • Pregabalin is chemically known as (S)-3-(aminomethyl)-5-methylhexanoic acid.
  • The molecular formula of the drug is C8H17NO2.
  • Pregabalin is a white to off-white, crystalline solid with dissociation constants pKa1 of 4.2 and a pKa2 of 10.6.
  • It is freely soluble in water (with solubility of 3 mg/mL) and both basic and acidic aqueous solutions.
  • The melting point of Pregabalin is 186-188°C.

Available strength of Pregabalin

  • Pregabalin is available as capsule and oral solution for oral administration.
  • Pregabalin capsules are available in different strengths of 25, 50, 75, 100, 150, 200, 225, and 300 mg and marked with black ink on the cap and body.
  • 25 mg capsule: White, marked “Pfizer” on the cap and “PGN 25” on the body.
  • 50 mg capsule: White, marked “Pfizer” on the cap and “PGN 50” on the body. The body is also marked with a black band.
  • 75 mg capsule: White and orange, marked “Pfizer” on the cap and “PGN 75” on the body.
  • 100 mg capsule: Orange, marked “Pfizer” on the cap and “PGN 100” on the body.
  • 150 mg capsule: White, marked “Pfizer” on the cap and “PGN 150” on the body.
  • 200 mg capsule: Light orange, marked “Pfizer” on the cap and “PGN 200” on the body.
  • 225 mg capsule: White and orange, marked “Pfizer” on the cap and “PGN 225” on the body.
  • 300 mg capsule: White and light orange, marked “Pfizer” on the cap and “PGN 300” on the body.
  • Capsule contains Pregabalin as an active ingredient and lactose monohydrate, cornstarch, and talc as inactive ingredients.
  • The capsule shells consist of gelatin and titanium dioxide. However, the orange capsule shells contain red iron oxide and the white capsule shells consist of colloidal silicon dioxide and sodium lauryl sulfate.
  • Colloidal silicon dioxide which acts as a manufacturing aid may or may not be present in the capsule shells.
  • The ink that is used for imprinting consists of propylene glycol, shellac, potassium hydroxide, and black iron oxide.
  • Pregabalin oral solution is available in strength of 20 mg/mL as a clear, colorless solution in a white HDPE bottle with a polyethylene-lined closure.
  • The oral solution contains Pregabalin as an active ingredient, while propylparaben, sucralose, dibasic sodium phosphate anhydrous, monobasic sodium phosphate anhydrous, artificial strawberry #11545, methylparaben and purified water as inactive ingredients.

How does Pregabalin work (mode of action)

  • The exact mechanism of action of Pregabalin remains unclear and the proposed mechanism is based upon results involving genetically modified mice and compounds that are structurally related to the drug such as gabapentin.
  • The drug causes a decrease in the excitability of the neurons in the central nervous system by binding to the auxiliary subunit (α2-δ protein) of a voltage-gated calcium channel present on the neurons of the central nervous system.
  • Pregabalin causes a decrease of pro-nociceptive neurotransmitters (a calcium dependent process) in the spinal cord either by reduction of calcium currents or disruption of alpha2-delta containing-calcium channel trafficking.
  • These neurotransmitters are involved in the noradrenergic and serotonergic pathways that cause modulation of pain transmission in the spinal cord.
  • Besides this, Pregabalin also lowers the release of several other neurotransmitters, including glutamate, noradrenaline, and substance P possibly by modulation of calcium channel function. However, the significance of this effect remains unclear.
  • Although Pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors.
  • The sodium channels, opiate receptors, and cyclooxygenase enzymes do not play a role in the mechanism of action of Pregabalin.
  • The drug is also inactive at serotonin and dopamine receptors and does not inhibit reuptake of the serotonin, dopamine, or noradrenaline.

Recommended doses of Pregabalin

  • The dose of the drug Pregabalin varies among different patients.
  • The dose of the drug is dependent on its strength.
  • Besides, the number of doses per day, the time between doses, and the duration of the intake of medicine depend on the medical complication.
  • For oral dosage forms (in form of capsules and solution):
    • Diabetic nerve pain:
      • Adults—Initially, 50 milligrams (mg) thrice a day.Later, the dose may be adjusted by the doctor as needed. However, the dose should never exceed more than 300 mg per day.
      • Children—the dosage and usage is as directed by the doctor.
    • Spinal cord injury nerve pain:
      • Adults—Initially, 75 milligrams (mg) twice a day. Later, the dose may be adjusted by the doctor as needed. However, the dose should never exceed more than 600 mg per day.
      • Children— the dosage and usage is as directed by the doctor.
    • Postherpetic neuralgia:
      • Adults—Initially, 75 to 150 milligrams (mg) twice a day, or 50 to 100 mg thrice a day. Later, the dose may be adjusted by the doctor as needed. However, the dose should never exceed more than 600 mg per day.
      • Children— the dosage and usage is as directed by the doctor.
    • Epilepsy:
      • Adults—Initially, 75 milligrams (mg) twice a day or 50 mg thrice a day. Later, the dose may be adjusted by the doctor as needed. However, the dose should never exceed more than 600 mg per day.
      • Children— the dosage and usage is as directed by the doctor.
    • Fibromyalgia:
      • Adults—Initially, 75 milligrams (mg) twice a day. Later, the dose may be adjusted by the doctor as needed. However, the dose should never exceed more than 450 mg per day.
      • Children— the dosage and usage is as directed by the doctor.
    • Postherpetic neuralgia:
      • Adults—Initially, 75 to 150 milligrams (mg) twice a day, or 50 to 100 mg thrice a day. Later, the dose may be adjusted by the doctor as needed. However, the dose should never exceed more than 600 mg per day.
      • Children— the dosage and usage is as directed by the doctor.
Pregabalin Uses
                                                                                            Pregabalin prescriptions

When should I discontinue, withhold or modify the dose of Pregabalin

  • The usual dosing of the drug may vary depending upon the efficiency and side effects of the drug in a particular individual.
  • Do not use the medicine if you are hypersensitive or allergic to Pregabalin or any of its ingredients.
  • Pregabalin dose is usually modified under the supervision of doctor if you are taking any of the following antidepressants; tranquilizers; certain medications for diabetes; sedatives; antihistamines; narcotic pain medications; sleeping pills; medications for anxiety; medications for mental illness or seizures; and angiotensin converting enzyme (ACE) inhibitors.
  • Pregabalin use is contraindicated in children below the age of 18 years.
  • In case of patients with renal impairment specific recommendations and dosing of Pregabalin should be adjusted accordingly, since the drug is primarily eliminated through  the kidney.
  • Consult with your doctor and pharmacist if you are taking any prescription and non-prescription medications, herbal products, nutritional supplements or vitamins.
  • In elderly population dose of Pregabalin should be lowered to decrease the possibility side effects.
  • The dose of the drug is usually modified in case of diabetes; congestive heart failure;

low levels of blood platelets; bleeding disorder; depression; drug or alcohol addiction; or allergies.

What are the pharmacokinetic properties of the drug

  • Pharmacokinetic studies suggested that after oral administration, Pregabalin is rapidly absorbed and has oral bio-availability of >90%.
  • The drug does not bind to plasma proteins.
  • The apparent volume of distribution of the drug is approximately
  • It has been observed that after oral administration under fasting conditions, maximum (or peak) plasma concentration is achieved with in 4-5 hours.
  • The drug is metabolized in the humans in negligible concentration.
  • The average median half-life of Pregabalin is 3 hours.
  • The average steady state volume of distribution of the drug is 5L/Kg after oral administration.
  • The drug is primarily (approximately 90%) eliminated by renal system as unchanged drug in the urine. The N-methylated derivative of Pregabalin (major metabolite) accounts for 0.9% in the urine.

Which pregnancy category (A; B; C; D; X) has been assigned to Pregabalin

  • The Pregabalin is classified by US FDA pregnancy category: C
  • The use of Pregabalin in pregnant women should be initiated or stopped only under the supervision of doctor.
  • Studies in animals suggest an increase in the incidence of fetal structural abnormalities and developmental toxicity (growth retardation, lethality, functional impairment in reproductive and nervous system).
  • No controlled studies have been performed in case of human pregnancy and hence Pregabalin should only be administered during pregnancy when other alternatives are absent or benefit outweighs risk.
  • Studies indicate that Pregabalin crosses the placenta and shows an increased risk in male-mediated teratogenicity.
  • Studies are lacking regarding the excretion of the Pregabalin into breast milk as well as its effect on nursing babies. Therefore, breast-feeding is not recommended.
  • Despite these facts caution should be exercised when taking Pregabalin.

How to use Pregabalin

  • Pregabalin is available in capsule and solution form for oral administration.
  • The drug can be taken either with or without food twice or thrice a day.
  • It is also recommended to take drug at almost the same time every day.
  • Follow the instructions carefully as directed on prescription leaflet and take Pregabalin exactly as directed.
  • Do not change the dose of the drug as prescribed by your doctor since the dosage is based on patient medical condition, treatment responses and usage with other drugs.
  • The drug is usually initiated at a lower dose which may then be increased gradually during the first week of treatment under the prescription of the doctor
  • Do not take more or less amount of the drug or during shorter or longer time then prescribed.
  • Stopping Pregabalin abruptly may cause withdrawl symptoms including nausea, seizures, trouble falling asleep or staying asleep, diarrhea, or headaches.
  • Continue using Pregabalin even if you feel well for the prescribed time as directed by the doctor.
  • Do not stop talking the drug unless your doctor asks you to do so as it may result in side effects
  • If you have any queries about the drug immediately consult to your doctor to get information regarding any part you do not understand.
  • Do not share Pregabalin with any other person, even if they have the same symptoms as you have.
  • It is recommended to inform the doctor or dentist before you start with any medical, dental, emergency care or undergo any type of surgery.

How to store the drug

  • Pregabalin is stored at room temperature 15-30°C (59-86°F) in its original packing.
  • The drug should be kept away from children and pets.
  • Medicine should not be stored in the bathroom.
  • Store the medicine at room temperature away from moisture, heat, and light.

How to dispose expired Pregabalin

  • Throw away unused and opened, outdated or no longer used container.
  • Also dispose the old medicine after the expiration date.
  • Oral solution containing visible particulates should not be used.

Does Pregabalin has approval from government / FDA /or any other related agencies

  • The drug Pregabalin got approval from European Union in 2004 for the treatment of peripheral neuropathic pain and as a therapy for partial seizures in patients with epilepsy.
  • Pregabalin got approval from US Food and Drug Administration (FDA) in December 2004 to treat diabetic neuropathic pain, epilepsy, and postherpetic neuralgia.
  • The drug came into U.S. market in fall 2005.
  • The drug Lyrica (Pregabalin) was approved by FDA in June 2007 for the treatment of fibromyalgia and was the first drug to be approved for this indication.
  • Pregabalin was approved by the EU in 2007 for treatment of generalized anxiety disorder.
  • The generic versions of the drug came into existence in Russia (2011) and Canada (2013).

Other uses of the drug

  • Pregabalin may also be used for other uses not listed here. It is advisable to ask your doctor or pharmacist for more information.

What special dietary precautions should I follow

  • Take diet as prescribed by your doctor otherwise follow usual diet.
  • Avoid consumption of alcohol during administration of Pregabalin as it may augment the nervous system side effects associated with the drug including drowsiness, dizziness, impairment in thinking and judgment, and difficulty concentrating.

What special precautions should I follow/ What should I avoid while using Pregabalin

  • Before taking Pregabalin, tell your doctor about your medical history or any type of allergy.
  • Consult with your doctor and pharmacist if you are taking any prescription and non-prescription medications, vitamins, herbal products or nutritional supplements.
  • It is recommended to avoid the use of alcohol while taking Pregabalin as alcohol leads to an increase in the drowsiness which is often associated with the use of this drug.
  • It is advisable to avoid driving, operating machines or doing dangerous activities while you take Pregabalin.
  • Discuss with your doctor or dentist about your consumption of Pregabalin if you are having surgery, including dental surgery.
  • It is recommended to complete the entire course of the drug (full prescribed length of time) even if the symptoms improve before the infection is completely cleared.
  • Do not stop taking Pregabalin until you do not finish the prescription as it lead to the development of withdrawl symptoms such as diarrhea, headaches, trouble falling asleep or staying asleep, seizures, or nausea.
  • Take medical advice about the use of Pregabalin during pregnancy and breastfeeding.
  • It is recommended for the male partners to consult with the physician or doctor if they plan for a child while taking Pregabalin as the drug has shown decreased fertility in male animals and also birth defects in the offspring of male and female when treated with drug.
  • It is recommended to avoid the use of the drug in children who are below 18 years.

Pregabalin side effects

In addition to the associated benefits, Pregabalin may put forth undesirable side effects that require medical attention. These effects fall in various categories: more common, less common or those that fade away with time during drug intake as the body gets acclimatized to the medicine. It is always recommended to consult a doctor if you encounter any of the side effects or when the side effects continue for a longer duration.

Some of the commonly occurring side effects but requiring medical attention are outlined as:

  • Dizziness
  • Gas or bloating
  • Tiredness
  • Dry mouth
  • Nausea or vomiting
  • Lack of coordination
  • Constipation
  • High or elevated mood
  • Speech problems
  • Weight gain
  • Weakness
  • Trouble concentrating
  • Headache
  • Muscle twitching
  • Anxiety
  • Confusion
  • Memory problems
  • Back pain
  • Increased appetite
  • Loss of balance
  • Uncontrollable shaking of a part of the body
  • Swelling of the feet, ankles, arms, hands, or lower legs

Serious side effects can also be encountered in some cases. It is advisable to stop the intake of the drug in such circumstances and consult your doctor. These include:

  • Blisters
  • Rash or hives
  • Blurred or double vision, or other changes in your eyesight
  • Itching
  • Swelling of the eyes, throat, tongue, face, lips, mouth, gums, head or neck
  • Shortness of breath
  • Wheezing
  • Muscle pain, weakness , or soreness
  • Chest pain

The consumption of Pregabalin may also elicit mental health problems in certain circumstances. Doctor should be contacted if you encounter any of these symptoms:

  • Agitation
  • Anxiety
  • Acting on dangerous impulses
  • Withdrawal from friends and family
  • Abnormally excited mood
  • Depression
  • Panic attacks
  • Restlessness
  • Aggressive or violent behavior
  • Irritability
  • Suicidal actions or thoughts

Besides these, Pregabalin may also be associated with some other side effects. These include:

  • Nervous system side effects: ataxia, neuropathy, dizziness, tremor, confusion, speech disorder, abnormal thinking, incoordination, twitching, and nervousness
    • Frequently occurring- anxiety, hypertonia, depersonalization, paresthesia, hypesthesia, stupor, twitching, and nystagmus.
    • Infrequently occurring– hypokinesia, agitation, hyperesthesia, hostility, hallucinations, abnormal dreams, apathy, aphasia, hyperkinesia, dysarthria, hyperalgesia, hypotonia, and neuralgia.
    • Rarely occurring coma, hypoalgesia, dyskinesia, encephalopathy, delusions, Guillain-Barre syndrome, peripheral neuritis, psychotic depression, addiction, delirium, manic reaction, intracranial hypertension, cerebellar syndrome, dystonia, trismus, and schizophrenic reaction, paranoid reaction.
  • Metabolic side effects: hypoglycaemia, weight gain, edema, and peripheral edema, Rarely occurring- urate crystalluria and decreased glucose tolerance.
  • Gastrointestinal side effects: constipation, dry mouth, diarrhea, vomiting, nausea flatulence, and increased appetite.
    • Frequently occurring– gastroenteritis.
    • Infrequently occurring– colitis, tongue edema, cholecystitis, esophagitis, gastrointestinal hemorrhage, gastritis, dysphagia, mouth ulceration, pancreatitis, and rectal hemorrhage.
    • Rarely occurring- esophageal ulcer and aphthous stomatitis.
  • General side effects: accidental injury, infection, pain, chest pain, facial edema, flu syndrome, headache, and back pain.
    • Frequently occurring– fever and abdominal pain
    • Infrequently occurring– cellulitis, abscess, neck rigidity, pelvic pain, photosensitivity, chills, and suicide attempt.
    • Rarely occurring- intentional injury, ascites, shock, hangover, retroperitoneal fibrosis, granuloma, and suicide.
  • Ocular side effects: blurred vision, reduced visual acuity, and visual field changes. Frequently occurring– diplopia and conjunctivitis.
    • Infrequently occurring– dry eyes, accommodation abnormality, retinal vascular disorder, eye hemorrhage, photophobia, and retinal edema.
    • Rarely occurring- blindness, parosmia, iritis, night blindness, keratoconjunctivitis, papilledema, corneal ulcer, extraocular palsy, uveitis, keratitis, miosis, ophthalmoplegia, optic, ptosis, and atrophy.
  • Other side effects:
    • Frequently occurring– tinnitus, weight gain, and Otitis media.
    • Infrequently occurring– taste loss, and taste perversions.
  • Cardiovascular side effects: edema, primarily peripheral edema.
    •  Infrequently occurring– heart failure, postural hypotension, deep thrombophlebitis, syncope, and hypotension.
    • Rarely occurring- depressed ST and ventricular fibrillation.
  • Respiratory side effects: bronchitis and dyspnea.
    • Rarely occurring- bronchiolitis, apnea, yawn, hiccup, lung edema, lung fibrosis, and laryngismus.
  • Genitourinary side effects: urinary incontinence.
    • Frequently occurring– anorgasmia, impotence, and urinary frequency.
    • Infrequently occurring– kidney calculus, nephritis, metrorrhagia, albuminuria, dysuria, abnormal ejaculation, urinary retention, hematuria, menorrhagia, leukorrhea, and oliguria.
    • Rarely occurring- female lactation, bladder neoplasm, acute kidney failure, epididymitis, cervicitis, dyspareunia, and glomerulitis.
  • Musculoskeletal side effects: myasthenia.
    • Frequently occurring– leg cramps, arthralgia, myalgia, and myasthenia.
    • Infrequently occurring– arthrosis.
    • Rarely occurring- generalized spasm.
  • Oncologic side effects: hemangiosarcoma.
  • Hypersensitivity side effects:
    • Frequently occurring– allergic reactions (blisters, wheezing, rash, hives, dyspnea, and skin redness).
    • Rarely occurring- anaphylactoid reactions.
  • Hematologic side effects:
    • Frequently occurring– ecchymosis.
    • Infrequently occurring– eosinophilia, thrombocytopenia, lymphadenopathy, leukopenia, anemia, leukocytosis, and hyperchromic anemia.
    • Rarely occurring- purpura, thrombocytopenia, polycythemia, myelofibrosis, and decreased prothrombin.
  • Dermatologic side effects:
    • Frequently occurring– pruritus.
    • Infrequently occurring– alopecia, skin ulcer, vesiculobullous eczema, urticaria, and dry skin rash.
    • Rarely occurring- skin necrosis, angioedema, subcutaneous nodule, Stevens-Johnson syndrome, skin atrophy, lichenoid dermatitis, melanosis, exfoliative dermatitis, pustular rash, and skin nodule.

What should I do in case of overdose

  • Try to avoid taking the overdose of the drug. If you overdose the drug contact with your doctor or pharmacist for symptomatic and supportive measures including monitoring of vital signs and observation of the clinical status of the patient.
  • No specific antidote exists for the overdose of the drug and hence, elimination of unabsorbed drug should be attempted by emesis or gastric lavage.
  • Take precautions to maintain the airways.
  • Hemodialysis may be recommended depending upon patient’s clinical state or in patients with significant renal impairment.
  • In case you or some other person has taken overdose of this medication contact your local poison control center at 1-800-222-1222 or emergency room immediately.

What should I do in case of missed a dose

  • In case of missed dosage, take it as soon as you remember and maintain a regular dosing schedule.
  • Skip the missed dose if it is almost time for your next scheduled dose.
  • Keep in mind to not use a double dose to make up a missed dose.

Pregabalin drug interactions

Pregabalin may interact with one of the following drugs. Care should be taken when you are taking these medications together. It is advisable that you do not start, stop or change the medication by your own and without professional consult.

  • Heart medications, including angiotensin converting enzyme (ACE) inhibitors such as benazepril (Lotensin, Lotrel), captopril (Capoten, Capozide), and enalapril (Vasotec, iVaseretic, Lexxel): these medications may result in an increased risk of development of angioedema.
  • Gabapentine: Pregabalin and Gabapentin coadministration requires decrease in dosing of both the drugs so as to lower the associated side effects. The pharmacokinetics of Gabapentin remains unchanged upon single- and multiple-dose administration in presence of Pregabalin. The level of Pregabalin absorption remains unaltered with a small decrease in the rate of absorption when coadministered with Gabapentin.
  • Antidiabetic drugs: Coadministration of Pregabalin and antidiabetic drugs such as pioglitazone (Actos, Duetact) and rosiglitazone (Avandia, Avandamet, Avandaryl) belonging to the thiazolidinedione class result in weight gain and/or fluid retention, thereby either worsening or leading to heart failure. It is therefore advised to exercise caution when these drugs are concomitantly administered.
  • Antiepileptic drugs: The pharmacokinetics of the drug Pregabalin and antiepileptic drugs such as valproic acid, carbamazepinephenytoin, topiramate, phenobarbital, and, lamotrigine or commonly used antiepileptic drugs remains unchanged when these drugs are coadministered. However, coadministration of antiepileptic drugs and Pregabalin should be cautiously monitored for increase in suicidal thoughts or behavior.
  • Antidepressants: The serotonergic effects associated with Pregabalin enable it to fatally interact with other serotonergics such as antidepressants (including serotonin-norepinephrine reuptake inhibitors, tricyclic antidepressants, monoamine oxidase inhibitors, selective serotonin reuptake inhibitors, noradrenergic and specific serotonergic antidepressants, serotonin antagonists, etc.).
  • Oral Contraceptive: Pregabalin does not affect the oral contraceptives such as norethindrone and ethinyl estradiol.
  • Monoamine oxidase inhibitors or MAO-B inhibitor (e.g., Selegiline): These are chemicals which inhibit the activity of the monoamine oxidase enzyme family and classically used to treat depression. MAO-B acts through increasing the levels of dopamine and norepinephrine. Pregabalin is a general CNS depressant, that affects GABA, glutamate, norepinephrine, and substance P, via its effect on calcium ion channels. Coadministration of these drugs results in a perfectly safe interaction.
Pregabalin drug interaction
                                                                                                             Pregabalin drug interaction

Other drugs that interact with Pregabalin and augments the side effects such as dizziness or sleepiness associated with Pregabalin includes

  • Cold or allergy medicine
  • Sedatives or sleeping pills,
  • Muscle relaxants like baclofen, and
  • Tranquilizers or drugs used to treat anxiety, including lorazepam (Ativan)
  • Narcotic pain medications, including oxycodone (OxyContin, Percocet), Morphine and Codeine: these medicines in combination with Pregabalin may also result in the increased chances of constipation.

This is not a complete list of drugs that interact with Pregabalin. Tell your doctor about all medications you take including prescription, over the counter, vitamin, nutritional supplements and herbal products etc. Never start a new medication without consulting your doctor.

Does Pregabalin have any interaction with diseases

Pregabalin may interact with one or more than one of the following disease conditions.

  • Diabetes: Pregabalin use may be associated with an increased risk of skin ulceration in the diabetic patients and hence they should be watched for skin damage while on Pregabalin therapy. Besides Coadministration of Pregabalin and antidiabetic drugs may also cause an increase in weight gain and fluid retention. The dose of the drug should therefore be adjusted accordingly.
  • Angioedema (characterized by swelling of face, mouth and neck): Pregabalin should be administered cautiously in patients who have earlier had angioedema or who are taking other drugs associated with angioedema as Pregabalin use may increase the risk of development of angioedema in these patients.
  • Hypersensitivity: Pregabalin should be administered with caution in patients who are hypersensitive to the drug or any of its constituents.
  • Rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption: Since the drug consists of lactose, its use is not recommended in these people.
  • Renal impairment: The drug Pregabalin is primarily eliminated by the renal system. The risk of toxic reactions to the drug is likely to increase in patients with impaired renal function The dose of the drug should therefore be adjusted in patients with decreased renal function including geriatric population.
  • Seizures disorders: Pregabalin is associated with increased frequency of seizures in patients with seizures disorders. The drug should therefore be withdrawn gradually in these patients in order to decrease this frequency of seizures.
  • Congestive heart failure: Due to scarcity of data on congestive heart failure patients with New York Heart Association (NYHA) Class III or IV cardiac status, the drug should be administered very cautiously in these patients.
  • Elderly population: Pregabalin clearance tends to get decreased with increasing age consistent with age-related decreases in creatinine clearance. The dose of the drug should therefore be adjusted in patients with age-related compromised renal function.

Where can I get more information

Your pharmacist or health care provider can provide more information about Pregabalin.

Clinical research and current scenario of the drug

  • Clinical studies indicate an increase in the level of serum creatinine kinase (CK, creatine phosphokinase, CPK) at least 3 times the upper limit of normal in 2 or 1% of patients receiving the drug Pregabalin or placebo, respectively.
  • Controlled clinical trials suggest potentially clinically important decreases in platelet count (thrombocytopenia; which is defined as 20% below baseline level and less than 150,000/cu m) in 3 or 2% of patients receiving the drug Pregabalin or placebo, respectively.
  • Randomized clinical experiments indicate that Pregabalin is not associated with an increase in bleeding related adverse effects.
  • Studies suggest a mild prolongation of the PR interval (mean increase; 3-6 msec) in patients who receive Pregabalin dosages of at least 300 mg daily.
  • Studies indicate the development of Edema (mainly peripheral edema) in patients receiving Pregabalin.
  • Clinical studies indicate an increase in weight gain depending upon dosage and duration of exposure to Pregabalin in patients who are administered Pregabalin. The increase in weight was not associated with gender, baseline body mass index (BMI), or age and was not limited to patients with edema.
  • Studies indicated that blurred vision in 6 or 2% of patients who were administered Pregabalin or placebo, respectively, got resolved in the majority of cases with continued dosing; with less than 1% of patients requiring discontinuance of the drug.
  • Preclinical studies in animals (rat) treated with Pregabalin indicate an increased risk of male-mediated teratogenicity.
  • In vitro and in vivo studies in bacteria or mammalian systems indicate Pregabalin to be nonmutagenic and nonclastogenic and did not induce unscheduled DNA synthesis in mouse or rat hepatocytes.
  • Studies suggest improvement of postoperative analgesia by Pregabalin compared with placebo at the expense of visual disturbances and sedation.

References from chemical, biological and toxicological databases

  • DrugBank: Pregabalin.
  • Pregabalin: MedlinePlus Drug Information.
  • Pregabalin | C8H17NO2 – PubChem.
  • Wikipedia.
  • Pregabalin | C8H17NO2 | ChemSpider. 4589156.html
  • Lyrica medication guide – U.S. Food and Drug Administrat
  • Clinical utility, safety, and efficacy of pregabalin in the treatment of fibromyalgia.
  • Efficacy and safety of pregabalin in generalised anxiety disorder: A critical review of the literature.
  • Diabetic neuropathic pain: Physiopathology and treatment.
  • Pregabalin for painful diabetic peripheral neuropathy: strategies for dosing, monotherapy vs. combination therapy, treatment-refractory patients, and adverse events.
  • Management of chronic spinal cord dysfunction.
  • Pregabalin for the treatment of social anxiety disorder.
  • Impact of pregabalin on acute and persistent postoperative pain: a systematic review and meta-analysis.
  • Pregabalin: a review of its use in adults with generalized anxiety disorder.
  • Pregabalin: latest safety evidence and clinical implications for the management of neuropathic pain.
  • Pregabalin’s abuse potential: a mini review focusing on the pharmacological profile.
  • Pregabalin add-on for drug-resistant partial epilepsy.
  • Pregabalin as a probable cause of thrombocytopenia: presentation of two clinical cases and review of literature.

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About Dr. Manish Goyal 38 Articles
Manish Goyal, obtained his Bachelor of Science degree in Biology from Rajasthan University in 2002. In 2005 he was granted a Master of Science in Biology from the same institution. In 2007, he has joined the Department of Infectious Diseases and Immunology, CSIR-Indian Institute of Chemical Biology where he has completed his doctoral studies. The focus of his research is on infectious disease, using excellent cutting edge tools of protein biochemistry, molecular biology and cell biology. Manish is the recipient of multiple awards including, D. P. Burma Best Poster Awards in 81st Annual meeting of Society of Biological Chemist, Receipt of the Ranbaxy Science Foundation Young research scholar award 2012 in the field of biomedical science, and INSPIRE young faculty award by Department of Science and Technology, Govt. of India.