Pygaba 75

Pygaba 75

pregabalin

Manufacturer:

MacroPhar

Distributor:

MacroPhar Lab
Full Prescribing Info
Contents
Pregabalin.
Description
Each capsule contains 75 mg of pregabalin.
Action
ATC code: N03AX16.
Pharmacology: Pharmacodynamics: Pregabalin is an antiepileptic, a gamma-aminobutyric acid analogue ((s)-3-(aminomethyl)-5-methylhaxanoic acid).
Mechanism of action: Pregabalin binds to an auxiliary subunit (α2-ẟ protein) of voltage-gated calcium channels in the central nervous system.
Pharmacokinetics: Absorption: Pregabalin is rapidly absorbed after oral doses and peak plasma concentrations occur within 1.5 hours. Oral bioavailability is about 90%. The rate but not the extent absorption is reduced if given with food but this is not clinically significant. Steady state is achieved after 1 to 2 days.
Distribution: In humans, the apparent volume of distribution of pregabalin following oral administration is approximately 0.5 L/kg. Pregabalin is not bound to plasma proteins.
Metabolism: Pregabalin undergoes negligible metabolism in humans.
Excretion: Pregabalin is eliminated by renal excretion 90% as unchanged drug. The mean elimination half-life is 6.3 hours. Pregabalin is removed by hemodialysis.
Indications/Uses
Treatment of central and peripheral neuropathic pain in adults which includes diabetic peripheral neuropathy and post-herpetic neuralgia.
As adjunctive therapy in adults with partial seizures with or without secondary generalization.
Treatment of Generalized Anxiety Disorder (GAD) in adults.
Management of fibromyalgia.
Dosage/Direction for Use
The dose range is 150 to 600 mg per day given orally in 2 or 3 divided doses.
Neuropathic pain: Pregabalin treatment can be started at a dose of 150 mg per day. Based on individual patient response and tolerability, the dosage may be increased to 300 mg per day after an interval of 3 to 7 days, and if needed, to a maximum dose of 600 mg per day after an additional 7-day interval.
Epilepsy: Pregabalin treatment can be started with a dose of 150 mg per day. Based on individual patient response and tolerability, the dosage may be increased to 300 mg per day after 1 week. The maximum dosage of 600 mg per day may be achieved after an additional week.
Generalized Anxiety Disorder: The dosage range is 150 to 600 mg per day given as two or three divided doses. The need for treatment should be reassessed regularly.
Pregabalin treatment can be started with a dose of 150 mg per day. Based on individual patient response and tolerability, the dosage may be increased to 300 mg per day after 1 week. Following an additional week the dosage may be increased to 450 mg per day. The maximum dosage of 600 mg per day may be achieved after additional week.
Fibromyalgia: The usual dose range for most patients is 300 to 450 mg per day given in two divided doses. Some patients may derive additional benefit at 600 mg per day. Dosing should begin at 75 mg two times a day (150 mg/day) and may be increased to 150 mg two times a day (300 mg/day) within 1 week based on efficacy and tolerability. Patients who do not experience sufficient benefit with 300 mg/day may be further increased to 225 mg two times a day (450 mg/day). If needed, in some patients, based on individual response and tolerability, the dose may be increased to maximum dosage of 600 mg/day after an additional week.
Discontinuation of therapy: When discontinuing pregabalin, taper off gradually over at least 1 week.
Special Population: Renal impairment: In patients with renal function impairment, dosage adjustment should be based on creatinine clearance (CrCl), as indicated in the following Table 1 determined using the Cockcroft-Gault formula, the formula show below. (See Equation.)

Click on icon to see table/diagram/image

For patients undergoing hemodialysis, the pregabalin daily dose should be adjusted based on renal function, a supplementary dose should be given immediately following every 4-hour hemodialysis treatment. (See Table 1.)

Click on icon to see table/diagram/image

Hepatic impairment: No dosage adjustment is required for patients with hepatic impairment.
Children: The safety and efficacy of pregabalin in children have not been established.
Elderly: Elderly patients may require a dose reduction of pregabalin due to a decreased renal function.
Method of Administration: Pregabalin is for oral use only and may be taken with or without food.
Overdosage
Symptoms: The most commonly reported adverse events observed when pregabalin was taken in overdose included affective disorder, somnolence, confusional state, depression, agitation, and restlessness.
Treatment: There is no specific antidote for overdose with pregabalin. Treatment of pregabalin overdose should be general supportive care given to patients including monitoring of vital signs and observation of the clinical status and may include hemodialysis if necessary.
Contraindications
Hypersensitivity to the active substance or to any of the excipients.
Warnings
Warning based on the Ministry of Public Health Announcement: 1. Pregabalin may cause drowsiness, should not drive a car or operate machinery and do not drink alcohol while taking this medicine.
2. This medicine may cause hematologic disorder.
3. Do not use this medicine in pregnant women because it may cause birth defect.
4. Should use with caution in patients with hepatic or renal impairment.
Special Precautions
Effect on weight gain/edema may be additive with the thiazolidinedione class of antidiabetic agents, use caution when coadministering these agents, particularly in patients with prior cardiovascular disease.
There have been postmarketing reports of hypersensitivity reactions (skin redness, blisters, hives, rash, dyspnea, and wheezing), including cases of angioedema. Discontinue pregabalin immediately in patients with these symptoms.
Pregabalin may cause somnolence/sedation and dizziness. Advise patients to not drive a car or operate other complex machinery until they have gained the ability to assess whether this medication impairs their ability to drive or perform other tasks.
Visual disturbances (blurred vision, decreased acuity and visual field changes) have been associated with pregabalin therapy, inform patients to notify their physician if changes in visual occur.
Pregabalin has been associated with discontinuation symptoms including insomnia, nausea, headache, anxiety, hyperhidrosis, and diarrhea following abrupt cessation and increases in seizure frequency (when used as an epileptic) may occur.
Pregabalin is not known to be active at receptor sites associated with drugs of abuse. As with any CNS active drugs, clinicians should carefully evaluate patients for history of drug abuse and observe them for signs of pregabalin misuse or abuse (e.g., development of tolerance, dose escalation, drug-seeking behavior).
The risk of toxic reactions to pregabalin may be greater in patients with impaired renal function. Take care in dose selection and adjust dose based on CrCl values in these patients.
Use In Pregnancy & Lactation
Pregnancy: Category C.
There are no adequate data in pregnant women. Therefore, use pregabalin during pregnancy only if the benefit to the mother clearly outweighs the potential risk to the fetus. Effective contraception must be used in women of child-bearing potential.
Lactation: Pregabalin is excreted in the milk of lactating women. The effects of pregabalin on infants is unknown, a decision must be made whether to discontinue breast-feeding or to discontinue from pregabalin therapy taking into account the benefit of breast-feeding for the child and the benefit of therapy of the woman.
Adverse Reactions
Frequency of adverse effects may be influenced by dose or concurrent therapy. As shown in the following table. (See Table 2.)

Click on icon to see table/diagram/image

There have been postmarketing reports including angioedema, breast enlargement, diarrhea, dizziness, gynecomastia, headache, nausea, hypersensitivity (skin redness, blisters, hives, rash, dyspnea and wheezing). Following abrupt discontinuation: anxiety, hyperhidrosis, insomnia, nausea, headache and diarrhea.
Drug Interactions
Since pregabalin undergoes negligible metabolism in humans, pharmacokinetics of the drug are unlikely to be affected by other agents through metabolic interaction. In addition, pregabalin does not bind to plasma proteins, a pharmacokinetic interaction with drugs that are highly protein bound is unlikely.
Pharmacokinetic interaction unlikely with anticonvulsants (e.g., phenytoin, carbamazepine, valproate, lamotrigine, phenobarbital, topiramate). Concomitant administration of gabapentin with pregabalin did not alter pharmacokinetics of gabapentin although the rate, but not the extent, of absorption of pregabalin was decreased slightly. Tiagabine does not appear to effect the pharmacokinetics of pregabalin.
Glyburide, insulin and metformin do not appear to affect the pharmacokinetics of pregabalin. Potential pharmacologic interaction with thiazolidinediones (e.g., increased risk of weight gain and peripheral edema).
Pharmacokinetic interaction with lorazepam, oxycodone and alcohol is unlikely. Potential pharmacologic interaction (e.g., additive effects on cognitive and gross motor functioning); no clinically important effects on respiration.
Potential pharmacologic interaction with angiotensin-converting enzyme (ACE) inhibitiors (e.g., increased risk of developing angioedema).
Potential pharmacologic interaction (e.g., additive CNS depressant effects) with concurrent administration of CNS depressants, including opiates and benzodiazepines.
Pharmacokinetic interaction with oral contraceptives is unlikely.
Storage
Keep in tight container, store below 30°C.
ATC Classification
N03AX16 - pregabalin ; Belongs to the class of other antiepileptics.
Presentation/Packing
Hard cap 75 mg (red, white hard gelatin capsule No. 4, overprinted "MCP" and "75" with black ink on capsule containing white powder) x 4 x 14's.
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