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Product Name
:
GABALYR
Chemical Name
:
Pregabalin
Therapeutic Category
:
Central nervous system drugs
Pharmacologic Category
:
Analgesic, Anticonvulsant
Pharmaceutical Form
:
Capsules
Composition
:
Pregabalin 25mg/ 100mg/ 200mg/ 300mg
Dosing
 
Dosing: Adult

Fibromyalgia: Oral: Initial: 150 mg daily in divided doses (75 mg twice daily); may be increased to 300 mg daily (150 mg twice daily) within 1 week based on tolerability and effect; may be further increased to 450 mg daily (225 mg twice daily). Maximum dose: 450 mg daily (dosages up to 600 mg daily were evaluated with no significant additional benefit and an increase in adverse effects)

Neuropathic pain, diabetes-associated: Oral: Initial: 150 mg daily in divided doses (50 mg 3 times daily); may be increased within 1 week based on tolerability and effect; maximum dose: 300 mg daily (dosages up to 600 mg daily were evaluated with no significant additional benefit and an increase in adverse effects)

Neuropathic pain, spinal cord injury associated: Oral: Initial: 150 mg daily in divided doses (75 mg twice daily); may be increased to 300 mg daily (150 mg twice daily) within 1 week based on tolerability and effect; further titration to 600 mg daily (300 mg twice daily) after 2-3 weeks may be considered in patients who do not experience sufficient relief of pain provided they are able to tolerate pregabalin. Maximum dose: 600 mg daily

Partial-onset seizures (adjunctive therapy): Oral: Initial: 150 mg daily in divided doses (75 mg twice daily or 50 mg 3 times daily); may be increased based on tolerability and effect (optimal titration schedule has not been defined). Maximum dose: 600 mg daily

Postherpetic neuralgia: Oral: Initial: 150 mg daily in divided doses (75 mg twice daily or 50 mg 3 times daily); may be increased to 300 mg daily within 1 week based on tolerability and effect; further titration (to 600 mg daily) after 2-4 weeks may be considered in patients who do not experience sufficient relief of pain provided they are able to tolerate pregabalin. Maximum dose: 600 mg daily

Note: Discontinuing therapy: Pregabalin should not be abruptly discontinued; taper dosage over at least 1 week


Dosing: Geriatric

Refer to adult dosing.


Dosing: Renal Impairment

Renal function may be estimated using the Cockcroft-Gault formula. Then determine recommended dosage regimen based on the indication-specific total daily dose for normal renal function (Cl cr ≥60 mL/minute). For example, if the indication-specific daily dose is 450 mg daily for normal renal function, the daily dose should be reduced to 225 mg daily (in 2-3 divided doses) for a creatinine clearance of 30-60 mL/minute (see table).

 

Pregabalin Renal Impairment Dosing

Cl cr

(mL/minute)

Total Pregabalin Daily Dose

(mg/day)

Dosing Frequency

Posthemodialysis supplementary dosage (as a single additional dose):

25 mg/day schedule: Single supplementary dose of 25 mg or 50 mg

25-50 mg/day schedule: Single supplementary dose of 50 mg or 75 mg

50-75 mg/day schedule: Single supplementary dose of 75 mg or 100 mg

75 mg/day schedule: Single supplementary dose of 100 mg or 150 mg

≥60 (normal renal function)

150

300

450

600

2-3 divided doses

30-60

75

150

225

300

2-3 divided doses

15-30

25-50

75

100-150

150

1-2 divided doses

<15

25

25-50

50-75

75

Single daily dose

Use
 

Management of neuropathic pain associated with diabetic peripheral neuropathy or with spinal cord injury; management of postherpetic neuralgia; adjunctive therapy for partial-onset seizure disorder; management of fibromyalgia

Adverse Reactions
 

>10%:

Cardiovascular: Peripheral edema (≤16%)

Central nervous system: Dizziness (8% to 45%), somnolence (4% to 36%), ataxia (1% to 20%), headache (5% to 14%), fatigue (5% to 11%)

Gastrointestinal: Weight gain (≤16%), xerostomia (1% to 15%)

Neuromuscular & skeletal: Tremor (≤11%)

Ocular: Blurred vision (1% to 12%), diplopia (≤12%)

Miscellaneous: Infection (3% to 14%), accidental injury (2% to 11%)

1% to 10%:

Cardiovascular: Edema (≤8%), chest pain (1% to 4%), hypertension (2%), hypotension (2%)

Central nervous system: Neuropathy (2% to 9%), thinking abnormal (≤9%), confusion (≤7%), euphoria (≤7%), speech disorder (≤7%), attention disturbance (4% to 6%), amnesia (≤6%), incoordination (≤6%), pain (2% to 5%), insomnia (4%), memory impaired (1% to 4%), vertigo (1% to 4%), hypoesthesia (2% to 3%), feeling abnormal (1% to 3%), anxiety (2%), lethargy (1% to 2%), drunk feeling (1% to 2%), disorientation (≤2%), depersonalization (≥1%), fever (≥1%), hypertonia (≥1%), sedation (≥1%), stupor (≥1%), nervousness (≤1%)

Dermatologic: Decubitus ulcer (3%), facial edema (≤3%), bruising (≥1%), pruritus (≥1%)

Endocrine & metabolic: Fluid retention (2% to 3%), hypoglycemia (1% to 3%), libido decreased (≥1%)

Gastrointestinal: Constipation (≤10%), appetite increased (2% to 7%), nausea (5%), flatulence (≤3%), vomiting (1% to 3%), abdominal distension (2%), abdominal pain (≥1%), gastroenteritis (≥1%)

Genitourinary: Incontinence (≤3%), anorgasmia (≥1%), impotence (≥1%), urinary frequency (≥1%)

Hematologic: Thrombocytopenia (≥1%)

Neuromuscular & skeletal: Balance disorder (2% to 9%), abnormal gait (≤8%), weakness (2% to 7%), arthralgia (3% to 6%), twitching (≤5%), muscle spasm (2% to 4%), back pain (≤4%), myoclonus (≤4%), CPK increased (3%), neck pain (3%), pain in extremity (3%), joint swelling (2%), paresthesia (2%), leg cramps (≥1%), myalgia (≥1%), myasthenia (1%)

Ocular: Visual abnormalities (≤5%), eye disorder (≤2%), conjunctivitis (≥1%), nystagmus (≥1%)

Otic: Otitis media (≥1%), tinnitus (≥1%)

Respiratory: Nasopharyngitis (8%), sinusitis (4% to 7%), pharyngolaryngeal pain (1% to 3%), bronchitis (≤3%), dyspnea (≤3%)

Miscellaneous: Flu-like syndrome (1% to 2%), allergic reaction (≥1%)

Contraindications
 
Hypersensitivity to pregabalin or any component of the formulation
Warnings / Precautions Drug
 

Concerns related to adverse effects:

• Angioedema: Angioedema has been reported; may be life-threatening; use with caution in patients with a history of angioedema episodes. Concurrent use with other drugs known to cause angioedema (eg, ACE inhibitors) may increase risk.

• CNS effects: Dizziness and somnolence are commonly reported; effects generally occur shortly after initiation and occur more frequently at higher doses. Patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

• Hypersensitivity: Hypersensitivity reactions, including skin redness, blistering, hives, rash, dyspnea, and wheezing have been reported; discontinue treatment of hypersensitivity occurs.

• Peripheral edema: Use may cause peripheral edema; use with caution in patients with heart failure (NYHA Class III or IV) due to limited data in this patient population. In addition, 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.

• Platelet count: May decrease platelet count. Severe thrombocytopenia is extremely rare.

• PR interval: May cause mild prolongation of PR interval. Clinical significance unknown.

• Rhabdomyolysis: Has been associated with increases in CPK and rare cases of rhabdomyolysis; patients should be instructed to notify their prescriber if unexplained muscle pain, tenderness, or weakness, particularly if fever and/or malaise are associated with these symptoms.

• Suicidal ideation: Pooled analysis of trials involving various antiepileptics (regardless of indication) showed an increased risk of suicidal thoughts/behavior (incidence rate: 0.43% treated patients compared to 0.24% of patients receiving placebo); risk observed as early as 1 week after initiation and continued through duration of trials (most trials ≤24 weeks). Monitor all patients for notable changes in behavior that might indicate suicidal thoughts or depression; notify healthcare provider immediately if symptoms occur.

• Visual disturbances: Blurred vision, decreased acuity and visual field changes have been associated with therapy; patients should be instructed to notify their physician if these effects are noted.

• Weight gain: Use may cause weight gain; weight gain generally associated with dose and duration (average weight gain was 5.2 kg for patients receiving pregabalin for ≥2 years); weight gain was not limited to patients with edema and did not appear to be associated with baseline BMI, gender, age, or loss of glycemic control in diabetic patients.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with severe cardiovascular disease, including heart failure; weight gain and/or peripheral edema may occur.

• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment required.

Concurrent drug therapy issues:

• Sedatives: Effects with other sedative drugs or ethanol may be potentiated.

Other warnings/precautions:

• Tumorigenic potential: Increased incidence of hemangiosarcoma noted in animal studies; significance of these findings in humans is unknown.

• Withdrawal: Anticonvulsants should not be discontinued abruptly because of the possibility of increasing seizure frequency; therapy should be withdrawn gradually to minimize the potential of increased seizure frequency, unless safety concerns require a more rapid withdrawal. Tapering over at least 1 week is recommended.

Interactions
 

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Antidiabetic Agents (Thiazolidinedione): Pregabalin may enhance the fluid-retaining effect of Antidiabetic Agents (Thiazolidinedione). Risk C: Monitor therapy

Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Risk X: Avoid combination

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of CNS depressants used in combination with buprenorphine. Consider avoiding other CNS depressants in patients thought to be at high risk of buprenorphine overuse or self-injection. Risk D: Consider therapy modification

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy

Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Ketorolac (Nasal): May diminish the therapeutic effect of Anticonvulsants. Risk C: Monitor therapy

Ketorolac (Systemic): May diminish the therapeutic effect of Anticonvulsants. Risk C: Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Mefloquine: May diminish the therapeutic effect of Anticonvulsants. Mefloquine may decrease the serum concentration of Anticonvulsants. Management: Mefloquine is contraindicated for malaria prophylaxis in persons with a history of convulsions. Monitor anticonvulsant concentrations and treatment response closely with concurrent use. Risk D: Consider therapy modification

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification

Metyrosine: CNS Depressants may enhance the sedative effect of Metyrosine. Risk C: Monitor therapy

Mirtazapine: CNS Depressants may enhance the CNS depressant effect of Mirtazapine. Risk C: Monitor therapy

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Risk D: Consider therapy modification

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy

Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy

Sodium Oxybate: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. Risk D: Consider therapy modification

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider therapy modification

Pregnancy
 
Pregnancy Risk Factor

C

Pregnancy Implications

Increased incidence of fetal abnormalities, particularly skeletal malformations, were observed in animal studies. Male-mediated teratogenicity has been observed in animal reproduction studies; implications in humans are not defined. Impaired male and female fertility has been noted in animal studies.

Lactation
 

Excretion in breast milk unknown/not recommende

Monitoring Parameters
 

Measures of efficacy (pain intensity/seizure frequency); degree of sedation; symptoms of myopathy or ocular disturbance; weight gain/edema; skin integrity (in patients with diabetes); suicidality (eg, suicidal thoughts, depression, behavioral changes)

Mechanism of Action
 

Binds to alpha 2 -delta subunit of voltage-gated calcium channels within the CNS, inhibiting excitatory neurotransmitter release. Although structurally related to GABA, it does not bind to GABA or benzodiazepine receptors. Exerts antinociceptive and anticonvulsant activity. Decreases symptoms of painful peripheral neuropathies and, as adjunctive therapy in partial seizures, decreases the frequency of seizures. Pregabalin may also affect descending noradrenergic and serotonergic pain transmission pathways from the brainstem to the spinal cord.

Pharmacodynamics / Kinetics
 

Onset of action: Pain management: Effects may be noted as early as the first week of therapy.

Distribution: V d : 0.5 L/kg

Protein binding: 0%

Metabolism: Negligible

Bioavailability: >90%

Half-life elimination: 6.3 hours

Time to peak, plasma: 1.5 hours (3 hours with food)

Excretion: Urine (90% as unchanged drug; minor metabolites)

 
   
 
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