Pramipexole (pramipexole di-HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Pramipexole dihydrochloride is a nonergot-derivative dopamine receptor agonist.
Pramipexole dihydrochloride, a synthetic benzothiazolamine derivative, is a nonergot-derivative dopamine receptor agonist. Pramipexole demonstrates high binding specificity for and intrinsic activity at dopamine D2 receptors compared with other dopamine receptor agonists (e.g., bromocriptine, pergolide), having a higher affinity for the D3 receptor subtype than for the D2 or D4 subtypes. Pramipexole binds with moderate affinity to alpha2-adrenergic receptors but has little or no affinity for alpha1- or beta-adrenergic, acetylcholine, dopamine D1, or serotonin (5-hydroxytryptamine (5-HT)) receptors.
The exact mechanism of action of pramipexole in the management of parkinson disease has not been fully elucidated. There is considerable evidence that manifestations of parkinsonian syndrome, regardless of the cause of the syndrome, are related to depletion of dopamine in the corpus striatum. While levodopa is believed to act principally by increasing dopamine concentration in the brain, pramipexole appears to act by directly stimulating postsynaptic dopamine receptors in the corpus striatum.
The exact mechanism of action of pramipexole in the management of restless legs syndrome remains to be determined, but is thought to involve the dopaminergic system.
USES: Pramipexole is used alone or with other medications to treat Parkinson's disease. It can improve your ability to move and decrease shakiness (tremor), stiffness, slowed movement, and unsteadiness. It may also decrease the number of episodes of not being able to move ("on-off syndrome").
This medication is also used to treat a certain medical condition (restless legs syndrome - RLS) that causes an unusual urge to move the legs. Symptoms usually occur at night along with uncomfortable/unpleasant feelings in the legs. This medication can decrease these symptoms and thereby improve sleep.
Pramipexole is a dopamine agonist that works by helping to restore the balance of a certain natural substance (dopamine) in the brain.
Generic name: pramipexole di-HCl
Pronunciation: (pram-ih-PEX-ole)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Pramipexole
Indications
The following indications are listed for Pramipexole:
- Idiopathic Parkinsonism
- Restless Leg Syndrome
Also known as: Anxietas Tibiarum, Ekbom Syndrome, Paralysis Agitans, Primary Parkinson's Disease, Restless Legs.
Dosing
Dosage of pramipexole dihydrochloride is expressed in terms of the monohydrated form of the salt.
Pramipexole therapy is initiated at a low dosage and titrated slowly based on response and tolerability. Increases in blood pressure and heart rate have been observed in healthy individuals when dosage was titrated more quickly (i.e., every 3 days) than recommended.
If pramipexole therapy is interrupted for a substantial period of time, retitration may be warranted.
Because dosage of pramipexole is titrated to clinical response, routine dosage adjustment based solely on age is not necessary in geriatric patients.
Pramipexole dihydrochloride is administered orally as conventional (immediate-release) tablets or extended-release tablets; the extended-release tablets are FDA-labeled for use only in the treatment of parkinson disease. For the management of parkinson disease, pramipexole is administered as immediate-release tablets in 3 equally divided doses daily or as extended-release tablets given once daily. When used for the management of restless legs syndrome (RLS), pramipexole is administered as immediate-release tablets once daily 2-3 hours before bedtime.
Pramipexole extended-release tablets should be swallowed whole and should not be chewed, crushed, or divided.
Administration of the immediate-release tablets with food decreases the rate, but not the extent, of absorption; time to peak concentration is delayed by about 1 hour. Administration of the extended-release tablets with food increases peak plasma concentrations by approximately 20% and delays time to peak concentration by approximately 2 hours, but does not affect the extent of exposure. Therefore, both the immediate-release and extended-release tablets may be administered without regard to meals; however, taking the drug with food may reduce the occurrence of nausea.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
There are no contraindications to the use of pramipexole.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Common adverse effects in patients with early parkinson disease (who are not receiving concomitant levodopa) include nausea, dizziness, somnolence, insomnia, asthenia, fatigue, muscle spasms, dry mouth, constipation, hallucinations, general edema, and peripheral edema.
Common adverse effects in patients with advanced parkinson disease (who are receiving concomitant levodopa) include postural hypotension, dyskinesia, extrapyramidal syndrome, insomnia, dizziness, hallucinations, accidental injury, headache, dream abnormalities, confusion, asthenia, nausea, anorexia, constipation, somnolence, dystonia, dry mouth, gait abnormalities, hypertonia, amnesia, and urinary frequency.
Common adverse effects in patients with RLS include nausea, headache, fatigue, insomnia, somnolence, abnormal dreams, diarrhea, nasal congestion, influenza, and pain in extremity.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of pramipexole in pediatric patients have not been established.
There are no adequate data on the developmental risks associated with the use of pramipexole in pregnant women; the teratogenic potential of the drug has not been completely established in animal studies. No adverse developmental effects were observed in studies conducted in rabbits; although increased embryolethality was observed in rat studies, this was thought to result from a species-specific effect of pramipexole on prolactin. In rats, inhibition of postnatal growth was observed at pramipexole dose exposures similar to those in humans.
It is not known whether pramipexole is distributed into human milk; the drug is distributed into milk in rats. The effects of pramipexole on the breast-fed infant or on milk production are not known. The known benefits of breast-feeding should be considered along with the mother's clinical need for pramipexole and any potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.
Because pramipexole inhibits prolactin secretion, the drug is expected to inhibit lactation.
Due to age-related changes in renal function, clearance of pramipexole is reduced (by about 30%) and elimination half-life is increased (from approximately 8.5 to 12 hours) in geriatric patients older than 65 years of age compared with younger adults.
Geriatric patients with parkinson disease may be at increased risk of hallucinations; no other apparent differences in safety or efficacy have been observed between geriatric patients and younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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