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Adverse Effects and Precautions Interactions Pharmacokinetics Uses 91 2 3. Montplaisir J, et a!. Pramipexole in the treatment of restless legs Sifrol; Ger.: Oprymea; Pramip; Sifrol; Gr.: Glepark; Mariprax; Abuse. Like other antimuscarinics (see also under Trihex­ Bur J Neuro/ 2000; 7 27-31. syndrome: a follow-up study. (suppl l): Medopexol; Miraleton; Miraparkin; Mirapexin; Hong Kong: yphenidyl Hydrochloride, p. 918.1) procyclidine has been 4. Saletu M, et al. Acute placebo-controlled sleep laboratory studies and Mirapex; Hung.: Mirapexin; Oprymea; Pramitenorm; Indon.: clinical follow-up with pramipexole in restless legs syndrome. Bur Arch abused for its euphoriant effects. 1•2 Sifrol; Irl.: Glepark; Meroximer; Miramel; Mirapexin; Mirole; Psychiatry Clin Neurosci 2002; 252: 185-94. 1. McGucken RB, et al. Teenage procyclidine abuse. Lancet 1985; i: 1514. 5. Silber MH, et at. Pramipexole in the management of restless legs Oprymea; Sifrol; Israel: Sifrol; Trimexol; Ital. : Ezaprev; Mari­ 2. Dooris B, Reid C. Feigning dystonia to feed an unusual drug addiction. J syndrome: an extended study. Sleep 2003; 26: 819-21. prax; Miparkan; Miraper; Mirapexin; Miviren; Pramigen; Acrid Emerg Med 2000; 17: 311. 6. Stiasny-Kolster K, Oertel WH. Low-dose pramipexole in the manage­ Ramixole; Jp n: BI-Sifrol; Mirapex; Malaysia: Sifrol; Mex.: ment of restless legs syndrome: an open label trial. Neuropsychobiology Sifrol; Neth.: Glepark; Mirapexin; Oprymea; Pramipexolane; 2004; 50: 65-70. Pramithon; Sifrol; Norw. : Sifrol; NZ: Sifrol; Philipp.: Sifrol; Interactions 7. Winkelman JW, et al. Efficacy and safety of pramipcxole in restless legs syndrome. Neurology 2006; 67: 1034-9. Pol. : Miparkan; Mirapexin; Neliprax; Oprymea; Pramixil; Rit­ As for antimuscarinics in general (see Atropine Sulfate, 8. Oertel WH, et a!. Pramipexole RLS Study Group. Efficacy ofpramipexole morest; Sifrol; Port.: Ezaprev; Mirapexin; Oprymea; Sifrol; p. 1312.3). (MnparreKc); in restless legs syndrome: a six-week, multicenter, randomized, double­ Rus.: Mirapex S.Afr. : Pexola; Singapore: Sifrol; Paroxetine increases plasma-procyclidine concentrations blind study (effect-RLS study). Mov Disord 2007; 22: 2l3-I9. Spain: Mirapexin; Swed.: Derinik; Oprymea; Sifrol; Switz.: and it is recommended that the dose of procyclidine should Sifrol; Thai.: Sifrol; Turk. : Parkyn; Parson; Pexola; UK: Mira­ be reduced if antimuscarinic effects are seen in patients Adverse Effectsand Precautions pexin; Ukr.: Mirapex (MHpaneKc); Miraxol (MupaKcon); USA: Mirapex; Venez. : Sifrol!Mirapex. receiving both drugs. As for Bromocriptine, p. 896.3. Pramipexole should be used with caution in patients Pharmacokinetics with renal impairment and reduced doses are recom­ mended. Procyclidine Hydrochloride Procyclidine hydrochloride is absorbed from the gastro­ Ophthalmological monitoring is recommended at regular intestinal tract and bioavailability has been reported to be {BANM, r!NNM} 75% after oral doses; it disappears rapidly from the tissues. intervals or if vision abnormalities occur. Procyclidine given intravenously acts within 5 to 20 Incidence of adverse effects. References, minutes and has a duration of effect of up to 4 hours. The l. Etminan M, et al. Comparison of the risk of adverse events with mean plasma elimination halfRlife after oral or intravenous pramipexole and ropinirole in patients with Parkinson's disease: a meta­ doses is about 12 hours. About one-fifth of an oral dose is analysis. Drug Safety 2003; 26: 439-44. metabolised in the liver, mainly by the cytochrome P450 isoenzymes, followed by conjugation with glucuronic acid. Effects on mental function. Pramipexole has been asso­ A small amount of unchanged drug is excreted in the urine. dated with attacks of sudden onset of sleep, sometimes without any prior feeling of drowsiness, that can occur at References. l. Whiteman PD, et al. Pharmacokinetics and pharmacodynamics of any time during treatment. Licensed product information procydidine in man. Eur J Clin Pharmaco/ 1985; 28: 73-8. states that the incidence of daytime somnolence is increased at daily doses of pramipexole hydrochloride t higher than 1.5 mg. A retrospective analysis1 of data to P..r�P.?.r?_ ic:>n.S......... ................................................................... evaluate the incidence and nature of somnolence in Pharmacopoeios. In Br. and US. ProprietaryPreparations (details are given in Volume B) patients receiving pramipexole in clinical studies showed BP 2014: (Procyclidine Hydrochloride). A white, odour!ess Austria: Kemadrin; Belg.: that for patients with moderate or severe somnolence, the Single-ingredient Preparations. or almost odourless, crystalline powder. Sparingly soluble in Kemadrin; Cz.: Kemadrin; Denm.: Kemadrin; Ger.: Osnervan; onset of worst-reported somnolence occurred at a mean water; soluble in alcohol; practically insoluble in acetone Hung.: Kemadrin; India: Kemadrin; Irl.: Kemadrin; Israel: daily dose of around 4mg (range: 0.75 to 4.5 mg) . and in ether. A I% solution in water has a pH of 4.5 to 6.5. Kemadrin; NZ: Kemadrin; Spain: Kemadren; Switz.: Kemadrin; For further reports of daytime somnolence occurring in USP 36: (Procyclidine Hydrochloride). A white crystalline UK: Arpicolin; Kemadrin. patients receiving dopamine agonists including pramipex­ powder, having a moderate characteristic odour. Soluble I ole, see under Levodopa, p. 905.2. PharmacopoeialPreparations in 35 of water, I in 9 of alcohol, I in 6 of chloroform, and I For reference to disturbed behaviour including BP 2014: Procyclidine Injection; Procyclidine Tablets; in II 000 of ether; insoluble in acetone. pH of a I% solution USP 36: Procyclidine Hydrochloride Tablets. excessive gambling reported in patients with Parkinson's in water is between 5.0 and 6.5. Store in a dry place in disease receiving dopamine agonists, including pramipex­ airtight containers. Protect from light. o!e, see under Levodopa, p. 905.2. I. Hauser RA, et al. Prarnipexole-induced somnolence and episodes of daytime sleep. Mov Disord 2000; 15: 658-63. Uses and Administration Porphyria. The Drug Database for Acute Porphyria, com­ Procyclidine hydrochloride is a tertiary amine antimusca­ piled by the Norwegian Porphyria Centre (NAPOS) and rinic with actions and uses similar to those of the Porphyria Centre Sweden, classifies pramipexole as trihexyphenidyl (p. 917.3). It is used for the symptomatic probably not porphyrinogenic; it may be used as a drug of treatment of parkinsonism (p. 889.1), including the first choice and no precautions are needed. 1 alleviation of the extrapyramidal syndrome induced by I. The Drug Database for Acute Porphyria. Available at: http://www. drugs such as phenothiazines, but, like other antimusca­ drugs-porphyria.org (accessed 30/09/11) rinics, is of no value against tardive dyskinesias. It has been used in the treatment of dystonias (but see under Uses and Interactions Administration of Levodopa, p. 903.3); for doses in children, As for Bromocriptine, p. 899.1. Cimetidine is reported to see below. reduce the renal clearance of pramipexole. In parkinsonism, the initial oral dose of 2.5 mg three Caution is advised when other sedating drugs or alcohol times daily may be increased gradually by 2.5 to 5 mg every are used with pramipexole because of possible additive 2 or 3 days (or by 2.5 mg daily if used for drug-induced Profile effects and the risk of precipitating sudden onset of sleep extrapyramidal syndrome) until the optimum maintenance (see above). dose, usually 10 to 30mg daily in 3 (or occasionally 4) Profenamine hydrochloride is a phenothiazine derivative divided doses, is reached; daily doses of up to 60 mg have with antimuscarinic, adrenergic-blocking, antihistaminic, References. occasionally been required. As a rule, postencephalitic I. Wright CE, et al. Influence of probenecid and dmetidine on pramipexole local anaesthetic, and ganglion-blocking properties. Adverse pharmacokinetics. Clin Pharmacal Ther 1996; 59: 183. patients tolerate and require the larger doses; elderly and effects associated with phenothiazines may occur, especially arteriosclerotic patients may require smaller doses. with high doses (see under Chlorpromazine, p. 1047.2). Pharmacokinetics In an emergency such as acute dystonias, 5 to 10 mg Profenamine has been used in the symptomatic treatment of may be given by intravenous injection; higher doses have parkinsonism (p. 889. 1 ), including the alleviation of the Pramipexole is readily absorbed from the gastrointestinal sometimes been used. The intramuscular route has also extrapyramidal syndrome induced by drugs such as other tract and peak plasma concentrations have occurred within been employed: 5 to I 0 mg may be given as a single phenothiazines, but, like other antimuscarinics (see about 2 hours in fasting patients and in about 3 hours when injection, repeated if necessary after 20 minutes to a Atropine Sulfate, p. 1310.2), is of no value against tardive given with food. Oral bioavailability is reported to be about maximum of 20 mg daily. Parenteral doses are usually dyskinesias. It has been used in a usual initial oral dose of 90%. Pramipexole is widely distributed throughout the effective within 5 to 10 minutes but may need 30 minutes to 50 mg three times daily, gradually increased to 500 mg or body and plasma-protein binding is less than 20%. produce relief. more daily in divided doses, according to response. Metabolism is minimal and more than 90% of a dose is excreted via renal tubular secretion unchanged into the r t urine. Elimination half-lives of 8 to 12 hours have been Administration in children.
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