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Trihexyphenidyl

HCID 5572
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TeilstruktursucheÄhnliche Strukturen suchen

Grundinformationen

CAS
144-11-6
Standard-SMILES
OC(CCN1CCCCC1)(c1ccccc1)C1CCCCC1
InChIKey
HWHLPVGTWGOCJO-UHFFFAOYSA-N
Summenformel
C20H31NO
Durchschnittliche Molmasse
301,5 g/mol
Monoisotopische Masse
301,24056461

Überblick

Trihexyphenidyl is an amine.

Namen und Bezeichner

Bevorzugter Name
Trihexyphenidyl
IUPAC
1-cyclohexyl-1-phenyl-3-piperidin-1-ylpropan-1-ol
Lokaler Name
Trihexyphenidyl
Englischer Name
Trihexylphenedyl
Summenformel
C20H31NO
Molmasse
301.47

Namen und Synonyme

trihexyphenidylBenzhexol144-11-6TriphenidylTrihexyphenidyleBenzhexolumTrihexifenidiloTrihexyphenidylumApo-Trihex1-cyclohexyl-1-phenyl-3-(piperidin-1-yl)propan-1-ol1-Piperidinepropanol, alpha-cyclohexyl-alpha-phenyl-6RC5V8B7PO
Weitere Namen anzeigen
ArtaneTrihexylphenidylBenzoxolrihexylphenedylTrihexylphenedylParkinane retard
NSC-12268DTXSID40237055-20-02-00231 (Beilstein Handbook Reference)TriesifenidilePacitanePargitanApoTrihexAtan

Datenbank-Bezeichner

CAS
144-11-6
PubChem CID
5572
DTXSID
DTXSID4023705
ChEMBL
CHEMBL1490
ChEBI
CHEBI:9720
UNII
6RC5V8B7PO

Eigenschaften

Berechnete Struktureigenschaften

XLogP
4,5
Polarare Oberfläche (TPSA)
23,5 Ų
H-Brücken-Donoren
1
H-Brücken-Akzeptoren
2
Frei drehbare Bindungen
5
Schwere Atome
22
Formalladung
0
Komplexität
314

Experimentelle und physikochemische Eigenschaften

Drugs · 2 Einträge

Pharmaceuticals

Pharmaceuticals -> Antipsychotics

LogP · 3 Einträge

log Kow = 4.49

4.5

4.49

Solubility · 2 Einträge

Crystals; decomp at 258.5 °C; pH of 1% aq soln 5.5-6.0; solubility (g/100 mL): water at 25 °C 1.0, alcohol 6, chloroform 5; more soluble in methanol; very slightly soluble in ether, benzene /Hydrochloride/

3.14e-03 g/L

Human Drugs · 3 Einträge

Breast Feeding; Lactation; Milk, Human; Antiparkinson Agents; Muscarinic Antagonists; Parasympatholytics

Pharmaceuticals

Medicines for central nervous system disorders

Melting Point · 2 Einträge

114 °C

258.5 °C

Physical DescriptionSolid
Dissociation Constants8.7
Collision Cross Section · 2 Einträge

Sicherheit und Regulatorisches

Sicherheitsangaben dienen nur zur Orientierung und ersetzen weder das Sicherheitsdatenblatt (SDB) des Lieferanten noch geltende Vorschriften oder eine fachliche Bewertung.

GHS-Klassifizierung

GHS Classification · 4 Einträge

Danger

H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]

P264, P270, P301+P316, P321, P330, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 2 reports by companies from 1 notifications to the ECHA C&L Inventory.

Gefahrenhinweise

Regulatory Information · 2 Einträge

REACH registered substance: Trihexyphenidyl (EC: 205-614-4)

1-Piperidinepropanol, .alpha.-cyclohexyl-.alpha.-phenyl-: Does not have an individual approval but may be used under an appropriate group standard

Other Safety InformationIMAP assessments - 1-Piperidinepropanol, .alpha.-cyclohexyl-.alpha.-phenyl-: Human health tier I assessment
FDA Requirements · 1 Eintrag

The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed prescription drug products, incl trihexyphenidyl hydrochloride, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. /Trihexyphenidyl hydrochloride/

Hazard Classes and CategoriesAcute Tox. 3 (100%)

Sicherheit und Schutzausrüstung

Storage ConditionsTrihexyphenidyl hydrochloride tablets should be stored in tight containers at 15-30 °C. Trihexyphenidyl hydrochloride elixir should be stored at controlled room temperature (20-25 °C); freezing of the elixir should be avoided.

Chemie und Industrie

Pharmakologische Informationen

ATC Code · 4 Einträge

N04AA01

N - Nervous system

QN - Nervous system

N04AA01

Protein BindingData regarding the extent of trihexyphenidyl protein binding in plasma are not readily available. Trihexyphenidyl is 36.13-41.92% bound to albumin under controlled conditions in a dialysis bag.
Pharmacodynamics · 1 Eintrag

Trihexyphenidyl is an antimuscarinic indicated as an adjunct in the treatment of parkinsonism or as a treatment for drug-induced extrapyramidal symptoms. It has a long duration of action as it does not need to be given every day. It has a wide therapeutic window, with acute toxicity being non fatal in doses as high as 300 mg. Patients should have their iridocorneal angle examined before and intraocular pressure monitored during therapy. Patients should be counselled regarding the risk of anhidrosis and hyperthermia.

Mechanism of Action · 4 Einträge

Trihexyphenidyl is a non-selective muscarinic acetylcholine receptor antagonist but binds with higher affinity to the M1 subtype. In vivo studies have shown that trihexyphenidyl demonstrates higher affinity for central muscarinic receptors located in the cerebral cortex and lower affinity for those located peripherally. Other studies suggest that trihexyphenidyl may modify nicotinic acetylcholine receptor neurotransmission, leading indirectly to enhanced dopamine release in the striatum. Although the anticholinergic has proven to be useful in the treatment of symptoms associated with Parkinson’s disease or other movement disorders, its mechanism of action has yet to be fully elucidated.

Cerebral blood flow and oxygen metabolism were studied in six previously untreated patients with Parkinson's disease (PD) before and after anticholinergic treatment using positron emission tomography (PET) and compared with six controls. The PET study and an assessment of the disability and cognitive impairment were performed before and after administration of 6 mg trihexyphenidyl for 5 to 11 weeks. All PD patients showed improvements in motor symptoms after the trihexyphenidyl treatment. Cognitive function did not significantly differ between before and after trihexyphenidyl treatment. However, after trihexyphenidyl treatment, regional cerebral blood flow (rCBF) and regional oxygen metabolic rate (rCMRO2) decreased by 15% in the striatum and by 10% in all cortical areas contralateral to predominantly symptomatic limbs, and by 10% in the ipsilateral striatum and all cortical areas, significantly below the values of controls in most cerebral cortices and striatum. These findings suggest that trihexyphenidyl inhibits the cortical cholinergic system and significantly decreases rCBF and rCMRO2 in the cerebral cortices without cognitive impairment in untreated patients with PD.

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Auf dieser SeiteGrundinformationenÜberblickNamen und BezeichnerEigenschaftenSicherheit und RegulatorischesChemie und IndustrieZugehörige ReaktionenNotizen zur Verbindung
EC Number
205-614-4
Nikkaji
J19.358E、J5.826B

175.1 Ų [M+H]+ [CCS Type: DT; Method: single field calibrated]

173.72 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

Other Experimental Properties · 3 Einträge

White or slightly off white, crystalline powder ... very faint odor /Hydrochloride/

Crystals from isopropyl alcohol; mp: 264 °C; specific optical rotation: -30 deg at 20 °C/D (c = 0.4% in chloroform). Specific optical rotation: -25 deg at 20 °C/D (c = 0.4% in ethanol). /L-form hydrochloride/

Free base mp 112-113 °C. /L-form/

Physikochemische Eigenschaften

Schmelzpunkt
258.5 °C · 258.5°C
Siedepunkt
442.59 °C · 442.59°C (rough estimate)
Dichte
0.9941 · 0.9941 (rough estimate)
Brechungsindex
1.5614 · 1.5614 (estimate)
pka
14.31 · 14.31±0.29(Predicted)
NIST chemische Informationen
Trihexyphenidyl(144-11-6)
Disposal Methods · 1 Eintrag

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Toxikologische Informationen

Treatment · 1 Eintrag

Treatment of acute overdose involves symptomatic and supportive therapy. Gastric lavage or other methods to limit absorption should be instituted. A small dose of diazepam or a short-acting barbiturate may be administered if CNS excitation is observed. Phenothiazines are contraindicated because the toxicity may be intensified due to their antimuscarinic action, causing coma. Respiratory support, artificial respiration or vasopressor agents may be necessary. Hyperpyrexia must be reversed, fluid volume replaced and acid-balance maintained. Urinary catheterization may be necessary. It is not known if Trihexyphenidyl is dialyzable. (L1712)

Interactions · 3 Einträge

When trihexyphenidyl hydrochloride is used concomitantly with levodopa, the usual dose of each may need to be reduced. Careful adjustment is necessary, depending on side effects and degree of symptoms control. /Trihexylphenidyl hydrochloride/

...CENTRALLY ACTING ANTICHOLINERGIC AGENTS THAT MAY EXACERBATE TARDIVE DYSKINESIA /CAUSED BY CHLORPROMAZINE/ INCL...TRIHEXYPHENIDYL.

Trihexyphenidyl, applied in doses of 30 and 50 mg/kg (ip), did not influence the electroconvulsive threshold per se but when combined with valproate, strongly enhanced its anticonvulsant activity against maximal electroshock-induced seizures /in mice/ lowering the ED50 from 206 to 103 and 46 mg/kg, respectively. The chimney test and retention testing in mice revealed that administration of ... trihexyphenidyl at 30 mg/kg (ip) together with valproate in doses of 130 or 103 mg/kg (ip), respectively, resulted in motor impairment and caused impairment of long-term memory, similar to the effects of valproate alone, when applied at its ED50 against maximal electroshock. ... trihexyphenidyl /did not/ alter the total level of valproate in plasma. ...

Hepatotoxicity · 1 Eintrag

Trihexyphenidyl has not been reported to cause serum aminotransferase elevations, but it has not been evaluated for effects on serum enzyme levels in a prospective manner. Trihexyphenidyl was cited as the cause of two cases of acute liver injury resulting in death in the Japanese literature, but few details were given and there have been no other reports of such injury in the literature in the subsequent 40 years. Thus, trihexyphenidyl must be a very rare cause of liver injury, if it occurs at all.

Adverse Effects · 1 Eintrag

Adverse effects of trihexyphenidyl are frequently dose-dependent but usually decrease over time as tolerance develops and the body adapts to the drug. Even with all of the adverse effects considered, trihexyphenidyl demonstrated dramatic and consistent improvement of neurologic defects in people between the ages of 16 and 86 over a 5-year course. Confusion and delirium frequently occur in older patients or patients with psychiatric disorders.

Exposure RoutesOral. Trihexyphenidyl is rapidly absorbed from the gastrointestinal tract.
Toxicity Summary · 2 Einträge

Signs and Symptoms of Overdose

Trihexyphenidyl is a selective M1 muscarinic acetylcholine receptor antagonist. It is able to discriminate between the M1 (cortical or neuronal) and the peripheral muscarinic subtypes (cardiac and glandular). Trihexyphenidyl partially blocks cholinergic activity in the CNS, which is responsible for the symptoms of Parkinson's disease. It is also thought to increase the availability of dopamine, a brain chemical that is critical in the initiation and smooth control of voluntary muscle movement.

Signs and SymptomsSymptoms of overdose include mydriasis, dryness of mucous membranes, red face, atonic states of bowels and bladder, and hyperthermia in high doses. Central consequences are agitation, confusion, and hallucinations.
Human Toxicity Excerpts · 5 Einträge

/SIGNS AND SYMPTOMS/ ... In a group of 22 psychiatric patients receiving long-term antipsychotic medication concurrently with trihexyphenidyl the effects of trihexyphenidyl withdrawal were studied double-blind and placebo controlled. Anxiety, psychotic symptoms, extrapyramidal symptoms and salivary flow were monitored. Blood pressure, pulse, sleep duration, weight and body temperature were recorded daily. The result was a recognizable withdrawal syndrome indicated by an increase in anxiety with various physical complaints, as well as evidence of orthostatic hypotension and tachycardia. A temporary deterioration was noted in psychotic symptomatology and extrapyramidal symptoms. The majority of the parameters regained baseline values, indicating the symptoms were related to the discontinuation of trihexyphenidyl and supporting the existence of a withdrawal syndrome.

/SIGNS AND SYMPTOMS/ In Brazil, the medicinal misuse of trihexyphenidyl has been observed among several segments of society. The present study was conducted in the city of Sao Paulo during 2002 to characterize this abuse. A sample of 21 users and 16 ex-users was interviewed using qualitative methodology; the subjects were single, unemployed, male polydrug users, who used trihexyphenidyl in order to attain states of mental alterations, mainly hallucinations and deliriums. Trihexyphenidyl is consumed in association with alcohol, other licit drugs (benzodiazepines), or illicit drugs, impairing cognitive functions such as memory, attention, and learning, intervening with some activities of users' daily life.

/CASE REPORTS/ ... Two case reports of trihexyphenidyl abuse /are described/. In one of the cases a double-blind, placebo-controlled withdrawal was conducted and monitored on a number of physiological parameters and the Hamilton Anxiety Rating Scale. A recognizable withdrawal syndrome followed discontinuation of the drug. ...

/CASE REPORTS/ ... The case presented is of anti-cholinergic abuse by a chronic schizophrenic who abused trihexyphenidyl, up to 200 mg per day, to achieve an euphoric effect. The drug was partly prescribed in psychiatric clinics, but mostly bought in the drugstore. The discontinuance of trihexyphenidyl produced anxiety, which was relieved by anxiolytics. The patient also feigned extrapyramidal symptoms to get anticholinergic injections during drug abstinence. ...

For more Human Toxicity Excerpts (Complete) data for TRIHEXYPHENIDYL (13 total), please visit the HSDB record page.

Carcinogen ClassificationNo indication of carcinogenicity to humans (not listed by IARC).
Drug Induced Liver Injury · 5 Einträge

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

trihexyphenidyl

DILI Negative

Oral

DOI:10.1016/j.drudis.2019.09.022

Non-Human Toxicity Excerpts · 2 Einträge

/LABORATORY ANIMALS: Neurotoxicity/ An amnesic effect ... induced by trihexyphenidyl and biperiden, clinically used in the parkinsonism and schizophrenic patients, /was studied/ by using passive avoidance tasks. Both of these drugs (0.1-10 mg/kg, sc) showed dose-dependent amnesic effects in the acquisition and retrieval phases. However, the effect induced by trihexyphenidyl was transient, whereas that of biperiden was long-lasting. To clarify the reason for the different duration of the amnesic activity, binding to the muscarinic receptor was examined. In the Scatchard analysis, trihexyphenidyl competed with [(3)H]quinuclidinyl benzilate ([(3)H]QNB) on the muscarinic receptor (showed increased K(d) and unchanged B(max) value), while biperiden decreased [(3)H]QNB binding (B(max) value) significantly. Furthermore, in an exchange assay for receptor inactivation, trihexyphenidyl binding to muscarinic receptors was exchanged by [(3)H]QNB completely, but biperiden decreased the exchangeable binding of [(3)H]QNB in a dose dependent manner (0.1-100 nM). ...

/LABORATORY ANIMALS: Neurotoxicity/ The purpose of the present study was to make a comparative assessment of potential cognitive effects of benactyzine (0.3 mg/kg), biperiden (0.11 mg/kg), caramiphen (10 mg/kg), procyclidine (3 mg/kg), and trihexyphenidyl (0.12 mg/kg) separately and each in combination with physostigmine (0.1 mg/kg). The results showed that benactyzine, caramiphen, and trihexyphenidyl reduced rats' innate preference for novelty, whereas biperiden and procyclidine did not. When benactyzine, caramiphen, and trihexyphenidyl were combined with physostigmine the cognitive impairment disappeared. This counteracting effect, however, caused changes in locomotor and rearing activities not seen by each drug alone. Acetylcholinesterase inhibitors and anticholinergics used as prophylactics can offset each other, but exceptions are observed in a previous study when a very potent anticholinergic (scopolamine) or a high dose of procyclidine still results in cognitive deficits in spite of coadministration with physostigmine.

Populations at Special RiskThe /apolipoprotein E/ epsilon4 allele in healthy elderly was associated with increased subjective mental slowing after trihexyphenidyl anticholinergic challenge.

Regulatorische Informationen

FDA Requirements · 1 Eintrag

The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed prescription drug products, incl trihexyphenidyl hydrochloride, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. /Trihexyphenidyl hydrochloride/

Sicherheitsdaten

Toxizität
LD50 ipr-mus: 150 mg/kg ARZNAD 21,1727,71
Giftige Stoffe Daten
144-11-6(Hazardous Substances Data)

In common with other antimuscarinic agents, trihexyphenidyl produces an atropine-like blocking action on parasympathetic-innervated peripheral structures, including smooth muscle. In addition, trihexyphenidyl exhibits a direct spasmolytic action on smooth muscle and exhibits weak mydriatic, antisialagogue, and cardiovagal blocking effects. The exact mechanism of action of trihexyphenidyl in parkinsonian syndrome is not understood but may result from blockade of efferent impulses and from central inhibition of cerebral motor centers. In small doses, trihexyphenidyl depresses the CNS but larger doses cause cerebral excitement resembling the signs of atropine toxicity.

In vivo microdialysis was used to study the effect of the non-selective muscarinic antagonist, trihexyphenidyl, on the decarboxylation of levodopa (L-dopa) in the striatum of hemi-Parkinson rats. In normal rats, continuous perfusion of trihexyphenidyl (1 mM) via the microdialysis probe induced a significant increase in striatal dopamine release, followed by a decrease to below baseline values. A similar effect was observed, though less pronounced, in denervated striatum of rats with a unilateral 6-hydroxydopamine lesion of the nigrostriatal pathway. In these hemi-Parkinson rats, continuous striatal perfusion of trihexyphenidyl had no effect on the biotransformation of locally applied L-dopa (2 uM for 20 min) to dopamine in either intact or denervated striatum. However, systemic administration of trihexyphenidyl (1.5 mg/kg ip) produced an attenuation of the L- dopa-induced dopamine release in the intact striatum (contralateral to the lesion) of hemi-Parkinson rats. This effect was absent in the denervated striatum of these animals. We confirmed that L-dopa induces an increase in striatal dopamine output which is influenced by the severity of the dopaminergic denervation. The absence of an effect of trihexyphenidyl locally applied in the striatum, on biotransformation of L-dopa suggests that the site of action of antimuscarinic drugs may not be in the striatum and, therefore, remains unclear.

Biological Half-Life · 3 Einträge

The mean elimination half life of trihexyphenidyl is 3.2 ± 0.3 hours.

Twenty-four male subjects were randomized to receive two oral dosage forms of trihexyphenidyl HCl (alpha-cyclohexyl-alpha-phenyl-1-piperidinepropanol HCl). The dosage regimens were (1) a 5-mg immediate release (IR) tablet given twice daily at time zero and 12 hr later, and (2) two 5-mg sustained-release (SR) capsule formulations given daily. ... The mean elimination half-life (t1/2) was similar (p greater than 0.05) after the SR (10.1 hr) and IR (8.7 hr) formulations. /Trihexylphenidyl hydrochloride/

Using a sensitive radioreceptor assay for anticholinergic drugs, trihexyphenidyl /was assayed/ in human serum and ... its pharmacokinetics following short-term and long-term administration to patients with dystonia /was studied/. ... Elimination followed first-order kinetics and was rapid, with a half-life of 3.7 + or - 0.4 (SEM) hours. There was no relationship between half-life and peak serum level, age, duration of therapy, or etiology or severity of dystonia. ...

Metabolism/Metabolites · 3 Einträge

Data regarding the metabolism of trihexyphenidyl are not readily available. However, it is likely not heavily metabolized.

Benzhexol and three of its metabolites excreted in urine in man have been investigated by glc.--mass spectrometry. Three isomeric hydroxylated metabolites were identified as the 1-(hydroxycyclohexyl)-1-phenyl-3-piperidinopropan-1-ols. 3. The amounts of benzhexol and its identified metabolites have been semiquantitatively determined after a single oral dose in two healthy adults. Approx. 56% of the dose was excreted as the hydroxylated metabolites. The levels of benzhexol excreted were too low to be measured by the techniques used.

Half Life: 3.3-4.1 hours

MeSH Pharmacological Classification · 2 Einträge

Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists.

Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.

Absorption, Distribution and Excretion · 6 Einträge

Trihexyphenidyl is absorbed from the gastrointestinal tract. Trihexyphenidyl reaches a Cmax of 7.2 ng/mL, with a Tmax of 1.3 hours, and an AUC of 201 ng\*h/mL.

Data regarding the route of elimination of trihexyphenidyl are not readily available. However, it is likely eliminated predominantly in the urine.

Using a sensitive radioreceptor assay for anticholinergic drugs, trihexyphenidyl /was assayed/ in human serum and ... its pharmacokinetics following short-term and long-term administration to patients with dystonia /was studied/. Previously untreated patients had a biphasic semilogarithmic plot of serum concentration-time consisting of an initial rapid distribution phase and a later slower elimination phase. Patients on long-term treatment showed only the slower elimination phase. Elimination followed first-order kinetics and was rapid, with a half-life of 3.7 + or - 0.4 (SEM) hours. There was no relationship between half-life and peak serum level, age, duration of therapy, or etiology or severity of dystonia. Although acute anticholinergic side effects paralleled the rise and fall of serum anticholinergic levels, the response of dystonia did not.

Trihexyphenidyl is rapidly absorbed from the GI tract. Following oral administration of trihexyphenidyl hydrochloride tablets, the onset of action occurs within 1 hour, peak effects last 2-3 hours, and the duration of action is 6-12 hours. The metabolic fate of trihexyphenidyl has not been determined; the drug is excreted in the urine, probably as unchanged drug. /Trihexylphenidyl hydrochloride/

The subcellular distribution of biperiden (BP), trihexyphenidyl (TP) and (-)-quinuclidinyl benzylate (QNB) in brain, heart and lung following high dose (3.2 mg/kg) iv administration was investigated in rats. The subcellular distribution of BP or TP used clinically conformed with that of QNB, a typical potent central muscarinic antagonist. The concentration-time courses of the brain subcellular fractions for these drugs were of two types which decreased slowly and in parallel to the plasma concentration. The subcellular distribution in the brain and heart was dependent on the protein amount of each fraction. The percent post-nuclear fraction (P2) of the total concentration in the lung was characteristically about 3-5 times larger than that in the heart. It was elucidated that the distribution in the lung differs from that in the brain and heart, with high affinity which is not dependent on the protein amount in the P2 fraction containing lysosomes. On the other hand, at a low dose (650 ng/kg) of 3H-QNB, each fraction as a percentage of the total concentration in the brain increased in synaptic membrane and synaptic vesicles and decreased in nuclei and cytosol as compared with the high dose. These results show that although the tissue concentration-time courses of anticholinergic drugs appear to decrease simply in parallel to plasma concentration, the subcellular distribution exhibits a variety of patterns among various tissues.

Twenty-four male subjects were randomized to receive two oral dosage forms of trihexyphenidyl HCl (alpha-cyclohexyl-alpha-phenyl-1-piperidinepropanol HCl). The dosage regimens were (1) a 5-mg immediate release (IR) tablet given twice daily at time zero and 12 hr later, and (2) two 5-mg sustained-release (SR) capsule formulations given daily. The number of adverse experiences following the SR formulation were approximately 50% of those for the IR formulation, the peak concentration (Cmax) after the SR formulation was significantly lower (p less than 0.05) than that after the first dose of the IR formulation, and the time to reach Cmax (tmax) was significantly longer after the SR formulation (p less than 0.05). The SR formulation maintained serum concentrations above 50, 60, and 70% of Cmax values for average time periods of 11.7, 9.4, and 5.9 hr, respectively, compared with values of 1.8, 1.2, and 0.9 hr after the IR formulation; the differences were all significant (p less than 0.05). The mean elimination half-life (t1/2) was similar (p greater than 0.05) after the SR (10.1 hr) and IR (8.7 hr) formulations. The statistical power of the study was 98.1% to detect a 20% difference in the area under the curve from time zero to time infinity (AUC0----infinity) between formulations. Although the AUC0----infinity after the SR formulation was statistically smaller (p less than 0.05) than after the IR tablet, the difference was less than 20%. Therefore, the SR formulation was bioequivalent to the IR tablet formulation of trihexyphenidyl. /Trihexylphenidyl hydrochloride/

Cellular LocationsMembrane

Verwendung und Herstellung

Uses · 5 Einträge

Synthetic antispasmodic ... adjunct in the treatment of all forms of parksinonism (postencephalitic, arteriosclerotic, and idiopathic) /Trihexylphenidyl hydrochloride/

THERAP CAT: Antiparkinsonian /Trihexylphenidyl hydrochloride/

MEDICATION

Use (kg; approx.) in Germany (2009): >10

Indicated for the treatment of parkinson's disease and extrapyramidal reactions caused by drugs.

Impurities1-phenyl-3-(piperidine-1-yl)propan-1-one
Methods of Manufacturing · 2 Einträge

ACETOPHENONE & PIPERIDINE ARE CAUSED TO UNDERGO MANNICH CONDENSATION WITH FORMALDEHYDE... 3-PIPERIDINOPROPIOPHENONE THUS PRODUCED IS ISOLATED & SUBJECTED TO TYPICAL GRIGNARD REACTION WITH CYCLOHEXYLMAGNESIUM CHLORIDE TO YIELD...TRIHEXYPHENIDYL BASE. HYDROCHLORIDE IS...PREPD BY...PPTN WITH...HYDROGEN CHLORIDE. /HCL/

Adamson, Wilkinson, US 2682543 (1954 to Burroughs Wellcome); Denton, US 2716121 (1955 to American Cyanamide). /Trihexyphenidyl hydrochloride/

Formulations/Preparations · 2 Einträge

Trade Names. Artane (Lederle), Bentex (Steinhard), Broflex (Bio-Med), Pargitan (KabiVitrum), Parkinane (Lederle), Triphenidone (Toho). /Trihexylphenidyl hydrochloride/

Oral: Elixir: 2 mg/5 mL Trihexyphenidyl Hydrochloride Elixir (Mikart), (Pharmaceutical Associates), (Pharmaceutical Ventures). Tablets: 2 mg Trihexyphenidyl Hydrochloride Tablets (URL), (Vintage), (Watson), (West-Ward); 5 mg Trihexyphenidyl Hydrochloride Tablets (URL), (Vintage), (Watson), (West-Ward). /Trihexypheridyl hydrochloride/

Use ClassificationPharmaceuticals
General Manufacturing InformationTRIHEXYPHENIDYL MAY BE COMBINED WITH OTHER ANTIPARKINSONIAN DRUGS.

Anwendungen

VerwendenAnticholinergic; antiparkinsonian.

Vor- und nachgelagerte Produkte

Vorgelagerte Rohstoffe

PiperidinHydrogenchloridMagnesiumBromcyclohexanAcetophenonParaformaldehyde

Anbieter32 Anbieter

北京华美互利生物化工010-56205725 · [email protected]
Hebei Chuanghai Biotechnology Co., Ltd+86-17732866630 · [email protected]
上海麦克林生化科技股份有限公司021-50706066 15221275939 · [email protected]
河北创海生物科技有限公司+86-86-13131129325 · [email protected]
江苏艾康生物医药研发有限公司025-025-66113011 15955137747 · [email protected]
Dayang Chem (Hangzhou) Co.,Ltd.+86-0571-88938639 17705817739 · [email protected]
Hebei Yanxi Chemical Co., Ltd.+86-17531190177 · [email protected]
LGM Pharma1-(800)-881-8210 · [email protected]
Syntechem Co.,Ltd[email protected]
上海隆盛化工有限公司58099637 13585536065 · [email protected]
宝鸡缔都医药化工有限公司029-81145305 17791533577 · [email protected]
天津普西唐生物医药科技有限公司010-60605840 · [email protected]
青岛海智微元生物科技有限公司18317699790 18317699790 · [email protected]
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