Details
Stereochemistry | RACEMIC |
Molecular Formula | C19H29NO.ClH |
Molecular Weight | 323.901 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.OC(CCN1CCCC1)(C2CCCCC2)C3=CC=CC=C3
InChI
InChIKey=ZFSPFXJSEHCTTR-UHFFFAOYSA-N
InChI=1S/C19H29NO.ClH/c21-19(17-9-3-1-4-10-17,18-11-5-2-6-12-18)13-16-20-14-7-8-15-20;/h1,3-4,9-10,18,21H,2,5-8,11-16H2;1H
Procyclidine is a muscarinic antagonist that crosses the blood-brain. Procyclidine hydrochloride (brand name Kemadrin) is a synthetic antispasmodic compound of relatively low toxicity. It has been shown to be useful for the symptomatic treatment of parkinsonism (paralysis agitans) and extrapyramidal dysfunction caused by tranquilizer therapy. Procyclidine hydrochloride was developed at The Wellcome Research Laboratories as the most promising of a series of antiparkinsonism compounds produced by chemical modification of antihistamines. Kemadrin is indicated in the treatment of parkinsonism including the postencephalitic, arteriosclerotic, and idiopathic types. Partial control of the parkinsonism symptoms is the usual therapeutic accomplishment. Procyclidine hydrochloride is usually more efficacious in the relief of rigidity than tremor; but tremor, fatigue, weakness, and sluggishness are frequently beneficially influenced. It can be substituted for all the previous medications in mild and moderate cases. For the control of more severe cases, other drugs may be added to procyclidine therapy as indications warrant. The mechanism of action is unknown. It is thought that procyclidine acts by blocking central cholinergic receptors, and thus balancing cholinergic and dopaminergic activity in the basal ganglia. Pharmacologic tests have shown that procyclidine hydrochloride has an atropine-like action and exerts an antispasmodic effect on smooth muscle. It is a potent mydriatic and inhibits salivation. It has no sympathetic ganglionblocking activity in doses as high as 4 mg/kg, as measured by the lack of inhibition of the response of the nictitating membrane to preganglionic electrical stimulation.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL216 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2253700 |
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Target ID: CHEMBL245 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1426023 |
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Target ID: CHEMBL211 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2253700 |
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Target ID: CHEMBL1821 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2253700 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | KEMADRIN Approved UseKEMADRIN (procyclidine hydrochloride) is indicated in the treatment of parkinsonism including the postencephalitic, arteriosclerotic, and idiopathic types. Partial control of the parkinsonism symptoms is the usual therapeutic accomplishment. Procyclidine hydrochloride is usually more efficacious in the relief of rigidity than
tremor; but tremor, fatigue, weakness, and sluggishness are frequently beneficially influenced. It can be substituted for all the previous medications in mild and moderate cases. For the control of more severe cases, other drugs may be added to procyclidine therapy as indications warrant. Launch Date1955 |
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Primary | KEMADRIN Approved UseKEMADRIN (procyclidine hydrochloride) is indicated in the treatment of parkinsonism including the postencephalitic, arteriosclerotic, and idiopathic types. Partial control of the parkinsonism symptoms is the usual therapeutic accomplishment. Procyclidine hydrochloride is usually more efficacious in the relief of rigidity than
tremor; but tremor, fatigue, weakness, and sluggishness are frequently beneficially influenced. It can be substituted for all the previous medications in mild and moderate cases. For the control of more severe cases, other drugs may be added to procyclidine therapy as indications warrant. Launch Date1955 |
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Primary | KEMADRIN Approved UseKEMADRIN (procyclidine hydrochloride) is indicated in the treatment of parkinsonism including the postencephalitic, arteriosclerotic, and idiopathic types. Partial control of the parkinsonism symptoms is the usual therapeutic accomplishment. Procyclidine hydrochloride is usually more efficacious in the relief of rigidity than
tremor; but tremor, fatigue, weakness, and sluggishness are frequently beneficially influenced. It can be substituted for all the previous medications in mild and moderate cases. For the control of more severe cases, other drugs may be added to procyclidine therapy as indications warrant. Launch Date1955 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
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116 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3987788 |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROCYCLIDINE HYDROCHLORIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
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2007 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3987788 |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROCYCLIDINE HYDROCHLORIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2705 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3987788 |
10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PROCYCLIDINE HYDROCHLORIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
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12.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3987788 |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROCYCLIDINE HYDROCHLORIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
11.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3987788 |
10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PROCYCLIDINE HYDROCHLORIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
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10 mg single, intravenous Dose: 10 mg Route: intravenous Route: single Dose: 10 mg Sources: |
healthy, 22-48 years n = 6 Health Status: healthy Age Group: 22-48 years Sex: M+F Population Size: 6 Sources: |
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250 mg single, oral Overdose Dose: 250 mg Route: oral Route: single Dose: 250 mg Co-administed with:: amoxapine(2500 mg) Sources: |
unhealthy, 26 years n = 1 Health Status: unhealthy Condition: schizo-affective disorder Age Group: 26 years Sex: F Population Size: 1 Sources: |
Other AEs: Pancreatitis... |
15 mg single, oral Highest studied dose |
unhealthy n = 13 Health Status: unhealthy Condition: Schizophrenia Population Size: 13 Sources: |
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250 mg single, oral Highest studied dose|Studied dose |
unhealthy n = 9 Health Status: unhealthy Condition: duodenal ulcer Population Size: 9 Sources: |
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50 mg single, intramuscular Dose: 50 mg Route: intramuscular Route: single Dose: 50 mg Sources: |
unhealthy n = 3 |
AEs
AE | Significance | Dose | Population |
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Pancreatitis | 1 patient | 250 mg single, oral Overdose Dose: 250 mg Route: oral Route: single Dose: 250 mg Co-administed with:: amoxapine(2500 mg) Sources: |
unhealthy, 26 years n = 1 Health Status: unhealthy Condition: schizo-affective disorder Age Group: 26 years Sex: F Population Size: 1 Sources: |
PubMed
Title | Date | PubMed |
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Death attributed to ventricular arrhythmia induced by thioridazine in combination with a single Contac C capsule. | 1978 Oct 7 |
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Sleep disturbance associated with fluphenazine HCl: a case report. | 1979 Jul |
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Ethopropazine and benztropine in neuroleptic-induced parkinsonism. | 1979 Mar |
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Toxic neurological reaction to lithium/thioridazine. | 1983 Apr 2 |
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Neuroleptic malignant syndrome. | 1983 Jun 18 |
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Effects of mianserin in neuroleptic-induced parkinsonism. | 1986 |
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Pimozide-induced depression associated with polyuria and polydipsia. | 1992 Apr |
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Anti-nicotinic properties of anticholinergic antiparkinson drugs. | 1998 Nov |
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Effects of advanced candidate anticonvulsants under two rodent models of 'counting'. | 2001 Dec |
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Combination anticonvulsant treatment of soman-induced seizures. | 2001 Dec |
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Nasal absorption of procyclidine in rats and dogs. | 2001 Jun |
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Physostigmine as treatment for severe CNS anticholinergic toxicity. | 2001 Sep |
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Acute dystonic reaction in an elderly patient with mood disorder after titration of paroxetine: possible mechanisms and implications for clinical care. | 2002 Dec |
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Pharmacological agents, hippocampal EEG, and anticonvulsant effects on soman-induced seizures in rats. | 2003 Jun |
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Cognitive side effects in rats caused by pharmacological agents used to prevent soman-induced lethality. | 2004 Jan 12 |
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Development of a screening method for the most commonly abused anticholinergic drugs in Jordan; trihexyphenidyl, procyclidine and biperiden. | 2004 Oct |
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Self-reported parkinsonian symptoms in the EPIC-Norfolk cohort. | 2005 Aug 24 |
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Soman-induced convulsions in rats terminated with pharmacological agents after 45 min: neuropathology and cognitive performance. | 2005 Jan |
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Protection by a transdermal patch containing physostigmine and procyclidine of soman poisoning in dogs. | 2005 Nov 21 |
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Primary care use of antipsychotic drugs: an audit and intervention study. | 2005 Nov 29 |
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Abdominal pain with rigidity secondary to the anti-emetic drug metoclopramide. | 2006 May |
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Pharmacological therapies against soman-induced seizures in rats 30 min following onset and anticonvulsant impact. | 2006 Oct 24 |
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The combination of donepezil and procyclidine protects against soman-induced seizures in rats. | 2007 Apr 15 |
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Stuttering priapism--a review of the therapeutic options. | 2008 Aug |
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Amisulpride plus valproate vs haloperidol plus valproate in the treatment of acute mania of bipolar I patients: a multicenter, open-label, randomized, comparative trial. | 2008 Jun |
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Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method. | 2010 Dec |
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Identification of neuronal target areas for nerve agents and specification of receptors for pharmacological treatment. | 2010 Dec |
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Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. | 2011 Jul 14 |
Patents
Sample Use Guides
For initial treatment is 2.5 mg administered three times daily after meals. If well tolerated, this dose may be gradually increased to 5 mg three times a day and occasionally 5 mg given before retiring. In some cases smaller doses may be employed with good therapeutic results.
Route of Administration:
Oral
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NCI_THESAURUS |
C38149
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CHEMBL86715
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m9151
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CQC932Z7YW
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216-141-8
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SUB04054MIG
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Procyclidine hydrochloride
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100000085102
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DBSALT001008
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142443
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207841
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C47689
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757293
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DTXSID8045357
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1567004
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1508-76-5
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ACTIVE MOIETY
SUBSTANCE RECORD