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Procyclidine (United States: Not available): Drug information

Procyclidine (United States: Not available): Drug information
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For additional information see "Procyclidine (United States: Not available): Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: Canada
  • PDP-Procyclidine [DSC]
Pharmacologic Category
  • Anti-Parkinson Agent, Anticholinergic;
  • Anticholinergic Agent
Dosing: Adult
Extrapyramidal symptoms

Extrapyramidal symptoms:

Note: Anticholinergic agents are not recommended for the treatment of akathisia or tardive dyskinesia (Ref). Duration of therapy is based on the severity of extrapyramidal symptom reaction, pharmacologic profile of the causative agent (eg, half-life, adverse effects), and patient risk factors (Ref). Some experts recommend attempting taper and discontinuation after several weeks to months (Ref).

Oral: Initial: 2.5 mg 3 times daily after meals; increase in 2.5 mg daily increments until symptomatic relief; usual dose: 10 to 20 mg/day in divided doses.

Parkinsonism

Parkinsonism: Oral: Initial: 2.5 mg 3 times daily after meals; if tolerated, gradually increase to 5 mg 3 times daily after meals and 5 mg at bedtime as needed. Lower dosages may be effective in some patients; if bedtime dose is not tolerated, may omit and administer total daily dose in 3 equally divided daytime doses.

Conversion from alternative therapy: Gradually initiate procyclidine 2.5 mg 3 times daily (may be used to replace all or part of alternative therapy); titrate dosage up (procyclidine) and/or down (alternative therapy) until satisfactory effect is achieved with procyclidine monotherapy.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.

Dosing: Liver Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.

Dosing: Older Adult

Avoid use (Ref).

Adverse Reactions

The following adverse drug reactions are derived from product labeling unless otherwise specified.

Frequency not defined:

Cardiovascular: Tachycardia (Holloman 1997)

Gastrointestinal: Constipation (Holloman 1997), epigastric distress, nausea, vomiting, xerostomia (Holloman 1997)

Genitourinary: Urinary retention (Holloman 1997)

Hypersensitivity: Hypersensitivity reaction

Nervous system: Dizziness, memory impairment (Hollman 1997), myasthenia

Ophthalmic: Blurred vision (Holloman 1997), mydriasis

Contraindications

Angle-closure glaucoma

Warnings/Precautions

Concerns related to adverse effects:

• Anhidrosis/hyperthermia: Anticholinergic agents may cause anhidrosis and hyperthermia, which may be severe; use with caution in hot weather or during exercise. The risk is increased in hot environments, particularly in the elderly, patients with alcohol use disorder, patients with CNS disease, and those with prolonged outdoor exposure.

• CNS effects: May be associated with restlessness, confusion, hallucinations, or other CNS effects, particularly in the elderly and generally at higher dosages; intensification of symptoms or toxic psychosis may occur in patients with mental disorders. Dose reductions/discontinuation of therapy may be necessary. May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with tachycardia, cardiac arrhythmias, hypertension, or hypotension.

• GI obstruction: Use with caution in patients with obstructive disease of the GI.

• Hepatic impairment: Use with caution in patients with hepatic impairment.

• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture or retention.

• Renal impairment: Use with caution in patients with renal impairment.

• Tardive dyskinesia: Not recommended for use in patients with tardive dyskinesia unless concomitant Parkinson disease or tardive dystonia exists (Kang 1986).

Special populations:

• Older adult: Frequently develop increased sensitivity and require strict dosage regulation - side effects may be more severe in older adult patients with atherosclerotic changes.

Product Availability

Not available in the US

Generic Equivalent Available: US

Yes

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral:

Generic: 2.5 mg [DSC], 5 mg [DSC]

Administration: Adult

Oral: Administer after meals to minimize stomach upset and anticholinergic effects.

Use: Labeled Indications

Note: Not available in the United States.

Extrapyramidal symptoms: Management of medication-induced extrapyramidal symptoms.

Parkinsonism: Treatment of parkinsonism, including postencephalitic, arteriosclerotic, and idiopathic types.

Medication Safety Issues
Older adult: high-risk medication:

Beers Criteria: Avoid for the prevention or treatment of extrapyramidal symptoms caused by antipsychotics. In the treatment of Parkinson disease, more effective agents are available (Beers Criteria [AGS 2023]).

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Acetylcholinesterase Inhibitors: May decrease therapeutic effects of Agents with Clinically Relevant Anticholinergic Effects. Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Acetylcholinesterase Inhibitors. Risk C: Monitor

Aclidinium: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk X: Avoid

Acrivastine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Amantadine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Benperidol: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Benperidol. Risk C: Monitor

Benztropine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Benztropine. Risk C: Monitor

Betel Nut: May decrease therapeutic effects of Procyclidine. Risk C: Monitor

Biperiden: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Biperiden. Risk C: Monitor

Bornaprine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Bornaprine. Risk C: Monitor

Botulinum Toxin-Containing Products: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Bromperidol: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Bromperidol. Risk C: Monitor

Buclizine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Buclizine. Risk C: Monitor

Cannabinoid-Containing Products: Agents with Clinically Relevant Anticholinergic Effects may increase tachycardic effects of Cannabinoid-Containing Products. Risk C: Monitor

Chlorprothixene: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Chlorprothixene. Risk C: Monitor

Cimetropium: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Cimetropium. Risk X: Avoid

CloZAPine: Agents with Clinically Relevant Anticholinergic Effects may increase constipating effects of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider Therapy Modification

Cyclizine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Darifenacin: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Darifenacin. Risk C: Monitor

Dicyclomine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Dicyclomine. Risk C: Monitor

Dimethindene (Systemic): Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Dimethindene (Systemic). Risk C: Monitor

DroNABinol: Agents with Clinically Relevant Anticholinergic Effects may increase tachycardic effects of DroNABinol. Risk X: Avoid

Eluxadoline: Agents with Clinically Relevant Anticholinergic Effects may increase constipating effects of Eluxadoline. Risk X: Avoid

Fesoterodine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Fesoterodine. Risk C: Monitor

FluPHENAZine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Gastrointestinal Agents (Prokinetic): Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Gastrointestinal Agents (Prokinetic). Risk C: Monitor

Gepotidacin: May decrease anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Glucagon: Agents with Clinically Relevant Anticholinergic Effects may increase adverse/toxic effects of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor

Glycopyrrolate (Oral Inhalation): Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Glycopyrrolate (Oral Inhalation). Risk X: Avoid

Glycopyrrolate (Systemic): Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Glycopyrrolate (Systemic). Risk C: Monitor

Glycopyrronium (Topical): May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk X: Avoid

Ipratropium (Nasal): May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Ipratropium (Oral Inhalation): May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk X: Avoid

Itopride: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Itopride. Risk C: Monitor

Levosulpiride: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Levosulpiride. Risk X: Avoid

Lisuride: Procyclidine may increase adverse/toxic effects of Lisuride. Risk X: Avoid

Maprotiline: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Maprotiline. Risk C: Monitor

Melperone: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Metergoline: May increase adverse/toxic effects of Anticholinergic Anti-Parkinsonian Agents. Risk C: Monitor

Methotrimeprazine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Methotrimeprazine. Risk C: Monitor

Methscopolamine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Methscopolamine. Risk C: Monitor

Mirabegron: Agents with Clinically Relevant Anticholinergic Effects may increase adverse/toxic effects of Mirabegron. Risk C: Monitor

Nitroglycerin: Agents with Clinically Relevant Anticholinergic Effects may decrease absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor

OLANZapine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of OLANZapine. Risk C: Monitor

Opioid Agonists: Agents with Clinically Relevant Anticholinergic Effects may increase adverse/toxic effects of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Risk C: Monitor

Opipramol: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Oxatomide: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk X: Avoid

OxyBUTYnin: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of OxyBUTYnin. Risk C: Monitor

PARoxetine: May increase serum concentration of Procyclidine. Risk C: Monitor

Perazine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Perphenazine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Perphenazine. Risk C: Monitor

Potassium Chloride: Agents with Clinically Relevant Anticholinergic Effects may increase ulcerogenic effects of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid

Potassium Citrate: Agents with Clinically Relevant Anticholinergic Effects may increase ulcerogenic effects of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid

Pramlintide: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. These effects are specific to the GI tract. Risk X: Avoid

Promethazine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Promethazine. Risk C: Monitor

Propantheline: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Propantheline. Risk C: Monitor

Propiverine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

QuiNIDine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Ramosetron: Agents with Clinically Relevant Anticholinergic Effects may increase constipating effects of Ramosetron. Risk C: Monitor

Revefenacin: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Revefenacin. Risk X: Avoid

Rivastigmine: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Rivastigmine. Rivastigmine may decrease therapeutic effects of Agents with Clinically Relevant Anticholinergic Effects. Management: Use of rivastigmine with an anticholinergic agent is not recommended unless clinically necessary. If the combination is necessary, monitor for reduced anticholinergic effects. Risk D: Consider Therapy Modification

Scopolamine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Scopolamine. Risk C: Monitor

Secretin: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider Therapy Modification

Sofpironium: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Sofpironium. Risk X: Avoid

Thiazide and Thiazide-Like Diuretics: Agents with Clinically Relevant Anticholinergic Effects may increase serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor

Thiothixene: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Thiothixene. Risk C: Monitor

Tiapride: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Tiapride. Risk C: Monitor

Tiotropium: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Tiotropium. Risk X: Avoid

Tolterodine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Tolterodine. Risk C: Monitor

Topiramate: Agents with Clinically Relevant Anticholinergic Effects may increase adverse/toxic effects of Topiramate. Risk C: Monitor

Tricyclic Antidepressants: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Tricyclic Antidepressants. Risk C: Monitor

Trimethobenzamide: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Trimethobenzamide. Risk C: Monitor

Trospium: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Trospium. Risk C: Monitor

Umeclidinium: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk X: Avoid

Zuclopenthixol: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Zuclopenthixol. Risk C: Monitor

Pregnancy Considerations

Safe use during pregnancy has not been established.

Breastfeeding Considerations

It is not known if procyclidine is present in breast milk.

Dietary Considerations

Should be taken after meals to minimize stomach upset and anticholinergic effects.

Monitoring Parameters

Heart rate, anticholinergic effects (ie, CNS, bowel and bladder function).

Mechanism of Action

Thought to act by blocking excess acetylcholine at cerebral synapses; many of its effects are due to its pharmacologic similarities with atropine; it exerts an antispasmodic effect on smooth muscle, is a potent mydriatic; inhibits salivation

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: 45 to 60 minutes (Whiteman 1985)

Duration: Significant autonomic effects have been observed up to 12 hours (Whiteman 1985)

Distribution: Vd: 1 L/kg (Whiteman 1985)

Metabolism: Hydroxylation of the alicyclic groups (Brocks 1999)

Bioavailability: ~75% (Whiteman 1985)

Half-life elimination: ~12.6 hours (Whiteman 1985)

Time to peak: ~1.1 hour (Whiteman 1985)

Excretion: Urine (predominantly as metabolites) (Whiteman 1985)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Kemadrin;
  • (AT) Austria: Kemadrin;
  • (AU) Australia: Kemadrin;
  • (BD) Bangladesh: Kdrine | Kemadrin | Opsodrin | Parkaid | Perkinil;
  • (BE) Belgium: Kemadrin;
  • (CH) Switzerland: Kemadrin;
  • (CZ) Czech Republic: Kemadrin;
  • (DE) Germany: Osnervan;
  • (EG) Egypt: Procykinol;
  • (ES) Spain: Kemadren;
  • (FI) Finland: Kemadrin;
  • (FR) France: Kemadrine;
  • (GB) United Kingdom: Arpicolin | Kemadrin | Muscinil | Procyclidine | Procyclidine aps | Procyclidine berk | Procyclidine cox | Procyclidine dc | Procyclidine kent | Procyclidine opus;
  • (HU) Hungary: Kemadrin;
  • (IE) Ireland: Arpicolin | Kemadrin | Procyclidine;
  • (IL) Israel: Kemadrin;
  • (IN) India: Aldine | Axeps | Cyclid | Dine | Kemadrin | Lepark | Modin | Parklid | Pcdine | Procydin | Prolid | Trodin;
  • (IT) Italy: Kemadrin;
  • (JO) Jordan: Kemadrin;
  • (JP) Japan: Kemadrin;
  • (KR) Korea, Republic of: Paroma | Pharma procyclidine | Proimer | Youngproma;
  • (KW) Kuwait: Kemadrin;
  • (LB) Lebanon: Kemadrin;
  • (LT) Lithuania: Kemadrin;
  • (LU) Luxembourg: Kemadrin;
  • (LV) Latvia: Kemadrin;
  • (MY) Malaysia: Kemadrin;
  • (NL) Netherlands: Kemadrin;
  • (NZ) New Zealand: Kemadrin;
  • (PK) Pakistan: Cyclidine | Epsent | Kemadrin | Kempro | Oclidin | Procholidin | Procye | Prosyclidine | Zyclidine;
  • (PR) Puerto Rico: Kemadrin;
  • (QA) Qatar: Kemadrin;
  • (SA) Saudi Arabia: Kemadrin;
  • (SE) Sweden: Kemadrin;
  • (SI) Slovenia: Kemadrin;
  • (SK) Slovakia: Kemadrin;
  • (TN) Tunisia: Kemadrine;
  • (UY) Uruguay: Kemadrin
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  7. Kreyenbuhl J, Buchanan RW, Dickerson FB, Dixon LB; Schizophrenia Patient Outcomes Research Team (PORT). The Schizophrenia Patient Outcomes Research Team (PORT): updated treatment recommendations 2009. Schizophr Bull. 2010;36(1):94-103. doi: 10.1093/schbul/sbp130 [PubMed 19955388]
  8. Procyclidine [product monograph]. Montreal, Quebec, Canada: Pendopharm, Division of Pharmascience Inc; February 2014
  9. Whiteman PD, Fowle AS, Hamilton MJ, et al. Pharmacokinetics and pharmacodynamics of procyclidine in man. Eur J Clin Pharmacol. 1985;28(1):73-78. [PubMed 3987788]
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