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Pharmacologic Category
Anti-Parkinson Agent, Anticholinergic; Anticholinergic Agent
Dosing: Adult
Parkinson disease: 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
Extrapyramidal side effects: 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 daily in divided doses
* See Dosage and Administration in AHFS Essentials for additional information.
Dosing: Geriatric
Avoid use (Beers Criteria [AGS 2019]).
Dosing: Renal Impairment: Adult
There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.
Dosing: Hepatic Impairment: Adult
There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.
Use: Labeled Indications
Note: Not available in the US
Parkinson disease: Treatment of parkinsonism, including postencephalitic, arteriosclerotic, and idiopathic types.
Extrapyramidal side effects: Relieves symptoms (eg, dystonia, dyskinesia, akathisia, and parkinsonism) induced by phenothiazine or rauwolfia compounds during treatment of mental depression.
* See Uses in AHFS Essentials for additional information.
Clinical Practice Guidelines
Canadian Neurological Sciences Federation, “Canadian Guidelines on Parkinson’s Disease,” 2012
Administration: Oral
Administer after meals to minimize stomach upset and anticholinergic effects.
Dietary Considerations
Should be taken after meals to minimize stomach upset and anticholinergic effects.
Storage/Stability
Store at 15°C to 30°C (59°F to 86°F).
Medication Safety Issues
Geriatric patients: High-risk medication:
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, alcoholics, 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.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Special populations:
• Elderly: Frequently develop increased sensitivity and require strict dosage regulation - side effects may be more severe in elderly patients with atherosclerotic changes.
* See Cautions in AHFS Essentials for additional information.
Geriatric Considerations
Anticholinergic agents are generally not well tolerated in the elderly and their use should be avoided when possible. In the elderly, anticholinergic agents should not be used as prophylaxis against extrapyramidal symptoms.
Pregnancy Considerations
Safe use during pregnancy has not been established.
Breast-Feeding Considerations
It is not known if procyclidine is excreted in breast milk.
Adverse Reactions
Frequency not defined.
Central nervous system: Dizziness
Dermatologic: Skin rash
Gastrointestinal: Constipation, epigastric distress, nausea, vomiting, xerostomia
Hypersensitivity: Hypersensitivity reaction
Neuromuscular & skeletal: Weakness
Ophthalmic: Blurred vision, mydriasis
<1%, postmarketing, and/or case reports: Suppurative parotitis (acute)
* See Cautions in AHFS Essentials for additional information.
Toxicology
Metabolism/Transport Effects
None known.
Drug Interactions Open Interactions
Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy
Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy
Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Exceptions: Cannabidiol. Risk C: Monitor therapy
Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy
Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination
CloZAPine: Anticholinergic Agents may enhance the constipating effect 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
Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination
Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy
Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy
Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination
Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy
Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination
Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy
Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy
Opioid Agonists: Anticholinergic Agents may enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Risk C: Monitor therapy
Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect 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 combination
Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Risk X: Avoid combination
Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk D: Consider therapy modification
Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy
Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination
Secretin: Anticholinergic Agents may diminish the therapeutic effect 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
Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy
Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination
Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy
Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Monitoring Parameters
Symptoms of EPS or Parkinson's disease, pulse, anticholinergic effects (ie, CNS, bowel and bladder function)
Product Availability
Not available in the US
Dosage Forms: Canada
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Elixir, Oral:
Generic: 2.5 mg/5 mL (500 mL)
Tablet, Oral:
Generic: 2.5 mg, 5 mg
Anatomic Therapeutic Chemical (ATC) Classification
- N04AA04
Generic Available (US)
Yes
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
Pharmacodynamics/Kinetics
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)
Local Anesthetic/Vasoconstrictor Precautions
No information available to require special precautions
Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation) and dry throat and nose. Prolonged use of antidyskinetics may decrease or inhibit salivary flow, contributing to discomfort and dental disease (ie, caries, oral candidiasis, and periodontal disease).
Effects on Bleeding
No information available to require special precautions
Related Information
Index Terms
Procyclidine Hydrochloride
References
2019 American Geriatrics Society Beers Criteria Update Expert Panel. American Geriatrics Society 2019 updated AGS Beers Criteria for potentially inappropriate medication use in older adults. J Am Geriatr Soc. 2019;67(4):674-694. doi: 10.1111/jgs.15767.[PubMed 30693946]
Brocks DR, “Anticholinergic Drugs Used in Parkinson’s Disease: An Overlooked Class of Drugs from a Pharmacokinetic Perspective,” J Pharm Pharm Sci, 1999, 2(2):39-46.[PubMed 10952768]
Feinberg M, “The Problems of Anticholinergic Adverse Effects in Older Patients,” Drugs Aging, 1993, 3(4):335-48.[PubMed 8369593]
Rogiers V, Paeme G, Sonck W, et al, “Metabolism of Procyclidine in Isolated Rat Hepatocytes,” Xenobiotica, 1987, 17(7):849-57.[PubMed 3660855]
Procyclidine [product monograph]. Montreal, Quebec, Canada: Pendopharm, Division of Pharmascience Inc; February 2014
Whiteman PD, Fowle AS, Hamilton MJ, et al, “Pharmacokinetics and Pharmacodynamics of Procyclidine in Man,” Eur J Clin Pharmacol, 1985, 28(1):73-8.[PubMed 3987788]
Brand Names: International
Akinetic (BD); Cyclid (BD); Emadrin (PK); Kemadrin (AE, AT, AU, BB, BD, BE, BG, BH, BM, BS, BZ, CH, CY, CZ, DK, EE, EG, ES, FI, FR, GB, GR, GY, HN, HU, IE, IL, IN, IQ, IR, IT, JM, JO, KW, LB, LU, LY, MT, NL, NZ, OM, PT, QA, RU, SA, SE, SI, SK, SR, SY, TR, TT, UY, YE); Osnervan (DE); Picidin (BD); Proimer (KR); Youngproma (KR)
Last Updated 2/20/20
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