Procyclidine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Drug-induced extrapyramidal symptoms, Parkinsonism
Adult: Initially, 2.5 mg tid, increased gradually by 2.5-5 mg every 2-3 days if required or by 2.5 mg daily for drug-induced extrapyramidal symptoms. Maintenance: 10-30 mg daily in 3-4 divided doses. Up to 60 mg daily may be required in some cases.
Elderly: Lower doses are required.

Parenteral
Drug-induced extrapyramidal symptoms, Parkinsonism
Adult: Emergency cases: IV: 5-10 mg, higher doses may be needed; IM: 5-10 mg as a single dose, may repeat after 20 min if needed. Max: 20 mg/day.
Elderly: Lower doses are required.
Chống chỉ định
Patient w/ myasthenia gravis, untreated urinary retention, closed angle glaucoma, GI obstruction.
Thận trọng
Patient w/ mental disorders, CV disease (e.g. tachycardia, cardiac arrhythmias, hypertension, hypotension). Hepatic and renal impairment. Avoid abrupt withdrawal. Elderly. Pregnancy and lactation.
Phản ứng phụ
Dry mouth, mydriasis, blurred vision, lightheadedness, giddiness, disorientation, GI effects (e.g. nausea, vomiting, epigastric distress, constipation), allergic reaction (e.g. rash), muscular weakness; vertigo, confusion, hallucinations at high doses; tremor, acute suppurative parotitis.
Thông tin tư vấn bệnh nhân
This drug may cause blurred vision, dizziness, confusion or disorientation, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor symptoms of extrapyramydal syndrome or Parkinson's disease, pulse, anticholinergic effects (e.g. CNS, bowel and bladder function).
Quá liều
Symptoms: Stimulant effects (e.g. agitation, restlessness, confusion, sleeplessness lasting up to ≥24 hr; euphoria, anxiety, aggressive behaviour; dilated pupils that are nonreactive to light; disorientation (lasting for 1-4 days); CNS depression (e.g. somnolence, reduced consciousness, and occasionally coma); tachycardia. Management: Use activated charcoal to reduce absorption w/in 1-2 hr of ingestion (or possibly longer in view of its likely effects on gastric motility). Consider gastric lavage only if clinically appropriate. May give diazepam inj if convulsions occur.
Tương tác
Increased plasma concentrations w/ paroxetine. Enhanced anticholinergic action w/ MAOIs and other anticholinergic drugs. Reduced therapeutic effect w/ cholinergic drugs. May antagonise the effect of parasympathomimetic agents. May reduce the absorption and therapeutic effect of sublingual or buccal nitrate tab. May reduce the efficacy of levodopa. May antagonise the GI effects of cisapride, domperidone and metoclopramide. May potentiate the vagolytic effects of quinidine. May reduce the absorption of ketoconazole.
Food Interaction
Alcohol may potentiate the CNS effects of procyclidine.
Tác dụng
Description: Procyclidine is postulated to act by blocking excess acetylcholine at the muscarinic receptor; many of its effects are due to its pharmacologic similarities w/ atropine.
Onset: W/in 5-20 min (IV).
Duration: Up to 4 hr (IV).
Pharmacokinetics:
Absorption: Adequately absorbed from the GI tract. Bioavailability: 75% (oral). Time to peak plasma concentration: Approx 1 hr.
Distribution: Disappears rapidly from the tissues. Volume of distribution: 1 L/kg.
Metabolism: Undergoes hepatic metabolism (approx one-fifth of oral dose) by CYP450 isoenzymes, then conjugated w/ glucuronic acid.
Excretion: Via urine as unchanged drug (small amounts). Plasma elimination half-life: Approx 12 hr (oral/IV).
Đặc tính

Chemical Structure Image
Procyclidine

Source: National Center for Biotechnology Information. PubChem Database. Procyclidine, CID=4919, https://pubchem.ncbi.nlm.nih.gov/compound/Procyclidine (accessed on Jan. 23, 2020)

Bảo quản
Store between 15-30°C. Protect from moisture.
Phân loại MIMS
References
Anon. Procyclidine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 18/11/2014.

Buckingham R (ed). Procyclidine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 18/11/2014.

Kemadrin 5 mg/mL Solution for Injection (Auden Mckenzie Ltd - Pharma Division). MHRA. https://products.mhra.gov.uk/. Accessed 18/11/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Procyclidine Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 18/11/2014.

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