Procyclidine; Uses, Dosage, Side Effects, Drug Interactions Procyclidine is a muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism. It is only found in individuals that have used or taken this drug. It is a muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism. [PubChem]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. Many of its effects are due to its pharmacologic similarities with atropine. Procyclidine exerts an antispasmodic effect on smooth muscle and may produce mydriasis and reduction in salivation. Procyclidine is an anticholinergic drug principally used for the treatment of drug-induced parkinsonism, akathisia and acute dystonia; Parkinson disease; and idiopathic or secondary dystonia. Mechanism of Action of Procyclidine 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. Many of its effects are due to its pharmacologic similarities with atropine. Procyclidine exerts an antispasmodic effect on smooth muscle and may produce mydriasis and reduction in salivation. Procyclidine has an atropine-like action on parasympathetic-innervated peripheral structures including smooth muscle. Its antispasmodic effects are thought to be related to the blockage of central cholinergic receptors M1, M2, and M4. It is used to treat symptomatic Parkinsonism and extrapyramidal dysfunction caused by antipsychotic agents. Indications of Procyclidine Parkinsonism Parkinsonian Syndromes Extra-pyramidal symptoms Treatment of all forms of Parkinson’s Disease, as well as control of extrapyramidal reactions induced by antipsychotic agents. It is used in patients with parkinsonism and akathisia, and to reduce the side effects of antipsychotic treatment given for schizophrenia. Procyclidine is also a second-line drug for the treatment of Parkinson’s disease. It improves tremor but not rigidity or bradykinesia. Procyclidine is also sometimes used for the treatment of dystonia (but not tardive dyskinesia), a rare disorder that causes abnormal muscle contraction, resulting in twisting postures of limbs, trunk, or face. Contra-Indications of Procyclidine Myasthenia gravis Closed angle glaucoma High blood pressure Coronary artery disease Chronic heart failure Chronic lung disease A Change in saliva secretion Failure of esophageal sphincter to relax Inflammation of esophagus from backflow of stomach Acid Stomach ulcer Narrowing of the opening between the stomach and small Intestine A hiatal hernia Ulcerated colon Severe ulcerative colitis Toxic megacolon Paralysis of the intestines Stomach or intestine blockage Atony of colon Liver problems Kidney disease with a reduction in kidney function Blockage of the urinary bladder Urinary tract blockage Enlarged prostate Down syndrome Drowsiness Fast heartbeat Cannot empty bladder Toxin from microorganisms causing diarrhea Bleeding causing blood pressure or heart problems Dysreflexia Dosage of Procyclidine Strengths: 2.5 mg, 5 mg 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. 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. Side Effects of Procyclidine The most common nausea, vo miting, stomach pain, indigestion, constipation, diarrhea; fever, flu symptoms, cough, sore throat, sneezing, runny nose; nervousness, depression, sleep problems (insomnia); a headache, dizziness, drowsiness, memory problems, unusual thoughts; rash, hair loss, bruising; weakness, tremors, problems with balance or walking; swelling in your hands or feet; vision problems, ringing in your ears; or changes in appetite, weight gain. More common Black, tarry stools bleeding gums bloating or swelling of the face, arms, hands, lower legs, or feet blood in the urine or stools confusion a cough or hoarseness crying delusions dementia depersonalization diarrhea difficult or labored breathing dysphoria euphoria fever or chills Less common Abnormal dreams the absence of or decrease in body movement anxiety bloody nose bloody or cloudy urine blurred vision burning, crawling, itching, numbness, prickling, “pins and needles”, or tingling feelings change in personality change in walking and balance changes in patterns and rhythms of speech chest pain lack of appetite lack of coordination large, flat, blue or purplish patches in the skin leg cramps lip smacking or puckering loss of bladder control Drug Interactions of Procyclidine Procyclidine may interact with following drug, supplements, & may change the efficacy of drugs antihistamines (e.g,.cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine) antiseizure medications (e.g., clobazam, ethosuximide, felbamate, levetiracetam, phenobarbital, phenytoin, primidone, topiramate, valproic acid, zonisamide) aripiprazole “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole) benzodiazepines (e.g., alprazolam, diazepam, lorazepam) beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol) calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil) captopril celecoxib chloroquine cholecalciferol cyclosporine dantrolene domperidone “gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin) gabapentin H2 antagonists (e.g., famotidine, ranitidine) mirabegron montelukast non-steroidal anti-inflammatory medications (NSAIDs;e.g., diclofenac, ibuprofenserotonin antagonists (anti-emetic medications;, naproxen) phosphodiesterase 5 inhibitors (e.g., sildenafil, tadalafil, vardenafil) quinolone antibiotics (e.g., levofloxacin, norfloxacin, moxifloxacin) selective serotonin reuptake inhibitors (SSRIs; e.g., paroxetine, fluoxetine, citalopram) e.g., granisetron, ondansetron) “statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin,simvastatin) theophylline thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, metolazone) tramadol tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, Pregnancy & Lactation of Procyclidine FDA pregnancy category C. Pregnancy Procyclidine is in the FDA pregnancy category C. This means that it is not known whether procyclidine will harm an unborn baby. Do not take this medication without first talking to your doctor if you are pregnant. Lactation Certain medicines should not be used during pregnancy or breastfeeding. However, other medicines may be safely used in pregnancy or breastfeeding providing the benefits to the mother outweigh the risks to the unborn baby. Always inform your doctor if you are pregnant or planning a pregnancy, References DrugBank http://www.drugbank.ca/drugs/DB00387 http://www.drugbank.ca/drugs/DB00387 https://www.drugs.com/mtm/procyclidine.html https://www.drugs.com/cdi/procyclidine-tablets.html EPA DSStox https://comptox.epa.gov/dashboard/dsstoxdb/results? https://www.webmd.com/drugs/2/drug-14104/procyclidine-oral/details/list-contraindications European Chemicals Agency (ECHA) https://echa.europa.eu/information-on-chemicals Human Metabolome Database (HMDB) http://www.hmdb.ca/metabolites/HMDB0014531 HSDB https://toxnet.nlm.nih.gov/cgi-bin/sis/search/r?dbs+hsdb:@term+@rn+@rel+77-37-2 FDA Orange Book https://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm MassBank of North America (MoNA) http://mona.fiehnlab.ucdavis.edu/spectra/browse? SpectraBase https://spectrabase.com/compound/K4sA9f5TbCZ#3GwIXfop4XO https://spectrabase.com/compound/K4sA9f5TbCZ#BZRVDG5m65X https://spectrabase.com/compound/K4sA9f5TbCZ#96sDqImaAxI https://spectrabase.com/compound/K4sA9f5TbCZ#JQK6tcHYsec https://spectrabase.com/compound/K4sA9f5TbCZ#EoTQRgcHZAM https://spectrabase.com/compound/K4sA9f5TbCZ#shTMNJDw7H https://spectrabase.com/compound/K4sA9f5TbCZ#AzkhIS6ElMm https://spectrabase.com/compound/K4sA9f5TbCZ#JqmyKtbYFtr NIST http://www.nist.gov/srd/nist1a.cfm Springer Nature Read more … WHO ATC https://www.whocc.no/atc/ https://www.whocc.no/atc_ddd_index/ Wikipedia https://www.wikidata.org/wiki/Q27289967 https://en.wikipedia.org/wiki/Procyclidine https://en.wikipedia.org/wiki/Olanzapine https://pubchem.ncbi.nlm.nih.gov Show More