Procyclidine; Uses, Dosage, Side Effects, Drug Interactions

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