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Pirenzepine
Allopathy
Prescription Required
DCGI (Drugs Controller General of India)
Schedule H
Pirenzepine is an Anticholinergic agent of drug belonging to Treatment of peptic ulcer.
Pirenzepine is an antimuscarinic agent used to treat peptic ulcers, gastric ulcers, and duodenal ulcers.
The bioavailability of pirenzepine is approximately 20-30%.Pirenzepine is 12% bound to plasma proteins. It has Poor diffusion across blood brain barrier.Pirenzepine is 10% excreted unchanged in urine, the rest in faeces. The elimination half-life is about 12 hours.
Pirenzepine shows side effects like Dry mouth, blurred vision.
Pirenzepine is available in the form of an Oral Tablet.
Pirenzepine is available in India, US, Australia, China, Japan, Singapore, and Malaysia.
Pirenzepine belongs to the Treatment of peptic ulcer acts as an Anticholinergic agent.
Pirenzepine is a muscarinic receptor antagonist and binds to the muscarinic acetylcholine receptor. The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins.
The Data of Onset and duration of action of Pirenzepine is not clinically established.
Pirenzepine is available in the form of an Oral Tablet.
Pirenzepine tablet is taken orally, usually 2 to 3 times daily or 3 to 4 times daily.
Pirenzepine is an antimuscarinic agent used to treat peptic ulcers, gastric ulcers, and duodenal ulcers.
Pirenzepine is an Anticholinergic agent of drug belonging to Treatment of peptic ulcer.
Pirenzepine is a muscarinic receptor antagonist and binds to the muscarinic acetylcholine receptor. The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins.
Pirenzepine is approved for use in the following clinical indications
- Peptic ulcer, gastric ulcer, and duodenal ulcer.
- Peptic ulcer
Adults: Oral: 50 mg 2 to 3 times daily or 25 mg 3 to 4 times daily.
Pirenzepine is available in various strengths as 25 and 50mg.
Pirenzepine is available in the form of Oral tablet.
Pirenzepine is contraindicated in patients with
- Hypersensitivity to pirenzepine or any excipients
- Paralytic ileus
- Pregnancy
- Caution should be exercised in patients with End Stage Renal Disease (ESRD), and hypersensitivity.
Common
- Dry mouth, blurred vision.
- Enhanced effect when used other drugs with antimuscarinic properties and MAOIs.
The common side effects of Pirenzepine include the following
Common side effects
Dry mouth, blurred vision.
Pharmacodynamic
Pirenzepine belongs to a group of medications called antispasmodics/anticholinergics. These medications are used to relieve cramps or spasms of the stomach, intestines, and bladder. Pirenzepine is used to treat duodenal or stomach ulcers or intestine problems. It can be used together with antacids or other medicine in the treatment of peptic ulcer. It may also be used to prevent nausea, vomiting, and motion sickness.
Pharmacokinetics
- Absorption
The bioavailability of pirenzepine is approximately 20-30%.
- Distribution
Pirenzepine is 12% bound to plasma proteins. It has Poor diffusion across blood brain barrier.
- Metabolism and Excretion
Pirenzipine is 10% excreted unchanged in urine, the rest in faeces. The elimination half life is about 12 hours.
- Siatkowski RM, Cotter SA, Crockett RS, Miller JM, Novack GD, Zadnik K, US Pirenzepine Study Group. Two-year multicenter, randomized, double-masked, placebo-controlled, parallel safety and efficacy study of 2% pirenzepine ophthalmic gel in children with myopia. Journal of American Association for Pediatric Ophthalmology and Strabismus. 2008 Aug 1;12(4):332-9.
- Engelhardt D, Karl R, Kolb HJ, Inthorn D, König N, Büll U, Hölzel D. Comparison between cimetidine-pirenzepine and antacids for the prevention of stress hemorrhage in intensive care patients. A controlled clinical study on 125 patients. Deutsche Medizinische Wochenschrift (1946). 1985 Jun 1;110(23):908-14.
- Suzuki T, Higuchi T, Kagami T, Uotani T, Yamade M, Tani S, Hamaya Y, Iwaizumi M, Osawa S, Sugimoto K, Miyajima H. Effects of pirenzepine on vonoprazan-induced gastric acid inhibition and hypergastrinemia. European Journal of Clinical Pharmacology. 2021 Jul;77(7):971-8.
- https://go.drugbank.com/drugs/DB00670
- https://www.mims.com/malaysia/drug/info/pirenzepine?mtype=generic
- https://www.uptodate.com/contents/pirenzepine-international-drug-information-concise?search=pirenzepine&source=panel_search_result&selectedTitle=1~2&usage_type=panel&kp_tab=drug_international&display_rank=1#F4288675
- https://www.medindia.net/doctors/drug_information/pirenzepine.htm#Contraindications
- https://mypsych.nhsggc.org.uk/medicines-companion/non-formulary-unlicensed/pirenzepine/