Peringatan Keamanan

The most common adverse reactions reported in patients treated with propiverine include dry mouth, headache, accommodation disorder, constipation, abdominal pain, dyspepsia and fatigue L2315.

Propiverine may cause drowsiness and blurred vision. This may impair the ability to exert activities that require mental alertness such as operating a motor vehicle or other machinery, or to perform hazardous work while taking this drug L2315.

There have been reports of QT interval prolongation with antimuscarinic medications in the same class of drugs of propiverine hydrochloride. Some drugs that may cause QT/QTc interval prolongation may increase the risk of a rare, but serious ventricular arrhythmia called torsades de pointes. Patients at risk for QT/QTc interval prolongation, such as those with diagnosed heart failure, long QT syndrome, recent significant hypokalemia episodes or receiving other drugs known to prolong QT/QTc, should be closely monitored while treated with propiverine. Patients who experience prolonged QT/QTc or symptoms of possible arrhythmias including dizziness, palpitations or fainting should be electrocardiographically evaluated and monitored for electrolyte disturbances L2315.

Propiverine, like other anticholinergics, induces mydriasis. Therefore, the risk to induce acute angle-closure glaucoma in individuals predisposed with narrow angles of the anterior chamber may be increased. Drugs of this class, including propiverine, have been reported to induce or precipitate acute angle-closure glaucoma L2315.

No clinical data are available on the use of propiverine in pregnant women. Studies in animals have shown reproductive toxicity L2315.

Propiverine

DB12278

small molecule approved investigational

Deskripsi

Propiverine is a widely used antimuscarinic drug with a mixed mode of action in the treatment of symptoms associated with overactive bladder (OAB) A32576.

Overactive bladder (OAB) is a chronic condition of the lower urinary tract characterized by urinary urgency, increased frequency of urination, and nocturia (frequent waking during the night to urinate). OAB has a negative impact on quality of life and may lead to leakage and inconvenient urinary accidents L2327, L2328. Overactive bladder syndrome affects millions of elderly individuals in the United States and shows equal prevalence in men and women. The impact of OAB on quality of life is sometimes devastating, especially to elderly patients with other medical conditions L2328.

Propiverine hydrochloride is a bladder detrusor muscle relaxant drug with dual antimuscarinic and calcium-modulating properties for the treatment of OAB L2317.

Struktur Molekul 2D

Berat 367.4813
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) In three studies including a total of 37 healthy volunteers mean elimination half-life was 14.1, 20.1 and 22.1 hours, respectively [L2315].
Volume Distribusi In one study, the volume of distribution was calculated in 21 healthy volunteers after intravenous (IV) administration of propiverine hydrochloride was measured to range from 125 to 4731 (average 2791) indicating, that a large amount of available propiverine is distributed to peripheral compartments [L2324].
Klirens (Clearance) Mean total clearance after single dose administration of 30 mg is 371 mL/min (191 – 870 mL/min) [L2315].

Absorpsi

Propiverine is rapidly absorbed from the gastrointestinal tract with maximum plasma concentrations attained after 2.3 hours. the mean absolute bioavailability of mictonorm 15 mg tablets (propiverine) is 40.5 %. It undergoes heavy first-pass metabolism in the liver L2315.

Metabolisme

The major metabolites were found to be as follows; 4-piperidyl diphenylpropoxyacetate (DM-P-4), 1-methyl-4-piperidyl benzilate (Dpr-P-4) and 1-methyl-4-piperidyl diphenyl-(2 carboxy) ethoxyacetate (?-COOH-P-4) in the liver, Dpt-p-4, DM-P-4 in the kidney, and DM-P-4, DPr-P-4 in the lung L2323. In the same pharmacokinetic study, All pharmacologically active compounds such as the unchanged compound, 1-methyl-4-piperidyl benzilate N-oxide (DPr-P-4 (N?O)), Dpt-p-4 and 1-methyl-4-piperidyl diphenylpropoxyacetate N-oxide (P-4 (N?O)) were present in the urinary bladder, a target organ for P-4, at higher concentrations than in the plasma L2323. Propiverine is metabolized by both intestinal and hepatic enzymes. The main metabolic pathway involves the oxidation of the piperidyl-N and is mediated by CYP 3A4 and flavin-containing monooxygenases (FMO) 1 and 3 and results in the formation of the second main metabolite M-5, the plasma concentration of which is greater in concentration that of the parent substance propiverine. Four metabolites have been identified in the urine following propiverine ingestion; 3 them are pharmacologically active metabolites that may contribute to its therapeutic effect (M-5, M-6, M-23) L2325. The mean absolute bioavailability of propiverine IR 15 mg is 40.5% L2315.

Rute Eliminasi

Following the ingestion of 30 mg propiverine, 60% radioactivity was recovered in urine and 21% was recovered in feces within 12 days. Less than 1% of an oral dose is excreted unchanged in the urine L2315.

Interaksi Makanan

3 Data
  • 1. Take at the same time every day.
  • 2. Take separate from meals. PrMictoryl Pediatric (propiverine hydrochloride) tablets should be taken at least 1 hour before meals as high-fat meals reduce the bioavailability of PrMictoryl.
  • 3. Take with or without food. Mictoryl (propiverine hydrochloride) modified-release capsules can be taken with or without food as food does not affect its bioavailability.

Interaksi Obat

1488 Data
Valsartan Propiverine may decrease the antihypertensive activities of Valsartan.
Remikiren Propiverine may decrease the antihypertensive activities of Remikiren.
Guanadrel Propiverine may decrease the antihypertensive activities of Guanadrel.
Olmesartan Propiverine may decrease the antihypertensive activities of Olmesartan.
Minoxidil Propiverine may decrease the antihypertensive activities of Minoxidil.
Treprostinil Propiverine may decrease the antihypertensive activities of Treprostinil.
Trandolapril Propiverine may decrease the antihypertensive activities of Trandolapril.
Benazepril Propiverine may decrease the antihypertensive activities of Benazepril.
Candoxatril Propiverine may decrease the antihypertensive activities of Candoxatril.
Moexipril Propiverine may decrease the antihypertensive activities of Moexipril.
Nitroglycerin Propiverine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Propiverine may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Propiverine may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil Propiverine may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Propiverine may decrease the antihypertensive activities of Eprosartan.
Quinapril Propiverine may decrease the antihypertensive activities of Quinapril.
Telmisartan Propiverine may decrease the antihypertensive activities of Telmisartan.
Deserpidine Propiverine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Propiverine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Propiverine may decrease the antihypertensive activities of Trimethaphan.
Bretylium Propiverine may decrease the antihypertensive activities of Bretylium.
Captopril Propiverine may decrease the antihypertensive activities of Captopril.
Cilazapril Propiverine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Propiverine may decrease the antihypertensive activities of Saprisartan.
Spirapril Propiverine may decrease the antihypertensive activities of Spirapril.
Debrisoquine Propiverine may decrease the antihypertensive activities of Debrisoquine.
Diethylnorspermine Propiverine may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Propiverine may decrease the antihypertensive activities of Temocapril.
Rauwolfia serpentina root Propiverine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Angiotensin 1-7 Propiverine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Propiverine may decrease the antihypertensive activities of Imidapril.
BQ-123 Propiverine may decrease the antihypertensive activities of BQ-123.
Dihydralazine Propiverine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Propiverine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Propiverine may decrease the antihypertensive activities of Guanoxan.
Delapril Propiverine may decrease the antihypertensive activities of Delapril.
Vincamine Propiverine may decrease the antihypertensive activities of Vincamine.
Linsidomine Propiverine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Propiverine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Propiverine may decrease the antihypertensive activities of Tolonidine.
Endralazine Propiverine may decrease the antihypertensive activities of Endralazine.
Cadralazine Propiverine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Propiverine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Propiverine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Propiverine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Propiverine may decrease the antihypertensive activities of Guanoclor.
Candesartan Propiverine may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Propiverine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Propiverine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Propiverine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Propiverine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Propiverine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Propiverine may decrease the antihypertensive activities of Quinaprilat.
Enalapril Propiverine may decrease the antihypertensive activities of Enalapril.
Bosentan Propiverine may decrease the antihypertensive activities of Bosentan.
Losartan Propiverine may decrease the antihypertensive activities of Losartan.
Irbesartan Propiverine may decrease the antihypertensive activities of Irbesartan.
Sitaxentan Propiverine may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Propiverine may decrease the antihypertensive activities of Ambrisentan.
Pinacidil Propiverine may decrease the antihypertensive activities of Pinacidil.
Riociguat Propiverine may decrease the antihypertensive activities of Riociguat.
Aliskiren Propiverine may decrease the antihypertensive activities of Aliskiren.
Selexipag Propiverine may decrease the antihypertensive activities of Selexipag.
Ramipril Propiverine may decrease the antihypertensive activities of Ramipril.
Perindopril Propiverine may decrease the antihypertensive activities of Perindopril.
Levamlodipine Propiverine may decrease the antihypertensive activities of Levamlodipine.
Azilsartan medoxomil Propiverine may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Propiverine may decrease the antihypertensive activities of Diazoxide.
Aclidinium The risk or severity of adverse effects can be increased when Propiverine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Propiverine.
Mirabegron The risk or severity of urinary retention can be increased when Propiverine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Propiverine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Propiverine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Propiverine.
Tiotropium The risk or severity of adverse effects can be increased when Propiverine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Propiverine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Propiverine is combined with Umeclidinium.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Propiverine.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Propiverine.
Omapatrilat Propiverine may decrease the antihypertensive activities of Omapatrilat.
Rescinnamine Propiverine may decrease the antihypertensive activities of Rescinnamine.
Epicaptopril The risk or severity of hypertension can be increased when Epicaptopril is combined with Propiverine.
Taxifolin The risk or severity of hypertension can be increased when Taxifolin is combined with Propiverine.
1-benzylimidazole The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Propiverine.
Saralasin The risk or severity of hypertension can be increased when Saralasin is combined with Propiverine.
Tyramine The risk or severity of hypertension can be increased when Tyramine is combined with Propiverine.
Atipamezole The risk or severity of hypertension can be increased when Atipamezole is combined with Propiverine.
Idazoxan The risk or severity of hypertension can be increased when Propiverine is combined with Idazoxan.
Ebselen The risk or severity of hypertension can be increased when Propiverine is combined with Ebselen.
Tramazoline The risk or severity of hypertension can be increased when Propiverine is combined with Tramazoline.
Fenozolone The risk or severity of hypertension can be increased when Propiverine is combined with Fenozolone.
Xenon The risk or severity of hypertension can be increased when Propiverine is combined with Xenon.
Buflomedil The risk or severity of hypertension can be increased when Propiverine is combined with Buflomedil.
Mefenorex The risk or severity of hypertension can be increased when Propiverine is combined with Mefenorex.
Quinoline Yellow WS The risk or severity of hypertension can be increased when Propiverine is combined with Quinoline Yellow WS.
Dutasteride The risk or severity of hypertension can be increased when Dutasteride is combined with Propiverine.
Methylergometrine The risk or severity of hypertension can be increased when Methylergometrine is combined with Propiverine.
Finasteride The risk or severity of hypertension can be increased when Finasteride is combined with Propiverine.
Solifenacin The risk or severity of hypertension can be increased when Solifenacin is combined with Propiverine.
Dihydroergocornine The risk or severity of hypertension can be increased when Dihydroergocornine is combined with Propiverine.

Target Protein

Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M5 CHRM5
Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C
Alpha-1A adrenergic receptor ADRA1A
Muscarinic acetylcholine receptor M4 CHRM4

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23288694
    McKeage K: Propiverine: a review of its use in the treatment of adults and children with overactive bladder associated with idiopathic or neurogenic detrusor overactivity, and in men with lower urinary tract symptoms. Clin Drug Investig. 2013 Jan;33(1):71-91. doi: 10.1007/s40261-012-0046-9.
  • PMID: 3208795
    Haustein KO, Huller G: On the pharmacokinetics and metabolism of propiverine in man. Eur J Drug Metab Pharmacokinet. 1988 Apr-Jun;13(2):81-90.
  • PMID: 12452898
    Chess-Williams R: Muscarinic receptors of the urinary bladder: detrusor, urothelial and prejunctional. Auton Autacoid Pharmacol. 2002 Jun;22(3):133-45.
  • PMID: 16406943
    Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9.
  • PMID: 27750360
    Sakakibara F, Takahama K, Nanri M, Sasaki E: Pharmacological Properties of Propiverine Contribute to Improving Lower Urinary Tract Dysfunctions in Rats with Spinal Cord Injuries. Drug Res (Stuttg). 2016 Sep;66(9):464-469. doi: 10.1055/s-0042-110855. Epub 2016 Oct 17.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Mictoryl
    Capsule, extended release • 30 mg • Oral • Canada • Approved
  • Mictoryl
    Capsule, extended release • 45 mg • Oral • Canada • Approved
  • Mictoryl Pediatric
    Tablet • 5 mg • Oral • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul