Product Information
Registration Status: ActiveSPIRIVA RESPIMAT, 2.5 MICROGRAM, SOLUTION FOR INHALATION is approved to be sold in Singapore with effective from 2009-04-30. It is marketed by BOEHRINGER INGELHEIM SINGAPORE PTE LTD, with the registration number of SIN13642P.
This product contains Tiotropium 0.0025mg/actuation in the form of SOLUTION. It is approved for RESPIRATORY (INHALATION) use.
This product is manufactured by Boehringer Ingelheim Pharma GmbH & Co.KG in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Tiotropium is a long-acting, 24 hour, anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD). Tiotropium is a muscarinic receptor antagonist, on topical application it acts mainly on M3 muscarinic receptors located in the airways to produce smooth muscle relaxation, thus producing a bronchodilatory effect.
Indication
Used in the management of chronic obstructive pulmonary disease (COPD).
Mechanism of Action
Tiotropium is a muscarinic receptor antagonist, often referred to as an antimuscarinic or anticholinergic agent. Although it does not display selectivity for specific muscarinic receptors, on topical application it acts mainly on M3 muscarinic receptors located in the airways to produce smooth muscle relaxation, thus producing a bronchodilatory effect.
Pharmacokinetics
- Absorption
- Bioavailability is 19.5% following administration by inhalation. Oral solutions of tiotropium have an absolute bioavailability of 2-3%.
- Distribution
- * 32 L/kg
- Metabolism
- The extent of biotransformation appears to be small. This is evident from a urinary excretion of 74% of unchanged substance after an intravenous dose to young healthy volunteers. Tiotropium, an ester, is nonenzymatically cleaved to the alcohol N–methylscopine and dithienylglycolic acid, neither of which bind to muscarinic receptors. In vitro experiments with human liver microsomes and human hepatocytes suggest that a fraction of the administered dose (74% of an intravenous dose is excreted unchanged in the urine, leaving 25% for metabolism) is metabolized by cytochrome P450–dependent oxidation and subsequent glutathione conjugation to a variety of Phase II metabolites. Via inhibition studies, it is evident that CYP450 2D6 and 3A4 are involved in the metabolic pathway that is responsible for the elimination of a small part of the administered dose.
- Elimination
Clearance
* 880 mL/min [young healthy volunteers receiving IV administration] * Renal cl=326 mL/min [COPD patients (<58 years)] * Renal cl=163 mL/min [COPD patients (>70 years)]
Toxicity
No mortality was observed at inhalation tiotropium doses up to 32.4 mg/kg in mice, 267.7 mg/kg in rats, and 0.6 mg/kg in dogs. These doses correspond to 7,300, 120,000, and 850 times the recommended human daily dose on a mg/m2 basis, respectively.
Active Ingredient/Synonyms
Tiotropium | Tiotropium |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.