Product Information
Registration Status: ActiveTRIMBOW PRESSURISED INHALATION SOLUTION 100/6/12.5 mcg PER ACTUATION is approved to be sold in Singapore with effective from 2020-04-02. It is marketed by ORIENT EUROPHARMA PTE LTD, with the registration number of SIN15924P.
This product contains Beclometasone Dipropionate 0.1mg/actuation,Formoterol Fumarate 0.006mg/actuation, and Glycopyrronium 0.0125mg/actuation in the form of AEROSOL, METERED. It is approved for RESPIRATORY (INHALATION) use.
This product is manufactured by Chiesi Farmaceutici SpA in ITALY.
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
Beclomethasone dipropionate is a prodrug of the free form, beclomethasone (beclomethasone-17-monopropionate). An anti-inflammatory, synthetic corticosteroid, it is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma and allergic rhinitis (seasonal and perennial). Beclometasone dipropionate is also being investigated for oral treatment in mild-to-moderate Crohn's disease of ileal or ileal-right colonic localisation and for "topical" use mild-to-moderate graft versus host disease. It is marketed under several brand names such as Qnasl (US) and Rivanase AQ (Canada).
Indication
Used in the maintenance treatment of asthma as prophylactic therapy in patients 5 years of age and older, and in treating symptoms for allergic rhinitis (seasonal or perennial) in patients 12 years of age and older. Also being investigated for oral treatment in mild-to-moderate Crohn's disease of ileal or ileal-right colonic localisation and for "topical" use mild-to-moderate graft versus host disease.
Mechanism of Action
Unbound corticosteroids cross cell membranes and bind with high affinity to specific cytoplasmic receptors. The result includes inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, suppression of humoral immune responses, and reduction in edema or scar tissue. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. For the investigated use in the treatment of GvHD or Crohn's, beclometasone acts by binding to interleukin-13 to inhibit cytokines, which in turn inhibits inflammatory chemicals downstream.
Pharmacokinetics
- Absorption
- Mean peak plasma concentration was 88pg/ml at 0.5 hour.
- Distribution
- The steady state volume of distribution for beclomethasone dipropionate is 20 L, and for it's active metabolite, beclomethasone-17-monopropionate, it is much larger at 424 L.
- Metabolism
- Metabolism mediated via esterase enzymes that are found in most tissues. Undergoes rapid and extensive conversion to beclomenthasone-17-monopropionate (17-BMP) during absorption
- Elimination
Clearance
High plasma clearance after intravenous administration (150 and 120 L/hour).
Toxicity
The acute toxicity of beclometasone dipropionate is low. The only harmful effect that follows inhalation of large amounts of the drug over a short period of time is suppression of hypothalamic-pituitary-adrenal (HPA) function. Chronic: The excessive use of beclometasone dipropionate over a long period could lead to adrenal suppression.
Active Ingredient/Synonyms
(11β,16β)-9-chloro-11-hydroxy-16-methyl-17,21-bis(1-oxopropoxy)pregna-1,4-diene-3,20-dione | 9-chloro-11β-hydroxy-16β-methylpregna-1,4-diene-3,20-dione 17,21-dipropionate | 9-chloro-16β-methyl-11β,17,21-trihydroxypregna-1,4-diene-3,20-dione 17,21-dipropionate | beclometasone 17,21-dipropionate | Beclometasone dipropionate | Beclomethasone dipropionate |
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.
Mechanism of Action
4-Methoxyamphetamine is a seratogenic drug of the amphetamine class. The drug acts as a potent and selective serotonin releasing agent. It binds to alpha receptors to mediate these effects.
Active Ingredient/Synonyms
(2RS)-1-(4-methoxyphenyl)propan-2-amine | 4-methoxyamfetamine | D,L-p-methoxyamphetamine | Formoterol fumarate related compound G | P-methoxyamfetamine | P-methoxyamphetamine | Paramethoxyamphetamine | 4-Methoxyamphetamine |
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.
Description
Glycopyrronium (as the bromide salt glycopyrrolate) is a synthetic anticholinergic agent with a quaternary ammonium structure. A muscarinic competitive antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics. In October 2015, glycopyrrolate was approved by the FDA for use as a standalone treatment for Chronic obstructive pulmonary disease (COPD), as Seebri Neohaler.
Indication
For use as a preoperative antimuscarinic to reduce salivary, tracheobronchial, and pharyngeal secretions, to reduce the volume and free acidity of gastric secretions and to block cardiac vagal inhibitory reflexes during induction of anesthesia and intubation. Also used to treat chronic obstructive pulmonary disease (COPD).
Mechanism of Action
Glycopyrrolate binds competitively to the muscarinic acetylcholine receptor. Like other anticholinergic (antimuscarinic) agents, it inhibits the action of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic effector cells of smooth muscle, cardiac muscle, the sinoatrial node, the atrioventricular node, exocrine glands and, to a limited degree, in the autonomic ganglia. Thus, it diminishes the volume and free acidity of gastric secretions and controls excessive pharyngeal, tracheal, and bronchial secretions.
Pharmacokinetics
- Absorption
- Rapidly absorbed (1-2 minutes) after intravenous injection
- Distribution
- Metabolism
- Elimination
Toxicity
Side effects include dry mouth, difficult urinating, heachaches, diarrhea and constipation. The medication also induces drowsiness or blurred vision. LD50=709 mg/kg (rat, oral).
Active Ingredient/Synonyms
Glycopyrrolate cation | Glycopyrrolate ion | Glycopyrronium cation | Glycopyrronium ion | Glycopyrronium |
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.