Product Information
Registration Status: ActiveGANFORT PF EYE DROPS (BIMATOPROST 0.3MG/ML, TIMOLOL 5.0MG/ML) is approved to be sold in Singapore with effective from 2016-03-11. It is marketed by ALLERGAN SINGAPORE PTE LTD, with the registration number of SIN14966P.
This product contains Bimatoprost 0.3mg/ml, and Timolol 5mg/ml in the form of OPHTHALMIC SOLUTION, STERILE. It is approved for OPHTHALMIC use.
This product is manufactured by Allergan Pharmaceuticals Ireland in IRELAND.
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
Bimatoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a prostaglandin analogue that works by increasing the outflow of aqueous fluid from the eyes. It binds to the prostanoid FP receptor.
Indication
For the reduction of elevated intraocular pressure in patients with open angle glaucoma or ocular hypertension who are intolerant of other intraocular pressure lowering medications or insufficiently responsive (failed to achieve target IOP determined after multiple measurements over time) to another intraocular pressure lowering medication.
Mechanism of Action
Bimatoprost is believed to lower intraocular pressure (IOP) in humans by increasing outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes. Bimatoprost reduces the pressure in the eye by mimicking the action of a naturally-occuring prostaglandin. Prostaglandins are a group of chemicals found in many places in the body. In the eye, they increase the drainage of the aqueous humour out of the eyeball. Bimatoprost is a synthetic compound related to one of the natural prostaglandins, and works by increasing the drainage of aqueous humour out of the eyeball. Bimatoprost may also lower the rate of aqueous formation in the eye. Both these effects decrease the pressure within the eye.
Pharmacokinetics
- Absorption
- Systemically absorbed when administered to the eye.
- Distribution
- * 0.67 L/kg
- Metabolism
- Bimatoprost undergoes oxidation, N-deethylation and glucuronidation to form a variety of metabolites.
- Elimination
Clearance
* 1.5 L/hr/kg [Healthy subjects receiving IV administration of 3.12 ug/kg]
Toxicity
In oral (by gavage) mouse and rat studies, doses up to 100 mg/kg/day did not produce any toxicity. This dose expressed as mg/m2 is at least 70 times higher than the accidental dose of one bottle of bimatoprost for a 10 kg child.
Active Ingredient/Synonyms
(Z)-7-((1R,2R,3R,5S)-3,5-Dihydroxy-2-((1e,3S)-3-hydroxy-5-phenyl-1-pentenyl)cyclopentyl)-N-ethyl-5-heptenamide | Bimatoprostum | Bimatoprost |
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
A beta-adrenergic antagonist similar in action to propranolol. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of migraine disorders and tremor. [PubChem]
Indication
In its oral form it is used to treat high blood pressure and prevent heart attacks, and occasionally to prevent migraine headaches. In its opthalmic form it is used to treat open-angle and occasionally secondary glaucoma.
Mechanism of Action
Like propranolol and nadolol, timolol competes with adrenergic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle and beta(2)-receptors in the bronchial and vascular smooth muscle. Beta(1)-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. Beta(2)-blockade results in an increase in peripheral vascular resistance. The exact mechanism whereby timolol reduces ocular pressure is still not known. The most likely action is by decreasing the secretion of aqueous humor.
Pharmacokinetics
- Absorption
- Bioavailability is about 60%
- Distribution
- Metabolism
- Primarily hepatic (80%) via the cytochrome P450 2D6 isoenzyme.
- Elimination
Toxicity
LD50=1190 mg/kg (oral, mice), LD50=900 mg/kg (oral, rat). Symptoms of overdose include drowsiness, vertigo, headache, and atriventricular block.
Active Ingredient/Synonyms
(S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol | Timolol | Timolol anhydrous | Timololo | Timololum | Timolol |
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.