Topimide
Topimide Uses, Dosage, Side Effects, Food Interaction and all others data.
Topimide binds to and blocks the receptors in the muscles of the eye (muscarinic receptor M4). Topimide acts by blocking the responses of the iris sphincter muscle to the iris and ciliary muscles to cholinergic stimulation, producing dilation of the pupil and paralysis of the ciliary muscle.
Topimide is an anticholinergic drug and that works by non‐selectively blocking muscarinic receptors to cause mydriasis and cycloplegia. It relaxes the pupillary sphincter to dilate the pupil. The onset of tropicamide‐induced mydriasis is about 10 to 15 minutes, with optimal effect occurring 25 to 30 minutes post-administration. Mydriasis caused by tropicamide wears off within four to eight hours, but it was seen up to 24 hours in some individuals. Topimide causes accommodation by causing contraction of the ciliary muscle. The cycloplegic effect occurs within 20 to minutes following administration, with a duration of action of four to 10 hours. Topimide can elevate intraocular pressure. The ophthalmic use of tropicamide is not typically associated with serious systemic adverse events.
One randomized pilot study showed that oral tropicamide alleviated perceived symptoms of sialorrhea in patients with Parkinson's Disease: anticholinergics are believed to restore the dopaminergic to cholinergic activity imbalance in neurodegenerative diseases. Similarly in one case report, tropicamide administered via ophthalmic solution relieved clozapine-induced sialorrhea. Interestingly, in rodent models, tropicamide suppressed drug-induced tremulous jaw movements which are often used as a model of parkinsonian tremor: the significance of this finding requires further investigations.
Trade Name | Topimide |
Generic | Tropicamide |
Tropicamide Other Names | Tropicamid, Tropicamida, Tropicamide, Tropicamidum |
Type | |
Formula | C17H20N2O2 |
Weight | Average: 284.3529 Monoisotopic: 284.152477894 |
Protein binding | The extent of protein binding has not been established. Tropicamide binds to albumin.[A230168] |
Groups | Approved, Investigational |
Therapeutic Class | Mydriatic and Cycloplegic agents |
Manufacturer | |
Available Country | Taiwan |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
For mydriasis and cycloplegia for diagnostic procedure, for the treatment of acute and subacute iridocyclitis, chronic iridocyclitis, Adhesions and disruptions of iris and ciliary body, Sclera and iris operations
Topimide is also used to associated treatment for these conditions: Diagnostic procedures
How Topimide works
Muscarinic acetylcholine receptors are involved in numerous ocular functions. The M3 subtype is predominantly expressed by smooth muscle cells of the sphincter pupillae, which is a circular muscle of the iris, and ciliary muscles. In response to light or binding of acetylcholine, M3 receptor signalling leads to contraction of the sphincter pupillae and pupil constriction. Contraction of the ciliary muscle via M3 receptor signalling also leads to accommodation, adjusting the lens for near vision. The eye is also innervated by parasympathetic nerves: ciliary ganglion neurons project to the ciliary body and the sphincter pupillae muscle of the iris to control ocular accommodation and pupil constriction.
Topimide is a non-selective muscarinic antagonist that binds to all subtypes of muscarinic receptors. By binding to muscarinic receptors, tropicamide relaxes the pupillary sphincter muscle and causes pupil dilation. By blocking the muscarinic receptors of the ciliary body, tropicamide also prevents accommodation. Like other muscarinic antagonists, tropicamide inhibits the parasympathetic drive, allowing the sympathetic nervous system responses to dominate. Topimide is thought to ameliorate sialorrhea by blocking M4 receptors expressed on salivary glands and reducing hypersalivation.
Dosage
Topimide dosage
For refraction:Instill one or two drops of 1% solution in the eye(s), repeated in five minutes. If patient is not seen within 20 to 30 minutes, an additional drop may be instilled to prolong mydriatic effect.
For examination of fundus:instill one or two drops of 0.5% solution 15 to 20 minutes prior to examination. Individuals with heavily pigmented irides may require higher strength or more doses.
Side Effects
Transient stinging, blurred vision, photophobia and superficial punctate keratitis have been reported with the use of tropicamide. Increased intraocular pressure has been reported following the use of mydriatics. Dryness of the mouth, tachycardia, headache, allergic reactions, nausea, vomiting, pallor, central nervous system disturbances and muscle rigidity have been reported with the use of tropicamide.
Toxicity
Oral LD50 is 865 mg/kg in rats and 565 mg/kg in mice. Intraperitoneal LD50 is 1210 mg/kg in rats and 695 mg/kg in mice. Subcutaneous LD50 is 872 mg/kg in rats and 665 mg/kg in mice.
There is limited information on tropicamide overdose. Systemic adverse effects, such as tachycardia, central nervous system disturbances, and muscle rigidity have been reported with the use of tropicamide. Psychotic reactions, behavioral disturbances, and vasomotor or cardio-respiratory collapse have been reported with the use of anticholinergic in children.
Precaution
The lacrimal sac should be compressed by digital pressure for 2-3 minutes after instillation to avoid excessive systemic absorption.
Interaction
Topimide may interfere with the antihypertensive action of carbachol, pilocarpine, or ophthalmic cholinesterase inhibitors.
Food Interaction
No interactions found.Volume of Distribution
No information can be found.
Elimination Route
Following ocular administration of 40 μL drops of 0.5% tropicamide in female subjects, tropicamide reached its mean peak concentration in plasma of 2.8 ± 1.7 ng/mL (mean ± SD) at five minutes.
Half Life
Topimide has a plasma half-life of 30 minutes.
Clearance
No information can be found.
Elimination Route
No information can be found.
Pregnancy & Breastfeeding use
Pregnancy Category C. Topimide should be given to a pregnant woman only if clearly needed. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when tropicamide is administered to a nursing woman.
Contraindication
Contraindicated in persons showing hypersensitivity to any component of Topimide.
Storage Condition
Store at 15° to 25°C . Do not refrigerate or store at high temperatures. Keep container tightly closed.
Innovators Monograph
You find simplified version here Topimide
Topimide contains Tropicamide see full prescribing information from innovator Topimide Monograph, Topimide MSDS, Topimide FDA label
FAQ
What is Topimide used for?
Topimide is used in the eye to widen your pupils, so they won't respond to light. It is normally used for diagnostic procedures.
How does Topimide work?
Topimide relaxes the pupillary sphincter muscle and causes pupil dilation. By blocking the muscarinic receptors of the ciliary body, tropicamide also prevents accommodation.
What are the common side effects of Topimide?
Common side effects of Topimide are include:
- Clumsiness or unsteadiness
- confusion
- fast heartbeat
- flushing or redness of face
- hallucinations (seeing, hearing, or feeling things that are not there)
- increased thirst or dryness of mouth
- skin rash
- slurred speech
- swollen stomach in infants
- unusual behavior, especially in children
- unusual drowsiness, tiredness, or weakness
How safe is Topimide?
Topimide is a safe drug used for pupillary dilation prior to a comprehensive eye exam or ocular procedure.
Is Topimide safe during pregnancy?
This drug should be used during pregnancy only if clearly needed.Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
Is Topimide safe during breastfeeding?
A single use of this drug is not likely to interfere with breastfeeding. Long-term use may inhibit lactation, producing signs in the nursing infant.Placing pressure over the tear duct for at least 1 minute after instillation can substantially decrease the amount of drug excreted in breast milk.
Is Topimide safe during breastfeeding?
A single use of this drug is not likely to interfere with breastfeeding. Long-term use may inhibit lactation, producing signs in the nursing infant.Placing pressure over the tear duct for at least 1 minute after instillation can substantially decrease the amount of drug excreted in breast milk.
Can I drink alcohol with Topimide?
Side effects from this drug may get worse if you drink alcohol-containing drinks. If you have persistent stomach upset, vomit blood or what looks like coffee grounds, or have black, tarry stools, contact your health care provider immediately.
Can I drive after taking Topimide?
Topimide eye drops allow your doctor to examine your eye more easily. The drops can cause blurred vision which may last for several hours. Do not drive and do not use tools or machines until your vision is clear again.
How long does it take Topimide to wear off?
Its optimal effect occurs 25 to 30 minutes post-administration.Typically, mydriasis reverses within 4 to 8 hours. However, it may take 24 hours for the mydriatic effect to wear off in some individuals.
How to use Topimide?
To apply eye drops, wash your hands first. To avoid contamination, do not touch the dropper tip or let it touch your eye or any other surface.
If you are wearing contact lenses, remove them before using this medication. Ask your doctor when you may replace your contact lenses.
When do I use Topimide?
It is used before eye examinations, such as cycloplegic refraction and examination of the fundus of the eye. Topimide may also be used before and after eye surgery.
Can Topimide be used in children?
Given the small amount of residual accommodation present after the application of Topimide, it can be concluded that 1% Topimide is an effective cycloplegic agent for myopic children.
How often can I use Topimide?
Adults one drop of 1% solution, repeated once in five minutes. Children one drop of 0.5 to 1% solution, repeated once in five minutes.
Can I overdose on Topimide?
If you take too much Topimide call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away. If Topimide is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur.
Does Topimide cause Cycloplegia?
Topimide is used to cause mydriasis and cycloplegia for eye exams or ocular procedures.
Does Topimide affect accommodation?
Topimide gave rise to a reduction in the amplitude of accommodation which tended to vary inversely with the age of the patient.
Does Topimide causes Pediatric?
Infants and young children and children with blond hair or blue eyes may be especially sensitive to the effects of Topimide. This may increase the chance or severity of some of the side effects during treatment.