| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vivo |
Ninety percent of rats given cyclopentolate (20 mg/kg) survive[3].
|
|---|---|
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The product is absorbed after use in the eye. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation There is currently no information regarding the use of cyclopentonide during lactation. Anticholinergic drugs may interfere with breastfeeding. A single use of ophthalmic cyclopentonide is unlikely to interfere with breastfeeding; however, with prolonged use, the infant should be observed for signs of reduced milk production (e.g., unsatisfied, poor weight gain). To significantly reduce the amount of medication that enters breast milk after using eye drops, press your finger against the tear duct near the corner of your eye for at least 1 minute, then blot away any excess medication with absorbent tissue. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk Anticholinergic drugs may inhibit lactation in animals by suppressing the secretion of growth hormone and oxytocin. Anticholinergic drugs can also lower serum prolactin levels in non-lactating women. Prolactin levels in established lactating mothers may not affect their ability to breastfeed. |
| References |
[1]. Öner V, Bulut A, Öter K. The effect of topical anti-muscarinic agents on subfoveal choroidal thickness in healthy adults. Eye (Lond). 2016;30(7):925‐928.
[2]. Ishikawa H, DeSantis L, Patil PN. Selectivity of muscarinic agonists including (+/-)-aceclidine and antimuscarinics on the human intraocular muscles. J Ocul Pharmacol Ther. 1998;14(4):363‐373. [3]. Öner V, Bulut A, Öter K. The effect of topical anti-muscarinic agents on subfoveal choroidal thickness in healthy adults. Eye (Lond). 2016;30(7):925‐928. |
| Additional Infomation |
Cyclopentolate is a carboxylic acid ester formed by the condensation of (1-hydroxycyclopentyl)(phenyl)acetic acid and N,N-dimethylethanolamine. It is a tertiary amine antimuscarinic drug, acting similarly to atropine. Its hydrochloride salt is commonly used in ophthalmic diagnosis, achieving therapeutic effects through mydriasis (excessive pupillary dilation) and cycloplegia (cycloplegic repression). Cyclopentolate has a faster onset of action than atropine, but a shorter duration of action. It can be used as a mydriatic, parasympathetic blocker, muscarinic receptor antagonist, and diagnostic agent. It is a carboxylic acid ester, a tertiary amine compound, and a tertiary alcohol. Functionally, it is related to (1-hydroxycyclopentyl)phenylacetic acid and N,N-dimethylethanolamine.
A parasympathetic blocking anticholinergic drug used only for mydriasis or cycloplegia. A parasympathetic blocking anticholinergic drug used only for mydriasis or cycloplegia. See also: Cyclopentanol hydrochloride (salt form). Drug Indications Primarily used for mydriasis and cycloplegia to aid in diagnosis. Mechanism of Action Cyclopentonide causes pupillary dilation (mydriasis) and prevents the eye from adjusting to near vision (cycloplegia) by blocking muscarinic receptors. Pharmacodynamics Cyclopentonide is an antimuscarinic drug, belonging to the same class as atropine and scopolamine. Cyclopentonide blocks receptors (muscarinic receptors) in the ocular muscles. These receptors are involved in controlling pupil size and lens shape. Therefore, cyclopentonide relaxes the iris sphincter and ciliary muscle. When applied topically to the eye, it rapidly produces strong cycloplegia and mydriasis, reaching maximum effect within 15 to 60 minutes; recovery usually occurs within 24 hours. In patients with darker iris pigmentation, the onset and duration of cycloplegia and mydriasis are slower. |
| Molecular Formula |
C17H25NO3
|
|---|---|
| Molecular Weight |
291.39
|
| Exact Mass |
291.183
|
| CAS # |
512-15-2
|
| Related CAS # |
Cyclopentolate hydrochloride;5870-29-1
|
| PubChem CID |
2905
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.136g/cm3
|
| Boiling Point |
409.7ºC at 760mmHg
|
| Melting Point |
134-136
139 °C (hydrochloride salt) |
| Flash Point |
201.5ºC
|
| Index of Refraction |
1.555
|
| LogP |
2.18
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
21
|
| Complexity |
331
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C)CCOC(=O)C(C1=CC=CC=C1)C2(CCCC2)O
|
| InChi Key |
SKYSRIRYMSLOIN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H25NO3/c1-18(2)12-13-21-16(19)15(14-8-4-3-5-9-14)17(20)10-6-7-11-17/h3-5,8-9,15,20H,6-7,10-13H2,1-2H3
|
| Chemical Name |
2-(dimethylamino)ethyl 2-(1-hydroxycyclopentyl)-2-phenylacetate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4318 mL | 17.1591 mL | 34.3183 mL | |
| 5 mM | 0.6864 mL | 3.4318 mL | 6.8637 mL | |
| 10 mM | 0.3432 mL | 1.7159 mL | 3.4318 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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