| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In the atrium of guinea pigs, homotropine (20 μM) alone results in a dosage ratio of 259, and when paired with hexamethonium bromide, it only yields a dose ratio of 95.0[1]. The muscarinic receptors in the stomach (pA2 = 7.13) and the atria (pA2 = 7.21) that mediate force (pA2 = 7.07) and rate (pA2 = 7.13) are affinities for homotropine[2].
|
|---|---|
| ln Vivo |
Rats given a 9 mm x 5 mm conical suppository containing homotropine methylbromide experience rapid blocking of the effects of intravenous acetylcholine on blood pressure and of vagal stimulation on pulse rate[3].
|
| Animal Protocol |
Animal/Disease Models: Male albino rats[3]
Doses: 9 mm x 5 mm conical suppository Route of Administration: By suppository Experimental Results: Blocked cardiovascular responses to vagal stimulation and acetylcholine; 10-20 min after insertion of the suppository the effects of vagal stimulation over a range of 2-16 Hz, 5 V, on pulse rate was virtually abolished and remained unchanged at 45-60 min. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Pharmacokinetic data are unavailable. Absorption, Distribution and Excretion ... |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation Currently, there is no information available regarding the use of Homatopine hydrobromide during lactation. Anticholinergic drugs may interfere with breastfeeding. A single use of ophthalmic Homatopine hydrobromide 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 entering breast milk after using eye drops, press the tear duct at the corner of the eye for at least 1 minute, then wipe 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 can inhibit lactation in animals, possibly 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. Protein binding No pharmacokinetic data available. |
| References |
|
| Additional Infomation |
Homatropine is a monocarboxylic acid. It is an anticholinergic drug that antagonizes muscarinic acetylcholine receptors. It is used in combination with hydrocodone (dihydrocodeine) tartrate (trade name Hycodan) to relieve cough symptoms, and is available in oral tablets and solutions. Homatropine is available in subtherapeutic doses of methylhomatropine bromide to prevent intentional overdose. Homatropine hydrobromide has been used in ophthalmology as a cycloplegic to temporarily paralyze accommodation and induce pupillary dilation; however, the U.S. Food and Drug Administration (FDA) has not approved the safety and efficacy of this therapeutic use. Homatropine is a cholinergic muscarinic receptor antagonist. Its mechanism of action is as a cholinergic muscarinic receptor antagonist. Homatropine is a synthetic tertiary amine alkaloid with antimuscarinic properties. Homatropine is a competitive inhibitor of acetylcholine on muscarinic receptors, blocking parasympathetic nerve excitation. See also: Homatropine (note moved to). Drug Indications When used in combination with hydrocodone antitussives, it can be used as an antidote for overdose. It can also be used in ophthalmic solutions to induce mydriasis. FDA Label Mechanism of Action Homatropine is a competitive muscarinic receptor antagonist with its acetyl group replaced by a large aromatic group. It is expected to act similarly to atropine, producing a similar parasympathetic blocking effect. Homatropine inhibits the response of the iris sphincter by blocking muscarinic receptors and cholinergic signaling pathways, resulting in the loss of pupillary light reflex during mydriasis. It also inhibits the ciliary body's response to cholinergic stimulation.
Pharmacodynamics Homatropine is an anticholinergic drug that produces typical anticholinergic effects, causing mydriasis and ciliary muscle paralysis. Other effects of structure-related atropine may also apply to homatropine, including secretion inhibition, tachycardia, smooth muscle relaxation, and central nervous system excitation. |
| Molecular Formula |
C16H21NO3
|
|---|---|
| Molecular Weight |
275.342844724655
|
| Exact Mass |
275.152
|
| CAS # |
87-00-3
|
| Related CAS # |
Homatropine Bromide;51-56-9;Homatropine methylbromide;80-49-9;Homatropine hydrochloride;637-21-8
|
| PubChem CID |
5282593
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.21 g/cm3
|
| Boiling Point |
403.3ºC
|
| Melting Point |
100ºC
|
| Flash Point |
197.7ºC
|
| LogP |
1.826
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
20
|
| Complexity |
340
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
O([C@@H]1C[C@@H]2CC[C@@H](N2C)C1)C(=O)C(C1C=CC=CC=1)O
|
| InChi Key |
ZTVIKZXZYLEVOL-DGKWVBSXSA-N
|
| InChi Code |
InChI=1S/C16H21NO3/c1-17-12-7-8-13(17)10-14(9-12)20-16(19)15(18)11-5-3-2-4-6-11/h2-6,12-15,18H,7-10H2,1H3/t12-,13+,14?,15?
|
| Chemical Name |
[(1S,5R)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 2-hydroxy-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 | 3.6319 mL | 18.1594 mL | 36.3187 mL | |
| 5 mM | 0.7264 mL | 3.6319 mL | 7.2637 mL | |
| 10 mM | 0.3632 mL | 1.8159 mL | 3.6319 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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