| Size | Price | Stock | Qty |
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| 5g |
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Based on minimal excretion of other phenothiazine derivatives, it appears that occasional short-term use of promethazine for the treatment of nausea and vomiting poses little risk to the breastfed infant. With repeated doses, observe infants for excess sedation. Because promethazine can lower basal prolactin secretion, promethazine might interfere with the establishment of lactation if given during labor before lactation is well established or with a sympathomimetic such as pseudoephedrine. An antiemetic without potent histamine blocking action is preferred in nursing mothers. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Unlike most phenothiazines, promethazine usually causes a reduction in basal prolactin secretion in nonnursing women. In one small study, women given promethazine with meperidine and secobarbital during labor, had the time to lactogenesis II prolonged by 14 hours. Women given meperidine or secobarbital without promethazine had lactogenesis II prolonged 7 hours compared to unmedicated women, but the difference was not statistically significant. The effect of postpartum promethazine is not known, but it might interfere with the establishment of lactation if given in the early postpartum period. |
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| References |
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| Additional Infomation |
Promethazine hydrochloride is an odorless white to faint yellow crystalline powder. Bitter taste. A 10% solution in water has a pH of 3.5-5.0. (NTP, 1992)
Promethazine hydrochloride is the hydrochloride salt of promethazine. It has a role as an antipruritic drug, a H1-receptor antagonist, a local anaesthetic, an antiemetic, a sedative, an anti-allergic agent, an anticoronaviral agent and a geroprotector. It contains a promethazine(1+). Promethazine Hydrochloride is the hydrochloride salt form of promethazine, a phenothiazine derivative with antihistaminic, sedative and antiemetic properties. Promethazine hydrochloride selectively blocks peripheral H1 receptors thereby diminishing the effects of histamine on effector cells. Promethazine hydrochloride also blocks the central histaminergic receptors, thereby depressing the reticular system causing sedative and hypnotic effects. In addition, promethazine hydrochloride also has centrally acting anticholinergic properties and probably mediates nausea and vomiting by acting on the medullary chemoreceptive trigger zone. A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals. See also: Promethazine (has active moiety); Phenothiazine (subclass of); Codeine Phosphate; Promethazine Hydrochloride (component of) ... View More ... |
| Molecular Formula |
C17H21CLN2S
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|---|---|
| Molecular Weight |
320.8800
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| Exact Mass |
320.111
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| CAS # |
58-33-3
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| Related CAS # |
Promethazine-d4 hydrochloride;1173018-74-0
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| PubChem CID |
6014
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| Appearance |
White to off-white solid powder
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| Density |
1.131 g/cm3
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| Boiling Point |
403.7ºC at 760 mmHg
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| Melting Point |
230-232°C
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| Flash Point |
198ºC
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| LogP |
5.106
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
298
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XXPDBLUZJRXNNZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20N2S.ClH/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19;/h4-11,13H,12H2,1-3H3;1H
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| Chemical Name |
N,N-dimethyl-1-phenothiazin-10-ylpropan-2-amine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~311.64 mM)
DMSO : ~50 mg/mL (~155.82 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 120 mg/mL (373.97 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1164 mL | 15.5821 mL | 31.1643 mL | |
| 5 mM | 0.6233 mL | 3.1164 mL | 6.2329 mL | |
| 10 mM | 0.3116 mL | 1.5582 mL | 3.1164 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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