Effects During Pregnancy and Lactation
◉ Overview of Lactation Use
Limited data suggest that levodopa is rarely excreted into breast milk, and sustained-release formulations may result in less drug transfer to the infant from breast milk compared to immediate-release formulations. Multiple studies have shown that levodopa can lower serum prolactin levels during lactation. For mothers who have established lactation, prolactin levels may not affect their ability to breastfeed. Although some mothers with Parkinson's disease have been able to successfully breastfeed without significant adverse effects while using relatively low doses of levodopa and carbidopa, the long-term effects of levodopa use on breastfeeding have not been fully assessed. ◉ Effects on Breastfed Infants
A mother with Parkinson's disease took 200 mg of sustained-release levodopa and 50 mg of carbidopa four times daily. She successfully breastfed her infant, who developed normally at age 2.
A 37-year-old Israeli woman with Parkinson's disease became pregnant while receiving continuous infusions of 20 mg/mL levodopa and 5 mg/mL carbidopa gel. She breastfed her infant for 3 months during treatment, but the extent of breastfeeding and the dosage of the gel were not specified in the paper. The infant's psychomotor development was considered normal at 10 months of age.
◉ Effects on Lactation and Breast Milk
Levodopa can lower serum prolactin levels in normal women and patients with hyperprolactinemia, and can suppress abnormal lactation in patients with galactorrhea, although not always. For mothers who have established lactation, their prolactin levels may not affect their ability to breastfeed.
A mother with Parkinson's disease took 200 mg of sustained-release levodopa and 50 mg of carbidopa four times daily. She successfully breastfed her infant.
On the 3rd day postpartum, five women took 500 mg of levodopa or 5 mg of bromocriptine orally, followed by 10 mg of metoclopramide three hours later. Bromocriptine has a stronger inhibitory effect on basal serum prolactin than levodopa. In the following 3 hours, patients taking levodopa experienced elevated serum prolactin levels after taking metoclopramide, while this was not observed in patients taking bromocriptine. Six postpartum women, 2 to 4 days old but not breastfeeding, were given 500 mg of levodopa orally on day 1 and 100 mg of levodopa plus 35 mg of carbidopa orally on day 2. Both regimens suppressed basal serum prolactin levels. However, levodopa alone reduced prolactin levels by 78%, while the lower-dose combination only reduced them by 51%. The maximum effect of both regimens occurred approximately 2 hours after administration. Seven postpartum women who breastfed approximately 7 times daily during the first week of postpartum were given 500 mg of levodopa orally, and their serum prolactin response was investigated. On day 2, they began taking 50 mg of carbidopa orally every 6 hours for 2 days. On the third day, they received a single oral dose of 50 mg carbidopa and 125 mg levodopa. Baseline serum prolactin levels decreased 30 minutes after levodopa administration and 45 minutes after the combination therapy. The maximum decreases were observed at 120 minutes post-administration, with a 62% decrease in the levodopa-only group and a 48% decrease in the combination therapy group, but the differences between the two regimens were not statistically significant. A 37-year-old Israeli woman with Parkinson's disease became pregnant while receiving continuous infusion of 20 mg/mL levodopa and 5 mg/mL carbidopa gel. She breastfed for three months during the treatment period, but the extent of breastfeeding and the gel dosage were not specified in the paper.

[1]. Effects of various drugs on 3,4-dihydroxyphenylalanine (DL-DOPA)-induced excitation (agressive behavior) in mice. Toxicol Appl Pharmacol. 1970 Nov;17(3):597-604.

DOPA is a hydroxyphenylalanine with hydroxyl substituents at the 3 and 4 positions of its benzene ring. It is a human metabolite. DOPA is a hydroxyphenylalanine, a tyrosine derivative, and also a non-protein-derived α-amino acid. It has been reported that DL-DOPA is found in cactus (Opuntia ficus-indica), beet (Beta vulgaris), and spiny bean (Mucuna pruriens), and there is relevant data available. DL-DOPA is a racemic mixture of the dopamine precursor L-DOPA (levodopa) and D-DOPA, and possesses anti-Parkinson's disease properties. L-DOPA is converted to dopamine by dopa decarboxylase and can cross the blood-brain barrier (BBB). Levodopa is decarboxylated in the brain to produce dopamine, which stimulates dopaminergic receptors, thereby compensating for the depletion of endogenous dopamine in Parkinson's disease. Phenylalanine is a β-hydroxylated derivative of phenylalanine. D-type dihydroxyphenylalanine has lower physiological activity than L-type and is often used in experiments to determine whether the pharmacological effects of levodopa are stereoselective.
See also: Levodopa (note moved to).

C9H11NO4

197.1879

197.069

63-84-3

DL-Dopa-d6

836

White to off-white solid powder

1.468 g/cm3

448.39ºC at 760 mmHg

270-272ºC(lit.)

224.978ºC

0.752

4

5

3

14

209

0

WTDRDQBEARUVNC-UHFFFAOYSA-N

InChI=1S/C9H11NO4/c10-6(9(13)14)3-5-1-2-7(11)8(12)4-5/h1-2,4,6,11-12H,3,10H2,(H,13,14)

2-amino-3-(3,4-dihydroxyphenyl)propanoic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~62.5 mg/mL (~316.95 mM)

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)