, commonly abbreviated as quinine HCl dihydrate, is a white, crystalline substance derived from the bark of the cinchona tree. It belongs to the class of medications known as antimalarials, primarily used to treat and prevent malaria caused by Plasmodium falciparum. The "dihydrate" suffix indicates that this particular form of quinine hydrochloride contains two water molecules per molecule of the drug, which affects its physical properties such as solubility and stability.
Quinine HCl dihydrate works by interfering with the parasite's ability to metabolize heme, an essential component of its diet derived from the breakdown of hemoglobin in red blood cells. This disruption leads to the accumulation of toxic compounds within the parasite, ultimately causing its death. Besides its antimalarial activity, quinine HCl dihydrate has also been employed in the treatment of muscle cramps and leg pains associated with certain medical conditions, although its use in these indications has declined due to the availability of more specific and safer therapies.
Despite its therapeutic benefits, quinine HCl dihydrate carries a risk of serious side effects, including cinchonism, a constellation of symptoms that may include tinnitus, headache, blurred vision, and nausea. Therefore, its use is tightly regulated and typically reserved for cases where other, safer alternatives are ineffective or contraindicated. Additionally, careful monitoring and dose adjustment are necessary to minimize adverse reactions, especially in patients with renal or hepatic impairment.
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| C20H29ClN2O4 | |
| 396.18 | |
| 396.91 | |
| m/z | 396.18 (100.0%), 398.18 (32.0%), 397.18 (21.6%), 399.18 (6.9%), 398.19 (2.2%) |
| C, 60.52; H, 7.36; Cl, 8.93; N, 7.06; O, 16.12 |
is a versatile compound with multiple medical and research applications. Its antimalarial, antipyretic, analgesic, and anti-inflammatory properties make it a valuable drug in the treatment of malaria and other conditions. Additionally, its potential as a potassium channel inhibitor and antiviral agent opens up new possibilities for research and drug development. However, further studies are needed to fully understand its mechanisms of action and to confirm its safety and efficacy in various applications.
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Well-known for its antimalarial properties. It has been used to treat malaria, particularly in cases where other drugs are not effective or cannot be used.
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Besides its anti-malarial activity, it also possesses antipyretic (fever-reducing) and analgesic (pain-relieving) properties. These characteristics make it useful in managing fever and pain associated with malaria and other conditions.
Anti-inflammatory Effects:
Research has shown that exhibits anti-inflammatory activities. This makes it a potential candidate for treating inflammatory conditions, although further studies are needed to confirm its efficacy and safety in such applications.
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Acting as a potassium channel inhibitor, specifically inhibiting the WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses. This property makes it a valuable tool in studying the physiological and pharmacological effects of potassium channels.
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Studies have indicated that can inhibit the proliferation of certain viruses, such as Dengue virus (DENV), in vitro. This suggests its potential use in antiviral research and the development of new antiviral therapies.
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Preliminary research has shown that may have antitumor effects, as it has been observed to reduce tumor size and weight in certain animal models. However, more extensive and in-depth studies are required to confirm its efficacy and safety in cancer treatment.
It may also have applications in other fields, such as chemistry and biochemistry, where its unique properties can be utilized for various research purposes. However, these applications are less common and require further exploration and validation.
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Malaria is a life-threatening disease caused by parasites that are transmitted to humans through the bites of infected female Anopheles mosquitoes. It remains one of the world's most significant public health challenges, particularly in tropical and subtropical regions. The parasites, belonging to the Plasmodium genus, primarily invade red blood cells, leading to symptoms such as fever, chills, and flu-like illness. In severe cases, malaria can cause anemia, cerebral malaria, and respiratory distress, often resulting in death if not treated promptly.
Transmission of malaria is closely linked to environmental factors, including climate, weather, and ecology. Poor sanitation, inadequate housing, and limited access to healthcare exacerbate its spread, especially in rural and underserved communities. The disease disproportionately affects children under five and pregnant women, who are more susceptible to severe complications.
Efforts to combat malaria involve a multifaceted approach, including vector control through the use of insecticide-treated nets and indoor residual spraying, early diagnosis and treatment with effective medications, and preventive measures like vaccination and chemoprevention in high-risk groups. The global community, led by initiatives like the World Health Organization (WHO) and Roll Back Malaria Partnership, is striving to eliminate malaria by reducing incidence and mortality rates drastically.
Continuous research and innovation are crucial for developing new tools and strategies to overcome challenges posed by drug resistance and insecticide resistance in mosquitoes. Collaborative efforts and investments in malaria control are vital to achieving the global health goal of malaria elimination.
The molecular formula of Quinine Hydrochloride Dihydrate is C₂₀H₂₉ClN₂O₄, and its molecular weight is 396.91 g/mol. Its structure consists of a quinoline ring and a quinoline base group. The tertiary amino nitrogen atom of the quinoline base has strong basicity and can form a stable hydrochloride with hydrochloric acid. The presence of the dihydrate form indicates that the molecules are combined with the crystalline water through hydrogen bonds, enhancing its physical stability.
Solubility: At 20℃, the water solubility is 62.5g /L. It is readily soluble in ethanol, glycerol and chloroform, and slightly soluble in ether.
Stability: Sensitive to light, should be stored away from light. The solid state can be stored for 2 years at -20℃, but the stability of the solution state is significantly reduced.
The production of Quinine Hydrochloride Dihydrate is mainly based on the extraction and chemical modification of natural quinine. The core steps include:
Natural quinine is mainly extracted from the bark of the Cinchona spp. The cinchona tree is native to the Andes Mountains in South America and is now widely planted in tropical regions such as Indonesia, India and Congo. The quinine content in the bark is approximately 2% to 8%, and crude products are obtained through solvent extraction or ultrasonic-assisted extraction.
Crude product purification: Impurities are removed through acid-base precipitation, recrystallization or chromatographic separation (such as silica gel column chromatography) to obtain high-purity quinine base.
Hydrochloride formation: Dissolve Quinine base in ethanol or water, slowly add concentrated hydrochloric acid to pH 1-2, stir, cool and crystallize, then filter to obtain Quinine Hydrochloride.
Preparation of dihydrate: By controlling crystallization conditions (such as temperature and humidity), the product combines with crystalline water to form dihydrate.
Continuous crystallization technology: By using a continuous crystallizer to control the particle size distribution of crystals, the uniformity of the product is improved.
Online monitoring: The reaction process is monitored in real time by HPLC or UV-Vis spectroscopy to ensure product quality.
The purity of pharmaceutical-grade products is usually >= 98% (detected by HPLC).
Impurity control: Limit the content of by-products such as dihydroquinine to <= 2%.
Melting point: 115-116℃ (Decomposition)
Moisture content: The content of crystalline water is determined by the Karl Fischer method to ensure the stability of the dihydrate structure.
Potassium channel inhibitory activity: Its inhibitory effect on voltage-gated potassium channels (such as KCa5.1) was verified by electrophysiological experiments (IC₅₀=169 μM).
Traditional antimalarial drugs: used to treat chloroquine-resistant malaria, but gradually replaced by artemisinin derivatives due to side effects (such as hypoglycemia and tinnitus);
Potassium channel modulators: Research on their potential therapeutic value in diseases such as arrhythmia and neuroprotection.
Used for antiviral research (such as inhibiting the replication of dengue virus).
The global market size is approximately 120 million US dollars (data from 2023), with an annual growth rate of about 3%.
The major consumer countries include India, China and the United States, among which India accounts for more than 40% of the demand due to the high incidence of malaria.
The cinchona tree has a long planting cycle (5 to 7 years) and is vulnerable to pests and diseases. It is necessary to explore synthetic biology or cell culture techniques to replace natural extraction.
Develop solvent-free crystallization or enzyme-catalyzed synthesis methods to reduce the use of organic solvents and waste emissions.
Expand its application in fields such as anti-tumor and anti-inflammation;
Prepare targeted delivery systems by integrating nanotechnology to reduce side effects.
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