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Levamisole

Levamisole: Know How To Use Safely&Effectively

Levamisole, also named levamisole hydrochloride. It is a drug for removing intestinal worms and regulating biological reactions, and also for roundworm, hookworm, pinworm, and strongylodiasis of faecalis. (–)-Levamisole (hydrochloride) (Item No. 14874) is an analytical reference material categorized as imidazothiazole. It is used as a cutting agent with cocaine, and levamisole-adulterated cocaine has led to cutaneous vasculopathy in some individuals. This product is intended for research and forensic applications.

(This term is approved by the National Administration of Traditional Chinese Medicine)

English nameLevamisole
Chinese nameZuoxuanmizuo
Drug typeAntienteric insect medicine, biological reaction regulation medicine
Prescription typePrescription drugs
Levamisole

Composition

  • The main ingredient of this product is levamisole hydrochloride.

Character

  • Levamisole hydrochloride tablets: white tablets or sugar-coated tablets, white after removing the coating.
  • Levamisole hydrochloride particles: soluble particles.
  • Levamisole hydrochloride syrup: brown clear viscous liquid; Taste sweet.
  • Levamisole hydrochloride pagoda sugar: tower sugar with crepe.
  • Levamisole hydrochloride liniment: colorless or light yellow clear liquid, with a slight alcohol taste.

Indications

Levamisole Hydrochloride tablets/Levamisole hydrochloride granules/Levamisole hydrochloride syrup/Levamisole hydrochloride pagoda sugar:

  • It has a good effect on roundworm, hookworm, pinworm, and strongylodiasis of faecalis. Because of its highly effective rate in a single dose, it is suitable for group therapy. The activity against adult and microfilariae of Filariae banneri, Filariae Maleae, and onchocerae was higher than that of ethamizine, but the long-term efficacy was poor.

Levamisole hydrochloride liniment:

  • A variety of immune disorders and immune disorders can use it, such as recurrent upper respiratory tract infections, allergic asthma, allergic rhinitis, chronic hepatitis b, hepatitis b virus carriers, recurrent oral mucosa ulcer, malignant tumor, rheumatoid arthritis, and human papillomavirus infection caused by the wart class immune treatment of skin diseases.

Specifications

  • Levamisole hydrochloride tablets: 25mg; 50 mg.
  • Levamisole hydrochloride particles: 10g: 50mg.
  • Levamisole hydrochloride syrup: 10ml: 20mg.
  • Levamisole hydrochloride pagoda sugar: 15mg.
  • Levamisole hydrochloride liniment: 5ml: contains 500mg Levamisole hydrochloride.

Usage

Levamisole Hydrochloride tablets/Levamisole hydrochloride granules/Levamisole hydrochloride syrup/Levamisole hydrochloride pagoda sugar:

  • Smoke insect repellent: orally, adults 15-25mg/kg, fasting or bedtime take, children dosage 2-3mg/kg.
  • Hookworm repellent: orally, 1.5-25mg/kg, once a night, for 3 days.
  • The treatment of filariasis: 4-6mg/kg, divided into 2-3 times, continuous for 3 days.

Levamisole hydrochloride liniment:

  • For external use: open the seal of the bottle and gently squeeze the liquid. Apply it to the skin of the legs, upper arms, or abdomen with drops, one dose (5ml) each time for adults, once every other day or twice a week; The best dose for children is 10mg/KG of body weight. Use tongs to clamp the remaining liquid for next time reuse. For hepatitis B, 6 months of free treatment is a course of treatment, and for other diseases, 2-3 months of immunotherapy is a course of treatment, or as prescribed by the doctor.

Chemical usage

  • These secondary standards are qualified certification reference substances. These are suitable for several analytical applications, including but not limited to drug release testing, drug method development for qualitative and quantitative analysis, food and beverage quality control testing, and other calibration requirements.
  • Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
  • It has both immune stimulation and immune suppression. It is very effective in treating roundworm disease (hookworm infection). Useful in chemotherapy for colorectal cancer, probably due to its stimulation of IL-1 production and direct activation of macrophages.
Levamisole

Clinical application and guidelines

  • Yuanqiang Lu studied the efficacy of levamisole combined with low-dose cyclosporine in the treatment of non-severe aplastic anemia and obtained the results that the levels of neutrophils, platelets, and hemoglobin and the total clinical response rate in the study group were significantly higher than those in the control group. ([A]. The Editorial Department of International Laboratory Medicine, Chongqing Health Information Center: 2018 International Journal of Laboratory Medicine annual conference proceedings [C]. Editorial Department of International Laboratory Medicine Press, Chongqing Health Information Center: Editorial Department of International Laboratory Medicine Press,2018:2.)
  • Yanfei Lin, Qin Zhang, and Fangfang Gao concluded that levamisole hydrochloride can improve the immune capacity of immunocompromised mice by studying the effects of Levamisole hydrochloride on the immune function of immunocompromised mice. ([J]. Food & drug science,2018,20(06):460-464.)

Adverse reaction

  • Generally mild. Side effects include nausea, vomiting, abdominal pain, taste disturbance, fatigue, dizziness, headache, joint pain, disturbance of consciousness, insomnia, fever, influenza-like disease group, hypotension, vasculitis, rash, photosensitive dermatitis, etc. Occasionally see proteinuria, individual visible granulocytopenia, thrombocytopenia, a few even appear granulocytopenia (often reversible). It often occurs in patients with rheumatoid tumors and can also cause transient hairstyle and Arthus allergic reactions, possibly atopic responses caused by stimulation of T cells. In individual cases, ataxia, paresthesia, or blurred vision may occur.
  • Occasionally, there are local allergic phenomena such as rash and itchy skin, which can disappear after stopping the drug.

Prohibited persons

  • Liver and kidney function, hepatitis activity period, early pregnancy, or schistosomiasis.

Matters needing attention

  • It is easy to induce granulocytosis in patients with rheumatoid arthritis after taking this product.
  • Use with caution in patients with Sjogren’s syndrome.
  • Rheumatoid arthritis and Sjogren’s syndrome patients when treated with this product, the first week use 50 mg per day, the second week for 100 mg daily, and after the third week for 150 mg daily. Most of these patients have side effects, such as erythema papula, arthralgia aggravated with swelling, muscle pain, flu disease) group, insomnia, a disorder of the mind. But after attacking the amount, the symptoms can reappear.

Levamisole hydrochloride liniment:

  • Clean the skin of the applicator area (scrub with a warm and wet towel), and apply the applicator after it is good for transdermal absorption.
  • Do not touch water for 24 hours after applying for the medicine.
  • It is easy to irritate the skin by keeping the product on the skin for a long time. It is recommended to clean the product within 48 hours after application.
  • If there are symptoms such as local skin itching and another drug dermatitis after using, stop the medicine and apply dermatitis cream to relieve itching. Then it can be resolved by itself.
  • When the character of the product changes, it is prohibited to use.
Levamisole

Drug interaction

  • When combined with a pyrimidine, it can treat severe hookworm infection and improve the effect of expelling Necator americanus.
  • Combination with thiabendazole can treat mixed infections of intestinal nematodes.
  • Sequential application with ethylamine citrate can treat filariasis infection.
  • Should not be used with tetrachloroethylene, so as not to increase its toxicity.
  • It can enhance the anticoagulant double coumarin pharmacological action.
  • Similar to alcohol sulfur when used with alcohol.
  • When taken with phenytoin, the blood concentration of the latter can be improved.

Pharmacokinetics

Levamisole hydrochloride tablets, Levamisole hydrochloride granules, Levamisole hydrochloride syrup, Levamisole hydrochloride pagoda sugar:

  • It will quickly absorb after oral administration. Peak blood concentration can achieve 50mg/ml within 2 hours after 150mg administration. And T1/2 is metabolized in the liver for 4 hours. This product and its metabolites can be excreted from urine (most), faeces, and the respiratory tract, which can also be detected in milk.

Levamisole hydrochloride liniment:

  • It can be absorbed through the skin. After about 20 hours, it can reach the steady-state blood concentration and maintain the effective concentration of immune regulation for more than 36 hours.

Storage

  • Keep sealed in a cool dry place.

Execution standard

  • Levamisole Hydrochloride tablets: Chinese Pharmacopoeia 2010 Edition II.
  • Levamisole hydrochloride granules: Chinese Pharmacopoeia 2015 Edition II.
  • Levamisole Hydrochloride syrup: Chinese Pharmacopoeia 2015 Edition II.
  • Levamisole hydrochloride pagoda sugar: Issued by the Ministry of Health standard Part II, Volume II.
  • Levamisole hydrochloride liniment: State Food and Drug Administration National Drug Standard WS1-XG–016-2000.

Levamisole hydrochloride Basic information

Product Name:Levamisole hydrochloride
Synonyms:1-b)thiazole,2,3,5,6-tetrahydro-6-phenyl-,monohydrochloride,(s)-imidazo(;1-b)thiazole,2,3,5,6-tetrahydro-6-phenyl-,monohydrochloride,l-(-)-imidazo(;1-b]thiazole,2,3,5,6-tetrahydro-6-phenyl-,monohydrochloride,(S)-Imidazo[2;citarinl;decaris;Imidazo[2,1-b]thiazole,2,3,5,6-tetrahydro-6-phenyl-,monohydrochloride,(S)-;kw-2-le-t;L-2,3,5,6-Tetrahydro-6-phenylimidazo-[2,1-6]-thiazole
CAS:16595-80-5
MF:C11H13ClN2S
MW:240.75
EINECS:240-654-6
Mol File:16595-80-5.mol

Levamisole hydrochloride Chemical Properties

Melting point 266-267 °C(lit.)
alpha -128 º (c=5, H2O)
refractive index -126 ° (C=1, H2O)
Fp 9℃
storage temp. 2-8°C
solubility Freely soluble in water, soluble in ethanol (96 per cent), slightly soluble in methylene chloride.
form Crystalline Powder
color White to almost white
Water Solubility 210 g/L (20 ºC)
Merck 14,5459
BRN 4358988
InChIKeyLAZPBGZRMVRFKY-HNCPQSOCSA-N
CAS DataBase Reference16595-80-5(CAS DataBase Reference)
EPA Substance Registry SystemLevamisole hydrochloride (16595-80-5)

Acquisition path

  • Hubei Amarvel Biotech Co.Ltd is committed to the production of pharmaceutical intermediates, which can provide high purity and good quality raw materials. If your company wants to purchase some legal raw materials, please browse this page and consult us.

Reference

  • [A]. The Editorial Department of International Laboratory Medicine, Chongqing Health Information Center: 2018 International Journal of Laboratory Medicine annual conference proceedings  
  • [C]. Editorial Department of International Laboratory Medicine Press, Chongqing Health Information Center: Editorial Department of International Laboratory Medicine Press,2018:2.
  • [J]. Food & drug science,2018,20(06):460-464.

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