Levamisole
Levamisole Uses, Dosage, Side Effects, Food Interaction and all others data.
Levamisole is the active laevo-isomer of tetramisole. It works by paralysing susceptible intestinal worms which are then excreted from the intestines. Levamisole also enhances cellular immune responses in humans.
Levamisole is a synthetic imidazothiazole derivative that has been widely used in treatment of worm infestations in both humans and animals. As an anthelmintic, it probably works by targeting the nematode nicotinergic acetylcholine receptor. As an immunomodulator, it appears that Levamisole is an immunostimulant which has been shown to increase NK cells and activated T-cells in patients receiving this adjuvantly along with 5FU for Stage III colon cancer.
| Trade Name | Levamisole |
| Availability | Discontinued |
| Generic | Levamisole |
| Levamisole Other Names | Levamisol, Levamisole, Levamisolum |
| Related Drugs | Keytruda, carboplatin, capecitabine, pembrolizumab, fluorouracil, doxorubicin, cyclophosphamide, Avastin, Xeloda, vincristine |
| Weight | 40mg, 40mg/5ml, |
| Type | Tablet, Syrup, Oral |
| Formula | C11H12N2S |
| Weight | Average: 204.291 Monoisotopic: 204.072119084 |
| Protein binding | 20-25% |
| Groups | Approved, Investigational, Vet approved, Withdrawn |
| Therapeutic Class | Anti-helminthic |
| Manufacturer | Essential Drugs Company Ltd |
| Available Country | Bangladesh, United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Levamisole is a fast acting drug which acts on nematode nerve ganglia paralysing the worm’s musculature within seconds of contact. Unable to maintain their position, the worms are then ejected by normal peristaltic movement, usually within 24 hours of levamisole administration. Although it is certain that levamisole primarily influences the neuromuscular system of nematodes, it is possible that in some helminthes the inhibition of the fumarate reductase system contributes to the anthelmintic efficacy of levamisole. Levamisole is used for the treatment of infections by the following gastrointestinal wormspecies:
- Ascaris lumbricoides: Roundworm
- Necator americanus: Hookworm
- Ancylostoma duodenal: Hookworm
- E nterobius vermicularis: Pinworm
- Trichuris trichuria: Whipworm
- Strongyloides stercoralis: Threadworm
- Trichostrongylus colubriformis
Levamisole is also used to associated treatment for these conditions: Adenocarcinoma of Colon, Ancylostoma duodenale infection, Ascaris lumbricoides infection, Carcinoma, Colorectal, Enterobius vermicularis infection, Necatoriasis due to necator americanus, Strongyloides Stercoralis Infection, Trichuris Infection
How Levamisole works
The mechanism of action of levamisole as an antiparasitic agent appears to be tied to its agnositic activity towards the L-subtype nicotinic acetylcholine receptors in nematode muscles. This agonistic action reduces the capacity of the males to control their reproductive muscles and limits their ability to copulate. The mechanism of action of Levamisole as an anticancer drug in combination with fluorouracil is unknown. The effects of levamisole on the immune system are complex. The drug appears to restore depressed immune function rather than to stimulate response to above-normal levels. Levamisole can stimulate formation of antibodies to various antigens, enhance T-cell responses by stimulating T-cell activation and proliferation, potentiate monocyte and macrophage functions including phagocytosis and chemotaxis, and increase neutrophil mobility, adherence, and chemotaxis.
Dosage
Levamisole dosage
The following doses of Levamisole are given as a single administration, preferably after a light meal.
- Age 1-4 year: 1 Tablets or5 mlSyrup
- Age 5-15 year: 2 Tablets or10 mlSyrup
- Age 16year and over: 3 Tablets or 15 mlSyrup
In cases of severe hookworm infection it is suggested that a second standard dose be given one or seven days after the first, whichever timing is feasible.
Side Effects
Side-effects are infrequent. They are usually mild and transient and include nausea, vomiting, abdominal pain, giddiness(dizziness) and headache. An encephalopathylike syndrome has been reported to have occurred in a few patients two or three weeks after treatment.
Toxicity
LD50 = 40 mg/kg (Pigs, subcutaneous); LD50 = 180 mg/kg (rat, oral)
Precaution
Effect on ability to drive or operate machinery: There is no evidence to suggest that Levamisole , used for anthelmintic purpose, will produce sedation. Mild and transient giddiness is an infrequent side-effect of treatment. No precautions are suggested concerning the ability to drive or operate machinery.
In case of concurrent microfilaraemia transient fever may occur.
Interaction
May increase toxicity of phenytoin. Increases bioavailability of ivermectin; decreases bioavailability of albendazole. Alcohol causes disulfiram-like reaction.
Food Interaction
- Take on an empty stomach.
Levamisole Alcohol interaction
[Moderate] GENERALLY AVOID:
Case histories have suggested that levamisole is associated with some side effects (including headache, fever, shivers, and dizziness) that suggest an disulfiram-like interaction with alcohol.
These side effects could be alleviated by total abstinence from alcohol.
No mechanism has been established for this interaction.
Patients receiving levamisole should avoid alcohol.
Levamisole Drug Interaction
Unknown: 5-hydroxytryptophan, charcoal, acetaminophen, aspirin, diphenhydramine, sucralfate, loratadine, dehydroepiandrosterone, diltiazem, doxycycline, multivitamin with iron, multivitamin, lysine, levothyroxine, atropine / diphenoxylate, metoprolol, acetaminophen, bioflavonoids, quetiapine, itraconazole
Elimination Route
Levamisole is rapidly absorbed (2 hours) from the gastrointestinal tract.
Half Life
4.4-5.6 hours (biphasic)
Pregnancy & Breastfeeding use
Although studies in animals have shown that Levamisole produces no teratogenic effects, current medical practice requires that the benefits of any drug used during pregnancy should be weighed against the possible dangers.
Contraindication
There is no absolute contra-indication to the use of Levamisole
Acute Overdose
Counter possible anticholinesterase activity with e.g. atropine. Control blood pressure and respiration . Do not use sedatives.
Storage Condition
Tablet: Store in room temperature and protect from moisture.
Syrup: Store in room temperature and protect from light.
Innovators Monograph
You find simplified version here Levamisole
FAQ
What is Levamisole used for?
Levamisole is a medication used to treat parasitic worm infections, specifically ascariasis and hookworm infections. Levamisole is an immunomodulatory agent that was used to treat various cancers before being withdrawn from the United States market in 2000 because of adverse effects.
Is Levamisole safe for humans?
Although not available for human use, Levamisole remains widely used in veterinary medicine for treating worms in livestock and domesticated animals. The Levamisole can cause agranulocytosis, as well as vasculitis, which prompted the FDA ban on human use.
Is Levamisole toxic?
Toxicity of Levamisole is generally described as mild with nausea, diarrhea, and leukopenia being the most significant adverse effects with fatigue, dermatitis, and stomatitis also seen.
How does Levamisole work?
Levamisole works by suppressing the enzyme activity in the muscle of the worm, causing paralysis and death.
What are the common side effects of Levamisole?
- Metallic taste
- Nausea Anxiety or nervousness
- Dizziness
- Headache
- Mental depression
- Nightmares
- Pain in joints or muscles
- Skin rash or itching
- Trouble in sleeping
- Unusual tiredness or sleepiness
- Vomiting
- Blurred vision
- Confusion
- Convulsions (seizures)
- Lip-smacking or puffing
- Numbness, tingling, or pain in the face, hands, or feet
- Paranoia (feelings of persecution)
- Puffing of cheeks
- Rapid or worm-like movements of the tongue
- Trembling or shaking
- Trouble in walking
- Uncontrolled movements of arms and legs
Common side effects of Levamisole are include:
Is Levamisole safe during pregnancy?
Animal studies have revealed evidence of embryotoxicity. There are no controlled data in human pregnancy. Levamisole should only be given during pregnancy when benefit outweighs risk.
Is Levamisole safe during breastfeeding?
The World Health Organization recommends against breastfeeding with maternal Levamisole therapy.
Can I drink alcohol with Levamisole?
You should avoid drinking alcohol, it can increase some of the side effects of Levamisole. This can cause nausea, dizziness, vomiting, and upset stomach. It is important to tell your doctor about all other medications you use, including vitamins and herbs.
Can I drive after taking Levamisole?
Some people may feel dizzy or tired while taking this medicine. Do not drive unless you are feeling well.
How do I take Levamisole?
Levamisole has been prescribed to treat a variety of parasitic worm infections. It ought to be taken with food. Do not crush or chew or break the tablet. Swallow the whole thing with a full glass of wate.
How much Levamisole should I take?
The recommended dose is 150mg/day, in 3 equally divided doses, by mouth for 3 days. Maintenance- three-day course every two weeks for a year.
How long does it take Levamisole to work?
Levamisole is readily absorbed from the gastrointestinal tract and metabolized in the liver. Its time to peak plasma concentration is 1.5–2 hours.
How long does Levamisole stay in my system?
The plasma elimination half-life is fairly quick at 3–4 hours which can contribute to not detecting Levamisole intoxication. The metabolite half-life is 16 hours. Levamisole excretion is primarily through the kidneys, with about 70% being excreted over 3 days.
Can I take Levamisole for a long time?
Do not take more or less of it, and do not take it more often than your doctor ordered. The exact amount of medicine you need has been carefully worked out.
How much Levamisole should I take?
Maintenance- three-day course every two weeks for a year.
Who should not take Levamisole?
Patients who have a reported allergy to any of the other ingredients in Levamisole should stop taking it. In addition, patients with asthma should avoid using Levamisole.
What happens if I miss a dose?
If you miss a dose of Levamisole, skip the missed dose and go back to your regular dosing schedule. Do not double doses. Call your doctor or pharmacist for instructions.
What happen if I take too much Levamisole?
Taking too much may increase the chance of side effects, while taking too little may not improve your condition. If you vomit shortly after taking a dose of Levamisole, check with your doctor. You will be told whether to take the dose again or to wait until the next scheduled dose.
Can Levamisole affects my heart?
With a view to cardiac function, Levamisole can cause right heart failure. Furthermore, effects on heart rate have been observed including severe bradycardia, tachycardia and ventricular fibrillation, as well as cardiac dysrhythmias.
Can Levamisole affect my kidney?
Levamisole laced Cocaine Led to ANCA Vasculitis and Kidney Damage.
