Tag Archives: Albendazole

ABZEE (Albendazole suspension)

ABZEE (Albendazole suspension)

Indications

Anthelmintic indicated in single or mixed worms infestations including roundworms, hookworms, pinworms, whipworms, threadworms, tapeworms and strongyloides stercoralis. Also in the treatment of hydatid cysts, neurocysticercosis, giardia (duodenalis or intestinalis or lamblia) infections.

Contraindications

Contraindicated inpregnancy. Adequate non-hormonal contraceptive measures must be taken during and for one month after therapy. Also it is contraindicated in patients hypersensitive to the benzimidazole class of compounds.

Side effects and adverse reactions

Albendazole is usually well tolerated and adverse effects occur only in small percentage of patients. The adverse effects are usually mild and transient. They include abdominal pain, diarrhea, headache and dizziness.

Adverse effects have been reported more frequently when high doses are used for the treatment of hydatid disease and neurocysticercosis.

Hematologic: Leukopenia. There have been rare reports of granulocytopenia, pancytopenia, agranulocytosis, or thrombocytopenia.

Dermatologic: rash, urticaria

Hypersensitivity: allergic reactions

Renal: acute renal failure related to albendazole therapy has been observed.

Drug interactions

Dexamethasone: Steady-state trough concentrations of albendazole sulfoxide were about 56% higher when 8 mg dexamethasone was coadministered with each dose of ablendazole (15mg/kg/day) in eight neurocysticercosis patients.

Praziquatel: in the fed state, praziquantel (40mg/kg) increased mean maximum plasma concentration and area under the curve of albendazole sulfoxide by about 50% in helathy subjects compared with a separate group of subjects hiven albendazole alone.

Cimetidine: Albendazole sulfoxide concentrations in bile and cystic fluid were increased about 2-fold) in hydatid cyst patients treated with cimetidine (10mg/kg/day) compared with albendazole (20mg/kg/day) alone.

Theophylline: the pharmacokinetics of theophylline (aminophylline 5.8 mg/kg infused over 20 minutes) were unchanged following a single oral dose of albendazole (400mg) in 6 healthy subjects

Precautions and warnings

Albendazole should not be used during pregnancy and if a patient becomes pregnant while taking this drug, the drug should be discontinued immediately and the patient should be apprised of the potential hazard to the fetus. Women of childbearing age should be cautioned against becoming pregnant while on albendazole or within 1 month of completing treatment.

Albendazole is excreted in animal milk. It is not known whether it is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when albendazole is administered to a nursing woman.

Liver function tests and blood counts before and every two weeks should be performed during high dose therapy for hydatid disease. Experience in children under the age of 6 years is limited. Albendazole should be taken with food.

Rare fatalities associated with the use of albendazole have been reported due to granulocytopenia or pancytopenia.

Patients being treated for neurocysticercosis should receive appropriate steroid and anticonvulsant therapy as required. Oral or intravenous corticosteroids should be considered to prevent cerebral hypertensive episodes during the first week of anticysticeral therapy. Cysticercosis may, in rare cases, involve the retina. Before initiating therapy for neurocysticercosis, the patient should be weighed against the possibilty of retinal damage caused by albendazole-induced changes to the retinal lesion.

Dosage and administration

10 ml (400mg) of Albendazole suspension as a single dose in both adults and children over two years of age. The usual dose in children between on and two years of age is 5 ml (200mg) of albendazole suspension as a single dose. In heavy mixed infestation involving Strongyloides or Taeniasis, a single daily dose may be inadequate and the dose may be given for three consecutive days.

If the patient is not cured after three weeks, a second course of treatment may be given. No special procedures, such as fasting or purging are required.

Albendazole has not been adequately studied in children under one year of age.

For Hydatid disease: 15mg/kg/day divided bid PO for 1-6 months (max: 800mg/day)

For Neurocysticercosis: 15mg/kg/day divided bid PO for 28 days (max: 800mg/day)

For Giardiasis (dose in children over 2 years of age): 400mg daily dose (10ml suspension) for five days

VUMTREX (Levamisole)

VUMTREX (Levamisole)

Levamisole Hydrochloride is an anthelmintic agent, active against intestinal nematode worms. It acts by paralyzing the worms which are then eliminated from the intestines. The paralysis is produced by a ganglion-stimulating effect in the nematodes

Pharmacokinetics

Levamisole is rapidly absorbed from the gastro-intestinal tract and eliminated from the plasma. It is extensively metabolized in the liver by p-hydroxylation. Elimination, mainly of the p-hydroxylated metabolite conjugated with glucoronic acid, is virtually complete via the urine and faeces, within 2 days of a dose.

Indications

Levamisole is very effective against Ascaris lumbricoides (roundworms) where it is considered to be the drug of choice. It is also used in hookworm infections (Ancylostoma duodenale & Necator americanus).

Levamisole has also shown some effect against Enterobius vermicularis (Pinworm, threadworm), Trichuris trichiura (whipworm) and Strongyloides stercoralis.

Dosage: as a single dose

Tablets

Children: 1-5 years: one tablet

                  5-15 years: two tablets

Adults: 3 tablets

Syrup:

Children: 1-5 years: 5ml (one teaspoonful)

                  5-15 years 10ml (two teaspoonfuls)

Adults: 15 ml (three teaspoonfuls)

Side effects

When given as a single dose Levamisole is well tolerated with side effects being limited to gastrointestinal disturbances such as nausea, vomiting and abdominal pain. Dizziness, headaches and skin rash may also occur. Blood disorders like agranulocytosis, neutropenia, leucopenia and thrombocytopenia may occur.

Contraindication

Levamisole is contraindicated in patients with advanced liver or kidney disease and in patients with blood disorders.

WOMIBAN® (Albendazole)

WOMIBAN® (Albendazole)

Albendazole is a broad spectrum antiparasitic that exhibits vemicidal, ovicidal and lavicidal activity in animal and human studies. The results of studies with benzimidazole anthelminitics using sensitive and resistant strains were consistent with tubuline binding being the primary mechanism of action for all drugs in this class

Pharmacokinetics

Albendazole is poorly absorbed from the gastrointestinal tract due to its low aqueous solubility, albendazole concentrations are negligible or undetectable in plasma, as it is readily converted to the sulfoxide metabolite prior to reaching systemic circulation. The systemic antihelmintic activity has been attributed to the primary metabolite-albendazole sulfoxide. Oral bioavailability appears to be enhanced when albendazole is co-administered with a fatty meal, as evidenced by higher plasma concentrations of albendazole-sulfoxide, as compaired to fasted state.

Maximum plasma concentrations (Cmax) of albendazole sulfoxide are typically achieved 2 to 5 hours after dosing and are on average 1.31 mcg/ml (range 0.46 to 1.58 mcg/ml) following oral doses of albendazole (400mg). The mean apparent terminal elimination half-life of albendazole sulfoxide typically ranges from 8-12 hours. Albendazole sulfoxide is widely distributed throughout the body including into the bile and CSF.

Albendazole is rapidly converted in the liver to the primary metabolite, albendazole sulfoxide which is further metabolized to albendazole sulfone and other primary oxidative metabolites that have been identified in human urine. Urinary excretion of albendazole sulfoxide is a minor elimination pathway with less than 1% of the dose recovered in the urine. Biliary elimination presumably accounts for a portion of elimination as evidenced by biliary concentration of albendazole sulfoxide similar to those achieved in plasma. Following single dose administration of 200 to 300 mg (approximately 10mg/kg), in children aged 6 to 13 years with hydatid disease, albendazole sulfoxide pharmacokinetics were similar to those observed in adults.

Indications

Albendazole is effective in the treatment of single and mixed intestinal nematode infestations such as ascariasis, enterobias, ancylostomiasis and trichuriasis. It is also used in treatment of tapeworm infections like Taenia saginata (beef tapeworm), Taenia solium (pork tapeworm) and Hymenolepis nana (dwarf tapeworm). Albendazole is also used in the treatment of Echinococcus granulosus (Hydatid cyst), Neurocysticerosis filariasis, cutaneous larva migrains, toxocariasis and cysticercosis

Contraindications

Womiban (albendazole) is contraindicated in patients with known hypersensitivity to the albendazole class of compounds or any of the components of Womiban

Warnings

Rare fatalities associated with the use of albendazole have been reported due to granulocytopenia or pancytopenia. Blood counts should be monitored at the beginning of 28 days cycle of therapy and every 2 weeks, while on therapy with albendazole. Albendazole should not be used in pregnant women, excerpt in clinical circumstances where no alternative management is appropriate.

“Patient should not become pregnant for at least one month following cessation of albendazole therapy. If a patient becomes pregnant while taking this drug, albendazole should be immediately discontinued”

Precautions

Patients being treated for neurocysticercosis should receive appropriate steroid and anticonvulsant therapy as required.

Pregnancy and lactation

There are no adequate and well-controlled studies of ablendazole administration in pregnant women. Albendazole should be used in pregnancy only if the potential benefits justify the risks to the foetus. Caution should be exercised when albendazole is administered to a nursing mother.

Use in children

No significant problems have been encountered in patients as young as one year when treated with albendazole and the efficacy appears to be similar to adults.

Use in elderly

Experience in patients 65 years of age or older is limited. No problem associated with an older population have been observed.

Side effects

At usual dosages side effects are generally restricted to GI tract such as transient abdominal pain and diarrhea. High doses as in hydatid cyst can cause side effects like allergic reactions, raised liver enzyme values, alopecia, bone marrow depression and raised serum amylase values.

Drug interactions

Albendazole acts on the enzyme cytochrome p450. Hence it may increase the ophylline levels in the blood.

BENPHAM (Albendazole)

Albendazole is a broad-spectrum anthelmintic. Animals and human studies have shown that albendazole exhibits vermicidal, ovicidal and larvicidal activity. The drug is thought to exert its anthelmintic effect by blocking glucose uptake in the susceptible helminthes, thereby depleting the energy level until it becomes inadequate for survival. These events may be a consequence of the binding and subsequent inhibition of parasite tubulin polymerization by albendazole and its metabolites, although the drug also binds to human tubulin

Indications

Albendazole is indicated for use on the following

  1. Hookworm (Ancyclostoma, Necator)
  2. Roundworm (Ascaris)
  3. Threadworm (Enterobius)
  4. Whipworm (Trichuris)
  5. Strongyloides
  6. Tapeworm (Taenia spp)
  7. Opisthorchis
  8. Hydatid disease (Echinococcus)

Contraindications

  • Hypersensitivity
  • Pregnancy

Side effects

Albendazole may create nausea/vomiting, epigastric distress, dizziness, pruritis, dry mouth, diarrhea, leucopenia, agranulocytosis, hypospermia.

Precautions

Hepatorenal impairment, bone marrow depression. Administer within 7 days of the normal menstrual cycle in women of childbearing age. Adequate non-hormonal contraceptive measures must be taken during and for 1 month following the treatment. LFT and blood counts every two months following high dose therapy.

Dosage

Adult: 400mg as single dose in strongyloidiasis; 400mg once daily for 3 consecutive days

Hydatid disease: 400mg twice daily with meals for 28 days. The therapy may be repeated after 14 days intervals for a total of 3 cycles

Children: 1-2 years: 200mg as a single dose

Above 2 years: the same as adult dose

Storage conditions

Store below 30°c in a dry & dark place. Keep out of reach of children.

Resources

WORMOL (Mebendazole)

Mebendazole is a benzimidazole carbamate derivative with broad spectrum anthelmintic activity. It is particularly active against gastro-intestinal nematodes (roundworms) and some cestodes (tapeworms). Activity against some larval stage and ova has also been demonstrated.

It appears to act by irreversible inhibition of glucose uptake in susceptible worms resulting in depletion of their energy stores, glycogen and adenosine triphosphate, resulting in their slow death.

Pharmacokinetics

Mebendazole is poorly absorbed from the gastro-intestinal tract and undergoes extensive first-pass elimination, being metabolized in the liver, eliminated in the bile as unchanged drug and metabolites and excreted in the faeces.

Only about 2% of a dose is excreted unchanged or as metabolites in the urine.

Indications:

Infestation with any of the following and in mixed infections

  • Threadworms (Pinworms, Enterobius vermicularis)
  • Roundworms (Askaris lumbricoides)
  • Whipworm (Trichuris trichiura)
  • Hookworm (Ancylostoma duodenale, Necator americanus)

Dosage

For adult and children over 2 years

  • Threadworm infestations: one tablet to be chewed as a single dose or 5ml (one teaspoonful) of the suspension to be taken as a single dose, repeated if necessary after 2 to 3 weeks
  • Roundworm, Hookworm, Whipworm and mixed infections: one tablet to be chewed twice daily or 5ml of the suspension to be taken twice daily for 3 consecutive days.
Side effects/cautions
  • Nausea, vomiting, abdominal pain, diarrhea and pruritus may occasionally occur.
  • No serious reactions have been reported
  • Use with caution in pregnancy
Contraindications:

Children under two years

Resources

Levamisole: Anthelminthic agent

Group: anthelminthic agent
Tablet 40 mg, 50 mg (as hydrochloride)
Syrup 40 mg/5 ml

General information

Levamisole, the (-)-isomer of tetramisole, acts by paralysing the musculature of susceptible nematodes. Unable to maintain their anchorage, the worms are ejected by normal peristaltic action, usually within 24 hours.


Levamisole is rapidly and almost completely absorbed from the gastrointestinal tract. Peak plasma concentrations occur within 2 hours and the plasma half-life is about 4 hours. It is extensively metabolized in the liver and is excreted in the urine as metabolites and unchanged drug.

Levamisole is used with another cancer medicine (fluorouracil) to help make it work better against cancer of the colon.

Levamisole is available only with your doctor’s prescription.

Dosing

The dose of levamisole will be different for different patients. Follow your doctor’s orders or the directions on the label. The following information includes only the average doses of levamisole. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

Missed Dose

If you miss a dose of levamisole, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Levamisole

(-)-(S)-2,3,5,6-tetrahydro-6-phenylimidazol[2,1-b]thiazole].

Clinical applications

Levamisole, the levorotatory and biologically active isomer of the racemic tetramisole, was discovered by Janssen Pharmaceutica in 1966 and developed as a broad-spectrum anthelmintic for use in a variety of mammalian and avian species. While widely used as an antiparasitic agent in ruminants, with a number of immunomodulatory uses still under development in humans and other species, levamisole has not found wide application as an anthelmintic in dogs and cats, principally because of the narrow therapeutic index.

Pharmacodynamics

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.

Mechanism of action

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.

Levamisole Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Less common

  • Fever or chills
  • unusual feeling of discomfort or weakness

Rare

  • Black, tarry stools
  • blood in urine or stools
  • cough or hoarseness
  • lower back or side pain
  • painful or difficult urination
  • pinpoint red spots on skin
  • unusual bleeding or bruising

Check with your doctor as soon as possible if any of the following side effects occur:

Less common

  • Sores in mouth and on lips

Rare

  • Blurred vision
  • confusion
  • convulsions (seizures)
  • lip smacking or puffing
  • numbness, tingling, or pain in face, hands, or feet
  • paranoia (feelings of persecution)
  • puffing of cheeks
  • rapid or worm-like movements of tongue
  • trembling or shaking
  • trouble in walking
  • uncontrolled movements of arms and legs

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Diarrhea
  • metallic taste
  • nausea

Less common

  • 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

Levamisole may cause a temporary loss of hair in some people. After treatment has ended, normal hair growth should return.

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Interactions
Albendazole: The bioavailability of Albendazole can be increased when combined with Levamisole

Ivermectin: The bioavailability of Ivermectin can be increased when combined with Levamisole.

Food Interactions

·  Take on an empty stomach.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

References

·         https://www.drugbank.ca/drugs/DB00848

·         https://www.drugs.com/cons/levamisole.html

·        http://apps.who.int/medicinedocs/en/d/Jh2922e/3.2.2.html

·        https://www.sciencedirect.com/topics/neuroscience/levamisole

  •      Stephen W Page, in Small Animal Clinical Pharmacology (Second Edition), 2008
  •      Anahid Jewett, Han-Ching Tseng, in Pharmacology and Therapeutics for Dentistry (Seventh Edition), 2017

·  P.J.J. van Genderen, in Side Effects of Drugs Annual, 2009

· P.J.J. van Genderen, in Side Effects of Drugs Annual, 2008

·          

Identification of Patients with Ascariasis

Identification of Patients with Ascariasis

Ascariasis: is one of the commonest infections of the small intestine. Caused by a nematode called Ascaris lumbricoides ( round worm) 

Mode of Transmission of Ascariasis

• Common ways of acquiring ascariasis include failure to adhere to hygienic practices such as washing hands before food preparation and proper storage of food.
• Therefore the disease is related to poor sanitation and hygiene.
• Infection is acquired from ingestion of food contaminated with mature eggs
• The usual vehicles are fruits and other raw food
• Children are more frequently infected and have higher worm burden than adults because they like putting contaminated objects into their mouths
• Heavy infection in children can contribute to under-nutrition.
• Adults have much lighter infections, although re-infection can occur throughout life.

Signs and Symptoms of Ascariasis

• Fever
• Cough
• Abdominal discomfort, restlessness and insomnia (sleeplessness)
• Eosinophilia due to allergic reaction
• Intestinal obstruction
• Passing adult worm in the stool or vomitus
• Obstructive jaundice

Treatment of Ascariasis

• Treatment is effective only against the adult worms.
• The drugs of choice are as follows:

o Albendazole: for children 2-5 years a single dose of 200mg and for older children and adults, one dose of 400mg is given.

o Mebendazole: a single dose 500mg.

o Levamisole: a single of 2.5mg/kg body weight.

o Piperazine (antepar): syrup at a dose of 150mg/kg body weight (to a maximum of 4g) as a single dose.

Note that these drugs are given between meals . They should be avoided during the first three months of pregnancy.

Prevention and Control of Ascariasis 

• Environmental measures such as provision of adequate and safe water supplies. Proper disposal of faeces 

• prevention of faecal contamination of food and water Discourage use of fresh  human faeces as manure 

• Health education on: 

o Proper use of latrines o Personal hygiene e.g. washing hands after using toilet or before handling food 

o Washing fruits and vegetables before eating 

o Use of dry racks for utensils so that they are above the soil and dust 

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