Ivermectol
Ivermectol Uses, Dosage, Side Effects, Food Interaction and all others data.
Ivermectol selectively binds and with high affinity to glutamate-gated chloride ion channels, which occur in invertebrate nerve and muscle cells leading to an increase in the permeability of cell membranes to chloride ions with hyperpolarization of the nerve or muscle cell and, ultimately, death of the parasite.
Ivermectol is a semisynthetic, anthelminitic agent. It is an avermectin which a group of pentacyclic sixteen-membered lactone (i.e. a macrocyclic lactone disaccharide) derived from the soil bacterium Streptomyces avermitilis. Avermectins are potent anti-parasitic agents. Ivermectol is the most common avermectin. It is a broad spectrum antiparasitic drug for oral administration. It is sometimes used to treat human onchocerciasis (river blindness). It is the mixture of 22,23-dihydro-avermectin B1a (at least 90%) and 22,23-dihydro-avermectin B1b (less than 10%).
| Trade Name | Ivermectol |
| Availability | Prescription only |
| Generic | Ivermectin |
| Ivermectin Other Names | Ivermectin, Ivermectina, Ivermectine, Ivermectinum |
| Related Drugs | albendazole, Albenza, Stromectol, moxidectin, Mintezol |
| Type | Tablet |
| Formula | C95H146O28 |
| Weight | Average: 1736.1589 Monoisotopic: 1735.000064088 |
| Protein binding | 93% |
| Groups | Approved, Investigational, Vet approved |
| Therapeutic Class | Anti-helminthic |
| Manufacturer | Sun Pharma, Ranbaxy Laboratories (sun Pharma) |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Ivermectol is used for the treatment of the following infections:
Strongyloidiasis of the intestinal tract. Ivermectol is used for the treatment of intestinal (i.e., nondisseminated) strongyloidiasis due to the nematode parasite Strongyloides stercoralis.
This indication is based on clinical studies of both comparative and open-label designs, in which 64-100% of infected patients were cured following a single 200-mcg/kg dose of ivermectin.
Onchocerciasis: Ivermectol is used for the treatment of onchocerciasis due to the nematode parasite Onchocerca volvulus.
This indication is based on randomized, double-blind, placebo-controlled and comparative studies conducted in 1427 patients in onchocerciasis-endemic areas of West Africa. The comparative studies used diethylcarbamazine citrate (DEC-C).
NOTE: Ivermectol has no activity against adult Onchocerca volvulus parasites. The adult parasites reside in subcutaneous nodules which are infrequently palpable. Surgical excision of these nodules (nodulectomy) may be considered in the management of patients with onchocerciasis, since this procedure will eliminate the microfilariae-producing adult parasites.
Ivermectol is also used to associated treatment for these conditions: Acne Rosacea, Ascaris lumbricoides infection, Cutaneous larva migrans, Demodicidosis, Gnathostomiasis, Mansonella ozzardi infection, Mansonella streptocerca infection, Oesophagostomiasis, Onchocerciasis, Pediculosis Capitis, Scabies, Trichuriasis, Wuchereria bancroftii infection
How Ivermectol works
Ivermectol binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate muscle and nerve cells of the microfilaria. This binding causes an increase in the permeability of the cell membrane to chloride ions and results in hyperpolarization of the cell, leading to paralysis and death of the parasite. Ivermectol also is believed to act as an agonist of the neurotransmitter gamma-aminobutyric acid (GABA), thereby disrupting GABA-mediated central nervous system (CNS) neurosynaptic transmission. Ivermectol may also impair normal intrauterine development of O. volvulus microfilariae and may inhibit their release from the uteri of gravid female worms.
Dosage
Ivermectol dosage
Oral
Filariasis:
- Adult: Dosing regimen depends on the causative agent. Mansonella streptocerca 150 mcg/kg as a single dose; Mansonella ozzardi 200 mcg/kg as a single dose.
- Child: ≥15 kg: Dosing regimen depends on the causative agent. Mansonella streptocerca 150 mcg/kg as a single dose; Mansonella ozzardi 200 mcg/kg as a single dose.
Scabies:
- Adult: Sarcoptes scabiei 200 mcg/kg as a single dose, repeat dose in 2 wk.
- Child: ≥15 kg: Sarcoptes scabiei 200 mcg/kg as a single dose, repeat dose in 2 wk.
Onchocerciasis:
- Adult:150 mcg/kg as a single dose; retreatment may be given every 6-12 mth until adult worms die.
- Child: >5 yr and ≥15kg: 150 mcg/kg as a single dose every 6-12 mth until adult worms die.
Ascariasis:
- Adult: Ascaris lumbricoides 150-200 mcg/kg as a single dose.
- Child: ≥15 kg: Ascaris lumbricoides 150-200 mcg/kg as a single dose.
Strongyloidiasis:
- Adult: 200 mcg/kg as a single dose for 1-2 days.
- Child: >15 kg: 200 mcg/kg as a single dose for 1-2 days.
Gnathostomiasis:
- Adult: Gnathostoma spinigerum: 200 mcg/kg once daily for 2 days.
- Child: ≥15 kg: Gnathostoma spinigerum: 200 mcg/kg once daily for 2 days.
Should be taken on an empty stomach.
Side Effects
Diarrhoea, nausea, vomiting, dizziness, pruritus, urticaria, rash, arthralgia, fever, myalgia, asthenia, postural hypotension, tachycardia, oedema, lymphadenopathy, sore throat, cough, headache, somnolence, transient eosinophilia, raised liver enzyme values.
Toxicity
LD50 = 29.5 mg/kg (Mouse, oral). LD50 = 10 mg/kg (Rat, oral). Adverse effects include muscle or joint pain, dizziness, fever, headache, skin rash, fast heartbeat.
Precaution
Concurrent Loa loa infection, impaired blood-brain barrier function due to infection.
Interaction
Bioavailability may be increased by alcohol, levamisole.
Food Interaction
- Take on an empty stomach.
Ivermectol Alcohol interaction
[Moderate] GENERALLY AVOID:
Alcohol may increase the plasma concentrations of ivermectin.
The mechanism of interaction is unknown.
In 20 healthy, nonsmoking patients with onchocerciasis, mean plasma ivermectin concentrations at 1, 3 and 4 hours post-dose (150 mcg/kg) were approximately 34% to 40% higher in the group given the medication with 750 mL of beer (4.5% v/v alcohol) than in controls who ingested the medication with water.
There were no side effects in either study or control subjects.
However, there have been anecdotal reports of increased central nervous system adverse effects and postural hypotension in patients who combined ivermectin with alcohol.
Patients receiving ivermectin therapy should preferably avoid the consumption of alcohol to prevent any undue adverse effects of ivermectin.
Ivermectol Drug Interaction
Unknown: diphenhydramine, diphenhydramine, ubiquinone, ubiquinone, acetylcysteine, acetylcysteine, bioflavonoids, bioflavonoids, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, zinc sulfate, zinc sulfate, cetirizine, cetirizine
Volume of Distribution
The volume of distribution is 3 to 3.5 L/kg and it does not cross the blood-brain barrier.
Elimination Route
Moderately well absorbed. Improved absorption with high fat meal.
Half Life
16 hours (also reported at 22-28 hours)
Elimination Route
Ivermectol is metabolized in the liver, and ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1% of the administered dose excreted in the urine.
Pregnancy & Breastfeeding use
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindication
Hypersensitivity. Pregnancy and lactation. Children <15 kg body weight.
Storage Condition
Store below 30°C.
Innovators Monograph
You find simplified version here Ivermectol
Ivermectol contains Ivermectin see full prescribing information from innovator Ivermectol Monograph, Ivermectol MSDS, Ivermectol FDA label
FAQ
What is Ivermectol used for ?
Ivermectol is an anti-parasite medication used to treat parasitic diseases. Ivermectol is used to prevent and treat heartworm and acariasis, among other indications.
How safe is Ivermectol?
Ivermectol is considered safe for use in humans when used in normal doses. But it's still possible to experience side effects while taking this medication.
How to use Ivermectol?
Take Ivermectol by mouth with a full glass of water on an empty stomach at least 1 hour before a meal. Ivermectol is usually taken as a single dose or series of doses, or as directed by your doctor.
What are the common side effects of Ivermectol?
Common side effects of Ivermectol are include:
- tiredness
- loss of energy
- stomach pain
- loss of appetite
- nausea
- vomiting
- diarrhea
- dizziness
- sleepiness or drowsiness
- itchiness
Is Ivermectol safe during pregnancy?
The risk versus benefit should be considered in pregnant women heavily infected with parasites, especially during mass distribution of Ivermectol in endemic areas. The advantage of treatment may outweigh any potential risk to the infant.
Is Ivermectol safe during breastfeeding?
Ivermectol is excreted into human milk in low concentrations. The manufacturer recommends that treatment during nursing only occur if the risk of delayed treatment to the mother outweighs the possible risk to the infant. One review article recommends the use of ivermectin in lactating women after the infant is 7 days old.
Can I drink alcohol with Ivermectol?
Using alcohol with Ivermectol can increase the blood levels or add to the side effects of Ivermectol.
Can I drive after taking Ivermectol?
Do not drive or operate heavy machinery until you know how this medication affects you.
How does Ivermectol work?
Ivermectol work by paralysing the parasite or inactivating the parasite gut.
How long does Ivermectol take to work ?
Ivermectol should take effect within 1 to 2 hours.
Should I take Ivermectol morning or night?
Ivermectol is best taken as a single dose with a full glass of water on an empty stomach (1 hour before breakfast), unless otherwise directed by your doctor.
Does Ivermectol affect blood pressure?
You can also overdose on Ivermectol, hypotension (low blood pressure).
Is Ivermectol hard on the kidneys?
Ivermectol can cause glomerular and tubular disturbances in patients with onchocerciasis; however, these are minor and do not seem to be clinically relevant.
Does Ivermectol raise blood sugar?
Ivermectol displays antidiabetic activities by reducing blood glucose and cholesterol levels, and also by improving insulin sensitivity in an FXR-dependent manner.
Who should not take Ivermectol?
You will need to have a stool exam after taking Ivermectol to make sure the infection is gone. Some patients may need to take another dose of Ivermectol to treat the infection. Ivermectol may make you feel dizzy. To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
What happens if I miss a dose?
Since Ivermectol is usually given in a single dose, you may not be on a dosing schedule. If you are on a schedule, take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
What happens if I overdose?
Seek emergency medical attention.
How long does Ivermectol stay in my system?
barnd starts to leave your bloodstream after about 18 hours, but it stays in your intestines and continues to kill any worms there for 12 days.
Does cause hair loss?
A lack of these nutrients can contribute to hair loss.
Does Ivermectol cause blood clots?
Ivermectol has a minimal effect on coagulation and concern about mass treatment for this reason appears to be unjustified.
Does Ivermectol help anxiety?
Ivermectol did not induce anxiety-like behavior neither affected corticosterone levels of juvenile rats.
Can Ivermectol help asthma?
This is the first study to demonstrate that Ivermectol is an effective suppressor of inflammation and may be efficacious in the treatment of non-infectious airway inflammatory diseases such as allergic asthma.
