Equimax

Equimax Uses, Dosage, Side Effects, Food Interaction and all others data.

Ivermectin 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.

Ivermectin 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. Ivermectin 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%).

An anthelmintic used in most schistosome and many cestode infestations.

Praziquantel is an anthelmintic used in most schistosome and many cestode infestations. Praziquantel effects the permeability of the cell membrane resulting in the contraction of schistosomes. The drug further causes vacuolization and disintegration of the schistosome tegument. The effect is more marked on adult worms compared to young worms. An increased calcium influx may play an important role. Secondary effects are inhibition of glucose uptake, lowering of glycogen levels and stimulation of lactate release. The action of praziquantel is limited very specifically to trematodes and cestodes; nematodes (including filariae) are not affected.

Trade Name Equimax
Generic Ivermectin + Praziquantel
Type For animal use only
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Equimax
Equimax

Uses

Ivermectin is used for the treatment of the following infections:

Strongyloidiasis of the intestinal tract. Ivermectin 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: Ivermectin 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: Ivermectin 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.

Praziquantel is an anthelmintic medication used to treat a number of parasitic worm infections such as schistosomiasis.

For the treatment of infections due to all species of schistosoma.

Equimax 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 infectionCestode infections, Cysticercosis, Liver fluke infection, Trematode infections, Schistosoma infection

How Equimax works

Ivermectin 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. Ivermectin 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. Ivermectin may also impair normal intrauterine development of O. volvulus microfilariae and may inhibit their release from the uteri of gravid female worms.

Praziquantel works by causing severe spasms and paralysis of the worms' muscles. This paralysis is accompanied - and probably caused - by a rapid Ca 2+ influx inside the schistosome. Morphological alterations are another early effect of praziquantel. These morphological alterations are accompanied by an increased exposure of schistosome antigens at the parasite surface. The worms are then either completely destroyed in the intestine or passed in the stool. An interesting quirk of praziquantel is that it is relatively ineffective against juvenile schistosomes. While initially effective, effectiveness against schistosomes decreases until it reaches a minimum at 3-4 weeks. Effectiveness then increases again until it is once again fully effective at 6-7 weeks. Glutathione S-transferase (GST), an essential detoxification enzyme in parasitic helminths, is a major vaccine target and a drug target against schistosomiasis. Schistosome calcium ion channels are currently the only known target of praziquantel.

Dosage

Equimax 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.

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.

Rapidly absorbed (80%)

Half Life

16 hours (also reported at 22-28 hours)

0.8-1.5 hours (in serum)

Elimination Route

Ivermectin 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

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