Ivermectin Tablets - Uses, Dose, Side effects

Ivermectin is a semisynthetic antihelminthic drug that causes cell death by hyperpolarization and increasing the permeability of cells.

Ivermectin Uses:

  • Onchocerciasis:

    • It is used to treat the immature form of Onchocerca volvulus (onchocerciasis).
    • It is not effective against the adult form of Onchocerca volvulus. The adult parasites reside in the skin and maybe palpated as subcutaneous nodules. These subcutaneous nodules can be excised surgically (as these adults parasites produce microfilariae).
  • Intestinal Strongyloidiasis:

    • Treatment of intestinal strongyloidiasis caused by Strongyloides stercoralis.
  • Off Label Use of Ivermectin in Adults:

    • Ascariasis
    • Demodicosis
    • Gnathostomiasis
    • Hookworm-related cutaneous larva migrans
    • Lice
    • Mansonella ozzardi infection
    • Mansonella streptocerca infection
    • Prevention and control of scabies,
    • Treatment of Scabies
    • Trichuriasis
    • Wucheria bancrofti infection
  • Ivermectin use in the treatment of COVID-19 (Coronavirus) infection:

    • A recent study demonstrated that a single treatment of ivermectin in cell cultures reduced viral load by 5000 times in 48 hours [Ref].

Ivermectin Dose in Adults:

Ivermectin Dose in the treatment of Onchocerciasis:

  • 150 mcg/kg orally as a single dose.
  • Retreatment every 3 to 12 months may be required until the patient is asymptomatic.

Ivermectin Dose in the treatment of Intestinal Strongyloidiasis:

  • 200 mcg/kg/day orally for 1 to 2 days.

Ivermectin Dose in the treatment of Ascariasis due to Ascaris lumbricoides:

  • 200 mcg/kg orally as a single dose.

Ivermectin Dose in the treatment of Demodicosis due to Demodex folliculorum and Demodex brevis:

  • 200 mcg/kg orally as a single dose, followed by topical permethrin or
  • 200 mcg/kg as 2 doses, one week apart.

Ivermectin Dose in the treatment of Gnathostomiasis due to Gnathostoma spinigerum:

  • 200 mcg/kg orally as a single dose.

Ivermectin Dose in the treatment of Hookworm-related cutaneous larva migrans:

  • 200 mcg/kg orally as a single dose
  • Additional doses may be required by patients with hookworm folliculitis.

Ivermectin Dose in the treatment of Lice:

  • Pediculus humanus capitis:

    • 400 mcg/kg/dose orally every 7 days for 2 doses.
  • Pediculus humanus corporis:

    • 200 mcg/kg/dose orally every seven days for 3 doses.
  • Pediculosis pubis (due to Phthirus pubis and pubic lice):

    • 250 mcg/kg/dose orally every 7 days for 2 doses or
    • 250 mcg/kg/dose every 14 days for 2 doses.

Ivermectin Dose in the treatment of Mansonella ozzardi infection:

  • 6 mg orally as a single dose.

Ivermectin Dose in the treatment of Mansonella streptocerca infection:

  • 150 mcg/kg orally as a single dose.

Dose in the treatment of Scabies due to Sarcoptes scabiei:

  • Classic scabies that is treatment-resistant or the patient is unable to tolerate topical medications:

    • 200 mcg/kg orally as a single dose
    • The dose may be repeated dose in 7 to 14 days (CDC 2017; CDC [Workowski 2015])
  • Treatment of Crusted scabies (Norwegian Scabies):

    • 200 mcg/kg orally as a single dose on days 1, 2, 8, 9, and 15 in combination with topical permethrin 5% cream.
    • Severe cases may require additional ivermectin treatment on days 22 and 29.
  • Prevention and control of scabies:

    • 200 mcg/kg orally as a single dose.

Dose in the treatment of Trichuriasis due to Trichuris trichiura:

  • 200 mcg/kg/day orally for 3 days.

Dose in the treatment of Wucheria bancrofti infection:

  • 200 to 400 mcg/kg orally as a single dose in combination with albendazole.

Ivermectin Dose in Childrens:

Ivermectin Dose in the treatment of Ascariasis due to Ascaris lumbricoides (roundworm):

  • Children ≥15 kg and Adolescents:

    • 150 to 200 mcg/kg/dose orally as a single dose.

Ivermectin Dose in the treatment of Cutaneous larva migrans (dog and cat hookworm):

  • Children ≥15 kg and Adolescents:

    • 200 mcg/kg orally once a day for 1 to 2 days.

Filariasis:

  • Mansonella ozzardi (Children ≥15 kg and Adolescents):

    • 200 mcg/kg/dose orally as a single dose.
  • Mansonella streptocerca (Children ≥15 kg and Adolescents):

    • 150 mcg/kg/dose orally as a single dose.

Ivermectin Dose in the treatment of Wuchereria bancrofti in Children ≥15 kg and Adolescents:

    • 200 mcg/kg/dose orally as a single dose given in combination with albendazole.

Ivermectin Dose in the treatment of Gnathostomiasis due to Gnathostoma spinigerum in Children ≥15 kg and Adolescents:

    • 200 mcg/kg orally once daily for 2 days.

Ivermectin Dose in the treatment of Onchocerciasis (Onchocerca volvulus, river blindness):

  • Children ≥15 kg and Adolescents:

    • 150 mcg/kg/dose orally as a single dose.
    • The dose may be repeated every 6 to 12 months until the patient is asymptomatic.
    • For the prevention of blindness due to ocular onchocerciasis, the doses are repeated every 3 to 12 months.

Ivermectin Dose in the treatment of Pediculosis (lice infestation):

Note: Repeat doses are necessary for eradication as Ivermectin is not ovicidal.

  • Head lice in children 15 kgs or more and adolescents:

    • 400 mcg/kg/dose orally on days 1 and 8 or
    • 200 mcg/kg/dose repeated once after 10 days.
  • Pubic lice in Children 15 Kgs or more and adolescents: 

    • 250 mcg/kg/dose orally for 2 doses administered 14 days apart.

Ivermectin Dose in the treatment of Scabies due to Sarcoptes scabiei:

  • Children ≥15 kg and Adolescents:

    • 200 mcg/kg/dose orally for 2 doses administered at least 7 days apart.
    • The second course may be given 14 days apart.

Ivermectin Dose in the treatment of Strongyloidiasis:

  • Children ≥15 kg and Adolescents:

    • 200 mcg/kg orally once a day for 2 days.
    • A repeat therapy may be required in immunocompromised patients or patients with disseminated disease.

Ivermectin Dose in the treatment of whipworm (Trichuriasis due to Trichuris trichiura): 

  • Children ≥15 kg and Adolescents:

    • 200 mcg/kg orally once a day for 3 days.

Ivermectin weight-based dosing tables:

Weight-Based Dosing to Provide ~150 mcg/kg

Patient Weight (kg)

Single Oral Dose

15 to 25 3 mg
26 to 44 6 mg
45 to 64 9 mg
65 to 84 12 mg
≥85 150 mcg/kg

Weight-Based Dosing to Provide ~200 mcg/kg

Patient Weight (kg)

Single Oral Dose

15 to 24 3 mg
25 to 35 6 mg
36 to 50 9 mg
51 to 65 12 mg
66 to 79 15 mg
≥80 200mcg/kg

Ivermectin Pregnancy Risk Category: C

  • Animal studies have shown adverse outcomes for fetal health.
  • In the treatment of pediculosis pavia or scabies in pregnant ladies, agents other than ivermectin are recommended.

Ivermectin use during breastfeeding:

  • It can be found in low levels in breastmilk.
  • If there is no clear benefit to the infant, the manufacturer recommends against using it during pregnancy.
  • Other agents are preferred for the treatment of pediculosis pénis or scabies in breastfeeding women.

Ivermectin dose in kidney disease:

The manufacturer has not provided any adjustment in the dose in patients with kidney disease.

Ivermectin dose in liver disease:

The manufacturer has not provided any adjustment in the dose in patients with liver disease.


Common Side Effects of Ivermectin:

  • Dermatologic:

    • Pruritus
    • Dermatological Reaction
  • Hematologic & Oncologic:

    • Lymphadenitis
  • Neuromuscular & Skeletal:

    • Arthralgia
    • Synovitis
  • Miscellaneous:

    • Fever

Uncommon Side Effects Of Ivermectin:

  • Cardiovascular:

    • Tachycardia
    • Peripheral Edema
    • Facial Edema
    • Orthostatic Hypotension
  • Central Nervous System:

    • Dizziness
  • Gastrointestinal:

    • Diarrhea
    • Nausea
  • Hematologic & Oncologic:

    • Eosinophilia
    • Decreased White Blood Cell Count
    • Increased Hemoglobin
  • Hepatic:

    • Increased Serum ALT
    • Increased Serum AST

Contraindication to Ivermectin:

Allergy reactions to ivermectin and any component of the formulation

Warnings and precautions

  • Systemic and cutaneous reactions:

    • It has been shown to cause systemic and cutaneous reactions, as well as opthalmological reactions in patients with onchocerciasis.
    • These cutaneous and systemic reactions with variable severity may be associated with the death microfilariae.
    • These reactions may also occur in patients who receive ivermectin treatment for onchocerciasis.
    • Supportive treatments may be used to treat cutaneous or systemic reactions such as hydration, parenteral corticosteroids (for hypertension), and hydration.
    • Patients with mild disease may be treated with antihistamine and/ or aspirin. For severe Mazzoti reactions, there is no treatment.
  • Loiasis:

    • Patients who have been exposed to Loa Loa in the endemic regions (west and central Africa), should undergo a pre-treatment as well as a post-treatment assessment.
    • If concomitant loiasis is present, patients receiving treatment for onchocerciasis can develop severe and sometimes fatal encephalopathy.

Ivermectin (systemic): Drug Interaction

Risk Factor C (Monitor therapy)

Azithromycin (Systemic)

Ivermectin serum concentration might rise (Systemic).

BCG Vaccine (Immunization)

Antibiotics may reduce the BCG vaccine's therapeutic effect (Immunization).

Erdafitinib

P-glycoprotein/ABCB1 Substrates serum levels can rise.

Lactobacillus and Estriol

The therapeutic effects of Lactobacillus and Estriol may be reduced by antibiotics.

Lumacaftor

May lower the level of P-glycoprotein/ABCB1 Substrates in the serum. The serum concentration of P-glycoprotein/ABCB1 Substrates may rise when using lumacaftor.

P-glycoprotein/ABCB1 Inducers

May decrease the serum concentration of Pglycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.).

P-glycoprotein/ABCB1 Inhibitors

May increase the serum concentration of Pglycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of pglycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.).

Ranolazine

P-glycoprotein/ABCB1 Substrates serum levels can rise.

Vitamin K Antagonists (eg, warfarin)

Ivermectin (Systemic) might make Vitamin K Antagonists' anticoagulant effects even more potent.

Risk Factor D (Consider therapy modification)

Sodium Picosulfate

Antibiotics may reduce Sodium Picosulfate's therapeutic impact. Management: If a patient previously used or is currently using an antibiotic, think about utilising an alternative product for bowel cleansing prior to a colonoscopy.

Typhoid Vaccine

The Typhoid Vaccine's therapeutic benefits may be reduced by antibiotics. The only strain impacted is the live attenuated Ty21a strain. Treatment: Patients receiving systemic antibacterial drugs should refrain from receiving the live attenuated typhoid vaccination (Ty21a). It is recommended to wait at least 3 days following the last dose of antibacterial medication before administering this vaccine.

Risk Factor X (Avoid combination)

BCG (Intravesical)

Antibiotics may lessen BCG's therapeutic effects (Intravesical).

Cholera Vaccine

The therapeutic benefit of the cholera vaccine may be reduced by antibiotic use. Management: Cholera vaccine should not be administered to individuals taking systemic antibiotics or within 14 days after taking oral or parenteral antibiotics.

Lasmiditan

P-glycoprotein/ABCB1 Substrates serum levels can rise.

 

Monitor:

  • Skin and eye microfilariae counts
  • periodic ophthalmologic exams
  • follow up stool examinations

How to administer Ivermectin?

  • It is given orally with water and on an empty stomach.

For the treatment of Pediculosis pubis and scabies:

  • It is best advised with food to increase its bioavailability in the epidermis.

Mechanism of action of Ivermectin:

  • It is semisynthetic antihelminthic drug. 
  • It is a strong agonist for glutamate-gated ion channels, which are found mainly in the nerves of invertebrates.
  • The binding of ivermectin into these channels increases the permeability to chlorideions in these cell membranes, leading to hyperpolarization of nerves and muscles that ultimately leads to the death the parasite.

Absorption: Well absorbed when taken orally.

Distribution: The liver and fat cells contain large quantities of it. The blood-brain barrier is not crossed by it.

Protein binding: About 93% of the drug is bound to proteins primarily to albumin.

Metabolism: Hepatic via CYP3A4 (major), CYP2D6 (minor), and CYP2E1 (minor)

Half-life elimination: 18 hours

The time to reach peak serum concentration is about 4 hours.

Excretion: Feces and urine (<1%)


Ivermectin Brand Names (International):

  • Stromectol
  • Ascapil
  • Detebencil
  • Ectin
  • Ivactin
  • Iver P
  • Ivermect
  • Ivermine
  • Ivertal
  • Iverx
  • Iverzine
  • Ivexterm
  • Ivomec
  • Kaonol
  • Kilox
  • Leverctin
  • Maikeding
  • Mectizan
  • Quamox
  • Quanox Gotas
  • Razimectin
  • Revectina
  • Sanifer
  • Scabo
  • Securo
  • Soolantra
  • Stromectol
  • Veratin
  • Vermectil
  • Vermectin
  • Vermokill
  • Yvermil

Ivermectin Brand Names in Pakistan:

Ivermectin 3 mg Tablets

Ivermec Genix Pharma (Pvt) Ltd
Mactovin Valor Pharmaceuticals
Mectin Highnoon Laboratories Ltd.
Odiver Goodman Laboratories

 

Ivermectin 6 mg Tablets

Felvot Wilshire Laboratories (Pvt) Ltd.
Iveratan Biogen Pharma
Iverlex Ambrosia Pharmaceuticals
Ivermite Atco Laboratories Limited
Iverterm Pearl Pharmaceuticals
Mectimite Pharma Health Pakistan (Pvt) Ltd
Mectis Genome Pharmaceuticals (Pvt) Ltd
Odiver Goodman Laboratories
Scabi-Mect Seatle Pharma Pakistan (Pvt) Ltd.
Scabimac Wise Pharmaceuticals (Pvt) Ltd
Stiver Wns Field Pharmaceuticals
Vectin Xenon Pharmaceuticals (Pvt) Ltd.