Moxidectin - Uses, Dose, MOA, Brands, Side effects

Adult patients with onchocerciasis caused by an infection with Onchocerca volvulus who are 12 years of age or older receive treatment with the anti-helminthic medication moxectin.

Moxidectin Uses:

  • Onchocerciasis:

    • It is approved for the treatment of onchocerciasis caused by an infection with Onchocerca volvulus in individuals aged 12 and older.
    • Limitations of use: It is important to note that the drug does not kill adult O. volvulus. Patients should be followed and evaluated subsequently. The safety and efficacy of repeated administration of the drug have not been studied.

Moxidectin dose in adults:

Moxidectin Dose in the treatment of Onchocerciasis:

  • 8 mg orally as a single dose.

Moxidectin dose in children:

Moxidectin Dose in the treatment of Onchocerciasis:

  • Children ≥12 years and Adolescents:

    • 8 mg orally as a single dose.

Pregnancy Risk Category: C

  • Studies on animal reproduction have revealed negative pregnancy results. Clinical trials suggested long-term contraception for females due to the drug's lengthy half-life.

Use during breastfeeding:

  • Breastmilk is the best way to flush out the drug.
  • Manufacturers recommend that you stop breastfeeding. They also advise that you weigh the risks and benefits of drug therapy for the mother as well as the potential exposure of your baby to the drug.

Dose in Kidney disease:

  • CrCl <30 mL/minute or ESRD:

    • There are no dosage adjustments provided in the manufacturer’s labeling (it has not been studied).
  • CrCl ≥30 mL/minute:

    • No dosage change is required.

Dose in Liver disease:

There are no dosage adjustments provided in the manufacturer’s labeling (it has not been studied).


Common Side Effects of Moxidectin:

  • Dermatologic:

    • Pruritus
    • Skin Rash
  • Cardiovascular:

    • Postural Orthostatic Tachycardia
    • Hypotension
    • Peripheral Edema
    • Tachycardia
    • Orthostatic Hypotension
  • Endocrine & Metabolic:

    • Hyponatremia
  • Gastrointestinal:

    • Abdominal Pain
    • Diarrhea
    • Enteritis
    • Gastroenteritis
  • Hematologic & Oncologic:

    • Eosinophilia
    • Lymphocytopenia
    • Leukocytosis
    • Neutropenia
  • Central Nervous System:

    • Headache
    • Chills
    • Lymph Node Pain
    • Dizziness
  •  
  • Neuromuscular & Skeletal:

    • Musculoskeletal Pain
  • Respiratory:

    • Flu-Like Symptoms
    • Cough
  • Miscellaneous:

    • Fever

Less Common Side Effects of Moxidectin:

  • Cardiovascular:

    • Symptomatic orthostatic hypotension
  • Endocrine & metabolic:

    • Increased gamma-glutamyl transferase
  • Hepatic:

    • Hyperbilirubinemia
    • Raised serum alanine aminotransferase
    • Raised serum aspartate aminotransferase
  • Hematologic & oncologic:

    • Eosinopenia
  •  
  • Ophthalmic:

    • Eye pain
    • Eye pruritus
    • Visual impairment
    • Allergic conjunctivitis
    • Eyelid edema
    • Conjunctival hyperemia
    • Ocular hyperemia
    • Increased lacrimation

Frequency of side effects not defined:

  • Dermatologic:

    • Mazzotti reaction

 


Contraindications to Moxidectin:

The manufacturer's labeling does not list any contraindications.

Warnings and precautions

  • Mazzoti reaction:

    • Mazzoti reactions are serious host inflammation responses that can be triggered by the death of microfilariae. It can manifest as cutaneous, systemic, or ophthalmological reactions. Usually, it resolves within a week to two weeks after treatment has begun.
    • Higher microfilariae burden patients are more at risk.
    • Patients may require supportive treatment including intravenous hydration, parenteral corticosteroids, antihistamines, and aspirin.
  • Orthostatic hypotension

    • Postural hypotension is a condition that can occur in the first two days after treatment begins. Hypotension can be treated by lying down or spontaneously.
  • Loiasis:

    • Before initiating treatment, patients who have been exposed should be checked for Loa Loa infection. Concomitant Loa Loa infections can lead to serious encephalopathy, which could be fatal if they are exposed to Moxidectin.

Monitoring parameters:

  • Monitor for the skin microfilariae counts;
  • Keep an eye out for the Mazzotti reaction's warning signs and symptoms, such as symptomatic orthostatic hypotension.
  • In individuals who have been exposed to endemic locations like Loa Loa, test them for loiasis before therapy. 

How to administer Moxidectin?

It may be administered orally without regard to meals.


Mechanism of action of Moxidectin:

  • This medication fights helminths. Gamma-aminobutyric acid (GABA) receptors, glutamate-gated chloride channels, and/or APT-binding cassette transporters are among the receptors it binds to.
  • This increases the permeability of cells, increases the influx of chloride ions, hyperpolarization, and paralyzes the muscles.
  • It reduces motility, excretion of immunomodulatory protein, and the fertility of adult worms male and female. 
  • It is effective against O. volvulus microfilariae, but it does not kill adult worms.

Protein binding:

  • Unknown

Metabolism:

  • Minimal

Half-life elimination:

  • 23.3 days (559 hours)

Time to peak:

  • 4 hours

Excretion:

  • Feces: 2% (as unchanged drug)

Moxidectin International Brand Names:

  • Cydectin
  • Moxidecton
  • Moxidec
  • Equimoxin

Moxidectin  Brand Names in Pakistan:

No Brands Available in Pakistan.

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