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Moxidectin (United States: Not available): Drug information

Moxidectin (United States: Not available): Drug information
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Pharmacologic Category
  • Anthelmintic
Dosing: Adult
Onchocerciasis

Onchocerciasis:

Note: For individuals from Loa loa–endemic areas, rule out co-infection prior to moxidectin administration to avoid life-threatening encephalopathy.

Oral: 8 mg as a single dose.

Dosing: Kidney Impairment: Adult

CrCl ≥30 mL/minute: No dosage adjustment necessary.

CrCl <30 mL/minute or ESRD: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Liver Impairment: Adult

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

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric

(For additional information see "Moxidectin (United States: Not available): Pediatric drug information")

Onchocerciasis

Onchocerciasis: Note: For individuals from Loa loa–endemic areas, rule out coinfection prior to moxidectin administration to avoid potential life-threatening encephalopathy.

Children ≥4 years and Adolescents:

13 to <15 kg: Oral: 4 mg as a single dose.

15 to <30 kg: Oral: 6 mg as a single dose.

≥30 kg: Oral: 8 mg as a single dose.

Dosing: Kidney Impairment: Pediatric

Children ≥4 years and Adolescents: Oral:

CrCl ≥30 mL/minute: No dosage adjustment necessary.

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

Dosing: Liver Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for children, adolescents, and adults, unless otherwise noted.

>10%:

Cardiovascular: Hypotension (30%), orthostatic hypotension (22%), peripheral edema (11%), tachycardia (39%; including non-orthostatic tachycardia [18%]; postural orthostatic tachycardia [34%])

Dermatologic: Pruritus (65%), skin rash (37%)

Endocrine & metabolic: Hyponatremia (12%)

Gastrointestinal: Abdominal pain (31%), diarrhea (≤15%), enteritis (≤15%), gastroenteritis (≤15%)

Hematologic & oncologic: Eosinophilia (74%; severe: 18%), leukocytosis (25%), lymphocytopenia (48%; grade 3: 23%), neutropenia (20%; grade 4: 7%)

Immunologic: Lymph node pain (13%)

Nervous system: Chills (≤27%), dizziness (12%), headache (58%)

Neuromuscular & skeletal: Musculoskeletal pain (64%)

Respiratory: Cough (17%), flu-like symptoms (23%)

Miscellaneous: Fever (≤27%)

1% to 10%:

Hematologic & oncologic: Eosinopenia (5%)

Hepatic: Hyperbilirubinemia (3%), increased gamma-glutamyl transferase (>5 × ULN: 3%), increased serum alanine aminotransferase (>5 × ULN: 1%), increased serum aspartate aminotransferase (>5 × ULN: 1%)

Ophthalmic: Allergic conjunctivitis (2%), conjunctival hyperemia (≤2%), eye discomfort (2%; including abnormal sensation in eyes, foreign body sensation of eye), eye pain (8%), eye pruritus (7%), eyelid edema (2%), increased lacrimation (1%), ocular hyperemia (≤2%), visual impairment (3%; including blurred vision, decreased visual acuity)

Postmarketing: Miscellaneous: Mazzotti reaction (associated with onchocerciasis; including cutaneous, ophthalmological, systemic) (Kanza 2024; Opoku 2018)

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Warnings/Precautions

Concerns related to adverse effects:

• Mazzoti reaction: Moxidectin treatment may cause cutaneous, ophthalmological, and/or systemic reactions (Mazzoti reaction) of varying severity, due to allergic and inflammatory host responses to the death of microfilariae. These reactions generally occur and resolve in the first week post-treatment. Risk may be increased in patients with higher microfilarial burden. Treatment of severe Mazzoti reactions is not definitive, but includes supportive care (eg, hydration and/or parenteral corticosteroids) to treat postural hypotension. Antihistamines and/or aspirin have been used for most mild to moderate reactions.

• Orthostatic hypotension: Orthostatic hypotension may occur, most commonly on the first 1 to 2 days after treatment. Decrease in blood pressure was transient and managed by resuming recumbency.

Disease-related concerns:

• Loiasis: Pretreatment assessment for loiasis is recommended in any patient with exposure to Loa loa-endemic areas; serious, sometimes fatal, encephalopathy may occur following treatment with moxidectin in onchocerciasis patients with concomitant loiasis.

Other warnings/precautions:

• Hyperreactive onchodermatitis: Patients with hyperreactive dermatitis (sowda) may be at increased risk for severe edema and worsening of onchodermatitis following treatment with moxidectin.

Product Availability

There are no plans for commercial distribution of moxidectin in the US. Product will be available for onchocerciasis endemic parts of the world.

Dosage Forms: US

Tablet, oral

Generic: 2 mg [500s] [contains lactose, sodium lauryl sulfate]

Administration: Adult

Oral: Administer without regard to meals.

Administration: Pediatric

Oral: May be taken without regard to food.

Use: Labeled Indications

Onchocerciasis: Treatment of onchocerciasis due to Onchocerca volvulus in adult and pediatric patients ≥4 years of age and weighing ≥13 kg.

Limitations of use: Moxidectin does not kill adult O. volvulus parasites; follow-up evaluation is advised. Safety and efficacy of repeat administration of moxidectin in patients with O. volvulus has not been studied.

Metabolism/Transport Effects

None known.

Drug Interactions

There are no known significant interactions.

Reproductive Considerations

Patients who could become pregnant were required to use long-acting contraception during clinical studies (Awadzi 2014; Korth-Bradley 2011), likely due to the long terminal half-life of moxidectin.

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies.

Breastfeeding Considerations

Moxidectin is present in breast milk.

Breast milk concentrations of moxidectin were evaluated in 12 lactating women who were given a single oral dose of moxidectin 8 mg at 21 to 100 weeks postpartum. All decided to wean their infants and discontinue breastfeeding before the study. Maternal milk and serum were collected at specified intervals for 28 and 90 days after the dose, respectively. Concentrations of moxidectin were higher in breast milk than maternal serum, and both were greatest at the beginning of the sampling period and decreased over time. Moxidectin continued to be present in breast milk on day 28. Approximately 0.701 ± 0.299% of the maternal dose was collected in breast milk. The mean relative infant dose (RID) of moxidectin was calculated to be 8.73 ± 3.17% of the maternal dose (based on actual maternal weight and a 5 kg infant) (Korth-Bradley 2011).

Due to adverse events observed in animal studies (including weight loss and death), breastfeeding is not recommended by the manufacturer during therapy and for 7 days after the last dose of moxidectin.

Monitoring Parameters

Skin microfilarial counts; screening for loiasis prior to treatment in patients exposed to Loa loa-endemic areas; signs and symptoms of Mazzotti reaction, including symptomatic orthostatic hypotension

Mechanism of Action

Moxidectin, an anthelminthic agent, is active against the microfilariae of O. volvulus, but not effective in killing the adult worms. Studies with other nematodes suggest moxidectin binds to glutamate-gated chloride ions channels, gamma-aminobutyric acid (GABA) receptors, and/or APT-binding cassette transporters. This leads to increased permeability, influx of chloride ions, hyperpolarization, and muscle paralysis. There is also a reduction in motility of all stages of the parasite, excretion of immunomodulatory proteins, and the fertility of both male and female adult worms.

Pharmacokinetics (Adult Data Unless Noted)

Distribution: Vd: 2,421 ± 1,658 L.

Protein binding: Unknown.

Metabolism: Minimal.

Half-life elimination:

Children ≥4 years and Adolescents:

Weight 13 to <15 kg: ~12.5 days (299 hours).

Weight 15 to <30 kg: ~14.1 days (338.2 hours).

Weight ≥30 kg: ~22.7 days (545.8 hours).

Adults: 23.3 days (559 hours).

Time to peak: Children ≥4 years and Adolescents: Mean range: 3.4 to 3.5 hours; Adults: 4 hours.

Excretion: Feces: 2% (as unchanged drug).

  1. Awadzi K, Opoku NO, Attah SK, Lazdins-Helds J, Kuesel AC. A randomized, single-ascending-dose, ivermectin-controlled, double-blind study of moxidectin in Onchocerca volvulus infection. PLoS Negl Trop Dis. 2014;8(6):e2953. doi: 10.1371/journal.pntd.0002953. [PubMed 24968000]
  2. Kanza EM, Nyathirombo A, Larbelee JP, et al. Onchocerca volvulus microfilariae in the anterior chambers of the eye and ocular adverse events after a single dose of 8 mg moxidectin or 150 µg/kg ivermectin: results of a randomized double-blind Phase 3 trial in the Democratic Republic of the Congo, Ghana and Liberia. Parasit Vectors. 2024;17(1):137. doi:10.1186/s13071-023-06087-3 [PubMed 38491528]
  3. Korth-Bradley JM, Parks V, Chalon S, et al. Excretion of moxidectin into breast milk and pharmacokinetics in healthy lactating women. Antimicrob Agents Chemother. 2011;55(11):5200-5204. doi: 10.1128/AAC.00311-11. [PubMed 21896908]
  4. Moxidectin [prescribing information]. Melbourne, Victoria, Australia: Medicines Development for Global Health; February 2025.
  5. Opoku NO, Bakajika DK, Kanza EM, et al. Single dose moxidectin versus ivermectin for Onchocerca volvulus infection in Ghana, Liberia, and the Democratic Republic of the Congo: a randomised, controlled, double-blind phase 3 trial. Lancet. 2018;392(10154):1207-1216. doi:10.1016/S0140-6736(17)32844-1 [PubMed 29361335]
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