Moxidectin
FDA Drug Information • Also known as: Moxidectin
- Brand Names
- Moxidectin
- Route
- ORAL
- Dosage Form
- TABLET
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
11 DESCRIPTION Moxidectin Tablets contain moxidectin, an anthelmintic drug and a macrocyclic lactone of the milbemycin class derived from the actinomycete Streptomyces cyanogriseus. The chemical name of moxidectin is (2aE,4E,5'R,6R,6'S,8E,11R,13S,15S,17aR,20R,20aR,20bS)-6'-[(E)-1,3-dimethyl-1-butenyl]-5',6,6',7,10,11,14,15,17a,20,20a,20b-dodecahydro-20,20b-dihydroxy-5',6,8,19-tetramethylspiro[11,15-methano-2H,13H,17H-furo[4,3,2-pq][2,6]benzodioxacyclooctadecin-13,2'-[2H]pyran]-4',17(3'H)-dione 4'-(E)-(O-methyloxime). The structural formula is: Figure 1 : Moxidectin Structure Moxidectin is a white or pale-yellow, amorphous powder. The empirical formula is C 37 H 53 NO 8 and the molecular weight is 639.82 Dalton. Moxidectin is readily soluble in organic solvents such as methylene chloride, diethyl ether, ethanol, acetonitrile, and ethyl acetate. It is only slightly soluble in water (0.51 mg/L) and the melting point range for moxidectin powder is 145°C to 154°C. Moxidectin Tablets are for oral administration. Each tablet contains 2 mg of moxidectin. The tablets are uncoated and include the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, lactose anhydrous, magnesium stearate, microcrystalline cellulose and sodium lauryl sulfate. Figure 1: Moxidectin Structure
What Is Moxidectin Used For?
1 INDICATIONS AND USAGE Moxidectin Tablets are indicated for the treatment of onchocerciasis due to Onchocerca volvulus in adult and pediatric patients aged 4 years and older and weighing at least 13 kg [see Clinical Studies ( 14 )] . Limitations of Use: Moxidectin Tablets does not kill adult Onchocerca volvulus (O. volvulus) parasites . Follow-up evaluation is advised. The safety and efficacy of repeat administration of Moxidectin Tablets in patients with O . volvulus has not been studied. Moxidectin is an anthelmintic indicated for the treatment of onchocerciasis due to Onchocerca volvulus in adults and pediatric patients aged 4 years and older and weighing at least 13 kg. ( 1 ) Limitations of Use: Moxidectin Tablets do not kill adult Onchocerca volvulus (O. volvulus) parasites. Follow-up is advised. ( 1 ) The safety and efficacy of repeat administration of Moxidectin Tablets in patients with O . volvulus has not been studied. ( 1 )
Dosage and Administration
2 DOSAGE AND ADMINISTRATION Recommended Dosage in Adult Patients : Take 8 mg (four 2 mg tablets) as a single oral dose, with or without food. ( 2.1 ) Recommended Dosage in Pediatric P atients (4 Years of Age and Older and Weighing at Least 13 kg): See Table below. ( 2.2 ) Body Weight Dose Number of 2 mg Tablets 13 kg to less than 15 kg 4 mg 2 15 kg to less than 30 kg 6 mg 3 Greater than or equal to 30 kg 8 mg 4 2.1 Recommended Dosage in Adult Patients The recommended dosage of Moxidectin Tablets in adult patients is a single dose of 8 mg (four 2 mg tablets) taken orally with or without food [see Clinical Pharmacology ( 12.3 )]. 2. 2 Recommended Dosage in Pediatric Patients (4 Years of Age and Older and Weighing at Least 13 kg) The recommended dosage of Moxidectin Tablets in pediatric patients aged 4 years and older and weighing at least 13 kg is described in Table 1 below. Administer Moxidectin Tablets as a single dose taken orally with or without food [see Clinical Pharmacology ( 12.3 ) ]. Table 1: Recommended Dosage of Moxidectin Tablets in Pediatric Patients 4 Years of Age and Older and Weighing at Least 13 kg Body Weight Dose Number of 2 mg Tablets 13 kg to less than 15 kg 4 mg 2 15 kg to less than 30 kg 6 mg 3 Greater than or equal to 30 kg 8 mg 4
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described in greater detail in other labeling sections: Cutaneous, Ophthalmological and/or Systemic Adverse Reactions [see Warnings and Precautio ns ( 5.1 )] Symptomatic Orthostatic Hypotension [see Warnings and Precautions ( 5.2 )] Encephalopathy in Loa loa Co-infected Patients [see Warnings and Precautions ( 5.3 )] Edema and Worsening of Onchodermatitis [see Warnings and Precautions ( 5.4 )] The most common adverse reactions (incidence > 10%) in adult and pediatric patients (12 to less than 18 years of age) in Trial 1 were eosinophilia, pruritus, musculoskeletal pain, headache, lymphocytopenia, tachycardia, rash, abdominal pain, hypotension, pyrexia, leukocytosis, influenza-like illness, neutropenia, cough, diarrhea/gastroenteritis/enteritis, lymph node pain, dizziness, hyponatremia and peripheral swelling. ( 6.1 ) The most common adverse reactions (incidence > 5%) in pediatric patients (4 to less than 18 years of age) in Trial 3 were abdominal pain and diarrhea. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Medicines Development for Global Health at 1-800-MDGH-456 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under varying controlled conditions, adverse reaction rates observed in one clinical trial cannot be directly compared to rates observed in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Clinical Trials Experience in Adults and Pediatric Patients (12 Years to Less than 18 Years of Age) The safety of Moxidectin Tablets was evaluated in two randomized, double-blind, active-controlled studies in patients with confirmed onchocerciasis (Trial 1 and Trial 2) [see Clinical Studies ( 14 )] . In Trial 1, 978 patients (including 53 pediatric patients aged 12 to less than 18 years) received Moxidectin Tablets as a single oral dose of 8 mg and 494 patients received ivermectin (including 24 pediatric patients aged 12 to less than 18 years) as a single oral dose of approximately 150 mcg/kg. In Trial 2, 127 patients aged 18 years or older received Moxidectin Tablets as a single oral dose ranging from 2 mg (this is not an approved dose) to 8 mg (38 received the recommended 8 mg dose) and 45 patients aged 18 years or older received ivermectin as a single oral dose of approximately 150 mcg/kg. Most Common Adverse Reactions No patients withdrew from either trial due to adverse reactions. Adverse Reactions reported in Trial 1 in > 10% of patients are summarized in Table 2. Most were related to physical, vital signs and laboratory changes associated with Mazzotti reaction [see Warnings and Precautions ( 5.1 )] . Table 2: Adverse Reactions Occurring in > 10% of Moxidectin-treated Patients with Onchocerciasis in Trial 1 Adverse Reaction Moxidectin N = 978 n (%) Ivermectin N = 494 n (%) Eosinophilia 721 (74) 390 (79) Pruritus 640 (65) 268 (54) Musculoskeletal pain a 623 (64) 257 (52) Headache 566 (58) 267 (54) Lymphocytopenia* 470 (48) 215 (44) Tachycardia b 382 (39) 148(30) Orthostatic tachycardia c 333 (34) 130 (26) Non-orthostatic tachycardia d 179 (18) 57 (12) Rash e 358 (37) 103 (21) Abdominal pain f 305 (31) 173 (35) Hypotension g 289 (30) 125 (25) Orthostatic hypotension h 212 (22) 81 (16) Pyrexia/Chills 268 (27) 88 (18) Leukocytosis 240 (25) 125 (25) Influenza like illness 226 (23) 102 (21) Neutropenia** 197 (20) 112 (23) Cough 168 (17) 88 (18) Lymph node pain 129 (13) 28 (6) Dizziness 121 (12) 44 (9) Diarrhea/Gastroenteritis/Enteritis 144 (15) 84 (17) Hyponatremia 112 (12) 65 (13) Peripheral swelling 107 (11) 30 (6) a Includes “myalgia”, “arthralgia”, “musculoskeletal pain”, “pain” and “back pain” b Includes “orthostatic heart rate increased”, “postural orthostatic tachycardia syndrome”, “heart rate increased” and “sinus tachycardia” c Includes “orthostatic heart rate increased” and “postural orthostatic tachycardia syndrome”...
Drug Interactions
7 DRUG INTERACTIONS 7.1 Midazolam (CYP3A4 substrate) In healthy subjects, concomitant administration of a single 8 mg oral dose of Moxidectin Tablets did not have an effect on the pharmacokinetics of midazolam [ see Clinical Pharmacology ( 12.3 ) ]. Moxidectin can be co-administered with CYP3A4 substrates.
Contraindications
4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary Available data from clinical trials on the use of Moxidectin Tablets in pregnant women are insufficient to establish whether there is a moxidectin-associated risk for major birth defects and miscarriage . Moxidectin administered orally to pregnant rats during the period of organogenesis was not associated with significant embryo-fetal developmental effects at doses of approximately 15 times the recommended human dose based on body surface area (BSA) comparison. When moxidectin was dosed orally to pregnant rabbits during the period of organogenesis, no embryo-fetal developmental effects were observed at oral doses of moxidectin up to 24 times the recommended human dose based on BSA comparison ( see Data ) . Daily administration of moxidectin by oral gavage to maternal female rats during organogenesis and through lactation was associated with decreased survival, adverse clinical signs, and decreased body weights in first-generation offspring during the lactation period at a moxidectin dose less than 2-times the recommended human dose based on BSA comparison. Additional findings in first-generation offspring at the same dose included delays in pinna unfolding, eye opening, and vaginal opening. Other parameters, including reproduction and neurological development in first-generation offspring were not affected at any moxidectin dose ( see Data ) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In a rat embryo-fetal development study, daily oral administration of moxidectin at 12 mg/kg/day (approximately 15 times the recommended human dose of 8 mg based on BSA comparison) during Gestation Days (GDs) 6...
Overdosage
10 OVERDOSAGE No specific antidote is available for overdose with Moxidectin Tablets. If overdose occurs, the patient should be monitored for evidence of toxicity. Treatment of overdose with Moxidectin Tablets consists of general supportive measures including monitoring of vital signs as well as observation of the clinical status of the patient. Supportive therapy, if indicated, should include parenteral fluids and electrolytes, respiratory support (oxygen and mechanical ventilation if necessary) and pressor agents if clinically significant hypotension is present.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING Moxidectin Tablets containing 2 mg moxidectin are white to pale yellow uncoated oval-shaped tablets, debossed on one side with “AKKA”. Each high-density polyethylene bottle contains 500 tablets (NDC 71705-050-01), a silica gel desiccant and rayon coil. Store below 30°C (86°F). Protect from light. Once open, the full contents of the container should be used within 24 hours and discard any unused content.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.