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Prévia do material em texto

Official reprint from UpToDate
www.uptodate.com © 2024 UpToDate, Inc. and/or its affiliates. All Rights Reserved.
Brand Names: US
Stromectol
Pharmacologic Category
Anthelmintic
Dosing: Adult
®
Ivermectin (systemic): Drug information
2024© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
Contributor Disclosures
For additional information see "Ivermectin (systemic): Patient drug information" and "Ivermectin
(systemic): Pediatric drug information"
For abbreviations, symbols, and age group definitions show table
Ascariasis (alternative agent) (off-label use):
Note: For patients with complications (eg, intestinal obstruction, acute
cholangitis), initiate therapy after resolution of acute symptoms (Ref).
Oral: 150 to 200 mcg/kg as a single dose (Ref).
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Ascariasis 
Demodex folliculitis (off-label use): Oral: 200 mcg/kg once weekly for 2 doses (Ref).
Demodex folliculitis 
Gnathostomiasis, cutaneous (off-label use):
Note: Not recommended for CNS disease due to inflammatory response from
dying larvae (Ref).
Gnathostomiasis, cutaneous 
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Oral: 200 mcg/kg once daily for 2 days (Ref).
Hookworm-related cutaneous larva migrans (off-label use): Oral: 200 mcg/kg once
daily for 1 or 2 days (Ref).
Hookworm-related cutaneous larva migrans 
Lice, refractory (off-label use):
Note: Reserve for patients with an insufficient response to topical therapy (Ref).
Optimal dose, dosing interval, and frequency are uncertain (Ref).
Pediculus capitis: Oral: 200 mcg/kg once weekly for 2 doses (Ref); some experts
suggest 400 mcg/kg once weekly for 2 doses (Ref).
Pediculosis pubis: Oral: 200 mcg/kg once weekly for 2 doses (Ref); some experts
suggest 250 mcg/kg once, with a repeat dose in 7 to 14 days (Ref).
Lice, refractory 
Mansonella infection (off-label use):
Note: For individuals from Loa loa–endemic areas, rule out co-infection prior to
ivermectin administration to avoid life-threatening encephalopathy (Ref).
Mansonella ozzardi: Oral: 150 mcg/kg as a single dose (Ref).
Mansonella streptocerca infection (alternative agent): Oral: 150 mcg/kg as a single
dose (Ref).
Mansonella infection 
Onchocerciasis:
Note: For individuals from Loa loa–endemic areas, rule out co-infection prior to
ivermectin administration to avoid life-threatening encephalopathy (Ref).
Oral: 150 mcg/kg once; repeat dose every 3 to 6 months until asymptomatic (Ref).
For patients outside endemic areas or in areas with low transmission,
doxycycline therapy is initiated 1 week after the initial ivermectin dose (Ref).
Onchocerciasis 
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Scabies (off-label use):
Note: For cohabitants or other individuals who have had prolonged skin-to-skin
contact within the previous 6 weeks, simultaneous treatment is recommended
(Ref).
Classic scabies, treatment: Oral: 200 mcg/kg once; repeat dose in 7 to 14 days (Ref).
Crusted scabies, treatment: Oral: 200 mcg/kg once daily in combination with
permethrin for 3, 5, or 7 nonconsecutive days depending on infection severity
(eg, for 3 days: give on days 1, 2, and 8; for 5 days: give on days 1, 2, 8, 9, and
15; for 7 days: give on days 1, 2, 8, 9, 15, 22, and 29) (Ref).
Scabies 
Strongyloidiasis:
Note: For individuals from Loa loa–endemic areas, rule out co-infection prior to
ivermectin administration to avoid life-threatening encephalopathy (Ref).
Uncomplicated infection:
Patients who are immunocompetent: Oral: 200 mcg/kg once daily for 1 or 2
days (Ref).
Patients who are immunocompromised: Oral: 200 mcg/kg once daily for 2
days; repeat dosing regimen in 2 weeks (Ref).
Severe, disseminated infection: Oral: 200 mcg/kg once daily until symptoms have
resolved and stool and/or sputum examination is negative for ≥2 weeks (Ref).
Some experts suggest switching to an alternative approach for patients who
are immunocompromised or critically ill with persistently positive (eg, ≥3 days)
stool examination (Ref). For patients with persistent immunosuppression after
clinical improvement, some experts use suppressive ivermectin 200 mcg/kg
once monthly for ≥6 months (Ref).
Strongyloidiasis 
Trichuriasis (whipworm) (alternative agent) (off-label use): Oral: 600 mcg/kg once
daily for 3 days in combination with albendazole (Ref).
Trichuriasis 
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Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring
dose/frequency adjustment or avoidance. Consult drug interactions database for more
information.
Dosing: Kidney Impairment: Adult
The renal dosing recommendations are based upon the best available evidence and clinical
expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts,
PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
Altered kidney function: No dosage adjustment necessary for any degree of kidney
dysfunction (<1% excreted in the urine) (Ref).
Hemodialysis, intermittent (thrice weekly): Unlikely to be significantly dialyzed (highly
protein bound; large V ): No supplemental dose or dosage adjustment necessary (Ref).
Peritoneal dialysis: Unlikely to be significantly dialyzed (highly protein bound; large V ): No
dosage adjustment necessary (Ref).
CRRT: No dosage adjustment necessary (Ref).
PIRRT (eg, sustained, low-efficiency diafiltration): No dosage adjustment necessary (Ref).
Dosing: Hepatic Impairment: Adult
There are no dosage adjustments provided in manufacturer’s labeling.
Dosing: Older Adult
Refer to adult dosing.
Dosing: Pediatric
(For additional information see "Ivermectin (systemic): Pediatric drug information")
Dosage guidance:
Safety: For individuals from Loa loa-endemic areas, rule out coinfection prior to
ivermectin administration to avoid life-threatening encephalopathy (Ref).
Dosing: Description of ivermectin use in infants and children weighing <15 kg is limited
due to theoretical risk for CNS adverse events, however it has been used in this
population for a variety of indications with no reports of serious adverse events (Ref).
Following the indication-specific dosing information are weight-band dosing tables to
assist with calculation and rounding of doses.
d
d
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Ascariasis; roundworm 
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https://www.uptodate.com/contents/ivermectin-systemic-pediatric-drug-information?search=ivermectin&topicRef=83315&source=see_link
Ascariasis (Ascaris lumbricoides); roundworm (alternative agent): Limited data
available: Children ≥15 kg and Adolescents: Oral: 150 to 200 mcg/kg/dose as a
single dose (Ref).
Gnathostomiasis, cutaneous: Limited data available:Children ≥15 kg and
Adolescents: Oral: 200 mcg/kg/dose once daily for 2 days (Ref).
Gnathostomiasis, cutaneous 
Hookworm-related cutaneous larva migrans: Limited data available: Children ≥15 kg
and Adolescents: Oral: 200 mcg/kg as a single dose (Ref).
Hookworm-related cutaneous larva migrans 
Lice (alternative agent): Limited data available: Note: Ivermectin is not ovicidal;
therefore, repeat doses are necessary to eradicate infestation:
Head lice: Children ≥15 kg and Adolescents: Oral: 200 to 400 mcg/kg/dose for 2
doses administered 9 to 10 days apart. Dosing at the higher end of the range
(ie, 400 mcg/kg/dose) may result in fewer treatment failures (Ref).
Pubic lice: Children ≥15 kg and Adolescents: Oral: 250 mcg/kg/dose for 2 doses
administered 7 to 14 days apart (Ref).
Lice 
Mansonella infection:
Mansonella ozzardi: Limited data available: Children ≥15 kg and Adolescents: Oral:
150 mcg/kg as a single dose (Ref).
Mansonella streptocerca : Limited data available: Children ≥15 kg and Adolescents:
Oral: 150 mcg/kg as a single dose (Ref).
Mansonella infection 
Onchocerciasis (Onchocerca volvulus); river blindness:
Onchocerciasis; river blindness 
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Weight-band dosing: Weight-band dosing tables are provided to assist with calculation and
rounding of doses; refer to indication-specific dosing for details.
Weight-Band Dosing to Provide
~150 mcg/kg
Patient Weight Single Oral Dose
15 to 25 kg 3 mg
26 to 44 kg 6 mg
45 to 64 kg 9 mg
65 to 84 kg 12 mg
Weight-Band Dosing to Provide
~200 mcg/kg
Patient Weight Single Oral Dose
Children ≥15 kg and Adolescents: Oral: 150 mcg/kg/dose every 3 to 6 months until
asymptomatic (Ref). Ivermectin is only effective against microfilariae; if
treatment of macrofilariae is desired, doxycycline may be initiated 1 week after
ivermectin treatment (Ref).
Scabies: Limited data available: Children ≥15 kg and Adolescents: Oral: 200
mcg/kg/dose for 2 doses administered at 7 to 14 days apart (Ref).
Scabies 
Strongyloidiasis:
Children ≥15 kg and Adolescents: Oral: 200 mcg/kg/dose once daily for 1 to 2 days.
Patients with hyperinfection and disseminated disease may need prolonged or
repeated treatment (eg, daily treatment until stool and/or sputum exams are
negative for 2 weeks) (Ref).
Strongyloidiasis 
Trichuriasis ( Trichuris trichiura); whipworm: Limited data available: Children ≥15 kg
and Adolescents: Oral: 200 mcg/kg/dose once daily for 3 days (Ref).
Trichuriasis; whipworm 
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Patient Weight Single Oral Dose
15 to 24 kg 3 mg
25 to 35 kg 6 mg
36 to 50 kg 9 mg
51 to 65 kg 12 mg
66 to 79 kg 15 mg
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring
dose/frequency adjustment or avoidance. Consult drug interactions database for more
information.
Dosing: Kidney Impairment: Pediatric
There are no dosage adjustments provided in the manufacturer's labeling.
Dosing: Hepatic Impairment: Pediatric
There are no dosage adjustments provided in the manufacturer's labeling.
Adverse Reactions (Significant): Considerations
CNS effects including neurotoxicity (eg, ataxia, confusion, disorientation,
encephalopathy, impaired consciousness [including coma], stupor, tremor) and
central nervous system depression with subsequent breathing difficulties, have
rarely been reported in humans, but are well known to occur in animals (Ref).
Theoretical risk for CNS effects in infants and young children due to immature
blood-brain barrier has been extrapolated from animal data and has minimized
use in patients <15 kg. Existing data in younger pediatric patients are limited, with
recent evaluations describing ivermectin use in patients <15 kg for a variety of
indications with no reports of serious adverse events (Ref).
Mechanism: CNS effects occur when ivermectin crosses the blood-brain barrier into
the spinal cord, midbrain or cerebrum and blocks important neuronal
transmission that involves glutamate or gamma-amino butyric acid (Ref). In
infants and young children, it has been proposed that ivermectin may cross
the immature blood-brain barrier, resulting in CNS toxicity (Ref). In patients
with a well-developed blood-brain barrier, the neurological adverse effects of
ivermectin are thought to occur when the ATP-binding cassette subfamily B
member 1 (ABCB1) transporter (also known as P-glycoprotein) is altered and
fails to prevent the uptake of ivermectin into the brain (Ref).
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CNS effects 
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Onset: Rapid; typically occurs within hours of dosing, although has also been
described as late as 7 days after administration (Ref).
Risk factors:
• Immature blood-brain barrier (Ref)
• Body weight <15 kg as a surrogate marker for an immature blood-brain
barrier (Ref)
• Mutation in ABCB1 (P-glycoprotein) transporter (Ref)
A variety of delayed hypersensitivity reactions, ranging from skin rash to severe
cutaneous adverse reactions (SCAR), including Stevens-Johnson syndrome/toxic
epidermal necrolysis and drug reaction with eosinophilia and systemic
symptoms have been reported with ivermectin use (Ref).
Mechanism: Non–dose-related; immunologic. Delayed hypersensitivity reactions,
including rashes (often maculopapular) and SCARs are T-cell-mediated (Ref).
Onset: Delayed hypersensitivity reactions: Varied. SCARs usually occur within 1 to 8
weeks after initiation (Ref), although cases associated with ivermectin have
been reported within 3 days after receiving a single dose (Ref).
Hypersensitivity reactions (delayed) 
Ivermectin may cause an immunologic post-treatment reaction, also known as a
Mazzoti reaction, which is associated with pruritus, skin rash, fever, fatigue,
lymphadenopathy, arthralgia, tachycardia, hypotension (including orthostatic
hypotension), edema, and abdominal pain (Ref). Most cases have been reported
in association with the treatment of onchocerciasis, but cases have also been
reported in association with the treatment of other infections (eg, scabies) (Ref).
Symptoms are mostly mild and usually resolve in 4 days; however, cases of coma
and death have been reported, although these deaths are often attributed to Loa
loa-associated encephalopathy (Ref). Serious Mazzoti reactions are estimated to
occur in 19% to 81% of patients exposed to ivermectin for the treatment of filarial
parasites, which is disproportionality more than other antinematodal drugs (Ref).
Mechanism: Non–dose-related; immunologic. Ivermectin exerts a strong
microfilaricidal effect on filariae, leading to a destruction of microfilariae. In
patients with high densities of microfilariae in the skin or blood, this may
Immunologic post-treatment reaction (Mazzoti reaction) 
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Adverse Reactions
The following adverse drug reactions and incidences are derived from product labeling unless
otherwise specified.
≥10%: Miscellaneous: Mazzotti reaction (associated with onchocerciasis: pruritus: 28%; fever:
23%; skin edema, papular rash, pustular rash, and urticaria: ≤23%; arthralgia and
synovitis: ≤9%; lymphadenitis [axillary node: 4% to 11%, cervical node: 1% to 5%, inguinal
node: 13% to 14%, other lymph node: 2% to 3%])
1% to 10%:
Cardiovascular: Orthostatic hypotension (1%), peripheral edema (3%), tachycardia (4%)
Dermatologic: Pruritus (associatedwith strongyloidiasis: 3%)
Gastrointestinal: Diarrhea (2%), nausea (2%)
Hematologic & oncologic: Decreased white blood cell count (3%), eosinophilia (3%),
increased hemoglobin (1%)
Hepatic: Increased serum alanine aminotransferase (2%), increased serum aspartate
aminotransferase (2%)
Hypersensitivity: Facial edema (1%)
Nervous system: Dizziness (3%)
Ophthalmic: Inflammation of limbus of eyes (4% to 6%), punctate cataract (1% to 2%)
<1%:
Dermatologic: Skin rash, urticaria (associated with strongyloidiasis)
Gastrointestinal: Abdominal pain, anorexia, constipation, vomiting
induce complex inflammatory reactions resulting in local tissue damage and
degradation of host structures (Ref).
Onset: Varied; within 1 to 7 days of therapy initiation (Ref).
Risk factors:
• High densities of microfilariae (ie, the larval stages of the filarial parasites)
(Ref)
• Treatment of filarial parasites (Ref)
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Hematologic & oncologic: Anemia, leukopenia
Nervous system: Asthenia, drowsiness, fatigue, headache, tremor, vertigo
Neuromuscular & skeletal: Myalgia
Ophthalmic: Vision loss
Frequency not defined:
Cardiovascular: Chest discomfort
Gastrointestinal: Abdominal distention
Postmarketing:
Cardiovascular: Hypotension
Dermatologic: Stevens-Johnson syndrome (Oshikoya 2020), toxic epidermal necrolysis
(Oshikoya 2020)
Hepatic: Hepatitis (Veit 2006), increased liver enzymes, increased serum bilirubin
Hypersensitivity: Drug reaction with eosinophilia and systemic symptoms (Kerneuzet
2018)
Nervous system: Central nervous system depression (Chandler 2018), neurotoxicity
(including ataxia, confusion, disorientation, encephalopathy, impaired consciousness
[including coma], stupor) (Baudou 2020; Chandler 2018), seizure (Chandler 2018)
Ophthalmic: Abnormal sensation in eyes, anterior uveitis, chorioretinitis (including
choroiditis), conjunctival hemorrhage, conjunctivitis, diplopia (Campillo 2021), eyelid
edema, keratitis
Respiratory: Exacerbation of asthma
Contraindications
Hypersensitivity to ivermectin or any component of the formulation
Warnings/Precautions
Special populations:
• Immunocompromised patients: Repeated treatment may be required in
immunocompromised patients (eg, HIV); control of extraintestinal strongyloidiasis
may necessitate suppressive (once monthly) therapy.
Other warnings/precautions:
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• Appropriate use: Onchocerca volvulus: Ivermectin has no activity against adult O. volvulus
parasites. L. loa: Ivermectin is not active against adult worms.
Dosage Forms: US
Excipient information presented when available (limited, particularly for generics); consult
specific product labeling.
Tablet, Oral:
Stromectol: 3 mg
Generic: 3 mg
Generic Equivalent Available: US
Yes
Pricing: US
Tablets (Ivermectin Oral)
3 mg (per each): $4.97
Tablets (Stromectol Oral)
3 mg (per each): $5.58
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided
as reference price only. A range is provided when more than one manufacturer's AWP price is
available and uses the low and high price reported by the manufacturers to determine the
range. The pricing data should be used for benchmarking purposes only, and as such should
not be used alone to set or adjudicate any prices for reimbursement or purchasing functions
or considered to be an exact price for a single product and/or manufacturer. Medi-Span
expressly disclaims all warranties of any kind or nature, whether express or implied, and
assumes no liability with respect to accuracy of price or price range data published in its
solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or
consequential damages arising from use of price or price range data. Pricing data is updated
monthly.
Administration: Adult
Oral: Administer on an empty stomach with water (manufacturer’s labeling). Some experts
recommend administering with food to increase absorption (Ref).
Administration: Pediatric
Oral: The manufacturer recommends administration on an empty stomach with water.
However, some experts recommend administering with food to increase absorption;
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(For additional information: Launch drug interactions program)
administration with a high-fat meal as compared to fasted increased bioavailability ~2.5 times
in healthy volunteers (Ref).
Use: Labeled Indications
Onchocerciasis: Treatment of onchocerciasis due to the immature form of Onchocerca
volvulus.
Limitations of use: Ivermectin has no activity against adult Onchocerca volvulus parasites.
The adult parasites reside in subcutaneous nodules, which are infrequently palpable.
Surgical excision may be considered since removal of these nodules will eliminate the
microfilariae-producing adult parasites.
Strongyloidiasis: Treatment of intestinal (eg, nondisseminated) strongyloidiasis due to
Strongyloides stercoralis.
Use: Off-Label: Adult
Ascariasis; Demodex folliculitis; Gnathostomiasis, cutaneous; Hookworm-related cutaneous
larva migrans; Lice, refractory; Mansonella infection; Scabies; Trichuriasis
Medication Safety Issues
Metabolism/Transport Effects
Substrate of CYP3A4 (minor), P-glycoprotein/ABCB1 (minor); Note: Assignment of
Major/Minor substrate status based on clinically relevant drug interaction potential
Drug Interactions
Note: Interacting drugs may not be individually listed below if they are part of a group
interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a
complete list of drug interactions by individual drug name and detailed management
recommendations, use the drug interactions program by clicking on the “Launch drug
interactions program” link above.
KIDs List: Ivermectin (systemic), when used in infants <1 year of age, is identified
on the Key Potentially Inappropriate Drugs in Pediatrics (KIDs) list and should
be avoided due to risk of encephalopathy (weak recommendation; low quality
of evidence) (PPA [Meyers 2020]).
Pediatric patients: High-risk medication: 
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Bacillus clausii: Antibiotics may diminish the therapeutic effect of Bacillus clausii.
Management: Bacillus clausii should be taken in between antibiotic doses during
concomitant therapy. Risk D: Consider therapy modification
BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Risk X:
Avoid combination
BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine
(Immunization). Risk C: Monitor therapy
Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine.
Management: Avoid cholera vaccine in patients receiving systemic antibiotics, and within
14 days following the use of oral or parenteral antibiotics. Risk X: Avoid combination
Fecal Microbiota (Live) (Oral): May diminish the therapeutic effect of Antibiotics. Risk X: Avoid
combination
Fecal Microbiota (Live) (Rectal): Antibiotics may diminish the therapeutic effect of Fecal
Microbiota (Live) (Rectal). Risk X: Avoid combination
Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies): Antibiotics may
diminish the therapeutic effect of Immune Checkpoint Inhibitors (Anti-PD-1,-PD-L1, and -
CTLA4 Therapies). Risk C: Monitor therapy
Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and
Estriol. Risk C: Monitor therapy
Mycophenolate: Antibiotics may decrease serum concentrations of the active metabolite(s) of
Mycophenolate. Specifically, concentrations of mycophenolic acid (MPA) may be reduced.
Risk C: Monitor therapy
Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate.
Management: Consider using an alternative product for bowel cleansing prior to a
colonoscopy in patients who have recently used or are concurrently using an antibiotic.
Risk D: Consider therapy modification
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the
live attenuated Ty21a strain is affected. Management: Avoid use of live attenuated
typhoid vaccine (Ty21a) in patients being treated with systemic antibacterial agents.
Postpone vaccination until 3 days after cessation of antibiotics and avoid starting
antibiotics within 3 days of last vaccine dose. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Ivermectin (Systemic) may enhance the anticoagulant
effect of Vitamin K Antagonists. Risk C: Monitor therapy
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Food Interactions
Bioavailability appears to be increased with food, but the extent of the interaction is
uncertain. When administered following a high-fat meal, bioavailability has been shown to
increase 1.18- to 2.57-fold with a wide range of doses studied (6 to 30 mg) (Duthaler 2020;
Guzzo 2002; Miyajima 2016). Management: The manufacturer recommends to administer on
an empty stomach, although some experts recommend administering with food to increase
absorption (CDC [Workowski 2021]; Currie 2010).
Reproductive Considerations
Evaluate pregnancy status prior to use in patients who may become pregnant; patients
arriving as refugees from specific countries should not be given ivermectin for the
presumptive treatment of intestinal parasites without a reliable history of their last menstrual
period (CDC 2019a).
Pregnancy Considerations
Outcome information following maternal use of ivermectin during pregnancy is primarily
limited to inadvertent exposure during mass treatment programs (Chippaux 1993; Gyapong
2003; Ndyomugyenyi 2008; Nicolas 2020; Pacqué 1990; Westlake 2020).
The decision to use ivermectin during pregnancy should consider the specific indication (eg,
onchocerciasis or Strongyloides infection) and the risk of disease progression in the absence of
treatment (CDC 2021; CDC 2022) Although use in pregnancy is likely low risk, other agents are
currently recommended for the treatment of pediculosis pubis or scabies in pregnant
patients (CDC [Workowski 2021]).
Breastfeeding Considerations
Ivermectin is present in breast milk.
Peak ivermectin breast milk concentrations generally occurred between 4 hours (n=2) and 6
hours (n=2) after a single maternal dose; although the peak breast milk concentration
occurred at 12 hours in one patient (Ogbuokiri 1994; Rodari 2020).
The decision to use ivermectin in a patient who is breastfeeding should consider the specific
indication (eg, onchocerciasis or Strongyloides infection) and the risk of disease
progression in the absence of treatment (CDC 2021; CDC 2022). Although use is likely low
risk, other agents are currently recommended for the treatment of pediculosis pubis or
scabies in patients who are breastfeeding (CDC [Workowski 2021]). Breastfeeding
patients arriving as refugees from specific countries should not be given ivermectin for
the presumptive treatment of intestinal parasites during their first week postpartum
(CDC 2019a).
5/30/24, 7:58 PM Ivermectin (systemic): Drug information - UpToDate
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Monitoring Parameters
Skin and eye microfilarial counts, periodic ophthalmologic exams; follow up stool
examinations; signs and symptoms of neurotoxicity.
Mechanism of Action
Ivermectin is a semisynthetic anthelminthic agent; it binds selectively and with strong affinity
to glutamate-gated chloride ion channels which occur in invertebrate nerve and muscle cells.
This leads to increased permeability of cell membranes to chloride ions then
hyperpolarization of the nerve or muscle cell, and death of the parasite.
Pharmacokinetics (Adult Data Unless Noted)
Absorption: Well absorbed in the fasting state (Baraka 1996; Edwards 1988; Okonkwo 1993);
may be increased with a high-fat meal (Duthaler 2020; Guzzo 2002; Miyajima 2013).
Distribution: V :
Children 2 to 5 years: Median range: 7.46 to 8.26 L/kg (Schulz 2019).
Children 6 to 12 years: Median range: 8.58 to 10.4 L/kg (Schulz 2019).
Adults: 3.1 to 3.5 L/kg in healthy volunteers; mean 9.9 L/kg (range: 6.9 to 15.3 L/kg) in
patients with onchocerciasis; high concentration in the liver and adipose tissue; does
not readily cross the blood-brain barrier (Gonzalez Canga 2008; Okonkwo 1993).
Protein binding: ~93% primarily to albumin (Gonzalez Canga 2008).
Metabolism: Hepatic via CYP3A4 (major), CYP2D6 (minor), and CYP2E1 (minor).
Half-life elimination:
Children 2 to 5 years: Median range: 16.3 to 17.3 hours (Schulz 2019).
Children 6 to 12 years: Median range: 18.1 to 19.1 hours (Schulz 2019).
Adults: 18 hours.
Time to peak, serum: ~4 hours.
Excretion: Feces; urine (<1%).
Brand Names: International
d
For country code abbreviations ( show table)
(AE) United Arab Emirates: Imectin; (AR) Argentina: Iver p | Ivercass | Ivermectina Monserrat eclair
International Brand Names by Country 
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