SOOLANTRA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SOOLANTRA (SOOLANTRA).
Ivermectin, a macrocyclic lactone, binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate nerve and muscle cells, leading to increased chloride ion influx, hyperpolarization, and paralysis of parasites. It also has anti-inflammatory properties by inhibiting cytokine production and chemotaxis in human cells.
| Metabolism | Primarily hepatic via CYP3A4; minor contribution from CYP2D6 and other enzymes. Ivermectin is a substrate of P-glycoprotein. |
| Excretion | Primarily fecal (biliary) elimination of unchanged drug and metabolites; renal excretion accounts for <1% of the dose. |
| Half-life | Terminal half-life is approximately 8 days (range 5-10 days) following topical application; prolonged due to slow release from skin reservoir. |
| Protein binding | Approximately 99% bound to plasma proteins. |
| Volume of Distribution | Apparent volume of distribution is not determined for topical route; systemic absorption minimal (approximately 0.5% of applied dose), so Vd is not clinically applicable. |
| Bioavailability | Topical bioavailability is approximately 0.5% of the applied dose; oral bioavailability is not relevant as drug is not administered systemically. |
| Onset of Action | Clinical improvement in inflammatory lesions of rosacea noted within 2-4 weeks of once-daily topical application. |
| Duration of Action | Sustained effect with once-daily dosing; improvement maintained with continued use; full therapeutic effect may require 12 weeks. |
Apply a pea-sized amount to the affected area(s) once daily, in the evening. Rub in gently. Use on face only.
| Dosage form | CREAM |
| Renal impairment | No dosage adjustment required for renal impairment; not studied in severe renal impairment. |
| Liver impairment | No dosage adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B); not studied in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Safety and efficacy in pediatric patients below 18 years of age have not been established. |
| Geriatric use | No specific geriatric dosing adjustments; use based on clinical response and tolerability; clinical studies did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SOOLANTRA (SOOLANTRA).
| Breastfeeding | It is unknown whether ivermectin is excreted in human milk after topical application. Following oral administration, ivermectin is excreted in breast milk with a milk-to-plasma ratio of approximately 0.5. Due to low systemic absorption after topical use, the amount ingested by a nursing infant is expected to be minimal. Caution is advised; use only if clearly needed. |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. In animal reproduction studies, subcutaneous administration of ivermectin (the active ingredient) during organogenesis at doses equivalent to 0.3 to 3 times the maximum recommended human dose based on AUC resulted in maternal toxicity and fetal malformations (cleft palate, clubbed forepaws) at the high dose. However, systemic absorption following topical application of SOOLANTRA is minimal (<10 ng/mL). Based on animal data and low systemic exposure, the risk is considered low, but use during pregnancy only if clearly needed. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to ivermectin or any component of the formulation."]
| Precautions | ["Not for oral, ophthalmic, or intravaginal use.","Skin irritation or allergic reactions may occur.","Avoid contact with eyes.","Use in pregnancy only if clearly needed (Pregnancy Category C)."] |
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| Fetal Monitoring | No specific maternal or fetal monitoring required beyond routine prenatal care. Inadvertent oral ingestion or excessive topical use may warrant monitoring for systemic effects. |
| Fertility Effects | No studies on fertility have been conducted with SOOLANTRA. In animal studies with oral ivermectin at doses up to 3 times the maximum recommended human dose, no adverse effects on fertility were observed. Due to minimal systemic absorption, effects on fertility are unlikely. |