Spinosad

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# Overview
Spinosad is a Dermatological Agent that is FDA approved for the treatment of head lice.   Common adverse reactions include application site erythema and ocular erythema.

# Adult Indications and Dosage

## FDA-Labeled Indications and Dosage (Adult)

### Indications
- Spinosad Topical Suspension is indicated for the topical treatment of head lice infestation in patients four (4) years of age and older.
- Spinosad Topical Suspension should be used in the context of an overall lice management program:
- Wash (in hot water) or dry-clean all recently worn clothing, hats, used bedding and towels.
- Wash personal care items such as combs, brushes and hair clips in hot water
- A fine-tooth comb or special nit comb may be used to remove dead lice and nits.

### Dosage
- For topical use only. Spinosad Topical Suspension is not for oral, ophthalmic, or intravaginal use.
- Shake bottle well. Apply sufficient Spinosad Topical Suspension to cover dry scalp, then apply to dry hair. Depending on hair length, apply up to 120 mL (one bottle) to adequately cover scalp and hair. Leave on for 10 minutes, then thoroughly rinse off Spinosad Topical Suspension with warm water. If live lice are seen 7 days after the first treatment, a second treatment should be applied. Avoid contact with eyes.

## Off-Label Use and Dosage (Adult)

### Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Spinosad in adult patients.

### NonGuideline-Supported Use
There is limited information regarding Off-Label NonGuideline-Supported Use of Spinosad in adult patients.

# Pediatric Indications and Dosage

## FDA-Labeled Indications and Dosage (Pediatric)

### Indications
- Spinosad Topical Suspension is indicated for the topical treatment of head lice infestation in patients four (4) years of age and older.
- Spinosad Topical Suspension should be used in the context of an overall lice management program:
- Wash (in hot water) or dry-clean all recently worn clothing, hats, used bedding and towels.
- Wash personal care items such as combs, brushes and hair clips in hot water
- A fine-tooth comb or special nit comb may be used to remove dead lice and nits.

### Dosage
- For topical use only. Spinosad Topical Suspension is not for oral, ophthalmic, or intravaginal use.
Shake bottle well. Apply sufficient Spinosad Topical Suspension to cover dry scalp, then apply to dry hair. Depending on hair length, apply up to 120 mL (one bottle) to adequately cover scalp and hair. Leave on for 10 minutes, then thoroughly rinse off Spinosad Topical Suspension with warm water. If live lice are seen 7 days after the first treatment, a second treatment should be applied. Avoid contact with eyes.

## Off-Label Use and Dosage (Pediatric)

### Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Spinosad in pediatric patients.

### NonGuideline-Supported Use
There is limited information regarding Off-Label NonGuideline-Supported Use of Spinosad in pediatric patients.

# Contraindications
- None

# Warnings
- Spinosad Topical Suspension contains benzyl alcohol and is not recommended for use in neonates and infants below the age of 6 months. Systemic exposure to benzyl alcohol has been associated with serious adverse reactions and death in neonates and low birth-weight infants

# Adverse Reactions

## Clinical Trials Experience
- Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in clinical practice.
- Spinosad Topical Suspension was studied in two randomized, active-controlled trials (N=552) in subjects with head lice; the results are presented in Table 1.
- Other less common reactions (less than 1% but more than 0.1%) were application site dryness, application site exfoliation, alopecia, and dry skin.
- Systemic safety was not assessed in pediatric subjects under 4 years of age as laboratory parameters were not monitored in these controlled studies.

## Postmarketing Experience
There is limited information regarding Postmarketing Experience of Spinosad in the drug label.

# Drug Interactions
There is limited information regarding Spinosad Drug Interactions in the drug label.

# Use in Specific Populations

### Pregnancy
Pregnancy Category (FDA): B
- There are no adequate and well-controlled studies with Spinosad Topical Suspension in pregnant women. Studies in humans did not assess for the absorption of benzyl alcohol contained in Spinosad Topical Suspension. Reproduction studies conducted in rats and rabbits were negative for teratogenic effects. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
- No comparisons of animal exposure with human exposure are provided in this labeling due to the low systemic exposure noted in the clinical pharmacokinetic study which did not allow for the determination of human AUC values that could be used for this calculation.
- Systemic embryofetal development studies were conducted in rats and rabbits. Oral doses of 10, 50 and 200 mg/kg/day spinosad were administered during the period of organogenesis (gestational days 6  15) to pregnant female rats. No teratogenic effects were noted at any dose. Maternal toxicity occurred at 200 mg/kg/day. Oral doses of 2.5, 10, and 50 mg/kg/day spinosad were administered during the period of organogenesis (gestational days 7  19) to pregnant female rabbits. No teratogenic effects were noted at any dose. Maternal toxicity occurred at 50 mg/kg/day.
- A two-generation dietary reproduction study was conducted in rats. Oral doses of 3, 10, and 100 mg/kg/day spinosad were administered to male and female rats from 10-12 weeks prior to mating and throughout mating, parturition, and lactation. No reproductive/developmental toxicity was noted at doses up to 10 mg/kg/day. In the presence of maternal toxicity, increased dystocia in parturition, decreased gestation survival, decreased litter size, decreased pup body weight, and decreased neonatal survival occurred at a dose of 100 mg/kg/day.
Pregnancy Category (AUS):
- Australian Drug Evaluation Committee (ADEC) Pregnancy Category
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Spinosad in women who are pregnant.

### Labor and Delivery
There is no FDA guidance on use of Spinosad during labor and delivery.

### Nursing Mothers
- Spinosad, the active ingredient in Spinosad Topical Suspension is not systemically absorbed; and therefore, will not be present in human milk. However, Spinosad Topical Suspension contains benzyl alcohol, which may be systemically absorbed through the skin, and the amount of benzyl alcohol excreted in human milk with use of Spinosad Topical Suspension is unknown. Caution should be exercised when Spinosad Topical Suspension is administered to a lactating woman. A lactating woman may choose to pump and discard breast milk for 8 hours (5 half-lives of benzyl alcohol) after use to avoid infant ingestion of benzyl alcohol.

### Pediatric Use
- The safety and effectiveness of Spinosad Topical Suspension have been established in pediatric patients 4 years of age and older with active head lice infestation.
- Safety in pediatric patients below the age of 4 years has not been established. Spinosad Topical Suspension is not recommended in pediatric patients below the age of 6 months because of the potential for increased systemic absorption due to a high ratio of skin surface area to body mass and the potential for an immature skin barrier.
- Spinosad Topical Suspension contains benzyl alcohol which has been associated with serious adverse reactions and death in neonates and low birth-weight infants. The "gasping syndrome" (characterized by central nervous system depression, metabolic acidosis, gasping respirations, and high levels of benzyl alcohol and its metabolites found in the blood and urine) has been associated with benzyl alcohol dosages >99 mg/kg/day in neonates and low-birthweight infants. Additional symptoms may include gradual neurological deterioration, seizures, intracranial hemorrhage, hematologic abnormalities, skin breakdown, hepatic and renal failure, hypotension, bradycardia, and cardiovascular collapse.
- The minimum amount of benzyl alcohol at which toxicity may occur is not known. Premature and low-birthweight infants, as well as patients receiving high dosages, may be more likely to develop toxicity

### Geriatic Use
Clinical studies of Spinosad Topical Suspension did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

### Gender
There is no FDA guidance on the use of Spinosad with respect to specific gender populations.

### Race
There is no FDA guidance on the use of Spinosad with respect to specific racial populations.

### Renal Impairment
There is no FDA guidance on the use of Spinosad in patients with renal impairment.

### Hepatic Impairment
There is no FDA guidance on the use of Spinosad in patients with hepatic impairment.

### Females of Reproductive Potential and Males
There is no FDA guidance on the use of Spinosad in women of reproductive potentials and males.

### Immunocompromised Patients
There is no FDA guidance one the use of Spinosad in patients who are immunocompromised.

# Administration and Monitoring

### Administration
- topical

### Monitoring
There is limited information regarding Monitoring of Spinosad in the drug label.

# IV Compatibility
There is limited information regarding IV Compatibility of Spinosad in the drug label.

# Overdosage
If oral ingestion occurs, seek medical advice immediately.

# Pharmacology

## Mechanism of Action
- Spinosad causes neuronal excitation in insects. After periods of hyperexcitation, lice become paralyzed and die.

## Structure
- Spinosad Topical Suspension, is a slightly opaque, light orange colored, viscous topical suspension.
- Spinosad, the active ingredient, is derived from the fermentation of a soil actinomycete bacterium, Saccharopolyspora spinosa.
- Spinosad is a mixture of spinosyn A and spinosyn D in a ratio of approximately 5 to 1 (spinosyn A to spinosyn D).
- Spinosyn A: The chemical name is: 1H-as-Indacenooxacyclododecin-7,a5-dione, 2-(6-deoxy-2,3,4-tri-O-methyl-alpha- L-mannopyranosyl)oxy]-13-2R,5S,6R)-5-(dimethylamino) tetrahydro-6-methyl-2H-pyran-2-yloxy-9-ethyl- 2,3,3a,5a,5b,6,9,10,11,12,13,14,16a,16b-tetradecahydro-14-metyl-, (2R,3aS,5aR,5bS,9S,13S,14R,16aS,16bR)-
- Spinosyn D: The chemical name is: 1H-as-Indaceno3,2- doxacyclododecin-7,15-dione, 2-(6-deoxy-2,3,4-tri-O-methyl-alpha- L-mannopyranosyl)oxy-13-2R,5S,6R)-5-(dimethylamino) tetrahydro-6-methyl-2H-pyran-2-yl]oxy]-9-ethyl- 2,3,3a,5a,5b,6,9,10,11,12,13,14,16a,16b-tetradecahydro-4,14-dimetyl-, (2S,3aSR,5aS,5bS,9S,13S,14R,16aS,16bS)-
- Spinosad Topical Suspension contains 9 mg spinosad per gram in a viscous, slightly opaque, light orange colored vehicle consisting of Water, Isopropyl Alcohol, Benzyl Alcohol, Hexylene Glycol, Propylene Glycol, Cetearyl Alcohol, Stearalkonium Chloride, Ceteareth-20, Hydroxyethyl Cellulose, Butylated Hydroxytoluene, FD&C Yellow #6.

## Pharmacodynamics
The pharmacodynamics of Spinosad Topical Suspension has not been studied.

## Pharmacokinetics
- An open-label, single-center study was conducted over a period of seven days to determine the pharmacokinetic profile of spinosad 1.8% in pediatric subjects with head lice infestation. Fourteen (14) subjects, 4  15 years of age, with head lice were enrolled into the study. All subjects applied a single topical (scalp) treatment of spinosad 1.8% for 10 minutes, after which the test article was washed off, and subjects underwent plasma sampling. Plasma samples were analyzed by a validated LC/MS/MS method. Results demonstrated that spinosad was below the limit of quantitation (3ng/mL) in all samples. The bioavailability of benzyl alcohol from Spinosad Topical Suspension is unknown as plasma concentrations of benzyl alcohol were not determined in these subjects.

## Nonclinical Toxicology
- In an oral (diet) mouse carcinogenicity study, spinosad was administered to CD-1 mice at doses of 0.0025, 0.008, and 0.036% in the diet (approximately 3.4, 11.4, and 50.9 mg/kg/day for males and 4.2, 13.8, and 67.0 mg/kg/day for females) for 18 months. No treatment-related tumors were noted in the mouse carcinogenicity study up to the highest doses evaluated in this study of 50.9 mg/kg/day in male mice and 13.8 mg/kg/day in female mice. Female mice treated with a dose of 67.0 mg/kg/day were not evaluated in this study due to high mortality.
- In an oral (diet) rat carcinogenicity study, spinosad was administered to Fischer 344 rats at doses of 0.005, 0.02, 0.05, and 0.1% in the diet (approximately 2.4, 9.5, 24.1 and 49.4 mg/kg/day for males and 3.0, 12.0, 30.1 and 62.8 mg/kg/day for females) for 24 months. No treatment-related tumors were noted in the rat carcinogenicity study in male or female rats up to the highest doses evaluated in this study of 24.1 mg/kg/day in male rats and 30.1 mg/kg/day in female rats. Rats in the highest dose group in this study were not evaluated due to high mortality.
- Spinosad demonstrated no evidence of mutagenic or clastogenic potential based on the results of four in vitro genotoxicity tests (Ames assay, mouse lymphoma L5178Y assay, Chinese hamster ovary cell chromosome aberration assay, and rat hepatocyte unscheduled DNA synthesis assay) and one in vivo genotoxicity test (mouse bone marrow micronucleus assay).
- Oral administration of spinosad (in diet) to rats, throughout mating, gestation, parturition and lactation, demonstrated no effects on growth, fertility or reproduction, at doses up to 10 mg/kg/day

# Clinical Studies
- Two multicenter, randomized, investigator-blind, activecontrolled studies were conducted in 1038 subjects 6 months of age and older with head lice infestation. A total of 552 subjects were treated with Spinosad Topical Suspension. For the evaluation of efficacy, the youngest subject from each household was considered to be the primary subject of the household, and other members in the household were enrolled in the study as secondary subjects, and evaluated for all safety parameters.
- In Study 1, 91 primary subjects were randomized to Spinosad Topical Suspension, and 89 primary subjects were randomized to permethrin 1%. In Study 2, 83 and 84 primary subjects were randomized to Spinosad Topical Suspension and permethrin 1%, respectively.
- In both studies, all subjects who were treated on Day 0 returned for efficacy evaluation at Day 7. Subjects with live lice present at Day 7 received a second treatment. Subjects who were lice free on Day 7 were to return on Day 14 for evaluation. Subjects with live lice and who received a second treatment were to return on Days 14 and 21.
- Efficacy was assessed as the proportion of primary subjects who were free of live lice 14 days after the final treatment. Table 2 contains the proportion of primary subjects who were free of live lice in each of the two trials.

# How Supplied
- Spinosad Topical Suspension, 0.9% is a slightly opaque, light orange colored, viscous liquid, supplied in 4 oz (120 mL) high density polyetheylene (HDPE) bottles. NDC 28595-570-04

## Storage
- Store at 25C (77F); excursions permitted to 15 to 30C (59 to 86F).
- Keep out of reach of children

# Images

## Drug Images

## Package and Label Display Panel

### PRINCIPAL DISPLAY PANEL - 120 ML BOTTLE CARTON

### Ingredients and Appearance

# Patient Counseling Information
The patient should be instructed as follows:
- Shake bottle well immediately prior to use
- Use Spinosad Topical Suspension only on dry scalp and dry scalp hair.
- Do not swallow.
- Avoid contact with eyes. If Spinosad Topical Suspension gets in or near the eyes, rinse thoroughly with water.
- Wash hands after applying Spinosad Topical Suspension
- Use Spinosad Topical Suspension on children only under direct supervision of an adult.
- If pregnant or breastfeeding, consult a physician before use.

### PATIENT INFORMATION
PATIENT INSTRUCTIONS FOR USE

# Precautions with Alcohol
- Alcohol-Spinosad interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

# Brand Names
- SPINOSAD

# Look-Alike Drug Names
- There is limited information regarding look alike drug names.

# Drug Shortage Status

# Price