Malathion Lotion USP, 0.5% | MALATHION
For topical use only. Not for oral or ophthalmic use.
Malathion lotion contains 0.005 g of malathion per mL in a vehicle of isopropyl alcohol (78%), terpineol, dipentene, and pine needle oil. The chemical name of malathion is (±) - [(dimethoxyphosphinothioyl) - thio] butanedioic acid diethyl ester. Malathion has a molecular weight of 330.36, represented by CHOPS, and has the following chemical structure:
Malathion is an organophosphate agent which acts as a pediculicide by inhibiting cholinesterase activity in vivo. Inadvertent transdermal absorption of malathion has occurred from its agricultural use. In such cases, acute toxicity was manifested by excessive cholinergic activity, i.e., increased sweating, salivary and gastric secretion, gastrointestinal and uterine motility, and bradycardia (see OVERDOSAGE ). Because the potential for transdermal absorption of malathion from malathion lotion is not known at this time, strict adherence to the dosing instructions regarding its use in children, method of application, duration of exposure, and frequency of application is required.
Malathion lotion is indicated for patients infected with Pediculus humanus capitis (head lice and their ova) of the scalp hair.
Malathion lotion is contraindicated for neonates and infants because their scalps are more permeable and may have increased absorption of malathion. Malathion lotion should also not be used on individuals known to be sensitive to malathion or any of the ingredients in the vehicle.
Keep out of reach of children. Close eyes tightly during product application. If accidentally placed in the eye, flush immediately with water. Use only on scalp hair.
There are no special laboratory tests needed in order to use this medication.
Carcinogenesis, mutagenesis and impairment of fertility have not been studied with malathion lotion (0.5% pharmaceutical grade malathion). However, following long-term oral administration of technical grade malathion to rodents via dietary supplementation, increased incidences of hepatocellular neoplastic lesions were observed in B6C3F1 mice dosed for 18 months at malathion doses greater than 1500 mg/kg/day, and in female F344 rats dosed for 2 years at malathion doses greater than 400 mg/kg/day. These tumors occurred only in association with severe hepatic toxicity and chronic suppression of acetylcholinesterase activity, or at doses causing excessive mortality. Based on body surface area, doses at which carcinogenic effects were observed in rodents following life-time exposures to malathion were approximately 14- to 26-fold greater than the maximum dose anticipated in a 10 kg child following a single use of malathion lotion, assuming 100% bioavailability. Actual systemic exposures are expected to be less than 10% of the administered dose.
The malathion of greater than pharmaceutical-grade purity used in malathion lotion has not been tested for genotoxicity. The technical-grade malathion (95% pure) was found to be negative in Salmonella typhimurium, equivocally positive in the mouse lymphoma cell assay, 577 and positive in in vitro chromosomal aberration and sister chromatid exchange assays. Fifteen separate in vitro gene mutation studies with malathion of unknown purity have reported negative results, while three studies reported malathion to be mutagenic in bacterial cells. Both technical grade (94–96.5%) and purified (98-99%) malathion have been reported to cause chromosomal aberrations and sister chromatid exchanges in vitro in human and hamster cell lines. In vivo chromosomal aberration and micronucleus studies of technical-grade malathion are reported to be positive, whereas an in vivo chromosomal aberration study of >99% pure malathion was reported to be negative. Furthermore, mice exposed to malathion in their drinking water for 7 weeks demonstrated no evidence of chromosome damage in bone marrow cells, spermatogonia, or primary spermatocytes. Lack of details makes independent evaluation of the results of these assays impossible. Ashby and Purchase have suggested that impurities may be responsible for some of the observed genetic activity of malathion.
Reproduction studies performed with malathion in rats at doses over 180 fold greater than those anticipated in a 60 kg adult (based on body surface area and assuming 100% bioavailability) revealed no evidence of impaired fertility.
There was no evidence of teratogenicity in studies in rats and rabbits at doses up to 900 mg/kg/day and 100 mg/kg/day malathion, respectively. A study in rats failed to show any gross fetal abnormalities attributable to feeding malathion up to 2,500 ppm (~ 200 mg/kg/day) in the diet during a three - generation evaluation period. These doses were approximately 40 to 180 times higher than the dose anticipated in a 60 kg adult (based on body surface area and assuming 100% bioavailability). Because animal reproduction studies are not always predictive of human responses, this drug should be used (or handled) during pregnancy only if clearly needed.
Malathion in an acetone vehicle has been reported to be absorbed through human skin to the extent of 8% of the applied dose. However, percutaneous absorption from the malathion lotion, 0.5% formulation has not been studied, and it is not known whether malathion is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when malathion lotion is administered to (or handled by) a nursing mother.
The safety and effectiveness of malathion lotion in children less than 6 years of age has not been established via well-controlled trials.
Malathion has been shown to be irritating to the skin and scalp. Accidental contact with the eyes can result in mild conjunctivitis.
It is not known if malathion lotion has the potential to cause contact allergic sensitization.
Consideration should be given, as part of the treatment program, to the high concentration of isopropyl alcohol in the vehicle.
Malathion, although a weaker cholinesterase inhibitor than some other organophosphates, may be expected to exhibit the same symptoms of cholinesterase depletion after accidental ingestion orally. If accidentally swallowed, vomiting should be induced promptly or the stomach lavaged with 5% sodium bicarbonate solution.
Severe respiratory distress is the major and most serious symptom of organophosphate poisoning requiring artificial respiration, and atropine may be needed to counteract the symptoms of cholinesterase depletion.
Repeat analyses of serum and RBC cholinesterase may assist in establishing the diagnosis and formulating a long - range prognosis.
Further treatment is generally not necessary. Other family members should be evaluated by a physician to determine if infested, and if so, receive treatment.
Two controlled clinical trials evaluated the pediculicidal activity of malathion lotion. Patients applied the lotion to the hair and scalp in quantities, up to a maximum of 2 fl. oz., sufficient to thoroughly wet the hair and scalp. The lotion was allowed to air dry and was shampooed with Prell shampoo 8 to 12 hours after application. Patients in both the malathion lotion group and in the vehicle group were examined immediately after shampooing, 24 hours after, and 7 days after for the presence of live lice. Results are shown in the following table:
The presence or absence of ova at day 7 was not evaluated in these studies. The presence or absence of live lice or ova at 14 days following treatment was not evaluated in these studies. The residual amount of malathion on hair and scalp is unknown.
|Treatment||Immediately After||24 Hrs. After||7 Days After|
Malathion Lotion USP, 0.5%, is supplied in bottles of 2 fl. oz. (59 mL) NDC 51672-5277-4. Store at controlled room temperature 20° - 25°C (68° - 77°F) [see USP Controlled Room Temperature].
Flammable. Keep away from heat and open flame.
Issued: August, 200970829-0809-0 577
|Mfd. by:||Taro Pharmaceutical Industries Ltd., Haifa Bay, Israel 26110|
Taro Pharmaceuticals U.S.A., Inc., Hawthorne, NY 10532
TARO is a registered trademark of Taro Pharmaceuticals U.S.A., Inc.
2 fl oz (59 mL)
In isopropyl alcohol (78%),terpineol, dipentene andpine needle oil.
WARNING: Contains flammable alcohol.Avoid smoking, open flame and hair dryers.Allow hair to dry naturally and uncovered.
TARO PHARMACEUTICALS U.S.A., INC.
Drugs and Medications
Malathion Lotion, USP 0.5%
Malathion Lotion, USP 0.5%
Ovide (malathion) Lotion, 0.5%
In this study, 24 adult patients with head lice will be treated with a topical malathion head lice treatment; 12 patients will be treated with a novel product, Malathion Gel, 0.5%, and oth...
In this study, Malathion Gel 0.5% will be compared to Nix (permethrin 1%) as a treatment for head lice in patients 2 years of age and older. Malathion Gel 0.5% is a new formulation of an e...
Current treatments for head lice include over-the-counter products such as permethrin and prescription products such as OVIDE (malathion 0.5%) lotion. In a previous phase II study, a nove...
The purpose of this study is to compare 2 single doses of ivermectin as tablets with 2 single applications of malathion 0.5% lotion (Days 1 and 8) in clearing head lice, in patients who ha...
In a previous phase II study, the safety and efficacy of a novel formulation of malathion 0.5% was evaluated in patients 2 years of age and older. Based on the results of that study, this...
Discriminating concentrations (DCs) of malathion, coumaphos, fenvalerate and fipronil were determined to monitor acaricide resistance in field conditions. The LC99 values with 95% confidence interval ...
The present study aimed at verifying the usefulness of dietary 2.5% bee-pollen (BP) or propolis (PROP) to overcome the genotoxic and endocrine disruptive effects of malathion polluted water in Oreochr...
Understanding how ecological interactions mitigate the impacts of perturbations such as pesticides in biological communities is an important basic and applied question for ecologists. In aquatic ecosy...
The sugarcane borer Diatraea saccharalis is widely known as the main pest of sugarcane crop, causing increased damage to the entire fields. Measures to control this pest involve the use of chemicals a...
Pesticide-induced endocrine disruption often mimics sex steroidal action resulting in physiological functional disarray of hypothalamo-hypophyseal-gonadal (HHG) system at multiple levels. Among variou...