Abamectin
| 来源-本站收集整理 | 作者-本站 | 2014-08-13

ABAMECTIN

CASRN: 71751-41-2
Chemical structure for ABAMECTIN



Human Health Effects:


Evidence for Carcinogenicity:
Cancer Classification: Group E - Evidence of Non-carcinogenicity for Humans
[USEPA Office of Pesticide Programs, Health Effects Division, Science Information Management Branch: "Chemicals Evaluated for Carcinogenic Potential" (April 2006)] **QC REVIEWED**


Human Toxicity Excerpts:
STUDY OBJECTIVE: Avermectins have been used in the control of parasites and insects; however, human data concerning poisoning are lacking. This study investigated the clinical spectrum of avermectin poisoning. METHODS: A retrospective study was conducted to evaluate patients with avermectin poisoning reported to a poison center from September 1993 through December 1997. RESULTS: Eighteen patients with abamectin (Agri-Mek; 2% wt/wt abamectin) exposure and 1 with ivermectin (Ivomec; 1% wt/vol ivermectin) ingestion were identified. There were 14 male and 5 female patients, ranging in age from 15 to 83 years. Most patients were exposed as a result of attempted suicide (14). Oral ingestion (15) was the most common route of exposure. Four patients were asymptomatic, and 8 had minor symptoms after a mean ingestion of 23 mg/kg abamectin (4.2 to 67 mg/kg), or after dermal and inhalation contact. Seven patients manifested severe symptoms, such as coma (7), aspiration with respiratory failure (4), and hypotension (3), after a mean ingestion of 100.7 mg/kg avermectin (15.4 mg/kg for ivermectin and 114.9 mg/kg for abamectin). All 7 patients received intensive supportive care; 1 patient died 18 days later as a result of multiple organ failure. CONCLUSION: Ingestion of a large dose of avermectin may be associated with life-threatening coma, hypotension, and subsequent aspiration.
[Chung K et al; Ann Emerg Med 34 (1): 51-7 (1991)] **PEER REVIEWED**


Skin, Eye and Respiratory Irritations:
Mild eye irritant; non-irritating to skin (rabbits).
[Tomlin, C.D.S. (ed.). The Pesticide Manual - World Compendium. 10th ed. Surrey, UK: The British Crop Protection Council, 1994., p. 4] **PEER REVIEWED**


Probable Routes of Human Exposure:
Occupational exposure to abamectin may occur through dermal contact with this compound at workplaces where abamectin is produced or used(SRC). A study of worker re-entry exposure in greenhouses showed that abamectin present on chrysanthemum seedlings as dislodgeable foliar residues, following both low- and high-volume spraying at 0.09 g ai/1000 sq m, had half-lives of 1.1 and 2.4 days, respectively(1). A study of worker exposure to abamectin on 12 rose culture farms in greenhouses found that dermal exposure was 13 ug/hr approximately 23 hours after treatment; similar exposure levels were found for workers involved with bundling and sorting(2).
[(1) Brouwer DH et al; Bull Environ Contam Toxicol 58: 976-84 (1997) (2) Brouwer R et al; Arch Environ Contam Toxicol 23: 273-80 (1992)] **PEER REVIEWED**


Emergency Medical Treatment:


Emergency Medical Treatment:
EMT Copyright Disclaimer:
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The following Overview, *** IVERMECTIN AND RELATED AGENTS ***, is relevant for this HSDB record chemical.

Life Support:
o   This overview assumes that basic life support measures
       have been instituted.
Clinical Effects:
0.2.1 SUMMARY OF EXPOSURE
   0.2.1.1 ACUTE EXPOSURE
     A)  USES: Avermectins are macrocyclic lactones used for
         control of nematode and arthropod parasites. Ivermectin
         0.5% topical lotion is used for the topical treatment
         of head lice infestations. Oral ivermectin is indicated
         for the treatment of nondisseminated strongyloidiasis
         of the intestinal tract and Onchocerciasis (river
         blindness), due to the non-adult stage of nematode
         parasite Onchocerca volvulus. Abamectin, doramectin,
         and eprinomectin are agricultural miticides and
         insecticides. Selamectin is a topical parasiticide.
         Moxidectin is a parasiticide given to animals (ie,
         dogs, cats, livestock, horses) for the prevention,
         treatment and/or control of parasites, such as
         heartworms. Moxidectin is from the milbemycin class,
         and is a semisynthetic derivative of nemadectin.
     B)  PHARMACOLOGY: The macrocyclic lactone (macrolide)
         antimicrobial class contains 2 closely related chemical
         groups, avermectins and milbemycins. These 2 chemical
         groups have a large complex macrocyclic backbone and
         have been produced by fermentation of soil dwelling
         fungal organisms (genus Streptomyces). Ivermectin is a
         semisynthetic antiparasitic drug and a member of the
         avermectin class. It binds selectively and with high
         affinity to glutamate-gated chloride ion channels in
         invertebrate muscle and nerve cells of the
         microfilaria. This binding causes an increase in the
         permeability of the cell membrane to chloride ions and
         results in hyperpolarization of the cell, leading to
         paralysis and death of the parasite. Ivermectin also is
         believed to act as an agonist of the neurotransmitter
         gamma-aminobutyric acid (GABA), thereby disrupting
         GABA-mediated central nervous system (CNS)
         neurosynaptic transmission.
     C)  EPIDEMIOLOGY: Overdose is rare.
     D)  WITH THERAPEUTIC USE
      1)  Ivermectin is generally well-tolerated following
          therapeutic use. Pruritus and tachycardia have been
          reported.
     E)  WITH POISONING/EXPOSURE
      1)  MILD TO MODERATE TOXICITY: Rash, urticaria, pruritus,
          edema, headache, dizziness, somnolence, asthenia,
          nausea, vomiting, abdominal pain, diarrhea, and mild
          tachycardia have been reported.
      2)  SEVERE TOXICITY: In severe overdose, seizures, coma,
          aspiration pneumonia, metabolic acidosis, respiratory
          failure, and hypotension may develop.
      3)  DRUG INTERACTION: Ivermectin is thought to potentiate
          GABA activity. Other drugs, such as barbiturates,
          benzodiazepines and valproic acid, which also enhance
          GABA activity, may increase its toxicity.
      4)  ANIMAL STUDIES: In animals, high dose ivermectin may
          produce a CNS toxicosis consisting of tremors, ataxia,
          weakness, incoordination, recumbency, dehydration and
          coma.
  0.2.3 VITAL SIGNS
   0.2.3.1 ACUTE EXPOSURE
     A)  WITH POISONING/EXPOSURE
      1)  Mild tachycardia, hypotension, fever, and hypothermia
          have been reported.
  0.2.4 HEENT
   0.2.4.1 ACUTE EXPOSURE
     A)  ANIMAL STUDIES: Mydriasis has been reported during
         pharmacological testing in dogs.
     B)  WITH THERAPEUTIC USE
      1)  Sore throat has been observed.
     C)  WITH POISONING/EXPOSURE
      1)  Mydriasis developed in one pupil of a child who
          accidentally ingested 7 mg/kg.
      2)  When accidentally sprayed into the eye of an adult,
          only stinging resulted.
  0.2.13 HEMATOLOGIC
   0.2.13.1 ACUTE EXPOSURE
     A)  WITH THERAPEUTIC USE
      1)  Prolonged prothrombin times and hematoma formation
          have been reported as side effects of ivermectin
          treatment.
  0.2.15 MUSCULOSKELETAL
   0.2.15.1 ACUTE EXPOSURE
     A)  WITH THERAPEUTIC USE
      1)  Arthralgia, synovitis, bone pain, and myalgia have
          been reported.
  0.2.20 REPRODUCTIVE HAZARDS
    A)  Ivermectin is classified as FDA pregnancy category C. In
        a study of pregnant women who received ivermectin, no
        adverse effects were observed. However, ivermectin has
        the potential for crossing the blood-brain barrier
        following high doses and causing CNS effects. In animal
        studies, ivermectin has resulted in cleft palate
        following doses at or near levels that are maternotoxic
        in mice, rats and rabbits. Ivermectin is excreted in
        breast milk at low concentrations. Breast milk
        concentrations were a mean of 14 nanograms/mL following
        administration of oral ivermectin to nursing mothers.
  0.2.23 OTHER
   0.2.23.1 ACUTE EXPOSURE
     A)  WITH THERAPEUTIC USE
      1)  Swelling and tenderness of the lymph glands has been
          reported.
Laboratory:
A)  No specific laboratory tests are necessary in patients
       with mild overdose.
   B)  Plasma concentrations are not readily available or
       clinically useful in the management of overdose.
   C)  Monitor vital signs and mental status following
       significant overdose. Monitor serum electrolytes, pulse
       oximetry and respiratory status in patients with severe
       overdose.
   D)  Monitor serum electrolytes in patients with significant
       vomiting and/or diarrhea.
Treatment Overview:
0.4.2 ORAL EXPOSURE
    A)  MANAGEMENT OF MILD TO MODERATE TOXICITY
     1)  Treatment is symptomatic and supportive. Manage mild
         hypotension with IV fluids.
    B)  MANAGEMENT OF SEVERE TOXICITY
     1)  Treatment is symptomatic and supportive. Treat seizures
         with IV benzodiazepines; barbiturates or propofol may
         be needed if seizures persist or recur. Treat severe
         hypotension IV 0.9% NaCl at 10 to 20 mL/kg. Add
         dopamine or norepinephrine if unresponsive to fluids.
         Treat severe metabolic acidosis (pH less than 7.1) with
         sodium bicarbonate 1 to 2 mEq/kg. Consider intravenous
         lipid emulsion in patients with dysrhythmias,
         hypotension or severe CNS toxicity secondary to
         ivermectin intoxication.
    C)  DECONTAMINATION
     1)  PREHOSPITAL: Prehospital gastrointestinal
         decontamination is not recommended because of the
         potential for CNS depression or persistent seizures and
         subsequent aspiration.
     2)  HOSPITAL: Consider activated charcoal if the overdose
         is recent, the patient is not vomiting, and is able to
         maintain airway.
    D)  AIRWAY MANAGEMENT
     1)  Ensure adequate ventilation and perform endotracheal
         intubation early in patients with respiratory or CNS
         depression or hemodynamic instability.
    E)  ANTIDOTE
     1)  None
    F)  ENHANCED ELIMINATION
     1)  Hemodialysis is unlikely to be of value because of the
         high degree of protein binding and large volume of
         distribution.
    G)  PATIENT DISPOSITION
     1)  HOME CRITERIA: A patient with an inadvertent exposure,
         that remains asymptomatic can be managed at home.
     2)  OBSERVATION CRITERIA: Patients with a deliberate
         overdose, and those who are symptomatic should be
         observed with frequent monitoring of vital signs.
         Patients that remain asymptomatic can be discharged.
     3)  ADMISSION CRITERIA: Patients should be admitted for
         severe vomiting, profuse diarrhea, severe abdominal
         pain, dehydration, and electrolyte abnormalities.
         Patients with unstable vital signs, persistent
         seizures, coma, metabolic acidosis, or respiratory
         failure should also be admitted.
     4)  CONSULT CRITERIA: Consult a poison center or medical
         toxicologist for assistance in managing patients with
         severe toxicity or in whom the diagnosis is not clear.
    H)  PITFALLS
     1)  When managing a suspected overdose, the possibility of
         multidrug involvement should be considered.
    I)  PHARMACOKINETICS
     1)  Ivermectin is absorbed orally, parenterally, and
         dermally. Tmax: 3 to 5 hours after oral dosing. Protein
         binding: approximately 93%. Vd: 46.9 L. Ivermectin and
         its metabolites are most likely excreted in the bile.
         Elimination half-life: oral, 10 to 18 hours (may be 1
         to 4 days in various animal species).
    J)  DIFFERENTIAL DIAGNOSIS
     1)  Includes other chemicals or drugs that cause
         hypotension (eg, vasodilators, beta blockers, calcium
         channel blockers), metabolic acidosis (eg,
         salicylates), or CNS depression (eg, toxic alcohols,
         benzodiazepines, opiates/opioids, antipsychotic
         medications). Diseases or exposures that produce acute
         respiratory distress (eg, inhalation of acid or
         alkaline mists, asthma, COPD).
Range of Toxicity:
A)  TOXICITY: An oral ivermectin dose of 100 to 130 mg (6.6
       to 8.7 mg/kg) produced vomiting, somnolence, and mild
       cardiovascular symptoms in a 15 kg child. Ingestion of 1
       gram (ivermectin) or 2.5 to 12 grams (abamectin) has
       resulted in serious toxicity. THERAPEUTIC DOSE: 150 to
       200 mcg/kg.

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