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Ivermectin

Ivermectin structure

CAS No:
70288-86-7
Chemical Name:
Ivermectin
Synonyms:
Ivermectin;Hyvermectin;MK 933;22,23-Dihydroavermectin B1;Ivomec;Eqvalan;Heartgard 30;Mectizan;Pandex;Phoenectin;Jetamec;Equimec;Equimec Paste;L 640471;Cardomec;Zimecterin;Cardotek 30;Stromectol;Ivectin;Heartgard;Vermic;Uvemec;Cevamec;Oramec;Ivertin;Noramectin;Ivosint;Bimectin;Vetmec;Noromectin;Bovinet;Bagomectina;Equirat Gold;Cardotek Plus;Equimectrin;Virbamec LA;Iversalt;Oramectin;Ivermec;Ivomec Gold;Mukhnet I;Solantra;Soolantra;Ivermectin B1a-ivermectin B1b mixture;118710-50-2;74564-75-3;1014990-52-3
Categories:
Active Pharmaceutical Ingredients > Antiparasitic Drugs

Description

Ivermectin is a widely used antiparasitic agent in human and veterinary medicine. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs).

Ivermectin is an antiinfective agent with activity against several parasitic nematodes and scabies and is the treatment of choice for onchocerciasis (river blindness). It is typically given as one or two oral doses. Ivermectin therapy has been associated with minor, self-limiting serum aminotransferase elevations and very rare instances of clinically apparent liver injury.|A mixture of mostly avermectin H2B1a (RN 71827-03-7) with some avermectin H2B1b (RN 70209-81-3), which are macrolides from STREPTOMYCES avermitilis. It binds glutamate-gated chloride channel to cause increased permeability and hyperpolarization of nerve and muscle cells. It also interacts with other CHLORIDE CHANNELS. It is a broad spectrum antiparasitic that is active against microfilariae of ONCHOCERCA VOLVULUS but not the adult form.

Ivermectin Basic Attributes

Molecular Weight：

875.09300

Exact Mass：

874.50800

EC Number：

274-536-0

DSSTox ID：

DTXSID7040235

ATC Code：

D - Dermatologicals|P - Antiparasitic products, insecticides and repellents

HScode：

2932999099

Characteristics

PSA：

170.06000

XLogP3：

5.60140

Appearance：

white to off-white solid

Water Solubility：

H2O: ≤1.0% KF

Storage Conditions：

2-8ºC

Toxicity：

LD50 in dogs, rhesus monkeys (mg/kg): about 80, more than 24 orally. (MSDS Merck & Co. Inc., 2003)

Safety Information

Packing level：

Hazard category：

6.1(a)

Transport codes：

UN 2811 6.1/PG 2

wgk germany：

hazard class code：

R61; R25; R36; R36/38; R22

safety instructions：

53-26-45-36

Marks：

Precautionary statement(s)：

Missing Phrase - N15.00950417

Hazard Statements：

H300

GHS Classification：

|Danger|H300 (99.4%): Fatal if swallowed [Danger Acute toxicity, oral]|P201, P202, P260, P264, P270, P273, P280, P281, P301+P310, P302+P352, P307+P311, P308+P313, P312, P314, P321, P322, P330, P361, P363, P391, P405, and P501|Aggregated GHS information provided by 334 companies from 21 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Hepatotoxicity：

Single dose therapy with ivermectin has been associated with a low rate of serum aminotransferase elevations. A single case of clinically apparent liver injury has been reported after ivermectin use (Case 1). The onset of injury occurred 1 month after a single dose and was characterized by a hepatocellular pattern of serum enzyme elevations without jaundice. Recovery was rapid and complete. In trials of ivermectin to prevent SARS-CoV-2 infection and to ameliorate the course of early as well as severe COVID-19, serum aminotransferase elevations were not uncommon but were no more frequent among patients receiving ivermectin than among those receiving placebo or a comparator drug.

Drug Information

Drug Indication：

Treatment of rosacea

LiverTox Summary：

Drug Classes：

Anthelmintic Agents

MeSH：

Drugs used to treat or prevent parasitic infections. (See all compounds classified as Antiparasitic Agents.)|Pesticides designed to control insects that are harmful to man. The insects may be directly harmful, as those acting as disease vectors, or indirectly harmful, as destroyers of crops, food products, or textile fabrics. (See all compounds classified as Insecticides.)

MeSH Entry Terms：

Eqvalan

Ivermectin Use and Manufacturing

Uses

1. Beta-lactamase inhibitor; antibiotic
2. Antiparasitic
3. Positive allosteric modulator of 伪7 neuronal nicotinic acetylcholine receptor; also modulates glutamate-GABA-activated chloride channels.
4. Semi-synthetic derivative of Abamectin; consists of a mixture of not less than 80% component B1a and not more than 20% component B1b. Antihelmintic (Onchocerca)

Use Classification：

Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Animal Drugs -> FDA Approved Animal Drug Products (Green Book) -> Active Ingredients|Veterinary Drug -> ANTHELMINTHIC_AGENT; -> JECFA Functional Classes

Food Additive Classes：

Veterinary Drug -> ANTHELMINTHIC_AGENT;

Computed Properties

Molecular Weight:875.1
XLogP3:4.1
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:14
Rotatable Bond Count:8
Exact Mass:874.50785703
Monoisotopic Mass:874.50785703
Topological Polar Surface Area:170
Heavy Atom Count:62
Complexity:1680
Undefined Atom Stereocenter Count:20
Undefined Bond Stereocenter Count:3
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Material

Triphenylphosphine

Price Analysis

Make your Ivermectin purchase based on the price and market insights! ECHEMI provides professional market insights with prices for you to make a better choice. Learn more on Ivermectin prices .

Drug Function and Efficacy

Ivermectin is a derivative of avermectin and is an oral semi-synthetic broad-spectrum antiparasitic drug. It selectively binds with high affinity to the glutamate-gated chloride ion channels in invertebrate nerve cells and muscle cells, increasing the permeability of cell membranes to chloride ions, causing hyperpolarization of nerve cells or muscle cells, and paralyzing or killing parasites. It is effective against most nematodes (but not all nematodes) in each life cycle; it is effective against microfilariae of Onchocerca volvulus, but not against adults; it is also effective against fecal strongyles that are only in the intestine.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Ivermectin chewable tablets
Ingredients	Chemical name: The main components of this product are ivermectin B1a and ivermectin B1b. The chemical name of ivermectin B1a is 5-O-demethyl-22,23-dihydroavermectin A1a, and the chemical name of ivermectin B1b is 5-O-demethyl-25-de(1-methylpropyl)-22,23-dihydro-25-(1-methylethyl)avermectin A1a. Chemical structure: Ivermectin B1aR=-C2H5Molecular formula: C48H74O14Molecular weight: 875.10Ivermectin B1bR=-CH3Molecular formula: C47H72O14Molecular weight: 861.07
Indication	There is currently a lack of detailed research data.
Specifications	3mg
Manufacturer	Zhejiang Hisun Pharmaceutical Co., Ltd.

Ivermectin Tablets
Ingredients	The main ingredients of this product are ivermectin B1a and ivermectin B1b.
Indication	Not yet clear.
Specifications	6mg
Manufacturer	Zhejiang Hisun Pharmaceutical Co., Ltd.

Ivermectin Capsules
Ingredients	The main ingredients of this product are ivermectin B1a and ivermectin B1b. The chemical name of ivermectin B1a is (5-O-demethyl-22,23-dihydroavermectin A1a); the chemical name of ivermectin B1b is (5-O-demethyl-25-de(1-methylpropyl)-22,23-dihydro-avermectin A1a).
Indication	Not yet clear.
Specifications	3mg
Manufacturer	Zhejiang Hisun Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

HOVIONE PHARMASCIENCE LTD

United States
Active
Zhejiang Hisun Pharmaceutical Co., Ltd.

China
Active
Hovione PharmaScience Limited

Japan
Active

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