The anti-A antibodies displayed by Pyrantel (10 nM-10 µM; 72 hours) were good. suum and anti-N (0-168.2 M; 72 h). Activities of American Nus [1][2].

In hamsters with Vibrio ceylonali infections, pyrantel (10 mg/kg; po; single dose) can reduce the worm load by 87.2% and achieve a deworming rate of 63.4% [2].

Cell viability assay [2]
Cell Types: Nepenthes americana
Tested Concentrations: 0-168.2 M (0-100 µg/mL)
Incubation Duration: 72 hrs (hours)
Experimental Results: Inhibitory effect on third-stage larvae and adults of Nepenthes americana, IC50 The values are 2.0 and 7.6 mg/ml respectively.

Animal/Disease Models: Male Syrian golden hamster (3 weeks old; A. ceylanicum infection) [2].
Doses: 10 mg/kg
Route of Administration: Oral; single.
Experimental Results: The worm load reduction rate and deworming rate were 87.2% and 63.4% respectively.

Absorption, Distribution and Excretion
Pyrantel is poorly absorbed from the GI tract of humans,. Peak serum concentrations occur 1–3 hours after a single dose.
Approximately 50% of an oral dose is excreted unchanged in feces; 7% excreted in urine as unchanged drug and metabolites.
... POORLY ABSORBED FROM GI TRACT ... LESS THAN 15% IS EXCRETED IN THE URINE AS PARENT DRUG & METABOLITES. THE MAJOR PROPORTION OF AN ADMINISTERED DOSE IS RECOVERED IN FECES. /PYRANTEL PAMOATE/
THOUGH ALMOST COMPLETELY INSOL, THE PAMOATE SALT IS ABSORBED SLIGHTLY; 1% OF UNCHANGED & 3% OF METABOLIZED DRUG APPEAR IN THE URINE. /PAMOATE/

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Metabolism / Metabolites
Pyrantel is administered orally. The poor solubility of the pamoate salt offers the advantage of reduced absorption from the gastrointestinal tract and allows the drug to reach and act against parasites in the large intestine. Metabolism of pyrantel is rapid. The absorbed drug is partly metabolized in the liver.

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Biological Half-Life
In pigs, following intravenous administration, pyrantel exhibited a half-life of 1.75 +/- 0.19 h.

Hepatotoxicity
Pyrantel therapy has not been clearly associated with elevations in serum aminotransferase levels nor has its use been linked to cases of clinically apparent liver injury.
Likelihood score: E (unlikely cause of clinically apparent liver injury).

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Interactions
THE EFFECTS OF PYRANTEL ARE BLOCKED BY PREVIOUS EXPOSURE OF ASCARIS MUSCLE TO PIPERAZINE. /PAMOATE/

[1]. Oxantel is an N-type (methyridine and nicotine) agonist not an L-type (levamisole and pyrantel) agonist: classification of cholinergic anthelmintics in Ascaris. Int J Parasitol. 2004 Aug;34(9):1083-90.

[2]. In vitro and in vivo efficacy of Monepantel (AAD 1566) against laboratory models of human intestinal nematode infections. PLoS Negl Trop Dis. 2011 Dec;5(12):e1457.

Therapeutic Uses
Antinematodal Agents; Neuromuscular Depolarizing Agents
Pyrantel pamoate is an alternative ... in the treatment of ascariasis and enterobiasis. High cure rates have been achieved after a single oral dose ... Similarly, high cure rates have been obtained against Ancylostoma, N. americanus, and Trichostrongylus.
IT IS RECOMMENDED...AS AN ALTERNATE DRUG IN TREATMENT OF ROUNDWORM INFECTIONS & IS UNDER INVESTIGATION FOR USE IN TRICHOSTRONGYLUS SPECIES INFECTIONS. /PAMOATE/
THREE CONSECUTIVE DAILY DOSES ARE GENERALLY MORE EFFECTIVE IN HOOKWORM INFECTIONS. THIS DRUG IS ESSENTIALLY INEFFECIVE AGAINST WHIPWORMS. /PAMOATE/
For more Therapeutic Uses (Complete) data for PYRANTEL (10 total), please visit the HSDB record page.

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Drug Warnings
... HAS NOT BEEN STUDIED IN PREGNANT WOMEN. THUS, ITS USE IN PREGNANT PATIENTS AND CHILDREN LESS THAN 2 YEARS OF AGE IS NOT RECOMMENDED. BECAUSE PYRANTEL PAMOATE & PIPERAZINE ARE MUTUALLY ANTAGONISTIC WITH RESPECT TO THEIR NEUROMUSCULAR EFFECTS ON PARASITES, THE TWO SHOULD NOT BE USED TOGETHER. /PYRANTEL PAMOATE/
VET: CAUSES NEUROMUSCULAR BLOCK IN IN VITRO & IN IN VIVO TRIALS. ...STRONG CHOLINESTERASE INHIBITOR & MAY CAUSE HYPERTENSION... USE WITH CAUTION IN WEAK OR DEBILITATED ANIMALS. /TARTRATE/
Adverse effects of pyrantel pamoate are usually mild, infrequent, and transient, disappearing when the drug is discontinued. The most common adverse effects are GI disturbances, including nausea, vomiting, tenesmus, anorexia, diarrhea, abdominal cramps, and gastralgia. Adverse GI effects may be related to expulsion of the helminths. Other less frequent adverse effects of pyrantel include headache, dizziness, drowsiness, insomnia, rash, fever, and weakness. minimal, transient increases in serum concentrations of AST (SGOT) have been reported in a small number of patients receiving the drug. Although ototoxicity, optic neuritis, and hallucinations with confusion and paresthesia have been reported rarely, evidence of a causal relationship to the drug is lacking. /Pyrantel pamoate/
Patients should be advised to contact a physician if abdominal cramps, nausea, vomiting, diarrhea, headache, or dizziness, which may be associated with pyrantel pamoate use, persists or becomes bothersome. Patients undertaking self-medication of enterobiasis with the drug should be advised to contact a physician if worms other than pinworms are present before or after therapy with the drug or if symptoms of enterobiasis persist. /Pyrantel pamoate/
For more Drug Warnings (Complete) data for PYRANTEL (7 total), please visit the HSDB record page.

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Pharmacodynamics
It has similar properties to both competitive and depolarizing neuromuscular blocking agents, which leads to the understanding of the paralytic effect of the drug has on parasites, ultimately resulting in the death of the parasite,.

C11H14N2S

206.30726

594.182

15686-83-6

Pyrantel pamoate;22204-24-6;Pyrantel tartrate;33401-94-4

708857

Crystals from methanol
Yellow, crystalline solid

1.13g/cm3

324.4ºC at 760mmHg

178-179ºC

150ºC

2.13E-17mmHg at 25°C

6.26

0

2

2

14

248

0

CN1CCCN=C1/C=C/C2=CC=CS2

YSAUAVHXTIETRK-AATRIKPKSA-N

InChI=1S/C11H14N2S/c1-13-8-3-7-12-11(13)6-5-10-4-2-9-14-10/h2,4-6,9H,3,7-8H2,1H3/b6-5+

1-methyl-2-[(E)-2-thiophen-2-ylethenyl]-5,6-dihydro-4H-pyrimidine

Pyrantel Pyrequan Pyrantelum Strongid Pirantele Pin-X

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)