Pyrantel

594.685

206.31

239-774-1

4QIH0N49E7

DTXSID5023538

Crystals from methanol|Yellow, crystalline solid

P - Antiparasitic products, insecticides and repellents

2934999090

43.8

6.26020

1.13±0.1 g/cm3(Predicted)

178-179 °C

324.4±44.0 °C(Predicted)

150ºC

Insoluble in water, slightly soluble in dimethylformamide, and soluble in dimethyl sulfoxide.

Odorless

Tasteless

143 Ų [M+H]+ [CCS Type: TW]

DECOMP SLOWLY IN LIGHT; RELATIVELY STABLE IN HEAT. /PAMOATE/

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

Mild adverse effects include nausea, vomiting, diarrhea, headache, and dizziness. LD50 in rats is 535 mg/kg. Reported effects in humans in case of overdose include gastrointestinal disturbance, central nervous system effects, and superficial skin reactions. In one study, serum aspartate aminotransferase (AST) and serum alanine-aminotransferase (ALT) values were increased in approximately 2% of patients. Pyrantel should be used with caution in patients with severe malnutrition or anemia. Supportive therapy is recommended for anemic, dehydrated, or malnourished patients before administration of the drug. Pyrantel pamoate has been placed in pregnancy category C. This refers to the fact that animal studies have revealed adverse effects on the fetus (teratogenic/embryocidal, or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus.Data on the use of pyrantel pamoate in pregnant women are quite limited. In mass treatment programs for which the World Health Organization (WHO) has observed that the benefits of treatment outweigh the risks, WHO allows the use of pyrantel pamoate in the 2nd and 3rd trimesters of pregnancy, due to the fact that the effects of pyrantel on birth outcome are uncertain. The risk of treatment in pregnant women already known to have an infection needs to be balanced with the risk of disease progression if treatment were to be omitted. Individuals with liver disease are more susceptible to the toxicity in cases of pyrantel overexposure,. There are no data regarding the presence of pyrantel in breast milk. Pyrantel is poorly absorbed from the GI tract; therefore, excretion into breast milk may be minimal. Some experts recommend that a single dose of pyrantel therapy may be given to breastfeeding women.

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.

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

For the treatment of enterobiasis including roundworm (ascariasis), pinworm (enterobius) and hookworm (strongyloides) and hookworm (ancylostoma) in the pyrantel pamoate form. Pyrantel is available in various formulations for humans, dogs, and cats as the pamoate (US Pharmacopeia nomenclature) or embonate (European Pharmacopoeia nomenclature) salt, which contains 34.7% pyrantel base combined with pamoic acid.,. Pyrantel pamoate (embonate) ingested orally is effective for removal and control of ascarid and hookworm infections in puppies and dogs (adult Toxocara canis, Toxascaris leonina, Ancylostoma tubaeforme, An. braziliense, Uncinaria stenocephala), cats (adult Toxocara cati, Toxa. leonina, An. caninum, An. braziliense, U. stenocephala), horses and ponies (adult and immature Parascaris equorum, adult Strongylus vulgaris, S. edentatus, S. equinus, Cyathostomes (Triodontophorus spp., Cyathostomum spp., Cylicodontophorus spp., Cylicocyclus spp., Cylicostephanus spp., Poteriostomum spp.), Oxyuris equi, Anoplocephala perfoliata), swine (adult Ascaris suum, Oesophagostomum dentatum), and humans (adult A. lumbricoides, Enterobius vermicularis, An. duodenale, Necator americanus).

Pyrantel is a nonabsorbed anthelmintic agent with activity against intestinal nematodes such as pinworms and roundworms. Pyrantel therapy has not been reported to cause serum aminotransferase elevations or clinically apparent liver injury.

Anthelmintic Agents

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.

... 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.

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,.

Substances used in the treatment or control of nematode infestations. They are used also in veterinary practice. (See all compounds classified as Antinematodal Agents.)|Drugs that interrupt transmission at the skeletal neuromuscular junction by causing sustained depolarization of the motor end plate. These agents are primarily used as adjuvants in surgical anesthesia to cause skeletal muscle relaxation. (See all compounds classified as Neuromuscular Depolarizing Agents.)

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/

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.

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

By promoting the release of acetylcholine, inhibiting cholinesterase, and stimulating ganglionic neurons, pyrantel serves as a depolarizing neuromuscular blocking agent in helminths. This causes extensive depolarization of the helminth muscle membrane, resulting in tension to the helminth's muscles, leading to paralysis and release of their attachment to the host organism intestinal walls. This action is unlike piperazine, which is a hyperpolarizing neuromuscular blocking agent that causes relaxation of the helminth muscles, leading to a subsequent detachment from the intestinal wall. Excretion of the parasites in the feces occurs by normal peristalsis.|PYRANTEL & ITS ANALOGS ARE DEPOLARIZING NEUROMUSCULAR BLOCKING AGENTS. THEY INDUCE MARKED, PERSISTENT ACTIVATION OF NICOTINIC RECEPTORS, WHICH RESULTS IN SPASTIC PARALYSIS OF THE WORM. PYRANTEL ALSO INHIBITS CHOLINESTERASES. /PYRANTEL PAMOATE AND ANALOGS/|PYRANTEL ... CAUSES A SLOWLY DEVELOPING CONTRACTURE OF PREPARATIONS OF ASCARIS AT 1% OF THE CONCENTRATION OF ACETYLCHOLINE REQUIRED TO PRODUCE THE SAME EFFECT. IN SINGLE MUSCLE CELLS OF THIS HELMINTH, PYRANTEL CAUSES DEPOLARIZATION & INCREASED SPIKE-DISCHARGE FREQUENCY, ACCOMPANIED BY INCREASE IN TENSION.

Pyrantel

CP-10,423-18; Banmith; Strongid /Tartrate/|Pyrantel Embonate; CP-10423-16; Antiminth; Cobantril; Combantrin; Early Bird; Helmex; Helmintox; Piranver /Pamoate/|PYRANTEL PAMOATE, USP ... IS SUPPLIED AS AN OFFICIAL ORAL SUSPENSION: EACH MILLILITER CONTAINS 50 MG OF THE BASE. /PAMOATE/

VET: THE US NOW PERMITS ITS USE IN SWINE, BUT LIMITS ITS RESIDUES IN THEIR EDIBLE TISSUES @ 10 PPM FOR LIVER & KIDNEY, & 1 PPM IN MUSCLE. THIS IS ACCOMPLISHED BY WITHHOLDING ANY TREATED FEEDS FOR @ LEAST 24 HR BEFORE SLAUGHTERING. /TARTRATE/

SPECTROPHOTOMETRIC DETERMINATION IN FEEDS. /TARTRATE/

Pharmaceuticals -> Animal Drugs -> Approved in Taiwan