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NEO-PENOTRAN PESSARY

Product Information

Registration Status: Active

SIN11180P

NEO-PENOTRAN PESSARY is approved to be sold in Singapore with effective from 1999-07-10. It is marketed by INTEGA PTE LTD, with the registration number of SIN11180P.

This product contains Metronidazole 500mg, and Miconazole 100mg in the form of SUPPOSITORY. It is approved for VAGINAL use.

This product is manufactured by EMBIL PHARMACEUTICAL CO LTD in TURKEY.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Product Reference
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Description

A nitroimidazole used to treat amebiasis; vaginitis; trichomonas infections; giardiasis; anaerobic bacteria; and treponemal infections. It has also been proposed as a radiation sensitizer for hypoxic cells. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985, p133), this substance may reasonably be anticipated to be a carcinogen (Merck, 11th ed).

Indication

For the treatment of anaerobic infections and mixed infections, surgical prophylaxis requiring anaerobic coverage, Clostridium difficile-associated diarrhea and colitis, Helicobacter pylori infection and duodenal ulcer disease, bacterial vaginosis, Giardia lamblia gastro-enteritis, amebiasis caused by Entamoeba histolytica, acne rosacea (topical treatment), and Trichomonas infections.

Mechanism of Action

Metronidazole is a prodrug. Unionized metronidazole is selective for anaerobic bacteria due to their ability to intracellularly reduce metronidazole to its active form. This reduced metronidazole then covalently binds to DNA, disrupt its helical structure, inhibiting bacterial nucleic acid synthesis and resulting in bacterial cell death.

Pharmacokinetics

Absorption
Well absorbed (at least 80%) with peak plasma concentrations achieved in 1-3 hours following oral administration of therapeutic doses of immediate release formulation.
Distribution
Metabolism
Hepatic metabolism by hydroxylation, oxidation, and glucuronidation.
Elimination

Toxicity

LD50=500 mg/kg/day (orally in rat). Adverse effects include reversible peripheral neuropathy with prolonged therapy, CNS toxicity, disulfiram effect with alcohol, dark red-brown urine, metallic taste, nausea, epigastric distress, dizziness, vertigo and paresthesias associated with high doses, and neutropenia (reversible and mild).

Active Ingredient/Synonyms

1-(2-hydroxy-1-ethyl)-2-methyl-5-nitroimidazole | 1-(2-hydroxyethyl)-2-methyl-5-nitroimidazole | 1-(beta-Ethylol)-2-methyl-5-nitro-3-azapyrrole | 1-(beta-Hydroxyethyl)-2-methyl-5-nitroimidazole | 1-(beta-Oxyethyl)-2-methyl-5-nitroimidazole | 1-(β-ethylol)-2-methyl-5-nitro-3-azapyrrole | 1-(β-hydroxyethyl)-2-methyl-5-nitroimidazole | 1-(β-oxyethyl)-2-methyl-5-nitroimidazole | 2-methyl-1-(2-hydroxyethyl)-5-nitroimidazole | 2-methyl-3-(2-hydroxyethyl)-4-nitroimidazole | 2-methyl-5-nitroimidazole-1-ethanol | Metronidazol | Metronidazolum | Metronidazole |


Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.


Description

An imidazole antifungal agent that is used topically and by intravenous infusion. [PubChem]

Indication

For topical application in the treatment of tinea pedis (athlete’s foot), tinea cruris, and tinea corporis caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum, in the treatment of cutaneous candidiasis (moniliasis), and in the treatment of tinea versicolor.

Mechanism of Action

Miconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Miconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

Toxicity

Oral, mouse: LD50 = 3800 mg/kg; Oral, rat: LD50 = 3 gm/kg. Ingestion of the amounts of the components contained in a tube of cream are unlikely to produce overdosage and toxic effects.

Active Ingredient/Synonyms

1-(2,4-Dichloro-beta-((2,4-dichlorobenzyl)oxy)phenethyl)imidazole | 1-[2-(2,4-Dichloro-benzyloxy)-2-(2,4-dichloro-phenyl)-ethyl]-1H-imidazole | Daktarin iv | Miconazole | Monistat iv (tn) | Miconazole |


Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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