Acute Porphyria Drug Database

Monograph

J05AJ01 - Raltegravir
Propably not porphyrinogenic
PNP

Rationale
Raltegravir does not inhibit or induce CYP enzymes. Side effects such as nausea, vomiting and diarrhoea may be potentially porphyrinogenic through reduction in carbohydrate intake.
Therapeutic characteristics
Raltegravir is indicated in combination with other anti-retroviral medicinial products for the treatment of human immunodeficiency virus (HIV-1) infection in adults. Common reported side effects that can be confused with an acute porphyria attack are abdominal pain, diarrhoea, nausea and vomiting. Other common side effects are insomnia.
Metabolism and pharmacokinetics
In vitro and in vivo studies have shown that raltregravir is mainly metabolised via a UGT1A1 mediated glucuronidation pathway (SPC, Zhang 2010). The elimination half-life is 9 hours. In vitro-studies indicates that raltegravir is not a substrate of CYP450 enzymes. It does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 nor does it induce CYP3A4 (SPC). An in vivo study has shown that raltegravir does not affect the plasma level of midazolam, a sensitive probe CYP3A4 substrate. This indicates that it does not induce or inhibit CYP3A4 (Iwamoto 2008).
Similar drugs
Explore alternative drugs in similar therapeutic classes J05A / J05AJ or go back.

References

# Citation details PMID
*Scientific articles
1. Drug interactions evaluation: an integrated part of risk assessment of therapeutics.
Zhang L, Reynolds KS, et al. Toxicol Appl Pharmacol. 2010 Mar 1;243(2):134-45.
20045016
*Summary of Product Characteristics
2. Norwegian medicines agency. Summary of Product Characteristics (SPC). Raltegravir.
3. The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Raltegravir. Last edition: February 2013.

Tradenames
This list comprises raw data collected from different countries. In some cases, a more comprehensive list of available drug packages is included. Consequently, very similar terms may therefore appear multiple times. Bold names are the searchable terms, while the gray names that follow are all mapped to the bolded term.
Note: The cleaning is done automatically by a proprietary algorithm, and it may produce errors. We strive to improve it continuously.


Isentress 100 mg kauwtabletten · Isentress 100 mg, granulaat voor orale suspensie · Isentress 25 mg kauwtabletten · Isentress 400 mg filmomhulde tablet · Isentress 600 mg, filmomhulde tablet Isentress · Isentress 100 mg compr. ? croquer · Isentress 100 mg susp. buv. (gran.) sachet · Isentress 25 mg compr. ? croquer · Isentress 400 mg compr. pellic. · Isentress 600 mg compr. pellic. Isentress 100 mg Comprimidos Masticables · Isentress 25 mg Comprimidos Masticables · Isentress 400 mg Comprimidos Recubiertos con Pelicula · Isentress 600 mg Comprimidos Recubiertos con Pelicula · Raltegravir dr. Reddys 600 mg Comprimidos Recubiertos con Pelicula efg ISENTRESS 400 mg · ISENTRESS 600 mg Isentress · Raltegravir Isentress Isentress Isentress Isentress Isentress · Raltegravir Day Zero · Raltegravir Zentiva Isentress Isentress Isentress®
 
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