Ritonavir

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Structural formula
Ritonavir.svg
General
Non-proprietary name Ritonavir
Molecular formula C 37 H 48 N 6 O 5 S 2
External identifiers / databases
CAS number 155213-67-5
EC number 605-001-5
ECHA InfoCard 100.125.710
PubChem 392622
ChemSpider 347980
DrugBank DB00503
Wikidata Q422618
Drug information
ATC code

J05 AE03

Drug class

Protease inhibitor

Mechanism of action

Inhibition of HIV protease

properties
Molar mass 721.0 g mol −1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling
no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Ritonavir (RTV) is a drug from the group of HIV protease inhibitors and is used to treat HIV infections and AIDS . In the course of what is known as highly active antiretroviral therapy (HAART = highly active antiretroviral therapy ), it is combined with other active ingredients ( nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs)) to increase their effectiveness.

history

Ritonavir was developed by Abbott Laboratories and approved by the US FDA in March 1996 . It was one of the first antiretroviral drugs in this class. The combination of the two protease inhibitors lopinavir and ritonavir was approved under the trade name Kaletra . Ritonavir is also part of the combination therapy Viekirax ® of AbbVie for the treatment of hepatitis C .

A combination of lopinavir and ritonavir is being tested in clinical trials against COVID-19 .

Mechanism of action

With this structure, ritonavir is able to inhibit the body's own liver enzyme cytochrome P450 CYP3A4 , which is able to convert protease inhibitors into ineffective metabolites . This makes it possible to use less protease inhibitors. However, the inhibition of CYP3A4 is problematic in that it also affects the metabolism of numerous other drugs and makes them difficult to dose.

Side effects and contraindications

Nausea, diarrhea; As a result of the inhibition of liver metabolism, there are numerous interactions with other drugs ( steroid hormones , antihistamines , calcium antagonists , tricyclic antidepressants , neuroleptics , antimycotics , opioids ). An increase in transaminases can also be observed. Other interactions have far more dangerous consequences. Several deaths have been published after taking ritonavir and amphetamines or MDMA / ecstasy or the narcotic 4-hydroxybutanoic acid (“liquid ecstasy”), which is often used as a recreational drug (Henry 1998, Harrington 1999, Hales 2000). Ritonavir in particular inhibits the metabolism of amphetamines (speed) or MDMA (ecstasy), ketamines or LSD (review in: Antoniou 2002).

Trade names

Monopreparations : Norvir (D, A, CH)

Combination preparations : Combination with lopinavir : Kaletra (D, A, CH)

Individual evidence

  1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
  2. ↑ Anja Martini, Christian Drosten : Coronavirus Update. (PDF) Episode 22. In: ndr.de. Norddeutscher Rundfunk, March 26, 2020, p. 4 f. , accessed on March 27, 2020 .

Web links