2. Rivaroxaban
• Brand name: Xarelto, Zarlan
• Active ingredient: Rivaroxaban
• FDA approval date: 7/1/2011
• Dosage forms: Tablets
-----References: uptodate.com, drugs.com, FDA website.
3. Indications
• Rivaroxaban is used to treat or prevent blood
clots as in venous thromboembolism VTE.
• Rivaroxaban is sometimes used to lower your
risk of a blood clot coming back after you have
received treatment for blood clots for at least
6 months.
4. Mechanism of action
• Rivaroxaban is a selective inhibitor of factor Xa. Rivaroxaban
inhibits free Xa, and prothrombin converging to thrombin
activity.
• Rivaroxaban has no direct effect on platelet aggregation, but
indirectly inhibits it by inhibiting Xa, rivaroxaban decreases
thrombin generation.
5. Administration :
- 2.5 mg or 10 mg tablets: May take with or
without food
- 15 mg or 20 mg tablets: Take with food
6. Origin :
- Rivaroxaban was initially developed by Bayer
pharma ( German company ) . In the United
States, it is marketed by Janssen
Pharmaceutical (a part of Johnson & Johnson).
It was the first available direct factor Xa
inhibitor which is taken by mouth.
10. Pregnancy category :
• Limited available data in pregnant women are
insufficient to inform a drug-associated risk of
adverse developmental outcomes
• Use with caution in pregnant patients because
of the potential for pregnancy related
hemorrhage and/or emergent delivery;
anticoagulant effect cannot be reliably
monitored with standard laboratory testing
11. Doses
The duration of therapy and dose selection should be
individualized after careful assessment of the treatment
benefit against the risk.
* If a dose is missed, the patient should take rivaroxaban
immediately to ensure intake of 30 mg per day. ** If an only
dose/ day was missed, the patient should take rivaroxaban
immediately. The dose should not be doubled within the same
day.
Time period Dosing schedule
Treatment and
prevention of recurrent
DVT and PE
Day 1 - 21 15 mg twice daily*
Day 22 onwards 20 mg once daily**
Prevention of recurrent
DVT and PE
Following completion of
at least 6 months therapy
for DVT or PE
10 mg once daily or
20 mg once daily
12. Doses (cont.)
• The dose for children and adolescent is
calculated based on body weight. In case of 30
to 50 kg child a once daily dose of 15 mg is
recommended.
• Where as with body weight of 50 kg or more a
once daily dose of 20 mg is recommended.
13. Renal/Hepatic dosage
adjustments
• Renal impairment
o Adults and children:
Use is not recommended in patients with severe renal
impairment.
When the recommended dose is 10 mg once daily for
mild and moderate renal impairment, no dose
adjustment is necessary.
• Hepatic impairment
Rivaroxaban is contraindicated in patients with hepatic
disease including cirrhotic patients.
No clinical data is available in children with hepatic
impairment.
14. Drug-Drug & Drug-Food
interactions
• Interaction with other medicinal products
Such as ketoconazole, posaconazole or HIV
protease inhibitors. These active substances are
strong inhibitors of both CYP3A4.
Care is taken if patients are treated with
(NSAIDs), acetylsalicylic acid, or selective
serotonin reuptake inhibitors (SSRIs).
• There is no food interactions with rivaroxaban.
Therefore, no dietary changes is taken into
considerations.
15. Warnings/Precautions
• Hemorrhagic risk is increased with aging
• Renal impairment
• Patients with cancer
Cancer patients have higher risk of bleeding and
thrombosis.
• Patients with prosthetic valves
• Dermatological reactions
Patients appear to be at highest risk for these
reactions early in the course of therapy.
Therapy with rivaroxaban should be designed to
achieve more benefits than the risks in general.
