PHARMACODYNAMIC INTERACTIONS1

Nitrate
NITRATES

Co-administration of Adempas with nitrates or nitric oxide donors
(such as amyl nitrite) in any form is contraindicated because of hypotension.

PDE
PDE INHIBITORS

Co-administration of Adempas with specific PDE-5 inhibitors (such as sildenafil, tadalafil, or vardenafil) and nonspecific PDE inhibitors (such as dipyridamole or theophylline) is contraindicated because of hypotension. Clinical experience with co-administration of Adempas and other phosphodiesterase inhibitors (such as milrinone, cilostazole, roflumilast) is limited.

To transition patients to and from a PDE-5 inhibitor to Adempas,
follow the timing information in the Dosing and Administration Guide.

PDE-5=phosphodiesterase type 5

Pharmacokinetic interactions considerations1

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If your patient is a smoker
  • Plasma concentrations in smokers are reduced by 50% to 60% compared to nonsmokers
  • Doses higher than 2.5 mg 3x a day may be considered to match exposure seen in nonsmoking patients
  • A dose reduction should be considered in patients who stop smoking
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IF YOUR PATIENT TAKES STRONG CYP AND P-gp/BCRP INHIBITORS

Concomitant use of riociguat with strong cytochrome CYP inhibitors and P-gp/BCRP inhibitors such as azole antimycotics (for example, ketoconazole, itraconazole) or HIV protease inhibitors (such as ritonavir) increase riociguat exposure and may result in hypotension.

  • Consider a starting dose of 0.5 mg 3x a day when initiating Adempas in patients
  • Monitor for signs and symptoms of hypotension on initiation and on treatment with strong CYP and P-gp/BCRP inhibitors
  • A dose reduction should be considered in patients who may not tolerate the hypotensive effect of riociguat

CYP=cytochrome P450; P-gp/BCRP=P-glycoprotein/breast cancer resistance protein

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IF YOUR PATIENT TAKES STRONG CYP3A INDUCERS

Strong inducers of CYP3A (such as rifampin, phenytoin, carbamazepine, phenobarbital, or St. John's Wort) may significantly reduce riociguat exposure. Data are not available to guide dosing of riociguat when strong CYP3A inducers are co-administered.

CYP3A=cytochrome P450, family 3, subfamily A

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IF YOUR PATIENTS TAKE ANTACIDS

Antacids such as aluminum hydroxide/magnesium hydroxide decrease riociguat absorption and should not be taken within 1 hour of taking Adempas.

Enrollment

Help your patients manage possible side effects.

Download the patient guide here.

MORE IMPORTANT SAFETY INFORMATION LESS IMPORTANT SAFETY INFORMATION
References:
  1. Adempas Prescribing Information. Whippany, NJ. Bayer Pharmaceuticals Inc., 2018.

Managing Adempas