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205, Al Qaizi Building, Al Muteena Street, Deira , AE
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61ada6f34f2f65c992cd3f60 ADEMPAS 2.5 MG 42 TAB. https://cdn1.storehippo.com/s/6052eead9e1cf8aa024c48c8/61ada6ec497f215d492d3559/webp/adempas-2-5-mg-42-tab-.jpg

What is Adempas and how is it used?

Adempas (riociguat) is a soluble guanylate cyclase stimulator used to treat adults with two forms of pulmonary hypertension.

What are side effects of Adempas?

Common side effects of Adempas include:

DESCRIPTION

Adempas (riociguat) is a tablet for oral administration. Riociguat is methyl 4,6-diamino-2-[1-(2-fluorobenzyl)-1Hpyrazolo [3,4-b]pyridin-3-yl]-5-pyrimidinyl(methyl)carbamate with the following structural formula:

ADEMPAS (riociguat) Structural Formula Illustration

C20H19FN8O2

Riociguat is a white to yellowish, crystalline, non-hygroscopic substance with a molecular weight of 422.42 g/mol. In solid form it is stable to temperature, light, and humidity.

The solubility at 25°C in water: 4 mg/L, in ethanol: 800 mg/L, in 0.1 HCl (pH 1): 250 mg/L and in buffer (phosphate) pH 7: 3 mg/L. In the pH range of 2 to 4 the solubility showed strong pH-dependency. Solubility increases at lower pH values.

Each round film-coated tablet contains 0.5 mg (1.0, 1.5, 2.0, 2.5 mg) riociguat. The inactive ingredients are cellulose microcrystalline, crospovidone, hypromellose 5cP, lactose monohydrate, magnesium stearate, sodium laurylsulfate, hydroxypropylcellulose, hypromellose 3cP, propylene glycol, and titanium dioxide. Adempas 1, 1.5, 2, and 2.5 mg tablets contain, in addition, ferric oxide yellow. Adempas 2 and 2.5 mg tablets contain, in addition, ferric oxide red.

Drug Description

What is Adempas and how is it used?

Adempas (riociguat) is a soluble guanylate cyclase stimulator used to treat adults with two forms of pulmonary hypertension.

What are side effects of Adempas?

Common side effects of Adempas include:

WARNING

EMBRYO-FETAL TOXICITY

Do not administer Adempas to a pregnant female because it may cause fetal harm [see CONTRAINDICATIONS, WARNINGS AND PRECAUTIONS and Use In Specific Populations].

Females of reproductive potential: Exclude pregnancy before the start of treatment, monthly during treatment, and 1 month after stopping treatment. To prevent pregnancy, females of reproductive potential must use effective forms of contraception during treatment and for one month after stopping treatment [see DOSAGE AND ADMINISTRATION, WARNINGS AND PRECAUTIONS,and Use In Specific Populations].

For all female patients, Adempas is available only through a restricted program called the Adempas Risk Evaluation and Mitigation Strategy (REMS) Program [see WARNINGS AND PRECAUTIONS].

Indications

INDICATIONS

Chronic-Thromboembolic Pulmonary Hypertension

Adempas is indicated for the treatment of adults with persistent/recurrent chronic thromboembolic pulmonary hypertension (CTEPH), (WHO Group 4) after surgical treatment, or inoperable CTEPH, to improve exercise capacity and WHO functional class [see Clinical Studies].

Pulmonary Arterial Hypertension

Adempas is indicated for the treatment of adults with pulmonary arterial hypertension (PAH), (WHO Group 1), to improve exercise capacity, WHO functional class and to delay clinical worsening.

Efficacy was shown in patients on Adempas monotherapy or in combination with endothelin receptor antagonists or prostanoids. Studies establishing effectiveness included predominately patients with WHO functional class II–III and etiologies of idiopathic or heritable PAH (61%) or PAH associated with connective tissue diseases (25%) [see Clinical Studies].

Dosage

DOSAGE AND ADMINISTRATION

Recommended Dosage In Adult Patients

The recommended starting dosage is 1 mg taken 3 times a day. For patients who may not tolerate the hypotensive effect of Adempas, consider a starting dose of 0.5 mg taken three times a day. If systolic blood pressure remains greater than 95 mmHg and the patient has no signs or symptoms of hypotension, up-titrate the dose by 0.5 mg taken three times a day. Dose increases should be no sooner than 2 weeks apart. The dose can be increased to the highest tolerated dosage, up to a maximum of 2.5 mg taken three times a day. If at any time, the patient has symptoms of hypotension, decrease the dosage by 0.5 mg taken three times a day.

Crushed Tablets

For patients who are unable to swallow whole tablets, Adempas may be crushed and mixed with water or soft foods (such as applesauce) immediately before administration [see CLINICAL PHARMACOLOGY].

Dosage Interruption

If a dose is missed, advise patients to continue with the next regularly scheduled dose.

In case Adempas is interrupted for 3 days or more, re-titrate Adempas.

Pregnancy Testing In Females Of Reproductive Potential

Obtain pregnancy tests prior to start of treatment and monthly during treatment [see Use In Specific Populations].

Use In Patients Who Smoke

Consider titrating to dosages higher than 2.5 mg three times a day, if tolerated, in patients who smoke. A dose decrease may be required in patients who stop smoking [see DRUG INTERACTIONS and CLINICAL PHARMACOLOGY].

Strong CYP And P-Gp/BCRP Inhibitors

Consider a starting dose of 0.5 mg, three times a day when initiating Adempas in patients receiving strong cytochrome P450 (CYP) and P-glycoprotein/breast cancer resistance protein (P-gp/BCRP) inhibitors such as azole antimycotics (for example, ketoconazole, itraconazole) or HIV protease inhibitors (for example, ritonavir). Monitor for signs and symptoms of hypotension on initiation and on treatment with strong CYP and P-gp/BCRP inhibitors [see WARNINGS AND PRECAUTIONSDRUG INTERACTIONS and CLINICAL PHARMACOLOGY].

Transitioning To And From Adempas

  • Discontinue sildenafil at least 24 hours prior to administering Adempas [see CONTRAINDICATIONS and DRUG INTERACTIONS].
  • Discontinue tadalafil at least 48 hours prior to administering Adempas [see CONTRAINDICATIONS and DRUG INTERACTIONS]. Consider initiating Adempas at a starting dose of 0.5 mg in patients at risk of hypotension [see Recommended Dosage In Adult Patients]. Monitor for signs and symptoms of hypotension on initiation.
  • Discontinue Adempas at least 24 hours prior to administering a PDE5-inhibitor [see Recommended Dosage In Adult PatientsCONTRAINDICATIONS, and DRUG INTERACTIONS ]. Monitor for signs and symptoms of hypotension on initiation.

HOW SUPPLIED

Dosage Forms And Strengths

Tablets: film-coated, round, bi-convex:

  • 0.5 mg, white, with “BAYER” cross on one side and “0.5” and “R” on the other side
  • 1 mg, pale-yellow, with “BAYER” cross on one side and “1” and “R” on the other side
  • 1.5 mg, yellow-orange, with “BAYER” cross on one side and “1.5” and “R” on the other side
  • 2 mg, pale orange, with “BAYER” cross on one side and “2” and “R” on the other side
  • 2.5 mg, red-orange, with “BAYER” cross on one side and “2.5” and “R” on the other side

Storage And Handling

Adempas (riociguat) tablets are film-coated, round, and debossed with the “Bayer cross” on one side.

  Color Debossing Side 2 NDC 50419-xxx-xx
  Bottle of 9 Bottle of 90 Blister of 42
0.5 mg White 0.5 R 250-91 250-01 250-03
1 mg Pale yellow 1 R 251-91 251-01 251-03
1.5 mg Yellow-orange 1.5 R 252-91 252-01 252-03
2 mg Pale orange 2 R 253-91 253-01 253-03
2.5 mg Red-orange 2.5 R 254-91 254-01 254-03

Store at 25°C (77°F); excursions are permitted from 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

Manufacturer: n/a. Revised: Jan 2018

The following serious adverse reactions are discussed elsewhere in the labeling:

DRUG INTERACTIONS

Pharmacodynamic Interactions With Adempas

Nitrates

Co-administration of Adempas with nitrates or nitric oxide donors (such as amyl nitrite) in any form is contraindicated because of hypotension [see CONTRAINDICATIONS and CLINICAL PHARMACOLOGY].

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. Do not administer within 24 hours of sildenafil. Do not administer 24 hours before or within 48 hours after tadalafil [see DOSAGE AND ADMINISTRATION]. Clinical experience with co-administration of Adempas and other phosphodiesterase inhibitors (for example, milrinone, cilostazole, roflumilast) is limited.

Pharmacokinetic Interactions With Adempas

Smoking

Plasma concentrations in smokers are reduced by 50% to 60% compared to nonsmokers. Based on pharmacokinetic modeling, for patients who are smokers, doses higher than 2.5 mg three times a day may be considered in order to match exposure seen in nonsmoking patients. Safety and effectiveness of Adempas doses higher than 2.5 mg three times a day have not been established. A dose reduction should be considered in patients who stop smoking [see DOSAGE AND ADMINISTRATION and CLINICAL PHARMACOLOGY].

Strong CYP And P-Gp/BCRP Inhibitors

Concomitant use of riociguat with strong cytochrome CYP inhibitors and Pgp/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 3 times a day when initiating Adempas in patients receiving strong CYP and P-gp/BCRP inhibitors. 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 [see DOSAGE AND ADMINISTRATION, WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY].

Strong CYP3A Inducers

Strong inducers of CYP3A (for example, 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 [see CLINICAL PHARMACOLOGY].

Antacids

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

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ADEMPAS 2.5 MG 42 TAB.

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Description of product

What is Adempas and how is it used?

Adempas (riociguat) is a soluble guanylate cyclase stimulator used to treat adults with two forms of pulmonary hypertension.

What are side effects of Adempas?

Common side effects of Adempas include:

DESCRIPTION

Adempas (riociguat) is a tablet for oral administration. Riociguat is methyl 4,6-diamino-2-[1-(2-fluorobenzyl)-1Hpyrazolo [3,4-b]pyridin-3-yl]-5-pyrimidinyl(methyl)carbamate with the following structural formula:

ADEMPAS (riociguat) Structural Formula Illustration

C20H19FN8O2

Riociguat is a white to yellowish, crystalline, non-hygroscopic substance with a molecular weight of 422.42 g/mol. In solid form it is stable to temperature, light, and humidity.

The solubility at 25°C in water: 4 mg/L, in ethanol: 800 mg/L, in 0.1 HCl (pH 1): 250 mg/L and in buffer (phosphate) pH 7: 3 mg/L. In the pH range of 2 to 4 the solubility showed strong pH-dependency. Solubility increases at lower pH values.

Each round film-coated tablet contains 0.5 mg (1.0, 1.5, 2.0, 2.5 mg) riociguat. The inactive ingredients are cellulose microcrystalline, crospovidone, hypromellose 5cP, lactose monohydrate, magnesium stearate, sodium laurylsulfate, hydroxypropylcellulose, hypromellose 3cP, propylene glycol, and titanium dioxide. Adempas 1, 1.5, 2, and 2.5 mg tablets contain, in addition, ferric oxide yellow. Adempas 2 and 2.5 mg tablets contain, in addition, ferric oxide red.

Drug Description

What is Adempas and how is it used?

Adempas (riociguat) is a soluble guanylate cyclase stimulator used to treat adults with two forms of pulmonary hypertension.

What are side effects of Adempas?

Common side effects of Adempas include:

WARNING

EMBRYO-FETAL TOXICITY

Do not administer Adempas to a pregnant female because it may cause fetal harm [see CONTRAINDICATIONS, WARNINGS AND PRECAUTIONS and Use In Specific Populations].

Females of reproductive potential: Exclude pregnancy before the start of treatment, monthly during treatment, and 1 month after stopping treatment. To prevent pregnancy, females of reproductive potential must use effective forms of contraception during treatment and for one month after stopping treatment [see DOSAGE AND ADMINISTRATION, WARNINGS AND PRECAUTIONS,and Use In Specific Populations].

For all female patients, Adempas is available only through a restricted program called the Adempas Risk Evaluation and Mitigation Strategy (REMS) Program [see WARNINGS AND PRECAUTIONS].

Indications

INDICATIONS

Chronic-Thromboembolic Pulmonary Hypertension

Adempas is indicated for the treatment of adults with persistent/recurrent chronic thromboembolic pulmonary hypertension (CTEPH), (WHO Group 4) after surgical treatment, or inoperable CTEPH, to improve exercise capacity and WHO functional class [see Clinical Studies].

Pulmonary Arterial Hypertension

Adempas is indicated for the treatment of adults with pulmonary arterial hypertension (PAH), (WHO Group 1), to improve exercise capacity, WHO functional class and to delay clinical worsening.

Efficacy was shown in patients on Adempas monotherapy or in combination with endothelin receptor antagonists or prostanoids. Studies establishing effectiveness included predominately patients with WHO functional class II–III and etiologies of idiopathic or heritable PAH (61%) or PAH associated with connective tissue diseases (25%) [see Clinical Studies].

Dosage

DOSAGE AND ADMINISTRATION

Recommended Dosage In Adult Patients

The recommended starting dosage is 1 mg taken 3 times a day. For patients who may not tolerate the hypotensive effect of Adempas, consider a starting dose of 0.5 mg taken three times a day. If systolic blood pressure remains greater than 95 mmHg and the patient has no signs or symptoms of hypotension, up-titrate the dose by 0.5 mg taken three times a day. Dose increases should be no sooner than 2 weeks apart. The dose can be increased to the highest tolerated dosage, up to a maximum of 2.5 mg taken three times a day. If at any time, the patient has symptoms of hypotension, decrease the dosage by 0.5 mg taken three times a day.

Crushed Tablets

For patients who are unable to swallow whole tablets, Adempas may be crushed and mixed with water or soft foods (such as applesauce) immediately before administration [see CLINICAL PHARMACOLOGY].

Dosage Interruption

If a dose is missed, advise patients to continue with the next regularly scheduled dose.

In case Adempas is interrupted for 3 days or more, re-titrate Adempas.

Pregnancy Testing In Females Of Reproductive Potential

Obtain pregnancy tests prior to start of treatment and monthly during treatment [see Use In Specific Populations].

Use In Patients Who Smoke

Consider titrating to dosages higher than 2.5 mg three times a day, if tolerated, in patients who smoke. A dose decrease may be required in patients who stop smoking [see DRUG INTERACTIONS and CLINICAL PHARMACOLOGY].

Strong CYP And P-Gp/BCRP Inhibitors

Consider a starting dose of 0.5 mg, three times a day when initiating Adempas in patients receiving strong cytochrome P450 (CYP) and P-glycoprotein/breast cancer resistance protein (P-gp/BCRP) inhibitors such as azole antimycotics (for example, ketoconazole, itraconazole) or HIV protease inhibitors (for example, ritonavir). Monitor for signs and symptoms of hypotension on initiation and on treatment with strong CYP and P-gp/BCRP inhibitors [see WARNINGS AND PRECAUTIONSDRUG INTERACTIONS and CLINICAL PHARMACOLOGY].

Transitioning To And From Adempas

  • Discontinue sildenafil at least 24 hours prior to administering Adempas [see CONTRAINDICATIONS and DRUG INTERACTIONS].
  • Discontinue tadalafil at least 48 hours prior to administering Adempas [see CONTRAINDICATIONS and DRUG INTERACTIONS]. Consider initiating Adempas at a starting dose of 0.5 mg in patients at risk of hypotension [see Recommended Dosage In Adult Patients]. Monitor for signs and symptoms of hypotension on initiation.
  • Discontinue Adempas at least 24 hours prior to administering a PDE5-inhibitor [see Recommended Dosage In Adult PatientsCONTRAINDICATIONS, and DRUG INTERACTIONS ]. Monitor for signs and symptoms of hypotension on initiation.

HOW SUPPLIED

Dosage Forms And Strengths

Tablets: film-coated, round, bi-convex:

  • 0.5 mg, white, with “BAYER” cross on one side and “0.5” and “R” on the other side
  • 1 mg, pale-yellow, with “BAYER” cross on one side and “1” and “R” on the other side
  • 1.5 mg, yellow-orange, with “BAYER” cross on one side and “1.5” and “R” on the other side
  • 2 mg, pale orange, with “BAYER” cross on one side and “2” and “R” on the other side
  • 2.5 mg, red-orange, with “BAYER” cross on one side and “2.5” and “R” on the other side

Storage And Handling

Adempas (riociguat) tablets are film-coated, round, and debossed with the “Bayer cross” on one side.

  Color Debossing Side 2 NDC 50419-xxx-xx
  Bottle of 9 Bottle of 90 Blister of 42
0.5 mg White 0.5 R 250-91 250-01 250-03
1 mg Pale yellow 1 R 251-91 251-01 251-03
1.5 mg Yellow-orange 1.5 R 252-91 252-01 252-03
2 mg Pale orange 2 R 253-91 253-01 253-03
2.5 mg Red-orange 2.5 R 254-91 254-01 254-03

Store at 25°C (77°F); excursions are permitted from 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

Manufacturer: n/a. Revised: Jan 2018

The following serious adverse reactions are discussed elsewhere in the labeling:

DRUG INTERACTIONS

Pharmacodynamic Interactions With Adempas

Nitrates

Co-administration of Adempas with nitrates or nitric oxide donors (such as amyl nitrite) in any form is contraindicated because of hypotension [see CONTRAINDICATIONS and CLINICAL PHARMACOLOGY].

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. Do not administer within 24 hours of sildenafil. Do not administer 24 hours before or within 48 hours after tadalafil [see DOSAGE AND ADMINISTRATION]. Clinical experience with co-administration of Adempas and other phosphodiesterase inhibitors (for example, milrinone, cilostazole, roflumilast) is limited.

Pharmacokinetic Interactions With Adempas

Smoking

Plasma concentrations in smokers are reduced by 50% to 60% compared to nonsmokers. Based on pharmacokinetic modeling, for patients who are smokers, doses higher than 2.5 mg three times a day may be considered in order to match exposure seen in nonsmoking patients. Safety and effectiveness of Adempas doses higher than 2.5 mg three times a day have not been established. A dose reduction should be considered in patients who stop smoking [see DOSAGE AND ADMINISTRATION and CLINICAL PHARMACOLOGY].

Strong CYP And P-Gp/BCRP Inhibitors

Concomitant use of riociguat with strong cytochrome CYP inhibitors and Pgp/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 3 times a day when initiating Adempas in patients receiving strong CYP and P-gp/BCRP inhibitors. 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 [see DOSAGE AND ADMINISTRATION, WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY].

Strong CYP3A Inducers

Strong inducers of CYP3A (for example, 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 [see CLINICAL PHARMACOLOGY].

Antacids

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

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