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• 145 Huguenot Street, New Rochelle, NY 10801 • A Nonprofi t Publication IN THIS ISSUE starts on next page In Brief: Testosterone and Cardiovascular Risk ...p 17 Riociguat Adempas for Pu

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The Medical Letter®

On Drugs and Therapeutics Published by The Medical Letter, Inc • 145 Huguenot Street, New Rochelle, NY 10801 • A Nonprofi t Publication

IN THIS ISSUE (starts on next page)

In Brief: Testosterone and Cardiovascular Risk p 17

Riociguat (Adempas) for Pulmonary Hypertension p 17

Low-Dose Diclofenac (Zorvolex) for Pain p 19

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The Medical Letter®

On Drugs and Therapeutics Published by The Medical Letter, Inc • 145 Huguenot Street, New Rochelle, NY 10801 • A Nonprofi t Publication

FORWARDING OR COPYING IS A VIOLATION OF U.S AND INTERNATIONAL COPYRIGHT LAWS 17

ALSO IN THIS ISSUE

Low-Dose Diclofenac (Zorvolex)

for Pain p 19

IN BRIEF

Testosterone and Cardiovascular Risk

Prompted by the recent publication of 2 retrospective

stud-ies, the FDA has announced that it is investigating the risk

of stroke, heart attack, and death in men taking

FDA-ap-proved testosterone products.1

The fi rst study examined the records of 8709 men with

low testosterone levels (<300 ng/dL) who underwent

coronary angiography between 2005 and 2011; 1223 of

these men started testosterone therapy after a median

of 531 days following coronary angiography Three years

after coronary angiography, the Kaplan-Meier estimated

cumulative percentages of men who died or had a

myo-cardial infarction (MI) or ischemic stroke were 26% of

those treated with testosterone and 20% of those who

were not treated with the hormone, a hazard ratio of 1.29

(95% CI 1.04-1.58; P=0.02).2

The second study compared the rate of nonfatal MI

dur-ing the 90 days after fi lldur-ing a prescription with the rate

in the prior year in 56,000 men given a prescription for

testosterone and in 167,000 given a phosphodiesterase

type 5 inhibitor (sildenafi l [Viagra] or tadalafi l [Cialis]) In

the testosterone group as a whole, the

post/pre-prescrip-tion rate ratio was 1.36, but in men >65 years old it was

2.19 and in younger men with a history of heart disease

it was 2.90 In men who received a prescription for

silde-nafi l or tadalafi l, the rate ratio was 1.08 for all ages, 1.15

for those >65 years old, and 1.40 for younger men with a

history of heart disease.3

A recent meta-analysis of randomized, placebo-controlled

trials of testosterone therapy also found an increased risk of

cardiovascular-related events in men treated with the

hor-mone (odds ratio [OR] 1.54; 95% CI 1.09-2.18); an analysis

by funding source found that the risk was greater in trials not

funded by the pharmaceutical industry (OR 2.06 vs 0.89).4

1 FDA Drug Safety Communication January 31, 2014: FDA evalu-ating risk of stroke, heart attack and death with FDA-approved testosterone products Available at www.fda.gov/drugs/drugsafe-ty/ucm383904.htm Accessed February 24, 2014.

2 R Vigen et al Association of testosterone therapy with mortality, myocardial infarction, and stroke in men with low testosterone levels JAMA 2013; 310:1829.

3 WD Finkle et al Increased risk of non-fatal myocardial infarction following testosterone therapy prescription in men PLoS One 2014; 9:e85805.

4 L Xu et al Testosterone therapy and cardiovascular events among men: a systematic review and meta-analysis of placebo-controlled randomized trials BMC Med 2013; 11:108.

The FDA has approved the sGC stimulator riociguat

(rye” oh sig’ ue at; Adempas – Bayer) for oral

treat-ment of pulmonary arterial hypertension (PAH) and chronic thromboembolic pulmonary hypertension (CTEPH) following surgery or when surgery is not an option It is the fi rst drug to be approved for treatment

of CTEPH

Riociguat (Adempas) for Pulmonary

Hypertension

Table 1 Pharmacology

Drug class Soluble guanylate cyclase (sGC) stimulator Route Oral

Formulation 0.5, 1, 1.5, 2, 2.5 mg tablets Tmax 1.5 hrs Metabolism Primarily by CYP1A1, 3A, 2C8 and 2J2 Elimination Feces (53%); urine (40%)

Elimination half-life 12 hrs (patients), 7 hrs (healthy subjects)

DRUGS FOR PAH — Current management of PAH

usually includes warfarin (Coumadin, and others) and furosemide (Lasix, and generics) Oral drugs approved

for PAH include the phosphodiesterase type 5 (PDE5)

inhibitors sildenafi l (Revatio, and generics) and tadalafi l (Adcirca), the endothelin receptor antagonists bosen-tan (Tracleer), ambrisenbosen-tan (Letairis), and, most

recent-ly, macitentan (Opsumit), a nonselective endothelin

re-ceptor antagonist derived from bosentan.1 Patients with more advanced disease can be treated with a systemic prostacyclin (see Table 2)

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18 The Medical Letter • Volume 56 • Issue 1437 • March 3, 2014

Table 2 Some Drugs for Pulmonary Arterial Hypertension

Soluble Guanylate Cyclase (sGC) Stimulator

Riociguat – Adempas (Bayer) Oral 0.5, 1, 1.5, 2, 2.5 mg tabs 1-2.5 mg tid $7500.00

Endothelin Receptor Antagonists

Nonselective

Macitentan – Opsumit (Actelion) Oral 10 mg tabs 10 mg once/day 6840.00

Bosentan – Tracleer Oral 62.5, 125 mg tabs 62.5 mg bid (for 4 wks) 7050.00 (Actelion) then 125 mg bid

Selective

Ambrisentan – Letairis (Gilead) Oral 5, 10 mg tabs 5-10 mg once/day 6893.30

Phosphodiesterase 5 (PDE5) Inhibitors

S ildenafi l – generic Oral 20 mg tabs 20 mg tid 239.40

Revatio2

Tadalafi l – Adcirca (Eli Lilly) Oral 20 mg tabs 40 mg once/day 1899.00

Prostacyclins

Iloprost – Ventavis (Actelion) Inhalation 10 and 20 mcg ampules 2.5-5 mcg/inhalation 6-9 times/day 15,210.00 3

Epoprostenol – generic Continuous IV 0.5 and 1.5 mg in 17 mL 20-40 ng/kg/min 4

1145.54 5

Flolan (Gilead) infusion single-use vials 1850.74 5

Veletri (Actelion) 0.5 and 1.5 mg in 10 mL 1849.92 5

single-use vials Treprostinil 6 –

Remodulin (United Therapeutics) Continuous SC or IV 1, 2.5, 5, 10 mg/mL 40-160 ng/kg/min 7 7132.95 5

infusion multi-dose vials

Tyvaso (United Therapeutics) Inhalation 1.74 mg/2.9 mL ampules 8

9 breaths (54 mcg) qid 13,018.00 9

1 Approximate wholesale acquisition cost (WAC) for 30 days’ treatment at the lowest usual dosage Source: Analy$ource® Monthly (Selected from FDB MedKnowledge™) February 5, 2014 Reprinted with permission by FDB, Inc All rights reserved ©2014 www.fdbhealth.com/policies/drug-pricing-policy Actual retail prices may be higher Ancillary costs will substantially increase the cost of non-oral drugs.

2 Also available in an IV formulation for patients on oral sildenafi l who are temporarily unable to take oral medication Also approved in a powder for oral suspension.

3 Cost of 180 ampules of either strength.

4 Initial dosage recommended is 2 ng/kg/min with subsequent increases of 2 ng/kg/min every 15 minutes or longer as tolerated Dosage requirements tend to increase over time Average dosage after 6 months is about 20-40 ng/kg/min

5 Cost for a 70-kg patient

6 The FDA recently approved an extended-release oral formulation of treprostinil (Orenitram) that will be available soon.

7 Initial dosage recommended is 1.25 ng/kg/min, or half if poorly tolerated, with subsequent increases of 1.25 ng/kg/min weekly for the fi rst 4 weeks, then 2.5 ng/kg/min weekly thereafter Average dosage after 9 months is about 60 ng/kg/min

8 Initial dosage is 3 breaths (18 mcg) 4 times daily, or 1-2 breaths if poorly tolerated then increasing to 3 breaths The dosage should be increased by an additional 3 breaths

at 1-2 week intervals as tolerated The target and maximum dosage is 9 breaths (54 mcg) 4 times daily.

9 Cost of 7 foil pouches containing 4 ampules each.

TREATMENT OF CTEPH — In CTEPH, residual

thromboemboli obstruct pulmonary arteries, leading to

an increase in pulmonary vascular resistance and

sub-sequently to progressive pulmonary hypertension and

right heart failure The treatment of choice is

pulmo-nary endarterectomy, which can be curative but is not

an option in many patients because of distal occlusion

or comorbidities About 10% of patients who undergo

surgery continue to experience pulmonary

hyperten-sion.2 Drugs for PAH have been used off-label to treat

patients with CTEPH.3

MECHANISM OF ACTION — Riociguat is a soluble

guanylate cyclase (sGC) stimulator sGC binds to

nitric oxide (NO), forming an enzyme that promotes

synthesis of the signaling molecule cyclic guanosine

monophosphate (cGMP) Pulmonary hypertension

is associated with impaired synthesis of NO and

in-suffi cient stimulation of the NO-sGC-cGMP pathway

Riociguat acts both by directly stimulating sGC

inde-pendently of NO, and by increasing the sensitivity of sGC to NO

CLINICAL STUDIES — PAH – In a 12-week,

double-blind trial (PATENT-1), 443 patients with symptomatic PAH were randomized to individually adjusted dos-ages of riociguat capped at either 1.5 or 2.5 mg 3 times daily, or to placebo.4 At the end of the study, the mean 6-minute walk distance was longer by 31 meters in the 1.5-mg group and by 30 meters in the 2.5-mg group, compared to a decrease of 6 meters in the placebo group Time to clinical worsening, a sec-ondary endpoint, was also longer in patients treated with riociguat

CTEPH – A 16-week, double-blind trial (CHEST-1) in

261 patients with inoperable CTEPH or persistent or re-current pulmonary hypertension despite surgery found that riociguat titrated to a maximum of 2.5 mg 3 times daily increased 6-minute walk distance by 39 meters, compared to a decrease of 6 meters with placebo.5

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19 The Medical Letter • Volume 56 • Issue 1437 • March 3, 2014

Low-Dose Diclofenac (Zorvolex) for Pain

The FDA has approved Zorvolex (Iroko), a low-dose

oral formulation of the relatively COX-2 selective NSAID diclofenac, for treatment of mild-to-moderate acute pain

in adults

Zorvolex is available as 18- and 35-mg capsules

Oth-er oral formulations of diclofenac include immediate-release, extended-immediate-release, and enteric-coated tablets and capsules in strengths ranging from 25 to 100 mg Diclofenac is also available topically as a transdermal

patch (Flector), a gel (Voltaren Gel), and a solution (Pennsaid).

THE NEW FORMULATION — Each capsule of Zorvolex

contains diclofenac as submicron particles The reduction

in particle size increases surface area, leading to faster dissolution and absorption of the drug A single-dose crossover study compared the new 35-mg formulation

of diclofenac to diclofenac potassium 50 mg in healthy subjects Taken without food, Tmax was about 1 hour for both formulations; Cmax and AUC were about 26% and 23% lower, respectively, with the new formulation Taking

Zorvolex with food delayed its Tmax by 2.32 hours and

reduced its Cmax by 60% and its AUC by 11%

CLINICAL STUDIES — Approval of Zorvolex was

based on the results of a double-blind clinical trial in

428 patients with moderate-to-severe pain following bunionectomy Patients were randomized to diclofenac

18 mg or 35 mg 3 times daily, celecoxib 200 mg twice daily after a 400-mg loading dose, or placebo At 12 hours, pain intensity with diclofenac 18 and 35 mg was reduced from baseline by 48% and 51%, respectively, compared to 24% with placebo At 24 hours, pain in-tensity was reduced by 69% and 73% versus 52% All

of these differences from placebo were statistically sig-nifi cant Compared with celecoxib, overall reductions in pain intensity were greater with diclofenac 35 mg and similar with diclofenac 18 mg.1

Extension Trials – In long-term extensions of both

tri-als (PATENT-2 and CHEST-2), treatment was unblinded

after 8 weeks Exploratory analyses at 12 weeks found

that patients taking riociguat increased their 6-minute

walk distance from the original baseline by 53 meters in

PATENT-2 and by 63 meters in CHEST-2.4,5

ADVERSE EFFECTS — Adverse effects of riociguat

(>5%) that occurred more frequently than with placebo

in clinical trials were headache, dyspepsia/gastritis,

dizziness, nausea, diarrhea, hypotension, vomiting,

anemia, gastroesophageal refl ux, and constipation

Hypotension occurred in 10% of patients taking

rio-ciguat compared to 4% of those taking placebo

Seri-ous hemorrhagic events, including one fatal case,

oc-curred in 2.4% of patients treated with the drug and in

none with placebo

PREGNANCY — Riociguat is contraindicated for use

during pregnancy (category X) It is available for women

only through a restricted access program

DRUG INTERACTIONS — Because of the risk of

hy-potension, riociguat is contraindicated for use with

ni-trates, nitric oxide donors (such as amyl nitrite), PDE5

inhibitors (such as sildenafi l) and nonspecifi c PDE

in-hibitors (such as dipyridamole or theophylline)

Concomitant use of riociguat with strong CYP and

P-glycoprotein/breast cancer resistance protein (P-gp/

BCRP) inhibitors (such as ketoconazole, itraconazole,

and ritonavir) can increase riociguat serum

concentra-tions and the risk of hypotension

Plasma concentrations of riociguat are reduced by

50-60% in smokers compared to nonsmokers Antacids

such as aluminum hydroxide/magnesium hydroxide

re-duce absorption of riociguat

DOSAGE AND ADMINISTRATION — The

recom-mended starting dosage of riociguat is 1 mg 3 times

daily The dose can be increased by 0.5 mg every 2

weeks up to the maximum of 2.5 mg 3 times daily

In patients who cannot tolerate the drug’s hypotensive

effects, or in those taking concomitant strong CYP and

P-gp/BCRP inhibitors, the starting dosage can be

low-ered to 0.5 mg 3 times daily Riociguat dosages higher

than 2.5 mg 3 times daily may be considered for

pa-tients who smoke Dosage reductions may be

neces-sary for patients who stop smoking Antacids should not

be taken within 1 hour of taking riociguat

CONCLUSION — Riociguat (Adempas) can improve

exercise capacity in patients with pulmonary arterial

hypertension (PAH) and in those with chronic thrombo-embolic pulmonary hypertension (CTEPH) □

1 Macitentan (Opsumit) for pulmonary arterial hypertension Med Lett Drugs Ther 2014; 56:15.

2 J Pepke-Zaba et al Chronic thromboembolic pulmonary hyperten-sion (CTEPH): results from an international prospective registry Circulation 2011; 124:1973.

3 M Delcroix Chronic post-embolic pulmonary hypertension: a new target for medical therapies? Eur Respir Rev 2013; 22:258

4 HA Ghofrani et al Riociguat for the treatment of pulmonary arterial hypertension N Engl J Med 2013; 369:330.

5 HA Ghofrani et al Riociguat for the treatment of chronic thrombo-embolic pulmonary hypertension N Engl J Med 2013; 369:319.

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On Drugs and Therapeutics

EDITOR IN CHIEF: Mark Abramowicz, M.D

EXECUTIVE EDITOR: Gianna Zuccotti, M.D., M.P.H., F.A.C.P., Harvard Medical School EDITOR: Jean-Marie Pfl omm, Pharm.D

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Corinne Z Morrison, Pharm.D., Michael P Viscusi, Pharm.D.

CONSULTING EDITORS: Brinda M Shah, Pharm.D., F Peter Swanson, M.D CONTRIBUTING EDITORS:

Carl W Bazil, M.D., Ph.D., Columbia University College of Physicians and Surgeons Vanessa K Dalton, M.D., M.P.H., University of Michigan Medical School Eric J Epstein, M.D., Albert Einstein College of Medicine

Jane P Gagliardi, M.D., M.H.S., F.A.C.P Duke University School of Medicine Jules Hirsch, M.D., Rockefeller University

David N Juurlink, BPhm, M.D., Ph.D., Sunnybrook Health Sciences Centre Richard B Kim, M.D., University of Western Ontario

Hans Meinertz, M.D., University Hospital, Copenhagen Sandip K Mukherjee, M.D., F.A.C.C., Yale School of Medicine Dan M Roden, M.D., Vanderbilt University School of Medicine Esperance A.K Schaefer, M.D., M.P.H., Harvard Medical School

F Estelle R Simons, M.D., University of Manitoba Neal H Steigbigel, M.D., New York University School of Medicine Arthur M F Yee, M.D., Ph.D., F.A.C.R., Weill Medical College of Cornell University SENIOR ASSOCIATE EDITOR: Amy Faucard

MANAGING EDITOR: Susie Wong ASSISTANT MANAGING EDITOR: Liz Donohue PRODUCTION COORDINATOR: Cheryl Brown EXECUTIVE DIRECTOR OF SALES: Gene Carbona FULFILLMENT & SYSTEMS MANAGER: Cristine Romatowski DIRECTOR OF MARKETING COMMUNICATIONS: Joanne F Valentino VICE PRESIDENT AND PUBLISHER: Yosef Wissner-Levy

Founded in 1959 by Arthur Kallet and Harold Aaron, M.D.

Copyright and Disclaimer: The Medical Letter is an independent nonprofi t organization that provides health care professionals with unbiased drug prescribing recommendations The edi-torial process used for its publications relies on a review of published and unpublished litera-ture, with an emphasis on controlled clinical trials, and on the opinions of its consultants The Medical Letter is supported solely by subscription fees and accepts no advertising, grants, or donations No part of the material may be reproduced or transmitted by any process in whole

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Copyright 2014 ISSN 1523-2859

The Medical Letter • Volume 56 • Issue 1437 • March 3, 2014

Coming Soon in The Medical Letter:

Golimumab (Simponi) for Ulcerative Colitis

Drugs for Gout

Tobramycin Inhalation (Bethkis) for Cystic Fibrosis

Coming Soon in Treatment Guidelines:

Drugs for Peptic Ulcer Disease and GERD Drugs for Hypertension

In a randomized, double-blind trial in 305 patients with

osteoarthritis, diclofenac 35 mg three times daily for 12

weeks was signifi cantly more effective than placebo

in relieving pain; twice-daily administration of the drug

was not signifi cantly better than placebo.2

ADVERSE EFFECTS — NSAIDs frequently cause

small increases in aminotransferase activity; serious

hepatotoxicity is rare, but may occur more frequently

with diclofenac An increased risk of serious

cardio-vascular events has been reported with some NSAIDs;

the risk appeared to be highest with diclofenac.3 In the

12-week osteoarthritis trial, no serious gastrointestinal,

cardiovascular, or renal adverse events were reported

with diclofenac 35 mg 3 times daily.4

DRUG INTERACTIONS — Diclofenac is metabolized

primarily by CYP2C9; co-administration with CYP2C9

inhibitors (such as fl uconazole) may increase its serum

concentrations and toxicity.5 Like other NSAIDs,

diclof-enac may decrease the effectiveness of diuretics, beta

blockers, ACE inhibitors and some other

antihyperten-sive drugs, may increase the toxicity of lithium,

metho-trexate, and cyclosporine, and may increase the risk of

gastrointestinal bleeding in patients taking warfarin

DOSAGE, ADMINISTRATION, AND COST — The

rec-ommended dosage of Zorvolex is 18 mg or 35 mg three

times daily It can be taken with or without food, but its

effectiveness may be reduced when taken with food A

single Zorvolex capsule of either strength costs $2.50,

compared to about $0.70 for one 50-mg tablet of

ge-neric diclofenac potassium.6

CONCLUSION — NSAIDs can cause serious adverse

effects and should be used in the lowest effective dosage

Zorvolex, a new low-dose oral formulation of diclofenac,

is more effective than placebo in relieving acute pain

How it compares in effi cacy or safety to oral

immediate-release diclofenac potassium, which is available

generi-cally, or to any other traditional NSAID, is unknown □

1 A Gibofsky et al Lower-dose diclofenac submicron particle capsules

provide early and sustained acute patient pain relief in a phase 3

study Postgrad Med 2013; 125:130.

2 A Gibofsky et al A phase 3 study of lower-dose diclofenac submicron

particle capsules demonstrates effective pain relief in patients with

os-teoarthritis Osteoarthritis Cartilage 2013; 21(4) suppl:S267 Abs 518.

3 Drugs for pain Treat Guidel Med Lett 2013; 11:31.

4 C Young and MC Hochberg Safety of lower-dose diclofenac

sub-micron particle capsules dosed up to 12 weeks in patients with

os-teoarthritis Arthritis Rheum 2013; 65(10) suppl:S915 Abs 2149.

5 Inhibitors and inducers of CYP enzymes and P-glycoprotein Med

Lett Drugs Ther 2013; 55:e44.

6 Approximate wholesale acquisition cost (WAC) Source: Analy$ource

Monthly (Selected from FDB MedKnowledge ™ ) February 5, 2014

Re-printed with permission by FDB, Inc All rights reserved © 2014

www.fdb-health.com/policies/drug-pricing-policy Actual retail prices may be higher.

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Issue 1437 Questions

(Correspond to questions #25-30 in Comprehensive Exam #70, available July 2014)

Riociguat (Adempas) for Pulmonary Hypertension

1 Which of the following are used to manage PAH?

c sildenafi l

d all of the above

2 Riociguat taken for 12 weeks increased the 6-minute walk distance from baseline by about:

3 In clinical trials, 10% of patients treated with riociguat experienced:

Low-Dose Diclofenac (Zorvolex) for Pain

4 Compared to diclofenac potassium 50 mg, the AUC and Cmax of Zorvolex

35 mg were about:

5 A 56-year-old woman with mild osteoarthritis of the knee treated fairly

successfully with acetaminophen has seen advertisements for Zorvolex and

asks if she could try it instead She has had atrial fi brillation for 10 years, for which she takes warfarin and a beta blocker You could tell her that:

a Zorvolex may be less convenient than acetaminophen because

taking it with food could decrease its effectiveness

b diclofenac could increase the risk of gastrointestinal bleeding in

patients taking warfarin

c diclofenac could decrease the effectiveness of the beta blocker

d all of the above

6 Compared to other NSAIDs, diclofenac is more likely to cause:

a gastric ulcer

b renal toxicity

c serious hepatotoxicity

d all of the above

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attention to clinical trials, pathophysiology, dosage and administration, drug metabolism and interactions, and patient management Activity participants will make independent and informed therapeutic choices in their practice Upon completion of this program, the participant will be able to:

1 Review the effi cacy and safety of riociquat (Adempas) for treatment of pulmonary arterial hypertension.

2 Review the effi cacy and safety of a new lower-dose formulation of diclofenac (Zorvolex) for treatment of pain.

Privacy and Confi dentiality: The Medical Letter guarantees our fi rm commitment to your privacy We do not sell any

of your information Secure server software (SSL) is used for commerce transactions through VeriSign, Inc No credit card information is stored.

IT Requirements: Windows 98/NT/2000/XP/Vista/7/8, Pentium+ processor, Mac OS X+ w/compatible processor;

Microsoft IE 6.0+, Mozilla Firefox 2.0+ or any other compatible Web browser Dial-up/high-speed connection.

Have any questions? Call us at 800-211-2769 or 914-235-0500 or e-mail us at: custserv@medicalletter.org

Continuing Medical Education Program

medicalletter.org/cme

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