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New Drugs of 2007 Part 1 . Presented by: Sara Tebbe, PharmD Drugs Covered: aliskiren (Tekturna ® ) ambrisentan (Letairis TM ) amlodipine/olmesartan (Azor ® ) eculizumab (Soliris ® ) lidocaine (Zingo TM ). Aliskiren. Tekturna ®.

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new drugs of 2007 part 1

New Drugs of 2007Part 1

Presented by: Sara Tebbe, PharmD

Drugs Covered: aliskiren (Tekturna®)

ambrisentan (LetairisTM)

amlodipine/olmesartan (Azor®)

eculizumab (Soliris®)

lidocaine (ZingoTM)

aliskiren

Aliskiren

Tekturna®

Manufactured by: Novartis

www.prescribingreference.com

aliskiren tekturna
Aliskiren (Tekturna®)

Therapeutic Class

  • Antihypertensive: Renin Inhibitor

Indications

  • Hypertension alone or in combination with other

antihypertensive agents

Tekturna® (Aliskiren) Package Insert. East Hanover, NJ: Novartis. September 2007.

aliskiren tekturna4
Mechanism of action

Decreases the plasma renin activity (PRA); which is responsible for converting angiotensinogen to angiotensin I

Pharmacokinetics

Absorption: Bioavailability of

~ 2.5%. With a high fat meal, mean AUC & Cmax are decreased by 71% and 85%

Distribution: Steady state reached at 7-8 days

Metabolism: CYP3A4 enzyme

Elimination: Approximately ¼ appears in the urine as parent drug; unknown how much of the absorbed dose is metabolized

Aliskiren (Tekturna®)

Tekturna® (Aliskiren) Package Insert. East Hanover, NJ: Novartis. September 2007.

aliskiren tekturna5
Aliskiren (Tekturna®)

www.uspharmacist.com

aliskiren tekturna6
Aliskiren (Tekturna®)

Dosing and Administration

  • Starting dose of aliskiren is 150 mg PO daily
  • Dose may be increased to a max of 300 mg PO daily

Cost

  • ~ $1.89 for 150 mg tab and $2.38 for 300 mg tab

Patient Education

  • Potential to cause hypotension
  • Medication should be taken at the same time daily
  • If patient forgets to take medication, take it as soon as remembered; do not double dose
  • Medication should NOT be administered with a high fat meal

Tekturna® (Aliskiren) Package Insert. East Hanover, NJ: Novartis. September 2007.

aliskiren tekturna7
Aliskiren (Tekturna®)

Contraindications & Precautions

  • Pregnancy category: C - first trimester; D - second and third trimesters
  • Caution in patients with severe renal dysfunction
  • Concurrent use of ACE-Inhibitor or ARB and the risk of hyperkalemia

Drug Interactions

  • Co-administration of irbesartan reduced the Cmax of aliskiren by ~ 50%
  • Co-administration of atorvastatin results in a 50% increase in the Cmax and AUC of aliskiren after multiple dosing
  • Co-administration of ketoconazole results in an 80% increase in plasma levels of aliskiren
  • Co-administration of furosemide results in a 30% reduction of AUC and 50% reduction of Cmax of aliskiren

Adverse Effects

  • Angioedema, other edema (face, hands, whole body), diarrhea, abdominal pain, dyspepsia, hyperkalemia and cough

Tekturna® (Aliskiren) Package Insert. East Hanover, NJ: Novartis. September 2007.

aliskiren tekturna8
Aliskiren (Tekturna®)

Pool JL, et al. Am J Hypertens. 2007;20:11-20.

aliskiren tekturna9
Aliskiren (Tekturna®)

Strasser RH, et al. J Hum Hyperten. 2007;21:780-87.

aliskiren tekturna10
Aliskiren (Tekturna®)

Place in Therapy

  • May be used as monotherapy for the treatment of hypertension
  • May be used as add-on anti-hypertensive medication to agents such as ACE-I, ARBs, and diuretics

Clinical Pearls

  • If used with an ACE-I, ARB or aldosterone antagonist; potassium levels should be monitored frequently

ACE-I: Angiotensin Converting Enzyme Inhibitor

ARB: Angiotensin Receptor Blocker

ambrisentan

Ambrisentan

Letairis™

Manufactured by: Gilead

www.prescribingreference.com

ambrisentan letairis
Ambrisentan (Letairis™)

Therapeutic Class

  • Endothelin Receptor Antagonist (ERA)

Indications

  • Pulmonary arterial hypertension (PAH) WHO Group I
  • PAH patients with symptoms, to improve exercise capacity and delay clinical worsening

Letairis™ (ambrisentan) Package Insert. Foster City, CA: Gilead. June 2007.

ambrisentan letairis13
Mechanism of action

Ambrisentan is a selective endothelin-A (ETA) receptor antagonist approved for use in PAH

Pharmacokinetics

Absorption: Rapidly absorbed; food has no effect on absorption

Distribution:Highly bound (99%) to plasma proteins

Metabolism: Through CYP3A4, CYP2C19, and uridine 5'-diphosphate glucuronosyltransferases (UGTs) 1A9S, 2B7S and 1A3S

Elimination: Non-renal pathways; half-life of 9-15 hours

Ambrisentan (Letairis™)

www.body.aol.com

Letairis™ (ambrisentan) Package Insert. Foster City, CA: Gilead. June 2007.

ambrisentan letairis14
Ambrisentan (Letairis™)

Dosing and Administration

  • Initiate treatment at 5 mg by mouth daily
  • Increase dose to 10 mg if tolerated (max)

Cost

  • ~ $165 per tablet ( 5 mg or 10 mg)

Patient Education

  • Tablets may be taken with or without food
  • Tablets may NOT be split, crushed, or chewed

Letairis™ (ambrisentan) Package Insert. Foster City, CA: Gilead. June 2007.

ambrisentan letairis15
Ambrisentan (Letairis™)

Contraindications & Precautions

  • Pregnancy category X
  • Potential liver injury, dose-dependent
  • Monitor for hematologic changes (hemoglobin and hematocrit)
  • Co-administration of ambrisentan and cyclosporine

Drug Interactions

  • P-glycoprotein and UGT inducers
  • Potent inhibitor of P-glycoprotein, OATP, and CYP3A4
  • CYP3A4 or 2C19 Inhibitors

Adverse Effects

  • Peripheral edema, nasal congestion, flushing, and headache

Letairis™ (ambrisentan) Package Insert. Foster City, CA: Gilead. June 2007.

OATP: Organic Anion Transporting Polypeptide

ambrisentan letairis16
Ambrisentan (Letairis™)

Galie N, et al. J Am Coll Card. 2004; 43(12):5S-12S.

6-MWD: 6-minute walk distance

ambrisentan letairis17
Ambrisentan (Letairis™)

Place in Therapy

  • Add on agent for the treatment of pulmonary arterial hypertension (following treatment with CCBs and/or sildenafil)
  • May be used as monotherapy or with other agents to treat PAH

Clinical Pearls

  • Minimal liver abnormalities as compared to bosentan

CCB: calcium channel blocker

amlodipine olmesartan

Amlodipine/Olmesartan

Azor®

Manufactured by: Daiichi-Sankyo

www.prescribingreference.com

amlodipine olmesartan azor
Amlodipine/Olmesartan (Azor®)

Therapeutic Class

  • Anti-hypertensive: Calcium Channel Blocker (CCB) and Angiotensin II Receptor Blocker (ARB)

Indications

  • Hypertension alone or with other antihypertensive agents

Azor® (amlodipine/olmesartan) Package Insert. Parsippany, NJ: Daiichi-Sankyo. December 2007.

amlodipine olmesartan azor20
Amlodipine/Olmesartan (Azor®)

Mechanism of action

  • Amlodipine works by inhibiting the transmembrane influx of calcium ions in cardiac and vascular smooth muscle
  • Olmesartan inhibits the vasoconstrictor effects of angiotensin II

Azor® (amlodipine/olmesartan) Package Insert. Parsippany, NJ: Daiichi-Sankyo. December 2007.

amlodipine olmesartan azor21
Pharmacokinetics (amlodipine)

Absorption: Bioavailability ~ 64% to 90%

Distribution: ~ 93% bound to plasma proteins, reaches steady-state in 7-8 days

Metabolism: ~ 90% is converted to inactive metabolites via hepatic metabolism

Elimination: 10% (parent compound) and 60% (metabolites) are excreted in the urine; effective half-life of ~ 45 hours

Pharmacokinetics (olmesartan)

Absorption: Bioavailability ~ 26%

Distribution: Highly bound to plasma proteins (99%); reaches steady-state in 3-5 days

Metabolism: Olmesartan medoxomil converted to olmesartan during absorption and no further metabolism of olmesartan

Elimination: 35%-50% is eliminated in the feces; effective half-life of ~ 7 hours

Amlodipine/Olmesartan (Azor®)

Azor® (amlodipine/olmesartan) Package Insert. Parsippany, NJ: Daiichi-Sankyo. December 2007.

amlodipine olmesartan azor22
Amlodipine/Olmesartan (Azor®)

Dosing and Administration

  • Initiate at 5/20 mg PO daily and titrate to desired BP goal
  • Available as 5/20, 5/40, 10/20 or 10/40 mg tablets

Cost

  • Between $1.86 and $2.68 per tablet

Patient Education

  • Potential to cause hypotension
  • Take this medication at the same time each day
  • If patient forgets to take medication take it as soon as remembered; do not double dose

Azor® (amlodipine/olmesartan) Package Insert. Parsippany, NJ: Daiichi-Sankyo. December 2007.

amlodipine olmesartan azor23
Amlodipine/Olmesartan (Azor®)

Contraindications & Precautions

  • Pregnancy category: C - first trimester; D - second through third trimesters
  • Caution in severe renal and/or hepatic dysfunction
  • Concurrent use of ACE-I or ARB and risk of hyperkalemia
  • Caution in patients with severe obstructive coronary artery disease or congestive heart failure

Drug Interactions

  • No clinically significant drug interactions

Adverse Effects

  • Edema, dizziness, palpitation, and flushing

Azor® (amlodipine/olmesartan) Package Insert. Parsippany, NJ: Daiichi-Sankyo. December 2007.

slide24

Amlodipine/Olmesartan (Azor®)

Azor® (amlodipine/olmesartan) Package Insert. Parsippany, NJ: Daiichi-Sankyo. December 2007.

amlodipine olmesartan azor25
Amlodipine/Olmesartan (Azor®)

Place in Therapy

  • This combination product may be appropriate for patients who desire a smaller pill burden
  • May also be used as an add-on anti-hypertensive medication

Clinical Pearls

  • If compliance is an issue or if this agent is cheaper through insurance, amlodipine/olmesartan may be beneficial to the patient.
eculizumab

Eculizumab

Soliris®

Manufactured by: Alexion Pharmaceuticals

www.prescribingreference.com

eculizumab soliris
Eculizumab (Soliris®)

Therapeutic Class

  • Monoclonal antibody

Indications

  • Paroxysmal nocturnal hemoglobinuria (PNH)

Soliris® (eculizumab) Package Insert. Chesire, CT: Alexion. June 2007.

eculizumab soliris28
Mechanism of action

Monoclonal antibody that specifically binds to and inhibits the terminal complement mediated intravascular hemolysis in PNH patients

Pharmacokinetics

Distribution: Volume of distribution ~ 7.7 L

Elimination: Half life ~ 272 ± 82 hours

Eculizumab (Soliris®)

www.soliris.net

Soliris® (eculizumab) Package Insert. Chesire, CT: Alexion. June 2007.

eculizumab soliris29
Eculizumab (Soliris®)

Dosing and Administration

  • 600 mg every 7 days for 4 weeks, followed by
  • 900 mg for the fifth dose 7 days later, then
  • 900 mg every 14 days thereafter

Cost

  • 300mg vial is ~ $4992

Patient Education

  • Patients must be vaccinated against meningococcus
  • Potential for serious hemolysis when eculizumab is discontinued

Soliris® (eculizumab) Package Insert. Chesire, CT: Alexion. June 2007.

eculizumab soliris30
Eculizumab (Soliris®)

Contraindications & Precautions

  • May have an increased susceptibility to infections
  • May result in infusion reactions
  • Pregnancy category C

Drug Interactions

  • No drug interactions have been studied or reported

Adverse Effects

  • Meningococcal infections, headache, back pain, nausea, fatigue and cough

Soliris® (eculizumab) Package Insert. Chesire, CT: Alexion. June 2007.

eculizumab soliris31
Eculizumab (Soliris®)

Hillmen P, et al. N Engl J Med.2006;355:1233-43.

eculizumab soliris32
Eculizumab (Soliris®)

Hillmen P, et al. Blood. 2007;110 (12):4123-28.

eculizumab soliris33
Eculizumab (Soliris®)

Place in Therapy

  • Only pharmacologic agent indicated to treat PNH

Clinical Pearls

  • Do not initiate in patients with N. meningitidis infection or who are not vaccinated against N. meningitidis
lidocaine

Lidocaine

Zingo™

Manufactured by: Anesiva

www.prescribingreference.com

lidocaine zingo
Lidocaine (Zingo™)

Therapeutic Class

  • Amide local anesthetic

Indications

  • To provide local analgesia prior to venipuncture or peripheral intravenous cannulation in children 3-18 years of age
  • Zingo (lidocaine) Package Insert. Tempe, AZ: Anesiva. September 2007.
lidocaine zingo36
Mechanism of action

Amide-type local anesthetic agent that blocks sodium ion channels required for the initiation and conduction of neuronal impulses, resulting in local anesthesia

Pharmacokinetics

Absorption: Single doses do not produce any detectable plasma concentration of lidocaine

Distribution: N/A

Metabolism: Unknown if lidocaine is metabolized in the skin

Elimination: N/A

Lidocaine (Zingo™)
  • Zingo (lidocaine) Package Insert. Tempe, AZ: Anesiva, Inc. September 2007.
lidocaine zingo37
Lidocaine (Zingo™)

Dosing and Administration

  • Use one application (0.5 mg lidocaine hydrochloride) to the site of venipuncture or intravenous cannulation approximately 1-3 minutes before insertion
  • Only one more application may be used on a new location if there is a failed attempt for venous access

Cost

  • Unavailable

Patient Education

  • Loud sound released upon administration / activation
  • Skin reactions may occur with irritation / allergy
  • Zingo (lidocaine) Package Insert. Tempe, AZ: Anesiva, Inc. September 2007.
lidocaine zingo38
Lidocaine (Zingo™)

Contraindications & Precautions

  • Pregnancy category B
  • Safety use in children under the age of 3 has not been evaluated
  • Patients with a history of known sensitivity to amide local anesthetics

Drug Interactions

  • None

Adverse Effects

  • Erythema, edema, petechiae, bruising, burning and pain
  • Zingo (lidocaine) Package Insert. Tempe, AZ: Anesiva, Inc. September 2007.
lidocaine zingo39
Lidocaine (Zingo™)
  • Zingo (lidocaine) Package Insert. Tempe, AZ: Anesiva, Inc. September 2007.
lidocaine zingo40
Lidocaine (Zingo™)

Place in Therapy

  • Local analgesia prior to venipuncture or IV cannulation
  • Main use is found in pediatric patient population; especially children afraid of needle sticks

Clinical Pearls

  • Analgesia seen within 1-3 minutes and will diminish 10 minutes after administration
  • Do not use multiple applications at the same location
  • Zingo (lidocaine) Package Insert. Tempe, AZ: Anesiva, Inc. September 2007.
learning assessment

Learning Assessment

Question Time!

slide42

Patient SP is being seen today in his PCP office and it was noted that his BP was 164/102. He is currently taking lisinopril 40 mg PO daily and furosemide 20 mg PO BID. Which of the following medications would be an option to control his hypertension?

  • Ambrisentan (LetairisTM)
  • Meloxicam (Mobic®)
  • Aliskiren (Tekturna®)
  • Lidocaine (ZingoTM)
what is the main benefit of amlodipine olmesartan azor
What is the main benefit of (amlodipine/olmesartan) Azor®?
  • Less expensive
  • More effective antihypertensive
  • Reduced pill burden
  • Less adverse effects
what is the most common adverse effect noted with ambrisentan letairis tm
What is the most common adverse effect noted with ambrisentan (LetairisTM)?
  • Hypotension
  • Peripheral edema
  • Dry cough
  • Sedation
prior to use with eculizumab soliris it is important that all patients be vaccinated against this
Prior to use with eculizumab (Soliris®), it is important that all patients be vaccinated against this?
  • Varicella
  • Meningococcus
  • Typhoid fever
  • Papillomavirus
slide46

4 year old ML is in the ER awaiting peripheral IV cannulation to administer IV fluids and is scared of the pain associated with the procedure. Which product could you recommend that might provide local analgesia for BP that is approved for pediatric use?

  • Benzocaine (Orajel®)
  • Procaine (Novocain®)
  • Lidocaine (Zingo®)
  • Eculizumab (Soliris®)
slide47
What is the onset of action of lidocaine used to provide topical analgesia to BP in the previous question?
  • 15 minutes
  • Instantly
  • 15-30 minutes
  • 1-3 minutes
what is the recommended dose range for aliskiren tekturna tm
What is the recommended dose range for aliskiren (TekturnaTM)?
  • 15 – 30 mg PO Daily
  • 100 - 300 mg PO TID
  • 25 – 50 grams BID
  • 150 – 300 mg PO Daily
slide49
Which of the following is NOT a benefit of ambrisentan (LetairisTM) when compared to bosentan (TracleerTM)?
  • No drug interactions with sildenafil or warfarin
  • Fewer adverse reactions
  • Once daily dosing
  • Less risk of hepatotoxicity
slide50
Which of the following should not be considered when initiating a patient on (amlodipine/olmesartan) Azor®?
  • Serum potassium levels
  • Blood pressure
  • Patient age
  • Renal function
slide51

True or False: Eculizumab (Soliris®) has been studied against other monoclonal antibodies for the treatment of paroxysmal nocturnal hemoglobinuria (PNH)?

  • True
  • False
questions
Questions?

Sara Tebbe, PharmD

The Methodist Hospital

6565 Fannin Street, DB1-09

Houston, TX 77030

srtebbe@tmhs.org

new drugs of 2007 part 153

New Drugs of 2007 Part 1

Presented by: Brandi Polder, Pharm.D.

Drugs Covered: Estradiol (Evamist™)

Histrelin acetate (Supprelin® LA)

Lanreotide acetate (Somatuline Depot®)

Levocetirizine dihydrochloride (Xyzal®)

Retapamulin (Altabax™)

estradiol

Estradiol

Evamist™

Manufactured by: Vivus, Inc.

www.prescribingreference.com

http://www.evamist.com/

estradiol evamist
Estradiol (Evamist™)

Therapeutic Class

  • Hormone and hormone modifier

Indications

  • For the treatment of moderate to severe vasomotor symptoms due to menopause

Evamist™ [package insert]. St. Louis, MO: Ther-Rx; 2007.

estradiol evamist56
Mechanism of action

Development and maintenance of the female reproductive system and secondary sexual characteristics

Pharmacokinetics

Absorption: Steady state after 7-8 days of application

Distribution:Widely distributed

Metabolism: Liver

Elimination: Urine

Dose Adjustments: Hepatic impairment – contraindicated

Estradiol (Evamist™)

Evamist™ [package insert]. St. Louis, MO: Ther-Rx; 2007.

estradiol evamist57
Estradiol (Evamist™)

Dosing and Administration

  • One spray (90mcL) once daily to the forearm
  • Increase to two to three sprays daily based upon clinical response

Cost

  • Unavailable

Patient Education

  • Side effects of estrogen therapy
  • Do not start estradiol transdermal spray if you have unusual vaginal bleeding, currently have or have had certain cancers including breast or cervical cancer, had a stroke or heart attack within the past year, currently have or have had blood clots, currently have or have had liver problems, are allergic to any of the ingredients

Evamist™ [package insert]. St. Louis, MO: Ther-Rx; 2007.

estradiol evamist58
Estradiol (Evamist™)

Contraindications

  • Undiagnosed abnormal genital bleeding
  • Known, suspected, or history of cancer of the breast
  • Known or suspected estrogen-dependent neoplasia
  • Deep vein thrombosis or pulmonary embolism
  • Active or recent arterial thromboembolic disease
  • Known liver dysfunction or disease
  • Known or suspected pregnancy

Precautions

  • An increased risk of invasive breast cancer has been reported with the use of estrogens plus progestins
  • Estrogens increase the risk of gallbladder disease
  • Monitor thyroid function in patients on thyroid replacement therapy

Evamist™ [package insert]. St. Louis, MO: Ther-Rx; 2007.

estradiol evamist59
Estradiol (Evamist™)

Drug Interactions

  • Inducers and inhibitors of CYP3A4

Adverse Effects

  • Most common: headache, breast tenderness and nipple pain (20%), nausea (3%), application site reactions (1.3%)

Evamist™ [package insert]. St. Louis, MO: Ther-Rx; 2007.

estradiol evamist60
Estradiol (Evamist™)

http://www.centerwatch.com/patient/drugs/dru958.html

estradiol evamist61
Estradiol (Evamist™)
  • Results continued:

http://www.centerwatch.com/patient/drugs/dru958.html

estradiol evamist62
Estradiol (Evamist™)

Place in Therapy

  • For patients with moderate to severe vasomotor symptoms due to menopause who want to try an alternative dosage form
    • Sensitivity to the patch adhesive
    • Gel is too messy

Evamist™ [package insert]. St. Louis, MO: Ther-Rx; 2007.

histrelin acetate

Histrelin acetate

Supprelin® LA

Manufactured by: Indevus Pharmaceuticals, Inc.

www.prescribingreference.com

histrelin acetate supprelin la
Histrelin acetate (Supprelin® LA)

Therapeutic Class

  • Endocrine-Metabolic Agent; Gonadotropin Releasing Hormone Agonist

Indications

  • For the treatment of children with central precocious puberty (CPP)

Supprelin® LA [package insert]. Lexington, MA: Indevus; 2007.

histrelin acetate supprelin la65
Mechanism of action

Luteinizing hormone-releasing hormone (LH-RH) agonist that inhibits gonadotropin secretion

Increases levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) upon initiation of treatment but decreases at continuous administration of the drug

Pharmacokinetics

Absorption: Bioavailability: 92%

Distribution:Vd: 58.4 L +/- 7.86 L ; Protein binding: 29.5% +/- 8.9% unbound

Metabolism: Hepatic

Elimination half-life: 3.92 h +/- 1.01 h

Dose Adjustments: none

Histrelin acetate (Supprelin® LA)

Supprelin® LA [package insert]. Lexington, MA: Indevus; 2007.

histrelin acetate supprelin la66
Histrelin acetate (Supprelin® LA)

Dosing and Administration

  • One implant inserted subcutaneously in the inner aspect of the upper arm once a year

Cost

  • Unavailable

Patient Education

  • Avoid wetting the arm with the implant for 24 hours and refrain from heavy lifting or strenuous exertion of the arm with the implant for 7 days after implant insertion
  • May cause pain, swelling, or redness in or around the incision site
  • Report new or worsening bone pain, weakness or numbness in legs, hematuria, or dysuria
  • Advise caregiver that the child may experience initial new-onset or worsening of puberty symptoms, but that symptoms should resolve within 4 weeks

Supprelin® LA [package insert]. Lexington, MA: Indevus; 2007.

histrelin acetate supprelin la67
Histrelin acetate (Supprelin® LA)

Contraindications

  • History of hypersensitivity to GnRH or GnRH analogs
  • Females who are or may become pregnant

Precautions

  • Initial transient increases of estradiol and/or testosterone may cause a temporary worsening of symptoms
  • Implant insertion is a surgical procedure

Drug Interactions

  • No formal interaction studies have been performed

Adverse Effects

  • Most common – injection site reactions (51.1%)

Supprelin® LA [package insert]. Lexington, MA: Indevus; 2007.

histrelin acetate supprelin la68
Histrelin acetate (Supprelin® LA)

Hirsch HJ, et al. Pediatrics 2005;116:e798-e802.

histrelin acetate supprelin la69
Histrelin acetate (Supprelin® LA)

Eugster EA, et al. The Journal of Clinical Endocrinology & Metabolism 2007;92(5):1697-1704.

histrelin acetate supprelin la70
Histrelin acetate (Supprelin® LA)

Place in Therapy

  • For those patients who would prefer a yearly implant

Supprelin® LA [package insert]. Lexington, MA: Indevus; 2007.

lanreotide acetate

Lanreotide acetate

SomatulineDepot®

Manufactured by: Ipsen Pharma Biotech, Inc.

www.prescribingreference.com

lanreotide acetate somatuline depot
Lanreotide acetate (Somatuline Depot®)

Therapeutic Class

  • Endocrine-Metabolic Agent, Somatostatin Analog

Indications

  • For the long-term treatment of acromegalic patients who have had an inadequate response to or cannot be treated with surgery and/or radiotherapy

Somatuline® Depot [package insert]. Signes, France: Ipsen Pharma Biotech; 2007.

lanreotide acetate somatuline depot73
Mechanism of action

High affinity for human somatostatin receptors (SSTR)

Has dose-dependent reductions in GH and/or IGF-1 levels, enabling normalization of levels in acromegalic patients

Also an inhibitor of various endocrine, neuroendoocrine, exocrine, and paracrine functions

Pharmacokinetics

Absorption: Bioavailability - 73.4% (60 mg), 69% (90 mg), 78.4% (120 mg)

Distribution:Vd - 0.74 L/kg

Metabolism: CYP450; possible 3A4 inhibitor

Elimination: Fecal - < 0.5% unchanged; Renal - < 5%

Dose Adjustments: Start dose is 60mg in moderate and severe renal or hepatic impairment

Lanreotide acetate (Somatuline Depot®)

Somatuline® Depot [package insert]. Signes, France: Ipsen Pharma Biotech; 2007.

lanreotide acetate somatuline depot74
Lanreotide acetate (Somatuline Depot®)

Dosing and Administration

  • Dose range 60mg to 120mg every 4 weeks
  • Injected in superior external quadrant of the buttock

Cost

  • Unavailable

Patient Education

  • Store at 2-8°C in the original container
  • You will receive the injection every 4 weeks as directed by your doctor. After 3 months, your doctor should check your levels of GH and IGF-1, talk to you about your symptoms, and adjust your dose as needed. If you miss an injection, talk with your doctor as soon as possible to advise another injection.

Somatuline® Depot [package insert]. Signes, France: Ipsen Pharma Biotech; 2007.

lanreotide acetate somatuline depot75
Lanreotide acetate (Somatuline Depot®)

Contraindications & Precautions

  • Contraindications – None
  • Gallstones
  • Hypo- and/or hyperglycemia
  • Slight decreases in thyroid function
  • Decrease in heart rate
  • Cyclosporine
  • Somatostatin analogs may decrease the metabolic clearance of compounds metabolized by CYP450 enzymes

Adverse Effects

  • Most common – diarrhea (37%), cholelithiasis (20%), abdominal pain (19%), nausea (11%), anemia (7%), and injection site reactions (9%)

Somatuline® Depot [package insert]. Signes, France: Ipsen Pharma Biotech; 2007.

lanreotide acetate somatuline depot76
Lanreotide acetate (Somatuline Depot®)

Caron PH, et al. The Journal of Clinical Endocrinology & Metabolism 2007;87(1):99-104.

lanreotide acetate somatuline depot77
Lanreotide acetate (Somatuline Depot®)

Ronchi CL, et al. Clinical Endocrinology 2007;67:512-9.

lanreotide acetate somatuline depot78
Lanreotide acetate (Somatuline Depot®)

Place in Therapy

  • For acromegalic patients who have had an inadequate response to or cannot be treated with surgery and/or radiotherapy

Somatuline® Depot [package insert]. Signes, France: Ipsen Pharma Biotech; 2007.

levocetirizine dihydrochloride

Levocetirizine dihydrochloride

Xyzal®

Manufactured by: Sanofi Aventis

www.prescribingreference.com

levocetirizine dihydrochloride xyzal
Levocetirizine dihydrochloride (Xyzal®)

Therapeutic Class

  • Antihistamine; H1- blocker

Indications

  • Relief of symptoms associated with seasonal and perennial allergic rhinitis
  • Treatment of uncomplicated skin manifestations of chronic idiopathic urticaria

Xyzal™ [Package Insert]. Bridgewater, NJ: 2007.

levocetirizine dihydrochloride xyzal81
Mechanism of action

Active enantiomer of cetirizine

Inhibits H1 receptors

Pharmacokinetics

Absorption: Rapidly and extensively absorbed

Distribution:Vd - 0.4L/kg; plasma protein binding in vitro – 91-92%

Metabolism: CYP3A

Elimination: Urine – 85.4%;

Feces – 12.9%

Dose Adjustments: Renal impairment - Adjust the dose in patients 12 years of age with decreased renal function

Levocetirizine dihydrochloride (Xyzal®)

Xyzal™ [Package Insert]. Bridgewater, NJ: 2007.

levocetirizine dihydrochloride xyzal82
Levocetirizine dihydrochloride (Xyzal®)

Dosing and Administration

  • 6-11 years old – 2.5 mg once daily in pm
  • ≥ 12 years of age – 5 mg once daily in pm

Cost

  • Cost: 5 mg tablet $253.13 (for 90 tablets) - $84.38/month

Patient Education

  • Avoid activities requiring mental alertness or coordination until drug effects are realized
  • May cause nasopharyngitis, xerostomia, and pharyngitis, as well as pyrexia, cough, and epistaxis in children 12 and under
  • Tablet may be broken in half to achieve correct dose for a child
  • Do not drink alcohol or take other CNS depressants

Xyzal™ [Package Insert]. Bridgewater, NJ: 2007.

Morris & Dickson website: www.mdwebportal.net

levocetirizine dihydrochloride xyzal83
Levocetirizine dihydrochloride (Xyzal®)

Contraindications

  • End-stage renal disease (CrCl ≤ 10 mL/min) and patients undergoing hemodialysis
  • Known hypersensitivity to levocetirizine, cetirizine, or any product ingredient
  • Pediatric patients aged 6 - 11 years with impaired renal function

Precautions

  • Avoid engaging in hazardous occupations requiring complete mental alertness such as driving or operating machinery
  • Avoid concurrent use alcohol or other central nervous system depressants

Xyzal™ [Package Insert]. Bridgewater, NJ: 2007.

levocetirizine dihydrochloride xyzal84
Levocetirizine dihydrochloride (Xyzal®)

Drug Interactions

  • Unlikely to produce pharmacokinetic interactions through inhibition or induction of liver drug-metabolizing enzymes
  • Theophylline
  • Ritonavir

Adverse Effects

  • Most common (rate ≥2% and > placebo) – drowsiness (6%), nasopharyngitis (6%), fatigue (2%), dry mouth (3%), and pharyngitis (subjects ≥12 years old) and pyrexia (4%), drowsiness (3%), cough (3%), and epistaxis (2%) (children 6-12 years old)

Xyzal™ [Package Insert]. Bridgewater, NJ: 2007.

levocetirizine dihydrochloride xyzal85
Levocetirizine dihydrochloride (Xyzal®)

Potter PC. Ann Allergy Asthma Immunol 2005;95:175-80.

levocetirizine dihydrochloride xyzal86
Levocetirizine dihydrochloride (Xyzal®)

Caronica GW, et al. Respiratory Medicine. 2006;100:1706-15.

levocetirizine dihydrochloride xyzal87
Levocetirizine dihydrochloride (Xyzal®)

Place in Therapy

  • For patients with seasonal and perennial allergic rhinitis or uncomplicated skin manifestations of chronic idiopathic urticaria who may get too sleepy with cetirizine or other histamine blockers

Xyzal™ [Package Insert]. Bridgewater, NJ: 2007.

retapamulin

Retapamulin

Altabax™

Manufactured by: GlaxoSmithKline

www.prescribingreference.com

retapamulin altabax
Retapamulin (Altabax™)

Therapeutic Class

  • Antibacterial agent

Indications

  • For use in patients ≥ 9 months for the topical treatment of impetigo due to Staphylococcus aureus (methicillin-susceptible isolates only) or Streptococcus pyogenes

Altabax ™ [package insert]. Research Triangle Park, NC: GlaxoSmithKline; 2007.

retapamulin altabax90
Mechanism of action

Semisynthetic derivative of pleuromutilin

Inhibits peptidyl transfer, blocks P-site interactions, and prevents the normal creation of active 50S ribosomal subunits

Pharmacokinetics

Absorption: Low systemically

Distribution:~ 94% bound to human plasma proteins. VD has not been determined

Metabolism: CYP3A4

Elimination: Unknown

Dose Adjustments: None

Retapamulin (Altabax™)

Altabax ™ [package insert]. Research Triangle Park, NC: GlaxoSmithKline; 2007.

retapamulin altabax91
Retapamulin (Altabax™)

Dosing and Administration

  • Apply a thin layer to the affected area twice daily for 5 days

Cost

  • Cost: 5gm $48.25; 10gm $72.61; 15gm $88.78 (AWP)

Patient Education

  • Wash hands after application
  • For external use only
  • Use the medication for the full time recommended by the healthcare provider
  • If no improvement in symptoms within 3 to 4 days of starting therapy, notify the healthcare provider
  • May cause reactions at the site of application

Altabax ™ [package insert]. Research Triangle Park, NC: GlaxoSmithKline; 2007.

retapamulin altabax92
Retapamulin (Altabax™)

Contraindications and Precautions

  • Contraindications - none
  • Local irritation
  • Potential for microbial overgrowth
  • Pregnancy category B

Drug Interactions

  • Oral ketoconazole
  • Unlikely to affect the metabolism of other P450 substrates
  • Effect of concurrent application of retapamulin and other topical products to the same area of skin has not been studied

Adverse Effects

  • Most common (≤2%) – application site irritation
  • Other (<1%)– application site pain, erythema, and contact dermatitis

Altabax ™ [package insert]. Research Triangle Park, NC: GlaxoSmithKline; 2007.

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Retapamulin (Altabax™)

Altabax ™ [package insert]. Research Triangle Park, NC: GlaxoSmithKline; 2007

retapamulin altabax94
Retapamulin (Altabax™)

Oranje, AP, et al. Dermatology 2007;215:331-40.

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Retapamulin (Altabax™)

Place in Therapy

  • For patients who would prefer a twice daily regimen opposed to a three times daily regimen for the topical treatment of impetigo

Clinical Pearls

  • Believed to have no resistance patterns

Altabax ™ [package insert]. Research Triangle Park, NC: GlaxoSmithKline; 2007.

learning assessment96

Learning Assessment

Question Time!

slide97

A patient with central precocious puberty is about to receive an injection of histrelin. She also has moderate renal impairment. This is a problem because

  • The dose of histrelin will have to be decreased.
  • Histrelin is contraindicated in patients with renal impairment.
  • There is no problem. There is no dosage adjustment for histrelin.
  • The dose of histrelin will have to be increased.
slide98

A patient with seasonal allergic rhinitis. He has tried fexofenadine, diphenhydramine, and cetirizine with no success. Another antihistamine option may be

  • Dextrocetirizine
  • Levocetirizine
  • Levothyroxine
  • Flonase
slide99

A patient on the Lanreotide injection is taking the following medications: cyclosporine, aspirin, docusate, and fexofenadine. Which of the patient’s medications could interact with the Lanreotide?

  • Cyclosporine
  • Aspirin
  • Docusate
  • Fexofenadine
slide100
Retapamulin ointment, 1%, is a pleuromutilin antibiotic. The advantage it has over other treatments available is that
  • It is applied 4 times daily
  • It is applied 2 times daily
  • It is applied once daily
  • It is applied 3 times daily
slide101

A patient in the hospital is having severe vasomotor symptoms associated with menopause. Her past medical history is significant for breast cancer. She doesn’t like the estradiol patch because it irritates her skin. Thus, her order for the estradiol transdermal spray would be a good option.

  • TRUE
  • FALSE
slide102

A 10 year old patient with impetigo walks into the dermatologist’s office. Upon further investigation, it was known that he has a case caused by S. pyogenes. What could the dermatologist prescribe for this patient?

  • Retapamulin ointment
  • Histrelin acetate
  • Neosporin
  • Azithromycin
a disadvantage of the estradiol transdermal spray is that
A disadvantage of the estradiol transdermal spray is that
  • It is not an effective treatment for severe vasomotor symptoms due to menopause
  • You can not take it on an empty stomach
  • It could require dosing up to three sprays per day
  • You have to dose adjust in renal impairment patients
slide104

An acromegalic patient is about to start the Lanreotide injection. The patient has severe hepatic impairment and therefore his initial dose would be

  • 50mg every 4 weeks
  • 60mg every 2 weeks
  • 60mg every 4 weeks
  • 50mg every 2 weeks
slide105
The greatest advantage that histrelin has over it’s comparative therapies for the treatment of central precocious puberty is that
  • It’s inexpensive
  • It is dosed monthly
  • It is dosed yearly
  • There are no comparative therapies. Histrelin is the only treatment for central precocious puberty available on the market.
slide106

A patient with end-stage renal disease has a prescription for Xyzal 5mg PO daily. You, as the pharmacist, know you need to call the physician and recommend that

  • The dose needs to be reduced to 2.5mg daily
  • The dose needs to be reduced to 2.5mg twice weekly
  • Xyzal not be used since it is contraindicated in patients with a creatinine clearance of <10 mL/min
  • The dose should be increased
questions107
Questions?

Brandi Polder, PharmD

The Methodist Hospital

6565 Fannin Street, DB1-09

Houston, TX 77030

blpolder@tmhs.org