Postmenopausal agents

Initial U.S. Approval:  2013
BRISDELLE is a selective serotonin reuptake inhibitor (SSRI) indicated for the treatment of moderate to severe vasomotor symptoms associated with menopause (VMS) (1)
Limitation of Use: BRISDELLE is not indicated for the treatment of any psychiatric condition

Mechanism of Action:
Nonclinical studies have shown that paroxetine is an SSRI. BRISDELLE is not an estrogen, and its mechanism of action for the treatment of VMS is unknown.

Initial U.S. Approval:  2013

Mechanism of Action: DUAVEE pairs conjugated estrogens with bazedoxifene. Conjugated estrogens and bazedoxifene function by binding to and activating estrogen receptors (ER) a and ß, which vary in proportion from tissue to tissue. Conjugated estrogens are composed of multiple estrogens and are agonists of ER- a and ß. Bazedoxifene is an estrogen agonist/antagonist that acts as an agonist in some estrogen-sensitive tissues and an antagonist in others (e.g., uterus). The pairing of conjugated estrogens with bazedoxifene produces a composite effect that is specific to each target tissue. The bazedoxifene component reduces the risk of endometrial hyperplasia that can occur with the conjugated estrogens component.
Pharmacodynamic studies have not been conducted with DUAVEE.

INDICATIONS AND USAGE:  DUAVEE is a combination of conjugated estrogens with an estrogen agonist/antagonist indicated for treatment of the following conditions in women with a uterus:
Treatment of moderate to severe vasomotor symptoms associated with menopause (1.1)
Prevention of postmenopausal osteoporosis (1.2)

Limitation of Use: DUAVEE should be used for the shortest duration consistent with treatment goals and risks for the individual woman

HOW SUPPLIED: Tablet containing conjugated estrogens 0.45 mg and bazedoxifene 20 mg

Drug Updates:  OSPHENA ® (ospemifene) tablets, for oral use
[Drug information  /  PDF]  
Dosing:  Click (+) next to Dosage and Administration section (drug info link)

Initial U.S. Approval:  2013

Mechanism of Action: OSPHENA is an estrogen agonist/antagonist with tissue selective effects. Its biological actions are mediated through binding to estrogen receptors. This binding results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism).

WARNING: ENDOMETRIAL CANCER AND
CARDIOVASCULAR DISORDERS
See full prescribing information for complete boxed warning.

OSPHENA is an estrogen agonist/antagonist with tissue selective effects. In the endometrium, OSPHENA has estrogen agonistic effects. There is an increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adding a progestin to estrogen therapy reduces the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer.

Estrogen-alone therapy has an increased risk of stroke and deep vein thrombosis (DVT). OSPHENA 60 mg had cerebral thromboembolic and hemorrhagic stroke incidence rates of 0.72 and 1.45 per thousand women, respectively vs. 1.04 and 0 per thousand women, respectively in placebo. For deep vein thrombosis, the incidence rate for OSPHENA 60 mg is 1.45 per thousand women vs. 1.04 per thousand women in placebo.

INDICATIONS AND USAGE:
OSPHENA is an estrogen agonist/antagonist indicated for the treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause.

CONTRAINDICATIONS:

1. Undiagnosed abnormal genital bleeding
2. Known or suspected estrogen-dependent neoplasia
3. Active DVT, pulmonary embolism (PE), or a history of these conditions
4. Active arterial thromboembolic disease (for example, stroke and myocardial infarction [MI]), or a history of these conditions
5. Known or suspected pregnancy

DOSAGE AND ADMINISTRATION:
One tablet taken orally once daily with food .

DOSAGE FORMS AND STRENGTHS
Tablet: 60 mg

Local monograph

Initial U.S. Approval:  2017

Mechanism of Action:
Abaloparatide is a PTHrP(1-34) analog which acts as an agonist at the PTH1 receptor (PTH1R). This results in activation of the cAMP signaling pathway in target cells. In rats and monkeys, abaloparatide had an anabolic effect on bone, demonstrated by increases in BMD and bone mineral content (BMC) that correlated with increases in bone strength at vertebral and/or nonvertebral sites

INDICATIONS AND USAGE:
TYMLOS is indicated for the treatment of postmenopausal women with osteoporosis at high risk for fracture defined as a history of osteoporotic fracture, multiple risk factors for fracture, or patients who have failed or are intolerant to other available osteoporosis therapy. In postmenopausal women with osteoporosis, TYMLOS reduces the risk of vertebral fractures and nonvertebral fractures [see Clinical Studies (14)].

Limitations of Use
Because of the unknown relevance of the rodent osteosarcoma findings to humans, cumulative use of TYMLOS and parathyroid hormone analogs (e.g., teriparatide) for more than 2 years during a patient’s lifetime is not recommended.

DOSAGE AND ADMINISTRATION: PDF
2.1 Recommended Dosage
The recommended dosage of TYMLOS is 80 mcg subcutaneously once daily.
Cumulative use of TYMLOS and parathyroid hormone analogs (e.g., teriparatide) for more than 2 years during a patient’s lifetime is not recommended [see Warnings and Precautions (5.1)].
Patients should receive supplemental calcium and vitamin D if dietary intake is inadequate.

2.2 Administration Instructions
Administer TYMLOS as a subcutaneous injection into the periumbilical region of the abdomen. Rotate the site of the injection every day and administer at approximately the same time every day. Do not administer intravenously or intramuscularly.
Administer the first several doses where the patient can sit or lie down if necessary, in case symptoms of orthostatic hypotension occur [see Warnings and Precautions (5.2) and Adverse Reactions (6.1)].
TYMLOS is a clear and colorless solution. Visually inspect TYMLOS for particulate matter and discoloration prior to administration. Do not use if solid particles appear or if the solution is cloudy or colored.
Provide appropriate training and instruction to patients and caregivers on the proper use of the TYMLOS pen.

HOW SUPPLIED:
Injection: 3120 mcg/1.56 mL (2000 mcg/mL) in a single-patient-use prefilled pen. The prefilled pen delivers 30 doses of TYMLOS, each containing 80 mcg of abaloparatide in 40 mcL of a sterile, clear, colorless solution.