Premarin is the brand name for a compound drug consisting of conjugated estrogens. Isolated from mare's urine (PREgnant MARes' urINe), it is manufactured by Wyeth Pharmaceuticals and has been marketed since 1942. It is available in oral forms - Premarin 0.3, Premarin 0.45, Premarin 0.625 and Premarin 1.25. It is also produced as Premarin cream for topical application.

Angeliq - Mode of Action

Angeliq tablets contain two active ingredients, estradiol hemihydrate  and drospirenone. These are forms of the main female sex hormones, oestrogen and progesterone. Estradiol hemihydrate is a naturally occuring form of oestrogen and drospirenone is a synthetic form of progesterone.

Clinical Value of Angeliq

Angeliq is an HRT (hormone replacement therapy) preparation suitable for women who have not had a hysterectomy and who have symptoms or problems associated with the menopause.

The progestogen in ANGELIQ® tablets drospirenone, is different from the progestin found in other HRTs.

While many synthetic progestogens are derived from the male hormone, testosterone, drosperinone is derived from spironolactone and this most closely resembles and acts like the hormone progesterone made by your body.

ANGELIQ tablets (drospirenone/estradiol), with the unique hormone drsp®, offer rapid relief from moderate to severe menopausal symptoms such as hot flashes, night sweats and vaginal dryness in a once-a-day pill.

Angeliq:-

  • Provides rapid relief from moderate to severe menopausal symptoms such as hot flashes and night sweats
  • Provides relief from vaginal symptoms such as dryness, itching and burning
  • Offers combination (estrogen and progestin) hormone therapy (HT) in a once-a-day pill
  • Is the only HT with the unique drospirenone
  • Contains estradiol, a plant-based estrogen that’s been used in HT for over 20 years

ANGELIQ has been proven to effectively relieve moderate to severe hot flashes, night sweats and vaginal symptoms.

  • In clinical trials, on average, women had almost a 30% reduction in hot flashes and night sweats after the first week. Four weeks after starting ANGELIQ, symptoms had dropped by 70% and by 12 weeks, symptoms were reduced by 90%.
  • It has been shown that treatment with Angeliq is both safe and tolerable.
  • Most adverse events are mild or moderate degree of intensity.
  • It is efficacious0702 and safe in the treatment of hot flushes and other climacteric symptoms in postmenopausal women.0701 Angeliq is safe and well tolerated in hypertensive postmenopausal women.0703
  • Combination therapy with DRSP/E2 significantly lowers blood pressure in postmenopausal women with hypertension. This may provide benefit for cardiovascular risk reduction in this population.0501

Related Medical Abstracts - Click on the paper title:-

HRT and The Menopause

The menopause is defined as the last menstrual period. We tend to to consider the menopause to be that period of time when a woman ceases to have reproductive capability. Strictly speaking that span of time is not the menopause but the climacteric.

At the menopause, the ovaries lose much of their function. There is a fall in hormone production, notably oestrogen.

As oestrogen protects the heart and bones, post menopause the risks of osteoporosis and heart disease increase.

A natural menopause occurs at the time nature intended. Artificial menopause tends to be medically related. This is usually surgical - the ovaries are removed typically during hysterectomy. Radiation may also cause a menopause.

What are the symptoms and signs of the menopause?

The declining levels of ovarian hormones can cause distressing symptoms:

Strictly speaking these are symptoms of the menopause. A sign is an observation by a doctor during examination.

In the short-term, the menopause may be associated with distressing symptoms. At least four out of five women are troubled by menopausal symptoms. These relate to the:-

In the longer-term, there are significant risks of morbidity (disease) and preventable early mortality (death). There is a wealth of evidence proving that the deficiency in reproductive hormones accelerates the ageing processes of the arteries (atherosclerosis Q 26.23) and the skeleton (osteoporosis – Q 26.24).

How can the menopause be treated?

The mainstay of treatment is hormone replacement therapy - HRT. HRT is particularly effective relief for hot flushes (flashes) and night sweats.

There are benefits and risks of HRT. HRT may reduce the rate of these degenerative processes and possibly reverse the trends leading to reduced morbidity (illness) and delayed mortality (death). Provided you remain healthy, you should continue to have the physical and mental ability to care for, and enjoy, your family. HRT is likely to help you feel and be healthier.

How do we decide which will be the most appropriate HRT for me?


Figure 28.1

Figure 28.1 is a flowchart indicating the salient questions to be addressed when considering the HRT options. There are three main questions leading to the appropriate options:

First, have you had a hysterectomy ?

If your womb has been removed (hysterectomy), oestrogen replacement can be prescribed alone; there is generally no need for progestogens. If the womb has not been removed and oestrogen were prescribed unopposed, there would be a chance of the endometrium (womb lining) becoming unduly thickened with a risk of bleeding problems and on rare occasions malignancy (HRT and progestogen).?

Secondly, if your womb is still present, are you still seeing your periods?

If periods are occurring spontaneously HRT would be supplementing the natural hormone cycle. In addition to the oestrogen replacement your doctor would suggest a progestogen for 10 to 12 days each month to ensure a regular withdrawal bleed. This prevents your endometrium (lining of the womb) becoming too thick. If you have not reached your menopause and a non-bleed variety of HRT were prescribed you would almost certainly have irregular bleeding.

Finally, if your womb is still present and the menopause has already occurred, do you wish to have a regular withdrawal bleed?

There is a choice of prescribing the progestogen se quentially to produce a regular withdrawal bleed or prescribing the progestogen on a daily (non-cyclical) regimen: This continuous combined HRT provides the benefits of HRT without “periods”. A blood hormone test can be arranged to provide a guide as to whether you have reached your menopause ( Q 26.14).

 


 

Menopause and HRT (BMA Family Doctor)

Menopause and HRT (BMA Family Doctor)

 

What side-effects could I experience when I start Angeliq?

You will probably have no difficulties as Angeliq is simply ‘replacing’ a natural hormone deficiency.

  • You may experience mastalgia (breast discomfort) initially but this usually settles quickly by itself or with pyridoxine (vitamin B6) 50mg twice daily or gamolenic acid up to 320 mg daily.
  • If you have not had a hysterectomy , there may be a little spotting of blood during the first month or so.
  • Around the menopause, there is a tendency to gain weight, whether you take HRT or not (Q 28.22).


Angeliq is a continuous form of combined HRT. Each tablet contains both estradiol and drospirenone, so that a dose of both hormones is taken daily. This type of HRT does not produce a monthly withdrawal bleed, and so is suitable for women whose periods have already stopped, eg for postmenopausal women who have not had a period for at least 12 months.

In December 2003, a review of the available evidence on the risks and benefits of HRT by the Medicines and Healthcare products Regulatory Agency (MHRA) and the Committee on Safety of Medicines (CSM) in the UK, concluded that the risks of using HRT long-term to prevent osteoporosis in women aged over 50 years exceed the benefits. As a result, this medicine should not be used as a first-line option for preventing postmenopausal osteoporosis in women over 50. However, it may be used as a second-line option for women at high risk of fractures who cannot take other medicines that are licensed for preventing osteoporosis.

Women considered to be at risk of developing fractures following the menopause include those who have had an early menopause, those with a family history of osteoporosis, those who have had recent prolonged corticosteroid therapy (eg prednisolone), those with a small thin frame, and smokers.

  • Women taking any form of HRT should have regular medical and gynaecological check-ups. Your need for continued HRT should be reviewed with your doctor at least once a year.
  • A woman is considered fertile for two years after her last menstrual period if she is under 50, or for one year if over 50. HRT does not provide contraception for women who fall within this group. If a potentially fertile women is taking HRT but also requires contraception, a non-hormonal method (eg condoms) should be used.

     

Use with caution in
 

  • Close family history of breast cancer (eg mother, sister or grandmother has had the disease).
  • History of benign breast lumps (fibrocystic breast disease).
  • History of fibroids in the womb.
  • History of obesity.
  • Severe varicose veins.
  • Smokers.
  • History of high blood pressure (hypertension) -
  • History of migraines or severe headaches.
  • History of epilepsy.
  • History of asthma.
  • History of an ear disorder that may cause hearing loss (otosclerosis).
  • History of irregular brown patches appearing on the skin, usually of the face, during pregnancy or previous use of hormone preparations such as contraceptive pills (chloasma). Women with a tendency to this condition should minimise their exposure to the sun or UV light while taking HRT.

     

Contraindications:
 

  • Known, suspected, or past history of breast cancer.
  • Untreated overgrowth of the lining of the womb (endometrial hyperplasia).
  • Vaginal bleeding of unknown cause.
  • Women with a blood clot in a vein of the leg (deep vein thrombosis) or in the lungs (pulmonary embolism), or a past history of these conditions where the cause is unknown.
  • Women who have recently had a stroke caused by a blood clot.
  • Women who have recently had a heart attack.
  • Angina pectoris.
  • Active liver disease.
  • History of liver disease when liver function has not returned to normal.
     

The following medicines may potentially reduce the blood levels and effect of Angeliq, which could result in recurrence of symptoms or irregular bleeding:

 

  • antiepileptic medicines such as carbamazepine, phenytoin, phenobarbital and primidone
  • barbiturates such as amobarbital
  • nevirapine or efavirenz for HIV infection
  • protease inhibitors for HIV infection such as ritonavir and nelfinavir
  • rifamycin antibiotics such as rifabutin and rifampicin
  • the herbal remedy St John's wort (Hypericum perforatum).

     



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Answers to FAQs on women's health, patient information and medical advice by David A Viniker MD FRCOG, Consultant Obstetrician and Gynaecologist (Gynecologist - OBGYN), Department of Obstetrics and Gynaecology, Whipps Cross University Hospital, London

Premarin HRT
Women's Health