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Antiandrogens

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Spironolactone (Aldactone, Spiritone)

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Flutamide (Eulexin)

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Nilutamide (Anandron, Nilandron)

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Bicalutamide (Casodex)

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Ketoconazole (Nizoral)

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Bicalutamide

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Cyproterone

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Dienogest

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MDV3100

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5-alpha reductase inhibitors

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Finasteride

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Duasteride

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Gonadotropin-releasing hormone antagonist

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  • The body contains a hormone called Gonaderelin. Gonaderelin is a Gonadotropin-releasing hormone (GnRH).[1] GnRH is made by neurons in the hypothalamus. GnRH is also known as Luteinizing-hormone-releasing hormone (LHRH)[1][2]
  • LHRH acts on LHRH receptors in the pituitary gland,[1] causing luteinising hormone (LH) to be produced by the pituitary gland[1][3] in the brain.[3]
  • LH causes testosterone to be produced by the testes[1] (and by the adrenal glands?[3])
  • A GrNH antagonist binds to the LHRH receptors and stops the production of LH, which stops the production of testosterone

GnRH antagonists such as Degarelix block the LHRH receptors on the pituitary gland, stopping production of LH which in turn stops the production of testosterone. People who use Degarelix no longer produce testosterone.

As of 2005, Cetrorelix is mainly used for in vitro fertilization protocols, but research is currently being carried out in benign prostatic hypertrophy.[4] Ganirelix is only used in medically assisted procreation.[4] Abarelix is used in the United States as a monthly "depot" injection for the treatment of prostate cancer resistant to other therapies.[4] Other molecules including orally active antagonists are in the course of clinical evaluation or in preclinical phases. The development of this therapeutic class is hampered by conflicting industrial interests and also by problems of tolerability in particular because of the side effects due to induced histamine release.[4] The current indications in France are therefore limited to Assisted Reproductive Technology, and, recently, prostate cancer pending comparative studies versus agonists.[4] The indications under development are endometriosis, myoma and precocious puberty, fields in which agonists have already been found to be effective.[4] Male contraception seems to have a future however this therapeutic regimen remains very expensive.[4] Finally, in benign prostatic hypertrophy, the antagonists administrated intermittently may be used to rapidly improve urinary flow.[4]




Cetrorelix

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Ganirelix

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Abarelix

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Degarelix

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Gonadotropin-releasing hormone agonist aka LHRH analogues

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At a glance: Hypothalamus->GnRH/LHRH->pituitary gland->LH->testes->testosterone->5-alpha-reductase->dihydrotestosterone

  • The body contains a hormone called Gonaderelin. Gonaderelin is a Gonadotropin-releasing hormone (GnRH).[1] GnRH is made by neurons in the hypothalamus. GnRH is also known as Luteinizing-hormone-releasing hormone (LHRH)[1][2]
  • LHRH acts on LHRH receptors in the pituitary gland,[1] causing luteinising hormone (LH) to be produced by the pituitary gland[1][3] in the brain.[3]
  • LH causes testosterone to be produced by the testes[1] (and by the adrenal glands?[3])
  • A GrNH agonist binds to the LHRH receptors[1] and increases[1] the production of LH, which increases[1] the production of testosterone.
  • However, chronic administration of GrNH agonists desensitises the pituitary gland.[1] This means that it produces less and less LH.[1][3] In turn, that leads to a reduction in testosterone levels.[3][1]
  • When the administration of GrNH agonists is stopped, hormone levels return to normal.[5]

Buserelin

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Leuprorelin

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Triptorelin

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Histrelin

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Nafarelin

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Deslorelin

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Goserelin (Zoladex)

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How it works

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Sources[3][6][2][5][1]

  • The body contains a hormone called Gonaderelin. Gonaderelin is a Gonadotropin-releasing hormone (GnRH).[1] GnRH is also known as Luteinizing-hormone-releasing hormone (LHRH)[1][2]
  • LHRH acts on LHRH receptors in the pituitary gland,[1] causing luteinising hormone (LH) to be produced by the pituitary gland[1][3] in the brain.[3]
  • LH causes testosterone to be produced by the testes[1] (and by the adrenal glands?[3])
  • Zoladex contains the active ingredient goserelin acetate (aka Goserelin).[1]
  • Goserelin is an artificial analogue of (GnRH).[1] It acts on the LHRH receptors in the pituitary gland, in the same way as natural gonadorelin does.[1] So initially, goserelin causes the pituitary gland to increase production of LH.[1]
  • However, chronic administration of Goserelin desensitises the pituitary gland.[1] This means that it produces less and less LH.[1][3] In turn, that leads to a reduction in testosterone levels.[3][1]
  • When the medication is stopped, hormone levels return to normal.[5]

How it is given

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Zoladex is given by injection under the skin of the abdomen (subcutaneously).[3] It is given as an injection every four weeks,[3] or as a longer-acting preparation every 12 weeks.[3]

Side effects

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Blood-sugar levels increase

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If you are diabetic, your blood-sugar levels may be slightly higher than usual and may need more regular monitoring.[3]

Bone pain

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Bone pain[6]

Diabetes

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There may be an increased risk of developing heart disease or diabetes when taking Zoladex.[3]

Depression

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Depression[6]

Gynaecomastia

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Slight breast swelling and tenderness known as gynaecomastia.[3][6]

Headache

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Headache is common (1-10%)[6]

Heart disease

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There may be an increased risk of developing heart disease or diabetes when taking Zoladex.[3]

Hot flushes

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These can be quite common,[3] or very common (greater than 10%)[6] but many find that the hot flushes wear off after a period of time.[3] There are a number of ways to help reduce or control hot flushes and sweats.[3] Some find it helps to cut down on tea, coffee, nicotine and alcohol.[3] Hormones called progestogens[3] or some antidepressants[3] may be helpful in controlling hot flushes. Some find complementary therapies helpful.

Impotence

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Erection difficulties (impotence)[3][6] can occur. These effects often return to normal after stopping the drug.[3] Some find that these problems carry on after treatment is over.[3]

Libido

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Loss of sex drive (libido)[3][6] can occur. These effects often return to normal after stopping the drug.[3] Some find that these problems carry on after treatment is over.[3]

Osteoporosis (bone thinning)

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Osteoporosis[3][6] may occur if taking Zoladex for longer periods of time. It is accompanied by discomfort in your bones or joints.[3]

Skin rashes

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Some people experience skin rashes.[3][6]

Sore joints

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Some people may have soreness in their joints,[3][6] but this is usually mild and will stop when the treatment is finished.[3]

Tiredness

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You may notice that you gain weight and feel less energetic than usual. This usually improves when hormonal treatment stops.[3]

Temporary increase in testosterone levels

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There may be a temporary increase in testosterone levels[3] for the first few days of Zoladex treatment.[3] This increase may cause bone pain,[3] or problems passing urine.[3]

If used for prostate cancer, the temporary increase in testosterone levels may cause a temporary increase in the size of the tumour.[3] This is known as "tumour flare"[3] and is normal. It should improve in a few weeks.[3] Other types of hormonal therapy such as cyproterone acetate,[3] flutamide[3] or bicalutamide[3] may be given for the first few weeks of starting Zoladex to prevent tumour flare.

Weight gain

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You may notice that you gain weight and feel less energetic than usual. This usually improves when hormonal treatment stops.[3]

Summary

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Sources[7]

Criterion What does that mean? Value Notes
Protein binding Proteins in the bloodstream act as a sponge: chemicals that bind to them become inactive but then stay in the body longer and can seep out gradually after dosage stops. So the higher the percentage the longer it stays in the body 27.3%[7] It doesn't stay in the body long-term

Summary2

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Tradename INN Type SPC PIL Notes
Aldactazide Spironolactone Antiandrogen
Aldactone Spironolactone Antiandrogen [1] [2]
Anandron Nilutamide Antiandrogen
Androcur Cyproterone Antiandrogen
Antagon Ganirelix Gonadotropin-releasing hormone antagonist
Avodart Dutasteride 5-alpha-reductase inhibitor
Berlactone Spironolactone Antiandrogen
Calutide Bicalutamide Antiandrogen
Casodex Bicalutamide Antiandrogen
Casodex Bicalutamide Antiandrogen
Cetrotide Cetrorelix Gonadotropin-releasing hormone antagonist
CinnaFact Buserelin Gonadotropin-releasing hormone agonist
Ciproterona Cyproterone Antiandrogen
Cosudex Bicalutamide Antiandrogen
Cyprohexal Cyproterone Antiandrogen
Cyprone Cyproterone Antiandrogen
Cyprostat Cyproterone Antiandrogen
Cyproteron Cyproterone Antiandrogen
Cyproteronum Cyproterone Antiandrogen
Decapeptyl Triptorelin Gonadotropin-releasing hormone agonist
Diphereline Triptorelin Gonadotropin-releasing hormone agonist
Eligard Leuprorelin Gonadotropin-releasing hormone agonist
Eulexin Flutamide Antiandrogen
Firmagon Degarelix Gonadotropin-releasing hormone antagonist
Flutamin Flutamide Antiandrogen
Gonapeptyl Triptorelin Gonadotropin-releasing hormone agonist
Kalumid Bicalutamide Antiandrogen
Lupron Leuprorelin Gonadotropin-releasing hormone agonist
Metrelef Buserelin Gonadotropin-releasing hormone agonist
Neoproxil Cyproterone Antiandrogen
Nilandron Nilutamide Antiandrogen
Nizoral Ketoconazole Antiandrogen
not yet approved MDV3100 Antiandrogen
Novo-Spiroton Spironolactone Antiandrogen
Ovuplant Deslorelin Gonadotropin-releasing hormone agonist
Oxandrin Oxandrolone Antiandrogen
Plenaxis Abarelix Gonadotropin-releasing hormone antagonist
Procur Cyproterone Antiandrogen
Propecia Finasteride 5-alpha-reductase inhibitor
Proscar Finasteride 5-alpha-reductase inhibitor
Prostap Leuprorelin Gonadotropin-releasing hormone agonist [3][4] [5][6] [7]
Siterone Cyproterone Antiandrogen
Spiractin Spironolactone Antiandrogen
Spirotone Spironolactone Antiandrogen
Supprelin Histrelin Gonadotropin-releasing hormone agonist
Suprefact Buserelin Gonadotropin-releasing hormone agonist
Synarel Nafarelin Gonadotropin-releasing hormone agonist
Trelstar Triptorelin Gonadotropin-releasing hormone agonist
Vantax Histrelin Gonadotropin-releasing hormone agonist
Verospiron Spironolactone Antiandrogen
Viadur Leuprorelin Gonadotropin-releasing hormone agonist n/a n/a
Visanne Dienogest Antiandrogen n/a n/a Qlaira (a female contraceptive) includes dienogest as well as estradiol valerate
Zoladex Goserelin Gonadotropin-releasing hormone agonist [8] [9] [10]

Summary3

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INN/USAN Type NHS Choices eMC Guides eMC NDO NELM PubMed Method Freq Notes
Abarelix Gonadotropin-releasing hormone antagonist ? ? ? [11] ? [12] ? ?
Bicalutamide Antiandrogen [13] [14] [15] ? [16] [17] Tablet Once a day
Buserelin or Buserelin acetate Gonadotropin-releasing hormone agonist [18] [19] [20] ? [21] [22] Injection Once a day
Cetrorelix or Cetrorelix acetate Gonadotropin-releasing hormone antagonist [23] [24] [25] [26] [27] [28] Injection Once a day
Cyproterone or Cyproterone acetate Antiandrogen [29] [30] [31] ? [32] [33] Tablet Twice a day
Degarelix Gonadotropin-releasing hormone antagonist ? ? [34] [35] [36] [37] Injection Once a month
Deslorelin or Deslorelin acetate Gonadotropin-releasing hormone agonist ? ? ? ? ? [38] ? ?
Dienogest Antiandrogen ? ? [39] [40] ? [41] Tablet Once a day
Dutasteride 5-alpha-reductase inhibitor [42] [43] [44] ? [45] [46] Tablet Once a day
Epristeride 5-alpha-reductase inhibitor ? ? ? ? ? [47] ? ?
Finasteride 5-alpha-reductase inhibitor [48] [49] [50] ? [51] [52] Tablet Once a day
Flutamide Antiandrogen ? ? ? ? [53] [54] ? ?
Ganirelix or Ganirelix acetate or Ganirelix diacetate Gonadotropin-releasing hormone antagonist ? [55] [56] ? [57] [58] Injection Once a day
Goserelin or Goserelin acetate Gonadotropin-releasing hormone agonist [59] [60] [61] ? [62] [63] Injection Once every three months
Histrelin or Histrelin acetate Gonadotropin-releasing hormone agonist ? [64] [65] [66] [67] [68] Implant Once a year
Ketoconazole Antiandrogen [69] [70] [71] ? [72] [73] ? ?
Leuprorelin or Leuprolide acetate or Leuprorelin acetate Gonadotropin-releasing hormone agonist [74] [75] [76] ? [77] [78] Injection Once every three months
MDV3100 Antiandrogen ? ? ? [79] ? [80] ? ?
Nafarelin or Nafarelin acetate Gonadotropin-releasing hormone agonist [81] [82] [83] ? [84] [85] Nasal Twice a day
Nilutamide Antiandrogen ? ? ? [86] ? [87] ? ?
Oxandrolone Antiandrogen ? ? ? ? [88] [89] ? ?
Spironolactone Antiandrogen [90] [91] [92] ? [93] [94] Tablet Once a day
Triptorelin or Triptorelin acetate or Triptorelin pamoate Gonadotropin-releasing hormone agonist [95] [96] [97] [98] [99] [100] Injection Once every six months


Abarelix

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  • Developmental Status: UK: None, EU: Launched, US: Discontinued, UK launch Plans: Available only to registered users, Actual UK launch date: none
  • Probably not reasonably available in UK

Bicalutamide

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  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • are female
  • have liver problems
  • Side-effects
  • Very common: breast enlargement in men, breast pain or tenderness, skin rash or rashes, weakness
  • Common: abnormal laboratory test results, anaemia, blood in the urine, chest pain, constipation, decreased libido, depression, dry skin,erectile dysfunction, feeling dizzy, flatulence, hair loss, hair overgrowth or hair regrowth, hot flushes, indigestion, itching liver problems - some of these may be fatal. Seek medical advice if you develop jaundice - loss of appetite, nausea, oedema, sleepiness, stomach pain, weight gain
  • Uncommon: angioedema, hypersensitivity reactions, lung problems - some of these may be fatal, urticaria
  • 5.3 Preclinical safety data
  • Bicalutamide is a pure and potent androgen receptor antagonist in experimental animals and humans. The main secondary pharmacological action is induction of CYP 450 dependent mixed function oxidases in liver. Enzyme induction has not been observed in humans. Target organ changes, including tumour induction (Leydig cells, thyroid, liver) in animals, are clearly related to the primary and secondary pharmacological action of bicalutamide. Enzyme induction has not been observed in man and none of these findings is considered to have relevance to the treatment of patients with prostate cancer. Atrophy of seminiferous tubules is a predicted class effect with anti-androgens and has been observed for all species examined. Full reversal of testicular atrophy was 24 weeks after a 12 month repeated dose toxicity study in rats, although functional reversal was evident in reproduction studies 7 weeks after the end of an 11 week dosing period. A period of subfertility or infertility should be assumed in man. Genotoxicity studies did not reveal any mutagenic potential of bicalutamide.

Buserelin

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  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are allergic or sensitive to or have had a bad reaction to benzalkonium chloride and luteinizing hormone releasing hormone in the past
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • are breast-feeding
  • are pregnant
  • have depression
  • have diabetes
  • have had your testicles removed
  • have high blood pressure
  • have prostate cancer which is not sensitive to hormones
  • have risk factors for osteoporosis such as: family history of osteoporosis, drinking alcohol heavily or smoking
  • Side-effects
  • Very common:
  • Common:
  • Uncommon:
  • Rare:
  • Unknown: abnormal laboratory test results, acne, appetite changes, blood problems, breast enlargement in men, changes to smell and taste, changes to weight, concentration problems, constipation, decreased libido, depression or worsening of depression, diarrhoea, dry eyes - your eyes may become irritated if you wear contact lenses - dry skin, eye or eyesight problems, face oedema, feeling anxious, feeling dizzy, feeling drowsy, feeling nervous, feelings of pressure behind the eye, hair loss, hair overgrowth, headaches, hearing problems, hoarse voice, hot flushes, hypersensitivity reactions such as redness of the skin, itching, skin rashes, urticaria, breathing problems, allergic asthma, or anaphylaxis which may lead to shock, impotence, lowering of bone mineral density - this may lead to osteoporosis or bone fracture, memory problems, mood changes, nail problems, nausea, nose and throat irritation, nose bleed, oedema of the extremities, pain or stiffness of the muscles or joints, palpitations, paraesthesiae, reduced glucose tolerance - people with diabetes may need to adjust their anti-diabetic therapy - sleeping problems, stomach pain, testicular problems, thirst, tinnitus, tiredness, tumours, vomiting, worsening of cancer symptoms at the beginning of treatment such as tumour pain, worsening of bone pain if you have cancer which has spread to your bones, kidney problems, neurological problems such as weakness of leg muscles, difficulty urinating, thromboembolism or a general feeling of being unwell, worsening of diabetes, worsening of raised blood pressure
  • eMC: [110]
  • NDO: ?
  • NELM: [111]
  • PubMed: [112]
  • Method: Injection
  • Freq: Once a day
  • Notes: not advisable: too many side effects, no info on reversibility, injection once a day

Cetrorelix

[edit]
  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are allergic or sensitive to or have had a bad reaction to gonadotrophin releasing hormone or substances similar to gonadotrophin releasing hormone in the past
  • are allergic or sensitive to or have had a bad reaction to protein-containing hormones in the past
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • are breast-feeding
  • are postmenopausal
  • are pregnant
  • are prone to allergies
  • have kidney problems
  • have liver problems
  • have or have had an allergic disease
  • Side-effects
  • Very common:
  • Common: injection site problems such as redness, itching and swelling, ovarian hyperstimulation syndrome
  • Uncommon: headaches, hypersensitivity reactions including allergies or anaphylactic reactions - some of these may be fatal. Seek immediate medical advice if you develop anaphylactic or allergic reactions - nausea
  • Rare:
  • Unknown:
  • 5.3 Preclinical safety data: Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity to reproduction. No target organ toxicity could be observed from acute, subacute and chronic toxicity studies in rats and dogs following subcutaneous administration of cetrorelix. No signs of medicinal product-related local irritation or incompatibility were noted in dogs after intravenous, intra-arterial and paravenous injection when cetrorelix was administered in doses clearly above the intended clinical use in man. Cetrorelix showed no mutagenic or clastogenic potential in gene and chromosome mutation assays.
  • Developmental Status: UK: Discontinued, EU: Discontinued, US: Discontinued, UK launch Plans: Available only to registered users, Actual UK launch date: n/a
  • Comments: Dec 09: Further development unlikely following failure of 2 PIII studies [10].
  • NELM: [117]
  • PubMed: [118]
  • Method: Injection
  • Freq: Once a day
  • Notes: Few known side-effects, but no studies in men. Unsuitable because of delivery system and not available in UK anyway

Cyproterone

[edit]
  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • have a cancer other than prostate cancer
  • have a wasting disease
  • have depression
  • have diabetes
  • have Dubin-Johnson syndrome
  • have liver disease
  • have or have had a meningioma
  • have or have had liver tumours
  • have or have had thromboembolic problems such as a heart attack, a stroke, pulmonary embolism or deep vein thrombosis
  • have Rotor syndrome
  • have sickle cell anaemia
  • Side-effects
  • Very common: decreased libido, erectile dysfunction, inhibition of gonadal function, reduced sexual drive, reduced sperm production and volume of semen - these may lead to fertility problems
  • Common: a feeling of lack of interest or lack of energy, breast enlargement, and tenderness, breathing difficulties, changes to weight, depressed mood - you or your carer must seek immediate medical advice if your depression worsens, feeling restless, hot flushes, liver problems including jaundice - seek immediate medical advice if you develop jaundice. Some liver problems may be fatal - sweating, tiredness
  • Uncommon: skin rash or rashes
  • Rare: benign breast lumps, galactorrhoea, hypersensitivity reactions
  • Unknown: adrenal problems, blood problems, changes in carbohydrate tolerance - this may lead to changes in diabetic control - dry skin, hair problems including loss of body hair, increased growth of scalp hair, female pattern pubic hair growth or lighter hair colour, improvement in existing acne, meningioma, osteoporosis, thromboembolism
  • Side-effects
  • Very common: Decreased libido, erectile dysfunction, reduced sexual drive and inhibition of gonadal function. These changes are reversible after discontinuation of therapy.
  • Common: Direct hepatic toxicity, including jaundice, hepatitis and hepatic failure has been observed in patients treated with Cyprostat. At dosages of 100 mg and above, cases with fatal outcome have also been reported. Most reported fatal cases were in men with advanced carcinoma of the prostate. Toxicity is dose related and develops, usually, several months after treatment has begun.
  • NDO: ?
  • NELM: [122]
  • PubMed: [123]
  • Method: Tablet
  • Freq: Twice a day
  • Notes: Binds to plasma proteins heavily, heavily liver toxic, good reversibility. Not recommended by me for long-term use

Degarelix

[edit]
  • Side-effects
  • Very common: Hot flushes, injection site pain and redness.
  • Common: Gynaecomastia*, testicular atrophy*, erectile dysfunction*, Musculoskeletal pain and discomfort, Hyperhidrosis (incl. night sweats)* , rash, Liver transaminases increased, Weight increase*, Anaemia*, injection site swelling, node and hardness • chills, fever or influenza-like illness after the injection • trouble sleeping, tiredness, weakness, dizziness, headache • increased weight, nausea, elevated levels of some liver enzymes • excessive sweating (including night sweats)
  • Uncommon: testicular pain, breast pain, pelvic pain, genital irritation, ejaculation failure, Osteoporosis/osteopenia, arthralgia, muscular weakness, muscle spasms, joint swelling/stiffness, Urticaria, skin nodule, alopecia, pruritus, erythema, Bilirubin increased, alkaline phosphatase increased, Hyperglycemia/Diabetes mellitus, cholesterol increased, weight decreased, appetite decreased, changes in blood calcium, loss of sexual desire, impotence, reduced size of testicles, testicular pain, breast swelling, pelvic pain, prostatitis (inflammation of the prostate gland), prostate tenderness, backwards ejaculation (ejaculation to urinary bladder) • depression, anxiety • rash, skin redness, locally changed skin color, loss of hair, soft nails • allergic reactions, hives • cough • decreased appetite, constipation, diarrhoea, vomiting, dry mouth, abdominal discomfort • anaemia • high blood pressure, changes in ECG (1st degree atrio-ventricular block, QT-prolongation), fainting • varicose vein (enlarged and twisted vein), localised oedema (localised swelling) • musculoskeletal pain, muscular weakness • frequent urination, urinary urgency (must hurry to pass urine), impaired renal function, decreased weight • tinnitus
  • Rare
  • Unknown
  • Plasma binding: Plasma protein binding is estimated to be approximately 90%.
  • 5.3 Preclinical safety data: Animal reproduction studies showed that degarelix caused infertility in male animals. This is due to the pharmacological effect; and the effect was reversible. Preclinical studies on safety pharmacology, repeated dose toxicity, genotoxicity, and carcinogenic potential revealed no special hazard for humans. Both in vitro and in vivo studies showed no signs of QT prolongation. No target organ toxicity was observed from acute, subacute and chronic toxicity studies in rats and monkeys following subcutaneous administration of degarelix. Drug-related local irritation was noted in animals when degarelix was administered subcutaneously in high doses.
  • Developmental Status: UK: Launched, EU: Launched, US: Launched, UK launch Plans: Available only to registered users, Actual UK launch: 1/05/2009
  • NELM: [126]
  • PubMed: [127]
  • Method: Injection
  • Freq: Once a month
  • Notes: Few side effects, injected once a month, reversible, available in UK, *but* few studies, 90% plasma protein binding, and may only be available for advanced hormone-dependent prostate cancer in adult men

Deslorelin

[edit]

Dienogest

[edit]
  • Developmental Status: UK: Approved (Licensed), EU: Approved (Licensed), US: None, UK launch Plans: Available only to registered users, Actual UK launch date: ?
  • Comments: Dec 09: Approved in the EU for treatment of endometriosis (3). 25/01/2010 17:15:51
  • NELM: ?
  • PubMed: [131]
  • Method: ?
  • Freq: ?
  • Notes: Only available as Qlaira, a contraceptive pill, which also contains estradiol valerate. No data on males. Not suitable at this stage

Dutasteride

[edit]
  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are allergic or sensitive to or have had a bad reaction to 5-alpha reductase inhibitors in the past
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • have kidney problems
  • have liver problems
  • Side-effects
  • Very common:
  • Common: breast enlargement or tenderness, decreased libido, ejaculation problems, impotence
  • Uncommon:
  • Rare:
  • Unknown: allergic reactions including rash, itching, urticaria and angioedema, heart problems,
  • Side-effects
  • Very common:
  • Common: • impotence (not able to achieve or maintain an erection) • decreased sex drive (libido) • difficulty with ejaculation • breast enlargement or tenderness (gynecomastia) • dizziness when taken with tamsulosin.
  • Uncommon:
  • Rare:
  • Unknown: • skin rash (which can be itchy) • hives (like a nettle rash) • swelling of the eyelids, face, lips, arms or legs.
  • NDO: ?
  • NELM: ignored for speed purposes
  • PubMed: ignored for speed purposes
  • Method: Tablet
  • Freq: Once a day
  • Notes: A bit meh: reversible, but so what

Epristeride

[edit]

Finasteride

[edit]
  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are a man who is likely to father a child
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • are female
  • are taking finasteride, one of the ingredients in Propecia, for other medical problems
  • have galactose intolerance
  • have glucose-galactose malabsorption problems
  • have Lapp lactase deficiency
  • have liver problems
  • Side-effects
  • Very common:
  • Common: decreased libido, ejaculation problems, erectile dysfunction,
  • Uncommon:
  • Rare:
  • Very rare:
  • Unknown: abnormal laboratory test results, breast cancer - seek immediate medical advice if you have changes in your breast such as breast enlargement, breast pain or tenderness, lumps or nipple discharge - hypersensitivity reactions including rash, itching, urticaria and swelling of the lips and face, infertility, may affect the results for certain tests, pain in the testes, palpitations
  • 4.8 Undesirable effects
  • The most common adverse effects are impotence and reduced libido. These effects usually occur at the beginning of the treatment and in the majority of patients are of a transient nature on continued treatment
  • Side-effects
  • Very common: Impotence
  • Common: Reduced libido, Reduced volume of ejaculate, ejaculation disorder (e.g. decrease volume of ejaculate), Tenderness of the male breast / gynecomastia, Skin rash
  • Uncommon: Testicular pain
  • Rare: Pruritus, Urticaria, Hypersensitivity reactions such as swelling of the face and lips
  • Very rare: Breast secretion, Breast nodules
  • Unknown: Somnolence
  • NDO: ?
  • NELM: ignored for speed purposes
  • PubMed: ignored for speed purposes
  • Method: Tablet
  • Freq: Once a day
  • Notes: Meh. May be worth switching to duasteride from this

Flutamide

[edit]

Ganirelix

[edit]
  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • are allergic to gonadotrophin releasing hormone or substances similar to gonadotrophin releasing hormone
  • are breast-feeding
  • are pregnant
  • have an allergic disease
  • have kidney problems
  • have liver problems
  • Side-effects
  • Very common: injection site problems such as redness or swelling
  • Common:
  • Uncommon: general feeling of being unwell, headaches, nausea
  • Rare:
  • Very rare: hypersensitivity reactions such as skin rashes, facial swelling and breathing difficulties, worsening of eczema
  • Unknown: distension of the stomach, ectopic pregnancy, miscarriage, ovarian hyperstimulation syndrome, pelvic pain
  • Side-effects
  • Very common: injection site problems such as redness or swelling
  • Common: local skin reactions at the site of injection (predominantly redness, with or without swelling). The local reaction normally disappears within 4 hours of administration.
  • Uncommon: headache, nausea and malaise.
  • Very rare: more widespread possibly allergic reactions, cases of hypersensitivity reactions including various symptoms such as rash, facial swelling and dyspnoea have been reported among patients administered with Orgalutran. Worsening of a pre-existing eczema has been reported in one subject after the first Orgalutran dose.
  • Unknown: In addition, side effects are reported which are known to occur with controlled ovarian hyperstimulation treatment (e.g. abdominal pain, ovarian hyperstimulation syndrome (OHSS), ectopic pregnancy (when the embryo develops outside the womb) and miscarriage (see the patient information leaflet of the FSH-containing preparation you are treated with)).
  • NDO: ?
  • NELM: ignored for speed purposes
  • PubMed: ignored for speed purposes
  • Method: Injection
  • Freq: Once a day
  • Notes: Few side effects, but no data on reversibility, use in males, and the delivery system is useless

Goserelin

[edit]
  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • have bone problems
  • have diabetes
  • have or have had depression
  • have or have had high blood pressure
  • have risk factors for developing problems with your spinal cord or kidneys
  • have risk factors for osteoporosis such as: a family history of osteoporosis, drinking alcohol heavily or smoking
  • Side-effects
  • Very common: decreased libido, erectile dysfunction, hot flushes, sweating
  • Common: blood pressure changes, breast enlargement in men, heart attack, heart problems, injection site problems, lowering of bone mineral density, paraesthesiae, reduced glucose tolerance - people with diabetes may need to adjust their anti-diabetic therapy - skin rash or rashes, worsening of cancer symptoms at the beginning of treatment - you may get bone pain or problems with your spinal cord or kidneys
  • Uncommon: breast tenderness, hypersensitivity reactions, joint pain
  • Rare: anaphylactic reactions
  • Very rare: pituitary gland problems, psychosis or psychotic-like behaviour
  • Unknown: abnormal laboratory test results, depression, diabetes, liver problems, may affect the results for certain tests, mood changes, pneumonia, pulmonary embolism
  • Side-effects
  • Very common: Libido decreased, Hot flush, Hyperhidrosis, Erectile dysfunction
  • Common: Glucose tolerance impaired, Paraesthesia, Spinal cord compression, Cardiac failure, myocardial infarction, Blood pressure abnormal, Rash, Bone pain, Gynaecomastia, Injection site reaction, Bone density decreased (see section 4.4)
  • Uncommon: Drug hypersensitivity, Arthralgia, Ureteric obstruction, Breast tenderness
  • Rare: Anaphylactic reaction
  • Very rare: Pituitary tumour, Pituitary haemorrhage, Psychotic disorder
  • Unknown: Mood altered, depression
  • 5.2 Pharmacokinetic properties
  • Administration of Zoladex LA every 12 weeks ensures that exposure to goserelin is maintained with no clinically significant accumulation. Zoladex is poorly protein bound and has a serum elimination half-life of two to four hours in subjects with normal renal function. The half-life is increased in patients with impaired renal function. For the compound given in a 10.8 mg depot formulation every 12 weeks this change will not lead to any accumulation. Hence, no change in dosing is necessary in these patients. There is no significant change in pharmacokinetics in patients with hepatic failure.
  • 5.3 Preclinical safety data
  • Following long-term repeated dosing with Zoladex, an increased incidence of benign pituitary tumours has been observed in male rats. Whilst this finding is similar to that previously noted in this species following surgical castration, any relevance to humans has not been established. In mice, long-term repeated dosing with multiples of the human dose produced histological changes in some regions of the digestive system. This is manifested by pancreatic islet cell hyperplasia and a benign proliferative condition in the pyloric region of the stomach, also reported as a spontaneous lesion in this species. The clinical relevance of these findings is unknown.
  • NDO: ?
  • NELM: ignored for speed purposes
  • PubMed: ignored for speed purposes
  • Method: Injection
  • Freq: Once every three months
  • Notes: Good delivery system, stacks of side effects, no notes on reversibility

Histrelin

[edit]
  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are allergic or sensitive to or have had a bad reaction to latex, LHRH or LHRH analogues in the past
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • are female
  • have diabetes
  • have kidney problems
  • have liver problems
  • have risk factors for developing cardiovascular problems
  • have risk factors for developing metabolic problems
  • Side-effects
  • Very common: hot flushes
  • Common: blushing, breast enlargement in men, constipation, decreased libido, depression, difficulty sleeping, erectile dysfunction, exercise induced shortness of breath, feeling dizzy, hair overgrowth, headaches, increased blood sugar levels, injury or reactions at the implantation site including: redness, tenderness, swelling, inflammation, pain or the squeezing out of the implant from the implantation site, joint pain, kidney problems, liver problems, painful extremities, testicular atrophy, tiredness, urinary retention, urinating more or more often, weakness, weight gain
  • Uncommon: abnormal laboratory test results, anaemia, appetite gain, back pain, blood in the urine, breast pain or tenderness, bruising, collection of blood under the skin, feeling irritable, fluid retention, food cravings, general feeling of being unwell, genital itching, heart problems, high levels of cholesterol or other lipids in the blood, itching, kidney stones, lethargy, metabolic problems such as glucose intolerance or worsening of diabetes, muscle problems, muscle spasm, nausea, neck pain, night sweats, oedema of the extremities, pain, painful urination, palpitations, sensation of cold, sexual dysfunction, stent blockage, stomach discomfort, sweating, tremors, weight loss, worsening of pain
  • Rare: skin infections
  • Unknown: increased risk of bone fractures, lowering of bone mineral density - this may lead to osteoporosis - worsening of cancer symptoms at the beginning of treatment - these may include joint pain, bone pain, neuropathy, blood in the urine, urinary retention, weakness, paraesthesiae or paralysis. Your prescriber may give you other medicines at the beginning of your treatment with Vantas to help prevent the worsening of symptoms
  • 4.8 Undesirable effects: See above
  • 5.2 Pharmacokinetic properties: The fraction of drug unbound in plasma measured in vitro was 29.5 % ± 8.9 % (mean value ± SD).
  • 5.3 Preclinical safety data: Administration of histrelin in laboratory animals was associated with atrophy of reproductive organs and reduced fertility. This is due to the pharmacological effect and full reversibility was demonstrated after cessation of administration.
  • Developmental Status: UK: Launched, EU: Launched, US: Launched, UK launch Plans: Available only to registered users, actual UK launch date: 01/07/2009
  • Comments: Jul 09: Vantas implant launched in the UK for the palliative treatment of advanced prostate cancer (7,8). 29/06/2009 14:06:37
  • NELM: ignored for speed purposes
  • PubMed: ignored for speed purposes
  • Method: Implant
  • Freq: Once a year
  • Notes: Good reversibility, good delivery system, available in UK.

Ketoconazole

[edit]

Leuprorelin

[edit]
  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are allergic or sensitive to or have had a bad reaction to gonadotrophin releasing hormone or substances similar to gonadotrophin releasing hormone in the past
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • have cancer which has spread to your spine
  • have depression
  • have diabetes
  • have pituitary gland tumours
  • have risk factors for developing problems with your spinal cord or kidneys
  • have urinary problems
  • Side-effects
  • Very common:
  • Common:
  • Uncommon:
  • Rare:
  • Very rare:
  • Unknown: abnormal laboratory test results, anaphylactic reactions, anorexia, blood problems, breast enlargement in men, changes in glucose tolerance - this may lead to or worsen diabetes, changes to weight, chills, decreased libido, depression or worsening of depression, diarrhoea, difficulty sleeping, eye or eyesight problems, feeling dizzy, fever, headaches, hot flushes, hypersensitivity reactions including skin rashes, itching, urticaria, wheezing, or lung problems, impotence, injection site problems such as irritation, jaundice, joint pain, liver problems, lowered blood pressure, lowering of bone mineral density, metabolic problems, muscle pain or tenderness, muscle weakness, nausea, oedema of the extremities, palpitations, paraesthesiae, paralysis, pulmonary embolism, raised blood pressure, spinal fractures, sweating, testicular problems, tiredness, vomiting, worsening of cancer symptoms at the beginning of treatment such as bone pain, neurological problems or urinary problems, worsening of pituitary problems
  • 4.8 Undesirable effects
  • "Expected" (Very common?): Impotence and decreased libido
  • "Often" (Common?): hot flushes and sometimes sweating.
  • "Occasionally" (Uncommon?): Orchiatrophy and gynaecomastia
  • Rare: Thrombocytopenia and leucopenia, Anaphylactic reactions
  • Very rare: cases of pituitary apoplexy have been reported following initial administration in patients with pituitary adenoma.
  • "infrequently"/"may occur" (unknown?): A reduction in bone mass, peripheral oedema, pulmonary embolism, hypertension, palpitations, fatigue, muscle weakness, diarrhoea, nausea, vomiting, anorexia, fever/chills, headache (occasionally severe), hot flushes, arthralgia, myalgia, dizziness, insomnia, depression, paraesthesia, visual disturbances, weight changes, hepatic dysfunction, jaundice, increases in liver function test values (usually transient) and irritation at the injection site. Changes in blood lipids and alteration of glucose tolerance have also been reported which may affect diabetic control. Hypersensitivity reactions including rash, pruritis, urticaria and, rarely, wheezing or interstitial pneumonitis have also been reported. Spinal fracture, paralysis, hypotension and worsening of depression have been reported (see 'Special Warnings and Precautions for Use' section 4.4).
  • Note: In cases where a "tumour flare" occurs after PROSTAP therapy, an exacerbation may occur in any symptoms or signs due to disease, for example, bone pain, urinary obstruction, weakness of the lower extremities and paraesthesia. These symptoms subside on continuation of therapy.
  • NDO: ?
  • NELM: ignored for speed purposes
  • PubMed: ignored for speed purposes
  • Method: Injection
  • Freq: Once every three months
  • Notes: Good delivery, no info on reversibility, impostence/decreased libido is expected

MDV3100

[edit]
  • Developmental Status: UK: Phase III Clinical Trials, EU: Phase III Clinical Trials, US: Phase III Clinical Trials, UK launch Plans: Available only to registered users, Actual UK launch date: n/a
  • NELM: ignored for speed purposes
  • PubMed: ignored for speed purposes
  • Method: ?
  • Freq: ?
  • Notes: Not yet past clinical trial stage

Nafarelin

[edit]

Nilutamide

[edit]
  • Developmental Status: UK: None, EU: Launched, US: Launched, UK launch Plans: Available only to registered users, Actual UK launch date:
  • Comments: In the US, nilutamide is indicated for use in combination with surgical castration for treating metastatic prostate cancer (3).21/05/2010 16:00:26. Launched in EU in Dec 96. Not marketed in UK. (2) 09/04/2009 12:41:49
  • NELM: ignored for speed purposes
  • PubMed: ignored for speed purposes
  • Method: ?
  • Freq: ?
  • Notes: Not released in UK

Oxandrolone

[edit]

Spironolactone

[edit]
  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are about to have a procedure under general or local anaesthesia
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • are elderly
  • are not passing any urine
  • have Addison's disease
  • have kidney problems
  • have liver problems
  • have metabolic problems
  • Side-effects
  • Very common:
  • Common:
  • Uncommon:
  • Rare:
  • Very rare:
  • Unknown: abnormal laboratory test results, benign breast tumours, blood and bone marrow problems, breast enlargement in men, breast pain or discomfort, changes in libido, confusion, dizziness, gastrointestinal problems, general feeling of being unwell, hair loss, hair overgrowth, itching, kidney problems, leg cramps, liver problems, may affect the results for certain tests, menstrual problems, metabolic problems - some of these metabolic problems may lead to heart problems in certain people which may be fatal - nausea, skin rash or rashes, Stevens-Johnson syndrome, urticaria
  • 4.8 Undesirable effects
  • Very common:
  • Common: gastritis, gastric bleeding, stomach cramps, diarrhoea, vomiting and ulceration
  • Uncommon: ataxia, drowsiness, dizziness, headache and clumsiness
  • Rare: agranulocytosis, eosinophilia and thrombocytopenia, Hyperkalemia (severe hyperkalaemia may result in paralysis, flaccid paraplegia and cardiac arrhythmias with subsequent cardiovascular collapse. This can be fatal in patients with impaired renal function). Hyponatraemia. Hypersensitivity occur rarely and are usually mild but very occasionally may be severe causing swelling, shock and collapse. Shortness of breath, skin rash or itching. Urticaria and alopecia. Gynaecomastia may develop in association with the use of spironolactone. Development appears to be related to both dosage level and duration of therapy and is usually reversible once therapy is discontinued. In rare instances some breast enlargement may persist. Alteration in voice pitch may also occur on rare occasions which may not be reversible.
  • Very rare:
  • Unknown: transient elevations in blood urea nitrogen (BUN) especially in patients with renal impairment, Electrolyte disturbances, lethargy, hepatotoxicity, Skin rashes. Osteomalacia. Acute renal failure, particularly in those with pre-existing renal impairment. Impotence and decreased sexual ability has been reported (This is usually reversible on discontinuation of spironolactone). Breast tenderness and increased hair growth in females, irregular menstrual periods and sweating have been reported.
  • 5.2 Pharmacokinetic properties: Distribution – Although the plasma half life of spironolactone itself is short (1.3 hours) the half lives of the active metabolites are longer (ranging from 2.8 to 11.2 hours). Spironolactone is estimated to be 90% protein bound. Volume of distribution, extent of tissue accumulation and ability to cross the blood brain barrier are not known. Spironolactone or its metabolites may cross the placental barrier and canrenone is secreted breast milk.
  • NDO: ?
  • NELM: ignored for speed purposes
  • PubMed: ignored for speed purposes
  • Method: Tablet
  • Freq: Once a day
  • Notes: Reversible, good delivery. However, protein binding is huge, and it can cause a buildup of potassium and liver damage

Triptorelin

[edit]
  • Contraindications. Your prescriber may only prescribe this medicine with special care or may not prescribe it at all if you:
  • are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
  • have cancer which has spread to your spine
  • have had your testicles removed
  • have problems with your spinal cord
  • have prostate cancer which is not sensitive to hormones
  • Side-effects
  • Very common: decreased libido, hot flushes, impotence
  • Common: breast enlargement in men, feeling irritable, feelings of depression, headaches, hypersensitivity reactions such as itching, skin rashes or fever, injection site problems such as pain, joint pain, muscle pain or tenderness, nausea, sleeping problems, sweating, tiredness
  • Uncommon: abnormal laboratory test results, anaphylactic reactions, changes to weight, dry mouth, hair loss, loss of appetite, raised blood pressure, reduced growth of facial hair, stomach pain, testicular problems, thromboembolism, worsening of asthma
  • Rare:
  • Very rare:
  • Unknown: bone problems, lowering of bone mineral density, worsening of cancer symptoms at the beginning of treatment - seek immediate medical advice if you get urinary problems, kidney problems, bone pain, problems with your spinal cord, muscle tiredness, weakness, paraesthesiae or leg oedema
  • 4.8 Undesirable effects
  • Very common: Hot flush
  • Common: Asthenia, Dizziness, Erectile dysfunction, Fatigue, Headache, Injection site reaction, Loss of libido, musculoskeletal pain, Nausea, Oedema, Pain in extremity
  • Uncommon: Abdominal pain, Acne, Alanine aminotransferase increased, Alopecia, Anorexia, Arthralgia, Aspartate aminotransferase increased, Blood creatinine increased, Blood urea increased, Breast pain, Constipation, Depression, diarrhoea, Dyspnoea, Gout, Gynaecomastia, Hyperhidrosis, Hypertension, Increased appetite, Insomnia, Irritability, Lethargy, Mood swings, Muscle cramp, Muscular weakness, Myalgia, Pain, Paraesthesia, Pruritus, Rash, Rigors, Somnolence, Testicular atrophy, Testicular pain, Tinnitus, Vomiting, Weight increased
  • Rare: Abdominal distension, Abnormal sensation in eye, Anaphylactic reaction, Blister, Blood alkaline phosphatase increased, Body temperature increased, Chest pain, Confusional state, Decreased activity, Diabetes mellitus, Dry mouth, Dysgeusia, Dysstasia, Ejaculation failure, Epistaxis, Euphoric mood, Flatulence, Hypersensitivity, Hypotension, Influenza like illness, Joint stiffness, Joint swelling, Memory impairment, Musculoskeletal stiffness, Nasopharyngitis, Orthopnoea, Osteoarthritis, Purpura, Pyrexia, Vertigo, Visual disturbance, Weight decreased
  • 5.1 Pharmacodynamic properties
  • Once the castration levels of testosterone have been achieved by the end of the first month, serum testosterone levels are maintained for as long as the patients receive their injection according to the recommended posology. This results in accessory sexual organ atrophy. These effects are generally reversible upon discontinuation of the medicinal product. The effectiveness of treatment can be monitored by measuring serum levels of testosterone and prostate specific antigen. As shown during the clinical trial programme, there was a 97% median relative reduction in PSA at Month 6 for Decapeptyl SR 22.5mg.
  • 5.2 Pharmacokinetic properties
  • Since there is no evidence that triptorelin at clinically relevant concentrations binds to plasma proteins, medicinal productinteractions involving binding-site displacement are unlikely.
  • UK: None, EU: Launched, US: Pre-registration (Filed), UK launch Plans: Available only to registered users, Actual UK launch date: n/a
  • NELM: ignored for speed purposes
  • PubMed: ignored for speed purposes
  • Method: Injection
  • Freq: Once every six months
  • Notes: good delivery, good side effects, (probably) reversible. May not be available in UK

References

[edit]
  1. ^ a b c d e f g h i j k l m n o p q r s t u v w x y z aa ab ac Zoladex (goserelin), http://www.netdoctor.co.uk
  2. ^ a b c d GENERIC NAME: GOSERELIN - INJECTION (go-SIR-eh-lin) BRAND NAME(S): Zoladex http://www.medicinenet.com/goserelin-injection/article.htm
  3. ^ a b c d e f g h i j k l m n o p q r s t u v w x y z aa ab ac ad ae af ag ah ai aj ak al am an ao ap aq ar as at au av aw ax Goserelin for prostate cancer (Zoladex®), http://www.macmillan.org.uk
  4. ^ a b c d e f g h [GnRH antagonists: present and future
  5. ^ a b c Goserelin: MedlinePlus Drug Information
  6. ^ a b c d e f g h i j k Goserelin, http://www.patient.co.uk
  7. ^ a b Protein binding, Wiki page on plasma binding
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