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Flutamide

Posted by admin on July 20th, 2010 No Comments

(British Approved Name, US Adopted Name, rINN)

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: Flutamid; Flutamida; Flutamidas; Flutamidi; Flutamidum; Sch-13521
BAN: Flutamide
USAN: Flutamide
INN: Flutamide [rINN (en)]
INN: Flutamida [rINN (es)]
INN: Flutamide [rINN (fr)]
INN: Flutamidum [rINN (la)]
INN: Флутамид [rINN (ru)]
Chemical name: α´,α´,α´-Trifluoro-4´-nitroisobutyro-m-toluidide; α,α,α-Trifluoro-2-methyl-4´-nitro-m-propionotoluidide
Molecular formula: C11H11F3N2O3 =276.2
CAS: 13311-84-7
ATC code: L02BB01
Read code: y02p1

Pharmacopoeias. In Europe and US.

European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Flutamide). A pale yellow, crystalline powder. Practically insoluble in water; freely soluble in alcohol and in acetone. Protect from light.

The United States Pharmacopeia 31, 2008 (Flutamide). A pale yellow, crystalline powder. Practically insoluble in water, in liquid paraffin, and in petroleum spirit; freely soluble in acetone, in ethyl acetate, and in methyl alcohol; soluble in chloroform and in ether. Store in airtight containers. Protect from light.

Adverse Effects and Precautions

The most frequently reported adverse effects with flutamide are hot flushes and reversible gynaecomastia or breast tenderness, sometimes accompanied by galactorrhoea. Nausea, vomiting, diarrhoea, increased appetite, anorexia, and sleep disturbances may occur. There have been reports of skin reactions, including epidermal necrolysis, and of liver damage, sometimes fatal. Other adverse effects reported in patients receiving flutamide include anaemias, haemolysis, headache, dizziness, malaise, blurred vision, anxiety, depression, decreased libido, impotence, and hypertension. Abdominal pain, chest pain, dyspnoea, and cough have been reported rarely. Discoloration of the urine to amber or yellow-green can be caused by the presence of flutamide and/or its metabolites.

Flutamide should be used with care in patients with cardiovascular disease because of the possibility of fluid retention. It should also be used with caution in patients with hepatic impairment and is contra-indicated in those with severe impairment. Regular liver function testing is recommended in all patients: therapy should be stopped or dosage reduced if there is evidence of hepatotoxicity.

Effects on the blood. A report of methaemoglobinaemia in an elderly man was attributed to flutamide. A study of 45 patients given flutamide found no cases of methaemoglobinaemia, but the authors noted a further 3 published case reports.

Effects on the liver. Hepatitis occurred in a 79-year-old man taking flutamide 750 mg daily as sole therapy after a prostatectomy, but a subsequent study in 1091 patients given flutamide 250 mg three times daily as part of a regimen for prostate cancer found marked signs of liver damage only in 4, of whom only 2 had clinical evidence of hepatotoxicity. In the USA, the FDA had 46 reports of patients with hepatotoxicity associated with flutamide up to December 1994. Of these patients, 20 died from progressive liver disease. Further cases have continued to be reported. Early tapering of the dose, stopping therapy, or switching to another anti-androgen may resolve hepatotoxic effects. Patients with chronic viral hepatitis may be at higher risk of developing hepatotoxicity with anti-androgen therapy.

Effects on the lungs. In a review of 78 cases of pneumonitis reported to the FDA between 1998 and 2000 that were associated with bicalutamide, flutamide, or nilutamide, it was found that 14 patients had died of respiratory failure. It was estimated that the incidence of pneumonitis was highest for nilutamide (0.77%), but lower for flutamide (0.04%) and brcalutamrde (0.01%).

Effects on the skin. Photosensitivity reactions have been reported in patients receiving flutamide. Some consider it to be an early manifestation of SLE.

Gynaecomastia. Gynaecomastia and breast pain are frequent adverse effects of nonsteroidal anti-androgens used to treat prostate cancer. Nearly 90% of patients treated with bicalutamide in the Early Prostate Cancer programme experienced breast pain, gynaecomastia, or both. Some patients who develop gynaecomastia will accept it as a tolerable adverse effect of therapy but others will require specifrc treatment, and a number of different measures have been tried for both prevention and treatment. The risk of breast changes can be reduced by the use of prophylactic low-dose irradiation of the breast area before nonsteroidal anti-androgen therapy is started. However, skin irritation can occur, and the long-term risk for development of breast cancer is unknown. Irradiation is unlikely to be effective once breast enlargement has occurred but it can help to reduce pain. Empirical use of oral analgesics or topical local anaesthetics may be considered for breast pain. Specifrc surgical treatment to reduce breast tissue includes liposuction and breast tissue excision.

Hormonal therapy using tamoxifen or anastrozole has been suggested, largely based on reports of benefit in various patient groups with gynaecomastia. Two randomised controlled studies of men who were treated with bicalutamide for prostate cancer found that prophylactic tamoxifen was effective for the prevention of gynaecomastia and breast pain, but that anastrozole was no better than placebo. One of these studies also assessed the use of these drugs as treatment and found that gynaecomastia and breast pain resolved in at least 65% of patients treated with tamoxifen, but only in about 18% of those treated with anastrozole. Tamoxifen is considered to be more effective than radiotherapy for prevention of gynaecomastia.

Interactions

Flutamide may increase the effect of warfarin, see Antineoplastics.

Pharmacokinetics

Flutamide is reported to be rapidly and completely absorbed from the gastrointestinal tract with peak plasma concentrations occurring 1 hour after a dose. It is rapidly and extensively metabolised; the major metabolite (2-hydroxyflutamide) possesses anti-androgenic properties. The half-life of the metabolite is about 6 hours. Both flutamide and 2-hydroxyflutamide are more than 90% bound to plasma proteins. Excretion is mainly in the urine with only minor amounts appearing in the faeces.

Uses and Administration

Flutamide is a nonsteroidal compound with anti-androgenic properties which appears to act by inhibiting the uptake and/or binding of androgens in target tissues. It is used, usually with gonadorelin analogues, in the palliative treatment of prostatic carcinoma. The usual oral dose is 250 mg three times daily. When used in combination therapy UK licensed product information recommends that flutamide treatment should be started at least 3 days before the gonadorelin analogue to suppress any ‘flare’ reaction; however, in some other countries it is recommended that treatment with both agents be begun simultaneously for optimum effect.

Congenital adrenal hyperplasia. For mention of the use of flutamide with testolactone to block androgenic effects in congenital adrenal hyperplasia.

Hirsutism. Anti-androgens (usually cyproterone or spironolac-tone) are widely used for the drug treatment of hirsutism. Flutamide has no particular advantage in this context; one study has found flutamide to be more effective than spironolactone in inhibiting hirsutism, but others found them to be of similar efficacy, and the risk of hepatotoxicity with flutamide is a problem. Nonetheless, flutamide has continued to be investigated.

Malignant neoplasms. Androgen blockade, which may include the use of flutamide, is used in the management of meta-static hormone-responsive prostate cancer; once the cancer begins to progress despite such therapy, stopping flutamide occasionally produces paradoxical disease regression. Promising preliminary results have also followed the use of flutamide in patients with adenocarcinoma of the pancreas.

Polycystic ovary syndrome. Flutamide has been used, usually with metformin, in the management of polycystic ovary syndrome; additive effects have been reported with this combination.

Preparations

The United States Pharmacopeia 31, 2008: Flutamide Capsules.

Single-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed

Argentina: Asoflut; Dedile; Eulexin¤; Flutaplex; Flutax¤; Flutepan; Flutrax; FTDA¤; Olter¤; Australia: Eulexin; Flutamin; Fugerel; Austria: Afluta; Androbloc; Flutabene; Flutahexal; Flutastad; Fugerel; Belgium: Eulexin; Flutaplex¤; Brazil: Biomida; Eulexin; Tecnoflut; Teflut; Canada: Euflex; Chile: Androdor¤; Drogenil; Etaconil; Flulem; Czech Republic: Andraxan; Flucinom; Flutacan; Prostandril; Xadaren; Denmark: Eulexin; Fluprosin; Flutacan¤; Flutaplex¤; Profamid; Finland: Eulexin; Profamid; France: Eulexine; Prostadirex; Germany: Apimid; Flumid; Fluta; Flutamex¤; Flutexin; Fugerel; Prostica; Prostogenat¤; Testac¤; Testotard; Greece: Adiprost; Elbat; Flucinom; Flutaplex; Palistop; Prostamide; Tremexal; Hong Kong: Flutan¤; Fugerel; Hungary: Cytamid; Flutam; Fugerel; India: Cytomid; Prostamid; Ireland: Androstat; Drogenil; Israel: Eulexin; Italy: Drogenil; Eulexin; Fluprost; Virflutam¤; Malaysia: Flutan; Flutaplex; Fugerel¤; Mexico: Eulexin; Fluken; Flulem; Tafenil; Netherlands: Drogenil; Eulexin; Norway: Eulexin; New Zealand: Eulexin; Flutamin; Flutol¤; Portugal: Draxon¤; Eulexin; Russia: Flutamid (Флутамид); Flutaplex (Флутаплекс); South Africa: Eulexin; Flutahexal; Flutaplex; Singapore: Fugerel¤; Spain: Eulexin; Flutandrona; Flutaplex; Grisetin; Oncosal; Prostacur; Sweden: Eulexin; Flutacan¤; Switzerland: Flucinome; Thailand: Flutan; Fugerel; United Kingdom: Chimax; Drogenil; United States: Eulexin¤; Venezuela: Eulexin

Posted in Drugs

Aminoglutethimide

Posted by admin on July 20th, 2010 No Comments

(British Approved Name, rINN)

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: Aminoglutethimid; Aminoglutethimidum; Aminoglutetimid; Aminoglutetimida; Aminoglutetimidas; Aminoglutetimidi; Ba-16038
BAN: Aminoglutethimide
INN: Aminoglutethimide [rINN (en)]
INN: Aminoglutetimida [rINN (es)]
INN: Aminoglutéthimide [rINN (fr)]
INN: Aminoglutethimidum [rINN (la)]
INN: Аминоглутетимид [rINN (ru)]
Chemical name: 2-(4-Aminophenyl)-2-ethylglutarimide; 3-(4-Aminophenyl)-3-ethylpiperidine-2,6-dione
Molecular formula: C13H16N2O2 =232.3
CAS: 125-84-8
ATC code: L02BG01
Read code: y02oN

Pharmacopoeias. In China, Europe, and US.

European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Aminoglutethimide). A white or slightly yellow, crystalline powder. Practically insoluble in water; freely soluble in acetone; soluble in methyl alcohol.

The United States Pharmacopeia 31, 2008 (Aminoglutethimide). A white or creamy-white, fine, crystalline powder. Very slightly soluble in water; readily soluble in most organic solvents. It forms water-soluble salts with strong acids. The pH of a 0.1% solution in dilute methyl alcohol (1 in 20) is between 6.2 and 7.3.

Adverse Effects

The most frequent adverse effects reported with aminoglutethimide include drowsiness, lethargy, and skin rashes (sometimes with fever); these generally diminish after the first 6 weeks of therapy. Dizziness and nausea occasionally occur. Leucopenia, thrombocytopenia, agranulocytosis, or severe pancytopenia have occurred rarely. Adrenal insufficiency may rarely occur, and there have been reports of other endocrine disturbances including hypothyroidism, and virilisation. Other rare effects include ataxia, headache, depression, gastrointestinal disturbances, hy-percholesterolaemia, and orthostatic hypotension. Overdosage may lead to CNS depression and impairment of consciousness, electrolyte disturbances, and respiratory depression.

Effects on the liver. Aminoglutethimide has been associated with reports of cholestatic jaundice, accompanied by rash and fever, and probably due to an idiosyncratic hypersensitivity reaction. It has been suggested that liver function tests should be carried out in patients receiving aminoglutethimide who develop fever and eruptions.

Effects on the lungs. Pulmonary infiltrates in a patient who developed progressive dyspnoea on starting therapy with aminoglutethimide were found to be due to diffuse alveolar damage and haemorrhage; thrombocytopenia was present but prothrombin and bleeding times were normal. The patient’s gas exchange and chest radiographs improved on stopping aminoglutethimide and giving corticosteroids. Blood and pulmonary eosinophilia, which resolved on stopping aminoglutethimide therapy, has also been reported.

Lupus. SLE occurred in a patient who received aminoglutethimide, and resolved when the drug was withdrawn. In another report, however, a patient with a lupus-like syndrome had a reduction in disease activity when tamoxifen therapy was changed to aminoglutethimide.

Precautions

Aminoglutethimide inhibits adrenal steroid production so supplementary glucocorticoid therapy with hydro cortisone must normally be given, although supplementation may not be necessary in patients with Cushing’s syndrome. Some patients also require a mineralocorticoid. It has been suggested that aminoglutethimide should be temporarily withdrawn in patients who undergo shock or trauma, or develop intercurrent infection. Blood pressure, blood counts, and serum electrolytes should be regularly monitored during aminoglutethimide therapy and periodic monitoring of liver and thyroid function is recommended. Aminoglutethimide should not be given during pregnancy as pseudohermaphroditism may occur in the fetus.

Aminoglutethimide frequently causes drowsiness: patients so affected should not drive or operate machinery.

Porphyria. Aminoglutethimide has been associated with acute attacks of porphyria and is considered unsafe in porphyric patients.

Interactions

The rate of metabolism of some drugs is increased by aminoglutethimide; patients also taking warfarin or other coumarin anticoagulants, theophylline, tamoxifen, medroxyprogesterone, or oral hypoglycaemics, may require increased dosages of these drugs. The metabolism of dexamethasone is also accelerated, which limits its value for corticosteroid supplementation in patients receiving aminoglutethimide. Use with diuretics may lead to hyponatraemia, while alcohol may potentiate the central effects of aminoglutethimide.

Pharmacokinetics

Aminoglutethimide is well absorbed after oral doses, with peak plasma concentrations occurring after 1 to 4 hours. It is metabolised in the liver, primarily to N-hydroxylaminoglutethimide and N-acetylaminoglutethimide, and appears to induce its own metabolism. The half-life, which is reported to be about 13 hours after a single dose, is decreased to around 9 hours after about 2 weeks of continuous therapy. Aminoglutethimide is excreted in urine, about half a dose being excreted unchanged and the remainder as metabolites. Only about 20 to 25% of a dose is bound to plasma protein.

Half-life. A study in 17 patients showed that the plasma half-life of aminoglutethimide had a mean value of 15.5 hours after single doses but fell to 8.9 hours during multiple-dose therapy. This marked reduction could largely be attributed to a decrease in the volume of distribution; auto-induction of metabolism might be of less importance in decreasing half-life than had been previously suggested.

Uses and Administration

Aminoglutethimide is an analogue of glutethimide and was formerly used for its weak anticonvulsant properties. Aminoglutethimide blocks the production of adrenal steroids and acts as an aromatase inhibitor to block the conversion of androgens to oestrogens (the major source of oestrogens in women without ovarian function). It was used in the treatment of meta-static breast cancer in postmenopausal or oophorect-omised women and as palliative treatment in men with advanced prostatic cancer.

Aminoglutethimide has also been used in the treatment of Cushing’s syndrome. Usual oral doses range from 1 to 2 g daily, in divided doses.

The dextroisomer of aminoglutethimide, dexaminoglutethimide has been investigated.

Preparations

British Pharmacopoeia 2008: Aminoglutethimide Tablets

The United States Pharmacopeia 31, 2008: Aminoglutethimide Tablets

Single-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed

Argentina: Orimeten¤; Australia: Cytadren; Austria: Orimeten¤; Belgium: Orimeten¤; Brazil: Orimeten¤; Canada: Cytadren¤; Chile: Orimeten¤; Czech Republic: Orimeten¤; France: Orimetene¤; Germany: Orimeten¤; Rodazol¤; Hong Kong: Orimetene; Ireland: Orimeten¤; Israel: Orimetene¤; Italy: Orimeten¤; Malaysia: Orimetene¤; Netherlands: Orimeten¤; Norway: Orimeten¤; New Zealand: Cytadren¤; Russia: Mamomit (Мамомит); Orimeten (Ориметен)¤; South Africa: Aminoblastin¤; Orimeten¤; Spain: Orimeten¤; Sweden: Orimeten¤; Switzerland: Orimetene¤; United Kingdom: Orimeten¤; United States: Cytadren

Posted in Drugs

Nilutamide

Posted by admin on July 20th, 2010 No Comments

(British Approved Name, US Adopted Name, rINN)

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: Nilutamid; Nilutamida; Nilutamidi; Nilutamidum; RU-23908
BAN: Nilutamide
USAN: Nilutamide
INN: Nilutamide [rINN (en)]
INN: Nilutamida [rINN (es)]
INN: Nilutamide [rINN (fr)]
INN: Nilutamidum [rINN (la)]
INN: Нилутамид [rINN (ru)]
Chemical name: 5,5-Dimethyl-3-(α,α,α-trifluoro-4-nitro-m-tolyl)-imidazolidine-2,4-dione
Molecular formula: C12H10F3N3O4 =317.2
CAS: 63612-50-0
ATC code: L02BB02

Pharmacopoeias. In Europe.

European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Nilutamide). A white or almost white powder. Very slightly soluble in water; freely soluble in acetone; soluble in anhydrous ethanol. Protect from light.

Adverse Effects and Precautions

As for Flutamide. Interstitial pneumonitis has occurred in patients receiving nilutamide, and the drug is contra-indicated in those with severe respiratory insufficiency.

Effects on the eyes. Reversible visual disturbances, particularly delayed dark adaptation, have been associated with nilutamide. Although some consider such visual disturbances to be mild and generally well tolerated, others suggest that these, together with alcohol intolerance and, more seriously, effects on the lung, mean that other nonsteroidal anti-androgens should be preferred.

Interactions

Patients receiving nilutamide may exhibit intolerance to alcohol.

Pharmacokinetics

Nilutamide is rapidly and completely absorbed from the gastrointestinal tract. It is extensively metabolised although it may inhibit its own metabolism to some extent after multiple doses. About 60% of an oral dose of nilutamide is eliminated in the urine and less than 10% in the faeces, with an elimination half-life of 41 to 49 hours.

Uses and Administration

Nilutamide is a nonsteroidal anti-androgen that is used similarly to flutamide in the treatment of prostatic carcinoma. It is given orally in a dose of 300 mg daily, usually starting on the same day that the patient undergoes orchidectomy or receives treatment with a gonadorelin analogue. Dosage may be reduced to 150 mg daily after 1 month.

Single-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed

Argentina: Anandron; Australia: Anandron; Brazil: Anandron; Canada: Anandron; Czech Republic: Anandron; Denmark: Anandron¤; Finland: Anandron¤; France: Anandron; Greece: Anandron; Hungary: Anandron; Mexico: Anandron; Netherlands: Anandron; Norway: Anandron¤; Portugal: Anandron; Sweden: Anandron; United States: Nilandron

Posted in Drugs

Histrelin

Posted by admin on July 19th, 2010 No Comments

US Adopted Name, rINN

Drug Nomenclature

Synonyms: ORF-17070; RWJ-17070
USAN: Histrelin
INN: Histrelin [rINN (en)]
INN: Histrelina [rINN (es)]
INN: Histréline [rINN (fr)]
INN: Histrelinum [rINN (la)]
INN: Гистрелин [rINN (ru)]
Chemical name: 5-Oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-Nτ-benzyl-d-histidyl-l-leucyl-l-argininyl-N-ethyl-l-prolinamide
Molecular formula: C66H86N18O12 =1323.5
CAS: 76712-82-8
ATC code: H01CA03

Histrelin Acetate

INN: Histrelin Acetate [rINNM (en)]
INN: Acetato de histrelina [rINNM (es)]
INN: Histréline, Acétate d’ [rINNM (fr)]
INN: Histrelini Acetas [rINNM (la)]
INN: Гистрелина Ацетат [rINNM (ru)]
Molecular formula: C66H86N18O12,xC2H4O2,yH2O
CAS: 220810-26-4
ATC code: H01CA03

Adverse Effects and Precautions

As for Gonadorelin.

Uses and Administration

Histrelin is an analogue of gonadorelin with similar properties. A subcutaneous implant containing histrelin acetate 50 mg, and designed to release histrelin acetate 50 to 60 micrograms daily for 12 months, is used in the palliative treatment of advanced prostate cancer. Histrelin is used in the treatment of precocious puberty in children. It has also been investigated in disorders related to the menstrual cycle, and in the treatment of acute porphyr-ias.

Administration in children. For the suppression of gonadal sex hormone production in children with central precocious puberty, histrelin acetate has been given by subcutaneous inj ection in usual doses equivalent to histrelin 10 micrograms/kg daily. Alternatively, a subcutaneous implant containing histrelin acetate 50 mg and designed to release histrelin acetate 65 micrograms daily for 12 months may be used. The implant is not recommended for children under 2 years of age. References.

Proprietary Preparations

Malaysia: Vantas

USA: Supprelin; Vantas

Posted in Drugs

Triptorelin

Posted by admin on July 17th, 2010 No Comments

Drug Approvals

(British Approved Name, US Adopted Name, rINN)

International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish):

Synonyms: d-Trp6-LHRH; AY-25650; BIM-21003; BN-52014; CL-118532; Triptorelina; Triptoreline; [6-d-Tryptophan] luteinising hormone-releasing factor
BAN: Triptorelin
USAN: Triptorelin
INN: Triptorelin [rINN (en)]
INN: Triptorelina [rINN (es)]
INN: Triptoréline [rINN (fr)]
INN: Triptorelinum [rINN (la)]
INN: Трипторелин [rINN (ru)]
Chemical name: 5-Oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-tryptophyl-l-leucyl-l-arginyl-l-prolylglycinamide
Molecular formula: C64H82N18O13 =1311.4
CAS: 57773-63-4
ATC code: L02AE04
Read code: y08C6

Triptorelin Acetate

Drug Approvals

(British Approved Name Modified, rINNM)

Synonyms: Triptoreliiniasetaatti; Triptorelina, acetato de; Triptorelinacetat; Triptorelini Acetas
BAN: Triptorelin Acetate [BANM]
INN: Triptorelin Acetate [rINNM (en)]
INN: Acetato de triptorelina [rINNM (es)]
INN: Triptoréline, Acétate de [rINNM (fr)]
INN: Triptorelini Acetas [rINNM (la)]
INN: Трипторелина Ацетат [rINNM (ru)]
Molecular formula: C64H82N18O13, C2H4O2 =1371.5
CAS: 140194-24-7
ATC code: L02AE04

Triptorelin Diacetate

Drug Approvals

(British Approved Name Modified, rINNM)

International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish):

BAN: Triptorelin Diacetate [BANM]
INN: Triptorelin Diacetate [rINNM (en)]
INN: Diacetato de triptorelina [rINNM (es)]
INN: Triptoréline, Diacetate de [rINNM (fr)]
INN: Triptorelini Diacetas [rINNM (la)]
INN: Трипторелина Диацетат [rINNM (ru)]
Molecular formula: C64H82N18O13,2C2H4O2 =1431.6
CAS: 105581-02-0
ATC code: L02AE04

Triptorelin Embonate

Drug Approvals

(British Approved Name Modified, rINNM)

BAN: Triptorelin Embonate [BANM]
USAN: Triptorelin Pamoate
INN: Triptorelin Embonate [rINNM (en)]
INN: Embonato de triptorelina [rINNM (es)]
INN: Triptoréline, Embonate de [rINNM (fr)]
INN: Triptorelini Embonas [rINNM (la)]
INN: Трипторелина Ембонат [rINNM (ru)]
Molecular formula: C64H82N18O13,C23H16O6 =1699.8
CAS: 124508-66-3
ATC code: L02AE04

Adverse Effects and Precautions

As for Gonadorelin.

Local reactions. For reference to local reactions occurring following injection of gonadorelin analogues, including triptorelin, see Leuprorelin Acetate.

Sepsis. A report of 2 patients in whom triptorelin therapy led to sepsis caused by expulsion of necrotic fibroids through the cervix.

Interactions

As for Gonadorelin.

Pharmacokinetics

Triptorelin is rapidly absorbed after subcutaneous injection, with peak plasma concentrations achieved about 40 minutes after a dose. The biological half-life has been stated to be about 7.5 hours, although longer half-lives have been reported in patients with prostate cancer, and shorter half-lives in some groups of healthy subjects.

Uses and Administration

Triptorelin is an analogue of gonadorelin with similar properties. It is used for the suppression of go-nadal sex hormone production in the treatment of malignant neoplasms of the prostate, deviant sexual behaviour in men, precocious puberty, and in the management of endometriosis, female infertility, and uterine fibroids. Triptorelin may be given as the base, acetate, diacetate, or embonate, although for some preparations stated to contain the acetate or diacetate it is not always clear which has actually been used. Doses are usually given in terms of the base, and the following are each equivalent to about 1 mg of triptorelin:

• triptorelin acetate, 1.05 mg

• triptorelin diacetate, 1.09 mg

• triptorelin embonate, 1.30 mg

Triptorelin is given as a daily subcutaneous injection, or as an intramuscular or subcutaneous depot preparation lasting a month or longer.

In the palliative treatment of advanced prostate cancer, a dose equivalent to triptorelin 3 or 3.75 mg is given intramuscularly as a depot preparation every 4 weeks the first dose may be preceded by 100 micrograms daily for 7 days by subcutaneous injection. In some countries, depot preparations containing 3.75 mg may be given subcutaneously instead. A longer-acting depot preparation that contains the equivalent of triptorelin 11.25 mg is given once every 12 to 13 weeks. In some countries, depot doses of 3 mg once every 4 weeks or 11.25 mg once every 12 to 13 weeks may also be used for medical therapy in locally advanced disease. An anti-androgen such as cyproterone acetate may be given for several days before beginning therapy with triptorelin and continued for about 3 weeks to avoid the risk of a disease flare.

An 11.25-mg intramuscular depot preparation, given every 12 weeks, may be used in the management of deviant sexual behaviour in men. The addition of an anti-androgen should be considered when starting therapy, to counteract the initial rise in serum-testosterone concentrations.

Similar doses of the 3- or 3.75-mg depot preparations may be given for up to 6 months in the management of endometriosis or uterine fibroids, with treatment begun during the first 5 days of the menstrual cycle. The 11.25-mg depot may be used as an alternative for endometriosis. In the management of female infertility doses of 100 micrograms subcutaneously daily, with gonadotrophins, have been recommended from the second day of the menstrual cycle for about 10 to 12 days.

In children with precocious puberty a dose equivalent to triptorelin 50 micrograms/kg from the 3-mg depot preparation may be given intramuscularly every 4 weeks. Alternatively, using the 3.75-mg preparation, doses of 1.875 mg for children weighing less than 20 kg, 2.5 mg for children of 20 to 30 kg, or 3.75 mg for children of more than 30 kg may be given intramuscularly or subcutaneously the first 3 doses should be given at 14-day intervals, with further doses given every 4 weeks. The longer acting 11.25-mg depot preparation, given intramuscularly once every 3 months, is another alternative.

Delayed and precocious puberty. Gonadorelin analogues such as triptorelin are used in the management of central precocious puberty. They may also be effective in delayed puberty although they are most likely to be helpful where this is due to hypogonadism. Triptorelin has been used to differentiate gonadotrophin deficiency from constitutional delayed puberty, although one study found it to be less accurate than a test using human chorionic gonadotrophin.

Disturbed behaviour. Combined therapy with triptorelin, which suppressed testosterone secretion by inhibiting the pituitary-gonadal axis, and supportive psychotherapy, has been tried in the treatment of men with paraphilias: a reduction in abnormal sexual thoughts and behaviours has been reported, although the study was uncontrolled.

Endometriosis. Gonadorelin analogues are effective in the management of endometriosis, but the need for long-term therapy to prevent recurrence limits their value because of the risk of osteoporosis ‘add-back’ therapy (hormone replacement) can be used to prevent this. References.

Fibroids. Gonadorelin analogues have been used as an alternative to surgery in the treatment of uterine fibroids, despite some concern that this may complicate the diagnosis of malignancy. References to the use of triptorelin.

Growth retardation. As discussed gonadorelin analogues have been given with growth hormone to short girls without growth hormone deficiency, in an attempt to delay puberty and bone maturation and thus maximise the final height achieved. Use in growth hormone-deficient children has also been investigated. However, there is some doubt about the extent of benefit, and in any case the concept of such treatment in children who are not clinically deficient in growth hormone is controversial, and some authorities do not consider it appropriate. References to the use of triptorelin.

Infertility. Gonadorelin analogues are used in the management of infertility related to hypogonadotrophic hypogonadism in both men and women. For a discussion of infertility and its management, including the role of gonadorelin analogues.

Malignant neoplasms. Triptorelin, like other gonadorelin analogues, may be used in the production of androgen blockade in patients with prostate cancer.

Porphyria. Triptorelin has been used successfully to suppress premenstrual exacerbations of acute intermittent porphyria, in doses of 3.75 mg by intramuscular depot injection given monthly.lt To reduce the risk of osteoporosis, ‘add-back’ therapy with topical oestrogen and oral calcium was used in one case, and tibolone in another.

Proprietary Preparations

Argentina: Decapeptyl Gonapeptyl

Austria: Decapeptyl Pamorelin

Belgium: Decapeptyl

Brazil: Neo Decapeptyl

Chile: Decapeptyl

Czech Republic: Decapeptyl Diphereline

Denmark: Decapeptyl Pamorelin

Finland: Decapeptyl

France: Decapeptyl Gonapeptyl

Germany: Decapeptyl Pamorelin

Greece: Arvekap Gonapeptyl

Hong Kong: Decapeptyl Diphereline

Hungary: Decapeptyl Diphereline

India: Decapeptyl

Ireland: Decapeptyl Gonapeptyl

Israel: Decapeptyl Diphereline

Italy: Decapeptyl Gonapeptyl

Malaysia: Decapeptyl

Mexico: Trelstar †

The Netherlands: Decapeptyl Gonapeptyl Pamorelin

Poland: Decapeptyl Diphereline

Portugal: Decapeptyl

Russia: Decapeptyl Diphereline

South Africa: Decapeptyl

Singapore Decapeptyl

Spain: Decapeptyl Gonapeptyl

Sweden: Decapeptyl Moapar

Switzerland: Decapeptyl

Thailand: Decapeptyl Diphereline

Turkey: Decapeptyl

UK: Decapeptyl Gonapeptyl

USA: Trelstar

Venezuela: Decapeptyl

Posted in Drugs

Finasteride

Posted by admin on June 11th, 2010 No Comments

Drug Approvals

(British Approved Name, US Adopted Name, rINN)

International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish): Finasterid; Finasterida; Finasteridas; Finasteride; Finasteridi; Finastendum; Finasztend; MK-906; MK-0906; YM-152.

Pharmacopoeias. In Europe and US.

European Pharmacopoeia, 6th ed. (Finasteride). A white or almost white crystalline powder. It exhibits polymorphism. Practically insoluble in water freely soluble in dehydrated alcohol and in dichloromethane. Protect from light.

The United States Pharmacopeia 31, 2008 (Finasteride). A white to off-white crystalline solid. Very slightly soluble in water freely soluble in alcohol and in chloroform. Store in airtight containers.

Adverse Effects

The most commonly reported adverse effects of finasteride are decreased libido, erectile dysfunction, ejaculation disorders, and reduced volume of ejaculate. Breast tenderness and enlargement (gynaecomastia) may occur, and there have been reports of hypersensi-tivity reactions such as swelling of the lips and face, pruritus, urticaria, and rashes. Testicular pain has also been reported.

Incidence of adverse effects. In a study using prescription event monitoring data, the most commonly reported adverse effects of finasteride in 14 772 patients were impotence or ejacula-tory failure (2.1% of patients), reduced libido (1%), and breast disorders such as gynaecomastia (0.4%). Adverse effects reported in a single patient each, and verified on rechallenge, were ex-foliative dermatitis, perioral numbness, and swollen glands. Finasteride appeared to be associated with ataxia in 1 patient and wheeziness in another.

Effects on the breast. Gynaecomastia was the adverse effect of finasteride most frequently reported to the FDA between June 1992 and February 1995 (a total of 214 reports). The onset after therapy ranged from 14 days to 2.5 years, and the condition could be unilateral or bilateral. Mastectomy was performed in 12 men. Of the 86 men for whom follow-up information was available, partial or complete remission of gynaecomastia occurred in 80%, and no change occurred in 20%. In 2 of the cases, primary intra-ductal breast carcinoma was subsequently found, although 1 probably had breast cancer before finasteride therapy. Continued surveillance of the relationship between finasteride and breast cancer is required.

Effects on mental function. Depression has been reported in 20 patients given finasteride for the treatment of alopecia. In most cases the depression began about 3 to 4 months after starting finasteride, and resolved within a few weeks of stopping it. In 2 patients rechallenged with finasteride, depression recurred within 2 weeks of restarting the drug.

Precautions

Finasteride should be used with caution in hepatic impairment. When used for benign prostatic hyperplasia, finasteride should be used with caution in men at risk of obstructive uropathy. Patients should be evaluated for prostatic carcinoma before and during therapy. Use of finasteride decreases concentrations of serum markers of prostate cancer such as prostate specific antigen (PSA) by up to 50% even when cancer is present, and reference values should be adjusted accordingly the ratio of free to total PSA (percent free PSA) remains constant.

Studies in animals suggest finasteride could produce feminisation (hypospadia) of a male fetus if used in pregnant women therefore, its use is contra-indicated in women who are or may become pregnant. In addition, it is recommended that women in this category should not handle crushed or broken finasteride tablets. Finasteride has been detected in semen, therefore use of a condom is recommended if the patient’s sexual partner is, or may become, pregnant.

Pharmacokinetics

Finasteride is absorbed after oral doses, and peak plasma concentrations are achieved in 1 to 2 hours. The mean bioavailability has variously been reported as 63% and 80%. It is about 90% bound to plasma protein. Finasteride crosses the blood-brain barrier, and is distributed into semen. It is metabolised in the liver, primarily by the cytochrome P450 isoenzyme CYP3 A4, and excreted in urine and faeces as metabolites. The mean terminal half-life is about 6 hours in patients under 60 years of age but may be prolonged to about 8 hours in those 70 years of age or older.

Uses and Administration

Finasteride is an azasteroid that inhibits the type-2 iso-form of 5α-reductase, the enzyme responsible for conversion of testosterone to the more active dihydrotestos-terone, and therefore has anti-androgenic properties. It is given orally in a dose of 5 mg daily in the management of benign prostatic hyperplasia to cause regression of the enlarged prostate and to improve symptoms it may reduce the incidence of acute urinary retention and the need for surgery. Response may be delayed and treatment may be required for 6 months or more to assess whether benefit has been achieved.

In the treatment of male-pattern baldness (alopecia androgenetica) in men, finasteride is given orally in a dose of 1 mg daily. In general, use for 3 months or more is required before benefit is seen, and effects are reversed within 12 months of ceasing therapy.

Alopecia. In men with male-pattern baldness (alopecia), treatment with oral finasteride for 12 months resulted in an 11 % increase in vertex hair count, which was maintained in those who continued therapy. Extension of this study to 5 years found that long-term treatment with finasteride maintained beneficial effects, or at least slowed hair loss. The use of oral finasteride for this purpose has been reviewed. Some efficacy has also been found with topical finasteride.

Although finasteride is contra-indicated in women who are or may become pregnant (see Precautions, above), it has been investigated in the treatment of male-pattern baldness in postmeno-pausal women. However, a 1-year placebo-controlled study found no benefit from finasteride. There has been a report of benefit from finasteride in 4 women with hair loss due to hyper-androgenism.

Benign prostatic hyperplasia. Finasteride is used in the management of benign prostatic hyperplasia. It produces moderate reductions in prostate volume, although this takes a number of months and is not always associated with much symptomatic improvement therapy must be continued indefinitely for benefit to be maintained. A 4-year study found that finasteride reduced the probability of surgery and acute urinary retention in men with symptomatic benign prostate hyperplasia with prostatic enlargement. Although the need for prostatectomy was reduced by 55% it was pointed out that only 6% extra patients would benefit from treatment with finasteride. For every 100 men treated, 7 finasteride and 13 placebo recipients required surgery. A 2-year, open-label follow-up of this study reported that the reductions in probability of surgery and acute urinary retention were maintained. It was also found that in patients who switched from placebo to finasteride, these measures decreased to become similar to those recorded in men already receiving finasteride. A comparative 12-month study found the alpha blocker terazosin to be more effective than finasteride in relieving symptoms and improving peak urine flow rates the combination of finasteride plus terazosin was no more effective than terazosin alone. Moreover, although finasteride reduced prostatic volume, it was no more effective than placebo, a finding that is at odds with previous placebo-controlled studies. It has been suggested that the smaller median prostate size in this study may explain the negative findings, and that men with larger prostates do benefit from finasteride. Similar results were reported in a 12-month study using doxazosin. Later results from a large study showed that over a longer period of 4 or more years the combination of doxazosin and finasteride reduced the risk of clinical progression more than either drug alone. The combination of an alpha blocker and 5a-reductase inhibitor is therefore considered to be a suitable option for patients with urinary symptoms and demonstrable prostatic enlargement, and who are at significant risk of progression.

Hirsutism. Finasteride is reported to be effective for the treatment of hirsutism in women. It should be noted that finasteride should not be used in women who are or may become pregnant (see Precautions, above).

Malignant neoplasms of the prostate. Finasteride appears to have little effect in established prostate cancer,’ but is under investigation for its prevention. The results of 1 small study of its effects on the prostate found little evidence to support its use for prevention of malignancy in patients at high risk. In healthy men, a large controlled study, the Prostate Cancer Prevention Trial (PCPT), found that 7 years of finasteride prophylaxis reduced the incidence of prostate cancer by about 25% compared with placebo, but this benefit was offset by an increased risk of high-grade tumours associated with finasteride. The risk-benefit implications of these results have been debated, although some commentaries” suggest that preventive use would be justified, at least in selected patients. Further analysis of the PCPT data found that finasteride had introduced a detection bias for both prostate cancer and for high-grade prostate cancer. Finasteride increased the sensitivity of prostate specific antigen (PSA) testing, implying that the PCPT primary findings of increased risk of high-grade tumours were due, at least in part, to improved detection. The reported 25% decrease in prostate cancer incidence was also likely to be an underestimate. The European Association of Urology has endorsed a recommendation that prostate cancer management guidelines be updated to reflect these findings.

Preparations

British Pharmacopoeia 2008: Finasteride Tablets

The United States Pharmacopeia 31, 2008: Finasteride Tablets.

Proprietary Preparations

Argentina: Anatine † Andropel Avertex Conef † Daric Eutiz † Finasterin Fin-prostat Flutiamik Folcres HPB Nasteril Pelicrep † Propecia Proscar Pros-min Prostanil Prostanovag Prostene Renacidin Sutrico Tealep Tricofarma Urofin Urototal Vetiprost

Austral.: Propecia Proscar

Austria: Propecia Proscar

Belgium: Proscar

Brazil: Alfasin Capyla Finalop Finastec Finastil Flaxin Nasterid Nasterid A Pracap Prohair † Pronasteron Propecia Proscar Prostide Reduscarf

Canada: Propecia Proscar

Chile: Apeplus † Prohair Proscar Saniprostol Vastus

Czech Republic: Androfin Apo-Finas Duromeran Edufil Finajel † Finanorm Finard Finex Finpros Gefin Ibition Lekoprost Mostrafin Penester Propecia Proscar Radicut

Denmark: Propecia Proscar

Finland: Gefina Propecia Proscar

France: Chibro-Proscar Propecia

Germany: Propecia Proscar

Greece: Pervil Poruxin Propecia Proscar

Hong Kong: Propecia Proscar

Hungary: Finpros Proscar Prosterid

India: Fincar Finpecia Ultrafinaf

Indonesia: Finaxal Finpro Proscar Prostacom Reprostom

Ireland: Proscar

Israel: Pro-Cure Propecia

Italy: Finastid Genaprost Propecia Proscar Prostide

Malaysia: Propecia Proscar

Mexico: Propeshia Proscar

The Netherlands: Finaburg Propecia Proscar

Norway: Proscar

New Zealand: Propecia Proscar

Philippines: Propecia Proscar

Poland: Ambulase Finaride Finaster Lifin Penester Propecia Proscar Zasterid

Portugal: Propecia Proscar Prostacide Prostafin Zidoril Zylfina

Russia: Finast Penester Proscar Prosterid

South Africa: Propecia Proscar

Singapore Propecia Proscar

Spain: Eucoprost Propecia Proscar

Sweden: Propecia Proscar

Switzerland: Propecia Proscar

Thailand: Firide Harifin Propecia Proscar

Turkey: Dilaprost Finarid Propecia Proscar Prosterit

UK: Propecia Proscar

USA: Propecia Proscar

Venezuela: Finast † Nasterol Propecia Proscar Prosdina †

Multi-ingredient

Argentina: Tricoplus Conef †

India: Urimax F

Posted in Drugs

Alfuzosin Hydrochloride

Posted by admin on June 8th, 2010 No Comments

Drug Approvals

(British Approved Name Modified, US Adopted Name, rINN)

International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish): Alfutsosiinihydrokloridi; Alfuzosin Hidroklorur; Alfuzosine, chlorhydrate d’ Alfuzosin-hydrochlorid; Alfuzosinhydroklorid; Alfuzosini hydrochloridum; Alfuzozin-hidroklorid; Alfuzozino hidrochloridas; Hidrocloruro de alfuzosina; SL-77499-10; SL-77499 (alfuzosin).

Pharmacopoeias. In Europe.

European Pharmacopoeia, 6th ed. (Alfuzosin Hydrochloride). Awhite or almost white, slightly hygroscopic, crystalline powder. Freely soluble in water sparingly soluble in alcohol practically insoluble in dichlo-romethane. A 2% solution in water has apH of 4.0 to 5.5. Store in airtight containers. Protect from light.

Adverse Effects, Treatment, and Precautions

As for Prazosin Hydrochloride. Alfuzosin may be more selective for the urinary tract and vasodilator effects may be less frequent. It should be avoided in severe hepatic impairment, and doses may need to be reduced in mild to moderate hepatic impairment and in renal impairment (see below).

Incidence of adverse effects. In postmarketing surveillance involving 13 389 patients given alfuzosin 2.5 mg three times daily by mouth for benign prostatic hyperplasia, about 3.7% of patients failed to complete treatment because of adverse effects. These were mostly vasodilatory in nature (vertigo or dizziness, syncope or malaise, hypotension, and headache), and were more common in patients over 75 years of age and during the first week of treatment.

Surgical procedures. Alpha blockers, including alfuzosin, have been associated with intraoperative floppy iris syndrome in cataract surgery patients. For further details, see under Tamsu-losin, p.2197.

Interactions

As for Prazosin Hydrochloride. Potent inhibitors of the cytochrome P450 isoenzyme CYP3A4, such as ketoconazole, itraconazole, and ritonavir, may increase blood concentrations of alfuzosin.

Pharmacokinetics

Alfuzosin is readily absorbed after oral doses and peak plasma concentrations generally occur 0.5 to 3 hours after a dose bioavailability is about 64%. Absorption from modified-release preparations is improved if given with food. It is extensively metabolised in the liver, mainly by the cytochrome P450 isoenzyme CYP3A4, to inactive metabolites that are excreted primarily in faeces via the bile. Only about 11% of a dose is excreted unchanged in the urine. Alfuzosin has a plasma elimination half-life of 3 to 5 hours. It is 90% bound to plasma proteins.

Uses and Administration

Alfuzosin is an alpha1-adrenoceptor blocker with actions similar to those of prazosin. It acts preferentially on receptors in the lower urinary tract and is therefore used in benign prostatic hyperplasia to relieve symptoms of urinary obstruction, including acute urinary retention.

Alfuzosin is given orally as the hydrochloride. Like other alpha1-adrenoceptor blockers, it may cause collapse in some patients after the first dose, which should therefore be given just before bedtime to reduce the risk. Doses may need to be reduced in patients with hepatic or renal impairment (see below) the initial dose should also be reduced in the elderly.

In benign prostatic hyperplasia, the usual dose of alfuzosin hydrochloride is 2.5 mg three times daily, increased to 10 mg daily if necessary. In elderly patients, and those receiving treatment for hypertension, a lower initial dose of 2.5 mg twice daily should be considered. A modified-release preparation may also be used in a dose of 10 mg once daily after a meal.

In patients aged over 65 years catheterised for acute urinary retention associated with benign prostatic hyperplasia, a modified-release preparation may be given in a dose of 10 mg once daily after a meal for 3 to 4 days.

Administration in hepatic or renal impairment. In patients with mild to moderate hepatic impairment the initial dose of alfuzosin hydrochloride should be 2.5 mg daily, increased to 2.5 mg twice daily according to response modified-release preparations are not recommended.

In patients with renal impairment, 2.5 mg twice daily should be given initially, adjusted according to response. Although UK and US licensed product information advises caution with the use of modified-release preparations in severe renal impairment (creatinine clearance below 30 mL/minute), a study in patients with varying degrees of renal impairment (including severe) suggested that no dose reduction was necessary.

Preparations

Proprietary Preparations:

Argentina: Dalfaz UroXatral

Austria: Urion † Xatral

Belgium: Xatral

Brazil: Xatral

Canada: Xatral

Chile: UroXatral

Czech Republic: Alfuzostad Xatral

Denmark: Xatral Fin. Xatral

France: Urion Xatral

Germany: Urion UroXatral

Greece: Alfuprost Alfural Alfuzin Innosensitive Spedamyl Xatral

Hong Kong: Xatral

Hungary: Alfetim Alfuzostad

India: Flotral

Indonesia: Xatral

Ireland: Xatral

Israel: Xatral

Italy: Mittoval Xatral

Malaysia: Xatral

Mexico: Xatral

The Netherlands: Mittoval Urion UroXatral Xatral

Norway: Xatral

Philippines: Xatral

Poland: Alfuzostad Dalfaz

Portugal: Benestan

Russia: Dalfaz

South Africa: Xatral

Singapore Xatral

Spain: Alfetim † Benestan Unibenestan

Sweden: Xatral

Switzerland: Xatral

Thailand: Xatral

Turkey: Xatral

UK: Besavar Xatral

USA: UroXatral

Venezuela: Xatral.

Posted in Drugs

DOCETAXEL

Posted by admin on June 5th, 2010 No Comments

DOCETAXEL (doe-seh-TAX-ell)

Other Names for this Medication (Brand Name):

Taxotere

Appearance:

Injection: Clear solution for injection, as an intravenous infusion.

Why this Medication is Used

Docetaxel may be used for the treatment of lung, prostate or breast cancers. It may also be used for treatment of other cancers.

How do you take this Medication

Injection: Docetaxel is added to an intravenous bag of fluid and infused into your bloodstream over one or two hours by your chemotherapy nurse.

Precautions

• Docetaxel usually causes temporary hair loss, but may rarely be permanent (including scalp hair, body hair, eyebrows, eyelashes, and pubic hair), starting 2 to 3 weeks after your treatment.

• Your doctor will prescribe dexamethasone tablets for you to take at home before and after each Docetaxel injection, to help prevent allergic reaction and water retention. It is very important that you take these tablets exactly as directed by your doctor.

• This chemotherapy should not be used if you are pregnant or breast-feeding. It is important to discuss birth control with your doctor (Note: birth control pills alone are not recommended as the only birth control method). Birth control should also be used by female partners, if you are a male taking this medication

• It is important to tell your doctor if you have chickenpox (or have recently been exposed to someone who has had chickenpox), shingles, kidney disease or liver disease. Any of these conditions could affect therapy with this medication.

• Due to increased risk of infection check with your doctor before having any vaccinations. Check with your doctor, before any surgery or dental work.

• Do not take ASA without your doctor’s knowledge and consent.

> If a doctor has advised you to take ASA to prevent heart disease or stroke, please discuss this with your oncologist (cancer doctor) before starting treatment.

> Do not use ASA (Aspirin®, acetylsalicylic acid) for headache, fever, or occasional aches and pains; use acetaminophen (Tylenol®) instead. Many non-prescription medications contain ASA; always ask your pharmacist’s advice when choosing a product.

For more information on this medication, please call your doctor, pharmacist or nurse.

SIDE EFFECTS PREVENTION WHAT YOU SHOULD DO
MORE COMMON:
• Signs of infection/ fever, chills, cough • Limit contact with people who are sick or have colds. Rest often. Wash your hands often. • Keep a thermometer at home. Recognize signs of infection. Phone your doctor or go to the emergency department right away if your

temperature is over 38° C or 100° F. You may need antibiotics.
• Low white blood cells
• Eye tearing (with weekly treatment) • Notify your doctor or nurse as soon as you notice any increase in this tearing
• Hair loss (from head and body). • A wig, hat, cap, scarf or hairpiece may be worn.
• Your hair will usually regrow, once all of your treatments are over.
• Red, itchy skin; skin shedding • Contact your doctor or nurse if these bother you.
• Nail changes, yellow-orange colour or becoming brittle
• Water retention in arms and legs • Your doctor may order some medications to prevent fluid retention • Contact your doctor or nurse as soon as possible
LESS COMMON:
• Numbness and tingling in hands and feet • Check with your doctor or nurse if this is bothersome
• Nausea and vomiting • Take medicine for nausea and vomiting as ordered by your doctor. Continue drinking clear fluids. Get fresh air and rest. • If you vomit within 1 hour of taking antiemetic medication, you may take another dose. Phone your doctor if vomiting lasts more than 24 hours or nausea longer than 2 days.
• Diarrhea • Limit hot, spicy, and fried foods; limit foods and drinks with caffeine. • Drink plenty of fluids. Phone your doctor if diarrhea lasts longer than 24 to 48 hours or you feel weak.
• Shortness of breath • Tell your doctor or nurse as soon as possible.
• Flushing of face
• Skin rash, itch
• Sores in the mouth or the lips • Maintain good mouth hygiene. Brush teeth with a soft toothbrush. Use a mouthrinse that does not contain alcohol. Avoid hot, spicy and acidic foods. • Check with your doctor or nurse as soon as you notice sores on mouth or lips.
• fatigue
• muscle aches
RARE:
• Severe shortness of breath, severe skin reactions • Contact your doctor IMMEDIATELY.
• Numbness, tingling in hands, pain in joints, muscles • Check with your doctor or nurse if these bother you.
Posted in Drugs

TAMSULOSIN

Posted by admin on May 18th, 2010 No Comments

TAMSULOSIN (tam-SOO-loe-sin)

Other Names for this Medication (Brand names): Flomax, Harnal, Omnic, Pradif, Tamsolusin, Tamsulosina [INN-Spanish], Tamsulosine [INN-French], Tamsulosinum [INN-Latin]

Appearance

Half orange-yellow and tan capsule marked with “FLOMAX 0.4 mg” on the orange side and “BI 58″ on the tan side.

Why this Medication is Used

Tamsulosin is used in the treatment of benign prostatic hyperplasia or BPH (enlargement of the prostate gland) by relaxing muscles in the prostate and bladder, resulting in improved urine flow and reduced BPH symptoms.

How do you take this Medication

The usual dose is 0.4 mg once per day but this may be adjusted by your doctor to 0.8 mg per day depending on the patient and/or severity of the symptoms of BPH. Tamsulosin may be taken 30 minutes following the same meal every day. If you interrupt your treatment for several days or more, resume treatment at one capsule/day, after consulting your doctor.

Precautions

• Make sure to schedule regular check-ups with your doctor while taking tamsulosin.

• Do not crush, chew or open capsules of tamsulosin, as the capsules are specially made to regulate the release of tamsulosin into the blood stream.

• Avoid driving or operating dangerous machinery for 12 hours after the initial or any increase in dose until you know how this medication will affect you.

• Tell your doctor if you are taking any of the following medications: Blood pressure lowering agents, Cimetidine and Warfarin.

• Store in a cool dry place at room temperature. Keep out of reach of children.

For more information on this medication, please call your doctor, pharmacist or nurse.

SIDE EFFECTS PREVENTION WHAT YOU SHOULD DO
MORE COMMON
• Dizziness, sleepiness

• Abnormal ejaculation

• Runny nose, cough

 • Avoid sudden changes in posture.

• Take medication at bedtime (or after dinner).

 • These effects should diminish over time.

• Contact your doctor if the symptoms continue to bother you.

• Contact your doctor if the symptoms continue to bother you.
LESS COMMON
• Insomnia • Contact your doctor if the symptoms continue to bother you.
RARE
• Flu symptoms, chills, neck pain • STOP taking the medication and contact your doctor IMMEDIATELY.
Posted in Drugs

MITOXANTRONE

Posted by admin on May 15th, 2010 No Comments

MITOXANTRONE (my-toe-ZAN-trone)

Other Names for this Medication (Brand Names): Mitox, Novantron, Novantrone

Appearance

Injection: A dark blue clear liquid for injection into the bloodstream.

Why this Medication is Used

This medication may be used alone, or in combination with other drugs, for the treatment of breast cancer, prostate cancer, acute myelogenous leukemia, liver cancer and Non-Hodgkin’s lymphoma.

How do you take this Medication

Injection: Mitoxantrone is injected into your vein by your chemotherapy nurse over a few minutes.

Precautions

• Your urine may be coloured blue-green for 1 or 2 days after your treatment. Your body eliminates the drug through both your urine and bowel movements. Wash your hands thoroughly after using the bathroom. In addition, the whites of your eyes may have a slight blue colour during treatment.

• Your doctor may ask you to drink plenty of clear fluids so that you will pass more urine.

• This medication may affect your heart after several treatments. Your doctor may order special heart tests, from time to time, to see how your heart is working.

• Tell your chemotherapy nurse immediately if you feel pain at injection site.

• This chemotherapy should not be used if you are pregnant or breast-feeding. It is important to discuss birth control with your doctor (Note: birth control pills alone are not recommended as the only birth control method). Birth control should also be used by female partners, if you are a male taking this medication

• It is important to tell your doctor if you have chickenpox (or have recently been exposed to someone who has had chickenpox), shingles, kidney disease or liver disease. Any of these conditions could affect therapy with this medication.

• Due to increased risk of infection check with your doctor before having any vaccinations. Check with your doctor, before any surgery or dental work.

• Do not take ASA without your doctor’s knowledge and consent.

> If a doctor has advised you to take ASA to prevent heart disease or stroke, please discuss this with your oncologist (cancer doctor) before starting treatment.

> Do not use ASA (aspirin, acetylsalicylic acid) for headache, fever, or occasional aches and pains; use acetaminophen (Tylenol) instead. Many non-prescription medications contain ASA; always ask your pharmacist’s advice when choosing a product.

For more information on this medication, please call your doctor, pharmacist or nurse.

SIDE EFFECTS PREVENTION WHAT YOU SHOULD DO
MORE COMMON:
• Nausea and Vomiting

• Signs of infection: fever, chills, cough, sore throat, burning on urination.

• Low white blood cells

 • Take prescribed medicine for nausea and vomiting. Continue drinking clear fluids.

• Limit your contact with people who are sick or have colds. Rest often. Wash your hands often.

 • If you vomit within 1 hour of taking antinausea medication you may take another tablet. If you are unable to take tablets, a suppository may be ordered. Get fresh air and rest. Phone your doctor if vomiting lasts more than 24 hours or nausea longer than 48 hours.

• Keep a thermometer at home. Recognize signs of infection. Phone your doctor or go to the emergency department right away if your temperature is over 38° C or 100° F. You may need antibiotics..
LESS COMMON:
• Bruising or bleeding. Black, tar-like stools. Red spots on skin.

• Sore, red eyes.

 • Use sharp objects with care. Use a soft toothbrush. Tell your doctor before dental work is done.

• Avoid touching your eyes unnecessarily.

 • Phone your doctor immediately if bleeding or bruising is unusual or will not stop; or go to the Emergency Department.

• Avoid bright lights. Apply cool, wet face cloth to soothe.

• Tell your doctor on your next visit.
RARE:
• Sores in the mouth or the lips

• Blue discolouring at place of injection

• Pain or redness at place of injection

• Skin rash.

• Fast/irregular heartbeats; shortness of breath, trouble breathing; swelling of feet.

• Hair thinning (from head and body).

 • Maintain good mouth hygiene. Brush teeth often with a soft toothbrush. Avoid hot, spicy and acidic foods. • Check with your doctor or nurse as soon as you notice sores on mouth or lips.

• If painful, apply warm, wet face cloth to the area several times a day.

• Tell your doctor or nurse

• Tell your doctor as soon as possible.

• Contact your doctor IMMEDIATELY!

• Special heart tests may be ordered

• A wig, hat, cap, scarf or hairpiece may be worn.

• Your hair will regrow, once all of your treatments are over.
Posted in Drugs
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