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Category: Topics: Other Drugs

Proscar (Finasteride)

Clinico-pharmacological group Drug for the treatment of benign prostatic hyperplasia Release form, composition and packing Tablets, coated blue color film; in the form of an apple, with the engraving “of MSD 72 ‘on one side and” PROSCAR “- on the other. 1 tab. finasteride 5 mg Excipients: lactose monohydrate, pregelatinized starch (corn), sodium salt of […]

Clinico-pharmacological group

Drug for the treatment of benign prostatic hyperplasia

Release form, composition and packing

Tablets, coated blue color film; in the form of an apple, with the engraving “of MSD 72 ‘on one side and” PROSCAR “- on the other.

1 tab.
finasteride 5 mg

Proscar-MSDExcipients: lactose monohydrate, pregelatinized starch (corn), sodium salt of carboxymethyl ether of starch, iron oxide yellow, docusate sodium, microcrystalline cellulose, magnesium stearate.

Composition of coating film: methylhydroxypropylcellulose, hydroxypropylcellulose, titanium dioxide, talc, indigo carmine aluminum lake.

14 pcs. – Blisters (1) – boxes cardboard.
14 pcs. – Blisters (2) – boxes cardboard.

testimony

Treatment of benign prostatic hyperplasia in order to:

– Prevention of urological complications (reduced risk of acute urinary retention) and to reduce the need for surgical procedures (including transurethral resection of the prostate and prostatectomy);

– Reducing the size of an enlarged prostate gland, improve urine flow and decrease the severity of symptoms associated with benign prostatic hyperplasia.

Therapy of Proscar is indicated in patients with an enlarged prostate.

Disease
Prostate adenoma
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Contraindications

– Hypersensitivity to the drug.

Proscar is not indicated for use in women and children.

With caution is prescribed to patients with large residual urine volume and / or significantly reduced urine current (should be carefully monitored for obstructive uropathy).

Dosage

The recommended dose is 5 mg (1 tab.) 1 times / day regardless of the meal.

Proscar may be used alone or in combination with doxazosin .

For patients with renal failure of varying severity (with a decrease in QC to 9 ml / min) is not required for individual selection of doses, as pharmacokinetic studies did not reveal any changes in the distribution of finasteride in these patients.

For older patients is also no need for dose selection, although the pharmacokinetic studies indicate that the removal of finasteride in patients older than 70 years, several reduced.

Side effects

The study PLESS safety assessment was performed in 1524 patients treated with Proscar 5 mg / day and 1516 patients receiving placebo for 4 years. At 4.9% (74) of the patients treated were canceled due to side effects attributed to Proscar, compared with 3.3% (50) of patients receiving placebo. At the same time 3.7% (57) patients treated with Proscar, and 2.1% (32) of patients treated with placebo, the treatment was canceled due to sexual dysfunction, which was the most frequently observed side effect.

In the first year of treatment of impotence, decreased libido, and ejaculation disorder were more common in patients treated with Proscar compared with placebo. When using Proscar for 2-4 year study the incidence of the above side-effects in patients taking Proscar, did not differ from that of patients receiving placebo.

From the reproductive system: tenderness of the testicles, impotence, decreased libido, ejaculation disorders, reduction of volume of ejaculate.

From endocrine system: an increase in pain and breast tenderness.

Allergic reactions: rash, pruritus, urticaria, angioneurotic edema of the lips and face.

With prolonged use of Proscar no increase in the frequency and severity of side effects, and the number of cases of sexual dysfunction associated with taking the drug is reduced during prolonged therapy.

safety and tolerability profile in the combined treatment with finasteride 5 mg / day and doxazosin 4 or 8 mg / day with a comparable safety and tolerability of each of said drugs in isolation.

The 7-year placebo-controlled study (which was included in 18,882 healthy men) on the results of the biopsy (in 9060 men), cancer of the prostate was diagnosed in 18.4% of patients treated with Proscar and 24.4% of patients receiving placebo. In 280 men (6.4%) in the Proscar and 237 men (5.1%) in the placebo group based on the results of the biopsy was diagnosed with prostate cancer, estimated at 7-10 Gleason. Approximately 98% of all cases of cancer tumor was intracapsular (stage T1 or T2).

From the laboratory parameters: reduction of prostate-specific antigen.

Overdose

Proscar Patients received a single dose of 400 mg and in multiple doses up to 80 mg / day for 3 months, with no adverse effects were detected.

Recommendations for specific treatment Proscar no overdose.

Drug interactions

There were no clinically significant interaction with other medications Proscar.

Apparently, Proscar has no appreciable effect on the activity of isoenzymes of cytochrome P 450 and the pharmacokinetics of drugs whose metabolism data isozymes are involved. The combined use of Proscar with propranolol, digoxin, glyburide, warfarin, theophylline, with ACE inhibitors, acetaminophen, acetylsalicylic acid, alpha-blockers, beta-blockers, calcium channel blockers , nitrates, diuretics, blockers of histamine H 2 receptor antagonists, inhibitors of GMG KoA-reductase inhibitors, NSAIDs, quinolones and benzodiazepines were found clinically significant manifestations of drug interactions.

special instructions

The effect on the level of prostate-specific antigen and diagnosis of prostate cancer

So far, not shown positive clinical effect of Proscar patients with prostate cancer. Patients with BPH and elevated PSA level in controlled clinical trials (with a few definitions of PSA and biopsy of the prostate gland) Proscar therapy had no effect on the incidence of prostate cancer. The overall incidence of prostate cancer was not significantly different in patients treated with Proscar or placebo.

Before treatment Proscar and periodically during treatment with rectal examination should be performed, as well as the study of other methods to determine the presence of prostate cancer. Determination of Serum PSA is also used for prostate cancer. In general, when the initial level above 10 ng PSA / ml requires a wider examination of the patient, including, if necessary, the purpose of biopsy. When the level of PSA in the 4-10 ng / mL is recommended to further examination of the patient. There is considerable overlap in PSA levels in prostate cancer patients, and patients who do not have the disease. Consequently, BPH in men with normal PSA value does not allow to exclude prostate cancer, regardless of treatment Proscar. Initial PSA levels below 4 ng / ml did not exclude the presence of prostate cancer.

Proscar causes a decrease in serum PSA of approximately 50% in patients with BPH even in the presence of prostate cancer. In this connection it should be borne in mind that the reduction in PSA levels in patients with BPH treated with Proscar not exclude concomitant prostate cancer.

It is shown that in patients treated with Proscar for 6 months or more, PSA values ​​should be doubled for comparison with their normal values ​​of this indicator in patients who are not receiving treatment. This adjustment preserves the sensitivity and specificity of PSA analysis and the ability to detect prostate cancer.

Any sustained increase in PSA levels of patients treated with finasteride, requires a thorough examination to determine the cause, which may be in non-compliance with the use of Proscar.

Proscar does not significantly reduce the percentage of free PSA (ratio of free PSA to total). This indicator remains constant even under the influence of Proscar. If the percentage of free PSA is used, correction values ​​of this index is not required for the diagnosis of prostate cancer.

Effects on laboratory parameters

The concentration of PSA in serum is correlated with patient age and prostate volume and prostate volume, in turn, depends on the age of the patient. In determining the PSA level should be noted that this figure is reduced in patients taking Proscar. In most patients, a rapid decrease in PSA is observed in the first months of therapy, after which it takes place to stabilize at a new level, which is usually half the value measured prior to initiating therapy. In this regard, patients taking Proscar for 6 months or more, it is necessary to double the value of PSA for its comparison with normal males without taking Proscar.

Pregnancy and lactation

Women of childbearing age and pregnant women should avoid contact with crushed or loss of integrity of the drug Proscar tablets because of the possibility of penetration of finasteride in the body of the pregnant woman and the subsequent risk for the development of the male fetus.

Due to the ability of inhibitors of 5-alpha-reductase type II inhibit the conversion of testosterone to dihydrotestosterone, these drugs, including finasteride, may cause abnormalities of prenatal form of the external genitalia in male fetus.

Proscar coated tablets, and this prevents contact with finasteride provided that the tablets are not milled and have not lost integrity.

Avodart (Dutasteride)

Avodart – drug in capsules, which acts directly on the prostate tissue, reducing its dimensions, and is intended for the treatment and prevention of benign prostate tumors. It also reduces the risk of acute urinary retention, eliminating the need for surgery. Avodart capsules made of gelatin, yellow, produced in blister packs of ten capsules, three […]

Avodart (Dutasteride)Avodart – drug in capsules, which acts directly on the prostate tissue, reducing its dimensions, and is intended for the treatment and prevention of benign prostate tumors. It also reduces the risk of acute urinary retention, eliminating the need for surgery.

Avodart capsules made of gelatin, yellow, produced in blister packs of ten capsules, three or nine blisters in the package. It may appoint in conjunction with other drugs that affect hormone metabolism. Its price usually ranges from 1,500 to 2,500 rubles for thirty capsules.

Avodart mechanism of action, indications for use

The active ingredient Avodart – dutasteride. It affects the hormonal metabolism of the prostate gland, due to which the hormone-dependent tissue is reduced in size without surgery. Write mainly in the feces, it is processed by the liver.

Tests were conducted on groups of men between 18 and 87 years of age did not play value in the treatment of drug, elderly people carry it no worse than the young. According to the instructions shown Avodart men with benign prostate cancer, prostate hyperplasia, as well as acute urinary retention.

Contraindications

Contraindications to the use of only serves hypersensitivity to the drug. When diagnosed with liver failure Avodartsleduet used with caution. Do not take it as women and children, since there is no data on the use of the drug in them.

Dosage Avodart

By taking Avodart instructions regardless of the meal, one capsule once a day. One capsule contains 0.5 mg of active substance. Do not open or chew the capsule, since the drug causes irritation of the mucous membranes of the mouth and throat. Overdose occurs rarely, if occurs, the treatment can be carried out by the symptoms, there is no specific antidote.

Side Effects Avodart

 

Very rarely (less than one case per ten thousand) possible violation of potency, decreased sexual desire, allergic reactions, increase in mammary glands. Occasionally there is baldness, hair fall mainly on the body. Possible pain in the testicles, and depression. Interaction with other drugs clinically unimportant.

Avodart reduces sperm count about twice, reducing their mobility and the number of sperm with long-term (longer than 52 weeks) administration. However, after the discontinuation of these indicators are restored.

Features of the drug

Dutasteride, which is part of Avodart, is able to penetrate through the skin, so you should avoid contact with damaged capsules to people who did not take, especially children. In case of contact, immediately wash the contaminated skin with soap and water.

When the drug is not difficult to diagnose prostate cancer, but before use, make sure benign tumors and in the process constantly monitor room her condition as during clinical trials it has been observed a slight increase in the number of cases of degeneration of benign prostatic hyperplasia in cancer in people taking the drug.

Comments about Avodart

Subjective improvement of health in the patients receiving Avodart comes quickly, but it is necessary to take at least six months, so that the effect can be assessed objectively. Negative reviews are caused mainly by the fact that the patient does not maintain the required reception time. Sometimes there is a reduced sensitivity of the prostate gland hormone, then may appear insufficient feedback on the effectiveness of the drug, but this happens very rarely.

On the side effects complaints are also very rare, usually well tolerated. Reviews from physicians urology and andrology usually also positive. If you experience side effects in the patient and his complaints and sharply negative reviews about Avodart drug overturned.

Pharmacological Effects
Dutasteride inhibitory effect on 5α-reductase isozymes of both types. That it stops the conversion of testosterone to the androgen DHT, which is associated with the development of hyperplastic changes in the tissues of the prostate (RV). In drug treatment, a decrease in plasma concentrations of 85-90% DHT. The therapy following changes are observed drug Avodart:
– a decrease in size of the prostate;
– Improvement of urination;
– Reduce the likelihood of acute urinary retention;
– Reducing the need for surgical intervention.

 Indications

The drug Avodart is indicated for benign hyperplasia of the prostate character.

 

Dosage
Standard dosage capsules Avodart: 1 capsule / day. The capsule is used as a whole, without regard to meals. The course of treatment over six months. Dose adjustment for patients with renal insufficiency is not carried out.

Side effects
Receiving Avodart medication may be accompanied by:
– hives;
– Erectile dysfunction;
– Rash;
– Gynecomastia;
– Itching;
– Decreased libido;
– Localized swelling.

 

Contraindications
The drug Avodart is not indicated in case of:
– hypersensitivity to dutasteride;
– Hypersensitivity to the auxiliary components;
– Hypersensitivity to inhibitors of 5α-reductase.

With care prescribe Avodart with hepatic insufficiency.

 

Pregnancy
The drug is absolutely contraindicated and not appropriate to the destination pregnant.

 

Drug interactions

The drug, a group of drugs Possible interactions result
verapamil Reduced clearance of dutasteride
Diltiazem Reduced clearance of dutasteride

 

Overdose
No cases of overdose with severe symptoms have been recorded. Antidote No specific nature. If you notice any unusual symptoms should seek qualified therapeutic help.

 

Product form
The drug is available in capsule form. Filling Machine are as follows:
– 30 capsules / pack;
– 90 capsules / pack.

 

Storage conditions
Storage temperature Avodart capsules – up to 30 degrees Celsius. The suitability of the drug for use – 4 years.

 

Ingredients
1 capsule contains dutasteride Avodart 500 mg. Auxiliary components: mono-, di-glycerides of capric / caprylic acids, gelatin, butylhydroxytoluene, yellow iron oxide, glycerol, titanium dioxide.

 

Therapeutic

Drugs used for diseases of the prostate

The nosological classification (ICD-10)

Prostatic hyperplasia (N40)

 

The active ingredient is:  dutasteride

 

ATC:  G04CB02

 

Manufacturer:  by GlaxoSmithKline

 

Additionally,
with damage to the capsules can not be contacted his hands, as the drug penetrates through the skin.
Before and during the treatment it is carried out a study of the prostate gland, PSA determination.
At the rate of reaction does not affect Avodart medication.

 

Attention!
Description “of the drug Avodart ” on this page is a simplified and enlarged version of the official instructions for use. Before purchasing or using the product, you should consult your doctor and see the summary approved by the manufacturer.
Preparation of information being provided is for informational purposes and should not be used as a guide to self-healing. Only a doctor can decide on the appointment of the drug, and to determine the doses and methods of application.

FG-4592 (Roxadustat). Oral EPO, or Altitude Pill

A few days ago, The New York Times broke the story about the two cases of doping in cycling. On the surface, that might not seem interesting news. We probably will not spend much time on the positive cases of doping are Anabolic.org, as our readers are well aware that the efficiency enhancing drugs (PED) […]

FG-4592 (Roxadustat)A few days ago, The New York Times broke the story about the two cases of doping in cycling. On the surface, that might not seem interesting news. We probably will not spend much time on the positive cases of doping are Anabolic.org, as our readers are well aware that the efficiency enhancing drugs (PED) use is entrenched in many sports, agree with him or not. But the story is very interesting times, given the drug involved. In both cases involved FG-4592, also known as roxadustat, which is a new type of erythropoiesis stimulating agent. This drug is still in the research phase, and it is not available as a prescription anywhere in the world. We get a lot of questions about it raleigh personal trainers, and thought that the rapid introduction was in order.

First, let’s discuss how it works. FG-4592 (roxadustat) aims to hypoxia sensing path (how the body perceives low oxygen content). This drug acts as a specific inhibitor of the enzyme prolyl hydroxylase domain (PHD). By blocking its target PHD enzyme preparation stabilizes the protein known as HIF-2 & alpha; (Hypoxia-inducible factor 2 & alpha;), which is largely found in the kidney. Kidney HIF-2α directly controls the transcription and the production of erythropoietin (EPO), a protein that stimulates the production of red blood cells. Very simply put, the FG-4592 (roxadustat) tricks your body into thinking the oxygen levels are low. We could call it “the height of the tablet,” if we want to, as its effects on HIF-2A mimic some of the changes observed hcg calculator when a person rises to a great height.

Another great thing about this drug is that it is not a large complex of a peptide as erythropoietin (EPO) and its analogues, the main alloying agents in this class now. FG-4592 is a small molecule, with the added benefit is very stable and orally bioavailable. It may be given instead of tablets injection. This is likely to make it attractive to a larger number of athletes. EPO drugs had a reputation for pretty niched so far. They have not been widely adopted by athletes, except for the most competitive laps. They are difficult to use, potentially dangerous, and bear the discomfort and stigma injection. While we are not clear on the safety FG-4592 and other drugs like it, we see the potential for this class of drugs to be taken by a much wider body of athletes, considering that you just have to swallow the tablet.

But wait … The New York Times quoted the representative AstraZeneca Abigail Bozarth, as they say, “There’s no other drug like FG-4592.” Perhaps there is an accurate statement, if you view it with a chemical structure very strong point of view. In fact, FG-4592 is one of the many new PHD inhibitors under development, even currently in clinical evaluation for the treatment of anemia. Some other well-known agents include AKB-6548 Akebia, in BAY85-3934 from Bayer, FG-2216 and it (fg 4592 doping) developed by FibroGen and GSK1278863 company GlaxoSmithKline. There are actually 22 trials was recorded pure barre tulsa in the United States for PHD inhibitors until now. I’ve included a quick chart that highlights their plan for review, taken from a recent article in the journal Stem Cells Translational Medicine.

It is still too early to draw conclusions about the FG-4592, or PHD inhibitors in general. There appears to be ample evidence suggesting these agents work to support the production of red cells, as in theory. But then again, none of these drugs has not yet been fully evaluated for safety. Until now, no toxic effects were seen. There is still a lot we do not know about them, however, and, of course, they can be optimally used. We must remember that erythropoiesis is potentially dangerous to tinker winstrol before and after with the system. This can be a fine line between the increase in hematocrit (red cell density) to such an extent that improves performance, and one that is largely endangers the individual with thickened blood and the risk of heart attack or stroke. Potential for lightweight “the EPO pill” causes a lot of issues and problems. At this point, I think it’s better not to experiment with FG-4592 the black market. We will probably learn a lot more about this in the coming months and years. At the same time, it’s really an interesting topic. Of course, I try to follow her.