AVODART™
/ DUTASTERIDE
The Biggest News In Hair Loss Treatment Since Propecia
On October 9,
2002 the FDA granted clearance to GlaxoSmithKline for Avodart
or dutasteride as the most recent hair loss treatment medicine.
The biggest news in hair loss treatment since Propecia.
WHAT IS AVODART
OR DUTASTERIDE?
Dutasteride is finally a reality under the brand name Avodart™
!
Approval for
NDA#21-319/s-001 was granted by the FDA on October 9, 2002.
This is the biggest
news in hair loss treatment since FDA gave clearance for Propecia
in December 1997. What is really interesting is Avodart IS NOT
a hair loss drug!
Avodart™
(Dutasteride) is approved for the treatment of Benign Prostatic
Hyperplasia (BPH). BPH is a non-cancerous enlargement of the
prostate glands. It is fairly common among older men aged 50
or above. BPH usually manifest in a variety of lower urinary
tract symptoms (LUTS) such as urinary frequency, urgency, nighttime
urination, decrease in urinary stream, incomplete emptying and
incontinence.
Avodart is a
synthetic 4-azasteroid compound and it is the first FDA approved
medication that can inhibit both types of 5-alpha reductase (5AR),
an enzyme that is commonly believed to responsible for the conversion
of testosterone to 5 alpha-dihydrotestosterone (DHT). It is widely
indicated that DHT is the main androgen accountable for prostate
growth and male pattern baldness.
ACTIVE INGREDIENTS
Avodart standard dosage is 0.5mg of the active ingredient dutasteride
per soft gelatin capsule. The capsule is composed by dissolving
0.5mg of dutaseride in a blend of mono-di-glycerides caprylic/capric
acid and butylated hydroxytoluene. Additional ingredients include
BSE-free bovine gelatin, glycerin and yellow ferric oxide.
TOPICAL DUTASTERIDE
Dutasteride is normally availalbe in its raw form, you might
even be able to blend your own Dutasteride topical solution.
It was reported in Avodart's prescribing information that the
medication is absorbed through the skin too. Dutasteride is a
white-yellowish powder that becomes insoluble in water, but it
can easily be dissolved in ethanol (44mg/mL), methanol (64 mg/mL)
and polyethylene glycol 400 (3mg/mL) too. It should be noted
that the effectiveness of Dutasteride or Avodart as a hair loss
treatment has not been clinically established to date.
DUTASTERIDE
vs FINASTERIDE
Unlike Finasterdie (Propecia or Proscar) which only inhibits
Type II 5AR, Dutasteride functions as a dual 5AR inhibitors and
have been proven to be more effective as an treatment for BPH
and possibly pattern hair loss or baldness. Dutasteride has shown
to exhibit significantly less inter-individual variation in the
level of DHT suppression compared to Finasteride.
STANDARD DOSE
Scientists have evaluated the effectiveness of Dutasteride at
various daily dosages, ranging from 0.01 mg, 0.05 mg, 0.5 mg,
2.5 mg, and 5.0 mg per day. It was found that the highest suppression
of DHT was achieved with 2.5 mg or 5.0 mg per day. A daily dosage
of 2.5 mg or 5.0 mg, Dutasteride suppresses close to 100% of
the DHT whereas 5.0 mg daily dosage of Finasteride only suppresses
close to 70% of the DHT. The level of DHT suppression does not
seem to different significantly between 2.5 mg and 5.0 mg. A
daily dose of 0.5mg, DHT inhibiton is close to 90%.
MAXIMUM EFFECT
According to Avodart or dutasteride's prescribing information,
the maximum effect of dutasteride can be observed within 1 to
2 weeks. "After 1 and 2 weeks of daily application with
dutasteride 0.5mg, median serum DHT concentrations were reduced
by 85% and 90% respectively." Thoses treated with a daily
dosage of 0.5mg dutasteride for 2 years, the median decrease
in serum DHT concentration was over 92% for both year 1 and year
2 of the 2-year trial.
SIDE EFFECTS,
WARNINGS, CONCERNS
1) Women or children should not use Avodart™ or dutasteride.
2) Women who
are pregnant should not handle Avodart™ for concern of potential
risks to a male fetus.
3) No measurable
bone mineral density level change was noticed in test patients
after a 52 weeks trial.
4) Men using
Avodart™ or dutasteride should not donate blood for at least
6 months after use for concern of possible administration of
dutasteride tainted blood by transfusion to pregnant female patients.
5) Men with liver
problems should avoid using Avodart™.
6) Patients'
ejaculate volume may decrease as a result of taking Avodart™.
A small number of the test patients experienced impotence and
a reduction in libido.
7) No clinically
significant change in hormone levels were perceived in test patients.
8) No clinically
significant changes in sperm concentration, sperm motility or
sperm morphology although some subjects reported reduction in
ejaculate volume.
9) A 2-year statistical
summary revealed that sexual adverse events such as impotence,
decreased libido, and ejaculation disorder decreased with the
duration of the treatment. Fewer incidences of adverse sexual
events were reported over time.
OPTIMAL DOSAGE
FOR HAIR LOSS
For the treatment of BPH it is recommendation to take 1 x 0.5mg
capsule orally every day with or without food.
For treating
hair loss a daily dose of 2.5mg daily seems to generate the favorable
results.
GENUINE AVODART™
Avodart™ pills are oblong, opaque, dull yellow, gelatin
capsules with the word "GX CE2" clearly printed in
red on one side. Avodart™ is packaged in bottles of 100
(NDC 0173-0712-00) with child resistant closures. You may also
find genuine Avodart™ in blister packs of 70 capsules (NDC
0173-0712-01).
STORAGE
15-30 degrees Celsius or 59 - 86 degrees F.
HALF-LIFE
Half-life refers
to the period of time (usually in hours) required for one-half
the dose of a drug to be excreted from the body. The following
half-life information about Avodart™ or dutasteride is found
in the prescribing information:
"The half-life
of dutasteride is approximately 5 weeks at steady state. The
average steady-state serum dutasteride concentration was 40 ng/mL
following 0.5 mg/day for 1 year. By following daily dosing, dutasteride
serum concentrations achieve 65% of steady-state concentration
after 1 month and approximately 90% after 3 months. Due to the
long half-life of dutasteride, serum concentrations remain detectable
(greater than 0.1 ng/mL) for up to 4 to 6 months after discontinuation
of treatment."
Avodart or Dutasteride
has relatively much longer half-life than Propecia. However,
that does not mean you can reap substantial cost savings because
in the long run, you have to sustain the same amount of medication
in your body in order to obtain beneficial results. The true
significance of long half-life is that you may use flexible dosing
schemes. You can take a small amount daily or a larger dose less
frequently. However, the concept is to average the same amount
of 0.5mg in your body by taking 0.5mg daily or 3.5mg weekly.
Keep in mind
that Avodart or Dutasteride has a long half-life, it does not
necessarily mean that the medication will simply stay fixed at
the highest "peak" level all the time.