i was off on the amounts.  the 4 month is 30 mg instead of the
22.5.......

~ curtis

=========

Lupron Depot is indicated for the palliative treatment of advanced
prostate cancer, for management of endometriosis, in combination with
iron for the preoperative treatment of anemia caused by uterine
fibroids, and for the treatment of children with central precocious
puberty.

Lupron Depot® - 4 Month 30 mg, Lupron Depot® - 3 Month 22.5 mg, and
Lupron Depot® 7.5 mg are indicated for the palliative treatment of
advanced prostate cancer. These dosages are not approved for use in
women. The most common side effect associated with Lupron Depot is hot
flashes. Like other treatment options, LH-RH agonists may cause
impotence. Symptoms may worsen over the first few weeks of treatment.
Periodic monitoring of PSA and serum testosterone levels is recommended.

Lupron Depot® - 4 Month 30 mg
(leuprolide acetate for depot suspension)

Lupron Depot® - 3 Month 22.5 mg
(leuprolide acetate for depot suspension)

Lupron Depot® 7.5 mg
(leuprolide acetate for depot suspension)

Gynecology

Lupron Depot® - 3 Month 11.25 mg and Lupron Depot® 3.75 mg are
indicated for the management of endometriosis and in combination with
iron for the preoperative treatment of anemia caused by uterine
fibroids. Side effects associated with Lupron Depot are generally those
related to hypoestrogenism, including vasomotor flushes, headaches, and
vaginal dryness. After 6 months of therapy with Lupron Depot 3.75 mg,
vertebral bone density decreased by an average of 3.2%, compared with
pretreatment value.

Lupron Depot® - 3 Month 11.25 mg
(leuprolide acetate for depot suspension)

Lupron Depot® 3.75 mg
(leuprolide acetate for depot suspension)

Pediatric

Lupron Depot-PED® 7.5 mg, 11.25 mg, and 15 mg are indicated for the
treatment of children with central precocious puberty. In clinical
studies, the most frequently reported adverse event related to therapy
with Lupron Depot-PED was an injection site reaction seen in 5% of
children in combined studies. The recommended starting dose of
Lupron-PED is 0.3 mg/kg/4 weeks (minimum 7.5 mg). Inadequate dosing may
result in poor control of the pubertal process.

Lupron Depot-PED®
(leuprolide acetate for depot suspension)

7.5 mg, 11.25 mg and 15 mg

 

knowledge is power - growing old is mandatory - growing wise is optional    
"Many more men die with prostate cancer than of it. Growing old is
invariably fatal. Prostate cancer is only sometimes so."
http://community.webtv.net/PALMER_ENT/doc

SUPREFACT® i (Injectable)
SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):
SUPREFACT® i (Injectable)

COMPOSITION:
Each 1 mL of the aqueous solution contains 1,05 mg buserelin acetate
corresponding to 1 mg buserelin base as the active ingredient.
As preservative: Benzyl alcohol 1,0% m/m.

PHARMACOLOGICAL

CLASSIFICATION:
Category A: 21.10: Trophic hormones.

PHARMACOLOGICAL ACTION:
Suprefact contains buserelin, an analogue of the natural gonadorelin
(GnRH, HLH-RH) with a long duration of action.
Gonadorelin stimulates both synthesis and release of the gonadotropins
LH and FSH. The latter then stimulates steroid biosynthesis in the
gonads. Studies of the behaviour of the receptor sites, both of gonadal
LH-receptors and pituitary GnRH-receptors have shown that long-term
stimulation leads at first to an increase but then to a reduction in the
stimulability of both gonadotropins and sexual steroid levels. The
dose-level and time interval between individual doses of GnRH are
determinant factors for the receptor loss as indicated in animal
studies.

The suppressive effect is fully reversible. Genuine gonadorelin is bound
to receptors for only a short time. It is degraded within 30 to 60
minutes by arylamidase and its activity thus abolished. For therapeutic
use the highly-potent, therefore long-active analogue buserelin, has
been developed. Enzymic degradation is inhibited by substitution of the
amino acid, glycine, at two sites in the molecule.
Buserelin is thus bound to the receptors for a longer time and is
effective for more than three hours.
Its elimination half-life from serum does not differ significantly from
that of gonadorelin.
Buserelin produces much greater receptor-loss than gonadorelin.
At adequate dose-levels, administration three times daily is sufficient.
Suprefact is capable of inhibiting both gonadotropin release, from the
pituitary and gonadal steroid-biosynthesis and is thus indicated for the
treatment of hormone-dependent tumours such as prostatic carcinoma. Of
particular importance is the complete reversibility of the suppressive
effect, thus permitting temporal control of the pituitary-gonad-axis.

INDICATIONS:

Prostatic carcinoma in which suppression of testosterone production is
indicated.

CONTRA-INDICATIONS:

Suprefact should not be used if the tumour is found to be insensitive to
the medicine, after surgical removal of the testes, or after treatment
with oestrogen therapy.
Should not be used in patients who are hypersensitive to benzyl alcohol
or to buserelin acetate.

DOSAGE AND DIRECTIONS FOR USE:

Introduction of suppressive therapy: The patient should be admitted to
hospital and 0,5 mL Suprefact i (for injection) injected
sub-cutaneously 3 times a day at 8 hourly intervals, for a period of
7 days. This dose is equivalent to 1,5 mg buserelin daily and is
independent of body mass.
Continuation of suppressive therapy: On the 8th day of treatment, the
regimen of treatment is changed from the previously given subcutaneous
form to the Suprefact ns Nasal Spray and the duration of treatment is
determined by the doctor.

SIDE-EFFECTS AND SPECIAL
PRECAUTIONS:

At the start of treatment with Suprefact there is a temporary rise in
sex hormones, which usually remains within the normal range. In a few
patients this rise may be associated with an increase in the symptoms of
the disease, such as bone pain, impaired micturition, muscular weakness
in the legs as manifestation of temporary activation of the tumour.
These symptoms usually subside spontaneously without necessitating
withdrawal of Suprefact.
According to present information, however, they can be avoided by
additionally prescribing an antiandrogen (e.g. cyproterone acetate,
flutamide) at the start of treatment. It is therefore advisable in
patients in whom temporary increase in size of tumour may lead to urinal
tract obstruction, paresis due to increased pressure on the spinal cord,
or increased intracranial pressure (in rare cases with brain metastases)
to administer an antiandrogen about five days before the start of
Suprefact treatment and continue it for three to four weeks in
conjunction with the Suprefact therapy until the sex hormones have
fallen to a satisfactory level.
Owing to the suppression of sex hormone synthesis, hot flushes are to be
expected in the majority of cases and loss of potency and libido occur
in all cases. Also as a result of the suppression of sex hormones,
breast enlargement and depressive moods may rarely occur. Patients with
a known history of depression should be monitored carefully.
Infrequently, hypersensitivity reactions to buserelin or benzyl alcohol
may occur, such as reddening of the skin and urticaria-like skin changes
and exanthema.
Allergic (anaphylactic) shock is rare, but acutely life-threatening if
it does occur (for recommended measures, see below).
Other side effects reported include thrombosis with pulmonary embolism,
nausea, vomiting, diarrhoea, dizziness and transient headache.
Subcutaneous treatment with Suprefact i injection is regarded as a
pre-treatment, which is replaced on the 8th day by an intranasal spray.
No serum testosterone tests are carried out during the first week of
treatment. Instructions for the tests recommended during long-term
treatment are given in the package insert of the special dosage form,
Suprefact ns Nasal Spray.
Monitoring of the clinical effect of Suprefact i injection is carried
out by the methods generally used in prostatic carcinoma. As the
testosterone level in the serum does not fall immediately after the
start of treatment, the onset of the clinical effect may also be
delayed.
There are no known interactions between buserelin and any other
concomitant medication.
At the start of the treatment with Suprefact, a transient activation of
the tumour may occur. In the rare instances, symptoms of neurological
disorders (e.g. muscular weakness in the legs) may develop, which in
isolated cases are serious.
Emergency measures to be taken in the event of anaphylactic shock:
The following emergency measures are generally recommended: At the first
signs (sweating, nausea, cyanosis) interrupt the injection immediately
and perform venous cannulation.
In addition to the usual emergency measures, ensure that the patient is
kept flat with the legs raised and airways patent. Emergency drug
therapy:
Immediately epinephrine (adrenaline) i.v.: Dilute 1 mL of commercially
available epinephrine solution 1:1°000 to 10 mL. In the first
instance slowly inject 1 mL of this dilution (equivalent to 0,1 mg
epinephrine) while monitoring pulse and blood pressure (watch for
disturbances of cardiac rhythm). The administration of epinephrine may
be repeated. Then glucocorticoids i.v., e.g. 250 -1000 mg
methylprednisolone. The glucocorticoid administration may be repeated.
Subsequently volume substitution i.v., e.g. plasma expanders, human
albumin, balanced electrolyte solution.
Other therapeutic measures: Artificial respiration, oxygen inhalation,
antihistaminics.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:

There are no known symptoms of over-dosage.

IDENTIFICATION:

A clear, colourless to pale yellowish solution in a multidose vial of
5,5 mL

PRESENTATION:

Packs of two 5,5 mL multidose vials.

STORAGE INSTRUCTIONS:

Store between 2°C and 25°C.
Do not freeze.
Keep out of reach of children.
The date of first withdrawal should be noted down on the label. Once
opened, the vials should be stored at 25°C and for not longer than 2
weeks.

REGISTRATION NUMBER:

V/21.10/169

NAME AND BUSINESS ADDRESS OF THE APPLICANT:

NORISTAN LIMITED
326 Marks Street, Waltloo, Pretoria

DATE OF PUBLICATION OF THIS PACKAGE INSERT:

January 1988.
HOECHST Pharmaceuticals, Division of
NORISTAN LIMITED
WALTLOO, PRETORIA
PHSX - G43 - 0037

knowledge is power - growing old is mandatory - growing wise is optional    
"Many more men die with prostate cancer than of it. Growing old is
invariably fatal. Prostate cancer is only sometimes so."
http://community.webtv.net/PALMER_ENT/doc